JP2007505149A5 - - Google Patents
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- JP2007505149A5 JP2007505149A5 JP2006526389A JP2006526389A JP2007505149A5 JP 2007505149 A5 JP2007505149 A5 JP 2007505149A5 JP 2006526389 A JP2006526389 A JP 2006526389A JP 2006526389 A JP2006526389 A JP 2006526389A JP 2007505149 A5 JP2007505149 A5 JP 2007505149A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- cycloalkyl
- cycloheteroalkyl
- prodrug
- alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000003710 aryl alkyl group Chemical group 0.000 claims description 36
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 36
- 125000001072 heteroaryl group Chemical group 0.000 claims description 33
- 238000000034 method Methods 0.000 claims description 28
- 239000000651 prodrug Substances 0.000 claims description 28
- 229940002612 prodrug Drugs 0.000 claims description 28
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 27
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 24
- 125000000217 alkyl group Chemical group 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 22
- 239000001257 hydrogen Substances 0.000 claims description 22
- 125000003118 aryl group Chemical group 0.000 claims description 21
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 21
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 21
- 125000002252 acyl group Chemical group 0.000 claims description 18
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 18
- 125000003107 substituted aryl group Chemical group 0.000 claims description 18
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical class NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims description 14
- 206010046543 Urinary incontinence Diseases 0.000 claims description 12
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 12
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 9
- 239000012453 solvate Substances 0.000 claims description 9
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 125000004429 atom Chemical group 0.000 claims description 3
- 125000005842 heteroatom Chemical group 0.000 claims description 3
- 229910052760 oxygen Inorganic materials 0.000 claims description 3
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 3
- 229910052717 sulfur Inorganic materials 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 239000002552 dosage form Substances 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- -1 4- Imidazolylmethyl Chemical group 0.000 claims 2
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000003143 4-hydroxybenzyl group Chemical group [H]C([*])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010066218 Stress Urinary Incontinence Diseases 0.000 claims 1
- 208000000921 Urge Urinary Incontinence Diseases 0.000 claims 1
- 239000011324 bead Substances 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 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 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 229960002870 gabapentin Drugs 0.000 claims 1
- 238000002513 implantation Methods 0.000 claims 1
- 238000001361 intraarterial administration Methods 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 230000003902 lesion Effects 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 230000009245 menopause Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 210000004877 mucosa Anatomy 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- 230000003204 osmotic effect Effects 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 229960001233 pregabalin Drugs 0.000 claims 1
- AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 208000022170 stress incontinence Diseases 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 239000012730 sustained-release form Substances 0.000 claims 1
- 230000009747 swallowing Effects 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 230000001960 triggered effect Effects 0.000 claims 1
- 206010046494 urge incontinence Diseases 0.000 claims 1
- 0 COC(CC1(C*)CCCCC1)=* Chemical compound COC(CC1(C*)CCCCC1)=* 0.000 description 1
- 150000001204 N-oxides Chemical class 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US50258503P | 2003-09-11 | 2003-09-11 | |
| US50521003P | 2003-09-22 | 2003-09-22 | |
| US51228803P | 2003-10-17 | 2003-10-17 | |
| US53874804P | 2004-01-22 | 2004-01-22 | |
| PCT/US2004/029944 WO2005025562A1 (en) | 2003-09-11 | 2004-09-13 | Treating and/or preventing urinary incontinence using prodrugs of gaba analogs |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007505149A JP2007505149A (ja) | 2007-03-08 |
| JP2007505149A5 true JP2007505149A5 (enExample) | 2007-09-13 |
Family
ID=34317683
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006526389A Pending JP2007505149A (ja) | 2003-09-11 | 2004-09-13 | ギャバ類似体のプロドラッグを用いる尿失禁の治療および／あるいは予防 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US7700652B2 (enExample) |
| EP (1) | EP1670451A4 (enExample) |
| JP (1) | JP2007505149A (enExample) |
| KR (1) | KR20060119971A (enExample) |
| AU (1) | AU2004272111A1 (enExample) |
| CA (1) | CA2537837A1 (enExample) |
| IL (1) | IL174409A0 (enExample) |
| MX (1) | MXPA06002731A (enExample) |
| NO (1) | NO20061625L (enExample) |
| NZ (1) | NZ545884A (enExample) |
| WO (1) | WO2005025562A1 (enExample) |
Families Citing this family (23)
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| CA2541752C (en) | 2003-10-14 | 2012-01-03 | Xenoport, Inc. | Crystalline form of gamma-aminobutyric acid analog |
| EP1811986B1 (en) | 2004-11-04 | 2014-03-26 | XenoPort, Inc. | Gabapentin prodrug sustained release oral dosage forms |
| CA2617546C (en) | 2005-08-03 | 2014-07-15 | Boehringer Ingelheim International Gmbh | Use of flibanserin in the treatment of obesity |
| WO2007027476A2 (en) * | 2005-08-26 | 2007-03-08 | Xenoport, Inc. | Treating premature ejaculation using gabapentin and pregabalin prodrugs |
| NL2000281C2 (nl) * | 2005-11-02 | 2007-08-07 | Pfizer Prod Inc | Vaste farmaceutische samenstellingen die pregabaline bevatten. |
| WO2008000760A1 (en) * | 2006-06-30 | 2008-01-03 | Boehringer Ingelheim International Gmbh | Flibanserin for the treatment of urinary incontinence and related diseases |
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| AU2004267100B2 (en) * | 2003-08-20 | 2010-10-07 | Xenoport, Inc. | Acyloxyalkyl carbamate prodrugs, methods of synthesis and use |
| CA2537837A1 (en) | 2003-09-11 | 2005-03-24 | Xenoport, Inc. | Treating and/or preventing urinary incontinence using prodrugs of gaba analogs |
| CA2538802C (en) * | 2003-09-17 | 2015-01-27 | Xenoport, Inc. | Treating or preventing restless legs syndrome using prodrugs of gaba analogs |
| CA2541752C (en) * | 2003-10-14 | 2012-01-03 | Xenoport, Inc. | Crystalline form of gamma-aminobutyric acid analog |
| CA2551859C (en) * | 2003-12-30 | 2011-10-04 | Xenoport, Inc. | Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof |
| EP1811986B1 (en) * | 2004-11-04 | 2014-03-26 | XenoPort, Inc. | Gabapentin prodrug sustained release oral dosage forms |
| US20060222700A1 (en) | 2005-04-05 | 2006-10-05 | Groenewoud Pieter J | Tablet and capsule form of liquid active ingredient |
| RU2403013C2 (ru) | 2005-12-16 | 2010-11-10 | Ханми Фарм. Ко., Лтд. | Твердая дисперсия, содержащая активный ингредиент с низкой температурой плавления, и содержащая ее таблетка для перорального введения |
| WO2008060572A1 (en) * | 2006-11-14 | 2008-05-22 | Xenoport, Inc. | Use of gabapentin and pregabalin prodrugs for treating tinnitus |
| CA2672044A1 (en) * | 2006-12-08 | 2008-06-19 | Xenoport, Inc. | Use of prodrugs of gaba analogs for treating diseases |
| CA2674610C (en) * | 2007-01-11 | 2013-06-18 | Xenoport, Inc. | Sustained release oral dosage forms of a prodrug of r-baclofen and methods of treatment |
-
2004
- 2004-09-13 CA CA002537837A patent/CA2537837A1/en not_active Abandoned
- 2004-09-13 MX MXPA06002731A patent/MXPA06002731A/es not_active Application Discontinuation
- 2004-09-13 JP JP2006526389A patent/JP2007505149A/ja active Pending
- 2004-09-13 AU AU2004272111A patent/AU2004272111A1/en not_active Abandoned
- 2004-09-13 NZ NZ545884A patent/NZ545884A/en unknown
- 2004-09-13 US US10/940,884 patent/US7700652B2/en not_active Expired - Fee Related
- 2004-09-13 WO PCT/US2004/029944 patent/WO2005025562A1/en not_active Ceased
- 2004-09-13 EP EP04788728A patent/EP1670451A4/en not_active Withdrawn
- 2004-09-13 KR KR1020067005033A patent/KR20060119971A/ko not_active Withdrawn
-
2006
- 2006-03-20 IL IL174409A patent/IL174409A0/en unknown
- 2006-04-10 NO NO20061625A patent/NO20061625L/no not_active Application Discontinuation
-
2010
- 2010-03-09 US US12/720,414 patent/US20100166825A1/en not_active Abandoned
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