149456-21-3Relevant academic research and scientific papers
BICYCLIC DERIVATIVES AS P38 KINASE INHIBITORS
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Page/Page column 32, (2010/11/25)
New bicyclic derivatives of formula (I); wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.
ORGANIC COMPOUNDS
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Page/Page column 94, (2010/11/27)
Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer (such as prostate or breast cancer), osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
2,2-Dialkylnaphthalen-1-ones as new potassium channel activators
Almansa,Gomez,Cavalcanti,Rodriguez,Carceller,Bartroli,Garcia-Rafanell,Forn
, p. 2121 - 2133 (2007/10/02)
A new series of 2,2-dialkylnaphthalen-1-one potassium channel activators has been prepared, and their in vitro relaxant activities in isolated rat portal vein and guinea pig tracheal spirals as well as their oral antihypertensive effect in spontaneously hypertensive rats have been evaluated. The group of 1,2-dihydro-4-(1,2-dihydro-2-oxo-1-pyridyl)-2,2- dimethylnaphthalen-1-ones with an electron-withdrawing substituent at the 6- position contain the most active compounds and 1,2-dihydro-4-(1,2-dihydro-2- oxo-1-pyridyl)-2,2-dimethyl-1-oxonaphthalene-6-carbonitrile, 17f (UR-8225), has been selected for further pharmacological development.
Tetralones with pharmacological activity
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, (2008/06/13)
The present invention relates to new tetralones having the formula I: STR1 wherein: R1 and R2 represent hydrogen, halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, pentafluoroethyl, ethynyl, trimethylsilylethynyl, C1-4 alkylcarbonylamino being the amino optionally substituted by a C1-4 alkyl group; R3 is hydrogen or C1-4 alkyl, and R4 is C1-4 alkyl, or R3 and R4 together form a C2-5 polymethylene chain; either R5 represents hydroxyl, acetoxy or formyloxy and R6 and R7 are both hydrogen, or R5 together with R6 form a carbonyl group and R7 is hydrogen, or R5 and R7 together form a bond and R6 is hydrogen; R8 is, among others, 1,2-dihydro-2-oxo-1-pyridyl, 2,3-dihydro-1-oxo-1H-isoindol-2-yl, 2-oxo-1-pyrrolidinyl, 2-oxo-1-pyperidinyl. The invention also relates to a procedure for their preparation and to pharmaceutical compositions containing them. These compounds are antihypertensive and bronchodilator agents.
