公开(公告)号：US20140128361A1

公开(公告)日：2014-05-08

申请号：US14148703

申请日：2014-01-06

申请人： Pharmacopeia Drug Discovery, Inc. ,  Merck Sharp & Dohme Corp.

发明人： Jared N. Cumming ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voight ,  Yusheng Wu ,  Ying Huang ,  Yan Xia ,  Samuel Chackalamannil ,  Tao Guo ,  Douglas W. Hobbs ,  Thuy X.H. Le ,  Jeffrey H. Lowrie ,  Kurt W. Salonz ,  Suresh D. Babu

IPC分类号： C07D243/08 ,  C07D233/32 ,  C07D205/04

CPC分类号： C07D243/08 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/26 ,  C07D209/52 ,  C07D211/26 ,  C07D211/46 ,  C07D217/18 ,  C07D233/32 ,  C07D241/04 ,  C07D241/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06

摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, whereinR1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

摘要翻译： 公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中R1是R是-C（O）-N（R27）（R28），或其余的变量如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。 还公开了治疗认知或神经变性疾病的药物组合物和方法，其包含式I化合物与除式I以外的分泌抑制剂抑制剂，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非 - 甾族抗炎药，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂或抗淀粉样蛋白抗体。

公开(公告)号：US09062007B2

公开(公告)日：2015-06-23

申请号：US14148703

申请日：2014-01-06

申请人： Pharmacopeia Drug Discovery, Inc. ,  Merck Sharp & Dohme Corp.

发明人： Jared N. Cumming ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voight ,  Yusheng Wu ,  Ying Huang ,  Yan Xia ,  Samuel Chackalamannil ,  Tao Guo ,  Douglas W. Hobbs ,  Thuy X. H. Le ,  Jeffrey H. Lowrie ,  Kurt W. Saionz ,  Suresh D. Babu

IPC分类号： C07D233/32 ,  C07D403/12 ,  A61K31/4166 ,  A61K31/4178 ,  C07D243/08 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/26 ,  C07D209/52 ,  C07D211/26 ,  C07D211/46 ,  C07D217/18 ,  C07D241/04 ,  C07D241/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/14 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D205/04

CPC分类号： C07D243/08 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/26 ,  C07D209/52 ,  C07D211/26 ,  C07D211/46 ,  C07D217/18 ,  C07D233/32 ,  C07D241/04 ,  C07D241/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06

摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

摘要翻译： 公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中R1是R是-C（O）-N（R27）（R28），或其余的变量如说明书中所定义。 还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。 还公开了治疗认知或神经变性疾病的药物组合物和方法，其包含式I化合物与除式I以外的分泌抑制剂抑制剂，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非 - 甾族抗炎药，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂或抗淀粉样蛋白抗体。

公开(公告)号：US20160367563A1

公开(公告)日：2016-12-22

申请号：US15250338

申请日：2016-08-29

申请人： Merck Sharp & Dohme Corp.

发明人： Jack D. Scott ,  Andrew W. Stamford ,  Eric J. Gilbert ,  Jared N. Cumming ,  Ulrich Iserloh

IPC分类号： A61K31/549

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）化合物：及其立体异构体，以及所述化合物立体异构体的药学上可接受的盐，其中R 1，R 2，R 3，R 4 ，R 5，R 9，环A，环B，m，n，p，-L 1 - ， - L 2 - 和-L 3 - 独立地如本文所定义。 令人惊奇地发现本发明的新型亚氨基二氮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 2”）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病在内的淀粉样蛋白β（A 2）蛋白相关的病理学的方法。

公开(公告)号：US09475785B2

公开(公告)日：2016-10-25

申请号：US14633952

申请日：2015-02-27

申请人： Merck Sharp & Dohme Corp.

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： C07D417/04 ,  C07D285/18 ,  A61K31/00 ,  A61K31/54 ,  A61K45/06 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D403/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D213/89 ,  C07D417/10 ,  C07C309/30 ,  C07D487/04 ,  A61K31/549 ,  C07D213/26 ,  A61K31/495 ,  C07D239/14

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：及其立体异构体，以及所述化合物立体异构体的药学上可接受的盐，其中R 1，R 2，R 3，R 4 ，R 5，R 9，环A，环B，m，n，p，-L 1 - ， - L 2 - 和-L 3 - 独立地如本文所定义。 令人惊奇地发现本发明的新型亚氨基二氮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 2”）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病在内的淀粉样蛋白β（A 2）蛋白相关的病理学的方法。

公开(公告)号：US20150307465A1

公开(公告)日：2015-10-29

申请号：US14633952

申请日：2015-02-27

申请人： Merck Sharp & Dohme Corp.

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： C07D285/18 ,  C07D417/10 ,  C07D487/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D417/04 ,  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): 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。

公开(公告)号：US20150105354A1

公开(公告)日：2015-04-16

申请号：US14575418

申请日：2014-12-18

申请人： Merck Sharp & Dohme Corp. ,  Pharmacopeia, LLC

发明人： Zhaoning Zhu ,  Brian McKittrick ,  Zhong-Yue Sun ,  Yuanzan C. Ye ,  Johannes H. Voigt ,  Corey Strickland ,  Elizabeth M. Smith ,  Andrew W. Stamford ,  William J. Greenlee ,  Robert D. Mazzola, JR. ,  John Caldwell ,  Jared N. Cumming ,  Lingyan Wang ,  Yusheng Wu ,  Ulrich Iserloh ,  Tao Guo ,  Thuy X.H. Le ,  Kurt W. Saionz ,  Suresh D. Babu ,  Rachael C. Hunter

IPC分类号： C07D233/88 ,  C07D401/04 ,  A61K31/4439 ,  C07D405/06 ,  A61K31/4178 ,  C07D401/06 ,  A61K31/454 ,  C07D407/06 ,  C07D403/06 ,  A61K31/5377 ,  C07D235/02 ,  A61K31/4184 ,  A61K31/655 ,  C07D405/14 ,  C07D401/14 ,  A61K31/4545 ,  A61K31/4725 ,  A61K45/06 ,  A61K31/4168

CPC分类号： C07D233/88 ,  A61K31/4168 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/655 ,  A61K45/06 ,  C07D233/46 ,  C07D233/70 ,  C07D235/02 ,  C07D239/22 ,  C07D239/70 ,  C07D271/07 ,  C07D273/00 ,  C07D295/15 ,  C07D401/04 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/10 ,  C07D403/12 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D407/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  Y02A50/411

摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

公开(公告)号：US20160264538A1

公开(公告)日：2016-09-15

申请号：US14653671

申请日：2013-12-16

申请人： Jared N. CUMMING ,  Jack D. SCOTT ,  Andrew W. STAMFORD ,  Ulrich ISERLOH ,  Santhosh Francis NEELAMKAVIL ,  Pengcheng Patrick SHAO ,  Jonathan E. WILSON ,  MERCK SHARP & DOHME CORP.

发明人： Jared N. Cumming ,  Jack D. Scott, JR. ,  Andrew W. Stamford ,  Ulrich Iserloh ,  Santhosh Francis Neelamkavil ,  Pengcheng Patrick Shao ,  Jonathan E. Wilson

IPC分类号： C07D285/24 ,  C07D471/04 ,  C07D417/12 ,  C07D513/10 ,  C07D519/00

CPC分类号： C07D285/24 ,  C07D285/20 ,  C07D417/12 ,  C07D471/04 ,  C07D513/10 ,  C07D519/00

摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. 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:

公开(公告)号：US09416129B2

公开(公告)日：2016-08-16

申请号：US14433298

申请日：2013-10-14

申请人： Merck Sharp & Dohme Corp.

发明人： Eric J. Gilbert ,  Jared N. Cumming ,  Andrew W. Stamford ,  Younong Yu ,  Jack D. Scott ,  Ulrich Iserloh ,  Lingyan Wang ,  John P. Caldwell

IPC分类号： C07D417/14 ,  C07D417/10 ,  C07D417/04 ,  A61K31/549 ,  A61K45/06 ,  C07D495/04

CPC分类号： C07D417/14 ,  A61K31/549 ,  A61K45/06 ,  C07D417/10 ,  C07D495/04

摘要： In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula are as defined herein. 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 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噻嗪二氧化物化合物，包括式（I）化合物：（I）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，其中中环 在本文中作为“环B”）是三环取代基是任选取代的6元环，并且式中所示的各个残基如本文所定义。 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。

公开(公告)号：US20160043774A1

公开(公告)日：2016-02-11

申请号：US14653681

申请日：2013-12-16

申请人： Merck Sharp & Dohme Corp.

发明人： Jared N. Cumming ,  David Earl Kaelin, JR. ,  Jack D. Scott ,  Andrew W. Stamford ,  Ulrich Iserloh

IPC分类号： H04B5/00 ,  G06F1/16 ,  H01P11/00 ,  H01P3/14

CPC分类号： G06F1/1616 ,  C07D513/10

摘要： In its many embodiments, the present invention provides certain C2-ring-substituted thiadiazine compounds, including compounds Formula (I): (structure represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R4, ring A, RA, m, -L1-, RL, and ring C are as defined herein. 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，本发明提供了某些C2环取代的噻二嗪化合物，包括式（I）：（其结构）或其互变异构体的化合物和所述化合物和所述互变异构体的药学上可接受的盐，其中R1，R4，环 A，RA，m，-L1-，RL和环C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，包括用于治疗阿尔茨海默氏病的药物组合物。

公开(公告)号：US20150284379A1

公开(公告)日：2015-10-08

申请号：US14433298

申请日：2013-10-14

申请人： MERCK SHARP & DOHME CORP.

发明人： Eric J. Gilbert ,  Jared N. Cumming ,  Andrew W. Stamford ,  Younong Yu ,  Jack D. Scott ,  Ulrich Iserloh ,  Lingyan Wang ,  John P. Caldwell

IPC分类号： C07D417/14 ,  A61K45/06 ,  C07D495/04 ,  A61K31/549 ,  C07D417/10

CPC分类号： C07D417/14 ,  A61K31/549 ,  A61K45/06 ,  C07D417/10 ,  C07D495/04

摘要： In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula are as defined herein. 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 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噻嗪二氧化物化合物，包括式（I）化合物：（I）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，其中中环 在本文中作为“环B”）是三环取代基是任选取代的6元环，并且式中所示的各个残基如本文所定义。 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。