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1.发明授权1-(2-m-methanesulfonamidophenylethyl)-4-(m-trifluoromethylphenyl) piperazine and pharmaceutically acceptable salts and solvents thereof 失效1-（2-间甲磺酰氨基苯乙基）-4-（间 - 三氟甲基苯基）哌嗪及其药学上可接受的盐和溶剂公开(公告)号：US06864262B2
公开(公告)日：2005-03-08
申请号：US10432413
申请日：2001-11-16
IPC分类号： C07D295/12 , A61K31/495 , A61K45/06 , A61P13/10 , C07D295/135
CPC分类号： C07D295/135 , A61K31/495 , A61K45/06 , A61K2300/00
摘要： The present invention provides a compound of the formula (I) and the pharmaceutically acceptable salts and solvates thereof, which is useful for treating bladder over-activity or urinary incontinence.
摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐和溶剂合物，其可用于治疗膀胱过度活动或尿失禁。
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公开(公告)号：US07214673B2
公开(公告)日：2007-05-08
申请号：US10505805
申请日：2003-03-17
申请人： Thomas Daniel Aicher , Zhaogen Chen , Joseph Herman Krushinski, Jr. , Yvan Le Huerou , Marta Maria Pineiro-Nunez , Kevin Michael Ruley , John Mehnert Schaus , Dennis Charles Thompson , David Edward Tupper , Ying Chen , Margaret Mary Faul , Vincent Patrick Rocco
发明人： Thomas Daniel Aicher , Zhaogen Chen , Joseph Herman Krushinski, Jr. , Yvan Le Huerou , Marta Maria Pineiro-Nunez , Kevin Michael Ruley , John Mehnert Schaus , Dennis Charles Thompson , David Edward Tupper , Ying Chen , Margaret Mary Faul , Vincent Patrick Rocco
IPC分类号： A61P25/00 , A61K31/55 , C07D243/10
CPC分类号： C07D487/04 , C07D243/38 , C07D495/04 , C07D513/04
摘要： Described herein are antipyschotic compounds of formula (I) wherein, A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R1 is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH, wherein R3 is (C1-2) alkyl; R2 is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl, wherein R4 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, or optionally substituted phenyl, R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; Z is one or two substituents independently selected from hydrogen, halogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, SO2NR8R9, NR8SO2R7, NR8R9, or optionally substituted phenyl, wherein R7 is hydrogen, (C1-6) alkyl, fluorinated alkyl, or optionally substituted phenyl, R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; and salts, solvates, and crystal forms thereof. Also described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorder, and pharmaceutical formulations of the compounds of formula (I).
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3.发明授权5-substituted-3-(1,2,3,6-tetrahydropyridin-4-yl)-and 3-(piperidin-4-yl)-1h-indoles: 5-HT.sub.1F agonists 失效5-取代-3-（1,2,3,6-四氢吡啶-4-基） - 和3-（哌啶-4-基）-1H-吲哚：5-HT1F激动剂
公开(公告)号：US5962474A
公开(公告)日：1999-10-05
申请号：US977526
申请日：1997-11-24
申请人： James Edmund Audia , Bruce Anthony Dressman , James Joseph Droste , James Erwin Fritz , Stephen Warren Kaldor , Daniel James Koch , Joseph Herman Krushinski, Jr. , Jeffrey Scott Nissen , Vincent Patrick Rocco , John Mehnert Schaus , Dennis Charles Thompson
发明人： James Edmund Audia , Bruce Anthony Dressman , James Joseph Droste , James Erwin Fritz , Stephen Warren Kaldor , Daniel James Koch , Joseph Herman Krushinski, Jr. , Jeffrey Scott Nissen , Vincent Patrick Rocco , John Mehnert Schaus , Dennis Charles Thompson
IPC分类号： A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , A61P25/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , A61K31/40
CPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D409/14 , Y02P20/582
摘要： This invention provides novel 5-HT.sub.1F agonists of Formula I ##STR1## where A--B, R,R.sup.1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.
摘要翻译： 本发明提供式I的新型5-HT1F激动剂，其中A-B，R，R 1和X如说明书中所定义，其可用于治疗偏头痛及相关疾病。
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4.发明授权5-Substituted-3-(1,2,3,6-tetrahydropyridin-4-yl)-and 3-(piperidin-4-yl)-1H-indoles: new 5-HT.sub.1F agonists 失效5-取代的3-（1,2,3,6-四氢吡啶-4-基） - 和3-（哌啶-4-基）-1H-吲哚：新的5-HT1F激动剂
公开(公告)号：US5708008A
公开(公告)日：1998-01-13
申请号：US619783
申请日：1996-03-20
申请人： James Edmund Audia , Bruce Anthony Dressman , James Joseph Droste , James Erwin Fritz , Stephen Warren Kaldor , Daniel James Koch , Joseph Herman Krushinski, Jr. , Jeffrey Scott Nissen , Vincent Patrick Rocco , John Mehnert Schaus , Dennis Charles Thompson
发明人： James Edmund Audia , Bruce Anthony Dressman , James Joseph Droste , James Erwin Fritz , Stephen Warren Kaldor , Daniel James Koch , Joseph Herman Krushinski, Jr. , Jeffrey Scott Nissen , Vincent Patrick Rocco , John Mehnert Schaus , Dennis Charles Thompson
IPC分类号： A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/54 , A61P25/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14
CPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D409/14 , Y02P20/582
摘要： This invention provides novel 5-HT.sub.1F agonists of Formula I ##STR1## where A--B, R, R.sup.1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.
摘要翻译： 本发明提供式I的新型5-HT1F激动剂，其中A-B，R，R 1和X如说明书中所定义，其可用于治疗偏头痛及相关疾病。
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公开(公告)号：US06777428B1
公开(公告)日：2004-08-17
申请号：US09890741
申请日：2001-12-04
IPC分类号： C07D21122
CPC分类号： C07D401/06 , C07D211/22 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to a compound of formula I and a process for making: or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT1F receptors and inhibiting neuronal protein extravasation in a mammal.
摘要翻译： 本发明涉及式I化合物及其制备方法：或其药用酸加成盐; 其可用于激活哺乳动物中的5-HT1F受体并抑制神经元蛋白质外渗。
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公开(公告)号：US5874427A
公开(公告)日：1999-02-23
申请号：US59768
申请日：1998-04-14
IPC分类号： A61P25/04 , A61K31/437 , A61K31/4375 , A61K31/55 , A61P25/06 , A61P43/00 , C07D455/02 , C07D455/03 , C07D471/04 , C07D519/00 , A61K31/435
CPC分类号： C07D455/00 , C07D471/04
摘要： This invention provides novel 5-HT.sub.1F agonists of the Formula ##STR1## in which X, Y, E, R, A, B, and n are as defined in the specification, which are useful for the treatment of migraine and associated disorders.
摘要翻译： 本发明提供了本发明的新颖的5-HT1F激动剂，其中X，Y，E，R，A，B和n如说明书中所定义，其可用于治疗偏头痛及相关疾病。
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7.发明授权公开(公告)号：US08044090B2
公开(公告)日：2011-10-25
申请号：US12504242
申请日：2009-07-16
申请人： Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
发明人： Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
IPC分类号： A61K31/4045 , A61K31/137 , C07D209/14
CPC分类号： C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要： The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.
摘要翻译： 本发明提供作为5-HT 6受体拮抗剂的式（I）化合物。
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公开(公告)号：US20110144091A1
公开(公告)日：2011-06-16
申请号：US12961714
申请日：2010-12-07
申请人： Macklin Brian Arnold , Thomas James Beauchamp , Emily Jane Canada , Erik James Hembre , Jianliang Lu , John Robert Rizzo , John Mehnert Schaus , Qing Shi
发明人： Macklin Brian Arnold , Thomas James Beauchamp , Emily Jane Canada , Erik James Hembre , Jianliang Lu , John Robert Rizzo , John Mehnert Schaus , Qing Shi
IPC分类号： A61K31/55 , C07D487/04 , A61P3/04 , A61P3/00
CPC分类号： C07D487/04
摘要： This invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof; as well as a method for treating obesity, a method for treating diabetes, and a pharmaceutical composition.
摘要翻译： 本发明提供式I化合物或其药学上可接受的盐; 以及用于治疗肥胖症的方法，治疗糖尿病的方法和药物组合物。
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9.发明授权公开(公告)号：US07157488B2
公开(公告)日：2007-01-02
申请号：US10472741
申请日：2002-03-15
申请人： Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
发明人： Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
IPC分类号： A61K31/4045 , A61K31/137 , C07D209/14 , C07C211/00
CPC分类号： C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要： The present invention provides compounds of formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are antagonists of the 5-HT6 receptor. The present invention further provides a method of treating disorders associated with 5-HT6 receptors, including schizophrenia, anxiety, Alzheimer's disease, and cognitive disorders selected from the group consisting of age-related cognitive decline, mild cognitive impairment, and dementia, comprising: administering to a patient in need thereof an effective amount of a compound of formula I.
摘要翻译： 本发明提供式I化合物其药学上可接受的盐及其药物组合物，它们是5-HT 6受体的拮抗剂。 本发明还提供了一种治疗与5-HT 6受体相关的疾病的方法，包括精神分裂症，焦虑症，阿尔茨海默氏病和认知障碍，其选自年龄相关的认知衰退，轻度认知 损伤和痴呆，包括：向有需要的患者施用有效量的式I化合物。
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公开(公告)号：US5817671A
公开(公告)日：1998-10-06
申请号：US969851
申请日：1997-11-14
IPC分类号： A61P25/04 , A61K31/00 , A61K31/437 , A61K31/444 , A61K31/4545 , A61P25/06 , A61P43/00 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04 , A61K31/00 , A61K31/437 , A61K31/444 , A61K31/4545
摘要： This invention provides 5-HT.sub.1F agonists of Formula I: ##STR1## where A--B, X, and R are as defined in the specification. The invention also encompasses pharmaceutical formulations employing compounds of Formula I as well as methods of treating conditions associated with 5-HT.sub.1F activation employing these compounds or compositions. The invention also provides intermediates useful for the preparation of the compounds of Formula I.
摘要翻译： 本发明提供式I的5-HT1F激动剂：其中A-B，X和R如说明书中所定义。 本发明还包括使用式I化合物的药物制剂以及使用这些化合物或组合物治疗与5-HT1F活化相关的病症的方法。 本发明还提供了可用于制备式I化合物的中间体。
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