DE69902754T2 - 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 inhibitoren

Info

Publication number
DE69902754T2
DE69902754T2 DE69902754T DE69902754T DE69902754T2 DE 69902754 T2 DE69902754 T2 DE 69902754T2 DE 69902754 T DE69902754 T DE 69902754T DE 69902754 T DE69902754 T DE 69902754T DE 69902754 T2 DE69902754 T2 DE 69902754T2
Authority
DE
Germany
Prior art keywords
compounds
urokinase
inhibitors
methylamidines
amidines
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.)
Expired - Lifetime
Application number
DE69902754T
Other languages
English (en)
Other versions
DE69902754D1 (de
Inventor
R Illig
L Subasinghe
B Hoffman
J Wilson
Jonathan Rudolph
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
3 Dimensional Pharmaceuticals 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 3 Dimensional Pharmaceuticals Inc filed Critical 3 Dimensional Pharmaceuticals Inc
Application granted granted Critical
Publication of DE69902754D1 publication Critical patent/DE69902754D1/de
Publication of DE69902754T2 publication Critical patent/DE69902754T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • 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
DE69902754T 1998-02-09 1999-02-09 Heteroaryl-amidinen,-methylamidinen und -guanidinen als protease inhibitoren, insbesondere als urokinase inhibitoren Expired - Lifetime DE69902754T2 (de)

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 (2)

Publication Number Publication Date
DE69902754D1 DE69902754D1 (de) 2002-10-10
DE69902754T2 true DE69902754T2 (de) 2003-08-07

Family

ID=22117801

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69902754T Expired - Lifetime DE69902754T2 (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 (de)
JP (1) JP2002502852A (de)
AT (1) ATE223408T1 (de)
AU (1) AU765072B2 (de)
CA (1) CA2321025A1 (de)
DE (1) DE69902754T2 (de)
NZ (1) NZ506507A (de)
WO (1) WO1999040088A1 (de)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
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
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
NZ513701A (en) * 1999-02-09 2001-09-28 Dimensional Pharm Inc Heteroaryl amidines, methylamidines and guanidines as protease inhibitors
WO2002057273A1 (en) * 2001-01-20 2002-07-25 Trigen Limited Serine protease inhibitors comprising a hydrogen-bond acceptor
WO2002070517A2 (en) * 2001-03-02 2002-09-12 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
US7838560B2 (en) * 2002-03-11 2010-11-23 The Medicines Company (Leipzig) Gmbh Urokinase inhibitors, production and use thereof
AU2003251384B2 (en) * 2002-05-28 2009-01-29 3-Dimensional Pharmaceuticals, Inc. Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
EP1394159A1 (de) * 2002-08-13 2004-03-03 Warner-Lambert Company LLC Neue Thiophen-Derivate, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Zusammensetzungen
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
NZ544674A (en) * 2003-07-10 2009-03-31 Achillion Pharmaceuticals Inc Substituted arylthiourea derivatives useful as inhibitors of viral replication
US7674822B2 (en) 2004-11-24 2010-03-09 Wyeth PTP1b inhibitors
WO2006136419A2 (en) * 2005-06-24 2006-12-28 Wilex Ag Use of urokinase inhibitors for the treatment and/or prevention of neuropathological diseases
RU2425045C2 (ru) * 2005-12-27 2011-07-27 Ф. Хоффманн-Ля Рош Аг Производные арил-изоксазол-4-ил-имидазола
US20090324581A1 (en) 2006-05-09 2009-12-31 Daiichi Sankyo Company Limited Heteroarylamide lower carboxylic acid derivative
US7985763B2 (en) 2007-04-10 2011-07-26 National Health Research Institutes Hepatitis C virus inhibitors
WO2008154091A1 (en) 2007-06-08 2008-12-18 National Health Research Institutes Thiourea derivatives
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
CA2766643C (en) 2009-07-08 2017-01-03 Dermira (Canada), Inc. Tofa analogs useful in treating dermatological disorders or conditions
SG10201806370QA (en) * 2013-08-28 2018-08-30 Medivation Tech Llc Heterocyclic compounds and methods of use
JP2018507235A (ja) 2015-03-04 2018-03-15 メディベイション テクノロジーズ エルエルシー ステロール調節エレメント結合タンパク質（ｓｒｅｂｐ）阻害剤
CA2978627A1 (en) 2015-03-04 2016-09-09 Medivation Technologies, Inc. Srebp blockers for use in treating liver fibrosis, elevated cholesterol and insulin resistance

Family Cites Families (11)

* 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
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
EP0724435B1 (de) * 1993-10-21 2002-08-14 G.D. Searle & Co. Amidino-derivate nützlich als no synthase-hemmer
IL112795A (en) * 1994-03-04 2001-01-28 Astrazeneca Ab Derivatives of peptides as antithrombotic drugs, their preparation, and pharmaceutical preparations 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
KR100689923B1 (ko) * 1998-01-26 2007-03-09 애보트 게엠베하 운트 콤파니 카게 트롬빈 억제제
JP2002501044A (ja) * 1998-01-26 2002-01-15 ビーエーエスエフ アクチェンゲゼルシャフト カリクレインプロテアーゼ阻害剤としての複素環アミジン

Also Published As

Publication number Publication date
NZ506507A (en) 2003-08-29
DE69902754D1 (de) 2002-10-10
CA2321025A1 (en) 1999-08-12
EP1054886B1 (de) 2002-09-04
AU2666599A (en) 1999-08-23
EP1054886A1 (de) 2000-11-29
ATE223408T1 (de) 2002-09-15
AU765072B2 (en) 2003-09-11
JP2002502852A (ja) 2002-01-29
WO1999040088A1 (en) 1999-08-12

Similar Documents

Publication Publication Date Title
DE69902754T2 (de) Heteroaryl-amidinen,-methylamidinen und -guanidinen als protease inhibitoren, insbesondere als urokinase inhibitoren
GEP20074098B (en) Lactam-containing compounds and derivatives thereof as factor xa inhibitors
MY106529A (en) Series protease inhibitors
DE69736777D1 (de) Amidinohydrazone als protease-inhibitoren
MXPA01008084A (es) Heteroarilamidinas, metilamidinas y guanidinas como inhibidores de proteasa.
DE60028045D1 (de) Neue bernsteinsäure derivative als cysteine-protease-inhibitoren
ATE303988T1 (de) Inhibitoren von serin proteasen
MY136133A (en) New mandelic acid derivatives and their use as thrombin inhibitors
HUP0203130A2 (hu) Hexahidrofuro[2,3-b]furán-3-il-N-{3-(1,3-benzodioxol-5-il-szulfonil)-(izobutil)-amino-1-benzil-2-(hidroxi-propil)}-karbamát mint retrovírus-proteáz-gátló
MX9404114A (es) Nuevos derivados de peptidos.
TR199802536T2 (xx) Yeni amino asit t�revleri,trombin inhibit�rleri olarak kullan�lmalar�.
NZ333394A (en) Amidino derivatives and their use as thrombin inhibitors
ZA959819B (en) Substituted heterocylic compounds useful as inhibitors of (serine protease) human neutrophil elastase
MY116539A (en) New amino acid derivatives
TR200003028T2 (tr) Yeni ikame edilmiş amidler, bunların üretimi ve kullanımı.
ATE338030T1 (de) Amidine-inhibitoren der serine-proteasen
BR9612360A (pt) Inibidores de amidino protease
EE200000322A (et) Uued ühendid
BR9610876A (pt) Inibidores de protease de guanidino
ATE407116T1 (de) Neue amidino-derivate und deren verwendung als thrombin-inhibitoren
SE0102921D0 (sv) Pharmaceutically useful compounds

Legal Events

Date Code Title Description
8364 No opposition during term of opposition