US 12,122,750 B2
AT2R antagonists and uses thereof
Thomas James Beauchamp, Fishers, IN (US); Zhaogen Chen, Carmel, IN (US); Scott Eugene Conner, Carmel, IN (US); Jon Andre Erickson, Carmel, IN (US); Maria Cristina Garcia Paredes, Carmel, IN (US); Jayana Pankajkumar Lineswala, Brownsburg, IN (US); Emanuele Sher, Hampton (GB); Bishnu Thapa, Greenwood, IN (US); and Leonard Larry Winneroski, Whitestown, IN (US)
Assigned to Eli Lilly and Company, Indianapolis, IN (US)
Filed by Eli Lilly and Company, Indianapolis, IN (US)
Filed on May 11, 2023, as Appl. No. 18/315,533.
Claims priority of provisional application 63/342,828, filed on May 17, 2022.
Claims priority of provisional application 63/413,691, filed on Oct. 6, 2022.
Prior Publication US 2023/0373919 A1, Nov. 23, 2023
Int. Cl. C07D 211/62 (2006.01); C07D 401/04 (2006.01); C07D 401/06 (2006.01); C07D 405/12 (2006.01); C07D 405/14 (2006.01); C07D 471/04 (2006.01)
CPC C07D 211/62 (2013.01) [C07D 401/04 (2013.01); C07D 401/06 (2013.01); C07D 405/12 (2013.01); C07D 405/14 (2013.01); C07D 471/04 (2013.01)] 28 Claims
 
1. A compound of formula (I):

OG Complex Work Unit Chemistry
wherein:
R1 is C1-C6 alkyl, C3-C6 cycloalkyl, C3-C9 heterocycloalkyl, or C6-C10 aryl, wherein the C1-C6 alkyl, C3-C6 cycloalkyl, C3-C9 heterocycloalkyl, or C6-C10 aryl is optionally substituted with one or more R1a;
each R1a independently is halogen, C1-C6 alkyl, C1-C6 alkoxyl, or C3-C6 cycloalkyl;
R2 is C1-C6 alkyl, C3-C6 cycloalkyl, C3-C9 heterocycloalkyl, or C6-C10 aryl, wherein the C1-C6 alkyl, C3-C6 cycloalkyl, C3-C9 heterocycloalkyl, or C6-C10 aryl is optionally substituted with one or more R2a;
each R2a independently is halogen, C1-C6 alkyl, C1-C6 alkoxyl, or C3-C6 cycloalkyl;
R3 is H or C1-C6 alkyl;
X is C5-C10 heteroaryl, C6-C10 aryl,

OG Complex Work Unit Chemistry
wherein the C5-C10 heteroaryl or C6-C10 aryl is optionally substituted with one or more Xa;
each Xa independently is halogen, C1-C6 alkyl, C1-C6 alkoxyl, or C3-C6 cycloalkyl;
R4 is H, C1-C6 alkyl, C3-C6 cycloalkyl, or C6-C10 aryl, wherein the C1-C6 alkyl, C3-C6 cycloalkyl, or C6-C10 aryl is optionally substituted with one or more R4a;
each R4a independently is halogen, cyano, C1-C6 alkyl, C1-C6 alkoxyl, or C3-C6 cycloalkyl;
R5 is H, C1-C6 alkyl, C3-C6 cycloalkyl, or C6-C10 aryl, wherein the C1-C6 alkyl, C3-C6 cycloalkyl, or C6-C10 aryl is optionally substituted with one or more R5a;
each R5a independently is halogen, cyano, C1-C6 alkyl, C1-C6 alkoxyl, or C3-C6 cycloalkyl;
R6 is H or C1-C6 alkyl;
R7 is C1-C6 alkyl, C3-C6 cycloalkyl, or C6-C10 aryl, wherein the C1-C6 alkyl, C3-C6 cycloalkyl, or C6-C10 aryl is optionally substituted with one or more R7a;
each R7a independently is halogen, cyano, or C3-C6 cycloalkyl;
R8 is H, halogen, or C1-C6 alkyl;
R9 is H, halogen, or C1-C6 alkyl, wherein R8 and R9 may alternatively come together to form a C3-C6 cycloalkyl;
R10 and R11 are each H or R10 and R11 together form an oxo;
R12 is C1-C6 alkyl, C3-C6 cycloalkyl, C6-C10 aryl, C1-C3-(phenyl), or C3-C10 heterocycloalkyl wherein the C1-C6 alkyl, C3-C6 cycloalkyl, C6-C10 aryl, C1-C3-(phenyl), or C3-C10 heterocycloalkyl is optionally substituted with one or more R12a; and
each R12a independently is halogen, cyano, C1-C6 alkyl, C1-C6 alkoxyl, or C3-C6 cycloalkyl,
or a pharmaceutically acceptable salt thereof.