- PYRROLIDINE OR THIAZOLIDINE CARBOXYLIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERSAS AS AGONISTS OF G- PROTEIN COUPLED RECEPTOR 43 (GPR43)
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The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.
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Page/Page column 204
(2011/07/07)
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- Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists
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This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2).
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Page/Page column 33
(2010/11/25)
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- Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs
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Anthranilamides 4 and 5 were designed and synthesized as selective and orally bioavailable factor Xa inhibitors. Structural modifications aimed at lowering their lipophilicity were performed at the central phenyl ring and at the S4 binding biphenyl region by incorporating water solublizing substituents. The resulting compounds (e.g., 7, 8, 14, 30a, and 32b) are highly potent in vitro, and show improved activity in human plasma-based thrombin generation assay.
- Zhang, Penglie,Bao, Liang,Zuckett, Jingmei F.,Goldman, Erick A.,Jia, Zhaozhong J.,Arfsten, Ann,Edwards, Susan,Sinha, Uma,Hutchaleelaha, Athiwat,Park, Gary,Lambing, Joseph L.,Hollenbach, Stanley J.,Scarborough, Robert M.,Zhu, Bing-Yan
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p. 983 - 987
(2007/10/03)
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- PIPERAZINE AND HOMOPIPERAZINE COMPOUNDS
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Compounds are provided having a piperazine or homopiperazine ring which are useful in the treatment of thrombosis.
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- Factor xa inhibitors with aryl-amidines and derivatives, and prodrugs thereof
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The present invention relates to a compound with aryl-amidines, particularly amidinoaryl-cyclopropanes, amidinoarylmethyl-pyrroles, amidinoaryl-benzenes, amidinoaryl-pyridines, or amindonoaryl-alanines, represented by formula (1), a pharmaceutically acceptable salt, a prodrug, a hydrate, a solvate or an isomer thereof, which are inhibitors of coagulation enzyme, factor Xa (FXa). The present invention also relates to a pharmaceutical composition containing the compound, and a method of using the same as an anticoagulant agent for treatment and prevention of thrombosis disorders.
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- The Effects of Substituents on the Rate of Saponification of Biphenyl-4-carboxylates
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Second-order rate constants have been measured for the saponification of methyl 2'-, 3'-, and 4'-substituted biphenyl-4-carboxylates at several temperatures in 85percent (w/w) methanol-water and activation parameters have been calculated.The Hammett equation applies very well to the saponification of 3'- and 4'-substituted biphenyl-4-carboxylates with ?-constants evaluated by the FMMF method.The effect of 2'-substituents is understandable in terms of ?-electron steric effects.
- Ananthakrishnanadar, Ponnambalanad.,Kannan, Nagarathnam
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