Patent SG-11201805927Y-A (SG)
Title: Spiroheptane salicylamides and related compounds as inhibitors of rock
Inventor: SMITH II LEON M
IPC: C07D513/04
Filed: 2017-01-13
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, - Organization 11111111011110111010101111101011111011101110111101111011001101111101111011111 International Bureau ... .... ..Yjd (10) International Publication Number (43) International Publication Date ..... .... WO 2017/123860 Al 20 July 2017 (20.07.2017) WIPO I PCT (51) International Patent Classification: New Jersey 08534 (US). LADZIATA, Vladimir; c/o Bris- CO7D 401/14 (2006.01) CO7D 401/12 (2006.01) tol-Myers Squibb Company, 311 Pennington-Rocky Hill A61K 31/437 (2006.01) CO7D 413/12 (2006.01) Road, Pennington, New Jersey 08534 (US). DELUCCA, A61K 31/4427 (2006.01) CO7D 471/04 (2006.01) Indawati; c/o Bristol-Myers Squibb Company, 311 Pen- CO7D 231/12 (2006.01) CO7D 471/12 (2006.01) nington-Rocky Hill Road, Pennington, New Jersey 08534 CO7D 231/18 (2006.01) CO7D 513/04 (2006.01) (US). PINTO, Donald, J., P.; c/o Bristol-Myers Squibb CO7D 231/54 (2006.01) CO7D 213/64 (2006.01) Company, 311 Pennington-Rocky Hill Road, Pennington, (21) New Jersey 08534 (US). ORWAT, Michael J.; c/o Bris- International Application Number: PCT/US2017/013323 tol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, New Jersey 08534 (US). DILGER, An- (22) International Filing Date: drew K.; c/o Bristol-Myers Squibb Company, 311 Pen- 13 January 2017 (13.01.2017) nington-Rocky Hill Road, Pennington, New Jersey 08534 (US). PABBISETTY, Kumar Balashanmuga; c/o Bris- tol-Myers Squibb Company, 311 Pennington-Rocky Hill (26) Publication Language: English Road, Pennington, New Jersey 08534 (US). YANG, Wu; c/o Bristol-Myers Squibb Company, 311 Penning- (30) Priority Data: ton -Rocky Hill Road, Pennington, New Jersey 08534 (US). 62/278,122 13 January 2016 (13.01.2016) US SHAW, Scott A.; c/o Bristol-Myers Squibb Company, 311 (71) Applicant: BRISTOL-MYERS SQUIBB COMPANY Pennington-Rocky Hill Road, Pennington, New Jersey [US/US]; Route 206 and Province Line Road, Princeton, 08534 (US). GLUNZ, Peter W.; c/o Bristol-Myers Squibb New Jersey 08543 (US). Company, 311 Pennington-Rocky Hill Road, Pennington, New Jersey 08534 (US). PANDA, Manoranjan; c/o SYN- = (72) Inventors: SMITH II, Leon M.; c/o Bristol-Myers Squibb GENE INTERNATIONAL LIMITED, Biocon Special Company, 311 Pennington-Rocky Hill Road, Pennington, Economic Zone, Biocon Park, Plot No. 2 & 3, Bommas- [Continued on next page] (54) Title: SPIROHEPTANE SALICYLAMIDES AND RELATED COMPOUNDS AS INHIBITORS OF ROCK (57) : The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutic- () ally-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhib- R 6 , A itors. This invention also relates to pharmaceutical composi- N R1 tions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, R2 autoimmune, fibrotic, and/or inflammatory disorders using the same. R 13 --.....„ _ R I 3 ---- R 12 o 12 ix ......__ (I) R\" (R 3 0_4 1-1 NH2 © GC en ei ,-1 IN ,-1 © ei O WO 2017/123860 Al MIDEDIMOMOIDEIR010130H01110MEHMEMOVOIMIE andra Industrial Area IV Phase, Jigani Line Road Born- (84) Designated States (unless otherwise indicated, for every (74) masandra Bangalore, Karnataka 560 099 (IN). Agents: LIU, Hong et al.; Bristol-Myers Squibb Corn- pany, Route 206 & Province Line Road, Princeton, New Jersey 08543 (US). kind of regional protection available): ARIPO (BW, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, TZ, UG, ZM ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, ur , TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, GH, SZ, DE, LT, (81) Designated States (unless otherwise indicated, for every LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, kind of national protection available): AE, AG, AL, AM, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, GN, GQ, GW, KM, ML, MR, NE, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, Declarations under Rule 4.17: SN, TD, TG). SE, GA, 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, — of inventorship (Rule 4.17(iv)) KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, Published: LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, — with international search report (Art. 21(3)) 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.