公开(公告)号：US11639355B2

公开(公告)日：2023-05-02

申请号：US16979202

申请日：2019-03-12

Applicant: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD. ,  MEDSHINE DISCOVERY INC.

Inventor： Kevin X Chen ,  Xiaobing Yan ,  Jianglei Huang ,  Yuekun Nie ,  Guoping Hu ,  Jian Li ,  Shuhui Chen ,  Jiaqiang Dong ,  Tie-Lin Wang

IPC: C07D239/22 ,  C07D487/04 ,  A61P35/00 ,  C07D519/00

Abstract: Disclosed is a novel class of MDM2-p53 inhibitor compounds having an imidaxopyrolone structure, and specifically disclosed are compounds represented by formulas (I-1) and (I-2) and pharmaceutically acceptable salts thereof.

公开(公告)号：US20190284192A1

公开(公告)日：2019-09-19

申请号：US16348877

申请日：2017-11-10

Applicant: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Inventor： Yonghan HU ,  Dongmei CAI ,  Jiuxiang ZHU ,  Ping DONG ,  Jiaqiang DONG ,  Tie-Lin WANG

IPC: C07D487/04 ,  C07D487/14 ,  C07D471/14 ,  C07D471/04

Abstract: Disclosed in the present invention are a nitrogenous macrocyclic compound, a preparation method therefor, a pharmaceutical composition and an application thereof. The present invention provides a nitrogenous macrocyclic compound represented by formula III-0, a tautomer thereof, an optical isomer thereof, a hydrate thereof, a solvate thereof, a pharmacologically acceptable salt thereof, or a prodrug thereof. The compound can be effectively bond with bromodomains of a BET family: BRD4, BRD3, BRD2, and BRDT, so as to adjust transcription of a downstream gene c-myc and a related target gene thereof, and further to adjust a downstream signal path and play a particular role, comprising treating diseases such as inflammatory diseases, cancers, and AIDS.

公开(公告)号：US20220017463A1

公开(公告)日：2022-01-20

申请号：US17295878

申请日：2019-10-17

Applicant: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Inventor： Huijun HE ,  Shenyi SHI ,  Jianyu LU ,  Charles Z. DING ,  Lihong HU ,  Bin SHI ,  Wenqian YANG ,  Jiaqiang DONG ,  Tie-Lin WANG

IPC: C07D209/30

Abstract: Provided are a salt form of an estrogen receptor down-regulator, a crystalline form thereof, and a preparation method therefor.

公开(公告)号：US20190337938A1

公开(公告)日：2019-11-07

申请号：US16345271

申请日：2017-10-30

Applicant: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Inventor： Jianyu LU ,  Charles Z. DING ,  Xu ZENG ,  Huijun HE ,  Shuhui CHEN ,  Lihong HU ,  Jiaqiang DONG ,  Tie-Lin WANG

IPC: C07D471/04 ,  A61P35/00

Abstract: Disclosed in the present invention is a type of indole substituted piperidine compounds as an estrogen receptor degrading agent. Specifically disclosed are a compound as shown in formula (I), a pharmaceutically acceptable salt, hydrate or prodrug thereof, a preparation method therefor, a pharmaceutical composition thereof, and a use thereof as an estrogen receptor degrading agent in the treatment of estrogen receptor positive breast cancers.

公开(公告)号：US12098127B2

公开(公告)日：2024-09-24

申请号：US17295878

申请日：2019-10-17

Applicant: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Inventor： Huijun He ,  Shenyi Shi ,  Jianyu Lu ,  Charles Z. Ding ,  Lihong Hu ,  Bin Shi ,  Wenqian Yang ,  Jiaqiang Dong ,  Tie-Lin Wang

IPC: C07D209/30

CPC classification number: C07D209/30 ,  C07B2200/13

Abstract: Provided are a salt form of an estrogen receptor down-regulator, a crystalline form thereof, and a preparation method therefor

公开(公告)号：US11034653B2

公开(公告)日：2021-06-15

申请号：US16648943

申请日：2018-09-25

Applicant: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Inventor： Huijun He ,  Jianyu Lu ,  Weidong Li ,  Shenyi Shi ,  Zhijuan Chen ,  Charles Z. Ding ,  Lihong Hu ,  Tie-Lin Wang ,  Jiaqiang Dong

IPC: C07D209/18

Abstract: Disclosed are a crystal form of an estrogen receptor inhibitor and a preparation method therefor, in particular disclosed are a crystal form A of a compound of formula (I) and a preparation method therefor, and the use of the crystal form in the preparation of a drug for treating breast cancer.

公开(公告)号：US20200317660A1

公开(公告)日：2020-10-08

申请号：US16763377

申请日：2018-11-12

Applicant: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Inventor： Chengde WU ,  Jingjie HUANG ,  Tao YU ,  Jiaqiang DONG ,  Tie-Lin WANG ,  Jie LI ,  Jian LI ,  Shuhui CHEN

IPC: C07D417/14 ,  C07D401/04 ,  C07D409/14 ,  C07D405/14 ,  C07D413/14 ,  A61P35/04

Abstract: The present invention relates to a series of quinazolinone compounds and applications thereof as PI3Kα inhibitors. In particular, the present invention relates to a compound shown in formula (I) and a tautomer or pharmaceutically acceptable salt thereof.

公开(公告)号：US10519143B2

公开(公告)日：2019-12-31

申请号：US16087861

申请日：2017-03-24

Applicant: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Inventor： Jianyu Lu ,  Charles Z. Ding ,  Lihong Hu ,  Huijun He ,  Shuhui Chen ,  Jiaqiang Dong ,  Tie-Lin Wang

IPC: A61K31/437 ,  C07D409/06 ,  C07D403/12 ,  A61K31/404 ,  C07D209/18 ,  C07D401/06 ,  C07D405/06 ,  A61P35/00

Abstract: Disclosed is a new indole compound, in particular, the compound as shown in formula (I), and a preparation method, pharmaceutical composition and use thereof as an estrogen receptor down-regulator in preparing drugs for treating estrogen receptor-positive breast cancer.

公开(公告)号：US20180079749A1

公开(公告)日：2018-03-22

申请号：US15561003

申请日：2016-03-24

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA,CHINESE ACADEMY OF SCIENCES ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Inventor： Jingkang SHEN ,  Tao MENG ,  Ting YU ,  Lanping MA ,  Xin WANG ,  Lin CHEN

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: Provided is a process of synthesizing a substituted pyridine and pyrimidine compound. Particularly, provided is a method for preparing a compound of formula III via a compound of formula II′, wherein the definition of each of groups is as described as the description. Compound with other methods, the method in the present invention has features of high yield and a result product being easier to separate.

公开(公告)号：US20210230164A1

公开(公告)日：2021-07-29

申请号：US16979202

申请日：2019-03-12

Applicant: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD. ,  MEDSHINE DISCOVERY INC.

Inventor： Kevin X CHEN ,  Xiaobing YAN ,  Jianglei HUANG ,  Yuekun NIE ,  Guoping HU ,  Jian LI ,  Shuhui CHEN ,  Jiaqiang DONG ,  Tie-Lin WANG

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00

Abstract: Disclosed is a novel class of MDM2-p53 inhibitor compounds having an imidaxopyrolone structure, and specifically disclosed are compounds represented by formulas (I-1) and (I-2) and pharmaceutically acceptable salts thereof. (I-1), (I-2)