Class / Patent application number | Description | Number of patent applications / Date published |
544114000 | Diazine ring | 62 |
20090253906 | ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN - The compounds of the present invention are represented by the chemical structure found in Formula (I): | 10-08-2009 |
20100286390 | PYRIDAZINONE COMPOUNDS AND P2X7 RECEPTOR INHIBITORS - Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases. | 11-11-2010 |
20120071651 | Processes for Preparing 1,2-Substituted Cyclopropyl Derivatives - The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H | 03-22-2012 |
20120184736 | METHOD FOR PRODUCING A 3-(SUBSTITUTED-OXY)-4-PYRIDAZINOL DERIVATIVE - Disclosed is a method for producing a 3-(substituted oxy)-4-pyridazinol derivative represented by the general formula (I), which comprises reacting a compound represented by the general formula (III) with a compound represented by the general formula (IV) in the presence or absence of a base and in the presence or absence of a solvent. According to the present invention, a 3-(substituted oxy)-4-pyridazinol derivative represented by the general formula (I) can be produced in high yield and with high selectivity. | 07-19-2012 |
544115000 | The diazine ring is one of the cyclos in a polycyclo ring system | 5 |
20090030196 | PIM KINASE INHIBITORS AS CANCER CHEMOTHERAPEUTICS - Inhibitors of Pim kinases, ways to make them and methods of treating patients using them are disclosed. | 01-29-2009 |
20110190489 | Novel Tricyclic Compounds - The invention provides a compound of Formula (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), or (Il) as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions. | 08-04-2011 |
20120022253 | INDAZOLE, BENZISOXAZOLE, AND BENZISOTHIAZOLE KINASE INHIBITORS - Compounds having the formula | 01-26-2012 |
20120178926 | METHODS FOR PREPARING PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS - A method of preparing a compound represented by Structural Formula (I): | 07-12-2012 |
20120277425 | TETRAHYDROPTERIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - 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. | 11-01-2012 |
544120000 | 1,4-Diazine ring | 26 |
20090198053 | Pyrazine Derivatives and Uses Thereof in Renal Monitoring - The present invention relates to pyrazine derivatives such as those represented by Formulas (I) and (II) below. X | 08-06-2009 |
20100105899 | Integrated Photoactive Small Molecules and Uses Thereof - This invention is directed to the general method of transforming non-photoactive bioactive small molecule compounds of known structure and function into photoactive analogs of the small molecules which exhibit both photoactivity and the original biological targeting activity. The general method for the design of the photoactive analogs of the small molecules includes: (a) selecting a desired bioactive molecule; (b) identifying the region of the molecule that contains an aromatic or a heteroaromatic motif; and (c) either replacing said motif with a photoactive functional group of similar size, or modifying said motif to make it photoactive. Other aspects include photoactive analog compounds and photodiagnostic and phototherapeutic uses thereof. | 04-29-2010 |
20100249405 | Organic Compounds - The present invention relates to novel IAP inhibitor compounds of formula I: | 09-30-2010 |
20110319614 | Organic Compounds - The present invention relates to novel IAP inhibitor compounds of formula I: | 12-29-2011 |
544121000 | Piperazine ring | 22 |
20090318689 | Processes To Make Apoptosis Promoters - Processes to make compounds, including N-acylsulfonamide apoptosis promoters are disclosed. | 12-24-2009 |
20100056779 | SYNTHESIS OF METHYL NONACTATE DERIVATIVES - Methyl nonactate is converted into a variety of different triazoloamide antibacterial agents by a reaction scheme involving (1) inversion of the secondary alcohol of the methyl nonactate to produce the corresponding azidoester, (2) converting the azido ester to the corresponding azidoamide, and (3) converting the azido group of the azidoamide to a triazole to produce the corresponding triazoloamide. | 03-04-2010 |
20100286391 | NOVEL PROCESSES FOR THE PREPARATION OF CYCLOPROPYL-AMIDE DERIVATIVES - The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor. | 11-11-2010 |
20110166346 | NOVEL NAPTHALIMIDE-BENZIMIDAZOLE HYBRIDS AS POTENTIAL ANTITUMOR AGENTS AND PROCESS FOR THE PREPARATION THEREOF - The present invention provides the compounds of general formula 5 and 9 useful as potential antitumour agents against human cancer cell lines. The present invention further provides the process for preparation of napthalimide-benzimidazole hybrids of general formula 5 and 9, n-1-2, R=n-methylpiperazine or morpholine (Formula 9), wherein: n=2-3, m=2-3 and R=n-methylpiperazine or morpholine. | 07-07-2011 |
20110269959 | PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES - The invention relates to a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-cyclohexyl}-carbamide derivatives of general formula (I) by reacting the compound of formula (III) with a carbamoylchloride of general formula (II) which comprises carrying out the reaction in a mixture of a solvent and concentrated aqueous solution of an alkali hydroxide at a temperature between 40-100° C. in the presence of a phase transfer catalyst, separating the phases and washing the organic layer then removing the solvent and drying the compound of formula (I) obtained until its weight is constant. | 11-03-2011 |
20110275803 | PROCESS FOR SYNTHESIZING OXIDIZED LACTAM COMPOUNDS - The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I: | 11-10-2011 |
20110275804 | PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF - The invention relates to a new process for the preparation of compounds of general formula (I) wherein
| 11-10-2011 |
20120029191 | NOVEL PROCESSES FOR THE PREPARATION OF CYCLOPROPYL-AMIDE DERIVATIVES - The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor. | 02-02-2012 |
20120071652 | Novel Piperazines, Pharmaceutical Compositions and Methods of Use Thereof - Disclosed are novel piperazine derivatives that act as agonists of the α7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds. | 03-22-2012 |
20120071653 | Human Adam-10 Inhibitors - The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. | 03-22-2012 |
20120283433 | NOVEL PROCESSES FOR THE PREPARATION OF CYCLOPROPYL-AMIDE DERIVATIVES - The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor. | 11-08-2012 |
20120302746 | 3-PYRIDYLCARBONYL-PIPERAZINYLSULFONYL DERIVATIVES - The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Ca | 11-29-2012 |
20130144056 | Human Adam-10 Inhibitors - The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. | 06-06-2013 |
20130203987 | AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME - Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 08-08-2013 |
20130253188 | NOVEL COMPOUNDS - Compounds of formula (I) | 09-26-2013 |
20130261299 | PYRIDAZINYL DERIVATIVES AS SMO INHIBITORS - The present invention relates to compounds of formula I: | 10-03-2013 |
20130267701 | AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME - Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 10-10-2013 |
20130267702 | AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME - Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 10-10-2013 |
20140051852 | Process for Synthesizing Oxidized Lactam Compounds - The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I: | 02-20-2014 |
20140066621 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. | 03-06-2014 |
20140206865 | Human Adam-10 Inhibitors - The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. | 07-24-2014 |
20150329541 | APOPTOSIS INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. | 11-19-2015 |
544122000 | 1,3-Diazine ring | 27 |
20080249304 | PROCESS FOR PREPARING SUBSTITUTED DIAMINOPYRIMIDINE OXIMES - The present invention is directed to a process for chemoselective substitution on a halopyrimidine carboxaldehyde having multiple reactive sites and subsequent stereoselective oxime formation. | 10-09-2008 |
20090176981 | Stereoisomerically Enriched 3-Aminocarbonyl Bicycloheptene Pyrimidinediamine Compounds And Their Uses - The present invention provides stereoisomers and stereoisomeric mixtures of 3-amino carbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers. | 07-09-2009 |
20090326222 | BENZOTHIAZOLE CYCLOBUTYL AMINE DERIVATIVES - Compounds of formula (I) | 12-31-2009 |
20100190979 | DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - Provided herein are compounds of the formula (I): | 07-29-2010 |
20110046370 | 1,3,6-SUBSTITUTED INDOLE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASE - Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient. | 02-24-2011 |
20110319615 | INSECTICIDAL PYRIMIDINYL ARYL HYRDRAZONES - Pyrimidinyl aryl hydrazones are effective at controlling insects. | 12-29-2011 |
20120065395 | 2,4 (4,6) PYRIMIDINE DERIVATIVES - The present invention concerns the compounds of formula | 03-15-2012 |
20120271048 | NOVEL 1,6-DISUBSTITUTED INDOLE COMPOUNDS AS PROTEIN KINASE INHIBITORS - Disclosed are a 1,6-substituted indole compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of cancers caused by abnormal cell growth comprising the compound as an effective ingredient. | 10-25-2012 |
20130005964 | SULFONYL AMIDE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH - The present invention relates to a compound of the formula I | 01-03-2013 |
20130012704 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention relates to compounds of formula (I) | 01-10-2013 |
20130030171 | Pyrimidinyl Aryl Urea Derivatives being FGF Inhibitors - The invention relates to heteroaryl aryl ureas of the formula IA, | 01-31-2013 |
20130116431 | Novel HSP90 Inhibitor - Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.) | 05-09-2013 |
20130172552 | Novel Small-Molecule Inhibitors of Rac1 in Metastatic Breast Cancer - A novel inhibitor of Rac activity based on the structure of the established Rac/Rac-GEF inhibitor NSC23766 is discloses. The compound EHop-016, with an IC50 of 1.1 μM, is a 100-fold more efficient inhibitor of Rac activity than NSC23766. EHop-016 is specific for Rac1 and Rac3 at concentrations ≦5 mM. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells, EHop-016 (≦5 mM) inhibits the association of the Rac-GEF Vav2 with a nucleotide-free Rac1(G15A), which has a high affinity for activated GEFs. EHop-016 does not affect the association of the Rac-GEF Tiam-1 with Rac1(G15A) at similar concentrations. EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac-downstream effects of p21-activated kinase (PAK)1 activity and directed migration of metastatic cancer cells. At low concentrations (<5 μM), EHop-016 does not affect cell viability. | 07-04-2013 |
20150087827 | METHOD FOR THE PREPARATION OF TRIAZOLE COMPOUNDS - The present invention relates to a process for preparing 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-ol (I—enol form) or 2-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one (I—keto form) and sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate (II) from 1,2,3-triazole (III), methyl bromoacetate (IV-Me-Br) or ethyl bromoacetate (IV-Et-Br), 4,6-dichloropyrimidine (VIII), morpholine (IX) and hydrazine (XII). | 03-26-2015 |
20150099875 | METHODS OF REGIOSELECTIVE SYNTHESIS OF 2,4-DISUBSTITUTED PYRIMIDINES - The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions. | 04-09-2015 |
20160009660 | 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES | 01-14-2016 |
20160145240 | HETEROARYLAMINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - A heteroarylamine compound includes protein kinase inhibition activity, a pharmaceutically acceptable salt thereof and a pharmaceutical composition for preventing and treating a disease caused by abnormal cell growth, which contains the compound as an active ingredient. | 05-26-2016 |
20160159750 | POLYMER FILM, RETARDATION FILM, POLARIZING PLATE, LIQUID CRYSTAL DISPLAY, AND COMPOUND - Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Q | 06-09-2016 |
20160200706 | Imidazole-1-yl pyrimidine derivatives, or pharmacutically acceptable salt thereof, and pharmaceutic composition comprising the same as an active ingredient | 07-14-2016 |
544123000 | Oxygen bonded directly to the diazine ring | 8 |
20090156804 | INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF - The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: | 06-18-2009 |
20100113775 | 2-SUBSTITUTED-6-HETEROCYCLIC PYRIMIDONE DERIVATIVES AS TAU PROTEIN KINASE 1 INHIBITORS - A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein each R | 05-06-2010 |
20110003988 | 3-METHYL-2- ( (2S) -2- (4- (3-METHYL-L, 2, 4-0XADIAZ0L-5-YL) PHENYL) MORPHOLINO) -6- (PYRIM-IDIN-4-YL) PYRIMIDIN-4 (3H) -ONE AS TAU PROTEIN KINASE INHIBITOR - A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: | 01-06-2011 |
20110021773 | 6-PYRIMIDINYL-PYRIMID-4-ONE DERIVATIVE - A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: | 01-27-2011 |
20110251385 | INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF - The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: | 10-13-2011 |
20110257392 | INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF - The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: | 10-20-2011 |
20120059165 | INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF - A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromophenylmorpholine with a hexacyanoferrate(II) or a hydrate thereof at a temperature of from 110° C. to 140° C. in a reaction mixture comprising a Na | 03-08-2012 |
20140221648 | TH17 DIFFERENTIATION MARKERS FOR ACNE AND USES THEREOF - A method is described for using IL-12R 1/IL-23R, CCR6, BATF, AHR, STAT3, IRF4 crucial actors in Th17 cells differentiation as markers for acne. Also described are method of their use to diagnose acne, to screen inhibitors of Th17 differentiation. In particular, methods are described for inhibiting IL12R 1/IL-23R, CCR6, BATF, AHR, STAT3, IRF4 and the use of these screened inhibitors in acne treatment. | 08-07-2014 |