MXPA06002731A

MXPA06002731A - Tratamiento y/o prevencion de incontinencia urinaria utilizando profarmacos de analogos de gaba.

Tratamiento y/o prevencion de incontinencia urinaria utilizando profarmacos de analogos de gaba.

Info

Publication number: MXPA06002731A
Authority: MX; Mexico
Prior art keywords: substituted; cycloalkyl; butyl; alkyl; prodrug
Prior art date: 2003-09-11

Application number

MXPA06002731A

Other languages

English (en)

Spanish (es)

Inventor

Ronald W Barrett

Original Assignee

Xenoport Inc

Priority date

2003-09-11

Filing date

2004-09-13

Publication date

2006-06-05

2004-09-13 Application filed by Xenoport Inc filed Critical Xenoport Inc

2006-06-05 Publication of MXPA06002731A publication Critical patent/MXPA06002731A/es

Links

239000000651 prodrug Substances 0.000 title claims abstract description 134
229940002612 prodrug Drugs 0.000 title claims abstract description 134
206010046543 Urinary incontinence Diseases 0.000 title claims abstract description 59
BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical class NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims abstract description 82
238000000034 method Methods 0.000 claims abstract description 79
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 31
-1 4-imidazolylmethyl Chemical group 0.000 claims description 687
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 105
125000001072 heteroaryl group Chemical group 0.000 claims description 102
239000001257 hydrogen Substances 0.000 claims description 101
229910052739 hydrogen Inorganic materials 0.000 claims description 101
UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims description 99
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 96
125000003710 aryl alkyl group Chemical group 0.000 claims description 94
125000000753 cycloalkyl group Chemical group 0.000 claims description 86
125000000217 alkyl group Chemical group 0.000 claims description 76
125000003118 aryl group Chemical group 0.000 claims description 72
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 62
239000003814 drug Substances 0.000 claims description 60
239000002552 dosage form Substances 0.000 claims description 59
125000000547 substituted alkyl group Chemical group 0.000 claims description 58
125000002252 acyl group Chemical group 0.000 claims description 56
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 56
229940079593 drug Drugs 0.000 claims description 55
125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 54
125000004446 heteroarylalkyl group Chemical group 0.000 claims description 53
125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 51
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 51
229960002870 gabapentin Drugs 0.000 claims description 50
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 49
125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 49
SVSARCCKBMZNMR-UHFFFAOYSA-N [1-[2-[methyl-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethyl]amino]ethyl]pyridin-4-ylidene]methyl-oxoazanium;dichloride Chemical compound [Cl-].[Cl-].C1=CC(=C[NH+]=O)C=CN1CCN(C)CCN1C=CC(=C[NH+]=O)C=C1 SVSARCCKBMZNMR-UHFFFAOYSA-N 0.000 claims description 48
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 48
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 47
125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 47
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 45
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 45
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239000012730 sustained-release form Substances 0.000 claims description 40
238000013268 sustained release Methods 0.000 claims description 39
238000011282 treatment Methods 0.000 claims description 37
125000003107 substituted aryl group Chemical group 0.000 claims description 34
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125000004404 heteroalkyl group Chemical group 0.000 claims description 28
229910052799 carbon Inorganic materials 0.000 claims description 26
150000003839 salts Chemical class 0.000 claims description 24
AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims description 21
125000004429 atom Chemical group 0.000 claims description 19
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230000002265 prevention Effects 0.000 claims description 15
230000003204 osmotic effect Effects 0.000 claims description 14
239000012453 solvate Substances 0.000 claims description 13
230000001225 therapeutic effect Effects 0.000 claims description 12
206010066218 Stress Urinary Incontinence Diseases 0.000 claims description 11
125000004432 carbon atom Chemical group C* 0.000 claims description 11
208000022170 stress incontinence Diseases 0.000 claims description 11
150000001204 N-oxides Chemical class 0.000 claims description 10
239000006187 pill Substances 0.000 claims description 9
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 8
208000000921 Urge Urinary Incontinence Diseases 0.000 claims description 6
125000003545 alkoxy group Chemical group 0.000 claims description 6
239000006186 oral dosage form Substances 0.000 claims description 6
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125000003143 4-hydroxybenzyl group Chemical group [H]C([*])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 claims description 5
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229910052760 oxygen Inorganic materials 0.000 claims description 5
229910052717 sulfur Inorganic materials 0.000 claims description 5
230000001360 synchronised effect Effects 0.000 claims description 5
125000005415 substituted alkoxy group Chemical group 0.000 claims description 4
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230000037406 food intake Effects 0.000 claims 1
238000002513 implantation Methods 0.000 claims 1
210000004400 mucous membrane Anatomy 0.000 claims 1
150000001875 compounds Chemical class 0.000 description 102
239000002253 acid Substances 0.000 description 64
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125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 description 53
239000000203 mixture Substances 0.000 description 47
125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 description 39
125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 37
125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 37
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210000003932 urinary bladder Anatomy 0.000 description 36
206010021639 Incontinence Diseases 0.000 description 33
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