HK1038561A1 - 用作类胰蛋白酶抑制剂的肽基杂环酮类化合物 - Google Patents

用作类胰蛋白酶抑制剂的肽基杂环酮类化合物 Download PDF

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Publication number
HK1038561A1
HK1038561A1 HK02100110.3A HK02100110A HK1038561A1 HK 1038561 A1 HK1038561 A1 HK 1038561A1 HK 02100110 A HK02100110 A HK 02100110A HK 1038561 A1 HK1038561 A1 HK 1038561A1
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HK
Hong Kong
Prior art keywords
heterocyclic ketones
tryptase inhibitors
peptidyl
ketones useful
prevention
Prior art date
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HK02100110.3A
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English (en)
Chinese (zh)
Inventor
J. Costanzo Michael
E. Maryanoff Bruce
C. Yabut Stephen
Original Assignee
Ortho-Mcneil Pharmaceutical, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ortho-Mcneil Pharmaceutical, Inc. filed Critical Ortho-Mcneil Pharmaceutical, Inc.
Publication of HK1038561A1 publication Critical patent/HK1038561A1/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
HK02100110.3A 1999-01-27 2000-01-13 用作类胰蛋白酶抑制剂的肽基杂环酮类化合物 HK1038561A1 (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11760299P 1999-01-27 1999-01-27
US60/117,602 1999-01-27
PCT/US2000/000883 WO2000044733A1 (en) 1999-01-27 2000-01-13 Peptidyl heterocyclic ketones useful as tryptase inhibitors

Publications (1)

Publication Number Publication Date
HK1038561A1 true HK1038561A1 (zh) 2002-03-22

Family

ID=22373811

Family Applications (1)

Application Number Title Priority Date Filing Date
HK02100110.3A HK1038561A1 (zh) 1999-01-27 2000-01-13 用作类胰蛋白酶抑制剂的肽基杂环酮类化合物

Country Status (24)

Country Link
US (2) US6469036B1 (https=)
EP (1) EP1147097A1 (https=)
JP (1) JP2002535394A (https=)
KR (1) KR20010110422A (https=)
CN (1) CN1353701A (https=)
AR (1) AR022427A1 (https=)
AU (1) AU3208500A (https=)
BG (1) BG105762A (https=)
BR (1) BR0007778A (https=)
CA (1) CA2361479A1 (https=)
CZ (1) CZ20012722A3 (https=)
EA (1) EA200100815A1 (https=)
EE (1) EE200100391A (https=)
HK (1) HK1038561A1 (https=)
HR (1) HRP20010601A2 (https=)
HU (1) HUP0201295A3 (https=)
IL (1) IL144577A0 (https=)
NO (1) NO20013666L (https=)
SK (1) SK10742001A3 (https=)
TR (1) TR200102766T2 (https=)
TW (1) TWI229669B (https=)
WO (1) WO2000044733A1 (https=)
YU (1) YU61401A (https=)
ZA (1) ZA200106995B (https=)

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DK1268419T3 (da) * 2000-03-27 2006-10-02 Applied Research Systems Farmaceutisk aktive pyrrolidinderivater som BAX-inhibitorer
US6960597B2 (en) * 2000-06-30 2005-11-01 Orth-Mcneil Pharmaceutical, Inc. Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
US6589978B2 (en) * 2000-06-30 2003-07-08 Hoffman-La Roche Inc. 1-sulfonyl pyrrolidine derivatives
US6797461B2 (en) * 2000-10-27 2004-09-28 Promega Corporation Tryptase substrates and assay for tryptase activity using same
CA2433713A1 (en) * 2001-01-05 2002-07-18 Kyowa Hakko Kogyo Co., Ltd. Preventives for arthritis
JP2004518688A (ja) 2001-01-30 2004-06-24 ブリストル−マイヤーズ　スクイブ　カンパニー ファクターＸａ阻害剤のスルホンアミドラクタムおよびその方法
GB0103765D0 (en) * 2001-02-15 2001-04-04 Affitech As Assay
EP1455765A2 (en) * 2001-12-13 2004-09-15 Kowa Company Ltd. Use of protease-activated receptor-2 inhibitor in the manufacture of a medicament for treating delayed hypersensitivity
WO2003101381A2 (en) * 2002-05-29 2003-12-11 Merck & Co., Inc. 1,2 diamido cycloalkyl sodium channel blockers
DE10249304B4 (de) * 2002-10-22 2006-09-28 Cytec Surface Specialties Germany Gmbh & Co. Kg Wäßrige Beschichtungsmittel
US7205384B2 (en) 2003-08-05 2007-04-17 Ortho-Mcneil Pharmaceutical Inc. Process for preparing peptidyl heterocyclic ketone derivatives
US20050176755A1 (en) * 2003-10-31 2005-08-11 Dyatkin Alexey B. Aza-bridged-bicyclic amino acid derivatives as alpha4 integrin antagonists
ATE371649T1 (de) * 2004-02-10 2007-09-15 Janssen Pharmaceutica Nv Pyridazinonharnstoffe als antagonisten von a4- integrinen
JP2008510726A (ja) * 2004-08-20 2008-04-10 エントレメッド インコーポレイテッド プロテイナーゼ活性化受容体アンタゴニストを含む組成物および方法
GB0507577D0 (en) * 2005-04-14 2005-05-18 Novartis Ag Organic compounds
JP5270538B2 (ja) * 2006-05-23 2013-08-21 アイアールエム・リミテッド・ライアビリティ・カンパニー チャネル活性化プロテアーゼ阻害剤としての化合物および組成物
CA2651762A1 (en) * 2006-05-23 2007-11-29 Irm Llc Compounds and compositions as channel activating protease inhibitors
KR101131238B1 (ko) 2007-02-09 2012-03-30 아이알엠 엘엘씨 채널 활성화 프로테아제 억제제로서의 화합물 및 조성물
AU2008214217B2 (en) * 2007-02-09 2011-10-13 Irm Llc Compounds and compositions as channel activating protease inhibitors
MX2009008493A (es) * 2007-02-09 2009-08-20 Irm Llc Compuestos y composiciones como inhibidores de la proteasa activadora de canal.
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EP2714716B1 (en) 2011-06-02 2018-04-11 Socpra Sciences Santé Et Humaines S.E.C. Matriptase inhibitors and uses thereof against orthomyxoviridae infections
CN103145598B (zh) * 2011-12-07 2014-10-15 北京京卫顺康医药科技发展有限公司 一种奥沙西罗晶体及含有该晶体的组合物
HRP20181197T1 (hr) * 2013-10-29 2018-11-30 Biomarin Pharmaceutical Inc. Derivati n-(1-hidroksi-3-(pirolidinil)propan-2-il)pirolidin-3-karboksamida kao inhibitori glukozilceramid sintaze
PT3204352T (pt) 2014-10-06 2020-09-23 Cortexyme Inc Inibidores de lisina-gingipaína
WO2016144654A1 (en) * 2015-03-09 2016-09-15 Washington University Inhibitors of growth factor activation enzymes
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Also Published As

Publication number Publication date
ZA200106995B (en) 2002-11-25
JP2002535394A (ja) 2002-10-22
EP1147097A1 (en) 2001-10-24
US7132418B2 (en) 2006-11-07
WO2000044733A1 (en) 2000-08-03
IL144577A0 (en) 2002-05-23
HUP0201295A3 (en) 2002-10-28
KR20010110422A (ko) 2001-12-13
AR022427A1 (es) 2002-09-04
NO20013666D0 (no) 2001-07-26
SK10742001A3 (sk) 2002-08-06
EE200100391A (et) 2002-10-15
BR0007778A (pt) 2002-06-04
CN1353701A (zh) 2002-06-12
TR200102766T2 (tr) 2001-12-21
HUP0201295A2 (en) 2002-09-28
YU61401A (sh) 2005-07-19
HRP20010601A2 (en) 2002-08-31
NO20013666L (no) 2001-09-26
US6469036B1 (en) 2002-10-22
EA200100815A1 (ru) 2002-08-29
CA2361479A1 (en) 2000-08-03
BG105762A (en) 2002-03-29
CZ20012722A3 (cs) 2002-08-14
TWI229669B (en) 2005-03-21
AU3208500A (en) 2000-08-18
US20030008829A1 (en) 2003-01-09

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