公开(公告)号：US10988440B2

公开(公告)日：2021-04-27

申请号：US16740466

申请日：2020-01-12

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Shiming Peng

IPC: C07C255/34 ,  A61P25/28 ,  A61P3/04 ,  C07D277/30 ,  C07D277/46 ,  C07D213/57 ,  C07D237/14 ,  C07D239/36 ,  C07D241/24 ,  C07D251/16 ,  C07D241/52 ,  C07D471/04 ,  C07D213/80 ,  C07D241/20 ,  C07D285/08 ,  C07D295/185 ,  C07D241/12 ,  C07D249/08 ,  C07D261/12 ,  C07D239/42 ,  C07D215/233 ,  C07D277/56 ,  C07D249/12 ,  C07D211/82 ,  C07D487/04 ,  C07D235/08 ,  C07D231/14 ,  C07D209/08 ,  C07D239/26 ,  C07D233/56 ,  C07D277/24 ,  C07D261/08 ,  C07D307/46 ,  C07D257/04 ,  C07D213/75 ,  C07D277/64 ,  C07C255/43

Abstract: The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

公开(公告)号：US20190183842A1

公开(公告)日：2019-06-20

申请号：US16283117

申请日：2019-02-22

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Shiming Peng

IPC: A61K31/277 ,  A61K9/00 ,  A61K45/06 ,  A61P27/02

CPC classification number: A61K31/277 ,  A61K9/0051 ,  A61K31/397 ,  A61K31/426 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4402 ,  A61K31/4453 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/535 ,  A61K45/06 ,  A61P27/02 ,  A61K2300/00

Abstract: The invention provides use of entacapone, an entacapone derivative or a stereoisomer, hydride, or pharmaceutically-acceptable salt thereof, in a person in need thereof, to treat or inhibit macular degeneration or age-related macular degeneration, and related compostions.

公开(公告)号：US20200148628A1

公开(公告)日：2020-05-14

申请号：US16740466

申请日：2020-01-12

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Shiming Peng

IPC: C07C255/34 ,  C07C255/43 ,  C07D277/64 ,  C07D213/75 ,  C07D257/04 ,  C07D307/46 ,  C07D261/08 ,  C07D277/24 ,  C07D233/56 ,  C07D239/26 ,  C07D209/08 ,  C07D231/14 ,  C07D235/08 ,  C07D487/04 ,  C07D211/82 ,  C07D249/12 ,  C07D277/56 ,  C07D215/233 ,  C07D239/42 ,  C07D261/12 ,  C07D249/08 ,  C07D241/12 ,  C07D295/185 ,  C07D285/08 ,  C07D241/20 ,  C07D213/80 ,  C07D471/04 ,  C07D241/52 ,  C07D251/16 ,  C07D241/24 ,  C07D239/36 ,  C07D237/14 ,  C07D213/57 ,  C07D277/46 ,  C07D277/30 ,  A61P3/04 ,  A61P25/28

Abstract: The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

公开(公告)号：US20180118665A1

公开(公告)日：2018-05-03

申请号：US15853653

申请日：2017-12-22

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Shiming Peng

IPC: C07C255/34 ,  A61P3/04 ,  A61P25/28

CPC classification number: C07C255/34 ,  A61P3/04 ,  A61P25/28 ,  C07C255/43 ,  C07D209/08 ,  C07D211/82 ,  C07D213/57 ,  C07D213/75 ,  C07D213/80 ,  C07D215/233 ,  C07D231/14 ,  C07D233/56 ,  C07D235/08 ,  C07D237/14 ,  C07D239/26 ,  C07D239/36 ,  C07D239/42 ,  C07D241/12 ,  C07D241/20 ,  C07D241/24 ,  C07D241/52 ,  C07D249/08 ,  C07D249/12 ,  C07D251/16 ,  C07D257/04 ,  C07D261/08 ,  C07D261/12 ,  C07D277/24 ,  C07D277/30 ,  C07D277/46 ,  C07D277/56 ,  C07D277/64 ,  C07D285/08 ,  C07D295/185 ,  C07D307/46 ,  C07D471/04 ,  C07D487/04

Abstract: The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

公开(公告)号：US20210238127A1

公开(公告)日：2021-08-05

申请号：US17233488

申请日：2021-04-18

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Shiming Peng

IPC: C07C255/34 ,  A61P25/28 ,  A61P3/04 ,  C07D277/30 ,  C07D277/46 ,  C07D213/57 ,  C07D237/14 ,  C07D239/36 ,  C07D241/24 ,  C07D251/16 ,  C07D241/52 ,  C07D471/04 ,  C07D213/80 ,  C07D241/20 ,  C07D285/08 ,  C07D295/185 ,  C07D241/12 ,  C07D249/08 ,  C07D261/12 ,  C07D239/42 ,  C07D215/233 ,  C07D277/56 ,  C07D249/12 ,  C07D211/82 ,  C07D487/04 ,  C07D235/08 ,  C07D231/14 ,  C07D209/08 ,  C07D239/26 ,  C07D233/56 ,  C07D277/24 ,  C07D261/08 ,  C07D307/46 ,  C07D257/04 ,  C07D213/75 ,  C07D277/64 ,  C07C255/43

Abstract: The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

公开(公告)号：US10682329B2

公开(公告)日：2020-06-16

申请号：US16018095

申请日：2018-06-26

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Gang Zhi ,  Jijie Chai ,  Shiming Peng ,  Nannan Hou

IPC: A61K31/277 ,  A61K45/06 ,  C12Q1/6883

Abstract: Obesity is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-obesity medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-obesity medicament.

公开(公告)号：US10004715B2

公开(公告)日：2018-06-26

申请号：US14147531

申请日：2014-01-04

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Gang Zhi ,  Jijie Chai ,  Shiming Peng ,  Nannan Hou

IPC: A61K31/277 ,  A61K45/06

CPC classification number: A61K31/277 ,  A61K45/06 ,  C12Q1/6883 ,  C12Q2600/156 ,  A61K2300/00

Abstract: Obesity is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-obesity medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-obesity medicament.

公开(公告)号：US10980766B2

公开(公告)日：2021-04-20

申请号：US16283117

申请日：2019-02-22

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Shiming Peng

IPC: A61K31/277 ,  A61P27/02 ,  A61K9/00 ,  A61K45/06 ,  A61K31/397 ,  A61K31/426 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4402 ,  A61K31/4453 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/535

Abstract: The invention provides use of entacapone, an entacapone derivative or a stereoisomer, hydride, or pharmaceutically-acceptable salt thereof, in a person in need thereof, to treat or inhibit macular degeneration or age-related macular degeneration, and related compostions.

公开(公告)号：US10532976B2

公开(公告)日：2020-01-14

申请号：US15853653

申请日：2017-12-22

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Shiming Peng

IPC: C07C255/34 ,  A61P25/28 ,  A61P3/04 ,  C07D277/30 ,  C07D277/46 ,  C07D213/57 ,  C07D237/14 ,  C07D239/36 ,  C07D241/24 ,  C07D251/16 ,  C07D241/52 ,  C07D471/04 ,  C07D213/80 ,  C07D241/20 ,  C07D285/08 ,  C07D295/185 ,  C07D241/12 ,  C07D249/08 ,  C07D261/12 ,  C07D239/42 ,  C07D215/233 ,  C07D277/56 ,  C07D249/12 ,  C07D211/82 ,  C07D487/04 ,  C07D235/08 ,  C07D231/14 ,  C07D209/08 ,  C07D239/26 ,  C07D233/56 ,  C07D277/24 ,  C07D261/08 ,  C07D307/46 ,  C07D257/04 ,  C07D213/75 ,  C07D277/64 ,  C07C255/43

Abstract: The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

公开(公告)号：US20180303788A1

公开(公告)日：2018-10-25

申请号：US16018095

申请日：2018-06-26

Applicant: National Institute of Biological Sciences, Beijing

Inventor： Niu Huang ,  Gang Zhi ,  Jijie Chai ,  Shiming Peng ,  Nannan Hou

IPC: A61K31/277 ,  A61K45/06

Abstract: Obesity is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-obesity medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-obesity medicament.