公开(公告)号：US20230391790A1

公开(公告)日：2023-12-07

申请号：US18236207

申请日：2023-08-21

Applicant: TARO PHARMACEUTICALS INC.

Inventor： Curtis HARWIG ,  Jeremy D. PETTIGREW ,  Jennifer CROSS ,  Jeyaprakashnarayanan SEENISAMY ,  Mahesh Narayan KEREGADDE ,  Karthikeyan IYANAR

IPC: C07D493/10 ,  A61P29/00 ,  C07D231/54 ,  C07D401/08 ,  C07D403/08 ,  C07D417/08

CPC classification number: C07D493/10 ,  A61P29/00 ,  C07D231/54 ,  C07D401/08 ,  C07D403/08 ,  C07D417/08

Abstract: Compounds of formula (I): wherein, R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

公开(公告)号：US11760746B2

公开(公告)日：2023-09-19

申请号：US17349288

申请日：2021-06-16

Applicant: Gilead Sciences, Inc.

Inventor： Sachin Dhar ,  Alex Goldberg ,  Lars V. Heumann ,  Zilin Huang ,  Vinh Xuan Ngo ,  Trevor James Rainey ,  Dietrich P. Steinhuebel ,  Xianghong Wang ,  Scott Alan Wolckenhauer

IPC: C07D213/24 ,  C07D401/14 ,  C07D401/12 ,  C07D495/10 ,  C07D339/06 ,  C07C59/50 ,  C07D231/56 ,  C07C45/67 ,  C07D213/61 ,  C07D231/54

CPC classification number: C07D401/14 ,  C07C45/673 ,  C07C59/50 ,  C07D213/61 ,  C07D231/54 ,  C07D231/56 ,  C07D339/06 ,  C07D401/12 ,  C07D495/10 ,  C07C2602/18 ,  C07C45/673 ,  C07C49/427

Abstract: The present disclosure relates to methods and intermediates useful for preparing a compound of formula I.




or a co-crystal, solvate, salt or combination thereof.

公开(公告)号：US20230286920A1

公开(公告)日：2023-09-14

申请号：US18309977

申请日：2023-05-01

Applicant: Massachusetts Institute of Technology

Inventor： Ronald T. Raines ,  Brian Gold ,  Jesús M. Dones ,  Nile S. Abularrage ,  Brian James Graham

IPC: C07D221/16 ,  C07D471/04 ,  C07D249/16 ,  C07D231/54 ,  C07C13/547

CPC classification number: C07D221/16 ,  C07D471/04 ,  C07D249/16 ,  C07D231/54 ,  C07C13/547 ,  C07C2603/36

Abstract: Provided herein are dibenzocyclooctyne compounds useful as reagents in 1,3-dipolar cycloaddition reactions, and methods for their preparation.

公开(公告)号：US11746091B2

公开(公告)日：2023-09-05

申请号：US17024752

申请日：2020-09-18

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Robert M. Jones ,  Sangdon Han ,  Lars Thoresen ,  Jae-Kyu Jung ,  Sonja Strah-Pleynet ,  Xiuwen Zhu ,  Yifeng Xiong ,  Dawei Yue

IPC: C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  C07F9/6558 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07F9/65583

Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

公开(公告)号：US20230234940A1

公开(公告)日：2023-07-27

申请号：US18150955

申请日：2023-01-06

Applicant: Aptabio Therapeutics Inc.

Inventor： Soo Jin LEE ,  Sung Hwan MOON ,  Sooho BAN ,  Eunsil LEE ,  Eun Jung SHIN ,  Yoo-Kyung GOH

IPC: C07D401/14 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D231/54 ,  C07D401/12 ,  C07D417/04 ,  C07D413/04 ,  C07D405/04 ,  C07D403/04 ,  A61P39/06 ,  A61P35/00 ,  A61P11/00 ,  A61P1/16

CPC classification number: C07D401/14 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D231/54 ,  C07D401/12 ,  C07D417/04 ,  C07D413/04 ,  C07D405/04 ,  C07D403/04 ,  A61P39/06 ,  A61P35/00 ,  A61P11/00 ,  A61P1/16

Abstract: The Present invention provides a novel pyrazole derivative compound represented by Chemical formula 1, a stereoisomer thereof, a solvate thereof, an isotopic variant thereof, a tautomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.




(In the above, A, B and R, and the like are the same as defined in the description of the invention.)

公开(公告)号：US20230148214A1

公开(公告)日：2023-05-11

申请号：US17908977

申请日：2021-03-05

Applicant: ESCAPE Bio, Inc.

Inventor： Albert W. Garofalo ,  Jacob Bradley Schwarz ,  Fabio Maria Sabbatini ,  Silvia Bernardi ,  Marco Migliore ,  Federica Budassi ,  Claudia Beato

IPC: C07D491/052 ,  C07D231/54 ,  C07D401/12 ,  C07D487/04 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D491/052 ,  C07D231/54 ,  C07D401/12 ,  C07D487/04 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.

公开(公告)号：US10059674B2

公开(公告)日：2018-08-28

申请号：US15152922

申请日：2016-05-12

Applicant: ACT PHARMA CO., LTD.

Inventor： Zhaopeng Liu ,  Yanna Liu ,  Yanqiu Shi ,  Chengmei Zhang

IPC: C07D231/54

CPC classification number: C07D231/54

Abstract: The invention discloses an indenopyrazole small-molecule tubulin inhibitor, which is characterized by having a structure represented by general formula I: wherein R represents NH2 or NHOH; the invention also discloses a preparation method of the indenopyrazole compound, or pharmaceutical salts thereof. The compound of the present invention is an indenopyrazole small-molecule tubulin inhibitor having a novel structure, and has very strong proliferation inhibition activity to human hepatocellular carcinoma (HepG2) cells, human prostate carcinoma (PC3) cells, human cervical carcinoma (HeLa) cells, human breast adenocarcinoma (MCF-7) cells, and human leukemia (K562) cells; the compound is similar to colchicine in mechanism of action, and thus capable of inhibiting tubulin polymerization; the compound is significant for enhancing the specificity and effectiveness of drugs, reducing toxic and side effects, preventing drug tolerance, and so on.

公开(公告)号：US20180155359A9

公开(公告)日：2018-06-07

申请号：US15676726

申请日：2017-08-14

Applicant: Aquinox Pharmaceuticals (Canada) Inc.

Inventor： Lloyd F. Mackenzie ,  Thomas B. MacRury ,  Curtis Harwig ,  David Bogucki ,  Jeffery R. Raymond ,  Jeremy D. Pettigrew

IPC: C07D493/10 ,  C07D333/20 ,  C07D307/52 ,  C07C35/21 ,  C07D307/42 ,  C07D277/64 ,  C07D277/28 ,  C07D261/20 ,  C07D231/56 ,  C07D231/54 ,  C07D221/16 ,  C07D215/227 ,  C07D213/82 ,  C07D213/75 ,  C07D213/38 ,  C07D211/58 ,  C07C335/10 ,  C07C275/22 ,  C07C255/30 ,  C07C233/23 ,  C07C215/38 ,  C07C35/23 ,  C07C2602/24 ,  C07C2601/14

CPC classification number: C07D493/10 ,  A61K31/416 ,  C07C35/21 ,  C07C35/23 ,  C07C215/26 ,  C07C215/38 ,  C07C233/23 ,  C07C255/30 ,  C07C275/22 ,  C07C335/10 ,  C07C2601/14 ,  C07C2602/24 ,  C07D211/58 ,  C07D213/30 ,  C07D213/38 ,  C07D213/75 ,  C07D213/82 ,  C07D215/227 ,  C07D221/16 ,  C07D221/18 ,  C07D231/54 ,  C07D231/56 ,  C07D261/20 ,  C07D277/24 ,  C07D277/28 ,  C07D277/64 ,  C07D307/42 ,  C07D307/52 ,  C07D333/16 ,  C07D333/20

Abstract: Compounds of formula (II): wherein R1, R2, R5 and R13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

公开(公告)号：US20180090691A1

公开(公告)日：2018-03-29

申请号：US15825798

申请日：2017-11-29

Applicant: Universal Display Corporation

Inventor： Jason BROOKS ,  Geza Szigethy ,  Glenn Morello ,  Jun Deng ,  Peter I. Djurovich ,  Hsiao-Fan Chen

IPC: H01L51/00 ,  C07D403/02 ,  C07D221/18 ,  C07D231/54

CPC classification number: H01L51/0072 ,  C07D221/18 ,  C07D231/54 ,  C07D403/02 ,  C07D471/16 ,  C07D498/16 ,  C07D513/16 ,  C07F7/0812 ,  C07F7/1804 ,  C07F15/0033 ,  C07F15/0086 ,  C09K11/025 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/1011 ,  C09K2211/1014 ,  C09K2211/1022 ,  C09K2211/1044 ,  C09K2211/1088 ,  C09K2211/185 ,  H01L51/0073 ,  H01L51/0074 ,  H01L51/0085 ,  H01L51/0087 ,  H01L51/5016

Abstract: Imidazophenanthridine ligands and metal complexes are provided. The compounds exhibit improved stability through a linking substitution that links a nitrogen bonded carbon of an imidizole ring to a carbon on the adjacent fused aryl ring. The compounds may be used in organic light emitting devices, particularly as emissive dopants, providing devices with improved efficiency, stability, and manufacturing. In particular, the compounds provided herein may be used in blue devices having high efficiency.

公开(公告)号：US20170362250A1

公开(公告)日：2017-12-21

申请号：US15676726

申请日：2017-08-14

Applicant: Aquinox Pharmaceuticals (Canada) Inc.

Inventor： Lloyd F. Mackenzie ,  Thomas B. MacRury ,  Curtis Harwig ,  David Bogucki ,  Jeffery R. Raymond ,  Jeremy D. Pettigrew

IPC: C07D493/10 ,  C07D307/52 ,  C07C35/21 ,  C07D307/42 ,  C07D277/64 ,  C07D277/28 ,  C07D261/20 ,  C07D231/56 ,  C07D231/54 ,  C07D221/16 ,  C07D215/227 ,  C07D213/82 ,  C07D213/75 ,  C07D213/38 ,  C07D211/58 ,  C07C335/10 ,  C07C275/22 ,  C07C255/30 ,  C07C233/23 ,  C07C215/38 ,  C07C35/23 ,  C07D333/20 ,  C07C2602/24 ,  C07C2601/14

CPC classification number: C07D493/10 ,  A61K31/416 ,  C07C35/21 ,  C07C35/23 ,  C07C215/26 ,  C07C215/38 ,  C07C233/23 ,  C07C255/30 ,  C07C275/22 ,  C07C335/10 ,  C07C2601/14 ,  C07C2602/24 ,  C07D211/58 ,  C07D213/30 ,  C07D213/38 ,  C07D213/75 ,  C07D213/82 ,  C07D215/227 ,  C07D221/16 ,  C07D221/18 ,  C07D231/54 ,  C07D231/56 ,  C07D261/20 ,  C07D277/24 ,  C07D277/28 ,  C07D277/64 ,  C07D307/42 ,  C07D307/52 ,  C07D333/16 ,  C07D333/20

Abstract: Compounds of formula (II): wherein R1, R2, R5 and R13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.