公开(公告)号：US11413272B2

公开(公告)日：2022-08-16

申请号：US16616515

申请日：2018-05-25

申请人： Oxford University Innovation Limited

发明人： Tharindi Panduwawala ,  Peter Brandt ,  David Wang ,  Mounir Andaloussi ,  Jürgen Brem ,  Christopher J. Schofield

IPC分类号： C07D207/34 ,  A61K31/403 ,  A61P31/04 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/407 ,  A61K31/4164 ,  C07D209/42 ,  C07D209/70 ,  C07D233/90 ,  C07D405/04

摘要： The present invention relates to compounds of Formula (I) that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection. (Formula (I))

公开(公告)号：US20220073452A1

公开(公告)日：2022-03-10

申请号：US17238529

申请日：2021-04-23

申请人： Valo Early Discovery, Inc.

发明人： Kenneth W. Bair ,  Nicholas Barczak ,  Bingsong Han ,  David R. Lancia, JR. ,  Cuixian Liu ,  Matthew W. Martin ,  Pui Yee Ng ,  Aleksandra Rudnitskaya ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Xiaozhang Zheng

IPC分类号： C07C259/06 ,  A61K31/185 ,  C07D221/20 ,  A61K31/438 ,  A61K31/277 ,  C07D209/44 ,  A61K31/4035 ,  C07D295/155 ,  A61K31/451 ,  C07D471/10 ,  A61K31/435 ,  C07D487/10 ,  A61K31/407 ,  C07D495/10 ,  A61K31/397 ,  C07D235/14 ,  A61K31/4184 ,  C07D233/68 ,  A61K31/417 ,  C07D213/56 ,  A61K31/44 ,  C07D241/08 ,  A61K31/495 ,  C07D417/04 ,  A61K31/4439 ,  A61K31/5377 ,  C07D471/04 ,  C07D401/14 ,  C07D213/75 ,  C07D213/81 ,  C07D215/12 ,  C07D317/68 ,  C07D231/14 ,  C07D231/18 ,  C07D233/36 ,  C07D233/38 ,  C07D333/70 ,  C07D401/04 ,  C07D401/12 ,  C07D235/30 ,  C07D239/20 ,  C07D239/22 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D241/12 ,  C07D417/12 ,  C07D249/18 ,  C07D257/04 ,  C07D261/18 ,  C07D487/04 ,  C07D487/08 ,  C07D491/10 ,  C07D207/10 ,  C07D493/08 ,  C07D207/267 ,  C07D498/04 ,  C07D209/08 ,  C07D277/56 ,  C07D209/42 ,  C07D209/46 ,  C07D513/10 ,  C07D211/16 ,  C07D211/58 ,  C07D295/192 ,  C07D213/65 ,  C07D307/68

摘要： The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.

公开(公告)号：US20210179614A1

公开(公告)日：2021-06-17

申请号：US17263580

申请日：2019-07-31

申请人： FIMECS, INC.

发明人： Yusuke TOMINARI ,  Yoshihide TOMATA ,  Kanae GAMO ,  Naomi KITAMOTO

IPC分类号： C07D471/04 ,  C07D209/42 ,  C07D231/14 ,  C07D231/56 ,  C07D235/08 ,  C07D403/06 ,  C07D413/14 ,  C07D403/12 ,  C07D487/04 ,  C07D487/08 ,  C07D209/08 ,  C07D495/14 ,  C07D417/14

摘要： One of the purposes of the present invention is to provide a heterocyclic derivative that has an IAP (particularly XIAP) binding (inhibiting) activity. Another of the purposes of the present invention is to provide a heterocyclic derivative that has an IAP (particularly XIAP) binding (inhibiting) activity and exhibits a protein degradation induction activity. The present invention provides a compound represented by formula (I) (the symbols in the formula are as defined in the present Description) and salts thereof.

公开(公告)号：US10975120B2

公开(公告)日：2021-04-13

申请号：US16204557

申请日：2018-11-29

申请人： Novartis AG

发明人： Aimee Richardson Usera ,  Zachary Hayes Robinson ,  Jennifer Stroka Cobb

IPC分类号： C07K5/103 ,  C07K5/083 ,  C07K5/062 ,  A61K49/00 ,  C07C271/22 ,  C07C317/28 ,  C07K1/13 ,  C07K5/072 ,  A61K47/64 ,  C07D229/02 ,  C07D257/08 ,  C07D209/42 ,  C07K7/02 ,  A61K38/06 ,  A61K38/05 ,  A61K38/07 ,  A61K38/00

摘要： The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.

公开(公告)号：US20210032202A1

公开(公告)日：2021-02-04

申请号：US16899931

申请日：2020-06-12

申请人： Novartis AG

发明人： Jan JIRICEK ,  Ravinder Reddy KONDREDDI ,  Paul William SMITH

IPC分类号： C07D209/42 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D491/056 ,  A61K31/404

摘要： A compound of Formula (1) is provided that has been shown to be useful for treating a disease, disorder or syndrome that is mediated by the transportation of essential molecules in the mmpL3 pathway: wherein R1, R2, R3, R4, R5 and R6 are as defined herein.

公开(公告)号：US10858319B2

公开(公告)日：2020-12-08

申请号：US16190334

申请日：2018-11-14

申请人： IOMet Pharma Ltd.

发明人： Phillip M. Cowley ,  Alan Wise ,  Michael Kiczun ,  Susan Davis

IPC分类号： C07D401/12 ,  C07D209/42 ,  A61K45/06 ,  C07D263/58 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04 ,  C07D409/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/475 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/437 ,  A61K31/4355 ,  A61K31/424 ,  A61K31/423 ,  A61K31/4188 ,  A61K31/4184 ,  A61K31/407 ,  A61K31/405 ,  A61K31/4045 ,  A61K31/404

摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X1, X2, X3, X4, and X5 may be the same or different and each is independently selected from C, N and O; each atom having a dotted line may independently have a double bond or a single bond, provided that valencies at each atom are maintained; each R1, R2, R3, R4, and R7 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X1, X2, X3, X4, and X5 are maintained; one or two R6 groups may be present and are selected from H and a substituted or unsubstituted organic group, provided that the number of R6 groups present is such that the valency of the carbon atom to which they are attached is maintained, and provided that at least one R6 is an organic group comprising an atom double-bonded to an oxygen atom (preferably a carbonyl group or a sulphonyl group) at an α-, β-, or γ-position to the carbon atom to which the R6 is attached and in which the atom double-bonded to an oxygen atom is also bonded to a hetero-atom.

公开(公告)号：US10849883B2

公开(公告)日：2020-12-01

申请号：US16073934

申请日：2017-02-01

申请人： BioCryst Pharmaceuticals, Inc.

发明人： Pravin L. Kotian ,  Yarlagadda S. Babu ,  Weihe Zhang ,  Lakshminarayana Vogeti ,  Minwan Wu ,  Venkat R. Chintareddy ,  Krishnan Raman

IPC分类号： A61K31/416 ,  C07D231/56 ,  C07D403/04 ,  C07D209/42 ,  C07D209/12 ,  C07D403/06 ,  C07D403/12 ,  C07D401/06 ,  C07D487/04 ,  C07D209/48 ,  C07D209/40 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D401/12 ,  C07D405/12 ,  A61P21/04 ,  A61P25/28 ,  A61P9/00 ,  A61P37/06 ,  A61P13/10

摘要： Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity.

公开(公告)号：US20200317613A1

公开(公告)日：2020-10-08

申请号：US16768211

申请日：2018-11-29

申请人： Dana-Farber Cancer Institute, Inc. ,  The Scripps Research Institute

发明人： Bruce M. Spiegelman ,  Jonathan Z Long ,  Hua Lin ,  Theodore Kamenecka ,  Patrick Griffin

IPC分类号： C07D211/60 ,  C07D217/22 ,  C07D215/48 ,  C07D209/42 ,  A61P29/02

摘要： Uncoupling of respiration is a well-recognized process that increases respiration and heat production in cells. Provided herein are chemical uncouplers of respiration that are compounds of Formula (I). Also provided are methods for preventing or treating metabolic disorders and modulating metabolic processes using compound of Formula (I).

公开(公告)号：US10758534B2

公开(公告)日：2020-09-01

申请号：US16258024

申请日：2019-01-25

申请人： Vertex Pharmaceuticals Incorporated

发明人： Mark Thomas Miller ,  Corey Anderson ,  Vijayalaksmi Arumugam ,  Brian Richard Bear ,  Hayley Marie Binch ,  Jeremy J. Clemens ,  Thomas Cleveland ,  Erica Conroy ,  Timothy Richard Coon ,  Bryan A. Frieman ,  Peter Diederik Jan Grootenhuis ,  Raymond Stanley Gross ,  Sara Sabina Hadida-Ruah ,  Haripada Khatuya ,  Pramod Virupax Joshi ,  Paul John Krenitsky ,  Chun-Chieh Lin ,  Gulin Erdogan Marelius ,  Vito Melillo ,  Jason McCartney ,  Georgia McGaughey Nicholls ,  Fabrice Jean Denis Pierre ,  Alina Silina ,  Andreas P. Termin ,  Johnny Uy ,  Jinglan Zhou

IPC分类号： C07D213/82 ,  A61K31/506 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/44 ,  C07D213/84 ,  C07D231/14 ,  A61K31/415 ,  C07D209/42 ,  A61K31/404 ,  C07D401/12 ,  A61K31/4439 ,  C07D401/14 ,  C07D231/12 ,  A61K31/497 ,  C07D417/12 ,  C07D405/14 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4525 ,  A61J1/03 ,  C07D403/12 ,  C07D413/14 ,  C07D213/73 ,  C07D231/20 ,  C07D401/04 ,  C07D235/24 ,  C07D403/10 ,  C07D239/34 ,  C07D407/12 ,  C07D209/18 ,  C07D209/49 ,  C07D213/64

摘要： The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

公开(公告)号：US20200270210A1

公开(公告)日：2020-08-27

申请号：US16872949

申请日：2020-05-12

申请人： GlaxoSmithKline Intellectual Property (No. 2) Limited

发明人： Philip Stewart TURNBULL ,  Rodolfo Cadilla

IPC分类号： C07D209/14 ,  A61K31/404 ,  C07D209/42 ,  C07D401/06 ,  C07D209/10 ,  C07D209/08

摘要： This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.