公开(公告)号：US06306859B1

公开(公告)日：2001-10-23

申请号：US09516137

申请日：2000-03-01

Applicant: Wayne E. Childers ,  Michael G. Kelly ,  Gan Zhang ,  Yvette L. Palmer ,  Edward J. Podlesny

Inventor： Wayne E. Childers ,  Michael G. Kelly ,  Gan Zhang ,  Yvette L. Palmer ,  Edward J. Podlesny

IPC: A61K31495

CPC classification number: C07D295/185 ,  C07D295/13 ,  C07D403/10

Abstract: Compounds of the Formula (I) wherein R2, Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic neuron-related diseases.

Abstract translation: 式（I）的化合物，其中R2，Y，X和n如本说明书中所定义，该化合物可用于治疗与5-羟色胺能神经元相关疾病相关的病症。

公开(公告)号：US06239134B1

公开(公告)日：2001-05-29

申请号：US09515049

申请日：2000-02-25

Applicant: Annmarie L. Sabb ,  Robert L. Vogel ,  Michael G. Kelly ,  Yvette L. Palmer ,  Wayne E. Childers

Inventor： Annmarie L. Sabb ,  Robert L. Vogel ,  Michael G. Kelly ,  Yvette L. Palmer ,  Wayne E. Childers

IPC: A61K31496

CPC classification number: C07D285/10 ,  C07D417/12

Abstract: The present invention provides compounds of the general formula (1): wherein: two atoms of X, Y, or Z are nitrogen and the third atom is sulfur or oxygen; R is H, halogen, OH, SH, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, phenoxy, thiophenoxy, phenyl or substituted phenyl; A is C, CH, or N; R1 is aryl, heteroaryl, or cycloalkyl groups, optionally substituted by from 1 to 3 substituents selected from C1-C6 alkyl, C1-C6 alkoxy; CF3, Cl, Br, F, CN, or CO2CH3; R2is H or alkyl R3 is C1-C6 alkyl, optionally substituted aryl, optionally substituted 5- or 6-membered heteroaryl, C3 to C8 cycloalkyl optionally substituted by C1-C6 alkyl, or a 3 to 8-membered heterocyclic ring containing one or more heteroatoms selected from O, S or N; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders using these compounds.

Abstract translation: 本发明提供通式（1）的化合物：其中X，Y或Z的两个原子是氮，第三个原子是硫或氧; R是H，卤素，OH，SH，C 1 -C 6烷基， C 1 -C 6烷氧基，C 1 -C 6硫代烷基，苯氧基，硫代苯氧基，苯基或取代的苯基; A是C，CH或N; R 1是芳基，杂芳基或环烷基，任选地被1至3个选自C1- C6烷基，C1-C6烷氧基; CF 3，Cl，Br，F，CN或CO 2 CH 3; R 2为H或烷基R 3为C 1 -C 6烷基，任选取代的芳基，任选取代的5或6元杂芳基，任选被C 1 -C 6烷基取代的C 3至C 8环烷基， 含有一个或多个选自O，S或N的杂原子的3至8元杂环; 或其药学上可接受的盐，以及使用这些化合物治疗中枢神经系统疾病的药物组合物和方法。

公开(公告)号：US5126367A

公开(公告)日：1992-06-30

申请号：US719881

申请日：1991-06-21

Applicant: Gary P. Stack ,  Magid A. Abou-Gharbia ,  Wayne E. Childers, Jr.

Inventor： Gary P. Stack ,  Magid A. Abou-Gharbia ,  Wayne E. Childers, Jr.

IPC: C07D319/20

CPC classification number: C07D319/20

Abstract: A compound of the formula: ##STR1## wherein the dotted line represents optional unsaturation; R.sup.1 is hydrogen, alkyl, alkoxy, alkanoyloxy, hydroxy, halo, nitro, amino, alkylamino, dialkylamino and alkanoylamino; X is O, S or CH.sub.2 ; n is an integer 2, 3 or 4; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydrogen, lower alkyl, phenyl or benzyl; R.sup.4 is one of the structures ##STR2## in which m is one of the integers 0, 1 or 2; R.sup.5 is H or CH.sub.3 ; Z is H.sub.2 or O; Y is OCO, NHCO, NHCONH, CONH, and in addition, when R.sup.4 is II, Y may be NHSO.sub.2 CH.sub.2 ; or a pharmaceutically acceptable salt thereof are useful as antipsychotic/anxiolytic agents.

Abstract translation: 下式的化合物：其中虚线表示任选的不饱和度; R 1是氢，烷基，烷氧基，烷酰氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基和烷酰基氨基; X是O，S或CH 2; n是整数2,3或4; R2是氢或低级烷基; R3是氢，低级烷基，苯基或苄基; R4是其中m是整数0,1或2之一的结构之一; R5是H或CH3; Z是H 2或O; Y是OCO，NHCO，NHCONH，CONH，另外当R4是II时，Y可以是NHSO2CH2; 或其药学上可接受的盐可用作抗精神病药/抗焦虑剂。