CN102822192B - 作为尘螨1型肽酶变应原抑制剂的丙酮酰胺化合物 - Google Patents

作为尘螨1型肽酶变应原抑制剂的丙酮酰胺化合物 Download PDF

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CN102822192B
CN102822192B CN201180014350.8A CN201180014350A CN102822192B CN 102822192 B CN102822192 B CN 102822192B CN 201180014350 A CN201180014350 A CN 201180014350A CN 102822192 B CN102822192 B CN 102822192B
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CN102822192A (zh
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克莱福·鲁滨逊
张集慧
大卫·罗纳德·加罗德
特雷弗·罗伯特·佩里奥尔
加里·卡尔·牛顿
凯丽·詹金斯
丽贝卡·伊丽莎白·比弗斯
梅里埃尔·鲁特·马约尔
马克·理查德·斯图尔特
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University of Manchester
City St George’s, University of London
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University of Manchester
St Georges Hospital Medical School
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Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
GB201001070D0 (en) 2010-01-22 2010-03-10 St George's Hospital Medical School Theraputic compounds and their use
KR20150065885A (ko) * 2012-10-11 2015-06-15 에프. 호프만-라 로슈 아게 케토아마이드 이뮤노프로테아좀 억제제
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US20160331783A1 (en) * 2014-01-13 2016-11-17 The General Hospital Corporation Bisamide compounds as allosteric effectors for reducing the oxygen-binding affinity of hemoglobin
WO2015106240A1 (en) 2014-01-13 2015-07-16 The General Hospital Corporation Heteroaryl disulfide compounds as allosteric effectors for increasing the oxygen-binding affinity of hemoglobin
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US20240317801A1 (en) * 2020-12-17 2024-09-26 Disc Medicine, Inc. Peptidomimetic matriptase 2 inhibitors and uses thereof
US20250064789A1 (en) * 2022-03-01 2025-02-27 Westvac Biopharma Co., Ltd. Ketoamide derivatives and pharmaceutical uses thereof
WO2024028417A1 (en) 2022-08-03 2024-02-08 Institut National de la Santé et de la Recherche Médicale New composition for the treatment and/or prevention of vitiligo

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990005739A1 (en) * 1988-11-15 1990-05-31 Miller Chad G Carboxyl terminal peptide and protein sequencing
US6235929B1 (en) * 1991-12-27 2001-05-22 Georgia Tech Research Corporation Tripeptide α-ketoamides

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3149159A (en) 1962-04-16 1964-09-15 Smith Kline French Lab Substituted 7-aminoalkylbicyclo-[4. 2. 0] octa-1, 3, 5-trienes
EP0100673A2 (en) 1982-08-02 1984-02-15 The Research Foundation Of State University Of New York A method of enhancing neurofiber regrowth
EP0672648B1 (en) 1989-04-15 1998-09-23 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Threo (2R,3S)-3-amino-2-hydroxypentanoic acid and threo (2R,3S)-3-(p-methoxy-benzyloxycarbonyl/FMOC) amino-2-hydroxy-pentanoic acid
DE4331135A1 (de) 1993-09-14 1995-03-16 Bayer Ag Neue antiviral wirksame valinhaltige Pseudopeptide
US5580854A (en) 1994-03-04 1996-12-03 Mount Sinai School Of Medicine Of The City University Of New York Substrate-related peptidyl-aldehyde inhibitors of the proteolytic activity of the multicatalytic proteinase complex
CA2200964A1 (en) 1994-11-24 1996-05-30 Takeda Chemical Industries, Ltd. Alpha-ketoamide derivatives as cathepsin l inhibitor
JPH08208462A (ja) * 1994-11-24 1996-08-13 Takeda Chem Ind Ltd カテプシンｌ阻害剤
CA2215211A1 (en) 1995-03-31 1996-10-03 Takeda Chemical Industries, Ltd. Cysteine protease inhibitor
DE69633623T2 (de) * 1995-07-17 2005-12-01 Medivir Uk Ltd. Cystein-Protease-Inhibitoren für die Behandlung von allergischen Krankheiten verursacht duch IgE
AU728373B2 (en) 1995-12-07 2001-01-11 Scripps Research Institute, The HIV protease inhibitors
AU1599497A (en) 1996-02-16 1997-09-02 Bayer Aktiengesellschaft Oxime- and nitron-substituted pseudopeptides with an anti-viral action
CA2225325A1 (en) 1997-12-19 1999-06-19 The University Of British Columbia Hemiasterlin analogs
PL204619B1 (pl) 1998-03-19 2010-01-29 Vertex Pharma Pochodna peptydowa, kompozycja farmaceutyczna zawierająca taką pochodną i zastosowanie pochodnej peptydowej
US7521068B2 (en) 1998-11-12 2009-04-21 Elan Pharma International Ltd. Dry powder aerosols of nanoparticulate drugs
AU2055301A (en) 1999-12-03 2001-06-12 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
JP2002030053A (ja) * 2000-07-13 2002-01-29 Senju Pharmaceut Co Ltd α−ケトアミド誘導体の製造法
SK742003A3 (en) 2000-07-21 2003-06-03 Schering Corp Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
EP1553964A4 (en) * 2002-09-25 2009-08-12 Georgia Tech Res Inst KETOAMID INHIBITORS IN CHRONIC NERVE DISEASES
JP3858080B2 (ja) 2003-11-12 2006-12-13 株式会社信州Ｔｌｏ アレルゲン分解剤、および抗アレルゲン羽毛
JP2009503027A (ja) 2005-08-03 2009-01-29 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング アルツハイマー病ｉｉの治療のための置換エタン−１，２−ジアミン
WO2007041775A1 (en) 2005-10-10 2007-04-19 The University Of Queensland Cysteine protease inhibitors incorporating azide groups
GB201001070D0 (en) 2010-01-22 2010-03-10 St George's Hospital Medical School Theraputic compounds and their use
GB201011411D0 (en) 2010-07-06 2010-08-18 St Georges Hosp Medical School Therapeutic compounds and their use

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990005739A1 (en) * 1988-11-15 1990-05-31 Miller Chad G Carboxyl terminal peptide and protein sequencing
US6235929B1 (en) * 1991-12-27 2001-05-22 Georgia Tech Research Corporation Tripeptide α-ketoamides

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Hepatitis C NS3 protease inhibition by peptidyl-alpha ketoamide inhibitors:kinetic mechanism and structure;LIU Y et.al;《ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS》;20040115;第421卷(第2期);207-216 *

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