公开(公告)号：US11634413B2

公开(公告)日：2023-04-25

申请号：US17445096

申请日：2021-08-16

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： Melissa Fleury ,  Adam D. Hughes

IPC分类号： C07D405/12 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/421 ,  C07D231/14 ,  C07D231/20 ,  C07D249/04 ,  C07D261/18 ,  C07D263/38 ,  A61K45/06

摘要： In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

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：US11130731B2

公开(公告)日：2021-09-28

申请号：US16535002

申请日：2019-08-07

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 ,  A61P5/00 ,  C07D403/12 ,  A61P37/00 ,  A61P35/00 ,  A61P3/00 ,  A61P25/00 ,  A61P1/00 ,  C07D215/36 ,  C07D401/12 ,  C07D487/04 ,  C07D493/04 ,  A61P17/00 ,  C07D213/71 ,  C07D309/08 ,  C07D311/18 ,  C07D311/60 ,  C07D217/22 ,  C07D217/24 ,  C07D495/04 ,  C07D217/02 ,  C07D221/18 ,  C07D241/42 ,  C07D307/68 ,  C07D311/16 ,  C07D333/52 ,  C07D307/82 ,  C07D307/64 ,  C07D307/18 ,  C07D277/36 ,  C07D498/04 ,  C07D207/38 ,  C07D495/06 ,  C07D271/12 ,  C07D261/18 ,  C07D249/12 ,  C07D249/06 ,  C07D249/04 ,  C07D417/12 ,  C07D241/44 ,  C07D317/62 ,  C07D231/18 ,  C07D333/34 ,  C07D333/62 ,  C07C311/60 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D241/24 ,  C07D235/02 ,  C07D401/06

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.

公开(公告)号：US11098035B2

公开(公告)日：2021-08-24

申请号：US16510406

申请日：2019-07-12

申请人： Proteostasis Therapeutics, Inc.

发明人： Cecilia M. Bastos ,  Benito Munoz ,  Bradley Tait

IPC分类号： C07D413/12 ,  A61K31/42 ,  A61K31/4245 ,  C07D413/14 ,  C07D409/14 ,  C07D417/12 ,  C07D261/18 ,  C07D307/54 ,  C07D405/12 ,  C07D407/12 ,  A61K31/422 ,  A61K31/433 ,  A61K31/5377 ,  A61K45/06 ,  C07D307/68 ,  G01N33/50

摘要： The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.

公开(公告)号：US20210155576A1

公开(公告)日：2021-05-27

申请号：US16948872

申请日：2020-10-05

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： Melissa Fleury ,  Adam D. Hughes

IPC分类号： C07C229/22 ,  C07D249/18 ,  A61K31/4192 ,  A61K45/06 ,  C07D231/20 ,  A61K31/415 ,  C07D405/12 ,  A61K31/4155 ,  A61K31/4439 ,  C07D401/04 ,  C07D405/14 ,  C07D231/14 ,  C07D261/18 ,  A61K31/42 ,  C07D249/04 ,  C07D249/12 ,  A61K31/4196 ,  C07D257/04 ,  A61K31/41 ,  A61K31/675 ,  C07F9/6503 ,  C07D231/18 ,  C07D253/08 ,  C07C271/22 ,  C07D207/26 ,  C07D263/38

摘要： In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

公开(公告)号：US20210094907A1

公开(公告)日：2021-04-01

申请号：US16981654

申请日：2019-03-21

申请人： NORTHWESTERN UNIVERSITY

发明人： Ali Shilatifard ,  Kaivvei Liang ,  Edwin R. Smith ,  Gary E. Schiitz ,  Rama K. Mishra ,  Kristen Stoltz

IPC分类号： C07C235/74 ,  C07C235/78 ,  C07D241/20 ,  C07D213/40 ,  C07D257/06 ,  C07D271/07 ,  C07D277/46 ,  C07D213/75 ,  C07D239/42 ,  C07D261/18 ,  C07D231/14 ,  C07D239/36 ,  A61P35/00

摘要： Disclosed are compounds which may be utilized to inhibit transcription by RNA Polymerase II (Pol II), and in particular to disrupt the Super Elongation Complex (SEC). The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with the biological activity of SEC, and in particular, diseases and disorders that are associated with high levels of expression of genes whose expression is SEC-dependent and that promote, support, or otherwise are required for the disease or disorder such as cancers.

公开(公告)号：US20210032213A1

公开(公告)日：2021-02-04

申请号：US16831638

申请日：2020-03-26

申请人： Escient Pharmaceuticals, Inc.

发明人： Adam Yeager ,  Brandon Selfridge ,  Marcos Sainz ,  Esther Martinborough ,  Marcus Boehm ,  Liming Huang

IPC分类号： C07D265/30 ,  C07C69/78 ,  C07C255/41 ,  C07D277/64 ,  C07D241/24 ,  C07D213/79 ,  C07D333/38 ,  C07D261/18

摘要： Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I). or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

公开(公告)号：US20210002235A1

公开(公告)日：2021-01-07

申请号：US16977761

申请日：2019-03-13

申请人： Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

发明人： Songliang Wu ,  Jianfeng Mou ,  Haiying He

IPC分类号： C07D261/18

摘要： Disclosed herein a crystal structure of a caspase inhibitor, and more specifically a crystal structure of an (S)-3-((S)-2-(5-(2-chlorophenyl)isoxazole-3-formylamide)proponamide)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)valeric acid, a preparation method therefor, a crystal polymer, a pharmaceutical composition and uses thereof. The compound A of formula (I) disclosed herein exhibits high crystal structure stability, low hygroscopicity, and advantageously shows physical properties, safety and metabolic stability while having relatively high pharmaceutical value.

公开(公告)号：US20200345727A1

公开(公告)日：2020-11-05

申请号：US16761390

申请日：2018-11-02

申请人： Calico Life Sciences LLC ,  AbbVie Inc.

发明人： Kathleen Ann Martin ,  Carmela Sidrauski ,  Jennifer M. Frost ,  Marina Pliushchev ,  Yunsong Tong ,  Lawrence A. Black ,  Xiangdong Xu ,  Lei Shi ,  Qingwei I. Zhang ,  SeungWon Chung ,  Ramzi Farah Sweis ,  Michael J. Dart ,  John T. Randolph ,  Kathleen J. Murauski

IPC分类号： A61K31/4965 ,  A61K45/06 ,  C07D261/18 ,  C07D263/34 ,  C07D241/20 ,  A61K31/421 ,  A61K31/42 ,  A61K31/437 ,  C07D471/04 ,  C07D487/04 ,  C07D333/38 ,  C07D307/68 ,  A61K31/381 ,  A61K31/519 ,  A61K31/341 ,  A61K31/415 ,  A61K31/426 ,  A61K31/425 ,  C07D275/03 ,  C07D277/56 ,  C07D231/14 ,  C07D495/04 ,  A61K31/4985 ,  C07D237/20 ,  C07D413/04 ,  C07D285/06 ,  C07D317/46 ,  A61K31/36 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/4196 ,  C07D249/10 ,  C07D217/26 ,  A61K31/472 ,  A61K31/196 ,  C07C233/62 ,  C07D401/04 ,  A61K31/4427 ,  A61K31/5355

摘要： Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

公开(公告)号：US10738040B2

公开(公告)日：2020-08-11

申请号：US16190964

申请日：2018-11-14

申请人： Proteostasis Therapeutics, Inc.

发明人： Cecilia M. Bastos ,  Benito Munoz ,  Bradley Tait

IPC分类号： C07D261/08 ,  C07D413/12 ,  C07F7/18 ,  C07D413/14 ,  C07D231/12 ,  C07D233/61 ,  C07D417/12 ,  C07D261/18 ,  C07D285/12 ,  A61K31/16 ,  A61K31/42 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/695 ,  A61K45/06 ,  C07C243/36

摘要： The present disclosure features disclosed compounds which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound.