JP2010532373A5 - - Google Patents
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- Publication number
- JP2010532373A5 JP2010532373A5 JP2010515115A JP2010515115A JP2010532373A5 JP 2010532373 A5 JP2010532373 A5 JP 2010532373A5 JP 2010515115 A JP2010515115 A JP 2010515115A JP 2010515115 A JP2010515115 A JP 2010515115A JP 2010532373 A5 JP2010532373 A5 JP 2010532373A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- lopinavir
- methylbutan
- dihydroquinoline
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims description 168
- KJHKTHWMRKYKJE-SUGCFTRWSA-N Kaletra Chemical compound N1([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=2C=CC=CC=2)NC(=O)COC=2C(=CC=CC=2C)C)CC=2C=CC=CC=2)CCCNC1=O KJHKTHWMRKYKJE-SUGCFTRWSA-N 0.000 claims description 66
- 150000001875 compounds Chemical class 0.000 claims description 65
- 229960004525 lopinavir Drugs 0.000 claims description 65
- -1 3-Chloro-2-fluorobenzyl Chemical group 0.000 claims description 57
- 102000002004 Cytochrome P-450 Enzyme System Human genes 0.000 claims description 47
- 108010015742 Cytochrome P-450 Enzyme System Proteins 0.000 claims description 47
- 150000001735 carboxylic acids Chemical class 0.000 claims description 43
- 239000003814 drug Substances 0.000 claims description 31
- NCDNCNXCDXHOMX-UHFFFAOYSA-N Ritonavir Natural products C=1C=CC=CC=1CC(NC(=O)OCC=1SC=NC=1)C(O)CC(CC=1C=CC=CC=1)NC(=O)C(C(C)C)NC(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-UHFFFAOYSA-N 0.000 claims description 30
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 claims description 30
- 229960000311 ritonavir Drugs 0.000 claims description 30
- 239000000203 mixture Substances 0.000 claims description 17
- 239000002552 dosage form Substances 0.000 claims description 12
- 241000725303 Human immunodeficiency virus Species 0.000 claims description 8
- 241000282412 Homo Species 0.000 claims description 7
- JUZYLCPPVHEVSV-LJQANCHMSA-N elvitegravir Chemical compound COC1=CC=2N([C@H](CO)C(C)C)C=C(C(O)=O)C(=O)C=2C=C1CC1=CC=CC(Cl)=C1F JUZYLCPPVHEVSV-LJQANCHMSA-N 0.000 claims description 6
- 208000036142 Viral infection Diseases 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- 230000009385 viral infection Effects 0.000 claims description 5
- NDCFBPDNHOZORS-UHFFFAOYSA-N 1,2-dihydroquinoline-3-carboxylic acid Chemical compound C1=CC=C2NCC(C(=O)O)=CC2=C1 NDCFBPDNHOZORS-UHFFFAOYSA-N 0.000 claims description 4
- 241000700605 Viruses Species 0.000 claims description 4
- YNJUTIFLXNSGAO-CQSZACIVSA-N 1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid Chemical compound OC[C@H](C(C)C)N1C=C(C(O)=O)C(=O)C=2C1=CC(OC)=CC=2 YNJUTIFLXNSGAO-CQSZACIVSA-N 0.000 claims description 2
- QROPNBKULZRDMD-UHFFFAOYSA-N 7-methoxy-4-oxo-1h-quinoline-3-carboxylic acid Chemical compound N1C=C(C(O)=O)C(=O)C=2C1=CC(OC)=CC=2 QROPNBKULZRDMD-UHFFFAOYSA-N 0.000 claims description 2
- 239000003443 antiviral agent Substances 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 230000000069 prophylactic effect Effects 0.000 claims description 2
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 230000003612 virological effect Effects 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims 26
- 230000009885 systemic effect Effects 0.000 description 2
- DTYLXDLAOLOTKT-UHFFFAOYSA-N 1,4-dihydroquinoline-3-carboxylic acid Chemical compound C1=CC=C2CC(C(=O)O)=CNC2=C1 DTYLXDLAOLOTKT-UHFFFAOYSA-N 0.000 description 1
- 238000000034 method Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94732507P | 2007-06-29 | 2007-06-29 | |
| US60/947,325 | 2007-06-29 | ||
| PCT/US2008/068351 WO2009006203A1 (en) | 2007-06-29 | 2008-06-26 | Therapeutic compositions and the use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013142320A Division JP5769762B2 (ja) | 2007-06-29 | 2013-07-08 | 治療組成物およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010532373A JP2010532373A (ja) | 2010-10-07 |
| JP2010532373A5 true JP2010532373A5 (enExample) | 2011-07-21 |
| JP5547067B2 JP5547067B2 (ja) | 2014-07-09 |
Family
ID=39817166
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010515115A Expired - Fee Related JP5547067B2 (ja) | 2007-06-29 | 2008-06-26 | 治療組成物およびその使用 |
| JP2013142320A Expired - Fee Related JP5769762B2 (ja) | 2007-06-29 | 2013-07-08 | 治療組成物およびその使用 |
| JP2015094705A Withdrawn JP2015143277A (ja) | 2007-06-29 | 2015-05-07 | 治療組成物およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013142320A Expired - Fee Related JP5769762B2 (ja) | 2007-06-29 | 2013-07-08 | 治療組成物およびその使用 |
| JP2015094705A Withdrawn JP2015143277A (ja) | 2007-06-29 | 2015-05-07 | 治療組成物およびその使用 |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US20090093482A1 (enExample) |
| EP (1) | EP2167089A1 (enExample) |
| JP (3) | JP5547067B2 (enExample) |
| KR (1) | KR20100028656A (enExample) |
| CN (2) | CN103356622A (enExample) |
| AP (1) | AP2490A (enExample) |
| AR (1) | AR067184A1 (enExample) |
| AU (1) | AU2008270634B2 (enExample) |
| BR (1) | BRPI0813955A2 (enExample) |
| CA (1) | CA2691736A1 (enExample) |
| CO (1) | CO6251236A2 (enExample) |
| EA (1) | EA200971096A1 (enExample) |
| EC (1) | ECSP109889A (enExample) |
| IL (1) | IL202745A0 (enExample) |
| MX (1) | MX2009013828A (enExample) |
| NZ (1) | NZ582089A (enExample) |
| SG (1) | SG182228A1 (enExample) |
| TW (1) | TW200916103A (enExample) |
| UA (1) | UA103881C2 (enExample) |
| WO (1) | WO2009006203A1 (enExample) |
| ZA (1) | ZA201000468B (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070219243A1 (en) * | 2005-12-30 | 2007-09-20 | Kearney Brian P | Method for improving the pharmacokinetics of HIV integrase inhibitors |
| KR101477822B1 (ko) | 2006-07-07 | 2015-01-02 | 길리애드 사이언시즈, 인코포레이티드 | 치료제의 약동학 특성의 모듈레이터 |
| ES2536923T3 (es) | 2006-09-12 | 2015-05-29 | Gilead Sciences, Inc. | Proceso e intermedios para preparar inhibidores de la integrasa del VIH |
| PT3150586T (pt) * | 2007-02-23 | 2020-03-31 | Gilead Sciences Inc | Moduladores de propriedades farmacocinéticas de agentes terapêuticos |
| SG182229A1 (en) * | 2007-06-29 | 2012-07-30 | 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 |
| EA201591353A1 (ru) | 2008-05-02 | 2016-01-29 | Джилид Сайэнс, Инк. | Применение частиц твердого носителя для улучшения технологических характеристик фармацевтического агента |
| US20130203759A1 (en) * | 2010-04-09 | 2013-08-08 | Faranak Nikfar | ATAZANAVIR SULFATE FORMULATIONS WITH IMPROVED pH EFFECT |
| US20130274254A1 (en) * | 2010-12-21 | 2013-10-17 | Gilead Sciences, Inc. | Inhibitors of cytochrome p450 (cyp3a4) |
| US9089574B2 (en) | 2011-11-30 | 2015-07-28 | Emory University | Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections |
| HK1204980A1 (en) * | 2012-03-01 | 2015-12-11 | Gilead Sciences, Inc. | Spray dried formulations |
| EP2880017B1 (en) | 2012-08-03 | 2016-10-05 | Gilead Sciences, Inc. | Process and intermediates for preparing integrase inhibitors |
| EA030003B1 (ru) | 2012-12-21 | 2018-06-29 | Джилид Сайэнс, Инк. | Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции |
| DK3019503T3 (da) | 2013-07-12 | 2017-11-20 | Gilead Sciences Inc | Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner |
| NO2865735T3 (enExample) | 2013-07-12 | 2018-07-21 | ||
| TWI744723B (zh) | 2014-06-20 | 2021-11-01 | 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 |
| NO2717902T3 (enExample) | 2014-06-20 | 2018-06-23 | ||
| TW201613936A (en) | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
| TWI695003B (zh) | 2014-12-23 | 2020-06-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
| WO2016106050A1 (en) | 2014-12-26 | 2016-06-30 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| CA2980362C (en) | 2015-04-02 | 2020-02-25 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| EP4233846B1 (en) | 2015-06-30 | 2024-12-04 | Gilead Sciences, Inc. | Pharmaceutical formulations |
| RU2020116571A (ru) | 2017-12-07 | 2021-11-22 | Эмори Юниверсити | N4-гидроксицитидин и производные и связанные с этим противовирусные применения |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5696270A (en) * | 1989-05-23 | 1997-12-09 | Abbott Laboratories | Intermediate for making retroviral protease inhibiting compounds |
| GB8927913D0 (en) * | 1989-12-11 | 1990-02-14 | Hoffmann La Roche | Amino acid derivatives |
| 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 |
| US7176220B2 (en) * | 2002-11-20 | 2007-02-13 | Japan Tobacco Inc. | 4-oxoquinoline compound and use thereof as pharmaceutical agent |
| 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 |
| US8633219B2 (en) * | 2004-05-21 | 2014-01-21 | Japan Tobacco Inc. | Combination therapy |
| US20060058286A1 (en) * | 2004-09-16 | 2006-03-16 | Mark Krystal | Methods of treating HIV infection |
| US20070219243A1 (en) * | 2005-12-30 | 2007-09-20 | Kearney Brian P | Method for improving the pharmacokinetics of HIV integrase inhibitors |
| 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 |
| KR101477822B1 (ko) * | 2006-07-07 | 2015-01-02 | 길리애드 사이언시즈, 인코포레이티드 | 치료제의 약동학 특성의 모듈레이터 |
| ES2536923T3 (es) * | 2006-09-12 | 2015-05-29 | Gilead Sciences, Inc. | Proceso e intermedios para preparar inhibidores de la integrasa del VIH |
| SG182229A1 (en) * | 2007-06-29 | 2012-07-30 | 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 |
| EA201591353A1 (ru) * | 2008-05-02 | 2016-01-29 | Джилид Сайэнс, Инк. | Применение частиц твердого носителя для улучшения технологических характеристик фармацевтического агента |
| US20110000941A1 (en) * | 2009-07-06 | 2011-01-06 | Volk J Patrick | Apparatus and System for Carrying a Digital Media Player |
-
2008
- 2008-06-26 WO PCT/US2008/068351 patent/WO2009006203A1/en not_active Ceased
- 2008-06-26 SG SG2012046926A patent/SG182228A1/en unknown
- 2008-06-26 AR ARP080102760A patent/AR067184A1/es not_active Application Discontinuation
- 2008-06-26 US US12/147,220 patent/US20090093482A1/en not_active Abandoned
- 2008-06-26 US US12/666,995 patent/US20110009411A1/en not_active Abandoned
- 2008-06-26 NZ NZ582089A patent/NZ582089A/xx not_active IP Right Cessation
- 2008-06-26 TW TW097123981A patent/TW200916103A/zh unknown
- 2008-06-26 CN CN2013101948825A patent/CN103356622A/zh active Pending
- 2008-06-26 EA EA200971096A patent/EA200971096A1/ru unknown
- 2008-06-26 JP JP2010515115A patent/JP5547067B2/ja not_active Expired - Fee Related
- 2008-06-26 UA UAA200913904A patent/UA103881C2/ru unknown
- 2008-06-26 CA CA002691736A patent/CA2691736A1/en not_active Abandoned
- 2008-06-26 KR KR1020107001984A patent/KR20100028656A/ko not_active Ceased
- 2008-06-26 MX MX2009013828A patent/MX2009013828A/es not_active Application Discontinuation
- 2008-06-26 AP AP2009005083A patent/AP2490A/xx active
- 2008-06-26 BR BRPI0813955A patent/BRPI0813955A2/pt not_active IP Right Cessation
- 2008-06-26 CN CN200880022821A patent/CN101743004A/zh active Pending
- 2008-06-26 AU AU2008270634A patent/AU2008270634B2/en not_active Ceased
- 2008-06-26 EP EP20080781024 patent/EP2167089A1/en not_active Withdrawn
-
2009
- 2009-12-15 IL IL202745A patent/IL202745A0/en unknown
- 2009-12-21 CO CO09146050A patent/CO6251236A2/es not_active Application Discontinuation
-
2010
- 2010-01-21 EC EC2010009889A patent/ECSP109889A/es unknown
- 2010-01-21 ZA ZA2010/00468A patent/ZA201000468B/en unknown
-
2013
- 2013-07-08 JP JP2013142320A patent/JP5769762B2/ja not_active Expired - Fee Related
-
2014
- 2014-05-19 US US14/281,790 patent/US20140343062A1/en not_active Abandoned
-
2015
- 2015-05-07 JP JP2015094705A patent/JP2015143277A/ja not_active Withdrawn
-
2016
- 2016-10-19 US US15/298,070 patent/US20170136000A1/en not_active Abandoned
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