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AR006311A1 - Un inhibidor de la serina proteasa - Google Patents

Un inhibidor de la serina proteasa

Info

Publication number
AR006311A1
AR006311A1 ARP970100834A ARP970100834A AR006311A1 AR 006311 A1 AR006311 A1 AR 006311A1 AR P970100834 A ARP970100834 A AR P970100834A AR P970100834 A ARP970100834 A AR P970100834A AR 006311 A1 AR006311 A1 AR 006311A1
Authority
AR
Argentina
Prior art keywords
chr2
amino acid
r2ooc
alkyl
optionally substituted
Prior art date
Application number
ARP970100834A
Other languages
English (en)
Original Assignee
Akzo Nobel Nv
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 Akzo Nobel Nv filed Critical Akzo Nobel Nv
Publication of AR006311A1 publication Critical patent/AR006311A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • C07K5/0222Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. Pro, Trp
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06104Dipeptides with the first amino acid being acidic
    • C07K5/06113Asp- or Asn-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Un compuesto que tiene la fórmula (I), que comprende: A es H, D, L alfa- hidroxiacetilo opcionalmente substituido, R1, R1-O-C(O)-, R1-C(O)-,R1-SO2-,R2OOC-(CHR2)m-SO2-, R2OOC-(CHR2)m-, H2NCO-(CHR2)m, o un grupo N-protector, en donde R1 essele ccionado entre (1-12C)alquilo, (2-12C)alquenilo,(2-12C)-alquinilo y (3-8C)ciacloalquilo, grupos que pueden ser opcionalmente substituidos con (3-8C)cicloalquilo, (1-6C)-alcoxi, oxo, OH, COOH, CF3 ohalógeno, y de (6-14C)arilo,(7-15C)aralqu ilo y (8-16)aralquenilo, cuyos grupos arilo pueden ser opcionalmente substituidos con (1-6C)alquilo,(3-8C)-cicloalquilo, (1-6C)alcoxi, OH, COOH, CF3 o halógeno; cada grupo R2 es independientemente H o tiene el mismosignificado que R1; m es 1, 2 o 3; Bes un enlace, un aminoácido de la fórmula -NH-CH[(CH2)pC(O)OH]-C(O)- o un derivado éster del mismo y siendo p igual a 0, 1, 2 o 3, -N((1-12C)alquilo-CH2-CO-, -N((2-12C)alquinilo)-CH2-CO-,-N(bencilo)-CH2-CO-, D-1-Tiq, D-3-T iq, D-Atc, Aic, D-1-Piq, D-3-Piq o un -L o D-aminoácido que tiene unacadena lateral hidrófoba, básica o neutra, aminoácido que puede estar opcionalmente substituido con N-(1-6C)alquilo; o A y Bjuntos son el residuoR3R4N-CHR5-C(O)-, en dond e R3 y R4 independientemente son R1, R1-O-C(O)-, R1-SO2-, R2OOC-(CHR2)m-SO2-, R2OOC-(CHR2)m-, H2NCO-(CHR2)m-, o un grupoN-protector, o uno de R3 y R4 está conectado con R5 para formar un anillo de5 o 6 miembros junto con N-C al cual están uni dos, anillo que puede serfusionado con un anillo de 6 miembros alifático o aromático; y R5 es una cadena lateral hidrófoba, básica o neutra; X es un L-aminoácido con una cadenalateral hidrófoba,serina, treonina, un aminoácido cíclico que cont iene opcionalmente un heteroátomo adicional seleccionado entre N, O o S, y
ARP970100834A 1996-03-01 1997-03-03 Un inhibidor de la serina proteasa AR006311A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP96200545 1996-03-01

Publications (1)

Publication Number Publication Date
AR006311A1 true AR006311A1 (es) 1999-08-25

Family

ID=8223738

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP970100834A AR006311A1 (es) 1996-03-01 1997-03-03 Un inhibidor de la serina proteasa

Country Status (22)

Country Link
US (1) US6218365B1 (es)
EP (1) EP1012164B1 (es)
JP (1) JP2000506838A (es)
KR (1) KR19990087416A (es)
CN (1) CN1212705A (es)
AR (1) AR006311A1 (es)
AT (1) ATE277074T1 (es)
AU (1) AU715765B2 (es)
BR (1) BR9707812A (es)
CA (1) CA2246722A1 (es)
CZ (1) CZ277998A3 (es)
DE (1) DE69730871D1 (es)
HU (1) HUP9901503A3 (es)
ID (2) ID16105A (es)
IL (1) IL120311A (es)
NO (1) NO983992L (es)
NZ (1) NZ331486A (es)
PL (1) PL328665A1 (es)
TR (1) TR199801705T2 (es)
TW (1) TW523513B (es)
WO (1) WO1997031939A1 (es)
ZA (1) ZA971733B (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2289625A1 (en) 1997-05-15 1998-11-19 Charles Van Jackson Antithrombotic compound
US6344450B1 (en) * 1999-02-09 2002-02-05 Bristol-Myers Squibb Company Lactam compounds and their use as inhibitors of serine proteases and method
JP2002542165A (ja) 1999-04-09 2002-12-10 ビーエーエスエフ アクチェンゲゼルシャフト トロンビンインヒビターのプロドラッグ
WO2002006280A2 (en) * 2000-07-13 2002-01-24 Millennium Pharamaceuticals, Inc. INHIBITORS OF FACTOR Xa
WO2002060894A2 (en) 2001-01-30 2002-08-08 Bristol-Myers Squibb Company Sulfonamide lactam inhibitors of factor xa
US6716869B2 (en) * 2001-12-17 2004-04-06 Pharmacia Corporation Protease inhibitors of the coagulation cascade isolated from Dysidea sponges
AU2003248584A1 (en) * 2002-03-01 2003-09-16 Warner-Lambert Company Llc Method of treating osteoarthritis
US7439226B2 (en) * 2003-09-30 2008-10-21 The United States Of America As Represented By The Department Of Health And Human Services Serine protease inhibitors
JP2008521853A (ja) * 2004-12-02 2008-06-26 プロビオドルグ エージー 神経疾患治療用の新規化合物
RU2419626C2 (ru) 2006-05-23 2011-05-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
RU2419625C2 (ru) * 2006-05-23 2011-05-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
EA016327B1 (ru) 2007-02-09 2012-04-30 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
JP2010518097A (ja) * 2007-02-09 2010-05-27 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
WO2017222914A1 (en) 2016-06-21 2017-12-28 Inception 4, Inc. Carbocyclic prolinamide derivatives
EP3472149B1 (en) 2016-06-21 2023-08-30 Orion Ophthalmology LLC Heterocyclic prolinamide derivatives
DE102020103516B4 (de) 2020-02-11 2023-12-07 Universität Zu Lübeck Antivirale Wirkstoffe mit breiter Aktivität
US11124497B1 (en) 2020-04-17 2021-09-21 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
US11174231B1 (en) 2020-06-09 2021-11-16 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
KR20230040386A (ko) * 2020-06-09 2023-03-22 파르데스 바이오사이언시스, 인크. 시스테인 프로테아제의 억제제 및 이의 사용 방법
AU2021289665A1 (en) 2020-06-10 2022-12-15 Aligos Therapeutics, Inc. Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections
IL309732A (en) 2021-07-09 2024-02-01 Aligos Therapeutics Inc Antiviral compounds
WO2023043816A1 (en) 2021-09-17 2023-03-23 Aligos Therapeutics, Inc. Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2159834A1 (en) * 1993-04-30 1994-11-10 Daniel F. Veber Thrombin inhibitors
US5672582A (en) * 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
IL112795A (en) * 1994-03-04 2001-01-28 Astrazeneca Ab Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them
JPH10503176A (ja) * 1994-06-17 1998-03-24 コーバス インターナショナル, インコーポレイテッド 酵素インヒビターとしての3−アミノ−2−オキソ−1−ピペリジン酢酸誘導体
JPH0820597A (ja) * 1994-07-07 1996-01-23 Meiji Seika Kaisha Ltd トロンビン阻害作用を有する複素環カルボニル化合物
WO1996019483A1 (en) * 1994-12-22 1996-06-27 Biochem Pharma Inc. Low molecular weight bicyclic thrombin inhibitors
PL328307A1 (en) * 1996-02-13 1999-01-18 Akzo Nobel Nv Serinic protease inhibitors

Also Published As

Publication number Publication date
HUP9901503A3 (en) 2001-10-29
TR199801705T2 (xx) 1998-12-21
KR19990087416A (ko) 1999-12-27
IL120311A0 (en) 1997-06-10
EP1012164A1 (en) 2000-06-28
WO1997031939A1 (en) 1997-09-04
EP1012164B1 (en) 2004-09-22
CZ277998A3 (cs) 1999-02-17
ID16104A (id) 1997-09-04
HUP9901503A2 (hu) 1999-08-30
ZA971733B (en) 1997-09-10
DE69730871D1 (de) 2004-10-28
ID16105A (id) 1997-09-04
NZ331486A (en) 1999-07-29
NO983992D0 (no) 1998-08-31
AU715765B2 (en) 2000-02-10
TW523513B (en) 2003-03-11
AU1795697A (en) 1997-09-16
ATE277074T1 (de) 2004-10-15
JP2000506838A (ja) 2000-06-06
CN1212705A (zh) 1999-03-31
CA2246722A1 (en) 1997-09-04
BR9707812A (pt) 1999-07-27
IL120311A (en) 2001-10-31
NO983992L (no) 1998-10-30
PL328665A1 (en) 1999-02-15
US6218365B1 (en) 2001-04-17

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