KR20100028656A - 치료 조성물 및 그의 용도 - Google Patents
치료 조성물 및 그의 용도 Download PDFInfo
- Publication number
- KR20100028656A KR20100028656A KR1020107001984A KR20107001984A KR20100028656A KR 20100028656 A KR20100028656 A KR 20100028656A KR 1020107001984 A KR1020107001984 A KR 1020107001984A KR 20107001984 A KR20107001984 A KR 20107001984A KR 20100028656 A KR20100028656 A KR 20100028656A
- Authority
- KR
- South Korea
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- lopinavir
- oxo
- 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.)
- Ceased
Links
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| CN103479584A (zh) | 2008-05-02 | 2014-01-01 | 吉里德科学公司 | 固体载体颗粒在改善药物制剂加工性中的应用 |
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| TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
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| TR201905009T4 (tr) | 2015-04-02 | 2019-05-21 | Gilead Sciences Inc | Polisiklik-karbamoilpiridon bileşikleri ve bunların farmasötik kullanımları. |
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| US5413999A (en) * | 1991-11-08 | 1995-05-09 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
| US5484926A (en) * | 1993-10-07 | 1996-01-16 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
| US5914332A (en) * | 1995-12-13 | 1999-06-22 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5849911A (en) * | 1996-04-22 | 1998-12-15 | Novartis Finance Corporation | Antivirally active heterocyclic azahexane derivatives |
| US6087383A (en) * | 1998-01-20 | 2000-07-11 | Bristol-Myers Squibb Company | Bisulfate salt of HIV protease inhibitor |
| WO2004046115A1 (ja) * | 2002-11-20 | 2004-06-03 | Japan Tobacco Inc. | ４−オキソキノリン化合物及びそのｈｉｖインテグラーゼ阻害剤としての利用 |
| US20060111933A1 (en) * | 2003-10-09 | 2006-05-25 | Steven Wheeler | Adaptive medical decision support system |
| MY134672A (en) * | 2004-05-20 | 2007-12-31 | Japan Tobacco Inc | Stable crystal of 4-oxoquinoline compound |
| EP2229945A1 (en) * | 2004-05-21 | 2010-09-22 | Japan Tobacco, Inc. | Combinations comprising a 4-isoquinolone derivative and anti-HIV agents |
| US20060058286A1 (en) * | 2004-09-16 | 2006-03-16 | Mark Krystal | Methods of treating HIV infection |
| BRPI0620865A2 (pt) * | 2005-12-30 | 2011-11-29 | Gilead Sciences Inc | métodos para melhorar a farmacocinética de inibidores das integrases do hiv |
| US20090233964A1 (en) * | 2005-12-30 | 2009-09-17 | Gilead Sciences, Inc. | Methods for improving the pharmacokinetics of hiv integrase inhibitors |
| WO2007092802A1 (en) * | 2006-02-09 | 2007-08-16 | Boehringer Ingelheim International Gmbh | Method for treating hiv infection through co-administration of tipranavir and gs 9137 |
| SI2049506T2 (sl) * | 2006-07-07 | 2024-07-31 | Gilead Sciences, Inc. | Modulatorji farmakokinetičnih lastnosti terapevtikov |
| BRPI0716752A2 (pt) * | 2006-09-12 | 2013-09-17 | Gilead Sciences Inc | processo e intermediÁrios para preparo de inibidores de intergrase |
| NZ582086A (en) * | 2007-06-29 | 2012-07-27 | Gilead Sciences Inc | Therapeutic compositions and the use thereof |
| AR068403A1 (es) * | 2007-09-11 | 2009-11-18 | Gilead Sciences Inc | Proceso e intermediarios para la preparacion de inhibidores de integrasa |
| CN103479584A (zh) * | 2008-05-02 | 2014-01-01 | 吉里德科学公司 | 固体载体颗粒在改善药物制剂加工性中的应用 |
| US20110000941A1 (en) * | 2009-07-06 | 2011-01-06 | Volk J Patrick | Apparatus and System for Carrying a Digital Media Player |
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2008
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- 2008-06-26 TW TW097123981A patent/TW200916103A/zh unknown
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- 2008-06-26 US US12/147,220 patent/US20090093482A1/en not_active Abandoned
- 2008-06-26 AP AP2009005083A patent/AP2490A/xx active
- 2008-06-26 CN CN200880022821A patent/CN101743004A/zh active Pending
- 2008-06-26 AU AU2008270634A patent/AU2008270634B2/en not_active Ceased
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- 2008-06-26 US US12/666,995 patent/US20110009411A1/en not_active Abandoned
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- 2008-06-26 CN CN2013101948825A patent/CN103356622A/zh active Pending
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2013
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2014
- 2014-05-19 US US14/281,790 patent/US20140343062A1/en not_active Abandoned
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Also Published As
| Publication number | Publication date |
|---|---|
| JP2015143277A (ja) | 2015-08-06 |
| JP2013199494A (ja) | 2013-10-03 |
| JP2010532373A (ja) | 2010-10-07 |
| WO2009006203A1 (en) | 2009-01-08 |
| EA200971096A1 (ru) | 2010-08-30 |
| AU2008270634B2 (en) | 2014-01-16 |
| AP2009005083A0 (en) | 2009-12-31 |
| SG182228A1 (en) | 2012-07-30 |
| CN101743004A (zh) | 2010-06-16 |
| CO6251236A2 (es) | 2011-02-21 |
| IL202745A0 (en) | 2010-06-30 |
| AP2490A (en) | 2012-10-04 |
| ZA201000468B (en) | 2011-06-29 |
| CA2691736A1 (en) | 2009-01-08 |
| CN103356622A (zh) | 2013-10-23 |
| ECSP109889A (es) | 2010-03-31 |
| US20170136000A1 (en) | 2017-05-18 |
| JP5547067B2 (ja) | 2014-07-09 |
| US20140343062A1 (en) | 2014-11-20 |
| AR067184A1 (es) | 2009-09-30 |
| US20090093482A1 (en) | 2009-04-09 |
| EP2167089A1 (en) | 2010-03-31 |
| BRPI0813955A2 (pt) | 2017-05-09 |
| US20110009411A1 (en) | 2011-01-13 |
| NZ582089A (en) | 2013-01-25 |
| MX2009013828A (es) | 2010-03-10 |
| AU2008270634A1 (en) | 2009-01-08 |
| JP5769762B2 (ja) | 2015-08-26 |
| UA103881C2 (ru) | 2013-12-10 |
| TW200916103A (en) | 2009-04-16 |
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