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公开(公告)号:US20230406844A1
公开(公告)日:2023-12-21
申请号:US18248407
申请日:2021-10-27
申请人: Peter H. FULLER , Anmol GULATI , Solomon D. KATTAR , Mitchell H. KEYLOR , Kaila A. MARGREY , Xin YAN , MERCK SHARP & DOHME CORP.
发明人: Peter H. Fuller , Anmol Gulati , Solomon D. Kattar , Mitchell H. Keylor , Kaila A. Margrey , Xin Yan
IPC分类号: C07D405/12 , C07D405/14 , C07D413/04 , C07D401/04 , C07D471/04 , C07D401/14 , C07D471/08 , C07D217/22 , C07D409/14
CPC分类号: C07D405/12 , C07D405/14 , C07D413/04 , C07D401/04 , C07D471/04 , C07D401/14 , C07D471/08 , C07D217/22 , C07D409/14
摘要: The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. 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 LRRK-2 kinase is involved.
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公开(公告)号:US11845715B2
公开(公告)日:2023-12-19
申请号:US17405989
申请日:2021-08-18
申请人: THE UNIVERSITY OF QUEENSLAND , THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN
发明人: Luke O'Neill , Rebecca Coll , Matthew Cooper , Avril Robertson , Kate Schroder
IPC分类号: C07C311/56 , A61P17/00 , C07D403/12 , C07D249/12 , C07D249/04 , C07D241/42 , A61P25/00 , A61P37/00 , C07D495/04 , C07D241/44 , C07D277/36 , C07D307/68 , C07D487/04 , C07D215/36 , C07D249/06 , C07D311/16 , C07D401/06 , C07D401/12 , A61P3/00 , C07C311/60 , C07D213/71 , C07D217/22 , C07D221/18 , C07D317/62 , C07D333/34 , A61P1/00 , A61P35/00 , C07D217/02 , C07D241/24 , C07D271/12 , C07D413/12 , C07D417/12 , A61P5/00 , C07D307/18 , C07D307/64 , C07D311/60 , C07D333/52 , C07D333/62 , C07D405/12 , C07D495/06 , C07D217/24 , C07D235/02 , C07D311/18 , C07D407/12 , C07D231/18 , C07D307/82 , C07D309/08 , C07D493/04 , C07D207/38 , C07D261/18 , C07D498/04
CPC分类号: C07C311/56 , A61P1/00 , A61P3/00 , A61P5/00 , A61P17/00 , A61P25/00 , A61P35/00 , A61P37/00 , C07C311/60 , C07D207/38 , C07D213/71 , C07D215/36 , C07D217/02 , C07D217/22 , C07D217/24 , C07D221/18 , C07D231/18 , C07D235/02 , C07D241/24 , C07D241/42 , C07D241/44 , C07D249/04 , C07D249/06 , C07D249/12 , C07D261/18 , C07D271/12 , C07D277/36 , C07D307/18 , C07D307/64 , C07D307/68 , C07D307/82 , C07D309/08 , C07D311/16 , C07D311/18 , C07D311/60 , C07D317/62 , C07D333/34 , C07D333/52 , C07D333/62 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D493/04 , C07D495/04 , C07D495/06 , C07D498/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07C2603/10
摘要: The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.
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公开(公告)号:US20230339960A1
公开(公告)日:2023-10-26
申请号:US18342977
申请日:2023-06-28
申请人: Pfizer Inc.
发明人: JOHN DAVID TRZUPEK , KATHERINE LIN LEE , MARK EDWARD BUNNAGE , SEUNGIL HAN , DAVID HEPWORTH , FRANK ELDRIDGE LOVERING , JOHN PAUL MATHIAS , NIKOLAOS PAPAIOANNOU , BETSY SUSAN PIERCE , JOSEPH WALTER STROHBACH , STEPHEN WAYNE WRIGHT , CHRISTOPH WOLFGANG ZAPF , LORI KRIM GAVRIN , ARTHUR LEE , DAVID RANDOLPH ANDERSON , KEVIN JOSEPH CURRAN , CHRISTOPH MARTIN DEHNHARDT , EDDINE SAIAH , JOEL ADAM GOLDBERG , XIAOLUN WANG , HORNG-CHIH HUANG , RICHARD VARGAS , MICHAEL DENNIS LOWE , AKSHAY PATNY
IPC分类号: C07D491/056 , C07F7/18 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C69/94 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/273 , C07D209/52 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , A61K31/40
CPC分类号: C07D491/056 , C07F7/1804 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C69/94 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/273 , C07D209/52 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , A61K31/40
摘要: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,
as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.-
公开(公告)号:US20180127432A1
公开(公告)日:2018-05-10
申请号:US15862691
申请日:2018-01-05
申请人: Pfizer Inc.
发明人: John David Trzupek , Katherine Lin Lee , Mark Edward Bunnage , Seungil Han , David Hepworth , Frank Eldridge Lovering , John Paul Mathias , Nikolaos Papaioannou , Betsy Susan Pierce , Joseph Walter Strohbach , Stephen Wayne Wright , Christoph Wolfgang Zapf , Lori Krim Gavrin , Arthur Lee , David Randolph Anderson , Kevin Joseph Curran , Christoph Martin Dehnhardt , Eddine Saiah , Joel Adam Goldberg , Xiaolun Wang , Horng-Chih Huang , Richard Vargas , Michael Dennis Lowe , Akshay Patny
IPC分类号: C07D491/056 , C07D239/88 , C07D239/86 , C07D263/24 , C07D207/267 , A61K31/40 , C07D207/08 , C07F7/18 , C07D209/52 , C07D498/04 , C07D207/273 , C07C69/94 , C07D217/24 , C07D217/22 , C07D217/02 , C07D405/14 , C07D401/14 , C07D487/04 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D407/14 , C07D215/48 , C07D207/26 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/4015
CPC分类号: C07D491/056 , A61K31/40 , A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07C69/94 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/273 , C07D209/52 , C07D215/48 , C07D217/02 , C07D217/22 , C07D217/24 , C07D239/86 , C07D239/88 , C07D263/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07F7/1804
摘要: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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公开(公告)号:US09919998B2
公开(公告)日:2018-03-20
申请号:US15116787
申请日:2015-02-06
发明人: Richard H. Ebright , Yon W. Ebright , Soma Mandal , Richard Wilde , Shengjian Li
IPC分类号: C07C233/88 , A61K31/167 , A61K31/341 , A61K31/4402 , A61K31/4409 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/38 , C07D215/40 , C07D217/22 , C07D317/66 , C07D319/18 , C07D231/56 , C07D333/38 , C07D333/66 , C07D235/06 , C07D401/12 , C07D237/30 , C07D405/12 , C07D409/12 , C07D241/04 , C07D249/06 , C07D249/08 , C07D249/18 , C07D471/04 , C07D257/04 , C07D487/04 , C07D265/30 , C07D207/14 , C07D277/62 , C07D209/40 , C07D209/42 , C07D211/58 , C07D295/135 , C07D295/155 , C07D295/185 , C07D295/205 , C07D307/82 , C07C237/20 , A01N37/22 , A01N43/10 , A01N43/30 , A01N43/32 , A01N43/36 , A01N43/40 , A01N43/50 , A01N43/52 , A01N43/56 , A01N43/60 , A01N43/62 , A01N43/647 , A01N43/78 , A01N43/90 , A01N37/24 , A01N43/38 , A01N43/48 , A01N43/653 , A01N43/713 , A01N43/84 , C07D209/08 , C07D333/54
CPC分类号: C07C233/88 , A01N37/22 , A01N37/24 , A01N43/10 , A01N43/30 , A01N43/32 , A01N43/36 , A01N43/38 , A01N43/40 , A01N43/48 , A01N43/50 , A01N43/52 , A01N43/56 , A01N43/60 , A01N43/62 , A01N43/647 , A01N43/653 , A01N43/713 , A01N43/78 , A01N43/84 , A01N43/90 , A61K31/167 , A61K31/341 , A61K31/4402 , A61K31/4409 , C07C237/20 , C07C2602/08 , C07C2602/10 , C07D207/14 , C07D209/08 , C07D209/40 , C07D209/42 , C07D211/58 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/38 , C07D215/40 , C07D217/22 , C07D231/56 , C07D235/06 , C07D237/30 , C07D241/04 , C07D249/06 , C07D249/08 , C07D249/18 , C07D257/04 , C07D265/30 , C07D277/62 , C07D295/135 , C07D295/155 , C07D295/185 , C07D295/205 , C07D307/82 , C07D317/66 , C07D319/18 , C07D333/38 , C07D333/54 , C07D333/66 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要: The invention provides compounds having activity as bacterial RNA polymerase inhibitors and antibacterial agents, as well as compositions comprising the compounds and methods for their use. Specifically, phenylalanineamide and tyrosinamide compounds are disclosed that have inhibitory activity toward mycobacterium tuberculosis RNA polymerase. Use of these compounds in the treatment or prevention of M. tuberculosis infections in a mammal, is disclosed.
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公开(公告)号:US09868707B2
公开(公告)日:2018-01-16
申请号:US14652705
申请日:2013-12-19
发明人: Anthony Pinkerton , Patrick Maloney , Paul Hershberger , Satyamaheshwar Peddibhotla , Michael Hedrick , Lawrence Barak , Marc Caron
IPC分类号: C07D239/94 , A61K31/517 , A61K31/519 , A61K31/506 , C07D403/04 , A61K45/06 , A61K31/5377 , A61K9/00 , A61K47/26 , A61K47/38 , A61K9/48 , C07D403/12 , C07D401/14 , C07D215/42 , C07D217/22 , C07D401/04 , C07D401/12 , C07D405/04 , C07D471/04
CPC分类号: C07D239/94 , A61K9/0019 , A61K9/4866 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K45/06 , A61K47/26 , A61K47/38 , C07D215/42 , C07D217/22 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D471/04 , A61K2300/00
摘要: Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
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公开(公告)号:US09849122B2
公开(公告)日:2017-12-26
申请号:US15142461
申请日:2016-04-29
IPC分类号: C07D217/22 , A61K31/472 , A61K31/4725 , C07D409/12 , A61K31/557 , A61K31/5575 , A61K31/559 , A61K9/00 , A61K9/08 , A61K47/48
CPC分类号: A61K31/472 , A61K9/0048 , A61K9/08 , A61K31/4725 , A61K31/557 , A61K31/5575 , A61K31/559 , A61K47/54 , A61K47/55 , C07D217/22 , C07D409/12 , A61K2300/00
摘要: Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt.
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公开(公告)号:US09840468B1
公开(公告)日:2017-12-12
申请号:US15395068
申请日:2016-12-30
IPC分类号: C07D217/02 , C07D217/22
CPC分类号: C07D217/02 , C07C201/12 , C07D217/22 , C07C205/57
摘要: Described are methods for the preparation of 6-aminoisoquinoline, a useful intermediate compound in the synthesis of kinase inhibitors.
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公开(公告)号:US20170240558A1
公开(公告)日:2017-08-24
申请号:US15589485
申请日:2017-05-08
IPC分类号: C07D491/153
CPC分类号: C07D491/153 , C07D217/22 , C07D221/18 , C07D317/68 , C07D491/056
摘要: Sanguinarine analogs as PP2C inhibitors are disclosed for the treatment of various cancers, as well as methods of synthesizing such analogs.
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公开(公告)号:US20170174620A1
公开(公告)日:2017-06-22
申请号:US15327485
申请日:2015-07-22
发明人: Herman O. SINTIM , Shizuka NAKAYAMA , Dimpy KALIA , Jie ZHOU , Min GUO , Jinbing LIU , Changhao WANG , Rena LAPIDUS
IPC分类号: C07C257/18 , C07D217/22 , C07D471/04 , C07D413/12 , C07D401/04 , C07C245/24 , C07D401/12
CPC分类号: A61K31/472 , A61K31/4725 , C07C245/24 , C07C257/18 , C07C279/18 , C07D217/22 , C07D401/04 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要: Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.
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