公开(公告)号：US07981903B2

公开(公告)日：2011-07-19

申请号：US12671960

申请日：2008-08-06

Applicant: Stanley Dawes Chamberlain ,  Felix Deanda, Jr. ,  Roseanne Gerding ,  Masaichi Hasegawa ,  Kevin Kuntz ,  Huangshu Lei ,  Yasushi Miyazaki ,  Naohiko Nishigaki ,  Samarjit Patnaik ,  Aniko Redman ,  John Brad Shotwell ,  Kirk Stevens ,  Joseph Wilson ,  Bin Yang

Inventor： Stanley Dawes Chamberlain ,  Felix Deanda, Jr. ,  Roseanne Gerding ,  Masaichi Hasegawa ,  Kevin Kuntz ,  Huangshu Lei ,  Yasushi Miyazaki ,  Naohiko Nishigaki ,  Samarjit Patnaik ,  Aniko Redman ,  John Brad Shotwell ,  Kirk Stevens ,  Joseph Wilson ,  Bin Yang

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC classification number: C07D487/04 ,  C07D487/14

Abstract: Novel pyrrolopyrimidines as shown in formula (I): and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.

Abstract translation: 式（I）所示的新型吡咯并嘧啶及其药学上可接受的衍生物。 该化合物可用于抑制IGF-1R。

公开(公告)号：US20230158025A1

公开(公告)日：2023-05-25

申请号：US17995519

申请日：2021-04-22

Applicant: Li LUI ,  Ya-qin ZHANG ,  Surendra KARAVADHI ,  Juan MARUGAN ,  Matthew HALL ,  Min SHEN ,  Samarjit PATNAIK ,  UNIVERSITY OF UTAH RESEARCH FOUNDATION ,  NATIONAL INSTITUTES OF HEALTH

Inventor： Li Lui ,  Ya-qin Zhang ,  Surendra Karavadhi ,  Juan Marugan ,  Matthew Hall ,  Min Shen ,  Samarjit Patnaik ,  Kent Lai ,  Manshu Tang ,  Francis G. Whitby ,  Christopher P. Hill ,  Bijina Balakrishna

IPC: A61K31/506 ,  A61K31/5377 ,  A61K31/527

CPC classification number: A61K31/506 ,  A61K31/5377 ,  A61K31/527

Abstract: Described herein are compounds that inhibit galactokinase (GALK) and other kinases and methods for producing the same. Also described are methods for using Structure-Activity Relationships (SAR) to develop compounds with enhanced activity.

公开(公告)号：US20140249145A1

公开(公告)日：2014-09-04

申请号：US13991816

申请日：2011-12-08

Applicant: Juan Jose Marugan ,  Noel Southall ,  Ehud Goldin ,  Wei Zheng ,  Samarjit Patnaik ,  Ellen Sidransky ,  Omid Motabar ,  Wendy Westbroek

Inventor： Juan Jose Marugan ,  Noel Southall ,  Ehud Goldin ,  Wei Zheng ,  Samarjit Patnaik ,  Ellen Sidransky ,  Omid Motabar ,  Wendy Westbroek

IPC: C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61P43/00 ,  C07D487/04

Abstract: Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and methods of use of these compounds in treating lysosomal storage disorders such as Gaucher disease are described herein. The compounds are of general Formula (I) in which variables R1-R7 and X are described in the application.

Abstract translation: 本文描述了取代的吡唑并嘧啶和二氢吡唑并嘧啶及其相关化合物，其制备方法，含有这些化合物的组合物，以及这些化合物在治疗溶酶体贮积症如戈谢病中的应用方法。 化合物是通式（I），其中变量R1-R7和X在本申请中描述。

公开(公告)号：US20100204196A1

公开(公告)日：2010-08-12

申请号：US12671960

申请日：2008-08-06

Applicant: Stanley Dawes Chamberlain ,  Felix Deanda, JR. ,  Roseanne Gerding ,  Masaichi Hasegawa ,  Kevin Kuntz ,  Huangshu Lei ,  Yasushi Miyazaki ,  Naohiko Nishigaki ,  Samarjit Patnaik ,  Aniko Redman ,  John Brad Shotwell ,  Kirk Stevens ,  Joseph Wilson ,  Bin Yang

Inventor： Stanley Dawes Chamberlain ,  Felix Deanda, JR. ,  Roseanne Gerding ,  Masaichi Hasegawa ,  Kevin Kuntz ,  Huangshu Lei ,  Yasushi Miyazaki ,  Naohiko Nishigaki ,  Samarjit Patnaik ,  Aniko Redman ,  John Brad Shotwell ,  Kirk Stevens ,  Joseph Wilson ,  Bin Yang

IPC: A61K31/397 ,  C07D487/04 ,  A61K31/519 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D487/14

Abstract: Novel pyrrolopyrimidines as shown in formula (I): and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.

Abstract translation: 式（I）所示的新型吡咯并嘧啶及其药学上可接受的衍生物。 该化合物可用于抑制IGF-1R。

公开(公告)号：US09353117B2

公开(公告)日：2016-05-31

申请号：US13991816

申请日：2011-12-08

Applicant: Juan Jose Marugan ,  Noel Southall ,  Ehud Goldin ,  Wei Zheng ,  Samarjit Patnaik ,  Ellen Sidransky ,  Omid Motabar ,  Wendy Westbroek

Inventor： Juan Jose Marugan ,  Noel Southall ,  Ehud Goldin ,  Wei Zheng ,  Samarjit Patnaik ,  Ellen Sidransky ,  Omid Motabar ,  Wendy Westbroek

IPC: A61K31/519 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61P43/00 ,  C07D487/04

Abstract: Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and methods of use of these compounds in treating lysosomal storage disorders such as Gaucher disease are described herein. The compounds are of general Formula (I) in which variables R1-R7 and X are described in the application.

Abstract translation: 本文描述了取代的吡唑并嘧啶和二氢吡唑并嘧啶及其相关化合物，其制备方法，含有这些化合物的组合物，以及这些化合物在治疗溶酶体贮积症如戈谢病中的应用方法。 化合物是通式（I），其中变量R1-R7和X在本申请中描述。

公开(公告)号：US20140155420A1

公开(公告)日：2014-06-05

申请号：US13978820

申请日：2012-01-10

Applicant: Rui Zhao ,  Heide L. Ford ,  Noel Southall ,  Erika Englund ,  Samarjit Patnaik ,  Marc Ferrer ,  Wei Zheng ,  Seameen Dehdashti ,  Juan Marugan

Inventor： Rui Zhao ,  Heide L. Ford ,  Noel Southall ,  Erika Englund ,  Samarjit Patnaik ,  Marc Ferrer ,  Wei Zheng ,  Seameen Dehdashti ,  Juan Marugan

IPC: A61K31/443 ,  A61K31/4174 ,  A61K31/277 ,  A61K31/4709 ,  A61K31/255 ,  A61K31/155

CPC classification number: A61K31/443 ,  A61K31/15 ,  A61K31/155 ,  A61K31/255 ,  A61K31/277 ,  A61K31/4174 ,  A61K31/4709

Abstract: The invention provides small molecule inhibitors of EYA2 phosphatase activity and EYA2 binding to Six1. These inhibitors are proposed for use in methods of treating cancer in a subject, such as those involving Six1 and/or EYA2 disregulation. In some embodiments, the invention further provides for the administration of a second cancer therapy to the subject.

Abstract translation: 本发明提供EYA2磷酸酶活性的小分子抑制剂和与Six1结合的EYA2。 这些抑制剂被提出用于治疗受试者的癌症的方法，例如涉及Six1和/或EYA2失调的那些。 在一些实施方案中，本发明进一步提供对受试者施用第二次癌症治疗。