公开(公告)号：US06930105B2

公开(公告)日：2005-08-16

申请号：US10271349

申请日：2002-10-15

Applicant: Jian-Min Fu

Inventor： Jian-Min Fu

IPC: A61K31/5383 ,  A61K31/554 ,  A61K51/00 ,  A61P3/04 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  C07D498/22 ,  C07D513/22 ,  C07D265/28

CPC classification number: C07D498/22 ,  C07D513/22

Abstract: The present invention provides compounds of Formula (I): wherein R1, R2, R3, R4, R5, and R6, have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT2C activity is desired.

Abstract translation: 本发明提供式（I）的化合物：其中R 1，R 2，R 3，R 4， >，R 5和R 6具有说明书中定义的任何值，以及包含该化合物的药物组合物。 本发明还提供治疗方法以及可用于制备式（I）化合物的方法和中间体。 该化合物是5-HT配体，并且可用于治疗需要调节5-HT 2C活性的疾病。

公开(公告)号：US20050101613A1

公开(公告)日：2005-05-12

申请号：US10839055

申请日：2004-05-05

Applicant: Jeffrey Corbett ,  Michael Ennis ,  Kristine Frank ,  Jian-Min Fu ,  Robert Hoffman ,  Patrick Verhoest

Inventor： Jeffrey Corbett ,  Michael Ennis ,  Kristine Frank ,  Jian-Min Fu ,  Robert Hoffman ,  Patrick Verhoest

IPC: C07D213/72 ,  C07D239/42 ,  A61K31/506 ,  A61K31/4439 ,  C07D43/02

CPC classification number: C07D239/42 ,  C07D213/72

Abstract: This invention relates to compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with CRF, receptors, including human CRF, receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety-related disorders such as anxiety, and mood disorders such as major depression.

Abstract translation: 本发明涉及式I化合物，其立体异构体，其药学上可接受的盐，其前药或其前药的药学上可接受的盐。 该化合物与CRF，受体（包括人类CRF）受体相互作用。 本发明还涉及使用本发明化合物治疗病症或病症的方法，所述疾病或病症的治疗可以通过拮抗CRF受体如CNS疾病或疾病，特别是焦虑相关疾病例如焦虑来实现或促进 ，以及心理障碍如重度抑郁症。

公开(公告)号：US06465495B1

公开(公告)日：2002-10-15

申请号：US09363877

申请日：1999-07-29

Applicant: Arlindo L. Castelhano ,  Jian-Min Fu

Inventor： Arlindo L. Castelhano ,  Jian-Min Fu

IPC: C07D21302

CPC classification number: C07D213/64 ,  A61K31/4412 ,  A61K31/675 ,  C07D409/04 ,  C07F9/58 ,  C07F9/59

Abstract: Novel pyridone mimetics are disclosed which are useful for the treatment of SH2 domain related diseases.

Abstract translation: 公开了可用于治疗SH2结构域相关疾病的新型吡啶酮模拟物。

公开(公告)号：US5814628A

公开(公告)日：1998-09-29

申请号：US762984

申请日：1996-12-10

Applicant: Jian-Min Fu ,  Ashok Tehim ,  Robert A. Kirby

Inventor： Jian-Min Fu ,  Ashok Tehim ,  Robert A. Kirby

IPC: C07D267/20 ,  C07D401/14 ,  A61K31/55 ,  C07D403/14

CPC classification number: C07D267/20

Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCI, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO; X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--; Y is selected from CH and N; Z is cyano R.sub.1 represents C.sub.1-4 alkyl; m is 0, 1, 2 or 3; n is 0, 1 or 2; q is 1 or 2; and D is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.

Abstract translation: 本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基， 所以; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; Y选自CH和N; Z是氰基，R 1表示C 1-4烷基; m为0,1,2或3; n为0,1或2; q为1或2; 且D为5,6或7元饱和或不饱和的均聚或杂环; 及其酸加成盐，溶剂化物和水合物。 还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。