Entries |
Document | Title | Date |
20080261923 | Alkene Mimics - Ac-Phe-Tyr-phosphoSer-Ψ[CH═C]-Pro-Arg-NH | 10-23-2008 |
20080306025 | N-(PHOSPHONOALKYL)-AMINO ACIDS, DERIVATIVES THEREOF AND COMPOSITIONS AND METHODS OF USE - The present invention relates to an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof, the N-(phosphonoalkyl)-amino acid, related compound or derivative thereof being in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, other than N-(phosphonomethyl)-glycine or N,N-bis(phosphonomethyl)-glycine. Also included is a composition including an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, and a cosmetically or pharmaceutically acceptable vehicle for topical or systemic administration to a mammalian subject, as well as a method of administering an effective amount of such a composition for alleviating or improving a condition, disorder, symptom or syndrome associated with at least one of a nervous, vascular, musculoskeletal or cutaneous system. | 12-11-2008 |
20080312188 | Glycogen synthase kinase-3 inhibitors - Novel compounds designed to allow interactions with binding sites of GSK-3 and hence are capable of inhibiting GSK-3 activity, via inhibition of substrate binding are disclosed. Further disclosed are pharmaceutical compositions including same and methods of using same in the treatment of GSK-3 mediated conditions. | 12-18-2008 |
20080318901 | Novel Lysophosphatidic Acid Receptor Selective Antagonists - The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom. | 12-25-2008 |
20080318902 | TRIHETEROCYCLIC COMPOUNDS AND COMPOSITIONS THEREOF - The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus. | 12-25-2008 |
20080318903 | METHODS FOR TREATING CANCER - The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus. | 12-25-2008 |
20090048213 | Prodrug of cinnamide compound - The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) | 02-19-2009 |
20090069272 | Composition for treating bone disorders - Disclosed is a new composition of matter, substantially enantiomerically pure (1R,6S)-2-Azabicyclo-[4.3.0]nonane-8,8-diphosphonic acid, methods of preparing this new composition of matter, a pharmaceutical composition comprising the new composition, and administration of the composition in methods of treating bone disorders such as osteoporosis, osteolytic bone metastasis, rheumatoid arthritis and osteoarthritis. | 03-12-2009 |
20090075938 | TREATMENT OF DUCHENNE MUSCULAR DYSTROPHY - There are disclosed compound of Formula (1): A | 03-19-2009 |
20090131369 | Novel Benzimidazole(Thio)Carbamates with Antiparasitic Activity and the Synthesis Thereof - This invention relates to benzimidazole carbamates and (thio)carbamates corresponding to Formula I: | 05-21-2009 |
20090156555 | PYRROLOTRIAZINE ANILINE PRODRUG COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the Formula (I), including pharmaceutically acceptable salts thereof | 06-18-2009 |
20090156556 | AMINOPROPANOL DERIVATIVES - Compounds of formula I: | 06-18-2009 |
20090163443 | NOVEL COMPOUND, USEFUL FOR PANCREATIC LIPASE INHIBITION AND THE PROCESS FOR ISOLATION THEREOF - The present invention relates to a novel, Nonadeca-6-enoic acid-3-(hexadecyloxy-hydroxy-thiophosphoryloxy)-quinoxalin-2-yl ester designated as streptolipin, useful for pancreatic lipase inhibition, isolated from the culture of | 06-25-2009 |
20090163444 | PHOSPHO-INDOLES AS HIV INHIBITORS - 3-phosphoindole compounds for the treatment of retroviral infections, and particularly for HIV, are described. Also included are compositions comprising the 3-phosphoindole derivatives alone or in combination with one or more other anti-retroviral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds. | 06-25-2009 |
20090170812 | Transcription factor modulating compounds and methods of use thereof - Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms. | 07-02-2009 |
20090181930 | KINASE INHIBITORY PHOSPHONATE ANALOGS - The invention is related to phosphorus substituted kinase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. | 07-16-2009 |
20090186855 | COMPOUNDS AND METHODS FOR TREATING TOLL-LIKE RECEPTOR 2-RELATED DISEASES AND CONDITIONS - The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation. | 07-23-2009 |
20090192121 | NOVEL BISAMIDATE PHOSPHONATE PRODRUGS - Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: | 07-30-2009 |
20090221529 | HETEROCYCLES AND DERIVATIVES THEREOF AND METHODS OF MANUFACTURE AND THERAPEUTIC USE - This invention relates to the design, synthesis and use of synthetic vitamin D and other steroidal analogs. It further relates to the therapeutic use of such analogs and their manufacture. | 09-03-2009 |
20090270351 | PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS - The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the phosphorus derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the phosphorus derivatives in vivo. | 10-29-2009 |
20090318386 | ACTIVE COMPOUND COMBINATIONS HAVING INSECTICIDAL AND ACARICIDAL PROPERTIES - The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties. | 12-24-2009 |
20100004206 | WATER-SOLUBLE BENZOAZEPINE COMPOUND AND ITS PHARMACEUTICAL COMPOSITION - The present invention provides a benzoazepine compound represented by following general formula (1): | 01-07-2010 |
20100009935 | RESISTANCE-REPELLENT RETROVIRAL PROTEASE INHIBITORS - Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided. | 01-14-2010 |
20100022476 | PYRAZOLYLAMINO SUBSTITUTED QUINAZOLES FOR THE TREATMENT OF CANCER - The invention provided a compound of formula: (I) for use in the treatment of disease, in particular proliferative diseases such as cancer and for use in the preparation of medicaments for use in the treatment of proliferative diseases; the invention also processes for the preparation of such compounds, as well as pharmaceutical compositions containing them as active ingredient. | 01-28-2010 |
20100029591 | COMBINATIONS OF A PYRIMIDINE CONTAINING NNRTI WITH RT INHIBITORS - The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection. | 02-04-2010 |
20100069333 | ALPHA-HELIX MIMETICS AND METHOD RELATING TO THE TREATMENT OF CANCER STEM CELLS - The invention provides α-mimetic structures and a chemical library relating thereto. Additionally, the invention provides methods wherein α-mimetic compounds are used to treat cancer stem cells. | 03-18-2010 |
20100168063 | BICYCLIC PYRIMIDINONES AND USES THEREOF - The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided. | 07-01-2010 |
20100210594 | SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS - The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula | 08-19-2010 |
20100210595 | SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS - The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula | 08-19-2010 |
20100216745 | NOVEL CEPHEM COMPOUNDS USEFUL FOR THE TREATMENT OF BACTERIAL INFECTIONS - The present invention relates to new cephem compounds useful for the treatment of bacterial infections. The invention also relates to methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and to methods of treatment using the compounds. The new cephem compounds are stable, exhibit good solubility, and are particularly well suited for, e.g., parenteral administration for the treatment of bacterial infections. | 08-26-2010 |
20100240612 | Prenylated Bisphosphonates as Anti-tuberculosis Agents - The invention provides methods to treat a mycobacterium infection and methods to inhibit mycobacterial polyprenyl pyrophosphate synthesis with a compound of formula I. The invention also provides novel compounds of formula I as well as salts and prodrugs thereof. | 09-23-2010 |
20100279983 | NOVEL INHIBITORS OF BETA-LACTAMASE - This invention provides novel β-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases. Formula (I) or pharmaceutically acceptable salt thereof. | 11-04-2010 |
20100292187 | METHODS FOR TREATING HEPATITIS C - The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity. | 11-18-2010 |
20110009366 | BICYCLIC PYRIMIDINONES AND USES THEREOF - The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided. | 01-13-2011 |
20110065671 | BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS - The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bi-cyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient. | 03-17-2011 |
20110071114 | COMPOSITIONS AND METHODS FOR TREATING BACTERIAL INFECTIONS USING CEFTAROLINE - The present invention relates to compositions comprising ceftaroline or a prodrug thereof (e.g., ceftaroline fosamil) and methods for treating bacterial infections, such as complicated skin and structure infections (cSSSI) and community-acquired bacterial pneumonia (CABP) by administering ceftaroline or a prodrug thereof, (e.g., ceftaroline fosamil). | 03-24-2011 |
20110077221 | Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof - This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, prostate cancer and/or diseases or disorders of bone and muscle. | 03-31-2011 |
20110082110 | WATER-SOLUBLE BENZOAZEPINE COMPOUND AND ITS PHARMACEUTICAL COMPOSITION - The present invention provides a benzoazepine compound represented by following general formula (1): | 04-07-2011 |
20110098250 | WATER-SOLUBLE BENZOAZEPINE COMPOUND AND ITS PHARMACEUTICAL COMPOSITION - The present invention provides a benzoazepine compound represented by following general formula (1): | 04-28-2011 |
20110118210 | AMINOPROPANOL DERIVATIVES - Compounds of formula I: | 05-19-2011 |
20110124598 | CHEMICAL COMPOUNDS - The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 05-26-2011 |
20110172190 | AGENTS FOR PREVENTING AND TREATING DISORDERS INVOLVING MODULATION OF THE RYANODINE RECEPTORS - The present invention provides compounds of Formula I | 07-14-2011 |
20110183940 | CHEMICAL COMPOUNDS - The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 07-28-2011 |
20110190236 | CHEMICAL COMPOUNDS - The present invention features compounds that are prodrugs of HIIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 08-04-2011 |
20110195932 | Drug Combinations for the Treatment of Duchenne Muscular Dystrophy - Combinations comprising (or consisting essentially of) one or more compounds of formula (1) with one or more ancillary agents, to processes for preparing the combinations, and to various therapeutic uses of the combinations. Also provided are pharmaceutical compositions containing the combinations as well as a method of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia using the combinations. | 08-11-2011 |
20110195933 | PYRAZOLO[1,5-A]PYRIDINES AS MARK INHIBITORS - The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included. | 08-11-2011 |
20110212923 | Phosphate Derivatives of Substituted Benzoxazoles - The present invention relates to phosphate derivatives of estrogen receptor beta agonists, compositions thereof, preparations thereof, and uses thereof. Formula (I). | 09-01-2011 |
20110218174 | NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS - Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. | 09-08-2011 |
20110230443 | IMIDAZO[1,2-a] PYRIDINYL BISPHOSPHONATES - Novel imidazo[1,2-α]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders. | 09-22-2011 |
20110230444 | PHARMACEUTICAL COMBINATION COMPRISING A HSP 90 INHIBITOR AND A MTOR INHIBITOR - A pharmaceutical combination comprising an Hsp90 inhibitor and an mTOR inhibitor, and methods of using the combination to treat or prevent proliferative disorders. | 09-22-2011 |
20110257129 | ENANTIOMERICALLY PURE PHOSPHOINDOLES AS HIV INHIBITORS - 3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HIV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other anti-viral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds. | 10-20-2011 |
20110263532 | HALOFUGINONE ANALOGS FOR INHIBITION OF TRNA SYNTHETASES AND USES THEREOF - The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications. | 10-27-2011 |
20110263533 | NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS - Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension. | 10-27-2011 |
20110269716 | ANTIOXIDANT COMPOUNDS AND METHODS OF THEIR USE - The invention relates to antioxidant substituted isoindoline nitroxide compounds and their use in methods of treating or preventing diseases or disorders related to oxidative stress, methods of reducing oxidative stress and methods of protecting a subject from oxidative stress upon exposure to ionising radiation. Pharmaceutical compositions comprising the antioxidant compounds are also described. | 11-03-2011 |
20110288053 | ANTIVIRAL PHOSPHONATE ANALOGS - The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. | 11-24-2011 |
20110294758 | NOVEL ACTIVATORS OF GLUCOKINASE - The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same. | 12-01-2011 |
20110319362 | STAT3 LIGANDS AND THERAPEUTIC USES THEREOF - Inhibitors of STAT3 are disclosed. Methods of using the STAT3 inhibitors in the treatment of diseases and conditions wherein inhibition of STAT3 provides a benefit, like cancers, also are disclosed. | 12-29-2011 |
20120028923 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds. | 02-02-2012 |
20120028924 | CHEMICAL COMPOUNDS - The present invention relates to compounds of Formula (I) and/or Formula (Ia): | 02-02-2012 |
20120040935 | COMPOSITIONS USEFUL AS INHIBITORS OF VOLTAGE-GATED ION CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium 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. | 02-16-2012 |
20120046245 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. | 02-23-2012 |
20120129809 | LUNG CANCER TREATMENT - The invention provides a method for treating NSCLC, especially in cases of KRAS mutation, involving the administration of deforolimus. | 05-24-2012 |
20120129810 | COMBINATION ANTINEOPLASTIC THERAPY - The present invention is directed to methods of using a sirolimus drug and chloroquine or a quinoline derivative in combination. Methods of use are also described. | 05-24-2012 |
20120149665 | COMBINATION THERAPY FOR TREATING PROLIFERATIVE DISEASES - A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor. | 06-14-2012 |
20120178714 | Phosphorus-containing Compounds & Uses Thereof - This disclosure concerns a new family of phosphorus-containing compounds of Formula (I): | 07-12-2012 |
20120178715 | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS - Compounds of Formula I: and salts thereof in which R | 07-12-2012 |
20120184510 | COLD MENTHOL RECEPTOR-1 ANTAGONISTS - The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described. | 07-19-2012 |
20120196833 | PHOSPHORUS CONTAINING QUINAZOLINE COMPOUNDS AND METHODS OF USE - Disclosed are novel quinazoline derivatives containing phosphorus substitutions and methods for the treatment of hyperproliferative diseases (e.g. cancer) using the compounds. These compounds are type I receptor protein kinase inhibitors useful in treating disorders related to abnormal protein kinase activities such as cancer and inflammation in mammals. Also disclosed are pharmaceutical compositions containing the compounds, methods for the preparation of the compounds and their pharmaceutically acceptable salts. | 08-02-2012 |
20120208784 | SUBSTITUTED PROPANE PHOSPHINIC ACID DERIVATIVES - The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: | 08-16-2012 |
20120214766 | CANNABINOID RECEPTOR MODULATORS - The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease. | 08-23-2012 |
20120214767 | TRICYCLIC HETEROCYCLIC COMPOUNDS - Disclosed are compounds of Formula (I) | 08-23-2012 |
20120232035 | Bicyclic pyrimidinones and uses thereof - The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided. | 09-13-2012 |
20120277188 | WATER-SOLUBLE BENZOAZEPINE COMPOUND AND ITS PHARMACEUTICAL COMPOSITION - The present invention provides a benzoazepine compound represented by following general formula (1): | 11-01-2012 |
20120277189 | WATER-SOLUBLE BENZOAZEPINE COMPOUND AND ITS PHARMACEUTICAL COMPOSITION - The present invention provides a benzoazepine compound represented by following general formula (1): | 11-01-2012 |
20120277190 | PRODRUGS OF COMPOUNDS THAT INHIBIT TRPV1 RECEPTOR - Compounds of formula (I) | 11-01-2012 |
20120289481 | COMPOSITIONS AND METHODS FOR TREATING CANCER - The instant invention provides a method of treating a cancer selected from the group consisting of non-small cell lung cancer and breast cancer with an mTOR inhibitor and an αvβ3 integrin antagonist, wherein the mTOR inhibitor is ridaforolimus, everolimus, temsirolimus or a combination thereof. | 11-15-2012 |
20120295877 | Therapeutic Compounds - The present invention relates to compounds of Formula (I) and (Ia) | 11-22-2012 |
20130023495 | USES OF DGAT1 INHIBITORS - The present invention relates to the use of a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia. The present invention further relates to the use of a pharmaceutical composition comprising a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia. | 01-24-2013 |
20130029938 | Chemical Compounds - Compounds of Formula I and methods for treating metabolic disorders are disclosed. | 01-31-2013 |
20130029939 | NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME - Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure wherein R | 01-31-2013 |
20130053345 | BICYCLIC HETEROARLY ANALOGUES AS GPR119 MODULATORS - Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R | 02-28-2013 |
20130072457 | PYRAZOLYL QUINAZOLINE KINASE INHIBITORS - The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 03-21-2013 |
20130090310 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds. | 04-11-2013 |
20130102569 | 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. | 04-25-2013 |
20130157979 | PHOSPHATE ESTERS OF GYRASE AND TOPOISOMERASE INHIBITORS - The present invention relates to phosphate esters of compounds that inhibit bacterial gyrase and/or Topoisomerase IV and pharmaceutical compositions thereof. These phosphate esters are useful for treating bacterial infections. | 06-20-2013 |
20130165412 | CANNABINOID RECEPTOR MODULATORS - The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease. | 06-27-2013 |
20130178443 | PHENYLQUINAZOLINE DERIVATIVES - Novel quinazolinamide derivatives of the formula (I), in which R1-R43 and X have the meanings indicated in claim | 07-11-2013 |
20130203702 | HETEROCYCLYL-PYRIDINYL-BASED BIPHOSPHONIC ACID, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, COMPOSITION THEREOF AND METHOD OF USE THEREOF - The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds; | 08-08-2013 |
20130261086 | MACROCYCLIC KINASE INHIBITORS - Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial. | 10-03-2013 |
20130289001 | PANTOTHENATE DERIVATIVES FOR THE TREATMENT OF NEUROLOGIC DISORDERS - The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders. | 10-31-2013 |
20130289002 | GYRASE AND TOPOISOMERASE IV INHIBITORS - The present invention relates to a compound of formula (I) | 10-31-2013 |
20130310340 | METHOD OF TREATING MUSCULAR DEGRADATION - A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation. | 11-21-2013 |
20130331358 | Water-Soluble Benzoazepine Compound and Its Pharmaceutical Composition - The present invention provides a benzoazepine compound represented by following general formula (1): | 12-12-2013 |
20140005145 | COMBINATION BREAST CANCER THERAPY WITH HSP90 INHIBITORY COMPOUNDS | 01-02-2014 |
20140005146 | PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES | 01-02-2014 |
20140024618 | INDOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS - The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient. | 01-23-2014 |
20140024619 | Benzazepine Derivatives Useful as Vasopressin Antagonists - The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) | 01-23-2014 |
20140031318 | SOLID FORMS OF (R)-2-(5-(2-(3-ETHYLUREIDO)-6-FLUORO-7-(TETRAHYDROFURAN-2-YL)-1H-BENZO[d]- IMIDAZOL-5-YL)PYRIMIDIN-2-YL)PROPAN-2-YL DIHYDROGEN PHOSPHATE AND SALTS THEREOF - The invention relates to solid forms of the Formula (I) | 01-30-2014 |
20140038920 | TFEB PHOSPHORYLATION INHIBITORS AND USES THEREOF - The invention refers to TFEB phosphorylation inhibitors. Such molecules have a therapeutic applicability in all disorders that need induction of the cell authophagic/lysosomal system, such as lysosomal storage disorders, neurodegenerative diseases, hepatic diseases, muscle diseases and metabolic diseases. | 02-06-2014 |
20140045791 | COMBINATION THERAPY TO TREAT MYCOBACTERIUM DISEASES - The present invention relates to a compound of formula (I) | 02-13-2014 |
20140051664 | COMBINATION THERAPY OF HSP90 INHIBITORY COMPOUNDS WITH RADIOTHERAPY - Methods for treating cancer in a subject, comprising administering to the subject an effective amount of a compound represented by the following structural formula a tautomer, or a pharmaceutically acceptable salt thereof in combination with radiotherapy. The variables depicted in the structural formula are defined herein. | 02-20-2014 |
20140051665 | PROSTATE CANCER THERAPY WITH HSP90 INHIBITORY COMPOUNDS - Method for treating a subject with prostate cancer, comprising administering to the an effective amount of a compound represented by the following structural formula: a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein. | 02-20-2014 |
20140107073 | GDF-8 Inhibitors - Described are GCF-8 inhibitors of the formula (I), | 04-17-2014 |
20140128345 | VAGINAL MATRICES: NANOFIBERS FOR CONTRACEPTION AND PREVENTION OF HIV INFECTION - Described are drug delivery systems incorporating electrospun fibers that comprise and deliver physicochemically diverse drug compounds. Such fibers provide significant advantages in drug agent release, such as adaptability for solid dosage delivery to mucosal tissues. This is in addition to allowing for controlled drug release. Systems and methods for large-scale electrospinning productivity are described, including novel microarchitectures allowing for variable pharmacokinetics in drug release. | 05-08-2014 |
20140162984 | PHOSPHONOXY QUINAZOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE - Quinazoline derivatives of formula (I): | 06-12-2014 |
20140171392 | Use of an Adrenal Hormone-Modifying Agent - The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): | 06-19-2014 |
20140194388 | COMBINATION THERAPY OF HSP90 INHIBITORY COMPOUNDS WITH CHK INHIBITORS - A pharmaceutical composition comprising a CHK inhibitor, and an Hsp90 inhibitor according to the following formulae or tautomers, or pharmaceutically acceptable salts thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof, using pharmaceutical compositions described herein. | 07-10-2014 |
20140206649 | CANNABINOID RECEPTOR MODULATORS - Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB | 07-24-2014 |
20140221314 | TRICYCLIC INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE - The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof. | 08-07-2014 |
20140243287 | PYRAZOLE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS - The present invention relates to pyrazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. | 08-28-2014 |
20140256679 | CHEMICAL COMPOUNDS - The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 09-11-2014 |
20140256680 | COMBINATION THERAPY OF HSP90 INHIBITORS WITH BRAF INHIBITORS - A pharmaceutical combination comprising a BRAF inhibitor, and an Hsp90 inhibitor according to the following formulae (I): or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables are defined therein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein. | 09-11-2014 |
20140274958 | CEPHALOSPORIN COMPOSITIONS AND METHODS OF MANUFACTURE - Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step. | 09-18-2014 |
20140288025 | FATTY ACID ANTIVIRAL CONJUGATES AND THEIR USES - The invention relates to fatty acid antiviral conjugates; compositions comprising an effective amount of a fatty acid antiviral conjugate; and methods for treating or preventing a viral infection comprising the administration of an effective amount of a fatty acid antiviral conjugate. | 09-25-2014 |
20140296186 | 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 preventing or 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 composition comprising such a compound. | 10-02-2014 |
20140349968 | Compositions and Methods for Treating Cancer - The instant invention provides a method of treating a cancer selected from the group consisting of non-small cell lung cancer and breast cancer with an mTOR inhibitor and an αv62 3 integrin antagonist, wherein the mTOR inhibitor is ridaforolimus, everolimus, temsirolimus or a combination thereof. | 11-27-2014 |
20150011508 | COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS - The invention provides compounds of formulae (I) and (II) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases. | 01-08-2015 |
20150018312 | NITROGEN CONTAINING COMPOUNDS AND THEIR USE - Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed. | 01-15-2015 |
20150018313 | NOVEL 5-SUBSTITUTED BENZIMIDAZOLIUM COMPOUNDS - The present invention relates to compounds of general formula (I) | 01-15-2015 |
20150018314 | NOVEL BENZIMIDAZOLIUM COMPOUNDS - The present invention relates to compounds of general formula (I) | 01-15-2015 |
20150018315 | NOVEL TETRA- AND PENTASUBSTITUTED BENZIMIDAZOLIUM COMPOUNDS - The present invention relates to compounds of general formula (I) | 01-15-2015 |
20150045323 | PRODRUGS OF AMINO QUINAZOLINE KINASE INHIBITOR - Disclosed are compounds having the formula: | 02-12-2015 |
20150057250 | INHIBITORS OF OSTEOCLAST ACTIVITY FOR TREATING ARTHRITIS - Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions. The oral bioavailability of zoledronic acid can be enhanced by administering the zoledronic acid in the disodium salt form | 02-26-2015 |
20150065463 | PHOSPHONATE DERIVATIVES AND METHODS OF USE THEREOF IN THE TREATMENT OF ALZHEIMER'S DISEASE - Benzothiazole phosphonate analogs and methods of using the same to inhibit the activity of Amyloid Binding Alcohol Dehydrogenase and in the amelioration or treatment of Alzheimer's disease are provided. | 03-05-2015 |
20150072957 | Tazobactam Arginine Compositions - This disclosure provides compositions containing solid forms of tazobactam arginine, and methods of manufacturing and using these compositions. | 03-12-2015 |
20150099721 | TREATING CANCER WITH HSP90 INHIBITORY COMPOUNDS - A method for treating cancer with a mutation in ROS or RET, comprising identifying a subject with a cancer with a mutation in ROS or RET, and administering to the subject an effective amount of a compound according to formulae (I) OR (la) or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein. | 04-09-2015 |
20150111853 | CEPHALOSPORIN COMPOSITIONS AND METHODS OF MANUFACTURE - Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step. | 04-23-2015 |
20150111854 | SUBSTITUTED POLYCYCLIC CARBAMOYL PYRIDONE DERIVATIVE PRODRUG - The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity. | 04-23-2015 |
20150126477 | CANNABINOID RECEPTOR MODULATORS - Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB | 05-07-2015 |
20150133403 | Osteoclast Inhibitors for Knee Conditions - Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions. | 05-14-2015 |
20150141373 | Osteoclast Inhibitors for Knee Conditions - Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions. | 05-21-2015 |
20150141374 | Osteoclast Inhibitors for Knee Conditions - Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions. | 05-21-2015 |
20150148311 | NON-SYSTEMIC TGR5 AGONISTS - Compounds having the following structure (I): | 05-28-2015 |
20150148312 | OSTEOCLAST INHIBITORS FOR KNEE CONDITIONS - Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions. | 05-28-2015 |
20150299232 | GUANINE ANALOGS AS TELOMERASE SUBSTRATES AND TELOMERE LENGTH AFFECTORS - This invention relates to compounds useful for inhibiting telomere elongation. More specifically, the invention provides nucleotide analogs that are incorporated into telomeres by telomerase thereby inhibiting elongation of telomeres. The compounds are useful in treating cancer and other cell proliferative diseases. | 10-22-2015 |
20150307534 | CHEMICAL COMPOUNDS - Quinazoline derivatives of formula (I): | 10-29-2015 |
20150313899 | COMPOUNDS AND METHOD FOR TREATING AUTOIMMUNE DISEASES - Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I | 11-05-2015 |
20150329530 | ANTIBACTERIAL COMPUNDS - The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture. | 11-19-2015 |
20150329539 | 4-PYRIDINONETRIAZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS - The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R | 11-19-2015 |
20150335667 | CHEMICAL COMPOUNDS - The present invention features compounds that are prodrugs of HIV integrase inhibitors and therefore are useful in the delivery of compounds for the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC. | 11-26-2015 |
20150361120 | MACROLIDE INHIBITORS OF mTOR - The present invention relates to new macrolide inhibitors of mTOR, pharmaceutical compositions thereof, and methods of use thereof. | 12-17-2015 |
20150366885 | 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 preventing or 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 composition comprising such a compound. | 12-24-2015 |
20150368246 | TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C - The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. I | 12-24-2015 |
20160002249 | Fused Imidazole Derivatives Useful as IDO Inhibitors - Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosuppression associated with an infectious disease. | 01-07-2016 |
20160002273 | THIENO[3,2-D]PYRIMIDINE-6-CARBOXAMIDES AND ANALOGUES AS SIRTUIN MODULATORS - Provided herein are novel substituted thieno[3,2-d]pyrimidine-6-carboxamide sirtuin inhibitors and methods of use thereof. The sirtuin inhibitors may be used for inhibiting a sirtuin-mediated biological process, and, e.g. for treating and/or preventing diseases and disorders including, but not limited to cancer, neurodegenerative disease and inflammation. Also provided herein are pharmaceutical compositions comprising these sirtuin inhibitors and compositions comprising a sirtuin inhibitor in combination with another therapeutic agent. | 01-07-2016 |
20160022648 | THERAPEUTIC AGENT FOR MEIBOMIAN GLAND DYSFUNCTION - A compound represented by the formula (1): | 01-28-2016 |
20160046579 | THERAPEUTIC COMPOUNDS AND COMPOSITIONS - Compounds of general formula (I) and compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases. | 02-18-2016 |
20160046581 | Factor XIa Inhibitors - The present invention provides a compound of Formula (I) | 02-18-2016 |
20160046654 | Prodrugs Of Bicyclic Substituted Pyrimidine Type PDE-5 Inhibitors - Provided are prodrugs of a bicyclic substituted pyrimidine type PDE-5 inhibitors, pharmaceutically acceptable salts or stereoisomers thereof. Also provided are methods for preparing these prodrug compounds, pharmaceutical preparations, and pharmaceutical compositions, as well as a use of these compounds, pharmaceutical preparations and pharmaceutical compositions in the manufacture of medicaments for treatment and/or prophylaxis of sexual dysfunction and lower urinary tract symptoms. | 02-18-2016 |
20160068513 | FUSED PYRIMIDINE COMPOUNDS AND USE THEREOF - Fused pyrimidine compounds as kinase inhibitors, such as multi-kinase inhibitors, are provided. Fused pyrimidine compounds as IGF-IR inhibitors are provided. Fused pyrimidine compounds that are inhibitors of Trk receptors (e.g., Trk A, Trk B and Trk C) are provided also. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer. | 03-10-2016 |
20160083369 | HETEROCYCLIC COMPOUNDS AND USE THEREOF - Heterocyclic compounds of Formula (I) shown herein. Also disclosed are pharmaceutical compositions containing the heterocyclic compounds and methods of using the heterocyclic compounds to mobilize hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation. Further provided are methods for treating tissue injury, cancer, inflammatory disease, and autoimmune disease with the heterocyclic compounds. | 03-24-2016 |
20160115185 | PHOSPHATE ESTERS OF NORIBOGAINE - Disclosed herein are phosphate esters of noribogaine and dihydronoribogaine, and esters and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the methods of their use, including in the treatment of addiction and/or pain. | 04-28-2016 |
20160130284 | SELECTIVE CANCER TRACKING ERADICATOR AND THE USES THEREOF - The present invention discloses a new modality of photodynamic therapy (PDT) through the design of the present invention's truly dual-functional—PDT and imaging—gadolinium complex (Gd-N) with a molecular formula of: | 05-12-2016 |
20160145691 | NOVEL ESTROGEN RECEPTOR MUTATIONS AND USES THEREOF - Novel mutant ESR1 molecules and uses are disclosed. | 05-26-2016 |
20160184333 | MITOCHONDRIA-TARGETED ANTI-TUMOR AGENTS - Described are mitochondria-targeted anti-tumor agents, and methods of making and using the same for the treatment of disorders associated with unwanted cell proliferation. | 06-30-2016 |
20160186175 | BICYCLIC MORPHOLINO COMPOUNDS AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM - The present invention provides bicyclic morpholino compounds and oligomeric compounds prepared therefrom. More particularly, incorporation of one or more of the bicyclic morpholino compounds into an oligomeric compound is expected to enhance one or more properties of the oligomeric compound. Such oligomeric compounds can also be included in a double stranded composition. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. | 06-30-2016 |
20160199397 | Treatment of Dermatological Conditions | 07-14-2016 |
20160200750 | NOVEL CRYSTALLINE FORMS OF CEFTAROLINE FOSAMIL | 07-14-2016 |
20160201135 | NOVEL ESTROGEN RECEPTOR MUTATIONS AND USES THEREOF | 07-14-2016 |
20160376298 | PROTOTYPE SYSTEMS OF THERANOSTIC BIOMARKERS FOR IN VIVO MOLECULAR MANAGEMENT OF CANCER - The present invention relates to a theranostic system comprising a beacon and a compound selected from the group consisting of a quinazoline-based tyrosine kinase inhibitor and a natural product. The theranostic systems have use in the therapy and diagnosis of tyrosine kinase related malignancies. | 12-29-2016 |
20180021314 | THERAPEUTIC AGENT FOR MEIBOMIAN DYSFUNCTION | 01-25-2018 |
20180022752 | FUSED-RING COMPOUNDS, PHARMACEUTICAL COMPOSITION AND USES THEREOF | 01-25-2018 |
20180022766 | ETHER COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS | 01-25-2018 |
20190142851 | COMPOSITIONS COMPRISING A PSILOCYBIN DERIVATIVE AND A CANNABINOID | 05-16-2019 |
20190144424 | Macrophage Migration Inhibitory Factor Inhibitors, and Methods of Making and Using Same | 05-16-2019 |
20190144459 | INHIBITORS OF THE MENIN-MLL INTERACTION | 05-16-2019 |