- SUBSTITUTED HYDANTOINAMIDES AS ADAMTS7 ANTAGONISTS
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The application relates to substituted hydantoinamides of formula (I) as ADAMTS7 antagonists, to processes for their preparation, their use alone or in combination for the treatment or prophylaxis of diseases, in particular of cardiovascular diseases, including atherosclerosis, coronary artery disease (CAD), peripheral vascular disease (PAD), arterial occlusive disease or restenosis after angioplasty. R1 is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, heteroaryl or phenyl; R2 is hydrogen, cyano, halogen, alkylsulfonyl, alkyl, cycloalkyl or alkoxy; R3, R4, R5, R6, R7 and R8 are independently hydrogen, halogen, alkyl or alkoxy; most groups being optionally substituted; with the proviso that at least one of R2, R3, R4 is H; X1, X2, X3, X4, X5 and X6 are independently N or C; with the proviso that in each ring maximal one X is N.
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Page/Page column 227
(2021/05/21)
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- Ambient-Temperature Ortho C-H Arylation of Benzoic Acids with Aryl Iodides with Ligand-Supported Palladium Catalyst
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The ambient-temperature ortho C-H arylation of electron-deficient benzoic acids with aryl iodides has been achieved by using an Ac-Ile-OH-supported Pd catalyst. A wide range of unactivated benzoic acids could cross-couple an array of aryl iodides in moderate to excellent yields. The choice of HFIP as a solvent is crucial to realizing the mild C-H arylation, and the beneficial effect of the ligand on the reaction likely stems from the accelerated C-H activation process and the improved catalyst lifetime.
- Zhu, Changlei,Zhang, Yuanfei,Kan, Jian,Zhao, Huaiqing,Su, Weiping
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supporting information
p. 3418 - 3421
(2015/07/28)
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- GUT MICROSOMAL TRIGLYCERIDE TRANSPORT PROTEIN INHIBITORS
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Compounds represented by formula (I): are inhibitors of gut microsomal triglyceride transfer protein. Such compounds are useful in treating diseases or conditions such as diabetes and obesity, along with patients are risk for developing such diseases or conditions.
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Page/Page column 119
(2008/12/08)
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- N-BENZODIOXOLYL, N-BENZODIOXANYL AND N-BENZODIOXEPINYL ARYLCARBONXAMIDE DERIVATIVES, AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
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The present invention relates to a compound of the formula (I) : in which T, A, R, B Xi, Yi and n are as defined in Claim 1, and to the pharmaceutically usable derivatives, solvates and stereoisomers thereof, comprising a mixture thereof in all proportions, which can be used in the treatment of dyslipidaemia, and to pharmaceutical compositions comprising them.
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- Nonpeptide arginine vasopressin antagonists for both V(1A) and V2 receptors: Synthesis and pharmacological properties of 2-Phenyl-4'- [(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide derivatives
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A series of compounds structurally related to 4'-[(2,3,4,5-tetrahydro- 1H-1-benzazepin-1-yl)carbonyl]benzanilide was synthesized and demonstrated to have arginine vasopressin (AVP) antagonist activity for both V(1A) and V2 receptors. The introduction of a phenyl or a 4-substituted phenyl group into the ortho position of the benzoyl moiety resulted in an increase in both binding affinity and antagonistic activity. The 2-(4-methylphenyl) derivative (1g) exhibited high antagonistic activities for both V(1A) (8.6- fold) and V2 (38-fold) receptors and high oral activity (8.6-fold) compared with the 2-methyl lead compound (1a). Detail of the synthesis and the pharmacological properties of this series are presented.
- Matsuhisa, Akira,Tanaka, Akihiro,Kikuchi, Kazumi,Shimada, Yoshiaki,Yatsu, Takeyuki,Yanagisawa, Isao
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p. 1870 - 1874
(2007/10/03)
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- Biaryl aldehyde
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This invention relates to a method of synthesis of certain substituted carboxylic acids useful in lowering serum triglyceride and total cholesterol levels in mammals (including man) represented by the general formula I: wherein Ar1 is selected from STR1 Ar2 is selected from STR2 and R is selected from C1-5 alkyl, halogen, perhalo-C1-4 alkyl, C1-4 alkoxy, phenyl, C1-4 acyl, C1-6 alkoxycarbonyl, amino or hydroxy.
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