EA200100882A1 - Гетероарильные производные амидина, метиламидина и гуанидина (варианты), способ их получения, фармацевтическая композиция (варианты), способ ингибирования протеазы (варианты) и способ лечения различных заболеваний (варианты) - Google Patents

Гетероарильные производные амидина, метиламидина и гуанидина (варианты), способ их получения, фармацевтическая композиция (варианты), способ ингибирования протеазы (варианты) и способ лечения различных заболеваний (варианты)

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Publication number
EA200100882A1
EA200100882A1 EA200100882A EA200100882A EA200100882A1 EA 200100882 A1 EA200100882 A1 EA 200100882A1 EA 200100882 A EA200100882 A EA 200100882A EA 200100882 A EA200100882 A EA 200100882A EA 200100882 A1 EA200100882 A1 EA 200100882A1
Authority
EA
Eurasian Patent Office
Prior art keywords
options
spoda
products
hydroarial
guanida
Prior art date
Application number
EA200100882A
Other languages
English (en)
Inventor
Карл Р. Иллиг
Хуан Хосе Маруган
Джонатан М. Рудолф
Налин Л. Субасингх
Кеннет Дж. Уилсон
Джеймс Б. Хоффман
Original Assignee
3-Дименшенл Фамэсьютикэлс, Инк.
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.)
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Publication date
Application filed by 3-Дименшенл Фамэсьютикэлс, Инк. filed Critical 3-Дименшенл Фамэсьютикэлс, Инк.
Publication of EA200100882A1 publication Critical patent/EA200100882A1/ru

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    • 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

Настоящее изобретение направлено на соединения формулы (I), где Х представляет О, S или NR, где R-R, Y и Z имеют значения, определенные в описании, а также их гидраты, сольваты или фармацевтически приемлемые соли. Описаны также способы получения соединений формулы (I). Новые соединения настоящего изобретения являются сильными ингибиторами протеаз, особенно сериновых протеаз, подобных трипсину, таких как химотрипсин, трипсин, плазмин и урокиназа. Определенные соединения проявляют непосредственное селективное ингибирование урокиназы или являются промежуточными продуктами, используемыми для получения соединений, обладающих такой активностью.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200100882A 1999-02-09 1999-08-11 Гетероарильные производные амидина, метиламидина и гуанидина (варианты), способ их получения, фармацевтическая композиция (варианты), способ ингибирования протеазы (варианты) и способ лечения различных заболеваний (варианты) EA200100882A1 (ru)

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
EA200100882A1 true EA200100882A1 (ru) 2002-04-25

Family

ID=22933398

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200100882A EA200100882A1 (ru) 1999-02-09 1999-08-11 Гетероарильные производные амидина, метиламидина и гуанидина (варианты), способ их получения, фармацевтическая композиция (варианты), способ ингибирования протеазы (варианты) и способ лечения различных заболеваний (варианты)

Country Status (19)

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

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EP1569912B1 (en) 2002-12-03 2015-04-29 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
JP2005538953A (ja) * 2002-05-28 2005-12-22 ３−ディメンショナル ファーマシューティカルズ， インコーポレイテッド 新規チオフェンアミジン、それらの組成物、および補体媒介疾患および病気を治療する方法
US7482376B2 (en) * 2003-07-03 2009-01-27 3-Dimensional Pharmaceuticals, Inc. Conjugated complement cascade inhibitors
NZ544674A (en) * 2003-07-10 2009-03-31 Achillion Pharmaceuticals Inc Substituted arylthiourea derivatives useful as inhibitors of viral replication
US20090148382A1 (en) 2004-02-12 2009-06-11 Molecular Insight Pharmaceuticals, Inc. Technetium- and rhenium-bis(heteroaryl) complexes, and methods of use thereof
EP2344453B1 (en) * 2008-10-09 2016-12-28 The U.S.A. As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
MX2012000435A (es) 2009-07-08 2012-06-01 Dermira Canada Inc Analogos de acido 5-(tetradeciloxi)-2-furancarboxilico (tofa) utiles en el tratamiento de trastornos o afecciones dermatologicas.
CA2797694A1 (en) 2010-04-29 2011-11-03 The United States Of America, As Represented By The Secretary, Departmen T Of Health And Human Services Activators of human pyruvate kinase
CA2825306C (en) * 2011-01-25 2019-02-26 The Regents Of The University Of Michigan Bcl-2/bcl-xl inhibitors and therapeutic methods using the same
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EP2606726A1 (de) * 2011-12-21 2013-06-26 Bayer CropScience AG N-Arylamidine-substituierte trifluoroethylsulfid-Derivate als Akarizide und Insektizide
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Also Published As

Publication number Publication date
EP1150979A1 (en) 2001-11-07
IL144560A0 (en) 2002-05-23
HUP0201475A2 (hu) 2003-10-28
KR20010098982A (ko) 2001-11-08
NZ513701A (en) 2001-09-28
BG105866A (en) 2002-06-28
NO324887B1 (no) 2007-12-27
MXPA01008084A (es) 2004-09-10
ZA200106849B (en) 2002-11-20
SK11422001A3 (sk) 2002-04-04
AU5671799A (en) 2000-08-29
NO20013853L (no) 2001-10-09
PL351767A1 (en) 2003-06-16
NO20013853D0 (no) 2001-08-07
JP2002536446A (ja) 2002-10-29
CN1337961A (zh) 2002-02-27
BR9917036A (pt) 2002-07-30
CZ20012858A3 (cs) 2002-05-15
CA2362390A1 (en) 2000-08-17
WO2000047578A1 (en) 2000-08-17

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