534572-17-3Relevant academic research and scientific papers
piperidine-3,5-dicarboxamide derivatives and pharmaceutical composition for anti cancer containing the same as an active ingredient
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, (2021/03/25)
The present invention relates to a piperidine-3,5-dicarboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for preventing or treating cancer containing the same as an active ingredient. The compound according to the present invention exhibits an excellent effect of inhibiting anaplastic lymphoma kinase (ALK), and as a result, can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins, such as EML4-ALK and NPM-ALK. In addition, the compound can be useful for a pharmaceutical composition for preventing or treating the cancer since it is expected to effectively prevent recurrence of cancer.
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct renin inhibitors
Ehara, Takeru,Irie, Osamu,Kosaka, Takatoshi,Kanazawa, Takanori,Breitenstein, Werner,Grosche, Philipp,Ostermann, Nils,Suzuki, Masaki,Kawakami, Shimpei,Konishi, Kazuhide,Hitomi, Yuko,Toyao, Atsushi,Gunji, Hiroki,Cumin, Frederic,Schiering, Nikolaus,Wagner, Trixie,Rigel, Dean F.,Webb, Randy L.,Maibaum, Jurgen,Yokokawa, Fumiaki
, p. 787 - 792 (2014/08/05)
A cis-configured 3,5-disubstituted piperidine direct renin inhibitor, (syn,rac)-1, was discovered as a high-throughput screening hit from a target-family tailored library. Optimization of both the prime and the nonprime site residues flanking the central piperidine transition-state surrogate resulted in analogues with improved potency and pharmacokinetic (PK) properties, culminating in the identification of the 4-hydroxy-3,5-substituted piperidine 31. This compound showed high in vitro potency toward human renin with excellent off-target selectivity, 60% oral bioavailability in rat, and dose-dependent blood pressure lowering effects in the double-transgenic rat model.
Heterocyclic compound and use thereof
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Page/Page column 49, (2010/06/16)
Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
AMIDE COMPOUNDS AND USE OF THE SAME
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Page/Page column 136, (2012/02/06)
A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like
ORGANIC COMPOUNDS
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Page/Page column 18, (2009/01/24)
The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.
3 -M0N0- AND 3 , 5-DISUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS
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Page/Page column 134; 135-136, (2010/11/24)
The invention relates to 3,5-piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5- piperidine compound, and/or a method of treatment comprising administering a 3,5- piperidine compound, a method for the manufacture of a 3,5-piperidine compound, and novel intermediates and partial steps for their synthesis. Especially, the 3,5-piperidine compounds have the formula I, wherein the symbols have the meanings described in the specification.
An efficient synthesis of 3(S)-aminopiperidine-5(R)-carboxylic acid as a cyclic β,γ′-diamino acid
Park, Jin-Seong,Yeom, Chang-Eun,Choi, Soo Hyuk,Ahn, Yong Shik,Ro, Sunggu,Jeon, Young Ho,Shin, Dong-Kyu,Kim, B. Moon
, p. 1611 - 1614 (2007/10/03)
An orthogonally protected β,γ′-diamino acid 6 possessing conformationally-constrained ring system was synthesized as a novel cyclic amino acid analogue. This synthesis involves as key steps chemoselective enzymatic hydrolysis of cis-piperidine-3,5-dicarboxylic ester derivative followed by efficient kinetic resolution of the partially resolved half-acid to afford the C1-symmetric piperidine-3,5-dicarboxylic acid monoester in high enantiomeric excess (>98% ee). The optically active half-acid was transformed to the cyclic amino acid via Curtius-type rearrangement.
