公开(公告)号：US20230088365A1

公开(公告)日：2023-03-23

申请号：US17961978

申请日：2022-10-07

申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED

发明人： Tomomi Ikemoto ,  Misayo Sera ,  Naohiro Fukuda ,  Hideya Mizufune ,  Toshiaki Nagata ,  Takeshi Yamasaki

IPC分类号： C07D207/337 ,  C07D207/333 ,  C07D207/34 ,  C07D207/36 ,  C07D401/12 ,  C07D207/30 ,  C07D207/48

摘要： The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

公开(公告)号：US11555026B2

公开(公告)日：2023-01-17

申请号：US16890196

申请日：2020-06-02

申请人： Ikena Oncology, Inc.

发明人： Alfredo C. Castro ,  Catherine Anne Evans

IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D417/14 ,  C07D417/12 ,  C07D413/14 ,  C07D231/14 ,  C07D215/38 ,  C07D207/34 ,  A61P35/00 ,  A61P29/00 ,  C07D413/12 ,  A61K9/00

摘要： The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.

公开(公告)号：US11541029B2

公开(公告)日：2023-01-03

申请号：US13133021

申请日：2009-12-04

申请人： Chongxi Yu

发明人： Chongxi Yu

IPC分类号： C07C15/30 ,  C07C15/38 ,  A61K8/31 ,  A61K31/015 ,  A61K31/352 ,  C07D215/18 ,  A61K47/54 ,  C07D209/42 ,  C07D295/088 ,  C07D211/34 ,  C07D231/14 ,  C07D313/14 ,  C07D417/04 ,  C07D491/048 ,  C07D501/22 ,  C07D277/56 ,  C07D207/34

摘要： High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

公开(公告)号：US20220332684A1

公开(公告)日：2022-10-20

申请号：US17763114

申请日：2020-09-28

申请人： CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.

发明人： Pujun WANG ,  Meng GUO ,  Mingtong HU ,  Jie WU ,  Wangwei AO ,  Yinsheng ZHANG

IPC分类号： C07D207/34

摘要： Disclosed are a crystalline form of a five-membered N heterocyclic compound, particularly, a crystalline form of a compound as represented by formula I, and an application of the crystalline form in preparation of a medication for preventing or treating a disease benefiting from inhibition of capsid protein assembly.

公开(公告)号：US20220211665A1

公开(公告)日：2022-07-07

申请号：US17605934

申请日：2020-10-21

申请人： SUNSHINE LAKE PHARMA CO., LTD.

发明人： Jiancheng WANG ,  Xiaojun WANG ,  Yinglin ZUO ,  Yingxun ZHANG ,  Yingjun ZHANG ,  Bo CHI ,  Wei HAN ,  Xiaohong DING ,  Junnan ZENG

IPC分类号： A61K31/40 ,  A61K31/4025 ,  A61K45/06 ,  A61K31/616 ,  C07D207/34 ,  C07D405/06 ,  C07D405/04 ,  C07D401/04 ,  C07D417/12 ,  A61K31/428 ,  A61K31/4439

摘要： A pyrrole amide compound, a pharmaceutical composition thereof and use thereof. The compound or the pharmaceutical composition can be used as a mineralocorticoid receptor antagonist.

公开(公告)号：US20220185774A1

公开(公告)日：2022-06-16

申请号：US17425701

申请日：2019-09-27

申请人： CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.

发明人： Yinsheng ZHANG ,  Wangwei AO ,  Yuan LI ,  Hui WANG ,  Hangzhou SHEN ,  Jie NI ,  Huan ZHANG ,  Jie WU ,  Li ZHANG ,  Kai CAO ,  Peng LU ,  Xushi LIU ,  Jie WANG ,  Tianxiao ZHAO ,  Xingfeng GE ,  Dandan LU ,  Shuo CHEN ,  Xueqin MA ,  Wei SHI ,  Xiaojin WANG ,  Hongjiang XU

IPC分类号： C07D207/34 ,  A61P31/20

摘要： Provided is a compound of formula I or II, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and the medical uses thereof in treating diseases benefiting from the capsid protein assembly inhibitor, particularly diseases caused by hepatitis B virus infection.

公开(公告)号：US11230531B2

公开(公告)日：2022-01-25

申请号：US16783161

申请日：2020-02-05

申请人： University of Tennessee Research Foundation

发明人： Ramesh Narayanan ,  Duane D. Miller ,  Thamarai Ponnusamy ,  Dong-Jin Hwang ,  Yali He

IPC分类号： C07D231/16 ,  C07D207/34 ,  C07D233/68 ,  C07D207/06 ,  C07D295/15 ,  C07D249/08 ,  C07D213/84 ,  C07D239/74 ,  C07D401/12 ,  C07D249/04 ,  C07D209/08 ,  C07C255/60 ,  C07C317/46 ,  A61K31/4192 ,  A61K9/00 ,  A61K45/06 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/5375 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/517 ,  A61K31/277 ,  A61K31/4439 ,  A61K31/415

摘要： This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

公开(公告)号：US20210284606A1

公开(公告)日：2021-09-16

申请号：US17328165

申请日：2021-05-24

申请人： Roche Palo Alto LLC

发明人： Robert Greenhouse ,  Ralph New Harris, III ,  Saul Jaime-Figueroa ,  James M. Kress ,  David Bruce Repke ,  Russell Stephen Stabler

IPC分类号： C07C317/32 ,  C07C317/44 ,  C07D207/16 ,  C07D207/325 ,  C07D207/34 ,  C07D207/36 ,  C07D209/30 ,  C07D231/18 ,  C07D233/20 ,  C07D233/48 ,  C07D233/54 ,  C07D233/64 ,  C07D233/84 ,  C07D233/88 ,  C07D233/90 ,  C07D235/06 ,  C07D239/14 ,  C07D239/42 ,  C07D277/82 ,  C07D233/34 ,  C07D233/44 ,  C07D233/58

摘要： The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, R1 R5, R6 and R7 are as defined herein.

公开(公告)号：US20210236466A1

公开(公告)日：2021-08-05

申请号：US17257225

申请日：2019-07-02

申请人： IFM Due, Inc.

发明人： William R. Roush ,  Shankar Venkatraman ,  Gary Glick ,  Hans Martin Seidel

IPC分类号： A61K31/415 ,  A61K9/00 ,  A61K33/243 ,  A61K31/282 ,  A61K31/675 ,  A61K31/704 ,  A61K31/337 ,  A61K38/14 ,  A61K38/12 ,  A61K38/09 ,  A61K39/395 ,  A61K45/06 ,  A61K31/7048 ,  C07D231/40 ,  C07D233/88 ,  C07D401/04 ,  C07D471/04 ,  C07D417/04 ,  C07D207/34 ,  C07D409/04 ,  C07D401/12 ,  A61K31/4164 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4725

摘要： This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

公开(公告)号：US20210230135A1

公开(公告)日：2021-07-29

申请号：US17208474

申请日：2021-03-22

申请人： MITSUI CHEMICALS, INC.

发明人： Kei Yoshida ,  Takeo Wakita ,  Hiroyuki Katsuta ,  Akiyoshi Kai ,  Yutaka Chiba ,  Kiyoshi Takahashi ,  Hiroko Kato ,  Nobuyuki Kawahara ,  Michikazu Nomura ,  Hidenori Daido ,  Junji Maki ,  Shinichi Banba

IPC分类号： C07D333/38 ,  A01N37/44 ,  A01N43/08 ,  A01N43/10 ,  A01N43/12 ,  A01N43/16 ,  A01N43/30 ,  A01N43/42 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/78 ,  A01N43/80 ,  C07C237/42 ,  C07C317/40 ,  C07C323/42 ,  C07C327/48 ,  C07D207/416 ,  C07D213/64 ,  C07D213/73 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D215/52 ,  C07D231/14 ,  C07D231/16 ,  C07D239/30 ,  C07D241/24 ,  C07D263/34 ,  C07D275/03 ,  C07D277/56 ,  C07D307/24 ,  C07D307/68 ,  C07D307/84 ,  C07D309/08 ,  C07D309/28 ,  C07D317/62 ,  C07D333/68 ,  A01N43/40 ,  A01N37/22 ,  A01N43/60 ,  C07C237/48 ,  C07D207/34 ,  C07D239/28 ,  C07D261/18 ,  C07D307/85 ,  C07D317/46

摘要： A compound represented by Formula (1): The compound can be used as insecticides.