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1. 发明申请

US20160016975A1 C2-AZASPIRO IMINOTHIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译： C2-AZASPIRO三嗪类二氧化物作为BACE抑制剂，组合物及其使用
公开(公告)号：US20160016975A1
公开(公告)日：2016-01-21
申请号：US14774204
申请日：2014-03-11
申请人： Eric J. GILBERT , Jared N. CUMMING , Jack D. SCOTT , Wen-Lian WU , Duane A. BURNETT , Andrew W. STAMFORD , MERCK SHARP & DOHME CORP.
发明人： Eric J. Gilbert , Jared N. Cumming , Jack D. Scott , Wen-Lian Wu , Duane A. Burnett , Andrew W. Stamford
IPC分类号： C07D513/10
CPC分类号： C07D513/10
摘要： In its many embodiments, the present invention provides certain C2-azaspiro substituted iminothiazine dioxide compounds. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供某些C2-氮杂螺环取代的亚氨基噻嗪二氧化物化合物。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。

2. 发明授权

US09221839B2 C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use 有权
标题翻译： C5-C6氧环稠合的噻二嗪二氧化物作为BACE抑制剂，组合物及其应用
公开(公告)号：US09221839B2
公开(公告)日：2015-12-29
申请号：US14009883
申请日：2012-04-04
申请人： Jared N. Cumming , Eric J. Gilbert , Andrew W. Stamford
发明人： Jared N. Cumming , Eric J. Gilbert , Andrew W. Stamford
IPC分类号： C07D513/04 , A61K31/549 , A61K31/54 , A61K45/06
CPC分类号： C07D513/04 , A61K31/54 , A61K31/549 , A61K45/06 , A61K2300/00
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of ring A, ring B, ring C, R2, R3, R4, m, n, p, and -L1- is as defined herein. The novel compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括其化学式及互变异构体及其立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中环A，环B，环C，，R3，R4，m，n，p和-L1-如本文所定义。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括阿尔茨海默氏病。

3. 发明申请

US20140296222A1 IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
公开(公告)号：US20140296222A1
公开(公告)日：2014-10-02
申请号：US14221644
申请日：2014-03-21
申请人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming , Ulrich Iserloh
发明人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming , Ulrich Iserloh
IPC分类号： C07D417/12 , C07C309/30
CPC分类号： A61K31/549 , A61K31/00 , A61K31/495 , A61K31/54 , A61K45/06 , C07C309/30 , C07D213/26 , C07D213/89 , C07D239/14 , C07D285/18 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , A61K2300/00
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (“Aβ”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's disease, are also disclosed.

4. 发明申请

US20140128382A1 5-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO- AND DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译： 5代替IMINOTHIAZINES及其单和二氧化物作为BACE抑制剂，组合物及其使用
公开(公告)号：US20140128382A1
公开(公告)日：2014-05-08
申请号：US14110363
申请日：2012-04-12
申请人： Wen-Lian Wu , Duane A. Burnett , Andrew W. Stamford , Jared N. Cumming , Chad E. Bennett , Eric J. Gilbert , Jack D. Scott , Younong Yu , Xuanjia Peng
发明人： Wen-Lian Wu , Duane A. Burnett , Andrew W. Stamford , Jared N. Cumming , Chad E. Bennett , Eric J. Gilbert , Jack D. Scott , Younong Yu , Xuanjia Peng
IPC分类号： C07D279/12 , A61K45/06 , C07D417/04 , A61K31/541 , C07D498/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04 , A61K31/54 , C07D417/14
CPC分类号： C07D279/12 , A61K31/54 , A61K31/541 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and uses, including Alzheimer's disease, are also disclosed.
摘要翻译：本发明公开了某些亚氨基噻嗪化合物及其单 - 和二氧化物，包括式（I）化合物及其互变异构体和立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中式如本文所定义。本发明的化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物，及其制备和用途的方法，包括阿尔茨海默氏病。

5. 发明申请

US20120189642A1 IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译：三氮嗪二氧化物作为BACE抑制剂，组合物及其使用
公开(公告)号：US20120189642A1
公开(公告)日：2012-07-26
申请号：US13392955
申请日：2010-10-06
申请人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming , Ulrich Iserloh , Lingyan Wang , Wei Li
发明人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming , Ulrich Iserloh , Lingyan Wang , Wei Li
IPC分类号： A61K31/549 , C07D417/10 , C07D417/04 , A61K31/55 , A61K39/00 , A61P25/24 , A61P25/16 , A61P25/00 , A61P29/00 , A61P9/00 , A61P7/04 , A61P27/06 , A61P3/10 , A61P7/00 , A61P37/04 , A61K39/395 , A61P31/04 , C07D285/18
CPC分类号： C07D417/04 , C07D285/18 , C07D417/10
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (a) and include tautomers, solvates, prodrugs, esters, and deuterates thereof, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, ring C, m, n, p, q, -L1-, -L2-, L3-, and L4- is selected independently and as defined herein. The compounds of the invention have, surprisingly and advantageously, improved solution stability. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供某些亚氨基二嗪二氧化物化合物，包括式（a）化合物，并且包括其互变异构体，溶剂化物，前药，酯和氘代，以及所述化合物，互变异构体，溶剂合物，前药，酯，氘代，其中R1，R2，R3，R4，R5，R9，环A，环B，环C，m，n，p，q，-L1-，-L2，L3-和L4- 独立选择和如本文所定义。本发明的化合物令人惊奇地和有利地提高了溶液的稳定性。还公开了包含一种或多种这样的化合物（单独并与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与包括阿尔茨海默病在内的淀粉样蛋白β（A＆bgr））蛋白相关的病理学的方法。

6. 发明申请

US20140023668A1 C5-C6 OXACYCLIC-FUSED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译： C5-C6氧化亚铜二氧化物作为BACE抑制剂，组合物及其使用的化合物
公开(公告)号：US20140023668A1
公开(公告)日：2014-01-23
申请号：US14009883
申请日：2012-04-04
申请人： Jared N. Cumming , Eric J. Gilbert , Andrew W. Stamford
发明人： Jared N. Cumming , Eric J. Gilbert , Andrew W. Stamford
IPC分类号： C07D513/04 , A61K45/06 , A61K31/549
CPC分类号： C07D513/04 , A61K31/54 , A61K31/549 , A61K45/06 , A61K2300/00
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula: (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of ring A, ring B, ring C, R2, R3, R4, m, n, p, and -L1- is as defined herein. The novel compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（I）化合物及其互变异构体和立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中环A，环B，环C，R 2，R 3，R 4，m，n，p和-L 1如本文所定义。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括阿尔茨海默氏病。

7. 发明申请

US20120183563A1 IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE 有权
标题翻译：三氮嗪二氧化物作为BACE抑制剂，组合物及其使用
公开(公告)号：US20120183563A1
公开(公告)日：2012-07-19
申请号：US13392297
申请日：2010-10-06
申请人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming , Ulrich Iserloh , Jeffrey A. Misiaszek , Guoqing Li
发明人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming , Ulrich Iserloh , Jeffrey A. Misiaszek , Guoqing Li
IPC分类号： A61K31/549 , C07D285/18 , C07D417/14 , C07D471/04 , C07D495/04 , A61K31/55 , A61K39/395 , A61K39/00 , A61P29/00 , A61P31/04 , A61P37/04 , A61P5/50 , A61P25/28 , A61P25/16 , A61P25/00 , A61P3/10 , C07D417/04 , A61P7/04 , A61P7/00 , C07D417/12
CPC分类号： A61K31/549 , A61K31/00 , A61K31/495 , A61K31/54 , A61K45/06 , C07C309/30 , C07D213/26 , C07D213/89 , C07D239/14 , C07D285/18 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , A61K2300/00
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-,L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (Aβ) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（I）：（I）的化合物并包括其立体异构体，以及所述化合物立体异构体的药学上可接受的盐，其中R1，R2，R3，R4，R5 ，R9，环A，环B，m，n，p，-L1-，L2-和L3-是独立选择和如本文所定义的。令人惊奇地发现本发明的新型亚氨基二嗪二氧化物化合物表现出预期使其作为BACE抑制剂和/或用于治疗和预防与β-淀粉样蛋白（A＆bgr）生产相关的各种病症的优点的性质。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与包括阿尔茨海默氏病在内的淀粉样蛋白β（A＆bgr））蛋白相关的病理学的方法。

8. 发明授权

US09145426B2 Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use 有权
标题翻译：吡咯烷稠合的噻二嗪二氧化物化合物作为BACE抑制剂，组合物及其用途
公开(公告)号：US09145426B2
公开(公告)日：2015-09-29
申请号：US14009654
申请日：2012-04-02
申请人： Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming
发明人： Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming
IPC分类号： C07D513/04 , A61K31/549 , A61K45/06
CPC分类号： C07D513/04 , A61K31/549 , A61K45/06
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of W, Z, R1H, R2, R3, R4, ring A, ring B, m, n, p, and -L1- is as defined herein. The novel compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（I）化合物及其互变异构体和立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中W，Z，R 1 H， R2，R3，R4，环A，环B，m，n，p和-L1-如本文所定义。令人惊奇地发现本发明的新化合物表现出预期使其作为BACE抑制剂和/或用于治疗和预防与之相关的各种病症的优点。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括阿尔茨海默氏病。

9. 发明申请

US20140296221A1 IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译：三氮嗪二氧化物作为BACE抑制剂，组合物及其使用
公开(公告)号：US20140296221A1
公开(公告)日：2014-10-02
申请号：US14221640
申请日：2014-03-21
申请人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming
发明人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming
IPC分类号： C07D417/12 , C07C309/30
CPC分类号： A61K31/549 , A61K31/00 , A61K31/495 , A61K31/54 , A61K45/06 , C07C309/30 , C07D213/26 , C07D213/89 , C07D239/14 , C07D285/18 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , A61K2300/00
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (“Aβ”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（I）化合物：并包括其立体异构体，以及所述化合物立体异构体的药学上可接受的盐，其中R1，R2，R3，R4，R5，R9，环A，环B，m，n，p，-L 1 - ， - 2 - 和-L 3 - 独立地如本文所定义。令人惊讶地发现本发明的新型亚氨基二嗪二氧化物化合物表现出预期使其作为BACE抑制剂和/或用于治疗和预防与“淀粉样蛋白”（“A”）生产有关的各种病理学的优点的性质。还公开了包含一种或多种这样的化合物（单独并与一种或多种其它活性剂组合）的药物组合物，及其制备和用于治疗与淀粉样蛋白β（Aβ）蛋白（包括阿尔茨海默氏病）相关的病理学的方法。

10. 发明授权

US08729071B2 Iminothiadiazine dioxide compounds as BACE inhibitors, compositions and their use 有权
标题翻译：作为BACE抑制剂的二氢咪嗪二嗪化合物，组合物及其用途
公开(公告)号：US08729071B2
公开(公告)日：2014-05-20
申请号：US13392297
申请日：2010-10-06
申请人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming
发明人： Jack D. Scott , Andrew W. Stamford , Eric J. Gilbert , Jared N. Cumming
IPC分类号： A61K31/54 , C07D213/89 , C07D213/26
CPC分类号： A61K31/549 , A61K31/00 , A61K31/495 , A61K31/54 , A61K45/06 , C07C309/30 , C07D213/26 , C07D213/89 , C07D239/14 , C07D285/18 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , A61K2300/00
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (Aβ) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（I）：（I）的化合物并包括其立体异构体，以及所述化合物立体异构体的药学上可接受的盐，其中R1，R2，R3，R4，R5 ，R9，环A，环B，m，n，p，-L1-，L2-和L3-是独立选择和如本文所定义的。令人惊奇地发现本发明的新型亚氨基二嗪二氧化物化合物表现出预期使其作为BACE抑制剂和/或用于治疗和预防与β-淀粉样蛋白（A＆bgr）生产相关的各种病症的优点的性质。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与包括阿尔茨海默氏病在内的淀粉样蛋白β（A＆bgr））蛋白相关的病理学的方法。

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