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公开(公告)号：US11981636B2
公开(公告)日：2024-05-14
申请号：US17537110
申请日：2021-11-29
IPC分类号： C07D405/04 , C07D205/04 , C07D207/08 , C07D207/16 , C07D211/22 , C07D211/46 , C07D211/48 , C07D241/04 , C07D241/08 , C07D265/30 , C07D401/04 , C07D403/06 , C07D403/14 , C07D405/12 , C07D413/14 , C07D491/107
CPC分类号： C07D205/04 , C07D207/08 , C07D207/16 , C07D211/22 , C07D211/46 , C07D211/48 , C07D241/04 , C07D241/08 , C07D265/30 , C07D401/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/14 , C07D491/107
摘要： The present disclosure relates to novel compounds of Formula I
wherein each of Ra, Rb, Rd and Re is independently H; Rc is selected from the group consisting of H, hydroxyl, halo, alkyl, alkoxy, CF3, SO2CH3, and morpholino, R1 is selected from the group consisting of hydrogen, alkyl, phenyl, or —CH═C(CH3)2; and R2 is specific substituted cyclic amino groups. The invention also discloses pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurogenerative diseases, including Alzheimer's disease and cognitive decline.-
公开(公告)号：US20240018113A1
公开(公告)日：2024-01-18
申请号：US18372771
申请日：2023-09-26
发明人： Junko Maeda , Ikumi Kuriwaki , Kai Kitamura , Yumi Yamashita , Kenichi Kakefuda , Akio Kamikawa , Kenji Negoro , Wataru Hamaguchi , Ryushi Seo , Jeffrey Ciavarri
IPC分类号： C07D295/16 , C07D213/56 , C07D231/12 , C07D205/04 , C07D307/22 , C07D207/273 , C07D305/08 , C07D333/48 , C07D405/10 , C07D207/16 , C07D211/48 , C07C237/42 , C07C311/46 , C07C311/13 , C07D207/12 , C07D211/62 , C07C233/22 , C07D295/195 , C07C233/69 , C07C235/42 , C07D309/14 , C07D213/75 , C07D231/40 , C07D403/06 , C07C233/81 , C07D209/08 , C07D295/155 , C07D487/10 , C07D403/10 , C07D401/06 , C07D279/12 , C07D239/26
CPC分类号： C07D295/16 , C07D213/56 , C07D231/12 , C07D205/04 , C07D307/22 , C07D207/273 , C07D305/08 , C07D333/48 , C07D405/10 , C07D207/16 , C07D211/48 , C07C237/42 , C07C311/46 , C07C311/13 , C07D207/12 , C07D211/62 , C07C233/22 , C07D295/195 , C07C233/69 , C07C235/42 , C07D309/14 , C07D213/75 , C07D231/40 , C07D403/06 , C07C233/81 , C07D209/08 , C07D295/155 , C07D487/10 , C07D403/10 , C07D401/06 , C07D279/12 , C07D239/26
摘要： [Problem] A compound which is useful as a STING inhibitor is provided.
[Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.-
公开(公告)号：US20180194718A1
公开(公告)日：2018-07-12
申请号：US15806722
申请日：2017-11-08
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： C07C243/38 , C07D493/10 , C07D491/107 , A61K31/192 , C07D405/06 , C07D401/04 , C07D309/08 , C07D307/68 , C07D295/32 , C07D265/30 , C07D261/04 , C07D261/02 , C07D239/36 , C07D233/06 , C07D213/87 , C07D213/86 , C07D213/75 , C07D213/65 , C07D213/61 , C07D213/56 , C07D211/62 , C07D211/60 , C07D211/48 , C07D211/46 , C07D211/42 , C07D211/38 , C07D211/22 , C07D207/16 , C07D207/14 , C07D207/12 , C07D207/09 , C07D207/08 , C07D205/04 , C07C259/04 , C07C243/32 , C07C243/24 , C07C235/80 , C07C235/78 , C07C235/74 , C07C235/34 , C07C235/20 , C07C235/12 , C07C233/56 , A61K45/06 , A61K31/5375 , A61K31/495 , A61K31/4409 , A61K31/4406 , A61K31/44 , A61K31/42 , A61K31/4015 , A61K31/40 , A61K31/397 , A61K31/341 , A61K31/197
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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公开(公告)号：US20180155283A1
公开(公告)日：2018-06-07
申请号：US15537741
申请日：2015-12-18
发明人： Edward Holson , Florence Fevrier Wagner , Michel Weiwer , Edward Scolnick , Michelle Palmer , Luka Dordevic , Michael C. Lewis , Jennifer Q. Pan , Yan-Ling Zhang , Qihong Xu
IPC分类号： C07D207/12 , C07D211/18 , C07D211/38 , C07D211/42 , C07D211/48 , C07D211/58 , C07D211/62 , C07D211/70 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/10 , C07D491/048 , C07D491/052 , C07D491/056 , C07D491/107 , A61P25/16 , A61P25/18
CPC分类号： C07D207/12 , A61P25/16 , A61P25/18 , C07D211/18 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/48 , C07D211/58 , C07D211/62 , C07D211/70 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/10 , C07D491/048 , C07D491/052 , C07D491/056 , C07D491/107 , C07K14/70571
摘要： The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopammode inergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0-arrestin pathway and/or on the cAMP pathway.
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公开(公告)号：US09957229B2
公开(公告)日：2018-05-01
申请号：US15602693
申请日：2017-05-23
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Colin Zhang , Brian W. Metcalf , Chunhong He , Ding-Quan Qian
IPC分类号： C07D471/10 , C07D207/06 , A61K31/407 , C07D491/107 , C07D513/10 , C07D498/20 , C07D495/04 , C07D493/10 , C07D491/20 , C07D491/10 , C07D487/10 , C07D487/08 , C07D487/04 , C07D471/04 , C07D417/04 , C07D413/14 , C07D413/10 , C07D405/14 , C07D405/04 , C07D403/04 , C07D401/14 , C07D401/10 , C07D401/06 , C07D401/04 , C07D333/34 , C07D295/185 , C07D221/20 , C07D217/26 , C07D217/06 , C07D213/38 , C07D211/70 , C07D211/66 , C07D211/64 , C07D211/58 , C07D211/52 , C07D211/48 , C07D211/46 , C07D211/34 , C07D211/22 , C07D211/18 , C07D211/16 , C07D209/70 , C07D209/62 , C07D209/52 , C07D209/44 , C07D209/42 , C07D209/08 , C07D207/27 , C07D207/16 , C07D207/14 , C07D207/12 , C07D207/10 , C07D207/08 , A61K31/4439
CPC分类号： C07D207/06 , A61K31/407 , A61K31/4439 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/62 , C07D209/70 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/66 , C07D211/70 , C07D213/38 , C07D217/06 , C07D217/26 , C07D221/20 , C07D295/185 , C07D333/34 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/10 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D493/10 , C07D495/04 , C07D498/20 , C07D513/10
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
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公开(公告)号：US20180036436A1
公开(公告)日：2018-02-08
申请号：US15551612
申请日：2016-02-25
发明人： Zsolt BARANYAI , Zoltán GARDA , Simona GHIANI , Ferenc Krisztián KÁLMÁN , László KRUSPER , Alessandro MAIOCCHI , Gyula TIRCSÓ , Imre TOTH
IPC分类号： A61K49/10 , C07D295/185 , C07D211/42 , C07D211/46 , C07D211/48 , C07D207/34 , C07D211/62 , C07D211/16 , C07D295/192 , C07D491/107 , C07D221/22 , C07D471/08 , G01N33/58 , G01N24/08 , A61B5/055 , C07D207/325
CPC分类号： A61K49/106 , A61B5/055 , A61B2503/40 , A61K49/103 , C07C237/06 , C07D207/325 , C07D207/34 , C07D211/16 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/62 , C07D221/22 , C07D295/185 , C07D295/192 , C07D401/12 , C07D403/12 , C07D471/08 , C07D491/107 , G01N24/08 , G01N33/58
摘要： The present invention relates to novel substituted ethylenediaminetetraacetic acid bisamide derivatives, their complexes with Mn(II) ion and the use thereof as contrast agents for Magnetic Resonance Imaging (MRI) analysis.
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公开(公告)号：US09872852B2
公开(公告)日：2018-01-23
申请号：US14915782
申请日：2014-09-02
发明人： Louis S. Chupak , Xiaofan Zheng
IPC分类号： A61K31/381 , A61K31/396 , A61K31/40 , A61K31/4427 , A61K31/496 , C07C217/58 , C07C229/22 , C07C233/36 , C07C235/76 , C07C311/05 , C07D205/04 , C07D207/14 , C07D211/32 , C07D213/57 , C07D213/69 , C07D217/02 , C07D233/06 , C07D249/08 , C07D265/30 , A61K31/397 , A61K31/5375 , A61K31/44 , A61K31/4523 , A61K31/445 , A61K31/551 , A61K31/55 , C07D309/14 , C07D311/14 , C07D317/50 , C07D223/06 , C07D319/18 , C07D333/20 , C07D333/32 , C07D333/36 , C07D233/61 , C07D401/06 , C07D401/12 , C07D405/12 , C07D487/10 , C07D205/08 , C07D207/08 , C07D207/16 , C07D207/27 , C07C279/12 , C07D211/34 , C07D211/44 , C07D295/12 , C07D211/48 , C07D211/56 , C07D211/60 , C07D211/62 , C07D295/14 , C07D295/18 , C07D295/185 , C07D211/76 , C07D211/78 , C07D213/63 , C07D213/64 , C07D213/65 , C07C255/54 , C07C271/20 , C07C279/14 , C07C229/14 , C07C233/38 , C07C233/47 , C07C233/78 , C07C237/06 , C07K5/083 , C07C275/40 , C07D217/04 , C07D295/13 , C07D295/16 , C07D311/08
CPC分类号： A61K31/381 , A61K31/396 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/496 , A61K31/5375 , A61K31/55 , A61K31/551 , C07C217/58 , C07C229/14 , C07C229/22 , C07C233/36 , C07C233/38 , C07C233/47 , C07C233/78 , C07C235/76 , C07C237/06 , C07C255/54 , C07C271/20 , C07C275/40 , C07C279/12 , C07C279/14 , C07C311/05 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D205/04 , C07D205/08 , C07D207/08 , C07D207/14 , C07D207/16 , C07D207/27 , C07D211/32 , C07D211/34 , C07D211/44 , C07D211/48 , C07D211/56 , C07D211/60 , C07D211/62 , C07D211/76 , C07D211/78 , C07D213/57 , C07D213/63 , C07D213/64 , C07D213/65 , C07D213/69 , C07D217/02 , C07D217/04 , C07D223/06 , C07D233/61 , C07D249/08 , C07D265/30 , C07D279/12 , C07D295/12 , C07D295/13 , C07D295/14 , C07D295/16 , C07D295/18 , C07D295/185 , C07D309/14 , C07D311/08 , C07D311/14 , C07D317/50 , C07D319/18 , C07D333/20 , C07D333/32 , C07D333/36 , C07D401/06 , C07D401/12 , C07D405/12 , C07D487/10 , C07K5/0806 , C07K5/0808
摘要： Disclosed are compounds of Formula (I): (I). Also disclosed are methods of using such compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of virological diseases or disorders and cancer.
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公开(公告)号：US09708253B2
公开(公告)日：2017-07-18
申请号：US15109733
申请日：2015-01-05
发明人： Jingwu Duan , T. G. Murali Dhar , Bin Jiang , Ananta Karmakar , Arun Kumar Gupta , Zhonghui Lu , Carolyn A. Weigelt
IPC分类号： C07C317/20 , C07C317/24 , C07C317/30 , C07D205/04 , C07D207/27 , C07D211/46 , C07D211/78 , C07D213/30 , C07D231/12 , C07D213/81 , C07D213/82 , C07D309/08 , C07D231/14 , C07D231/56 , C07D401/04 , C07D403/04 , C07D237/08 , C07D237/20 , C07D237/24 , C07D405/04 , C07D239/28 , C07C317/46 , C07D241/24 , C07D249/04 , C07D471/04 , C07D207/277 , C07D277/60 , C07D295/096 , C07D211/48 , C07D211/62 , C07D295/185 , C07D213/56 , C07D213/71 , C07D213/75 , C07D309/04 , C07D335/02 , C07D401/06 , C07D401/12 , C07D295/205 , C07D213/40 , C07D231/54 , C07D237/22 , C07D249/06 , C07D277/82 , C07D295/16 , C07D295/195
CPC分类号： C07C317/20 , C07C317/24 , C07C317/30 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07D205/04 , C07D207/27 , C07D207/277 , C07D211/46 , C07D211/48 , C07D211/62 , C07D211/78 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/71 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/14 , C07D231/54 , C07D231/56 , C07D237/08 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/28 , C07D241/24 , C07D249/04 , C07D249/06 , C07D277/60 , C07D277/82 , C07D295/096 , C07D295/16 , C07D295/185 , C07D295/195 , C07D295/205 , C07D309/04 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D405/04 , C07D471/04
摘要： Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
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公开(公告)号：US20170015619A1
公开(公告)日：2017-01-19
申请号：US15219478
申请日：2016-07-26
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： C07C243/38 , A61K31/44 , C07D213/86 , A61K45/06 , A61K31/4406 , C07D307/68 , A61K31/341 , A61K31/192 , C07D213/87 , A61K31/4409
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
摘要翻译： 其中R1-R5和X如说明书中所定义，或其药学上可接受的盐。 这些化合物具有去血清抑制活性。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US09527830B2
公开(公告)日：2016-12-27
申请号：US14344681
申请日：2012-09-10
申请人： Shawn Walsh , Alexander Pasternak , Brian Cato , Paul E. Finke , Jessica Frie , Qinghong Fu , Dooseop Kim , Barbara Pio , Aurash Shahripour , Zhi-Cai Shi , Haifeng Tang
发明人： Shawn Walsh , Alexander Pasternak , Brian Cato , Paul E. Finke , Jessica Frie , Qinghong Fu , Dooseop Kim , Barbara Pio , Aurash Shahripour , Zhi-Cai Shi , Haifeng Tang
IPC分类号： C07D403/14 , C07D401/10 , C07D405/14 , C07D413/14 , C07D403/10 , C07D405/06 , C07D405/12 , C07D487/04 , C07D211/28 , C07D211/62 , C07D211/48 , C07D471/08
CPC分类号： C07D401/10 , C07D211/28 , C07D211/48 , C07D211/62 , C07D403/10 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/14 , C07D471/08 , C07D487/04
摘要： This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
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