| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 514158000 | The hetero ring is five-membered | 73 |
| 20100210603 | NOVEL SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE - The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. | 08-19-2010 |
| 20100305073 | AMIDE COMPOUNDS AS BOOSTERS OF ANTIVIRALS - The present invention relates to compounds that have CYP | 12-02-2010 |
| 20110105440 | HEXAHYDROCYCLOPENTYL[f]INDAZOLE SULFONAMIDES AND DERIVATIVES THEREOF AS SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS - The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included. | 05-05-2011 |
| 20110166110 | Fused Ring Azadecalin Glucocorticoid Receptor Modulators - The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 07-07-2011 |
| 20110183944 | SUSTAINED-RELEASE NSAID/HMG CoA REDUCTASE INHIBITOR COMPOSITIONS - Compositions for controlled release of one or more therapeutic agents where the composition is essentially free of excipients are disclosed. In particular, compositions comprising a HMG-CoA reductase inhibitor, particularly simvastatin, and a NSAID, such as a COX-2 inhibitor, particularly celecoxib, in which greater than 90% of the weight of the composition is made up of the HMG-CoA reductase inhibitor and NSAID are provided. | 07-28-2011 |
| 20110195939 | ANTITUMOR PROPERTIES OF NO MODIFIED PROTEASE INHIBITORS - HIV-protease inhibitors, particularly saquinavir, showed strong anticancer activity but numerous side effects limited its application. In order to overcome its toxicity original compounds were modified by covalent attachment of NO. The efficacy of parental and NO-modified drug was compared in vitro and in vivo. Anticancer activities of NO-modified saquinavir (Saq-NO) was monitored in vitro using assay for cell viability, proliferation, necrotic, autophagic and apoptotic cell death, differentiation, expression of intracellular molecules such as cyclin D3, p53 and Akt. Antitumor properties and toxicity of the compound was estimated in vivo. Saq-NO abrogated the viability of large spectrum of human and rodent tumor cell lines with IC50 significantly lower than parental drug and expressed strong antimelanoma action in vivo. In contrast to saquinavir, there was no detectable toxicity against primary cells in vitro and in vivo. Saq-NO permanently diminished cell proliferation by induction of cell cycle block accompanied with minor presence of tumor cell death. Repressed proliferation was coordinated with strong activation of p53 and differentiation of C6 and B16 cells into oligodendrocytes or “Schwan” like cells, respectively. Oppositely to general characteristic of saquinavir to inhibit Akt signalling, Saq-NO treatment resulted in transient and intensive upregulation of Akt. This antagonism between parental and modified compound could be the crucial for switch of saquinavir from toxic to completely untoxic drug. | 08-11-2011 |
| 20110195940 | Protease Inhibitors Having Enhanced Features - Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature. Exemplary potent HIV protease inhibitors are mono-m-PEG3-atazanavir, mPEGn-N-darunavir (wherein n is 3 or 5), mPEGn-NHCO-saquinavir (wherein n is 5 or 7), and di-mPEG3-atazanavir. | 08-11-2011 |
| 20110237554 | Combination therapies: inhibitors of GABA transaminase and NKCC1 - Inhibitors of NKCC1, such as bumetanide, when coadministered with inhibitors of GABA transaminase, such as vigabatrin, attenuate both the retinal toxicity and the intramyelinic edema. | 09-29-2011 |
| 20110245208 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF SOMATOSENSORY DISORDERS - A method of combating a somatosensory disorder in a subject, comprising administering to the subject an effective amount of a composition comprising bupranolol and/or pharmaceutically acceptable derivative(s) thereof. Compositions useful for such administration are described, including salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine, in which such salt, ester, solvate, etc. compound is in enantiomeric excess or homoenantiomeric in the R isomer thereof, or is formulated with racemic mixtures of the R and S stereoisomers of the salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine. Combination therapy compositions of opioid receptor agonists and such compounds are also described. A method is disclosed of referential genotypic screening of candidate subjects in connection with therapeutic intervention using the compositions of the disclosure to combat the somatosensory disorder. | 10-06-2011 |
| 20110257134 | CO-CRYSTALS OF TRAMADOL AND NSAIDs - The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs, processes for preparation of the same, their uses in pharmaceutical formulations, and for the treatment of various disorders, including pain. | 10-20-2011 |
| 20110263542 | METHODS TO TREAT PAIN USING AN ALPHA-2 ADRENERGIC AGONIST AND AN ENDOTHELIN ANTAGONIST - The present invention relates, in general to treatment of pain comprising administering an alpha-2 adrenergic agonist and an endothelin antagonist, wherein administration of the agents acts as an analgesic and ameliorates pain in a subject. | 10-27-2011 |
| 20110263543 | ANTI INFLAMMATORY COMPOUNDS - Biphenyl compounds of Formula (I) and Formula (II), and their pharmaceutically acceptable salts or solvates or prodrugs, their pharmaceutical compositions, their use and process of preparation are provided. Compounds of Formula (I) and Formula (II) are disclosed to exhibit anti-inflammatory properties. | 10-27-2011 |
| 20110263544 | 1-Phenylpyrrole Derivatives - The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R | 10-27-2011 |
| 20110269722 | PRODRUGS CONTAINING NOVEL BIO-CLEAVABLE LINKERS - The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I. | 11-03-2011 |
| 20110269723 | SPILL RESISTANT FORMULATIONS CONTAINING CLAYS - The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition. | 11-03-2011 |
| 20110301129 | GASTRIC RETENTIVE ORAL DOSAGE FORM WITH RESTRICTED DRUG RELEASE IN THE LOWER GASTROINTESTINAL TRACT - Controlled release oral dosage forms are provided for the continuous, sustained administration of a pharmacologically active agent to the upper gastrointestinal tract of a patient in whom the fed mode as been induced. The majority of the agent is delivered, on an extended release basis, to the stomach, duodenum and upper regions of the small intestine, with drug delivery in the lower gastrointestinal tract and colon substantially restricted. The dosage form comprises a matrix of a biocompatible, hydrophilic, erodible polymer with an active agent incorporated therein, wherein the polymer is one that both swells in the presence of water and gradually erodes over a time period of hours, with swelling and erosion commencing upon contact with gastric fluid, and drug release rate primarily controlled by erosion rate. | 12-08-2011 |
| 20110312921 | N-Myristoyl Transferase Inhibitors - The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors. | 12-22-2011 |
| 20120004198 | PHENYLALANINE DERIVATIVES AND THEIR USE AS NON-PEPTIDE GLP-1 RECEPTOR MODULATORS - Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder. | 01-05-2012 |
| 20120010178 | METHODS AND COMPOUNDS FOR TREATMENT OF NEURODEGENERATIVE DISORDERS - Methods, compounds and compositions for promoting motor neuron survival and the treatment of a neurodegenerative disorders such as Spinal Muscular Atrophy (SMA) are described herein. | 01-12-2012 |
| 20120035142 | POLYMORPHS OF DARUNAVIR - The present invention provides new pseudopolymorphic forms of darunavir as well as a novel amorphous form of darunavir, pharmaceutical compositions comprising these compounds, methods for their preparation and use thereof in treating retroviral infections, in particular, HIV infection. | 02-09-2012 |
| 20120046250 | METHODS AND COMPOSITIONS USEFUL IN TREATING CANCER AND REDUCING WNT MEDIATED EFFECTS IN A CELL - Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer. | 02-23-2012 |
| 20120083475 | INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. | 04-05-2012 |
| 20120129818 | Compositions and Methods for Treatment of Cardiovascular Disease - Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject. | 05-24-2012 |
| 20120172341 | COMPOSITIONS COMPRISING TRAMADOL AND CELECOXIB IN THE TREATMENT OF PAIN - The present invention relates to pharmaceutical compositions comprising tramadol and celecoxib and their uses as medicaments or analgesics, more particularly for the treatment of severe to moderate pain with an inflammation component. | 07-05-2012 |
| 20130029945 | Darunavir Polymorph and Process for Preparation Thereof - There is disclosed crystalline darunavir hydrate substantially free of any non-aqueous solvent. | 01-31-2013 |
| 20130109659 | PHARMACEUTICAL COMPOSITIONS OF CO-CRYSTALS OF TRAMADOL AND COXIBS | 05-02-2013 |
| 20130109660 | NOVEL PYRIMIDINECARBOXAMIDE DERIVATIVES | 05-02-2013 |
| 20130196955 | POLYMORPHISMS FOR PREDICTING DISEASE AND TREATMENT OUTCOME - The invention provides compositions and methods for determining the increased risk for recurrence of certain cancers and the likelihood of successful treatment with one or both of chemotherapy and radiation therapy. The methods comprising determining the type of genomic polymorphism present in a predetermined region of the gene of interest isolated from the subject or patient. Also provided are nucleic acid probes and kits for determining a patient's cancer risk and treatment response. | 08-01-2013 |
| 20130203710 | ANTIVIRAL COMPOUND AND COX-2 INHIBITOR COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES, INCLUDING COMBINATION OF FAMCICLOVIR AND CELECOXIB - The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib. | 08-08-2013 |
| 20130289004 | ANTI-STAPHYLOCOCCAL CELECOXIB DERIVATIVES - A method of treating infection by | 10-31-2013 |
| 20130296280 | EUTECTIC MIXTURE COMPRISING CELECOXIB AND POLOXAMER - The present invention relates to a eutectic mixture wherein poloxamer is added to the poorly soluble drug celecoxib to significantly increase the solubility and bioavailability of celecoxib. | 11-07-2013 |
| 20130296281 | Aryl Substituted Indoles and Their Use as Blockers of Sodium Channels - The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R | 11-07-2013 |
| 20130303492 | 3,5-DIAMINOPYRAZOLE KINASE INHIBITORS - Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition. | 11-14-2013 |
| 20130303493 | Triazole Compounds that Modulate HSP90 Activity - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound. | 11-14-2013 |
| 20130324501 | DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS - Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols according to formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme. | 12-05-2013 |
| 20130338119 | Pyrrolidinone Benzenesulfonamide Derivatives as Modulators of Ion Channels - The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 12-19-2013 |
| 20130345181 | PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS - The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I) | 12-26-2013 |
| 20140005150 | 3,4-DIARYLPYRAZOLES AS PROTEIN KINASE INHIBITORS | 01-02-2014 |
| 20140011775 | ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS - This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in parkinson's disease, huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description. | 01-09-2014 |
| 20140018327 | Pyrrole Derivatives as Nicotinic Acetylcholine Receptor Modulators for Use in the Treatment of Neurodegenerative Disorders Such as Alzheimer's and Parkinson's Disease - Disclosed is a compound of formula (I) wherein ‘a’ and R | 01-16-2014 |
| 20140024622 | COMPOSITIONS COMPRISING TRAMADOL AND CELECOXIB IN THE TREATMENT OF PAIN - The present invention relates to pharmaceutical compositions comprising tramadol and celecoxib and their uses as medicaments or analgesics, more particularly for the treatment of severe to moderate pain with an inflammation component. | 01-23-2014 |
| 20140038922 | WNT PROTEIN SIGNALLING INHIBITORS - The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis. | 02-06-2014 |
| 20140038923 | PYRAZOLE INHIBITORS OF COX-2 AND SEH - The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay. In addition, the compounds of the present invention also demonstrated to have potent anti-angiogenic effects toward endothelial cells (HUVEC) and inhibit angiogenesis in vitro, ex vivo and in vivo. The dual inhibitors of the present invention also demonstrate anti-angiogenic effect to slow breast tumor growth in vivo. | 02-06-2014 |
| 20140057879 | CO-CRYSTALS OF TRAMADOL AND COXIBS - The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain. | 02-27-2014 |
| 20140142070 | DARUNAVIR COMBINATION FORMULATIONS - This invention relates to solid oral dosage forms of the HIV inhibitor Darunavir and/or a pharmaceutically acceptable salt or solvate thereof, and combination formulations thereof. | 05-22-2014 |
| 20140243296 | Organic Compounds - A treatment regimen and dosage form comprising ritonavir and darunavir and their use in the treatment of HIV infection. | 08-28-2014 |
| 20140357600 | NOVEL ESTER CONTAINING COMPOSITIONS AND METHODS - Described herein are compositions (e.g., a pharmaceutical composition) and methods for controlling the delivery of a therapeutic agent, and their use in the treatment and/or prevention of diseases and disorders. | 12-04-2014 |
| 20140357601 | FAMCICLOVIR AND CELECOXIB COMBINATION THERAPY KIT FOR FUNCTIONAL SOMATIC SYNDROMES - The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib. | 12-04-2014 |
| 20150011514 | Celecoxib Compositions - Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to about 1000 mg in intimate mixture with one or more pharmaceutically acceptable excipients. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders. | 01-08-2015 |
| 20150051177 | METHODS AND COMPOSITIONS USEFUL IN TREATING CANCER AND REDUCING WNT MEDIATED EFFECTS IN A CELL - Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer. | 02-19-2015 |
| 20150072958 | HIV-1 PROTEASE INHIBITORS HAVING GEM-DI-FLUORO BICYCLIC P2-LIGANDS - Various embodiments of the present invention relate to, among other things, compounds and methods of using those compounds to treat an HIV infection. The compounds of the various embodiments of the present invention provide, among other things, therapeutic agents having enhanced penetration capability across the blood-brain barrier, such that they can enter the CNS to treat an HIV-1 infection in the CNS. | 03-12-2015 |
| 20150072959 | SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS - Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. | 03-12-2015 |
| 20150094284 | S-TRIAZOLYL ALPHA-MERCAPTO ACETANILIDES AS INHIBITORS OF HIV REVERSE TRANSCRIPTASE - A series of S-triazolyl α-mercaptoacetanilides having general structure (1) are provided, where Q is CO | 04-02-2015 |
| 20150141382 | NOVEL SOLVATES OF DARUNAVIR - The present invention relates to novel solvates of Darunavir of Formula I. | 05-21-2015 |
| 20150141383 | Darunavir Polymorph and Process for Preparation Thereof - There is disclosed crystalline darunavir hydrate substantially free of any non-aqueous solvent. | 05-21-2015 |
| 20150148318 | METHOD FOR INHIBITING GROWTH OF CANCER CELLS - A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 μM concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. | 05-28-2015 |
| 20150301060 | PREDICTIVE MARKERS FOR POLYAMINE INHIBITOR CANCER THERAPIES - The present disclosure relates to therapeutic methods and medical uses comprising the identification and use of cancer marker surrogates for increased polyamine expression. These markers may be used to identify patients who may be treated for diseases and disorders that are susceptible to polyamine synthesis inhibitors, and they can also be used to monitor therapeutic responses when such agents are used. More specifically, reduced levels of let-7 miRNA and elevated levels of LIN28 and HMGA2 proteins were found to correlate with elevated levels of polyamines and may be used for predicting the efficacy of cancer therapy us ing an ornithine decarboxylase (ODC1) inhibitor such as eflornithine (DFMO), suitably in combination with an NSAID such as sulindac. | 10-22-2015 |
| 20150328235 | METHODS AND MATERIALS FOR TREATING CALCIFIC AORTIC VALVE STENOSIS - This document provides methods and materials involved in treating cardiovascular conditions such as calcific aortic valve stenosis. For example, methods and materials for using sGC agonists or a combination of sGC agonists and PDE5A inhibitors to reduce calcification of heart valves and/or vessels or to slow progression of aortic sclerosis to calcific aortic valve stenosis are provided. | 11-19-2015 |
| 20150335614 | COMPOSITIONS FOR REDUCING BETA-AMYLOID-INDUCED NEUROTOXICITY COMPRISING BETA-SECRETASE INHIBITOR - Disclosed are a composition for reducing beta amyloid-induced neurotoxicity by inhibiting β-secretase activity, comprising a dibenzofuran derivative, and a method for preparing the same. Further disclosed is that the combination of the dibenzofuran derivative with a γ-secretase inhibitor or an anti-inflammatory agent shows higher activity with respect to reducing beta amyloid-induced neurotoxicity. | 11-26-2015 |
| 20160000736 | BACLOFEN AND ACAMPROSATE BASED THERAPY OF NEUROLOGICAL DISORDERS - The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid β toxicity. More specifically, the present invention relates to novel combinatorial therapies of Alzheimer's disease, Alzheimer's disease related disorders, amyotrophic lateral sclerosis, multiple sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on baclofen and acamprosate combination. | 01-07-2016 |
| 20160000764 | NEW SPIRO[3H-INDOLE-3,2'-PYRROLIDIN]-2(1H)-ONE COMPOUNDS AND DERIVATIVES AS MDM2-P53 INHIBITORS - The present invention relates to compounds of formula (I) | 01-07-2016 |
| 20160009702 | PYRAZOLE COMPOUNDS AND METHODS OF USE THEREOF | 01-14-2016 |
| 20160081989 | Substituted 1 H-Pyrrolo [2, 3-b] pyridine and 1 H-Pyrazolo [3, 4-b] pyridine Derivatives as Salt Inducible Kinase 2 (SIK2) Inhibitors - Compounds according to Formulas I, IA or IB: | 03-24-2016 |
| 20160089364 | PHARMACEUTICAL COMPOSITION AND THE USE THEREOF, AND APPLICATION REGIME OF SAID PHARMACEUTICAL COMPOSITION FOR ON-DEMAND CONTRACEPTION - The invention relates to a pharmaceutical composition for non-hormonal, on-demand contraception and to processes for preparing this pharmaceutical composition. The latter comprises 2H-indazole as novel EP2 receptor antagonists in combination with COX inhibitors. The invention furthermore provides a method for non-hormonal female-controlled on-demand contraception where a pharmaceutical composition comprising EP2 receptor antagonists in combination with COX inhibitors is taken on demand prior to expected sexual intercourse. | 03-31-2016 |
| 20160113936 | METHODS FOR MODULATING MONOCYTE FUNCTION - It has been discovered that HSP90 inhibitors can inhibit both the pro-inflammatory and pro-coagulatory potential of monocytes, in particular activated monocytes. One embodiment provides a method of inhibiting the pro-inflammatory phenotype of monocytes, preferably in human subjects, most preferably in human subjects having Sickle Cell Disease (SCD). A preferred HSP90 inhibitor is 5-(2,4-dihydroxy-5-isopropylphenyl)-N-ethyl-4-(4-(morpholinomethyl)phenyl)isoxazole-3-carboxamide (NVP-AUY922). | 04-28-2016 |
| 20160151337 | ANNELATED PYRROLES AND THEIR USE AS CRAC INHIBITORS | 06-02-2016 |
| 20160176857 | 3,5-DIAMINOPYRAZOLE KINASE INHIBITORS | 06-23-2016 |
| 20160184270 | SUBSTITUTED 2-IMIDAZOLIDINONES AND 2-IMIDAZOLONES AND THEIR USE IN THE TREATMENT OF CANCER - Compounds of formula (I) wherein R | 06-30-2016 |
| 20160200752 | COX-2-TARGETING, PLATINUM-CONTAINING CONJUGATES AND THEIR USE IN THE TREATMENT OF TUMORS AND CANCERS | 07-14-2016 |
| 20160376252 | ANDROGEN RECEPTOR MODULATORS AND USES THEREOF - Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors. | 12-29-2016 |
| 20180021357 | METHODS FOR TREATING BACTERIAL INFECTION | 01-25-2018 |
| 20190142738 | TRANSDERMAL FORMULATIONS FOR DELIVERY OF CELECOXIB AND ITS USE IN THE TREATMENT OF CELECOXIB-RESPONSIVE DISEASES AND CONDITIONS | 05-16-2019 |
| 20190142789 | THERAPEUTIC FORMULATIONS AND USES THEREOF | 05-16-2019 |
