EA200100882A1 - AMETHINE, METHYLAMIDINE AND GUANIDA HEAT HYDROARIAL PRODUCTS (OPTIONS) MATERIALS (OPTIONS), PHARMACEUTICAL COMPOSITION (OPTIONS), METHOD FOR INHIBING PROTEASE (OPTIONS) AND SPODA SPEEDS (OPTIONS), SPEED INHIBITION (OPTIONS) AND SPODA PRODUCTS (OPTIONS); - Google Patents

AMETHINE, METHYLAMIDINE AND GUANIDA HEAT HYDROARIAL PRODUCTS (OPTIONS) MATERIALS (OPTIONS), PHARMACEUTICAL COMPOSITION (OPTIONS), METHOD FOR INHIBING PROTEASE (OPTIONS) AND SPODA SPEEDS (OPTIONS), SPEED INHIBITION (OPTIONS) AND SPODA PRODUCTS (OPTIONS);

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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
Russian (ru)
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.
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Application filed by 3-Дименшенл Фамэсьютикэлс, Инк. filed Critical 3-Дименшенл Фамэсьютикэлс, Инк.
Publication of EA200100882A1 publication Critical patent/EA200100882A1/en

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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

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  • 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)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (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

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.The present invention is directed to compounds of formula (I), wherein X is O, S, or NR, where R — R, Y, and Z are as defined herein, as well as their hydrates, solvates, or pharmaceutically acceptable salts. Methods for preparing compounds of formula (I) are also described. 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 compounds exhibit direct selective inhibition of urokinase or are intermediate products used to produce compounds with such activity. The international application was published together with an international search report.

EA200100882A 1999-02-09 1999-08-11 AMETHINE, METHYLAMIDINE AND GUANIDA HEAT HYDROARIAL PRODUCTS (OPTIONS) MATERIALS (OPTIONS), PHARMACEUTICAL COMPOSITION (OPTIONS), METHOD FOR INHIBING PROTEASE (OPTIONS) AND SPODA SPEEDS (OPTIONS), SPEED INHIBITION (OPTIONS) AND SPODA PRODUCTS (OPTIONS); EA200100882A1 (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
EA200100882A1 true EA200100882A1 (en) 2002-04-25

Family

ID=22933398

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200100882A EA200100882A1 (en) 1999-02-09 1999-08-11 AMETHINE, METHYLAMIDINE AND GUANIDA HEAT HYDROARIAL PRODUCTS (OPTIONS) MATERIALS (OPTIONS), PHARMACEUTICAL COMPOSITION (OPTIONS), METHOD FOR INHIBING PROTEASE (OPTIONS) AND SPODA SPEEDS (OPTIONS), SPEED INHIBITION (OPTIONS) AND SPODA PRODUCTS (OPTIONS);

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)

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ZA200408711B (en) * 2002-05-28 2006-10-25 Dimensional Pharamaceuticals I Novel thiophene amidines, composition 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
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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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Also Published As

Publication number Publication date
JP2002536446A (en) 2002-10-29
KR20010098982A (en) 2001-11-08
PL351767A1 (en) 2003-06-16
CA2362390A1 (en) 2000-08-17
SK11422001A3 (en) 2002-04-04
NO20013853L (en) 2001-10-09
MXPA01008084A (en) 2004-09-10
IL144560A0 (en) 2002-05-23
NO20013853D0 (en) 2001-08-07
NO324887B1 (en) 2007-12-27
BR9917036A (en) 2002-07-30
CN1337961A (en) 2002-02-27
CZ20012858A3 (en) 2002-05-15
WO2000047578A1 (en) 2000-08-17
NZ513701A (en) 2001-09-28
ZA200106849B (en) 2002-11-20
AU5671799A (en) 2000-08-29
BG105866A (en) 2002-06-28
EP1150979A1 (en) 2001-11-07
HUP0201475A2 (en) 2003-10-28

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