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1. 发明申请

US20120088837A1 TETRALIN AND INDANE DERIVATIVES AND USES THEREOF 有权
标题翻译：四环素衍生物及其衍生物及其用途
公开(公告)号：US20120088837A1
公开(公告)日：2012-04-12
申请号：US13314525
申请日：2011-12-08
申请人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
发明人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
IPC分类号： A61K31/17 , A61P25/00 , C07C233/33 , A61P25/28 , C07C275/24 , A61K31/165
CPC分类号： C07C317/32 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/325 , C07D207/34 , C07D207/36 , C07D209/30 , C07D231/18 , C07D233/20 , C07D233/34 , C07D233/44 , C07D233/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D239/14 , C07D239/42 , C07D277/82
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
摘要翻译：式I化合物或其药学上可接受的盐，其中m，p，q，Ar，R 1和R 2如本文所定义。还提供了制备方法，组合物和使用式I化合物的方法。

2. 发明申请

US20080293751A1 Tetralin and indane derivatives and uses thereof 有权
标题翻译：四氢萘啶和茚满衍生物及其用途
公开(公告)号：US20080293751A1
公开(公告)日：2008-11-27
申请号：US11985459
申请日：2007-11-15
申请人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
发明人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
IPC分类号： A61K31/505 , C07C211/01 , C07C257/00 , C07C279/02 , A61K31/155 , C07D235/04 , C07C275/04 , C07C311/01 , A61P25/00 , A61K31/18 , A61K31/17 , A61K31/4184 , A61K31/135 , C07D233/54 , A61K31/4164 , C07D239/24
CPC分类号： C07C317/32 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/325 , C07D207/34 , C07D207/36 , C07D209/30 , C07D231/18 , C07D233/20 , C07D233/34 , C07D233/44 , C07D233/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D239/14 , C07D239/42 , C07D277/82
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
摘要翻译：式I化合物或其药学上可接受的盐，其中m，p，q，Ar，R 1和R 2如本文所定义。还提供了制备方法，组合物和使用式I化合物的方法。

3. 发明授权

US07312359B2 Tetralin and indane derivatives and uses thereof 有权
标题翻译：四氢萘啶和茚满衍生物及其用途
公开(公告)号：US07312359B2
公开(公告)日：2007-12-25
申请号：US11315706
申请日：2005-12-21
申请人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
发明人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
IPC分类号： C07C231/00 , C07D239/02 , C07D233/70 , A61K31/50 , A61K31/41 , A61K31/17 , A61K31/16
CPC分类号： C07C317/32 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/325 , C07D207/34 , C07D207/36 , C07D209/30 , C07D231/18 , C07D233/20 , C07D233/34 , C07D233/44 , C07D233/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D239/14 , C07D239/42 , C07D277/82
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
摘要翻译：式I化合物或其药学上可接受的盐，其中m，p，q，Ar，R 1和R 2如本文所定义。还提供了制备方法，组合物和使用式I化合物的方法。

4. 发明授权

US08093424B2 Tetralin and indane derivatives and uses thereof 有权
标题翻译：四氢萘啶和茚满衍生物及其用途
公开(公告)号：US08093424B2
公开(公告)日：2012-01-10
申请号：US11985459
申请日：2007-11-15
申请人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
发明人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
IPC分类号： C07C303/00 , C07C307/00 , C07C309/00 , C07C311/00 , C07C241/00 , C07C243/00 , C07C249/00 , C07C251/00
CPC分类号： C07C317/32 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/325 , C07D207/34 , C07D207/36 , C07D209/30 , C07D231/18 , C07D233/20 , C07D233/34 , C07D233/44 , C07D233/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D239/14 , C07D239/42 , C07D277/82
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
摘要翻译：式I化合物或其药学上可接受的盐，其中m，p，q，Ar，R 1和R 2如本文所定义。还提供了制备方法，组合物和使用式I化合物的方法。

5. 发明授权

US08889906B2 Tetralin and indane derivatives and uses thereof 有权
标题翻译：四氢萘啶和茚满衍生物及其用途
公开(公告)号：US08889906B2
公开(公告)日：2014-11-18
申请号：US13314525
申请日：2011-12-08
申请人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
发明人： Robert Greenhouse , Ralph New Harris, III , Saul Jaime-Figueroa , James M. Kress , David Bruce Repke , Russell Stephen Stabler
IPC分类号： C07C303/00 , C07C307/00 , C07C309/00 , C07C311/00 , A01N47/28 , A61K31/17 , A01N37/18 , A61K31/16 , C07D207/36 , C07D235/06 , C07D233/34 , C07D209/30 , C07D233/90 , C07D239/42 , C07C317/32 , C07C317/44 , C07D233/48 , C07D239/14 , C07D207/325 , C07D233/88 , C07D207/16 , C07D233/84 , C07D233/54 , C07D207/34 , C07D233/64 , C07D231/18 , C07D233/20 , C07D277/82
CPC分类号： C07C317/32 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/325 , C07D207/34 , C07D207/36 , C07D209/30 , C07D231/18 , C07D233/20 , C07D233/34 , C07D233/44 , C07D233/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D239/14 , C07D239/42 , C07D277/82
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
摘要翻译：式I化合物或其药学上可接受的盐，其中m，p，q，Ar，R 1和R 2如本文所定义。还提供了制备方法，组合物和使用式I化合物的方法。

6. 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。

7. 发明授权

US07638517B2 3-Amino-1-arylpropyl azaindoles and uses thereof 失效
标题翻译： 3-氨基-1-芳基丙基氮杂吲哚及其用途
公开(公告)号：US07638517B2
公开(公告)日：2009-12-29
申请号：US11605729
申请日：2006-11-29
申请人： Robert Greenhouse , Saul Jaime-Figueroa , Stephen M. Lynch , Lubica Raptova , Karin Ann Stein , Robert James Weikert
发明人： Robert Greenhouse , Saul Jaime-Figueroa , Stephen M. Lynch , Lubica Raptova , Karin Ann Stein , Robert James Weikert
IPC分类号： A61K31/519 , A61K31/506 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14
摘要： The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
摘要翻译：本发明提供下式的化合物或其药学上可接受的盐，溶剂合物或前药，其中p，Ar，R 1，R 2，R 3，R a，R b，R c，R d和R Re如本文所定义。还提供药物组合物，使用方法和制备化合物的方法。

8. 发明申请

US20100056499A1 3-AMINO-1-ARYLPROPYL AZAINDOLES AND USES THEREOF 审中-公开
标题翻译： 3-氨基-1-芳基丙氨酰胺及其用途
公开(公告)号：US20100056499A1
公开(公告)日：2010-03-04
申请号：US12619275
申请日：2009-11-16
申请人： Robert Greenhouse , Saul Jaime-Figueroa , Stephen M. Lynch , Lubica Raptova , Karin Ann Stein , Robert James Weikert
发明人： Robert Greenhouse , Saul Jaime-Figueroa , Stephen M. Lynch , Lubica Raptova , Karin Ann Stein , Robert James Weikert
IPC分类号： A61K31/519 , C07D487/04 , C07D471/04 , C07D471/16 , A61K31/551 , A61K31/437 , A61P25/24 , A61P25/22
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14
摘要： The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
摘要翻译：本发明提供下式的化合物或其药学上可接受的盐，溶剂合物或前药，其中p，Ar，R 1，R 2，R 3，R a，R b，R c，R d和R Re如本文所定义。还提供药物组合物，使用方法和制备化合物的方法。

9. 发明申请

US20060167255A1 Tetralin and indane derivatives and uses thereof 有权
标题翻译：四氢萘啶和茚满衍生物及其用途
公开(公告)号：US20060167255A1
公开(公告)日：2006-07-27
申请号：US11315706
申请日：2005-12-21
申请人： Robert Greenhouse , Ralph Harris , Saul Jaime-Figueroa , James Kress , David Repke , Russell Stabler
发明人： Robert Greenhouse , Ralph Harris , Saul Jaime-Figueroa , James Kress , David Repke , Russell Stabler
IPC分类号： A61K31/505 , C07D233/44
CPC分类号： C07C317/32 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07D207/16 , C07D207/325 , C07D207/34 , C07D207/36 , C07D209/30 , C07D231/18 , C07D233/20 , C07D233/34 , C07D233/44 , C07D233/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D239/14 , C07D239/42 , C07D277/82
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
摘要翻译：式I化合物或其药学上可接受的盐，其中m，p，q，Ar，R 1和R 2如本文所定义。还提供了制备方法，组合物和使用式I化合物的方法。

10. 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。

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