Entries |
Document | Title | Date |
20080207670 | Dermally Applicable Formulations For Treating Skin Diseases in Animals - The invention relates to pharmaceutical formulations comprising a tricyclic compound for the dermal treatment of skin diseases in animals. | 08-28-2008 |
20080207671 | Diagnosis and treatment of diseases arising from defects in the tuberous sclerosis pathway - The present invention relates to compositions, methods for identifying, and methods for treating abnormalities in TSC signaling pathways. In particular, the present invention relates to methods of diagnosing, treating and preventing disorders caused by defects in the TSC signaling pathway (e.g., TSC-1, TSC-2, TSC-1/TSC-2, Rheb, mTOR, S6K, and 4EBP-1) such as tuberous sclerosis, diabetes, and complications related to diabetes (e.g., insulin resistance, obesity, nephropathy). The present invention further relates to compositions for treating and preventing disorders such as tuberous sclerosis, diabetes, and complications related to diabetes (e.g., insulin resistance, obesity, nephropathy). | 08-28-2008 |
20080207672 | Methods of treating keratin hyperproliferation disorders using mTOR inhibitors - A method of treating or preventing keratin hyperproliferation skin disorders is set forth. The method includes the administration of an mTOR inhibitor to a subject afflicted with the hyperproliferation disorder. The mTOR inhibitor can be administered to the subject via any means known in the art including oral, topical, and transdermal administration. | 08-28-2008 |
20080214595 | Use Of Rapamycin Derivatives For The Treatment And/Or Prevention Of Cardiovas Cular Disorders - The present invention provides methods of treating and/or preventing cardiovascular disorders comprising administering rapamycin derivative compounds. | 09-04-2008 |
20080214596 | BIOMARKERS FOR SENSITIVITY OF PROLIFERATIVE DISEASES TO MTOR INHIBITORS - Disclosed is a method for determining the sensitivity of a proliferate disease in a subject to treatment with an mTOR inhibitor, comprising determining the level of expression and/or phosphorylation state of S6 in a sample derived from the subject, as well as related methods of treatment and uses. | 09-04-2008 |
20080234309 | MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE - The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: | 09-25-2008 |
20080249123 | WORTMANNIN-RAPAMYCIN CONJUGATE AND USES THEREOF - A rapamycin—wortmannin conjugate is described, in which the conjugate is formed by linking the rapamycin and wortmannin together in such a manner that the rapamycin and the wortmannin are separated following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described. | 10-09-2008 |
20080249124 | WORTMANNIN-RAPALOG CONJUGATE AND USES THEREOF - An anti-neoplastic wortmannin conjugate is described formed by a linking a rapalog and wortmannin. Such a linkage is removable following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described. | 10-09-2008 |
20080255177 | ANTI-TUMOR ACTIVITY OF CCI-779 IN PAPILLARY RENAL CELL CANCER - This invention provides the method or use of CCI-779 in the treatment of papillary renal cell carcinoma. | 10-16-2008 |
20080275076 | Pharmaceutical Compositions Comprising Sirolimus and/or an Analogue Thereof - The present invention relates to pharmaceutical compositions in particulate form or in solid dosage forms comprising sirolimus (rapamycin) and/or derivatives and/or analogues thereof. Compositions of the invention exhibit an acceptable bioavailability of sirolimus and/or a derivative and/or an analogue thereof. The pharmaceutical compositions of the invention are designed to release sirolimus in a controlled manner so that the plasma levels stays within the narrow therapeutic window that exist for this class of substances. An extended release profile, where the peak concentration has been reduced without loosing significant bioavailability, together with less variable absorption, is expected to improve the safety/efficacy ratio of the drug. Furthermore, compositions according to the invention provide for a significant reduced food effect and a delayed release of sirolimus is expected to reduce the number of gastro-intestinal related side effects. | 11-06-2008 |
20080280939 | Combination of Organic Compounds - The invention relates to a pharmaceutical combinations comprising an AT1 receptor blocker or pharmaceutically acceptable salts thereof and a mTOR inhibiting agent, e.g. rapamycin or a rapamycin derivative, optionally in the presence of a pharmaceutically acceptable carrier. | 11-13-2008 |
20080280940 | Rapamycin Derivative or an Impdh Inhibitor For Treating Polycystic Kidney Disease - A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5′-monophosphate dehydrogenase inhibitor or a rapamycin derivative. | 11-13-2008 |
20080287482 | Production of Polyketides and Other Natural Products - The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential use of novel FKBP-ligand analogues and host cells that produce these compounds. The invention is particularly concerned with methods for the efficient transformation of strains that produce FKBP analogues and recombinant cells in which cloned genes or gene cassettes are expressed to generate novel compounds such as polyketide (especially rapamycin) FKBP-ligand analogues, and to processes for their preparation, and to means employed therein (e.g. nucleic acids, vectors, gene cassettes and genetically modified strains). | 11-20-2008 |
20080287483 | Polyketides and Their Synthesis and Use - The rapamycin gene cluster is an example of a gene cluster which includes a gene (rapL) leading to the formation of a precursor compound (pipecolic acid, in this case) which is required for inclusion in the larger product (rapamycin) produced by the enzymes encoded by the cluster. We have produced a mutant strain containing a rapamycin gene cluster in which the rapL gene is disabled. The strain does not naturally produce rapamycin but does so if fed with pipecolic acid. By feeding with alternative carboxylic acids we have produced variants of rapamycins. Tests have shown biological activity. | 11-20-2008 |
20080293758 | Combination of a Steroid Sulfatase Inhibitor and an Ascomycin - A combination of a steroid sulfatase inhibitor and an ascomycin, which combination is useful as a pharmaceutical. | 11-27-2008 |
20080293759 | Method for Treating Cancer Based on the Modulation of Calcineurin - The present invention relates to methods for treating a haematopoietic tumor by administering a drug inhibiting calcineurin and/or the calcineurin/NFAT pathway, alone or in combination with other cancer therapy, pharmaceutical compositions useful in such methods, and screening methods for identifying a compound useful for treating a haematopoietic tumor. | 11-27-2008 |
20080312267 | Diagnosis and Treatment of Diseases Arising from Defects in the Tuberous Sclerosis Pathway - The present invention relates to compositions and methods for identifying abnormalities in TSC signaling pathways. In particular, the present invention relates to methods of diagnosing and treating disorders such as tuberous sclerosis, which are caused by mutations in the TSC genes. The present invention further relates to methods and compositions for treating cancers mediated by TSC signaling disorders. | 12-18-2008 |
20090023768 | RAPAMYCIN DERIVATIVES FOR TREATING NEUROBLASTOMA - A rapamycin derivative for use in the treatment of neuroblastome, optionally in combination with a second drug substance. | 01-22-2009 |
20090030028 | Tetrahydroquinolines - Disclosed are compounds of formula (I), wherein W, R, R | 01-29-2009 |
20090036479 | METHOD OF INHIBITING CHOROIDAL NEOVASCUARIZATION - The present invention relates to compositions and methods for inhibiting unwanted angiogenesis, particularly those of ocular tissues. The treatment, inhibition, and/or prevention of choroidal neovasculature (CNV) is provided, along with an animal model for CNV and imaging techniques that permit the screening of potential agents as anti-angiogenesis and anti-CNV agents. | 02-05-2009 |
20090042923 | Method of Treating Tumors with Azaxanthones - The use of azaxanthones for treating diseases associated with tumor cells which express one or more protein of S100 family, and in treating patients that have malignancies consisting of tumors of an epithelial or mesenchymal nature, where these compounds are effective in retarding the progression and/or metastasis of these tumors. | 02-12-2009 |
20090062326 | M3 MUSCARINIC RECEPTOR ANTAGONISTS FOR TREATMENT OF M3 MUSCARINIC RECEPTOR-EXPRESSING TUMORS - The present disclosure provides methods of treating a tumor using M3 muscarininc receptor antagonists, such as darifenacin. In some examples, the tumor expresses M3 muscarinic receptors, such as tumors associated with smoking. Also provided are compositions that can be used to practice such methods. | 03-05-2009 |
20090069366 | DEUTERIUM-ENRICHED TACROLIMUS - The present application describes deuterium-enriched tacrolimus, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-12-2009 |
20090076060 | DEUTERIUM-ENRICHED TEMSIROLIMUS - The present application describes deuterium-enriched temsirolimus, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090082386 | Ascomycin and pimecrolimus having reduced levels of desmethylascomycin and 32-deoxy-32-epichloro-desmethylascomycin respectively, and methods for preparation thereof - Provided is ascomycin that has a low level of an FK523 impurity, and pimecrolimus that has a low level of a 32-deoxy-32-epichloro-FK523 impurity, methods of preparing them, and the use of such pimecrolimus for preparing a pharmaceutical composition. | 03-26-2009 |
20090088449 | 4-ACYLAMINOPYRIDINE DERIVATIVE MEDIATED NEUROGENESIS - The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes methods based on use of a 4-acylaminopyridine derivative to stimulate or activate the formation of new nerve cells. | 04-02-2009 |
20090093510 | Use of Nitrooxyderivatives of Drug for the Treatment of Muscular Dystrophies - The present invention relates to the use of nitric oxide releasing compounds for retarding or reversing muscular dystrophies such as Duchenne and Becker dystrophies. | 04-09-2009 |
20090093511 | Mast cell stabilizers in the treatment of obesity - The present invention is directed to methods of treating or preventing the development of obesity by administering compounds that stabilize mast cells. In addition, it includes pharmaceutical compositions which have both a mast cell stabilizer and instructions regarding the use of the stabilizer in treating or preventing obesity. | 04-09-2009 |
20090099225 | Method for the production of propellant gas-free aerosols from aqueous medicament preparations - The present invention relates to pharmaceutical preparations in the form of aqueous solutions for the production of propellant-free aerosols. | 04-16-2009 |
20090105293 | USE OF THIENOPYRIDONE DERIVATIVES AS AMPK ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Use of thienopyridone derivatives of formula (I), in which B, R, R | 04-23-2009 |
20090105294 | Biosynthetic Gene Cluster for the Production of a Complex Polyketide - A polyketide synthase complex composed of polyketide synthase with 15 total modules, a non-ribosomal peptide synthetase with 1 module, and a cytochrome P450 hydroxylase is described. Also provided are novel | 04-23-2009 |
20090176819 | 39-Desmethoxy-39-Methyl Derivatives of Rapamycin - The present invention relates to novel 39-desmethoxy-39-methylrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxy-39-methylrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections. | 07-09-2009 |
20090176820 | POLYMORPHIC FORMS AND PROCESS - The invention relates to a process for the manufacture of enantiomerically enriched or pure compounds of formula I | 07-09-2009 |
20090209572 | 36-Des(3-Methoxy-4-Hydroxycyclohexyl) 36-(3-Hydroxycycloheptyl) Derivatives of Rapamycin for the Treatment of Cancer and Other Disorders - The present invention relates to novel 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections. | 08-20-2009 |
20090215812 | BIOMARKERS FOR EVALUATING LIKELIHOOD OF TUMOR SENSITIVITY TO AN MTOR INHIBITOR - The present invention provides compositions and methods for evaluating the likelihood that a tumor is sensitive to an mTOR inhibitor, e.g., rapamycin or a rapamycin analog. The invention provides FKBP proteins as biomarkers for predicting the likelihood that a tumor is sensitive to an mTOR inhibitor. The methods include assessing the expression or activity of an FKBP protein, e.g., FKBP 12, in a subject with a tumor or in a sample derived from a tumor. Additional biomarkers and biomarker combinations are also provided. The invention also provides kits containing, e.g., a validated antibody or ligand for assessing the expression or activity of an FKBP protein. | 08-27-2009 |
20090215813 | HISTONE DEACETYLASE INHIBITORS AS IMMUNOSUPPRESSANTS - A method of preventing or suppressing an immune response or immune mediated response comprising administering an effective amount of an histone deacetylase inhibitor compound alone or in combination with a second pharmacologically active agent. | 08-27-2009 |
20090221625 | COSMECEUTICAL COMPOSITION - Topical compositions comprising: —a physiologically acceptable alkanediol, ether diol or diether alcohol containing up to (8) carbon atoms; —water; and—optionally an unsaturated fatty alcohol; and optionally further conventional excipients, for use as a cosmeceutical, in particular for use in the repair or maintenance of skin barrier function. They are indicated for use in e.g. moisturizing skin, nail and mucosa and, when an optional pharmaceutically active agent is present, additionally in the treatment of various skin, nail and mucosal diseases. Also disclosed are compositions suitable for topical application to infants and babies for treating dry skin, and soothing skin irritated from diaper rash and scrapes. | 09-03-2009 |
20090221626 | AEROSOL FORMULATION FOR INHALATION CONTAINING AN ANTICHOLINERGIC AGENT - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X represents an anion, and containing at least one pharmacologically compatible organic acid and optionally additional pharmacologically compatible adjuvants and/or complexing agents. The cation of formula (1′) is contained in the preparation at a concentration of between 411 and 460.32 mg per 100 ml of medicament preparation. | 09-03-2009 |
20090239895 | Novel 3-thia-10-aza-phenanthrene derivatives - The compounds of formula I | 09-24-2009 |
20090247565 | Tyrosine Kinase Inhibitors - The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 10-01-2009 |
20090247566 | Pyrano [3,2-C] Pyridones and Related Heterocyclic Compounds as Pharmaceutical Agents for Treating Disorders Responsive to Apoptosis, Antiproliferation or Vascular Disruption, and the Use Thereof - A pharmaceutical composition comprising a pharmaceutically acceptable excipient or carrier and a compound Formula I: | 10-01-2009 |
20090247567 | BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 10-01-2009 |
20090253732 | Production Of Polyketides And Other Natural Products - The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. Therefore in aspect the present invention provides 17-desmethylrapamycin and analogues thereof, methods for their production, including recombinant strains, and isolation and uses of the compounds of the invention. In a further aspect the present invention provides for the use of 17-desmethylrapamycin and analogues thereof in the induction or maintenance of immunosuppression, the stimulation of neuronal regeneration or the treatment of cancer, B-cell malignancies, fungal infections, transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation vascular disease and fibrotic diseases, and in the regulation of wound healing. | 10-08-2009 |
20090253733 | RAPAMYCIN CARBONATE ESTERS - Certain embodiments include carbonate esters of rapamycin at position 42 that are synthesized by a lipase catalyzed regio-specific process. These compounds or a pharmaceutically acceptable salt thereof are useful in the treatment of organ and tissue transplant rejection, autoimmune disease, proliferative disorder, restenosis, cancer, or microbial infection. | 10-08-2009 |
20090270441 | MACROLIDES - The invention relates to the stabilization of poly-ene macrolides and to a particular macrolide obtained in crystalline form. | 10-29-2009 |
20090286823 | CCR1 Inhibitors useful for the treatment of multiple myeloma and other disorders - The invention relates to the use of inhibitors of CCR1 for the treatment of cancers and osteolytic bone disorders. In some embodiments, the invention relates to methods for the treatment of multiple myeloma, smoldering multiple myeloma and secondary bone cancers. | 11-19-2009 |
20090286824 | Pyridine Classical Cannabinoid Compounds and Related Methods of Use - Disclosed are compounds of the formula I: | 11-19-2009 |
20090306120 | TERPOLYMERS CONTAINING LACTIDE AND GLYCOLIDE - The present invention provides an amorphous terpolymer for a coating on an implantable device for controlling release of drug and methods of making and using the same. | 12-10-2009 |
20090325998 | SOIL TREATING AGENT OR SEED TREATING AGENT COMPRISING QUINOLINE COMPOUNDS OR SALTS THEREOF AS ACTIVE INGREDIENT,OR METHOD FOR PREVENTING PLANT DISEASES BY USING THE SAME - A soil treating agent or a seed treating agent having excellent prevention effects against various plant pathogens (particularly against rice blast) is provided. A soil treating agent or seed treating agent, comprising one or more compounds of the general formula (Ia), (Ib) or (Ic): | 12-31-2009 |
20100022578 | MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV replication of formula (I) | 01-28-2010 |
20100022579 | SUBSTITUTED TETRAHYDROQUINOLINES - Compounds of the formula (I), in which R | 01-28-2010 |
20100029705 | BETA-2-ADRENORECEPTOR AGONISTS - Compounds of formula | 02-04-2010 |
20100063084 | MULTI-PHASE RELEASE METHSCOPOLAMINE COMPOSITIONS - Formulations have been developed administering methscopolamine in multi-phases. In a preferred embodiment, the formulation contains methscopolamine in an immediate release. (“IR”) form and a sustained or delayed release (“DR”) form and/or poised release (“PR”) form. In another embodiment, the methscopolamine is released in a gradient, decreasing the side effects associated with rapidly elevated blood levels. In another embodiment the drug is bound to an ion-exchange resin, which can be suspended in a liquid or incorporated into a matrix for delayed, sustained and/or pulsed release. Dosage unit forms may be tablets, gels, liquids, capsules, beads, microparticles, films or lozenges. Multi-phase delivery can also be achieved through the use of a kit that provides for dosage escalation. This kit can be a blister pack or equivalent, wherein the drug is packaged so that a first dosage is taken, then sequentially larger dosages. The dosages can be the same in each unit, and instructions provided so that the correct dosage is obtained through the number of units and the time of administration or the dosages may be different, and the units ordered so dial the desired dosage administration profile is obtained when the patient takes the units in order as instructed. | 03-11-2010 |
20100069425 | GLUCOCORTICOID RECEPTOR MODULATOR AND METHODS OF USE - The present invention provides Compound (I): Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and methods for the treatment of inflammatory and immune disorders comprising administering to a patient in need thereof an effective amount of Compound (I) or a pharmaceutically acceptable salt thereof. | 03-18-2010 |
20100069426 | Therapeutic polymeric nanoparticles with mTor inhibitors and methods of making and using same - The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 1 to about 20 weight percent of a mTOR inhibitor; and about 70 to about 99 weight percent biocompatible polymer. | 03-18-2010 |
20100081681 | METHODS AND COMPOSITIONS FOR PREVENTING OR TREATING AGE-RELATED DISEASES - The invention provides methods for treating or preventing an age-related disease, condition, or disorder comprising administering a therapeutically effective amount of an inhibitor of TOR to a patient in need thereof. The invention also provides pharmaceutical compositions and topical formulations for treating or preventing an age-related disease, condition, or disorder comprising an inhibitor of TOR and a pharmaceutically acceptable carrier. In particular, the invention provides methods, pharmaceutical compositions, and topical formulations comprising rapamycin or an analog of rapamycin. | 04-01-2010 |
20100081682 | 39-Desmethoxy Derivatives of Rapamycin - The present invention relates to 39-desmethoxyrapamycin derivatives and their uses thereof. The present invention provides for the use of these compounds in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections. | 04-01-2010 |
20100087474 | MATERIALS AND METHODS FOR ENHANCED DEGRADATION OF MUTANT PROTEINS ASSOCIATED WITH HUMAN DISEASE - The invention features compositions and methods that are useful for treating or preventing a protein conformation disease in a subject by enhancing the degradation of misfolded proteins in vivo. | 04-08-2010 |
20100105717 | TACROLIMUS FOR IMPROVED TREATMENT OF TRANSPLANT PATIENTS - An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form. | 04-29-2010 |
20100113501 | Ophthalmic Composition Comprising Ascomycin - This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis. | 05-06-2010 |
20100130526 | Methods for Disease Therapy - The present invention discloses disease-linked SNPs, microRNAs, and microRNA-targeted mRNAs relevant to the pathogenesis of several major human disorders including, but not limited to, multiple types of cancers, type 2 diabetes, type 1 diabetes, Crohn's disease, coronary artery disease, hypertension, rheumatoid arthritis, bipolar disorder. Also provided are methods for the identification of disease phenotype-defining sets of SNPs, microRNAs, and mRNAs that are defined here as a “consensus disease phenocode” as well as methods of using the information provided by these consensus disease phenocodes for various diagnostic, prognostic, and/or therapeutic applications. | 05-27-2010 |
20100130527 | INDIVIDUALIZED CANCER TREATMENT - Methods to formulate treatments for individual cancer patients by assessing genomic and/or phenotypic differences between cancer and normal tissues and integrating the results to identify dysfunctional pathways are described. | 05-27-2010 |
20100152224 | SCOPINE MODULATORS OF MUSCARINIC ACETYLCHOLINE RECEPTOR - The present invention relates to new scopine modulators of muscarinic acetylcholine receptors, pharmaceutical compositions thereof, and methods of use thereof. | 06-17-2010 |
20100168151 | NOVEL PROCESSES FOR PREPARING 6-(DIFLUOROMETHOXY)[1]BENZOFURO[3,2-C]PYRIDINE-9-CARBALDEHYDE, A NOVEL INTERMEDIATE FOR THE SYNTHESIS OF PDE IV INHIBITORS - The present invention relates to novel processes for preparing 6-(difluoromethoxy)[1] benzofuro[3,2-c]pyridine-9-carbaldehyde, which is a novel and useful intermediate for preparing compounds with PDE4 inhibitory activity, such as 3,5-dichloro-4-(6-difluoromethoxybenzo[4,5]furo[3,2-c]pyridin-9-ylcarboxamido)-1-pyridiniumolate. | 07-01-2010 |
20100173928 | Phosphorylation and regulation of AKT/PKB by the rictor-mTOR complex - In certain aspects, the invention relates to methods for identifying compounds which modulate Akt activity mediated by the rictor-mTOR complex and methods for treating or preventing a disorder that is associated with aberrant Akt activity. | 07-08-2010 |
20100179182 | PHARMACEUTICAL FORMULATION - The present invention provides processes for making and forms of solid dispersions of pharmaceutical active ingredients. | 07-15-2010 |
20100184798 | Methods to Predict Cholesterol Elevations during Immunosuppressant Therapy - This invention provides methods to predict the degree of elevation of serum cholesterol levels in patients treated with immunosuppressive medication. This invention also provides treatment strategies based on these predictions and kits to carry out these methods. | 07-22-2010 |
20100197719 | MEDICAMENT COMPOSITIONS CONTAINING ANTICHOLINERGICALLY-EFFECTIVE COMPOUNDS AND BETAMIMETICS - A pharmaceutical composition comprising:
| 08-05-2010 |
20100210679 | PREVENTIVE AND THERAPEUTIC MEDICAMENT FOR GASTROESOPHAGEAL REFLUX DISEASE - The compound of the following formula: | 08-19-2010 |
20100210680 | TRICYCLIC HETEROCYCLIC DERIVATIVES - The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction. | 08-19-2010 |
20100227878 | NOSCAPINE ANALOGS AND THEIR USE IN TREATING CANCERS, INCLUDING DRUG-RESISTANT CANCERS - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. While the antitussive plant alkaloid, noscapine, binds tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyses pointed to a proton at position 9 of the isoquinoline ring that can be modified without compromising tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the isoquinoline ring kill human cancer cells resistant to other anti-microtubule agents, such as vincas and taxanes. Representative analogs include the 9-nitro, 9-bromo-, 9-iodo-, and 9-fluoro-noscapines, which bind tubulin and induce apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. Surprisingly, treatment with one of the analogs, 9-nitro-nos, at doses as high as 100 μM, did not affect the cell cycle profile of normal human fibroblasts. This selectivity for cancer cells represents a unique edge over the other available antimitotics. The compounds can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, the compounds are novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs. | 09-09-2010 |
20100227879 | LIQUID FORMULATIONS FOR TREATMENT OF DISEASES OR CONDITIONS - Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; non-dispersed mass-forming liquid formulations which form a gel or gel-like substance in an aqueous medium; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration, or wet age-related macular degeneration in a subject. The liquid formulations may comprise rapamycin or other therapeutic agents. | 09-09-2010 |
20100249172 | 9-CHLORO NOSCAPINE AND ITS USE IN TREATING CANCERS, INCLUDING DRUG-RESISTANT CANCERS - 9-Chloro-nos, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-chloro-nos, and methods of preparation and use thereof are disclosed. 9-Chloro-nos is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-Chloro-nos can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-chloro-nos is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs. | 09-30-2010 |
20100249173 | DIHYDROQUINOLINONES AS ECTOPARASITICIDES - Disclosed are uses of dihydroquinolinone derivatives for combating ectoparasites on non-human animals. Example ectoparasites include, for example, representatives of the order acarina, including ticks and mites. Also disclosed are compositions containing dihydroquinolinone derivatives. | 09-30-2010 |
20100249174 | CCR1 ANTAGONISTS AND METHODS OF USE THEREFOR - The invention provides compounds having the formula: | 09-30-2010 |
20100267760 | Methods of and Combination Therapies for Treating or Delaying the Onset of Dyskinesia - Methods of treating or delaying onset of levodopa-induced dyskinesia in an individual comprise administering to the individual an effective amount of mammalian target of rapamycin (mTOR) inhibitor. Methods of treating or delaying onset of dyskinesia in an individual, wherein the dyskinesia is induced by administration of a drug causing abnormal protein expression in striatal medium-size spiny neurons (MSNs), comprise administering to the individual an effective amount of mTOR inhibitor. Further, a combination therapy for an individual having Parkinson's Disease comprises levodopa or a precursor or functional analogue thereof and mTOR inhibitor. | 10-21-2010 |
20100280060 | Methods of screening and compositions for life span modulators - Identification of nucleic acids involved in life span diseases and disorders or related diseases and disorders, and the use of such methods for identifying candidate agents which modulate life span diseases and disorders or related diseases and disorders are provided. Compositions and methods for treating life span diseases and disorders or related diseases and disorders are provided. Pharmaceutical compositions for treating life span diseases and disorders or related diseases and disorders are also provided | 11-04-2010 |
20100280061 | NOVEL ANALGESIC THAT BINDS FILAMIN A - A compound, composition and method are disclosed that can bind to FLNA and provide analgesia. A contemplated compound has a structure that corresponds to Formula I, wherein R | 11-04-2010 |
20100280062 | (E)-N--METHANESULFONAMIDE AS GLUCOCORTICOID RECEPTOR MODULATOR FOR THE TREATMENT OF RHEUMATOID ARTHRITIS - The present invention provides Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and discloses methods for the treatment of inflammatory and immune disorders comprising administering to a patient in need thereof an effective amount of Compound (I) or a pharmaceutically acceptable salt thereof. | 11-04-2010 |
20100292266 | Oxazolyl Piperidine Modulators of Fatty Acid Amide Hydrolase - Certain oxazolyl piperidine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis). | 11-18-2010 |
20100305150 | TUBEROUS SCLEROSIS TREATMENT - Rapamycin derivatives for use in the treatment of neurocutaneous disorders. | 12-02-2010 |
20100305151 | O-Methylated Rapamycin Derivatives For Alleviation And Inhibition Of Lymphoproliferative Disorders - The present invention relates to methods of alleviating and inhibiting a lymphoproliferative disorder in a mammal, the method comprising administering one or more rapamycin derivatives (including rapamycin) to the mammal. Further, the invention provides a method for identifying agents which are useful for alleviating and inhibiting a lymphoproliferative disorders, as well as a method for identifying agents which are capable of inhibiting metastasis of lymphatic tumors in a mammal. | 12-02-2010 |
20100331356 | SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEMS - Self-microemulsifying drug delivery systems and microemulsions used to enhance the solubility of pharmaceutical ingredients comprising a polyoxyethylene sorbitan fatty acid ester emulsifier; a fatty acid ester co-emulsifier and an oil. | 12-30-2010 |
20110021553 | IMMUNOSUPPRESSIVE MACROLIDE POWDER FOR ORAL SUSPENSION - The present invention describes pharmaceutical compositions that comprise a tacrolimus powder for oral suspension that exhibits great stability as a powder for suspension and also, once prepared, as the extemporaneous suspension, without the formation of cake-like clusters, same having a satisfactory flavour and a pleasant aroma. The invention also describes the method for preparing the pharmaceutical compositions, same being a dry method that comprises mixing tacrolimus and pre-sieved pharmaceutically acceptable carriers for a suitable length of time, and the use of the pharmaceutical compositions for treating and preventing rejection of transplanted organs and atopic dermatitis. | 01-27-2011 |
20110028506 | Pharmaceutical Composition For Preventintion And Treatment Of Restenosis Comprising Isoxazole Derivatives - There is provided a pharmaceutical composition for prevention and treatment of restenosis comprising isoxazole derivatives. The pharmaceutical composition includes a therapeutic effective amount of isoxazole derivatives represented by Formula 1 or pharmaceutically available salts thereof. The pharmaceutical composition may be useful to prevent and treat vascular restenosis since the pharmaceutical composition shows an anti-restenosis activity and accelerates the re-endothelization. | 02-03-2011 |
20110028507 | PYRIDINE DERIVATIVES AND METHODS OF USE THEREOF - Disclosed herein are pyridine derivatives, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, pharmaceutical compositions comprising the same, and methods of modulating the level or activity of HIF in a subject, inhibiting hydroxylation of HIF α in a subject, modulating expression of HIF-regulated genes in a subject, treating an HIF-related disorder in a subject, increasing levels of endogenous EPO in a subject, or treating a disorder in a subject, using the disclosed compounds. | 02-03-2011 |
20110028508 | NOVEL PROCESS FOR THE PREPARATION OF SCOPINE ESTERS - The present invention relates to novel processes for the preparation of scopine esters and their quaternary salts. In particular, the present invention relates to a process for the preparation of tiotropium bromide, pharmaceutical compositions comprising tiotropium bromide and the use of such compositions in the treatment of respiratory disorders. | 02-03-2011 |
20110034503 | RAPAMYCIN AND ITS DERIVATIVES FOR THE TREATMENT OF LIVER-ASSOCIATED FIBROSING DISORDERS - A method for treating liver-associated fibrosing disorders or lupus, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula optionally in conjunction with a co-agent. | 02-10-2011 |
20110039876 | SOLUTION FORMULATIONS OF SIROLIMUS AND ITS ANALOGS FOR CAD TREATMENT - Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic drugs, agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the formation of blood clots. Therapeutic agents may also be delivered to the region of a disease site. In regional delivery, liquid formulations may be desirable to increase the efficacy and deliverability of the particular drug. Also, the devices may be modified to promote endothelialization. Various materials and coating methodologies may be utilized to maintain the drugs, agents or compounds on the medical device until delivered and positioned. In addition, the devices utilized to deliver the implantable medical devices may be modified to reduce the potential for damaging the implantable medical device during deployment. Medical devices include stents, grafts, anastomotic devices, perivascular wraps, sutures and staples. In addition, various polymer combinations may be utilized to control the elution rates of the therapeutic drugs, agents and/or compounds from the implantable medical devices. | 02-17-2011 |
20110071186 | ORGANIC COMPOUNDS - This invention is directed to ophthalmic compositions comprising an ascomycin for once-a-day administration. | 03-24-2011 |
20110098317 | USE OF UNSATURATED SPHINGOSINE COMPOUNDS AS CHEMOTHERAPEUTIC AGENTS FOR THE TREATMENT OF CANCER - The present invention is directed to unsaturated sphingosine compounds which are useful as therapeutic agents for the treatment of cancer and for the treatment of other diseases including diabetes and infection with intracellular bacteria. This invention is also directed to methods of using the compounds and pharmaceutical compositions comprising the compounds in treating these diseases. | 04-28-2011 |
20110118297 | Tivozanib and Temsirolimus in Combination - A method of treating a tumor in a human patient is disclosed. The method comprises co-administering to the patient: (a) a dose of 1.5 mg tivozanib per day; and (b) a dose of 25 mg temsirolimus per week. In some embodiments of the invention, the tivozanib is administered on a repeating schedule of one dose per day for three weeks, followed by one week without tivozanib administration. The disclosed method is particularly suitable for treatment of renal cell carcinoma. | 05-19-2011 |
20110118298 | COMPOSITIONS, KITS, AND METHODS FOR IDENTIFICATION, ASSESSMENT, PREVENTION, AND THERAPY OF CANCER - Described herein are compositions, kits, and methods for determining whether subjects having cancer(s) are likely to respond to treatment with an HSP90 inhibitor, as a single agent or in combination therapy. Further described are methods for prognosing a time course of disease in a subject having such cancer. | 05-19-2011 |
20110136852 | Rapamycin Derivative or an Impdh Inhibitor for Treating Polycystic Kidney Disease - A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5′-monophosphate dehydrogenase inhibitor or a rapamycin derivative. | 06-09-2011 |
20110152307 | OPHTHALMIC COMPOSITION COMPRISING ASCOMYCIN - This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis. | 06-23-2011 |
20110166172 | Rapamycin Carbonic Ester Analogues, Pharmaceutical Compositions, Preparations and Uses Thereof - Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl. | 07-07-2011 |
20110184010 | METHOD OF TREATING MANTLE CELL LYMPHOMA - This invention provides the use of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) in the treatment or inhibition of mantle cell lymphoma. | 07-28-2011 |
20110201639 | STABILIZED TACROLIMUS COMPOSITION - The invention relates to a stable pharmaceutical composition comprising comprising a solid dispersion of tacrolimus in a vehicle further comprising a stabilizing agent capable of providing a pH below 7 in the composition, as measured after re-dispersion in water, and preventing or reducing the formation upon storage of major degradation products of tacrolimus, in particular the 8-epitacrolimus. | 08-18-2011 |
20110201640 | TRICYCLIC COMPOUND - Provided is a tricyclic compound having a PPAR γ agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R | 08-18-2011 |
20110212988 | TACROLIMUS PREPARATION FOR EXTERNAL APPLICATIONS - The present invention provides tacrolimus containing ointment having low dermal irritation and excellent stability. It was found that an ointment comprising triacetin as a solubilizer for tacrolimus may sufficiently solubilize tacrolimus, has low dermal irritation and excellent stability. Preferably, the ointment of the present invention is an o/o type (oil-in-oil type) ointment in which tacrolimus-solubilized triacetin droplets are dispersed in an ointment base, preferably a mixture of beeswax and petrolatum. | 09-01-2011 |
20110224245 | Treatment Of Neurological Disorders Using Huperzine - Methods and compositions containing huperzine for direct delivery to central nervous system (CNS) tissue are used to alleviate pain and for the prevention and/or treatment of seizures and epilepsy. The invention is also directed to methods and compositions for using huperzine for the prevention and/or treatment of neuropathic pain and orthostatic hypotension. | 09-15-2011 |
20110224246 | PHARMACEUTICAL COMPOSITIONS COMPRISING ASCOMYCIN - The invention relates to pharmaceutical compositions comprising an ascomycin in dissolved form and a pharmaceutically acceptable cellulose derivative for prevention or reduction of crystal growth. | 09-15-2011 |
20110230515 | COMPOUNDS AND METHODS FOR TREATMENT AND PREVENTION OF DISEASES - A prodrug compound of a rapamycin analog and methods for inhibiting, treating, and preventing mammalian diseases. | 09-22-2011 |
20110230516 | CCR1 Antagonists and Methods of Use Therefor - The invention provides compounds having the formula: | 09-22-2011 |
20110237617 | THIENO[2,3-C] ISOQUINOLINES FOR USE AS INHIBITORS OF PARP - The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula: | 09-29-2011 |
20110251231 | Modified release compositions comprising tacrolimus - A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents. | 10-13-2011 |
20110251232 | Modified release compositions comprising tacrolimus - A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents. | 10-13-2011 |
20110263632 | Solid dispersions comprising tacrolimus - A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and/or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability. | 10-27-2011 |
20110275659 | Tacrolimus For Improved Treatment Of Transplant Patients - An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form. | 11-10-2011 |
20110281906 | SUSTAINED RELEASE FORMULATION FOR TACROLIMUS - A sustained release pharmaceutical composition for tacrolimus, comprising a solid dispersion containing tacrolimus or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a dissolution rate of tacrolimus after 4 hours from the beginning of a dissolution test is less than 35%, is disclosed. | 11-17-2011 |
20110288114 | COMPOSITIONS FOR THE TREATMENT OF FIBROTIC DISEASES OR CONDITIONS - A method of treating a fibrotic disease or condition in a patient comprising administering noscapine and a pharmaceutical carrier to said patient. | 11-24-2011 |
20110294844 | 9-AMINONOSCAPINE AND ITS USE IN TREATING CANCERS, INCLUDING DRUG-RESISTANT CANCERS - 9-aminonoscapine, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-aminonoscapine, and methods of preparation and use thereof are disclosed. 9-aminonoscapine is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-aminonoscapine can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-aminonoscapine is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs. | 12-01-2011 |
20110294845 | PARENTERAL FORMULATIONS - This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent. | 12-01-2011 |
20110301189 | STABLE PHARMACEUTICAL COMPOSITIONS OF RAPAMYCIN ESTERS - A stable pharmaceutical compositions of Rapamycin Esters, in particular Rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid that is free of antioxidants and a process of preparing the same. | 12-08-2011 |
20110306630 | PHARMACEUTICAL COMPOSITIONS COMPRISING COLLOIDAL SILICON DIOXIDE - A pharmaceutical composition comprising a macrolide solid dispersion, a disintegrant and colloidal silicon dioxide, wherein the composition comprises 1 to 5% colloidal silicon dioxide by weight. | 12-15-2011 |
20120010234 | USE OF VEGF-D IN THE DIAGNOSIS OF LYMPHANGIOLEIOMYOMATOSIS (LAM) DISEASE - Described herein are methods of diagnosing lymphangioleiomyomatosis (LAM) that permits differentiating LAM from another lung disorder. Methods of treatment are also provided. | 01-12-2012 |
20120015971 | OPHTHALMIC COMPOSITION COMPRISING ASCOMYCIN - This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis. | 01-19-2012 |
20120022095 | TOPICAL RAPAMYCIN FOR TREATMENT OF FACIAL ANGIOFIBROMAS IN TUBEROUS SCLEROSIS - The present disclosure provides for a method and a topical composition to treat facial angiofibromas in Tuberous Sclerosis by applying from about 0.25% to about 2% rapamycin to a small body surface area. | 01-26-2012 |
20120029009 | Tacrolimus For Improved Treatment Of Transplant Patients - An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form. | 02-02-2012 |
20120041019 | PROTEASE INHIBITORS - Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV. | 02-16-2012 |
20120046311 | CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREOF - Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: | 02-23-2012 |
20120059027 | TACROLIMUS INJECTION PREPARATION - A tacrolimus injection preparation comprising tacrolimus, polyoxyethylene castor oil (35), and non-aqueous solvent is disclosed. Preferably the weight ratio of polyoxyethylene castor oil (35) to tacrolimus in the injection preparation is 0-20:1. The injection preparation significantly decreased the clinical risk. | 03-08-2012 |
20120059028 | THIENO [2, 3-B] PYRIDINE DERIVATIVES AS VIRAL REPLICATION INHIBITORS - The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity. | 03-08-2012 |
20120065222 | DEVICES AND METHODS FOR REDUCING SCAR TISSUE FORMATION - Disclosed is a cytostatic drug attached to a sterile sheet that is designed to be placed between internal body tissues to prevent the formation of post-operative adhesions, which adhesions are really scar tissue formation. This sheet onto or into which the drug is placed may be either a permanent implant or it may be biodegradable. By impregnating an existing product such as the Johnson & Johnson SURGICEL™ absorbable hemostat gauze-like sheet with an anti-proliferative drug such as sirolimus, the biodegradable, drug impregnated mesh would act as a barrier to cell proliferation and hence be a deterrent to the formation of adhesions or scar tissue. Another embodiment of this invention is a cytostatic drug attached to a sheet that is placed at the site of an anastomosis to decrease scar tissue formation from within the vessel at the site of the anastomosis. | 03-15-2012 |
20120065223 | SOLID FORMS OF A CHEMOKINE RECEPTOR ANTAGONIST AND METHODS OF USE THEREOF - The citrate salt of (S)-4-(4-Chloro-phenyl)-1-{3-[7-(1-hydroxy-1-methyl-ethyl)-11H-10-oxa-1-aza-dibenzo[a,d]cyclohepten-5-ylidene]-propyl}-3,3-dimethyl-piperidin-4-ol, which may be used in pharmaceutical applications, is disclosed. The crystalline Citrate Salt, including particular single crystal forms and combinations of the single crystalline forms, are also discussed. Mixtures for forming the crystalline salts are discussed. As well, methods of producing the Citrate Salt, and crystalline forms thereof, and using such Citrate Salt, and crystalline forms thereof, in treating diseases associated with aberrant leukocyte recruitment, activation, or recruitment and activation are also discussed. | 03-15-2012 |
20120071500 | MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE - The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: | 03-22-2012 |
20120077837 | ANTI-TUMOR AGENT - A combination therapy for tumor is provided. Disclosed is a method of treating tumor, the method comprises administering to a patient, a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and everolimus represented by Formula (II): | 03-29-2012 |
20120077838 | Beta-2-Adrenoreceptor Agonists - Compounds of formula | 03-29-2012 |
20120101120 | PURE ISOMERS OF TRITOQUALINE - The invention provides an isolated stereoisomer of tritoqualine having the structure of FIG. | 04-26-2012 |
20120115896 | ISOGENIC HUMAN CELL LINES COMPRISING MUTATED CANCER ALLELES AND PROCESS USING THE CELL LINES - Isogenic human cell lines comprising at least one mutated cancer allele under the control of the cell line endogenous promoter, which corresponds to the wild-type cancer allele promoter are disclosed, as well as an in vitro process for determining sensitivity/resistance of a patient suffering from a tumor to a pharmacological agent comprising the following steps: a) identifying at least one mutated cancer allele in a tissue affected by a tumor of said patient; b) providing an isogenic human cell line representative of the tissue, wherein the cell line comprises at least the identified mutated cancer allele, which is under the control of the cell line endogenous promoter corresponding to the wild-type cancer allele promoter; c) putting in contact said cell line with the pharmacological agent; d) determining a variation of proliferation, apoptosis or cytotoxicity of the cell line in presence of the pharmacological agent; wherein the variation of proliferation, apoptosis car cytotoxicity indicative of the sensitivity/resistance of the patient tumor to the pharmacological agent. | 05-10-2012 |
20120115897 | Aryl (Ethanoic) Propanoic Acid Ascorbyl Ester, Preparation Method Thereof And Medicament Containing The Same - The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children. The aryl (ethanoic) propanoic acid ascorbyl ester can be converted into ascorbyl ester derivatives and the addition salts of the derivatives with pharmaceutical acid or pharmaceutical alkaline, which can improve the water solubility thereof, facilitate intravenously administration, reduce the onset time, improve the bioavailability, reduce the stimulation effect to gastrointestinal tract, and enhance the penetrating capacity to hemato encephalic barrier, and can be used as a novel medicament to be applied for antiphlogistic, antipyresis, analgesia, treatment of arthritis, dysmenorrheal, multiple sclerosis, pneumonia cystic fibrosis and patent ductus arteriosus of premature infants, and prevention and treatment of cerebral apoplexy, hypoxic-ischemic brain damage, senile dementia and certain cancers. | 05-10-2012 |
20120122913 | COMBINATION OF CURCUMINOIDS AND MTOR INHIBITORS FOR THE TREATMENT OF TAUOPATHIES - Methods, uses, compositions, combinations and kits relating to the decrease of Tau protein levels, and prevention and/or treatment of diseases or disorders associated with Tau protein (Tauophathies), such as Alzheimer's disease, using a curcuminoid and a mammalian target rapamycin (mTOR) inhibitor, are described. | 05-17-2012 |
20120136023 | Inhibitors of HIV Replication - The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication. | 05-31-2012 |
20120172389 | TREATMENT OF FIBROSING DISORDERS - A method for treating liver-associated fibrosing disorders or lupus, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula | 07-05-2012 |
20120178775 | METHODS FOR TREATING FRONTOTEMPORAL LOBAR DEGENERATION WITH UBIQUITINATED INCLUSIONS (FTLD-U) - Methods for rescuing learning, memory and/or motor function deficits associated with frontotemporal lobar degeneration with ubiquitinated inclusions (FTLD-U) are disclosed. The method comprises: a) administering to an animal having FTLD-U a therapeutically effective amount of an autophagy inducer; b) causing a decrease in the amount of ubiquitinated TDP-43 aggregation forms in the brain of the animal; and c) causing an improvement of the learning, memory capacities and/or motor function of the animal. | 07-12-2012 |
20120190705 | METHODS OF INHIBITING CHOROIDAL NEOVASCULARIZATION - The present invention relates to compositions and methods for inhibiting unwanted angiogenesis, particularly those of ocular tissues. The treatment, inhibition, and/or prevention of choroidal neovasculature (CNV) is provided, along with an animal model for CNV and imaging techniques that permit the screening of potential agents as anti-angiogenesis and anti-CNV agents. | 07-26-2012 |
20120202841 | Topical Compositions Comprising Ascomycins - The present invention relates to a composition for topical administration comprising an ascomycin and a carrier vehicle comprising means to retain water in the outer skin layer and means to hinder water evaporating from the skin. | 08-09-2012 |
20120202842 | 2-HETEROARYLCARBOXYLIC ACID AMIDES - The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. | 08-09-2012 |
20120208836 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF OBESITY AND RELATED DISORDERS - Provided herein are compositions and methods for the treatment of obesity and related disorders, including, but not limited to insulin resistance, diabetes, and hepatic steatosis. For example, in some embodiments, pharmaceutically acceptable compositions and methods are provided employing amlexanox, a derivative thereof, or a pharmaceutically acceptable salt thereof, alone or in combination with other agents and/or medical interventions, for the treatment, prevention, and management of such diseases and conditions. | 08-16-2012 |
20120214834 | IMMUNE ENHANCEMENT COMPOSITION AND KIT AND USE THEREOF - An immune enhancement composition is disclosed. The immune enhancement composition includes rapamycin, substituted quinoline and a pharmaceutically acceptable carrier, diluent, excipient or a combination thereof. An immune enhancement kit containing the two aforementioned compounds and a use of a combination containing the two aforementioned compounds as an immune enhancement composition are also disclosed. The application of the composition, kit and use is advantageous for promoting the activity of the immune system. | 08-23-2012 |
20120214835 | SENSITIZER, KIT AND USE FOR CANCER THERAPY - A cancer therapy sensitizer is disclosed. The cancer therapy sensitizer includes rapamycin and substituted quinoline. The present invention discloses a cancer therapy sensitization kit containing the two aforementioned compounds and a use of a combination of the two aforementioned compounds as a cancer therapy sensitizer as well. The application of the cancer therapy sensitizer, the kit and the use of the present invention is advantageous for improving the treatment effect of cancer therapies. | 08-23-2012 |
20120214836 | SENSITIZER, PHARMACEUTICAL COMPOSITION, KIT AND USE FOR TARGET THERAPY - A target therapy sensitizer including rapamycin and substituted quinoline is disclosed. In addition, a pharmaceutical composition containing the sensitizer, a target therapy sensitization kit containing the two aforementioned compounds, and a use of a combination of the two aforementioned compounds as a target therapy sensitizer are also disclosed. The application of the target therapy sensitizer, pharmaceutical composition, kit and use is advantageous for improving the treatment effect of target therapies. | 08-23-2012 |
20120214837 | SUBSTITUTED 6,7-DIALKOXY-3-ISOQUINOLINOL DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE 10 (PDE10A) - The invention relates to compounds of the formula | 08-23-2012 |
20120220619 | Rapamycin Derivative or an Impdh Inhibitor for Treating Polycystic Kidney Disease - A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5′-monophosphate dehydrogenase inhibitor or a rapamycin derivative. | 08-30-2012 |
20120252834 | NOVEL USE AND METHOD OF RAPAMYCIN TO TREAT TOXIC SHOCK - Rapamycin is used for prevention and treatment of toxic shock. The toxic shock is induced, for example, by a toxin, such as | 10-04-2012 |
20120252835 | STABLE TEMSIROLIMUS COMPOSITION AND PROCESS OF PREPARING SAME - The present disclosure describes a stable composition of Temsirolimus for parenteral administration. The composition includes BHA or BHT as anti-oxidants and alcoholic solvent. The pH of the composition is below 5.0. The composition also can include a chelating agent and/or a surfactant. A method of producing the composition is also described. | 10-04-2012 |
20120283285 | TREATMENT OF SOLID TUMORS WITH RAPAMYCIN DERIVATIVES - Rapamycin derivatives have interesting effects in the treatment of solid tumours, optionally in combination with a chemotherapeutic agent. | 11-08-2012 |
20120289536 | Pharmaceutical Compositions Comprising Colloidal Silicon Dioxide - A pharmaceutical composition comprising a macrolide solid dispersion, a disintegrant and colloidal silicon dioxide, wherein the composition comprises 1 to 5% colloidal silicon dioxide by weight. | 11-15-2012 |
20120295933 | TREATMENT OF COPD, GASTRO-ESOPHAGEAL REFLUX DISEASE (GERD), FOOD ALLERGIES AND OTHER GASTROINTESTINAL CONDITIONS AND DISORDERS AMELIORATED BY PROPER HISTAMINE MANAGEMENT USING A COMBINATION OF HISTIDINE DECARBOXYLASE INHIBATORS, LRA DRUGS, ANTI-H1 AND/OR ANTI-H2 DRUGS - The invention provides a method for the treatment of COPD and/or gastrointestinal disease conditions ameliorated by histamine management in a subject, comprising administering to the subject an effective amount of a histidine decarboxylase inhibitor. | 11-22-2012 |
20120302595 | FKBP52-TAU INTERACTION AS A NOVEL THERAPEUTICAL TARGET FOR TREATING THE NEUROLOGICAL DISORDERS INVOLVING TAU DYSFUNCTION - The invention relates generally to neuro-protection and repair in neurological disorders involving Tau dysfunction (including Alzheimer's disease). The invention describes AND INCLUDES a direct interaction between proteins FKBP52 and Tau. More particularly, the invention relates to a method for screening a drug for the prevention and treatment of neurological disorders involving Tau dysfunction comprising the following steps: a) determining the ability of a candidate compound, to modulate the interaction between a Tau polypeptide and a FKBP52 polypeptide and b) selecting positively the candidate compound that modulates said interaction. The present invention finally relates to diagnostic, prognostic, and monitoring assays of neurological disorders involving Tau dysfunction. | 11-29-2012 |
20120309780 | MICELLE COMPOSITION OF POLYMER AND PASSENGER DRUG - Hydrophobic drugs become more practical for treatments by being encapsulated in micelle compositions for increasing solubility. Micelle compositions may include an excipient tocopherol and/or prodrug formulations of the drug. Micelles extend the time period the drug remains in the micelles to improve drug circulation time and thereby drug delivery. Hydrophobic drugs for micelle encapsulation may include rapamycin, geldanamycin, and paclitaxel. Administration of these micelle compositions does not require Cremophor EL or Tween 80, avoiding serious side effects associated with these products which would previously accompany such drug administration. | 12-06-2012 |
20130005758 | MANUFACTURE, METHOD AND USE OF DRUG-ELUTING MEDICAL DEVICES FOR PERMANENTLY KEEPING BLOOD VESSELS OPEN - The invention relates to stents and catheter balloons having optimized coatings for eluting rapamycin as well as methods for manufacturing these coatings. | 01-03-2013 |
20130018069 | SUSTAINED RELEASE DELIVERY SYSTEMS FOR THE PREVENTION AND TREATMENT OF HEAD AND NECK CANCERS - The present invention discloses a method of treating a head and neck cancer or preventing the development of pre-malignant lesions to this cancer, by administering locally to the oral cavity, a sustained release drug delivery system comprising a drug for the treatment of this cancer or for the prevention of said lesions, and at least one polymer, such that said system is attached to a surface in the oral cavity and remains attached thereto for at least 1 hour, accompanied by release of the drug and maintaining an effective therapeutic concentration thereof in the cavity, for at least 1 hour. Further are disclosed a sustained release drug delivery system and a liquid precursor varnish composition to this system. | 01-17-2013 |
20130040979 | CCR1 INHIBITORS USEFUL FOR THE TREAMENT OF MULTIPLE MYELOMA AND OTHER DISORDERS - The invention relates to the use of inhibitors of CCR1 for the treatment of cancers and osteolytic bone disorders. In some embodiments, the invention relates to methods for the treatment of multiple myeloma, smoldering multiple myeloma and secondary bone cancers. | 02-14-2013 |
20130040980 | CCI-779 CONCENTRATE FORMULATIONS - This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent. | 02-14-2013 |
20130059877 | TREATMENT OF SOLID TUMORS WITH RAPAMYCIN DERIVATIVES - Rapamycin derivatives have interesting effects in the treatment of solid tumours, optionally in combination with a chemotherapeutic agent. | 03-07-2013 |
20130059878 | TREATMENT OF DISEASES MODULATED BY A H4 RECEPTOR AGONIST - The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier. | 03-07-2013 |
20130096150 | Substituted Azoanthracene Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof - The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial. | 04-18-2013 |
20130109713 | ANTIMICROBIAL AGENTS | 05-02-2013 |
20130116271 | TACROLIMUS-CONTAINING OIL-IN-WATER TYPE CREAMY COMPOSITION - The purpose is to provide a tacrolimus-containing pharmaceutical composition which is a creamy preparation for external application having good feeling upon use and has high stability of a main ingredient contained therein (high main ingredient residual ratio), and allows easy control of skin concentration of the main ingredient. | 05-09-2013 |
20130150397 | RAPAMYCIN COMPOSITION - In one aspect, the present invention is directed to a dry, flowable and compressible rapamycin composition comprising a specific mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers. In other aspects, the present invention is directed to a method of making the composition. | 06-13-2013 |
20130165471 | 2-SUBSTITUTED-THIENOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS - Disclosed herein are 2-substituted-thienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula | 06-27-2013 |
20130172383 | TREATMENT OF FIBROSING DISORDERS - A method for treating liver-associated fibrosing disorders or lupus, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula | 07-04-2013 |
20130178494 | PHENYL N-MUSTARD LINKED TO DNA-AFFINIC MOLECULES OR WATER-SOLUBLE ARYL RINGS, METHOD AND THEIR USE AS CANCER THERAPEUTIC AGENTS - The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy. | 07-11-2013 |
20130184305 | PROCESS FOR PREPARATION OF NOVEL 42-O-(HETEROALKOXYALKYL) RAPAMICIN COMPOUNDS WITH ANTI-PROLIFERATIVE PROPERTIES - The invention discloses novel 42-0-(heteroalkoxyalkyl) rapamycin compounds of formula (1) and process for preparation thereof. These compounds are useful in the treatment of hyperproliferative vascular diseases such as restenosis and atherosclerosis Wherein, R denotes 3, 4 and 5 membered 3-hydroxy heteroalkoxyalkyl compounds selected from Tetrahydrofuran-3-ol, Oxetan-3-ol, Tetrahydropyran-3-ol, Tetrahydro-4- methyl furan-3-ol, Tetrahydro-2,5,5-trimethyl furan-3-ol, Tetrahydro-2,5-diethyl-2-methyl furan-3-ol, Tetrahydro-6-methoxy-2-methyl 2H-Pyran-3-ol and Tetrahydro-2,2-dimethyl-6-phenyl 2H-Pyran-3-ol. | 07-18-2013 |
20130197024 | LIQUID FORMULATIONS FOR TREATMENT OF DISEASES OR CONDITIONS - Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; non-dispersed mass-forming liquid formulations which form a gel or gel-like substance in an aqueous medium; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration, or wet age-related macular degeneration in a subject. The liquid formulations may comprise rapamycin or other therapeutic agents. | 08-01-2013 |
20130217717 | COMPOUND USEFUL FOR THE TREATMENT OF NONSENSE-MUTATION-MEDIATED DISEASES AND PHARMACEUTICAL COMPOSITION COMPRISING SAID COMPOUND - The present invention relates to the compound of formula (I) | 08-22-2013 |
20130225629 | TARGETING PI3K/MTOR SIGNALLING AND NEUTROPHIL RECRUITMENT FOR TREATMENT OF ENTERITIS - The presently disclosed subject matter generally relates to methods and compositions for treating enteritis. More particularly, the presently disclosed subject matter relates to methods and compositions for modulating a component of a PI3K/mTOR pathway. In some embodiments, the methods and compositions of the presently disclosed subject matter generally relates to the treatment of campylobacteriosis. More particularly, the methods and compositions of the presently disclosed subject matter relate to the treatment of campylobacteriosis by modulating a component of a PI3K/mTOR pathway. | 08-29-2013 |
20130225630 | TOPICAL RAPAMYCIN FOR TREATMENT OF FACIAL ANGIOFIBROMAS IN TUBEROUS SCLEROSIS - The present disclosure provides for a method and a topical composition to treat facial angiofibromas in Tuberous Sclerosis by applying from about | 08-29-2013 |
20130225631 | TOPICAL RAPAMYCIN FOR TREATMENT OF FACIAL ANGIOFIBROMAS IN TUBEROUS SCLEROSIS - The present disclosure provides for a method and a topical composition to treat facial angiofibromas in Tuberous Sclerosis by applying from about 0.25% to about 2% rapamycin to a small body surface area. | 08-29-2013 |
20130231362 | Mast Cell Stabilizers in the Treatment of Obesity - The present invention is directed to methods of treating or preventing the development of obesity by administering compounds that stabilize mast cells. In addition, it includes pharmaceutical compositions which have both a mast cell stabilizer and instructions regarding the use of the stabilizer in treating or preventing obesity. | 09-05-2013 |
20130245058 | MEDICAL PRODUCT WITH A PARTICLE-FREE COATING RELEASING AN ACTIVE SUBSTANCE - Embodiments described herein concern medical products, which come into contact with the organism, such as short-term implants and long-term implants, coated with at least one layer, containing a molecular-disperse distributed or dissolved active substance in at least one carrier and optionally one or more adjuvants, wherein the at least one layer forms a stably spreadable solution, methods for making this coating of stably spreadable solution and use of the medical products coated with the stably spreadable solution. | 09-19-2013 |
20130252997 | TREATING UNWANTED OCULAR CONDITION USING AN ASCOMYCIN MACROLACTAM - The present invention provides compositions and uses of an ascomycin macrolactam for the treatment of an unwanted ocular condition occurring in a patient undergoing treatment with a therapeutically active agent for the treatment of cancer. | 09-26-2013 |
20130252998 | CCI-779 FORMULATIONS FOR PARENTERAL ADMINISTRATION - This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent. | 09-26-2013 |
20130252999 | 2-PHENYL-4-QUINOLONES AS ANTICANCER AGENTS - 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na | 09-26-2013 |
20130253000 | TREATMENT OF SOLID TUMORS WITH RAPAMYCIN DERIVATIVES - The present invention is directed to the use of rapamycin derivatives for use in treating solid tumors, optionally in combination with a chemotherapeutic agent. | 09-26-2013 |
20130261148 | PROTECTED ANTIMICROBIAL COMPOUNDS FOR HIGH TEMPERATURE APPLICATIONS - Provided are protected antimicrobial compounds which are useful for controlling microorganisms in aqueous or water-containing systems, such as oil or gas field fluids, at elevated temperature. The antimicrobial compounds are of the formula I: | 10-03-2013 |
20130267550 | Compounds and Methods for Treating Aberrant Adrenocartical Cell Disorders - Methods and compositions are provided for treatment of disorders associated with aberrant adrenal cortex cell behavior, including (but not limited to) treatment of adrenocortical carcinoma (ACC), Cushing's syndrome and/or pituitary ACTH excess (Cushing's Disease). Such methods involve administration of an effective amount N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)-methyl)urea hydrochloride to the patient. | 10-10-2013 |
20130289063 | CCR1 ANTAGONISTS AND METHODS OF USE THEREFOR - The invention provides compounds having the formula: | 10-31-2013 |
20130296359 | TREATMENT OF SOLID TUMORS WITH RAPAMYCIN DERIVATIVES - The present invention is directed to the use of rapamycin derivatives for use in treating solid tumors, optionally in combination with a chemotherapeutic agent. | 11-07-2013 |
20130303565 | USE OF A NEW HISTAMINE H4 AGONIST FOR THE TREATMENT OF ACUTE LEUKEMIA - A method of treating leukemia by administering an H4 agonist of histamine, 7-amino-4,5,6-triethoxy-3-(5,6,7,8-tetrahydro-4-methoxy-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl) phthalide (tritoqualine), to a subject is provided. | 11-14-2013 |
20130310416 | Methods and Compositions for Preventing or Treating Age-Related Diseases - The invention provides methods for treating or preventing an age-related disease, condition, or disorder comprising administering a therapeutically effective amount of an inhibitor of TOR to a patient in need thereof. The invention also provides pharmaceutical compositions and topical formulations for treating or preventing an age-related disease, condition, or disorder comprising an inhibitor of TOR and a pharmaceutically acceptable carrier. In particular, the invention provides methods, pharmaceutical compositions, and topical formulations comprising rapamycin or an analog of rapamycin. | 11-21-2013 |
20130317053 | EXTERNALLY-USED DRUG FOR TREATING SKIN DISORDER AND METHOD FOR PRODUCING SAME - An external medicine of the present invention includes a gel composition or an ointment composition, each of which contains sirolimus and/or a derivative thereof. Accordingly, provided is an external medicine which enables sirolimus, in an amount sufficient to treat a skin disease, to be absorbed into an affected part without causing a side effect. | 11-28-2013 |
20130324570 | INHIBITORS OF LATE SV40 FACTOR (LSF) AS CANCER CHEMOTHERAPEUTICS - The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formulas (I)-(XXVI) as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC. | 12-05-2013 |
20130338183 | COMPOSITIONS AND METHODS FOR MOBILIZING STEM CELLS - The present invention relates to the field of hematopoietic stem cells. More specifically, the present invention provides methods and composition useful for peripheral blood stem cell mobilization. In one embodiment, a method of treating an organ transplant recipient comprises administering to the recipient a low dose of Tacrolimus in an amount sufficient to mobilize stem cells to the peripheral blood of the recipient. In a specific embodiment, the low dose of Tacrolimus is in the range of about 0.05 mg/kg to about 0.5 mg/kg. | 12-19-2013 |
20140011834 | STABLE FORMULATIONS, AND METHODS OF THEIR PREPARATION AND USE - Described herein are formulations comprising therapeutic agents, including but not limited to formulations comprising rapamycin, pharmaceutical formulations, unit dose forms, kits, methods of preparing formulations, and methods of using formulations. Such formulations and methods have increased stability. | 01-09-2014 |
20140018384 | QUINOLINONE DERIVATIVES FOR USE IN THE TREATMENT OF AN AUTOIMMUNE DISEASE AND/OR AN INFLAMMATORY DISEASE - There is provided compounds of formula I, wherein X | 01-16-2014 |
20140038998 | STABILIZED TACROLIMUS COMPOSITION - The invention relates to a stable pharmaceutical composition comprising comprising a solid dispersion of tacrolimus in a vehicle further comprising a stabilizing agent capable of providing a pH below 7 in the composition, as measured after re-dispersion in water, and preventing or reducing the formation upon storage of major degradation products of tacrolimus, in particular the 8-epitacrolimus. | 02-06-2014 |
20140045881 | GENES FREQUENTLY ALTERED IN PANCREATIC NEUROENDOCRINE TUMORS - Pancreatic Neuroendocrine Tumors (PanNETs) are a rare but clinically important form of pancreatic neoplasia. To explore the genetic basis of PanNETs, we determined the exomic sequences of ten non-familial PanNETs and then screened the most commonly mutated genes in 58 additional PanNETs. Remarkably, the most frequently mutated genes specify proteins implicated in chromatin remodeling: 44% of the tumors had somatic inactivating mutations in MEN-1, which encodes menin, a component of a histone methyltransferase complex; and 43% had mutations in genes encoding either of the two subunits of a transcription/chromatin remodeling complex consisting of DAXX (death-domain associated protein) and ATRX (alpha thalassemia/mental retardation syndrome X-linked). Clinically, mutations in the MEN1 and DAXX/ATRX genes were associated with better prognosis. We also found mutations in genes in the mTOR (mammalian target of rapamycin) pathway in 14% of the tumors, a finding that could potentially be used to stratify patients for treatment with mTOR inhibitors. | 02-13-2014 |
20140066472 | METHODS OF PREVENTING THE DEVELOPMENT OF MUCOSITIS AND RELATED DISORDERS - Disclosed is a method of preventing the development of mucositis in a subject undergoing radiation therapy or chemotherapy for a disease in need thereof comprising administering an effective amount of a mammalian target of rapamycin (mTOR) inhibitor, such as rapamycin, to the subject. Further disclosed is a method of increasing the lifespan of a normal oral keratinocyte and/or reducing oxidative stress in a normal epithelial cell, wherein the method comprises administering an effective amount of an mTOR inhibitor to a subject undergoing radiation therapy or chemotherapy for a disease in need thereof. | 03-06-2014 |
20140066473 | MODIFIED RELEASE COMPOSITIONS COMPRISING TACROLIMUS - A modified release composition comprising tacrolimus which is useful for the treatment or prevention of rejection reactions by transplantation of organs or tissues. | 03-06-2014 |
20140066474 | COMBINATION OF PHOSPHATIDYLINOSITOL-3-KINASE (PI3K) INHIBITOR AND A MTOR INHIBITOR - The present invention relates to a pharmaceutical combination comprising a phosphatidylinositol-3-kinase (PI3K) inhibitor compound which is a 2-carboxamide cycloamino urea derivative or a pharmaceutically acceptable salt thereof and at least one mammalian target of rapamycin (mTOR) inhibitor or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising such a combination; and the uses of such a combination in the treatment proliferative diseases, more specifically of mammalian target of rapamycin (mTOR) kinase dependent diseases. | 03-06-2014 |
20140073665 | MODIFIED RELEASE COMPOSITIONS COMPRISING TACROLIMUS - A modified release composition comprising tacrolimus which is useful for the treatment or prevention of rejection reactions by transplantation of organs or tissues. | 03-13-2014 |
20140088135 | IMMUNOSUPPRESSIVE MACROLIDE POWDER FOR ORAL SUSPENSION - The present invention describes pharmaceutical compositions that comprise a tacrolimus powder for oral suspension that exhibits great stability as a powder for suspension and also, once prepared, as the extemporaneous suspension, without the formation of cake-like clusters, same having a satisfactory flavour and a pleasant aroma. The invention also describes the method for preparing the pharmaceutical compositions, same being a dry method that comprises mixing tacrolimus and presieved pharmaceutically acceptable carriers for a suitable length of time, and the use of the pharmaceutical compositions for treating and preventing rejection of transplanted organs and atopic dermatitis. | 03-27-2014 |
20140094484 | SUSTAINED DELIVERY FORMULATIONS OF RAPAMYCIN COMPOUNDS - The present invention relates to a rapamycin sustained release delivery system for treatment of diseases responsive to rapamycin. The sustained release delivery system of the invention includes a flowable composition containing rapamycin or a rapamycin derivative, which is capable of providing an implant containing the rapamycin or derivative thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid and rapamycin or a rapamycin derivative. | 04-03-2014 |
20140094485 | SOLID STATE FORMS OF HIV INHIBITOR - The invention relates to a novel hemi-succinate salt form of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid and a novel crystalline form thereof, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection. | 04-03-2014 |
20140094486 | SOLID STATE FORMS OF HIV INHIBITOR - The invention relates to novel crystalline forms of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid, the hydrochloride salt thereof, novel crystalline forms of the hydrochloride salt, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection. | 04-03-2014 |
20140107148 | End-Capped Poly(Ester Amide) Copolymers - This invention relates to poly(ester amide)s (PEAs) comprising inactivated terminal amino and carboxyl groups, methods of synthesizing the inactivated PEAs and uses for them in the treatment of vascular diseases. | 04-17-2014 |
20140113928 | METHODS AND COMPOSITIONS FOR ENHANCING FERTILITY AND/OR INHIBITING PREGNANCY FAILURE AND RESTORING GLUCOSE TOLERANCE - Methods and compositions for enhancing fertility and/or inhibiting pregnancy failure, restoring glucose tolerance and/or preventing glucose intolerance and/or maintaining glucose homeostasis and/or inducing or enhancing weight loss, treating dyslipidemia, treating hypertestosteronism or hyperandrogenism, and/or treating type 2 diabetes in an individual in need thereof are provided. These involve compositions that inhibit expression of interferon-gamma (IFN-γ) or a downstream IFN-γ-stimulated gene, which is preferably a macrolide immunosuppressant compound. | 04-24-2014 |
20140113929 | MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV replication of formula (I) | 04-24-2014 |
20140121233 | Synthesis and Characterization of Second Generation Benzofuranone Ring Substituted Noscapine Analogs - Compound of Formula (I) and use thereof as microtubule modulating agents in the treatment of cancer are described herein. | 05-01-2014 |
20140121234 | INHALANT PROPELLANT-FREE AEROSOL FORMULATION - The invention relates to inhalant propellant-free aerosol formulations containing at least one inert, non-volatile auxiliary substance for adjusting defined droplet sizes. | 05-01-2014 |
20140135358 | Use of FK506 for the Treatment of Pulmonary Arterial Hypertension - A method of reducing pulmonary arterial hypertension in a mammal that employs FK506 is provided. In certain embodiments, the method comprises administering FK506 to a mammal having pulmonary arterial hypertension associated with defective MBPR2 signaling at a dosage sufficient to reduce blood pressure in the pulmonary artery of the mammal. | 05-15-2014 |
20140142134 | INHIBITORS OF BACTERIAL TYPE III SECRETION SYSTEM - Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as | 05-22-2014 |
20140179731 | Tacrolimus For Improved Treatment Of Transplant Patients - An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form. | 06-26-2014 |
20140187574 | USE OF RAPAMYCIN DERIVATIVES IN VASCULOPATHIES AND XENOTRANSPLANTATION - Use of a rapamycin derivative of formula I as defined in the claims for preventing or treating vasculopathies and manifestations of xenotransplantation. | 07-03-2014 |
20140194461 | RAPAMYCIN FORMULATIONS AND METHODS OF THEIR USE - Described herein are liquid rapamycin formulations. Described herein are methods of treating or preventing diseases or conditions, such as choroidal neovascularization, wet AMD and dry AMD, and preventing transition of dry AMD to wet AMD, using the liquid rapamycin formulations described herein. | 07-10-2014 |
20140206710 | Compound ambroxol hydrochloride composition and its preparation method - A compound ambroxol hydrochloride composition and a preparation method therefor, which relate to the field of medicine. 0.1%-99.9% by mass of ambroxol hydrochloride and 99.9%-0.1% by mass of scopolamine serving as main ingredients and mannitol are added into water for injection; stir to dissolve, then adjusting to pH 5.0 by adding an NaOH solution; add 0.1% of activated carbon with stirring for 30 minutes; filter out the activated carbon, and then filtering the liquid with 0.45 μm and 0.22 μm microporous filter membranes; fill the filtered liquid into a large plate or a vial; send into a lyophilizer, cool to −40° C., and hold the temperature for 2 hours; warm to −5° C. to 0° C. slowly to lyophilize the liquid, heat to 35° C., and hold the temperature for 3 hours; take out of the lyophilizer after lyophilizing to obtain a lyophilized powder injection containing ambroxol hydrochloride and scopolamine; crush the lyophilized powder injection under a sterile conditions, and sieve with a 180-mesh sieve to obtain sterile lyophilized powder containing ambroxol hydrochloride and scopolamine; and prepare various dosage forms by using the lyophilized powder as a raw material. | 07-24-2014 |
20140221418 | HYALURONIC ACID BASED COPOLYMERS - Hyaluronic acid (HA) conjugates or crosslinked HAs compositions for coating an implantable device are provided. The implantable device can be used for treating a disorder such as atherosclerosis, thrombosis, restenosis, high cholesterol, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, and combinations thereof. | 08-07-2014 |
20140256766 | TRANSMUCOSAL DRUG DELIVERY SYSTEM - Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH. | 09-11-2014 |
20140288115 | COMPOSITIONS AND METHODS FOR TREATING BRAIN CANCER - It is discovered that noscapine is effective in treating temozolomide (TMZ)-resistant brain cancer. Provided are compositions and methods of treating brain cancer patients, in particular those that are TMZ-resistant. The patients are treated by administration of a therapeutically effective amount of noscapine or an analog thereof. In certain aspects, TMZ is also administered to the patients. Examples of brain cancers include glioma such as glioblastoma multiforme. | 09-25-2014 |
20140296279 | INTRAVASCULAR DELIVERY OF NANOPARTICLE COMPOSITIONS AND USES THEREOF - The present invention provides methods of delivering a composition comprising nanoparticles that comprise a macrolide and an albumin by directly injecting the nanoparticle composition into the blood vessel wall or the tissue surrounding the blood vessel wall. The methods can be used for inhibiting negative remodeling or vascular fibrosis in the blood vessel and are useful for treating various diseases. | 10-02-2014 |
20140303201 | CANCER THERAPY - The subject invention provides for cancer therapy. | 10-09-2014 |
20140309253 | SUBSTITUTED 6,7-DIALKOXY-3-ISOQUINOLINOL DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE 10 (PDE 10A) - The invention relates to compounds of the formula | 10-16-2014 |
20140315942 | COMPOSITIONS FOR TRANSDERMAL DELIVERY OF mTOR INHIBITORS - The present invention is drawn to formulations for the transdermal delivery of rapamycin or other related compounds. Specifically, in one embodiment a formulation for transdermally delivering rapamycin includes an mTOR inhibitor, such as rapamycin, water, a polymer having surfactant properties, a polymer having thickening properties, a solvent for solubilizing the mTOR inhibitor, a glycol, a C | 10-23-2014 |
20140329848 | DEUTERATED AMLEXANOX - Provided herein is technology relating to deuterated amlexanox and particularly, but not exclusively, to compositions comprising deuterated amlexanox, methods of producing deuterated amlexanox, and uses of deuterated amlexanox. | 11-06-2014 |
20140336215 | Rhinitis Treatment Regimens - A method of treating rhinitis and rhinorrhea includes taking a daytime oral dosage unit containing a non-sedating antihistamine for treating rhinitis and an anticholinergic agent having limited capacity to cross blood-brain barrier for treating rhinorrhea, and taking a nighttime oral dosage unit containing a non-sedating anticholinergic agent that has limited capacity to cross blood-brain barrier and that is in a lower amount than the amount in the daytime oral dosage unit for treating rhinorrhea or no anticholinergic agent. A treatment regimen for rhinitis with rhinorrhea includes a daytime oral dosage unit containing a non-sedating antihistamine for treating rhinitis and an anticholinergic agent having limited capacity to cross blood-brain barrier for treating rhinorrhea, and a nighttime dosage unit containing a non-sedating anticholinergic agent that has limited capacity to cross blood-brain barrier and that is in a lower amount than the amount in the daytime oral dosage unit for treating rhinorrhea or no anticholinergic agent. | 11-13-2014 |
20140343090 | LOCAL DELIVERY OF WATER-SOLUBLE OR WATER-INSOLUBLE THERAPEUTIC AGENTS TO THE SURFACE OF BODY LUMENS - A method and device for local delivery of a water-insoluble therapeutic agent to the tissue of a normal or diseased body lumen is disclosed. An expandable structure of a medical disposable device, such as a balloon of a balloon catheter, is coated with a non-durable coating which comprises poly(HEMA) complexed with iodine and has a substantially water-insoluble therapeutic agent dispersed therein. The medical disposable device is inserted into a body lumen, and expanded to contact the non-durable coating against the body lumen and deliver the substantially water-insoluble therapeutic agent to the body lumen tissue. | 11-20-2014 |
20140343091 | BETA2-ADRENOCEPTOR AGONISTS - Compounds of formula | 11-20-2014 |
20140357660 | GENE EXPRESSION SIGNATURES OF NEOPLASM RESPONSIVENESS TO THERAPY - Gene signatures for determining whether a neoplasm (such as a multiple myeloma neoplasm) is sensitive to mTORi/HDACi combination therapy and/or for determining the prognosis of a neoplasm in a subject are described. Some embodiments include determining whether a neoplasm is sensitive to mTORi/HDACi combination therapy by predicting whether mTORi/HDACi combination therapy will successfully treat the neoplasm, for example increasing survival of the subject with the neoplasm. In some embodiments, determining the prognosis includes predicting the outcome (such as chance of survival) of the subject with a neoplasm. Also disclosed are reagents, for example arrays, for use with the disclosed methods, as well as computer implementation of the disclosed methods. | 12-04-2014 |
20140371259 | COMPOUNDS AND METHODS FOR INHIBITION OF AP ENDONUCLEASE-1/REDOX FACTOR-1 (HAPE1) ACTIVITY - A method for treating a neoplasm in a subject, comprising co-administering to the subject a therapeutically effective amount of an anticancer agent and a substituted 6,7-methylenedioxy-4-amino-quinoline, or a pharmaceutically acceptable salt or ester thereof. | 12-18-2014 |
20140378500 | METHODS FOR PREDICTING TUMOR REPONSE TO TARGETED THERAPIES - A method for identifying cancer patients that are likely to be responders or non-responders to a signal transduction pathway inhibitor is described. | 12-25-2014 |
20140378501 | SCOPOLAMINE FOR THE TREATMENT OF DEPRESSION AND ANXIETY - Provided are methods and compositions for the treatment of depression and anxiety. The compositions contain scopolamine, or an analog thereof, and can optionally include one or more psychoactive agents. Further provided is an inhaler containing scopolamine, or an analog thereof, in a pharmaceutically acceptable carrier. | 12-25-2014 |
20150011578 | METHODS FOR IMPROVING MUSCLE STRENGTH - The present invention relates to methods for improving muscle strength and treating muscular dystrophy. | 01-08-2015 |
20150018383 | BIOMARKERS OF RENAL DISORDERS - The present invention is directed to the use of marker for Akt2 activation in podocytes as a biomarker to predict toxicity of mTOR inhibitors. Another aspect of the invention relates to a method for preventing graft rejection comprising administering a selective mTORC1 or Akt1 inhibitor in a subject in need thereof. | 01-15-2015 |
20150057306 | COMPOSITIONS COMPRISING SCOPOLAMINE AND KETAMINE IN THE TREATMENT OF DEPRESSION - Described are compositions and methods for administering scopolamine and ketamine in the treatment of depression (e.g., Major Depressive Disorder and Treatment-Resistant Depression). | 02-26-2015 |
20150087671 | LOW BURST SUSTAINED RELEASE LIPOPHILIC AND BIOLOGIC AGENT COMPOSITIONS - A drug delivery composition including a lipophilic agent or a biologic agent and a polymer wherein the lipophilic agent exhibits sustained release and wherein there is less than 35% agent release within the first hour of elution. A drug delivery composition including a lipophilic agent or a biologic agent and a polymer wherein the elution profile is substantially linear, and wherein there is less than 35% agent release within the first hour of elution. The lipophilic agent may be crystalline and the biologic agent may be in active form. | 03-26-2015 |
20150133487 | TRITOQUALINE FOR USE IN THE TREATMENT OF CYSTIC FIBROSIS - This invention relates to tritoqualine for use in the treatment of cystic fibrosis or any one of its complications. The invention also relates to the method for the treatment of cystic fibrosis or any one of its complications by administering tritoqualine. The invention can be used to improve the condition of individuals with cystic fibrosis. | 05-14-2015 |
20150290176 | USE OF MTOR INHIBITORS TO TREAT VASCULAR COGNITIVE IMPAIRMENT - Disclosed are methods and compositions for the treatment or prevention of vascular cognitive impairment. The disclosed methods and compositions include rapamycin, a rapamycin analog, or another such inhibitor of the target of rapamycin (TOR). | 10-15-2015 |
20150328192 | RAPAMYCIN ANALOGS TARGETING PROTEASOME FUNCTION IN THE TREATMENT OF CANCER - The invention provides for treatment of cancers using a rapamycin analog, optionally including bortezomib. In particular, the invention addresses the treatment of bortezomib-resistant cancers using seco-rapamycin and optionally a second proteasome inhibitor. This invention relates to oncology and medicine, and more particularly to treatment of cancer. In particular, rapamycin analogs such as seco-rapamycin may be used advantageously to target the proteasome in cancer cells, optionally in conjunction with proteasome inhibitors such as bortezomib. | 11-19-2015 |
20150335623 | METHODS FOR IMPROVING MUSCLE STRENGTH - The present invention relates to methods for improving muscle strength and treating muscular dystrophy. | 11-26-2015 |
20150335794 | SMART COATING FOR IMPLANTABLE DEVICES - The present invention relates to a coating for medical implants. The coating contains an active agent that is intended to have an effect on the surrounding tissue after placement of the implant. This effect is activated in the presence of cells. The active agent is released from the coating under the direct influence of the cells. | 11-26-2015 |
20150344491 | [1,3] DIOXOLO [4,5-G] QUINOLINE-6(5H)THIONE DERIVATIVES AS INHIBITORS OF THE LATE SV40 FACTOR (LSF) FOR USE IN TREATING CANCER - The present invention relates generally to methods, compounds and/or compositions suitable for inhibiting, preventing and/or treating cancer, e.g. hepatocellular carcionoma (HCC). In some embodiments, the invention relates to the use of small-molecule compounds to inhibit, prevent and/or treat expression of the transcription factor Late SV40 Factor (LSF) for treatment of HCC or other cancer types. | 12-03-2015 |
20160016967 | ARYL AMIDE-BASED KINASE INHIBITORS - The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1. | 01-21-2016 |
20160022652 | METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF SYMPTOMS OF ANXIETY AND PANIC USING BETA ADRENERGIC RECEPTOR ANTAGONIST AND MUSCARINIC RECEPTOR ANTAGONIST COMBINATIONS - The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist. The invention provides methods for treating psychiatric condition or disorder or the symptoms thereof, including acute anxiety and panic comprising administering a pharmaceutical composition consisting essentially of a beta adrenergic receptor antagonist drug and an antiemetic muscarinic receptor antagonist drug in a therapeutically effective amount to stop or reduce the symptoms of anxiety and/or panic. The pharmaceutical compositions are administered as treatments immediately in advance of, at the onset of, or during an acute anxiety and/or panic episode. | 01-28-2016 |
20160022653 | METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF SYMPTOMS OF ANXIETY AND PANIC USING BETA ADRENERGIC RECEPTOR ANTAGONIST AND MUSCARINIC RECEPTOR ANTAGONIST COMBINATIONS - The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist. The invention provides methods for treating psychiatric condition or disorder or the symptoms thereof, including acute anxiety and panic comprising administering a pharmaceutical composition consisting essentially of a beta adrenergic receptor antagonist drug and an antiemetic muscarinic receptor antagonist drug in a therapeutically effective amount to stop or reduce the symptoms of anxiety and/or panic. The pharmaceutical compositions are administered as treatments immediately in advance of, at the onset of, or during an acute anxiety and/or panic episode. | 01-28-2016 |
20160024104 | THERAPEUTIC COMPOUNDS - The invention provides compounds of formula I: | 01-28-2016 |
20160030402 | SUSTAINED-RELEASE NANOPARTICLE COMPOSITIONS AND METHODS FOR USING THE SAME - The present invention is a composition composed of a therapeutic agent encapsulated in a copolymer of an N-alkylacrylamide, a vinyl monomer, and a polyethylene glycol (PEG) conjugate and a method for using the same in the treatment or prevention of a disease or condition. | 02-04-2016 |
20160060271 | DEUTERATED AMLEXANOX - Provided herein is technology relating to deuterated amiexanox and particularly, but not exclusively, to compositions comprising deuterated amiexanox, methods of producing deuterated amiexanox, and uses of deuterated amiexanox. Provided herein are deuteratecl amiexanox compounds for the treatment of obesity, insulin resistance, diabetes, and steatosis. In addition, the deuterated compounds are anti-inflammatory antiallergic immunomodulators. e.g., for the treatment of diseases associated with inflammation. The deuterium kinetic isotope effect associated with placing deuterium at the site of metabolic derivatization slows metabolic derivatization and thus increases the lifetime of the active drug in vivo. | 03-03-2016 |
20160067229 | BIOMARKERS FOR RESPONSE TO RAPAMYCIN ANALOGS - The present invention relates to the use of one or more biomarkers to evaluate the likelihood that a rapamycin analog would produce an anti-cancer effect in a subject. It is based, at least in part, on the results of experiments employing an integrated next-generation sequencing approach to interrogate spatially separated tumor specimens from the same individuals to decipher intra-tumor and intertumor heterogeneity and determine the oncogenomic basis of exceptional therapeutic benefit to rapalogs in kidney cancer patients. These experiments implicated loss of function mutations in TSC1 and/or TSC2 and/or gain-of-function of mTOR in therapeutic responsiveness to rapamycin analogs. Accordingly, in non-limiting embodiments, the present invention provides for assay methods and kits for determining the presence of loss of function mutations in TSC1 and/or TSC2 and/or gain-of-function of mTOR, and methods of using such determinations in selecting a therapeutic regimen for a cancer patient and in methods of treating cancer patients. In particular non-limiting embodiments, a plurality of tumor sites are evaluated and the composite effect of the genetic background on mTOR function is assessed. | 03-10-2016 |
20160074373 | METHODS AND COMPOSITIONS FOR INHIBITING HUMAN COPPER TRAFFICKING PROTEINS ATOX1 AND CCS - Compositions and methods concern organic molecules that bind to human Atox1 and CCS at the copper trafficking interface of these proteins. This binding suppresses copper trafficking, which leads to inhibition of cancer cell proliferation and tumor growth. In addition to serving as an effective treatment of cancer, these organic molecules inhibit cellular copper uptake and can be used as treatment of disorders of copper metabolism such as Wilson's disease, which is characterized by copper overload, as well as wound healing. | 03-17-2016 |
20160120853 | TACROLIMUS AND ANALOGUES THEREOF FOR MEDICAL USE - The present invention relates to a method of treating adverse fat accumulation and related conditions with very low doses of tacrolimus or a close structural analogue thereof. In particular this invention relates to treating adverse fat accumulation and/or sarcopenia and/or metabolic syndrome inpatients by administering tacrolimus in very low dose. Most particularly this invention relates to the use of tacrolimus in treating age related fat accumulation. | 05-05-2016 |
20160120860 | METHODS AND AGENTS FOR TREATING TYROSINASE-POSITIVE ALBINISM - Methods for treating a subject with tyrosinase-positive albinism; agents and compositions thereof for use in treating tyrosinase-positive albinism; and medicaments for treating tyrosinase-positive albinism are described herein. Such methods; agents and compositions thereof; and medicaments relate to chloroquine or rapamycin or compositions thereof and may further relate to nitisinone used in conjunction with the chloroquine or rapamycin or a composition of either of which. | 05-05-2016 |
20160128936 | RAPAMYCIN POWDERS FOR PULMONARY DELIVERY - The invention provides stable, spray-dried, particle formulations containing rapamycin, or pharmaceutically acceptable salts of rapamycin, which are useful for pulmonary administration to the respiratory tract of a patient for the treatment of disease. | 05-12-2016 |
20160130280 | ALKYLATION WITH AN ALKYL FLUOROALKYL SULFONATE - The present invention discloses a process for preparing a chemical compound comprising reacting a nucleophile with an alkyl fluoroalkyl sulfonate in the presence of a base of formula NR1R2R3, wherein R1 and R2 are independently 2-methyipropyl or isopropyl and R3 is —CH(R4)(R5), wherein R4 and R5 are identical or different alkyls that are optionally connected to form a ring. The invention also relates to a process for preparing an alkyl fluoroalkyl sulfonate. The invention further relates to a use of the base in a chemical reaction comprising an alkyl fluoroalkyl sulfonate. The process and uses are suitable for preparing chemical compounds, reactants or intermediates thereof, and in particular for preparing API or reactants, like for example everolimus or reactants for its preparation. | 05-12-2016 |
20160152543 | Inhibitors of viral replication, their process of preparation and their therapeutical uses | 06-02-2016 |
20160158219 | USE OF AN H4 AGONIST MOLECULE TO TREAT ACUTE LEUKEMIA - The present invention relates to the use of new chemical substances, the levogyre and dextrogyre enantiomers of (AMINO-7 TRIETHOXY-4, 5, 6 OXO-1 DIHYDRO-1, 3 ISOBENZOFURANNYL-3)-1 METHOXY-8 METHYL-2METHYLENEDIOXY-6, 7 TETRAHYDRO-, 2, 3, 4 ISOQUINOLEINE or tritoqualine, to treat acute myeloid or lymphoid leukemia, with the exception of type B leukemia. | 06-09-2016 |
20160175288 | MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE | 06-23-2016 |
20160176893 | RAPAMYCIN ANALOGUES AND THEIR PHARMACEUTICAL USE | 06-23-2016 |
20160184279 | METHODS OF TREATING PAIN AND/OR ITCH WITH SMALL MOLECULE INHIBITORS TARGETING AN mTOR PATHWAY - Methods of treating pain and/or itch in a targeted region of a subject and compositions and dosage forms therefor are described herein. Such methods can include topically administering a therapeutically effective amount of an mTOR pathway inhibitor to the subject. | 06-30-2016 |
20160184280 | METHODS OF PREVENTING THE DEVELOPMENT OF MUCOSITIS AND RELATED DISORDERS - Disclosed is a method of preventing the development of mucositis in a subject undergoing radiation therapy or chemotherapy for a disease in need thereof comprising administering an effective amount of a mammalian target of rapamycin (mTOR) inhibitor, such as rapamycin, to the subject. Further disclosed is a method of increasing the lifespan of a normal oral keratinocyte and/or reducing oxidative stress in a normal epithelial cell, wherein the method comprises administering an effective amount of an mTOR inhibitor to a subject undergoing radiation therapy or chemotherapy for a disease in need thereof. | 06-30-2016 |
20160193190 | Targeting Metabolic Adaptive Responses to Chemotherapy | 07-07-2016 |
20160251366 | DEUTERATED AMLEXANOX | 09-01-2016 |
20160251367 | SYNTHESIS OF TRITOQUALINE SALTS | 09-01-2016 |
20220135581 | CHROMENOPYRIDINE-BASED COMPOUNDS AND METHODS OF MAKING AND USE THEREOF - Chromenopyridine-based compounds are provided. In one aspect, the present disclosure provides a method for treating cancer in a subject in need thereof, the method comprising administering a therapeutically effective amount of a chromenopyridine-based compound to the subject. A representative compound is 2,4-diamino-7,8-dimethoxy-5-((4-methoxyphenyl)thio)-5H-chromeno[2,3-b]pyridine-3-carbonitrile (Compound 1). | 05-05-2022 |