- 1-(3-AMINOPROPYL) SUBSTITUTED CYCLIC AMINE COMPOUNDS, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by formula (I), pharmaceutically acceptable salts, enantiomers, diastereoisomers, racemates and mixtures thereof, and a method of synthesizing said 1-(3-aminopropyl) substituted cyclic amine compounds by using aromatic heterocyclic formaldehyde as raw material. Said compounds can be used as CCR 5 antagonist for the treatment of HIV infection.
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- CHEMOKING RECEPTOR ANTAGONISTS
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Disclosed herein are chemokine receptor antagonists of formula (I) wherein G1, X1, X2, and X3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
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Page/Page column 112; 115
(2013/03/26)
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- Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier
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By employing pharmacophore-based design and the privileged fragments reassembly, a series of piperidine-/tropane-/piperazine-bridged CCR5 antagonists were designed and synthesized via an efficient convergent synthesis strategy, with focus on the optimal choice of the basic center carrier structure. Significantly, the 4-amino-4-methylpiperidine bridged 1-acyl-1,3-propanediamine compounds were identified as a new class of nanomolar CCR5 antagonists, providing an efficient approach and novel scaffolds for further development of potent CCR5 inhibitors.
- Fan, Xing,Zhang, Hu-Shan,Chen, Li,Long, Ya-Qiu
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experimental part
p. 2827 - 2840
(2010/08/22)
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- 1-Amido-1-phenyl-3-piperidinylbutanes - CCR5 antagonists for the treatment of HIV: Part 2
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Optimisation of a series of 4-piperidinyltriazoles led to the identification of compound 28a which showed good whole cell antiviral activity, excellent selectivity over the hERG ion channel and complete oral absorption.
- Barber, Christopher G.,Blakemore, David C.,Chiva, Jean-Yves,Eastwood, Rachel L.,Middleton, Donald S.,Paradowski, Kerry A.
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scheme or table
p. 1499 - 1503
(2009/12/07)
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- Chemical compounds
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Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
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Page/Page column 33
(2008/06/13)
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- TRIAZOLYLPIPERIDINE DERIVATIVES AND USE THEREOF IN THERAPY
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The present invention provides compounds of formula (I) Wherein R1 , R2, R3 , R4 , Het and m are as defined in the description. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors.
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- CHEMICAL COMPOUNDS
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Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
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