US 12,390,460 B2
Treatment for obesity
Chiang J. Li, Cambridge, MA (US); Zoltan Derdak, Attleboro, MA (US); Darko Stevanovic, Jamaica Plain, MA (US); and Jifeng Liu, Winchester, MA (US)
Assigned to 1GLOBE BIOMEDICAL CO., LTD., Beijing (CN); and 1GLOBE HEALTH INSTITUTE LLC, Norwood, MA (US)
Appl. No. 17/276,821
Filed by 1GLOBE BIOMEDICAL CO., LTD., Beijing (CN); and 1GLOBE HEALTH INSTITUTE LLC, Norwood, MA (US)
PCT Filed Sep. 18, 2019, PCT No. PCT/US2019/051788
§ 371(c)(1), (2) Date Mar. 17, 2021,
PCT Pub. No. WO2020/061231, PCT Pub. Date Mar. 26, 2020.
Claims priority of provisional application 62/732,650, filed on Sep. 18, 2018.
Prior Publication US 2021/0275523 A1, Sep. 9, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/496 (2006.01); A61K 31/427 (2006.01); A61K 31/4439 (2006.01); A61K 45/06 (2006.01); A61P 3/04 (2006.01); A61P 3/10 (2006.01)
CPC A61K 31/496 (2013.01) [A61K 31/427 (2013.01); A61K 31/4439 (2013.01); A61K 45/06 (2013.01); A61P 3/04 (2018.01); A61P 3/10 (2018.01)] 11 Claims
OG exemplary drawing
 
1. A method for treating a condition selected from the group consisting of obesity, overweight, type II diabetes and the metabolic syndrome in a mammal, comprising administering to a mammalian subject in need thereof:
(a) a therapeutically effective amount of a pharmaceutical composition comprising a compound of Formula I:

OG Complex Work Unit Chemistry
or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt, solvate thereof that is effective in the treatment or prevention of a condition selected from the group consisting of obesity, overweight, type II diabetes and the metabolic syndrome in a mammal, and
wherein the symbols have the following meanings and are, for each occurrence, independently selected:
R1 is hydrogen, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycle or substituted heterocycle, aryl or substituted aryl, ORa, SRa, S(═O)2Re, S(═O)2ORe, C(═O)ORd, C(═O)Ra, or C(═O)NRbRc;
R2 is heterocycle or substituted heterocycle, aryl or substituted aryl;
R3 is hydrogen, alkyl or substituted alkyl;
R4, R7, and R8 are each independently hydrogen;
R5 is alkyl or substituted alkyl, heterocycle or substituted heterocycle, aryl or substituted aryl, amino or substituted amino;
R6 is hydrogen, halogen, cyano, nitro, CF3, OCF3, alkyl or substituted alkyl, or ORa;
Ra is hydrogen, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycle or substituted heterocycle, or aryl or substituted aryl;
Rb, Rc and Rd are independently hydrogen, alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, heterocycle or substituted heterocycle, or aryl or substituted aryl, or said Rb and Rc together with the N to which they are bonded optionally form a heterocycle or substituted heterocycle;
Re is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycle or substituted heterocycle, or aryl or substituted aryl; and
(b) a pharmaceutically acceptable excipient, carrier, or diluent.