HUP0100353A2 - Naphtamidine derivatives with urokinase inhibitor activity - Google Patents

Naphtamidine derivatives with urokinase inhibitor activity

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Publication number
HUP0100353A2
HUP0100353A2 HU0100353A HUP0100353A HUP0100353A2 HU P0100353 A2 HUP0100353 A2 HU P0100353A2 HU 0100353 A HU0100353 A HU 0100353A HU P0100353 A HUP0100353 A HU P0100353A HU P0100353 A2 HUP0100353 A2 HU P0100353A2
Authority
HU
Hungary
Prior art keywords
group
general formula
hydrogen atom
naphtamidine
derivatives
Prior art date
Application number
HU0100353A
Other languages
Hungarian (hu)
Inventor
Andrew G. Geyer
William J. Mcclellan
Todd W. Rockway
Kent D. Stewart
Moshe Weitzberg
Michael D. Wendt
Original Assignee
Abbott Laboratories
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 Abbott Laboratories filed Critical Abbott Laboratories
Publication of HUP0100353A2 publication Critical patent/HUP0100353A2/en
Publication of HUP0100353A3 publication Critical patent/HUP0100353A3/en

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    • 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
    • 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
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    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
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    • 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]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00—Antineoplastic agents
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    • C07C257/00—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
    • 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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    • C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
    • C07C259/18—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of six-membered aromatic rings
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    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
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    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/56—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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    • C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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Abstract

A találmány (I) általános képletű vegyületekre és ilyeneket tartalmazógyógyszerkészítményekre vonatkozik - a képletben Z jelentése (1)nitrogénatom, (2) metincsoport, vagy (3) -NR1R2 általános képlettelszubsztituált metincsoport, A jelentése (1) hidrogénatom, vagy (2) -LARA általános képletű csoport, B jelentése (1) hidrogénatom, vagy (2)-LBRB csoport, és C jelentése (1) hidrogénatom, vagy (2) -LC-RCáltalános képletű csoport, azzal a megkötéssel, hogy A, B vagy C közüllegalább az egyik hidrogénatomtól eltérő, és azzal a megkötéssel, hogyha A hidrogénatomtól eltérő, B és C közül legalább az egyikhidrogénatomtól eltérő, és A, B és C, valamint LA, LB és LC jelentéseegymástól függetlenül egy telített vagy telítetlen alifás, cikloalifásvagy aromás csoport. Az (I) általános képletű vegyületek urokinázgátlóhatásúak. ÓThe invention relates to compounds of general formula (I) and pharmaceutical preparations containing them - in the formula, Z means (1) a nitrogen atom, (2) a methine group, or (3) a substituted methine group of the general formula -NR1R2, A means (1) a hydrogen atom, or (2) -LARA a group of the general formula, B is (1) a hydrogen atom, or (2)-LBRB group, and C is (1) a hydrogen atom, or (2) a group of the general formula -LC-RC, with the proviso that among A, B or C, at least different from one hydrogen atom, with the proviso that if A is different from hydrogen, at least one of B and C is different from hydrogen, and A, B and C, and LA, LB and LC are independently a saturated or unsaturated aliphatic, cycloaliphatic or aromatic group. The compounds of general formula (I) are urokinase inhibitory. HE

HU0100353A 1997-07-25 1998-07-24 Naphtamidine derivatives with urokinase inhibitor activity HUP0100353A3 (en)

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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
EP1214303A1 (en) * 1999-08-31 2002-06-19 Merck & Co., Inc. Heterocyclic compounds and methods of use thereof
WO2001044172A1 (en) * 1999-12-15 2001-06-21 Axys Pharmaceuticals, Inc. Salicylamides as serine protease and factor xa 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
EP1395548A1 (en) 2001-02-26 2004-03-10 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
ES2656017T3 (en) 2004-06-24 2018-02-22 Vertex Pharmaceuticals Incorporated Conveyor modulators of the ATP binding cassette
DE102004045720A1 (en) * 2004-09-21 2006-03-23 Wilex Ag Stable dosage form of phenylalanine derivatives
ATE442842T1 (en) 2005-06-24 2009-10-15 Wilex Ag USE OF UROCINASIS INHIBITORS TO TREAT AND/OR PREVENT AMYOTROPHIC LATERAL SCLERosis (ALS)
WO2007022946A1 (en) 2005-08-21 2007-03-01 Abbott Gmbh & Co. Kg Heterocyclic compounds and their use as binding partners for 5-ht5 receptors
DK3219705T3 (en) 2005-12-28 2020-04-14 Vertex Pharma PHARMACEUTICAL COMPOSITIONS OF THE AMORPHIC FORM OF N- [2,4-BIS (1,1-DIMETHYLETHYL) -5-HYDROXYPHENYL] -1,4-DIHYDRO-4-OXOQUINOLIN-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
EP3330255B1 (en) 2009-03-20 2020-12-09 Vertex Pharmaceuticals Incorporated Process for making modulators of cystic fibrosis transmembrane conductance regulator
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
AU2013226076B2 (en) 2012-02-27 2017-11-16 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administration thereof
JP6746569B2 (en) 2014-10-07 2020-08-26 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
GB201617758D0 (en) 2016-10-20 2016-12-07 Almac Discovery Limited Pharmaceutical compounds
US11884647B2 (en) 2019-10-18 2024-01-30 The Regents Of The University Of California Compounds and methods for targeting pathogenic blood vessels
AR128577A1 (en) * 2022-03-01 2024-05-22 Syngenta Crop Protection Ag HERBICIDAL COMPOUNDS

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA928276B (en) * 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
US5340833A (en) * 1992-05-01 1994-08-23 Eisai Co., Ltd. Urokinase inhibitors
JP3457694B2 (en) * 1993-02-04 2003-10-20 第一製薬株式会社 Influenza prophylaxis and treatment
NZ296210A (en) * 1994-12-02 1998-05-27 Yamanouchi Pharma Co Ltd Amidinonaphthyl derivatives to inhibit activated blood coagulation factor x
AU735144B2 (en) * 1997-07-23 2001-07-05 Yamanouchi Pharmaceutical Co., Ltd. Novel hexahydro-1,4-diazepine derivatives or their salts

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HUP0100353A3 (en) 2001-11-28
IL133368A0 (en) 2001-04-30
NO996578D0 (en) 1999-12-30

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