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1. 发明授权

US07432283B2 Heterocyclic GABAA subtype selective receptor modulators 失效
标题翻译：杂环GABAA亚型选择性受体调节剂
公开(公告)号：US07432283B2
公开(公告)日：2008-10-07
申请号：US11061000
申请日：2005-02-18
申请人： David Garrett Loughhead , Sanja Novakovic , Counde O'Yang , David George Putman , Michael Soth
发明人： David Garrett Loughhead , Sanja Novakovic , Counde O'Yang , David George Putman , Michael Soth
IPC分类号： A01N43/40 , A61K31/445 , C07D295/00 , C07D211/00
CPC分类号： A61K31/437 , A61K31/5383 , C07D471/04 , C07D487/04
摘要： This invention relates to a method for modulating α2 subtype GABAA receptors with heterocyclic compounds of formula I, and salts, solvates and prodrugs thereof. The invention further relates to novel heteocyclic compounds and pharmaceutical compositions containing said compounds. In addition the invention relates to the treatment of depression, an anxiety disorder, a psychiatric disorder, a learning or cognitive disorder, a sleep disorder, a convulsive or seizure disorder or pain
摘要翻译：本发明涉及用式I杂环化合物调节α2亚型GABA A A受体的方法及其盐，溶剂合物和前药。本发明还涉及含有所述化合物的新颖的杂环化合物和药物组合物。此外，本发明涉及抑郁症，焦虑障碍，精神障碍，学习或认知障碍，睡眠障碍，惊厥或发作性疾病或疼痛的治疗

2. 发明授权

US07365211B2 Heterocyclic GABAA subtype selective receptor modulators 失效
标题翻译：杂环GABAA亚型选择性受体调节剂
公开(公告)号：US07365211B2
公开(公告)日：2008-04-29
申请号：US10916073
申请日：2004-08-11
申请人： Xao-Fa Lin , David Garrett Loughhead , Sanja Novakovic , Counde O'Yang , Michael Soth , David George Putman
发明人： Xao-Fa Lin , David Garrett Loughhead , Sanja Novakovic , Counde O'Yang , Michael Soth , David George Putman
IPC分类号： C07D231/54 , C07D231/56
CPC分类号： C07D409/04 , C07D231/56 , C07D401/04 , C07D403/06 , C07D405/04 , C07D417/04 , C07D471/04 , C07D487/04
摘要： This invention relates to a method for modulating α2 subtype GABAA receptors with heterocyclic compounds of formula I, and salts, solvates and prodrugs thereof. The invention further relates to said heterocyclic compounds and pharmaceutical compositions containing said compounds. In addition the invention relates to the treatment of depression, an anxiety disorder, a psychiatric disorder, a learning or cognitive disorder, a sleep disorder, a convulsive or seizure disorder or pain
摘要翻译：本发明涉及用式I杂环化合物调节α2亚型GABA A A受体的方法及其盐，溶剂合物和前药。本发明还涉及所述杂环化合物和含有所述化合物的药物组合物。此外，本发明涉及抑郁症，焦虑障碍，精神障碍，学习或认知障碍，睡眠障碍，惊厥或发作性疾病或疼痛的治疗

3. 发明授权

US5952331A Aryl pyrimidine derivatives 失效
标题翻译：芳基嘧啶衍生物
公开(公告)号：US5952331A
公开(公告)日：1999-09-14
申请号：US963390
申请日：1997-11-03
申请人： Jacob Berger , Lee Allen Flippin , Robert Greenhouse , Saul Jaime-Figueroa , Yanzhou Liu , Aubry Kern Miller , David George Putman , Klaus Kurt Weinhardt , Shu-Hai Zhao
发明人： Jacob Berger , Lee Allen Flippin , Robert Greenhouse , Saul Jaime-Figueroa , Yanzhou Liu , Aubry Kern Miller , David George Putman , Klaus Kurt Weinhardt , Shu-Hai Zhao
IPC分类号： C07D239/42 , C07D239/46 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D473/32 , A61K31/505
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D473/32 , Y10S514/826
摘要： The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists.
摘要翻译：芳基嘧啶衍生物及其药学上可接受的盐和N-氧化物显示出有用的药理学性质，包括作为选择性5HT2B拮抗剂的用途。

4. 发明授权

US5863924A Aryl pyrimidine derivatives 失效
标题翻译：芳基嘧啶衍生物
公开(公告)号：US5863924A
公开(公告)日：1999-01-26
申请号：US858964
申请日：1997-05-20
申请人： Jacob Berger , Lee Allen Flippin , Robert Greenhouse , Saul Jaime-Figueroa , Yanzhou Liu , Aubry Kern Miller , David George Putman , Klaus Kurt Weinhardt , Shu-Hai Zhao
发明人： Jacob Berger , Lee Allen Flippin , Robert Greenhouse , Saul Jaime-Figueroa , Yanzhou Liu , Aubry Kern Miller , David George Putman , Klaus Kurt Weinhardt , Shu-Hai Zhao
IPC分类号： A61K31/505 , A61K31/506 , A61K31/538 , A61K31/55 , A61P1/14 , A61P9/12 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/32 , C07D239/42 , C07D239/46 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D473/32
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D473/32
摘要： The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT.sub.2B -antagonists. The invention is also directed to formulations and methods for treatment.
摘要翻译：所公开的嘧啶衍生物及其药学上可接受的盐和N-氧化物显示出有用的药理学性质，特别是用作选择性5HT2B拮抗剂。本发明还涉及用于治疗的制剂和方法。

5. 发明授权

US07196088B2 Substituted tetrahydroisoquinolines and uses thereof 失效
标题翻译：取代的四氢异喹啉及其用途
公开(公告)号：US07196088B2
公开(公告)日：2007-03-27
申请号：US10791578
申请日：2004-03-02
申请人： David George Putman
发明人： David George Putman
IPC分类号： A61K31/496 , C07D401/04
CPC分类号： C07D401/12 , C07D217/08 , C07D217/24
摘要： The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein, n, X, Y, R1, R2, R3, R4 and R5 are as defined herein. The subject compounds are useful for treatment of 5-HT6 receptor antagonist-mediated diseases. Also provides are methods for preparing, compositions comprising, and methods for using the subject compounds.
摘要翻译：本发明提供下式的化合物：

6. 发明授权

US06787535B2 Indole derivatives with 5HT6 receptor affinity 失效
标题翻译：具有5HT6受体亲和力的吲哚衍生物
公开(公告)号：US06787535B2
公开(公告)日：2004-09-07
申请号：US10164660
申请日：2002-06-06
申请人： Colin Charles Beard , Robin Douglas Clark , Lawrence Emerson Fisher , Ralph New Harris, III , David Bruce Repke , David George Putman
发明人： Colin Charles Beard , Robin Douglas Clark , Lawrence Emerson Fisher , Ralph New Harris, III , David Bruce Repke , David George Putman
IPC分类号： A61K3133
CPC分类号： A61K31/405 , C07D209/30 , C07D401/04 , C07D401/12
摘要： This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein one of R5, R6 or R7 is a group of general Formula B, wherein W is a —CH— group or a nitrogen atom, and the other substituents are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要翻译：本发明涉及通常具有5-HT 6受体亲和性并由式I表示的化合物：其中R 5，R 6或R 7中的一个为通式B的基团，其中W为 -CH-基或氮原子，其它取代基如本文所定义; 或各异构体，异构体的外消旋或非外消旋混合物，或其药学上可接受的盐或溶剂合物。本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。

7. 发明授权

US5958934A Aryl pyrimidine derivatives and uses thereof 失效
标题翻译：芳基嘧啶衍生物及其用途
公开(公告)号：US5958934A
公开(公告)日：1999-09-28
申请号：US976418
申请日：1997-11-21
申请人： Jacob Berger , Lee Allen Flippin , Robert Greenhouse , Saul Jaime-Figueroa , Yanzhou Liu , Aubry Kern Miller , David George Putman , Klaus Kurt Weinhardt , Shu-Hai Zhao
发明人： Jacob Berger , Lee Allen Flippin , Robert Greenhouse , Saul Jaime-Figueroa , Yanzhou Liu , Aubry Kern Miller , David George Putman , Klaus Kurt Weinhardt , Shu-Hai Zhao
IPC分类号： A61K31/505 , C07D239/42
CPC分类号： A61K31/505 , C07D239/42
摘要： The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists. The 5-HT.sub.2B antagonist is a compound of the formula: ##STR1## wherein: R.sup.1 is hydrogen, alkyl, lower alkoxy, hydroxyalkyl, cycloalkyl, cycloalkyl lower alkyl, alkenyl, lower thioalkoxy, halo, fluoroalkyl, --NR.sup.6 R.sup.7, --CO.sub.2 R.sup.8, --O(CH.sub.2).sub.n R.sup.9, or lower alkyl optionally substituted with hydroxy, alkoxy, halo, or aryl; in whichn is 1, 2, or 3;R.sup.6 and R.sup.7 are hydrogen or lower alkyl;R.sup.8 is hydrogen or lower alkyl; andR.sup.9 is hydrogen, lower alkyl, hydroxy, hydroxy lower alkyl, lower alkenyl, or lower alkoxy;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, or lower fluoroalkyl;R.sup.3 is optionally substituted aryl other than pyridyl, thienyl, or furanyl;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, alkenyl, acyl, amino, amido, aryl, --(CH.sub.2).sub.m NR.sup.10 R.sup.11, or lower alkyl optionally substituted by amino, monosubstituted amino, disubstituted amino, hydroxy, carboxy, aryl, lower alkoxy, amido, alkoxy carbonyl, tetrahydrofuran-2-yl, hydroxyalkoxy, or sulfonamido;in whichR.sup.10 and R.sup.11 are hydrogen or lower alkyl; andR.sup.5 is hydrogen or lower alkyl; provided that:(i) when R.sup.3 is naphthyl, indol-1-yl, or 2,3-dihydroindol-1-yl, and R.sup.2, R.sup.4 and R.sup.5 are all hydrogen, R.sup.1 is not methyl;(ii) when R.sup.3 is phenyl or naphthyl, R.sup.1 is not --NR.sup.6 R.sup.7 ;(iii) when R.sup.3 is phenyl, R.sup.2 is not lower alkoxy, and R.sup.1 and R.sup.2 are not halo;(iv) when R.sup.3 is phenyl and R.sup.1 is H, R.sup.2 is not methyl; and(v) when R.sup.3 is 1,2,3,4-tetrahydroquinolinyl, R.sup.4 and R.sup.5 are hydrogen;or a pharmaceutically acceptable salt or N-oxide thereof.
摘要翻译：芳基嘧啶衍生物及其药学上可接受的盐和N-氧化物显示出有用的药理学性质，包括作为选择性5HT2B拮抗剂的用途。 5-HT2B拮抗剂是下式的化合物：其中：R 1是氢，烷基，低级烷氧基，羟基烷基，环烷基，环烷基低级烷基，烯基，低级硫代烷氧基，卤素，氟代烷基，-NR 6 R 7，-CO 2 R 8，-O ）n R 9或任选被羟基，烷氧基，卤素或芳基取代的低级烷基; 其中n为1,2或3; R6和R7是氢或低级烷基; R8是氢或低级烷基; 且R 9为氢，低级烷基，羟基，羟基低级烷基，低级烯基或低级烷氧基; R2是氢，低级烷基，低级烷氧基，卤素或低级氟代烷基; R 3是除吡啶基，噻吩基或呋喃基以外的任选取代的芳基; R4是氢，低级烷基，环烷基，烯基，酰基，氨基，酰氨基，芳基， - （CH2）mNR10R11或任选被氨基，单取代的氨基，二取代的氨基，羟基，羧基，芳基，低级烷氧基，烷氧基羰基，四氢呋喃-2-基，羟基烷氧基或磺酰氨基; 其中R10和R11是氢或低级烷基; R5是氢或低级烷基; 条件是：（i）当R 3是萘基，吲哚-1-基或2,3-二氢吲哚-1-基时，R 2，R 4和R 5都是氢，R 1不是甲基; （ii）当R3是苯基或萘基时，R1不是-NR6R7; （iii）当R3是苯基时，R2不是低级烷氧基，R1和R2不是卤素; （iv）当R3是苯基且R1是H时，R2不是甲基; 和（v）当R 3是1,2,3,4-四氢喹啉基时，R 4和R 5是氢; 或其药学上可接受的盐或N-氧化物。

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