DIAZEPAN DERIVATE ALS FAKTOR X INHIBITOR

Diazepane derivatives (I) are new. Diazepane derivatives of formula (I) and their salts are new. [Image] A : aryl or heteroaryl (both optionally substituted by 1-3 substituents); B : arylene or heteroarylene (both optionally substituted by 1-3 substituents); X 1CONR 4, NR 4CO, NR 4CH 2, OCH 2, CH 2O...

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Main Authors KOSHIO, HIROYUKI, KOGA, YUJI, SHIGENAGA, TAKESHI, HIRAYAMA, FUKUSHI, SEKI, NORIO, MIYUKIGAOKA, ISHIHARA, TSUKASA, SUGASAWA, KEIZO, KAWAZOE, SOUCHIROU, HACHIYA, SHUNICHIRO, MATSUMOTO, YUZO, MATSUKUBO OAZA AKAHAMA, SHIRAKI, RYOTA
Format Patent
LanguageGerman
Published 15.10.2006
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:Diazepane derivatives (I) are new. Diazepane derivatives of formula (I) and their salts are new. [Image] A : aryl or heteroaryl (both optionally substituted by 1-3 substituents); B : arylene or heteroarylene (both optionally substituted by 1-3 substituents); X 1CONR 4, NR 4CO, NR 4CH 2, OCH 2, CH 2O or CH=CH; X 3CONR 5or NR 5CO; R 1H, Alk (optionally substituted by aryl or heteroaryl), AlkOAlk, Cyc, aryl, heteroaryl, CycAlk or C=NR 6; Alk : lower alkyl; Cyc : 3-8C cycloalkyl; R 2OH, OAlk, OAlkOH, OSO 2OH, OSO 2AlkCOOH, OAlkCOOAlk, COOH, COOAlk or halo; R 3H, halo or Alk, and R 4-R 6H or Alk. ACTIVITY : Thrombolytic; anticoagulant; cerebroprotective; hemostatic; cardiant; antianginal; respiratory. MECHANISM OF ACTION : Factor-X inhibitor. In an assay using human factor Xa, 3-hydroxy-4'-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide (Ia) hydrochloric acid salt exhibited a CT 2of 1.71 mu M.
Bibliography:Application Number: AT20030029061T