Asymmetric ureas and medical uses thereof

A method of treating cachexia or gastroparesis by agonizing activity of a ghrelin receptor in a human subject comprising administering to said subject an effective amount of a ghrelin receptor agonist represented by formula (I):

• or a pharmaceutically acceptable salt thereof,
• wherein:
• R is selected from the group consisting of aryl, arylalkyl, optionally substituted with one or more independent R103 substituents;
• R1 is selected from the group consisting of hydroxy, amino, alkyl, alkenyl, cycloalkyl, halogen, alkoxy, alkoxyalkyl, aryl, arylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl and heteroarylalkyl, each optionally independently substituted with one or more independent R103 substituents;
• R2 is hydrogen;
• R3 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl, —C(O)R101, —C(O)OR101, —C(O)NR101R102, —S(O)2R102, —SR101 and —S(O)2NR101R102, optionally substituted with one or more independent R103 substituents;
• R4 is selected from the group consisting of alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl, —OR103, NR101R102, —C(O)R101, —C(O)OR101, —C(O)NR101R102, -alkylNR101R102, —S(O)2R102, —SR101 and —S(O)2NR101R102, optionally substituted with one or more independent R103 substituents;
• R5 is selected from the group consisting of alkyl, alkenyl, cycloalkyl, aryl, heterocycloalkyl, heteroaryl, heteroarylalkyl, oxide (═O), —C(O)R101, —C(O)OR101, —C(O)NR101R102, —S(O)2R102, —SR101 and —S(O)2NR101R102;
• R6, R7, R8, R9, R10, R11, R12, R13 and R14 are each independently selected from the group consisting of hydrogen, cyano, —NO2, —OR101, hydroxy, amino, alkyl, alkenyl, cycloalkyl, halogen, alkoxy, alkoxyalkyl, aryl, arylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl, —C(O)R101, —C(O)OR101, —C(O)NR101R102, —NR101R102, —NR101S(O)2R102, —NR101C(O)R102, —S(O)2R102, —SR101 and —S(O)2NR101R102, each optionally independently substituted with one or more independent R103 substituents;
• and
• R101, R102 and R103 are each independently selected from the group consisting of hydrogen, cyano, —NO2, —OR104, hydroxy, amino, alkyl, alkenyl, cycloalkyl, halogen, alkoxy, alkoxyalkyl, aryl, arylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, heteroarylalkyl, —C(O)R104, —C(O)OR104, —C(O)NR104R105, —NR104R105, —NR104S(O)2R105, —NR104C(O)R105, —S(O)2R104, —SR104 and —S(O)2NR104R105, each optionally independently substituted with one or more independent R103 substituents;
• or R101, R102, together with the atoms connecting the same, form a fused or non-fused mono, bicyclic or tricyclic heterocyclic or carbocyclic ring which is optionally independently substituted with one or more R103 substituents;
• and
• R104 and R105 are each independently selected from the group consisting of hydrogen, cyano, —NO2, hydroxy, hydroxyalkyl, amino, alkyl, alkenyl, cycloalkyl, halogen, alkoxy, alkoxyalkyl, aryl, arylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl and heteroarylalkyl.

A method of treating cachexia or gastroparesis by agonizing activity of a ghrelin receptor in a human subject comprising administering to said subject an effective amount of a ghrelin receptor agonist selected from one of the following compounds, or a pharmaceutically acceptable salt thereof:

• GA1
• 1-methyl-3-((R)-1-(naphthalen-1- yl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA2
• 1-methyl-3-((S)-1-(naphthalen-1- yl)ethyl)-1-(1,3,3,- trimethylpiperidin-4-yl)urea,
• GA3
• 1-methyl-3-(1-(naphthalen-1- yl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA4
• 3-(1-(4-methoxynaphthalen-1- yl)ethyl)-1-methyl-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA5
• 1-benzyl-3-((R)-1-(naphthalen-1- yl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA6
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (3-methoxybenzyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA7
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (2-fluorobenzyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA9
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- methyl-1-(1,3,3-trimethylpiperidin- 4-yl)urea,
• GA10
• 3-((R)-1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-(1,3- dimethylpiperidin-4-yl)-1-(3- methoxybenzyl)urea,
• GA11
• 1-benzyl-3-(1-(2,3- dichlorophenyl)propyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA12
• 3-((S)-1-(2,3- dichlorophenyl)ethyl)-1-methyl-1- (1,3,3-trimethylpiperidin-4-yl)urea,
• GA13
• 3-((R)-1-(2,3- dichlorophenyl)ethyl)-1-methyl-1- (1,3,3-trimethylpiperidin-4-yl)urea,
• GA14
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- methyl-1-(1,3,3-trimethylpiperidin- 4-yl)urea,
• GA15
• 1-benzyl-3-((S)-1-(naphthalen-1- yl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA16
• 1-benzyl-3-((R)-1-(naphthalen-1- yl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA17
• 1-benzyl-3-(1-(naphthalen-1- yl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA18
• 3-(1-(2,3-dichlorophenyl)propyl)- 1-methyl-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA19
• 3-(1-(2,3-difluorophenyl)ethyl)-1- methyl-1-(1,3,3-trimethylpiperidin- 4-yl)urea,
• GA20
• 1-benzyl-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA21
• 1-benzyl-3-(1-(2,3- difluorophenyl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA22
• 1-benzyl-3-(1-(4- methoxynaphthalen-1-yl)ethyl)-1- (1,3,3-trimethylpiperidin-4-yl)urea,
• GA23
• 3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methyl-1- (1,3,3-trimethylpiperidin-4-yl)urea,
• GA24
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- methyl-1-(1,2,2,5,5- pentamethylpiperidin-4-yl)urea,
• GA25
• methyl 2-(3-methyl-3-(1,3,3- trimethylpiperidin-4-yl)ureido)-2- (naphthalen-1-yl)acetate,
• GA26
• 3-(2-hydroxy-1-(naphthalen-1- yl)ethyl)-1-methyl-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA27
• 1-(4-chlorobenzyl)-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA28
• 1-benzyl-1-(3,3-diethyl-1- methylpiperidin-4-yl)-3-((S)-1- (naphthalen-1-yl)ethyl)urea,
• GA29
• 1-benzyl-1-(3,3-diethyl-1- methylpiperidin-4-yl)-3-((R)-1- (naphthalen-1-yl)ethyl)urea,
• GA30
• 1-benzyl-1-(3,3-diethyl-1- methylpiperidin-4-yl)-3-(1- (naphthalen-1-yl)ethyl)urea,
• GA31
• 3-(2-(benzyloxy)-1-(naphthalen-1- yl)ethyl)-1-methyl-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA32
• ethyl 4-(1-benzyl-3-(1-(2,3- dichlorophenyl)ethyl)ureido)-1,3- dimethylpiperidine-3-carboxylate,
• GA33
• 3-((R)-1-(2,3- dichlorophenyl)ethyl)-1-(3- methoxybenzyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA34
• 3-(2-cyclopropyl-1-(2,3- dichlorophenyl)ethyl)-1-(3- methoxybenzyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA35
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (3-hydroxybenzyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA36
• 1-benzyl-3-(1-(2,3- dichlorophenyl)ethyl)-1-(3- (hydroxymethyl)-1,3- dimethylpiperidin-4-yl)urea,
• GA37
• 1-benzyl-3-(1-(2,3- dihydroxyphenyl)ethyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA38
• 3-((R)-1-(2,3- dichlorophenyl)ethyl)-1-(3-(2- hydroxyethoxy)benzyl)-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA39
• 3-(1-(2,3-difluoro-4- methoxyphenyl)ethyl)-1-methyl-1- (1,3,3-trimethylpiperidin-4-yl)urea,
• GA40
• 3-(1-(2,3-dihydro-4- hydroxyphenyl)ethyl)-1-methyl-1- (1,3,3-trimethylpiperidin-4-yl)urea,
• GA41
• 4-(1-benzyl-3-(1-(2,3- dichlorophenyl)ethyl)ureido)-1,3- dimethylpiperidine-3-carboxylic acid,
• GA42
• ethyl 4-(3-(1-(2,3- dichlorophenyl)ethyl)-1- methylureido)-1,3- dimethylpiperidine-3-carboxylate,
• GA43
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (3-(hydroxymethyl)-1,3- dimethylpiperidin-4-yl)-1- methylurea,
• GA44
• 4-(3-(1-(2,3-dichlorophenyl)ethyl)- 1-methylureido)-1,3,3- trimethylpiperidine 1-oxide,
• GA45
• 3-(1-benzo[d][1,3]dioxol-5- yl)ethyl)-1-benzyl-1-(1,3,3- trimethylpiperidin-4-yl)urea,
• GA46
• 1-ethyl-1-(1-methylpiperidin-4-yl)- 3-(1-(naphthalen-1-yl)ethyl)urea,
• GA47
• 3-(1-(4-methoxynaphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA48
• 3-(2-hydroxy-1-(naphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA49
• 3-(2-hydroxy-1-(4- methoxynaphthalen-1-yl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA50
• 1-(1-methylpiperidin-4-yl)-3-(1- (naphthalen-1-yl)ethyl)-1-(pyridin- 3-ylmethyl)urea,
• GA51
• 1-cyclopentyl-1-(1- methylpiperidin-4-yl)-3-(1- (naphthalen-1-yl)ethyl)urea,
• GA52
• 1-methyl-3-(1-(naphthalen-1- yl)ethyl)-1-(piperidin-4-yl)urea,
• GA53
• 1-(1-acetylpiperidin-4-yl)-1- methyl-3-(1-(naphthalen-1- yl)ethyl)urea,
• GA54
• 1-methyl-1-(1- (methylsulfonyl)piperidin-4-yl)-3- (1-(naphthalen-1-yl)ethyl)urea,
• GA55
• 1-methyl-3-(1-(naphthalen-1- yl)ethyl)-1-(1-(pyridin-3- ylmethyl)piperidin-4-yl)urea,
• GA56
• 1-cyclohexyl-1-(1-methylpiperidin- 4-yl)-3-(1-(naphthalen-1- yl)ethyl)urea,
• GA57
• 1-(cyclohexylmethyl)-1-(1- methylpiperidin-4-yl)-3-(1- (naphthalen-1-yl)ethyl)urea,
• GA58
• 1-isopropyl-1-(1-methylpiperidin- 4-yl)-3-(1-(naphthalen-1- yl)ethyl)urea,
• GA59
• 1-(2-methoxyethyl)-1-(1- methylpiperidin-4-yl)-3-(1- (naphthalen-1-yl)ethyl)urea,
• GA60
• 1-(1-ethylpiperidin-4-yl)-1-methyl- 3-(1-(naphthalen-1-yl)ethyl)urea,
• GA61
• 1-ethyl-4-(1-methyl-3-(1- (naphthalen-1- yl)ethyl)ureido)piperidine 1-oxide,
• GA62
• 1-(cyclopropylmethyl)-1-(1- methylpiperidin-4-yl)-3-(1- (naphthalen-1-yl)ethyl)urea,
• GA63
• 3-(1-(2-methoxynaphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA64
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(1-(quinolin-4-yl)ethyl)urea,
• GA65
• tert-butyl 4-(1-methyl-3-(1- (naphthalen-1- yl)ethyl)ureido)piperidine-1- carboxylate
• GA66
• 1-(1-formylpiperidin-4-yl)-1- methyl-3-(1-(naphthalen-1- yl)ethyl)urea,
• GA67
• 3-(2-methoxy-1-(naphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA68
• 3-(3-methoxy-1-(naphthalen-1- yl)propyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA69
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(1-(naphthalen-1- yl)propyl)urea,
• GA70
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(1-(quinolin-5-yl)ethyl)urea,
• GA71
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(2-(naphthalen-1-yl)propan- 2-yl)urea,
• GA72
• 3-(1-(2-chloroquinolin-4-yl)ethyl)- 1-methyl-1-(1-methylpiperidin-4- yl)urea,
• GA73
• (S)-1-(1-methylpiperidin-4-yl)-3- (1-(naphthalen-1-yl)ethyl)-1- (pyridin-3-ylmethyl)urea,
• GA74
• (R)-1-(1-methylpiperidin-4-yl)-3- (1-(naphthalen-1-yl)ethyl)-1- (pyridin-3-ylmethyl)urea,
• GA75
• 1-isobutyl-1-(1-methylpiperidin-4- yl)-3-(1-(naphthalen-1- yl)ethyl)urea,
• GA76
• 1-(cyclobutylmethyl)-1-(1- methylpiperidin-4-yl)-3-(1- (naphthalen-1-yl)ethyl)urea,
• GA77
• 1-butyl-1-(1-methylpiperidin-4-yl)- 3-(1-(naphthalen-1-yl)ethyl)urea,
• GA78
• 3-(1-(2-methoxyquinolin-4- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA79
• 1-(1-methylpiperidin-4-yl)-3-(1- (naphthalen-1-yl)ethyl)-1-(pyridin- 2-ylmethyl)urea,
• GA80
• 1-(1-methylpiperidin-4-yl)-3-(1- (naphthalen-1-yl)ethyl)-1-(pyridin- 4-ylmethyl)urea,
• GA81
• (S)-1-ethyl-3-(1-(2- methoxyquinolin-4-yl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA82
• (R)-1-ethyl-1-(1-methylpiperidin- 4-yl)-3-(1-(naphthalen-1- yl)ethyl)urea,
• GA83
• 3-(2-hydroxy-1-(4- methoxynaphthalen-1-yl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA84
• 3-(2-hydroxy-1-(naphthalen-1- yl)ethyl)-1-(1-methylpiperidin-4- yl)-1-(pyridin-3-ylmethyl)urea,
• GA85
• 3-(2-methoxy-1-(4- methoxynaphthalen-1-yl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA86
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (3-hydroxybenzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA87
• 1-benzyl-1-(1,3-dimethylpiperidin- 4-yl)-3-((R)-1-(naphthalen-1- yl)ethyl)urea,
• GA88
• 1-(1,3-dimethylpiperidin-4-yl)-1- methyl-3-((R)-1-(naphthalen-1- yl)ethyl)urea,
• GA89
• 3-(1-(4-methoxynaphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA90
• (R)-3-(1-(4-methoxynaphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA91
• (S)-3-(1-(4-methoxynaphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA92
• 3-(1-(4,8-dimethoxynaphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA93
• 3-(1-(4- (methoxymethoxy)naphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA94
• 3-(2-(benzyloxy)-1-(2,3- dichlorophenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA95
• (R)-3-(2-(benzyloxy)-1-(2,3- dichlorophenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA96
• (S)-3-(2-(benzyloxy)-1-(2,3- dichlorophenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA97
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA98
• 1-benzyl-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA99
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (3-fluorobenzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA100
• 1-(2-chlorobenzyl)-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA101
• 3-(1-(3,5-difluorophenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA102
• 3-(1-(2-chlorophenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA103
• 3-(1-(3-fluorophenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA104
• 3-(1-(4-chlorophenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA105
• 3-(1-(2,4-difluorophenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA106
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(1-(o-tolyl)ethyl)urea,
• GA107
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(1-(4- (methylsulfonyl)phenyl)ethyl)urea,
• GA108
• 1-(cyclohexylmethyl)-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA109
• 1-(cyclopropylmethyl)-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA110
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- ethyl-1-(1-methylpiperidin-4- yl)urea,
• GA111
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (1-methylpiperidin-4-yl)-1- (pyridin-3-ylmethyl)urea,
• GA112
• 3-(1-(3-chlorophenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA113
• 1-benzyl-3-(1-(3- chlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA114
• 1-(3-chlorobenzyl)-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA115
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (2-methoxybenzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA116
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (3-methoxybenzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA117
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (4-fluorobenzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA118
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (2-fluorobenzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA119
• 1-(4-chlorobenzyl)-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA120
• 3-(1-(3,4-dichlorophenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA121
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (4-methoxybenzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA122
• 3-(1-(2,3-dichlorophenyl)propyl)- 1-ethyl-1-(1-methylpiperidin-4- yl)urea,
• GA123
• 1-(cyclohexylmethyl)-3-(1-(2,3- dichlorophenyl)propyl)-1-(1- methylpiperidin-4-yl)urea,
• GA124
• 3-(1-(2,3-difluorophenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA125
• 1-benzyl-3-(1-(2,3- difluorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA126
• 1-(cyclohexylmethyl)-3-(1-(2,3- difluorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA127
• (R)-3-(1-(2,3- dichlorophenyl)ethyl)-1-ethyl-1-(1- methylpiperidin-4-yl)urea,
• GA128
• 1-benzyl-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1,3- dimethylpiperidin-4-yl)urea,
• GA129
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (1,3-dimethylpiperidin-4-yl)-1- methylurea,
• GA130
• (S)-3-(1-(2,3- dichlorophenyl)ethyl)-1-ethyl-1-(1- methylpiperidin-4-yl)urea,
• GA131
• (R)-3-(1-(2,3- dichlorophenyl)ethyl)-1-ethyl-1-(1- methylpiperidin-4-yl)urea,
• GA132
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- ethyl-1-(1-methylpiperidin-4- yl)urea,
• GA133
• 3-((R)-1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-(1,3- dimethylpiperidin-4-yl)-1-(3- methoxybenzyl)urea,
• GA134
• 3-((S)-1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-(1,3- dimethylpiperidin-4-yl)-1-(3- methoxybenzyl)urea,
• GA135
• 3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-(1,3- dimethylpiperidin-4-yl)-1-(3- methoxybenzyl)urea,
• GA136
• 3-(1-(2,3-difluorophenyl)ethyl)-1- (1,3-dimethylpiperidin-4-yl)-1-(3- methoxybenzyl)urea,
• GA137
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- (4-(hydroxymethyl)benzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA138
• methyl 4-((3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4- yl)ureido)methyl)benzoate,
• GA139
• 3-(2-cyclopropyl-1-(2,3- dichlorophenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA140
• 3-(1-(2,3-dichlorophenyl)-2- hydroxyethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA141
• (R)-1-(2-chlorobenzyl)-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA142
• (S)-1-(2-chlorobenzyl)-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA143
• 1-(2-chlorobenzyl)-3-(1-(2,3- dichlorophenyl)ethyl)-1-(1- methylpiperidin-4-yl)urea,
• GA144
• 3-(1-(2,3-dimethoxyphenyl)ethyl)- 1-methyl-1-(1-methylpiperidin-4- yl)urea,
• GA145
• 3-(1-(2,3-difluoro-4- methoxyphenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA146
• 3-(1-(2,3-dichlorophenyl)-2- methoxyethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA147
• N-(2,3-dichloro-4-(1-(3-methyl-3- (1-methylpiperidin-4- yl)ureido)ethyl)phenyl)acetamide,
• GA148
• 3-(1-(4-amino-2,3- dichlorophenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA149
• 3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA150
• 1-ethyl-1-(1-methylpiperidin-4-yl)- 3-(1-(naphthalen-1-yl)-3-(3- (pyridin-3- yloxy)phenyl)propyl)urea,
• GA151
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(1-(naphthalen-1-yl)-3- (pyridin-3-yl)propyl)urea,
• GA152
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(3-morpholino-1- (naphthalen-1-yl)propyl)urea,
• GA153
• 1-ethyl-3-(3-(3-methoxyphenyl)-1- (naphthalen-1-yl)propyl)-1-(1- methylpiperidin-4-yl)urea,
• GA154
• 3-(3-(3-(benzyloxy)phenyl)-1- (naphthalen-1-yl)propyl)-1-ethyl-1- (1-methylpiperidin-4-yl)urea,
• GA155
• 1-ethyl-1-(1-methylpiperidin-4-yl)- 3-(1-(naphthalen-1-yl)-3-(pyridin- 3-yl)propyl)urea,
• GA156
• 3-(3-(3-(benzyloxy)phenyl)-1- (naphthalen-1-yl)propyl)-1-(1- methylpiperidin-4-yl)-1-(pyridin-3- ylmethyl)urea,
• GA157
• 3-(3-(3-(benzyloxy)phenyl)-1-(2,3- dichlorophenyl)propyl)-1-methyl- 1-(1-methylpiperidin-4-yl)urea,
• GA158
• 3-(2-(benzyloxy)-1-(2,3- dichlorophenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA159
• 3-(2-(benzyloxy)-1-(2,3- dichlorophenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA160
• 3-(1-(2,3-dichlorophenyl)-2-((3- (hydroxymethyl)benzyl)oxy)ethyl)- 1-methyl-1-(1-methylpiperidin-4- yl)urea,
• GA161
• 3-(2-(benzyloxy)-1-(2,3- dichlorophenyl)ethyl)-1-(2- chlorobenzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA162
• 3-(2-(benzyloxy)-1-(2,3- dichlorophenyl)ethyl)-1-(4- (hydroxymethyl)benzyl)-1-(1- methylpiperidin-4-yl)urea,
• GA163
• 3-(1-(2,3-dichlorophenyl)-2-((4- methoxybenzyl)oxy)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA164
• 3-(1-(2,3-dichlorophenyl)-2- (pyridin-4-ylmethoxy)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA165
• 3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methoxy- 1-(1-methylpiperidin-4-yl)urea,
• GA166
• (S)-3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methoxy- 1-(1-methylpiperidin-4-yl)urea,
• GA167
• (R)-3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methoxy- 1-(1-methylpiperidin-4-yl)urea,
• GA168
• 1-hydroxy-3-(1-(4- methoxynaphthalen-1-yl)ethyl)-1- (1-methylpiperidin-4-yl)urea,
• GA169
• (R)-1-hydroxy-3-(1-(4- methoxynaphthalen-1-yl)ethyl)-1- (1-methylpiperidin-4-yl)urea,
• GA170
• (S)-1-hydroxy-3-(1-(4- methoxynaphthalen-1-yl)ethyl)-1- (1-methylpiperidin-4-yl)urea,
• GA171
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- methoxy-1-(1-methylpiperidin-4- yl)urea,
• GA172
• (R)-3-(1-(2,3- dichlorophenyl)ethyl)-1-methoxy- 1-(1-methylpiperidin-4-yl)urea,
• GA173
• (S)-3-(1-(2,3- dichlorophenyl)ethyl)-1-methoxy- 1-(1-methylpiperidin-4-yl)urea,
• GA174
• 1-methoxy-3-(1-(4- methoxynaphthalen-1-yl)ethyl)-1- (1-methylpiperidin-4-yl)urea,
• GA175
• (R)-1-methoxy-3-(1-(4- methoxynaphthalen-1-yl)ethyl)-1- (1-methylpiperidin-4-yl)urea,
• GA176
• (S)-1-methoxy-3-(1-(4- methoxynaphthalen-1-yl)ethyl)-1- (1-methylpiperidin-4-yl)urea,
• GA177
• 3-(1-(2,3-dichlorophenyl)ethyl)-1- hydroxy-1-(1-methylpiperidin-4- yl)urea,
• GA178
• (R)-3-(1-(2,3- dichlorophenyl)ethyl)-1-hydroxy- 1-(1-methylpiperidin-4-yl)urea,
• GA179
• (S)-3-(1-(2,3- dichlorophenyl)ethyl)-1-hydroxy- 1-(1-methylpiperidin-4-yl)urea,
• GA180
• 3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-hydroxy- 1-(1-methylpiperidin-4-yl)urea,
• GA181
• (R)-3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-hydroxy- 1-(1-methylpiperidin-4-yl)urea,
• GA182
• (S)-3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-hydroxy- 1-(1-methylpiperidin-4-yl)urea,
• GA183
• 3-(1-(2,3-dichloro-4- (dimethylamino)phenyl)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA184
• 3-(1-(4-((4- methoxybenzyl)oxy)naphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA185
• 3-(1-(4-hydroxynaphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpyridin-4-yl)urea,
• GA186
• 3-(1-(4,5-dimethoxynaphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA187
• 3-(1-(2,3-dichlorophenyl)-2- (pyridin-3-ylmethoxy)ethyl)-1- methyl-1-(1-methylpiperidin-4- yl)urea,
• GA188
• 3-(1-(4-chlorobenzo[d][1,3]dioxol- 5-yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA189
• 3-(1-(2-chloro-3,4- dimethoxyphenyl)ethyl)-1-methyl- 1-(1-methylpiperidin-4-yl)urea,
• GA190
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(1-(2,3,4- trichlorophenyl)ethyl)urea,
• GA191
• 1-methyl-1-(1-methylpiperidin-4- yl)-3-(1-(4-(pyridin-4- ylmethoxy)naphthalen-1- yl)ethyl)urea,
• GA192
• 3-(1-(6-chloro[1,1′-biphenyl]-2- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA193
• 3-(1-(3-chloro-2-(pyridin-4- yl)phenyl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea,
• GA194
• 3-(1-(2,3-dichloro-4- methylphenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA195
• 3-(1-(3-chloro-2- methylphenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA196
• 3-(1-(2,3-dichlorophenyl)-2-((4- (hydroxymethyl)benzyl)oxy)ethyl)- 1-methyl-1-(1-methylpiperidin-4- yl)urea,
• GA197
• 3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA198
• (R)-3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA199
• (S)-3-(1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methyl-1- (1-methylpiperidin-4-yl)urea,
• GA201
• 3-((R)-1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methyl-1- (1,3,3-trimethylpiperidin-4-yl)urea,
• GA202
• 3-((S)-1-(2,3-dichloro-4- methoxyphenyl)ethyl)-1-methyl-1- (1,3,3-trimethylpiperidin-4-yl)urea, and
• GA203
• 3-(1-(4-(2- (benzyloxy)ethoxy)naphthalen-1- yl)ethyl)-1-methyl-1-(1- methylpiperidin-4-yl)urea.