专利号:US-9981949-B2 优先权日:2008-12-01 标题 :Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine 发明人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT 权利人:OYSTER POINT PHARMA INC 摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
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-2016111658-A1 优先权日:2015-01-07 标 题:Synthesis of thiosemicarbazone derivatives comprising sulphonamide group with potential anticonvulsant activity 发明人:IYIDOGAN AYSEGUL; EMRE EMINE ELCIN; TOPALFAKIOGÄžLU RAHIME BETÜL; KAYMAKÇIOÄžLU BEDIA; ARICIOÄžLU FEYZA 权利人:IYIDOGAN AYSEGUL; EMRE EMINE ELCIN 摘要:The present invention relates to the synthesis method of thiosemicarbazone derivatives comprising sulphonamide group and having high anticonvulsant/antiepileptic activity.
专利号:US-6417399-B1 优先权日:1997-01-14 标 题:Amelioration of neurological disorders by the administration of (2R),(3S), and/or (2S),3(S) stereoisomers of valnoctamide 发明人:BIALER MEIR; YAGEN BORIS; SPIEGELSTEIN OFER; ROEDER MICHAEL; SCHURIG VOLKER 权利人:YISSUM RES DEV CO 摘要:The present invention generally relates to the individual stereoisomers of the drug valnoctamide (a mixture of four stereoisomer kinds, VCD-valmethamide or 2-ethyl-3-methyl pentanamide) useful in treatment of neurological and psychotic disorders such as different kinds of epilepsy and affective disorders, and useful as tranquilizers and to treat pain, and to pharmaceutical compositions containing, as an active ingredient, these stereoisomers. The present invention further relates to a method for stereoselective separation and quantification of the four stereoisomers from a racemic mixture of VCD or plasma of patients treated with the racemic drug. The present invention further relates to a unique method for the synthesis of the individual stereoisomers.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
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