公开(公告)号：US20220106325A1

公开(公告)日：2022-04-07

申请号：US17263453

申请日：2019-07-26

Applicant: California Institute of Technology ,  The Regents Of The University Of California ,  1200 Pharma LLC

Inventor： Brendan M. O'Boyle ,  Justin A. Hilf ,  Scott C. Virgil ,  Alexander W. Sun ,  Brian M. Stoltz ,  Dylan Conklin ,  Martina S. McDermott ,  Neil A. O'Brien ,  Michael J. Palazzolo ,  Dennis Slamon ,  Michael D. Bartberger

IPC: C07D491/107 ,  C07D413/14 ,  C07D498/10 ,  C07D401/14 ,  C07D495/10 ,  A61P35/00

Abstract: The present disclosure provides compounds and compositions that are CDK inhibitors selective for CDK4 and/or CDK6, and methods of use thereof.

公开(公告)号：US11242350B2

公开(公告)日：2022-02-08

申请号：US16979833

申请日：2019-03-11

Applicant: Escalier Biosciences B.V.

Inventor： Raju Mohan ,  John Nuss ,  Jason Harris ,  Shendong Yuan

IPC: C07D487/10 ,  C07D205/04 ,  C07D211/24 ,  C07D471/10 ,  C07D495/10 ,  C07D211/54 ,  A61P17/06 ,  A61P37/06 ,  A61P19/02 ,  A61P1/00

Abstract: Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing ROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

公开(公告)号：US11220514B2

公开(公告)日：2022-01-11

申请号：US16624491

申请日：2018-06-19

Applicant: UNION therapeutics A/S

Inventor： Allan Carsten Dahl ,  Johan Eriksson Bajtner ,  Esben Paul Krogh Olsen ,  Bjørn Metzler

IPC: C07D495/10 ,  B01J21/16

Abstract: The present invention relates to novel methods for the preparation of 1,3-benzodioxole heterocyclic compounds of formula (I). The compounds are useful as PDE4 inhibitors.

公开(公告)号：US20210371429A1

公开(公告)日：2021-12-02

申请号：US17182744

申请日：2021-02-23

Applicant: NOVARTIS AG

Inventor： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  John William Giraldes ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Martin Sendzik ,  Troy Douglas Smith ,  Bakary-Barry Toure ,  Sarah Williams

IPC: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

Abstract: The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US11130751B2

公开(公告)日：2021-09-28

申请号：US16499421

申请日：2018-03-29

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： Patrick René Angibaud ,  Olivier Alexis Georges Querolle ,  Didier Jean-Claude Berthelot ,  Christophe Meyer ,  Matthieu Philippe Victor Willot ,  Lieven Meerpoel ,  Thierry François Alain Jean Jousseaume

IPC: C07D413/14 ,  C07D495/10 ,  A61P35/00

Abstract: The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

公开(公告)号：US11052076B2

公开(公告)日：2021-07-06

申请号：US16619573

申请日：2018-06-12

Applicant: UCB BIOPHARMA SRL

Inventor： Gareth Neil Brace ,  Rose Elizabeth Chappell ,  Hervé Jean Claude Deboves ,  Anne Marie Foley ,  Gregory Foulkes ,  Elizabeth Pearl Jones ,  Fabien Claude Lecomte ,  Joanna Rachel Quincey ,  Monika-Sarah Elisabeth Dorothea Schulze ,  Matthew Duncan Selby ,  Adam Peter Smalley ,  Richard David Taylor ,  Robert James Townsend ,  Zhaoning Zhu

IPC: C07D471/10 ,  C07D487/10 ,  C07D495/10 ,  C07D491/20 ,  A61K31/4439 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  C07D491/107 ,  C07D519/00

Abstract: A series of substituted spirocyclic 2-oxoindoline derivatives, and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

公开(公告)号：US10988441B2

公开(公告)日：2021-04-27

申请号：US16689252

申请日：2019-11-20

Applicant: Valo Early Discovery, Inc.

Inventor： Kenneth W. Bair ,  Nicholas Barczak ,  Bingsong Han ,  David R. Lancia, Jr. ,  Cuixian Liu ,  Matthew W. Martin ,  Pui Yee Ng ,  Aleksandra Rudnitskaya ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Xiaozhang Zheng

IPC: C07C259/06 ,  A61K31/185 ,  C07D221/20 ,  A61K31/438 ,  A61K31/277 ,  C07D209/44 ,  A61K31/4035 ,  C07D295/155 ,  A61K31/451 ,  C07D471/10 ,  A61K31/435 ,  C07D487/10 ,  A61K31/407 ,  C07D495/10 ,  A61K31/397 ,  C07D235/14 ,  A61K31/4184 ,  C07D233/68 ,  A61K31/417 ,  C07D213/56 ,  A61K31/44 ,  C07D241/08 ,  A61K31/495 ,  C07D417/04 ,  A61K31/4439 ,  A61K31/5377 ,  C07D471/04 ,  C07D401/14 ,  C07D213/75 ,  C07D213/81 ,  C07D215/12 ,  C07D317/68 ,  C07D231/14 ,  C07D231/18 ,  C07D233/36 ,  C07D233/38 ,  C07D333/70 ,  C07D401/04 ,  C07D401/12 ,  C07D235/30 ,  C07D239/20 ,  C07D239/22 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D241/12 ,  C07D417/12 ,  C07D249/18 ,  C07D257/04 ,  C07D261/18 ,  C07D487/04 ,  C07D487/08 ,  C07D491/10 ,  C07D207/10 ,  C07D493/08 ,  C07D207/267 ,  C07D498/04 ,  C07D209/08 ,  C07D277/56 ,  C07D209/42 ,  C07D209/46 ,  C07D513/10 ,  C07D211/16 ,  C07D211/58 ,  C07D295/192 ,  C07D213/65 ,  C07D307/68

Abstract: The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.

公开(公告)号：US10947212B2

公开(公告)日：2021-03-16

申请号：US16203298

申请日：2018-11-28

Applicant: CANON KABUSHIKI KAISHA

Inventor： Yosuke Nishide ,  Naoki Yamada ,  Hiroki Ohrui ,  Hironobu Iwawaki ,  Satoru Shiobara ,  Tomona Yamaguchi ,  Tetsuo Takahashi ,  Masumi Itabashi ,  Hirokazu Miyashita ,  Jun Kamatani

IPC: H01L27/30 ,  H01L51/00 ,  H01L51/42 ,  H01L51/44 ,  C07D333/78 ,  C07D513/04 ,  C07D409/14 ,  C07D409/12 ,  C07D405/06 ,  C07D495/10 ,  C07D491/048 ,  C07D417/12 ,  C07D307/93 ,  C07D409/06 ,  C07D495/20 ,  C07D405/14 ,  C07D405/12

Abstract: The present invention provides an organic compound represented by general formula [1] described in claims. In general formula [1], Ar1 and Ar2 are each independently selected from an aryl group and a heteroaryl group. In general formula [1], R1 to R3 are each a hydrogen atom or a substituent. R4 is an electron-withdrawing substituent. X1 is oxygen or sulfur. Y1 to Y3 are each independently selected from a carbon atom and a nitrogen atom.

公开(公告)号：US20210053976A1

公开(公告)日：2021-02-25

申请号：US16979833

申请日：2019-03-11

Applicant: Escalier Biosciences B.V.

Inventor： Raju MOHAN ,  John NUSS ,  Jason HARRIS ,  Shendong YUAN

IPC: C07D487/10 ,  C07D495/10 ,  C07D471/10 ,  C07D211/24 ,  C07D205/04 ,  A61P17/06 ,  A61P37/06 ,  A61P1/00 ,  A61P19/02

Abstract: Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing NROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

公开(公告)号：US20210009540A1

公开(公告)日：2021-01-14

申请号：US17031815

申请日：2020-09-24

Applicant: Valo Early Discovery, Inc.

Inventor： Xiaozhang Zheng ,  Pui Yee Ng ,  Bingsong Han ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Cuixian Liu ,  Aleksandra Rudnitskaya ,  David R. Lancia, JR. ,  David S. Millan ,  Matthew W. Martin

IPC: C07D267/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/04 ,  C07D267/12 ,  C07D243/14 ,  C07D291/08 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D498/04 ,  C07D498/08 ,  C07D493/08 ,  C07D413/08 ,  C07D491/107 ,  C07D495/10

Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.