公开(公告)号：US20250066290A1

公开(公告)日：2025-02-27

申请号：US18719384

申请日：2022-12-23

Applicant: IMMUNIC AG

Inventor： Christian GEGE ,  Andreas MÜHLER ,  Hella KOHLHOF ,  Daniel VITT

IPC: C07C317/28 ,  A61K31/165 ,  A61K31/18 ,  A61K31/277 ,  A61K31/341 ,  A61K31/357 ,  A61K31/381 ,  A61K31/40 ,  A61K31/41 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/437 ,  A61K31/4418 ,  A61K31/472 ,  A61K31/5375 ,  A61K45/06 ,  C07C233/60 ,  C07C255/16 ,  C07C255/46 ,  C07C317/26 ,  C07D207/34 ,  C07D213/64 ,  C07D217/02 ,  C07D257/04 ,  C07D263/56 ,  C07D265/30 ,  C07D271/07 ,  C07D277/68 ,  C07D307/30 ,  C07D317/60 ,  C07D333/38 ,  C07D405/04 ,  C07D471/04

Abstract: The invention relates to novel, optionally deuterated compounds of Formula (I) and their use as medicament.

公开(公告)号：US20240358019A1

公开(公告)日：2024-10-31

申请号：US18686170

申请日：2022-08-30

Applicant: BASF SE

Inventor： Marc Heinrich ,  Markus Kordes ,  Tobias Seiser ,  Gunther Zimmermann ,  Trevor William Newton ,  Gerd Kraemer

IPC: A01N43/40 ,  A01N43/10 ,  A01N43/36 ,  A01N43/54 ,  A01N43/58 ,  A01N43/78 ,  A01N43/80 ,  A01P13/00 ,  C07D207/34 ,  C07D213/75 ,  C07D237/20 ,  C07D239/42 ,  C07D261/14 ,  C07D277/56 ,  C07D333/38

CPC classification number: A01N43/40 ,  A01N43/10 ,  A01N43/36 ,  A01N43/54 ,  A01N43/58 ,  A01N43/78 ,  A01N43/80 ,  A01P13/00 ,  C07D207/34 ,  C07D213/75 ,  C07D237/20 ,  C07D239/42 ,  C07D261/14 ,  C07D277/56 ,  C07D333/38

Abstract: The present invention relates to malonamide compounds of the formula (I) where the variables are as defined in the claims and the description, and to compositions comprising these compounds. The invention also relates to the use of the said malonamide compounds or the corresponding compositions for controlling unwanted vegetation. Furthermore, the invention relates to methods of applying said malonamide compounds or the corresponding compositions.

公开(公告)号：US12116356B2

公开(公告)日：2024-10-15

申请号：US18106103

申请日：2023-02-06

Applicant: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.

Inventor： 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: C07D401/12 ,  C07D207/34 ,  C07D405/12 ,  C07D409/12

CPC classification number: C07D401/12 ,  C07D207/34 ,  C07D405/12 ,  C07D409/12

Abstract: A N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, and a pharmaceutical composition and use thereof, specifically relating to a compound as represented by formula I, 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 a medical use thereof. The medical use comprises the use in treating diseases benefiting from the capsid protein assembly inhibitor, and in particular, diseases caused by hepatitis B virus infection.

公开(公告)号：US11793823B2

公开(公告)日：2023-10-24

申请号：US17699784

申请日：2022-03-21

Applicant: SyneuRx International (Taiwan) Corp.

Inventor： Guochuan Emil Tsai ,  Yi-Wen Mao ,  Lu-Ping Lu ,  Wei-Hua Chang ,  Han-Yi Hsieh ,  Jhe Wei Hu ,  Tsai-Miao Shih ,  ChanHui Huang

IPC: C07D207/34 ,  A61K31/7048 ,  A23L33/10 ,  A23L33/00 ,  A61P25/18 ,  A61K31/235 ,  A61K31/36 ,  A61K31/40 ,  A61K31/415 ,  A61K31/7034 ,  C07C69/90 ,  C07D231/14 ,  C07D317/68 ,  C07H15/22 ,  C07H15/26

CPC classification number: A61K31/7048 ,  A23L33/10 ,  A23L33/40 ,  A61K31/235 ,  A61K31/36 ,  A61K31/40 ,  A61K31/415 ,  A61K31/7034 ,  A61P25/18 ,  C07C69/90 ,  C07D207/34 ,  C07D231/14 ,  C07D317/68 ,  C07H15/22 ,  C07H15/26 ,  A23V2002/00

Abstract: A compound of Formula (I):




or a pharmaceutically acceptable salt thereof, in which Ring X is a 3 to 7 membered monocyclic ring, at least one of R1, R2, R3, and R4 is OR5 or CH2OR5 and the other R1, R2, R3, and R4 each independently are halogen, OH, OR5, CH2OR5, CO2H, OC═OR6, (C═O)R6, R6, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, H, or absent. Also provided herein are therapeutic uses of the compound of Formula (I).

公开(公告)号：US11780821B2

公开(公告)日：2023-10-10

申请号：US16221398

申请日：2018-12-14

Applicant: Praxis Biotech LLC

Inventor： Jennifer Alfaro ,  Sebastian Belmar ,  Sebastian Bernales ,  Brahmam Pujala ,  Dayanand Panpatil ,  Bhawana Bhatt

IPC: C07D401/12 ,  A61P3/04 ,  A61P3/10 ,  A61P35/00 ,  C07D207/34 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/048

CPC classification number: C07D401/12 ,  A61P3/04 ,  A61P3/10 ,  A61P35/00 ,  C07D207/34 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/048

Abstract: Compounds and compositions for modulating fibroblast activation protein (FAP) are described. The compounds and compositions may find use as therapeutic agents for the treatment of diseases, including hyperproliferative diseases.

公开(公告)号：US20230234927A1

公开(公告)日：2023-07-27

申请号：US17929931

申请日：2022-09-06

Applicant: Rezolute, Inc. ,  ActiveSite Pharmaceuticals, Inc.

Inventor： Sukanto SINHA ,  Tamie Chilcote ,  Baburaj Krishnan ,  Ganapati Bhat ,  Vineet Malik

IPC: C07D231/14 ,  C07D307/68 ,  C07D277/56 ,  C07D207/34 ,  C07D333/38 ,  C07D249/04

CPC classification number: C07D231/14 ,  C07D307/68 ,  C07D277/56 ,  C07D207/34 ,  C07D333/38 ,  C07D249/04

Abstract: A process for preparing and purifying a compound of Formula I is provided:




thereof,



wherein the subscript m is an integer of from 0 to 3;
each Ra is independently selected from the group consisting of (C3-C8)cycloalkyl, (C1-C4)haloalkyl, halogen, —OH, —OR1, —SH, —SR1, —S(O)R1, —S(O)2R1, —SO2NH2, —C(O)NH2, —C(O)NHR1, —C(O)N(R1)2, —C(O)R1, —C(O)H, —CO2H, —CO2R1, —NO2, —NH2, —NHR1, —N(R1)2, wherein each R1 is independently (C1-C8)alkyl;
L is a linking group selected from the group consisting of a bond or CH2;
Qa, Qb, and Qc are each members independently selected from the group consisting of N, S, O and C(Rq) wherein each Rq is independently selected from the group consisting of H, C1-8 alkyl, halo and phenyl, and the ring having Qa, Qb, Qc and Y as ring vertices is a five-membered ring having two double bonds; and

Y is selected from the group consisting of C and N.

公开(公告)号：US20230233516A1

公开(公告)日：2023-07-27

申请号：US18147171

申请日：2022-12-28

Applicant: TECHFIELDS PHARMA CO., LTD

Inventor： Chongxi Yu

IPC: 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 ,  A61K8/31 ,  A61K31/015 ,  C07C15/30 ,  C07C15/38

CPC classification number: 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 ,  A61K8/31 ,  A61K31/015 ,  C07C15/30 ,  C07C15/38 ,  Y02A50/30

Abstract: The invention provides compositions or pharmaceutical compositions of novel 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 and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. 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：US20230088365A1

公开(公告)日：2023-03-23

申请号：US17961978

申请日：2022-10-07

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

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

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

Abstract: 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

Applicant: Ikena Oncology, Inc.

Inventor： Alfredo C. Castro ,  Catherine Anne Evans

IPC: 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

Abstract: 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

Applicant: Chongxi Yu

Inventor： Chongxi Yu

IPC: 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

Abstract: 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.