JPH11500120A - 新規なトロンビンインヒビター - Google Patents

新規なトロンビンインヒビター

Info

Publication number
JPH11500120A
JPH11500120A JP8524648A JP52464896A JPH11500120A JP H11500120 A JPH11500120 A JP H11500120A JP 8524648 A JP8524648 A JP 8524648A JP 52464896 A JP52464896 A JP 52464896A JP H11500120 A JPH11500120 A JP H11500120A
Authority
JP
Japan
Prior art keywords
alkyl
twenty
group
phenyl
boc
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.)
Ceased
Application number
JP8524648A
Other languages
English (en)
Japanese (ja)
Other versions
JPH11500120A5 (enExample
Inventor
ベーム ハンス−ヨアヒム
ヴォルフガング ヘフケン ハンス
ホルンベルガー ヴィルフリート
コーゼル シュテファン
マック ヘルムート
プファイファー トーマス
ザイツ ヴェルナー
ツィールケ トーマス
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.)
BASF SE
Original Assignee
BASF SE
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 BASF SE filed Critical BASF SE
Publication of JPH11500120A publication Critical patent/JPH11500120A/ja
Publication of JPH11500120A5 publication Critical patent/JPH11500120A5/ja
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • C07D213/60—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 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—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
    • 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
    • C07D207/10—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 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Pyridine Compounds (AREA)
JP8524648A 1995-02-17 1996-02-12 新規なトロンビンインヒビター Ceased JPH11500120A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
DE19505484.9 1995-02-17
DE19505484 1995-02-17
DE19506611 1995-02-24
DE19506611.1 1995-02-24
DE19507455.6 1995-03-03
DE19507455 1995-03-03
PCT/EP1996/000582 WO1996025426A1 (de) 1995-02-17 1996-02-12 Neue dipeptidische amidine als thrombin-inhibitoren

Publications (2)

Publication Number Publication Date
JPH11500120A true JPH11500120A (ja) 1999-01-06
JPH11500120A5 JPH11500120A5 (enExample) 2004-07-22

Family

ID=27214848

Family Applications (1)

Application Number Title Priority Date Filing Date
JP8524648A Ceased JPH11500120A (ja) 1995-02-17 1996-02-12 新規なトロンビンインヒビター

Country Status (26)

Country Link
US (3) US6030972A (enExample)
EP (1) EP0873356A1 (enExample)
JP (1) JPH11500120A (enExample)
KR (1) KR100388185B1 (enExample)
CN (1) CN1198839C (enExample)
AR (1) AR002277A1 (enExample)
AU (1) AU708001B2 (enExample)
BG (1) BG63697B1 (enExample)
BR (1) BR9607582A (enExample)
CA (1) CA2211109A1 (enExample)
CZ (1) CZ245797A3 (enExample)
EA (1) EA199700186A1 (enExample)
FI (1) FI973360L (enExample)
HR (1) HRP960075B1 (enExample)
HU (1) HUP9800263A3 (enExample)
IL (1) IL117165A0 (enExample)
MX (1) MX9706069A (enExample)
MY (1) MY132115A (enExample)
NO (1) NO973764L (enExample)
NZ (1) NZ302649A (enExample)
PL (1) PL321759A1 (enExample)
SI (1) SI9620037A (enExample)
SK (1) SK104697A3 (enExample)
TR (1) TR199700803T1 (enExample)
TW (1) TW450968B (enExample)
WO (1) WO1996025426A1 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006008609A (ja) * 2004-06-28 2006-01-12 Ube Ind Ltd ５−（４−テトラヒドロピラニル）ヒダントインの製法及びその中間体
JP2006045107A (ja) * 2004-08-04 2006-02-16 Ube Ind Ltd ４−テトラヒドロピラニルグリシンの製法
JP2007510651A (ja) * 2003-11-04 2007-04-26 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としての縮合フェニルアラニン誘導体
JP2013543850A (ja) * 2010-11-08 2013-12-09 上海医薬工業研究院 新規な化合物、その製造方法および用途

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US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
EP0873356A1 (de) * 1995-02-17 1998-10-28 Basf Aktiengesellschaft Neue dipeptidische amidine als thrombin-inhibitoren
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
US5914319A (en) * 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
SA96170106A (ar) * 1995-07-06 2005-12-03 أسترا أكتيبولاج مشتقات حامض أميني جديدة
AR005245A1 (es) * 1995-12-21 1999-04-28 Astrazeneca Ab Prodrogas de inhibidores de trombina, una formulación farmaceutica que las comprende, el uso de dichas prodrogas para la manufactura de un medicamento y un procedimiento para su preparacion
SE9602263D0 (sv) 1996-06-07 1996-06-07 Astra Ab New amino acid derivatives
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US5863929A (en) * 1996-06-25 1999-01-26 Eli Lilly And Company Anticoagulant agents
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds
DE19632772A1 (de) 1996-08-14 1998-02-19 Basf Ag Neue Benzamidine
DE19632773A1 (de) * 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren
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SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
EP1049673A1 (de) * 1998-01-26 2000-11-08 Basf Aktiengesellschaft Heterocyclische amidine als kallikrein protease inhibitoren
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HK1045846A1 (zh) 1999-04-09 2002-12-13 巴斯福股份公司 低分子量补体蛋白酶抑制剂
CN1349526A (zh) * 1999-04-09 2002-05-15 巴斯福股份公司 凝血酶抑制剂的前药
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DE19921346A1 (de) * 1999-05-10 2000-11-16 Basf Ag Sprühtrocknung von Thrombininhibitoren
EP1054017B1 (de) 1999-05-10 2004-10-13 Abbott GmbH & Co. KG Salze von Thrombininhibitoren
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DE10029015A1 (de) * 2000-06-15 2001-12-20 Curacyte Ag Hemmstoffe für den Gerinnungsfaktor Xa
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin inhibitors
DE10049937A1 (de) * 2000-10-06 2002-04-11 Knoll Ag Niedermolekulare Inhibitoren von Serinproteasen mit Polyhydroxyalkyl- und Polyhydroxycycloalkylresten
AR035216A1 (es) * 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
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DE10301300B4 (de) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
RU2228930C1 (ru) * 2003-05-20 2004-05-20 ООО "Исследовательский институт химического разнообразия" Замещенные 3-пиридилметиламины и фокусированная библиотека
US7781424B2 (en) * 2003-05-27 2010-08-24 Astrazeneca Ab Modified release pharmaceutical formulation
DE10342108A1 (de) 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
US7795205B2 (en) * 2004-04-12 2010-09-14 Canyon Pharmaceuticals, Inc. Methods for effecting regression of tumor mass and size in a metastasized pancreatic tumor
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US7524354B2 (en) * 2005-07-07 2009-04-28 Research Foundation Of State University Of New York Controlled synthesis of highly monodispersed gold nanoparticles
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TW202246215A (zh) 2015-12-18 2022-12-01 美商亞德利克斯公司 作為非全身ｔｇｒ５促效劑之經取代之４－苯基吡啶化合物

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007510651A (ja) * 2003-11-04 2007-04-26 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としての縮合フェニルアラニン誘導体
JP2006008609A (ja) * 2004-06-28 2006-01-12 Ube Ind Ltd ５−（４−テトラヒドロピラニル）ヒダントインの製法及びその中間体
JP2006045107A (ja) * 2004-08-04 2006-02-16 Ube Ind Ltd ４−テトラヒドロピラニルグリシンの製法
JP2013543850A (ja) * 2010-11-08 2013-12-09 上海医薬工業研究院 新規な化合物、その製造方法および用途

Also Published As

Publication number Publication date
CA2211109A1 (en) 1996-08-22
AR002277A1 (es) 1998-03-11
CN1175953A (zh) 1998-03-11
AU708001B2 (en) 1999-07-29
US6900319B2 (en) 2005-05-31
HRP960075B1 (en) 2004-10-31
BG101835A (bg) 1998-05-29
TR199700803T1 (xx) 1998-02-21
FI973360A7 (fi) 1997-08-15
PL321759A1 (en) 1997-12-22
EP0873356A1 (de) 1998-10-28
BG63697B1 (bg) 2002-09-30
CN1198839C (zh) 2005-04-27
HUP9800263A2 (hu) 1998-06-29
FI973360A0 (fi) 1997-08-15
CZ245797A3 (cs) 1998-06-17
HUP9800263A3 (en) 1998-07-28
HRP960075A2 (en) 1997-12-31
SK104697A3 (en) 1998-11-04
BR9607582A (pt) 1998-07-07
AU4875196A (en) 1996-09-04
US6444817B1 (en) 2002-09-03
MY132115A (en) 2007-09-28
FI973360L (fi) 1997-08-15
SI9620037A (sl) 1998-02-28
IL117165A0 (en) 1996-06-18
NZ302649A (en) 2000-01-28
MX9706069A (es) 1997-10-31
US20020169318A1 (en) 2002-11-14
WO1996025426A1 (de) 1996-08-22
KR19980702285A (ko) 1998-07-15
EA199700186A1 (ru) 1998-02-26
TW450968B (en) 2001-08-21
US6030972A (en) 2000-02-29
KR100388185B1 (ko) 2003-11-28
NO973764D0 (no) 1997-08-15
NO973764L (no) 1997-10-15

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