MXPA01008084A - Heteroaryl amidines, methylamidines and guanidines as protease inhibitors. - Google Patents

Heteroaryl amidines, methylamidines and guanidines as protease inhibitors.

Info

Publication number
MXPA01008084A
MXPA01008084A MXPA01008084A MXPA01008084A MXPA01008084A MX PA01008084 A MXPA01008084 A MX PA01008084A MX PA01008084 A MXPA01008084 A MX PA01008084A MX PA01008084 A MXPA01008084 A MX PA01008084A MX PA01008084 A MXPA01008084 A MX PA01008084A
Authority
MX
Mexico
Prior art keywords
compounds
methylamidines
guanidines
protease inhibitors
urokinase
Prior art date
Application number
MXPA01008084A
Other languages
Spanish (es)
Inventor
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 MXPA01008084A publication Critical patent/MXPA01008084A/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/26Heterocyclic 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
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (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)

Abstract

The present invention is directed to compounds of Formula (I) wherein X is O, S or NR7 and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula (I). The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
MXPA01008084A 1999-02-09 1999-08-11 Heteroaryl amidines, methylamidines and guanidines as protease inhibitors. MXPA01008084A (en)

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
MXPA01008084A true MXPA01008084A (en) 2004-09-10

Family

ID=22933398

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA01008084A MXPA01008084A (en) 1999-02-09 1999-08-11 Heteroaryl amidines, methylamidines and guanidines as protease inhibitors.

Country Status (19)

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

Families Citing this family (16)

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JP2003529536A (en) * 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 Methods of treating C1s-mediated diseases and conditions, and compounds and compositions therefor
EP1569912B1 (en) 2002-12-03 2015-04-29 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
KR20050009720A (en) * 2002-05-28 2005-01-25 3-디멘져널 파마슈티칼즈 인코오포레이티드 Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
US7482376B2 (en) 2003-07-03 2009-01-27 3-Dimensional Pharmaceuticals, Inc. Conjugated complement cascade inhibitors
BRPI0412502A (en) * 2003-07-10 2006-09-19 Achillion Pharmaceuticals Inc substituted arylthiourea derivatives useful as viral replication inhibitors
CN102219743A (en) 2004-02-12 2011-10-19 分子制药洞察公司 Technetium- and rhenium-bis(heteroaryl) complexes, and methods of use thereof
WO2010042867A2 (en) 2008-10-09 2010-04-15 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
WO2011005660A1 (en) 2009-07-08 2011-01-13 Valocor Therapeutics, 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
JP5998152B2 (en) * 2011-01-25 2016-09-28 ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン BCL-2 / BCL-XL inhibitor and therapeutic method using the same
AR086744A1 (en) * 2011-06-28 2014-01-22 Nippon Soda Co HETEROCICLIC COMPOUND CONTAINING NITROGEN AND FUNGICIDE FOR USE IN AGRICULTURE AND GARDENING
EP2606726A1 (en) * 2011-12-21 2013-06-26 Bayer CropScience AG N-Arylamidine-substituted trifluoroethylsulfide derivatives as acaricides and insecticides
TWI644899B (en) 2013-02-04 2018-12-21 健生藥品公司 Flap modulators
JP6424173B2 (en) 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 regulator
JP7301042B2 (en) * 2018-03-30 2023-06-30 住友化学株式会社 Heterocyclic compound and harmful arthropod control composition containing the same
CN109020837A (en) * 2018-07-27 2018-12-18 广东省石油与精细化工研究院 A kind of preparation method of 2- substituted-phenyl-B amidine hydrochloric acid salt

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US4220654A (en) * 1979-06-04 1980-09-02 Merck & Co., Inc. Cyclic imidazole cyanoguanidines
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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
ES2181726T3 (en) * 1993-10-21 2003-03-01 Searle & Co USED AMIDINODERIVATES AS NITRICO SINTASA OXIDE INHIBITORS.
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TW414795B (en) * 1996-07-01 2000-12-11 Yamanouchi Pharma Co Ltd A thiophene derivative and the pharmaceutical composition
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AU2424499A (en) * 1998-01-26 1999-08-09 Basf Aktiengesellschaft Heterocyclic amidines as callicrein protease inhibitors
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Also Published As

Publication number Publication date
WO2000047578A1 (en) 2000-08-17
NZ513701A (en) 2001-09-28
PL351767A1 (en) 2003-06-16
NO20013853D0 (en) 2001-08-07
HUP0201475A2 (en) 2003-10-28
NO20013853L (en) 2001-10-09
KR20010098982A (en) 2001-11-08
EP1150979A1 (en) 2001-11-07
NO324887B1 (en) 2007-12-27
JP2002536446A (en) 2002-10-29
CA2362390A1 (en) 2000-08-17
SK11422001A3 (en) 2002-04-04
CN1337961A (en) 2002-02-27
AU5671799A (en) 2000-08-29
IL144560A0 (en) 2002-05-23
BR9917036A (en) 2002-07-30
BG105866A (en) 2002-06-28
ZA200106849B (en) 2002-11-20
CZ20012858A3 (en) 2002-05-15
EA200100882A1 (en) 2002-04-25

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