WO1999026926A1 - Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors - Google Patents

Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors Download PDF

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Publication number
WO1999026926A1
WO1999026926A1 PCT/US1998/025185 US9825185W WO9926926A1 WO 1999026926 A1 WO1999026926 A1 WO 1999026926A1 US 9825185 W US9825185 W US 9825185W WO 9926926 A1 WO9926926 A1 WO 9926926A1
Authority
WO
WIPO (PCT)
Prior art keywords
methyl
amino
alkyl
compound
pyridinone
Prior art date
Application number
PCT/US1998/025185
Other languages
English (en)
French (fr)
Inventor
Tianbao Lu
Bruce E. Tomczuk
Thomas P. Markotan
Colleen Siedem
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.
Priority to BR9815325-0A priority Critical patent/BR9815325A/pt
Priority to EP98962838A priority patent/EP1036063B1/en
Priority to CA002311969A priority patent/CA2311969A1/en
Priority to DE69836346T priority patent/DE69836346T2/de
Priority to JP2000522084A priority patent/JP2001524467A/ja
Priority to AU17991/99A priority patent/AU751412B2/en
Priority to EA200000578A priority patent/EA004180B1/ru
Publication of WO1999026926A1 publication Critical patent/WO1999026926A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
PCT/US1998/025185 1997-11-26 1998-11-25 Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors WO1999026926A1 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
BR9815325-0A BR9815325A (pt) 1997-11-26 1998-11-25 Heteroaril, aminoguanidinas e alcóxiguanidinas eseu uso como inibidores da protease
EP98962838A EP1036063B1 (en) 1997-11-26 1998-11-25 Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
CA002311969A CA2311969A1 (en) 1997-11-26 1998-11-25 Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
DE69836346T DE69836346T2 (de) 1997-11-26 1998-11-25 Heteroaryl aminoguanidin- und alkoxyguanidinderivate und ihre verwendung als proteasehemmer
JP2000522084A JP2001524467A (ja) 1997-11-26 1998-11-25 ヘテロアリールアミノグアニジンおよびアルコキシグアニジンおよびプロテアーゼインヒビターとしてのこれらの使用
AU17991/99A AU751412B2 (en) 1997-11-26 1998-11-25 Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
EA200000578A EA004180B1 (ru) 1997-11-26 1998-11-25 Гетероарильные производные аминогуанидинов и алкоксигуанидинов (варианты), способ их получения и их применение в качестве ингибиторов протеаз

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US6647597P 1997-11-26 1997-11-26
US6732497P 1997-12-05 1997-12-05
US7910798P 1998-03-23 1998-03-23
US60/066,475 1998-03-23
US60/079,107 1998-03-23
US60/067,324 1998-03-23

Publications (1)

Publication Number Publication Date
WO1999026926A1 true WO1999026926A1 (en) 1999-06-03

Family

ID=27370979

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1998/025185 WO1999026926A1 (en) 1997-11-26 1998-11-25 Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors

Country Status (14)

Country Link
US (8) US6037356A (US06566379-20030520-C00113.png)
EP (1) EP1036063B1 (US06566379-20030520-C00113.png)
JP (1) JP2001524467A (US06566379-20030520-C00113.png)
AR (1) AR016702A1 (US06566379-20030520-C00113.png)
AT (1) ATE344246T1 (US06566379-20030520-C00113.png)
AU (1) AU751412B2 (US06566379-20030520-C00113.png)
BR (1) BR9815325A (US06566379-20030520-C00113.png)
CA (1) CA2311969A1 (US06566379-20030520-C00113.png)
DE (1) DE69836346T2 (US06566379-20030520-C00113.png)
EA (1) EA004180B1 (US06566379-20030520-C00113.png)
ES (1) ES2274587T3 (US06566379-20030520-C00113.png)
PL (1) PL340560A1 (US06566379-20030520-C00113.png)
TW (1) TWI222441B (US06566379-20030520-C00113.png)
WO (1) WO1999026926A1 (US06566379-20030520-C00113.png)

Cited By (30)

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WO1999064446A1 (en) * 1998-06-11 1999-12-16 3-Dimensional Pharmaceuticals, Inc. Pyrazinone protease inhibitors
WO2001004117A1 (en) * 1999-07-09 2001-01-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl protease inhibitors and diagnostic imaging agents
WO2001087852A1 (en) * 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
WO2002012193A1 (en) * 2000-08-07 2002-02-14 3-Dimensional Pharmaceuticals, Inc. Tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidines as integrin antagonists
WO2002012207A1 (en) * 2000-08-04 2002-02-14 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine protease inhibitors
WO2002028825A2 (en) * 2000-10-06 2002-04-11 3-Dimensional Pharmaceuticals, Inc. Aminopyridinyl-, aminoguanidinyl- and alkoxyguanidinyl- substituted phenyl acetamides as protease inhibitors
US6476016B2 (en) 2000-07-17 2002-11-05 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine pyrazinones as protease inhibitors
US6486174B2 (en) 2000-08-07 2002-11-26 3-Dimensional Pharmaceuticals, Inc. Tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidines as integrin antagonists
WO2003007984A1 (de) * 2001-07-16 2003-01-30 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verwendung von thrombin-inhibitoren zur behandlung von arthritis
US6624180B2 (en) 2000-11-20 2003-09-23 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6660885B2 (en) 2000-03-13 2003-12-09 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6686484B2 (en) 2000-04-17 2004-02-03 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
US6693121B2 (en) 2000-04-05 2004-02-17 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
WO2004091613A2 (en) * 2003-04-10 2004-10-28 3-Dimensional Pharmaceuticals, Inc. Substituted phenyl acetamides and their use as protease inhibitors
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
US6875791B2 (en) 2000-04-05 2005-04-05 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
WO2005110988A1 (en) * 2004-05-07 2005-11-24 Janssen Pharmaceutica, N.V. Pyridone compounds as inhibitors of bacterial type iii protein secretion systems
US6969715B2 (en) 2001-10-03 2005-11-29 Pharmacia Corporation 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
US7105559B2 (en) 2001-10-03 2006-09-12 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
US7262211B2 (en) 2001-12-04 2007-08-28 Dendreon Corporation Aromatic heterocyclic non-covalent inhibitors of urokinase and blood vessel formation
US8518934B2 (en) 2008-06-11 2013-08-27 Shonogi & Co., Ltd. Oxycarbamoyl compounds and the use thereof
US8563732B2 (en) 2007-05-31 2013-10-22 Shionogi & Co., Ltd. Oxyimino compounds and the use thereof
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TWI222441B (en) * 1997-11-26 2004-10-21 Dimensional Pharm Inc Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
NZ508005A (en) * 1998-04-24 2003-05-30 Dimensional Pharm Inc Amino acid amidinohydrazones, alkoxyguanidines and aminoguanidines useful as serine protease inhibitors
US6908919B2 (en) * 1999-05-19 2005-06-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6906068B1 (en) 1999-05-19 2005-06-14 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4 - triazinones useful as anticoagulants
PL352403A1 (en) * 1999-05-19 2003-08-25 Pharmacia Corp Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of coagulation cascade
AU5046600A (en) 1999-05-27 2000-12-18 3-Dimensional Pharmaceuticals, Inc. Oxazaheterocycles as protease inhibitors
JP2003509409A (ja) 1999-09-13 2003-03-11 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 アザシクロアルカノンセリンプロテアーゼ阻害剤
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WO2010134345A1 (ja) * 2009-05-20 2010-11-25 積水メディカル株式会社 血液凝固時間延長剤
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AU2011349022B2 (en) 2010-12-21 2017-04-13 The Medicines Company (Leipzig) Gmbh Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa
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Cited By (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999064446A1 (en) * 1998-06-11 1999-12-16 3-Dimensional Pharmaceuticals, Inc. Pyrazinone protease inhibitors
EP1589029A3 (en) * 1998-06-11 2006-01-18 Johnson & Johnson Pharmaceutical Research & Development L.L.C. Pyrazinone protease inhibitors
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6870056B1 (en) 1999-05-19 2005-03-22 Pharmacia Corporation Substitituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
US6420397B1 (en) 1999-07-09 2002-07-16 3-Dimensional Pharmaceuticals, Inc. Heteroaryl protease inhibitors and diagnostic imaging agents
WO2001004117A1 (en) * 1999-07-09 2001-01-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl protease inhibitors and diagnostic imaging agents
US6852761B2 (en) 2000-03-13 2005-02-08 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
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US6350764B2 (en) 2002-02-26
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US7402586B2 (en) 2008-07-22
US20040106633A1 (en) 2004-06-03
CA2311969A1 (en) 1999-06-03
BR9815325A (pt) 2001-12-26
US6566379B1 (en) 2003-05-20
DE69836346T2 (de) 2007-05-24
ATE344246T1 (de) 2006-11-15
AU1799199A (en) 1999-06-15
AU751412B2 (en) 2002-08-15
TWI222441B (en) 2004-10-21
US6037356A (en) 2000-03-14
US6706021B2 (en) 2004-03-16
DE69836346D1 (de) 2006-12-14
US6245763B1 (en) 2001-06-12
EP1036063A1 (en) 2000-09-20
US20030087921A1 (en) 2003-05-08
ES2274587T3 (es) 2007-05-16
US6472399B2 (en) 2002-10-29
EA200000578A1 (ru) 2001-02-26
US20030225115A1 (en) 2003-12-04
EP1036063B1 (en) 2006-11-02
US20020007070A1 (en) 2002-01-17
US20060211719A1 (en) 2006-09-21
JP2001524467A (ja) 2001-12-04
PL340560A1 (en) 2001-02-12
US20020086872A1 (en) 2002-07-04
US7029654B2 (en) 2006-04-18

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