公开(公告)号：US12221419B2

公开(公告)日：2025-02-11

申请号：US18192703

申请日：2023-03-30

Applicant: Florida State University Research Foundation, Incorporated.

Inventor： James H. Frederich ,  Megan M. Solans

IPC: C07C13/68 ,  C07C22/08 ,  C07C25/22 ,  C07C35/44 ,  C07C43/215 ,  C07C49/753 ,  C07C49/755 ,  C07D215/06 ,  C07D215/227 ,  C07D307/79

Abstract: In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein is versatile polyene cyclization strategy that exploits conjugated β-ionyl derivatives. Photomediated disruption of the extended π-system within these chromophores unveils a contra-thermodynamic polyene that engages in a Heck-type cyclization to afford [4.4.1]-propellanes. The connectivity of overbred polycycles generated from this process is controlled by the position of the requisite C-Halide bond. Thus, compared to conventional biomimetic polyene cyclization, this approach allows for complete control of regiochemistry and facilitates incorporation of both electron-rich and electron-deficient (hetero)aryl groups. This strategy was successfully applied to the total synthesis of abietanes such as, for example, taxodione and salviasperanol, two isomeric abietane-type diterpenes that previously could not be prepared along the same synthetic pathway.

公开(公告)号：US20240140912A1

公开(公告)日：2024-05-02

申请号：US18192703

申请日：2023-03-30

Applicant: Florida State University Research Foundation, Incorporated.

Inventor： James H. Frederich ,  Megan M. Solans

IPC: C07D215/227 ,  C07C13/68 ,  C07C22/08 ,  C07C25/22 ,  C07C35/44 ,  C07C43/215 ,  C07C49/753 ,  C07C49/755 ,  C07D215/06 ,  C07D307/79

CPC classification number: C07D215/227 ,  C07C13/68 ,  C07C22/08 ,  C07C25/22 ,  C07C35/44 ,  C07C43/215 ,  C07C49/753 ,  C07C49/755 ,  C07D215/06 ,  C07D307/79 ,  C07C2603/40

Abstract: In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein is versatile polyene cyclization strategy that exploits conjugated β-ionyl derivatives. Photomediated disruption of the extended π-system within these chromophores unveils a contra-thermodynamic polyene that engages in a Heck-type cyclization to afford [4.4.1]-propellanes. The connectivity of overbred polycycles generated from this process is controlled by the position of the requisite C-Halide bond. Thus, compared to conventional biomimetic polyene cyclization, this approach allows for complete control of regiochemistry and facilitates incorporation of both electron-rich and electron-deficient (hetero)aryl groups. This strategy was successfully applied to the total synthesis of abietanes such as, for example, taxodione and salviasperanol, two isomeric abietane-type diterpenes that previously could not be prepared along the same synthetic pathway.

公开(公告)号：US20230278962A1

公开(公告)日：2023-09-07

申请号：US18145902

申请日：2022-12-23

Applicant: THE KATHOLIEKE UNIVERSITEIT LEUVEN ,  SpringWorks Therapeutics, Inc. ,  VIB vzw

Inventor： Bart VANDERHOYDONCK ,  Arnaud MARCHAND ,  Aurélie CANDI ,  Matthias VERSELE

IPC: C07D223/16 ,  C07D215/227 ,  C07D471/04 ,  A61P35/00 ,  A61K45/06 ,  A61K31/55 ,  A61K31/4704 ,  A61K31/4375

CPC classification number: C07D223/16 ,  A61K31/4375 ,  A61K31/4704 ,  A61K31/55 ,  A61K45/06 ,  A61P35/00 ,  C07D215/227 ,  C07D471/04

Abstract: The present disclosure relates to novel compounds, to said compounds for use as a medicine, more in particular for the prevention or treatment of diseases mediated by activity of YAP/TAZ-TEAD transcription, yet more in particular for the prevention or treatment of cancer or fibrosis. The present disclosure also relates to a method for the prevention or treatment of said diseases comprising the use of the novel compounds.

公开(公告)号：US11713299B2

公开(公告)日：2023-08-01

申请号：US17089239

申请日：2020-11-04

Applicant: Global Blood Therapeutics, Inc.

Inventor： Ming Yu ,  Zhe Li

IPC: C07D471/04 ,  C07D215/38 ,  C07D401/12 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D215/20 ,  C07D215/227 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12

CPC classification number: C07D215/38 ,  C07D215/20 ,  C07D215/227 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052

Abstract: The present disclosure provides compounds of Formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.




where R1, alk, R2, Z1, Z2, X, R3, R4, B, a, and b are as described herein.

公开(公告)号：US20230180761A1

公开(公告)日：2023-06-15

申请号：US18166601

申请日：2023-02-09

Applicant: CORTEVA AGRISCIENCE LLC

Inventor： RONALD J. HEEMSTRA ,  RONALD ROSS, JR. ,  KYLE A. DEKORVER ,  KAITLYN GRAY ,  DANIEL I. KNUEPPEL ,  PETER VEDNOR ,  TIMOTHY P. MARTIN ,  JOSEPH D. ECKELBARGER ,  JOHN F. DAEUBLE, SR. ,  RICKY HUNTER ,  DAVID A. DEMETER ,  TONY K. TRULLINGER ,  ERICH W. BAUM ,  ZOLTAN L. BENKO ,  NAKYEN CHOY ,  GARY D. CROUSE ,  FANGZHENG LI ,  JEFFREY NISSEN ,  MONICA B. OLSON ,  MICHELLE RIENER ,  THOMAS C. SPARKS ,  FRANK J. WESSELS ,  MAURICE C. YAP

IPC: A01N53/00 ,  C07C255/46 ,  C07C255/57 ,  C07C255/60 ,  C07C259/10 ,  C07D213/84 ,  C07D213/89 ,  C07D215/227 ,  C07C271/28 ,  C07C271/66 ,  C07D215/38 ,  C07D231/56 ,  C07D233/36 ,  C07C311/08 ,  C07C311/46 ,  C07D235/30 ,  C07C317/28 ,  C07C317/40 ,  C07C317/50 ,  C07C323/41 ,  C07C323/42 ,  C07C323/59 ,  C07C331/12 ,  C07C381/10 ,  C07D205/04 ,  C07C237/42 ,  C07D207/452 ,  C07C255/29 ,  C07D209/49 ,  C07D213/75 ,  C07D213/81 ,  C07D309/14 ,  C07D231/12 ,  C07D331/04 ,  C07D333/36 ,  C07D249/08 ,  C07D207/10 ,  C07D285/06 ,  C07D295/32 ,  C07D305/08 ,  C07D207/273 ,  C07D233/80 ,  C07D261/12 ,  C07D263/26 ,  C07D277/36 ,  C07D307/33 ,  C07D333/48 ,  C07C237/22 ,  C07D213/56 ,  C07D277/30 ,  C07D307/52 ,  C07D333/60 ,  A01N37/22 ,  A01N37/34 ,  A01N41/10 ,  A01N43/40 ,  A01N43/60 ,  A01N43/653 ,  A01N43/707 ,  A01N43/82 ,  A01N43/90 ,  C07C233/63 ,  C07C233/65 ,  C07C317/14 ,  C07D241/20 ,  C07D253/07 ,  C07D487/04

CPC classification number: A01N53/00 ,  C07C255/46 ,  C07C255/57 ,  C07C255/60 ,  C07C259/10 ,  C07D213/84 ,  C07D213/89 ,  C07D215/227 ,  C07C271/28 ,  C07C271/66 ,  C07D215/38 ,  C07D231/56 ,  C07D233/36 ,  C07C311/08 ,  C07C311/46 ,  C07D235/30 ,  C07C317/28 ,  C07C317/40 ,  C07C317/50 ,  C07C323/41 ,  C07C323/42 ,  C07C323/59 ,  C07C331/12 ,  C07C381/10 ,  C07D205/04 ,  C07C237/42 ,  C07D207/452 ,  C07C255/29 ,  C07D209/49 ,  C07D213/75 ,  C07D213/81 ,  C07D309/14 ,  C07D231/12 ,  C07D331/04 ,  C07D333/36 ,  C07D249/08 ,  C07D207/10 ,  C07D285/06 ,  C07D295/32 ,  C07D305/08 ,  C07D207/273 ,  C07D233/80 ,  C07D261/12 ,  C07D263/26 ,  C07D277/36 ,  C07D307/33 ,  C07D333/48 ,  C07C237/22 ,  C07D213/56 ,  C07D277/30 ,  C07D307/52 ,  C07D333/60 ,  A01N37/22 ,  A01N37/34 ,  A01N41/10 ,  A01N43/40 ,  A01N43/60 ,  A01N43/653 ,  A01N43/707 ,  A01N43/82 ,  A01N43/90 ,  C07C233/63 ,  C07C233/65 ,  C07C317/14 ,  C07D241/20 ,  C07D253/07 ,  C07D487/04 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).

公开(公告)号：US20230113085A1

公开(公告)日：2023-04-13

申请号：US17439735

申请日：2020-03-13

Applicant: The General Hospital Corporation

Inventor： Xu Wu ,  Pranab Maiti ,  Chandrasekhar Abbineni ,  Krishna Chaitanya Talluri ,  Sunil Kumar Panigrahi ,  Gopala Krishna Jarugumilli ,  Yang Sun

IPC: C07D471/04 ,  C07C229/58 ,  C07C255/58 ,  C07C211/56 ,  C07D249/08 ,  C07D213/74 ,  C07D213/80 ,  C07C229/44 ,  C07C211/55 ,  C07D215/227 ,  C07D275/06 ,  C07C229/48 ,  C07D207/16 ,  C07D239/42 ,  C07D241/28 ,  C07D211/62 ,  C07D205/04 ,  C07D231/56 ,  C07D235/18 ,  C07D317/32 ,  C07D233/61 ,  C07D401/12 ,  C07D209/08 ,  C07D401/06 ,  C07D295/135 ,  C07C237/40 ,  C07C311/44

Abstract: The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

公开(公告)号：US11485708B2

公开(公告)日：2022-11-01

申请号：US16905979

申请日：2020-06-19

Applicant: CHEMOCENTRYX, INC.

Inventor： Viengkham Malathong ,  Pingchen Fan ,  Christopher Lange ,  Venkat Reddy Mali ,  Darren J. McMurtrie ,  Sreenivas Punna ,  Howard S. Roth ,  Rajinder Singh ,  Ju Yang ,  Penglie Zhang

IPC: C07D217/04 ,  A61K45/06 ,  C07D401/12 ,  A61K31/4725 ,  C07C217/58 ,  A61K31/137 ,  C07D211/58 ,  A61K31/4468 ,  A61K31/4545 ,  C07C229/16 ,  A61K31/197 ,  C07D207/06 ,  A61K31/40 ,  C07D319/18 ,  A61K31/357 ,  C07D213/64 ,  A61K31/4402 ,  C07D215/227 ,  A61K31/4704 ,  C07C309/14 ,  A61K31/185 ,  A61K31/472

Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1a, R1b, R1c, R1d, R2a, R2b, R3, R3a, R4, R5, R6, R7, R8 and the subscript n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

公开(公告)号：US11447471B2

公开(公告)日：2022-09-20

申请号：US16625446

申请日：2018-06-22

Applicant: KYOWA KIRIN CO., LTD.

Inventor： Tomohiro Danjo ,  Hiroki Yamada ,  Takahiro Nakajima

IPC: A61P35/00 ,  C07D263/56 ,  C07D263/57 ,  C07D267/14 ,  C07D277/64 ,  C07D307/83 ,  C07D307/86 ,  C07D313/08 ,  C07D405/12 ,  C07D213/63 ,  C07D213/643 ,  C07D213/75 ,  C07D215/227 ,  C07D215/233 ,  C07D215/26 ,  C07D215/38 ,  C07D215/40 ,  C07D217/02 ,  C07D311/58 ,  C07D311/68 ,  C07D333/66 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D491/052

Abstract: An object of the present invention is to provide an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The α,β-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: [wherein, “A” represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO2—, —NRX1— (wherein, RX1 represents hydrogen atom or lower alkyl), —CHRX2— (wherein, RX2 represents hydrogen atom or hydroxy), —CH═CH—, −CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

公开(公告)号：US11312668B2

公开(公告)日：2022-04-26

申请号：US17060801

申请日：2020-10-01

Applicant: AbbVie Deutschland GmbH & Co. KG ,  AbbVie Inc.

Inventor： Wilfried Braje ,  Katarina Britze ,  Justin D. Dietrich ,  Anais Jolit ,  Johannes Kaschel ,  Johanna Klee ,  Tanja Lindner

IPC: C07D213/74 ,  C07D215/227 ,  C07D239/26 ,  C07D239/42 ,  C07D307/36 ,  C07D307/81 ,  C07D311/58 ,  C07D405/04 ,  C07D409/04 ,  C07D471/04 ,  C07D495/04 ,  C07B63/04 ,  C07B43/06 ,  C07F5/02 ,  C07B43/04 ,  C07B37/04 ,  C07C41/46 ,  C07C67/62 ,  C07C209/90 ,  C07C213/10 ,  C07C231/22 ,  C07C253/32 ,  C07C269/08 ,  C07C273/18 ,  C07C303/42 ,  C07C319/26 ,  C07D205/04 ,  C07D207/34 ,  C07D209/08 ,  C07D209/48 ,  C07D211/06

Abstract: The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose.

公开(公告)号：US11261170B2

公开(公告)日：2022-03-01

申请号：US16879204

申请日：2020-05-20

Applicant: Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.

Inventor： Jiawang Zhu ,  Zhiquan Song ,  Dong Long ,  Lichun Wang ,  Jingyi Wang

IPC: C07D401/04 ,  A61P1/16 ,  C07D215/14 ,  C07D215/227 ,  C07D215/36 ,  C07D215/38 ,  C07D333/56 ,  C07D413/04

Abstract: The invention relates to an aromatic compound, pharmaceutical composition comprising the same, and a method for preparing the compound and an intermediate thereof. The invention also relates to use of the compound for the manufacture of a medicament for the prevention or treatment of a PPAR-related disease.