Claims
- 1. A compound, including all enatiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, said compound having the formula:
- 2. A compound according to claim 1 wherein R units are selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, 4-chlorophenyl, 4-hydroxyphenyl, 4-methylphenyl, and 4-acetoxyphenyl.
- 3. A compound according to claim 1 wherein W1 has the formula:
- 4. A compound according to claim 3 wherein R1 is cyclohexyl.
- 5. A compound according to claim 1 wherein W1 has the formula:
- 6. A compound according to claim 1 wherein W2 is a short chain substituted or non-substituted amide selected form the group consisting of —C(O)NHCH3; —C(O)NHCH2CH3; —C(O)NHCH(CH3)2; —C(O)NHCH2CH2CH3; —C(O)NH2; —C(O)NHCH2CH2CH2CH3; —C(O)NHCH2CH(CH3)2; —C(O)NHCH2CH═CHCH3; —C(O)NHCH2CH2CH(CH3)2; —C(O)NHCH2C(CH3)3; —C(O)NHCH2CH2SCH3; —C(O)NHCH2CH2OH; —NHC(O)CH3; —NHC(O)CH2CH3; and —NHC(O)CH2CH2CH3.
- 7. A compound according to claim 1 wherein W2 unit has the formula:
- 8. A compound according to claim 1 wherein W2 unit has the formula:
- 9. A compound according to claim 1 having the formula:
- 10. A compound according to claim 9 wherein R is 3-chlorophenyl.
- 11. A compound according to claim 9 wherein W1 is has the formula:
- 12. A compound according to claim 1 wherein W1 has the formula:
- 13. A compound according to claim 1 wherein W2 unit has the formula:
- 14. A compound according to claim 13 wherein W2 has the formula:
a) —(CH2)yNHC(O)NH2; b) —(CH2)yNHC(═NH)NH2; c) —(CH2)yNHC(═NCH3)NHCN; d) —(CH2)yNHC(═NNO2)NHCN; e) —(CH2)yNHC(═NCH3)NHNO2; f) —(CH2)yNHC(═NCN)NHNO2; and g) —(CH2)yNHC(═NCN)NH2; wherein y is 1, 2, or 3.
- 15. A compound according to claim 14 having the formula:
- 16. A compound according to claim 15 wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, 4-chlorophenyl, 4-hydroxyphenyl, 4-methylphenyl, and 4-acetoxy-phenyl.
- 17. A compound according to claim 16 wherein R is 3-chlorophenyl.
- 18. A compound, or a pharmaceutically acceptable salt thereof, having the formula:
- 19. A compound according to claim 18 wherein R units are selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, 4-chlorophenyl, 4-hydroxyphenyl, 4-methylphenyl, and 4-acetoxyphenyl.
- 20. A compound according to claim 18 wherein R2 is selected from the group consisting of:
i) thiazolyl, 2-methylthiazolyl, 4-mentylthiazolyl, 5-methylthiazolyl having the formula: 63ii) 1,3,4-thiadiazolyl, 2-methyl-1,3,4-thiadiazolyl having the formula: 64iii) 1,2,5-thiadiazolyl, 3-methyl-1,2,5-thiadiazolyl having the formula: 65iv) oxazolyl, 2-methyloxazolyl, 4-methyloxazolyl, 5-methyloxazolyl having the formula: 66v) imidazolyl, 2-methylimidazolyl, 5-methylimidazolyl having the formula: 67vi) 5-methyl-1,2,4-oxadiazolyl, 2-methyl-1,3,4-oxadiazolyl, 5-amino-1,2,4-oxadiazolyl, having the formula: 68vii) 1,2-dihydro[1,2,4]triazol-3-one-1-yl, 2-methyl-1,2-dihydro[1,2,4]triazol-3-one-5-yl, having the formula: 69viii) oxazolidin-2-one-3-yl; 4,4-dimethyloxazolidin-2-one-3-yl; imidazolidin-2-one-1-yl; 1-methylimidazolidin-2-one-1-yl, having the formula: 70ix) 2-methyl-1,3,4-oxadiazolyl, 2-amino-1,3,4-oxadiazolyl, 2-(N,N-dimethylamino)-1,3,4-oxadiazolyl, having the formula: 71
- 21. A compound according to claim 18 selected from the group having the formula:
- 22. A compound according to claim 21 wherein R is selected from the group consisting of phenyl, 3-fluorophenyl, 4-fluorophenyl, 3,5-difluorophenyl, 4-chlorophenyl, 4-hydroxyphenyl, 4-methylphenyl, and 4-acetoxyphenyl.
- 23. A composition comprising:
A) an effective amount of one or more melanocortin receptor ligands, said ligands having all enatiomeric and diasteriomeric forms and their pharmaceutically acceptable salts, said ligands having the formula: 73wherein R is a substituted or unsubstituted hydrocarbyl unit selected from the group consisting of:
a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; W1 is a pendant unit having the formula:: 74R1 is selected from the group consisting of:
i) hydrogen; ii) C3-C8 non-aromatic carbocyclic rings; iii) C6-C14 aromatic carbocyclic rings; iv) C1-C7 non-aromatic heterocyclic rings; and v) C3-C13 aromatic heterocyclic rings; R3a and R3b are each independently selected from the group consisting of
i) hydrogen; ii) methyl; and iii) R3a and R3b can be taken together to form a carbonyl unit; the index x has the value from 0 to 10; W2 is a pendant unit having the formula: 75R2 is selected from the group consisting of:
i) hydrogen; ii) C3-C8 non-aromatic carbocyclic rings; iii) C6-C14 aromatic carbocyclic rings; iv) C1-C7 non-aromatic heterocyclic rings; v) C3-C13 aromatic heterocyclic rings; vi) —C(Y)R4; vii) —C(Y)2R; viii) —C(Y)N(R4)2; ix) —C(Y)NR4N(R4)2; x) —CN; xi) —[C(R4)2]C(R4)2; xii) —N(R4)2; xiii) —NR4CN; xiv) —NR5C(Y)R4; xv) —NR5C(Y)N(R4)2; xvi) —NHN(R4)2; xvii) —NHOR4; xviii) —NO2; xix) —OR4; xx) and mixtures thereof; Y is —O—, —S—, ═O, ═S, ═NR4, —R4, and mixtures thereof; R4 is hydrogen, C1-C4alkyl, —OH, and mixtures thereof; R5 is hydrogen, halogen, and mixtures thereof; M is hydrogen or a salt forming cation; R3a and R3b are the same as above; the index y has the value from 0 to 10; and B) one or more pharmaceutically acceptable excipients.
- 24. A method for controlling weight gain in a human or higher mammal, said method comprising the step of administering to said human or higher mammal an effective amount of one or more melanocortin receptor ligands, said ligands having all enatiomeric and diasteriomeric forms and their pharmaceutically acceptable salts, said ligands having the formula:
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims priority under Title 35, United States Code 119(e) from Provisional Application Serial No. 60/376,727, filed Apr. 30, 2002.
Provisional Applications (1)
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Number |
Date |
Country |
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60376727 |
Apr 2002 |
US |