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
Links
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
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.
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU3998400A (en) * | 1999-02-09 | 2000-08-29 | 3-Dimensional Pharmaceuticals, Inc. | Methods of treating c1s-mediated diseases and conditions, and compounds and compositions therefor |
PL372246A1 (en) * | 2002-05-28 | 2005-07-11 | 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 |
NZ544674A (en) * | 2003-07-10 | 2009-03-31 | Achillion Pharmaceuticals Inc | Substituted arylthiourea derivatives useful as inhibitors of viral replication |
KR20070029148A (en) | 2004-02-12 | 2007-03-13 | 몰레큘러 인사이트 파마슈티칼스, 인크. | 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 |
MX2012000435A (en) | 2009-07-08 | 2012-06-01 | Dermira Canada Inc | Tofa analogs useful in treating dermatological disorders or conditions. |
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 |
SG192126A1 (en) * | 2011-01-25 | 2013-09-30 | Univ Michigan | Bcl-2/bcl-xl inhibitors and therapeutic methods 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 |
US9745328B2 (en) | 2013-02-04 | 2017-08-29 | Janssen Pharmaceutica Nv | Flap modulators |
TWI644899B (en) | 2013-02-04 | 2018-12-21 | 健生藥品公司 | Flap modulators |
BR112020019804A2 (en) * | 2018-03-30 | 2021-01-05 | Sumitomo Chemical Company, Limited | HETEROCYCLIC COMPOUND AND ARTHROPOD FEVER 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 |
Family Cites Families (19)
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 (en) * | 1983-01-28 | 1984-08-10 | Torii Yakuhin Kk | Amidine derivative |
DE3427865A1 (en) * | 1984-07-27 | 1986-02-06 | Torii & Co., Tokio/Tokyo | Amidino compounds, process for their preparation and pharmaceutical compositions containing these compounds |
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 |
US5821267A (en) * | 1993-10-21 | 1998-10-13 | G.D. Searle & Co. | Amidino derivatives useful as nitric oxide synthase inhibitors |
IL112795A (en) * | 1994-03-04 | 2001-01-28 | Astrazeneca Ab | Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them |
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 (en) * | 1996-08-14 | 1998-02-19 | Basf Ag | New thrombin inhibitors |
PE121699A1 (en) * | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | BICYCLE HETERO CYCLES DISSTITUTED AS INHIBITORS OF THROMBIN |
EP1051431A1 (en) * | 1998-01-26 | 2000-11-15 | Basf Aktiengesellschaft | Thrombin inhibitors |
WO1999037611A1 (en) * | 1998-01-26 | 1999-07-29 | Basf Aktiengesellschaft | Heterocyclic amidines as callicrein protease inhibitors |
EP1054886B1 (en) * | 1998-02-09 | 2002-09-04 | 3-Dimensional Pharmaceuticals, Inc. | Heteroaryl amidines, methylamidines and guanidines as protease inhibitors, in particular as urokinase inhibitors |
PL343112A1 (en) * | 1998-03-31 | 2001-07-30 | Warner Lambert Co | Quinolones as serine protease inhibitors |
JP2002509925A (en) * | 1998-03-31 | 2002-04-02 | ワーナー−ランバート・カンパニー | Benzoxazinone / benzothiazinone as serine protease inhibitor |
JP2002509923A (en) * | 1998-03-31 | 2002-04-02 | ワーナー−ランバート・カンパニー | Quinoxalinones as serine protease inhibitors such as factor Xa and thrombin |
-
1999
- 1999-08-11 EA EA200100882A patent/EA200100882A1/en unknown
- 1999-08-11 KR KR1020017010094A patent/KR20010098982A/en not_active Application Discontinuation
- 1999-08-11 JP JP2000598498A patent/JP2002536446A/en active Pending
- 1999-08-11 SK SK1142-2001A patent/SK11422001A3/en unknown
- 1999-08-11 CZ CZ20012858A patent/CZ20012858A3/en unknown
- 1999-08-11 CN CN99816415A patent/CN1337961A/en active Pending
- 1999-08-11 PL PL99351767A patent/PL351767A1/en not_active Application Discontinuation
- 1999-08-11 EP EP99943667A patent/EP1150979A1/en not_active Withdrawn
- 1999-08-11 HU HU0201475A patent/HUP0201475A2/en unknown
- 1999-08-11 AU AU56717/99A patent/AU5671799A/en not_active Abandoned
- 1999-08-11 NZ NZ513701A patent/NZ513701A/en not_active Application Discontinuation
- 1999-08-11 BR BR9917036-1A patent/BR9917036A/en not_active IP Right Cessation
- 1999-08-11 IL IL14456099A patent/IL144560A0/en unknown
- 1999-08-11 MX MXPA01008084A patent/MXPA01008084A/en unknown
- 1999-08-11 CA CA002362390A patent/CA2362390A1/en not_active Abandoned
- 1999-08-11 WO PCT/US1999/018065 patent/WO2000047578A1/en not_active Application Discontinuation
-
2001
- 2001-08-07 NO NO20013853A patent/NO324887B1/en not_active IP Right Cessation
- 2001-08-20 ZA ZA200106849A patent/ZA200106849B/en unknown
- 2001-09-01 BG BG105866A patent/BG105866A/en unknown
Also Published As
Publication number | Publication date |
---|---|
PL351767A1 (en) | 2003-06-16 |
NO20013853D0 (en) | 2001-08-07 |
KR20010098982A (en) | 2001-11-08 |
HUP0201475A2 (en) | 2003-10-28 |
ZA200106849B (en) | 2002-11-20 |
IL144560A0 (en) | 2002-05-23 |
EA200100882A1 (en) | 2002-04-25 |
CZ20012858A3 (en) | 2002-05-15 |
CN1337961A (en) | 2002-02-27 |
AU5671799A (en) | 2000-08-29 |
NO324887B1 (en) | 2007-12-27 |
NO20013853L (en) | 2001-10-09 |
SK11422001A3 (en) | 2002-04-04 |
JP2002536446A (en) | 2002-10-29 |
BG105866A (en) | 2002-06-28 |
WO2000047578A1 (en) | 2000-08-17 |
EP1150979A1 (en) | 2001-11-07 |
CA2362390A1 (en) | 2000-08-17 |
BR9917036A (en) | 2002-07-30 |
NZ513701A (en) | 2001-09-28 |
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