公开(公告)号：US20230183185A1

公开(公告)日：2023-06-15

申请号：US18054272

申请日：2022-11-10

申请人： NUFROMIX TECHNOLOGIES LIMITED

发明人： Joanne HOLLAND ,  Alex EBERLIN

IPC分类号： C07D237/32 ,  C07C65/05 ,  C07C65/03 ,  C07C65/10

CPC分类号： C07D237/32 ,  C07C65/05 ,  C07C65/03 ,  C07C65/10 ,  C07B2200/13

摘要： The invention relates to new 1:1 olaparib:hydroxybenzoic acid cocrystals. The invention also relates to new 2:1 olaparib:hydroxybenzoic acid cocrystals which may contain no water (anhydrous) or may optionally be hydrated. The invention also relates to pharmaceutical compositions containing an olaparib hydroxybenzoic acid cocrystal of the invention and a pharmaceutically acceptable carrier. The olaparib hydroxybenzoic acid cocrystals of the invention may be useful for the treatment of diseases that benefit from inhibition of poly (ADP-ribose) polymerase (PARP).

公开(公告)号：US11492351B2

公开(公告)日：2022-11-08

申请号：US17018738

申请日：2020-09-11

申请人： Mirati Therapeutics, Inc.

发明人： Thomas P. Bobinski ,  Christopher Ronald Smith ,  Matthew Arnold Marx ,  John Michael Ketcham ,  Aaron Craig Burns ,  John David Lawson ,  Svitlana Kulyk ,  Jon Kuehler ,  Anthony Ivetac

IPC分类号： C07D471/04 ,  C07D237/32 ,  C07D401/10 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D401/14 ,  C07D487/04 ,  C12N9/10

摘要： The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds of Formula (I) to pharmaceutical compositions comprising compounds of Formula (I) and to methods of use thereof, such as methods of treating cancer using the compounds of Formula (I) and pharmaceutical compositions comprising those compounds.

公开(公告)号：US20220340529A1

公开(公告)日：2022-10-27

申请号：US17525479

申请日：2021-11-12

申请人： Morphic Therapeutic, Inc.

发明人： Matthew G. Bursavich ,  Dawn M. Troast ,  Bryce A. Harrison ,  Blaise S. Lippa ,  Bruce N. Rogers ,  Kyle D. Konze ,  Aleksey I. Gerasyuto ,  Tyler Day ,  Fu-Yang Lin ,  Kristopher N. Hahn ,  Mats A. Svensson ,  Byungchan Kim ,  Cheng Zhong ,  Alexey A. Lugovskoy ,  Brian Sosa

IPC分类号： C07D213/64 ,  C07D401/06 ,  C07D413/14 ,  C07D401/14 ,  C07D401/12 ,  C07D241/18 ,  C07D413/12 ,  C07D487/04 ,  C07D239/90 ,  C07D237/32 ,  C07D205/08 ,  C07D471/04

摘要： Disclosed are small molecule antagonists of α4β7 integrin, and methods of using them to treat a number of specific diseases or conditions.

公开(公告)号：US11203575B2

公开(公告)日：2021-12-21

申请号：US15999050

申请日：2017-02-15

申请人： METRIOPHARM AG

发明人： Thomas Martin ,  Josef Breu ,  Juliane Fleissner ,  Wolfgang Brysch ,  Jörg Von Wegerer

IPC分类号： C07D237/32 ,  A61K9/00 ,  A61K9/12 ,  A61K45/06

摘要： A new method for producing a crystalline form of 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) is provided. Advantageous uses for this crystalline form as a detecting agent or as an agent for forensic purposes are disclosed, as well a pharmaceutical composition containing said crystalline form.

公开(公告)号：US11111218B2

公开(公告)日：2021-09-07

申请号：US15999447

申请日：2017-02-15

申请人： METRIOPHARM AG

发明人： Thomas Martin ,  Josef Breu ,  Juliane Fleissner ,  Wolfgang Brysch ,  Jörg Von Wegerer

IPC分类号： A61K31/502 ,  C07D237/32 ,  A61K9/00 ,  A61K45/06

摘要： A new crystalline form of 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) is provided. Advantageous uses for this crystalline form as a detecting agent or as an agent for forensic purposes are disclosed, as well a pharmaceutical composition containing said crystalline form.

公开(公告)号：US20210078994A1

公开(公告)日：2021-03-18

申请号：US16948312

申请日：2020-09-11

申请人： Mirati Therapeutics, Inc.

发明人： Thomas P. Bobinski ,  Christopher Ronald Smith ,  Matthew Arnold Marx ,  John Michael Ketcham ,  Aaron Craig Burns ,  John David Lawson ,  Svitlana Kulyk ,  Jon Kuehler ,  Anthony Ivetac

IPC分类号： C07D471/04 ,  C07D237/32 ,  C07D401/10 ,  C07D403/12 ,  C07D417/10 ,  C07D403/10 ,  C07D413/10 ,  C07D413/14

摘要： The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.

公开(公告)号：US20200017486A1

公开(公告)日：2020-01-16

申请号：US16511315

申请日：2019-07-15

申请人： Flatley Discovery Lab, LLC

发明人： Bridget M. Cole ,  Richard A. Nugent ,  Andrew Kolodziej ,  Karen Handley ,  Yevgen Barsukov

IPC分类号： C07D413/12 ,  A61K31/502 ,  A61K45/06 ,  C07D413/14 ,  C07D498/04 ,  A61K31/38 ,  A61K31/4245 ,  A61K31/443 ,  A61K31/47 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  C07D237/32 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D487/04 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D417/14 ,  C07D495/14 ,  C07D519/00

摘要： The invention relates to a compound of having the following formulae and methods of treating cystic fibrosis:

公开(公告)号：US20190389809A1

公开(公告)日：2019-12-26

申请号：US16562436

申请日：2019-09-06

申请人： RejuvGen Pharmaceuticals, Inc.

发明人： Faxiang LIANG ,  Yanling DING

IPC分类号： C07D237/32

摘要： The present disclosure provides a polyhydroxyphthalazinone compound, preparation method thereof and use thereof, wherein the general formula of chemical structure of the polyhydroxyphthalazinone compound is shown by the formula (I). The polyhydroxyphthalazinone compound disclosed by the present disclosure has a good effect on activating ERβ receptor, and it is expected to develop a novel ER-β receptor agonist.

公开(公告)号：US10449192B2

公开(公告)日：2019-10-22

申请号：US15904883

申请日：2018-02-26

申请人： KUDOS PHARMACEUTICALS LIMITED

发明人： Niall Morrison Barr Martin ,  Graeme Cameron Smith ,  Stephen Philip Jackson ,  Vincent Junior M Loh ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Frank Kerrigan ,  Alan Ashworth

IPC分类号： C07D237/32 ,  A61K31/502 ,  A61K31/00 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04 ,  C07D495/04 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D403/14 ,  A61K31/506 ,  A61N5/10 ,  C07D243/08

摘要： Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X═NRX then n is 1 or 2 and if X═CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.

公开(公告)号：US10239843B2

公开(公告)日：2019-03-26

申请号：US15533804

申请日：2015-12-11

申请人： CANCER RESEARCH TECHNOLOGY LIMITED

发明人： Alison E. McGonagle ,  Allan Jordan ,  Bohdan Waszkowycz ,  Colin Hutton ,  Ian Waddell ,  James R. Hitchin ,  Kate Mary Smith ,  Niall M. Hamilton

IPC分类号： A61K31/517 ,  C07D239/96 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D215/227 ,  C07D217/22 ,  C07D217/24 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D409/14 ,  C07D239/88 ,  C07D239/90 ,  C07D239/91 ,  C07D413/06 ,  C07D417/06 ,  C07D241/44 ,  C07D417/14 ,  C07D237/32 ,  C07D471/04

摘要： The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. 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 proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.