Patent SG-11201804936U-A (SG)
Title: Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels
Inventor: GRESHOCK THOMAS
IPC: A61P29/00
Filed: 2016-12-14
Abstract: EN N R (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/106226 Al 22 June 2017 (22.06.2017) WIPO I PCT (51) International Patent Classification: CO7D 285/08 (2006.01) A61K 31/4196 (2006.01) CO7D 417/12 (2006.01) A61K 31/551 (2006.01) CO7D 277/52 (2006.01) A61P 29/00 (2006.01) A61K 31/4168 (2006.01) A61P 11/14 (2006.01) A61K 31/4178 (2006.01) (21) International Application Number: PCT/US2016/066445 (22) International Filing Date: 14 December 2016 (14.12.2016) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/269,327 18 December 2015 (18.12.2015) US 62/290,235 2 February 2016 (02.02.2016) US 62/420,956 11 November 2016 (11.11.2016) US (71) Applicant (for all designated States except US): MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (72) Inventors; and (71) Applicants NZ, US only): GRESHOCK, Thomas, J. [US/US]; 770 Surrmeytown Pike, West Point, Pennsylvania 19486 (US). MULHEARN, James [US/US]; 770 Sum- neytown Pike, West Point, Pennsylvania 19486 (US). ZHENG, Junying [US/US]; 31 Newcomb Drive, New Providence, New Jersey 07074 (US). KIM, Ronald, M. [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jer- sey 07033 (US). ZHANG, Ting [CN/US]; 126 East Lin- coln Avenue, Rahway, New Jersey 07065-0907 (US). ROECKER, Anthony, J. [US/US]; 770 Surrmeytown Pike, West Point, Pennsylvania 19486 (US). WON, Wal- ter [US/US]; 950 Closter Rock Road, Alpine, New Jersey 08820 (US). NANTERMET, Philippe [US/US]; 770 Surrmeytown Pike, West Point, Pennsylvania 19486 (US). ANAND, Rajan [KE/US]; 22 Rainier Road, Fanwood, New Jersey 07012 (US). ZHOU, Gang [CN/US]; 111 Timothy Place, Bridgewater, New Jersey 08807 (US). WANG, Deping [US/US]; 770 Surrmeytown Pike, West Point, Pennsylvania 19486 (US). GUO, Liangqin [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jer- sey 07033 (US). (74) Common Representative: MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (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, 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). Decl arations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) [Continued on next page] = (54) Title: HYDROXYALKYLAMINE- AND HYDROXYCYCLOALKYLAMINE-SUBSTITUTED DIAMINE-ARYLSULFON- - AMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS (A) (57) : Disclosed are compounds of Formula A, or a salt thereof: Formula (A) wherein R I , R 2 , and E are defined herein, which compounds have properties for inhibiting Na„ 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same. 1111111111111101110101011111010111110111010110111111011101111111111111111110111111 W O 20 17 / 106 226 Al WO 2017/106226 Al 1#1101M01101DEIROIDEOM0101101101011101111MOVOIMIE as to the applicant's entitlement to claim the priority of Published: the earlier application (Rule 4.17(iii)) — with international search report (Art. 21(3))