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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (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)

Families Citing this family (36)

* 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
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
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
US6458952B1 (en) 1999-05-19 2002-10-01 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
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones 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
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones 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
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
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
WO2001068605A1 (en) 2000-03-13 2001-09-20 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
ATE289299T1 (de) 2000-04-05 2005-03-15 Pharmacia Corp Polyzyclisch aryl und heteroaryl substituierte 4- pyronen verwendbar als selektive hemmung von dem koagulationsprozess
EP1268428A2 (en) 2000-04-05 2003-01-02 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones 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
EP1351686A2 (en) 2000-11-20 2003-10-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines 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
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
HUP0304058A2 (hu) 2001-01-30 2004-04-28 Bristol-Myers Squibb Company Xa faktor szulfonamid-laktám inhibitorok és alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
DK1418905T3 (da) 2001-08-08 2007-09-10 Pentraxin Therapeutics Ltd Terapeutisk middel til depletering af en uönsket proteinpopulation fra plasma
GB0119370D0 (en) * 2001-08-08 2001-10-03 Univ London Therapeutic agent
WO2003093242A2 (en) 2001-10-03 2003-11-13 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
MXPA04003163A (es) 2001-10-03 2004-07-08 Pharmacia Corp Compuestos heterociclicos de 6 elementos utiles para inhibicion selectiva de la casdada de coagulacion.
GB0313386D0 (en) 2003-06-10 2003-07-16 Univ London Treatment of disease
US7850970B2 (en) 2003-08-26 2010-12-14 The Regents Of The University Of Colorado Inhibitors of serine protease activity and their use in methods and compositions for treatment of bacterial infections
SA04250414B1 (ar) * 2003-12-18 2007-07-31 استرازينيكا ايه بي مركبات -2- one 5,6-dihydropryidin جديدة مفيدة كمثبطات inhibitors للـــ trombin
US7951823B2 (en) 2006-05-23 2011-05-31 Irm Llc Compounds and compositions as channel activating protease inhibitors
EA016327B1 (ru) 2007-02-09 2012-04-30 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
EP2405925B1 (en) 2009-03-10 2015-01-14 Med Discovery Sa Kallikrein inhibitors for the treatment of neutropenia
KR20200139721A (ko) * 2018-03-28 2020-12-14 블레이드 테라퓨틱스, 인크. 섬유성 질환을 치료하는 방법
DE102020103516B4 (de) 2020-02-11 2023-12-07 Universität Zu Lübeck Antivirale Wirkstoffe mit breiter Aktivität

Family Cites Families (5)

* 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
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
AU4172397A (en) * 1996-09-06 1998-03-26 Biochem Pharma Inc. Lactam inhibitors of thrombin

Also Published As

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

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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.