- PYRAZOLO-TRIAZINE AND/OR PYRAZOLO-PYRIMIDINE DERIVATIVES AS SELECTIVE INHIBITOR OF CYCLIN DEPENDENT KINASE
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The present invention relates to pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[l,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.
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Page/Page column 50; 75-76
(2019/11/04)
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- SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, A and B are as defined herein. The invention also r
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Page/Page column 69
(2012/09/22)
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- Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13
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Matrix metalloproteases (MMPs) play an important role in cartilage homeostasis under both normal and inflamed disease states and, thus, have become attractive targets for the treatment of arthritic diseases. Herein, we describe the identification of a pot
- Taylor, Steven J.,Abeywardane, Asitha,Liang, Shuang,Muegge, Ingo,Padyana, Anil K.,Xiong, Zhaoming,Hill-Drzewi, Melissa,Farmer, Bennett,Li, Xiang,Collins, Brandon,Li, John Xiang,Heim-Riether, Alexander,Proudfoot, John,Zhang, Qiang,Goldberg, Daniel,Zuvela-Jelaska, Ljiljana,Zaher, Hani,Li, Jun,Farrow, Neil A.
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experimental part
p. 8174 - 8187
(2012/01/13)
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- ISOXAZOLE-PYRAZOLE DERIVATIVES
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The present invention is concerned with isoxazole-pyrazole derivatives of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
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- Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors
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A novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as c-Jun-N-terminal kinase (JNK) inhibitors is described. These compounds were synthesized via the condensation of 2-nitrobenzaldehydes and hydroxypyrazoles. The structure-activity relationships (SAR) and kinase selectivity profile of the inhibitors are also discussed. Compound 16 was identified as a potent JNK inhibitor with good cellular potency.
- Liu, Mei,Xin, Zhili,Clampit, Jill E.,Wang, Sanyi,Gum, Rebecca J.,Haasch, Deanna L.,Trevillyan, James M.,Abad-Zapatero, Cele,Fry, Elizabeth H.,Sham, Hing L.,Liu, Gang
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p. 2590 - 2594
(2007/10/03)
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- Substituted pyrazole derivatives
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New substituted pyrazole derivatives of general formula I are described STR1 in which R1, R2, R3, R4, R5 and R6 have the meanings given in the description, processes for their preparation, as well as intermediates, and their use as herbicides.
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- Substituted pyrazolypyrazoles and their use as herbicides
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STR1 The invention relates to new pyrazolylpyrazoles of general formula (I) in which R1, R2, R3, R4 and R5 have the meanings given in the description, processes for their preparation as well as intermediates, and their use as herbicides.
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- Enehydrazines, 34. The Addition of Methylhydrazine to Dimethyl Acetylenedicarboxylate is Reversible
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The cyclisation of the enehydrazine 1 to the pyrazolone 5 proceeds by cleavage of 1 to its educts 2 and 3 followed by their recombination to 4.Addition of 2 or 3 supresses the dissociation of 1, furthermore 2 and 3 could be separately captured from 1.
- Sucrow, Wolfgang,Bredthauer, Gerhard
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p. 1520 - 1524
(2007/10/02)
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- Enehydrazines, 35. Dimethyl-2-fumarate
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Reaction of the pyrazolone 4 with dimethyl acetylenedicarboxylate gives the title compound 1, the crystal structure analysis of which is presented.Heating of 1 leads to the lactone 2, which was synthesized through an independent route.
- Sucrow, Wolfgang,Auffenberg-Weddige, Katharina,Grosz, Klaus-Peter,Bredthauer, Gerhard,Pickardt, Joachim
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p. 1525 - 1530
(2007/10/02)
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