AR012631A1 - Inhibidores de la proteasa de serina - Google Patents

Inhibidores de la proteasa de serina

Info

Publication number
AR012631A1
AR012631A1 ARP980102014A ARP980102014A AR012631A1 AR 012631 A1 AR012631 A1 AR 012631A1 AR P980102014 A ARP980102014 A AR P980102014A AR P980102014 A ARP980102014 A AR P980102014A AR 012631 A1 AR012631 A1 AR 012631A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
halogen
amino acid
substituted
Prior art date
Application number
ARP980102014A
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 AR012631A1 publication Critical patent/AR012631A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

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

Abstract

Un compuesto de la formula (I) R1SO2-B-X-Z-C(O)-Y donde R! es R2OOC-(CHR2)m -o R2NH-CO-(CHR2)m-o se selecciona entre alquilo (1-12C), alquenilo (2-12C),dichos grupos pueden estar sustituidos opcionalmente por cicloalquilo (3-12C), alcoxi (1-6C), OH,COOR2, CF3 o halogeno, y entre arilo (6-14), aralquilo(7-15C) y aralquenilo (8-16), los grupos arílicos de los cuales pueden sustituirse, opcionalmente, por alquilo (1-6C), cicloalquilo (3-8C), alcoxi(1-6C), OH, COOH, CF3 o halogeno; m es 1, 2 o 3; cada grupo R2 es independientemente H, alquilo (1-12C), cicloalquilo (3-8C), arilo (6-14C) oaralquilo (7-15C), los grupos arilicos de los cuales pueden estar sustituidos por alquilo (1-6C), aklcoxi (1-6C) o halogeno; B es unenlace, un aminoácido deformula -NH-CH[(CH2)9C(O)OH]-C(O)- o un derivado de éster del mismo donde p es 1, 2 o 3, Gly, D-1-Piq, D-3-Piq, D-1-Tiq, D-3-Piq, D-3-Tiq, D-3-Tiq, D-Atc, Aico un L- o D-aminoácido con una cadena lateral hidrofoba, básica o neutra; X es un aminoácido con una cadena lateral hidrogoba, glutamina, serina, treonina, unaminoácido cíclico que contiene opcionalmente un heteroátomo adicional seleccionado entre N, O o S y opcionalmente sustituido por alquilo (1-6C),benciloxi u oxo, o X es ácido 2-amino-isobutírico, -NR2-CH2-C(O)- oel fragmento de la formula O donde n es 2, 3 o 4, W es CXH o N y R3 es H, fenilo o alquilo(1-6C); dichos grupos pueden estar sustituidos opcionalmente, por hidroxi, alcoxi (1-6C), COOH, COO(1-6C) alquilo, CONH2 o halogeno; Z es lisina o4-aminociclohesilglicina; Y es -NH-(1-6C) alquileno-C6H5, el grupo fenílico del cual puede estar sustituído por alquilo (1-6C), alcoxi (1-6C)o halogeno, oY es -OR4 o -NR5R6, donde R4 es H, alquilo (2-6C) o bencilo, y R5 y R6 son independientemente H, alcoxi (1-6C) o alquilo (1-6C) opcionalmente sustituidos
ARP980102014A 1997-05-02 1998-04-30 Inhibidores de la proteasa de serina AR012631A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP97201286 1997-05-02

Publications (1)

Publication Number Publication Date
AR012631A1 true AR012631A1 (es) 2000-11-08

Family

ID=8228278

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980102014A AR012631A1 (es) 1997-05-02 1998-04-30 Inhibidores de la proteasa de serina

Country Status (23)

Country Link
US (1) US6534495B1 (es)
EP (1) EP0979240B1 (es)
JP (1) JP2001524117A (es)
KR (1) KR20010012174A (es)
CN (1) CN1254345A (es)
AR (1) AR012631A1 (es)
AT (1) ATE264339T1 (es)
AU (1) AU729910B2 (es)
BR (1) BR9809342A (es)
CA (1) CA2287569A1 (es)
DE (1) DE69823178T2 (es)
DK (1) DK0979240T3 (es)
ES (1) ES2218827T3 (es)
HU (1) HUP0002942A3 (es)
ID (1) ID22904A (es)
NO (1) NO995316L (es)
NZ (1) NZ500620A (es)
PL (1) PL336589A1 (es)
PT (1) PT979240E (es)
RU (2) RU2183642C2 (es)
TR (1) TR199902692T2 (es)
WO (1) WO1998050420A1 (es)
ZA (1) ZA983629B (es)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9900043D0 (sv) * 1999-01-11 1999-01-11 Astra Ab New use
BR9916732A (pt) 1999-01-02 2001-09-25 Aventis Pharma Gmbh Derivados de ácido malÈnico, processo para a sua preparação, seu uso e composições farmacêuticas contendo-os (inibição da atividade do fator xa)
US6344450B1 (en) * 1999-02-09 2002-02-05 Bristol-Myers Squibb Company Lactam compounds and their use as inhibitors of serine proteases and method
US7704958B1 (en) 1999-03-05 2010-04-27 Bio Holding, Inc. Methods and compositions for inhibiting apoptosis using serine protease inhibitors
BR0010349B1 (pt) * 1999-05-07 2011-10-04 derivados de ácido propanóico que inibem a ligação de integrinas aos seus receptores.
US6723711B2 (en) 1999-05-07 2004-04-20 Texas Biotechnology Corporation Propanoic acid derivatives that inhibit the binding of integrins to their receptors
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
JP2000344739A (ja) 1999-06-01 2000-12-12 Sumitomo Chem Co Ltd Ｎ−保護−アゼチジン−２−カルボン酸の製造方法
US6774212B2 (en) 1999-12-03 2004-08-10 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis C virus NS3 protease
EP1127884A1 (en) 2000-02-26 2001-08-29 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use as inhibitor of factor XA activity and pharmaceutical compositions containing them
US6852761B2 (en) 2000-03-13 2005-02-08 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
WO2001077097A2 (en) 2000-04-05 2001-10-18 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
CA2405306A1 (en) 2000-04-05 2001-10-18 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
CA2405684A1 (en) 2000-04-17 2001-10-25 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
US6624180B2 (en) 2000-11-20 2003-09-23 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
WO2002060894A2 (en) 2001-01-30 2002-08-08 Bristol-Myers Squibb Company Sulfonamide lactam inhibitors of factor xa
GB0119370D0 (en) * 2001-08-08 2001-10-03 Univ London Therapeutic agent
WO2003013508A1 (en) 2001-08-08 2003-02-20 Pentraxin Therapeutics Limited Therapeutic agent for depletion of an unwanted protein population from plasma
WO2003093242A2 (en) 2001-10-03 2003-11-13 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
US6969715B2 (en) 2001-10-03 2005-11-29 Pharmacia Corporation 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
GB0313386D0 (en) 2003-06-10 2003-07-16 Univ London Treatment of disease
DK2520654T3 (en) 2003-08-26 2017-05-01 Univ Colorado Regents Inhibitors of serine protease activity and their use in methods and compositions for the treatment of bacterial infections
WO2007137080A2 (en) 2006-05-23 2007-11-29 Irm Llc Compounds and compositions as channel activating protease inhibitors
JP2010518099A (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
ES2534832T3 (es) 2009-03-10 2015-04-29 Med Discovery Sa Uso de inhibidores de serina proteasa en el tratamiento de la neutropenia
RU2020130012A (ru) * 2018-03-28 2022-04-29 Блэйд Терапьютикс, Инк. Способ лечения фиброзного заболевания
DE102020103516B4 (de) 2020-02-11 2023-12-07 Universität Zu Lübeck Antivirale Wirkstoffe mit breiter Aktivität

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA86746B (en) * 1985-02-04 1986-09-24 Merrell Dow Pharma Novel peptidase inhibitors
US5919765A (en) 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
IL119466A (en) * 1995-11-03 2001-08-26 Akzo Nobel Nv Thrombin inhibitors, their preparation and pharmaceutical compositions containing them
AU4172397A (en) * 1996-09-06 1998-03-26 Biochem Pharma Inc. Lactam inhibitors of thrombin

Also Published As

Publication number Publication date
US6534495B1 (en) 2003-03-18
NO995316D0 (no) 1999-11-01
AU729910B2 (en) 2001-02-15
TR199902692T2 (xx) 2000-07-21
WO1998050420A1 (en) 1998-11-12
CA2287569A1 (en) 1998-11-12
AU7652098A (en) 1998-11-27
EP0979240B1 (en) 2004-04-14
DE69823178T2 (de) 2005-06-23
JP2001524117A (ja) 2001-11-27
HUP0002942A3 (en) 2001-12-28
ATE264339T1 (de) 2004-04-15
EP0979240A1 (en) 2000-02-16
CN1254345A (zh) 2000-05-24
KR20010012174A (ko) 2001-02-15
RU2002104026A (ru) 2004-04-27
ES2218827T3 (es) 2004-11-16
ID22904A (id) 1999-12-16
NO995316L (no) 1999-11-01
DK0979240T3 (da) 2004-07-26
ZA983629B (en) 1998-11-04
PT979240E (pt) 2004-08-31
BR9809342A (pt) 2000-07-04
RU2183642C2 (ru) 2002-06-20
NZ500620A (en) 2000-10-27
HUP0002942A2 (hu) 2001-01-29
DE69823178D1 (de) 2004-05-19
PL336589A1 (en) 2000-07-03

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