143165-32-6Relevant articles and documents
4-SUBSTITUTED-CYCLOHEXYLAMINO-4-PIPERIDINYL-ACETAMIDE ANTAGONISTS OF CCR2
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Page/Page column 33, (2012/06/16)
The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
The discovery of novel cyclohexylamide CCR2 antagonists
Lanter, James C.,Markotan, Thomas P.,Zhang, Xuqing,Subasinghe, Nalin,Kang, Fu-An,Hou, Cuifen,Singer, Monica,Opas, Evan,McKenney, Sandra,Crysler, Carl,Johnson, Dana,Molloy, Christopher J.,Sui, Zhihua
scheme or table, p. 7496 - 7501 (2012/02/13)
As a result of further SAR studies on a piperidinyl piperidine scaffold, we report the discovery of compound 44, a potent, orally bioavailable CCR2 antagonist. While having some in vitro hERG activity, this molecule was clean in an in vivo model of QT pro
6-BENZYL-2,3,4,7-TETRAHYDRO-INDOLO[2,3-C]QUINOLINE COMPOUNDS
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Page/Page column 88-89, (2010/04/03)
The present invention pertains to 6-benzyl-2,3,4,7-tetrahydro-indolo[2,3-c]quinoline compounds of formula (I), as well as the resulting pharmaceutical compositions, and their use in the treatment or prophylaxis of diseases alleviated by inhibition of type 5 phosphodiesterases. Furthermore, the present invention pertains to the methods of manufacturing these 6-benzyl-2,3,4,7-tetrahydro-indolo[2,3-c]quinoline compounds.
Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives
Zhou, Dahui,Zhou, Ping,Evrard, Deborah A.,Meagher, Kristin,Webb, Michael,Harrison, Boyd L.,Huryn, Donna M.,Golembieski, Jeannette,Hornby, Geoffrey A.,Schechter, Lee E.,Smith, Deborah L.,Andree, Terrance H.,Mewshaw, Richard E.
, p. 6707 - 6723 (2008/12/21)
Based on the previously reported discovery lead, 3-(cis-4-(4-(1H-indol-4-yl)piperazin-1-yl)cyclohexyl)-5-fluoro-1H-indole (2), a series of related arylpiperazin-4-yl-cyclohexyl indole analogs were synthesized then evaluated as 5-HT transporter inhibitors
ARYLPIPERAZINYL-CYCLOHEXYL INDOLE DERIVATIVES FOR THE TREATMENT OF DEPRESSION
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Page 27, (2010/02/07)
Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise (I) wherein: Ra, R1, R2 and R3 are each, independently, hydrogen, or a substituent selected from halogen, CF3, alkyl, alkoxy, MeSO2, amino or aminocarbonyl (each optionally substituted by one or two groups selected from alkyl and benzyl) carboxy, or alkoxycarbonyl; or two adjacent of Ra and R1-4 together can form a 5-7 membered carbocyclic or heterocyclic ring which is optionally substituted by a substituent defined above; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, arylalkyl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, alkoxy or benzyloxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is CH or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.
α1b-adrenergic receptor antagonists
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Page/Page column 78, (2010/11/30)
There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1is hydrogen etc., B is bond, or B—N—R1forms a ring structure and is piperidine etc., n is 0, 1, etc., A is trimethylene, butylene, etc., Q is piperidine, isoindoline, etc.], or pharmacologically acceptable acid addition salts thereof, and α1B adrenoceptor antagonists composed of these substances. The invented compounds are antagonists having high affinity for α1B adrenoceptor and are useful as pharmaceutical agents for use in prophylaxis/therapy of diseases (e.g., hypertension) in which α1B adrenoceptor is involved or as pharmacological tools for elucidation of physiological activities mediated by α1B adrenoceptor.
Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors
Meagher, Kristin L,Mewshaw, Richard E,Evrard, Deborah A,Zhou, Ping,Smith, Deborah L,Scerni, Rosemary,Spangler, Taylor,Abulhawa, Susan,Shi, Xiaojie,Schechter, Lee E,Andree, Terrance H
, p. 1885 - 1888 (2007/10/03)
A series of indolylcyclohexylamines possessing potent and selective serotonin reuptake inhibition is reported. The most interesting compounds proved to have subnanomolar 5-HT transporter activity, and exhibited moderate 5-HT1A affinity.
3-[[(4-aryl-1-piperazinyl)alkyl]cyclohexyl]-1H-indoles as dopamine D2 partial agonists and autoreceptor agonists
Wustrow, David J.,Smith III, William J.,Corbin, Ann E.,Davis, M. Duff,Georgic, Lynn M.,Pugsley, Thomas A.,Whetzel, Steven Z.,Heffner, Thomas G.,Wise, Lawrence D.
, p. 250 - 259 (2007/10/03)
A series of arylpiperazines and tetrahydropyridines joined to indoles by semirigid cycloalkyl spacers were prepared. Target compounds were studied for their ability to bind to the DA D2 receptor in vitro and to inhibit dopamine synthesis and spontaneous l
SUBSTITUTED INDOLES AS CENTRAL NERVOUS SYSTEM AGENTS
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, (2008/06/13)
Substituted indoles and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and
