DE60010113T2 - N-guanidinalkylamide, verfahren zu ihrer herstellung und sie enthaltende pharmazeutische präparate - Google Patents

N-guanidinalkylamide, verfahren zu ihrer herstellung und sie enthaltende pharmazeutische präparate Download PDF

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Publication number
DE60010113T2
DE60010113T2 DE60010113T DE60010113T DE60010113T2 DE 60010113 T2 DE60010113 T2 DE 60010113T2 DE 60010113 T DE60010113 T DE 60010113T DE 60010113 T DE60010113 T DE 60010113T DE 60010113 T2 DE60010113 T2 DE 60010113T2
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Germany
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groups
formula
group
alkyl
substituted
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Expired - Lifetime
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DE60010113T
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English (en)
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DE60010113D1 (de
Inventor
Otmar Klingler
Gerhard Zoller
Elisabeth Defossa
Fahad Al-Obeidi
Armin Walser
James Ostrem
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Sanofi Aventis Deutschland GmbH
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Aventis Pharma Deutschland GmbH
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    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • 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]
    • 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
    • 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
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)
DE60010113T 1999-10-30 2000-10-21 N-guanidinalkylamide, verfahren zu ihrer herstellung und sie enthaltende pharmazeutische präparate Expired - Lifetime DE60010113T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP99121623A EP1095933A1 (en) 1999-10-30 1999-10-30 Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
EP99121623 1999-10-30
PCT/EP2000/010395 WO2001032611A1 (en) 1999-10-30 2000-10-21 N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them

Publications (2)

Publication Number Publication Date
DE60010113D1 DE60010113D1 (de) 2004-05-27
DE60010113T2 true DE60010113T2 (de) 2005-05-04

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DE60010113T Expired - Lifetime DE60010113T2 (de) 1999-10-30 2000-10-21 N-guanidinalkylamide, verfahren zu ihrer herstellung und sie enthaltende pharmazeutische präparate

Country Status (31)

Country Link
US (2) US6472562B1 (enExample)
EP (2) EP1095933A1 (enExample)
JP (1) JP4658430B2 (enExample)
KR (1) KR100981593B1 (enExample)
CN (1) CN1249026C (enExample)
AR (1) AR026257A1 (enExample)
AT (1) ATE264837T1 (enExample)
AU (1) AU776797B2 (enExample)
BR (1) BR0015186A (enExample)
CA (1) CA2389412C (enExample)
CZ (1) CZ301855B6 (enExample)
DE (1) DE60010113T2 (enExample)
DK (1) DK1228039T3 (enExample)
EE (1) EE05168B1 (enExample)
ES (1) ES2220553T3 (enExample)
HR (1) HRP20020372B1 (enExample)
HU (1) HUP0203627A3 (enExample)
IL (2) IL149209A0 (enExample)
ME (1) MEP54708A (enExample)
MX (1) MXPA02003805A (enExample)
NO (1) NO328016B1 (enExample)
NZ (1) NZ518607A (enExample)
PL (1) PL203859B1 (enExample)
PT (1) PT1228039E (enExample)
RS (1) RS50471B (enExample)
RU (1) RU2253651C2 (enExample)
SI (1) SI1228039T1 (enExample)
SK (1) SK286856B6 (enExample)
TR (1) TR200201181T2 (enExample)
WO (1) WO2001032611A1 (enExample)
ZA (1) ZA200203294B (enExample)

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ATE501164T1 (de) * 2003-07-04 2011-03-15 Lonza Ag Verbessertes verfahren für festphasensynthese
ES2597436T3 (es) 2007-09-28 2017-01-18 Portola Pharmaceuticals, Inc. Antídotos para inhibidores del factor Xa y procedimientos de uso de los mismos
CN101965335B (zh) 2008-01-04 2015-01-14 英特利凯恩有限责任公司 某些化学实体、组合物和方法
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
RU2377990C1 (ru) * 2008-07-23 2010-01-10 Федеральное Государственное Образовательное Учреждение Высшего Профессионального Образования "Южный Федеральный Университет" Антитромботическое средство, влияющее на регуляцию функциональной активности тромбоцитов
EP2364165B1 (en) 2008-11-14 2018-01-03 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents
PL3604510T3 (pl) * 2009-03-30 2025-07-28 Alexion Pharmaceuticals, Inc. Antidota na inhibitory czynnika xa i sposoby ich stosowania
PT2453910T (pt) * 2009-07-15 2016-12-07 Portola Pharm Inc Formulação de dose unitária de antídoto contra inibidores de fator xa para uso na prevenção de sangramento
EP2663309B1 (en) 2011-01-10 2017-03-15 Infinity Pharmaceuticals, Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
LT2914296T (lt) 2012-11-01 2018-09-25 Infinity Pharmaceuticals, Inc. Vėžio gydymas, panaudojant p13 kinazės izoformos moduliatorius
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
BR112018077021A2 (pt) 2016-06-24 2019-04-02 Infinity Pharmaceuticals, Inc. terapias de combinação
CN110357800B (zh) * 2018-04-09 2022-07-26 青岛海生洋润生物科技有限公司 脯氨酸衍生物及其在制备治疗心脑血管疾病药物中的应用
CN115317474A (zh) * 2021-05-10 2022-11-11 中国海洋大学 一种苯酰胍衍生物在用于制备预防和治疗神经系统疾病或心血管系统疾病的药物中的应用

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HU206372B (en) * 1990-09-03 1992-10-28 Richter Gedeon Vegyeszet Process for producing new oligopeptides which selectively inhibit proliferation of haemopoietic cells and pharmaceutical compositions comprising same
US5506134A (en) 1990-10-22 1996-04-09 Corvas International, Inc. Hypridoma and monoclonal antibody which inhibits blood coagulation tissue factor/factor VIIa complex
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US5371072A (en) * 1992-10-16 1994-12-06 Corvas International, Inc. Asp-Pro-Arg α-keto-amide enzyme inhibitors
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DE4326465A1 (de) * 1993-01-20 1995-02-09 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US5525623A (en) * 1993-03-12 1996-06-11 Arris Pharmaceutical Corporation Compositions and methods for the treatment of immunomediated inflammatory disorders
CZ296439B6 (cs) 1994-04-26 2006-03-15 Selectide Corporation Inhibitory faktoru Xa
PT798295E (pt) * 1994-12-02 2003-07-31 Yamanouchi Pharma Co Ltd Novo derivado de amidinonaftilo ou sal deste
US6342504B1 (en) * 1994-12-13 2002-01-29 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
EP1020434A4 (en) * 1997-08-27 2000-11-15 Kissei Pharmaceutical 3-AMIDINOANILINE DERIVATIVES, INHIBITORS OF THE ACTIVATED BLOOD COINTENANCE FACTOR X AND INTERMEDIATE PRODUCTS FOR PRODUCING BOTH
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Also Published As

Publication number Publication date
CA2389412A1 (en) 2001-05-10
SI1228039T1 (en) 2004-10-31
MEP54708A (en) 2011-05-10
NZ518607A (en) 2003-10-31
PT1228039E (pt) 2004-09-30
CA2389412C (en) 2009-12-01
ZA200203294B (en) 2003-01-29
NO20022022L (no) 2002-04-29
US6664393B2 (en) 2003-12-16
AU1026501A (en) 2001-05-14
EE05168B1 (et) 2009-06-15
SK286856B6 (sk) 2009-06-05
HK1050673A1 (en) 2003-07-04
PL203859B1 (pl) 2009-11-30
MXPA02003805A (es) 2004-10-15
CN1249026C (zh) 2006-04-05
AU776797B2 (en) 2004-09-23
IL149209A (en) 2007-06-03
DE60010113D1 (de) 2004-05-27
ATE264837T1 (de) 2004-05-15
TR200201181T2 (tr) 2002-09-23
ES2220553T3 (es) 2004-12-16
RU2253651C2 (ru) 2005-06-10
EE200200199A (et) 2003-06-16
US6472562B1 (en) 2002-10-29
RU2002114041A (ru) 2004-01-20
KR100981593B1 (ko) 2010-09-13
CZ301855B6 (cs) 2010-07-14
JP4658430B2 (ja) 2011-03-23
HUP0203627A2 (hu) 2003-03-28
HRP20020372A2 (en) 2004-08-31
AR026257A1 (es) 2003-02-05
KR20020047310A (ko) 2002-06-21
NO328016B1 (no) 2009-11-09
WO2001032611A1 (en) 2001-05-10
SK5782002A3 (en) 2002-10-08
RS50471B (sr) 2010-03-02
US20030162967A1 (en) 2003-08-28
HRP20020372B1 (hr) 2011-01-31
DK1228039T3 (da) 2004-08-16
CN1387508A (zh) 2002-12-25
CZ20021489A3 (cs) 2002-07-17
EP1228039B1 (en) 2004-04-21
IL149209A0 (en) 2002-11-10
PL354808A1 (en) 2004-02-23
JP2003513066A (ja) 2003-04-08
NO20022022D0 (no) 2002-04-29
YU29702A (sh) 2005-06-10
HUP0203627A3 (en) 2004-12-28
EP1228039A1 (en) 2002-08-07
BR0015186A (pt) 2002-07-23
EP1095933A1 (en) 2001-05-02

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Owner name: SANOFI-AVENTIS DEUTSCHLAND GMBH, 65929 FRANKFURT,