| Entries |
| Document | Title | Date |
|---|
| 20080234300 | Pyrimido[5,4-c] Quinoline-2, 4-Diamine Derivatives and Methods of Use Thereof - The present invention relates to pyrimido[5,4-c]quinoline-2,4-diamine derivatives, compositions comprising an effective amount of a Pyrimido[5,4-c]quinoline-2,4-diamine Derivative, methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of an Pyrimido[5,4-c]quinoline-2,4-diamine Derivative, methods for modulating PDK-1 activity, comprising administering to a subject in need thereof an effective amount of a Pyrimido[5,4-c]quinoline-2,4-diamine Derivative. The invention also relates to a process for preparing a Pyrimido[5,4-c]quinoline-2,4-diamine Derivative. | 09-25-2008 |
| 20080300264 | SUBSTITUTED THIATRIAZAACENAPHTHYLENE-6-CARBONITRILE KINASE INHIBITORS - The present invention is directed to substituted thiatriazaacenaphthylene-6-carbonitrile compounds of formula (I): | 12-04-2008 |
| 20090005402 | Medicine containing pyrimidine derivative - A drug for central diseases which contains a compound represented by general formula (I), or a pharmacologically acceptable salt thereof, as active component | 01-01-2009 |
| 20090018149 | 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and methods for medical intervention against mycobacterial infections - Described are 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of mycobacteria-induced infections and opportunistic infections, as well as compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene derivative and/or pharmaceutically acceptable salts thereof. Furthermore, the present application refers to the use of mycobacterial protein serine/threonine kinases for developing methods for detection and determination of these kinases for recognising and monitoring diseases and for controlling therapy of diseases. | 01-15-2009 |
| 20090023760 | Anti-cancer cyclopenta[G]quinazoline compounds - Cyclopenta[g]quinazolines of the formula (I): wherein: A is a group OR or NR | 01-22-2009 |
| 20090054471 | PYRIDOPYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USES AS ANTI-CANCER AND ANTI-DIABETE DRUGS - The present invention relates to pyridopyrazolopyrimidine derivatives that are useful pharmacological agents through the inhibition or antagonism of protein kinases, and to processes for the preparation and use of the same. In particular, the present invention relates to compounds that demonstrate protein tyrosine kinase and/or protein serine/threonine kinase inhibition. | 02-26-2009 |
| 20090054472 | Pyrazolopyrimidine Derivatives or Pharmaceutically Acceptable Salts Thereof - A pyrazolopyrimidine derivative represented by formula (1) and pharmaceutically acceptable salt thereof exhibit excellent inhibitory activity against MAPKAP-K2. Accordingly, medicines containing this compound as an active ingredient are expected to be effective for treating diseases mediated by MAPKAP-K2 such as, for example, inflammatory disorder, autoimmune diseases, destructive osteopathy, cancer and/or tumor growth. | 02-26-2009 |
| 20090062318 | TRICYCLIC COMPOUNDS HAVING CYTOSTATIC AND/OR CYTOTOXIC ACTIVITY AND METHODS OF USE THEREOF - The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders. | 03-05-2009 |
| 20090082373 | Uses of 2-[piperidinyl]methyl-2, 3-dihydroimidazo[1,2-c]quinazolin-5(6H)-one for providing an analgesic effect, anti-allergic effect and histamine H1 receptor antagonism effect - The present invention discloses new uses of 2-[piperidinyl]methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-one in providing an analgesic effect in a patient, treating passive cutaneous anaphylaxis in a patient, and in eliciting a histamine H | 03-26-2009 |
| 20090082374 | TRICYCLIC COMPOUNDS HAVING ANTIMITOTIC AND/OR ANTITUMOR ACTIVITY AND METHODS OF USE THEREOF - The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells. | 03-26-2009 |
| 20090088446 | PURINONE DERIVATIVES AS HM74A AGONISTS - The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease. | 04-02-2009 |
| 20090111837 | USE OF PDE7 INHIBITORS FOR THE TREATMENT OF NEUROPATHIC PAIN - The present invention relates to the use of a phosphodiesterase 7 (PDE7) inhibitor in the manufacture of a medicament for the treatment of neuropathic pain and to a method of treating neuropathic pain using an inhibitor of PDE7. | 04-30-2009 |
| 20090143415 | Tetrodotoxin And Its Derivatives For The Treatment Of Central-Nervously Derived Neuropathic Pain - The present invention refers to the use of a sodium channel blocker such as tetrodotoxin or saxitoxin, their analogues and derivatives as well as their physiologically acceptable salts, in medicinal products for human therapeutics for the treatment of central-nervously derived neuropathic pain. | 06-04-2009 |
| 20090170882 | Methods and compositions - Compounds, compositions and methods relating to kinesin inhibition are described herein. | 07-02-2009 |
| 20090192178 | mGluR1 ANTAGONISTS AS THERAPEUTIC AGENTS - In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J | 07-30-2009 |
| 20090197901 | VARIOLIN DERIVATIVES AND THEIR USE AS ANTITUMOR AGENTS - Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X | 08-06-2009 |
| 20090203719 | ENHANCING TREATMENT OF MDR CANCER WITH ADENOSINE A3 ANTAGONISTS - The present invention discloses the use of high affinity adenosine A | 08-13-2009 |
| 20090247559 | Benzofuropyrimidinones - A compound according to formula I: | 10-01-2009 |
| 20090270432 | 7-[2-[4-(6-FLUORO-3-METHYL-1,2-BENZISOXAZOL-5-YL)-1-PIPERAZINYL]ETHYL]-2-(- 1-PROPYNYL)-7H-PYRAZOLO-[4,3-e]-[1,2,4]-TRIAZOLO-[1,5-c]-PYRIMIDIN-5-AMINE - The compound having the structural formula I | 10-29-2009 |
| 20090286814 | HCV PROTEASE INHIBITORS - This invention relates to macrocyclic compounds of formula (I) or (II) shown in the specification. These compounds can be used to treat hepatitis C virus infection. | 11-19-2009 |
| 20090286815 | Pyrimidine Classical Cannabinoid Compounds and Related Methods of Use - Disclosed are compounds of the formula I: | 11-19-2009 |
| 20090298858 | POTENT PARP INHIBITORS - The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), | 12-03-2009 |
| 20090306107 | Organic Compounds - The present invention relates to compounds that are useful to inhibit, regulate and/or modulate tyrosine and serine/threonine kinase and kinase-like proteins, such as RAF kinase, a serine/threonine kinase that functions in the MAP kinase signaling pathway. The application is also concerned with compositions which contain these compounds, and methods of using them to treat tyrosine and serine/threonine kinase and kinase-like dependent diseases, such as angiogenesis, cancer and cardiac hypertrophy, and with other subject matter. | 12-10-2009 |
| 20100016341 | ASPARTYL PROTEASE INHIBITORS CONTAINING A TRICYCLIC RING SYSTEM - Disclosed are compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof or wherein R | 01-21-2010 |
| 20100029697 | SUBSTITUTED PYRIDO[3,2-E][1,2,4]TRIAZOLO[4,3-C]PYRIMIDINE DERIVATIVES AS CANNABINOID-1 RECEPTOR MODULATORS - Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer s disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness. | 02-04-2010 |
| 20100048592 | Use of sodium channel blockers for the management of musculoskeletal pain - The invention provides methods for managing musculoskeletal pain. The compounds useful in the methods of the invention are blockers of sodium ion channels, and in particular compounds that bind to the SS1 or SS2 extracellular mouth of the a-subunit thereof. Particularly useful compounds are saxitoxin and its derivatives and analogues and tetrodotoxin and its derivatives and analogues. | 02-25-2010 |
| 20100048593 | DEAZAFLAVIN COMPOUNDS AND METHODS OF USE THEREOF - The present invention features 5-deazaflavin compounds, pharmaceutical compositions of 5-deazaflavin compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more 5-deazaflavin compounds of the invention. | 02-25-2010 |
| 20100056549 | HIGHLY SOLUBLE PYRIMIDO-DIONE-QUINOLINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER - The present invention features pyrimido-dione-quinoline compounds having improved solubility, pharmaceutical compositions of substituted pyrimido-dione-quinoline compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more pyrimido-dione-quinoline compounds of the invention. | 03-04-2010 |
| 20100056550 | TRICYCLIC HETEROAROMATIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to novel substituted tricyclic heteroaromatic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 03-04-2010 |
| 20100056551 | Anti-cancer cyclopenta [G] quinazoline compounds - Cyclopenta[g]quinazolines of the formula (I):—wherein: A is a group OR or NR | 03-04-2010 |
| 20100069415 | 2,6-DIPHENYL-4,8-DIAZOADAMANTAN-1-ONE AND DERIVATIVES THEREOF, PROCESS OF MANUFACTURE AND USE FOR THE FORMULATION OF SOLUTIONS WITH STERILIZING AND DISINFECTANT EFFECT - A chemical compound having the following structural formula wherein optionally at least one of the phenyl —C | 03-18-2010 |
| 20100075998 | TRICYCLIC INDOLES AND (4,5-DIHYDRO) INDOLES - The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, | 03-25-2010 |
| 20100075999 | Process for the Preparation of Ethyl-N-(2,3-Dichloro-6-Nitrobenzyl)Glycine Hydrochloride - The invention relates to a process for the preparation of anagrelide, and for the preparation of intermediates for use in preparing anagrelide. The invention also relates to the intermediates per se, in particular compounds of Formula (V): | 03-25-2010 |
| 20100120805 | Fused Bicyclic and Tricyclic Pyrimidine Compounds as Tyrosine Kinase Inhibitors - Fused bicyclic or tricyclic compounds of formula (I): | 05-13-2010 |
| 20100137343 | SUBSTITUTED QUINAZOLINES - This invention relates to the discovery of 3- and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets. | 06-03-2010 |
| 20100144767 | Use of sodium channel blockers for the treatment of visceral pain or pain caused by cancer treatment - The invention provides methods for treating visceral pain and pain associated with therapy. The compounds useful in the methods of the invention are blockers of sodium ion channels, and in particular compounds that bind to the SS1 or SS2 extracellular mouth of the α-subunit thereof. Particularly useful compounds are saxitoxin and its derivatives and analogues and tetrodotoxin and its derivatives and analogues. | 06-10-2010 |
| 20100190808 | Tricyclic Compounds As Modulators of TNF-alpha Synthesis - The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-alpha or by PDE4, including but not limited to rheumatoid arthritis. | 07-29-2010 |
| 20100197707 | Platelet manipulation to reduce the incidence of and treat endovascular disease and its sequelae, to reduce the incidence of and treat arrhythmias and to reduce the incidence of malignancy - Manipulation of total body platelet activity via pharmacologic, mechanical, electrical or electronic means, or any combination thereof, or any other means, alone or in conjunction with manipulation of the activity of the coagulation cascade, for the purpose of reducing the incidence and severity of vascular disease in at risk populations, for the stabilization and reversal of said disease in patients already known to suffer from such disease, as well as for the purpose of reducing the incidence and severity of sequelae related to such disease, whether preclinical, subclinical or overtly manifested, or whether it is presently understood to be related to said vascular disease or not. | 08-05-2010 |
| 20100216824 | Anti-cancer cyclopenta [G]quinazonline compounds - Cyclopenta[g]quinazolines of the formula (I):— | 08-26-2010 |
| 20100273817 | Anti-cancer cyclopenta(g)quinazoline compounds - Cyclopenta[g]quinazolines of the formula (I):—wherein: A is a group OR or NR | 10-28-2010 |
| 20100292256 | (EN) 2-ALKYLAMINO-3-ARYLSULFONYL-CYCLOALCANO [e OR d] PYRAZOLO [1,5-A]PYRIMIDINES / ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND THE USE THEREOF - The invention relates to substituted 2-alkylamino-3-(arylsulfonyl)cycloalkyl[e or d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT | 11-18-2010 |
| 20100292257 | USES OF 2-[PIPERIDINYL] METHYL-2, 3-DIHYDROIMIDAZO [1,2-C] QUINAZOLIN-5 (6H)-ONE FOR PROVIDING AN ANALGESIC EFFECT, ANTI-ALLERGIC EFFECT AND HISTAMINE H1 RECEPTOR ANTAGONISM EFFECT - The present invention discloses new uses of 2-[piperidinyl]methyl-2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-one in providing an analgesic effect in a patient, treating passive cutaneous anaphylaxis in a patient, and in eliciting a histamine H | 11-18-2010 |
| 20100298360 | SMALL MOLECULE INHIBITORS OF PDZ INTERACTIONS - The present invention relates to compositions for use in the modulation of PDZ domain interactions with cognate ligands. Methods of assessing and characterizing PDZ domain interactions from various polypeptides also are provided. | 11-25-2010 |
| 20100317677 | Methods of Treating a Microbial Infection by Modulating RNase-L Expression and/or Activity - The invention relates to methods and compositions for treating a microbial infection. In the present invention, RNase-L activity has been shown to play an integral role in innate immunity and for defense against invading microbes. The present invention is drawn to exploiting the role of RNase-L in innate immunity for methods of treating a microbial infection. The present invention is also drawn to exploiting the role of RNase-L in innate immunity for methods of treating an immune related disease or disorder. | 12-16-2010 |
| 20100331351 | METHODS AND COMPOSITIONS FOR TREATING BACTERIAL INFECTION - The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections. | 12-30-2010 |
| 20110015214 | TRICYCLIC BENZO[4,5]THIENO-[2,3-D]PYRIMIDINE-4-YL-AMIN DERIVATIVES, THEIR SALTS, PROCESS FOR PRODUCING THE COMPOUNDS AND THEIR PHARMACEUTICAL USE - The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutically active agent and as pharmaceutical compositions for prophylaxis and/or treatment of proliferative diseases such as cancer. | 01-20-2011 |
| 20110039870 | TETRAHYDRO-PYRAZOLO[1,5-A]PYRIDO-PYRIMIDINES AS ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS, METHODS FOR THE PRODUCTION AND USE THEREOF - The present invention relates to serotonin 5-HT | 02-17-2011 |
| 20110059997 | SUBSTITUTED CYCLOALCANO[e AND d] PYRAZOLO [1,5-a]PYRIMIDINES/ANTAGONISTS OF SEROTONIN 5-HT6 RECEPTORS AND METHODS FOR PRODUCTION AND THE USE THEREOF - The invention relates to substituted 2-alkylsulfanyl-3-(arylsulfonyl)-cycloalkyl[e and d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, comprising the said conpounds as active ingredients, to novel medicaments and methods for treatment and prophylaxis of CNS diseases of humans and warm blooded animals pathogenesis of which is associated with 5-HT6 receptors. | 03-10-2011 |
| 20110065737 | HCV PROTEASE INHIBITORS - This invention relates to macrocyclic compounds of formula (I) shown in the specification. These compounds can be used to treat hepatitis C virus infection. | 03-17-2011 |
| 20110065738 | POLYCYCLIC GUANINE DERIVATIVES AND USE THEREOF - The present invention relates to Polycyclic Guanine Derivatives, compositions comprising the Polycyclic Guanine Derivatives and methods of using the Polycyclic Guanine Derivatives to treat pain or an inflammatory disease. | 03-17-2011 |
| 20110071170 | TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVES - A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1). | 03-24-2011 |
| 20110071171 | 2H- PYRIMIDO [2, 1-B] QUINAZOLIN-2-ONE DERIVATIVES AND THEIR USE AS PLATELET ANTI-AGGREGATIVE AGENTS - This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim | 03-24-2011 |
| 20110071172 | SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS - This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim (I): and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets. | 03-24-2011 |
| 20110071173 | IMIDAZOQUINAZOLINE DERIVATIVES AS ANAGRELIDE ANALOGUES FOR THE TREATMENT OF MYELOPROLIFIC DISEASES AND THROMBOTIC DISEASES - This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim | 03-24-2011 |
| 20110071174 | SUBSTITUTED QUINAZOLINES - This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim | 03-24-2011 |
| 20110077257 | SUBSTITUTED DIHYDRO, TRIHYDRO AND TETRAHYDRO CYCLOALKYLOXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF - The present disclosure relates to a series of 2-substituted-di- tri or tetra-hydro-8H-cyclopentaoxazolo[3,2-a]pyrimidin-8-ones and 2-substituted-di-, tetra-, or hexa-hydro-cyclohexaoxazolo[3,2-a]pyrimidin-9-ones of formula (I): | 03-31-2011 |
| 20110092525 | GABAA RECEPTOR MODULATORS - The resent invention relates to novel compounds of the general formula (I) having anxiolytic, anticonvulsant, sedative-hypnotic and myorelaxant conditions as well as anxiogenic, somnolytic and convulsant conditions in mammals, including humans, as GABA | 04-21-2011 |
| 20110105540 | 2-AMINO-9-[4-(4-METHOXY-PHENOXY)-PIPERIDIN-1-YL]-4-PHENYL-INDENO[1,2-D]PYR- IMIDIN-5-ONE AND ITS USE AS A HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONIST - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. | 05-05-2011 |
| 20110105541 | ALKYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. | 05-05-2011 |
| 20110105542 | PYRAZOLO--QUINAZOLINES - The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C | 05-05-2011 |
| 20110124666 | 3,4-DIHYDROPYRIMIDINE TRPA1 ANTAGONISTS - The present invention is related to novel 3,4-dihydropyrimidine compounds of formula (I) having TRPA1 receptor antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans. | 05-26-2011 |
| 20110130414 | NOVEL FUSED THIAZOLO AND OXAZOLO PYRIMIDINONES - The present invention relates to novel compounds, their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals. | 06-02-2011 |
| 20110144138 | SUBSTITUTED PYRIMIDO ISOQUINOLINE DERIVATIVES - Pyrimido isoquinoline derivatives represented by formula (I): | 06-16-2011 |
| 20110152298 | IMIDAZO [2,1-B] QUINAZOLIN-2-ONE DERIVATIVES AND THEIR USE AS PLATELET ANTI-AGGREGATIVE AGENTS - This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below where the substituents have the meanings defined in claim (I) and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets. | 06-23-2011 |
| 20110160233 | ANTI-VIRAL COMPOUNDS - Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections. | 06-30-2011 |
| 20110160234 | Tricyclic Compounds as Modulators of TNF-alpha Synthesis and as PDE4 Inhibitors - The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis. | 06-30-2011 |
| 20110178107 | HCV PROTEASE INHIBITORS - This invention relates to compounds of Formula (I), (II), or (III) shown in the specification. These compounds can be used to treat hepatitis C virus infection. | 07-21-2011 |
| 20110190324 | METHODS OF TREATING ATHEROSCLEROSIS - The present invention relates to adenosine A3 receptor antagonists and their use for the prevention and treatment of atherosclerosis by administering to a mammal, in need thereof, a therapeutically effective amount of an adenosine A3 receptor antagonist, or a pharmaceutically acceptable salt thereof, alone or in combination with other anti-atherosclerotic agents. | 08-04-2011 |
| 20110190325 | COMPOUNDS, THEIR SYNTHESES, AND THIER USES - Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections). | 08-04-2011 |
| 20110207757 | Tricyclic Compounds Having Cytostatic and/or Cytoxic Activity and Methods of Use Thereof - The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders. | 08-25-2011 |
| 20110237611 | CHEMICAL PERMEATION ENHANCERS ENHANCE NERVE BLOCKADE BY TOXINS - Chemical permeation enhancers (CPEs) improve access of local anesthetics to the nerve, thereby improving their performance. Surfactants, representing three CPE sub-groups: anionic, cationic, and nonionic surfactants, were co-injected with tetrodotoxin (TTX) or bupivacaine at the sciatic nerve of Sprague-Dawley rats. All enhancers produced marked concentration-dependent improvements in the frequency and duration of block with TTX but not bupivacaine. An in vitro toxicity assay showed a wide range of CPE myotoxicity, but in vivo histological assessment showed no signs of muscle or nerve damage at concentrations of CPEs that produced a half-maximal increase in the duration of block of TTX. There was no systematic relationship between the enhancers' charge or hydrophobicity and their enhancement of block duration or potency. Thus, CPEs can provide marked prolongation of nerve blockade from TTX, without apparent local tissue toxicity, and therefore enhance the clinical applicability of TTX for prolonged-duration local anesthesia. | 09-29-2011 |
| 20110288108 | TRICYCLIC COMPOUNDS HAVING ANTIMITOTIC AND/OR ANTITUMOR ACTIVITY AND METHODS OF USE THEREOF - The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells. | 11-24-2011 |
| 20120004250 | PYRIMIDINE CLASSICAL CANNABINOID COMPOUNDS AND RELATED METHODS OF USE - Disclosed are compounds of the formula I: | 01-05-2012 |
| 20120041007 | CDK INHIBITOR SALTS - The present invention relates to novel crystalline form(s) of water-soluble salts and of free base of a cdk inhibitor. Such crystal salts are for example fumarate, L-malate, maleate, succinate, adipate, malonate, glycolate, phosphate, mesylate, L-lactate, hydrochloride, di-hydrochloride, tri-hydrochloride. Hydrates and polymorphs of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application. | 02-16-2012 |
| 20120065217 | METHODS FOR PURIFYING PHYCOTOXINS, PHARMACEUTICAL COMPOSITIONS CONTAINING PURIFIED PHYCOTOXINS, AND METHODS OF USE THEREOF - Phycotoxins are purified from a mixture of phycotoxins produced in a continuous process. Cyanobacteria are produced in a continuous culture, then lyzed, the cells pelleted and extracted, and the extract purified using an organic solvent-aqueous mixture and repeated passage through a diatomaceous earth column. The column is washed with acetic acid, then the neosaxitoxin extracted with an alcohol-water mixture. The eluate is passed through activated charcoal columns, which are washed with distilled water to remove the retained pigments and impurities, the further purified by HPLC. In one embodiment, the process produces only neosaxitoxin and saxitoxin. In another embodiment, the process produces only GTX2/3. | 03-15-2012 |
| 20120157481 | TRICYCLIC PYRIMIDINE DERIVATIVES AS WNT ANTAGONISTS - The present invention relates to compounds having the general formula (I) with the definitions of X1-X3, Y1, Y2, L1, R1 and R2 given below and/or solvates, hydrates, esters and pharmaceutically acceptable salts thereof. Furthermore, the invention relates to the use of said compounds for modulating of the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer. | 06-21-2012 |
| 20120172381 | Tricyclic Compounds as Modulators of TNF-alpha Synthesis and as PDE4 Inhibitors - The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis. | 07-05-2012 |
| 20120178769 | NOVEL COMPOUNDS FOR INHIBITING EEF-2 KINASE ACTIVITY - The present invention discloses novel compounds for inhibiting eEF2 kinase and methods of use thereof. | 07-12-2012 |
| 20120196880 | PYRAZOLYL AND PYRIMIDINYL TRICYCLIC ENONES AS ANTIOXIDANT INFLAMMATION MODULATORS - Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: | 08-02-2012 |
| 20120202833 | TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVES - A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1). | 08-09-2012 |
| 20120238592 | Use and Application of a Pharmaceutical Composition Containing a Mixture of Natural-Origin Heterocylcial Guanidine - Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided. | 09-20-2012 |
| 20120252828 | PYRIDOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 10-04-2012 |
| 20120289523 | PYRROLO [3,2-E] [1,2,4] TRIAZOLO [1,5-A] PYRIMIDINES DERIVATIVES AS INHIBITORS OF MICROGLIA ACTIVATION - The invention relates to novel compounds useful in the treatment and prophylaxis of disease. Compounds of the formula (I) wherein X is halogen, independently selected form chlorine and fluorine and n is 0, 1 or 2, and their pharmaceutically acceptable salts are useful in the treatment and prophylaxis of diseases caused by activation of microglia, particularly Alzheimer's disease. | 11-15-2012 |
| 20120289524 | PYRROLO [3,2-E] [1,2,4] TRIAZOLO [1,5-A] PYRIMIDINES DERIVATIVES AS INHIBITORS OF MICROGLIA ACTIVATION - The invention relates to novel compounds useful in the treatment and prophylaxis of disease. Compounds of the formula (I): | 11-15-2012 |
| 20120322818 | PHYCOTOXINS AND USES THEREOF - Pharmaceutical compositions for interfering with neuronal transmission comprising an effective amount of at least one tricyclic 3,4-propinoperhydropurine and at least one additional compound are disclosed. Preparations for topical applications are provided that comprise an effective amount of the composition of the invention and a pharmacologically acceptable carrier. Methods of interfering with neuronal transmission comprising topical application of an effective amount of the at least one tricyclic 3,4-propinoperhydropurine are provided for treatment of a variety of indications that relate to muscle relaxation, anesthesia, muscle spasms and similar causes. | 12-20-2012 |
| 20130018063 | ORGANIC COMPOUNDS - The invention provides novel 7,8-dihydro-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2H]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C | 01-17-2013 |
| 20130096146 | Tricyclic Compounds Having Antimitotic and/or Antitumor Activity and Methods of Use Thereof - The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells. | 04-18-2013 |
| 20130102623 | Tricyclic Compounds Having Cytostatic and/or Cytotoxic Activity and Methods of Use Thereof - The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders. | 04-25-2013 |
| 20130123286 | Novel Fused Heterocyclic Derivatives Useful as c-Met Tyrosine Kinase Inhibitors - Certain novel fused quinazoline derivatives of formula (I) as c-Met inhibitors, their synthesis and their uses for treating a c-Met mediated disorder. Methods for treating a c-Met-mediated disorder are also disclosed in the invention. | 05-16-2013 |
| 20130158052 | PYRIMIDINE CLASSICAL CANNABINOID COMPOUNDS AND RELATED METHODS OF USE - Disclosed are compounds of the formula I: | 06-20-2013 |
| 20130178488 | TRICYCLIC COMPOUNDS, PREPARATION METHODS, AND THEIR USES - The present invention relates to novel compounds that inhibit Lp-PLA | 07-11-2013 |
| 20130184298 | DIHYDROBENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to dihydrobenzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 07-18-2013 |
| 20130190335 | FLUORESCENT ANTAGONISTS OF THE A3 ADENOSINE RECEPTOR - Disclosed are compounds of the formula (I) which are fluorescently labeled antagonists of the A | 07-25-2013 |
| 20130203789 | Novel Inhibitors of LYN Kinase and Methods Using Same - The invention includes compounds that inhibit LYN kinase activity. The invention further includes a method of treating, ameliorating or preventing cancer in a subject in need thereof, wherein the cancer is dependent on LYN kinase activity. | 08-08-2013 |
| 20130210845 | Tricyclic Proteasome Activity Enhancing Compounds - Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies. | 08-15-2013 |
| 20130225616 | CRYSTALLINE FORM OF PYRIMIDIO[6,1-A] ISOQUINOLIN-4-ONE COMPOUND - The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern. | 08-29-2013 |
| 20130245048 | 4-AZA-2, 3-DIDEHYDROPODOPHYLLOTOXIN COMPOUNDS AND PROCESS FOR THE PREPARATION THEREOF - The present invention provides 4-Aza-2,3-didehydropodophyllotoxin compound of general formula A (4a-4z and 4aa-4ae) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4-Aza-2,3-didehydropodophyllotoxin compounds (4a-4z and 4aa-4ae). | 09-19-2013 |
| 20130245049 | Novel Antiviral Compounds - The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection. | 09-19-2013 |
| 20130261140 | TRICYCLIC HETEROCYCLES USEFUL AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS - The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. I | 10-03-2013 |
| 20130281474 | FUSED TRICYCLIC INHIBITORS OF MAMMALIAN TARGET OF RAPAMYCIN - This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders. | 10-24-2013 |
| 20130310405 | SUBSTITUTED PYRIMIDO[1,2-B]INDAZOLES AND THEIR USE AS MODULATORS OF THE PI3K/AKT PATHWAY - Compounds of Formula (I), which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals. The compounds of formula (I) a: useful for the treatment of cancer. | 11-21-2013 |
| 20130331406 | NOVEL FUSED THIAZOLO AND OXAZOLO PYRIMIDINONES - The present invention relates to novel compounds, their pharmaceutically acceptable salts, and their isomers, steroisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals. | 12-12-2013 |
| 20140113920 | TRICYCLIC HETEROCYCLES USEFUL AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS - The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 04-24-2014 |
| 20140163051 | Use and Application of a Pharmaceutical Composition Containing a Mixture of Natural-Origin Heterocyclical Guanidine, For Cosmetology, Wound Healing, Focal Dystonia and Muscular Spasm- Related Clinical Pathologies - Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided. | 06-12-2014 |
| 20140163052 | FUSED TRICYCLIC DUAL INHIBITORS OF CDK 4/6 AND FLT3 - Compounds of Formula I are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula I have the following structure: | 06-12-2014 |
| 20140171456 | FUSED TRICYCLIC COMPOUNDS AS mTOR INHIBITORS - The present invention relates to certain pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine and dipyrazolopyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine or dipyrazolopyrimidine compounds. | 06-19-2014 |
| 20140221407 | USE AND APPLICATION OF A PHARMACEUTICAL COMPOSITION CONTAINING A MIXTURE OF NATURAL-ORIGIN HETEROCYCLICAL GUANIDINE, FOR COSMETOLOGY, WOUND HEALING, FOCAL DYSTONIA AND MUSCULAR SPASM- RELATED CLINICAL PATHOLOGIES - Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided. | 08-07-2014 |
| 20140275130 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 09-18-2014 |
| 20140275131 | ORGANIC COMPOUNDS - Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them. | 09-18-2014 |
| 20140288103 | Neosaxitoxin Combination Formulations for Prolonged Local Anesthesia - Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations. | 09-25-2014 |
| 20140329840 | MOLECULES WITH POTENT DHFR BINDING AFFINITY AND ANTIBACTERIAL ACTIVITY - 7-(substituted) derivatives of 7H-pyrrolo[3,2-f]-quinazoline-1,3-diamines, derivative thereof, and methods of using them are provided. The pharmaceutical formulations prepared from the compounds can be used to treat a variety of conditions, which include, but are not limited to bacterial and fungal infections. The compounds can also be used as a sterilizing or disinfecting agent. | 11-06-2014 |
| 20140329841 | Neosaxitoxin Combination Formulations for Prolonged Local Anesthesia - Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations. | 11-06-2014 |
| 20140343082 | ICOTINIB HYDROCHLORIDE, SYNTHESIS, CRYSTALLINE FORMS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF - The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride. | 11-20-2014 |
| 20140350036 | AGENTS THAT PREVENT OR REPAIR SKIN DAMAGE - The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides dermatological compositions comprising a compound of formula I or mixtures of one or more compounds of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for protecting skin or DNA from photodamage or repairing photodamaged skin or DNA. | 11-27-2014 |
| 20140371249 | CRYSTAL OF A FREE TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVE - To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like. | 12-18-2014 |
| 20140371250 | Tricyclic Compounds as Modulators of TNF-alpha Synthesis and as PDE4 Inhibitors - The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis. | 12-18-2014 |
| 20140378486 | PYRROLOQUINAZOLINE COMPOUNDS - Disclosed herein are acylated derivatives of 7H-pyrrolo[3,2-f]quinazoline-1,3-diamine and pharmaceutical compositions comprising said derivatives. | 12-25-2014 |
| 20140378487 | TRICYCLIC COMPOUNDS, PREPARATION METHODS, AND THEIR USES - The present invention relates to novel compounds that inhibit Lp-PLA | 12-25-2014 |
| 20150025093 | IRAK INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 01-22-2015 |
| 20150031713 | ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to benzoquinazilinone compounds of formula (I) | 01-29-2015 |
| 20150065528 | PARALYTIC SHELLFISH POISON - The invention concerns a paralytic shellfish poison for the treatment of itching in a human being or another mammal. | 03-05-2015 |
| 20150141444 | N-METHYL TETRAHYDROQUINOLINE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 05-21-2015 |
| 20150141445 | Tricyclic Compounds Having Cytostatic and/or Cytotoxic Activity and Methods of Use Thereof - The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders. | 05-21-2015 |
| 20150335646 | Pyrimido[4,5-b]quinoline-4,5(3H,10H)-diones - The invention relates to compound of the formula (I); or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it. | 11-26-2015 |
| 20150336965 | NOVEL ANTIVIRAL COMPOUNDS - The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection. | 11-26-2015 |
| 20150352115 | COMPOUNDS USEFUL FOR TREATING INJURIES FROM WARFARE AGENTS - Compounds and compositions for treating disorders related to TRPA1 are described herein. | 12-10-2015 |
| 20150374700 | TRICYCLIC COMPOUNDS AS MODULATORS OF TNF-ALPHA SYNTHESIS AND AS PDE4 INHIBITORS - The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to rheumatoid arthritis. | 12-31-2015 |
| 20160000790 | DRUG COMBINATION - The invention provides a composition which comprises (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a muscarinic receptor antagonist. | 01-07-2016 |
| 20160008363 | DRUG COMBINATION | 01-14-2016 |
| 20160009708 | COMPOUNDS USEFUL FOR TREATING DISORDERS RELATED TO TRPA1 | 01-14-2016 |
| 20160045506 | USE OF INHIBITORS OF BINDING BETWEEN A PAR-1 RECEPTOR AND ITS LIGANDS FOR THE TREATMENT OF GLIOMA - The present invention relates to a method of treating glioma in a subject. The method comprises selecting a subject having a glioma, providing an inhibitor of binding between a PAR-1 receptor and a ligand of the PAR-1 receptor, and administering the inhibitor to the selected subject under conditions effective to treat the glioma and/or prevent spread of tumor cells. Methods for inhibiting proliferation of glioma cells and/or precursors thereof and a method of screening for compounds suitable for treating glioma in subjects are also disclosed. | 02-18-2016 |
| 20160096837 | SUBSTITUTED 1,2,3,4-TETRAHYDROPYRIDO[3,4-E] PYRROLO[1,2-A]PYRIMIDINES AS KINASE INHIBITORS - The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. | 04-07-2016 |
| 20160137658 | POLYMORPHIC FORMS OF ICOTINIB MALEATE AND USES THEREOF - Provided are Icotinib maleate (the compound of Formula I) and polymorph forms thereof, and methods of preparing and using them. | 05-19-2016 |
| 20170233399 | ORGANIC COMPOUNDS | 08-17-2017 |
| 20190142832 | Marker for Cancer Prognosis and Methods Related Thereto | 05-16-2019 |
| 20190142836 | SMALL MOLECULE NF-kB INHIBITORS | 05-16-2019 |
| 20190144460 | COMPOUNDS AND METHODS | 05-16-2019 |
| 20190144465 | Macrocyclic MCL-1 inhibitors and methods of use | 05-16-2019 |
