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1. CN1264368 - Polyhydroxybutylpyrazines, their preparation and medicines containing them

Office Chine
Numéro de la demande 98807197.5
Date de la demande 15.07.1998
Numéro de publication 1264368
Date de publication 23.08.2000
Type de publication A
CIB
A61K 31/495
ANÉCESSITÉS COURANTES DE LA VIE
61SCIENCES MÉDICALE OU VÉTÉRINAIRE; HYGIÈNE
KPRÉPARATIONS À USAGE MÉDICAL, DENTAIRE OU POUR LA TOILETTE
31Préparations médicinales contenant des ingrédients actifs organiques 
33Composés hétérocycliques
395ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines
495ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p.ex. pipérazine
C07D 241/12
CCHIMIE; MÉTALLURGIE
07CHIMIE ORGANIQUE
DCOMPOSÉS HÉTÉROCYCLIQUES
241Composés hétérocycliques contenant des cycles diazine-1,4 ou diazine-1,4 hydrogéné
02non condensés avec d'autres cycles 
10comportant trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques
12avec uniquement des atomes d'hydrogène, des radicaux hydrocarbonés ou des radicaux hydrocarbonés substitués, liés directement aux atomes de carbone du cycle
CPC
A61K 31/495
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
C07D 241/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
241Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02not condensed with other rings
10having three double bonds between ring members or between ring members and non-ring members
12with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
Déposants Rhone-Poulenc Rorer S. A.
罗纳-布朗克罗莱尔股份有限公司
Inventeurs G. Bashiardes
G·巴施阿迪斯
J-C. Carry
J-C·卡瑞
M. Evers
M·艾沃斯
B·菲洛奇
S·米格纳尼
Mandataires chen wenbeng
中国国际贸易促进委员会专利商标事务所
Données relatives à la priorité 97/09059 17.07.1997 FR
Titre
(EN) Polyhydroxybutylpyrazines, their preparation and medicines containing them
(ZH) 多羟基丁基吡嗪、其制备方法和含有它们的药物
Abrégé
(EN)
The invention concerns medicines containing as active principle at least one compound of formula (I) in which: either (A) R9 and R10 represent each a -CH2OH radical and either R3 represents a methylene radical, R4 represents a -CHOH- radical and one of the radicals R1, R2, R5 and R6 represents a carbonyl, methylene, -CHF-, -CH(NHR7)- or -CH(OR8) radical and the others represent each a -CHOH-radical, or R2 and R5 represent each a -CHOH- radical, R3 represents a methylene radical and R1, R4 and R6 are identical and represent each a carbonyl, methylene, -CHF-, -CH(NHR7)- or -CH(OR8), or R1 and R6 represent each a -CHOH- radical, R3 represents a methylene radical and R2, R4 and R5 are identical and represent each a carbonyl, methylene, -CHF-, -CH(NHR7)- or -CH(OR8) radical, or R1, R4, R5 and R6 represent each a -CHOH- radical and -R2-R3- represents a -CH=CH-; or (B) R1, R2, R4, R5 and R6 represent each a -CHOH- radical, R3 represents a methylene radical, R9 represents a -CH2F or -CH2OH radical, R10 represents a -CH2F or -CH2OH, provided that R9 and R10 are not both a -CH2OH radical, the novel compounds of formula (I) and the method for preparing them.

(ZH)

本发明涉及含有至少一种式(Ⅰ)化合物或其一种立体异构体或这种化合物的盐作为活性组分的药物,其中(A)R9和R10每个代表-CH2OH,而R3代表亚甲基,R4代表-CHOH-,R1、R2、R5和R6中的一个代表羰基、亚甲基、-CHF-、-CH(NHR7)-或-CH(OR8),其他每个代表-CHOH-,或者R2和R5每个代表-CHOH-,R3代表亚甲基,R1、R4和R6相同,每个代表羰基、亚甲基、-CHF-、-CH(NHR7)-或-CH(OR8),或者R1和R6每个代表-CHOH-基,R3代表亚甲基,R2、R4和R5相同,每个代表羰基、亚甲基、-CHF-、-CH(NHR7)-或-CH(OR8),或者R1、R4、R5和R6每个代表-CHOH-而-R2-R3-代表-CH=CH-,或者(B)R1、R2、R4、R5和R6每个代表-CHOH-,R3代表亚甲基,R9代表-CH2F或-CH2OH,R10代表-CH2F或-CH2OH,但R9和R10不都是-CH2OH,还涉及新的式(Ⅰ)化合物及其制备方法。