公开(公告)号：US20240043443A1

公开(公告)日：2024-02-08

申请号：US18228452

申请日：2023-07-31

Applicant: CASE WESTERN RESERVE UNIVERSITY ,  BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM ,  UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION

Inventor： Sanford Markowitz ,  James K.V. Willson ,  Bruce Posner ,  Joseph Ready ,  Yongyou Zhang ,  Hsin-Hsiung Tai ,  Monica Antczak ,  Stanton Gerson ,  KiBeom Bae ,  Sung Yeun Yang ,  Amar Desai

IPC: C07D495/04 ,  C07C311/21 ,  C07D213/71 ,  C07D213/73 ,  C07D213/75 ,  C07D213/76 ,  C07D215/08 ,  C07D237/20 ,  C07D405/12 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D207/263 ,  C07D275/03 ,  C07D209/08 ,  C07D277/46 ,  C07D295/185 ,  A61K31/4365 ,  A61K31/519

CPC classification number: C07D495/04 ,  C07C311/21 ,  C07D213/71 ,  C07D213/73 ,  C07D213/75 ,  C07D213/76 ,  C07D215/08 ,  C07D237/20 ,  C07D405/12 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D207/263 ,  C07D275/03 ,  C07D209/08 ,  C07D277/46 ,  C07D295/185 ,  A61K31/4365 ,  A61K31/519 ,  C07C2601/14

Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.

公开(公告)号：US20230167078A1

公开(公告)日：2023-06-01

申请号：US17920679

申请日：2021-04-20

Applicant: Bayer Aktiengesellschaft ,  Deutsches Krebsforschungszentrum

Inventor： Norbert SCHMEES ,  Ulrike ROEHN ,  Dennis KIRCHHOFF ,  Kirstin PETERSEN ,  Thi Thanh Uyen NGUYEN ,  Mareike GREES ,  Nicolas WERBECK ,  Ulf BOEMER ,  Benjamin BADER ,  Detlef STOECKIGT ,  Dirk KOSEMUND ,  Rienk OFFRINGA ,  Corinna LINK ,  Katrin NOWAK-REPPEL

IPC: C07D277/46 ,  C07D417/06 ,  C07D417/12 ,  C07D487/04 ,  C07D417/14 ,  C07K16/28 ,  C07D417/10 ,  C07D471/08 ,  A61P35/00

CPC classification number: C07D277/46 ,  C07D417/06 ,  C07D417/12 ,  C07D487/04 ,  C07D417/14 ,  C07K16/2818 ,  C07K16/2827 ,  C07D417/10 ,  C07D471/08 ,  A61P35/00 ,  C07B2200/07

Abstract: The present invention covers aminothiazole compounds of general formula (I), in which R1, R2, R3 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase zeta (DGKζ) regulated disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20190231887A1

公开(公告)日：2019-08-01

申请号：US16255947

申请日：2019-01-24

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Alan Hornsby DAVIDSON ,  Alan Hastings DRUMMOND ,  Lindsey Ann NEEDHAM

IPC: A61K47/54 ,  C07D277/46 ,  C07D471/04 ,  C07C237/22 ,  C07D215/233 ,  C07D213/73

CPC classification number: A61K47/542 ,  A61K47/54 ,  C07C237/22 ,  C07C2601/08 ,  C07D213/73 ,  C07D215/233 ,  C07D277/46 ,  C07D471/04

Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

公开(公告)号：US10047040B2

公开(公告)日：2018-08-14

申请号：US15502512

申请日：2015-08-27

Applicant: Elanco Tiergesundheit AG

Inventor： Noelle Gauvry ,  Chouaib Tahtaoui

IPC: C07C311/08 ,  C07F7/08 ,  C07F5/02 ,  C07D295/155 ,  C07D333/24 ,  C07D231/12 ,  C07D213/61 ,  C07D231/56 ,  C07D213/56 ,  C07D239/30 ,  C07D239/26 ,  C07D277/30 ,  C07D213/84 ,  C07D333/28 ,  C07C311/21 ,  C07C311/14 ,  C07D309/06 ,  C07D249/08 ,  C07D277/64 ,  C07D277/60 ,  C07D277/56 ,  C07D285/135 ,  C07D333/78 ,  C07D277/46 ,  C07D277/54 ,  C07D263/50 ,  C07D275/03 ,  C07D317/66 ,  C07D209/08 ,  C07D215/06 ,  C07D487/04 ,  C07D237/26

CPC classification number: C07C311/08 ,  C07C235/56 ,  C07C307/10 ,  C07C311/09 ,  C07C311/10 ,  C07C311/14 ,  C07C311/21 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/40 ,  C07C2602/42 ,  C07D209/08 ,  C07D213/26 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/84 ,  C07D215/06 ,  C07D231/12 ,  C07D231/20 ,  C07D231/56 ,  C07D237/26 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D249/08 ,  C07D249/12 ,  C07D263/50 ,  C07D275/03 ,  C07D277/30 ,  C07D277/46 ,  C07D277/54 ,  C07D277/56 ,  C07D277/60 ,  C07D277/62 ,  C07D277/64 ,  C07D279/12 ,  C07D285/135 ,  C07D295/155 ,  C07D295/185 ,  C07D295/26 ,  C07D309/06 ,  C07D317/66 ,  C07D333/24 ,  C07D333/28 ,  C07D333/78 ,  C07D487/04 ,  C07F5/025 ,  C07F7/081 ,  C07F7/0812

Abstract: The present invention relates to a new compound of formula (I) wherein the variables have the meaning as indicated in the claims; or an enantiomer or salt thereof. The compounds of formula (I) are useful in the control of parasites, in particular endoparasites, in and on vertebrates.

公开(公告)号：US20180222874A1

公开(公告)日：2018-08-09

申请号：US15748515

申请日：2016-07-27

Applicant: Sanford Burnham Prebys Medical Discovery Institute

Inventor： Daniel Kelly ,  Richard Vega ,  Hampton Sessions ,  Teresa Leone ,  Byungyong Ahn ,  Satyamaheshwar Peddibhotla

IPC: C07D277/46 ,  A61K31/426 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/496 ,  A61K31/541 ,  C07D417/12 ,  A61K31/4439 ,  C07D417/04 ,  C07D277/82 ,  A61K45/06 ,  A61P3/10 ,  A61P3/04

CPC classification number: C07D277/46 ,  A61K31/426 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  A61P3/04 ,  A61P3/10 ,  C07D277/82 ,  C07D295/185 ,  C07D417/04 ,  C07D417/12

Abstract: Formulations and methods for reducing blood glucose and/or increasing insulin signaling in a subject have been developed. The formulations include SBI-477 and compounds based on SBI-477 i.e., SBI-477 analogs (collectively, SBI-477 compounds) and/or Mondo family inhibitors, in an effective amount to inhibit intracellular lipid accumulation and/or increase cellular glucose uptake when compared to levels in a control subject not administered the composition. Also disclosed are methods of reducing intracellular lipid accumulation and/or increase glucose uptake in a subject in need thereof. The method includes administering to the subject an effective amount of SBI-477 compounds and/or Mondo family inhibitor to reducing intracellular lipid accumulation and/or increase glucose uptake in the subject. Also disclosed are method for treating one or more Myc-driven cancers, including neuroblastoma, lung squamous cell carcinoma/lung adenocarcinoma, liver hepatocellular carcinoma, colon adenocarcinoma, acute myeloid leukemia, and breast invasive carcinoma.

公开(公告)号：US20180170863A1

公开(公告)日：2018-06-21

申请号：US15579143

申请日：2016-06-03

Applicant: LEAD PHARMA HOLDING B.V. ,  SANOFI

Inventor： Joseph Maria Gerardus Barbara CALS ,  Vera DE KIMPE ,  Sander Bernardus NABUURS ,  Cosimo Damiano CADICAMO ,  Jaap Gerardus Henricus LEMMERS

IPC: C07C317/32 ,  A61K31/167 ,  C07D233/61 ,  A61K31/4164 ,  C07D231/12 ,  A61K31/415 ,  C07D277/54 ,  A61K31/426 ,  C07D417/12 ,  A61K31/4439 ,  C07D333/36 ,  A61K31/381 ,  C07D409/04 ,  A61K31/4436 ,  C07D213/72 ,  A61K31/4402 ,  C07D263/32 ,  A61K31/421 ,  C07D249/08 ,  A61K31/4196 ,  C07D271/06 ,  A61K31/4245

CPC classification number: C07C317/32 ,  A61K31/167 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/4402 ,  A61K31/4436 ,  A61K31/4439 ,  C07C311/20 ,  C07C317/44 ,  C07C2601/02 ,  C07D213/72 ,  C07D213/75 ,  C07D231/12 ,  C07D233/61 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/46 ,  C07D277/54 ,  C07D333/36 ,  C07D409/04 ,  C07D417/12 ,  Y02A50/409

Abstract: Compounds according to Formula I: or a pharmaceutically acceptable salt thereof wherein: A1 is NR1 or CR1, with R1 being H or methyl, with methyl, if present, optionally being substituted with one or more F; the cyclopropyl moiety can be optionally substituted with one or more methyl and one or more F; A2-A5 are N or CR2-CR5, respectively, with the proviso that no more than two of the four positions A in A2-A5 can be simultaneously N; R2-R5 are independently H, halogen, amino, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-6)alkyl; R6 and R7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R2 and R3 together is carbonyl, all alkyl groups, if present, optionally being substituted with one or more F; R8 is H or C(1-6)alkyl; R9 is selected from the group consisting of Formula II, III, IV and V The compounds can be used as inhibitors of RORγ and are useful for the treatment of RORγ mediated diseases.

公开(公告)号：US09938236B2

公开(公告)日：2018-04-10

申请号：US14759385

申请日：2013-12-27

Applicant: DREXEL UNIVERSITY ,  BARUCH S. BLUMBERG INSTITUTE ,  ARBUTUS BIOPHARMA, INC.

Inventor： Xiaodong Xu ,  Ju-Tao Guo ,  Tong Xiao ,  Yanming Du ,  Timothy Block ,  Simon David Peter Baugh ,  Hong Ye

IPC: C07C311/16 ,  C07D213/75 ,  C07D213/76 ,  C07D309/04 ,  C07D215/38 ,  C07D215/42 ,  C07D217/24 ,  C07D319/18 ,  C07D231/40 ,  C07D231/42 ,  C07D239/26 ,  C07D261/14 ,  C07D263/48 ,  C07D263/50 ,  C07D203/26 ,  C07D263/58 ,  C07D205/04 ,  C07D277/46 ,  C07D277/52 ,  C07D211/96 ,  C07D295/26 ,  C07D295/30 ,  C07D213/40 ,  C07D305/08 ,  C07C309/89 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/20 ,  C07C311/48 ,  C07C233/66 ,  C07C317/14 ,  C07D295/32 ,  C07D319/16

CPC classification number: C07C311/16 ,  C07B2200/07 ,  C07C233/66 ,  C07C309/89 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/20 ,  C07C311/48 ,  C07C317/14 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D203/26 ,  C07D205/04 ,  C07D211/96 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D215/38 ,  C07D215/42 ,  C07D217/24 ,  C07D231/40 ,  C07D231/42 ,  C07D239/26 ,  C07D261/14 ,  C07D263/48 ,  C07D263/50 ,  C07D263/58 ,  C07D277/46 ,  C07D277/52 ,  C07D295/26 ,  C07D295/30 ,  C07D295/32 ,  C07D305/08 ,  C07D309/04 ,  C07D319/16 ,  C07D319/18

Abstract: The present invention provides novel compounds of formula (I) and methods of use thereof. In certain embodiments, the compounds of the invention are useful as nucleocapsid assembly inhibitors. In other embodiments, the compounds of the invention are useful as pregenomic RNA encapsidation inhibitors of Hepatitis B virus (HBV). In yet other embodiments, the compounds of the invention are useful for the treatment of viral infection, including HBV and related viral infections.

公开(公告)号：US09890117B2

公开(公告)日：2018-02-13

申请号：US15187163

申请日：2016-06-20

Applicant: Northwestern University ,  The General Hospital Corporation

Inventor： Richard B. Silverman ,  Hua Wang ,  Mohammad Khanfar ,  Aleksey G. Kazantsev

IPC: C07C311/21 ,  C07C311/16 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D213/85 ,  C07D217/04 ,  C07D207/16 ,  C07C317/44 ,  C07C323/49 ,  C07C323/42 ,  C07C257/18 ,  C07C255/60 ,  C07D295/26 ,  C07D305/06 ,  C07C311/29 ,  C07D213/76 ,  C07D213/80 ,  C07D223/04 ,  C07D237/20 ,  C07D239/42 ,  C07D261/14 ,  C07D271/113 ,  C07D277/46 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C323/62 ,  C07C311/47 ,  C07C317/22 ,  C07C317/34 ,  C07C323/20 ,  C07C235/60

CPC classification number: C07C311/21 ,  C07B2200/07 ,  C07C235/60 ,  C07C255/60 ,  C07C257/18 ,  C07C311/16 ,  C07C311/29 ,  C07C311/46 ,  C07C311/47 ,  C07C317/22 ,  C07C317/34 ,  C07C317/40 ,  C07C317/44 ,  C07C317/48 ,  C07C323/20 ,  C07C323/42 ,  C07C323/49 ,  C07C323/62 ,  C07C2601/02 ,  C07D207/16 ,  C07D213/75 ,  C07D213/76 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D213/85 ,  C07D217/04 ,  C07D223/04 ,  C07D237/20 ,  C07D239/42 ,  C07D261/14 ,  C07D271/113 ,  C07D277/46 ,  C07D295/26 ,  C07D305/06 ,  C07D311/16 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.

公开(公告)号：US09845332B2

公开(公告)日：2017-12-19

申请号：US15599769

申请日：2017-05-19

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Roland Gendron ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07D498/08 ,  C07D263/56 ,  C07D213/81 ,  C07D249/12 ,  C07D261/12 ,  C07D333/40 ,  C07D277/46 ,  C07D213/79 ,  C07D213/80 ,  C07D237/04 ,  C07D413/12 ,  C07D413/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/422 ,  A61K31/42 ,  C07D413/06 ,  C07D239/36 ,  C07D207/34 ,  C07D498/04 ,  C07D471/04 ,  C07D409/06 ,  C07D405/12 ,  C07D403/06 ,  C07D403/04 ,  C07D401/06 ,  C07D401/04 ,  C07D333/70 ,  C07D307/68 ,  C07D277/56 ,  C07D271/06 ,  C07D263/34 ,  C07D261/20 ,  C07D261/18 ,  C07D257/04 ,  C07D249/18 ,  C07D249/10 ,  C07D249/04 ,  C07D241/24 ,  C07D239/34 ,  C07D237/24 ,  C07D233/90 ,  C07D233/26 ,  C07D231/14 ,  C07D249/08

CPC classification number: C07D498/08 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/04 ,  C07D237/24 ,  C07D239/34 ,  C07D239/36 ,  C07D241/24 ,  C07D249/04 ,  C07D249/08 ,  C07D249/10 ,  C07D249/12 ,  C07D249/18 ,  C07D257/04 ,  C07D261/12 ,  C07D261/18 ,  C07D261/20 ,  C07D263/34 ,  C07D263/56 ,  C07D271/06 ,  C07D277/46 ,  C07D277/56 ,  C07D307/68 ,  C07D333/40 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D498/04

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US20170298082A1

公开(公告)日：2017-10-19

申请号：US15507375

申请日：2015-08-27

Applicant: Asceneuron SA

Inventor： Anna QUATTROPANI ,  Santosh S. KULKARNI ,  Awadut Gajendra GIRI

IPC: C07D513/04 ,  A61K31/454 ,  C07D417/12 ,  C07D413/14 ,  C07D413/12 ,  C07D405/14 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  C07D285/135 ,  C07D277/46 ,  A61K31/5377 ,  A61K31/519 ,  A61K31/517 ,  A61K31/506 ,  A61K31/501 ,  A61K31/498 ,  A61K31/497 ,  A61K31/496 ,  C07D417/14 ,  C07D487/04

CPC classification number: C07D513/04 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D277/46 ,  C07D285/135 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  A61K2300/00

Abstract: The disclosure relates to compounds of formula (I) useful in the treatment of tauopathies and Alzheimer's disease wherein A, R, W, Q, n, and m are described herein.