KR100863758B1 - 항문직장 장애의 치료 조성물 및 방법 - Google Patents
항문직장 장애의 치료 조성물 및 방법 Download PDFInfo
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- KR100863758B1 KR100863758B1 KR1020037001579A KR20037001579A KR100863758B1 KR 100863758 B1 KR100863758 B1 KR 100863758B1 KR 1020037001579 A KR1020037001579 A KR 1020037001579A KR 20037001579 A KR20037001579 A KR 20037001579A KR 100863758 B1 KR100863758 B1 KR 100863758B1
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- sphincter
- pde
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PCT/US2001/023971 WO2002009714A1 (en) | 2000-07-31 | 2001-07-30 | Compositions and methods for the treatment of anorectal disorders |
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IL (1) | IL154202A0 (es) |
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WO2010151004A2 (ko) | 2009-06-23 | 2010-12-29 | Yeo Oh-Young | 하이드록시클로로퀸을 함유하는 치핵 치료를 위한 국소투여용 주사제 조성물 |
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GB0020588D0 (en) * | 2000-08-21 | 2000-10-11 | Pfizer Ltd | Treatment of wounds |
US8987245B2 (en) | 2008-04-02 | 2015-03-24 | Jonathan R. Brestoff Parker | Composition and method for affecting obesity and related conditions |
US8598150B1 (en) | 2008-04-02 | 2013-12-03 | Jonathan R. Brestoff | Composition and method for affecting obesity and related conditions |
CN102145004B (zh) * | 2010-02-09 | 2012-03-21 | 鲁南制药集团股份有限公司 | 己酮可可碱在制备预防或治疗功能性便秘的药物中的用途 |
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Publication number | Priority date | Publication date | Assignee | Title |
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US5595753A (en) | 1995-04-14 | 1997-01-21 | President And Fellows Of Harvard College | Topical formulations and methods for treating hemorrhoidal pain and sphincter and smooth muscle spasm in the gastrointestinal tract |
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CN1298309A (zh) * | 1998-02-27 | 2001-06-06 | 同步神经元有限责任公司 | 治疗肛门区疼痛的方法及其组合物 |
AU764921B2 (en) * | 1998-12-14 | 2003-09-04 | Cellegy Pharmaceuticals, Inc. | Compositions and methods for the treatment of anorectal disorders |
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- 2001-07-30 WO PCT/US2001/023971 patent/WO2002009714A1/en not_active Application Discontinuation
- 2001-07-30 KR KR1020037001579A patent/KR100863758B1/ko not_active IP Right Cessation
- 2001-07-30 KR KR1020087015829A patent/KR20080068145A/ko not_active Application Discontinuation
- 2001-07-30 EP EP01957348A patent/EP1315499A4/en not_active Withdrawn
- 2001-07-30 AU AU2001279104A patent/AU2001279104A1/en not_active Abandoned
- 2001-07-30 MX MXPA03000931A patent/MXPA03000931A/es unknown
- 2001-07-30 JP JP2002515267A patent/JP2004516244A/ja not_active Withdrawn
- 2001-07-30 CA CA002417848A patent/CA2417848A1/en not_active Abandoned
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US5595753A (en) | 1995-04-14 | 1997-01-21 | President And Fellows Of Harvard College | Topical formulations and methods for treating hemorrhoidal pain and sphincter and smooth muscle spasm in the gastrointestinal tract |
Cited By (1)
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WO2010151004A2 (ko) | 2009-06-23 | 2010-12-29 | Yeo Oh-Young | 하이드록시클로로퀸을 함유하는 치핵 치료를 위한 국소투여용 주사제 조성물 |
Also Published As
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IL154202A0 (en) | 2003-07-31 |
JP2004516244A (ja) | 2004-06-03 |
CA2417848A1 (en) | 2002-02-07 |
WO2002009714A1 (en) | 2002-02-07 |
AU2001279104A1 (en) | 2002-02-13 |
WO2002009714A9 (en) | 2003-03-06 |
EP1315499A4 (en) | 2007-09-05 |
MXPA03000931A (es) | 2004-08-12 |
KR20080068145A (ko) | 2008-07-22 |
KR20030024826A (ko) | 2003-03-26 |
KR20100017750A (ko) | 2010-02-16 |
EP1315499A1 (en) | 2003-06-04 |
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