BR9809342A - Composto, composição farmacêutica, e, uso do composto - Google Patents

Composto, composição farmacêutica, e, uso do composto

Info

Publication number
BR9809342A
BR9809342A BR9809342-8A BR9809342A BR9809342A BR 9809342 A BR9809342 A BR 9809342A BR 9809342 A BR9809342 A BR 9809342A BR 9809342 A BR9809342 A BR 9809342A
Authority
BR
Brazil
Prior art keywords
compound
amino acid
pharmaceutical composition
tiq
piq
Prior art date
Application number
BR9809342-8A
Other languages
English (en)
Inventor
Anton Egbert Peter Adang
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 BR9809342A publication Critical patent/BR9809342A/pt

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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (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)
  • Hematology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (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

"COMPOSTO, COMPOSIçãO FARMACêUTICA, E, USO DO COMPOSTO" A invenção diz respeito a um composto tendo a fórmula (I) R^ 1^SO~ 2~-B-X-Z-C-(O)-Y B é uma ligação, um aminoácido da fórmula -NH-CH[(CH~ 2~)~ p~C(O)OH]-C(O)- ou um seu derivado éster, em que p é 1, 2 ou 3, Gly, D-1-Piq, D-3-Piq, D-1-Tiq, D-3-Tiq. D-Atc. Aic ou um aminoácido L ou D tendo uma cadeia lateral hidrofóbica, básica ou neutra; X é um aminoácido com uma cadeia lateral hidrofóbica, glutamina, serina, treonina, um aminoácido cíclico opcionalmente contendo um heteroátomo adicional selecionado de N, O ou S, e opcionalmente substituído por alquila (1-6C), alcóxi (1-6C), benzilóxi ou oxo, ou X é ácido 2-amino-isobutírico, -NR^ 2^-CH~ 2~-C(O)- ou o fragmento (I) em que n é 2, 3 ou 4, W é CH ou N, e R^ 3^ é H, alquila (1-6C) ou fenila, cujos grupos podem opcionalmente ser substituídos por hidróxi, alcóxi (1-6C), COOH, COOalquila (1-6C), CONH~ 2~ ou halogênio; Z é lisina ou 4-aminociclo-hexilglicina. Os compostos da invenção têm atividade anticoagulante e podem ser usados no tratamento ou prevenção de doenças relacionadas com a trombina. A variável R^ 1^ e Y são definidos na reivindicação 1.
BR9809342-8A 1997-05-02 1998-04-28 Composto, composição farmacêutica, e, uso do composto BR9809342A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP97201286 1997-05-02
PCT/EP1998/002587 WO1998050420A1 (en) 1997-05-02 1998-04-28 Serine protease inhibitors

Publications (1)

Publication Number Publication Date
BR9809342A true BR9809342A (pt) 2000-07-04

Family

ID=8228278

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9809342-8A BR9809342A (pt) 1997-05-02 1998-04-28 Composto, composição farmacêutica, e, uso do composto

Country Status (23)

Country Link
US (1) US6534495B1 (pt)
EP (1) EP0979240B1 (pt)
JP (1) JP2001524117A (pt)
KR (1) KR20010012174A (pt)
CN (1) CN1254345A (pt)
AR (1) AR012631A1 (pt)
AT (1) ATE264339T1 (pt)
AU (1) AU729910B2 (pt)
BR (1) BR9809342A (pt)
CA (1) CA2287569A1 (pt)
DE (1) DE69823178T2 (pt)
DK (1) DK0979240T3 (pt)
ES (1) ES2218827T3 (pt)
HU (1) HUP0002942A3 (pt)
ID (1) ID22904A (pt)
NO (1) NO995316D0 (pt)
NZ (1) NZ500620A (pt)
PL (1) PL336589A1 (pt)
PT (1) PT979240E (pt)
RU (2) RU2183642C2 (pt)
TR (1) TR199902692T2 (pt)
WO (1) WO1998050420A1 (pt)
ZA (1) ZA983629B (pt)

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SE9900043D0 (sv) * 1999-01-11 1999-01-11 Astra Ab New use
KR20010101355A (ko) 1999-01-02 2001-11-14 로버트 흐라이탁, 미쉘 베스트 신규한 말론산 유도체, 이의 제조 방법, 이의 용도 및이를 함유하는 약제학적 조성물(인자 ｘａ 활성 억제)
US6344450B1 (en) * 1999-02-09 2002-02-05 Bristol-Myers Squibb Company Lactam compounds and their use as inhibitors of serine proteases and method
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
US6723711B2 (en) 1999-05-07 2004-04-20 Texas Biotechnology Corporation Propanoic acid derivatives that inhibit the binding of integrins to their receptors
AU4826900A (en) * 1999-05-07 2000-11-21 Texas Biotechnology Corporation Propanoic acid derivatives that inhibit the binding of integrins to their receptors
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones 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
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones 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
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones 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
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
WO2001040262A1 (en) * 1999-12-03 2001-06-07 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
US6660885B2 (en) 2000-03-13 2003-12-09 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
WO2001077079A2 (en) 2000-04-05 2001-10-18 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
CA2405561A1 (en) 2000-04-05 2001-10-18 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
JP2004501077A (ja) 2000-04-17 2004-01-15 ファルマシア・コーポレーション 凝固カスケードの選択的阻害に有用な多環式アリールおよびヘテロアリール置換１，４−キノン
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
JP2004517074A (ja) 2000-11-20 2004-06-10 ファルマシア・コーポレーション 凝血カスケードを選択的に阻害するのに有用な置換された多環アリールおよびヘテロアリールピリジン類
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
HUP0304058A2 (hu) 2001-01-30 2004-04-28 Bristol-Myers Squibb Company Xa faktor szulfonamid-laktám inhibitorok és alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
GB0119370D0 (en) * 2001-08-08 2001-10-03 Univ London Therapeutic agent
ATE361068T1 (de) 2001-08-08 2007-05-15 Pentraxin Therapeutics Ltd Wirkstoff zur entfernung einer unerwünschten proteinpopulation aus dem plasma
BR0213092A (pt) 2001-10-03 2004-10-19 Pharmacia Corp Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação
CA2462645A1 (en) 2001-10-03 2003-11-13 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
GB0313386D0 (en) 2003-06-10 2003-07-16 Univ London Treatment of disease
PL2520654T3 (pl) 2003-08-26 2017-08-31 The Regents Of The University Of Colorado, A Body Corporate Inhibitory aktywności proteazy serynowej i ich zastosowanie w sposobach i kompozycjach do leczenia zakażeń bakteryjnych
JP2007514742A (ja) * 2003-12-18 2007-06-07 アストラゼネカ アクチボラグ トロンビンの阻害薬として有用な新規５，６−ジヒドロピリジン−２−オン化合物
US7951823B2 (en) 2006-05-23 2011-05-31 Irm Llc Compounds and compositions as channel activating protease inhibitors
KR20090108131A (ko) 2007-02-09 2009-10-14 아이알엠 엘엘씨 채널 활성화 프로테아제 억제제로서의 화합물 및 조성물
KR20120093754A (ko) 2009-03-10 2012-08-23 메드 디스커버리 에스에이 세린 프로테아제 저해제의 호중구감소증 치료에서의 용도
AU2019242595A1 (en) * 2018-03-28 2020-11-19 Blade Therapeutics, Inc. Method of treating fibrotic disease
DE102020103516B4 (de) 2020-02-11 2023-12-07 Universität Zu Lübeck Antivirale Wirkstoffe mit breiter Aktivität

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Publication number Priority date Publication date Assignee Title
ZA86746B (en) * 1985-02-04 1986-09-24 Merrell Dow Pharma Novel peptidase inhibitors
GB8728561D0 (en) * 1987-12-07 1988-01-13 Glaxo Group Ltd Chemical compounds
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
WO1998009987A1 (en) * 1996-09-06 1998-03-12 Biochem Pharma, Inc. Lactam inhibitors of thrombin

Also Published As

Publication number Publication date
PL336589A1 (en) 2000-07-03
AU729910B2 (en) 2001-02-15
RU2002104026A (ru) 2004-04-27
JP2001524117A (ja) 2001-11-27
PT979240E (pt) 2004-08-31
ZA983629B (en) 1998-11-04
DE69823178D1 (de) 2004-05-19
DE69823178T2 (de) 2005-06-23
CN1254345A (zh) 2000-05-24
EP0979240A1 (en) 2000-02-16
KR20010012174A (ko) 2001-02-15
CA2287569A1 (en) 1998-11-12
EP0979240B1 (en) 2004-04-14
AR012631A1 (es) 2000-11-08
WO1998050420A1 (en) 1998-11-12
NZ500620A (en) 2000-10-27
ID22904A (id) 1999-12-16
US6534495B1 (en) 2003-03-18
ES2218827T3 (es) 2004-11-16
RU2183642C2 (ru) 2002-06-20
NO995316L (no) 1999-11-01
DK0979240T3 (da) 2004-07-26
NO995316D0 (no) 1999-11-01
TR199902692T2 (xx) 2000-07-21
HUP0002942A2 (hu) 2001-01-29
ATE264339T1 (de) 2004-04-15
HUP0002942A3 (en) 2001-12-28
AU7652098A (en) 1998-11-27

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Legal Events

Date Code Title Description
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 1891 DE 03/04/2007.