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71. 发明授权

US5559246A Indole derivatives 失效
公开(公告)号：US5559246A
公开(公告)日：1996-09-24
申请号：US466650
申请日：1995-06-06
申请人： John E. Macor
发明人： John E. Macor
IPC分类号： A61K31/40 , C07D401/06 , C07D403/06
CPC分类号： A61K31/40 , C07D401/06 , C07D403/06
摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.

72. 发明授权

US5169947A 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines 失效
标题翻译： 3-（1,2,5,6-四氢吡啶基） - 吡咯并吡啶
公开(公告)号：US5169947A
公开(公告)日：1992-12-08
申请号：US763081
申请日：1991-09-20
申请人： John E. Macor
发明人： John E. Macor
IPC分类号： A61K31/44 , A61K31/445 , A61P3/04 , A61P3/06 , A61P25/18 , A61P25/24 , A61P25/26 , C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of the formula ##STR1## wherein one of A, B, D and E is N and the remaining three atoms are C; R.sup.1 and R.sup.2 are independently selected from hydrogen and C.sub.1 to C.sub.6 alkyl; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.8 alkoxy, phenyl-C.sub.1 -C.sub.6 alkoxy, phenoxy, --NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyl, and COOR.sup.9 wherein R.sup.9 is hydrogen or C.sub.1 -C.sub.6 alkyl, cyano, COOR.sup.10 wherein R.sup.10 is hydrogen or C.sub.1 -C.sub.6 alkyl, and CONR.sup.11 R.sup.12 where R.sup.11 and R.sup.12 are independently selected from hydrogen and C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof. The compounds are useful psychotherapeutics and may be used in treating obesity, depression and disorders wherein aggression is a symptom.
摘要翻译：其中A，B，D和E之一为N，其余三个原子为C; R 1和R 2独立地选自氢和C 1至C 6烷基; 并且R 3，R 4，R 5和R 6独立地选自氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 8烷氧基，苯基-C 1 -C 6烷氧基，苯氧基，-NR 7 R 8，其中R 7和R 8独立地选自氢， -C 6烷基，C 1 -C 6烷酰基和COOR 9，其中R 9是氢或C 1 -C 6烷基，氰基，COOR 10，其中R 10是氢或C 1 -C 6烷基，和CONR 11 R 12，其中R 11和R 12独立地选自氢和C 1 -C 6烷基，及其药学上可接受的盐。这些化合物是有用的精神治疗药物，可用于治疗肥胖症，抑郁症和其中攻击是症状的疾病。

73. 发明授权

US09045468B2 2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权
标题翻译： 2,5-亚甲基和2,5-乙基 - 四氢苯并氮杂衍生物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：US09045468B2
公开(公告)日：2015-06-02
申请号：US13211678
申请日：2011-08-17
申请人： Peter R. Guzzo , Shuang Liu , Kristen N. Ryan , Bruce F. Molino , Russell DeOrazio , Richard E. Olson , John E. Macor
发明人： Peter R. Guzzo , Shuang Liu , Kristen N. Ryan , Bruce F. Molino , Russell DeOrazio , Richard E. Olson , John E. Macor
IPC分类号： A61K31/55 , C07D453/00 , C07D519/00
CPC分类号： C07D453/00 , C07D519/00
摘要： The compounds of the present invention are represented by the following 2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives having formula (I): where the carbon atom designated * is in the R or S configuration when n is 1 and the substituents X and R1-R7 are as defined herein.
摘要翻译：本发明的化合物由以下具有式（I）的2,5-亚甲基 - 和2,5-亚乙基 - 四氢苯并吖庚因衍生物表示：当n为1时，其中指定为*为R或S构型的碳原子，取代基X和R 1 -R 7如本文所定义。

74. 发明授权

US08486952B2 Compounds for the reduction of β-amyloid production 有权
标题翻译：用于减少β-淀粉样蛋白生成的化合物
公开(公告)号：US08486952B2
公开(公告)日：2013-07-16
申请号：US12845045
申请日：2010-07-28
申请人： Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人： Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号： A01N43/54 , A01N43/90 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/497 , A61K31/00 , A61K31/535 , C07D239/70 , C07D491/00 , C07D495/00 , C07D471/00 , C07D413/00
CPC分类号： C07D403/12 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要： The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译：本公开提供了一系列调节β-淀粉样肽（β-AP）产生的式（I）化合物，并且可用于治疗阿尔茨海默病和其它受β-淀粉样蛋白肽（β-AP）产生影响的病症。

75. 发明授权

US08436000B2 Substituted carbamate derivatives as modulators of corticotropin-releasing factor receptor activity 有权
标题翻译：取代的氨基甲酸酯衍生物作为促肾上腺皮质激素释放因子受体活性的调节剂
公开(公告)号：US08436000B2
公开(公告)日：2013-05-07
申请号：US13055885
申请日：2009-07-29
申请人： Richard A. Hartz , Vijay T. Ahuja , John E. Macor
发明人： Richard A. Hartz , Vijay T. Ahuja , John E. Macor
IPC分类号： A61K31/497
CPC分类号： C07D241/22 , C07D401/12 , C07D401/14
摘要： The disclosure provides compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds are CRF receptor antagonists and may be useful for treating disorders associated with abnormal CRF levels or aberrant functioning of CRF receptors.
摘要翻译：本公开提供式（I）化合物，包括其盐，以及使用该化合物的组合物和方法。化合物是CRF受体拮抗剂，可用于治疗与CRF异常异常或CRF受体异常功能相关的疾病。

76. 发明授权

US08278320B2 Azabicyclo[2.2.1]heptane compounds as alpha-7 nicotinic acetylcholine receptor ligands 有权
标题翻译：氮杂双环[2.2.1]庚烷化合物作为α-7烟碱乙酰胆碱受体配体
公开(公告)号：US08278320B2
公开(公告)日：2012-10-02
申请号：US12907122
申请日：2010-10-19
申请人： Ivar M. McDonald , Robert A. Mate , James H. Cook, II , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , Matthew D. Hill , Haiquan Fang , John E. Macor
发明人： Ivar M. McDonald , Robert A. Mate , James H. Cook, II , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , Matthew D. Hill , Haiquan Fang , John E. Macor
IPC分类号： A61K31/438 , A61K31/439 , C07D471/08
CPC分类号： C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including Ia, Ib, Ic, or Id, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译：本公开提供式I化合物，包括Ia，Ib，Ic或Id，包括其盐，以及使用该化合物的组合物和方法。这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。

77. 发明申请

US20110269787A1 Azabicyclic Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands 有权
标题翻译： Azabicyclic化合物作为α-7烟碱乙酰胆碱受体配体
公开(公告)号：US20110269787A1
公开(公告)日：2011-11-03
申请号：US12911882
申请日：2010-10-26
申请人： Ivar M. McDonald , Robert A. Mate , James H. Cook, II , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
发明人： Ivar M. McDonald , Robert A. Mate , James H. Cook, II , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
IPC分类号： A61K31/438 , A61P25/18 , A61P3/10 , A61P19/02 , A61P1/02 , C07D498/20 , A61P25/28
CPC分类号： C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译：本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。

78. 发明申请

US20110245264A1 Modulators of G Protein-Coupled Receptor 88 有权
公开(公告)号：US20110245264A1
公开(公告)日：2011-10-06
申请号：US12895916
申请日：2010-10-01
申请人： Yingzhi Bi , Carolyn Diane Dzierba , Joanne J. Bronson , Kenneth Carson , Giovanni Cianchetta , Li Dong , Cynthia Fink , Michael Green , David Kimball , John E. Macor , Soojin Kwon , Jiancheng Wang , Yulian Zhang , Greg Zipp
发明人： Yingzhi Bi , Carolyn Diane Dzierba , Joanne J. Bronson , Kenneth Carson , Giovanni Cianchetta , Li Dong , Cynthia Fink , Michael Green , David Kimball , John E. Macor , Soojin Kwon , Jiancheng Wang , Yulian Zhang , Greg Zipp
IPC分类号： A61K31/496 , C07D333/24 , A61K31/381 , C07D409/12 , C07C233/60 , A61K31/165 , A61P25/28 , A61P25/18 , A61P25/16 , A61P25/30
CPC分类号： C07D333/24 , C07C233/60 , C07C2601/02
摘要： The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

79. 发明授权

US07981913B2 Isophthalates as beta-secretase inhibitors 有权
标题翻译：异酞酸酯作为β-分泌酶抑制剂
公开(公告)号：US07981913B2
公开(公告)日：2011-07-19
申请号：US12779986
申请日：2010-05-14
申请人： Lorin A. Thompson, III , Kenneth M. Boy , Jianliang Shi , John E. Macor
发明人： Lorin A. Thompson, III , Kenneth M. Boy , Jianliang Shi , John E. Macor
IPC分类号： A61K31/42 , C07D263/30
CPC分类号： C07D265/30 , C07D207/09 , C07D207/12 , C07D207/27 , C07D265/32 , C07D403/12 , C07D413/12 , C07D413/14
摘要： There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供了一系列取代的式（I）的间苯二甲酸酯或其立体异构体; 或其药学上可接受的盐，其中如本文所定义的W，R 3，R 5和R 6，其药物组合物和使用方法。这些新化合物通过分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地，抑制Aβ的生成。本公开涉及可用于治疗与淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

80. 发明授权

US07977362B2 Alpha-(N-benzenesulfonamido)cycloalkyl derivatives 有权
标题翻译： α-（N-苯磺酰氨基）环烷基衍生物
公开(公告)号：US07977362B2
公开(公告)日：2011-07-12
申请号：US12725810
申请日：2010-03-17
申请人： Dalton King , Zhaoxing Meng , Ivar M. McDonald , Richard E. Olson , John E. Macor
发明人： Dalton King , Zhaoxing Meng , Ivar M. McDonald , Richard E. Olson , John E. Macor
IPC分类号： A61K31/4245 , A61K31/421 , C07D271/06 , C07D263/32
CPC分类号： C07D271/06 , C07D263/32 , C07D273/02 , C07D413/12
摘要： Disclosed are compounds, pharmaceutical compositions containing the compounds, methods for using the compounds and processes for making the compounds. More specifically, the disclosure relates to alpha-(N-benzenesulfonamido)cycloalkyl compounds that may inhibit one or both of: (i) the functioning of a γ-secretase enzyme; or (ii) the production of β-amyloid. Such compounds may be beneficial in the treatment of Alzheimer's disease and other conditions. Representative compounds have the following formula I: wherein: A, R1, and R2 are described herein.
摘要翻译：公开了化合物，含有该化合物的药物组合物，使用该化合物的方法和制备该化合物的方法。更具体地，本公开涉及可以抑制以下之一或两者的α-（N-苯磺酰氨基）环烷基化合物：（i）γ-分泌酶的功能; 或（ii）生产β-淀粉样蛋白。这些化合物在治疗阿尔茨海默氏病和其他病症中可能是有益的。代表性的化合物具有下式I：其中：A，R 1和R 2在本文中描述。

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