Claims Analysis
Total Claims: 41
Claim 1
Independent Claim
401 words
Compounds of formula (I): [wherein: R 1 represents a C 1 -C 4 alkyl group having: (a) an amino or protected amino substituent on its a-carbon atom and (b) a carbocyclic aromatic substituent, a heterocyclic substituent or a heterocyclic-dithio substituent wherein the aromatic or heterocyclic ring is unsubstituted or has at least one amino, alkyl, hydroxy, alkoxy, halogen, nitro, mercapto or alkylthio substituent; R 2 represents a hydrogen atom, a C 1 -C 18 alkyl group, a C 2 -C 5 alkenyl group, a C 2 -C 5 alkenyl group having at least one halogen substituent, a C 2 -C 5 alkynyl group, a C 3 -C 7 cycloalkyl group, a C 5 -C 8 cycloalkenyl group, or a C 1 -C 4 alkyl group having one substituent selected from: ( c ) C3 - C7 cycloalkyl groups, C 5 - C 8 cycloalkenyl groups, aryl groups and 5- and 6-membered heterocyclic groups having at least one sulphur, nitrogen or oxygen hetero-atom and optionally at least one substituent selected from: (d) halogen atoms, hydroxy groups, alkoxy groups, aryloxy groups, aralkyloxy groups, aliphatic carboxylic acyloxy groups, mercapto groups, alkylthio groups, aliphatic carboxylic acylaminoalkylthio groups, arylthio groups, aralkylthio groups, alkylsulphinyl groups, alkylsulphonyl groups, arylsulphinyl groups, arylsulphonyl groups, amino groups, mono- and di- alkylamino groups, arylamino groups. aliphatic carboxylic acylamino groups, aromatic carboxylic acylamino groups, alkoxycarbonylamino groups, aralkyloxycarbonylamino groups, aliphatic carboxylic acyl groups, aromatic carboxylic acyl grougs carboxy groups, alkoxycarbonyl groups, aralkyloxycarbonyl groups, carbamoyl groups, mono-and di- alkylcarbamoyl groups, ureido groups, thioureido groups and guanidyl groups; R 3 represents an isobutyl, sec-butyl, benzyl or (C 3 -C 8 cycloalkyl)methyl group; X represents a group of formula -CH(-A-R 4 )-Y (in which: A represents a single bond or an alkylene group; R 4 represents a carboxy group; a protected carboxy group, a carbamoyl group, an N-substituted carbamoyl group, a carbazoyl group, an N-substituted carbazoyl group or an acyl group; and Y represents a hydroxy group, a mercapto group or a formyl group), or a group of formula -P(O)(R 5 )-OH (in which R 5 represents a substituted alkyl group having at least one carboxy, protected carboxy, N-substituted carbamoyl, carbazoyl, N-substituted carbazoyl, C 2 -C 7 aliphatic carboxylic acyl or aromatic carboxylic acyl substituent); provided that, where A represents an alkylene group and R 2 represents a 4-imidazolylmethyl group, R 4 does not represent a carbamoyl group or a formyl group]; and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
401 words
Compounds of formula (I): [wherein: R 1 represents a C 1 -C 4 alkyl group having: (a) an amino or protected amino substituent on its a-carbon atom and (b) a carbocyclic aromatic substituent, a heterocyclic substituent or a heterocyclic-dithio substituent wherein the aromatic or heterocyclic ring is unsubstituted or has at least one amino, alkyl, hydroxy, alkoxy, halogen, nitro, mercapto or alkylthio substituent; R 2 represents a hydrogen atom, a C 1 -C 18 alkyl group, a C 2 -C 5 alkenyl group, a C 2 -C 5 alkenyl group having at least one halogen substituent, a C 2 -C 5 alkynyl group, a C 3 -C 7 cycloalkyl group, a C 5 -C 8 cycloalkenyl group, or a C 1 -C 4 alkyl group having one substituent selected from: ( c ) C3 - C7 cycloalkyl groups, C 5 - C 8 cycloalkenyl groups, aryl groups and 5- and 6-membered heterocyclic groups having at least one sulphur, nitrogen or oxygen hetero-atom and optionally at least one substituent selected from: (d) halogen atoms, hydroxy groups, alkoxy groups, aryloxy groups, aralkyloxy groups, aliphatic carboxylic acyloxy groups, mercapto groups, alkylthio groups, aliphatic carboxylic acylaminoalkylthio groups, arylthio groups, aralkylthio groups, alkylsulphinyl groups, alkylsulphonyl groups, arylsulphinyl groups, arylsulphonyl groups, amino groups, mono- and di- alkylamino groups, arylamino groups. aliphatic carboxylic acylamino groups, aromatic carboxylic acylamino groups, alkoxycarbonylamino groups, aralkyloxycarbonylamino groups, aliphatic carboxylic acyl groups, aromatic carboxylic acyl grougs carboxy groups, alkoxycarbonyl groups, aralkyloxycarbonyl groups, carbamoyl groups, mono-and di- alkylcarbamoyl groups, ureido groups, thioureido groups and guanidyl groups; R 3 represents an isobutyl, sec-butyl, benzyl or (C 3 -C 8 cycloalkyl)methyl group; X represents a group of formula -CH(-A-R 4 )-Y (in which: A represents a single bond or an alkylene group; R 4 represents a carboxy group; a protected carboxy group, a carbamoyl group, an N-substituted carbamoyl group, a carbazoyl group, an N-substituted carbazoyl group or an acyl group; and Y represents a hydroxy group, a mercapto group or a formyl group), or a group of formula -P(O)(R 5 )-OH (in which R 5 represents a substituted alkyl group having at least one carboxy, protected carboxy, N-substituted carbamoyl, carbazoyl, N-substituted carbazoyl, C 2 -C 7 aliphatic carboxylic acyl or aromatic carboxylic acyl substituent); provided that, where A represents an alkylene group and R 2 represents a 4-imidazolylmethyl group, R 4 does not represent a carbamoyl group or a formyl group]; and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
291 words
Compounds as claimed in Claim 1. wherein: R 1 represents a group of formula R 13 -CH(NHR 12 )-, in which R 12 represents a hydrogen atom, or a 2-(2-methoxyethoxy)ethoxycarbonyl, benzyloxycarbonyl, p-aethozybenzyloxycarbonyi, t-butoxycarbonyl, 9-fluorenylmethoxycarbonyl, 2-nitrophenylthio, 3-nitropyrid-2-ylthio, 4-phenylbutyryl or 3-(3-nitropyrid-2-yldithio)propionyl group; and R 13 represents a benzyl, benzyl having at least one C 1 -C 4 alkyl, amino, C 1 -C 4 alkoxy, hydroxy, halogen, nitro, mercapto or C 1 -C 4 alkylthio substituent, 1-naphthylmethyl, 2-naphthylmethyl, 3-indolylmethyl, 5-quinolylmethyl, 4-quinolylmethyl, 2-pyridylmethyl. 3-pyridylmethyl or 4-pyridylmethyl group; R 2 represents a C 1 -C 10 alkyl group, a C 2 -C 5 alkenyl group, a C 2 -C 5 alkenyl group having at least one halogen substituent, a C 2 -C 4 alkynyl group, a C 3 -C 6 cycloalkyl group, a (C3-C6 cycloalkyl)methyl group, a C 5 -C 8 cycloalkenyl group, a (C 5 -C8 cycloalkenyl)methyi group, or a benzyl, 3-indolylmethyl, 2-thienylmethyl, 4-thiazolylmethyl, 2-thiazolylmenthyl 4-methyl-5-thiazolylmentyl, 2-pyridylmethyl. 3-pyridylmethyl, 4-pyridylmethyl, 4 -imidazolylmethyl. 2-pyrrolidinylmethyl, 1-(C 1 -C 4 alkyl)-2-pyrrolidinylmethyl, 1,3-thiazolidin-4-ylmethyl or 3-(C 1 -C 4 alkyl)-l,3-thiazolidin-4-ylmethyl group, or any such group wherein any C 1 -C 4 alkyl portion has at least one hydroxy, alkoxy, aralkyloxy, aliphatic carboxylic acyloxy, mercapto, alkylthio, alkylsulphinyl, alkylsulphonyl, amino, monoalkylamino, dialkylamino, aliphatic carboxylic acylamino, aromatic carboxylic acylamino, alkoxycarbonylamino, aralkyloxycarbonylamino, aliphatic carboxylic acyl, carboxy, alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl, carbamoyl, ureido or guanidyl substituent: R4 represents a protected carboxy group, a carbamoyl group, an N-substituted carbamoyl group, a carbazoyl group, an N-substituted carbazoyl group or an acyl group; Y represents a hydroxy or mercapto group; R represents an alkyl group having at least one protected carboxy, N-substituted carbamoyl, carbazoyl, N-substituted carbazoyl, C 2 -C 7 aliphatic carboxylic acyl or aromatic carboxylic acyl substituent; and R 3 represents an isobutyl, sec-butyl, cyclopropylmethyl, cyclopentylmethyl or cyclohexylmethyl group.
Claim 4
Dependent Claim
203 words
Compounds as claimed in Claim 1, wherein: R 1 represents a group of formula R 13 -CH(NHR 12 )- in which: R 12 represents a 2-(2-methoxyethoxy)ethoxycarbonyl, benzyloxycarbonyl, p-methoxybenzyloxycarbonyl. t-butoxycarbonyl, 9-fluorenylmethoxycarbonyl. 4-phenylbutyryl or 3-(3-nitropyrid-2-yldithio)propionyl group; and R 13 represents a benzyl group, a benzyl group having at least one C 1 -C 4 alkyl or C l -C 4 alkox y substituent, a 1-naphthylmethyl group, a 3-indolylmethyl group, a 5-quinolylmethyl group, a 4-quinolylmethyl group, a 2-pyridylmethyl group, a 3-pyridylmethyl group or a 4-pyridylmethyl group; R 2 represents a C 1 -C 10 alkyl group, an allyl group, a propargyl group, a cyclopropylmethyl group, a cyclopentylmethyl group, a cyclohexylmethyl group, a benzyl group, a 3-indolylmethyl group, a 2-thienylmethyl group, a 4-thiazolylmentyl group, a 2-thiazolylmethyl group, a 4-methyl-5-thiazolylmethyl group, a 2-pyridylmethyl group or a 4-imidazolylmethyl group; R 4 represents a protected carboxy group, a carbamoyl group, an N-substituted carbamoyl group, a carbazoyl group, an N-substituted carbazoyl group or an acyl group; Y represents a hydroxy or mercapto group; R 5 represents an alkyl group having at least one protected carboxy, N-substituted carbamoyl, carbazoyl, N-substituted carbazoyl, C 2 -C 7 aliphatic carboxylic acyl or aromatic carboxylic acyl substituent; and R 3 represents an isobutyl or sec-butyl group.
Claim 5
Dependent Claim
64 words
Compounds as claimed in Claim 1, wherein: R 2 represents an imidazolylmethyl group and is attached to a carbon atom having the S-configuration; R 3 represents an isobutyl or sec-butyl group; R 4 represents a carboxy, N-substituted carbamoyl, carbazoyl, N-substituted carbazoyl or carboxylic acyl group having at least 2 carbon atoms; and R , X, A and R are as defined in Claim 1.
Claim 6
Dependent Claim
1 words
N-(2-methylbutyl)-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-leucyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 7
Dependent Claim
1 words
N-(2-methylbutyl)-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-leucyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 8
Dependent Claim
1 words
N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-leucyl]amino-3(S)-hydroxy-6-methylheptanoyl}-L-isoleucinol
Claim 9
Dependent Claim
1 words
N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-leucyl]amino-3(S)-hydroxy-6-methylheptanoyl}-L-isoleucinol
Claim 10
Dependent Claim
1 words
N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-3-(2-thienyl)-DL-alanyl)amino-3(S)-hydroxy-6-methylheptanoyl}-L-isoleucinol
Claim 11
Dependent Claim
1 words
N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-3-(2-thienyl)-DL-alanyl)amino-3(S)-hydroxy-6-methylheptanoyl}-L-isoleucinol
Claim 12
Dependent Claim
1 words
N-(2-methylbutyl)-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-3-(1,3-thiazol-4-yl)-DL-alanylJamino-3(S)-hydroxy-6-methylheptanamide
Claim 13
Dependent Claim
1 words
N-(2-methylbutyl)-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-3-(1,3-thiazol-4-yl)-DL-alanylJamino-3(S)-hydroxy-6-methylheptanamide
Claim 14
Dependent Claim
1 words
N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-3-(1,3-thiazol-4-yl)-DL-alanyl]amino-3(S)-hydroxy-6-methylheptanoyl}-L-isoleucinol
Claim 15
Dependent Claim
1 words
N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-3-(1,3-thiazol-4-yl)-DL-alanyl]amino-3(S)-hydroxy-6-methylheptanoyl}-L-isoleucinol
Claim 16
Dependent Claim
1 words
4(S)-[N-benzyloxycarbonyl-3-(l-naphthyl)-L-alanyl-3-(4-thiazolyl)-DL-alanyl]amino-3(S)-hydroxy-6-methyl-N-(2-morpholinoethyl)heptanamide
Claim 17
Dependent Claim
1 words
4(S)-[N-benzyloxycarbonyl-3-(l-naphthyl)-L-alanyl-3-(4-thiazolyl)-DL-alanyl]amino-3(S)-hydroxy-6-methyl-N-(2-morpholinoethyl)heptanamide
Claim 18
Dependent Claim
1 words
N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-3-(2-pyridyl)-DL-alanyl]amino-3(S)-hydroxy-6-methylheptanoyl}-L-isoleucinol
Claim 19
Dependent Claim
1 words
N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-3-(2-pyridyl)-DL-alanyl]amino-3(S)-hydroxy-6-methylheptanoyl}-L-isoleucinol
Claim 20
Dependent Claim
1 words
N-(2-methylbutyl)-4(S)-{N-[2-(2-methoxyethoxy)-ethoxycarbonyl]-3-(l-naphthyl)-L-alanyl-L-histidyl}amino-3(S)-hydroxy-6-methylheptanamide
Claim 21
Dependent Claim
1 words
N-(2-methylbutyl)-4(S)-{N-[2-(2-methoxyethoxy)-ethoxycarbonyl]-3-(l-naphthyl)-L-alanyl-L-histidyl}amino-3(S)-hydroxy-6-methylheptanamide
Claim 22
Dependent Claim
1 words
N-ethyl-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 23
Dependent Claim
1 words
N-ethyl-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 24
Dependent Claim
2 words
14 N-sec-butyl-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 25
Dependent Claim
2 words
14 N-sec-butyl-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 26
Dependent Claim
2 words
15 N-isobutyl-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 27
Dependent Claim
2 words
15 N-isobutyl-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 28
Dependent Claim
2 words
16 4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl-N-(2-methylbutyl)heptanamide
Claim 29
Dependent Claim
2 words
16 4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl-N-(2-methylbutyl)heptanamide
Claim 30
Dependent Claim
3 words
17 N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl- heptanoyl}-L-isoleucinol
Claim 31
Dependent Claim
3 words
17 N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl- heptanoyl}-L-isoleucinol
Claim 32
Dependent Claim
3 words
18 N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl- heptanoyl}-L-leucinol
Claim 33
Dependent Claim
3 words
18 N-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl- heptanoyl}-L-leucinol
Claim 34
Dependent Claim
3 words
19 2-[2-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl- heptanamido}ethyl]-1-methylpyrrolidine
Claim 35
Dependent Claim
3 words
19 2-[2-{4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl- heptanamido}ethyl]-1-methylpyrrolidine
Claim 36
Dependent Claim
2 words
3-{4(S)-[N-benzyloxycarbonyl-3-(1-naghthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl- heptanamido}-6-methylheptan-1,3-diol
Claim 37
Dependent Claim
2 words
3-{4(S)-[N-benzyloxycarbonyl-3-(1-naghthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methyl- heptanamido}-6-methylheptan-1,3-diol
Claim 38
Dependent Claim
1 words
N-(1-ethyl-2-pyrrolidinylmethyl)-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 39
Dependent Claim
1 words
N-(1-ethyl-2-pyrrolidinylmethyl)-4(S)-[N-benzyloxycarbonyl-3-(1-naphthyl)-L-alanyl-L-histidyl]amino-3(S)-hydroxy-6-methylheptanamide
Claim 40
Dependent Claim
27 words
A pharmaceutical composition comprising at least one compound as claimed in any one of Claims 1 to 21 in admixture with a pharmaceutically acceptable carrier or diluent.
Claim 41
Dependent Claim
126 words
A process for preparing a compound as claimed in any one of Claims 1 to 21, which process comprises the steps: (i) reacting a compound of formula (II): (in which: R 1 is as defined in Claim 1; B represents a group of formula -NH-CH(R 2 )CO-, where R 2 is as defined in Claim 1; and m is 0 or 1) or a reactive derivative thereof with a compound of formula (III): (in which: B, R 3 and X are as defined in Claim 1; and n is 1 if m is 0 or 0 if m is 1); (ii) optionally subjecting the product to an acyl exchange reaction; and (iii) optionally converting any group represented by X to any other group represented by X.