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Modulators of protein tyrosine phosphatases

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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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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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Examples

Experimental program
Comparison scheme
Effect test

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...

Embodiment 2

[0344] 2-(Oxalyl-amino)-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid

[0345] M.p.: 230-231°C

[0346] Elemental analysis, calculated value (C 11 h 11 NO 5 S):

[0347] C, 49.07%; H, 4.12%; N, 5.20%. Measured value:

[0348] C, 49.87%; H, 4.37%; N, 5.06%.

Embodiment 3

[0350] 6-Benzyl-2-(oxalyl-amino)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxylic acid

[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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PUM

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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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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D333/66A61K31/38A61K31/381A61K31/382A61K31/395A61K31/403A61K31/4035A61K31/404A61K31/41A61K31/427A61K31/4355A61K31/4365A61K31/4375A61K31/444A61K31/5377A61P3/04A61P3/10A61P5/10A61P7/02A61P11/06A61P17/06A61P19/10A61P25/00A61P25/18A61P25/28A61P31/04A61P35/00A61P37/06A61P37/08C07DC07D209/08C07D209/14C07D209/18C07D333/62C07D333/68C07D495/04C07D495/10C07D495/18C07D497/04C07D513/04C07D513/14
CPCC07D495/04C07D209/14C07D333/66C07D403/14C07D409/06C07D409/12C07D417/12C07D495/10C07D495/18
Inventor 尼尔斯·P·H·莫勒亨里克·S·安德森拉斯·F·艾弗森奥利·H·奥尔森斯文·布兰纳丹尼尔·D·霍尔斯沃思法里德·巴克尔卢克·M·贾奇弗兰克·U·阿克斯托德·K·琼斯威廉·C·里普卡纪雨罗伊·T·乌耶达
Owner NOVO NORDISK AS
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