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41. 发明授权

US5792763A Serotonin 5-HT.sub.1F agonists 失效
标题翻译： 5-羟色胺5-HT1F激动剂
公开(公告)号：US5792763A
公开(公告)日：1998-08-11
申请号：US938739
申请日：1997-09-26
申请人： James E. Fritz , Stephen W. Kaldor , Sidney Xi Liang , Upinder Singh , Yao-Chang Xu
发明人： James E. Fritz , Stephen W. Kaldor , Sidney Xi Liang , Upinder Singh , Yao-Chang Xu
IPC分类号： A61K31/343 , A61K31/381 , A61K31/443 , A61K31/4525 , A61P25/06 , A61P43/00 , C07D307/81 , C07D333/58 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , A61K31/54 , A61K31/445 , A61K31/535 , C07D417/00
CPC分类号： C07D405/04 , C07D307/81 , C07D333/58 , C07D405/12 , C07D409/12
摘要： This invention provides novel 5-HT.sub.1F agonists of formula ##STR1## where X, Y, Z,and R are defined in the specification, which are useful for the prevention and treatment of migraine and associated disorders.
摘要翻译：本发明提供了新颖的式（I）的5-HT1F激动剂，其中X，Y，Z和R在说明书中定义，其可用于预防和治疗偏头痛及相关疾病。

42. 发明授权

US5736523A Antineoplastic heteronapthoquinones 失效
标题翻译：抗肿瘤异二氢醌
公开(公告)号：US5736523A
公开(公告)日：1998-04-07
申请号：US401493
申请日：1995-03-10
申请人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavallee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean Louis Kraus
发明人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavallee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean Louis Kraus
IPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08 , A61K31/70 , C07H15/24
CPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08
摘要： This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.
摘要翻译：本发明涉及萘醌衍生物，制备这些衍生物的方法和中间体，以及这些衍生物作为哺乳动物抗肿瘤剂的用途。

43. 发明授权

US5708187A 6-substituted-1,2,3,4-tetrahydro-9H-carbazoles and 7-substituted-10H-cyclohepta �7,6-B!indoles: New 5-HT.sub.1F agonists 失效
标题翻译： 6-取代-1,2,3,4-四氢-9H-咔唑和7-取代-10H-环庚[7,6-B]吲哚：新的5-HT1F激动剂
公开(公告)号：US5708187A
公开(公告)日：1998-01-13
申请号：US671465
申请日：1996-06-27
申请人： Michael Edward Flaugh , Anton Daniel Kiefer, Jr. , Clint Duane Walker , Yao-Chang Xu
发明人： Michael Edward Flaugh , Anton Daniel Kiefer, Jr. , Clint Duane Walker , Yao-Chang Xu
IPC分类号： C07D209/88 , C07D209/94
CPC分类号： C07D209/94 , C07D209/88
摘要： This invention provides novel 6-substituted-1,2,3,4-tetrahydro-9H-carbazoles and 7-substituted-10H-cyclohepta�7,6-b!indoles. These compounds are 5-HT.sub.1F agonists which are useful for the treatment of migraine and associated disorders.
摘要翻译：本发明提供新的6-取代-1,2,3,4-四氢-9H-咔唑和7-取代-10H-环庚三烯并[7,6-b]吲哚。这些化合物是可用于治疗偏头痛和相关疾病的5-HT1F激动剂。

44. 发明申请

US20150250799A1 Triazolopyridine Compounds 审中-公开
标题翻译：三唑并吡啶化合物
公开(公告)号：US20150250799A1
公开(公告)日：2015-09-10
申请号：US14716159
申请日：2015-05-19
申请人： Chao CHEN , Haibing DENG , Haibing Guo , Feng HE , Lei Jiang , Fang Liang , Yuan Mi , Huixin Wan , Yao-Chang Xu , Hongping Yu , Ji Yue Zhang
发明人： Chao CHEN , Haibing DENG , Haibing Guo , Feng HE , Lei Jiang , Fang Liang , Yuan Mi , Huixin Wan , Yao-Chang Xu , Hongping Yu , Ji Yue Zhang
IPC分类号： A61K31/551 , A61K31/496 , A61K31/5377 , A61K31/4709
CPC分类号： A61K31/551 , A61K31/437 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K45/06 , C07D471/04 , C07D491/107 , C07D519/00
摘要： The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
摘要翻译：本发明涉及式（I）的化合物及其盐：其中取代基如说明书中所定义; 用于治疗人或动物体的式（I）化合物，特别是关于c-Met酪氨酸激酶介导的疾病或病症; 使用式（I）化合物制备用于治疗这些疾病的药物; 包含式（I）化合物，任选在组合配偶体存在下的药物组合物，以及制备式（I）化合物的方法。

45. 发明申请

US20130245002A1 Triazolopyridine Compounds 有权
公开(公告)号：US20130245002A1
公开(公告)日：2013-09-19
申请号：US13613291
申请日：2012-09-13
申请人： Chao CHEN , Haibing DENG , Haibing GUO , Feng HE , Lei JIANG , Fang LIANG , Yuan MI , Huixin WAN , Yao-Chang XU , Hongping YU , Ji Yue ZHANG
发明人： Chao CHEN , Haibing DENG , Haibing GUO , Feng HE , Lei JIANG , Fang LIANG , Yuan MI , Huixin WAN , Yao-Chang XU , Hongping YU , Ji Yue ZHANG
IPC分类号： C07D471/04 , A61K31/496 , A61K31/5513 , A61K31/5377 , C07D491/107 , A61K45/06 , A61K31/437
CPC分类号： A61K31/551 , A61K31/437 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K45/06 , C07D471/04 , C07D491/107 , C07D519/00
摘要： The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).

46. 发明申请

US20120142681A1 HETEROCYCLIC HYDRAZONE COMPOUNDS 有权
标题翻译：杂环氢化合物
公开(公告)号：US20120142681A1
公开(公告)日：2012-06-07
申请号：US13389912
申请日：2010-08-10
申请人： Feng He , Miao Dai , Xingnian Fu , Yue Li , Lei Liu , Yuan Mi , Yao-chang Xu , Guoliang Xun , Zhengtian Yu , Ji Yue Zhang
发明人： Feng He , Miao Dai , Xingnian Fu , Yue Li , Lei Liu , Yuan Mi , Yao-chang Xu , Guoliang Xun , Zhengtian Yu , Ji Yue Zhang
IPC分类号： A61K31/5377 , A61K31/5025 , A61P29/00 , A61K31/4985 , A61K31/53 , A61P35/00 , C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
摘要翻译：本发明涉及式（I）的化合物及其盐：其中取代基如说明书中所定义; 用于治疗人或动物体的式（I）化合物，特别是关于c-Met酪氨酸激酶介导的疾病或病症; 使用式（I）化合物制备用于治疗这些疾病的药物; 包含式（I）化合物，任选在组合配偶体存在下的药物组合物，以及制备式（I）化合物的方法。

47. 发明授权

US07608629B2 (Piperidinyloxy)phenyl, (piperidinyloxy)pyridinyl, (piperidinylsulfanyl)phenyl and (piperidinylsulfanyl)pyridinyl compounds as 5-HT1F agonists 失效
标题翻译：（哌啶基氧基）苯基，（哌啶基氧基）吡啶基，（哌啶基硫烷基）苯基和（哌啶基硫烷基）吡啶基化合物作为5-HT1F激动剂
公开(公告)号：US07608629B2
公开(公告)日：2009-10-27
申请号：US10552131
申请日：2004-04-14
申请人： Maria-Jesus Blanco-Pillado , Dana Rae Benesh , Sandra Ann Filla , Kevin John Hudziak , Brian Michael Mathes , Daniel Timothy Kohlman , Bai-Ping Ying , Deyi Zhang , Yao-Chang Xu
发明人： Maria-Jesus Blanco-Pillado , Dana Rae Benesh , Sandra Ann Filla , Kevin John Hudziak , Brian Michael Mathes , Daniel Timothy Kohlman , Bai-Ping Ying , Deyi Zhang , Yao-Chang Xu
IPC分类号： A61K31/4545 , C07D401/14
CPC分类号： C07D401/12 , C07D211/44 , C07D211/46 , C07D211/54 , C07D401/14 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.
摘要翻译：本发明涉及式1的化合物及其药学上可接受的酸加成口。本发明的化合物可用于激活5-HT1F受体，抑制神经元蛋白质外渗，以及在哺乳动物，特别是人中治疗或预防偏头痛。

48. 发明授权

US07309702B2 Arylpiperazines having activity at the serotonin 1A receptor 失效
标题翻译：具有5-羟色胺1A受体活性的芳基哌嗪
公开(公告)号：US07309702B2
公开(公告)日：2007-12-18
申请号：US11225541
申请日：2005-09-13
申请人： Alexander Glenn Godfrey , Daniel Timothy Kohlman , John Cunningham O'Toole , Yao-Chang Xu , Tony Yantao Zhang , Jeffrey Forrester McKelvy
发明人： Alexander Glenn Godfrey , Daniel Timothy Kohlman , John Cunningham O'Toole , Yao-Chang Xu , Tony Yantao Zhang , Jeffrey Forrester McKelvy
IPC分类号： A61K31/497 , C07D241/04 , C07D401/04
CPC分类号： C07D295/088 , A61K31/495 , A61K31/496 , C07C45/004 , C07C45/29 , C07C45/40 , C07C45/515 , C07C45/59 , C07C45/68 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D213/74 , C07D295/104 , C07D295/108
摘要： A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.
摘要翻译：一系列芳基哌嗪化合物是用于治疗与5-羟色胺1 A受体相关或受其影响的病症的有效药物; 该化合物在该受体上是特别有效的拮抗剂，特别可用于缓解尼古丁和烟草戒断症状。

49. 发明申请

US20050222206A1 Pyridinoylpiperidines as 5-ht1f agonists 有权
标题翻译：吡啶基哌啶作为5-ht1f激动剂
公开(公告)号：US20050222206A1
公开(公告)日：2005-10-06
申请号：US10509770
申请日：2003-03-27
申请人： Michael Cohen , Daniel Kohlman , Sidney Liang , Vincent Mancuso , Yao-Chang Xu , Bai-Ping Ying , DeAnna Zacherl , Deyi Zhang , Frantz Victor
发明人： Michael Cohen , Daniel Kohlman , Sidney Liang , Vincent Mancuso , Yao-Chang Xu , Bai-Ping Ying , DeAnna Zacherl , Deyi Zhang , Frantz Victor
IPC分类号： A61K31/4545 , A61K31/506 , A61P15/00 , A61P15/10 , A61P17/14 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/34 , A61P43/00 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D41/02
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.
摘要翻译：本发明涉及式I化合物或其药学上可接受的酸加成盐，其中： R 1是C 1 -C 6烷基，取代的C 1 -C 6亚烷基烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 1 -C 3烷基，取代的C 3 -C 3烷基，取代的C 3 -C 3烷基，C 1 -C 3烷基，C 3 -C 3 - 苯基，取代的苯基，杂环或取代的杂环; R 2是氢，C 1 -C 3烷基，C 3 -C 6烷基，C 3 -C 3烷基，C 3 -C 3烷基，或者式II的基团R 3是氢或C 1 -C 6烷基， C 1 -C 3烷基; R 4是氢，卤素或C 1 -C 3烷基; R 5是氢或C 1 -C 3烷基; R 5是氢或C 1 -C 3烷基; R 6是氢或C 1 -C 6烷基; n为1〜6的整数。本发明的化合物可用于活化5-HT 1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。本发明还涉及合成式I化合物中的中间体的方法。

50. 发明授权

US06645967B2 Arylpiperazines having activity at the serotonin 1A receptor 失效
标题翻译：具有5-羟色胺1A受体活性的芳基哌嗪
公开(公告)号：US06645967B2
公开(公告)日：2003-11-11
申请号：US10022045
申请日：2001-12-18
申请人： Daniel Timothy Kohlman , Yao-Chang Xu
发明人： Daniel Timothy Kohlman , Yao-Chang Xu
IPC分类号： A61K31495
CPC分类号： C07D295/088 , A61K31/495 , A61K31/496 , C07C45/004 , C07C45/29 , C07C45/40 , C07C45/515 , C07C45/59 , C07C45/68 , C07C49/563 , C07C49/577 , C07C49/583 , C07C49/86 , C07D213/74 , C07D295/104 , C07D295/108
摘要： Described herein is a method for potentiating the action of a serotonin reuptake inhibitor in increasing the availability of serotonin, norepinephrin and dopamine in the brain, by administering to a patient an effective amount of a compound of the formula wherein Ar′ is a mono or bicyclic aryl or heteroaryl radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; R2 is phenyl, naphthyl or (C3-C12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R3 is selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; X is —(C═O)—; or a pharmaceutically acceptable salt, racemate, optical isomer or solvate thereof.
摘要翻译：本文描述了一种增强5-羟色胺再摄取抑制剂在增加脑中5-羟色胺，去甲肾上腺素和多巴胺的可利用性的作用的方法，其通过向患者施用有效量的式I的化合物Ar'为单环或双环芳基或被一个至三个选自氢，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基，（C 2 -C 6）烯基，（C 2 -C 6），（C 1 -C 6）烷基卤代，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; R 1是氢，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，，（C 2 -C 6）烯基，（C 2 -C 6）炔基，（C 1 -C 6）烷基卤代，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; R 3选自氢（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基，（C 2 -C 6） 6）链烯基，（C2-C6）炔基，（C1-C6）烷基卤代，（C3-C8）环烷基，（C3-C8）环烯基或卤素; X是 - （C = O） - ;或其药学上可接受的盐，外消旋物，旋光异构体或其溶剂化物。

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