Reference

Preparation of N-(cis-4-aminocyclohexyl)-2-(benzothienyloxy)nicotinamide derivatives as inhibitors of 3',5'-cyclic nucleotide phosphodiesterase 4 (PDE4)

Preparation of N-(cis-4-aminocyclohexyl)-2-(benzothienyloxy)nicotinamide derivatives as inhibitors of 3',5'-cyclic nucleotide phosphodiesterase 4 (PDE4). Smith, Mya Coral Helen; Watson, Christine Anne Louise (Pfizer Inc, UK). U.S. Pat. Appl. Publ. US 2005020639 A1 27 Jan 2005, 23 pp. (English). (United States of America). CODEN: USXXCO. CLASS: ICM: C07D049-02.Some commonly used reagents like 50-85-1 and 343929-61-3 are used in this experiment. APPLICATION: US 2004-896112 20 Jul 2004. PRIORITY: GB 2003-17471 25 Jul 2003; US 2003-2003/PV497088 22 Aug 2003. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1, 7, 28 This invention relates to nicotinamide derivs. of general formula (I) [R1 = H, halo, C1-4 alkyl; X = CH2, Y = S; or X = S and Y = CH2; Z = CO, SO2; R2 = each (un)substituted Ph, benzyl, naphthyl, heteroaryl or C3-8 cycloalkyl] or pharmaceutically acceptable salts or solvates thereof. These compds. are inhibitors of 3',5'-cyclic nucleotide phosphodiesterases (PDEs), i.e., PDE4A, PDE4B, PDE4C, and PDE4D which are isoforms or subtypes of the PDE4 isoenzyme family. They are particularly useful for the treatment of a great no. of inflammatory, respiratory, and allergic diseases, disorders or conditions and for wounds and some of them are in clin. development mainly for treatment of asthma, chronic obstructive lung disease (COPD), bronchitis, and emphysema. Thus, cis-N-(4-aminocyclohexyl)-2-(2,3-dihydrobenzo[b]thiophen-6-yloxy)-5-flu oronicotinamide (150 mg, 0.39 mmol), imidazo[1,2-a]pyridine-8-carboxylic acid (87 mg, 0.43 mmol), 1-hydroxybenzotriazole hydrate (58 mg, 0.43 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (82 mg, 0.43 mmol) and 4-methylmorpholine (47 mL, 0.43 mmol) were dissolved in CH2Cl2 (20 mL) and the reaction mixt. was stirred at room temp. for 18 h and was concd. in vacuo. The residue was dissolved in DMF (10 mL) and stirred at room temp. for 18 h to give, after workup and silica gel chromatog., 130 mg (63%) imidazo[1,2-a]pyridine-8-carboxylic acid [cis-4-[[[2-[(2,3-dihydrobenzo[b]thiophen-6-yl)oxy]-5-fluoropyridin-3-yl]ca rbonyl]amino]-cyclohexyl]amide (II). Antiinflammatory properties of the nicotinamide derivs. I were demonstrated by their ability to inhibit TNFa release from human peripheral blood mononuclear cells. II showed IC50 of 0.6 nM in the above assay. .

Potentiometric study of beryllium(II) salicylates

Potentiometric study of beryllium(II) salicylates. Abbasi, Shahid A.; Bhat, B. G.; Singh, R. S. (Dep. Chem., Indian Inst. Technol., Bombay, India). Indian J. Chem., Sect. A, 14A(9), 718-19 (English) 1976. CODEN: IJCADU. 50-85-1 and 61641-18-7 are cas registry numbers of chemicals which are used as reagents here. DOCUMENT TYPE: Journal CA Section: 68 (Phase Equilibriums, Chemical Equilibriums, and Solutions) Formation consts. of Be(II) complexes with salicylic acid and substituted salicylic acids were detd. by potentiometric titrns. in aq. solns. contg. 0.10M NaClO4. Ligand substituent effects on complex stability are discussed. .