Class / Patent application number | Description | Number of patent applications / Date published |
514253100 | The five-membered nitrogen hetero ring has chalcogen as a ring member | 49 |
20080221116 | ISOXAZOLINE ALPHA 1a/1d ADRENORECEPTOR ANTAGONISTS - The present invention relates to isoxazolines useful as selective α | 09-11-2008 |
20080255141 | 2-(3-AMINOARYL) AMINO-4-ARYL-THIAZOLES AND THEIR USE AS C-KIT INHIBITORS - Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferation metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors. | 10-16-2008 |
20080306083 | Biaryl Compounds Useful as Agonists of the Gpr38 Receptor - The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders. | 12-11-2008 |
20090105271 | PYRIDYL SULFONAMIDES AS MODULATORS OF ION CHANNELS - The present invention relates to pyridyl sulfonamide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 04-23-2009 |
20090170868 | TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF - The invention relates to compounds of formula IA | 07-02-2009 |
20090176796 | TRPV1 ANTAGONISTS INCLUDING AMIDE SUBSTITUENT AND USES THEREOF - The invention relates to compounds of formula IA″ | 07-09-2009 |
20090275594 | 3-HYDRAZONE PIPERAZINYL RIFAMYCIN DERIVATIVES USEFUL AS ANTIMICROBIAL AGENTS - The present invention is directed to novel 3-hydrazone piperazinyl rifamycin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes. | 11-05-2009 |
20090318464 | New Pyridine Analogues V - The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y | 12-24-2009 |
20100004258 | Novel Heterocyclic NF-kB Inhibitors - The present invention relates to compounds of the general formula (III): | 01-07-2010 |
20100010007 | PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR CCR5 - Compounds of formula (I): | 01-14-2010 |
20100041667 | Piperidine and pyrrolidine beta-secretase inhibitors for the treatment of alzheimer's disease - The present invention is directed to compounds of formula (I) | 02-18-2010 |
20100041668 | Compositions and methods for treating thrombocytopenia - The present invention in certain embodiments is directed to a pharmaceutical dosage form comprising a therapeutically effective amount of a first agent that agonizes a human TPO receptor by binding to the rhTPO binding site of the human TPO receptor; and a therapeutically effective amount of a second agent that agonizes the human TPO receptor by binding to a binding site of the human TPO receptor distinct from the rhTPO binding site. | 02-18-2010 |
20100048583 | Novel Heterocyclic NF-kB Inhibitors - The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, | 02-25-2010 |
20100093750 | COMBINATION TREATMENT OF SOLID CANCERS WITH ANTIMETABOLITES AND TYROSINE KINASE INHIBITORS - The present invention relates to a method for treating solid cancers including non-small 5 cell lung cancer, pancreatic, bladder, breast and ovarian cancer as well as advanced biliary tract cancers comprising administering at least one antineoplasticagent such as a nucleotide analog, for example gemcitabine, or an antimitotic such as docetaxel, in combination with a tyrosine kinase inhibitor selected from 2-aminoarylthiazoles and 2-aminoaryloxazoles. | 04-15-2010 |
20100113471 | 2-Aminoaryloxazole compounds as tyrosine kinase inhibitors - The present invention relates to novel compounds selected from 2-aminoaryloxazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors. | 05-06-2010 |
20100168124 | NOVEL HETEROCYCLIC SUBSTITUTED PYRIDINE COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY - The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: | 07-01-2010 |
20100222361 | 2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF - A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia. | 09-02-2010 |
20110059981 | New Pyridine Analogues V - The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y | 03-10-2011 |
20110086861 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER - Provided is a pharmaceutical composition including as an active component a compound of formula (I): | 04-14-2011 |
20110190314 | PHARMACEUTICAL COMPOSITIONS AND THEIR METHODS OF USE - The invention relates to a composition comprising a neuronal nicotinic receptor ligand and an α4β2 positive allosteric modulator, a method of using the same, and a related article of manufacture. | 08-04-2011 |
20110201620 | 2-(3-AMINOARYL) AMINO-4-ARYL-THIAZOLES AND THEIR USE AS C-KIT INHIBITORS - The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, and in particular of masitinib mesylate, for the preparation of a medicament for the treatment of GIST, to the use of this therapy for the treatment of GIST, and a method of treating mammals, including humans, suffering from GIST by administering to said mammal in need of such treatment an effective dose of masitinib, and in particular masitinib mesylate. | 08-18-2011 |
20110212973 | CARBAMATE COMPOUND OR SALT THEREOF - [Problems] A compound useful as an active ingredient for a pharmaceutical composition for treating FAAH-related diseases is provided. | 09-01-2011 |
20110224226 | COMPOSITIONS AND METHODS FOR INCREASING BLOOD PLATELET LEVELS IN HUMANS - Disclosed in certain embodiments is an oral pharmaceutical dosage form of a pharmaceutically acceptable excipient and an effective amount of 1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl]carbamoyl} pyridin-2-yl)piperadine-4-carboxylic acid (Formula I) or a pharmaceutically acceptable salt thereof, to increase platelet levels in humans. | 09-15-2011 |
20110301176 | IMIDAZOTHIAZOLE DERIVATIVES HAVING PROLINE RING STRUCTURE - There is provided compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. Compounds include imidazothiazole derivatives that can inhibit interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity. | 12-08-2011 |
20110306619 | 6-PHENYL-2-[((PIPERIDIN-4-YLMETHYL)-PIPERAZIN-1YL) OR PIPERAZIN 1-YLMETHYL)-PIPERIDIN-1-YL)]-IMIDAZO[2,1-B][1,3,4]THIADIAZOLE DERIVATIVES AND THEIR USE - Provided are heterocyclic compounds, their synthesis and pharmaceutical compositions including them for the treatment of disorders, in particular, cancer. | 12-15-2011 |
20120015957 | PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR - The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor. | 01-19-2012 |
20120059016 | PIPERIDINE AND PIPERAZINE DERIVATIVES AS AUTOTAXIN INHIBITORS - The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers. | 03-08-2012 |
20120065213 | C-MET PROTEIN KINASE INHIBITORS - Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory, neurological, or proliferative diseases or disorders. | 03-15-2012 |
20120196871 | PROCESS FOR THE SYNTHESIS OF 2-AMINOTHIAZOLE COMPOUNDS AS KINASE INHIBITORS - The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula I: | 08-02-2012 |
20120283268 | Thiazole and Thiophene Analogues, and Their Use in Treating Autoimmune Diseases and Cancers - Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed. | 11-08-2012 |
20120295918 | CANCER TREATMENT METHOD - Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human. | 11-22-2012 |
20120302579 | CANCER TREATMENT METHOD - Invented is a method of treating cancer and pre-cancerous syndromes in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal. | 11-29-2012 |
20130079351 | 2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF - A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia. | 03-28-2013 |
20130137703 | AMINOPYRIDINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 05-30-2013 |
20130172362 | Imidazothiazole Derivatives Having Proline Ring Structure - Compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and that exhibit anti-tumor activity are provided. Compounds provided by the present disclosure include imidazothiazole derivatives that inhibit interaction between Mdm2 protein and p53 protein and exhibit anti-tumor activity. | 07-04-2013 |
20130289045 | AMINOTHIAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHODS OF USING THE SAME - The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula I: | 10-31-2013 |
20130324551 | THIAZOLYLPHENYL-BENZENESULFONAMIDO DERIVATIVES AS KINASE INHIBITORS - Thiazolylphenyl-benzenesulfonamido derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. | 12-05-2013 |
20140038982 | CANCER TREATMENT METHOD - Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human. | 02-06-2014 |
20140206699 | PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE - The present invention relates to a compound of formula (IA), wherein G | 07-24-2014 |
20140249159 | HETEROCYCLIC COMPOUNDS - The invention relates to compounds of Formula I: wherein Ar | 09-04-2014 |
20140275107 | CANCER TREATMENT METHOD - Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human. | 09-18-2014 |
20140329829 | TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF - The disclosure relates to Compounds of Formula (I) | 11-06-2014 |
20150065519 | HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists. | 03-05-2015 |
20160007606 | MICROBIOCIDAL PYRAZOLE DERIVATIVES | 01-14-2016 |
20160022671 | TREATMENT OF MASTOCYTOSIS WITH MASITINIB - The treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), including administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt or solvate thereof, in particular in an appropriate dosage regimen. | 01-28-2016 |
20160089368 | TREATMENT OF MASTOCYTOSIS WITH MASITINIB - The treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), including the administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt or solvate thereof, in particular in an appropriate dosage regimen. | 03-31-2016 |
20160096811 | BENZOISOTHIAZOLE COMPOUNDS AND USE IN PREPARATION OF ANTIPSYCHOTIC DRUGS - Disclosed are benzoisothiazole compounds and a use in the preparation of anti-schizophrenia drugs. The benzoisothiazole compounds of the present invention not only have strong affinity for dopamine D | 04-07-2016 |
20160101102 | PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE - The present invention relates to a compound of formula (IA), wherein G | 04-14-2016 |
20160115153 | LANTHIONINE SYNTHETASE C-LIKE 2-BASED THERAPEUTICS - Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease. | 04-28-2016 |