YU97292A - N-fenilalanil i n-fenilglicil derivati dipeptida l-azetidin-2-karboksilne kiseline - Google Patents

N-fenilalanil i n-fenilglicil derivati dipeptida l-azetidin-2-karboksilne kiseline

Info

Publication number
YU97292A
YU97292A YU97292A YU97292A YU97292A YU 97292 A YU97292 A YU 97292A YU 97292 A YU97292 A YU 97292A YU 97292 A YU97292 A YU 97292A YU 97292 A YU97292 A YU 97292A
Authority
YU
Yugoslavia
Prior art keywords
formula
group
lower alkyl
hydrogen
radical
Prior art date
Application number
YU97292A
Other languages
English (en)
Inventor
R.T. Shuman
Original Assignee
Eli Lilly And Company
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 Eli Lilly And Company filed Critical Eli Lilly And Company
Publication of YU97292A publication Critical patent/YU97292A/sh

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

N-FENILALANIL I N-FENILGLICIL DERIVATI DIPEPTIDA L-AZETIDIN-2-KARBOKSILNE KISELINE, opisani su N-fenilalanil i N-fenilglicil derivati dipeptida L-azetidin-2-karboksilne kiseline formule u kojoj je A 1) grupa formule gde je R fenil grupa formule u kojoj su a i a' nezavisno vodonik, nizi alkil, nizi alkoksi, halogen, trifluorometil, hidroksi; hidroksimetil, amino, ili aminometil; a n je 0 ili 1; ili R je tienil, furil, naftil, ili naftil mono- ili disupstituisani nizim alkilom, nizim alkoksi, halogenom, amino, mono- ili di-(nizi alkil)amino, ili hidroksi; ili R je cikloheksandienil, cikloheksenil, cikloheksil ili ciklopentil; R1 je vodonik, metil ili etil; B je nizi alkil, nizi alkoksi, hidroksi, ili amino grupa formule -N(R2) (R3) gde su R2 i R3 nezavisno vodonik ili nizi alkil, ili R2 je vodoik, a R3 je C1-C6 alkanoil, halo supstituisani C2-C6 alkanoil, ili oksikarbonil grupa formule R4-OC(O)-gdeje R4 C1-C6 alkil, C2-C6 alkenil, C3-C7 cikloalkil, benzil, nitrobenzil, difenilmetil, ili fenil grupa kao sto je napred definisano; pod uslovom da, kada je R1 metil ili etil, B je drugaciji od metala ili etila; 2) biciklicna grupa formule 2 u kojoj je Q radikal sa jednim ugljenikovim atomom predstavljen sa , -CH2-, ili ili radikal sa dva ugljenikova atoma predstavljen sa -CH2-CH2-, , ili ; Y je radikal sa jednim ugljenikovim atomom predstalvjen sa -CH2- ili , ili radikal sa dva ugljenikova atoma predstavljen sa ; pod uslovom da je jedno, ali ne i oba Q i Y ili ; i dalje pod uslovom daje samo jedno Q i Y radikal sa dva ugljenikova atoma; R5 je vodonik ili oksikarbonil grupa, R4-OC(O)-, kao sto je napred definisano; a R6 je vodonik, nizi alkil, nizi alkoksi, halogen, hidroksi, trifluorometil, karboksi, karbamoil, ili aminosulfonil; a tackaste linije u okviru 6-clanog prstena oznacavaju aromaticni prsten ili perhidro prsten; i njihove farmaceutski prihvatljive, ne-toksicne soli, kao i postupak za njihovo dobijanje.
YU97292A 1991-11-12 1992-11-11 N-fenilalanil i n-fenilglicil derivati dipeptida l-azetidin-2-karboksilne kiseline YU97292A (sh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US79088591A 1991-11-12 1991-11-12

Publications (1)

Publication Number Publication Date
YU97292A true YU97292A (sh) 1995-10-24

Family

ID=25152024

Family Applications (1)

Application Number Title Priority Date Filing Date
YU97292A YU97292A (sh) 1991-11-12 1992-11-11 N-fenilalanil i n-fenilglicil derivati dipeptida l-azetidin-2-karboksilne kiseline

Country Status (19)

Country Link
EP (1) EP0542525B1 (sh)
JP (1) JP3159806B2 (sh)
KR (1) KR930009993A (sh)
CN (1) CN1074438A (sh)
AU (2) AU646767B2 (sh)
BR (1) BR9204361A (sh)
CA (1) CA2082748A1 (sh)
CZ (1) CZ333492A3 (sh)
DE (1) DE69226152T2 (sh)
ES (1) ES2120993T3 (sh)
FI (1) FI925124A (sh)
HU (1) HUT65858A (sh)
IL (1) IL103692A0 (sh)
MX (1) MX9206474A (sh)
NO (1) NO924326L (sh)
NZ (1) NZ245039A (sh)
TW (1) TW232686B (sh)
YU (1) YU97292A (sh)
ZA (1) ZA928581B (sh)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9103612D0 (sv) * 1991-12-04 1991-12-04 Astra Ab New peptide derivatives
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
US5780631A (en) * 1993-06-03 1998-07-14 Astra Aktiebolag Starting materials in the synthesis of thrombin and kininogenase inhibitors
US5602101A (en) * 1994-03-04 1997-02-11 Eli Lilly And Company Antithrombotic agents
US5484772A (en) * 1994-03-04 1996-01-16 Eli Lilly And Company Antithrombotic agents
CA2143533A1 (en) * 1994-03-04 1995-09-05 Kenneth D. Kurz Antithrombotic agents
US5885967A (en) * 1994-03-04 1999-03-23 Eli Lilly And Company Antithrombotic agents
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5439888A (en) * 1994-03-04 1995-08-08 Eli Lilly And Company Antithrombotic agents
US5436229A (en) * 1994-03-04 1995-07-25 Eli Lilly And Company Bisulfite adducts of arginine aldehydes
US5488037A (en) * 1994-03-04 1996-01-30 Eli Lilly And Company Antithrombotic agents
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
ZA951618B (en) * 1994-03-04 1996-08-27 Lilly Co Eli Antithrombotic agents
CA2184188A1 (en) * 1994-03-04 1995-09-08 Aaron Leigh Schacht Antithrombotic agents
ZA951617B (en) * 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
SE9404196D0 (sv) * 1994-12-02 1994-12-02 Astra Ab New antithrombotic formulation
NZ302649A (en) * 1995-02-17 2000-01-28 Basf Ag Dipeptide amidine derivatives, preparation and pharmaceutical compositions thereof
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
SA96170106A (ar) * 1995-07-06 2005-12-03 أسترا أكتيبولاج مشتقات حامض أميني جديدة
TWI238827B (en) 1995-12-21 2005-09-01 Astrazeneca Ab Prodrugs of thrombin inhibitors
SE9602263D0 (sv) 1996-06-07 1996-06-07 Astra Ab New amino acid derivatives
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds
WO1998051684A1 (en) 1997-05-15 1998-11-19 Eli Lilly And Company Antithrombotic compound
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
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
WO1999037668A1 (de) 1998-01-26 1999-07-29 Basf Aktiengesellschaft Thrombininhibitoren
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
NZ512714A (en) 1999-01-13 2003-10-31 Astrazeneca Ab Amidinobenzylamine derivatives useful as thrombin inhibitors
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
WO2001079208A1 (fr) * 2000-04-19 2001-10-25 Kaneka Corporation Nouveau derive d'azetidine et procede de preparation de celui-ci
SE0001803D0 (sv) 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
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
AR034517A1 (es) 2001-06-21 2004-02-25 Astrazeneca Ab Formulacion farmaceutica
SE0201659D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
SE0201661D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab New salts
US7781424B2 (en) 2003-05-27 2010-08-24 Astrazeneca Ab Modified release pharmaceutical formulation
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
JP2009528843A (ja) * 2006-03-06 2009-08-13 ヒューマジーン・インコーポレイテッド 組換えヒトトロンビンおよびフィブリノゲンの調製法
CN101190895B (zh) * 2006-11-30 2010-05-26 首都医科大学 N-[(3s)-1,2,3,4-四氢异喹啉-3-甲酰基]氨基酸、其制备方法及应用
TW200827336A (en) 2006-12-06 2008-07-01 Astrazeneca Ab New crystalline forms
CN101318933B (zh) * 2007-06-04 2010-08-11 北京大学 具有抗血栓活性的异喹啉化合物、其制备方法及应用
CN102127097A (zh) * 2010-01-15 2011-07-20 首都医科大学 N-（3s-1,2,3,4-四氢异喹啉-3-甲酰基）氨基酸铜络合物及其制备方法和应用

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4318904A (en) * 1980-04-25 1982-03-09 Research Corporation Peptide affinity labels for thrombin and other trypsin-like proteases
HU192646B (en) * 1984-12-21 1987-06-29 Gyogyszerkutato Intezet Process for preparing new n-alkyl-peptide aldehydes
SE9102462D0 (sv) * 1991-08-28 1991-08-28 Astra Ab New isosteric peptides

Also Published As

Publication number Publication date
DE69226152T2 (de) 1998-12-10
FI925124A0 (fi) 1992-11-11
AU2829892A (en) 1993-05-13
NZ245039A (en) 1994-12-22
EP0542525A3 (en) 1994-06-29
NO924326L (no) 1993-05-14
AU2831292A (en) 1993-05-13
DE69226152D1 (de) 1998-08-13
EP0542525A2 (en) 1993-05-19
CN1074438A (zh) 1993-07-21
CZ333492A3 (en) 1993-09-15
EP0542525B1 (en) 1998-07-08
HUT65858A (en) 1994-07-28
KR930009993A (ko) 1993-06-21
BR9204361A (pt) 1993-06-01
HU9203545D0 (en) 1993-01-28
CA2082748A1 (en) 1993-05-13
JP3159806B2 (ja) 2001-04-23
FI925124A (fi) 1993-05-13
JPH05221964A (ja) 1993-08-31
ES2120993T3 (es) 1998-11-16
ZA928581B (en) 1994-05-06
TW232686B (sh) 1994-10-21
IL103692A0 (en) 1993-04-04
MX9206474A (es) 1993-10-01
AU646767B2 (en) 1994-03-03
NO924326D0 (no) 1992-11-10

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