2-Chloro-3-cyanopyridine CAS NO.6602-54-6

Preparation of azaindazole compounds as CCR1 antagonists. Zhang, Penglie; Pennell, Andrew M. K.; Wright, John J. Kim; Chen, Wei; Leleti, Manmohan R.; …

Preparation of azaindazole compounds as CCR1 antagonists. Zhang, Penglie; Pennell, Andrew M. K.; Wright, John J. Kim; Chen, Wei; Leleti, Manmohan R.; Li, Yandong; Li, Lianfa; Xu, Yuan ( Chemocentryx, Inc., USA). PCT Int. Appl. WO 2007002293 A2 4 Jan 2007, 121pp. 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. APPLICATION: WO 2006-US24313 22 Jun 2006. PRIORITY: US 2005-693525P 22 Jun 2005. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 Title compds. I and II [R1 = alkyl, haloalkyl, cycloalkyl, etc.; R2a, R2c, R2d = H, halo, cyano, etc.; each of ring vertices a, b, c and d is selected from N and C(R3a), and from one to two of said ring vertices is N; R3a = H, halo, -ORf, etc.; Rf = H, alkyl, haloalkyl, etc.; m = 0-2], pharmaceutically acceptable salts, hydrates or N-oxides thereof were prepd. For example, 2-chloro-1-[4-(4-chloro-2-fluoro-5-methoxyphenyl)-2-(S)-methylpiperazin -1-yl]ethanone (1 .0 equiv) was reacted with 1H-pyrazolo[3,4-b]pyridine (1.2 equiv) and K2CO3 (10.0 equiv) in DMF at 80° for 1h, then chromatographed to give compd. III and IV. In CCR1 binding assays, each exemplified compd. III and IV exhibited the IC50 value of <1000 nM. Compds. I are claimed useful for the treatment of rheumatoid arthritis, multiple sclerosis, etc.Except for chemicals metioned above, 117007-51-9 and 6602-54-6 are also used. .