864136-41-4Relevant academic research and scientific papers
TREATMENT OF GVHD
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Paragraph 0267, (2015/11/18)
The invention relates to treatment of graft versus host disease (GVHD) using compounds that inhibit ROCK2. In preferred aspects, the present invention provides methods for the treatment of GVHD, including chronic GVHD ( cGVHD) using compounds having the formulae l-XXV, as set forth herein.
3-(PYRAZOLYL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS
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, (2014/01/18)
The present application relates to novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to pharmaceutically acceptable salts and compositions comprising the said novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives and their use in the treatment of various disorders.
TREATMENT OF OCULAR DISORDERS
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Paragraph 0239, (2014/04/18)
The invention provides methods of treatment of ocular disorders, including ocular disease with an angiogenic component. In certain embodiments, the treatment comprises administration of a ROCK2 inhibitor and an angiogenesis inhibitor. In certain embodiments, the ROCK2 inhibitor is ROCK2 selective. In certain embodiments, the angiogenesis inhibitor is a VEGF antagonist, for example, and VEGFR2 antibody.
Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: From the active site to the second phosphotyrosine binding site
Wilson, Douglas P.,Wan, Zhao-Kui,Xu, Wei-Xin,Kirincich, Steven J.,Follows, Bruce C.,Joseph-McCarthy, Diane,Foreman, Kenneth,Moretto, Alessandro,Wu, Junjun,Zhu, Min,Binnun, Eva,Zhang, Yan-Ling,Tam, May,Erbe, David V.,Tobin, James,Xu, Xin,Leung, Louis,Shilling, Adam,Tam, Steve Y.,Mansour, Tarek S.,Lee, Jinbo
, p. 4681 - 4698 (2008/03/13)
Protein tyrosine phosphatase 1B (PTP1B) is a negative regulator of the insulin and leptin receptor pathways and thus an attractive therapeutic target for diabetes and obesity. Starting with a high micromolar lead compound, structure-based optimization of
Inhibitors of protein tyrosine phosphatase 1B
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Page/Page column 166, (2008/06/13)
Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for example, 2-carboxyl, 3-carboxymethoxy, 5-aryl substituted thiophenes, can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.
