- NOVEL COMPOUND, ORGANIC CATION TRANSPORTER 3 DETECTION AGENT, AND ORGANIC CATION TRANSPORTER 3 ACTIVITY INHIBITOR
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[Problem] The present invention addresses the problem of providing a novel compound. The present invention also addresses the problem of providing an OCT3 detection agent or an OCT3 activity inhibitor, which comprises the novel compound. [Solution] A compound represented by formula (A), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. ????????R1-R2-R3-R4?????(A)
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Paragraph 0831-0832; 0834
(2016/08/17)
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- Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350)
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The HIV protease inhibitor (PI) ritonavir (RTV) has been widely used as a pharmacoenhancer for other PIs, which are substrates of cytochrome P450 3A (CYP3A). However the potent anti-HIV activity of ritonavir may limit its use as a pharmacoenhancer with other classes of anti-HIV agents. Ritonavir is also associated with limitations such as poor physicochemical properties. To address these issues a series of compounds with replacements at the P2 and/or P3 region was designed and evaluated as novel CYP3A inhibitors. Through these efforts, a potent and selective inhibitor of CYP3A, GS-9350 (cobicistat) with improved physiochemical properties was discovered.
- Xu, Lianhong,Liu, Hongtao,Hong, Allen,Vivian, Randy,Murray, Bernard P.,Callebaut, Christian,Choi, You-Chul,Lee, Melody S.,Chau, Jennifer,Tsai, Luong K.,Stray, Kirsten M.,Strickley, Robert G.,Wang, Jianhong,Tong, Leah,Swaminathan, Swami,Rhodes, Gerry R.,Desai, Manoj C.
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p. 995 - 999
(2014/02/14)
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- QUINAZOLINE DERIVATIVES AS ANTICANCER AGENTS
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A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blood
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Page/Page column 74
(2008/06/13)
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- TETRAHYDROCARBAZOLE DERIVATIVES USEFUL AS ANDROGEN RECEPTOR MODULATORS
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The present invention provides a compound of the formula: Formula I or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or ex
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Page/Page column 137-138
(2010/11/25)
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- C (2) -HETEROARYLMETHYL-C (4) -METHOXYMETHYL ACYL PYRROLIDINE COMPOUNDS AND THEIR USE FOR TREATING VIRAL INFECTIONS, ESPECIALLY HEPATITIS C VIRUS
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Anti-viral agents of Formula (Ia): wherein A represents hydroxyl; D represents 4-tert-butyl-3-ethenylphenyl or 4-tert-butyl-5-ethenyl-2-fluorophenyl; E represents 1,3-thiazol-2-yl; G represents methoxymethyl; J represents 1,3-thiazol-4-ylmethyl or 1H-pyra
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Page/Page column 23
(2010/11/26)
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- C (2) -HETEROARYLMETHYL-C (4) -PYRAZIN-2-YL ACYL PYRROLIDINE COMPOUNDS AND THEIR USER FOR TREATING VIRAL INFECTIONS, ESPECIALLY HEPATITICS C (HCV)
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Anti-viral agents of Formula (Ia) : wherein A represents hydroxy; B represents -C(O)R3; D represents 1,3-thiazol-2-yl; E represents pyrazin-2-yl; G represents 1,3-thiazol-4-ylmethyl or 1H-pyrazol-1-ylmethyl; R3 represents 4-tert-buty
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Page/Page column 21
(2010/11/26)
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- PYRROLIDINE DERIVATIVES FOR TREATING VIRAL INFECTIONS
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Anti-viral agents of Formula (Ia): wherein A represents hydroxy; D represents 3-bromo-4-tert-butylphenyl or 5-bromo-4-tert-butyl-2-fluorophenyl; E represents 1,3-thiazol-2-yl or 5-methylisoxazol-3-yl; G represents methoxymethyl; J represents 1,3-thiazol-4
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Page/Page column 20
(2010/11/26)
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- C (2) -HETEROARYLMETHYL-C (4) -PYRAZINYL-2-YL ACYL PYRROLIDINE COMPOUNDS AND THEIR USE FOR TREATING VIRAL INFECTIONS, ESPECIALLY HEPATITIS C VIRUS
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Anti-viral agents of Formula (Ia) : wherein A represents hydroxy; B represents -C(O)R3; D represents 1,3-thiazol-2-yl or 5-methylisoxazol-3-yl; E represents pyrazin-2-yl; G represents 1,3-thiazol-4-ylmethyl or 1H-pyrazol-1-ylmethyl; R3 /s
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Page/Page column 17-18
(2010/11/26)
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- DERIVATIVES OF THIOPHENE CARBOXILIC ACID AS ANTIVIRAL AGENT
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Anti-viral agents of compounds of Formuta (I) : wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.
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Page/Page column 32-33
(2010/11/28)
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- 4- (PYRAZINE-2-YL) -PYRROLIDINE-2-CARBOXYLIC ACID COMPOUNDS AND DERIVATIVES THEREOF AS HEPATITIS C VIRUS INHIBITORS
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Anti-viral agents of Formula (Ia) wherein: A represents hydroxy; B represents C(O)R3 wherein R3 is 4-tert-butyl-3-methoxyphenyl; D represents 1,3-thiazol-2-yl or 5-methyl-1,3-thiazol-2-yl; E represents pyrazin-2-yl; G represents 1,3-
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Page/Page column 19
(2008/06/13)
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- 4-METHOXYMETHYL-PYRROLIDINE-2-CARBOXYLIC ACID COMPOUNDS AND DERIVATIVES THEREOF AS HEPATITIS C VIRUS INHIBITORS
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Anti-viral agents of Formula (la) wherein: A represents hydroxy; D represents 4-tert-butyl-3-methoxyphenyl; E represents 1,3--thiazol-2-yl or 5-methyl-1,3-thiazol-2-yl; G represents methoxymethyl; J represents 1,3- thiazol-2-ylmethyl, 1,3-thiazol-4-ylmeth
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Page/Page column 19
(2010/11/08)
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- ACYL DIHYDRO PYRROLE DERIVATIVES AS HCV INHIBITORS
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Novel anti-viral agents of Formula (I) in which: A represents hydroxy; D represents aryl or heteroaryl; E represents hydrogen, C1-6alkyl, aryl, heteroaryl or heterocyclyl; G represents hydrogen or C1-6alkyl optionally substituted by
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Page/Page column 23
(2010/02/14)
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- Enantioselective synthesis of (S)-3-(4-thiazolyl)-2-tert- butoxycarbonylaminopropionic acid: A chiral building block for renin inhibitor
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(S)-3-(4-Thiazolyl)-2-tert-butoxycarbonylaminopropionic acid (6), an important structural constituent of the renin inhibitor, has been synthesized from (Z)-3-(4-thiazolyl)-2-benzoylaminoprop-2-enoic acid (4b) by enantioselective hydrogenation using the Ru
- Yuasa, Yoshifumi,Tsuruta, Haruki,Yuasa, Yoko
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p. 2385 - 2392
(2007/10/03)
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- Substituted phenyl compounds for the treatment of non-insulin dependent diabetes mellitus
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This invention provides compounds of formula I, having the structure 1wherein R1, R2, R3, R4, A, and B are as defined in the specification, or a pharmaceutically acceptable salt thereof, that are useful in treating metabolic disorders mediated by insulin resistance or hyperglycemia.
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- Triazolylated teritiary amine compound or salt thereof
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A triazolylated tertiary amine compound represented by general formula (I) or a salt thereof, having an aromatase inhibitory activity and being useful for preventing and treating breast cancer, mastopathy, endometriosis, prostatomergaly, etc., wherein A represents a single bond, lower alkylene or carbonyl; B represents lower alkyl, aryl, a 5- or 6-membered heterocyclic group, or a bicyclic fused heterocyclic group; D represents aryl, a 5- or 6-membered heterocyclic group, or a bicyclic fused heterocyclic group; and E represents 4H-1,2,4-triazolyl, 1H-1,2,4-triazolyl or 1H-1,2,3-triazolyl.
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- RETROVIRAL PROTEASE INHIBITING PIPERAZINE COMPOUNDS
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Retroviral protease inhibiting compounds of the formula: STR1 are disclosed.
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- 2-Alkoxy(and 2-alkoxyalkyl)-2-heterocyclic-thioacetamides for inhibiting gastric acid secretion
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The compounds are 2-alkoxy(and 2-alkoxyalkyl)-2-heterocyclic-thioacetamides which are inhibitors of gastric acid secretion.
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- 2-Alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides
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The compounds are 2-alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides, for example 2-methoxy-N-methyl-3-morpholino-2-(2-pyridyl)thiopropanamide, which are inhibitors of gastric acid secretion.
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- PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
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The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
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