公开(公告)号：US07056920B2

公开(公告)日：2006-06-06

申请号：US10799407

申请日：2004-03-12

Applicant: Jian-min Fu

Inventor： Jian-min Fu

IPC: C07D487/04 ,  A61K31/5025 ,  A61P25/22 ,  A61P25/24

CPC classification number: C07D487/04

Abstract: Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I): including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) R is H or Me.

公开(公告)号：US07041671B2

公开(公告)日：2006-05-09

申请号：US10799406

申请日：2004-03-12

Applicant: Jian-min Fu

Inventor： Jian-min Fu

IPC: C07D487/04 ,  A61K31/5025 ,  A61P25/22 ,  A61P25/24

CPC classification number: C07D487/04

Abstract: Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I): including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) R is H or Me.

Abstract translation: 公开了新的CRF受体拮抗剂及其用于治疗多种疾病的用途，包括表现出CRF过度分泌或与CRF或CRF受体如焦虑和抑郁症相关的疾病。 本发明的CRF受体拮抗剂具有式（I）的结构：包括立体异构体或立体异构体的混合物，药学上可接受的前药或其药学上可接受的盐，其中在式（I）中R是H或Me。

公开(公告)号：US06903090B2

公开(公告)日：2005-06-07

申请号：US10393968

申请日：2003-03-20

Applicant: Kristine E. Frank ,  Brad A. Acker ,  Michael D. Ennis ,  Jed F. Fisher ,  Jian-min Fu ,  William W. McWhorter, Jr. ,  Jeanette K. Morris ,  Donald Joseph Rogier ,  Eric Jon Jacobsen

Inventor： Kristine E. Frank ,  Brad A. Acker ,  Michael D. Ennis ,  Jed F. Fisher ,  Jian-min Fu ,  William W. McWhorter, Jr. ,  Jeanette K. Morris ,  Donald Joseph Rogier ,  Eric Jon Jacobsen

IPC: A61K31/55 ,  A61P3/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D487/04 ,  G06T3/00

CPC classification number: C07D487/04

Abstract: Disclosed are compounds of Formula (I): wherein R1-R4, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.

Abstract translation: 公开了式（I）的化合物：其中R 1 -R 4，p和q具有说明书中描述的任何值，以及其药用盐， 和含有这些化合物或盐的药物组合物。 化合物和盐是5-HT配体，可用于治疗其中涉及5-HT受体的活性的哺乳动物的疾病，病症和/或病症。 化合物和盐特别适用于治疗中枢神经系统疾病。

公开(公告)号：US06503899B2

公开(公告)日：2003-01-07

申请号：US09900508

申请日：2001-07-06

Applicant: Jian-min Fu

Inventor： Jian-min Fu

IPC: A61K3155

CPC classification number: C07D491/14 ,  A61K31/55

Abstract: The invention provides a compound of formula (I): wherein: R1-R5, m, n, p, and the bonds a and b represented by - - - have any of the values, specific values, or preferred values described in the specification; or a salt or solvate thereof. The invention also provides pharmaceutical compositions comprising such a compound, as well as intermediates and processes useful for preparing such a compound, and therapeutic methods including the administration of such a compound.

Abstract translation: 本发明提供式（I）化合物：其中：R 1 -R 5，m，n，p，和由 - 表示的键a和b具有本说明书中描述的任何值，具体值或优选值 ; 或其盐或溶剂合物。 本发明还提供包含这种化合物的药物组合物，以及可用于制备这种化合物的中间体和方法，以及包括给予这种化合物的治疗方法。

公开(公告)号：US5824676A

公开(公告)日：1998-10-20

申请号：US763255

申请日：1996-12-10

Applicant: Ashok Tehim ,  Jian-min Fu ,  Sumanas Rakhit

Inventor： Ashok Tehim ,  Jian-min Fu ,  Sumanas Rakhit

IPC: C07D243/38 ,  C07D267/20 ,  A61K31/55 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D243/38 ,  C07D267/20

Abstract: Described herein are 5-HT2 receptor-selective compounds of Formula I: ##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.CHCl, 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--; R.sub.1 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and R.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ; and acid addition salts, solvates and hydrates thereof. Their use as ligands for serotonin 5-HT2 receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the 5-HT2 receptor is implicated, such as hypertension, thrombosis, migraine, vasospasm, ischemia, depression, anxiety, schizophrenia, sleep disorders and appetite disorders is also described.

Abstract translation: 本文描述的是式I的5-HT 2受体选择性化合物：其中：A和B独立地选择，任选取代的饱和或不饱和的5-或6-元，均 - 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-; R1是任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-6烷基; 并且R 2，R 3和R 4独立地选自H和R 1; 及其酸加成盐，溶剂化物和水合物。 它们用作5-羟色胺5-HT2受体鉴定和药物筛选程序的配体，以及用作治疗其中涉及5-HT2受体的适应症的药物，例如高血压，血栓形成，偏头痛，血管痉挛，局部缺血，抑郁，焦虑， 还描述了精神分裂症，睡眠障碍和食欲障碍。