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A compound, C1-C6 technology, applied in the direction of drug combination, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc.
Inactive Publication Date: 2001-06-20
NOVO NORDISK AS +1
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It can be hypothesized that PTPase inhibitors may prevent differentiation and thus lead to continued proliferation by inhibiting OST-PTP or other PTPases
Method used
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Embodiment 1
[0333] 6-Benzoyl-2-(oxalyl-amino)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxylic acid monosodium salt
[0334] N-benzoyl-4-piperidone (20.0 g, 0.1 mol), ethyl cyanoacetate (10.9 ml, 0.1 mol), ammonium acetate in a three-necked reaction flask equipped with a Dean-Stark trap (2.0g) and acetic acid (6ml) in benzene (100ml) was heated at reflux for 1h. After the reaction mixture was cooled, it was diluted with ethyl acetate (100ml), washed with water (3×100ml), washed with saturated aqueous sodium chloride (80ml), and dried (MgSO 4 ), filtered, and evaporated in vacuo to obtain (1-benzoyl-piperidin-4-ylidene)-cyano-acetic acid ethyl ester in slow crystallization oil in quantitative yield.
[0335] A mixture of the above-mentioned benzoyl-piperidin-4-ylidene compound (10.0g, 0.034mol), sulfur (1.13g, 0.035mol), morpholine (6.5ml) in ethanol (35ml) was heated at 50°C 2h, and stirred overnight at room temperature. The precipitate was filtered, washed with 96% ethanol (3×50m...
[0351] Elemental analysis, calculated value (C 17 h 16 N 2 o 5 S,1.75H 2 O):
[0352] C, 52.10%; H, 5.01%; N, 7.15%. Measured value:
[0353] C, 52.11%; H, 4.81%; N, 7.01%.
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Abstract
The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTP alpha, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
Description
field of invention [0001] The present invention relates to novel compounds, processes for their preparation, compositions comprising these compounds, use of these compounds as medicines and their use in therapy, wherein such compounds having formula 1 are protein tyrosine phosphatases (PTPases ) such as pharmacologically effective inhibitors of PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP, etc. where A, R 1 , R 2 , R 3 , R 4 , R 16 and R 17 will be defined in more detail below. [0002] It has been found that PTPases play a major role in the intracellular modulation and regulation of basic cell signaling mechanisms related to metabolism, growth, proliferation and differentiation (Flint et al., The EMBO J.12:1937-46(1993) ; Fischer et al, Science 253:401-6 (1991)). Overexpression or altered activity of tyrosine phosphatases is also responsible for the symptoms and progression of various diseases (Wiener, et al., J. Natl. Cancer Inst. 86:372-8 (1994); Hunter and Coope...
Claims
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