-
公开(公告)号:US20190248753A1
公开(公告)日:2019-08-15
申请号:US16397172
申请日:2019-04-29
发明人: Mihir B. Mandal , David B. Olsen , Jing Su , Lihu Yang , Katherine Young , Takao Suzuki , Lanying You
IPC分类号: C07D263/20 , C07D487/04 , A61K45/06 , C07D417/10 , C07D413/06 , A61K31/541 , A61K31/4439 , A61K31/5377 , A61K31/553 , C07D413/04 , C07D417/14 , A61K31/437 , A61K31/4985 , A61K31/506 , C07D413/10 , A61K31/422 , A61K31/421 , C07D413/14 , A61K31/427 , C07D471/04
CPC分类号: C07D263/20 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/553 , A61K45/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , A61K2300/00
摘要: The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
-
公开(公告)号:US20190183901A1
公开(公告)日:2019-06-20
申请号:US16326284
申请日:2017-08-29
发明人: Brian Alvin JOHNS
IPC分类号: A61K31/537 , A61K31/54 , A61K31/513 , A61K31/427 , A61P31/18
CPC分类号: A61K31/537 , A61K31/427 , A61K31/513 , A61K31/54 , A61K31/541 , A61K31/553 , A61K31/7068 , A61P31/18 , C07D295/13 , C07D498/04 , A61K2300/00
摘要: Methods for treating HIV in a human using combinations of: bictegravir and one of two different maturation inhibitors are disclosed, as well as compositions containing such compounds are provided.
-
公开(公告)号:US20190144432A1
公开(公告)日:2019-05-16
申请号:US16244876
申请日:2019-01-10
发明人: Frank Bennett , Jinlong Jiang , Alexander Pasternak , Shuzhi Dong , Xin Gu , Jack D. Scott , Haiqun Tang , Zhiqiang Zhao , Yuhua Huang , Dexi Yang , Katherine Young , Li Xiao , Zhibo Zhang , Jianmin Fu
IPC分类号: C07D403/10 , A61K31/198 , C07D403/12 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/431 , A61K31/439 , A61K31/496 , A61K31/541 , A61K31/546 , C07D405/14 , C07D453/02 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08 , A61K31/407 , A61K31/5025 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D401/14 , A61P31/04 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/498 , C07D487/04 , A61K31/506 , C07D471/04 , C07D417/14 , C07D417/10 , C07D413/10 , C07D407/14 , C07D403/14 , C07D401/10 , C07D413/14 , A61K31/41
CPC分类号: C07D403/10 , A61K31/198 , A61K31/407 , A61K31/41 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/428 , A61K31/431 , A61K31/437 , A61K31/4375 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K31/546 , A61K45/06 , A61P31/04 , C07D401/10 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/10 , C07D493/04 , C07D493/08 , C07D495/08
摘要: The present invention relates to metallo-β-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
-
公开(公告)号:US20180319748A1
公开(公告)日:2018-11-08
申请号:US16035502
申请日:2018-07-13
IPC分类号: C07D213/74 , C07F9/6512 , C07H19/048 , A61K31/44 , A61K31/506 , A61K31/675 , C07D213/80 , C07D401/12 , C07D239/47 , C07D413/12 , C07H13/08 , C07H15/26 , C07F9/6558 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61K31/4439 , A61K31/706 , A61K31/553 , A61K31/551 , A61K31/541 , C07D405/12 , C07D453/02 , A61K31/4412 , A61K31/505 , A61K31/444 , A61K45/06 , A61K31/635 , A61K31/4375 , A61K31/7052
CPC分类号: C07D213/74 , A61K31/4375 , A61K31/44 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/553 , A61K31/635 , A61K31/675 , A61K31/7052 , A61K31/706 , A61K45/06 , C07D213/80 , C07D239/47 , C07D401/12 , C07D405/12 , C07D413/12 , C07D453/02 , C07F9/58 , C07F9/59 , C07F9/65031 , C07F9/6512 , C07F9/65583 , C07H13/08 , C07H15/26 , C07H19/048 , A61K2300/00
摘要: There are provided compounds of formula IIb, wherein: LG1 represents imidazolyl, chloro, or aryloxy; and Z1 represents a structural fragment of formula V: wherein R2 to R4, R5a, L and X1 to X3 have meanings given in the description, or a salt or protected derivative thereof, wherein said protected derivative is a compound in which the carboxyl moiety of R4 is protected as a C1-8 alkyl ester. The compounds have antiinflammatory activity, for example through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
-
公开(公告)号:US20180312474A1
公开(公告)日:2018-11-01
申请号:US15952073
申请日:2018-04-12
IPC分类号: C07D249/06 , A61K31/501 , C07D237/08 , A61K31/551 , A61K31/4995 , C07D487/08 , A61K31/4162 , C07D487/04 , A61K31/41 , C07D401/04 , A61K31/435 , C07D471/10 , A61K31/5383 , C07D498/08 , A61K31/5377 , C07D413/12 , C07D491/107 , C07D239/42 , A61K31/445 , C07D211/66 , A61K31/4196 , C07D249/08 , A61K31/454 , C07D401/12 , A61K31/4192 , C07D403/12 , A61K31/541 , C07D263/32 , C07D231/12 , C07D215/54 , C07D295/26 , A61K31/397 , C07D205/04 , A61K31/54 , C07D279/12 , A61K31/495 , C07D295/192 , A61K31/506 , C07D239/26 , A61K31/496 , C07C309/30 , C07B59/00 , C07C53/18 , A61K9/00 , A61P43/00 , A61P35/02 , A61P35/00 , A61P29/00 , A61K45/06 , A61K9/48 , A61K9/16
CPC分类号: C07D249/06 , A61K9/0053 , A61K9/1623 , A61K9/4858 , A61K31/397 , A61K31/41 , A61K31/4162 , A61K31/4192 , A61K31/4196 , A61K31/435 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/4995 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/54 , A61K31/541 , A61K31/551 , A61K45/06 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07B2200/13 , C07C53/18 , C07C309/30 , C07D205/04 , C07D211/66 , C07D215/54 , C07D231/12 , C07D237/08 , C07D239/26 , C07D239/42 , C07D249/08 , C07D263/32 , C07D279/12 , C07D295/192 , C07D295/26 , C07D401/04 , C07D401/12 , C07D403/12 , C07D413/12 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/107 , C07D498/08 , A61K2300/00
摘要: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
-
6.
公开(公告)号:US20180305359A1
公开(公告)日:2018-10-25
申请号:US16021551
申请日:2018-06-28
发明人: Samarendra N. MAITI , Dai NGUYEN , Jehangir KHAN , Rong LING
IPC分类号: C07D471/08 , C07D519/00 , A61K31/55 , A61K31/553 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61K31/439 , A61K31/4545 , A61K31/444 , A61K31/46 , A61K45/06 , C07D451/06
CPC分类号: C07D471/08 , A61K31/439 , A61K31/444 , A61K31/4545 , A61K31/46 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553 , A61K45/06 , C07D451/06 , C07D519/00 , A61K2300/00
摘要: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1 ,R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
-
公开(公告)号:US20180282301A1
公开(公告)日:2018-10-04
申请号:US15762229
申请日:2016-09-20
发明人: Stephen John ATKINSON , Emmanuel Hubert , Lee Andrew HARRISON , Thomas HAYHOW , David HOUSE , Matthew J. LINDON , Alexander G. PRESTON , Jonathan Thomas SEAL , IAN David WALL , Robert J. WATSON , James Michael WOOLVEN
IPC分类号: C07D401/12 , C07D405/12 , A61K31/4433 , A61K31/4545 , A61K31/4427 , A61K31/443 , A61K31/496 , C07D409/12 , A61K31/4436 , C07D401/14 , A61K31/5377 , A61K31/541
CPC分类号: C07D401/12 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D401/14 , C07D405/12 , C07D409/12
摘要: The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy
-
公开(公告)号:US10053454B2
公开(公告)日:2018-08-21
申请号:US14770230
申请日:2014-02-27
发明人: Michael A. Poss , David R. Tortolani , Ashok Vinayak Purandare , John S. Tokarski , Christopher P. Mussari , Muthoni G. Kamau , Dharmpal S. Dodd , Ashvinikumar V. Gavai , Daniel O'Malley , Tram N. Huynh , Wayne Vaccaro , Lalgudi S. Harikrishnan
IPC分类号: C07D413/04 , C07D413/10 , C07D413/14 , C07D417/14 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61K31/553
CPC分类号: C07D413/10 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61K31/553 , C07D413/04 , C07D413/14 , C07D417/14
摘要: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using the compositions in the treatment of various disorders.
-
公开(公告)号:US20180230137A1
公开(公告)日:2018-08-16
申请号:US15752000
申请日:2016-08-11
申请人: Zafgen, Inc.
发明人: Robert Zahler , James E. Vath
IPC分类号: C07D405/14 , A61K9/00 , C07D491/107 , C07D491/048 , C07D491/08 , C07D487/08 , C07D413/14 , A61P3/04
CPC分类号: C07D405/14 , A61K9/0019 , A61K31/397 , A61K31/4025 , A61K31/403 , A61K31/4155 , A61K31/4427 , A61K31/4523 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/541 , A61P3/04 , C07D401/14 , C07D405/12 , C07D413/08 , C07D413/14 , C07D417/14 , C07D487/08 , C07D491/048 , C07D491/08 , C07D491/107
摘要: Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
-
10.
公开(公告)号:US20180185378A1
公开(公告)日:2018-07-05
申请号:US15861248
申请日:2018-01-03
申请人: Cormedix Inc.
发明人: Robert DiLuccio
IPC分类号: A61K31/541 , C07D285/18 , A61K9/20 , A61K9/00 , A61P1/00
CPC分类号: A61K31/549 , A61K9/0031 , A61K9/0053 , A61K9/0065 , A61K9/06 , A61K9/2077 , A61K9/4866 , A61K9/5015 , A61K9/5073 , A61K31/541 , A61P1/00 , C07D285/18
摘要: This invention relates to the prophylactic and/or therapeutic application of antimicrobials that are, for example, administered orally as a delayed release formulation designed to release the drug to the distal small intestine and/or colon in high quantities and density, as a method for the prevention and/or treatment of infections in the colon.
-
-
-
-
-
-
-
-
-