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公开(公告)号:US20180251443A9
公开(公告)日:2018-09-06
申请号:US15537283
申请日:2015-12-16
发明人: Gary A. PIAZZA , Xi CHEN , Adam B. KEETON , Michael R. BOYD
IPC分类号: C07D317/64 , C07D307/54 , C07C235/32 , C07D207/14 , C07D213/75 , C07D211/56 , A61K31/341 , A61K31/36 , A61K31/401 , A61K31/40 , A61K31/44 , A61K31/445 , C07D307/52 , C07D307/38 , C07D213/24 , C07C233/58 , C07D405/12 , C07D235/30 , C07C237/20 , C07D207/337
CPC分类号: C07D317/64 , A61K31/165 , A61K31/167 , A61K31/216 , A61K31/341 , A61K31/36 , A61K31/40 , A61K31/401 , A61K31/421 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/445 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K45/06 , A61K2300/00 , C07C233/58 , C07C235/32 , C07C235/34 , C07C237/20 , C07C311/29 , C07C2601/02 , C07C2602/08 , C07D207/14 , C07D207/335 , C07D207/337 , C07D211/56 , C07D213/24 , C07D213/40 , C07D213/75 , C07D235/30 , C07D307/38 , C07D307/52 , C07D307/54 , C07D405/12 , G01N33/5748 , A61K2800/00
摘要: Disclosed are compounds, for example, a compound of formula I, wherein R, R0, R1-R8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.
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公开(公告)号:US20180221514A1
公开(公告)日:2018-08-09
申请号:US15748556
申请日:2016-08-17
IPC分类号: A61K49/20 , A61K31/015 , A61K31/05 , A61K31/353 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/53
CPC分类号: A61K49/20 , A61K31/015 , A61K31/05 , A61K31/353 , A61K31/4015 , A61K31/4178 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/53 , C07D207/14 , C07D207/20 , C07D207/273 , C07D491/052
摘要: The present invention provides methods of using nitroxide spin-labeled amyloid beta-binding compounds to image amyloid. The present invention also provides nitroxide spin-labeled amyloid beta-binding compounds
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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:US09994537B2
公开(公告)日:2018-06-12
申请号:US15672165
申请日:2017-08-08
IPC分类号: C07D295/205 , C07D207/08 , C07D471/10 , C07D417/04 , C07D403/04 , C07D401/04 , C07D295/26 , C07D265/30 , C07D207/12 , C07D211/38 , C07D211/58 , C07D207/14 , C07D211/14 , C07D498/08 , C07D211/62 , C07D487/04 , C07D207/16
CPC分类号: C07D295/205 , C07D207/08 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/14 , C07D211/38 , C07D211/58 , C07D211/62 , C07D265/30 , C07D295/26 , C07D401/04 , C07D403/04 , C07D417/04 , C07D471/10 , C07D487/04 , C07D498/08
摘要: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
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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:US20180105491A1
公开(公告)日:2018-04-19
申请号:US15784560
申请日:2017-10-16
IPC分类号: C07D207/14 , C07D401/08 , C07D403/04 , C07D471/10 , C07D243/08 , C07D409/08 , C07D487/10 , C07D471/04 , C07D487/04 , C07D413/12 , C07D271/06 , C07D413/04 , C07D413/14
CPC分类号: C07D207/14 , C07D209/96 , C07D213/57 , C07D243/08 , C07D271/06 , C07D295/205 , C07D401/08 , C07D403/04 , C07D409/08 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
摘要: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
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公开(公告)号:US20180099931A1
公开(公告)日:2018-04-12
申请号:US15726075
申请日:2017-10-05
申请人: AbbVie S.à.r.l. , Galapagos NV
发明人: Robert J. Altenbach , Andrew Bogdan , Sylvain Couty , Elsa De Lemos , Nicolas Desroy , Béranger Duthion , Gregory A. Gfesser , Stephen N. Greszler , Christopher Gaëtan Housseman , John R. Koenig , Philip R. Kym , Bo Liu , Marc J. Scanio , Xenia Searle , Xueqing Wang , Ming C. Yeung , Gang Zhao
IPC分类号: C07D207/14 , C07D207/48
CPC分类号: C07D207/14 , A61P11/00 , C07D207/48 , C07D401/04 , C07D401/14 , C07D405/06
摘要: The invention discloses compounds of Formula (I) wherein R1, R2, R2A, R3, R3A, R4, R4A, and R5 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
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公开(公告)号:US20180057455A1
公开(公告)日:2018-03-01
申请号:US15689115
申请日:2017-08-29
发明人: KAP-SUN YEUNG , Katharine A. Grant-Young , Juliang Zhu , Mark G. Saulnier , David B. Frennesson , David R. Langley , Piyasena Hewawasam , Tao Wang , Zhongxing Zhang , Zhaoxing Meng , Li-Qiang Sun , Eric Mull , Paul Michael Scola
IPC分类号: C07D207/12 , C07D211/66 , C07D207/16 , C07D403/12 , C07D401/12 , C07D207/14 , C07D211/22 , C07D213/38 , C07D401/14 , C07C237/06 , C07D295/088 , C07D205/04 , C07D213/85 , C07C217/18 , C07D213/73 , C07D405/12 , C07C255/24 , C07D413/14 , C07D405/14 , C07D213/79 , C07D231/12 , C07D239/26 , C07D277/28 , C07D211/90
CPC分类号: C07D207/12 , C07C217/18 , C07C217/28 , C07C217/58 , C07C229/14 , C07C235/08 , C07C237/04 , C07C237/06 , C07C255/24 , C07C255/25 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/66 , C07D211/90 , C07D213/38 , C07D213/42 , C07D213/55 , C07D213/73 , C07D213/79 , C07D213/85 , C07D231/12 , C07D239/26 , C07D277/28 , C07D295/088 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12
摘要: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
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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:US09815824B2
公开(公告)日:2017-11-14
申请号:US14900039
申请日:2014-06-27
申请人: Nektar Therapeutics
发明人: Neel K. Anand , Franco J. Duarte , Wen Zhang , Zhongxu Ren
IPC分类号: C07D409/12 , C07C233/05 , C07D207/09 , C07D401/12 , C07D295/125 , C07C233/40 , C07C205/04 , C07C333/00 , C07D241/04 , C07D207/12 , C07D207/14 , C07D213/56 , C07D333/48 , C07D213/61 , C07D205/04
CPC分类号: C07D409/12 , C07C233/05 , C07C233/40 , C07D205/04 , C07D207/09 , C07D207/12 , C07D207/14 , C07D213/56 , C07D213/61 , C07D241/04 , C07D295/125 , C07D333/48 , C07D401/12
摘要: Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof. The present disclosure relates to novel compounds and to their use as agonists of the kappa opioid receptor. The disclosure also relates to methods for preparation of the compounds and to pharmaceutical compositions containing such compounds. Kappa opioid agonists that exhibit full agonist properties at the kappa opioid receptor have been widely shown to be efficacious in preclinical models of pain, particularly visceral pain.
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