公开(公告)号：US20070088046A1

公开(公告)日：2007-04-19

申请号：US11581950

申请日：2006-10-13

申请人： Paola Ciapetti ,  Laurence Deyon ,  Camille-Georges Wermuth ,  Jean-Francois Pujol ,  Dinah Weissmann

发明人： Paola Ciapetti ,  Laurence Deyon ,  Camille-Georges Wermuth ,  Jean-Francois Pujol ,  Dinah Weissmann

IPC分类号： A61K31/4745 ,  C07D471/22

CPC分类号： C07D461/00

摘要： The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR′ wherein A represents a heteroatom and R′ represents a group selected from the group comprising linear or branched C1-C6 alkyl radicals, C2-C6 alkenyls, C2-C6 alkynyls, arylalkyls; esters comprising the formula —R1— CO—O—R2; amides comprising the formula —R3—CO—NZY, wherein Y and Z together can form a cycloalkyl radical or a heterocyclic radical, optionally substituted by one or more alkyl radicals; a radical selected from the group comprising alkyl radicals, alkenyls or alkynyls, substituted by at least one amine with formula —NZY; or one of the pharmaceutically-acceptable salts thereof, including the isomers, enantiomers and diastereoisomers thereof and mixtures thereof. The invention also relates to the use of the novel derivatives for the preparation of a pharmaceutical composition which is intended, in particular, for the treatment and/or prevention of depression, sleep-wake cycle disorders and symptomatic frontal disorders in cognitive components among humans.

摘要翻译： 本发明涉及具有式（I）的式14所示的衍生物，其中R表示自由基-AR'，其中A表示杂原子，R'表示选自 包括直链或支链C 1 -C 6烷基，C 2 -C 6亚烷基，C 2 -C 6亚烷基， C 2 -C 6炔基，芳基烷基; 包含式-R 1 -CO-O-R 2的酯; 酰胺，其包含式-NR 3 -CO-NZY，其中Y和Z一起可以形成任选被一个或多个烷基取代的环烷基或杂环基; 选自由至少一个具有式-NZY的胺取代的烷基，烯基或炔基的基团; 或其药学上可接受的盐之一，包括其异构体，对映体和非对映异构体及其混合物。 本发明还涉及新型衍生物用于制备药物组合物的用途，其特别用于治疗和/或预防人类中认知成分中的抑郁症，睡眠 - 苏醒循环障碍和症状性前额症。

公开(公告)号：US07354918B2

公开(公告)日：2008-04-08

申请号：US11581950

申请日：2006-10-13

申请人： Paola Ciapetti ,  Laurence Deyon ,  Camille-Georges Wermuth ,  Jean-François Pujol ,  Dinah Weissmann

发明人： Paola Ciapetti ,  Laurence Deyon ,  Camille-Georges Wermuth ,  Jean-François Pujol ,  Dinah Weissmann

IPC分类号： A61K31/5377 ,  A61K31/4375 ,  C07D413/14 ,  C07D471/22

CPC分类号： C07D461/00

摘要： The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical —AR′ wherein A represents a heteroatom and R′ represents a group selected from the group comprising linear or branched C1-C6 alkyl radicals, C2-C6 alkenyls, C2-C6 alkynyls, arylalkyls; esters comprising the formula —R1— CO—O—R2; amides comprising the formula —R3—CO—NZY, wherein Y and Z together can form a cycloalkyl radical or a heterocyclic radical, optionally substituted by one or more alkyl radicals; a radical selected from the group comprising alkyl radicals, alkenyls or alkynyls, substituted by at least one amine with formula —NZY; or one of the pharmaceutically-acceptable salts thereof, including the isomers, enantiomers and diastereoisomers thereof and mixtures thereof. The invention also relates to the use of the novel derivatives for the preparation of a pharmaceutical composition which is intended, in particular, for the treatment and/or prevention of depression, sleep-wake cycle disorders and symptomatic frontal disorders in cognitive components among humans.

摘要翻译： 本发明涉及具有式（I）的式14所示的衍生物，其中R表示自由基-AR'，其中A表示杂原子，R'表示选自 包括直链或支链C 1 -C 6烷基，C 2 -C 6亚烷基，C 2 -C 6亚烷基， C 2 -C 6炔基，芳基烷基; 包含式-R 1 -CO-O-R 2的酯; 酰胺，其包含式-NR 3 -CO-NZY，其中Y和Z一起可以形成任选被一个或多个烷基取代的环烷基或杂环基; 选自由至少一个具有式-NZY的胺取代的烷基，烯基或炔基的基团; 或其药学上可接受的盐之一，包括其异构体，对映体和非对映异构体及其混合物。 本发明还涉及新型衍生物用于制备药物组合物的用途，其特别用于治疗和/或预防人类中认知成分中的抑郁症，睡眠 - 苏醒循环障碍和症状性前额症。

公开(公告)号：US20050261372A1

公开(公告)日：2005-11-24

申请号：US10524869

申请日：2003-08-01

申请人： Kathleen Clarence-Smith ,  Jean-Marie Contreras ,  Laurence Deyon ,  Camille Wermuth

发明人： Kathleen Clarence-Smith ,  Jean-Marie Contreras ,  Laurence Deyon ,  Camille Wermuth

IPC分类号： A61P25/00 ,  A61K31/197 ,  A61K31/198 ,  A61K31/223 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00 ,  C07C229/22 ,  C07C237/12 ,  C07C271/22

CPC分类号： A61K31/197 ,  C07C2601/02

摘要： The use of R(+)-2-amino-3-hydroxypropanoic acid derivatives, nitrogen substituted by a (C1-C6)alkyl, (C3-C6)alkenyl, 3-oxo(C5-C6)alkyl, 3-oxo(C4-C6)alken-2-yl, phenyl(C1-C6)alkyl, phenyl(C2-C6)alkenyl, gem-diphenyl(C1-C6)alkyl, gem-diphenyl(C2-C6)alkenyl, (C1-C6)alcanoyl, optionally N-substituted alanyl, optionally N,N′-disubstituted lysinoyl, phenyl(C1-C6)alkylydene or gem-diphenyl(C1-C6)alkylidene group, and of the pharmaceutically acceptable salts thereof, for preparation of medicaments intended for the treatment of CNS diseases due to reduced glycinergic transmission, particularly for the treatment of autism, schizophrenia and Alzheimer's disease, is described.

摘要翻译： 使用R（+） - 2-氨基-3-羟基丙酸衍生物，被（C 1 -C 6 -C 6）烷基取代的氮，（C 1 -C 6） C 3 -C 6烯基，3-氧代（C 5 -C 6 -C 6）烷基，3-氧代（C < 烷基-2-基，苯基（C 1 -C 6 -C 6）烷基，苯基（C 1 -C 6 - C 2 -C 6 -C 6烯基，偕二苯基（C 1 -C 6 -C 6）烷基，偕 - 二苯基（C 1 -C 6 -C 6）烷基， 二苯基（C 2 -C 6 -C 6）烯基，（C 1 -C 6 -C 6）烷酰基，任选的N- 取代的丙氨酰基，任选的N，N'-二取代的赖氨酰基，苯基（C 1 -C 6 -C 6）烷基或偕二苯基（C 1 -C 6 - C 6 C 6亚烷基及其药学上可接受的盐，用于制备用于治疗由于甘氨酸转运降低引起的CNS疾病的药物，特别是用于治疗孤独症，精神分裂症和阿尔茨海默氏病， 被描述。