- DIHYDROISOQUINOLINE-2(1H)-CARBOXAMIDE AND RELATED COMPOUNDS AND THEIR USE IN TREATING MEDICAL CONDITIONS
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The invention provides dihydroisoquinoline-2(1H)-carboxamide and related compounds, pharmaceutical compositions, and their use in the treatment of medical conditions, such as cancer, and in inhibiting HPK1 activity.
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Paragraph 000573
(2019/11/04)
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- Dihydropyrazole GPR40 modulators
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The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
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Page/Page column 59
(2015/10/05)
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- PYRROLIDINE GPR40 MODULATORS
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The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
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Paragraph 00275
(2014/06/11)
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- 3,4′-Linked bis(piperidines) related to the haliclonacyclamine class of marine alkaloids: Synthesis using crossed-aldol chemistry and preliminary biological evaluations
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Compounds 2-5, incorporating various elements of the 3,4′- bis(piperidine) core associated with the sponge-derived alkaloid haliclonacyclamine A (HA, 1), have been prepared through, inter alia, aldol-type reactions of N-substituted piperidin-4-ones and certain derivatives. Screening of these compounds in various assays, including an ecological one, reveals that compound 5 exhibits allelochemical properties similar to those associated with HA itself.
- Banwell, Martin G.,Coster, Mark J.,Hungerford, Natasha L.,Garson, Mary J.,Su, Stephen,Kotze, Andrew C.,Munro, Murray H. G.
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experimental part
p. 154 - 161
(2012/01/17)
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- 2′ Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling
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Further optimization of the biaryl amide series via extensively exploring structure-activity relationships resulted in potent and subtype selective M 1 agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration. Synthesis, structure-activity relationships, subtype selectivity for M1 over M2-5, and DMPK properties of these novel compounds are described.
- Budzik, Brian,Garzya, Vincenzo,Shi, Dongchuan,Walker, Graham,Lauchart, Yann,Lucas, Adam J.,Rivero, Ralph A.,Langmead, Christopher J.,Watson, Jeannette,Wu, Zining,Forbes, Ian T.,Jin, Jian
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supporting information; scheme or table
p. 3545 - 3549
(2010/08/22)
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- SEROTONERGIC BENZOTHIOPHENES
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The present invention provides serotonergic benzothiophenes of Formula (I), where A, R, R, R, R, and R are as described in the specification.
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- CCR8 INHIBITORS
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Disclosed is an inhibitor of CCR8 that is represented by Structural Formula (I). Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a CCR8 inhibitor represented by Structural Formula (I). Also disclosed is a method of treating inflammatory disorders in a subject by administering a CCR8 inhibitor to the subject.
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- CCR8 INHIBITORS
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Disclosed are CCR8 inhibitors represented by Structural Formulas (I). The variables in Structural Formula (I) are described herein. Also disclosed are methods of treating a subject with a CCR8 mediated condition, especially asthma, by administering one of the disclosed CCR8 inhibitors to the subject.
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- SEROTONERGIC BENZOFURANS
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The present invention provides serotonergic benzofurans of Formula (I): where A, R, R, R, R, and R are as described in the specification.
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Page/Page column 24-25
(2010/02/04)
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- A STEREOSELECTIVE SYNTHESIS OF CIS-4-ACETONYL-1-BENZYL-3-ETHYLPIPERIDINE
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The title compound cis-1, a potential synthon for indole alkaloid synthesis, is prepared for the first time. The synthesis starts with the condensation of 3-ethyl-4-piperidone 2 with triethyl phosphonoacetate followed by stereoselective hydrogenation of t
- Bonjoch, Josep,Linares, Ana,Guardia, Manel,Bosch, Joan
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p. 2165 - 2174
(2007/10/02)
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