公开(公告)号：US11339130B1

公开(公告)日：2022-05-24

申请号：US17032529

申请日：2020-09-25

Applicant: Blade Therapeutics, Inc.

Inventor： Brad Owen Buckman ,  John Beamond Nicholas ,  Shendong Yuan ,  Marc Adler ,  Kumaraswamy Emayan ,  Jingyuan Ma

IPC: C07D233/90 ,  C07D417/14 ,  C07C233/05 ,  C07D209/20 ,  C07D231/14 ,  C07D249/06 ,  C07D263/34 ,  C07D271/04 ,  C07D275/03 ,  C07D285/06 ,  C07D307/68 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  A61P11/00

Abstract: Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

公开(公告)号：US11292801B2

公开(公告)日：2022-04-05

申请号：US16312916

申请日：2017-06-29

Applicant: Blade Therapeutics, Inc.

Inventor： Brad Owen Buckman ,  Shendong Yuan ,  John Beamond Nicholas ,  Jingyuan Ma ,  Kumaraswamy Emayan ,  Marc Adler

IPC: C07D498/18 ,  A61P1/16 ,  A61P13/12 ,  A61P11/00 ,  C07D245/06 ,  C07D267/00 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D471/18 ,  C07D498/04

Abstract: Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to macrocyclic α-keto amide derivatives and their use as therapeutic agents.

公开(公告)号：US10590084B2

公开(公告)日：2020-03-17

申请号：US16083189

申请日：2017-03-08

Applicant: Blade Therapeutics, Inc.

Inventor： Brad Owen Buckman ,  John Beamond Nicholas ,  Shendong Yuan ,  Marc Adler

IPC: C07D223/12 ,  C07D225/02 ,  C07D211/58 ,  C07K5/062 ,  A61P19/04 ,  A61K38/00

Abstract: The present technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer which are associated or mediated, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is also applicable to cyclic keto-amide compounds which inhibit myofibroblast differentiation.

公开(公告)号：US20190194139A1

公开(公告)日：2019-06-27

申请号：US16083189

申请日：2017-03-08

Applicant: Blade Therapeutics, Inc.

Inventor： Brad Owen Buckman ,  John Beamond Nicholas ,  Shendong Yuan ,  Marc Adler

IPC: C07D223/12 ,  C07D225/02 ,  C07D211/58 ,  A61P19/04

CPC classification number: C07D223/12 ,  A61K38/00 ,  A61P19/04 ,  C07D211/58 ,  C07D225/02 ,  C07K5/06034

Abstract: The present technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer which are associated or mediated, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is also applicable to cyclic keto-amide compounds which inhibit myofibroblast differentiation.

公开(公告)号：US20220324814A1

公开(公告)日：2022-10-13

申请号：US17718728

申请日：2022-04-12

Applicant: Blade Therapeutics, Inc.

Inventor： Brad Owen Buckman ,  John Beamond Nicholas ,  Shendong Yuan ,  Marc Adler ,  Kumaraswamy Emayan ,  Jingyuan Ma

IPC: C07D233/90 ,  A61P11/00 ,  C07C233/05 ,  C07D209/20 ,  C07D231/14 ,  C07D249/06 ,  C07D263/34 ,  C07D271/04 ,  C07D275/03 ,  C07D285/06 ,  C07D307/68 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14

Abstract: Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

公开(公告)号：US20210347727A1

公开(公告)日：2021-11-11

申请号：US16624849

申请日：2018-06-19

Applicant: BLADE THERAPEUTICS, INC.

Inventor： Brad Owen Buckman ,  Shendong Yuan ,  John Beamond Nicholas ,  Jingyuan Ma ,  Kumaraswamy Emayan ,  Marc Adler

IPC: C07C233/78 ,  A61P19/04 ,  C07D311/84 ,  C07D265/38 ,  C07D319/24 ,  C07D209/90 ,  C07D307/91 ,  C07C233/62 ,  C07D317/68 ,  C07C233/76

Abstract: Small molecule calpain modulator compositions and pharmaceutical compositions can be prepared and used as therapeutic agents. Exemplary compositions include non-macrocyclic a-keto amide derivatives. The therarapeutic agents can be used for treating fibrotic disease or a resulting secondary disease state or condition. The small molecules can competitively bind with calpastatin and/or inhibit calpain through contact with CAPN1, CAPN2, and/or CAPN9 enzymes.

公开(公告)号：US10934261B2

公开(公告)日：2021-03-02

申请号：US16337377

申请日：2017-09-27

Applicant: Blade Therapeutics, Inc.

Inventor： Brad Owen Buckman ,  John Beamond Nicholas ,  Shendong Yuan ,  Marc Adler ,  Kumaraswamy Emayan ,  Jingyuan Ma

IPC: C07D233/90 ,  A61P11/00 ,  C07C233/05 ,  C07D209/20 ,  C07D231/14 ,  C07D249/06 ,  C07D263/34 ,  C07D271/04 ,  C07D275/03 ,  C07D285/06 ,  C07D307/68 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14

Abstract: Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

公开(公告)号：US10894776B2

公开(公告)日：2021-01-19

申请号：US16337377

申请日：2017-09-27

Applicant: Blade Therapeutics, Inc.

Inventor： Brad Owen Buckman ,  John Beamond Nicholas ,  Shendong Yuan ,  Marc Adler ,  Kumaraswamy Emayan ,  Jingyuan Ma

IPC: C07D233/90 ,  A61P11/00 ,  C07C233/05 ,  C07D209/20 ,  C07D231/14 ,  C07D249/06 ,  C07D263/34 ,  C07D271/04 ,  C07D275/03 ,  C07D285/06 ,  C07D307/68 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14

Abstract: Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.