公开(公告)号：US20140179542A1

公开(公告)日：2014-06-26

申请号：US13940020

申请日：2013-07-11

Applicant: Sunesis Pharmaceuticals, Inc

Inventor： Jim Wells ,  Dan Erlanson ,  Andrew C. Braisted

IPC: G01N33/566

CPC classification number: G01N33/566 ,  G01N33/53 ,  Y10T436/24

Abstract: The present invention is directed to novel methods for rapidly and unambiguously identifying small organic molecule ligands for binding to biological target molecules. Small organic molecule ligands identified according to the methods of the present invention may find use, for example, as novel therapeutic drug lead compounds, enzyme inhibitors, labeling compounds, diagnostic reagents, affinity reagents for protein purification, and the like. Also presented are novel methods for identifying high affinity binding ligands for a biological target molecule of interest, wherein those methods comprise linking two or more small organic molecule ligands previously identified as being capable of binding to the biological target molecule of interest. Biological target molecules include, for example, polypeptides, nucleic acids, carbohydrates, nucleoproteins, glycoproteins, glycolipids and lipoproteins.

Abstract translation: 本发明涉及用于快速且明确地鉴定用于结合生物靶分子的小有机分子配体的新方法。 根据本发明方法鉴定的小有机分子配体可用于例如新型治疗药物铅化合物，酶抑制剂，标记化合物，诊断试剂，用于蛋白质纯化的亲和试剂等。 还提出了用于鉴定感兴趣的生物靶分子的高亲和力结合配体的新方法，其中这些方法包括将先前鉴定为能够结合目的生物靶标分子的两个或更多个小有机分子配体连接。 生物靶分子包括例如多肽，核酸，碳水化合物，核蛋白，糖蛋白，糖脂和脂蛋白。

公开(公告)号：US20140171660A1

公开(公告)日：2014-06-19

申请号：US13940157

申请日：2013-07-11

Applicant: Sunesis Pharmaceuticals, Inc.

Inventor： Anantha Sudhakar ,  Tamilarasan Subramani ,  Mohamed Sheik Mohamed Mu Rahuman ,  Ramar Subbiah

IPC: C07D207/16 ,  C07C59/245 ,  C07D207/14

CPC classification number: A61K31/4375 ,  A61K9/0019 ,  A61K9/08 ,  A61K45/06 ,  A61K47/10 ,  A61K47/20 ,  C07C59/245 ,  C07D207/16 ,  C07D471/04 ,  Y02P20/55

Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,45)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.

Abstract translation: 制备（+） - 1,4-二氢-7 - [（3S，4S）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基）-1 ，8-萘啶-3-羧酸。 还提供了包含（+） - 1,4-二氢-7 - [（3S，45）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基） ）-1,8-萘啶-3-羧酸，以及使用这种组合物的处理方法。

公开(公告)号：US11174243B2

公开(公告)日：2021-11-16

申请号：US16319506

申请日：2017-01-06

Applicant: Sunesis Pharmaceuticals, Inc. ,  Biogen MA Inc.

Inventor： J. Michael Macphee ,  Linda L. Neuman

IPC: C07D401/14 ,  A61P35/00 ,  C07C55/10 ,  A61K9/00

Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.

公开(公告)号：US20210017155A1

公开(公告)日：2021-01-21

申请号：US16802959

申请日：2020-02-27

Applicant: Sunesis Pharmaceuticals, Inc. ,  Biogen MA Inc.

Inventor： Brian T. HOPKINS ,  Timothy R. CHAN ,  Tracy J. JENKINS ,  Patrick CONLON ,  Xiongwei CAI ,  Michael HUMORA ,  Xianglin SHI ,  Ross A. MILLER ,  Andrew THOMPSON

IPC: C07D401/14

Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.

公开(公告)号：US09790229B2

公开(公告)日：2017-10-17

申请号：US15006061

申请日：2016-01-25

Applicant: Biogen MA Inc. ,  Sunesis Pharmaceuticals, Inc.

Inventor： Minna Bui ,  Patrick Conlon ,  Julio H. Cuervo ,  Daniel A. Erlanson ,  Junfa Fan ,  Bing Guan ,  Brian T. Hopkins ,  Tracy J. Jenkins ,  Gnanasambandam Kumaravel ,  Alexey A. Lugovskoy ,  Doug Marcotte ,  Noel Powell ,  Daniel Scott ,  Laura Silvian ,  Art Taveras ,  Deping Wang ,  Min Zhong

IPC: C07D487/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  A61K31/519

CPC classification number: C07D487/14 ,  A61K31/519 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04

Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.

公开(公告)号：US20170035741A1

公开(公告)日：2017-02-09

申请号：US15064498

申请日：2016-03-08

Applicant: Sunesis Pharmaceuticals, Inc.

Inventor： Anantha SUDHAKAR ,  Tamilarasan SUBRAMANI ,  Mohamed Sheik Mohamed Mujeebur RAHUMAN ,  Ramar SUBBIAH

IPC: A61K31/4375 ,  A61K9/00 ,  A61K45/06 ,  A61K9/08

CPC classification number: A61K31/4375 ,  A61K9/0019 ,  A61K9/08 ,  A61K45/06 ,  A61K47/10 ,  A61K47/20 ,  C07C59/245 ,  C07D207/16 ,  C07D471/04 ,  Y02P20/55

Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.

Abstract translation: 制备（+） - 1,4-二氢-7 - [（3S，4S）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基）-1 ，8-萘啶-3-羧酸。 还提供了包含（+） - 1,4-二氢-7 - [（3S，4S）-3-甲氧基-4-（甲基氨基）-1-吡咯烷基] -4-氧代-1-（2-噻唑基 ）-1,8-萘啶-3-羧酸，以及使用这种组合物的处理方法。

公开(公告)号：US20160376281A1

公开(公告)日：2016-12-29

申请号：US15006061

申请日：2016-01-25

Applicant: Biogen MA Inc. ,  Sunesis Pharmaceuticals, Inc.

Inventor： Minna Bui ,  Patrick Conlon ,  Julio H. Cuervo ,  Daniel A. Erlanson ,  Junfa Fan ,  Bing Guan ,  Brian T. Hopkins ,  Tracy J. Jenkins ,  Gnanasambandam Kumaravel ,  Alexey A. Lugovskoy ,  Doug Marcotte ,  Noel Powell ,  Daniel Scott ,  Laura Silvian ,  Art Taveras ,  Deping Wang ,  Min Zhong

IPC: C07D487/14 ,  C07D413/14 ,  C07D417/14 ,  C07D401/14 ,  C07D401/04 ,  C07D473/34

CPC classification number: C07D487/14 ,  A61K31/519 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04

Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.

Abstract translation: 本发明提供了可用作Btk抑制剂的化合物，其组合物及其使用方法。

公开(公告)号：US20160318935A1

公开(公告)日：2016-11-03

申请号：US15103756

申请日：2014-12-11

Applicant: BIOGEN MA INC. ,  SUNESIS PHARMACEUTICALS, INC.

Inventor： Brian T. Hopkins ,  Bin Ma ,  Timothy Raymond Chan ,  Gnanasambandam Kumaravel ,  Hua Miao ,  Andrea Bertolotti-Ciarlet ,  Kevin Otipoby

IPC: C07D487/04 ,  G01N33/573 ,  C07D513/04 ,  C07D473/00 ,  C07D519/00 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D473/00 ,  C07D513/04 ,  C07D519/00 ,  G01N33/573 ,  G01N2333/9121

Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.

Abstract translation: 本发明提供了可用作Bruton酪氨酸激酶抑制剂的化合物及其组合物，其表现出所需特性。

公开(公告)号：US20160311802A1

公开(公告)日：2016-10-27

申请号：US15103749

申请日：2014-12-11

Applicant: Biogen MA Inc. ,  Sunesis Pharmaceuticals, Inc.

Inventor： Brian T. Hopkins ,  Bin Ma ,  Timothy Raymond Chan ,  Lihong Sun ,  Lei Zhang ,  Gnanasambandam Kumaravel ,  Joseph P. Lyssikatos ,  Kevin Koch ,  Hua Miao

IPC: C07D403/12 ,  C07D495/04 ,  C07D409/14 ,  C07D487/04 ,  C07D513/04 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D401/14

CPC classification number: C07D403/12 ,  A61K31/506 ,  C07D239/30 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07F5/027

Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.

Abstract translation: 本发明提供了可用作Bruton酪氨酸激酶抑制剂的化合物及其组合物，并且其表现出所需特性。

公开(公告)号：US09394277B2

公开(公告)日：2016-07-19

申请号：US14406315

申请日：2013-06-07

Applicant: BIOGEN IDEC MA INC. ,  SUNESIS PHARMACEUTICALS, INC.

Inventor： Brian T. Hopkins ,  Patrick Conlon ,  Timothy R. Chan ,  Tracy J. Jenkins ,  Xiongwei Cai ,  Michael Humora ,  Xianglin Shi ,  Ross A. Miller ,  Andrew Thompson

IPC: A61K31/506 ,  C07D401/14

CPC classification number: C07D401/14

Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.

Abstract translation: 本发明提供了可用作Bruton酪氨酸激酶抑制剂的化合物及其组合物，并且其表现出所需特性。