CA2362390A1 - Heteroaryl amidines, methylamidines and guanidines as protease inhibitors - Google Patents

Heteroaryl amidines, methylamidines and guanidines as protease inhibitors Download PDF

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Publication number
CA2362390A1
CA2362390A1 CA002362390A CA2362390A CA2362390A1 CA 2362390 A1 CA2362390 A1 CA 2362390A1 CA 002362390 A CA002362390 A CA 002362390A CA 2362390 A CA2362390 A CA 2362390A CA 2362390 A1 CA2362390 A1 CA 2362390A1
Authority
CA
Canada
Prior art keywords
carboxamidine
methylthiothiophene
amino
thiazol
methylthio
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002362390A
Other languages
English (en)
French (fr)
Inventor
Carl R. Illig
Nalin L. Subasinghe
James B. Hoffman
Kenneth J. Wilson
M. Jonathan Rudolph
Juan Jose Marugan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
3 Dimensional Pharmaceuticals Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2362390A1 publication Critical patent/CA2362390A1/en
Abandoned legal-status Critical Current

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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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
CA002362390A 1999-02-09 1999-08-11 Heteroaryl amidines, methylamidines and guanidines as protease inhibitors Abandoned CA2362390A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24706299A 1999-02-09 1999-02-09
US09/247,062 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
CA2362390A1 true CA2362390A1 (en) 2000-08-17

Family

ID=22933398

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002362390A Abandoned CA2362390A1 (en) 1999-02-09 1999-08-11 Heteroaryl amidines, methylamidines and guanidines as protease inhibitors

Country Status (19)

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

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003529536A (ja) * 1999-02-09 2003-10-07 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 Ｃ１ｓ介在疾患および状態の処置法、およびそれのための化合物および組成物
CA2484822A1 (en) * 2002-05-28 2003-12-04 3-Dimensional Pharmaceuticals, Inc. Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
DK1569912T3 (en) 2002-12-03 2015-06-29 Pharmacyclics 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
US8685369B2 (en) 2004-02-12 2014-04-01 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
EP2451796B1 (en) 2009-07-08 2013-04-17 Dermira (Canada), Inc. Tofa analogs useful in treating dermatological disorders or conditions
US20130109672A1 (en) 2010-04-29 2013-05-02 The United States Of America,As Represented By The Secretary, Department Of Health And Human Service Activators of human pyruvate kinase
CN103562202B (zh) * 2011-01-25 2016-09-14 密执安大学评议会 Bcl-2/bcl-xl抑制剂和使用它们的治疗方法
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
JP6424173B2 (ja) * 2013-02-04 2018-11-14 ヤンセン ファーマシューティカ エヌ．ベー． Ｆｌａｐ調節因子
CN111918865B (zh) * 2018-03-30 2023-10-27 住友化学株式会社 杂环化合物和含有该杂环化合物的有害节肢动物防除组合物
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

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4220654A (en) * 1979-06-04 1980-09-02 Merck & Co., Inc. Cyclic imidazole cyanoguanidines
US4424367A (en) * 1982-08-19 1984-01-03 Norwich Eaton Pharmaceuticals, Inc. 5-(4-Aminophenyl)-2-thiophenecarboximidamide hydrochloride hemihydrate
JPS59139357A (ja) * 1983-01-28 1984-08-10 Torii Yakuhin Kk アミジン誘導体
DE3427865A1 (de) * 1984-07-27 1986-02-06 Torii & Co., Tokio/Tokyo Amidinoverbindungen, verfahren zu deren herstellung und diese verbindungen enthaltende pharmazeutische mittel
US5084466A (en) * 1989-01-31 1992-01-28 Hoffmann-La Roche Inc. Novel carboxamide pyridine compounds which have useful pharmaceutical utility
US5340833A (en) * 1992-05-01 1994-08-23 Eisai Co., Ltd. Urokinase inhibitors
GB9312761D0 (en) * 1993-06-21 1993-08-04 Wellcome Found Amino acid derivatives
PT724435E (pt) * 1993-10-21 2002-11-29 Searle & Co Derivados amidino uteis como inibidores de oxido nitrico sintase
ZA951617B (en) * 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
US5612353A (en) * 1995-06-07 1997-03-18 Rhone-Poulenc Rorer Pharmaceuticals Inc. Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds
TW414795B (en) * 1996-07-01 2000-12-11 Yamanouchi Pharma Co Ltd A thiophene derivative and the pharmaceutical composition
DE19632773A1 (de) * 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren
PE121699A1 (es) * 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma Heterociclos biciclicos disustituidos como inhibidores de la trombina
WO1999037611A1 (de) * 1998-01-26 1999-07-29 Basf Aktiengesellschaft Heterocyclische amidine als kallikrein protease inhibitoren
CA2317761A1 (en) * 1998-01-26 1999-07-29 Basf Aktiengesellschaft Thrombin inhibitors
NZ506507A (en) * 1998-02-09 2003-08-29 Dimensional Pharm Inc Heteroaryl amidine, methylamidine or guanidine derivatives useful as urokinase inhibitors
AU1917999A (en) * 1998-03-31 1999-10-18 Warner-Lambert Company Quinoxalinones as serine protease inhibitors such as factor xa and thrombin
KR20010042296A (ko) * 1998-03-31 2001-05-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 세린 프로테아제 억제제로서의 벤즈옥사지논/벤조티아지논
JP2002509928A (ja) * 1998-03-31 2002-04-02 ワーナー−ランバート・カンパニー セリンプロテアーゼ阻害剤としてのキノロン

Also Published As

Publication number Publication date
WO2000047578A1 (en) 2000-08-17
IL144560A0 (en) 2002-05-23
NZ513701A (en) 2001-09-28
HUP0201475A2 (hu) 2003-10-28
CZ20012858A3 (cs) 2002-05-15
MXPA01008084A (es) 2004-09-10
KR20010098982A (ko) 2001-11-08
JP2002536446A (ja) 2002-10-29
AU5671799A (en) 2000-08-29
BG105866A (en) 2002-06-28
NO324887B1 (no) 2007-12-27
NO20013853L (no) 2001-10-09
EP1150979A1 (en) 2001-11-07
ZA200106849B (en) 2002-11-20
CN1337961A (zh) 2002-02-27
BR9917036A (pt) 2002-07-30
NO20013853D0 (no) 2001-08-07
PL351767A1 (en) 2003-06-16
SK11422001A3 (sk) 2002-04-04
EA200100882A1 (ru) 2002-04-25

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EEER Examination request
FZDE Discontinued