公开(公告)号：US20190270726A1

公开(公告)日：2019-09-05

申请号：US16415862

申请日：2019-05-17

Applicant: Unity Biotechnology, Inc.

Inventor： Thomas W. von Geldern ,  Bradley Backes ,  Bing Chen

IPC: C07D403/06 ,  C07D233/54 ,  C07D233/64

Abstract: This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.

公开(公告)号：US10329279B2

公开(公告)日：2019-06-25

申请号：US15955474

申请日：2018-04-17

Applicant: Unity Biotechnology, Inc.

Inventor： Thomas W. von Geldern ,  Bradley Backes ,  Bing Chen

IPC: C07D403/06 ,  C07D233/54 ,  C07D233/64

Abstract: This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.

公开(公告)号：US20180362510A1

公开(公告)日：2018-12-20

申请号：US15955474

申请日：2018-04-17

Applicant: Unity Biotechnology, Inc.

Inventor： Thomas W. von Geldern ,  Bradley Backes ,  Bing Chen

IPC: C07D403/06 ,  C07D233/54 ,  C07D233/64

CPC classification number: C07D403/06 ,  C07D233/54 ,  C07D233/64

Abstract: This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.

公开(公告)号：US20200291050A1

公开(公告)日：2020-09-17

申请号：US16063135

申请日：2016-12-16

Applicant: Unity Biotechnology, Inc.

Inventor： Bradley Backes ,  Thomas W. von Geldern ,  Bing Chen

IPC: C07F9/6558 ,  C07F9/6509 ,  A61P43/00

Abstract: Compounds represented by Formula (I) and (II) and salts thereof are described herein. The compounds or salts of Formula (I) and (II) may be used to treat senescence-associated diseases and disorders.

公开(公告)号：US11111259B2

公开(公告)日：2021-09-07

申请号：US16063135

申请日：2016-12-16

Applicant: Unity Biotechnology, Inc.

Inventor： Bradley Backes ,  Thomas W. von Geldern ,  Bing Chen

IPC: C07F9/6558 ,  A61P43/00 ,  C07F9/6509

Abstract: Compounds represented by Formula (I) and (II) and salts thereof are described herein. The compounds or salts of Formula (I) and (II) may be used to treat senescence-associated diseases and disorders.

公开(公告)号：US09988368B1

公开(公告)日：2018-06-05

申请号：US15693061

申请日：2017-08-31

Applicant: Unity Biotechnology, Inc.

Inventor： Thomas W. von Geldern ,  Bradley Backes ,  Bing Chen

IPC: C07D403/06 ,  C07D233/54 ,  C07D233/64

CPC classification number: C07D403/06 ,  C07D233/54 ,  C07D233/64

Abstract: This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.