- PIPERIDINYL-3-(ARYLOXY)PROPANAMIDES AND PROPANOATES
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Disclosed are compounds of Formula (1), stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R5, R6,R7, R9, R10, R11, R12, X1, X2, X3, X4, X13, and X14 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (1), to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.
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- 3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00345
(2017/09/27)
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- Design, structure-activity relationship, and highly efficient asymmetric synthesis of 3-phenyl-4-benzylaminopiperidine derivatives as novel neurokinin-1 receptor antagonists
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We synthesized a series of novel 3-phenyl-4-benzylaminopiperidine derivatives that were identified as potent tachykinin NK1 receptor antagonists by structural modification of the 3-benzhydrylpiperidone derivative through high-throughput screening. N-{2-[(3R,4S)-4-({2-Methoxy-5-[5-(trifluoromethyl)- 1Htetrazol-1-yl]benzyl}amino)-3-phenyl-1-piperidinyl]-2-oxoethyl}acetamide ((+)-39) was found to be one of the most potent tachykinin NK1 receptor antagonists with high metabolic stability. Highly efficient asymmetric synthesis of (+)-39 was achieved via dynamic kinetic resolution.
- Shirai, Junya,Yoshikawa, Takeshi,Yamashita, Masayuki,Yamamoto, Yasuharu,Kawamoto, Makiko,Tarui, Naoki,Kamo, Izumi,Hashimoto, Tadatoshi,Ikeura, Yoshinori
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experimental part
p. 6430 - 6446
(2011/12/01)
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- Novel piperidyl derivatives of quinazoline and isoquinoline
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The invention pertains to new piperidyl-substituted quinazoline and isoquinoline derivatives that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds that are selective inhibitors of PDE10. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders.
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Page/Page column 16; 18
(2010/02/15)
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- PIPERIDINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
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The present invention provides a compound represented by the formula: ???wherein Ar is an aryl group, an aralkyl group or an aromatic heterocyclic group, each of which may be substituted, R1 is a hydrogen atom, an optionally substituted hydroca
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Page/Page column 45
(2008/06/13)
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