56326-98-8Relevant academic research and scientific papers
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
Sun, Daqing,Wang, Zhulun,Caille, Seb,Degraffenreid, Michael,Gonzalez-Lopez De Turiso, Felix,Hungate, Randall,Jaen, Juan C.,Jiang, Ben,Julian, Lisa D.,Kelly, Ron,McMinn, Dustin L.,Kaizerman, Jacob,Rew, Yosup,Sudom, Athena,Tu, Hua,Ursu, Stefania,Walker, Nigel,Willcockson, Maren,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
body text, p. 405 - 410 (2011/02/27)
The synthesis and SAR of a series of 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, highly selective, and orally bioavailable inhibitors demonstrating efficacy in both rat and non-human primate ex vivo pharmacodynamic models.
SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES AS RHO KINASE INHIBITORS
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Page/Page column 71, (2010/01/30)
The invention relates to substituted isoquinoline and isoquinolinones of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
CYCLOALKYLAMINE SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES
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Page/Page column 82, (2008/12/06)
The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
DI(HETERO)ARYLCYCLOHEXANE DERIVATIVES, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
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Page/Page column 95, (2009/01/24)
The present invention relates to di(hetero)arylcyclohexane derivatives of the formula (I), in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula (I), their use and pharmaceutical compositions comprising them.
Potent bradykinin B1 receptor antagonists: 4-Substituted phenyl cyclohexanes
Su, Dai-Shi,Lim, John L.,Markowitz, M. Kristine,Wan, Bang-Lin,Murphy, Kathy L.,Reiss, Duane R.,Harrell, C. Meacham,O'Malley, Stacy S.,Ransom, Rick W.,Chang, Raymond S.L.,Pettibone, Douglas J.,Tang, Cuyue,Prueksaritanont, Thomayant,Freidinger, Roger M.,Bock, Mark G.
, p. 3006 - 3009 (2008/02/04)
Selective bradykinin (BK) B1 receptor antagonists have been shown to be antinociceptive in animal models and could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure-activity relationships of the biphenyl moiety of the lead compound 1 provided a potent new structural class of BK B1 receptor antagonists.
Benzamide derivatives and uses related thereto
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Page/Page column 54-55; 63-64, (2008/06/13)
Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.
An efficient and scalable one-pot double Michael addition-Dieckmann condensation for the synthesis of 4,4-disubstituted cyclohexane β-keto esters
DeGraffenreid, Michael R.,Bennett, Sarah,Caille, Sebastien,De Turiso, Felix Gonzalez-Lopez,Hungate, Randall W.,Julian, Lisa D.,Kaizerman, Jacob A.,McMinn, Dustin L.,Rew, Yosup,Sun, Daqing,Yan, Xuelei,Powers, Jay P.
, p. 7455 - 7458 (2008/02/11)
(Chemical Equation Presented) A simple, scalable, and efficient one-pot methodology for the synthesis of 4,4-disubstituted cyclohexane β-keto esters from benzylic nitriles or esters and methyl acrylate promoted by potassium tert-butoxide is described. The process relies on a tandem double Michael addition-Dieckmann condensation reaction, which results in the formation of three discrete carbon-carbon bonds in a single pot, including a quaternary center. The method allows for the convenient and rapid synthesis of a variety of 4-aryl-4-cyano-2-carbomethoxycyclohexanone and 4-aryl-2,4- biscarbomethoxycyclohexanone building blocks for use in natural products synthesis and medicinal chemistry.
Anti-virally active pyridazinamines
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, (2008/06/13)
Anti-virally active pyridazinamines, compositions containing the same and methods of treating viral diseases in warm-blooded animals.
1-(Cyclohexyl)-4-aryl-4-piperidinecarboxylic acid derivatives
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, (2008/06/13)
Novel 1-(cyclohexyl)-4-aryl-4-piperidinecarboxylic acid derivatives, bearing in the 4-position of the cyclohexyl ring a cyano group and an aryl moiety, said compounds displaying useful antihistaminic properties.
