312924-69-9Relevant academic research and scientific papers
1-(3-AMINOPROPYL) SUBSTITUTED CYCLIC AMINE COMPOUNDS, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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, (2017/04/11)
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.
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists
Sasmal, Sanjita,Balaji, Gade,Kanna Reddy, Hariprasada R.,Balasubrahmanyam,Srinivas, Gujjary,Kyasa, Shivakumar,Sasmal, Pradip K.,Khanna, Ish,Talwar, Rashmi,Suresh,Jadhav, Vikram P.,Muzeeb, Syed,Shashikumar, Dhanya,Harinder Reddy,Sebastian,Frimurer, Thomas M.,Rist, ?ystein,Elster, Lisbeth,H?gberg, Thomas
scheme or table, p. 3157 - 3162 (2012/06/04)
Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays a role in metabolic and CNS disorders. The modeling-supported design, synthesis and multi-parameter optimization (biological activity, solubility, metabolic stability, hERG) of novel quinazoline derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified. Clusters of refined hMCHR1 homology models derived from the X-ray structure of the β2-adrenergic receptor, including extracellular loops, were developed and used to guide the design.
Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier
Fan, Xing,Zhang, Hu-Shan,Chen, Li,Long, Ya-Qiu
experimental part, p. 2827 - 2840 (2010/08/22)
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.
1-Amido-1-phenyl-3-piperidinylbutanes - CCR5 antagonists for the treatment of HIV: Part 2
Barber, Christopher G.,Blakemore, David C.,Chiva, Jean-Yves,Eastwood, Rachel L.,Middleton, Donald S.,Paradowski, Kerry A.
scheme or table, p. 1499 - 1503 (2009/12/07)
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.
CHEMICAL COMPOUNDS
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Page/Page column 24-25, (2009/09/05)
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
Chemical Compound
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Page/Page column 10, (2008/12/06)
The present invention relates to 4-{(1R,3R)-1-(3,5-difluorophenyl)-3-[4-(3-ethyl-5-isopropyl-4H-1,2,4-triazol-4-yl)piperidin-1-yl]butyl}-1-(methylsulfonyl)piperidine (I): or a pharmaceutically acceptable salt thereof, as well as to processes for preparing
TRIAZOLYLPIPERIDINE DERIVATIVES AND USE THEREOF IN THERAPY
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Page/Page column 28, (2010/11/25)
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.
