公开(公告)号：US20090275618A1

公开(公告)日：2009-11-05

申请号：US12441570

申请日：2007-10-22

申请人： David Scott Coffey ,  Jingdan Hu ,  Stacy Jo Keding ,  Joseph Herman Krushinski, JR. ,  John Mehnert Schaus ,  David Edward Tupper

发明人： David Scott Coffey ,  Jingdan Hu ,  Stacy Jo Keding ,  Joseph Herman Krushinski, JR. ,  John Mehnert Schaus ,  David Edward Tupper

IPC分类号： A61K31/4439 ,  C07D401/12 ,  A61P25/18 ,  A61P25/30 ,  A61P3/04 ,  A61P25/28

CPC分类号： C07D401/12 ,  C07D207/38

摘要： Compounds and pharmaceutical compositions of Formula (I) by blockade of the CB1 receptors via an inverse agonism mechanism which are useful for reducing body weight in mammals, cognitive impairment associated with schizophrenia, mitigating treatment emergent weight gain observed during treatment with antipsychotics and have increased bioavailability.

摘要翻译： 式（I）的化合物和药物组合物通过反义激动机制阻断CB1受体，其可用于减少哺乳动物的体重，与精神分裂症相关的认知障碍，减轻用抗精神病药治疗期间观察到的治疗出现的体重增加并且具有增加的生物利用度 。

公开(公告)号：US08168659B2

公开(公告)日：2012-05-01

申请号：US12441570

申请日：2007-10-22

申请人： David Scott Coffey ,  Jingdan Hu ,  Stacy Jo Keding ,  Joseph Herman Krushinski, Jr. ,  John Mehnert Schaus ,  David Edward Tupper

发明人： David Scott Coffey ,  Jingdan Hu ,  Stacy Jo Keding ,  Joseph Herman Krushinski, Jr. ,  John Mehnert Schaus ,  David Edward Tupper

IPC分类号： A61K31/4439 ,  C07D401/12

CPC分类号： C07D401/12 ,  C07D207/38

摘要： Compounds and pharmaceutical compositions comprising compounds of the Formula as CB1 receptor inverse agonists useful for reducing body weight in mammals, treating cognitive impairment associated with schizophrenia, and mitigating treatment emergent weight gain observed during treatment with antipsychotics.

摘要翻译： 化合物和药物组合物，其包含式为CB1受体反向激动剂的化合物，其可用于减少哺乳动物体内的体重，治疗与精神分裂症相关的认知障碍，以及减轻在用抗精神病药治疗期间观察到的治疗急性体重增加。

公开(公告)号：US07214673B2

公开(公告)日：2007-05-08

申请号：US10505805

申请日：2003-03-17

申请人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Joseph Herman Krushinski, Jr. ,  Yvan Le Huerou ,  Marta Maria Pineiro-Nunez ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Dennis Charles Thompson ,  David Edward Tupper ,  Ying Chen ,  Margaret Mary Faul ,  Vincent Patrick Rocco

发明人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Joseph Herman Krushinski, Jr. ,  Yvan Le Huerou ,  Marta Maria Pineiro-Nunez ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Dennis Charles Thompson ,  David Edward Tupper ,  Ying Chen ,  Margaret Mary Faul ,  Vincent Patrick Rocco

IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D243/10

CPC分类号： C07D487/04 ,  C07D243/38 ,  C07D495/04 ,  C07D513/04

摘要： Described herein are antipyschotic compounds of formula (I) wherein, A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R1 is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH, wherein R3 is (C1-2) alkyl; R2 is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl, wherein R4 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, or optionally substituted phenyl, R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; Z is one or two substituents independently selected from hydrogen, halogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, SO2NR8R9, NR8SO2R7, NR8R9, or optionally substituted phenyl, wherein R7 is hydrogen, (C1-6) alkyl, fluorinated alkyl, or optionally substituted phenyl, R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; and salts, solvates, and crystal forms thereof. Also described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorder, and pharmaceutical formulations of the compounds of formula (I).

公开(公告)号：US07384934B2

公开(公告)日：2008-06-10

申请号：US10523147

申请日：2003-07-28

申请人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Yvan LeHuerou ,  Fionna Mitchell Martin ,  Marta Maria Pineiro-Nunez ,  Vincent Patrick Rocco ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  David Edward Tupper

发明人： Thomas Daniel Aicher ,  Zhaogen Chen ,  Yvan LeHuerou ,  Fionna Mitchell Martin ,  Marta Maria Pineiro-Nunez ,  Vincent Patrick Rocco ,  Kevin Michael Ruley ,  John Mehnert Schaus ,  Patrick Gianpietro Spinazze ,  David Edward Tupper

IPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61P25/18

CPC分类号： C07D403/04 ,  C07D495/04 ,  C07D513/04

摘要： Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or —CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, NO2, CN, COR4, C(O)OR4, CONR5R6, NR5R6, SO2NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyly is unsubstituted or substituted with a phenyl; R4 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I)

公开(公告)号：US6034078A

公开(公告)日：2000-03-07

申请号：US886847

申请日：1997-07-01

申请人： John Fairhurst ,  Terrence Michael Hotten ,  David Edward Tupper ,  David Taiwai Wong

发明人： John Fairhurst ,  Terrence Michael Hotten ,  David Edward Tupper ,  David Taiwai Wong

IPC分类号： C07D495/04 ,  A61K31/55

CPC分类号： C07D495/04

摘要： Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or halo, and R.sup.2 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-6 cycloalkyl optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl in which the cycloalkyl group is optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, or optionally substituted phenyl-C.sub.1-4 alkyl; or a salt thereof. Such compounds are useful for treating a disorder of the central nervous system which is associated with the modulation of a 5-HT.sub.3 receptor.

摘要翻译： 下式的药物化合物，其中R 1是氢或卤素，且R 2是C 1-10烷基，C 2-10烯基，C 2-10炔基，任选被1至3个C 1-4烷基取代的C 3-6环烷基，C 3-6 环烷基-C 1-4烷基，其中环烷基任选被1至3个C 1-4烷基取代，或任选取代的苯基-C 1-4烷基; 或其盐。 这样的化合物可用于治疗与5-HT 3受体的调节相关的中枢神经系统病症。

公开(公告)号：US06384281B1

公开(公告)日：2002-05-07

申请号：US09958218

申请日：2001-10-03

申请人： Martine Keenan ,  Sandra Ginette Milutinovic ,  David Edward Tupper

发明人： Martine Keenan ,  Sandra Ginette Milutinovic ,  David Edward Tupper

IPC分类号： A61K3144

CPC分类号： C07C233/58 ,  C07C211/30 ,  C07C215/64 ,  C07C217/74 ,  C07C2602/20 ,  C07C2602/22 ,  C07D209/14 ,  C07D209/18 ,  C07D333/60

摘要： A pharmaceutical compound of formula (I) in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholino group, said group being optionally substituted with 1 to 3 C1-4alkyl substituents, R3 is a naphythyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; or a salt or ester thereof.

摘要翻译： 式（I）的药物化合物，其中R 1和R 2各自为氢或C 1-4烷基，或R 1和R 2与它们所连接的氮原子一起形成氮杂环丁烷基，吡咯烷基，哌啶基，哌嗪基或吗啉代基， 所述基团任选被1至3个C 1-4烷基取代基取代，R 3是萘基，吲哚基，苯并噻吩基，苯并呋喃基，苯并噻唑基，喹啉基或异喹啉基，所述基团任选被取代，n是1或2; 或其盐或酯。

公开(公告)号：US5817657A

公开(公告)日：1998-10-06

申请号：US748294

申请日：1996-11-13

申请人： Charles M. Beasley, Jr. ,  Jiban Kumar Chakrabarti ,  Terrence Michael Hotten ,  David Edward Tupper

发明人： Charles M. Beasley, Jr. ,  Jiban Kumar Chakrabarti ,  Terrence Michael Hotten ,  David Edward Tupper

IPC分类号： A61K31/551 ,  A61K31/5513 ,  A01N43/62

CPC分类号： A61K31/551 ,  A61K31/5513

摘要： 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-�2,3-b!�1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders relating to the use of psychoactive substances. The compound has the following structure: ##STR1##

摘要翻译： 2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂或其酸式盐具有药物性质，具有特别的用途 在治疗与使用精神活性物质有关的疾病方面。 该化合物具有以下结构：

公开(公告)号：US06008216A

公开(公告)日：1999-12-28

申请号：US122294

申请日：1998-07-24

申请人： Jiban Kumar Chakrabarti ,  Terrence Michael Hotten ,  David Edward Tupper

发明人： Jiban Kumar Chakrabarti ,  Terrence Michael Hotten ,  David Edward Tupper

IPC分类号： A01N43/62 ,  A61K31/551 ,  A61K31/5513 ,  C07D243/10

CPC分类号： A61K31/551 ,  A61K31/5513

摘要： 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system. The compound has the following structure: ##STR1##

摘要翻译： 2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂或其酸式盐具有药物性质，具有特别的用途 在治疗中枢神经系统疾病。 该化合物具有以下结构：

公开(公告)号：US09296710B2

公开(公告)日：2016-03-29

申请号：US14123768

申请日：2012-06-07

申请人： Teresa Tse Ki Man ,  James Allen Monn ,  Carlos Montero Salgado ,  Lourdes Prieto ,  David Edward Tupper ,  Lesley Walton

发明人： Teresa Tse Ki Man ,  James Allen Monn ,  Carlos Montero Salgado ,  Lourdes Prieto ,  David Edward Tupper ,  Lesley Walton

IPC分类号： C07D249/04 ,  C07D249/12 ,  C07D249/14

CPC分类号： C07D249/14 ,  C07D249/04 ,  C07D249/12

摘要： The present invention provides novel mGlu2 agonists useful in the treatment of bipolar disorder, schizophrenia, and generalized anxiety disorder.

摘要翻译： 本发明提供了可用于治疗双相障碍，精神分裂症和广泛性焦虑症的新型mGlu2激动剂。

公开(公告)号：US06169084A

公开(公告)日：2001-01-02

申请号：US09163769

申请日：1998-09-30

申请人： Charles Arthur Bunnell ,  Thomas Harry Ferguson ,  Barry Arnold Hendriksen ,  Manuel Vicente Sanchez-Felix ,  David Edward Tupper

发明人： Charles Arthur Bunnell ,  Thomas Harry Ferguson ,  Barry Arnold Hendriksen ,  Manuel Vicente Sanchez-Felix ,  David Edward Tupper

IPC分类号： A61K3155

CPC分类号： A61K9/0019 ,  A61K9/1617 ,  A61K31/551 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/24 ,  A61K47/26 ,  A61K47/28 ,  A61K47/32 ,  A61K47/36 ,  A61K47/38 ,  C07D495/04

摘要： The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.

摘要翻译： 本发明提供了奥氮平或奥氮平双羟萘酸或其溶剂合物的药学上可接受的含油或胆固醇微球制剂。 本发明还提供了新的奥氮平双羟萘酸盐或其溶剂化物。