Patent SG-11201407867V-A (SG)
Title: Dendrimer like amino amides possessing sodium channel blocker activity for the treatment of dry eye and other mucosal diseases
Inventor: JOHNSON MICHAEL ROSS
IPC: C07D241/32
Filed: 2013-05-29
Abstract: (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 2013/181232 A3 5 December 2013 (05.12.2013) WIPO I PCT (51) International Patent Classification: C07D 241/32 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/043080 29 May 2013 (29.05.2013) English English (30) Priority Data: 61/652,481 29 May 2012 (29.05.2012) (71) Applicant: PARION SCIENCES, INC. [US/US]; 2525 Meridian Parkway, Suite 260, Durham, North Carolina 27713 (US). (72) Inventors: JOHNSON, Michael, Ross; 53524 Bickett, Chapel Hill, NC 27517 (US). THELIN, William Robert; 6809 Knotty Pine Drive, Chapel Hill, NC 27517 (US). BOUCHER, Richard, C.; 1124 Pinehurst Drive, Chapel Hill, NC 27517 (US). (74) Agents: KELLY, James, J. et al.; Obion, Spivak, McClel­— land, Maier & Neustadt, L.L.P., 1940 Duke Street, Alexan­ dria, VA 22314 (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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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. Ug (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, 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). Published: with international search report (Art. 21(3)) [Continued on next page] (54) Title: DENDRIMER LIKE AMINO AMIDES POSSESSING SODIUM CHANNEL BLOCKER ACTIVITY FOR THE TREATMENT OF DRY EYE AND OTHER MUCOSAL DISEASES §. AMILORIDE 2 3 4 Hours Post-Dose -Vehicle (Normal Rat) •*Cmpd: 1 mM {ExLac Rat) \"Vehicle (ExLac Rat) (57) Abstract: Sodium channel blockers repres­ ented by the formula II, are provided where the structural variables are defined herein. The in­ vention also includes variety of compositions, a combinations and methods of treatment using these inventive sodium channel blockers. It is an object of the present invention to provide com­ pounds that are more potent and/or absorbed less rapidly from mucosal surfaces, such as ocular surfaces, and/or are less reversible as compared to known compounds. In particular, it is an ob­ ject of the present invention to provide methods of treatment which rely on rehydration of mucos­ al surfaces. CJ m CJ 00 Figure 1 1 IT NHR 1 X.'A!A 1 N-C—N NHR (I) WO 2013/181232 A3 I lllll llllllll II llllll III lllll lllll III III III lllll lllll lllll lllll lllll llll lllllll llll llll llll - before the expiration of the time limit for amending the (88 » Date of publication of the international search report: claims and to be republished in the event of receipt of * amendments (Rule 48.2(h))