CAS: 138117-50-7; 4-(3-(6-Oxo-3H-Purin-9(6H)-yl)Propanamido)Benzoic Acid

专利信息

专利号:US-6849735-B1
优先权日:2000-06-23
标 题:Methods of synthesis for 9-substituted hypoxanthine derivatives
发明人：GLASKY ALVIN J; BOLLINGER HEINRICH; MUELLER HANS RUDOLF
权利人:MERCK EPROVA AG
摘要:An improved method of synthesis of a 9-substituted hypoxanthine derivative comprises the steps of: (1) reacting aminocyanacetamide with triethyl orthoformate to form an imidoester derivative of aminocyanacetamide; (2) forming a compound having a reactive amino group on a hydrocarbyl moiety, the hydrocarbyl moiety being linked through an amide group to a physiologically active moiety or an esterified derivative of a physiologically active moiety including therein an esterified benzoyl group; (3) reacting the imidoester with the compound having the reactive amino group on the hydrocarbyl moiety to form a derivative of aminoimidazole-4-carboxamide substituted at the 1-position with a hydrocarbyl moiety linked through an amide group to a physiologically active moiety including therein an optionally esterified benzoyl group; (4) forming the six-membered heterocyclic ring of the purine moiety of the hypoxanthine by reacting the derivative of 5-aminoimidazole-4-carboxamide formed in step (3) with triethyl orthoformate to form a 9-substituted hypoxanthine compound substituted at the 9-position with a hydrocarbyl moiety linked through an amide group to a physiologically active moiety including therein an optionally esterified benzoyl group; and (5) hydrolyzing the ester of the optionally esterified benzoyl group if present.

专利号:US-2002040032-A1
优先权日:2000-07-07
标 题:Methods for stimulation of synthesis of synaptophysin in the central nervous system
发明人：GLASKY MICHELLE S; LAHIRI DEBOMOY K; FARLOW MARTIN R
摘要:A method of increasing the synthesis and/or secretion of synaptophysin comprises administering to a patient with a neurological disease or a patient at risk of developing a neurological disease an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The neurological disease can be a neurodegenerative disease such as Alzheimer's disease or a neurodevelopmental disorder such as Down's syndrome. Typically, the compound can pass through the blood-brain barrier. The purine moiety can be hypoxanthine or guanine. A particularly preferred purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide.

专利号:US-6407237-B1
优先权日:2001-02-21
标题 :Crystal forms of 9-substituted hypoxanthine derivatives
发明人：GLASKY ALVIN J; BOLLINGER HEINRICH; MUELLER HANS RUDOLF
权利人:NEOTHERAPEUTICS INC
摘要:The bifunctional compound N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide monopotassium salt occurs in a number of crystal forms which differ in their stability. Of these forms, the most stable is designated Type I, which is a monopotassium salt monohydrate in which the water is held as water of crystallization. Other crystalline forms, designated Type II and Type III, convert to Type I. Methods are disclosed for the synthesis of Type I and for the conversion of Type II or Type III to Type I.

专利号:US-6297226-B1
优先权日:1999-10-15
标 题 :Synthesis and methods of use of 9-substituted guanine derivatives
发明人：GLASKY ALVIN J
权利人:NEOTHERAPEUTICS INC
摘要:The present invention is directed to 9-substituted guanine derivatives in which the guanine moiety is linked to another moiety with physiological or pharmacological activity through a carboxamide linkage. The number of carbon atoms between the guanine moiety and the carboxamide linking group is typically from 1 to 6. In some cases, the chemical moieties can have carbon chains of different lengths within the moiety linked to guanine through the carboxamide linker. A large number of different chemical moieties can be linked to the guanine moiety. The invention also includes pharmaceutical compositions including the 9-substituted guanine derivatives and methods of use of the 9-substituted guanine derivatives.

专利号:WO-0204451-A2
优先权日:2000-07-07
标 题:Methods for stimulation of synthesis of synaptophysin in the central nervous system

专利号:WO-0204451-A3
优先权日:2000-07-07
标 题 :Methods for stimulation of synthesis of synaptophysin in the central nervous system