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HUP0105077A2 - Szerin-proteáz inhibitorok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Szerin-proteáz inhibitorok és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0105077A2
HUP0105077A2 HU0105077A HUP0105077A HUP0105077A2 HU P0105077 A2 HUP0105077 A2 HU P0105077A2 HU 0105077 A HU0105077 A HU 0105077A HU P0105077 A HUP0105077 A HU P0105077A HU P0105077 A2 HUP0105077 A2 HU P0105077A2
Authority
HU
Hungary
Prior art keywords
group
pharmaceutical compositions
factor
compositions containing
protease inhibitors
Prior art date
Application number
HU0105077A
Other languages
English (en)
Inventor
Ignacio Aliagas-Martin
Dean R. Artis
Michael S. Dina
John A. Flygare
Richard A. Goldsmith
Regina A. Munroe
Alan G. Olivero
Richard Pastor
Thomas E. Rawson
Kirk D. Robarge
Daniel P. Sutherlin
Kenneth J. Weese
Aihe Zhou
Yan Zhu
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.
Publication of HUP0105077A2 publication Critical patent/HUP0105077A2/hu
Publication of HUP0105077A3 publication Critical patent/HUP0105077A3/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03Sulfonamides 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
    • C07C311/05Sulfonamides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00Compounds 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
    • C07C257/10Compounds 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
    • C07C257/18Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08Sulfonamides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/12Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C07C311/13Sulfonamides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides 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
    • C07C311/18Sulfonamides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/22Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29Sulfonamides, 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/50Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/51Y being a hydrogen or a carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48Iso-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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

A találmány tárgyát az (I) általános képletű vegyületek képezik,amelyek szerin-proteáz enzimek (szöveti faktor (TF)/VIIa-faktor, VIIa-faktor, Xa-faktor, trombin és/vagy kallikrein) inhibitorai, éselőnyösen alkalmazhatók véralvadási rendellenességek megelőzéséreés/vagy kezelésére. Szintén a találmány tárgyát képezik az evegyületeket tartalmazó készítmények. A képletben <A< és <B< jelentéseegymástól függetlenül CH-csoport, CR3-csoport vagy nitrogénatom; Xjelentése C=O-; Y jelentése S(O)n-R1 csoport; n értéke 1 vagy 2; N1 ésN2 jelentése nirtogénatomok; Q és R1 jelentései: adott esetbenszubsztituált 1-10 szénatomos alkil-, aril-, heteroaril-,karbociklil-, heterociklil-alkil-, 2-10 szénatomos alkenil-,arilalkenilcsoport; R2 jelentése adott esetben szubsztituáltalkilcsoport; R3 jelentése hidrogénatom, 1-6 szénatomos alkilcsoport. Ó
HU0105077A 1999-01-13 2000-01-11 Serine protease inhibitors and pharmaceutical compositions containing them HUP0105077A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11577299P 1999-01-13 1999-01-13
US15202999P 1999-09-01 1999-09-01

Publications (2)

Publication Number Publication Date
HUP0105077A2 true HUP0105077A2 (hu) 2002-05-29
HUP0105077A3 HUP0105077A3 (en) 2005-04-28

Family

ID=26813550

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0105077A HUP0105077A3 (en) 1999-01-13 2000-01-11 Serine protease inhibitors and pharmaceutical compositions containing them

Country Status (19)

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

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Also Published As

Publication number Publication date
CN100488947C (zh) 2009-05-20
US20050186198A1 (en) 2005-08-25
WO2000041531A3 (en) 2001-08-16
EP1144373A3 (en) 2002-01-02
JP2002534449A (ja) 2002-10-15
NO20013462L (no) 2001-09-12
BR0008755A (pt) 2007-05-29
ES2251363T3 (es) 2006-05-01
DE60023266D1 (de) 2005-11-24
KR100838418B1 (ko) 2008-06-13
PL350042A1 (en) 2002-10-21
EP1144373B1 (en) 2005-10-19
US6919369B2 (en) 2005-07-19
IL144032A (en) 2006-06-11
US6472393B1 (en) 2002-10-29
NZ512736A (en) 2003-11-28
EP1144373A2 (en) 2001-10-17
US20030212071A1 (en) 2003-11-13
CN1342139A (zh) 2002-03-27
AU771776B2 (en) 2004-04-01
AU3345100A (en) 2000-08-01
CA2356934A1 (en) 2000-07-20
WO2000041531A2 (en) 2000-07-20
DE60023266T2 (de) 2006-07-13
KR20010101852A (ko) 2001-11-15
MXPA01007038A (es) 2002-07-30
ATE307111T1 (de) 2005-11-15
CZ20012508A3 (cs) 2002-02-13
HUP0105077A3 (en) 2005-04-28
NO20013462D0 (no) 2001-07-12
US20070037813A1 (en) 2007-02-15
IL144032A0 (en) 2002-04-21

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