CN102596321B - 可用作dpp-1抑制剂的炔基衍生物 - Google Patents

可用作dpp-1抑制剂的炔基衍生物 Download PDF

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CN102596321B
CN102596321B CN201080049814.4A CN201080049814A CN102596321B CN 102596321 B CN102596321 B CN 102596321B CN 201080049814 A CN201080049814 A CN 201080049814A CN 102596321 B CN102596321 B CN 102596321B
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phenyl
methyl
alkyl
compound
oxyl
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CN102596321A (zh
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M·H·帕克
D·J·赫拉斯塔
黄义方
A·B·雷茨
E·C·劳森
C·舒伯特
E·斯特罗贝尔
B·通格
K·怀特
M·P·温特斯
S·高希
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Janssen Pharmaceutica NV
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    • C07C237/16—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and unsaturated
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CN201080049814.4A 2009-10-29 2010-10-28 可用作dpp-1抑制剂的炔基衍生物 Expired - Fee Related CN102596321B (zh)

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US25617109P 2009-10-29 2009-10-29
US61/256171 2009-10-29
US61/256,171 2009-10-29
PCT/US2010/054445 WO2011059731A1 (en) 2009-10-29 2010-10-28 Alkynyl derivatives useful as dpp-1 inhibitors

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CN102596321A CN102596321A (zh) 2012-07-18
CN102596321B true CN102596321B (zh) 2014-11-19

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US (1) US8633322B2 (https=)
EP (1) EP2493571B1 (https=)
JP (1) JP5815542B2 (https=)
CN (1) CN102596321B (https=)
AU (1) AU2010319927B2 (https=)
ES (1) ES2513291T3 (https=)
WO (1) WO2011059731A1 (https=)

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Publication number Priority date Publication date Assignee Title
WO2012119941A1 (en) 2011-03-04 2012-09-13 Prozymex A/S Peptidyl nitrilcompounds as peptidase inhibitors
EP2825533B1 (en) 2012-03-13 2016-10-19 Basf Se Fungicidal pyrimidine compounds
AR091858A1 (es) 2012-07-25 2015-03-04 Sova Pharmaceuticals Inc INHIBIDORES DE CISTATIONIN-g-LIASA (CSE)
WO2015036059A1 (en) 2013-09-16 2015-03-19 Basf Se Fungicidal pyrimidine compounds
CA2923101A1 (en) 2013-09-16 2015-03-19 Basf Se Fungicidal pyrimidine compounds
CN115996923B (zh) 2020-08-26 2025-07-18 海思科医药集团股份有限公司 一种作为二肽基肽酶1抑制剂的腈衍生物及其用途

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US548021A (en) * 1895-10-15 Wiiitfield potter toomee
US4847241A (en) * 1985-08-14 1989-07-11 G. D. Searle & Co. Fluorenyl substituted tyrosyl dipeptide amides which are useful in treating pain
EP0574545B1 (en) 1991-03-06 1994-11-30 G.D. Searle & Co. Phenyl amidines derivatives useful as platelet aggregation inhibitors
US5424334A (en) 1991-12-19 1995-06-13 G. D. Searle & Co. Peptide mimetic compounds useful as platelet aggregation inhibitors
DE4321502A1 (de) 1993-06-29 1995-01-12 Bayer Ag Alkinol-substituierte Peptide, Verfahren zu ihrer Herstellung und ihre Verwendung als antiretrovirale Mittel
AU6490396A (en) 1995-07-14 1997-02-18 Smithkline Beecham Corporation Substituted-pent-4-ynoic acids
IL123164A (en) 1995-08-30 2001-03-19 Searle & Co Meta-guanidine urea thiourea or azacyclic amino benzoic acid derivatives and pharmaceutical compositions containing them
JP2002145897A (ja) 2000-11-10 2002-05-22 Kyorin Pharmaceut Co Ltd アミノ酸誘導体及びその製造法
CN100522976C (zh) * 2002-05-07 2009-08-05 神经研究公司 氮杂环乙炔基衍生物
HK1079787A1 (zh) * 2002-07-31 2006-04-13 Ranbaxy Laboratories Limited 用作毒蕈碱受体拮抗剂的3，6-二取代的氮杂双环[3．1．0]己烷衍生物
WO2004071448A2 (en) * 2003-02-12 2004-08-26 Transtech Pharma Inc. Substituted azole derivatives as inhibitors of protein tyrosine phosphatases
CA2514363A1 (en) * 2003-02-12 2004-08-26 Transtech Pharma, Inc. Substituted azole derivatives as therapeutic agents
EP1633702B1 (en) * 2003-05-30 2008-07-02 Prozymex A/S Protease inhibitors
US7638513B2 (en) * 2004-06-02 2009-12-29 Schering Corporation Compounds for the treatment of inflammatory disorders
DE102005009784B4 (de) 2005-03-03 2009-06-18 Technische Universität Darmstadt Peptid-Mimetika, Verfahren zur deren Herstellung, diese enthaltende pharmazeutische Zusammensetzung und deren Verwendung als Inhibitoren von Proteasomen und zur Induktion von Apoptose
AU2006230447A1 (en) * 2005-03-30 2006-10-05 Conforma Therapeutics Corporation Alkynyl pyrrolopyrimidines and related analogs as HSP90-inhibitors
US7807699B2 (en) 2006-03-21 2010-10-05 Joyant Pharmaceuticals, Inc. Dimeric pyrrolidine amide-containing small molecule apoptosis promoters
US7678894B2 (en) 2007-05-18 2010-03-16 Helicos Biosciences Corporation Nucleotide analogs
US20090264431A1 (en) 2007-08-20 2009-10-22 Palovich Michael R Novel cathepsin c inhibitors and their use
US7902181B2 (en) 2007-12-12 2011-03-08 Astrazeneca Ab Compounds 010

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