- Synthesis, characterization, and biological assessment of the four stereoisomers of the H3 receptor antagonist 5-fluoro-2-methyl-N-[2- methyl-4-(2-methyl[1,3′]bipyrrolidinyl-1′-yl)phenyl]benzamide
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This Letter describes the asymmetric synthesis of the four stereoisomers (8a-8d) of a potent and highly selective histamine H3 receptor (H3R) antagonist, 5-fluoro-2-methyl-N-[2-methyl-4-(2-methyl[1, 3′]bipyrrolidinyl-1′-yl) phenyl]be
- Gao, Zhongli,Hurst, William J.,Guillot, Etienne,Nagorny, Raisa,Pruniaux, Marie-Pierre,Hendrix, James A.,George, Pascal G.
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p. 4044 - 4047
(2013/07/25)
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- SUBSTITUTED N-HETEROARYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula ( Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described her
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Page/Page column 38-39
(2011/12/02)
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- SUBSTITUTED N-PHENYL SPIROLACTAM BIPYRROLIDINES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-phenyl spirolactam bipyrrolidines of formula (I). (Formula (I)) Wherein R1, R2, R3, R4, m, n, p and s are as described herein. More specifical
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Page/Page column 32
(2011/12/02)
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- SUBSTITUTED N-HETEROCYCLOALKYL BIPYRROLIDINYLPHENYL AMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N- heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). (Formula (I)) Wherein R, R1, R2, R3, R4, X, m, n and p are as describ
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Page/Page column 23
(2011/12/02)
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- SUBSTITUTED N-HETEROARYL BIPYRROLIDINE CARBOXAMIDES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). Wherein R1 R2, R3, R4, Q1, Q2, Q3, Q4, X, m
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Page/Page column 26-27
(2011/12/02)
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- SUBSTITUTED N-HETEROARYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of Formula (I). Wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this in
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Page/Page column 22
(2011/12/02)
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- SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). Wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of t
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Page/Page column 25
(2011/12/02)
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- SUBSTITUTED TETRAHYDROPYRAN SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I) Wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
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Page/Page column 38
(2010/06/20)
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- SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONES USED AS H3 MODULATORS
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The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I), wherein R1, R2, R3, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptor
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Page/Page column 32-33
(2010/06/20)
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- SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I), Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of th
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Page/Page column 35-36
(2009/05/28)
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- SUBSTITUTED N-PHENYL-BIPYRROLIDINE UREAS AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine ureas of formula (I) as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceuti
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Page/Page column 29-30
(2009/05/28)
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- SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF
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The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I) as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as phar
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Page/Page column 31
(2009/05/28)
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