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JO2994B1 - مثبطات البروتين الناقل لاستر الكولسترول ( cetp ) - Google Patents

مثبطات البروتين الناقل لاستر الكولسترول ( cetp )

Info

Publication number
JO2994B1
JO2994B1 JOP/2005/0091A JOP20050091A JO2994B1 JO 2994 B1 JO2994 B1 JO 2994B1 JO P20050091 A JOP20050091 A JO P20050091A JO 2994 B1 JO2994 B1 JO 2994B1
Authority
JO
Jordan
Prior art keywords
cetp
inhibitors
transfer protein
cholesterol ester
ester transfer
Prior art date
Application number
JOP/2005/0091A
Other languages
English (en)
Inventor
Ali Amjad
J Sinclair Peter
E Taylor Gayle
M Napolitano Joann
A Hunt Julianne
Lu Zhijian
J Smith Cameron
F Thompson Christopher
Deng Qiaolin
Quraishi Nazia
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Application granted granted Critical
Publication of JO2994B1 publication Critical patent/JO2994B1/ar

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/4015—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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • A—HUMAN NECESSITIES
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
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    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
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Abstract

مركبات لها تركيبات الصيغة 1 وتشمل الأملاح المقبولة صيدلانياً من هذه المركبات وهي عبارة عن مثبطات بروتين نقل استرات الكولسترول CETP وهي مفيدة في رفع كولسترول HDL وخفض كولسترول LDL وكذلك من أجل المعالجة والوقاية من التصلب العصيدي. وفي مركبات الصيغة I, B or R2 عبارة عن مجموعة فنيل لها بدائل اوثو اريل، هثرو سايكليك، بنزوهترو ساكليك أو بنزو سايكلو الكي، وموقع آخر على حلقة من 5 أعضاء ولها بديل اروماثي وهتيرو سايكليك وسايكلو الكيل وبنزو هترو سايكليك أو بنزو سايكلو الكي متصلة مباشرة بالحلقة أو متصلة بالحلقة من خلال CH2 .
JOP/2005/0091A 2004-07-02 2005-06-26 مثبطات البروتين الناقل لاستر الكولسترول ( cetp ) JO2994B1 (ar)

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