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1. 发明申请

US20200230140A1 N3-SUBSTITUTED IMINOPYRIMIDINONES AS ANTIMALARIAL AGENTS 审中-公开
公开(公告)号：US20200230140A1
公开(公告)日：2020-07-23
申请号：US16076400
申请日：2017-02-13
申请人： Merck Sharp & Dohme Corp. , The Walter and Eliza Hall Institute of Medical Research
发明人： Tanweer A. Khan , Jared N. Cumming , David B. Olsen , Justin A. Boddey , Alan F. Cowman , Brad E. Sleebs
IPC分类号： A61K31/513 , A61K31/527 , A61P33/06
摘要： The present invention provides methods of treating malaria comprising administration of an N3-substituted iminopyrimidinone of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables R1, R2, R3, R4, R5, A, B, L, m, and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

2. 发明申请

US20210379020A1 COMPOUNDS FOR THE TREATMENT OF MALARIA 有权
公开(公告)号：US20210379020A1
公开(公告)日：2021-12-09
申请号：US17399589
申请日：2021-08-11
申请人： Merck Sharp & Dohme Corp. , The Walter and Eliza Hall Institute of Medical Research
发明人： Tanweer A. Khan , Jared N. Cumming , David B. Olsen , Justin A. Boddey , Alan F. Cowman , Brad E. Sleebs
IPC分类号： A61K31/4168 , A61K31/4439 , A61K31/4178 , A61K31/422 , A61K31/4245 , A61K31/454 , A61K31/496 , A61K31/4985 , A61K31/495 , A61K31/5395 , B32B27/00 , B32B27/18 , B41J2/005 , B41M5/025 , B44C1/17 , A61P33/06 , A61K31/5377 , A61K45/06
摘要： The present invention provides methods of treating malaria by administration of a compound of Formula (I): or a pharmaceutically acceptable salt of said compound, to a subject in need thereof, wherein the variables X, R1, R3, R4, R5, A, B, L, m and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

3. 发明申请

US20200223220A1 COMPOUNDS FOR THE TREATMENT OF MALARIA 审中-公开
公开(公告)号：US20200223220A1
公开(公告)日：2020-07-16
申请号：US16827776
申请日：2020-03-24
申请人： Merck Sharp & Dohme Corp. , The Walter and Eliza Hall Institute of Medical Research
发明人： Tanweer A. Khan , Jared N. Cumming , David B. Olsen , Justin A. Boddey , Alan F. Cowman , Brad E. Sleebs
IPC分类号： B41J2/005 , B32B27/18 , B32B27/00 , B44C1/17 , B41M5/025
摘要： The present invention provides methods of treating malaria by administration of a compound of Formula (I): or a pharmaceutically acceptable salt of said compound, to a subject in need thereof, wherein the variables X, R1, R3, R4, R5, A, B, L, m and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

4. 发明申请

US20190046507A1 COMPOUNDS FOR THE TREATMENT OF MALARIA 审中-公开
公开(公告)号：US20190046507A1
公开(公告)日：2019-02-14
申请号：US16076462
申请日：2017-02-13
申请人： Merck Sharp & Dohme Corp. , The Walter and Eliza Hall Institute of Medical Research
发明人： Tanweer A. Khan , Jared N. Cumming , David B. Olsen , Justin A. Boddey , Alan F. Cowman , Brad E. Sleebs
IPC分类号： A61K31/4168 , A61K31/496 , A61K31/4985 , A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/4178 , A61K31/422 , A61K31/5377 , A61K45/06 , A61P33/06
摘要： The present invention provides methods of treating malaria by administration of a compound of Formula (I): or a pharmaceutically acceptable salt of said compound, to a subject in need thereof, wherein the variables X, R1, R3, R4, R5, A, B, L, m and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

5. 发明授权

US11766435B2 N3-substituted iminopyrimidinones as antimalarial agents 有权
公开(公告)号：US11766435B2
公开(公告)日：2023-09-26
申请号：US16076400
申请日：2017-02-13
申请人： Merck Sharp & Dohme LLC , The Walter and Eliza Hall Institute of Medical Research
发明人： Tanweer A. Khan , Jared N. Cumming , David B. Olsen , Justin A. Boddey , Alan F. Cowman , Brad E. Sleebs
IPC分类号： A61K31/4709 , A61K9/06 , A61K47/10 , A61K47/12 , A61P17/10 , A61P17/00 , A61P17/04 , A61P31/04 , A61K31/513 , A61P33/06 , A61K31/527 , A61K9/00 , A61K45/06
CPC分类号： A61K31/513 , A61K31/527 , A61P33/06 , A61K9/0019 , A61K9/0053 , A61K45/06
摘要： The present invention provides methods of treating malaria comprising administration of an N3-substituted iminopyrimidinone of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables R1, R2, R3, R4, R5, A, B, L, m, and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

6. 发明申请

US20160016921A1 S-IMINO-S-OXO-IMINOTHIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译： S-IMINO-S-OXO-IMINOTHIAZINE化合物作为BACE抑制剂，组合物及其使用
公开(公告)号：US20160016921A1
公开(公告)日：2016-01-21
申请号：US14774199
申请日：2014-03-11
申请人： Tanweer A. KHAN , Jack D. SCOTT , Jared N. CUMMING , MERCK SHARP & DOHME CORP.
发明人： Tanweer A. Khan , Jack D. Scott , Jared N. Cumming
IPC分类号： C07D279/12 , C07D417/12
CPC分类号： C07D279/12 , C07D417/12
摘要： In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful 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S-亚氨基-S-氧亚氨基噻嗪化合物，包括式（I）化合物：或其互变异构体和/或立体异构体，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RN，R1A，R1B，R2，R3，R4，环A，RA，m，L1-和RL如本文所定义。本发明的新化合物可用作BACE抑制剂，并且可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。

7. 发明申请

US20150175609A1 TREATING DIABETES WITH DIPEPTIDYL PEPTIDASE-IV INHIBITORS 有权
公开(公告)号：US20150175609A1
公开(公告)日：2015-06-25
申请号：US14415759
申请日：2013-07-18
申请人： Merck Sharp & Dohme Corp.
发明人： Tesfaye Biftu , Tanweer A. Khan
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , C07D231/00
摘要： The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase IV enzyme is involved.

8. 发明授权

US09428476B2 S-imino-S-oxo-iminothiadiazine compounds as BACE inhibitors, compositions, and their use 有权
标题翻译： S-亚氨基-S-氧代 - 亚氨基二嗪化合物作为BACE抑制剂，组合物及其用途
公开(公告)号：US09428476B2
公开(公告)日：2016-08-30
申请号：US14774200
申请日：2014-03-11
申请人： Merck Sharp & Dohme Corp.
发明人： Tanweer A. Khan , Jack D. Scott , Jared N. Cumming
IPC分类号： C07D285/18 , C07D417/12 , C07D419/12
CPC分类号： C07D285/18 , C07D417/12 , C07D419/12
摘要： In its many embodiments, the present invention provides provides certain S-imino-S-oxo iminothiadiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1, R2, R3, R4, ring A, RA, m, L1, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful 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S-亚氨基-S-氧亚氨基噻二嗪化合物，包括式（I）化合物：或其互变异构体和/或立体异构体，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RN，R1，R2，R3，R4，环A，RA，m，L1和RL如本文所定义。本发明的新化合物可用作BACE抑制剂，并且可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。

9. 发明授权

US09422255B2 S-imino-S-oxo-iminothiazine compounds as BACE inhibitors, compositions, and their use 有权
标题翻译： S-亚氨基-S-氧代 - 亚氨基噻嗪化合物作为BACE抑制剂，组合物及其用途
公开(公告)号：US09422255B2
公开(公告)日：2016-08-23
申请号：US14774199
申请日：2014-03-11
申请人： Merck Sharp & Dohme Corp.
发明人： Tanweer A. Khan , Jack D. Scott , Jared N. Cumming
IPC分类号： C07D279/12 , C07D417/12
CPC分类号： C07D279/12 , C07D417/12
摘要： In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful 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S-亚氨基-S-氧亚氨基噻嗪化合物，包括式（I）化合物：或其互变异构体和/或立体异构体，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RN，R1A，R1B，R2，R3，R4，环A，RA，m，L1-和RL如本文所定义。本发明的新化合物可用作BACE抑制剂，并且可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。

10. 发明申请

US20160016923A1 S-IMINO-S-OXO-IMINOTHIADIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译： S-IMINO-S-OXO-IMINOTHIADIAZINE化合物作为BACE抑制剂，组合物及其使用
公开(公告)号：US20160016923A1
公开(公告)日：2016-01-21
申请号：US14774200
申请日：2014-03-11
申请人： Tanweer A. KHAN , Jack D. SCOTT , Jared N. CUMMING , MERCK SHARP & DOHME CORP.
发明人： Tanweer A. Khan , Jack D. Scott , Jared N. Cumming
IPC分类号： C07D285/18 , C07D417/12
CPC分类号： C07D285/18 , C07D417/12 , C07D419/12
摘要： In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiadiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1, R2, R3, R4, ring A, RA, m, L1, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful 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S-亚氨基-3-氧亚氨基二嗪化合物，包括式（I）化合物或其互变异构体和/或立体异构体，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RN，R1，R2，R3，R4，环A，RA，m，L1和RL如本文所定义。本发明的新化合物可用作BACE抑制剂，并且可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。

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