JP4658430B2 - Ｎ−グアニジノアルキルアミド、その製造、その使用およびそれを含む医薬調製物 - Google Patents

Ｎ−グアニジノアルキルアミド、その製造、その使用およびそれを含む医薬調製物 Download PDF

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Publication number
JP4658430B2
JP4658430B2 JP2001534764A JP2001534764A JP4658430B2 JP 4658430 B2 JP4658430 B2 JP 4658430B2 JP 2001534764 A JP2001534764 A JP 2001534764A JP 2001534764 A JP2001534764 A JP 2001534764A JP 4658430 B2 JP4658430 B2 JP 4658430B2
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formula
group
alkyl
groups
hydrogen
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JP2003513066A5 (enExample
JP2003513066A (ja
Inventor
オトマール・クリングラー
ゲーアハルト・ツォラー
エリーザベト・デフォサ
ファハド・アル−オベイディ
アーミン・ウォールサー
ジェイムズ・オーストレム
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サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング
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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)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
JP2001534764A 1999-10-30 2000-10-21 Ｎ−グアニジノアルキルアミド、その製造、その使用およびそれを含む医薬調製物 Expired - Fee Related JP4658430B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP99121623.5 1999-10-30
EP99121623A EP1095933A1 (en) 1999-10-30 1999-10-30 Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
PCT/EP2000/010395 WO2001032611A1 (en) 1999-10-30 2000-10-21 N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them

Publications (3)

Publication Number Publication Date
JP2003513066A JP2003513066A (ja) 2003-04-08
JP2003513066A5 JP2003513066A5 (enExample) 2007-12-06
JP4658430B2 true JP4658430B2 (ja) 2011-03-23

Family

ID=8239305

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2001534764A Expired - Fee Related JP4658430B2 (ja) 1999-10-30 2000-10-21 Ｎ−グアニジノアルキルアミド、その製造、その使用およびそれを含む医薬調製物

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)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1644401E (pt) * 2003-07-04 2011-06-06 Lonza Ag Acesso melhorado para síntese em fase suportada
KR102069498B1 (ko) 2007-09-28 2020-01-23 포톨라 파마슈티컬스, 인코포레이티드 인자 Ｘａ 저해제에 대한 안티도트 및 그것을 사용하는 방법
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
BRPI0906473A8 (pt) 2008-01-04 2016-02-10 Intellikine Inc Certas entidades químicas, composições e métodos
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
CA2743496C (en) 2008-11-14 2018-03-27 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
EP2453910B1 (en) 2009-07-15 2016-08-31 Portola Pharmaceuticals, Inc. Unit dose formulation of antidote for factor xa inhibitors for use in preventing bleeding
EP3238722B1 (en) 2011-01-10 2019-03-13 Infinity Pharmaceuticals, Inc. 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
RU2702908C2 (ru) 2012-11-01 2019-10-14 Инфинити Фармасьютикалз, Инк. Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
EP3474856B1 (en) 2016-06-24 2022-09-14 Infinity Pharmaceuticals, Inc. Combination therapies
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
CN121221582A (zh) * 2021-05-10 2025-12-30 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
US5833982A (en) 1991-02-28 1998-11-10 Zymogenetics, Inc. Modified factor VII
US5788965A (en) 1991-02-28 1998-08-04 Novo Nordisk A/S Modified factor VII
US5371072A (en) * 1992-10-16 1994-12-06 Corvas International, Inc. Asp-Pro-Arg α-keto-amide enzyme inhibitors
DE4326465A1 (de) * 1993-01-20 1995-02-09 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
WO1994017635A1 (en) 1993-01-20 1994-08-04 Peter John Alexandrovics A line monitoring system
NZ263084A (en) * 1993-03-12 1997-08-22 Arris Pharm Corp Dipeptide derivatives, treatment of immunomediated inflammatory disorders
ZA953361B (en) 1994-04-26 1996-01-12 Selectide Corp Factor Xa inhibitors
NZ296210A (en) * 1994-12-02 1998-05-27 Yamanouchi Pharma Co Ltd Amidinonaphthyl derivatives to inhibit activated blood coagulation factor x
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
SE9703414D0 (sv) * 1997-09-23 1997-09-23 Astra Ab New compounds
BR9814340B1 (pt) 1997-12-24 2010-07-13 compostos derivados de indol, processo para a preparação dos mesmo e composição farmacêutica.
WO1999037643A1 (en) * 1998-01-26 1999-07-29 Yamanouchi Pharmaceutical Co., Ltd. Novel benzene-fused heterocyclic derivatives or salts thereof
EP0987274A1 (en) 1998-09-15 2000-03-22 Hoechst Marion Roussel Deutschland GmbH Factor VIIa Inhibitors
US6348482B1 (en) * 1999-05-05 2002-02-19 Merck & Co., Inc. Catechols as antimicrobial agents

Also Published As

Publication number Publication date
PL354808A1 (en) 2004-02-23
EP1228039A1 (en) 2002-08-07
EE200200199A (et) 2003-06-16
CA2389412C (en) 2009-12-01
AU1026501A (en) 2001-05-14
CZ301855B6 (cs) 2010-07-14
PT1228039E (pt) 2004-09-30
ZA200203294B (en) 2003-01-29
CA2389412A1 (en) 2001-05-10
RU2002114041A (ru) 2004-01-20
CZ20021489A3 (cs) 2002-07-17
WO2001032611A1 (en) 2001-05-10
DE60010113T2 (de) 2005-05-04
NZ518607A (en) 2003-10-31
HRP20020372A2 (en) 2004-08-31
AU776797B2 (en) 2004-09-23
TR200201181T2 (tr) 2002-09-23
US6664393B2 (en) 2003-12-16
US20030162967A1 (en) 2003-08-28
HRP20020372B1 (hr) 2011-01-31
NO20022022L (no) 2002-04-29
MEP54708A (en) 2011-05-10
AR026257A1 (es) 2003-02-05
CN1249026C (zh) 2006-04-05
YU29702A (sh) 2005-06-10
SI1228039T1 (en) 2004-10-31
PL203859B1 (pl) 2009-11-30
DK1228039T3 (da) 2004-08-16
IL149209A (en) 2007-06-03
IL149209A0 (en) 2002-11-10
RS50471B (sr) 2010-03-02
DE60010113D1 (de) 2004-05-27
KR20020047310A (ko) 2002-06-21
HUP0203627A2 (hu) 2003-03-28
ES2220553T3 (es) 2004-12-16
NO20022022D0 (no) 2002-04-29
US6472562B1 (en) 2002-10-29
MXPA02003805A (es) 2004-10-15
HUP0203627A3 (en) 2004-12-28
SK5782002A3 (en) 2002-10-08
EP1228039B1 (en) 2004-04-21
RU2253651C2 (ru) 2005-06-10
NO328016B1 (no) 2009-11-09
BR0015186A (pt) 2002-07-23
EP1095933A1 (en) 2001-05-02
EE05168B1 (et) 2009-06-15
KR100981593B1 (ko) 2010-09-13
CN1387508A (zh) 2002-12-25
SK286856B6 (sk) 2009-06-05
HK1050673A1 (en) 2003-07-04
ATE264837T1 (de) 2004-05-15
JP2003513066A (ja) 2003-04-08

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