Patent SG-11201907864Y-A (SG)
Title: PHARMACOLOGICALLY ACTIVE ALICYCLIC-SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES
Inventor: Borza István 
IPC: C07D487/04
Filed: 2018-03-12
Abstract: 1 O 1-1 00 1-1 O (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 20 September 2018 (20.09.2018) WIP0 I PCT Hu omit VIII °nolo Oil ioo milo111110 Elio ow (10) International Publication Number WO 2018/167630 Al (51) International Patent Classification: CO7D 487/04 (2006.01) A61P 19/00 (2006.01) A61K 31/519 (2006.01) A61P 25/00 (2006.01) (21) International Application Number: PCT/IB2018/051599 (22) International Filing Date: 12 March 2018 (12.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: P1700108 13 March 2017 (13.03.2017) HU (71) Applicant: RICHTER GEDEON NYRT. [HU/HU]; Gyomroi fit 19-21., H-1103 Budapest (HU). (72) Inventors: BORZA, Istvan; Margo Tivadar u. 218., H-1186 Budapest (HU). ROMAN, Viktor; Szent Istvan fit 3., 2030 Erd (HU). ELES, Janos; Ordogszikla fit 2., H-1121 Budapest (HU). HADADY, Zsuzsa; Felegyhazi T. u. 29., 4034 Debrecen (HU). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) Published: with international search report (Art. 21(3)) (54) Title: PHARMACOLOGICALLY ACTIVE ALICYCLIC-SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES OH { I) (57) : The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutical ly accept- able salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention al so relates to the process for producing such compounds. The inven- tion further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention al so provides a method for manufacture of medicaments useful in the treatment of such disorders.