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1. 发明授权

US5162336A Tetrahydro-pyrido-indoles as cholecystokinin and gastrin antagonists 失效
标题翻译：作为选择性蛋白和胃蛋白酶拮抗剂的四氢吡喃葡萄糖苷
公开(公告)号：US5162336A
公开(公告)日：1992-11-10
申请号：US573514
申请日：1990-08-24
申请人： Bruce F. Molino , Paul R. Darkes , William R. Ewing
发明人： Bruce F. Molino , Paul R. Darkes , William R. Ewing
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Disclosed are tetrahydro-pyrido-indoles having the general formula ##STR1## which are antagonists towards the neuropeptides cholexystokinin and gastrin processing valuable activities for the treatment of cholecystokinin or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems and their pharmaceutical compositions and processes for their preparation.
摘要翻译：公开了具有通式为“IMAGE”的四氢吡啶并吲哚，它们是拮抗神经肽胆碱酯酶和胃泌素处理胃肠，中枢神经和食欲调节系统的缩胆囊肿或胃泌素相关病症的有价值的活性及其药物组合物及其制备方法。

2. 发明授权

US5340801A Compounds having cholecystokinin and gastrin antagonistic properties 失效
标题翻译：具有缩胆囊素和胃泌素拮抗作用的化合物
公开(公告)号：US5340801A
公开(公告)日：1994-08-23
申请号：US697177
申请日：1991-05-08
申请人： William R. Ewing , Bruce F. Molino
发明人： William R. Ewing , Bruce F. Molino
IPC分类号： A61K38/00 , C07K5/02 , C07K5/078 , C07K5/097 , A61K31/40 , A61K37/43 , C07K5/06 , C07K5/08
CPC分类号： C07K5/06165 , C07K5/0202 , C07K5/0821 , A61K38/00
摘要： This invention relates to N-arylcarbamoyl proline analogues which are useful as cholecystokinin and gastrin antagonists, to pharmaceutical compositions including such proline analogues, and to their use in preventing or treating cholecystokinin or gastrin related disorders.
摘要翻译：本发明涉及可用作缩胆囊素和胃泌素拮抗剂的N-芳基氨基甲酰基脯氨酸类似物，包括这种脯氨酸类似物的药物组合物及其在预防或治疗胆囊收缩素或胃泌素相关病症中的用途。

3. 发明授权

US08987252B2 Aryloxy- and heteroaryloxy-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权
标题翻译：芳氧基和杂芳氧基取代的四氢苯并氮杂及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取
公开(公告)号：US08987252B2
公开(公告)日：2015-03-24
申请号：US12598912
申请日：2008-05-08
申请人： Shuang Liu , Yuh-lin Allen Yang , Aruna Sambandam , Bruce F. Molino , Richard E. Olson
发明人： Shuang Liu , Yuh-lin Allen Yang , Aruna Sambandam , Bruce F. Molino , Richard E. Olson
IPC分类号： A61K31/55 , C07D223/16 , C07D471/04 , C07D401/04 , C07D401/14 , C07D403/04
CPC分类号： C07D471/04 , C07D223/16 , C07D401/04 , C07D401/14 , C07D403/04
摘要： The aryloxy- and heteroaryloxy-substituted tetrahydrobenzazepine derivative compounds of the present invention are represented by formulae (I) (A-E) having the following structure where the carbon atom designated * is in the R or S configuration and the substituents X and R1—R9 are as defined herein.
摘要翻译：本发明的芳氧基 - 和杂芳氧基取代的四氢苯并吖庚因衍生物化合物由具有以下结构的式（I）（AE）表示，其中指定为*的碳原子为R或S构型，取代基X和R 1 -R 9为如本文所定义。

4. 发明授权

US08236796B2 Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权
标题翻译：芳基和杂芳基取代的四氢异喹啉及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取
公开(公告)号：US08236796B2
公开(公告)日：2012-08-07
申请号：US12417598
申请日：2009-04-02
申请人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
发明人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
IPC分类号： C07D403/04 , C07D217/02 , A61K31/47
CPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/00 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.
摘要翻译：本发明的化合物由式（I）中所示的化学结构表示：其中：指定为*的碳原子为R或S构型; 并且X是选自苯并呋喃基，苯并[b]噻吩基，苯并异噻唑基，苯并异恶唑基，吲唑基，吲哚基，异吲哚基，吲嗪基，苯并咪唑基，苯并恶唑基，苯并噻唑基，苯并三唑基，咪唑并[1,2-a ]吡啶基，吡唑并[1,5-a]吡啶基，[1,2,4]三唑并[4,3-a]吡啶基，噻吩并[2,3-b]吡啶基，噻吩并[3,2-b] 二氢苯并噻吩基，二氢苯并呋喃基，二氢苯并噻吩基，四氢萘基，喹啉基，异喹啉基，4H-喹啉基，9H-喹啉基，喹唑啉基，噌啉基，酞嗪基，喹喔啉基，苯并[1,2,3]三嗪基，苯并[1,2,4]三嗪基，2H-色烯基，4H-色烯基和稠合的双环碳环或稠合双环杂环，其任选被如所定义的取代基（数目为1至4）在R14; 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。

5. 发明授权

US07868010B2 Capped pyrazinoylguanidine sodium channel blockers 有权
标题翻译：封闭的吡嗪基胍钠通道阻滞剂
公开(公告)号：US07868010B2
公开(公告)日：2011-01-11
申请号：US12049968
申请日：2008-03-17
申请人： Michael R. Johnson , Bruce F. Molino , Jianzhong Zhang , Bruce Sargent
发明人： Michael R. Johnson , Bruce F. Molino , Jianzhong Zhang , Bruce Sargent
IPC分类号： A61K31/4965
CPC分类号： C07D241/26 , A61K31/4965 , A61K31/497 , C07D241/32 , C07D403/12 , C07D413/12 , C07D417/12 , C07D473/00 , C07D473/16
摘要： The invention relates to substituted pyrazinoylguanidine compounds. These compounds are useful as sodium channel blockers, and may be effective in treating a variety of conditions including chronic bronchitis and cystic fibrosis.
摘要翻译：本发明涉及取代的吡嗪基胍化合物。这些化合物可用作钠通道阻滞剂，并且可有效治疗各种病症，包括慢性支气管炎和囊性纤维化。

6. 发明授权

US07807834B2 Capped pyrazinoylguanidine sodium channel blockers 失效
标题翻译：封闭的吡嗪基胍钠通道阻滞剂
公开(公告)号：US07807834B2
公开(公告)日：2010-10-05
申请号：US11195758
申请日：2005-08-03
申请人： Michael R. Johnson , Bruce F. Molino , Bruce Sargent , Jianzhong Zhang
发明人： Michael R. Johnson , Bruce F. Molino , Bruce Sargent , Jianzhong Zhang
IPC分类号： C07D241/02
CPC分类号： C07D241/26 , A61K31/495 , A61K31/50 , A61K45/06
摘要： The present invention relates to group of pyrazinoylguanidine compounds useful as sodium channel blockers. The compounds may be used to promote promoting hydration of mucosal surfaces.
摘要翻译：本发明涉及可用作钠通道阻断剂的吡嗪基胍化合物组。该化合物可用于促进促进粘膜表面的水合。

7. 发明授权

US07799756B2 Processes for stereoselective synthesis of trans ISATX247 有权
标题翻译：用于立体选择性合成反式ISATX247的方法
公开(公告)号：US07799756B2
公开(公告)日：2010-09-21
申请号：US11572833
申请日：2005-07-26
申请人： Bruce F. Molino , Zhicai Yang , Jun-Ho Maeng , David D. Manning
发明人： Bruce F. Molino , Zhicai Yang , Jun-Ho Maeng , David D. Manning
IPC分类号： A61K38/13 , A61K38/12
CPC分类号： C07K7/645
摘要： The present invention relates to a process for preparation of a trans ISATX247 compound of the formula: where R1═H or D; R2═H or D; and R3═H or D, by application of organozirconium chemistry. The process involves reacting an acetyl cyclosporin aldehyde with an organozirconium reagent to provide acetyl cyclosporin diene (the acetate of trans ISATX247) and deacetylating the acetyl cyclosporin diene to produce the trans-isomer of ISATX247. The present invention also relates to a process for preparing the same trans ISATX 247 compound, using olefin cross metathesis. The process involves: olefin cross metathesis of acetyl cyclosporin A to afford acetyl cyclosporin α,β-unsaturated aldehyde; Wittig reaction of the acetyl cyclosporin α,β-unsaturated aldehyde to provide acetyl cyclosporin diene; and deacetylation of the acetyl cyclosporin diene to produce the trans ISATX247 compound. Also disclosed are processes for preparing an acetyl cyclosporin α,β-unsaturated aldehyde compound and a cyclosporin triene analogue compound.
摘要翻译：本发明涉及制备下式的反式ISATX247化合物的方法：其中R1 = H或D; R2 = H或D; 和R3 = H或D，通过应用有机锆化学。该方法包括使乙酰环孢菌素醛与有机锆试剂反应以提供乙酰环孢菌素二烯（反式ISATX247的乙酸酯），并使乙酰环孢素二烯脱乙酰以产生ISATX247的反式异构体。本发明还涉及使用烯烃交叉复分解制备相同的ISATX 247化合物的方法。该方法包括：乙酰环孢菌素A的烯烃交叉复分解，得到乙酰环孢菌素α，不饱和醛; 乙酰环孢菌素α和β-不饱和醛的维蒂希反应提供乙酰环孢素二烯; 和乙酰环孢菌素二烯的脱乙酰化产生反式ISATX247化合物。还公开了制备乙酰环孢菌素α，β-不饱和醛化合物和环孢菌素三烯类似物化合物的方法。

8. 发明申请

US20100210624A1 ARYLOXY- AND HETEROARYLOXY-SUBSTITUTED TETRAHYDROBENZAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN 有权
标题翻译： ARYLOXY-和HETEROARYLOXY取代的四氢苯并嗪和其用于阻断肾上腺素，多巴胺和丝氨酸蛋白酶
公开(公告)号：US20100210624A1
公开(公告)日：2010-08-19
申请号：US12598912
申请日：2008-05-08
申请人： Shuang Liu , Yuh-lin Allen Yang , Aruna Sambandam , Bruce F. Molino , Richard E. Olson
发明人： Shuang Liu , Yuh-lin Allen Yang , Aruna Sambandam , Bruce F. Molino , Richard E. Olson
IPC分类号： A61K31/55 , C07D223/16 , A61P21/00 , A61P25/16 , A61P25/28 , A61P3/04 , A61P3/10 , A61P15/00
CPC分类号： C07D471/04 , C07D223/16 , C07D401/04 , C07D401/14 , C07D403/04
摘要： The aryloxy- and heteroaryloxy-substituted tetrahydrobenzazepine derivative compounds of the present invention are represented by formulae (I) (A-E) having the following structure where the carbon atom designated * is in the R or S configuration and the substituents X and R1-R9 are as defined herein.
摘要翻译：本发明的芳氧基 - 和杂芳氧基取代的四氢苯并吖庚因衍生物化合物由具有以下结构的式（I）（AE）表示，其中指定为*的碳原子为R或S构型，取代基X和R 1 -R 9为如本文所定义。

9. 发明授权

US07696166B2 Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders 失效
标题翻译：使用环孢菌素炔/烯类似物来预防或治疗病毒性疾病
公开(公告)号：US07696166B2
公开(公告)日：2010-04-13
申请号：US11391023
申请日：2006-03-28
申请人： Bruce F. Molino
发明人： Bruce F. Molino
IPC分类号： A61K38/12
CPC分类号： A61K38/13 , A61K38/21 , A61K38/212
摘要： The present invention relates to methods of preventing or treating a mammal with a viral-induced disorder. The method involves administering to the mammal a therapeutically effective amount of a compound represented by Formula I, as shown below: or a pharmaceutically acceptable salt thereof, with X, R0, R1, and R2 defined herein, under conditions effective to prevent or treat the viral-induced disorder.
摘要翻译：本发明涉及用病毒诱导的病症预防或治疗哺乳动物的方法。该方法包括在有效预防或治疗哺乳动物的条件下向哺乳动物施用治疗有效量的由式I表示的化合物，如下所示：或其药学上可接受的盐，与本文定义的X，R0，R1和R2 病毒诱导的病症。

10. 发明授权

US07378391B2 Cyclosporin alkyne analogues and their pharmaceutical uses 失效
标题翻译：环孢菌素炔类似物及其药物用途
公开(公告)号：US07378391B2
公开(公告)日：2008-05-27
申请号：US11232360
申请日：2005-09-21
申请人： Bruce F. Molino , Zhicai Yang
发明人： Bruce F. Molino , Zhicai Yang
IPC分类号： A61K38/13
CPC分类号： C07K7/645 , A61K38/00
摘要： The compounds of the present invention are represented by the chemical structure found in Formula I: or a pharmaceutically acceptable salt thereof, with X, R0, R1, and R2 defined herein.
摘要翻译：本发明的化合物由式I所示的化学结构或其药学上可接受的盐表示，其中X，R 0，R 1和R 2， SUB> 2 。

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