Reference

Pyrano[3,2-c]pyridine derivatives as antihypertensives

Pyrano[3,2-c]pyridine derivatives as antihypertensives. Evans, John Morris; Stemp, Geoffrey; Cassidy, Frederick (Beecham Group PLC, UK). Eur. Pat. Appl. EP 205292 A2 17 Dec 1986, 22 pp. DESIGNATED STATES: R: BE, CH, DE, FR, GB, IT, LI, LU, NL, SE. (European Patent Organization) CODEN: EPXXDW. CLASS: ICM: C07D491-04. ICS: C07D491-10; A61K031-435. ICI: C07D491-04, C07D311-00, C07D221-00; C07D491-10, C07D311-00, C07D221-00. APPLICATION: EP 86-304139 30 May 1986. PRIORITY: GB 85-14538 8 Jun 1985; GB 85-27713 9 Nov 1985. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 The title compds. [I; X= O, S; R1,R2 = H, C1-4 alkyl; R1R2 = (CH2)n; R3 = H, OH, C1-6 alkoxy, C1-7 acyloxy; R4 = H; R3R4 = bond; R5 = H, (substituted) C1-6 alkyl, C2-6 alkenyl, amino, (substituted) (hetero)aryl, CO2R7; R6 = H, C1-6 alkyl; R5R6 = atoms to complete a heterocyclic ring; R7 = H, alkyl, amino; n = 2-5] and their pyridine N-oxides were prepd. as antihypertensives and bronchodilators. 4-Hydroxypyridine cyclocondensed with ClCMe2CYCH to give pyranopyridine II which was epoxidized via the bromohydrin. The epoxide reacted with 2-pyrrolidinone to give I [R1 = R2 = Me, R3 = OH, R4 = H, R5R6 = (CH2)3, X = O] (III). III at 1mg /kg p.o. 393-52-2 and 626-64-2 are just another two chemicals used in this study. reduced blood pressure by 39% in rats . .

Boronic acid-based compound b-lactamase inhibitors, their preparation, and methods using these compounds for the treatment of bacterial infection

Freire, Ernesto; Ross, Patrick; Xiao, Yingxin; Ottenbrite, Raphael; Luque, Irene (Fulcrum Pharmaceuticals, Inc.; The Johns Hopkins University, USA). PCT Int. Appl. WO 2005004799 A2 20 Jan 2005, 144 pp. 693235-39-1 and 393-52-2 are also occured in this study. 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, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: A61K. APPLICATION: WO 2004-US18624 10 Jun 2004. PRIORITY: US 2003-2003/PV477636 10 Jun 2003. DOCUMENT TYPE: Patent CA Section: 1 (Pharmacology) Section cross-reference(s): 29, 63 The invention provides non-b-lactam inhibitors of b-lactamases. In particular, the invention provides boronic acid-based compds. These compds. may be used with b-lactam antibiotics to bacterial infection, particularly b-lactam-antibiotic-resistant bacterial infections. These compds. are also antibacterial agents by themselves. The invention further provides methods of using such compds. Finally, the invention provides a pharmaceutical compn. comprising these compds. Compd. prepn. is described. .