公开(公告)号：US6034078A

公开(公告)日：2000-03-07

申请号：US886847

申请日：1997-07-01

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

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

IPC: C07D495/04 ,  A61K31/55

CPC classification number: C07D495/04

Abstract: 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.

Abstract translation: 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：US20140113944A1

公开(公告)日：2014-04-24

申请号：US14123768

申请日：2012-06-07

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

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

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

CPC classification number: C07D249/14 ,  C07D249/04 ,  C07D249/12

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

Abstract translation: 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颖的mGlu2激动剂。

公开(公告)号：US08168659B2

公开(公告)日：2012-05-01

申请号：US12441570

申请日：2007-10-22

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

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

IPC: A61K31/4439 ,  C07D401/12

CPC classification number: C07D401/12 ,  C07D207/38

Abstract: 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.

Abstract translation: 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：US07384934B2

公开(公告)日：2008-06-10

申请号：US10523147

申请日：2003-07-28

Applicant: 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

Inventor： 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: C07D403/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61P25/18

CPC classification number: C07D403/04 ,  C07D495/04 ,  C07D513/04

Abstract: 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：US5817655A

公开(公告)日：1998-10-06

申请号：US748292

申请日：1996-11-13

Applicant: Jiban Kumar Chakrabarti ,  Terrence Micharl Hotten ,  David Edward Tupper

Inventor： Jiban Kumar Chakrabarti ,  Terrence Micharl Hotten ,  David Edward Tupper

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

CPC classification number: A61K31/551 ,  A61K31/5513

Abstract: 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##

Abstract translation: 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，特别适用于 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：US5703232A

公开(公告)日：1997-12-30

申请号：US586431

申请日：1996-01-16

Applicant: Charles A. Bunnell ,  Terrence Michael Hotten ,  Samuel D. Larsen ,  David Edward Tupper

Inventor： Charles A. Bunnell ,  Terrence Michael Hotten ,  Samuel D. Larsen ,  David Edward Tupper

IPC: C07D495/04 ,  C07D243/10

CPC classification number: C07D495/04

Abstract: The invention provides lower alcohol solvates of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno�2,3-b!�1,5!benzodiazepine (olanzapine) and a process for making such lower alcohol solvates of olanzapine. The invention provides a method for using such solvates of olanzapine to prepare substantially pure anhydrous Form I 2-methyl-thieno-benzodiazepine.

Abstract translation: 本发明提供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（奥氮平）的低级醇溶剂化物和制备这种低级醇的方法 奥氮平的溶剂化物。 本发明提供了使用这种奥氮平溶剂合物制备基本上纯的无水形式I 2-甲基 - 噻吩并 - 苯并二氮杂的方法。

公开(公告)号：US4115574A

公开(公告)日：1978-09-19

申请号：US802381

申请日：1977-06-01

Applicant: Jiban Kumar Chakrabarti ,  David Edward Tupper

Inventor： Jiban Kumar Chakrabarti ,  David Edward Tupper

IPC: C07D333/38 ,  C07D333/68 ,  C07D495/04 ,  A61K31/495 ,  A61K31/55

CPC classification number: C07D333/68 ,  C07C323/00 ,  C07D333/38

Abstract: Thieno[1,5]benzodiazepines having useful CNS activity containing the novel tricyclic ring system: ##STR1## the 10-position being substituted by an amino, preferably a piperazino, group.

Abstract translation: 具有含有新型三环系统的有用CNS活性的噻吩并[1,5]苯并二氮杂：10位被氨基，优选哌嗪子基取代。

公开(公告)号：US4061774A

公开(公告)日：1977-12-06

申请号：US566502

申请日：1975-04-09

Applicant: Jiban Kumar Chakrabarti ,  Terrence Michael Hotten ,  David Edward Tupper

Inventor： Jiban Kumar Chakrabarti ,  Terrence Michael Hotten ,  David Edward Tupper

IPC: C07D295/096 ,  C07D303/06 ,  A61K31/13 ,  C07C87/40

CPC classification number: C07D295/096 ,  C07D303/06

Abstract: Novel 2-substituted-1-methylamino adamantanes of formula: ##STR1## where X is hydroxyl or halogeno, and R.sup.1, R.sup.2 and R.sup.3 are hydrogen or C.sub.1-4 alkyl or R.sup.2 and R.sup.3 together with the nitrogen form a heterocyclic ring, having anti-Parkinsonian activity, pharmaceutical formulations containing the active adamantanes and novel 4-protoadamantane spiro oxirane and 1,2-difunctionalized intermediates useful in the preparation of the final products of the invention.

Abstract translation: 新颖的2-取代-1-甲基氨基金刚烷，其结构式如下：其中X是羟基或卤素，R 1，R 2和R 3是氢或C 1-4烷基，或者R 2和R 3与氮一起形成杂环， 帕金森病活性，含有活性金刚烷的药物制剂和新的4-原金刚烷螺环氧乙烷和可用于制备本发明最终产物的1,2-二官能化中间体。