Detail of "774608-89-8"

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Heterocyclic non-peptide GnRH antagonists and their preparation, pharmaceutical compositions and use as disease preventive agents

All Rights Reserved. Heterocyclic non-peptide GnRH antagonists and their preparation, pharmaceutical compositions and use as disease preventive agents.Several substances are used for example 774608-89-8 and 918443-82-0 which are their cas registry numbers. Showell, Graham Andrew; Miller, David John; Glen, Angela; Cubillo de Dios, Maria Angeles; Merchant, Kevin; Mandal, Ajay Kumar (Paradigm Therapeutics Ltd., UK). PCT Int. Appl. WO 2007000582 A1 4 Jan 2007, 132pp. 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-GB2344 27 Jun 2006. PRIORITY: GB 2005-13176 28 Jun 2005; GB 2005-21278 19 Oct 2005; GB 2006-8846 4 May 2006. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 A compd. of formula I as GnRH antagonists and the pharmaceutical compn. has therapeutic utility. Compds. of formula I: wherein either B is absent and A and Z are the same or different and are each H, halo, alkyl, hydroxy, alkoxy, CN, C(Rc)2OH, -N(Rd)C(=X)Rc, -C(=X)N(Rc)(Rd), -S(O)m-Rc, -N(Rc)(Rd)S(O)2, -S(O)2N(Rc)(Rd), -N(Re)2, (un)substituted aryl, and (un)substituted O-aryl; B is present and is (CH2)n, C(Rb)2 or O, or B taken together with A or Z is C=C(Rb), C(Rb)=C, CH2-CH(Rb) and CH(Rb)-CH2; D is O and S(O)m; E is a bond, (CH2)n, N(Rd), (CH2)nN(Rd) and -(Rd)(CH2)n; F is C(=X); G is (CH2)n, N(Rd), (CH2)nN(Rd) and N(Rd)(CH2)n; J is a bond, O, N(RC)C(=X), C(=X)N(Rc), S(O)m,, N(Rc)S(O)m, S(O)nN(Rc), N(Re) and -N(Rg)(Rh); K is a bond, alkylene, (hetero)cycloalkylene, (hetero)cycloalkenylene, (hetero)arylene; and L is hydrogen,halo, CN, cycloalkyl, (heteroaryl, etc.; M is 5- to 6-membered (un)substituted heteroaryl; N is (un)substituted (hetero)arylene; Rb, Re, Rf are independently H and alkyl; Rc is alkyl, cycloalkyl, alkylaryl, alkylcycloalkyl and (un)substituted aryl; Rd is H, alkyl, (un)substituted aryl; Rg and Rh are independently H, cycloalkyl, and (un)substituted alkyl-cycloalkyl; X is O, and S; m is 0, 1 and 2; n is 0, 1, 2 and 3; R1 is H, halo, alkyl, aryl, etc.; and their pharmaceutically acceptable salts thereof, are claimed. Example compd. II was prepd. by hydrolysis of tert-Bu 2-(4,6-dimethyl-5-(2-(6-methoxy-3,3-dimethyl-2,3-dihydro-1H-inden-5-yl oxy)thiazole-4-carboxamido)pyrimidin-2-ylamino)ethyl(isopropyl)carba mate. All the invention compds. were evaluated for their GnRH antagonistic activity. From the assay, it was detd. that compd. II exhibited an IC50 value of 4 nM. .