WO1999005096A3 - Urokinase inhibitors - Google Patents

Urokinase inhibitors Download PDF

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Publication number
WO1999005096A3
WO1999005096A3 PCT/US1998/015386 US9815386W WO9905096A3 WO 1999005096 A3 WO1999005096 A3 WO 1999005096A3 US 9815386 W US9815386 W US 9815386W WO 9905096 A3 WO9905096 A3 WO 9905096A3
Authority
WO
WIPO (PCT)
Prior art keywords
urokinase
urokinase inhibitors
inhibitors
inhibiting
mammal
Prior art date
Application number
PCT/US1998/015386
Other languages
French (fr)
Other versions
WO1999005096A2 (en
Inventor
Andrew G Geyer
William J Mcclellan
Todd W Rockway
Kent D Stewart
Moshe Weitzberg
Michael D Wendt
Original Assignee
Abbott Lab
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
Priority to PL98339429A priority Critical patent/PL339429A1/en
Application filed by Abbott Lab filed Critical Abbott Lab
Priority to CA002294300A priority patent/CA2294300A1/en
Priority to BR9811099-3A priority patent/BR9811099A/en
Priority to JP51012199A priority patent/JP2002512636A/en
Priority to EP98937082A priority patent/EP1000018A2/en
Priority to IL13336898A priority patent/IL133368A0/en
Priority to SK1748-99A priority patent/SK174899A3/en
Priority to AU85874/98A priority patent/AU8587498A/en
Priority to HU0100353A priority patent/HUP0100353A3/en
Publication of WO1999005096A2 publication Critical patent/WO1999005096A2/en
Publication of WO1999005096A3 publication Critical patent/WO1999005096A3/en
Priority to BG103981A priority patent/BG103981A/en
Priority to NO996578A priority patent/NO996578L/en

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
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    • 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
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    • A61P15/18—Feminine contraceptives
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    • 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
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
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Abstract

Compounds having formula (I) are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.
PCT/US1998/015386 1997-07-25 1998-07-24 Urokinase inhibitors WO1999005096A2 (en)

Priority Applications (11)

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IL13336898A IL133368A0 (en) 1997-07-25 1998-07-24 Urokinase inhibitors
CA002294300A CA2294300A1 (en) 1997-07-25 1998-07-24 Urokinase inhibitors
BR9811099-3A BR9811099A (en) 1997-07-25 1998-07-24 Urokinase inhibitors
JP51012199A JP2002512636A (en) 1997-07-25 1998-07-24 Urokinase inhibitors
EP98937082A EP1000018A2 (en) 1997-07-25 1998-07-24 Urokinase inhibitors
PL98339429A PL339429A1 (en) 1997-07-25 1998-07-24 Urokinase inhibitors
SK1748-99A SK174899A3 (en) 1997-07-25 1998-07-24 Urokinase inhibitors
AU85874/98A AU8587498A (en) 1997-07-25 1998-07-24 Urokinase inhibitors
HU0100353A HUP0100353A3 (en) 1997-07-25 1998-07-24 Naphtamidine derivatives with urokinase inhibitor activity
BG103981A BG103981A (en) 1997-07-25 1999-12-10 Urokinase inhibitors
NO996578A NO996578L (en) 1997-07-25 1999-12-30 Urokinase inhibitors

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US90104097A 1997-07-25 1997-07-25
US08/901,040 1997-07-25

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Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000005214A2 (en) * 1998-07-24 2000-02-03 Pfizer Inc. Isoquinolines as urokinase inhibitors
US6504031B1 (en) 1998-08-06 2003-01-07 Milan Bruncko Naphthamidine urokinase inhibitors
GB9914486D0 (en) 1999-06-21 1999-08-18 Smithkline Beecham Plc Medicaments
JP4815083B2 (en) * 1999-08-31 2011-11-16 メルク・シャープ・エンド・ドーム・コーポレイション Heterocyclic compounds and methods of use thereof
US20020052343A1 (en) * 1999-12-15 2002-05-02 Allen Darin Arthur Salicylamides as serine protease inhibitors
EP1276722B1 (en) * 2000-04-25 2006-03-08 Abbott Laboratories Naphthamidine urokinase inhibitors
US6495562B1 (en) 2000-04-25 2002-12-17 Abbott Laboratories Naphthamidine urokinase inhibitors
DE10029014A1 (en) 2000-06-15 2001-12-20 Univ Schiller Jena Urokinase inhibitor, useful for treatment, prophylaxis or diagnosis of thromboembolic disease, comprising acylated 3- or 4-amidino-benzylamine derivative
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
WO2002070467A1 (en) * 2001-02-26 2002-09-12 4Sc Ag Derivatives of diphenylurea, diphenyloxalic acid diamide and diphenylsulfuric acid diamide and their use as medicaments
WO2003076391A2 (en) 2002-03-11 2003-09-18 Curacyte Ag Urokinase inhibitors, production and use thereof
US7053112B2 (en) * 2002-09-24 2006-05-30 Schering Aktiengesellschaft Imidazolidinedione analogs useful as anticoagulants and antithrombotics
DE10301300B4 (en) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Use of acylated 4-amidino- and 4-guanidinobenzylamines for the inhibition of plasma kallikrein
DE10342108A1 (en) 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basic substituted benzylamine analogs as coagulation factor Xa inhibitors, their preparation and use
US7545495B2 (en) 2004-04-27 2009-06-09 Abbott Laboratories Methods for visualizing crystals and distinguishing crystals from other matter within a biological sample
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
RS56037B1 (en) 2004-06-24 2017-09-29 Vertex Pharma Modulators of atp-binding cassette transporters
DE102004045720A1 (en) * 2004-09-21 2006-03-23 Wilex Ag Stable dosage form of phenylalanine derivatives
EP2087885A1 (en) 2005-06-24 2009-08-12 Wilex AG Use of urokinase inhibitors for the treatment and /or prevention of neuropathological diseases
US8686002B2 (en) 2005-08-21 2014-04-01 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as binding partners for 5-HT5 receptors
LT1993360T (en) 2005-12-28 2017-06-12 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
DE102006050672A1 (en) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh New glycylglycine derivatives with a benzylsulfonylamido group and an amidino-organylamido group at the opposite chain ends, used in drugs for reducing loss of blood, e.g. in operations
DK2408750T3 (en) 2009-03-20 2015-10-05 Vertex Pharma PROCESS FOR THE PREPARATION modulators of cystic fibrosis -TRANSMEMBRANKONDUKTANSREGULATOR
JP2011057661A (en) * 2009-08-14 2011-03-24 Bayer Cropscience Ag Pesticidal carboxamides
US8802700B2 (en) 2010-12-10 2014-08-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
BR112014021090B1 (en) 2012-02-27 2023-01-24 Vertex Pharmaceuticals Incorporated PHARMACEUTICAL COMPOSITION AND USE OF N-[2,4-BIS(1,1-DIMETHYLethyl)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE3-CARBOXAMIDE IN THE PREPARATION OF THE SAME
CN107250113B (en) 2014-10-07 2019-03-29 弗特克斯药品有限公司 The eutectic of the regulator of cystic fibrosis transmembrane conductance regulator
GB201617758D0 (en) 2016-10-20 2016-12-07 Almac Discovery Limited Pharmaceutical compounds
TW202128161A (en) 2019-10-18 2021-08-01 美國加利福尼亞大學董事會 Compounds and methods for targeting pathogenic blood vessels
WO2023165874A1 (en) * 2022-03-01 2023-09-07 Syngenta Crop Protection Ag Pyrimidinyl-oxy-quinoline based herbicidal compounds

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0540051A1 (en) * 1991-10-31 1993-05-05 Daiichi Pharmaceutical Co., Ltd. Aromatic amidine derivatives and salts thereof
EP0568289A2 (en) * 1992-05-01 1993-11-03 Eisai Co., Ltd. Benzothiophenes and thienothiophenes and related compounds useful, for example, as urokinase inhibitors
JPH06227971A (en) * 1993-02-04 1994-08-16 Dai Ichi Seiyaku Co Ltd Medicine for preventing and treating infection of influenza virus
WO1996016940A1 (en) * 1994-12-02 1996-06-06 Yamanouchi Pharmaceutical Co., Ltd. Novel amidinonaphthyl derivative or salt thereof
WO1999005124A1 (en) * 1997-07-23 1999-02-04 Yamanouchi Pharmaceutical Co., Ltd. Novel hexahydro-1,4-diazepine derivatives or salts thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0540051A1 (en) * 1991-10-31 1993-05-05 Daiichi Pharmaceutical Co., Ltd. Aromatic amidine derivatives and salts thereof
EP0568289A2 (en) * 1992-05-01 1993-11-03 Eisai Co., Ltd. Benzothiophenes and thienothiophenes and related compounds useful, for example, as urokinase inhibitors
JPH06227971A (en) * 1993-02-04 1994-08-16 Dai Ichi Seiyaku Co Ltd Medicine for preventing and treating infection of influenza virus
WO1996016940A1 (en) * 1994-12-02 1996-06-06 Yamanouchi Pharmaceutical Co., Ltd. Novel amidinonaphthyl derivative or salt thereof
EP0798295A1 (en) * 1994-12-02 1997-10-01 Yamanouchi Pharmaceutical Co. Ltd. Novel amidinonaphthyl derivative or salt thereof
WO1999005124A1 (en) * 1997-07-23 1999-02-04 Yamanouchi Pharmaceutical Co., Ltd. Novel hexahydro-1,4-diazepine derivatives or salts thereof

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Section Ch Week 9437, Derwent World Patents Index; Class B05, AN 94-299682, XP002098441 *
KATAKURA, S. ET AL: "Molecular model of an interaction between factor Xa and DX-9065a, a novel factor Xa inhibitor: contribution of the acetimidoylpyrrolidine moiety of the inhibitor to potency and selectivity for serine proteases", EUR. J. MED. CHEM. (1995), 30(5), 387-94 CODEN: EJMCA5;ISSN: 0223-5234, XP002098440 *
NAGAHARA T ET AL: "DEBASIC (AMIDINOARY) PROPANOIC ACID DERIVATIVES AS NOVEL BLOOD COAGULATION FACTOR XA INHIBITORS", JOURNAL OF MEDICINAL CHEMISTRY, vol. 37, no. 8, 15 April 1994 (1994-04-15), pages 1200 - 1207, XP000608128 *

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HUP0100353A3 (en) 2001-11-28
CA2294300A1 (en) 1999-02-04
ZA986594B (en) 1999-01-27
EP1000018A2 (en) 2000-05-17
KR20010014369A (en) 2001-02-26
JP2002512636A (en) 2002-04-23
PL339429A1 (en) 2000-12-18

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