HRP20010601A2 - Peptidyl heterocyclic ketones useful as tryptase inhibitors - Google Patents

Peptidyl heterocyclic ketones useful as tryptase inhibitors Download PDF

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Publication number
HRP20010601A2
HRP20010601A2 HR20010601A HRP20010601A HRP20010601A2 HR P20010601 A2 HRP20010601 A2 HR P20010601A2 HR 20010601 A HR20010601 A HR 20010601A HR P20010601 A HRP20010601 A HR P20010601A HR P20010601 A2 HRP20010601 A2 HR P20010601A2
Authority
HR
Croatia
Prior art keywords
alkyl
amino
substituents
perfluoro
substituted
Prior art date
Application number
HR20010601A
Other languages
English (en)
Croatian (hr)
Inventor
Michael
Bruce E Maryanoff
Stephen C Yabut
Original Assignee
Ortho Mcneil Pharm 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 Pharm Inc filed Critical Ortho Mcneil Pharm Inc
Publication of HRP20010601A2 publication Critical patent/HRP20010601A2/hr

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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)
HR20010601A 1999-01-27 2000-01-13 Peptidyl heterocyclic ketones useful as tryptase inhibitors HRP20010601A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11760299P 1999-01-27 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
HRP20010601A2 true HRP20010601A2 (en) 2002-08-31

Family

ID=22373811

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20010601A HRP20010601A2 (en) 1999-01-27 2000-01-13 Peptidyl heterocyclic ketones useful as tryptase inhibitors

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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US6346510B1 (en) 1995-10-23 2002-02-12 The Children's Medical Center Corporation Therapeutic antiangiogenic endostatin compositions
DE60120661T2 (de) * 2000-03-27 2007-07-05 Applied Research Systems Ars Holding N.V. Pharmazeutisch wirksame pyrrolidin-derivate als bax-inhibitoren
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.
ES2351323B1 (es) * 2009-06-26 2011-10-05 Institut Univ. De Ciència I Tecnologia, S.A. Bibliotecas de n-fenil-1-sulfonil-2-pirrolidinacarboxamidas para el descubrimiento de farmacos.
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
CA3004095A1 (en) 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
ES2992410T3 (es) 2016-09-16 2024-12-12 Lighthouse Pharmaceuticals Inc Inhibidores cetónicos de la lisina gingipaína
CN110944637A (zh) * 2017-05-10 2020-03-31 库特克希米公司 氨基吡啶化合物及其制备方法和使用方法
EP4159211A4 (en) * 2021-07-15 2024-10-30 National Center for Global Health and Medicine ASSOCIATED WITH PHYSIOLOGICAL ACTIVITY SUCH AS ANTIVIRAL ACTIVITY

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Also Published As

Publication number Publication date
ZA200106995B (en) 2002-11-25
HK1038561A1 (zh) 2002-03-22
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
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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