- BICYCLIC HETEROARYL SUBSTITUTED COMPOUNDS
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Disclosed are compounds of Formula (I) to (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII); or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a bicyclic heteroaryl group substituted with zero to 3 R3a; and R1, R2, R3a, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.
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Page/Page column 331
(2018/03/25)
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- Polymerizable compound, polymerizable composition, polymer, and optically anisotropic material
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The present invention relates to: a polymerizable compound (I), wherein Y1 to Y6 are a chemical single bond, —O—C(═O)—, —C(═O)—O— or the like, G1 and G2 are a divalent aliphatic group, Z1 and Z2 are an alkenyl group, Ax is a fused ring group represented by a formula (II), wherein X is —NR3—, an oxygen atom, a sulfur atom or the like, R3 is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, and D is a substituted or unsubstituted ring having 1 to 20 carbon atoms that includes at least one nitrogen atom, Ay is a hydrogen atom, an alkyl group, A1 is a trivalent aromatic group or the like, A2 and A3 are a divalent aromatic group having 6 to 30 carbon atoms or the like, and Q1 is a hydrogen atom, or an alkyl group having 1 to 6 carbon atoms.
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Page/Page column 37
(2016/12/26)
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- Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
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Paragraph 0122; 0123
(2018/10/03)
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- 7-HYDROXY-SPIROPIPIPERIDINE INDOLINYL ANTAGONISTS OF P2Y1 RECEPTOR
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The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of Ρ2Y1 receptor and may be used as medicaments in the treatment and/or prophylaxis of thromboembolic disorders.
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Paragraph 00224-00225
(2014/02/16)
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- HETEROCYCLIC PYRIDONE COMPOUND, AND INTERMEDIATE, PREPARATION METHOD AND USE THEREOF
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The present invention relates to a heterocyclic pyridone compound represented by General Formula (I), where the heterocyclic pyridone compound is used as a tyrosine kinase inhibitor, and particularly a c-Met inhibitor. The present invention also relates to intermediates for preparing heterocyclic pyridone compound and a preparation method. The present invention further relates to a pharmaceutical composition containing the heterocyclic pyridone compound as an active ingredient, and a use of the pharmaceutical composition in treatment of diseases associated with tyrosine kinase c-Met, especially cancer associated with c-Met, as a medicament.
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Paragraph 0258; 0259
(2014/08/06)
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- TRI-HETEROCYCLIC DERIVATIVES, PREPARATION PROCESS AND USES THEREOF
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The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
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Paragraph 0123; 0240; 0241
(2014/11/13)
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- TRI-HETEROCYCLIC DERIVATIVES, PREPARATION PROCESS AND USES THEREOF
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The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase
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Page/Page column 30
(2013/07/05)
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- NOVEL COMPOUNDS
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The invention is directed to certain novel compounds. Specifically, the invention directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity.
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Page/Page column 152
(2012/04/04)
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- QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic 7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
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Page/Page column 70-71
(2011/05/11)
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- Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes
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Type 2 diabetes is a polygenic disease which afflicts nearly 200 million people worldwide and is expected to increase to near epidemic levels over the next 10-15 years. Glucokinase (GK) activators are currently under investigation by a number of pharmaceu
- Bebernitz, Gregory R.,Beaulieu, Valerie,Dale, Bethany A.,Deacon, Richard,Duttaroy, Alokesh,Gao, Jiaping,Grondine, Melissa S.,Gupta, Ramesh C.,Kakmak, Mesut,Kavana, Michael,Kirman, Louise C.,Liang, Jinsheng,Maniara, Wieslawa M.,Munshi, Siralee,Nadkarni, Sunil S.,Schuster, Herbert F.,Stams, Travis,St. Denny, Irene,Taslimi, Paul M.,Vash, Brian,Caplan, Shari L.
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experimental part
p. 6142 - 6152
(2010/02/28)
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- QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
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Page/Page column 56-57
(2009/10/31)
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- A single-step preparation of thiazolo[5,4-b]pyridine- and thiazolo[5,4-c]pyridine derivatives from chloronitropyridines and thioamides, or thioureas
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(Chemical Equation Presented) A one-step synthesis of thiazolo[5,4-b] pyridines from an appropriately substituted chloronitropyridine and thioamide, or thiourea, is presented. In particular, the reaction was used to prepare a large number of 6-nitrothiazo
- Sahasrabudhe, Kiran P.,Estiarte, M. Angels,Tan, Darlene,Zipfel, Sheila,Cox, Matthew,O'Mahony, Donogh J. R.,Edwards, William T.,Duncton, Matthew A. J.
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experimental part
p. 1125 - 1131
(2010/03/01)
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- NEW AMINOTHIAZOLES AS FBPASE INHIBITORS FOR DIABETES
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Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.
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- THIAZOLOPYRIDINE DERIVATES, PHARMACEUTICAL CONDITIONS CONTAINING THEM AND METHODS OF TREATING GLUCOKINASE MEDIATED CONDITIONS
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The present invention provides compounds of the formula (I) which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may b
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Page/Page column 28
(2010/02/14)
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- SULFONAMIDE-THIAZOLPYRIDINE DERIVATIVES AS GLUCOKINASE ACTIVATORS USEFUL THE TREATMENT OF TYPE 2 DIABETES
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The present invention provides compounds of the formula (I), which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, Type 2 diabetes and obesity.
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Page/Page column 47
(2010/02/14)
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- SUBSTITUTED (THIAZOL-2-YL) -AMIDE OR SULFONAMIDE AS GLYCOKINASE ACTIVATORS USEFUL IN THE TREATMENT OF TYPE 2 DIABETES
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Compounds of the formula (I) provide pharmacological agents which are glucokinase activators and thus may be employed for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for prevention and treatm
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- Synthesis of analogues of the 2,3,6-triazaphenothiazine ring system
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Treatment of 2,3-dichloroquinoxalines with 2-amino-6-picoline-3-thiol gave a mixture of 2,3-bis(2-amino-6-picolinyl-3-thio)quinoxalines (16, R = H, Cl) and 2,3-bis (N,N-dimethylamino)quinoxalines (15, R = H, Cl) separated by fractional crystallization. A similar reaction of 3-amino-6-methoxypyridine-2(1H)-thione (9) with 4,5-dichloropyridazin-3(2H)-one (21) gave 4-chloro-5-(3-amino-6-methoxypyridyl-2-thio)pyridazin-3(2H)-one (22). Concentrated hydrochloric acid-catalysed cyclization of 22 gave the nonrearranged 7-methoxy-2,3,6-triazaphenothiazin-1(2H)-one. The action of compound 22 in refluxing glacial acetic acid gave, on the other hand, 7-methoxy-2,3,6-triazaphenothiazin-4(3H)-one via a Smiles rearrangement. These cyclized compounds are the first known derivatives of the new 2,3,6-triazaphenothiazine ring system.
- Okafor,Castle
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p. 199 - 203
(2007/10/02)
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