Reference

Aminopiperidines and their preparation, pharmaceutical compositions and use in the treatment of diseases assocd

with renin activity such as hypertension. Breitenstein, Werner; Ehrhardt, Claus; Maibaum, Juergen Klaus; Ostermann, Nils; Zimmermann, Juerg; Masuya, Keiichi; Konishi, Kazuhide; Yokokawa, Fumiaki; Kanazawa, Takanori; Jacoby, Edgar; Marzinzik, Andreas; Grosche, Philipp; Kawakami, Shimpei (Novartis A.-G.; Novartis Pharma G.m.b.H., Switz.). PCT Int. Appl. WO 2007006534 A2 18 Jan 2007, 232pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IS, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: C07D. APPLICATION: WO 2006-EP6733 10 Jul 2006. PRIORITY: GB 2005-14203 11 Jul 2005. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1, 63 The invention relates to 3,5-substituted piperidine compds. of formula I, and their use in the diagnostic and therapeutic treatment of a warm-blooded animal, esp. for the treatment of a disease that depends on activity of renin; the use of a compd. of that class for the prepn. of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compd. of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compd., and/or a method of treatment comprising administering a 3,5-substituted piperidine compd., a method for the manuf. of a 3, 5-substituted piperidine compd., and novel intermediates and partial steps for its synthesis. Compds. of formula I wherein R1 is H, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted aryl, (un)substituted heterocyclyl, and (un)substituted cycloalkyl; R2 and R4 are independently (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted aryl, (un)substituted heterocyclyl, (un)substituted cycloalkyl, and acyl; R3 is H, (un)substituted aryl, and (un)substituted alkyl; R3R4 together with N may form a satd. (un)substituted C3-7 ring; T is CH2 and CO; and their pharmaceutically acceptable salts thereof, are claimed. 1623-92-3 and 920294-21-9 which are cas registry numbers of substances are two of reagents here. Example compd. II·TFA was prepd. by sulfonylation of polymer-bound (3R*,RS*)-5-(2,2-diphenylethylcarbamoyl)piperidine-1-carboxylic acid 9H-fluoren-9-ylmethyl ester with 4-toluenesulfonyl chloride followed by deprotection of Fmoc and resin cleavage to give compd. II·TFA. All the invention compds. were evaluated for their renin inhibitory activity. .

Synthesis and anthelmintic activity of some new 6- and 7-isothiocyanato-2H-1,4-benzoxa(thia)zin-3(4H)-ones and benzoxa(thia)zin-3(4H)-thiones

Synthesis and anthelmintic activity of some new 6- and 7-isothiocyanato-2H-1,4-benzoxa(thia)zin-3(4H)-ones and benzoxa(thia)zin-3(4H)-thiones. Shridhar, D. R.; Rao, K. Srinivasa; Singh, A. N.; Rastogi, K.; Jain, M. L.; Gandhi, S. S.; Krishnan, V. S.There are some reagents like 89976-75-0 is used in this study. H.; Jogibhukta, M.; Lovekar, C. D.; et al. (Res. Cent., IDPL, Hyderabad 500 037, India). Indian J. Chem., Sect. B, 24B(12), 1263-7 (English) 1985. CODEN: IJSBDB. ISSN: 0376-4699. DOCUMENT TYPE: Journal CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 Title compds. I (X,X1 = O,S; R = H, alkyl, substituted Ph, aminoalkyl; R1 = H,Me; R2 = H, alkyl; R3 = 6-, 7-isothiocyanato) were prepd. from I (R3 = NO2) via I (R3 = NH2) for anthelmintic testing. Some I possess a significant degree of activity against Ancylostoma ceylanicum in hamsters as well as against Hymenolepis nana in mice. The most potent compd., 6-isothiocyanato-2,2-dimethyl-2H-1,4-benzoxazin-3(4H)-one is orally effective against hookworm infection in dogs and cats at 1 ′ 100 mg/kg orally and 1 ′ 17 mg/kg orally resp. Anthelmintic activity against Ascardia galli in chicks is also reported for this compd. .