- The expedient access to bromo-pyridine carbaldehyde scaffolds using gem-dibromomethyl intermediates
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A simple, efficient, and general two-step synthesis to bromo-pyridine carbaldehyde scaffolds is described. This direct route involves sequential reactions employing the dibromination of bromo-picolines followed by hydrolysis using an aqueous solution of calcium carbonate. Bromo-pyridine carbaldehyde scaffolds 1-7 were obtained in good overall yield. Bromo-dibromomethyl-pyridine intermediates have been isolated and characterized.
- Mandal, Ashis Baran,Augustine, John Kallikat,Quattropani, Anna,Bombrun, Agnes
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- OXAZOLE AND THIAZOLE DERIVATIVES AS SELECTIVE PROTEIN KINASE INHIBITORS (C-KIT)
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The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, A, Q, W and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.
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Page/Page column 66; 67
(2013/03/26)
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- Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors
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The histone deacetylases (HDACs) are able to regulate gene expression, and histone deacetylase inhibitors (HDACi) emerged as a new class of agents in the treatment of cancer as well as other human disorders such as neurodegenerative diseases. In the prese
- Thaler, Florian,Colombo, Andrea,Mai, Antonello,Amici, Raffaella,Bigogno, Chiara,Boggio, Roberto,Cappa, Anna,Carrara, Simone,Cataudella, Tiziana,Fusar, Fulvia,Gianti, Eleonora,Di Ventimiglia, Samuele Joppolo,Moroni, Maurizio,Munari, Davide,Pain, Gilles,Regalia, Nickolas,Sartori, Luca,Vultaggio, Stefania,Dondio, Giulio,Gagliardi, Stefania,Minucci, Saverio,Mercurio, Ciro,Varasi, Mario
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experimental part
p. 822 - 839
(2010/07/05)
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- IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES
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The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+-O- or CR3; Y is N, N+-O- or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
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Page/Page column 176-177
(2010/11/17)
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- AMINOTRIAZOLE DERIVATIVES AS ALX AGONISTS
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The invention relates to aminotriazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds. The compounds are useful for the prevention or treatment of diseases, which respond to the modulation of the ALX receptor such as inflammatory diseases.
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Page/Page column 83
(2009/07/18)
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- VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
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VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver; mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.
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Page/Page column 36
(2008/06/13)
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- Practical routes toward the synthesis of 2-halo- and 2-alkylamino-4-pyridinecarboxaldehydes
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We recently required an efficient synthesis of 2-halo- and 2-alkylamino-4-pyridinecarboxaldehydes. Several routes to these compounds were investigated resulting in efficient and practical procedures from readily available and inexpensive starting materials.
- Frey, Lisa F,Marcantonio, Karen,Frantz, Doug E,Murry, Jerry A,Tillyer, Richard D,Grabowski, Edward J.J,Reider, Paul J
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p. 6815 - 6818
(2007/10/03)
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