US 12,173,018 B2
Penicillin-binding protein inhibitors
Christopher J. Burns, Malvern, PA (US); Denis Daigle, Street, MD (US); Guo-Hua Chu, Exton, PA (US); Jodie Hamrick, New Holland, PA (US); Steven A. Boyd, Chester Springs, PA (US); Allison L Zulli, Chesterbrook, PA (US); Eugen F. Mesaros, Wallingford, PA (US); Stephen M. Condon, Glenmoore, PA (US); Robert E. Lee Trout, Collegeville, PA (US); Cullen L. Myers, Exton, PA (US); and Zhenrong Xu, Chalfont, PA (US)
Assigned to VENATORX PHARMACEUTICALS, INC., Malvern, PA (US)
Appl. No. 17/057,593
Filed by VenatoRx Pharmaceuticals, Inc., Malvern, PA (US)
PCT Filed May 23, 2019, PCT No. PCT/US2019/033813
§ 371(c)(1), (2) Date Nov. 20, 2020,
PCT Pub. No. WO2019/226931, PCT Pub. Date Nov. 28, 2019.
Claims priority of provisional application 62/772,056, filed on Nov. 27, 2018.
Claims priority of provisional application 62/676,793, filed on May 25, 2018.
Prior Publication US 2021/0198288 A1, Jul. 1, 2021
Int. Cl. A61P 31/04 (2006.01); C07F 5/02 (2006.01)
CPC C07F 5/025 (2013.01) [A61P 31/04 (2018.01)] 17 Claims
 
1. A compound or a pharmaceutically acceptable salt, solvate, stereoisomer, tautomer, or N-oxide thereof; having one of the following formulas:

OG Complex Work Unit Chemistry
wherein:
Ring A is a 6-membered heteroaryl;
each Y is independently halogen, optionally substituted alkyl, —OH, —OR34, —OC(═O)R34, —NR32R33, —NR32C(═O)R34, —NR32C(═O)OR34, —NR32S(═O)0,1,2NR32R33, —NR32S(═O)0,1,2R34, —C(═O)OH, —C(═O)OR34, or —C(═O)NR32R33;
R32 and R33 are independently hydrogen or optionally substituted alkyl;
R34 is optionally substituted alkyl;
p is 1-3;
R is hydrogen or alkyl;
each W1 and W2 is independently —C(═O)— or —C(R91)2—;
R90 is hydrogen or optionally substituted alkyl;
each R91 is independently hydrogen or optionally substituted alkyl;
u1 is 1 or 2;
u2 is 1 or 2;
Ra, Rb, and Rc are independently hydrogen, halogen, cyano, alkyl, or —OH;
Rd is hydrogen or alkyl;
Z is hydrogen, R61, —R60OC(═O)R61, or —R60OC(═O)OR61;
each R60 is independently —CH2— or —CH(CH3)—; and
each R61 is independently optionally substituted alkyl.