公开(公告)号：US20190337907A1

公开(公告)日：2019-11-07

申请号：US16402111

申请日：2019-05-02

Applicant: Esteban Masuda ,  Simon Shaw ,  Vanessa Taylor

Inventor： Esteban Masuda ,  Simon Shaw ,  Vanessa Taylor

IPC: C07D267/14 ,  C07D413/12 ,  C07D413/14 ,  C07D487/04 ,  A61P35/00

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US08530466B2

公开(公告)日：2013-09-10

申请号：US12867928

申请日：2009-02-20

Applicant: Esteban Masuda ,  Jochen Schmitz

Inventor： Esteban Masuda ,  Jochen Schmitz

IPC: A61K31/535

CPC classification number: A61K31/5383 ,  A61K31/662

Abstract: Novel methods and compositions for the prevention and treatment of all forms of atherosclerosis with 2,4-pyrimidinediamine compounds are described. Also disclosed is the coating of prosthetic devices, such as stents, with the compounds of the invention for the prevention and/or treatment of restenosis.

Abstract translation: 描述了用2,4-嘧啶二胺化合物预防和治疗所有形式的动脉粥样硬化的新方法和组合物。 还公开了将假体装置（例如支架）与本发明的化合物一起涂覆以预防和/或治疗再狭窄。

公开(公告)号：US20120245127A1

公开(公告)日：2012-09-27

申请号：US13487979

申请日：2012-06-04

Applicant: Esteban Masuda ,  Donald G. Payan ,  Elliot B. Grossbard ,  Somasekhar Bhamidipati ,  Rajinder Singh

Inventor： Esteban Masuda ,  Donald G. Payan ,  Elliot B. Grossbard ,  Somasekhar Bhamidipati ,  Rajinder Singh

IPC: A61K31/5383 ,  A61P35/02 ,  A61K31/505 ,  A61P35/00 ,  A61K31/675 ,  A61K31/5415

CPC classification number: A61K31/505 ,  A61K31/5383 ,  A61K31/542

Abstract: The present disclosure provides methods for the treatment of cell proliferative disorders by administration of a Syk kinase or Syk/Flt-3 kinase inhibitor. Cell proliferative disorders treatable by the methods include, hematopoietic neoplasms and virally associated tumors. The compounds are also directed to therapeutic or prophylactic inhibition of tumor metastasis.

Abstract translation: 本公开提供了通过施用Syk激酶或Syk / Flt-3激酶抑制剂治疗细胞增殖性疾病的方法。 可通过该方法治疗的细胞增殖性疾病包括造血赘生物和病毒相关的肿瘤。 该化合物还涉及肿瘤转移的治疗或预防性抑制。

公开(公告)号：US20120208785A1

公开(公告)日：2012-08-16

申请号：US13418306

申请日：2012-03-12

Applicant: Somasekhar Bhamidipati ,  Rajinder Singh ,  Thomas Sun ,  Esteban Masuda

Inventor： Somasekhar Bhamidipati ,  Rajinder Singh ,  Thomas Sun ,  Esteban Masuda

IPC: A61K31/675 ,  A61P37/08 ,  A61P17/02 ,  A61P29/00 ,  A61P37/00 ,  A61P5/16 ,  A61P7/06 ,  A61P21/04 ,  A61P1/16 ,  A61P31/14 ,  A61P1/04 ,  A61P19/04 ,  A61P17/00 ,  A61P19/08 ,  A61P25/00 ,  C07F9/6561

CPC classification number: A61K31/675 ,  A61K9/0053 ,  C07D498/04 ,  C07F9/6561

Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

Abstract translation: 本公开提供了前体药物的生物活性2,4-嘧啶二胺化合物，盐和水合物的前药，包含前体药物的组合物，用于合成前药的中间体和方法以及在各种应用中使用前药的方法。

公开(公告)号：US20100152218A1

公开(公告)日：2010-06-17

申请号：US12711534

申请日：2010-02-24

Applicant: Ankush Argade ,  Arvinder Sran ,  David Carroll ,  Jeffrey Clough ,  Kin Tso ,  Somasekhar Bhamidipati ,  Sambaiah Thota ,  Rajinder Singh ,  Vanessa Taylor ,  Hui Li ,  Esteban Masuda

Inventor： Ankush Argade ,  Arvinder Sran ,  David Carroll ,  Jeffrey Clough ,  Kin Tso ,  Somasekhar Bhamidipati ,  Sambaiah Thota ,  Rajinder Singh ,  Vanessa Taylor ,  Hui Li ,  Esteban Masuda

IPC: A61K31/505 ,  C07D239/48 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D239/48 ,  A61K31/505 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D498/04

Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.

公开(公告)号：US07723018B2

公开(公告)日：2010-05-25

申请号：US10651389

申请日：2003-08-28

Applicant: Robert Booher ,  Esteban Masuda ,  Valeria Ossovskaya ,  Brian Wong

Inventor： Robert Booher ,  Esteban Masuda ,  Valeria Ossovskaya ,  Brian Wong

IPC: C12Q1/00 ,  C12Q1/68 ,  G01N33/53 ,  G01N33/567

CPC classification number: A61K38/53 ,  A61K31/713 ,  C12Q1/6886 ,  C12Q2600/136 ,  G01N33/5011 ,  G01N33/5017 ,  G01N2510/00

Abstract: The present invention relates to regulation of the cell cycle. More particularly, the present invention is directed to nucleic acids encoding components of the ubiquitin ligation pathway, e.g., ubiquitin and ubiquitin-like molecules, E1, E2, and E3 proteins and their substrates, which are involved in modulation of cell cycle arrest. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate cell cycle arrest via modulation of the ubiquitin ligation pathway; as well as to the use of expression profiles and compositions in diagnosis and therapy related to cell cycle regulation and modulation of cellular proliferation, e.g., for treatment of cancer and other diseases of cellular proliferation.

Abstract translation: 本发明涉及细胞周期的调节。 更具体地，本发明涉及编码泛素连接途径的组分的核酸，例如参与调节细胞周期停滞的泛素和泛素样分子，E1，E2和E3蛋白及其底物。 本发明还涉及用于鉴定和使用包括小分子化学组合物，抗体，肽，环肽，核酸，RNAi，反义核酸和核酶的试剂的方法，其通过调节泛素连接途径调节细胞周期停滞; 以及在细胞周期调控和细胞增殖调节相关的诊断和治疗中使用表达谱和组合物，例如用于治疗癌症和其它细胞增殖疾病。

公开(公告)号：US07601713B2

公开(公告)日：2009-10-13

申请号：US11611568

申请日：2006-12-15

Applicant: Pingyu Ding ,  Ankush Argade ,  Dane Goff ,  Rajinder Singh ,  Esteban Masuda ,  Vanessa Taylor ,  Sacha Holland

Inventor： Pingyu Ding ,  Ankush Argade ,  Dane Goff ,  Rajinder Singh ,  Esteban Masuda ,  Vanessa Taylor ,  Sacha Holland

IPC: A61K31/519 ,  A61K31/52 ,  A61K31/517 ,  C07D498/04 ,  C07D487/04 ,  C07D473/16 ,  A61K31/5355 ,  A61K31/497 ,  A61K31/551 ,  C07D265/36 ,  C07D413/12 ,  C07D403/12 ,  C07D243/08 ,  A61P19/02 ,  C07D239/84 ,  C07D471/04 ,  C07D401/12

CPC classification number: C07D519/00 ,  A61K31/517 ,  C07D239/94 ,  C07D239/95 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D495/04 ,  C07D495/12

Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity. The compounds of the present invention are according to structural formula (I): or a salt or N-oxide thereof, wherein B is selected from

Abstract translation: 本公开提供了抑制蛋白激酶（例如JAK，Ax1或Syk激酶）的化合物，包含该化合物的组合物和使用该化合物抑制蛋白激酶并治疗和/或预防与不适当激酶活性相关疾病的方法。 本发明的化合物是根据结构式（I）：或其盐或N-氧化物，其中B选自

公开(公告)号：US20080003620A1

公开(公告)日：2008-01-03

申请号：US11608788

申请日：2006-12-08

Applicant: Esteban Masuda ,  Todd Kinsella ,  Justin Warner ,  Taisei Kinoshita ,  Mark Bennett ,  David Anderson

Inventor： Esteban Masuda ,  Todd Kinsella ,  Justin Warner ,  Taisei Kinoshita ,  Mark Bennett ,  David Anderson

IPC: G01N33/566

CPC classification number: C12N9/1205 ,  A61K31/00 ,  A61K31/7076

Abstract: The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize an adenosine kinase as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.

Abstract translation: 本发明提供能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用腺苷激酶作为替代分析物的化合物的方法和试剂盒以及使用该化合物的方法 各种体外，体外和体外上下文。

公开(公告)号：US20070298440A1

公开(公告)日：2007-12-27

申请号：US11608782

申请日：2006-12-08

Applicant: Todd Kinsella ,  Esteban Masuda ,  Mark Bennett ,  Justin Warner ,  David Anderson

Inventor： Todd Kinsella ,  Esteban Masuda ,  Mark Bennett ,  Justin Warner ,  David Anderson

IPC: G01N33/566 ,  G01N33/53

CPC classification number: G01N33/6869 ,  G01N33/566 ,  G01N33/6875 ,  G01N2333/70567

Abstract: The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a retinoid X receptor as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.

Abstract translation: 本发明提供能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用类视黄醇X受体作为替代分析物的化合物的方法和试剂盒以及使用该化合物的方法 在各种体外，体外和体外上下文中。

公开(公告)号：US07189523B2

公开(公告)日：2007-03-13

申请号：US10197919

申请日：2002-07-16

Applicant: Esteban Masuda ,  Todd M. Kinsella ,  Justin E. Warner ,  Taisei Kinoshita ,  Mark K. Bennett ,  David C. Anderson

Inventor： Esteban Masuda ,  Todd M. Kinsella ,  Justin E. Warner ,  Taisei Kinoshita ,  Mark K. Bennett ,  David C. Anderson

IPC: G01N33/566 ,  G01N33/567 ,  C07K4/00 ,  A61K45/00 ,  A61K38/00

CPC classification number: G01N33/6869 ,  C07K7/08 ,  G01N33/5052 ,  G01N2500/20

Abstract: The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a BAP-37 as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.

Abstract translation: 本发明提供能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用BAP-37作为替代分析物的这些化合物的方法和试剂盒以及使用该化合物的方法 在各种体外，体外和体外上下文中。