公开(公告)号：US20240269127A1

公开(公告)日：2024-08-15

申请号：US18608261

申请日：2024-03-18

Applicant: Hinova Pharmaceuticals Inc.

Inventor： Xing Wei ,  Tongtao Kuang ,  Jiang Chen ,  Chaowu Ai ,  Xinghai Li

IPC: A61K31/47 ,  A61K9/20 ,  A61K9/28 ,  C07D215/36

CPC classification number: A61K31/47 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2095 ,  A61K9/2866 ,  C07D215/36

Abstract: This patent document provides a sustained-release formulation comprising 1-40 parts of a quinoline compound, 100-300 parts of a filler, 50-200 parts of a sustained-release material and optionally 0.5-4 parts of a lubricant. Also provided are methods of treating diseases with the sustained-release formulation.

公开(公告)号：US11591301B2

公开(公告)日：2023-02-28

申请号：US16967077

申请日：2019-01-31

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Wu Du ,  Wen Ren ,  Haibin Lv ,  Haibo Li ,  Kun Wen ,  Jinyun He ,  Dekun Qin ,  Xinghai Li ,  Yuanwei Chen

IPC: C07D271/08 ,  C07D413/12

Abstract: A compound is represented by formula (I). A pharmaceutical composition contains the compound of formula (I). The compound is used in the preparation of an indoleamine-2,3-dioxygenase (IDO) inhibitor drug. The compound exhibits inhibition effect on IDO protease and metabolizes stably in the body. The compound or pharmaceutical composition thereof can be used for preparing an IDO inhibitor drug, and can also be used for preparing a drug for preventing and/or treating diseases having IDO-mediated tryptophan metabolic pathway pathological features.

公开(公告)号：US11447477B2

公开(公告)日：2022-09-20

申请号：US16956581

申请日：2018-12-20

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Wu Du ,  Chaowu Ai ,  Yu Li ,  Kun Wen ,  Haibin Lv ,  Wen Ren ,  Jinyun He ,  Dekun Qin ,  Xinghai Li ,  Yuanwei Chen

IPC: A61P35/00 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P27/12 ,  A61P31/18 ,  A61P37/02 ,  C07D413/12 ,  C07D413/14 ,  A61P3/00

Abstract: Provided is a compound represented by formula (I). Also provided are a pharmaceutical composition containing the compound of formula (I) and use of the compound in preparing indoleamine-2,3-dioxygenase (IDO) inhibitor drugs. The compound or the pharmaceutical composition thereof can be used for preparing drugs for preventing and/or treating diseases having pathological features of IDO-mediated tryptophan metabolic pathways.

公开(公告)号：US11926618B2

公开(公告)日：2024-03-12

申请号：US17753162

申请日：2020-08-20

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Wu Du ,  Yu Li ,  Haibo Li ,  Yuanwei Chen ,  Chengzhi Zhang ,  Xinghai Li

IPC: C07D403/12 ,  A61K31/53 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/14 ,  A61P5/16 ,  A61P9/10 ,  C07D253/075

CPC classification number: C07D403/12 ,  C07B2200/05

Abstract: A compound of formula (I) or an optical isomer thereof, and pharmaceutically acceptable salts, prodrugs, aquo-complexes or non-aqueous-solvent complexes thereof are provided. Experiments prove that, compared with a control compound MGL-3196, the compound of formula (I), which is obtained through specific substitution sites and specific substitution types, is higher in agonist activity to THR-beta and significantly improved in selectivity on THR-beta/THR-alpha. The compound can be used in preparing THR-beta agonist and drugs for treating adaption diseases (including dyslipidemia, hypercholesteremia, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease) applicable to the THR-beta agonist.

公开(公告)号：US11891379B2

公开(公告)日：2024-02-06

申请号：US17054080

申请日：2019-05-06

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Wu Du ,  Yu Li ,  Kun Wen ,  Xinghai Li ,  Yuanwei Chen

IPC: A61K31/506 ,  C07D403/12

CPC classification number: C07D403/12 ,  C07B2200/05

Abstract: This disclosure provides a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, hydrates or solvates thereof. In formula (I), R1-R18 are independently selected from hydrogen and deuterium respectively, but not all are hydrogen at the same time. The compound and salts, hydrates or solvates thereof can be used as FAK inhibitors, and used in the preparation of anti-cancer drugs, and compared with the undeuterated control compound Defactinib, the compound has significantly improved metabolic stability and pharmacokinetic properties.

公开(公告)号：US20210137890A1

公开(公告)日：2021-05-13

申请号：US17142440

申请日：2021-01-06

Applicant: Hinova Pharmaceuticals Inc.

Inventor： Xinghai Li ,  Yuanwei Chen

IPC: A61K31/4166 ,  A61P35/00

Abstract: Provided herein is a compound of Formula I having androgen receptor antagonistic properties and methods of using the compound to more efficiently and efficaciously reduce the concentration of prostate specific antigen (PSA) and treat male hormone-related diseases such as prostate cancer, breast cancer, alopecia, hair loss, acne and adolescent acne. Also provided are methods of reducing the plasma concentration of prostate specific antigen (PSA) in a subject with elevated PSA comprising administering to the subject a therapeutically effective amount of the compound.

公开(公告)号：US20250051347A1

公开(公告)日：2025-02-13

申请号：US18293289

申请日：2022-07-29

Applicant: Hinova Pharmaceuticals, Inc.

Inventor： Wu Du ,  Xinghai Li ,  Kun Wen ,  Dekun Qin ,  Shaohua Zhang ,  Song Chen ,  Jingyi Duan ,  Haibin Lv ,  Haibo Li ,  Yu Li ,  Jinyun He ,  Muyang Chen ,  Shijuan Liu ,  Yiwei Fu ,  Yikai Guan ,  Zhilin Tu

IPC: C07D491/107 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D519/00

Abstract: A compound as shown in formula I, or an optical isomer thereof, a solvate thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, a mixture form thereof, a metabolite thereof, a metabolic precursor thereof, or an isotope substitute form thereof. TB is a target recognition/binding portion, L is a linking portion, and U is a ubiquitin protease recognition/binding portion, the three portions being connected by means of chemical bonds. The compound can significantly down-regulate mutated androgen receptor (AR) proteins, and has good inhibitory activity on prostate cancer cell lines. The compound of formula I can be used for preparation of a protein degradation targeted chimera for targeted regulation of androgen receptors, and a drug for treating diseases correlated with regulation by androgen receptors, and has particularly good application prospects in drugs for treating prostate cancers and breast cancers.

公开(公告)号：US12162878B2

公开(公告)日：2024-12-10

申请号：US17160302

申请日：2021-01-27

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Lei Fan ,  Fei Wang ,  Xiaoquan Wu ,  Kexin Xu ,  Ke Chen ,  Tongchuan Luo ,  Shaohua Zhang ,  Yongxu Huo ,  Zhilin Tu ,  Xinghai Li ,  Yuanwei Chen

IPC: C07D471/04 ,  A61K45/06 ,  C07D519/00

Abstract: The compound of formula (I) has a good inhibitory effect on the proliferation of human prostate cancer cells CWR22RV1 and breast cancer cells; and combined use of the compound with an androgen receptor inhibitor HC-1119 significantly enhances the inhibitory effect on prostate cancer cells, and the inhibitory effect increases with increased concentration. The compound of formula (I) can not only be used independently to prepare an antineoplastic agent but can also be used in combination with other agents having antineoplastic effects, such as an androgen receptor inhibitor, or other targeting drugs etc., to prepare an antineoplastic agent having stronger therapeutic effects, especially an agent for treating prostate cancer and breast cancer.

公开(公告)号：US10450274B2

公开(公告)日：2019-10-22

申请号：US15781997

申请日：2016-12-06

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Lei Fan ,  Wu Du ,  Xinghai Li ,  Yuanwei Chen ,  Kexin Xu ,  Ke Chen ,  Shaohua Zhang ,  Tongchuan Luo

IPC: C07D215/36 ,  A61K31/47 ,  A61K31/4709 ,  C07D401/04 ,  C07D401/12

Abstract: Quinoline compounds and salts, hydrates or solvates serving as a selective uric acid reabsorption inhibitor, can be used in the treatment of hyperuricemia and gout by promoting uric acid to excrete from the body and reducing serum uric acid. Such compounds have the effect of reducing the uric acid in the animal body and human body.

公开(公告)号：US12194040B2

公开(公告)日：2025-01-14

申请号：US17418678

申请日：2019-12-24

Applicant: HINOVA PHARMACEUTICALS INC.

Inventor： Wu Du ,  Yu Li ,  Kun Wen ,  Xinghai Li ,  Yuanwei Chen

IPC: A61K31/506 ,  A61K39/395 ,  A61P35/00 ,  C07D403/12

Abstract: A deuterated compound as represented by formula (I) or an optical isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a hydrate, or a solvate thereof are presented. Compared with a compound before deuteration, the deuterated compound shows better pharmacokinetics, higher maximum plasma drug concentration, higher exposure, and longer half-life, and has more excellent metabolic performance. The deuterated compound can effectively inhibit FAK activity, and has good application prospect in preparation of FAK inhibitors and/or drugs for treating cancer. In addition, the use of the deuterated compound in combination with an anti-cancer drug (such as a PD-1 inhibitor) can achieve a synergistic effect, thereby significantly improving the tumor suppression effect, and providing a better choice for clinical cancer treatment.