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公开(公告)号：US07989464B2
公开(公告)日：2011-08-02
申请号：US12356867
申请日：2009-01-21
申请人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
发明人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00
CPC分类号： C07D495/14
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
摘要翻译： 在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂， 含有该化合物的药物组合物，以及使用该化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。
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公开(公告)号：US20090192178A1
公开(公告)日：2009-07-30
申请号：US12356867
申请日：2009-01-21
申请人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
发明人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
IPC分类号： A61K31/519 , C07D495/14 , A61P25/00
CPC分类号： C07D495/14
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
摘要翻译： 在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂， 含有该化合物的药物组合物，以及使用该化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。
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3.发明授权Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors 有权苯磺酰基 - 苯并二氢吡喃，二氢苯并噻喃，四氢萘和相关的γ分泌酶抑制剂公开(公告)号：US08569521B2
公开(公告)日：2013-10-29
申请号：US13267324
申请日：2011-10-06
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Anne Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Anne Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： C07D493/00
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译： 本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。 环烷基环或杂环烷基环可任选被一个或多个取代基取代。 一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如， 治疗阿尔茨海默病。
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4.发明授权Biaryltetrahydroisoquinoline piperidines as selective MCH receptor antagonists for the treatment of obesity and related disorders 失效作为治疗肥胖和相关疾病的选择性MCH受体拮抗剂的二芳基四氢异喹啉哌啶公开(公告)号：US07498441B2
公开(公告)日：2009-03-03
申请号：US10788109
申请日：2004-02-26
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D401/04 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention discloses compounds which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. Compounds of the invention generally have the structure: where the substituents are as defined herein.
摘要翻译： 本发明公开了作为黑色素浓缩激素（MCH）的新型拮抗剂的化合物，以及这些化合物的制备方法。 在其它方面，本发明涉及包含这样的MCH拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。 本发明的化合物通常具有以下结构：其中取代基如本文所定义。
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5.发明申请BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS 有权苯并呋喃酮，噻吗啉，四氢萘酮和相关的游离氨基酸酶抑制剂公开(公告)号：US20120264736A1
公开(公告)日：2012-10-18
申请号：US13267324
申请日：2011-10-06
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： A61K31/352 , C07D409/12 , A61K31/381 , C07D405/12 , A61K31/4433 , A61K31/496 , C07D487/08 , A61K31/4995 , C07D405/14 , A61K31/4545 , C07D413/08 , A61K31/5377 , C07D493/04 , C07D491/052 , A61P25/28 , C07D311/80
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译： 本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。 环烷基环或杂环烷基环可任选被一个或多个取代基取代。 一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如， 治疗阿尔茨海默病。
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6.发明授权Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors 有权苯磺酰基 - 苯并二氢吡喃，二氢苯并噻喃，四氢萘和相关的γ分泌酶抑制剂公开(公告)号：US08067621B2
公开(公告)日：2011-11-29
申请号：US11654821
申请日：2007-01-18
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： C07D493/00 , A61K31/35
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译： 本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。 环烷基环或杂环烷基环可任选被一个或多个取代基取代。 一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如， 治疗阿尔茨海默病。
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公开(公告)号：US20090082336A1
公开(公告)日：2009-03-26
申请号：US12264676
申请日：2008-11-04
申请人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Donalski
发明人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Donalski
IPC分类号： A61K31/55 , C07D495/14 , A61K31/519 , C12N5/06 , A61K31/5377
CPC分类号： C07D471/14 , C07D491/14 , C07D495/04 , C07D495/14 , C09B57/00
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
摘要翻译： 在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂， 含有该化合物的药物组合物，以及使用该化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。
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公开(公告)号：US07598259B2
公开(公告)日：2009-10-06
申请号：US11301672
申请日：2005-12-13
申请人： Julius J Matasi , Deen Tulshian , Duane A Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
发明人： Julius J Matasi , Deen Tulshian , Duane A Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D495/14
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
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公开(公告)号：US07485648B2
公开(公告)日：2009-02-03
申请号：US11152535
申请日：2005-06-14
申请人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
发明人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
IPC分类号： A01N43/54 , A61K31/505 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D471/14 , C07D491/14 , C07D495/04 , C07D495/14 , C09B57/00
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1—R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
摘要翻译： 在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂， 含有该化合物的药物组合物，以及使用该化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。
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公开(公告)号：US08664411B2
公开(公告)日：2014-03-04
申请号：US12665580
申请日：2008-07-01
申请人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul McNamara
发明人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul McNamara
IPC分类号： C07D311/80 , C07D493/04 , A61K31/352
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
摘要翻译： 公开了下式的新型γ-分泌酶抑制剂。 还公开了抑制γ-分泌酶，治疗神经变性疾病的方法和治疗阿尔茨海默氏病的方法。 还公开了在一个反应步骤中使用醛（或酮）和被两个吸电子基团取代的烷基的混合物制备烯烃的方法，并使该混合物与：（a）磺酰卤（例如磺酰氯） 和（b）磺酰基酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱式叔胺，或（d）芳基-C（O） - OC（O） - 芳基和碱式叔胺，或（e）杂芳基-C（O） - 卤化物和碱式叔胺，或（f）杂芳基-C（O）-OC（O） - 杂芳基和 碱性叔胺。
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