Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
499 words
A compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: Ar is a group of formula (a): wherein either R2 is C 1-6 alkoxy and one of R 3 , R 4 and R 5 is hydrogen and the other two are selected from hydrogen, halogen, CF 3 , C 1-6 alkylthio, C 1-7 acyl, C 1-10 carboxylic acylamino, C 1-6 alkyl S(O)n wherein n is 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl C l - 4 alkyl or phenyl C l - 4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF 3 , C l - 6 alkyl or C 1-6 alkoxy; or R 2 is hydrogen and R 3 , R 4 and R 5 are independently selected from hydrogen, C 1-6 alkyl, hydroxy, C l-6 alkoxy, C l - 6 alkylthio or halo; or any two on adjacent carbon atoms together are C l - 2 alkylenedioxy and the third is hydrogen, C 1-6 alkyl, C l-6 alkoxy or halo; or Ar is a group of formula (b): wherein W is CH 2 , O, S or NR 7 wherein R 7 is hydrogen, C 1-6 alkyl, C 3-7 alkenyl-methyl, phenyl or phenyl C 1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF 3 , C 1-6 alkoxy or C 1-6 alkyl; and V is CH or N; or W is CH or N and V is NR a where R a is as defined for R 7 above or CHR c where R c is as defined for R 6 below; R D is present when the COX linkage is attached at the phenyl ring, and is selected from hydrogen, halogen, CF 3 , hydroxy, C l-6 alkoxy or C l - 6 alkyl; R6 is hydrogen, halogen, CF 3 , C l - 6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, C l-7 acyl, C l - 7 acylamino, C 1-6 alkylsulphonylamino, N-(C 1-6 alkylsulphonyl)-N-C 1-4 alkylamino, C 1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C l - 4 alkylamino optionally N-substituted by one or two groups selected from C 1 _ 6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl C 1-4 alkyl, phenyl or phenyl C 1-4 alkyl groups or optionally N-disunstituted by C 4-5 polymethylene; X is NH; or O when Ar is of formula (a) and R 2 is hydrogen, or when Ar is a group of formula (b); Y is a group of formula (c), (d) or (e): wherein p and q are independently 0 or 1; Z is C 2 or C 3 polymethylene optionally substituted by one or two C 1-4 alkyl groups; and R 1 is hydrogen or C l - 6 alkyl or OR 1 is an in vivo hydrolysable acyloxy group.
Claim 2
Dependent Claim
499 words
A compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: Ar is a group of formula (a): wherein either R2 is C 1-6 alkoxy and one of R 3 , R 4 and R 5 is hydrogen and the other two are selected from hydrogen, halogen, CF 3 , C 1-6 alkylthio, C 1-7 acyl, C 1-10 carboxylic acylamino, C 1-6 alkyl S(O)n wherein n is 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl C l - 4 alkyl or phenyl C l - 4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF 3 , C l - 6 alkyl or C 1-6 alkoxy; or R 2 is hydrogen and R 3 , R 4 and R 5 are independently selected from hydrogen, C 1-6 alkyl, hydroxy, C l-6 alkoxy, C l - 6 alkylthio or halo; or any two on adjacent carbon atoms together are C l - 2 alkylenedioxy and the third is hydrogen, C 1-6 alkyl, C l-6 alkoxy or halo; or Ar is a group of formula (b): wherein W is CH 2 , O, S or NR 7 wherein R 7 is hydrogen, C 1-6 alkyl, C 3-7 alkenyl-methyl, phenyl or phenyl C 1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF 3 , C 1-6 alkoxy or C 1-6 alkyl; and V is CH or N; or W is CH or N and V is NR a where R a is as defined for R 7 above or CHR c where R c is as defined for R 6 below; R D is present when the COX linkage is attached at the phenyl ring, and is selected from hydrogen, halogen, CF 3 , hydroxy, C l-6 alkoxy or C l - 6 alkyl; R6 is hydrogen, halogen, CF 3 , C l - 6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, C l-7 acyl, C l - 7 acylamino, C 1-6 alkylsulphonylamino, N-(C 1-6 alkylsulphonyl)-N-C 1-4 alkylamino, C 1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C l - 4 alkylamino optionally N-substituted by one or two groups selected from C 1 _ 6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl C 1-4 alkyl, phenyl or phenyl C 1-4 alkyl groups or optionally N-disunstituted by C 4-5 polymethylene; X is NH; or O when Ar is of formula (a) and R 2 is hydrogen, or when Ar is a group of formula (b); Y is a group of formula (c), (d) or (e): wherein p and q are independently 0 or 1; Z is C 2 or C 3 polymethylene optionally substituted by one or two C 1-4 alkyl groups; and R 1 is hydrogen or C l - 6 alkyl or OR 1 is an in vivo hydrolysable acyloxy group.
Claim 3
Dependent Claim
42 words
A compound according to claim 1 of formula (II): wherein R2 1 is C 1-6 alkoxy; R4 1 is amino or C 1-7 alkanoylamino; R5 1 is halo or C l-6 alkylthio; and the remaining variables are as defined in claim 1.
Claim 4
Dependent Claim
26 words
A compound according to claim 2 wherein R 2 1 is methoxy, R 4 1 is amino and R 5 1 is chloro, bromo or methylthio.
Claim 5
Dependent Claim
25 words
A compound according to any one of claims 1, 2 or 3 wherein Y is a group of formula (e) as defined in claim 1.
Claim 6
Dependent Claim
16 words
A compound according to claim 4 wherein q is 0 in the group of formula (e).
Claim 7
Dependent Claim
18 words
A compound according to any one of claims 1 to 5 wherein R 1 is hydrogen or methyl.
Claim 8
Dependent Claim
24 words
4-Amino-5-chloro-2-methoxy-N-(1`-β-hydroxyethyl piperid-4-yl)benzamide, (exo)-4-amino-5-chloro-2-methoxy-N-(8'-β-hydroxyethyl -tropan-3'-yl)benzamide, (exo)-4-amino-5-chloro-2-methoxy-N-(8'-β-methoxyethyl- tropan-3'-yl)benzamide, (endo)-4-amino-5-chloro-2-methoxy-N-(8'-β-hydroxyethyl- tropan-3'-yl)benzamide, (endo)-4-amino-5-chloro-2-methoxy-N-(8'-p-methoxyethyl- tropan-3'-yl)benzamide, (endo)-N-(8'-P- hydroxyethyltropan-3'-yl) -1-methyl-indazole-3- carboxamide; or a pharmaceutically acceptable salt of any of the foregoing.
Claim 9
Dependent Claim
24 words
4-Amino-5-chloro-2-methoxy-N-(1`-β-hydroxyethyl piperid-4-yl)benzamide, (exo)-4-amino-5-chloro-2-methoxy-N-(8'-β-hydroxyethyl -tropan-3'-yl)benzamide, (exo)-4-amino-5-chloro-2-methoxy-N-(8'-β-methoxyethyl- tropan-3'-yl)benzamide, (endo)-4-amino-5-chloro-2-methoxy-N-(8'-β-hydroxyethyl- tropan-3'-yl)benzamide, (endo)-4-amino-5-chloro-2-methoxy-N-(8'-p-methoxyethyl- tropan-3'-yl)benzamide, (endo)-N-(8'-P- hydroxyethyltropan-3'-yl) -1-methyl-indazole-3- carboxamide; or a pharmaceutically acceptable salt of any of the foregoing.
Claim 10
Dependent Claim
148 words
A process for the preparation of a compound of formula (I) as defined in claim 1, which process comprises reacting a compound of formula (V): with a compound of formula (VI): wherein: G is COQ where Q is a group displaceable by a nucleophile, and L is NH 2 or OH or a reactive derivative thereof; R 11 is Z-OR 1 as defined in claim 1 or a hydrogenolysable protecting group; and the remaining variables are as hereinbefore defined; and thereafter optionally converting any R 2 , R 3 , R 4 , R 5 , R6 , Ra and Rb group or R 11 group to another R 2 , R 3 , R 4 , R 5 , R 6 , R a and R b group or to Z-OR 1 respectively, and. optionally forming a pharmaceutically acceptable salt of the resultant compound of formula (I).
Claim 11
Dependent Claim
3 words
3a-Amino-8-(β-hydroxyethyl)tropane or 3a-amino-8-(β-methoxyethyl)tropane.
Claim 12
Dependent Claim
3 words
3a-Amino-8-(β-hydroxyethyl)tropane or 3a-amino-8-(β-methoxyethyl)tropane.
Claim 13
Dependent Claim
25 words
A pharmaceutical composition comprising a compound of formula (I) as defined in claim 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
23 words
A compound of formula (I) as defined in claim 1, or a pharmaceutically acceptable salt thereof, for use as an active therapeutic substance.
Claim 15
Dependent Claim
49 words
Use of a compound of formula (I) as defined in claim 1, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment of disorders relating to impaired gastro-intestinal motility, emesis, migraine, cluster headaches, trigeminal neuralgia and/or cytotoxic agent or radiation induced nausea and vomiting.