专利号:US-6630602-B1 优先权日:1998-04-16 标题 :Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them 发明人:BIALER MEIR; SPIGELSTEIN OFER; YAGEN BORIS 权利人:YISSUM RES DEV CO 摘要:The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I:wherein R1 is a methyl or ethyl group; R2 is H, methyl or an ethyl group; R3 is ethyl or a propyl group; and R4 is a hydroxyl or amide group; and the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to. The present invention further relates to a method for the stereoselective synthesis of the 2S and 2R stereoisomer of PID and PIA. The present invention also relates to pharmaceutical compositions containing as an active ingredient a racemic mixture or stereoisomers of the compounds of the general formula (I), which are useful for the treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.
专利号:US-6969732-B2 优先权日:1999-04-12 标 题 :Propylisopropyl acetic acid and propylisopropyl acetamide stereoisomers, a method for their synthesis and pharmaceutical compositions containing them 发明人:BIALER MEIR; SPIGELSTEIN OFER; YAGEN BORIS 权利人:YISSUM RES DEV CO 摘要:The present invention relates to racemic propylisopropyl acetic acid and propylisopropyl acetamide and their isomers in their racemic and stereospecific forms, for use in treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines. The isomers are of the compound formula I n n R 1 is a methyl or ethyl group; R 2 is H, methyl or an ethyl group; R 3 is ethyl or a propyl group; and R 4 is a hydroxyl or amide group,n nand the total number of carbon atoms in said compound is 8, provided that when R1 is a methyl group and R4 is an amide group, R2 and R3 are not ethyl, further provided that when R1 is an ethyl and R4 a hydroxyl group, only stereoisomers of the compound are referred to.n nn The present invention further relates to a method for the stereoselective synthesis of the 2R stereoisomer of PID and PIA. The present invention also relates to pharmaceutical compositions containing as an active ingredient a racemic mixture or stereoisomers of the compounds of the general formula (I), which are useful for the treatment of neurological and psychotic disorders, and affective disorders and to treat pain, headaches and migraines.
专利号:WO-9630393-A1 优先权日:1995-03-27 标 题:A method for the synthesis of mixtures of compounds 发明人:BECKER KATHERINE; DEWITT SHEILA HOBBS 权利人:WARNER LAMBERT CO 摘要:Described is a method of synthesizing a plurality of compounds in a plurality of wells comprising the steps of: (a) providing a plurality of test wells in a plurality of arrays of the wells; (b) reacting in at least a one step reaction a first reagent with a plurality of reagents called building blocks in the test well to obtain a unique product designed to be the same in each array; and (c) continuing to react reagents such that there are multiple reagents resulting in mixtures of multiple different products in each well.
专利号:US-12280059-B2 优先权日:2019-02-21 标题 :Acyl-CoA synthetase 4 (ACSL4) inhibitory compound 发明人:PODESTÃ? ERNESTO J; MALOBERTI PAULA M; ORLANDO ULISES D; CASTILLO ANA F; SOLANO ANGELA R; LORENZANO MENNA PABLO; GOMEZ DANIEL E; SZAJNMAN SERGIO H; PRADA JESSICA G; RODRIGUEZ JUAN B 权利人:CONSEJO NACIONAL DE INVESTIGACIONES CIENTIFICAS Y TECN CONICET; UNIV NACIONAL DE QUILMES; UNIV BUENOS AIRES 摘要:A new compound of formula A for the treatment of aggressive and/or resistant tumors expressing acyl-CoA synthetase 4 (ACSL4) and/or depending on steroids action. More particularly, the compound of the present invention inhibits tumor growth in ACSL4-expressing breast and prostate cancers, inhibits steroid synthesis and sensitizes cells towards chemotherapeutic and hormone therapy agents. Pharmaceutical compositions comprising the ACSL4-inhibitory compound of the invention, pharmaceutical combinations thereof with other anticancer agents and use in therapy.