- COMBINATION THERAPY FOR TREATING MPS1
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The application is directed to compounds of formula (I) and their salts and solvates, wherein B, R1, R2, R3, R3', R4, R4', and R5 are as set forth in the specification, as well as to methods for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of, e.g., MPS1, optionally in combination with α-L-iduronidase or an analog or variant thereof, e.g., laronidase.
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Paragraph 0315-0318; 0420-0423
(2021/08/14)
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- Microwave-assisted efficient synthesis of pyrazole-fibrate derivatives as stimulators of glucose uptake in skeletal muscle cells
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The design and synthesis of a series of pyrazolo[3,4-d]pyrimidinones containing fibrate side chains have been accomplished by utilizing the concept of molecular hybridization. All the synthesized compounds were evaluated for the glucose uptake stimulatory effect in L6 rat skeletal muscle cells. Four compounds (3f, 3g, 3j and 3q) were found to show significant stimulation of glucose uptake. Further these four compounds have been examined for their Glut4 translocation stimulatory effect in L6-Glut4myc myotubes. Compound 3q was found to exert maximum increase in GLUT4myc translocation.
- Gupta, Sampa,Kant, Ruchir,Pandey, Shubham,Rai, Amit Kumar,Sashidhara, Koneni V.,Singh, L. Ravithej,Tamrakar, Akhilesh K.
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- Synthesis of pyrazole-carboxamides and pyrazole-carboxylic acids derivatives: Simple methods to access powerful building blocks
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Hybrid systems containing pyrazole moiety show a wide spectrum of biological activities. To access novel hybrids with pyrazole ring, in this work we synthesized twenty pyrazole-carboxylic acids and twenty pyrazole-carboxamides, using simple synthetic methods, to be used as building blocks in the development of new structures.
- Ferreira, Byanca Silva,Silva, Rafaela Corrêa,Souto, Bernardo Araújo,Dos Santos, Maurício Silva
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p. 335 - 343
(2021/09/07)
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- Microwave-assisted protocols for the expedited synthesis of pyrazolo[1,5-a] and [3,4-d]pyrimidines
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General, high-yielding MAOS protocols for the expedited synthesis of functionalized pyrazolo[1,5-a]pyrimidines and pyrazolo[3,4-b]pyrimidines, as well as their pyrazole precursors, are described amenable to an iterative analogue library synthesis strategy for lead optimization.
- Daniels, R. Nathan,Kim, Kwangho,Lebois, Evan P.,Muchalski, Hubert,Hughes, Mary,Lindsley, Craig W.
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p. 305 - 310
(2008/09/17)
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- 3-AMINO-PYRAZOLE-4-CARBOXAMIDE DERIVATIVES USEFUL AS INHIBITORS OF PROTEIN KINASES
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The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them
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Page/Page column 41
(2008/12/05)
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- TRIAZINE DERIVATIVES
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Compounds of the formula I wherein A represents a grouping of the formula in which R1 and R2 each individually represent hydrogen, halogen, trifluoromethyl, nitro, amino, cyano, C1-C6-alkyl, C1-C6-alkoxy, C3-C6-alkenyloxy, C1-C6-alkylthio, C114 C6-alkanoylamino, aryloxy, aryl-(C1-C6-alkyl), aryl-(C1-C6-alkoxy), aryl-(C1-C6-alkoxy)carbonylamino or a group of the formula ?O?CH2?R3 or R1 and R2 on adjacent carbon atoms together represent a group of the formula ?CH=CH?CH=CH? or ?CH2?CH2?O? and R3 represents hydroxy-(C1-C4-alkyl) or vicinal dihydroxy-(C2-C5-alkyl), and pharmaceutically acceptable acid addition salts of those compounds of formula I in which R1 and/or R2 represents amino, possess xanthine oxidase inhibiting activity and can be used as medicaments, particularly for the control or prevention of ischemia or gout. These compounds can be manufactured according to known methods.
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