US2002119910A1PendingUtilityA1
Compounds and compositions for delivering active agents
Est. expiryFeb 7, 2017(expired)· nominal 20-yr term from priority
Inventors:Andrea Leone-BayEric WangDonald J. SarubbiHarry LeipoldKoc-Kan HoDavid GschneidnerEugene N. Barantsevich
C07C 235/74C07D 311/30C07D 257/04C07C 235/64A61K 38/28C07D 311/12C07C 235/66C07C 243/38A61K 31/727C07C 233/54C07C 229/42C07C 235/38C07C 237/42C07C 233/83C07C 235/52C07C 271/28C07C 235/34A61K 31/195C07D 213/81A61K 31/445C07C 271/54A61K 9/1617A61K 38/21C07D 241/24C07D 311/24C07C 235/60A61K 31/4965C07C 235/24C07D 239/42C07C 233/81C07D 211/62C07C 233/51A61K 45/06C07C 237/12C07D 209/48C07C 237/36A61K 38/23C07C 235/56C07C 237/40C07D 295/192A61K 38/27C07C 237/20C07C 235/12C07C 233/69C07C 259/06C07D 213/82A61K 38/29
45
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Claims
Abstract
Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A composition comprising:
(A) at least one active agent; and (B) at least one carrier selected from the group consisting of 1 6-N-(3,5-dichloro-2-hydroxybenzoyl)aminocaproic acid 2 8(2-aminobenzoylamino)caprylic acid 3 8(2-trifluoromethoxy)benzoylamino caprylic acid 4 N-(2-hydroxybenzoyl)isonipecotic acid 5 4-[4-(2-aminobenzoylamino)phenyl]butyrylhydroxamic acid 6 4-(4-pentafluorobenzoyl)aminophenyl)butyric acid 7 4-(4-(3-anisoyl)aminophenyl)butyric acid 8 8-(3-anisoyl)aminocaprylic acid 10 4-(4-(2-nitrobenzenesulfonyl)aminophenyl)butyric acid 11 8-(2-nitrobenzenesulfonyl)aminocaprylic acid 12 6-(4-(salicyloyl)aminophenyl)hexanoic acid 13 8-(2-methoxylbenzoyl)amino caprylic acid 14 2-[4-Salicyloylamino)phenyl]ethyl methyl sulfone 15 1-Salicyloyl-2-succinyl hydrazide 16 3-(4-(2,5-dimethoxycinnamoyl)aminophenyl)propionic acid 17 4-(4-(2,5-dimethoxycinnamoyl)aminophenyl)butyric acid 18 1-salicyloyl-2-glutaryl hydrazide 19 Succinyl-4-aminosalicylic acid 20 8-(Phenoxyacetylamino)caprylic acid 21 8-(2-pyrazinecarbonyl)aminocaprylic acid 22 4-(4-(2-pyrazinecarbonyl)aminophenyl)butyric acid 23 6-(4-(N-2-Nitrobenzoyl)aminophenyl)hexanoic acid 24 6-(4-(N-2-aminobenzoyl)aminophenyl)hexanoic acid 25 4-(4-(2-(3-carboxyl)pyrazinecarboxyl)aminophenyl)butyric acid 26 4(2-Nitrobenzoyl)aminophenylsuccinic acid 27 8-(2-(trifluoromethoxy)benzoyl)aminocaprylic acid 28 29 8-(Benzylcarbonylamino)caprylic acid 30 8-(phenylcarbonylamino)caprylic acid 31 2-[4-(2-Methoxybenzoylamino)phenyl]ethyl H 2 PO 4 32 1-salicyloyl-2-suberyl hydrazide 33 4-(4-benzyloxycarbonylaminophenyl)butyric acid 34 4-(4-(2-hydroxynicotinoyl)aminophenyl)butyric acid 36 4-(4-phenyloxycarbonylaminophenyl)butyric acid 37 3-(2-methoxybenzoylamino)-1-propanol 38 8-(2-Hydroxynicotinoyl)aminocaprylic acid 39 6-(2-methoxybenzoyl)amino nicotinic acid 40 salicyloylglycine 41 4-(1-(2-pyrimidyl)piperazinoyl)butyric acid 42 8-(chromone-3-carbonyl)aminocaprylic acid 43 8-(vinylbenzoyl)aminocaprylic acid 44 4-(4-(chromone-3-carbonyl)aminophenyl)butyric acid 45 8-cinnamoylaminocaprylic acid 46 5-(N-salicyloylamino)valeric acid 47 9-(2-hydroxybenzamido)nonanic acid 48 N-(4-salicyloylamino)-6-caproic acid 49 4′-flavonic acid 50 11-cinnamoylaminoundecanoic acid 51 4-octanoylamino-3-hydroxybenzoic acid 52 (3Phenyl2,3dihydroxypropanoyl)8aminocaprylic acid 53 8-[N-(3-coumarincarbonyl)]aminocaprylic acid 54 8-[N-(4-chlorobenzoyl)]aminocaprylic acid 55 8-[N-3-fluorobenzoyl)]aminocaprylic acid 56 8-(N-2,5-Dihydroxybenzoyl)aminocaprylic acid 57 8-(N-2,3-Dimethoxybenzoyl)aminocaprylic acid 58 8-(N-2,4-Dihydroxybenzoyl)aminocaprylic acid 59 8-(N-2,5-Dimethoxybenzoyl)aminocaprylic acid 60 8-(N-3,5-Diacetyloxybenzoyl)aminocaprylic acid 61 8-(N-4-Hydroxybenzoyl)aminocaprylic acid (dimer) 62 8-(N-2,4-Dihydroxybenzoyl)aminocaprylic acid 63 10-(N-2-Methoxyanilino)sebalic acid 65 2-Methoxybenzenaminodecanoic acid 66 8-(N-benzoyl)aminocaprylic acid 68 8-[N-(4-fluorobenzoyl)]aminocaprylic acid 69 8-[N-(3-bromobenzoyl)]aminocaprylic acid 70 8-(4-(1,2-dihydroxyethyl)benzoyl)aminocaprylic acid 71 8-[N-(4-bromobenzoyl)]aminocaprylic acid 72 8-[N-(4-iodobenzoyl)]aminocaprylic acid 73 4-{4-[N-(2-iodoenzoyl)aminophenyl]}butyric acid 74 4-{4-[N-(1-hydroxy-2-naphthoyl)aminophenyl]}butyric acid 75 4-(4-(2,4-dimethoxylbenzoyl)aminophenyl)butyric acid 76 4-(o-anisoyl)aminophenylacetic acid 77 3-[4-(2,4-dimethoxybenzoyl)aminophenyl]propionic acid 78 4-{4-[N-(4-iodobenzoyl)]aminophenyl}butyric acid 80 4-{[N-2-bromobenzoyl)]aminophenyl}butyric acid 81 4-{4-[N-3-bromobenzoyl)aminophenyl]}butyric acid 82 8-(N-3,5 Dihydroxybenzoyl)aminocaprylic acid 83 8-(N-3,5-Dimethoxy 4-hydroxybenzoyl)aminocaprylic acid 84 8-(N-2-6-Dimethoxybenzoyl)aminocaprylic acid 85 4-{4-[N-(4-bromobenzoyl)aminophenyl]}butyric acid 86 8-(2-hydroxy-4-chlorobenzoyl)aminocaprylic acid 87 8-(N-2,6-Dihydroxybenzoyl)aminocaprylic acid 88 8-(N-2-Hydroxy6-methoxybenzoyl)aminocaprylic acid 89 8-(5-chloro-o-anisoyl)aminocaprylic acid 90 4-(4-(2,3-dimethoxybenzoyl)aminophenyl)butyric acid 91 4-(4-(5-chloro-o-anisoyl)aminophenyl)butyric acid 92 4-(4-(4-chloro-o-anisoyl)aminophenyl)butyric acid 93 8-(4-chloro-o-anisoyl)aminocaprylic acid 94 3-(4-(2,5-dimethoxybenzoyl)aminophenyl)propionic acid 95 4-{N-[4-(3-iodobenzoyl)aminophenyl]}butyric acid 96 7-cinnamoylaminoheptanoic acid 97 8-N-(3-iodobenzoyl)aminocaprylic acid 98 8-N-(4-methoxy-3-nitrobenzoyl)aminocaprylic acid 99 8-N-(2-methoxy-4-nitrobenzoyl)aminocaprylic acid 100 4-{N-[4-(2-methoxy-2-nitrobenzoyl)aminophenyl]}butyric acid 101 4-(4-(2,5-dimethyoxybenzoyl)aminophenyl)butyric acid 103 3-Indolebutyric acid 104 105 106 108 4-[4-N-(4-methoxy-3-nitrobenzoyl)aminophenyl]butyric acid 110 8-(N-2-hydroxy-5-iodobenzoyl)aminocaprylic acid 112 8-(N-2-hydroxy-4-nitrobenzoyl)aminocaprylic acid 113 4-[-N-(2-hydroxy-4-bromobenzoyl)aminophenyl]butyric acid 114 8-(N-2,3-Dihydroxybenzoyl)aminocaprylic acid 115 8-(N-3-methylsalicyloyl)aminocaprylic acid 116 8-(N-5-methylsalicyloyl)aminocaprylic acid 118 4-(4-(2-chloro-5-nitrobenzoyl)aminophenyl)butyric acid 119 4-{-[N-(2-hydroxy-5-iodobenzoyl)]aminophenyl}butyric acid 120 N-2-nitrophenyl-N′-(8-octanoic acid) urea 121 N-(2-methoxy-5-nitrophenyl) sebecoyl amide acid 123 8-[N-(2-acetoxy-3,5-dibromobenzoyl)]aminocaprylic acid 124 8-N-(2-chloro-6-fluorobenzoyl)aminocaprylic acid 125 126 8-N-(4-hydroxy-3-nitrobenzoyl)caprylic acid 127 4-(4-salicyloylaminophenyl)-4-oxobutyric acid 128 12-cinnamoyldodecanoic acid 129 4-{4-[N-(3-hydroxy-2-napthoyl)aminophenyl]}butyric acid 130 8-(4-chloro-3-nitrobenzoyl)aminocaprylic acid 131 8-(2-chloronicotinoyl)aminocaprylic acid 132 8-(2-chloro-5-nitrobenzoyl)aminocaprylic acid 133 4-(4-phthalimidophenyl)butyric acid 134 4-{4-[N-(3-hydroxy-2-napthoyl)aminophenyl]}propanoic acid 135 3-(4-(2,6-dimethoxybenzoyl)aminophenyl)propionic acid 137 8-(N-2-chloro-4-fluorobenzoyl)aminocaprylic acid 138 8-(2(1,2-dihydroisoindole-1-one))octanoic acid 139 8-(N-1-hyroxy-2-naphthoyl)aminocaprylic acid 140 8-(phthalimido)caprylic acid 142 6-(anisoyl)aminocaproic acid 143 4-(4-(4-chloro-3-nitrobenzoyl)aminophenyl)butyric acid 144 11-N-(1-hydroxy-2-naphthoyl)aminoundecanoic acid 145 Bis(N-2carboxylphenyl-N-(N′-8-octanoic acid)ureal) oxalyl diamide 146 2-[2-N-(2-chlorobenzoyl)aminoethoxy]ethanol 147 2-[2-N-(4-chlorobenzoyl)aminoethoxy]ethanol 148 4-(2-methoxybenzoyl)amino 3-carboxysulfoxide 149 4-(2-methoxybenzoyl)amino 3-carboxypropylsulfone 150 4-(4-(3-hydroxyphthalimido)phenyl)butyric acid 151 2-[2-N-(2-methoxybenzoyl)aminoethoxy)]ethanol 152 2-[2-N-(3-chlorobenzoyl)aminoethoxy)]ethanol 153 Bis(N-2-carboxyphenyl-N-(N′-3(4-aminophenyl)propionic acid)ureal) oxaylyl diamide 154 trans-4-(2-aminobenzamidomethyl)cyclohexamecarboxylic acid 155 11-N-(3,5-dichloro-2-hydroxybenzoyl)aminoundecanoic acid 156 2-[N-(2-bromobenzoyl)aminoethoxy]ethanol 157 7-N-(3,5-dichloro-2-hydroxybenzoyl)aminoheptanoic acid 158 N-[3,5-dichloro-2-hydroxybenzoyl-4(4-aminophenyl)]butyric acid 159 trans-4-(N-salicyloylaminomethyl)cyclohexane carboxylic acid 160 N-[3,5-dichloro-2-hydroxybenzoyl-3-(4-aminophenyl)]propionic acid 161 12-N-(3,5-dichloro-2-hydroxybenzoyl)aminododecanoic acid 162 N-(2-hydroxy-4-carboxy)-6-heptenamide 163 N-(2-bromobenzoyl)morpholine 164 8-N-cyclohexanoylaminocaprylic acid 165 2-[N-(2-iodobenzoyl)aminoethoxy]ethanol 166 5-(4-chloro-2-hydroxyanilinocarbonyl)valeric acid 167 8-(2-hydroxyphenoxy)-aminocaprylic acid 168 N-Salicoyl-5-(3-aminophenyl)valeric acid 169 4-(4-(2-ethoxylbenzoyl)aminophenyl)butyric acid 170 9-[2-(3-hydroxy)pyridylaminocarbonyl]nonanic acid 171 7-(2-hydroxyphenoxyacetyl)aminocaprylic acid 172 2-[N-(2-hydroxybenzoylamino)ethoxy]ethanol 173 4-[N-(3,5-dichloro-2-hydroxybenzoyl)]aminophenylacetic acid 174 8-(2-hydroxy-5-chloroanilinocarbonyl)octanoic acid 175 N-salicoyl-5-(4-aminophenyl)valeric acid 176 9-(2-hydroxy-5-methylanilinocarbonyl)nonanoic acid 177 5-(2-hydroxy-5-methylanilinocarbonyl)valeric acid 178 8-(pentafluorobenzoyl)aminocaprylic acid 179 3-(3-(salicyloyl)aminophenyl)propionic acid 180 8-(2-ethoxybenzoyl)aminocaprylic acid 181 4-(4-(2-Dimethylamino benzoic)aminophenyl)butyric acid 182 8-(3-Phenoxylpropionylamino)caprylic acid 183 4-(salicyloyl)aminophenylethyltetrazole 184 8(-(4(N-Saliciloyl-4aminophenyl)butyric)aminocaprylic acid [sic] 185 4-(4-(N-(2-Fluorocinnamoyl))aminophenyl) butyric 186 4-(4-(N-8(N-Salicyloyl)aminocaprylic)aminiphenyl)butyric acid 187 8-(p-anisoyl)aminocaprylic acid 188 8-(4-Hydroxybenzoyl)aminocaprylic acid 189 8-(3-Hydroxybenzoyl)aminocaprylic acid 190 8-(3,4,5-Trimethoxybenzoyl)aminocaprylic acid 191 8-(N-4-Methylsalicyloyl)aminocaprillic acid[sic] 192 N-10-(2-hydroxy-5-nitroanilino)decanoic acid 193 4-(4-(2-chloronicotinoyl)aminophenyl)butyric acid and a salt of any of the foregoing.
2 . A composition as defined in claim 1 , wherein said active agent is selected from the group consisting of a biologically active agent, a chemically active agent, or a combination thereof.
3 . A composition as defined in claim 2 , wherein said biologically active agent comprises at least one peptide, mucopolysaccharide, carbohydrate, or lipid.
4 . A composition as defined in claim 2 , wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, samatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, parathyroid hormone, desferrioxamine (DFO), or any combination thereof.
5 . A composition as defined in claim 4 , wherein said biologically active agent comprises an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, oxytosin, vasopressin, vancomycin, DFO, parathyroid hormone, and combinations thereof.
6 . A composition as defined in claim 1 , wherein said carrier comprises a poly(amino acid).
7 . A composition as defined in claim 1 , wherein said carrier comprises a polypeptide.
8 . A dosage unit form comprising
(A) a composition as defined in claim 1; and (B) (a) an excipient (b) a diluent, (c) a disintegrant, (d) a lubricant, (e) a plasticizer, (f) a colorant, (g) a dosing vehicle, or (h) any combination thereof.
9 . A composition as defined in claim 8 , wherein said active agent is selected from the group consisting of a biologically active agent, a chemically active agent, or a combination thereof.
10 . A composition as defined in claim 9 , wherein said biologically active agent comprises at least one peptide, mucopolysaccharide, carbohydrate, or lipid.
11 . A composition as defined in claim 9 , wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, samatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, parathyroid hormone, desferrioxamine (DFO), or any combination thereof.
12 . A composition as defined in claim 11 , wherein said biologically active agent comprises an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, oxytosin, vasopressin, vancomycin, DFO, parathyroid hormone, and combinations thereof.
13 . A dosage unit form comprising
(A) a composition as defined in claim 6 ; and (B) (a) an excipient (b) a diluent, (c) a disintegrant, (d) a lubricant, (e) a plasticizer, (f) a colorant, (g) a dosing vehicle, or (h) any combination thereof.
14 . A composition as defined in claim 13 , wherein said active agent is selected from the group consisting of a biologically active agent, a chemically active agent, or a combination thereof.
15 . A composition as defined in claim 14 , wherein said biologically active agent comprises at least one peptide, mucopolysaccharide, carbohydrate, or lipid.
16 . A composition as defined in claim 14 , wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, samatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, parathyroid hormone, desferrioxamine (DFO), or any combination thereof.
17 . A composition as defined in claim 16 , wherein said biologically active agent comprises an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, oxytosin, vasopressin, vancomycin, DFO, parathyroid hormone, and combinations thereof.
18 . A dosage unit form comprising
(A) a composition as defined in claim 7 ; and (B) (a) an excipient (b) a diluent, (c) a disintegrant, (d) a lubricant, (e) a plasticizer, (f) a colorant, (g) a dosing vehicle, or (h) any combination thereof.
19 . A composition as defined in claim 18 , wherein said active agent is selected from the group consisting of a biologically active agent, a chemically active agent, or a combination thereof.
20 . A composition as defined in claim 19 , wherein said biologically active agent comprises at least one peptide, mucopolysaccharide, carbohydrate, or lipid.
21 . A composition as defined in claim 19 , wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, samatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, parathyroid hormone, desferrioxamine (DFO), or any combination thereof.
22 . A composition as defined in claim 21 , wherein said biologically active agent comprises an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, oxytosin, vasopressin, vancomycin, DFO, parathyroid hormone, and combinations thereof.
23 . A dosage unit form as defined in claim 8 , comprising a tablet, a capsule, or a liquid.
24 . A dosage unit form as defined in claim 23 , wherein said dosing vehicle is selected from the group consisting of water, 1,2-propane diol, ethanol, or any combination thereof.
25 . A dosage unit form as defined in claim 13 , comprising a tablet, a capsule, or a liquid.
26 . A dosage unit form as defined in claim 25 , wherein said dosing vehicle is selected from the group consisting of water, 1,2-propane diol, ethanol, or any combination thereof.
27 . A dosage unit form as defined in claim 18 , comprising a tablet, a capsule, or a liquid.
28 . A dosage unit form as defined in claim 27 , wherein said dosing vehicle is selected from the group consisting of water, 1,2-propane diol, ethanol, or any combination thereof.
29 . A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 2 .
30 . A compound selected from the group consisting of
1
6-N-(3,5-dichloro-2-hydroxybenzoyl)aminocaproic acid
2
8(2-aminobenzoylamino)caprylic acid
3
8(2-trifluoromethoxy)benzoylamino caprylic acid
4
N-(2-hydroxybenzoyl)isonipecotic acid
5
4-[4-(2-aminobenzoylamino)phenyl]butyrylhydroxamic acid
6
4-(4-pentafluorobenzoyl)aminophenyl)butyric acid
7
4-(4-(3-anisoyl)aminophenyl)butyric acid
8
8-(3-anisoyl)aminocaprylic acid
10
4-(4-(2-nitrobenzenesulfonyl)aminophenyl)butyric acid
11
8-(2-nitrobenzenesulfonyl)aminocaprylic acid
12
6-(4-salicyloyl)aminophenyl)hexanoic acid
13
8-(2-methoxylbenzoyl)amino caprylic acid
14
2-[4-Salicyloylamino)phenyl]ethyl methyl sulfone
15
1-Salicyloyl-2-succinyl hydrazide
16
3-(4-(2,5-dimethoxycinnamoyl)aminophenyl)propionic acid
17
4-(4-(2,5-dimethoxycinnamoyl)aminophenyl)butyric acid
18
1-salicyloyl-2-glutaryl hydrazide
19
Succinyl-4-aminosalicylic acid
20
8-(Phenoxyacetylamino)caprylic acid
21
8-(2-pyrazinecarbonyl)aminocaprylic acid
22
4-(4-(2-pyrazinecarbonyl)aminophenyl)butyric acid
23
6-(4-(N-2-Nitrobenzoyl)aminophenyl)hexanoic acid
24
6-(4-(N-2-aminobenzoyl)aminophenyl)hexanoic acid
25
4-(4-(2-(3-carboxyl)pyrazinecarboxyl)aminophenyl)butyric acid
26
4(2-Nitrobenzoyl)aminophenylsuccinic acid
27
8-(2-trifluoromethoxy)benzoyl)aminocaprylic acid
28
29
8-(Benzylcarbonylamino)caprylic acid
30
8-(phenylcarbonylamino)caprylic acid
31
2-[4-(2-Methoxybenzoylamino)phenyl]ethyl H 2 PO 4
32
1-salicyloyl-2-suberyl hydrazide
33
4-(4-benzyloxycarbonylaminophenyl)butyric acid
34
4-(4-(2-hydroxynicotinoyl)aminophenyl)butyric acid
36
4-(4-phenyloxycarbonylaminophenyl)butyric acid
37
3-(2-methoxybenzoylamino)-1-propanol
38
8-(2-Hydroxynicotinoyl)aminocaprylic acid
39
6-(2-methoxybenzoyl)amino nicotinic acid
40
salicyloylglycine
41
4-(1-(2-pyrimidyl)piperazinoyl)butyric acid
42
8-(chromone-3-carbonyl)aminocaprylic acid
43
8-(vinylbenzoyl)aminocaprylic acid
44
4-(4-(chromone-3-carbonyl)aminophenyl)butyric acid
45
8-cinnamoylaminocaprylic acid
46
5-(N-salicyloylamino)valeric acid
47
9-(2-hydroxybenzamido)nonanic acid
48
N-(4-salicyloylamino)-6-caproic acid
49
4′-flavonic acid
50
11-cinnamoylaminoundecanoic acid
51
4-octanoylamino-3-hydroxybenzoic acid
52
(3Phenyl2,3dihydroxypropanoyl)8aminocaprylic acid
53
8-[N-(3-coumarincarbonyl)]aminocaprylic acid
54
8-[N-(4-chlorobenzoyl)]aminocaprylic acid
55
8-[N-3-fluorobenzoyl)]aminocaprylic acid
56
8-(N-2,5-Dihydroxybenzoyl)aminocaprylic acid
57
8-(N-2,3-Dimethoxybenzoyl)aminocaprylic acid
58
8-(N-2,4-Dihydroxybenzoyl)aminocaprylic acid
59
8-(N-2,5-Dimethoxybenzoyl)aminocaprylic acid
60
8-(N-3,5-Diacetyloxybenzoyl)aminocaprylic acid
61
8-(N-4-Hydroxybenzoyl)aminocaprylic acid (dimer)
62
8-(N-2,4-Dihydroxybenzoyl)aminocaprylic acid
63
10-(N-2-Methoxyanilino)sebalic acid
65
2-Methoxybenzenaminodecanoic acid
66
8-(N-benzoyl)aminocaprylic acid
68
8-[N-(4-fluorobenzoyl)]aminocaprylic acid
69
8-[N-(3-bromobenzoyl)]aminocaprylic acid
70
8-(4-(1,2-dihydroxyethyl)benzoyl)aminocaprylic acid
71
8-[N-(4-bromobenzoyl)]aminocaprylic acid
72
8-[N-(4-iodobenzoyl)]aminocaprylic acid
73
4-{4-[N-(2-iodobenzoyl)aminophenyl]}butyric acid
74
4-{4-[N-(1-hydroxy-2-naphthoyl)aminophenyl]}butyric acid
75
4-(4-(2,4-dimethoxylbenzoyl)aminophenyl)butyric acid
76
4-(o-anisoyl)aminophenylacetic acid
77
3-[4-(2,4-dimethoxybenzoyl) aminophenyl] propionic acid
78
4-{4-[N-(4-iodobenzoyl)] aminophenyl} butyric acid
80
4-{4-[N-2-bromobenzoyl)] aminophenyl} butyric acid
81
4{4-[N-3-bromobenzoyl) aminophenyl]} butyric acid
82
8-(N-3,5 Dihydroxybenzoyl)aminocaprylic acid
83
8-(N-3,5-Dimethoxy 4-hydroxybenzoyl)aminocaprylic acid
84
8-(N-2-6-Dimethoxybenzoyl)aminocaprylic acid
85
4-{[N-(4-bromobenzoyl)aminophenyl]}butyric acid
86
8-(2-hydroxy-4-chlorobenzoyl)aminocaprylic acid
87
8-(N-2,6-Dihydroxybenzoyl)aminocaprylic acid
88
8-(N-2-Hydroxy6-methoxybenzoyl)aminocaprylic acid
89
8-(5-chloro-o-anisoyl)aminocaprylic acid
90
4-(2-(2,3-dimethoxybenzoyl)aminophenyl)butyric acid
91
4-(4-(5-chloro-o-anisoyl)aminophenyl)butyric acid
92
4-(4-(4-chloro-o-anisoyl)aminophenyl)butyric acid
93
8-(4-chloro-o-anisoyl)aminocaprylic acid
94
3-(4-(2,5-dimethoxybenzoyl)aminophenyl)propionic acid
95
4-{N-[4-(3-iodobenzoyl)aminophenyl]}butyric acid
96
7-cinnamoylaminoheptanoic acid
97
8-N-(3-iodobenzoyl)aminocaprylic acid
98
8-N-(4-methoxy-3-nitrobenzoyl)aminocaprylic acid
99
8-N-(2-methoxy-4-nitrobenzoyl)aminocaprylic acid
100
4-{N-[4-(2-methoxy-4-nitrobenzoyl)aminophenyl]}butyric acid
101
4-(4-(2,5-dimethoxybenzoyl)aminophenyl)butyric acid
104
105
106
107
4-(4-(2,6-dimethoxybenzoyl)aminophenylbutyric acid
108
4-[4-N-(4-methoxy-3-nitrobenzoyl)aminophenyl]butyric acid
110
8-(N-2-hydroxy-5-iodobenzoyl)aminocaprylic acid
112
8-(N-2-hydroxy-4-nitrobenzoyl)aminocaprylic acid
113
4-[-N-(2-hydroxy-4-bromobenzoyl)aminophenyl]butyric acid
114
8-(N-2,3-Dihydroxybenzoyl)aminocaprylic acid
115
8-(N-3-methylsalicyloyl)aminocaprylic acid
116
8-(N-5-methylsalicyloyl)aminocaprylic acid
118
4-(4-(2-chloro-5-nitrobenzoyl)aminophenyl)butyric acid
119
4-{-[N-(2-hydroxy-5-iodobenzoyl)]aminophenyl}butyric acid
120
N-2-nitrophenyl-N′-(8-octanoic acid) urea
121
N-(2-methoxy-5-nitrophenyl) sebecoyl amide acid
123
8-[N-(2-acetoxy-3,5-dibromobenzoyl)]aminocaprylic acid
124
8-N-(2-chloro-6-fluorobenzoyl)aminocaprylic acid
125
126
8-N-(4-hydroxy-3-nitrobenzoyl)caprylic acid
127
4-(4-Salicyloylaminophenyl)-4-oxobutyric acid
128
12-cinnamoyldodecanoic acid
129
4-{4-[N-(3-hydroxy-2-napthoyl)aminophenyl]}butyric acid
130
8-(4-chloro-3-nitrobenzoyl)aminocaprylic acid
131
8-(2-chloronicotinoyl)aminocaprylic acid
132
8-(2-chloro-5-nitrobenzoyl)aminocaprylic acid
133
4-(4-phthalimidophenyl)butyric acid
134
4-{4-[N-(3-hydroxy-2-napthoyl)aminophenyl]}propanoic acid
135
3-(4-(2,6-dimethoxybenzoyl)aminophenyl)propionic acid
137
8-(N-2-chloro-4-fluorobenzoyl)aminocaprylic acid
138
8-(2-(1,2-dihydroisoindole-1-one))octanoic acid
139
8-(N-1-hydroxy-2-naphthoyl)aminocaprylic acid
140
8-(phthalimido)caprylic acid
142
6-(anisoyl)aminocaproic acid
143
4-(4-(4-chloro-3-nitrobenzoyl)aminophenyl)butyric acid
144
11-N-(1-hydroxy-2-naphthoyl)aminoundecanoic acid
145
Bis(N-2carboxylphenyl-N-(N′-8-octanoic acid)ureal)oxalyl diamide
146
2-[2-N-(2-chlorobenzoyl)aminoethoxy]ethanol
147
2-[2-N-(4-chlorobenzoyl)aminoethoxy]ethanol
148
4-(2-methoxybenzoyl)amino 3-carboxysulfoxide
149
4-(2-methoxybenzoyl)amino 3-carboxypropylsulfone
150
4-(4-(3-hydroxyphthalimido)phenyl)butyric acid
151
2-[2-N-(2-methoxybenzoyl)aminoethoxy)]ethanol
152
2-[2-N-(3-chlorobenzoyl)aminoethoxy)]ethanol
153
Bis(N-2-carboxyphenyl-N-(N′-3(4-aminophenyl)propionic acid)ureal)oxaylyl diamide
154
trans-4-(2-aminobenzamidomethyl)cyclohexamecarboxylic acid
155
11-N-(3,5-dichloro-2-hydroxybenzoyl)aminoundecanoic acid
156
2-[N-(2-bromobenzoyl)aminoethoxy]ethanol
157
7-N-(3,5-dichloro-2-hydroxybenzoyl)aminoheptanoic acid
158
N-[3,5-dichloro-2-hydroxybenzoyl-4(4-aminophenyl)]butyric acid
159
trans-4-(N-salicyloylaminomethyl)cyclohexane carboxylic acid
160
N-[3,5-dichloro-2-hydroxybenzoyl-3-(4-aminophenyl)]propionic acid
161
12-N-(3,5-dichloro-2-hydroxybenzoyl)aminododecanoic acid
162
N-(2-hydroxy-4-carboxy)-6-heptenamide
163
N-(2-bromobenzoyl)morpholine
164
8-N-cyclohexanoylaminocaprylic acid
165
2-[N-(2-iodobenzoyl)aminoethoxy]ethanol
166
5-(4-chloro-2-hydroxyanilinocarbonyl)valeric acid
167
8-(2-hydroxyphenoxy)-aminocaprylic acid
168
N-Salicoyl-5-(3-aminophenyl)valeric acid
169
4-(4-(2-ethoxylbenzoyl)aminophenyl)butyric acid
170
9-[2-(3-hydroxy)pyridylaminocarbonyl] nonanic acid
171
7-(2-hydroxyphenoxyacetyl)aminocaprylic acid
172
2-[N-(2-hydroxybenzoylamino)ethoxy]ethanol
173
4-[N-(3,5-dichloro-2-hydroxybenzoyl)]aminophenylacetic acid
174
8-(2-hydroxy-5-chloroanilinocarbonyl)octanoic acid
175
N-salicoyl-5-(4-aminophenyl)valeric acid
176
9-(2-hydroxy-5-methylanilinocarbonyl)nonanoic acid
177
5-(2-hydroxy-5-methylanilinocarbonyl)valeric acid
178
8-(pentafluorobenzoyl)aminocaprylic acid
179
3-(3-(salicyloyl)aminophenyl)propionic acid
180
8-(2-ethoxybenzoyl)aminocaprylic acid
181
4-(4-(2-Dimethylamino benzoic)aminophenyl)butyric acid
182
8-(3-Phenoxylpropionylamino)caprylic acid
183
4-(Salicyloyl)aminophenylethyltetrazole
184
8(-(4(N-Saliciloyl-4aminophenyl)butyric)aminocaprylic acid [sic]
185
4-(4-(N-(2-Fluorocinnamoyl))aminophenyl) butyric
186
4-(4-(N-8(N-Salicyloyl)aminocaprylic)aminophenyl)butyric acid
187
8-(p-anisoyl)aminocaprylic acid
188
8-(4-Hydroxybenzoyl)aminocaprylic acid
189
8-(3-Hydroxybenzoyl)aminocaprylic acid
190
8-(3,4,5-Trimethoxybenzoyl)aminocaprylic acid
191
8-(N-4-Methylsalicyloyl)aminocaprillic acid [sic]
192
N-10-(2-hydroxy-5-nitroanilino)decanoic acid
193
4-(4-(2-chloronicotinoyl)aminophenyl)butyric acid
and a salt of any of the foregoing.
31 . A method for preparing a composition, said method comprising mixing:
(A) at least one active agent; (B) at least one compound as defined in claim 31 ; and (C) optionally, a dosing vehicle.Join the waitlist — get patent alerts
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