2-Oxoethyl derivatives as immunosuppressants

Claim 2

A compound of the following structure wherein R' is a) hydrogen, b) linear or branched alkyl (C1-C8) which may be substituted independently or simultaneously up to two times by i) hydroxy, ii) phenyl which may be substituted by straight or branched alkyl (C1-C8), or straight or branched alkoxy (C1-C6), iii) cycloalkyl (C3-C10) which may be substituted by straight or branched alkyl (C1-C8), or straight or branched alkoxy (C1-C6), iv) bicycloalkyl (C6-C12) which may be substituted by straight or branched alkyl (C1-C10), or straight or branched alkoxy (C1-C6), v) tricycloalkyl (C7-C14) which may be substituted by straight or branched alkyl (C1-C8), or straight or branched alkoxy (C1-C6), vi) tetracycloalkyl (C10-C14), which may be substituted by straight or branched alkyl (C1-C8), or straight or branched alkoxy (C1-C6), or vii) morpholinyl, c) alkene (C3-C10), diene (C4-C10), or triene (C8-C18), which may be substituted independently or simultaneously up to three times by i) phenyl, ii) straight or branched alkyl (C1-C6), or iii) straight or branched alkoxy (C1-C6), d) cycloalkyl (C5-C10), or the cycloalkyl fragment where m is an integer of 0, 1, or 2, J, K, and L are independently or simultaneously i) hydrogen, ii) straight or branched alkyl (C1-C5), which may be substituted by phenyl, or straight or branched alkoxy (C1-C6), iii) straight or branched alkoxy (C1-C5), iii) phenyl, or iv) phenyl substituted by straight or branched alkyl (C1-C6), or chlorine, or straight or branched alkoxy (C1-C6), e) bicycloalkyl (C7-10), tricycloalkyl (C7-14), tetracycloalkyl (C10-C16), or pentacycloalkyl (C11-C20), which may be independently or simultaneously substituted up to 3 times with straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C6), or phenyl, f) the aryl derivatives tetrahydronaphthyl, benzothienyl, benzofuryl, benzopyranyl, furyl, pyridyl, pyranyl, 1,3-oxazolyl, or naphthyl, said aryl derivatives may be independently or simultaneously substituted up to two times by i) straight or branched alkyl (C1-C6), ii) straight or branched alkoxy (C1-C6), iii) halogen, where halogen is fluoro, chloro, bromo, or iodo, g) the piperonyl fragment where z is an integer of 1, or 2, and E 1 , E 2 , and E 3 can independently or simultaneously be hydrogen, straight or branched alkyl (C1-C6), straight or branched alkoxy (C1-C6), or chlorine, or h) the aryl derivative where U, V, and W can be independently or simultaneously i) hydrogen, ii) straight or branched alkyl (C1-C6), straight or branched alkoxy (C1-C6), phenyl, or phenoxy, these groups may be substituted by phenyl, straight or branched alkoxy (C1-C6), or phenoxy, iii) hydroxy, iv) halogen, v) nitro, or vi) benzoyl; Y is a covalent bond, oxygen, NR 7 , where R 7 is hydrogen, in addition, R'-Y- may also be where k is an integer of 1 or 2

Claim 3

R 8 is a) hydrogen, b) carboalkoxy with a straight or branched alkoxy (C1-C6), c) straight or branched alkyl (C1-C6) which may be substituted by phenyl, or straight or branched alkoxy (C1-C6), d) phenyl, or phenyl substituted by halogen,

Claim 4

R 8 is a) hydrogen, b) carboalkoxy with a straight or branched alkoxy (C1-C6), c) straight or branched alkyl (C1-C6) which may be substituted by phenyl, or straight or branched alkoxy (C1-C6), d) phenyl, or phenyl substituted by halogen,

Claim 5

R 9 is phenyl which may be substituted by straight or branched alkyl (C1-C6):

Claim 6

R 9 is phenyl which may be substituted by straight or branched alkyl (C1-C6):

Claim 7

R 2 and R 3 are defined as follows: one of R 2 and R 3 are hydrogen, and the other is hydrogen or straight or branched alkyl (C1-C6);

Claim 8

R 2 and R 3 are defined as follows: one of R 2 and R 3 are hydrogen, and the other is hydrogen or straight or branched alkyl (C1-C6);

Claim 9

n is an integer of 2 or 3;

Claim 10

n is an integer of 2 or 3;

Claim 11

A is oxygen or NR 10 , where R 10 is hydrogen or straight or branched alkyl (C1-C6);

Claim 12

A is oxygen or NR 10 , where R 10 is hydrogen or straight or branched alkyl (C1-C6);

Claim 13

R 4 and R 5 may independently or simultaneously be a) hydrogen, b) straight or branched alkyl (C1-C8) which may be substituted by i) phenyl, or phenyl substituted by hydroxy or alkoxy (C1-C2), ii) cycloalkyl (C5-C6), iii) alkylthio (C1-C6), iv) carboxamido, v) straight or branched alkoxy (C1-C6) which may be substituted by phenyl, c) phenyl, or d) cycloalkyl (C3-C7), which may be substituted by straight or branched alkyl (C1-C6), in addition, R 4 and R 5 , taken together can be -(CH 2 );-- where r is an integer of 4 or 5; G is one of the following fragments -HC = CH-, -CH2 CH2-, or -CH 2 - or one of the following fragments where R 12 is hydrogen or methyl, such that the carbonyl group is attached to the carbon bearing R 4 and R 5 and that NR 12 and oxygen are connected to R6, respectively; p is an integer of 0 or 1;

Claim 14

R 4 and R 5 may independently or simultaneously be a) hydrogen, b) straight or branched alkyl (C1-C8) which may be substituted by i) phenyl, or phenyl substituted by hydroxy or alkoxy (C1-C2), ii) cycloalkyl (C5-C6), iii) alkylthio (C1-C6), iv) carboxamido, v) straight or branched alkoxy (C1-C6) which may be substituted by phenyl, c) phenyl, or d) cycloalkyl (C3-C7), which may be substituted by straight or branched alkyl (C1-C6), in addition, R 4 and R 5 , taken together can be -(CH 2 );-- where r is an integer of 4 or 5; G is one of the following fragments -HC = CH-, -CH2 CH2-, or -CH 2 - or one of the following fragments where R 12 is hydrogen or methyl, such that the carbonyl group is attached to the carbon bearing R 4 and R 5 and that NR 12 and oxygen are connected to R6, respectively; p is an integer of 0 or 1;

Claim 15

R 6 is a) hydrogen, b) straight or branched alkyl (C1-C6) which may be substituted by i) phenyl, ii) phenyl substituted with straight or branched alkyl (C1-C6), straight or branched alkoxy (C1-C6), or iii) pyridyl, or c) phenyl, naphthyl, furyl, thiofuryl, cycloalkyl (C5-C8), bicycloalkyl (C6-C10), tricycloalkyl (C7-C12), tetracycloalkyl (C10-C16), pentacycloalkyl (C11-C20) or benzoyl, such groups may be substituted by i) an amine, ii) amino substituted by a straight or branched alkoxycarbonyl (C1-C6) that may be substituted by phenyl or an alkene (C2-C6), iii) amino substituted by alkanoyl (C1-C6), or benzoyl, iv) sulfonamide (-S0 2 NH 2 ), or v) hydroxy, or a straight or branched alkoxy (C1-C6), that may be substituted by phenyl; and said composition's pharmacuetically acceptable salts.

Claim 16

R 6 is a) hydrogen, b) straight or branched alkyl (C1-C6) which may be substituted by i) phenyl, ii) phenyl substituted with straight or branched alkyl (C1-C6), straight or branched alkoxy (C1-C6), or iii) pyridyl, or c) phenyl, naphthyl, furyl, thiofuryl, cycloalkyl (C5-C8), bicycloalkyl (C6-C10), tricycloalkyl (C7-C12), tetracycloalkyl (C10-C16), pentacycloalkyl (C11-C20) or benzoyl, such groups may be substituted by i) an amine, ii) amino substituted by a straight or branched alkoxycarbonyl (C1-C6) that may be substituted by phenyl or an alkene (C2-C6), iii) amino substituted by alkanoyl (C1-C6), or benzoyl, iv) sulfonamide (-S0 2 NH 2 ), or v) hydroxy, or a straight or branched alkoxy (C1-C6), that may be substituted by phenyl; and said composition's pharmacuetically acceptable salts.

Claim 17

A compound of the following structure wherein R' is a) hydrogen, b) linear or branched alkyl (C1-C6) which may be substituted i) once by hydroxy, ii) once by phenyl which may be substituted by straight or branched alkyl (C1-C4), or straight or branched alkoxy (C1-C6), iii) once by cycloalkyl (C3-C8) which may be substituted by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), iv) once by bicycloalkyl (C6-C10) which may be substituted by straight or branched alkyl (C1-C8), or straight or branched alkoxy (C1-C4), v) once by tricycloalkyl (C7-C12) which may be substituted by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), vi) once by tetracycloalkyl (C10-C12), which may be substituted by straight or branched alkyl (C1-C8), or straight or branched alkoxy (C1-C4), vii) up to two times by phenyl and cycloalkyl (C5-C7), or viii) up to two times by phenyl and morpholinyl, c) alkene (C3-C8), which may be substituted by phenyl, straight or branched alkyl (C1-C4), or straight or branched alkoxy (C1-C4), d) diene (C4-C7) substituted by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), e) triene (C10-C16) substituted up to three times by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), or f) cycloalkyl (C5-C10), or the cycloalkyl fragment where m is an integer of 0, 1, or 2, J, K, and L are independently or simultaneously i) hydrogen, ii) straight or branched alkyl (C1-C5), which may be substituted by phenyl, or straight or branched alkoxy (C1-C4), iii) phenyl, or iv) phenyl substituted by straight or branched alkyl (C1-C4), or chlorine, or straight or branched alkoxy (C1-C4), g) bicycloalkyl (C7-10) which may be substituted up to 3 times with straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), h) tricycloalkyl (C7-14) which may be substituted up to 3 times with straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), i) tetracycloalkyl (C10-C15) which may be substituted up to 3 times by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), j) naphthyl derivatives, or the heteroaryl derivatives benzothienyl, benzofuryl, benzopyranyl, furyl, pyridyl, pyranyl, or 1,3-oxazolyl, said derivatives may be substituted up to two times by i) straight or branched alkyl (C1-C6), ii) halogen, iii) or both, k) 1,2,3,4-tetrahydronaphthyl, I) the piperonyl fragment where z is an integer of 1, or 2, and E 1 , E 2 , and E 3 can be independently or simultaneously hydrogen, straight or branched alkyl (C1-C4), straight or branched alkoxy (C1-C4), or chlorine, m) the aryl derivative where U, V, and W can be independently or simultaneously i) hydrogen, ii) straight or branched alkyl (C1-C4), which may be substituted by phenyl, iii) straight or branched alkoxy (C1-C6) which may be substituted by phenyl, straight or branched alkoxy (C1-C4), or phenoxy, iv) hydroxy, v) phenyl, vi) halogen, vii) nitro, viii) benzoyl, or ix) phenoxy; Y is a covalent bond, oxygen, NR 7 , where R 7 is hydrogen, in addition, R'-Y- may also be where k is an integer of 1, or 2, R 8 is a) hydrogen, b) carboalkoxy with a straight or branched alkoxy (C1-C4), c) straight or branched alkyl (C1-C4) which may be substituted by phenyl, or straight or branched alkoxy (C1-C4), or d) phenyl, or phenyl substituted by halogen, R 9 is phenyl which may be substituted by alkyl (C1-C4); R 2 and R 3 are defined as follows: one of R 2 and R 3 are hydrogen, and the other is hydrogen or straight or branched alkyl (C1-C6); n is an integer of 2 or 3; A is oxygen or NR 10 , where R 10 is hydrogen or straight or branched alkyl (C1-C4); R 4 is a) hydrogen, b) straight or branched alkyl (C1-C6) which may be substituted by i) phenyl, or phenyl substituted by hydroxy or methoxy, ii) cycloalkyl (C5-C6), iii) alkylthio (C1-C6), iv) carboxamido, or v) straight or branched alkoxy (C1-C6) which may be substituted by phenyl, c) phenyl, or d) cycloalkyl (C3-C7), which may be substituted by straight or branched alkyl (C1-C6); R 5 is hydrogen or straight or branched alkyl (C1-C4), and R 4 and R 5 , taken together can be -(CH2)r-- where r is an integer of 4 or 5; G is one of the following fragments -HC = CH-, -CH2 CH2-, or -CH 2 - or one of the following fragments where the carbonyl group is attached to the carbon bearing R 4 and R 5 and NR 12 and oxygen are connected to R 6 , respectively, R 12 is hydrogen or methyl; p is an integer of 0 or 1; R 6 is a) hydrogen, b) straight or branched alkyl (C1-C4) which may be substituted by i) phenyl, ii) phenyl substituted with straight or branched alkyl (C1-C4), straight or branched alkoxy (C1-C4), or iii) 2- or 4-pyridyl, c) phenyl or naphthyl, which may be substituted by i) amine, ii) amino substituted by a straight or branched alkoxycarbonyl (C1-C6) that may be substituted by phenyl or an alkene (C2-C6), iii) amino substituted by alkanoyl (C1-C6), or benzoyl, iv) sulfonamide (-S0 2 NH 2 ), or v ) straight or branched alkoxy (C1-C6), that may be substituted by phenyl, d) benzoyl, e) furyl, or thiofuryl, or f) cycloalkyl (C5-C8), bicycloalkyl (C6-C10), tricycloalkyl (C7-C12), or tetracycloalkyl (C10-C14); and said composition's pharmacuetically acceptable salts.

Claim 18

A compound of the following structure wherein R' is a) hydrogen, b) linear or branched alkyl (C1-C6) which may be substituted i) once by hydroxy, ii) once by phenyl which may be substituted by straight or branched alkyl (C1-C4), or straight or branched alkoxy (C1-C6), iii) once by cycloalkyl (C3-C8) which may be substituted by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), iv) once by bicycloalkyl (C6-C10) which may be substituted by straight or branched alkyl (C1-C8), or straight or branched alkoxy (C1-C4), v) once by tricycloalkyl (C7-C12) which may be substituted by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), vi) once by tetracycloalkyl (C10-C12), which may be substituted by straight or branched alkyl (C1-C8), or straight or branched alkoxy (C1-C4), vii) up to two times by phenyl and cycloalkyl (C5-C7), or viii) up to two times by phenyl and morpholinyl, c) alkene (C3-C8), which may be substituted by phenyl, straight or branched alkyl (C1-C4), or straight or branched alkoxy (C1-C4), d) diene (C4-C7) substituted by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), e) triene (C10-C16) substituted up to three times by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), or f) cycloalkyl (C5-C10), or the cycloalkyl fragment where m is an integer of 0, 1, or 2, J, K, and L are independently or simultaneously i) hydrogen, ii) straight or branched alkyl (C1-C5), which may be substituted by phenyl, or straight or branched alkoxy (C1-C4), iii) phenyl, or iv) phenyl substituted by straight or branched alkyl (C1-C4), or chlorine, or straight or branched alkoxy (C1-C4), g) bicycloalkyl (C7-10) which may be substituted up to 3 times with straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), h) tricycloalkyl (C7-14) which may be substituted up to 3 times with straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), i) tetracycloalkyl (C10-C15) which may be substituted up to 3 times by straight or branched alkyl (C1-C6), or straight or branched alkoxy (C1-C4), j) naphthyl derivatives, or the heteroaryl derivatives benzothienyl, benzofuryl, benzopyranyl, furyl, pyridyl, pyranyl, or 1,3-oxazolyl, said derivatives may be substituted up to two times by i) straight or branched alkyl (C1-C6), ii) halogen, iii) or both, k) 1,2,3,4-tetrahydronaphthyl, I) the piperonyl fragment where z is an integer of 1, or 2, and E 1 , E 2 , and E 3 can be independently or simultaneously hydrogen, straight or branched alkyl (C1-C4), straight or branched alkoxy (C1-C4), or chlorine, m) the aryl derivative where U, V, and W can be independently or simultaneously i) hydrogen, ii) straight or branched alkyl (C1-C4), which may be substituted by phenyl, iii) straight or branched alkoxy (C1-C6) which may be substituted by phenyl, straight or branched alkoxy (C1-C4), or phenoxy, iv) hydroxy, v) phenyl, vi) halogen, vii) nitro, viii) benzoyl, or ix) phenoxy; Y is a covalent bond, oxygen, NR 7 , where R 7 is hydrogen, in addition, R'-Y- may also be where k is an integer of 1, or 2, R 8 is a) hydrogen, b) carboalkoxy with a straight or branched alkoxy (C1-C4), c) straight or branched alkyl (C1-C4) which may be substituted by phenyl, or straight or branched alkoxy (C1-C4), or d) phenyl, or phenyl substituted by halogen, R 9 is phenyl which may be substituted by alkyl (C1-C4); R 2 and R 3 are defined as follows: one of R 2 and R 3 are hydrogen, and the other is hydrogen or straight or branched alkyl (C1-C6); n is an integer of 2 or 3; A is oxygen or NR 10 , where R 10 is hydrogen or straight or branched alkyl (C1-C4); R 4 is a) hydrogen, b) straight or branched alkyl (C1-C6) which may be substituted by i) phenyl, or phenyl substituted by hydroxy or methoxy, ii) cycloalkyl (C5-C6), iii) alkylthio (C1-C6), iv) carboxamido, or v) straight or branched alkoxy (C1-C6) which may be substituted by phenyl, c) phenyl, or d) cycloalkyl (C3-C7), which may be substituted by straight or branched alkyl (C1-C6); R 5 is hydrogen or straight or branched alkyl (C1-C4), and R 4 and R 5 , taken together can be -(CH2)r-- where r is an integer of 4 or 5; G is one of the following fragments -HC = CH-, -CH2 CH2-, or -CH 2 - or one of the following fragments where the carbonyl group is attached to the carbon bearing R 4 and R 5 and NR 12 and oxygen are connected to R 6 , respectively, R 12 is hydrogen or methyl; p is an integer of 0 or 1; R 6 is a) hydrogen, b) straight or branched alkyl (C1-C4) which may be substituted by i) phenyl, ii) phenyl substituted with straight or branched alkyl (C1-C4), straight or branched alkoxy (C1-C4), or iii) 2- or 4-pyridyl, c) phenyl or naphthyl, which may be substituted by i) amine, ii) amino substituted by a straight or branched alkoxycarbonyl (C1-C6) that may be substituted by phenyl or an alkene (C2-C6), iii) amino substituted by alkanoyl (C1-C6), or benzoyl, iv) sulfonamide (-S0 2 NH 2 ), or v ) straight or branched alkoxy (C1-C6), that may be substituted by phenyl, d) benzoyl, e) furyl, or thiofuryl, or f) cycloalkyl (C5-C8), bicycloalkyl (C6-C10), tricycloalkyl (C7-C12), or tetracycloalkyl (C10-C14); and said composition's pharmacuetically acceptable salts.

Claim 19

A compound of the following structure wherein R 1 is a) hydrogen, b) linear or branched alkyl (C1-C6) which may be substituted by i) hydroxy, ii) phenyl, or phenyl substituted by straight or branched alkyl (C1-C4), iii) cycloalkyl (C3-C8) which may be substituted by straight or branched alkyl (C1-C4), iv) bicycloalkyl (C6-C9) which may be substituted by straight or branched alkyl (C1-C6), v) tricycloalkyl (C7-C12) which may be substituted by straight or branched alkyl (C1-C4), vi) tetracycloalkyl (C10-C12), which may be substituted by straight or branched alkyl (C1-C6), vii) both phenyl and cycloalkyl (C5-C6), or viii) both phenyl and morpholinyl, c) alkene (C3-C6), which may be substituted by phenyl, d) diene (C5-C6) substituted by straight or branched alkyl (C1-C4), e) triene (C13-C16) substituted up to three times by straight or branched alkyl (C1-C4), f) cycloalkyl (C5-C6), or the cycloalkyl fragment where m is an integer of 0, 1, or 2, J, K, and L are independently or simultaneously i) hydrogen, ii) straight or branched alkyl (C1-C5), iii) phenyl, or iv) phenyl substituted by straight or branched alkyl (C1-C4), or chlorine, or straight or branched alkoxy (C1-C4), g) bicycloalkyl (C7-8) which may be substituted up to 3 times with straight or branched alkyl (C1-C4), h) tricycloalkyl (C7-12) which may be substituted up to 2 times with straight or branched alkyl (C1-C6), i) tetracycloalkyl (C10-C12) which may be substituted up to 3 times by straight or branched alkyl (C1-C4), j) 2-benzothienyl substituted independently or simultaneously at least twice by either i) straight or branched alkyl (C1-C3), ii) chlorine, iii) or both, k) 2-furyl, I) 2-pyridyl, m) 2-naphthyl, n) 1,2,3,4-tetrahydronaphthyl, o) 2-benzopyranyl, p) 2-benzofuryl, q) the piperonyl fragment where z is an integer of 1, or 2, and E 1 , E 2 , and E 3 are hydrogen, or r) the aryl derivative where U, V, and W can be independently or simultaneously i) hydrogen, i) straight or branched alkyl (C1-C4), ii) straight or branched alkoxy (C1-C4), iii) alkoxy (C2) substituted by alkoxy (C2), or phenoxy, iv) hydroxy, v) phenyl, vi) fluorine, vii) chlorine, viii) bromine, ix) nitro, x) benzyloxy, xi) benzoyl, xii) phenoxy; Y is a covalent bond, oxygen, NR 7 , where R 7 is hydrogen; in addition, R'-Y- may also be where k is an integer of 1, or 2, R 8 is a) hydrogen, b) carboalkoxy with alkoxy (C1-C2), c) straight or branched alkyl (C1-C4) which may be substituted by phenyl, d) phenyl, R 9 is phenyl; R 2 and R 3 are defined as follows: one of R 2 and R 3 is hydrogen, and the other is hydrogen or straight or branched alkyl (C1-C4); n is an integer of 2 or 3; A is oxygen or NR 10 , where R 10 is hydrogen or methyl; R 4 is a) hydrogen, b) straight or branched alkyl (C1-C4) which may be substituted by i) phenyl, ii) cycloalkyl (C5-C6), iii) alkylthio (C1-C4), iv) carboxamido, or v) benzyloxy, or c) phenyl; R 5 is hydrogen or straight or branched alkyl (C1-C4), and R 4 and R 5 , taken together can be -(CH 2 ) r -- where r is integer 5; G is one of the following fragments -HC = CH-, -CH2 CH2-, or -CH 2 - or one of the following fragments where the carbonyl group is attached to the carbon bearing R 4 and R 5 and NR 12 and oxygen are connected to R 6 , respectively, R 12 is hydrogen or methyl; p is an integer of 0 or 1; R 6 is a) hydrogen, b) straight or branched alkyl (C1-C4) which may be substituted by i) phenyl, ii) phenyl substituted with alkoxy (C1-C2), iii) 2- or 4-pyridyl, c) phenyl which may be substituted by i) amino, ii) amino substituted by allyloxycarbonyl, iii) amino substituted by acetyl, iv) amino substituted by benzoyl, v) amino substituted by benzyloxycarbonyl, iii) sulfonamide (-SO 2 NH 2 ), or iv) straight or branched alkoxy (C1-C4), d) benzoyl, e) furyl, f) naphthyl, g) cycloalkyl (C5-C8), or h) tetracycloalkyl (C10-C12); and said composition's pharmacuetically acceptable salts.

Claim 20

A compound of the following structure wherein R 1 is a) hydrogen, b) linear or branched alkyl (C1-C6) which may be substituted by i) hydroxy, ii) phenyl, or phenyl substituted by straight or branched alkyl (C1-C4), iii) cycloalkyl (C3-C8) which may be substituted by straight or branched alkyl (C1-C4), iv) bicycloalkyl (C6-C9) which may be substituted by straight or branched alkyl (C1-C6), v) tricycloalkyl (C7-C12) which may be substituted by straight or branched alkyl (C1-C4), vi) tetracycloalkyl (C10-C12), which may be substituted by straight or branched alkyl (C1-C6), vii) both phenyl and cycloalkyl (C5-C6), or viii) both phenyl and morpholinyl, c) alkene (C3-C6), which may be substituted by phenyl, d) diene (C5-C6) substituted by straight or branched alkyl (C1-C4), e) triene (C13-C16) substituted up to three times by straight or branched alkyl (C1-C4), f) cycloalkyl (C5-C6), or the cycloalkyl fragment where m is an integer of 0, 1, or 2, J, K, and L are independently or simultaneously i) hydrogen, ii) straight or branched alkyl (C1-C5), iii) phenyl, or iv) phenyl substituted by straight or branched alkyl (C1-C4), or chlorine, or straight or branched alkoxy (C1-C4), g) bicycloalkyl (C7-8) which may be substituted up to 3 times with straight or branched alkyl (C1-C4), h) tricycloalkyl (C7-12) which may be substituted up to 2 times with straight or branched alkyl (C1-C6), i) tetracycloalkyl (C10-C12) which may be substituted up to 3 times by straight or branched alkyl (C1-C4), j) 2-benzothienyl substituted independently or simultaneously at least twice by either i) straight or branched alkyl (C1-C3), ii) chlorine, iii) or both, k) 2-furyl, I) 2-pyridyl, m) 2-naphthyl, n) 1,2,3,4-tetrahydronaphthyl, o) 2-benzopyranyl, p) 2-benzofuryl, q) the piperonyl fragment where z is an integer of 1, or 2, and E 1 , E 2 , and E 3 are hydrogen, or r) the aryl derivative where U, V, and W can be independently or simultaneously i) hydrogen, i) straight or branched alkyl (C1-C4), ii) straight or branched alkoxy (C1-C4), iii) alkoxy (C2) substituted by alkoxy (C2), or phenoxy, iv) hydroxy, v) phenyl, vi) fluorine, vii) chlorine, viii) bromine, ix) nitro, x) benzyloxy, xi) benzoyl, xii) phenoxy; Y is a covalent bond, oxygen, NR 7 , where R 7 is hydrogen; in addition, R'-Y- may also be where k is an integer of 1, or 2, R 8 is a) hydrogen, b) carboalkoxy with alkoxy (C1-C2), c) straight or branched alkyl (C1-C4) which may be substituted by phenyl, d) phenyl, R 9 is phenyl; R 2 and R 3 are defined as follows: one of R 2 and R 3 is hydrogen, and the other is hydrogen or straight or branched alkyl (C1-C4); n is an integer of 2 or 3; A is oxygen or NR 10 , where R 10 is hydrogen or methyl; R 4 is a) hydrogen, b) straight or branched alkyl (C1-C4) which may be substituted by i) phenyl, ii) cycloalkyl (C5-C6), iii) alkylthio (C1-C4), iv) carboxamido, or v) benzyloxy, or c) phenyl; R 5 is hydrogen or straight or branched alkyl (C1-C4), and R 4 and R 5 , taken together can be -(CH 2 ) r -- where r is integer 5; G is one of the following fragments -HC = CH-, -CH2 CH2-, or -CH 2 - or one of the following fragments where the carbonyl group is attached to the carbon bearing R 4 and R 5 and NR 12 and oxygen are connected to R 6 , respectively, R 12 is hydrogen or methyl; p is an integer of 0 or 1; R 6 is a) hydrogen, b) straight or branched alkyl (C1-C4) which may be substituted by i) phenyl, ii) phenyl substituted with alkoxy (C1-C2), iii) 2- or 4-pyridyl, c) phenyl which may be substituted by i) amino, ii) amino substituted by allyloxycarbonyl, iii) amino substituted by acetyl, iv) amino substituted by benzoyl, v) amino substituted by benzyloxycarbonyl, iii) sulfonamide (-SO 2 NH 2 ), or iv) straight or branched alkoxy (C1-C4), d) benzoyl, e) furyl, f) naphthyl, g) cycloalkyl (C5-C8), or h) tetracycloalkyl (C10-C12); and said composition's pharmacuetically acceptable salts.

Claim 21

A compound according to Claim 1 for the treatment of inflammations.

Claim 22

The compound of claim 3 comprising a composition represented by a structure selected from the group consisting of: L-lsoleucine, N-[1-(2-Benzyloxy-2-Oxoethyl)-L-Prolyl] Benzylamide; L-lsoleucine, N-[1-(2-Methoxy-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[l-(2-Phenyl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-Naphth-2-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(Biphenyl-4-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2-Methoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(5-Chloro-3-Methyl-benzo[B]thiophene-2-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(trans,trans-Hexa-2,4-dienyl-1-oxy)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(4-Chlorophenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(4-Methylphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(4-Methoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-Methyl-N-[1-(2-Phenyl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-Phenyl-2-Oxoethyl)-L-Homoproline] Benzylamide; L-Phenylglycine, N-[1-(2-Phenyl-2-Oxoethyl)-L-Proline Benzylamide; L-Isoleucine, N-[1-(1-Methyl-2-Phenyl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(3-Methoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(3,4-Dihydroxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-Methyl-N-[1-(2-Benzyloxy-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(Carbobenzyloxymethylene)-L-Homoproline Benzylamide; L-Isoleucine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(Carbo-tert-Butoxymethylene)-L-Proline] Benzylamide; L-Isoleucine, N-[1-(2-tert-Butyl-2-Oxoethyl)-L-Proline] Benzylamide; L-Isoleucine, N-[1-(2-(2,5-Dimethoxyphenyl)-2-Oxoethyl)-L-prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2,4-Dimethoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2-Nitrophenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(4-Nitrophenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(3-Benzyloxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2,4-Dimethylphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(4-Fluorophenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(4-Bromophenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2,4-Dichlorophenylcarbamoylmethyl)-L-Proline] Benzylamide; L-Isoleucine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Homoproline] Benzylamide; L-Isoleucine, N-[1-(2-Furan-2-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-Pyrid-2-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(Adamant-1-ylcarbamoylmethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(cis-Octahydro-pentalen-1-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-[2-(2,6,6-Trimethyl-Bicyclo[3.1.1]hept-3-yl)-2-Oxoethyl]-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(4-Pentylcyclohexyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(1,2,3,4-tetrahydro-Napththalen-2-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(1-Methyl-Cyclohexyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-Oxo-2-Tricyclo[3.3.1.0 3,7 ]Non-3-yl-Ethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-Oxo-3-(3-Methyl-Adamantan-1-yl)-Propyl)-L-Prolyl] Benzylamide; L-Proline, 1-(2-Adamantan-1-yl-2-Oxoethyl) Benzyl Ester; L-Isoleucine, N-[1-(2-(Biphenyl-4-yl)-2-Oxoethyl)-L-Prolyl] 1,2,3,4-Tetrahydroisoquinolinamide; L-Isoleucine, N-[l-(2-(Biphenyl-4-yl)-2-Oxoethyl)-L-Prolyl] Benzyl Ester; L-Isoleucine, N-[1-(2-(Biphenyl-4-yl)-2-Oxoethyl)-L-Prolyl] tert-Butylamide; L-Phenylalanine, N-[1-(2-(Biphenyl-4-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Methionine, N-[1-(2-(Biphenyl-4-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; Glycine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Valine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Leucine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Phenylalanine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Norvaline, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Norleucine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Asparagine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Serine-(O-Benzyl Ether), N-[l-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-β-Phenylalanine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Cyclohexylalanine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] alpha-(S)-methylbenzylamide; L-Isoleucine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] alpha-(R)-methylbenzylamide; L-Isoleucine, N-[1-(2-Adamantan-l-yl-2-Oxoethyl)-L-Prolyl] Pyridin-4-ylmethylamide; L-Isoleucine, N-[1-(2-Adamantan-l-yl-2-Oxoethyl)-L-Prolyl] Pyridin-2-ylmethylamide; L-Isoleucine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] 4-methoxybenzylamide; L-Isoleucine, N-[1-(2-Adamantan-1-yl-2-Oxoethyl)-L-Prolyl] 2-methoxybenzylamide; L-Isoleucine, N-[l-(Carboxymethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-[2-[N-(Piperidine-3-Carboxylic Acid Ethyl Ester)]-2-Oxoethyl]-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(1,4-Dioxa-8-aza-spiro[4.5]dec-8-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-[2-(N-(4-Benzylpiperidyl))-2-Oxoethyl]-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-[2-(2-Methylpiperidine)-2-Oxoethyl]-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2-Hydroxyethylamine)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-[2-(4-Phenylpiperazine)-2-Oxoethyl]-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-[2-(1-Pyrrolidine)-2-Oxoethyl]-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-[2-(N-Cyclopentylamino)-2-Oxoethyl]-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-[2-(N-(Phenylmethylamino))-2-Oxoethyl]-L-Prolyl] Benzylamide; L-lsoleucine, N-[1-[2-(N-(Cyclohexylmethylamino))-2-Oxoethyl]-L-Prolyl] Benzylamide; L-lsoleucine, N-[1-(2-(4-Phenylpiperidyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-lsoleucine, N-[1-(2-[1-(3,7,11 -Trimethyldodeca-2,6,10-tnen-1-ol)]-2-Oxoethyl)-L-Proline] Benzylamide; L-lsoleucine, N-[1-(2-(3-Phenyl-2-Propen-1-Oxy)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(3-Phenyl-3-Methyl-2-Propen-1-Oxy)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(1-Phenylpropoxy)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(1-Phenyl-1-Cyclohexylmethoxy)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(1-Phenyl-2-(4-Morpholino)Ethoxy)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2-Oxy-2-Methyladamant-2-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(Adamantan-2-ylcarbamoylmethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(Adamant-1-ylmethylcarbamoylmethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2-Methyl-1-(S)-Phenyl-1-Propoxy)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2-Methyl-1-(R)-Phenyl-1-Propoxy)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(4-tert-Butylcyclohexyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-Bicyclo[2.2.1 ]hept-2yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[l-(2-(Chroman-2-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide Hydrochloride Salt; L-Isoleucine, N-[l-(2-(Benzofuran-2-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide Hydrochloride Salt; L-Isoleucine, N-[1-(2-(3-Benzoyloxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(4-Benzoyloxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2-Benzoyloxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(3-Phenoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2-Phenoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(3,4,5-Triethoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(Benzo[1,3]dioxol-5-yl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-{2-Oxo-2-[4-(2-Phenoxyethoxy)-Phenyl]-Ethyl}-L-Prolyl]Benzylamide; L-Isoleucine, N-[1-(2-(4-Phenoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2,4,6-Trimethoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2,3-Dimethoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2,6-Dimethoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(1-(4-Methylphenyl)cyclohexyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(1-(4-Chlorophenyl)cyclohexyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2,3,4-Trimethoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(1-Phenylcyclohexyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; L-Isoleucine, N-[1-(2-(2,4,5-Trimethoxyphenyl)-2-Oxoethyl)-L-Prolyl] Benzylamide; 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] L-Proline Benzyl Ester Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] Benzylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-Phenethylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 3-Phenylpropylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 4-Phenylbutylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-(Pyrid-2-yl)ethylamide Dihydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-(4-aminophenyl)ethylamide Dihydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 3-(4-[N-Carboallyloxy]aminophenyl)propyl Ester Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-Phenyl-2 oxoethylamide; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] Tetrahydrofurfurylamide; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] Naphthalen-1-ylmethylamide; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-(4-Sulfamoylphenyl)ethylamide; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 4-Phenylpiperidenylamide; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 4-Methoxybenzamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 3-Methoxybenzamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-Methoxybenzamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] N-Methylphenethylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] (S)-a-methylbenzylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] (R)-a-methylbenzylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 1-methyl-3-phenylpropylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] Adamant-1-ylmethylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 1-(R)-(1-naphthyl)ethylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] Cyclohexylmethylamide; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] Diphenylmethylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] tert-Butylamide Hydrochloride; L-Proline, 1-2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 1,2-Diphenylethylamide Hydrochloride; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] Cyclohexyl amide Hydrochloride; 1-2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] L-Homoproline Benzyl Ester Hydrochloride; L-Homoproline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] Benzylamide Hydrochloride; L-Homoproline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] Adamant-1-ylmethylamide Hydrochloride; L-Homoproline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] tetrahydrofurfurylamide; L-Homoproline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-(4-Sulfamoylphenyl)ethylamide; L-Homoproline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] (S)-a-methylbenzylamide Hydrochloride; L-Homoproline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] (1-(S)-[2'-(S)-methylpropyl]-3-phenylprop-2-E-enyl)-amide; L-Homoproline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] (1-(S)-[2'-(S)-methylpropyl]-3-phenylpropyl)-amide; L-lsoleucine, N-[1-(2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl)-L-Homoprolyl] Benzylamide; L-[Prolino, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-(4-(N-Acetyl)aminophenyl)ethylamide; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-(4-(N-Benzoyl)aminophenyl)ethylamide; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-(4-(N-carboalloxy)aminophenyl)ethylamide; L-Proline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 2-(4-(N-Carbobenzyloxy)aminophenyl)ethylamide; L-Homoproline, 1-[2-(3,4,5-Trimethoxyphenyl)-2-Oxoethyl] 3-(4-(N-Carboallyloxy)aminophenyl)propyl Ester Hydrochloride; L-Proline, 1-[2-Adamantan-1-yl-2-Oxoethyl] 3-(4-(N-Carboallyloxy) aminophenyl)propyl Ester Hydrochloride; and L-Homoproline, 1-[2-Adamant-1-yl-2-Oxoethyl] 3-(4-(N-Carboallyloxy)aminophenyl)propyl Ester Hydrochloride.

Claim 23

A medicament containing at least one compound according to Claim 1.

Claim 24

Use of the compounds according to Claim 1 for the manufacturing of a composition for the treatment of inflammation.

Claim 25

A method for making the composition of claim 3, comprising the following steps: which are (a) coupling an N-protected imino acid to an amine or an alcohol to form a C-substituted, N-protected imino acid; (b) removing the protecting group from said C-substituted, N-protected imino acid; and (c) alkylating the resulting imino acid from step (b) at the nitrogen position with an a-halo ester, a-halo ketone, or an a-halo amide.

Claim 26

A method for making the composition of claim 3, comprising the following steps: which are a) deprotecting the 2-position of a first 2-oxoethyl derivative; and b) coupling the resulting acid derivative from step (a) to form a second 2-oxoethyl derivative.

Claim 27

A method for making the composition of claim 3, comprising the following steps: which are a) deprotecting the imino acid C-termini of a 2-oxoethyl derivative to form a 2-oxoethyl imino acid; and b) coupling said 2-oxoethyl imino acid resulting from step (a) with an amine or an alcohol to form a C-substituted, 2-oxoethyl imino acid derivative.