DE60023266D1 - Serinprotease-inhibitoren - Google Patents

Serinprotease-inhibitoren

Info

Publication number
DE60023266D1
DE60023266D1 DE60023266T DE60023266T DE60023266D1 DE 60023266 D1 DE60023266 D1 DE 60023266D1 DE 60023266 T DE60023266 T DE 60023266T DE 60023266 T DE60023266 T DE 60023266T DE 60023266 D1 DE60023266 D1 DE 60023266D1
Authority
DE
Germany
Prior art keywords
serine protease
protease inhibitors
compounds
factor
kallikrein
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
DE60023266T
Other languages
English (en)
Other versions
DE60023266T2 (de
Inventor
Ignacio Aliagas-Martin
R Artis
S Dina
A Flygare
A Goldsmith
A Munroe
G Olivero
Richard Pastor
E Rawson
D Robarge
P Sutherlin
J Weese
Aihe Zhou
Yan Zhu
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.)
Genentech Inc
Original Assignee
Genentech 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 Genentech Inc filed Critical Genentech Inc
Application granted granted Critical
Publication of DE60023266D1 publication Critical patent/DE60023266D1/de
Publication of DE60023266T2 publication Critical patent/DE60023266T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • 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
    • C07C311/18—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 to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/50—Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/51—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (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)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
DE60023266T 1999-01-13 2000-01-11 Serinprotease-inhibitoren Expired - Lifetime DE60023266T2 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US11577299P 1999-01-13 1999-01-13
US115772P 1999-01-13
US15202999P 1999-09-01 1999-09-01
US152029P 1999-09-01
PCT/US2000/000673 WO2000041531A2 (en) 1999-01-13 2000-01-11 Serine protease inhibitors

Publications (2)

Publication Number Publication Date
DE60023266D1 true DE60023266D1 (de) 2005-11-24
DE60023266T2 DE60023266T2 (de) 2006-07-13

Family

ID=26813550

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60023266T Expired - Lifetime DE60023266T2 (de) 1999-01-13 2000-01-11 Serinprotease-inhibitoren

Country Status (19)

Country Link
US (4) US6472393B1 (de)
EP (1) EP1144373B1 (de)
JP (1) JP2002534449A (de)
KR (1) KR100838418B1 (de)
CN (1) CN100488947C (de)
AT (1) ATE307111T1 (de)
AU (1) AU771776B2 (de)
BR (1) BR0008755A (de)
CA (1) CA2356934A1 (de)
CZ (1) CZ20012508A3 (de)
DE (1) DE60023266T2 (de)
ES (1) ES2251363T3 (de)
HU (1) HUP0105077A3 (de)
IL (2) IL144032A0 (de)
MX (1) MXPA01007038A (de)
NO (1) NO20013462L (de)
NZ (1) NZ512736A (de)
PL (1) PL350042A1 (de)
WO (1) WO2000041531A2 (de)

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ATE307111T1 (de) * 1999-01-13 2005-11-15 Genentech Inc Serinprotease-inhibitoren
WO2001023349A1 (fr) * 1999-09-30 2001-04-05 Mitsubishi Chemical Corporation Derives d'acylsulfonamide
AU1339302A (en) 2000-10-20 2002-05-06 Biocryst Pharm Inc Biaryl compounds as serine protease inhibitors
JP4179878B2 (ja) 2001-02-02 2008-11-12 中外製薬株式会社 ペプチド誘導体
DE10130374A1 (de) * 2001-06-23 2003-01-02 Boehringer Ingelheim Pharma Substituierte N-Acyl-anilinderivate, deren Herstellung und deren Verwendung als Arzneimittel
JP4898091B2 (ja) * 2002-03-11 2012-03-14 ザ メディシンズ カンパニー （ライプツィヒ） ゲーエムベーハー ウロキナーゼの阻害剤、それらの製造および使用
GB0207637D0 (en) * 2002-04-02 2002-05-15 Karobio Ab Novel compound
WO2003101941A2 (en) * 2002-05-31 2003-12-11 Genzyme Corporation Alpha acyloxyacetamides for kallikrein and urokinase inhibition
DE10301300B4 (de) * 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
EP1594845A4 (de) * 2003-02-11 2008-05-21 Bristol Myers Squibb Co Als serinproteaseinhibitoren geeignete benzolacetamidverbindungen
US7122559B2 (en) * 2003-02-11 2006-10-17 Bristol-Myers Squibb Company Phenylglycine derivatives useful as serine protease inhibitors
EP1628954A2 (de) * 2003-05-20 2006-03-01 Genentech, Inc. Acylsulfamidinhibitoren von faktor viia
WO2004113316A1 (en) * 2003-05-20 2004-12-29 Genentech, Inc. Benzofuran inhibitors of factor viia
DE10342108A1 (de) * 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
WO2006076246A2 (en) * 2005-01-10 2006-07-20 Bristol-Myers Squibb Company Phenylglycinamide derivatives useful as anticoagulants
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US7964619B2 (en) 2005-06-03 2011-06-21 The University Of North Carolina At Chapel Hill Teraryl components as antiparasitic agents
US8101636B2 (en) * 2005-06-03 2012-01-24 The University Of North Carolina At Chapel Hill Linear dicationic terphenyls and their aza analogues as antiparasitic agents
ATE455103T1 (de) * 2005-06-24 2010-01-15 Bristol Myers Squibb Co Als antikoagulationsmittel geeignete phenylglycinamid- und pyridylglycinamidderivate
DE602007011231D1 (de) 2006-03-24 2011-01-27 Eisai R&D Man Co Ltd Triazolonderivat
US7776832B2 (en) 2006-04-21 2010-08-17 Gem Pharmaceuticals, Llc Anticancer treatment with a combination of taxanes and 13-deoxyanthracyclines
DE102006050672A1 (de) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins
TW200831080A (en) * 2006-12-15 2008-08-01 Irm Llc Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
CA2674589A1 (en) 2007-01-12 2008-07-24 Biocryst Pharmaceuticals, Inc. Antiviral nucleoside analogs
EP2420239B1 (de) 2007-04-13 2015-01-14 Southern Research Institute Clomipramine als Anti-Angiogenese-Mittel
EP2178849A1 (de) * 2007-07-31 2010-04-28 Mallinckrodt Inc. Integrierte photoaktive wirkstoffe und ihre verwendung
JPWO2009038157A1 (ja) 2007-09-21 2011-01-06 エーザイ・アール・アンド・ディー・マネジメント株式会社 ２，３−ジヒドロ−イミノイソインドール誘導体
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WO2010036407A2 (en) 2008-05-15 2010-04-01 Biocryst Pharmaceuticals, Inc. Antiviral nucleoside analogs
CA2753282C (en) 2009-03-10 2017-11-28 Med Discovery Sa Use of serine protease inhibitors in the treatment of neutropenia
TW201206905A (en) 2010-05-20 2012-02-16 Eisai R & Amp D Man Co Ltd Prodrug of triazolone compound
WO2012004678A2 (en) 2010-07-07 2012-01-12 The Medicines Company (Leipzig) Gmbh Serine protease inhibitors
US9187484B2 (en) 2012-05-02 2015-11-17 Southern Research Institute Triazolopyridazine compounds, use as inhibitors of the kinase LRRK2, and methods for preparation thereof
WO2015123365A1 (en) 2014-02-11 2015-08-20 Mitokinin Llc Compositions and methods using the same for treatment of neurodegenerative and mitochondrial disease
CN108934162A (zh) 2015-12-16 2018-12-04 南方研究所 吡咯并嘧啶化合物、作为激酶lrrk2抑制剂的用途及其制备方法
WO2018094227A1 (en) 2016-11-17 2018-05-24 The University Of North Carolina At Chapel Hill Alkyl pyrrolopyrimidine analogs and methods of making and using same
US10450263B2 (en) 2017-02-10 2019-10-22 Southern Research Institute Benzo annulenes as antiviral agents
US11160826B1 (en) 2017-03-03 2021-11-02 United States Government As Represented By The Department Of Veterans Affairs Cholesterol lowering drugs for the treatment of hepatic encephalopathy
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CA3080193A1 (en) 2017-10-26 2019-05-02 Southern Research Institute Dipeptide analogs as tgf-beta inhibitors
US11103508B2 (en) 2017-10-31 2021-08-31 Southern Research Institute Substituted quinazoline sulfonamides as thioredoxin interacting protein (TXNIP) inhibitors
TW202010742A (zh) 2018-04-06 2020-03-16 美商百歐克斯製藥公司 取代的苯并呋喃、苯并吡咯、苯并噻吩及結構相關的補體抑制劑
US20210363170A1 (en) 2018-04-19 2021-11-25 Southern Research Institute 4'-thio-nucleotide and -nucleoside prodrugs for the treatment of cancer
EP3982976A4 (de) 2019-06-14 2023-11-01 Southern Research Institute 2,4,7-substituierte-7-deaza-2'-deoxy-2'-fluorarabinosyl-nukleosid und nukleotid-prodrugs und deren verwendungen
US11566019B2 (en) 2020-04-02 2023-01-31 Southern Research Institute 2-pyrimidone analogs as potent antiviral agents against alphaviruses
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Also Published As

Publication number Publication date
US6472393B1 (en) 2002-10-29
DE60023266T2 (de) 2006-07-13
EP1144373A2 (de) 2001-10-17
CA2356934A1 (en) 2000-07-20
EP1144373B1 (de) 2005-10-19
AU771776B2 (en) 2004-04-01
ATE307111T1 (de) 2005-11-15
IL144032A0 (en) 2002-04-21
PL350042A1 (en) 2002-10-21
HUP0105077A3 (en) 2005-04-28
AU3345100A (en) 2000-08-01
NZ512736A (en) 2003-11-28
US6919369B2 (en) 2005-07-19
US20050186198A1 (en) 2005-08-25
JP2002534449A (ja) 2002-10-15
US20070037813A1 (en) 2007-02-15
WO2000041531A3 (en) 2001-08-16
US20030212071A1 (en) 2003-11-13
WO2000041531A2 (en) 2000-07-20
KR20010101852A (ko) 2001-11-15
MXPA01007038A (es) 2002-07-30
NO20013462D0 (no) 2001-07-12
IL144032A (en) 2006-06-11
KR100838418B1 (ko) 2008-06-13
BR0008755A (pt) 2007-05-29
CZ20012508A3 (cs) 2002-02-13
ES2251363T3 (es) 2006-05-01
CN1342139A (zh) 2002-03-27
EP1144373A3 (de) 2002-01-02
CN100488947C (zh) 2009-05-20
NO20013462L (no) 2001-09-12
HUP0105077A2 (hu) 2002-05-29

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