公开(公告)号：US20240023549A1

公开(公告)日：2024-01-25

申请号：US18253822

申请日：2021-11-22

Applicant: CORTEVA AGRISCIENCE LLC

Inventor： ANN BUYSSE ,  ERIN HANCOCK ,  SUSANA LOPEZ ,  BRIAN LOY ,  STACY T. MEYER ,  JEFF PETKUS ,  ADRIAN TLAHUEXT-ACA ,  WEIWEI WANG ,  PULAN YU

IPC: A01N37/52 ,  C07C257/12 ,  C07D213/75 ,  C07D213/40 ,  C07D295/195 ,  C07D217/06 ,  C07D215/08 ,  C07C323/41 ,  C07D333/20 ,  C07D209/12 ,  C07D317/28 ,  C07D317/58 ,  C07D233/64 ,  C07D491/107 ,  C07D209/44 ,  A01N43/40 ,  A01N43/84 ,  A01N43/42 ,  A01N43/36 ,  A01N43/60 ,  A01N43/10 ,  A01N43/38 ,  A01N43/28 ,  A01N43/30 ,  A01N43/50 ,  A01N43/90 ,  A01N43/44 ,  C07D205/04 ,  C07D211/32 ,  A01P3/00

CPC classification number: A01N37/52 ,  C07C257/12 ,  C07D213/75 ,  C07D213/40 ,  C07D295/195 ,  C07D217/06 ,  C07D215/08 ,  C07C323/41 ,  C07D333/20 ,  C07D209/12 ,  C07D317/28 ,  C07D317/58 ,  C07D233/64 ,  C07D491/107 ,  C07D209/44 ,  A01N43/40 ,  A01N43/84 ,  A01N43/42 ,  A01N43/36 ,  A01N43/60 ,  A01N43/10 ,  A01N43/38 ,  A01N43/28 ,  A01N43/30 ,  A01N43/50 ,  A01N43/90 ,  A01N43/44 ,  C07D205/04 ,  C07D211/32 ,  A01P3/00

Abstract: This disclosure relates to aryl amidines of Formula I and their use as fungicides.

公开(公告)号：US20210115008A1

公开(公告)日：2021-04-22

申请号：US16970169

申请日：2019-02-15

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Jonathan E. Wilson ,  Francois Brucelle ,  Julian R. Levell

IPC: C07D401/04 ,  C07D231/12 ,  C07D237/08 ,  C07D295/135 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D213/75 ,  C07D231/40 ,  C07D487/04 ,  C07D491/107 ,  C07D413/04 ,  C07D417/04 ,  C07D209/08 ,  C07D215/08

Abstract: Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

公开(公告)号：US10982337B2

公开(公告)日：2021-04-20

申请号：US15769460

申请日：2016-10-17

Applicant: SCHLUMBERGER TECHNOLOGY CORPORATION

Inventor： Lynne Patricia Crawford ,  Evgeny Borisovich Barmatov ,  Trevor Lloyd Hughes ,  Man Yi Ho

IPC: C23F11/04 ,  C09K8/54 ,  C07D209/08 ,  C07D209/14 ,  C07D215/06 ,  C07D215/08 ,  C07D295/03

Abstract: A corrosion inhibiting compound with a general structure A-B or A-X-B for inhibition of corrosion of steel in acidic solution. A comprises a heterocyclic ring system having a plurality of cyclic Carbon atoms and at least one cyclic Nitrogen atom, wherein the at least one cyclic Nitrogen atom is neutral under neutral conditions and protonatable under acidic conditions. B comprises at least two unsaturated Carbon atoms. B may comprise a ring system or a polymerisable group.

公开(公告)号：US20190255046A1

公开(公告)日：2019-08-22

申请号：US15998610

申请日：2017-02-15

Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS

Inventor： Alan KOZIKOWSKI ,  Sida SHEN ,  Joel BERGMAN ,  Irina GAISINA

IPC: A61K31/498 ,  A61P35/00 ,  A61P37/00 ,  A61P25/28 ,  C07D241/44 ,  A61K31/5415 ,  C07D279/16 ,  A61K31/47 ,  C07D215/08

Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.

公开(公告)号：US10315996B2

公开(公告)日：2019-06-11

申请号：US15579111

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

IPC: C07C311/20 ,  C07C317/44 ,  C07C317/50 ,  C07D207/06 ,  C07D209/08 ,  C07D211/16 ,  C07D211/26 ,  C07D211/60 ,  C07D213/75 ,  C07D213/82 ,  C07D215/08 ,  C07D217/02 ,  C07D223/16 ,  C07D231/40 ,  C07D241/04 ,  C07D261/08 ,  C07D277/46 ,  C07D285/135 ,  C07D295/13 ,  C07D295/192 ,  C07D307/52 ,  C07D333/36 ,  C07D417/04 ,  C07D495/04

Abstract: Compounds according to Formula I: or a pharmaceutically acceptable salt wherein: A1 is NR1 or CR1, with R1 herein; the cyclopropyl moiety with one or more methyl and one or more F; A2-A5 are N or CR2-CR5, with no more than two of the four positions A in A2-A5 can be simultaneously N; R2-R5 are described; R6 and R7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R6 and R7 together is carbonyl, all alkyl groups, if substituted with one or more F; R8 is H or C(1-6)alkyl; A9-A12 are N or CR9-CR12, with no more than two of the four positions A in A9-A12 can be simultaneously N; R9-R12 herein; R13 and R14 herein; or R13 and R14 fused forming a ring having 5 to 7 atoms by joining R13 being C(1-6)alkyl or C(2-6)alkenyl. The RORγ compounds can treat RORγ mediated diseases.

公开(公告)号：US20190135718A1

公开(公告)日：2019-05-09

申请号：US16055898

申请日：2018-08-06

Applicant: President and Fellows of Harvard College

Inventor： Junying Yuan ,  Emily P. Hsu

IPC: C07C35/37 ,  C07C33/38 ,  C07D233/02 ,  C07D211/78 ,  C07D498/08 ,  C07D495/04 ,  C07D417/12 ,  C07D405/06 ,  C07D403/12 ,  C07D403/06 ,  C07D333/20 ,  C07D307/52 ,  C07D277/46 ,  C07D231/56 ,  C07D231/12 ,  C07D231/06 ,  C07D215/08 ,  C07D211/90 ,  C07D209/08 ,  C07D277/18

Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.

公开(公告)号：US09914719B2

公开(公告)日：2018-03-13

申请号：US14467946

申请日：2014-08-25

Applicant: Astex Therapeutics Ltd.

Inventor： Gianni Chessari ,  Miles Stuart Congreve ,  Martyn Frederickson ,  Christopher William Murray ,  Eva Figueroa Navarro ,  Alison Jo-Anne Woolford ,  Maria Grazia Carr ,  Robert Downham ,  Michael Alistair O'Brien ,  Theresa Rachel Phillips ,  Andrew James Woodhead

IPC: A61K31/454 ,  A61K31/496 ,  A61K31/445 ,  A61K31/4035 ,  C07D401/12 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D217/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10 ,  C07C65/21

CPC classification number: C07D401/12 ,  C07C65/21 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D217/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10

Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.

公开(公告)号：US20170305824A1

公开(公告)日：2017-10-26

申请号：US15427699

申请日：2017-02-08

Applicant: President and Fellows of Harvard College

Inventor： Junying Yuan ,  Emily P. Hsu

IPC: C07C35/37 ,  C07C33/38 ,  C07D417/12 ,  C07D405/06 ,  C07D403/12 ,  C07D403/06 ,  C07D333/20 ,  C07D307/52 ,  C07D277/46 ,  C07D277/18 ,  C07D233/02 ,  C07D231/56 ,  C07D231/12 ,  C07D231/06 ,  C07D215/08 ,  C07D211/90 ,  C07D211/78 ,  C07D209/08 ,  C07D495/04 ,  C07D498/08

CPC classification number: C07C35/37 ,  C07C33/38 ,  C07D209/08 ,  C07D211/78 ,  C07D211/90 ,  C07D215/08 ,  C07D231/06 ,  C07D231/12 ,  C07D231/56 ,  C07D233/02 ,  C07D277/18 ,  C07D277/46 ,  C07D307/52 ,  C07D333/20 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D417/12 ,  C07D495/04 ,  C07D498/08

Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.

公开(公告)号：US09790233B2

公开(公告)日：2017-10-17

申请号：US14395021

申请日：2013-04-16

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 A. Posner ,  Joseph Ready ,  Yongyou Zhang ,  Hsin-Hsiung Tai ,  Monika Antczak ,  Stanton Gerson ,  KiBeom Bae ,  Sung Yeun Yang ,  Amar Desai

IPC: C07D495/04 ,  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 ,  C07C311/21

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

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：US20170275301A1

公开(公告)日：2017-09-28

申请号：US15464430

申请日：2017-03-21

Applicant: HELSINN HEALTHCARE SA

Inventor： Claudio Giuliano ,  Antoine Daina ,  Claudio Pietra

IPC: C07D513/04 ,  C07C311/47 ,  C07C317/42 ,  C07D209/08 ,  C07D403/12 ,  C07D215/06 ,  C07D215/10 ,  C07D401/12 ,  C07D215/58 ,  C07D215/08 ,  C07D405/06 ,  C07D213/34 ,  C07D311/76 ,  C07D295/088 ,  C07D307/87 ,  C07D231/56 ,  C07D239/48 ,  C07D233/64 ,  C07D235/14 ,  C07D213/76 ,  C07D237/20 ,  C07D209/44 ,  C07D417/12 ,  C07D409/12 ,  C07D317/34 ,  C07D417/10 ,  C07D487/04 ,  C07D223/16 ,  C07D405/04 ,  C07D495/04 ,  C07D471/04 ,  C07D405/12 ,  C07D241/04 ,  C07D217/04 ,  C07D217/10 ,  C07D471/08 ,  C07D413/12 ,  C07D241/12

CPC classification number: C07D513/04 ,  C07C311/47 ,  C07C317/14 ,  C07C317/26 ,  C07C317/42 ,  C07C317/44 ,  C07C2601/02 ,  C07D209/04 ,  C07D209/08 ,  C07D209/44 ,  C07D213/34 ,  C07D213/76 ,  C07D215/06 ,  C07D215/08 ,  C07D215/10 ,  C07D215/58 ,  C07D217/04 ,  C07D217/10 ,  C07D223/16 ,  C07D231/56 ,  C07D233/64 ,  C07D235/14 ,  C07D237/20 ,  C07D239/26 ,  C07D239/48 ,  C07D241/04 ,  C07D241/12 ,  C07D295/088 ,  C07D307/87 ,  C07D311/76 ,  C07D317/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D495/04

Abstract: Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.