1595291-53-4

Upstream product

• 626-02-8 3-Iodophenol 
• 1250978-27-8 3-((3-iodophenoxy)methyl)pyridine 
• 73183-34-3 bis(pinacol)diborane 
• 6959-48-4 3-chloromethylpyridinium chloride 
• 214360-76-6 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenol 

Downstream Products

• 1595290-12-2 C₂₃H₁₈N₆O 
• 1595291-54-5 tert-butyl 1H-indazol-5-yl(2-(3-(pyridin-3-ylmethoxy)phenyl)pyrimidin-4-yl)carbamate 
• 1616474-11-3 2-chloro-4-(3-(pyridin-3-ylmethoxy)phenyl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidine 
• 1616474-12-4 C₁₈H₁₃ClN₄O 
• 1616474-32-8 N-(2-(piperidin-1-yl)ethyl)-3-((4-(3-(pyridin-3-ylmethoxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)benzamide 
• 1616474-30-6 N-(2-(piperidin-1-yl)ethyl)-2-(3-((4-(3-(pyridin-3-ylmethoxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)phenyl)acetamide 
• 1616474-28-2 N-(3-((2-(piperidin-1-yl)ethyl)carbamoyl)-5-((4-(3-(pyridin-3-ylmethoxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide 
• 1616474-26-0 N-(3-(2-oxo-2-((2-(piperidin-1-yl)ethyl)amino)ethyl)-5-((4-(3-(pyridin-3-ylmethoxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide 
• 1616474-24-8 N-(3-((4-(3-(pyridin-3-ylmethoxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide 
• 1616474-21-5 N-phenyl-4-(3-(pyridin-3-ylmethoxy)phenyl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine 
• 1616474-19-1 N-(2-(piperidin-1-yl)ethyl)-3-((4-(3-(pyridin-3-ylmethoxy)phenyl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)benzamide 
• 1616474-18-0 N-(2-(piperidin-1-yl)ethyl)-2-(3-((4-(3-(pyridin-3-ylmethoxy)phenyl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)phenyl)acetamide 
• 1616474-17-9 N-(3-((2-(piperidin-1-yl)ethyl)carbamoyl)-5-((4-(3-(pyridin-3-ylmethoxy)phenyl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide 
• 1616474-16-8 N-(3-(2-oxo-2-((2-(piperidin-1-yl)ethyl)amino)ethyl)-5-((4-(3-(pyridin-3-ylmethoxy)phenyl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide 

Relevant academic research and scientific papers

TREATMENT OF GVHD

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.

Synthesis and biological evaluation of substituted 2-anilino-7H- pyrrolopyrimidines as PDK1 inhibitors

An efficient and scalable route for a series of novel substituted 2-anilino-7H-pyrrolopyrimidine compounds as potential inhibitors of PDK1, an important regulator of the PI3K/Akt pathway that is dysregulated in many cancers, was developed and is described. The synthetic strategy was designed around Suzuki and Buchwald-Hartwig cross-couplings of a boronate fragment and various customised anilines sequentially with 2,4-dichloro-7-tosyl-7H- pyrrolopyrimidine. All fragments were constructed separately and cross-coupled to provide access to a range of novel compounds. Biological evaluation of these was undertaken, with modest inhibition observed.

TREATMENT OF OCULAR DISORDERS

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.