CN1066712C - 脯氨酰胺衍生物 - Google Patents

脯氨酰胺衍生物 Download PDF

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Publication number
CN1066712C
CN1066712C CN95100042A CN95100042A CN1066712C CN 1066712 C CN1066712 C CN 1066712C CN 95100042 A CN95100042 A CN 95100042A CN 95100042 A CN95100042 A CN 95100042A CN 1066712 C CN1066712 C CN 1066712C
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China
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alkyl
unsubstituted
substituted
alkoxy
group
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Expired - Fee Related
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CN95100042A
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English (en)
Chinese (zh)
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CN1121068A (zh
Inventor
大岛正裕
杉山重夫
兴津操
盛中泰洋
岩濑德道
菅原浩一
玉尾嘉邦
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Mitsubishi Chemical Corp
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Mitsubishi Chemical Corp
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Anticipated expiration legal-status Critical
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    • 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
    • C07D207/08—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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/60—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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • C07K5/06069—Ser-amino acid
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C07K5/06113—Asp- or Asn-amino acid
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN95100042A 1994-01-27 1995-01-27 脯氨酰胺衍生物 Expired - Fee Related CN1066712C (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP007733/1994 1994-01-27
JP007733/94 1994-01-27
JP773394 1994-01-27

Publications (2)

Publication Number Publication Date
CN1121068A CN1121068A (zh) 1996-04-24
CN1066712C true CN1066712C (zh) 2001-06-06

Family

ID=11673914

Family Applications (1)

Application Number Title Priority Date Filing Date
CN95100042A Expired - Fee Related CN1066712C (zh) 1994-01-27 1995-01-27 脯氨酰胺衍生物

Country Status (16)

Country Link
US (1) US5744487A (enExample)
EP (1) EP0669317B1 (enExample)
KR (1) KR950032114A (enExample)
CN (1) CN1066712C (enExample)
AT (1) ATE223378T1 (enExample)
AU (1) AU1025795A (enExample)
CA (1) CA2140598C (enExample)
DE (1) DE69528005T2 (enExample)
ES (1) ES2182852T3 (enExample)
FI (1) FI950309A7 (enExample)
HU (1) HUT72062A (enExample)
NO (1) NO950297L (enExample)
NZ (1) NZ270395A (enExample)
RU (1) RU95101048A (enExample)
TW (1) TW306917B (enExample)
ZA (1) ZA95631B (enExample)

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US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
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US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5561146A (en) * 1994-06-10 1996-10-01 Bristol-Myers Squibb Company Modified guanidino and amidino thrombin inhibitors
DE4421052A1 (de) * 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
DE4443390A1 (de) * 1994-12-06 1996-06-13 Basf Ag Neue dipeptidische p-Amidinobenzylamide mit N-terminalen Sulfonyl- bzw. Aminosulfonylresten
CA2210989A1 (en) * 1995-02-10 1996-08-15 Basf Aktiengesellschaft Thrombin inhibitors
SI9620037A (sl) * 1995-02-17 1998-02-28 Basf Aktiengesellschaft Novi trombinski inhibitorji
US5914319A (en) * 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
CA2176414A1 (en) * 1995-05-18 1996-11-19 S. David Kimball Acyl guanidine and amidine prodrugs
SA96170106A (ar) * 1995-07-06 2005-12-03 أسترا أكتيبولاج مشتقات حامض أميني جديدة
EP0846682B9 (en) * 1995-07-26 2003-05-14 Mitsubishi Chemical Corporation Penicillaminamide derivatives
TWI238827B (en) 1995-12-21 2005-09-01 Astrazeneca Ab Prodrugs of thrombin inhibitors
AU1990197A (en) * 1996-03-12 1997-10-01 Bristol-Myers Squibb Company Carbamyl guanidine and amidine prodrugs
US5811402A (en) * 1996-03-22 1998-09-22 Eli Lilly And Company Antithrombotic diamides
SE9602263D0 (sv) 1996-06-07 1996-06-07 Astra Ab New amino acid derivatives
WO1997049404A1 (en) 1996-06-25 1997-12-31 Eli Lilly And Company Anticoagulant agents
US6200967B1 (en) 1996-06-25 2001-03-13 Eli Lilly And Company Anticoagulant agents
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds
AR013084A1 (es) 1997-06-19 2000-12-13 Astrazeneca Ab Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados
US6117897A (en) * 1997-11-19 2000-09-12 Mitsubishi Chemical Corporation 1/2 sulfate of a [(S) -1- [(S) -2- [(trans-4- aminocyclohexylmethyl) carbamoyl]pyrrolidine-1-carbonyl]- 2-isopropylthio-2-methylpropyl]carbamic acid propyl ester
SE9704543D0 (sv) * 1997-12-05 1997-12-05 Astra Ab New compounds
SE9802939D0 (sv) 1998-09-01 1998-09-01 Astra Ab New process
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
DE60037183T2 (de) 1999-01-13 2008-10-09 Astrazeneca Ab Neue amidinbenzylamin-derivate und ihre verwendung als thrombin-inhibitoren
FR2791683A1 (fr) * 1999-03-30 2000-10-06 Synthelabo Derives de n-sulfonyl-dipeptides, leur preparation et leur application en therapeutique
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
US6316488B1 (en) * 1999-06-17 2001-11-13 Merck & Co., Inc. Antibiotic compound
SE0001803D0 (sv) 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
AU785260B2 (en) * 2000-08-11 2006-12-07 Wilex Ag Non-covalent inhibitors of urokinase and blood vessel formation
ATE517910T1 (de) * 2000-08-11 2011-08-15 Wilex Ag NICHT-KOVALENTE INHIBITOREN VON UROKINASE UND BLUTGEFÄßBILDUNG
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin inhibitors
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
US7129233B2 (en) 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
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US7195759B2 (en) * 2001-06-06 2007-03-27 The University Of Manitoba Therapeutic uses of glandular kallikrein
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AR034517A1 (es) 2001-06-21 2004-02-25 Astrazeneca Ab Formulacion farmaceutica
DK1485345T3 (da) 2002-03-11 2008-11-03 Curacyte Ag Urokinaseinhibitorer, deres fremstilling og anvendelse
SE0201661D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab New salts
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CN102464701B (zh) * 2010-11-08 2015-10-21 上海医药工业研究院 一类新型化合物、其制备方法及用途
CN103403018B (zh) * 2010-12-21 2015-08-19 医药公司（莱比锡）有限公司 胰蛋白酶样丝氨酸蛋白酶抑制剂,它们的制备以及作为凝结因子IIa和Xa的选择性抑制剂的用途
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Also Published As

Publication number Publication date
ZA95631B (en) 1995-10-05
TW306917B (enExample) 1997-06-01
FI950309A0 (fi) 1995-01-24
FI950309L (fi) 1995-07-28
RU95101048A (ru) 1996-10-27
CA2140598C (en) 2010-03-09
HUT72062A (en) 1996-03-28
ES2182852T3 (es) 2003-03-16
KR950032114A (ko) 1995-12-20
US5744487A (en) 1998-04-28
DE69528005T2 (de) 2003-04-17
DE69528005D1 (de) 2002-10-10
AU1025795A (en) 1995-08-03
HU9500240D0 (en) 1995-03-28
NZ270395A (en) 1997-06-24
FI950309A7 (fi) 1995-07-28
ATE223378T1 (de) 2002-09-15
NO950297L (no) 1995-07-28
CA2140598A1 (en) 1995-07-28
EP0669317A1 (en) 1995-08-30
EP0669317B1 (en) 2002-09-04
CN1121068A (zh) 1996-04-24
NO950297D0 (no) 1995-01-26

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