公开(公告)号：US20200369598A1

公开(公告)日：2020-11-26

申请号：US16988027

申请日：2020-08-07

申请人： XW LABORATORIES INC.

发明人： JIA-NING XIANG ,  XUESONG XU ,  XUAN ZHANG

IPC分类号： C07C69/78 ,  C07C255/57 ,  C07D213/79 ,  C07D213/80 ,  C07D309/12 ,  C07C271/22 ,  C07C271/34 ,  C07C69/612 ,  C07D317/64 ,  C07D333/38 ,  C07C229/08 ,  C07C233/47 ,  C07D207/16 ,  C07D307/68 ,  C07B59/00 ,  C07C69/76 ,  C07C69/24 ,  C07C229/36 ,  C07C69/608 ,  C07C317/44 ,  C07D277/56 ,  C07D211/46 ,  C07C69/738 ,  C07C69/28 ,  C07C69/22 ,  C07C69/34 ,  C07C69/618 ,  C07C69/74 ,  C07C69/96 ,  C07C229/34 ,  C07C317/14 ,  C07D207/12 ,  C07D211/44 ,  C07D277/30

摘要： Provided are prodrugs of gamma-hydroxybutyric acid as well as compositions and uses thereof.

公开(公告)号：US10807948B2

公开(公告)日：2020-10-20

申请号：US15556153

申请日：2016-03-04

申请人： PELOTON THERAPEUTICS, INC.

发明人： Darryl David Dixon ,  Jonas Grina ,  John A. Josey ,  James P. Rizzi ,  Stephen T. Schlachter ,  Eli M. Wallace ,  Bin Wang ,  Paul Wehn ,  Rui Xu ,  Hanbiao Yang

IPC分类号： C07C317/22 ,  C07C317/24 ,  C07C255/47 ,  C07C255/54 ,  C07C317/36 ,  C07C317/38 ,  C07C317/44 ,  C07C43/23 ,  C07C217/58 ,  C07C43/295 ,  C07C35/00 ,  C07C323/65 ,  C07C317/32 ,  C07C317/46 ,  C07D213/74 ,  C07D309/10 ,  C07D213/85 ,  C07D309/14 ,  C07D221/04 ,  C07D335/02 ,  C07D249/04 ,  C07D249/08 ,  C07D231/14 ,  C07D333/20 ,  C07D231/56 ,  C07C235/40 ,  C07D207/12 ,  C07C251/42 ,  C07D207/48 ,  C07D209/12 ,  C07D211/42 ,  C07D295/096 ,  C07D211/44 ,  C07D211/76 ,  C07D211/96 ,  C07D213/30 ,  C07D213/52 ,  C07D305/06 ,  C07D305/14 ,  C07D307/20 ,  C07D307/52 ,  A61P35/00 ,  C07D211/94 ,  C07D213/89 ,  C07D265/30 ,  C07D305/08

摘要： Disclosed herein are substituted indane derivatives useful as HIF-2α inhibitors. Pharmaceutical compositions comprising said indane derivatives and methods of using said indane derivatives for treating proliferative diseases, such as renal cell carcinoma and von Hippel-Lindau disease, and other conditions associated with HIF-2α activity are also disclosed.

公开(公告)号：US10807946B2

公开(公告)日：2020-10-20

申请号：US16363825

申请日：2019-03-25

申请人： Metabasis Therapeutics, Inc.

发明人： Jorge E. Gomez-Galeno ,  Raja K. Reddy ,  Paul D. Van Poelje ,  Robert Huerta Lemus ,  Thanh Huu Nguyen ,  Matthew P. Grote ,  Qun Dang ,  Scott J. Hecker ,  Venkat Reddy Mali ,  Mingwei Chen ,  Zhili Sun ,  Serge Henri Boyer ,  Haiqing Li ,  William Craigo

IPC分类号： C07C309/15 ,  C07D317/66 ,  C07C309/11 ,  C07C317/44 ,  C07C323/62 ,  C07D209/20 ,  C07D213/53 ,  C07D498/04 ,  C07D471/04 ,  C07D413/04 ,  C07D409/12 ,  C07D405/04 ,  C07D333/38 ,  C07C307/02 ,  C07D307/81 ,  C07D307/68 ,  C07D277/66 ,  C07D263/56 ,  C07D261/08 ,  C07D235/30 ,  C07D213/75

摘要： The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof and pharmaceutical compositions comprising the same.

公开(公告)号：US10710061B2

公开(公告)日：2020-07-14

申请号：US16087582

申请日：2017-03-22

申请人： Nanyang Technological University

发明人： Choon-Hong Tan ,  Xinyi Ye ,  Lili Zong

IPC分类号： B01J31/22 ,  C07C315/02 ,  B01J31/02 ,  C07D403/12 ,  C07D401/12 ,  C07D333/18 ,  C07D333/34 ,  C07D277/76 ,  C07D213/71 ,  C07D405/12 ,  C07D235/28 ,  B01J27/051 ,  B01J27/18 ,  B01J35/00 ,  B01J37/12 ,  C07B53/00 ,  C07C317/06 ,  C07C279/16 ,  C07C317/14 ,  C07C317/24 ,  C07C317/44

摘要： D The present invention relates to ion pair catalysts (I) comprising the cationic bisguanidinium ligand (A) and diperoxomolybdate anion (B). The present invention also relates to ion pair catalysts (III) comprising the cationic bisguanidinium ligand (C) and peroxotungstate anion (D). It further relates to the use of the said catalysts in the manufacture of enantiomerically enriched sulfoxides.

公开(公告)号：US20200216490A1

公开(公告)日：2020-07-09

申请号：US16717830

申请日：2019-12-17

申请人： The Salk Institute for Biological Studies

发明人： Ronald M. Evans ,  Michael Downes

IPC分类号： C07K5/062 ,  C07D333/38 ,  C07C233/75 ,  C07C317/44 ,  C07C237/32 ,  C07C235/84 ,  C07C235/48 ,  C07C235/42 ,  C07C233/73 ,  C07C259/06 ,  C07C255/57 ,  C07D307/83 ,  C07D307/81 ,  C07D307/54 ,  C07D305/06 ,  C07D213/56 ,  C07D295/155 ,  C07D209/34 ,  C07D205/04 ,  C07C233/87 ,  C07D417/12 ,  C07D417/10 ,  C07D417/04 ,  C07D413/12 ,  C07D413/04 ,  C07D409/12 ,  C07D405/12 ,  C07D405/10 ,  C07D405/04 ,  C07D401/12 ,  C07D401/04 ,  C07D333/24 ,  C07D231/12 ,  C07D309/06 ,  C07D307/68 ,  C07D213/64 ,  C07D213/40 ,  C07D295/13 ,  C07D271/12 ,  C07D407/12 ,  C07D309/04

摘要： Provided herein are deuterated compounds and compositions useful in increasing PPARδ activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

公开(公告)号：US20200207691A1

公开(公告)日：2020-07-02

申请号：US16816777

申请日：2020-03-12

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education

发明人： Billy W. Day ,  Neil Hukriede

IPC分类号： C07C29/80 ,  B01D15/18 ,  C07C317/44 ,  C07C323/52 ,  C07C323/56 ,  C07C323/60 ,  C07C323/62 ,  C07C229/18

摘要： Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.

公开(公告)号：US10697977B2

公开(公告)日：2020-06-30

申请号：US15613065

申请日：2017-06-02

申请人： The Regents of The University of California

发明人： Lan Huang ,  Scott D. Rychnovsky ,  Clinton Yu ,  Eric James Novitsky ,  Craig Bryant Gutierrez

IPC分类号： C07C317/44 ,  G01N33/68 ,  C07C315/04 ,  B01D15/34 ,  G01N30/88

摘要： Provided herein is synthesis of a novel acidic acid residue targeting sulfoxide-containing MS-cleavable homobifunctional cross-linker. The novel mass spectrometry-cleavable cross-linking agents can be used in mass spectrometry to facilitate structural analysis of intra-protein interactions in proteins and inter-protein interactions in protein complexes. Also disclosed herein are data based on the novel MS-cleavable homobifunctional cross-linker that are complimentary to amine-reactive sulfoxide-containing MS-cleavable reagents.

公开(公告)号：US20200087239A1

公开(公告)日：2020-03-19

申请号：US16685335

申请日：2019-11-15

申请人： GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

发明人： Ivan William HEMEON ,  Brian Salvatore SAFINA ,  Daniel SUTHERLIN

IPC分类号： C07C62/38 ,  C07C69/757 ,  C07C62/34 ,  C07C229/48 ,  C07D211/22 ,  C07C317/44 ,  C07C323/61 ,  A61P25/00 ,  A61P29/00 ,  A61P17/04 ,  C07C313/04

摘要： The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RAA, n, ring A, X1, L, m, X2, R2, R3, R4, R5, X, and R6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

公开(公告)号：US10590074B2

公开(公告)日：2020-03-17

申请号：US15830244

申请日：2017-12-04

申请人： THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human Services, Office of Technology Transfer, National Institutes of Health

发明人： Amy Hauck Newman ,  Oluyomi M. Okunola-Bakare ,  Jianjing Cao

IPC分类号： C07C323/60 ,  A61K45/06 ,  A61K31/135 ,  C07C317/44 ,  C07C317/28 ,  C07C323/25 ,  C07D295/08 ,  C07D295/088 ,  C07D295/108 ,  C07D295/185

摘要： Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds.

公开(公告)号：US10550071B2

公开(公告)日：2020-02-04

申请号：US15897796

申请日：2018-02-15

申请人： Salk Institute for Biological Studies ,  Mitobridge, Inc.

发明人： Ronald M. Evans ,  Michael Downes ,  Thomas J. Baiga ,  Joseph P. Noel ,  Emi Kanakubo Embler ,  Weiwei Fan ,  John F. W. Keana ,  Mark G. Bock ,  Arthur F. Kluge ,  Mike A. Patane

IPC分类号： A61K31/381 ,  A61K31/5377 ,  A61K31/44 ,  A61K31/4025 ,  A61K31/422 ,  A61K31/341 ,  A61K31/427 ,  A61K31/164 ,  A61K31/4178 ,  C07C233/87 ,  C07C255/57 ,  C07C317/44 ,  C07C233/73 ,  C07C235/42 ,  C07C235/48 ,  C07C235/84 ,  C07C237/22 ,  C07C237/32 ,  C07D309/06 ,  C07D405/04 ,  C07D405/10 ,  C07D407/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D207/04 ,  C07D271/12 ,  C07D209/34 ,  C07D295/13 ,  C07D305/06 ,  C07D307/83 ,  C07D231/12 ,  C07D333/24 ,  C07D405/12 ,  C07D213/56 ,  C07D307/54 ,  C07C237/48 ,  C07C259/06

摘要： Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).