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1. 发明授权

US06835745B2 Phenyl substituted thiophenes as estrogenic agents 失效
标题翻译：苯基取代的噻吩作为雌激素剂
公开(公告)号：US06835745B2
公开(公告)日：2004-12-28
申请号：US10340425
申请日：2003-01-10
申请人： Richard D. Coghlan , William F. Fobare , Heather A. Harris , James C. Keith, Jr. , Leo M. Albert
发明人： Richard D. Coghlan , William F. Fobare , Heather A. Harris , James C. Keith, Jr. , Leo M. Albert
IPC分类号： A61K3138
CPC分类号： A61K31/34 , A61K31/165 , A61K31/277 , A61K31/381 , C07D327/08 , C07D333/12
摘要： This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1, R2, R3, X, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供式I的雌激素受体调节剂，其具有结构，其中R 1，R 2，R 3，X和Y如说明书中所定义，或其药学上可接受的盐。

2. 发明授权

US06734208B2 Compounds and therapies for the prevention of vascular and non-vascular pathologies 失效
标题翻译：用于预防血管和非血管病变的化合物和疗法
公开(公告)号：US06734208B2
公开(公告)日：2004-05-11
申请号：US10170971
申请日：2002-06-13
申请人： David J. Grainger , James C. Metcalfe , Sudhakar Kasina
发明人： David J. Grainger , James C. Metcalfe , Sudhakar Kasina
IPC分类号： A61K3138
CPC分类号： A61K31/275 , A61K31/381 , C07D333/38 , G01N33/74 , G01N2333/495 , G01N2333/71 , G01N2800/108 , G01N2800/323
摘要： The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.
摘要翻译：本发明提供了治疗具有或具有与TGF-β缺乏相关的指征的哺乳动物的方法，包括施用一种或多种有效提高TGF-β水平的试剂。本发明还提供了提高TGF-β水平的新化合物，以及包含提高TGF-β水平的化合物的药物组合物，以及用于检测与内皮细胞活化相关的疾病的方法。

3. 发明授权

US06610734B2 Heterocyclic sulfonamide inhibitors of beta amyloid production 失效
标题翻译： β-淀粉样蛋白生成的杂环磺酰胺抑制剂
公开(公告)号：US06610734B2
公开(公告)日：2003-08-26
申请号：US10014304
申请日：2001-12-11
申请人： Anthony F. Kreft , Derek C. Cole , Kevin R. Woller , Joseph R. Stock , George Diamantidis , Dennis M. Kubrak , Kristina M. Kutterer , William J. Moore , David S. Casebier , Lynn Resnick
发明人： Anthony F. Kreft , Derek C. Cole , Kevin R. Woller , Joseph R. Stock , George Diamantidis , Dennis M. Kubrak , Kristina M. Kutterer , William J. Moore , David S. Casebier , Lynn Resnick
IPC分类号： A61K3138
CPC分类号： C07D409/12 , C07D307/64 , C07D333/34
摘要： Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are described.
摘要翻译：提供其中R1，R2，R3，R4，R5，R6，T，W，X，Y和Z如本文所定义的式（I）化合物及其药学上可接受的盐，水合物和/或前药。描述了使用这些化合物抑制β淀粉样蛋白生成和治疗阿尔茨海默病和唐氏综合征的方法。

4. 发明授权

US06599932B1 Alpha, beta-unsaturated sulfones for treating proliferative disorders 有权
标题翻译： α，β-不饱和砜用于治疗增殖性疾病
公开(公告)号：US06599932B1
公开(公告)日：2003-07-29
申请号：US10301332
申请日：2002-11-21
申请人： E. Premkumar Reddy , M. V. Ramana Reddy
发明人： E. Premkumar Reddy , M. V. Ramana Reddy
IPC分类号： A61K3138
CPC分类号： C07D207/333 , C07C317/10 , C07D213/34 , C07D277/36 , C07D307/10 , C07D333/18 , C07D333/42 , C07D333/48
摘要： Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: wherein: Q1 is selected from the group consisting of (a) a phenyl radical according to formula II wherein R1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, amino, C1-C6 trifluoroalkoxy and trifluoromethyl; (b) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl; and (c) an aromatic radical according to formula III wherein n1 is 1 or 2, Y1 and Y2 are independently selected from the group consisting of hydrogen, halogen, and nitro, and X1 is selected from the group consisting of oxygen, nitrogen, sulfur and and Q2 is selected from the group consisting of (d) a phenyl radical according to formula II, as defined above; (e) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl; (f) an aromatic radical according to formula IV wherein n1 is 1 or 2, Y3 and Y4 are independently selected from the group consisting of hydrogen, halogen, and nitro, and X2, X3 and X4 are independently selected from the group consisting of carbon, oxygen, nitrogen, sulfur and provided that not all of X2, X3 and X4 may be carbon; and (g) 1-piperazinyl; provided that at least one of Q1 or Q2 is other than a phenyl radical according to formula II; or a pharmaceutically acceptable salt thereof. Sulfones of formula V are also useful as antiproliferative agents, including, for example, anticancer agents: wherein: X is sulfur or oxygen; Ya and Yb are independently selected from the group consisting of hydrogen, halogen, and nitro; and R1-R5 are defined as above; or a pharmaceutically acceptable salt thereof.
摘要翻译：式I的砜可用作抗增殖剂，包括例如抗癌剂：其中：Q1选自（a）根据式II的苯基，其中R 1，R 2，R 3，R 4和R 5独立地选自由C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，氨基，C 1 -C 6三氟烷氧基和三氟甲基组成的组;（b）选自1- 萘基，2-萘基和9-蒽基; 和（c）根据式III的芳族基团，其中n1为1或2，Y1和Y2独立地选自氢，卤素和硝基，X1选自氧，氮，硫，Q2为选自（d）如上定义的根据式II的苯基;（e）选自1-萘基，2-萘基和9-蒽基的芳族基团;（f）芳族基团，其中n1为1或2，Y3和Y4独立地选自氢，卤素和硝基，X2，X3和X4独立地选自碳，氧，氮，硫和只要不是所有的X2，X3和X4都可以是碳; （g）1-哌嗪基;条件是Q1或Q2中的至少一个不是根据式II的苯基;或其药学上可接受的盐。式V的砜也可用作抗增殖剂，包括例如抗癌剂：其中：X为硫或氧; Ya和Yb独立地选自氢，卤素和硝基; 和R 1 -R 5如上定义;或其药学上可接受的盐。

5. 发明授权

US06552068B1 3-ethyl-, 3-propyl- or 3-butyl-chroman and thiochroman derivatives 失效
标题翻译： 3-乙基，3-丙基或3-丁基 - 苯并二氢吡喃和二氢苯并噻喃衍生物
公开(公告)号：US06552068B1
公开(公告)日：2003-04-22
申请号：US10149749
申请日：2002-06-13
申请人： JaeChon Jo , JongMin Kim , SungOh Ahn , JaeYoung Choi , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim
发明人： JaeChon Jo , JongMin Kim , SungOh Ahn , JaeYoung Choi , Kazumi Morikawa , Yoshitake Kanbe , Masahiro Nishimoto , MyungHwa Kim
IPC分类号： A61K3138
CPC分类号： C07D335/06 , C07D311/58
摘要： A compound having the following general formula (1): in which R1 represents an ethyl group, etc.; R2 represents a hydrogen atom, etc.; R3 represents a C1-C5 perhalogenoalkyl group, etc.; each of R4 and R5 independently represents a hydrogen atom, etc.; X represents an oxygen atom or a sulfur atom; m represents an integer of 2 to 14; and n represents an integer of 2 to 7; or an enantiomer of the compound, or a hydrate or a pharmaceutically acceptable salt of the compound or its enantiomer is advantageous in pharmaceutical use because of its anti-estrogenic activity.
摘要翻译：具有以下通式（1）的化合物：其中R1表示乙基等; R2表示氢原子等; R3表示C1-C5全卤代烷基等; R4和R5各自独立地表示氢原子等; X表示氧原子或硫原子，m表示2〜14的整数，和n表示2至7的整数;或化合物或其化合物或其对映异构体的水合物或药学上可接受的盐的对映异构体由于其抗雌激素活性而在药物应用中是有利的。

6. 发明授权

US06525087B2 Use of known agonists of the central cannabinoid receptor CB1 失效
标题翻译：使用已知的中枢大麻素受体CB1的激动剂
公开(公告)号：US06525087B2
公开(公告)日：2003-02-25
申请号：US09867021
申请日：2001-05-29
申请人： Joachim Mittendorf , Jürgen Dressel , Michael Matzke , Jürgen Franz , Peter Spreyer , Verena Vöhringer , Joachim Schumacher , Arno Friedl , Ervin Horvath , Frank Mauler , Jean-Marie-Viktor De Vry , Reinhard Jork
发明人： Joachim Mittendorf , Jürgen Dressel , Michael Matzke , Jürgen Franz , Peter Spreyer , Verena Vöhringer , Joachim Schumacher , Arno Friedl , Ervin Horvath , Frank Mauler , Jean-Marie-Viktor De Vry , Reinhard Jork
IPC分类号： A61K3138
CPC分类号： A61K31/13 , A61K31/00 , A61K31/05 , A61K31/121 , A61K31/131 , A61K31/16 , A61K31/164 , A61K31/232 , A61K31/352 , A61K31/353 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/436 , A61K31/473 , A61K31/5375 , A61K31/5377 , A61K31/5383
摘要： The present invention relates to the use of known agonists of the central cannabinoid receptor CB1 for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy and craniocerebral trauma.
摘要翻译：本发明涉及中枢大麻素受体CB1的已知激动剂用于预防和治疗神经变性疾病，特别是用于治疗脑中风和颅脑外伤的用途。

7. 发明授权

US06486194B2 Use of inhibitors of cyclooxygenase in the treatment of neurodegenerative diseases 失效
标题翻译：使用环氧合酶抑制剂治疗神经变性疾病
公开(公告)号：US06486194B2
公开(公告)日：2002-11-26
申请号：US09796211
申请日：2001-02-28
申请人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
发明人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
IPC分类号： A61K3138
CPC分类号： C07D275/02 , A61K31/10 , A61K31/341 , A61K31/381 , A61K31/425 , A61K31/426 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07C2601/08 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04
摘要： The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor. Although a wide range of COX-II inhibitors may be employed but it is preferred to employ compounds of the Formula I:
摘要翻译：本发明提供治疗神经变性疾病，特别是阿尔茨海默病的方法，其包括向有需要的人施用治疗有效量的非类固醇COX-II抑制剂。尽管可以使用大范围的COX-II抑制剂，但优选使用式I的化合物：

8. 发明授权

US06417221B1 Tropane analogs and methods for inhibition of monoamine transport 有权
标题翻译：托烷类似物和抑制单胺转运的方法
公开(公告)号：US06417221B1
公开(公告)日：2002-07-09
申请号：US09671534
申请日：2000-09-27
申请人： Peter C. Meltzer , Bertha K. Madras , Paul Blundell , Zhengming Chen
发明人： Peter C. Meltzer , Bertha K. Madras , Paul Blundell , Zhengming Chen
IPC分类号： A61K3138
CPC分类号： C07D451/02 , A61K31/18 , A61K31/198 , A61K31/405 , A61K38/00 , A61K51/0448 , A61K2123/00 , C07C69/753 , C07C2602/44 , C07D451/06 , C07D471/08 , C07D493/08
摘要： New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7- substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.
摘要翻译：描述了结合单胺转运蛋白的新的托烷类似物，特别是具有6-或7-取代基的8-氮杂，8-碳代和8-氧代正丙烷。本发明的化合物可以是外消旋的，纯的R-对映体或纯的S-对映异构体。某些优选的本发明化合物对于DAT与SERT具有高选择性。还描述了包含配制在药学上可接受的载体中的化合物的药物治疗组合物和通过使单胺转运蛋白与5-羟色胺重摄取抑制量的本发明化合物接触来抑制单胺转运蛋白的5-羟基 - 色胺再摄取的方法。用于实施本发明的优选的单胺转运蛋白包括多巴胺转运蛋白，5-羟色胺转运蛋白和去甲肾上腺素转运蛋白。

9. 发明授权

US06410587B1 Compounds and therapies for the prevention of vascular and non-vascular pathologies 失效
标题翻译：用于预防血管和非血管病变的化合物和疗法
公开(公告)号：US06410587B1
公开(公告)日：2002-06-25
申请号：US09567558
申请日：2000-05-05
申请人： David J. Grainger , James C. Metcalfe , Sudhakar Kasina
发明人： David J. Grainger , James C. Metcalfe , Sudhakar Kasina
IPC分类号： A61K3138
CPC分类号： A61K31/275 , A61K31/381 , C07D333/38 , G01N33/74 , G01N2333/495 , G01N2333/71 , G01N2800/108 , G01N2800/323
摘要： The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.
摘要翻译：本发明提供了治疗具有或具有与TGF-β缺乏相关的指征的哺乳动物的方法，包括施用一种或多种有效提高TGF-β水平的试剂。本发明还提供了提高TGF-β水平的新化合物，以及包含提高TGF-β水平的化合物的药物组合物，以及用于检测与内皮细胞活化相关的疾病的方法。

10. 发明授权

US06355671B1 SULFONATED DERIVATIVES OF CYCLIC PHENOL SULFIDES, PROCESS FOR THE PREPARATION THEREOF, SEPARATING AND RECOVERING AGENTS CONTAINING CYCLIC PHENOL SULFIDES, METHODS FOR SEPARATION AND RECOVERY THEREWITH, AND DRUG COMPOSITIONS CONTAINING THE SULFIDES 有权
标题翻译：循环酚硫化物的硫化衍生物，其制备方法，包含环状酚醛硫酸盐的分离和还原剂，其分离和回收方法以及含有硫化物的药物组合物
公开(公告)号：US06355671B1
公开(公告)日：2002-03-12
申请号：US09581089
申请日：2000-06-09
申请人： Sotaro Miyano , Nobuhiko Iki , Toyohisa Fujimoto , Fumio Hamada , Shingo Kato , Yoshiyuki Hiraishi , Hitoshi Kumagai , Mitsuharu Hasegawa , Setsuko Miyanari , Yoshihiro Sugawa , Masahiro Ishizuka
发明人： Sotaro Miyano , Nobuhiko Iki , Toyohisa Fujimoto , Fumio Hamada , Shingo Kato , Yoshiyuki Hiraishi , Hitoshi Kumagai , Mitsuharu Hasegawa , Setsuko Miyanari , Yoshihiro Sugawa , Masahiro Ishizuka
IPC分类号： A61K3138
CPC分类号： B01D15/00 , B01J20/22 , B01J20/26
摘要： A sulfonic acid compound of a cyclic phenol sulfide represented by formula (1): (wherein X represents a hydrogen atom, a hydrocarbon group, or an acyl group; M represents a hydrogen atom, an alkyl group, a metal, ammonium, (lower-alkyl)ammonium, (lower-alkanol)ammonium, a nitrogen-containing heterocyclic group, or an amino acid residue; Z represents Sm, SO, or SO2; m is an integer of from 1 to 7; and n is an integer of from 4 to 12, with the proviso that the plural X's, M's and Z's are each the same or different, and at least one of the plural M's is neither a hydrogen atom nor an alkyl group), or a salt thereof; a composition for separating and recovering an organic halogen compound or a monocyclic aromatic compound, comprising a cyclic phenol sulfide or a salt thereof, and a carrier; and a pharmaceutical composition a cyclic phenol sulfide or a pharmaceutically acceptable salt, and a carrier.
摘要翻译：由式（1）表示的环状苯酚硫化物的磺酸化合物:(其中X表示氢原子，烃基或酰基; M表示氢原子，烷基，金属，铵，（低级 - 烷基）铵，（低级链烷醇）铵，含氮杂环基或氨基酸残基; Z表示Sm，SO或SO2; m为1至7的整数; n为 4至12，条件是复数X，M和Z各自相同或不同，并且多个M中的至少一个既不是氢原子也不是烷基）或其盐; 用于分离和回收有机卤素化合物或单环芳族化合物的组合物，其包含环状苯酚硫化物或其盐和载体; 和药物组合物，环状苯酚硫化物或药学上可接受的盐，以及载体。

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