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.)
- Pending
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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)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US8048917B2 (en) * | 2005-04-06 | 2011-11-01 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
| US7186855B2 (en) | 2001-06-11 | 2007-03-06 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
| UA78974C2 (en) | 2001-10-20 | 2007-05-10 | Boehringer Ingelheim Pharma | Use of flibanserin for treating disorders of sexual desire |
| US10675280B2 (en) | 2001-10-20 | 2020-06-09 | Sprout Pharmaceuticals, Inc. | Treating sexual desire disorders with flibanserin |
| US7025745B2 (en) * | 2002-10-07 | 2006-04-11 | Advanced Cardiovascular Systems, Inc. | Method of making a catheter balloon using a tapered mandrel |
| EP1670451A4 (en) | 2003-09-11 | 2009-10-21 | Xenoport Inc | TREATMENT AND / OR PREVENTION OF URINARY INCONTINENCE AND PROMOTERS OF GABA ANALOGS |
| KR101096480B1 (ko) * | 2003-10-14 | 2011-12-20 | 제노포트 인코포레이티드 | 감마-아미노부티르산 유사체의 결정질 형태 |
| US8795725B2 (en) | 2004-11-04 | 2014-08-05 | Xenoport, Inc. | GABA analog prodrug sustained release oral dosage forms |
| EP1912650B8 (en) | 2005-08-03 | 2017-10-18 | Sprout Pharmaceuticals, Inc. | Use of flibanserin in the treatment of obesity |
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| NL2000281C2 (nl) * | 2005-11-02 | 2007-08-07 | Pfizer Prod Inc | Vaste farmaceutische samenstellingen die pregabaline bevatten. |
| ATE456369T1 (de) | 2006-06-30 | 2010-02-15 | Boehringer Ingelheim Int | Flibanserin zur behandlung von harninkontinenz und assoziierten erkrankungen |
| EA200970487A1 (ru) * | 2006-12-08 | 2009-12-30 | Ксенопорт, Инк. | Применение пролекарств аналогов гамк для лечения заболеваний |
| CN102058885B (zh) | 2006-12-22 | 2013-04-10 | 瑞蔻达蒂爱尔兰有限公司 | 采用α2δ配体和NSAID的下泌尿道疾病的联合治疗 |
| JP2010515754A (ja) * | 2007-01-11 | 2010-05-13 | ゼノポート，インコーポレイティド | Ｒ−バクロフェンのプロドラッグの徐放性経口剤形及び治療方法 |
| CL2008002693A1 (es) | 2007-09-12 | 2009-10-16 | Boehringer Ingelheim Int | Uso de flibanserina para el tratamiento de sintomas vasomotores seleccionados de sofocos, sudores nocturnos, cambios de estado de animo e irritabilidad |
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| JP5563483B2 (ja) * | 2008-01-25 | 2014-07-30 | ゼノポート，インコーポレイティド | アシロキシアルキルカルバメートプロドラッグの合成に使用されるアシロキシアルキルチオカーボネートの鏡像異性的な分解 |
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| NZ594648A (en) * | 2009-03-03 | 2013-12-20 | Xenoport Inc | Sustained release oral dosage forms of an r-baclofen prodrug |
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| US7662987B2 (en) | 2003-07-15 | 2010-02-16 | Xenoport, Inc. | Methods for synthesis of acyloxyalkyl compounds |
| KR101140559B1 (ko) | 2003-08-20 | 2012-07-05 | 제노포트 인코포레이티드 | 아실옥시알킬 카르바메이트 프로드러그, 합성 및 사용 방법 |
| EP1670451A4 (en) | 2003-09-11 | 2009-10-21 | Xenoport Inc | TREATMENT AND / OR PREVENTION OF URINARY INCONTINENCE AND PROMOTERS OF GABA ANALOGS |
| WO2005027850A2 (en) | 2003-09-17 | 2005-03-31 | Xenoport, Inc. | Treating or preventing restless legs syndrome using prodrugs of gaba analogs |
| KR101096480B1 (ko) | 2003-10-14 | 2011-12-20 | 제노포트 인코포레이티드 | 감마-아미노부티르산 유사체의 결정질 형태 |
| DK1716115T3 (da) | 2003-12-30 | 2013-05-27 | Xenoport Inc | Syntese af acyloxyalkylcarbamat-prodrug og mellemprodukter deraf |
| US8795725B2 (en) | 2004-11-04 | 2014-08-05 | Xenoport, Inc. | GABA analog 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 |
| ZA200806138B (en) | 2005-12-16 | 2009-11-25 | Hanmi Pharm Ind Co Ltd | Solid dispersion comprising an active ingredient having a low melting point and tablet for oral administration comprising same |
| MX2009005114A (es) | 2006-11-14 | 2009-07-16 | Xenoport Inc | Uso de los profarmacos gabapentina y pregabalina para tratar el tinnitus. |
| EA200970487A1 (ru) | 2006-12-08 | 2009-12-30 | Ксенопорт, Инк. | Применение пролекарств аналогов гамк для лечения заболеваний |
| JP2010515754A (ja) | 2007-01-11 | 2010-05-13 | ゼノポート，インコーポレイティド | Ｒ−バクロフェンのプロドラッグの徐放性経口剤形及び治療方法 |
-
2004
- 2004-09-13 EP EP04788728A patent/EP1670451A4/en not_active Withdrawn
- 2004-09-13 NZ NZ545884A patent/NZ545884A/en unknown
- 2004-09-13 CA CA002537837A patent/CA2537837A1/en not_active Abandoned
- 2004-09-13 KR KR1020067005033A patent/KR20060119971A/ko not_active Withdrawn
- 2004-09-13 JP JP2006526389A patent/JP2007505149A/ja active Pending
- 2004-09-13 WO PCT/US2004/029944 patent/WO2005025562A1/en not_active Ceased
- 2004-09-13 AU AU2004272111A patent/AU2004272111A1/en not_active Abandoned
- 2004-09-13 MX MXPA06002731A patent/MXPA06002731A/es not_active Application Discontinuation
- 2004-09-13 US US10/940,884 patent/US7700652B2/en not_active Expired - Fee Related
-
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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