公开(公告)号：US20210244717A1

公开(公告)日：2021-08-12

申请号：US17018196

申请日：2020-09-11

Applicant: Valo Early Discovery, Inc. ,  Genentech, Inc.

Inventor： Kenneth W. Bair ,  Timm R. Baumeister ,  Alexandre J. Buckmelter ,  Karl H. Clodfelter ,  Peter Dragovich ,  Francis Gosselin ,  Bingsong Han ,  Jian Lin ,  Dominic J. Reynolds ,  Bruce Roth ,  Chase C. Smith ,  Zhongguo Wang ,  Po-Wai Yuen ,  Xiaozhang Zheng

IPC: A61K31/4355 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D487/04 ,  C07D491/048

Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:

公开(公告)号：US20210206755A1

公开(公告)日：2021-07-08

申请号：US17124778

申请日：2020-12-17

Applicant: Valo Early Discovery, Inc.

Inventor： Xiaozhang Zheng ,  Pui Yee Ng ,  Aleksandra Rudnitskaya ,  David R. Lancia, JR.

IPC: C07D413/06 ,  C07D267/22

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 Formulae I or Formula II: where R, L, X1, X2, X3, X4, X5, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US20210186940A1

公开(公告)日：2021-06-24

申请号：US17130704

申请日：2020-12-22

Applicant: Valo Early Discovery, Inc.

Inventor： Xiaozhang Zheng ,  Pui Yee Ng ,  Mary-Margaret Zablocki

IPC: A61K31/438 ,  C07D401/04 ,  C07D221/20 ,  C07D401/06 ,  C07D209/54

Abstract: The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.

公开(公告)号：US10829460B2

公开(公告)日：2020-11-10

申请号：US16449675

申请日：2019-06-24

Applicant: Valo Early Discovery, Inc.

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

IPC: C07D265/36 ,  C07D413/12 ,  C07D413/06 ,  C07D401/04 ,  C07D279/16 ,  C07D491/107 ,  C07D413/10 ,  C07D471/04 ,  C07D417/06 ,  C07D513/04 ,  C07D487/04 ,  C07D265/34 ,  C07D279/14

Abstract: The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, L, X, W, Y1, Y2, Y3, and Y4 are described herein, useful as inhibitors of zinc-dependent histone deacetylases (HDACs) and in the treatment of diseases or disorders associated with HDACs.

公开(公告)号：US20220073452A1

公开(公告)日：2022-03-10

申请号：US17238529

申请日：2021-04-23

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：US20210246147A1

公开(公告)日：2021-08-12

申请号：US17022906

申请日：2020-09-16

Applicant: Valo Early Discovery, Inc.

Inventor： Kenneth W. Bair ,  Timm R. Baumeister ,  Alexandre J. Buckmelter ,  Karl H. Clodfelter ,  Bingsong Han ,  Judith D. Kuntz ,  Jian Lin ,  Dominic J. Reynolds ,  Chase C. Smith ,  Zhongguo Wang ,  Xiaozhang Zheng

IPC: C07D519/00 ,  C07D215/48 ,  C07D471/04 ,  C07D513/04 ,  A61K31/4545 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/497 ,  C07D495/04

Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below: Formula (I)

公开(公告)号：US20220363651A1

公开(公告)日：2022-11-17

申请号：US17238321

申请日：2021-04-23

Applicant: Valo Early Discovery, Inc.

Inventor： Xiaozhang Zheng ,  Pui Yee Ng ,  Bingsong Han ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Cuixian Liu ,  Heather Davis ,  Aleksandra Rudnitskaya ,  David R. Lancia, JR. ,  Kenneth W. Bair ,  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 disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US20210139439A1

公开(公告)日：2021-05-13

申请号：US17066385

申请日：2020-10-08

Applicant: Valo Early Discovery, Inc.

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

IPC: C07D265/36 ,  C07D413/12 ,  C07D413/06 ,  C07D401/04 ,  C07D279/16 ,  C07D491/107 ,  C07D413/10 ,  C07D471/04 ,  C07D417/06 ,  C07D513/04 ,  C07D487/04 ,  C07D265/34 ,  C07D279/14

Abstract: The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers or thereof, wherein R1, R2, R2′, L, X, W, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US10988450B2

公开(公告)日：2021-04-27

申请号：US16567007

申请日：2019-09-11

Applicant: Valo Early Discovery, Inc.

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

IPC: C07D491/08 ,  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 disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US10829461B2

公开(公告)日：2020-11-10

申请号：US16654704

申请日：2019-10-16

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: A61K31/553 ,  C07D267/14 ,  C07D407/06 ,  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 disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.