BR9917036A - Amidinas heteroarila, metilamidinas e guanidinas como inibidores de protease - Google Patents

Amidinas heteroarila, metilamidinas e guanidinas como inibidores de protease

Info

Publication number
BR9917036A
BR9917036A BR9917036-1A BR9917036A BR9917036A BR 9917036 A BR9917036 A BR 9917036A BR 9917036 A BR9917036 A BR 9917036A BR 9917036 A BR9917036 A BR 9917036A
Authority
BR
Brazil
Prior art keywords
compounds
protease inhibitors
methylamidines
guanidines
urokinase
Prior art date
Application number
BR9917036-1A
Other languages
English (en)
Inventor
Carl R Illig
Nalin L Subasinghe
James B Hoffman
Kenneth J Wilson
M Jonathan Rudolph
Juan Jose Marugan
Original Assignee
Dimensional 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 Dimensional Pharm Inc filed Critical Dimensional Pharm Inc
Publication of BR9917036A publication Critical patent/BR9917036A/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D417/14—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 three or more hetero rings

Abstract

"AMIDINAS HETEROARILA, METILAMIDINAS E GUANIDINAS COMO INIBIDORES DE PROTEASE". A presente invenção é dirigida aos compostos da fórmula (I) , onde X é O, S ou NR^ 7^ e R^ 1^-R^ 7^, Y e Z são estabelecidos na descrição, bem como hidratos, solvatos ou sais farmaceuticamente aceitáveis dos mesmos. Também são descritos processos para preparação dos compostos da fórmula (I). Os novos compostos da presente invenção são inibidores potentes de proteases, especialmente proteases serina semelhantes a tripsina, tais como, quimotripsina, tripsina, plasmino e uroquinase. Determinados compostos exibem inibição direta, seletiva de uroquinase, ou são intermediários úteis para formação dos compostos possuindo tal atividade.
BR9917036-1A 1999-02-09 1999-08-11 Amidinas heteroarila, metilamidinas e guanidinas como inibidores de protease BR9917036A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24706299A 1999-02-09 1999-02-09
PCT/US1999/018065 WO2000047578A1 (en) 1999-02-09 1999-08-11 Heteroaryl amidines, methylamidines and guanidines as protease inhibitors

Publications (1)

Publication Number Publication Date
BR9917036A true BR9917036A (pt) 2002-07-30

Family

ID=22933398

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9917036-1A BR9917036A (pt) 1999-02-09 1999-08-11 Amidinas heteroarila, metilamidinas e guanidinas como inibidores de protease

Country Status (19)

Country Link
EP (1) EP1150979A1 (pt)
JP (1) JP2002536446A (pt)
KR (1) KR20010098982A (pt)
CN (1) CN1337961A (pt)
AU (1) AU5671799A (pt)
BG (1) BG105866A (pt)
BR (1) BR9917036A (pt)
CA (1) CA2362390A1 (pt)
CZ (1) CZ20012858A3 (pt)
EA (1) EA200100882A1 (pt)
HU (1) HUP0201475A2 (pt)
IL (1) IL144560A0 (pt)
MX (1) MXPA01008084A (pt)
NO (1) NO324887B1 (pt)
NZ (1) NZ513701A (pt)
PL (1) PL351767A1 (pt)
SK (1) SK11422001A3 (pt)
WO (1) WO2000047578A1 (pt)
ZA (1) ZA200106849B (pt)

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WO2000047194A2 (en) * 1999-02-09 2000-08-17 3-Dimensional Pharmaceuticals, Inc. METHODS OF TREATING C1s-MEDIATED DISEASES AND CONDITIONS, AND COMPOUNDS AND COMPOSITIONS THEREFOR
BR0311419A (pt) * 2002-05-28 2005-04-05 Dimensional Pharm Inc Amidinas de tiofeno suas composições e métodos de tratamento de doenças e condições mediadas por complemento
AU2003302238A1 (en) 2002-12-03 2004-06-23 Axys Pharmaceuticals, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
US7482376B2 (en) * 2003-07-03 2009-01-27 3-Dimensional Pharmaceuticals, Inc. Conjugated complement cascade inhibitors
JP2007523868A (ja) * 2003-07-10 2007-08-23 アキリオン ファーマシューティカルズ，インコーポレーテッド ウイルス複製の阻害薬として有用な置換アリールチオウレア誘導体類
CA2555959A1 (en) 2004-02-12 2005-09-01 Molecular Insight Pharmaceuticals Technetium- and rhenium-bis(heteroaryl) complexes, and methods of use thereof
US8841305B2 (en) 2008-10-09 2014-09-23 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of the human pyruvate kinase M2 receptor
WO2011005660A1 (en) 2009-07-08 2011-01-13 Valocor Therapeutics, Inc. Tofa analogs useful in treating dermatological disorders or conditions
EP2563761A1 (en) 2010-04-29 2013-03-06 The U.S.A. As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
US8691184B2 (en) * 2011-01-25 2014-04-08 The Regents Of The University Of Michigan Bcl-2/Bcl-xL inhibitors and therapeutic methods using the same
AR086744A1 (es) * 2011-06-28 2014-01-22 Nippon Soda Co Compuesto heterociclico conteniendo nitrogeno y fungicida para el uso en agricultura y jardineria
EP2606726A1 (de) * 2011-12-21 2013-06-26 Bayer CropScience AG N-Arylamidine-substituierte trifluoroethylsulfid-Derivate als Akarizide und Insektizide
TWI644899B (zh) 2013-02-04 2018-12-21 健生藥品公司 Ｆｌａｐ調節劑
EP3495359A1 (en) 2013-02-04 2019-06-12 Janssen Pharmaceutica NV Flap modulators
BR112020019804A2 (pt) * 2018-03-30 2021-01-05 Sumitomo Chemical Company, Limited Composto heterocíclico e composição de controle de peste artrópode contendo o mesmo
CN109020837A (zh) * 2018-07-27 2018-12-18 广东省石油与精细化工研究院 一种2-取代苯基-乙脒盐酸盐的制备方法

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Also Published As

Publication number Publication date
SK11422001A3 (sk) 2002-04-04
NO324887B1 (no) 2007-12-27
WO2000047578A1 (en) 2000-08-17
MXPA01008084A (es) 2004-09-10
AU5671799A (en) 2000-08-29
EA200100882A1 (ru) 2002-04-25
JP2002536446A (ja) 2002-10-29
CZ20012858A3 (cs) 2002-05-15
ZA200106849B (en) 2002-11-20
KR20010098982A (ko) 2001-11-08
NO20013853L (no) 2001-10-09
EP1150979A1 (en) 2001-11-07
CA2362390A1 (en) 2000-08-17
NZ513701A (en) 2001-09-28
CN1337961A (zh) 2002-02-27
IL144560A0 (en) 2002-05-23
NO20013853D0 (no) 2001-08-07
HUP0201475A2 (hu) 2003-10-28
BG105866A (en) 2002-06-28
PL351767A1 (en) 2003-06-16

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

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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 1913 DE 04/09/2007.