公开(公告)号：USRE49594E1

公开(公告)日：2023-08-01

申请号：US16974363

申请日：2020-05-04

Applicant: Research Triangle Institute

Inventor： Scott P. Runyon ,  Rangan Maitra ,  Sanju Narayanan ,  James Barnwell Thomas ,  Kenneth S. Rehder ,  Srinivas Olepu

IPC: C07D491/107 ,  C07D403/12 ,  C07D231/14 ,  C07D403/06 ,  C07D407/12 ,  C07D413/12 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08

CPC classification number: C07D491/107 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4245 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D407/12 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08

Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.

公开(公告)号：US11708351B2

公开(公告)日：2023-07-25

申请号：US17366670

申请日：2021-07-02

Applicant: Achillion Pharmaceuticals, Inc.

Inventor： Jason Allan Wiles ,  Avinash S. Phadke ,  Milind Deshpande ,  Atul Agarwal ,  Dawei Chen ,  Venkat Rao Gadhachanda ,  Akihiro Hashimoto ,  Godwin Pais ,  Qiuping Wang ,  Xiangzhu Wang ,  Joel Charles Barrish ,  William Greenlee ,  Kyle J. Eastman

IPC: C07D401/14 ,  C07D403/14 ,  C07D409/14 ,  C07D471/04 ,  C07D471/08 ,  C07D491/107 ,  C07D498/10 ,  C07F5/02

CPC classification number: C07D401/14 ,  C07D403/14 ,  C07D409/14 ,  C07D471/04 ,  C07D471/08 ,  C07D491/107 ,  C07D498/10 ,  C07F5/027

Abstract: Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

公开(公告)号：US20230219969A1

公开(公告)日：2023-07-13

申请号：US18001191

申请日：2021-06-09

Applicant: Delix Therapeutics, Inc.

Inventor： Florence WAGNER ,  Noel Aaron POWELL ,  Milan CHYTIL ,  David E. OLSON

IPC: C07D491/147 ,  A61P25/28 ,  C07D491/056 ,  C07D471/04 ,  C07D487/04 ,  C07D209/08 ,  C07D491/107 ,  C07D471/08 ,  C07D403/04 ,  C07D403/08

CPC classification number: C07D491/147 ,  A61P25/28 ,  C07D491/056 ,  C07D471/04 ,  C07D487/04 ,  C07D209/08 ,  C07D491/107 ,  C07D471/08 ,  C07D403/04 ,  C07D403/08

Abstract: Disclosed herein are compounds, compositions, and methods for promoting neuronal growth and/or improving neuronal structure with the compounds and compositions disclosed herein. Also described are methods of treating diseases or disorders that are mediated by the loss of synaptic connectivity and/or plasticity, such as neurological diseases and disorders, with non-hallucinogenic psychoplastogens.

公开(公告)号：US20230219930A1

公开(公告)日：2023-07-13

申请号：US17914153

申请日：2021-03-12

Applicant: WHAN IN PHARMACEUTICAL CO., LTD. ,  KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Ge Hyeong LEE ,  Jee Yeon SEO ,  Jeong Heon YU ,  In Hae YE ,  Ho Chul SHIN ,  Jee Hee SUH ,  Seong Hwan KIM ,  Jin Sook SONG ,  Seong Hyeon SIM ,  Chong Hak CHAE ,  Hee Yeon KANG ,  Ji Hun LEE ,  Keon Ha HWANG

IPC: C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D491/107 ,  C07D413/14 ,  C07D491/18 ,  C07D487/04 ,  C07D471/04

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D491/107 ,  C07D413/14 ,  C07D491/18 ,  C07D487/04 ,  C07D471/04

Abstract: The present invention relates to a novel pyrimidine derivative, and a composition for preventing or treating neurodegenerative diseases and cancer, comprising same, the pyrimidine derivative having a LRRK2 protein inhibitory activity, and effectively passing through a blood-brain barrier (BBB) so as to be effectively used as a pharmaceutical composition for preventing or treating neurodegenerative diseases and cancer.

公开(公告)号：US11679107B2

公开(公告)日：2023-06-20

申请号：US17046528

申请日：2019-04-11

Applicant: Eisai R&D Management Co., Ltd.

Inventor： Andrew Cook ,  Dominic Reynolds ,  Cheng Zhong ,  Ryan Brawn ,  Shelby Ellery ,  Thiwanka Samarakoon ,  Xiang Liu ,  Sudeep Prajapati ,  Megan Sheehan ,  Jason T. Lowe ,  James Palacino

IPC: C07D405/06 ,  A61K31/496 ,  A61P35/00 ,  A61K9/00 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  A61K38/19 ,  A61K38/20 ,  A61K38/21 ,  A61K39/395 ,  C07D313/00 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D453/02 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D498/08

CPC classification number: A61K31/496 ,  A61K9/0053 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  A61K38/191 ,  A61K38/208 ,  A61K38/2013 ,  A61K38/2066 ,  A61K38/2086 ,  A61K38/217 ,  A61K39/3955 ,  A61P35/00 ,  C07D313/00 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D453/02 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D498/08 ,  C07B2200/05

Abstract: The present disclosure provides pladienolide compounds, pharmaceutical compositions containing such compounds, and pladienolide compounds for use in methods of medical treatment. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are pladienolide compounds for use in methods of treating cancers by administering at least one pladienolide compound disclosed herein and at least one additional therapy

公开(公告)号：US20230183217A1

公开(公告)日：2023-06-15

申请号：US18065259

申请日：2022-12-13

Applicant: Halia Therapeutics, Inc.

Inventor： David James Bearss ,  John Sai Keong Kauwe, III ,  Alexis Henri Abel Mollard

IPC: C07D403/14 ,  C07D239/47 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D491/107 ,  C07D498/08

CPC classification number: C07D403/14 ,  C07D239/47 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D491/107 ,  C07D498/08

Abstract: Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I):




or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R1a, R1b, R2, and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.

公开(公告)号：US20230167073A1

公开(公告)日：2023-06-01

申请号：US17919186

申请日：2021-04-15

Applicant: Teijin Pharma Limited

Inventor： Sakae SUGIYAMA ,  Takuya YOKOSAKA ,  Kunio MINAMIZONO ,  Asahi KAWANA ,  Toshiyuki KANEKO ,  Akinobu MARUYAMA ,  Kosuke SASAKI ,  Shinnosuke HOSODA ,  Masaki KOSHIMIZU ,  Susumu TAKEUCHI ,  Kenta KATO ,  Nagasree CHAKKA ,  Brett M. JOHNSON ,  Ryan D. WHITE ,  Wei ZHAO

IPC: C07D239/42 ,  C07D239/48 ,  C07D491/107 ,  C07D487/12 ,  C07D239/47 ,  C07D401/04 ,  C07D239/34 ,  C07D487/04 ,  C07D417/04 ,  C07D413/04 ,  C07D409/04 ,  C07D239/52 ,  C07D237/22 ,  C07D237/14 ,  C07D417/12 ,  C07D409/12 ,  C07D405/12 ,  C07D401/12 ,  C07D403/12 ,  C07D403/04 ,  C07D401/14 ,  C07D231/20 ,  C07D213/30 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D417/14 ,  C07D413/12 ,  C07D413/14 ,  C07D498/08 ,  C07D491/052

CPC classification number: C07D239/42 ,  C07D239/48 ,  C07D491/107 ,  C07D487/12 ,  C07D239/47 ,  C07D401/04 ,  C07D239/34 ,  C07D487/04 ,  C07D417/04 ,  C07D413/04 ,  C07D409/04 ,  C07D239/52 ,  C07D237/22 ,  C07D237/14 ,  C07D417/12 ,  C07D409/12 ,  C07D405/12 ,  C07D401/12 ,  C07D403/12 ,  C07D403/04 ,  C07D401/14 ,  C07D231/20 ,  C07D213/30 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D417/14 ,  C07D413/12 ,  C07D413/14 ,  C07D498/08 ,  C07D491/052

Abstract: A compound indicated by formula (I) or a pharmacologically acceptable salt thereof is provided as a compound that can be a therapeutic or prophylactic drug for TRPC6-related diseases, such as nephrotic syndrome, membranous nephropathy, acute renal failure, septicemia, chronic renal failure, diabetic nephropathy, pulmonary hypertension, acute lung injury, heart failure, malignant tumor, and muscular dystrophy. (In the formula, Ar1, Ar2, X1-X3, R1, R3, R7, R8, L1, and L2 are as defined in the specifications.)

公开(公告)号：US20230142119A1

公开(公告)日：2023-05-11

申请号：US17860589

申请日：2022-07-08

Applicant: Chugai Seiyaku Kabushiki Kaisha

Inventor： Kazutomo KINOSHITA ,  Kohsuke ASOH ,  Noriyuki FURUICHI ,  Toshiya ITO ,  Hatsuo KAWADA ,  Nobuya ISHII ,  Hiroshi SAKAMOTO ,  WooSang HONG ,  MinJeong PARK ,  Yoshiyuki ONO ,  Yasuharu KATO ,  Kenji MORIKAMI ,  Takashi EMURA ,  Nobuhiro OIKAWA

IPC: C07D209/58 ,  C07D209/88 ,  C07D307/77 ,  C07D307/92 ,  C07D333/50 ,  C07D333/76 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D491/107 ,  C07D209/56 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/7056 ,  C07D307/78 ,  C07D333/52 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/14 ,  C07D471/10 ,  C07F7/08 ,  C07H15/26

CPC classification number: C07D209/58 ,  C07D209/88 ,  C07D307/77 ,  C07D307/92 ,  C07D333/50 ,  C07D333/76 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D491/107 ,  C07D209/56 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/7056 ,  C07D307/78 ,  C07D333/52 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/14 ,  C07D471/10 ,  C07F7/0834 ,  C07H15/26

Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder:






(meanings of the symbols that are included in the formula are as given in the specification).

公开(公告)号：US20230133406A1

公开(公告)日：2023-05-04

申请号：US17820271

申请日：2022-08-17

Applicant: CHEMOCENTRYX, INC.

Inventor： Penglie ZHANG ,  Daniel R. MARSHALL ,  Howard S. ROTH ,  Aubrie HARLAND ,  Ju YANG ,  Christopher W. LANGE ,  Rebecca M. LUI ,  Antoni KRASINSKI

IPC: C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D417/14 ,  C07D491/107 ,  C07D487/10 ,  C07D401/12 ,  C07D491/20

Abstract: Compounds of formula (A) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6:

公开(公告)号：US20230126252A1

公开(公告)日：2023-04-27

申请号：US18048079

申请日：2022-10-20

Applicant: FORMA Therapeutics, Inc.

Inventor： Alex J. Buckmelter ,  Justin Andrew Caravella ,  Hongbin Li ,  Matthew W. Martin ,  Steven Mischke ,  David James Richard ,  Angela V. West

IPC: C07D471/18 ,  C07D403/12 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  C07D491/107

Abstract: The disclosure relates to USP30 Inhibitor Compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same.