公开(公告)号：US10807944B2

公开(公告)日：2020-10-20

申请号：US15301508

申请日：2015-03-30

申请人： University of Florida Research Foundation, Inc. ,  The Scripps Research Institute

发明人： Daiqing Liao ,  William R. Roush ,  Ryan L. Stowe

IPC分类号： C07C233/77 ,  A61K31/166 ,  C07C243/38 ,  A61K45/06 ,  C07C247/12 ,  C07D239/26 ,  C07D213/86 ,  A61K31/4406 ,  A61K31/505 ,  C07C233/78 ,  C07D213/44 ,  C07D239/48

摘要： The instant invention describes hydrazide-containing compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.

公开(公告)号：US10806738B2

公开(公告)日：2020-10-20

申请号：US16656271

申请日：2019-10-17

申请人： HMI Medical Innovations, LLC

发明人： Gerard M. Housey

IPC分类号： A61K31/5377 ,  C07D213/81 ,  C07D213/87 ,  C07D215/50 ,  C07D231/14 ,  C07D239/42 ,  C07D239/84 ,  C07D253/065 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  G01N33/574 ,  C07D239/48 ,  C07C243/38 ,  C07D213/77 ,  C07D213/86 ,  C07D215/38 ,  C07D253/075 ,  C07D403/12 ,  G01N33/573 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  G01N33/50 ,  A61K31/166 ,  A61K31/175 ,  A61K31/195 ,  A61K31/27 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/495 ,  A61K31/517

摘要： This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

公开(公告)号：US20200297644A1

公开(公告)日：2020-09-24

申请号：US16652387

申请日：2018-09-28

申请人： TriAct Therapeutics, Inc.

发明人： Thomas F. WHITE ,  Stephen M. NAVA

IPC分类号： A61K9/28 ,  A61K31/166 ,  A61K9/48 ,  A61K9/00 ,  A61K9/20 ,  A61K9/08 ,  A61K47/38 ,  A61K47/32 ,  A61K47/20 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/34

摘要： Disclosed herein are pharmaceutical compositions, formulations, and dosage forms and their use in the treatment of a cancer. Also disclosed herein are methods of treating a cancer in a subject in need thereof.

公开(公告)号：US10780072B2

公开(公告)日：2020-09-22

申请号：US15366819

申请日：2016-12-01

申请人： The Procter & Gamble Company ,  The Cleveland Clinic Foundation

发明人： Stanley Leon Hazen ,  Jose Carlos Garcia-Garcia ,  George Franklin Gerberick ,  John August Wos ,  David Thomas Stanton ,  Thomas Alfred Inglin ,  Michael Reilly ,  Angela Jane Deutsch ,  Jodie Michele Reed ,  David Blair Cody

IPC分类号： A61K31/26 ,  A61K31/166 ,  A61K31/216 ,  A61K31/22 ,  A61K31/325 ,  A61K31/351 ,  A61K45/06 ,  C07D213/04 ,  C07D295/13

摘要： The invention provides one or more methods of inhibiting the conversion of choline to trimethylamine (TMA) and lowering TMAO in an individual comprising administering to the individual one or more compositions comprising a compound set forth in Formula (I): wherein the compound is administered in an amount effective to inhibit formation of trimethylamine (TMA) from choline in the individual.

公开(公告)号：US20200281952A1

公开(公告)日：2020-09-10

申请号：US16879824

申请日：2020-05-21

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Alaric J. Dyckman ,  T.G. Murali Dhar ,  Hai-Yun Xiao ,  John L. Gilmore ,  Michael G. Yang ,  Zili Xiao ,  David Marcoux

IPC分类号： A61K31/695 ,  C07F7/08 ,  A61K31/135 ,  C07D215/14 ,  C07D241/04 ,  C07C323/29 ,  C07C251/38 ,  C07C251/42 ,  C07C251/44 ,  C07D209/46 ,  C07D213/38 ,  C07C275/26 ,  C07C217/74 ,  C07C323/25 ,  C07C235/46 ,  C07F9/54 ,  C07F9/572 ,  C07F9/09 ,  C07C215/42 ,  C07C217/52 ,  C07C217/58 ,  C07C219/24 ,  C07C233/41 ,  C07C233/65 ,  C07C251/50 ,  C07C251/52 ,  C07C251/54 ,  C07C271/34 ,  C07C317/28 ,  C07C317/32 ,  C07C321/16 ,  C07C321/22 ,  C07C321/28 ,  C07D213/32 ,  C07D213/69 ,  C07D213/70 ,  C07D215/12 ,  C07D217/24 ,  C07D231/12 ,  C07D231/20 ,  C07D239/26 ,  C07D241/12 ,  C07D277/24 ,  C07D305/08 ,  C07D309/06 ,  C07D309/12 ,  C07D311/58 ,  C07D311/76 ,  C07D319/20 ,  C07D333/16 ,  C07F9/117 ,  C07F9/62 ,  C07F9/6503 ,  C07F9/6509 ,  C07F9/655 ,  C07F9/6553 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K31/166 ,  A61K31/17 ,  A61K31/222 ,  A61K31/24 ,  A61K31/27 ,  A61K31/337 ,  A61K31/351 ,  A61K31/352 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/661

摘要： Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

公开(公告)号：US10745350B2

公开(公告)日：2020-08-18

申请号：US15748827

申请日：2016-07-30

申请人： CALGENT BIOTECHNOLOGY CO., LTD.

发明人： Yun Yen ,  Jing-ping Liou ,  Shiow-lin Pan

IPC分类号： A61K31/122 ,  A61K31/40 ,  A61K31/166 ,  A61K31/70 ,  C07D207/04 ,  A61K45/06 ,  A61P35/00 ,  C07D295/135 ,  C07D295/13 ,  C07C311/29 ,  C07C237/34 ,  C07D213/40 ,  C07C225/30 ,  C07C255/58 ,  C07D209/08 ,  C07D209/44 ,  C07D215/38 ,  C07D215/40 ,  A61K33/24 ,  A61K31/7048 ,  C07C235/54 ,  A61P25/14 ,  A61P25/28 ,  A61P3/10 ,  C07C237/48

摘要： The invention relates to new compounds with low cytotoxicity for blocking ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of treating disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders and autoimmune disorders and metabolic disorders.

公开(公告)号：US20200215047A1

公开(公告)日：2020-07-09

申请号：US16631422

申请日：2018-07-13

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

发明人： Yan Xu ,  Pei Tang ,  Marta Megan Wells

IPC分类号： A61K31/452 ,  A61K31/166 ,  A61K31/485 ,  A61K31/495 ,  A61P25/36 ,  A61P25/04

摘要： Compounds and methods for modulating the activity of receptors are disclosed. Some of the compounds modulate the activity of glycine receptors. Certain embodiments of the compounds are useful for treatment of pain, treatment of opioid addiction, and/or reduction of side effects attributable to opioid use.

公开(公告)号：US20200215039A1

公开(公告)日：2020-07-09

申请号：US16736081

申请日：2020-01-07

申请人： Curis, Inc.

发明人： Xiong Cai ,  Haixiao Zhai ,  Chengjung Lai ,  Changgeng Qian ,  Rudi Bao

IPC分类号： A61K31/4365 ,  C07D241/10 ,  C07D213/30 ,  A61K31/166 ,  C07D495/04

摘要： The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

公开(公告)号：US20200172901A1

公开(公告)日：2020-06-04

申请号：US16790788

申请日：2020-02-14

申请人： INSTITUT CURIE ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  ONXEO ,  INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE ,  UINVERSITE PARIS-SUD 11

发明人： MARIE DUTREIX ,  WAEL JDEY

IPC分类号： C12N15/11 ,  A61K45/06 ,  A61K31/711 ,  A61K31/166 ,  A61P35/00 ,  A61K31/55 ,  A61K31/713 ,  A61K31/454 ,  A61K31/502 ,  C12N15/117 ,  A61K31/4184

摘要： The present invention relates to the combination of a PARP inhibitor with a Dbait molecule for treating cancer.

公开(公告)号：US10646479B2

公开(公告)日：2020-05-12

申请号：US16586328

申请日：2019-09-27

申请人： Florida A&M University

发明人： Elizabeth Henderson ,  Tiffany Wilson Ardley ,  Kinfe Ken Redda ,  Madhavi Gangapuram

IPC分类号： A61K31/44 ,  A61K31/166 ,  A61P35/00 ,  C07D211/98 ,  A61K31/337 ,  A61K31/7068 ,  A61K31/704 ,  A61K31/4745 ,  A61K31/353 ,  A61K39/395 ,  A61K31/517

摘要： Disclosed herein is the use of N-(4-iodobenzoylamino)-5-ethyl-1,2,3,6-tetra-hydropyridine as a treatment for cancer.