UA78195C2 - Производные миндальной кислоты и их применения в качестве ингибиторов тромбина, фармацевтическая композиция на их основе - Google Patents

Производные миндальной кислоты и их применения в качестве ингибиторов тромбина, фармацевтическая композиция на их основе Download PDF

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UA78195C2
UA78195C2 UA2003054395A UA2003054395A UA78195C2 UA 78195 C2 UA78195 C2 UA 78195C2 UA 2003054395 A UA2003054395 A UA 2003054395A UA 2003054395 A UA2003054395 A UA 2003054395A UA 78195 C2 UA78195 C2 UA 78195C2
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rotamer
mixture
nmr
pab
age
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UA2003054395A
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English (en)
Ukrainian (uk)
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Тод ІНҐГАРДТ
Андерс ЙОГАНССОН
Арне СВЕНССОН
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Astrazeneca Ab
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Priority claimed from SE0102921A external-priority patent/SE0102921D0/xx
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Priority claimed from PCT/SE2001/002657 external-priority patent/WO2002044145A1/en
Publication of UA78195C2 publication Critical patent/UA78195C2/ru

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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07C205/59—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
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    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
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    • C07C45/71—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
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    • C07C59/40—Unsaturated compounds
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    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/732—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids
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    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
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    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
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    • 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
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    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
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    • 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
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    • 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
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    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Предложены соединения формулы 1, в которой Ra, R1, R2 и Y определены в описании, и их фармацевтически приемлемые производные (включая пролекарства), соединения и производные, которые могут применяться сами по себе или в качестве пролекарств, в качестве конкурентных ингибиторов трипсиноподобных сериновых протеаз, таких как тромбин, в частности при лечении состояний, где требуется ингибирование тромбина (например тромбоза), или в качестве антикоагулянтов.
UA2003054395A 2001-08-30 2001-11-30 Производные миндальной кислоты и их применения в качестве ингибиторов тромбина, фармацевтическая композиция на их основе UA78195C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE0102921A SE0102921D0 (sv) 2001-08-30 2001-08-30 Pharmaceutically useful compounds
PCT/SE2001/002657 WO2002044145A1 (en) 2000-12-01 2001-11-30 New mandelic acid derivatives and their use as throbin inhibitors

Publications (1)

Publication Number Publication Date
UA78195C2 true UA78195C2 (ru) 2007-03-15

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UA2003054395A UA78195C2 (ru) 2001-08-30 2001-11-30 Производные миндальной кислоты и их применения в качестве ингибиторов тромбина, фармацевтическая композиция на их основе

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EP (1) EP1423362B1 (ru)
JP (1) JP4386724B2 (ru)
CN (1) CN1301969C (ru)
AT (1) ATE435201T1 (ru)
AU (1) AU2002324410B2 (ru)
BR (1) BR0211847A (ru)
CA (1) CA2456426C (ru)
DE (1) DE60232802D1 (ru)
ES (1) ES2326963T3 (ru)
HU (1) HUP0401189A2 (ru)
IL (1) IL160068A0 (ru)
IS (1) IS7162A (ru)
NO (1) NO326496B1 (ru)
NZ (1) NZ531109A (ru)
PL (1) PL369325A1 (ru)
RU (1) RU2341516C2 (ru)
UA (1) UA78195C2 (ru)
UY (1) UY27425A1 (ru)
WO (1) WO2003018551A1 (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0201659D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
GB0503672D0 (en) * 2005-02-23 2005-03-30 Astrazeneca Ab New process
WO2008135525A2 (en) * 2007-05-02 2008-11-13 Boehringer Ingelheim International Gmbh Substituted azetidines, manufacturing and use thereof as medicaments
CA2727925A1 (en) * 2008-06-23 2009-12-30 Astrazeneca Ab New heterocyclic carboxamides for use as thrombin inhibitors

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SA96170106A (ar) * 1995-07-06 2005-12-03 أسترا أكتيبولاج مشتقات حامض أميني جديدة
ES2295004T3 (es) * 1999-01-13 2008-04-16 Astrazeneca Ab Nuevos derivados amidinobencilaminicos y su uso como inhibidores de trombina.

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HUP0401189A2 (hu) 2004-12-28
AU2002324410B2 (en) 2008-04-24
EP1423362B1 (en) 2009-07-01
CA2456426C (en) 2011-01-11
ATE435201T1 (de) 2009-07-15
EP1423362A1 (en) 2004-06-02
IL160068A0 (en) 2004-06-20
CA2456426A1 (en) 2003-03-06
NO326496B1 (no) 2008-12-15
ES2326963T3 (es) 2009-10-22
PL369325A1 (en) 2005-04-18
CN1301969C (zh) 2007-02-28
RU2341516C2 (ru) 2008-12-20
DE60232802D1 (de) 2009-08-13
JP2005504057A (ja) 2005-02-10
WO2003018551A1 (en) 2003-03-06
RU2004103625A (ru) 2005-06-20
IS7162A (is) 2004-02-26
NZ531109A (en) 2006-03-31
CN1549808A (zh) 2004-11-24
JP4386724B2 (ja) 2009-12-16
NO20040813L (no) 2004-02-24
UY27425A1 (es) 2003-03-31
BR0211847A (pt) 2004-09-08

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