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CAPLUS COPYRIGHT 2013 ACS
|Patent Number: ||WO 2012145471 |
|Title: ||Preparation of morpholinosulfonyl indole compounds as modulators of insulin-like growth factor I receptors and insulin receptors for treating cancer |
|Inventor(s): ||Balachandran, Sarala; Dinsmore, Christopher J.; Roychowdhury, Abhijit; Sharma, Rajiv; Vishwakarma, Ram Asrey |
|Patent Assignee(s): ||Merck Sharp & Dohme Corp., USA; Piramal Healthcare Ltd. |
|Source: ||PCT Int. Appl., 140pp. CODEN: PIXXD2 |
|Language: ||English |
The present invention relates to compds. of general formula I (wherein R1 is H, halo, NO2, etc.; R2 is H or C1-C6 alkyl; R3 is (un)substituted; heterocyclyl, C1-C6 alkylene, etc.; R9 is (un)substituted C6-C10aryl, (un)substituted 5-10 membered heterocyclyl, etc.) that are capable of inhibiting, modulating and/or regulating insulin-like-growth factor I receptors and insulin receptors and can be used for cancer treatment. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compds. Synthetic procedures for preparing I are exemplified. Example compound II was prepared in a 7-step synthesis that culminated in reaction of intermediate III with Et 4-oxopiperidine-1-carboxylate. Example compds. were tested in (1) in vitro IGF-IR and IR kinase assays, (2) antiproliferation assays using breast cancer and colon cancer cells, and (3) CYP inhibition assays.
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Note: Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced the abstract using additional information found in the patent. The original title of the PCT publication is Insulin-like growth factor-1 receptor inhibitors.