ATE223408T1 - Heteroaryl-amidinen,-methylamidinen und - guanidinen als protease inhibitoren, insbesondere als urokinase inhibitoren - Google Patents
Heteroaryl-amidinen,-methylamidinen und - guanidinen als protease inhibitoren, insbesondere als urokinase inhibitorenInfo
- Publication number
- ATE223408T1 ATE223408T1 AT99906845T AT99906845T ATE223408T1 AT E223408 T1 ATE223408 T1 AT E223408T1 AT 99906845 T AT99906845 T AT 99906845T AT 99906845 T AT99906845 T AT 99906845T AT E223408 T1 ATE223408 T1 AT E223408T1
- Authority
- AT
- Austria
- Prior art keywords
- compounds
- urokinase
- inhibitors
- methylamidines
- amidines
- Prior art date
Links
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 239000002797 plasminogen activator inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 108090000435 Urokinase-type plasminogen activator Proteins 0.000 abstract 2
- 102000003990 Urokinase-type plasminogen activator Human genes 0.000 abstract 2
- 229960005356 urokinase Drugs 0.000 abstract 2
- 108090000317 Chymotrypsin Proteins 0.000 abstract 1
- 108010088842 Fibrinolysin Proteins 0.000 abstract 1
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 102000035195 Peptidases Human genes 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 108090000631 Trypsin Proteins 0.000 abstract 1
- 102000004142 Trypsin Human genes 0.000 abstract 1
- 229960002376 chymotrypsin Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 229940012957 plasmin Drugs 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229960001322 trypsin Drugs 0.000 abstract 1
- 239000012588 trypsin Substances 0.000 abstract 1
- 108010036927 trypsin-like serine protease Proteins 0.000 abstract 1
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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P15/18—Feminine 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
- A61P17/06—Antipsoriatics
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (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)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Gynecology & Obstetrics (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7411098P | 1998-02-09 | 1998-02-09 | |
| PCT/US1999/002784 WO1999040088A1 (en) | 1998-02-09 | 1999-02-09 | Heteroaryl amidines, methylamidines and guanidines as protease inhibitors, in particular as urokinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE223408T1 true ATE223408T1 (de) | 2002-09-15 |
Family
ID=22117801
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT99906845T ATE223408T1 (de) | 1998-02-09 | 1999-02-09 | Heteroaryl-amidinen,-methylamidinen und - guanidinen als protease inhibitoren, insbesondere als urokinase inhibitoren |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP1054886B1 (enExample) |
| JP (1) | JP2002502852A (enExample) |
| AT (1) | ATE223408T1 (enExample) |
| AU (1) | AU765072B2 (enExample) |
| CA (1) | CA2321025A1 (enExample) |
| DE (1) | DE69902754T2 (enExample) |
| NZ (1) | NZ506507A (enExample) |
| WO (1) | WO1999040088A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6291514B1 (en) | 1998-02-09 | 2001-09-18 | 3-Dimensional Pharmaceuticals, Inc. | Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors |
| EP1150979A1 (en) * | 1999-02-09 | 2001-11-07 | 3-Dimensional Pharmaceuticals, Inc. | Heteroaryl amidines, methylamidines and guanidines as protease inhibitors |
| WO2000047194A2 (en) * | 1999-02-09 | 2000-08-17 | 3-Dimensional Pharmaceuticals, Inc. | METHODS OF TREATING C1s-MEDIATED DISEASES AND CONDITIONS, AND COMPOUNDS AND COMPOSITIONS THEREFOR |
| WO2002057273A1 (en) * | 2001-01-20 | 2002-07-25 | Trigen Limited | Serine protease inhibitors comprising a hydrogen-bond acceptor |
| AU2002242500A1 (en) * | 2001-03-02 | 2002-09-19 | Merck Frosst Canada And Co. | Cathepsin cysteine protease inhibitors |
| ATE399175T1 (de) * | 2002-03-11 | 2008-07-15 | Curacyte Ag | Hemmstoffe der urokinase, ihre herstellung und verwendung |
| US7109354B2 (en) * | 2002-05-28 | 2006-09-19 | 3-Dimensional Pharmaceuticals, Inc. | Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions |
| EP1394159A1 (fr) * | 2002-08-13 | 2004-03-03 | Warner-Lambert Company LLC | Nouveaux dérivés de thiophène, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent |
| GB0315111D0 (en) | 2003-06-27 | 2003-07-30 | Cancer Rec Tech Ltd | Substituted 5-membered ring compounds and their use |
| US7482376B2 (en) * | 2003-07-03 | 2009-01-27 | 3-Dimensional Pharmaceuticals, Inc. | Conjugated complement cascade inhibitors |
| EA010017B1 (ru) * | 2003-07-10 | 2008-06-30 | Ачиллион Фармасьютикалз, Инк. | Замещённые арилтиомочевины, применимые в качестве ингибиторов репликации вирусов |
| US7674822B2 (en) | 2004-11-24 | 2010-03-09 | Wyeth | PTP1b inhibitors |
| ES2329286T3 (es) * | 2005-06-24 | 2009-11-24 | Wilex Ag | Uso de inhibidores de uroquinasa para el tratamiento y/o la prevencion de enfermedades neuropatologicas. |
| PT1968973E (pt) * | 2005-12-27 | 2011-12-09 | Hoffmann La Roche | Derivados de aril-isoxazol-4-il-imidazol |
| JPWO2007129745A1 (ja) | 2006-05-09 | 2009-09-17 | 第一三共株式会社 | ヘテロアリールアミド低級カルボン酸誘導体 |
| US7985763B2 (en) | 2007-04-10 | 2011-07-26 | National Health Research Institutes | Hepatitis C virus inhibitors |
| TW200848016A (en) | 2007-06-08 | 2008-12-16 | Nat Health Research Institutes | Thiourea compound and composition of treating hepatitis C virus infection |
| TWI361808B (en) | 2008-01-08 | 2012-04-11 | Nat Health Research Institutes | Imidazolidinone and imidazolidinethione derivatives |
| US8198284B2 (en) | 2008-04-30 | 2012-06-12 | National Health Research Institutes | Treatment of neurodegenerative disorders with thiourea compounds |
| SG176983A1 (en) | 2009-07-08 | 2012-02-28 | Dermira Canada Inc | Tofa analogs useful in treating dermatological disorders or conditions |
| DK3038622T3 (en) * | 2013-08-28 | 2018-07-16 | Medivation Tech Llc | HETEROCYCLIC RELATIONS AND PROCEDURES FOR USE |
| EP3265088A1 (en) | 2015-03-04 | 2018-01-10 | Medivation Technologies LLC | Srebp blockers for use in treating liver fibrosis, elevated cholesterol and insulin resistance |
| WO2016141258A1 (en) | 2015-03-04 | 2016-09-09 | Medivation Technologies, Inc. | Sterol regulatory element-binding proteins (srebps) inhibitors |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4220654A (en) * | 1979-06-04 | 1980-09-02 | Merck & Co., Inc. | Cyclic imidazole cyanoguanidines |
| 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 |
| DE69431194T2 (de) * | 1993-10-21 | 2002-12-12 | G.D. Searle & Co., Chicago | Amidino-derivate nützlich als no synthase-hemmer |
| 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 (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 |
| CN1289341A (zh) * | 1998-01-26 | 2001-03-28 | Basf公司 | 凝血酶抑制剂 |
| EP1049673A1 (de) * | 1998-01-26 | 2000-11-08 | Basf Aktiengesellschaft | Heterocyclische amidine als kallikrein protease inhibitoren |
-
1999
- 1999-02-09 DE DE69902754T patent/DE69902754T2/de not_active Expired - Lifetime
- 1999-02-09 JP JP2000530517A patent/JP2002502852A/ja active Pending
- 1999-02-09 EP EP99906845A patent/EP1054886B1/en not_active Expired - Lifetime
- 1999-02-09 CA CA002321025A patent/CA2321025A1/en not_active Abandoned
- 1999-02-09 AU AU26665/99A patent/AU765072B2/en not_active Ceased
- 1999-02-09 NZ NZ506507A patent/NZ506507A/en unknown
- 1999-02-09 AT AT99906845T patent/ATE223408T1/de not_active IP Right Cessation
- 1999-02-09 WO PCT/US1999/002784 patent/WO1999040088A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| WO1999040088A1 (en) | 1999-08-12 |
| DE69902754T2 (de) | 2003-08-07 |
| AU765072B2 (en) | 2003-09-11 |
| AU2666599A (en) | 1999-08-23 |
| DE69902754D1 (de) | 2002-10-10 |
| EP1054886B1 (en) | 2002-09-04 |
| CA2321025A1 (en) | 1999-08-12 |
| EP1054886A1 (en) | 2000-11-29 |
| JP2002502852A (ja) | 2002-01-29 |
| NZ506507A (en) | 2003-08-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ATE223408T1 (de) | Heteroaryl-amidinen,-methylamidinen und - guanidinen als protease inhibitoren, insbesondere als urokinase inhibitoren | |
| MY106529A (en) | Series protease inhibitors | |
| GEP20074098B (en) | Lactam-containing compounds and derivatives thereof as factor xa inhibitors | |
| ATE341317T1 (de) | Amidinohydrazone als protease-inhibitoren | |
| DE60028045D1 (de) | Neue bernsteinsäure derivative als cysteine-protease-inhibitoren | |
| MXPA01008084A (es) | Heteroarilamidinas, metilamidinas y guanidinas como inhibidores de proteasa. | |
| NZ333394A (en) | Amidino derivatives and their use as thrombin inhibitors | |
| UA70976C2 (uk) | (гетеро)арилбіциклічні гетероарильні похідні, їх одержання та використання як інгібіторів протеаз | |
| MY136133A (en) | New mandelic acid derivatives and their use as thrombin inhibitors | |
| ATE303988T1 (de) | Inhibitoren von serin proteasen | |
| MX9404114A (es) | Nuevos derivados de peptidos. | |
| ZA959819B (en) | Substituted heterocylic compounds useful as inhibitors of (serine protease) human neutrophil elastase | |
| TR199802536T2 (xx) | Yeni amino asit t�revleri,trombin inhibit�rleri olarak kullan�lmalar�. | |
| NO930517L (no) | Benzimidazolylderivater, legemidler inneholdende disse, og fremgangsmaate for deres fremstilling | |
| BR9612360A (pt) | Inibidores de amidino protease | |
| NO20002848D0 (no) | Nye forbindelser | |
| BR9610876A (pt) | Inibidores de protease de guanidino | |
| DE60135665D1 (de) | Neue amidino-derivate und deren verwendung als thrombin-inhibitoren | |
| SE0102921D0 (sv) | Pharmaceutically useful compounds |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |