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) | US20110009411A1 (enExample) |
| EP (1) | EP2167089A1 (enExample) |
| JP (3) | JP5547067B2 (enExample) |
| KR (1) | KR20100028656A (enExample) |
| CN (2) | CN101743004A (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 (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1976517A1 (en) * | 2005-12-30 | 2008-10-08 | Gilead Sciences, Inc. | Methods for improving the pharmacokinetics of hiv integrase inhibitors |
| PL2049506T5 (pl) | 2006-07-07 | 2024-09-09 | Gilead Sciences, Inc. | Modulatory farmakokinetycznych właściwości leków |
| WO2008033836A2 (en) | 2006-09-12 | 2008-03-20 | Gilead Sciences, Inc. | Process and intermediates for preparing integrase inhibitors |
| MX2009008935A (es) * | 2007-02-23 | 2009-11-02 | Gilead Sciences Inc | Moduladores de las propiedades farmacocineticas de productos terapeuticos. |
| US20100331331A1 (en) * | 2007-06-29 | 2010-12-30 | Therapeutic Compositons And Use Thereof | 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 |
| MX2010011963A (es) | 2008-05-02 | 2010-12-06 | Gilead Sciences Inc | Uso de particulas trasportadoras solidas para mejorar la capacidad de procesamiento de un agente farmaceutico. |
| EP2555757B1 (en) * | 2010-04-09 | 2016-05-25 | Bristol-Myers Squibb Holdings Ireland | Atazanavir sulfate formulations with improved ph effect |
| US20130274254A1 (en) * | 2010-12-21 | 2013-10-17 | Gilead Sciences, Inc. | Inhibitors of cytochrome p450 (cyp3a4) |
| ES3018133T3 (en) | 2011-11-30 | 2025-05-14 | Univ Emory | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| HK1204980A1 (en) * | 2012-03-01 | 2015-12-11 | Gilead Sciences, Inc. | Spray dried formulations |
| AU2013296289B2 (en) | 2012-08-03 | 2017-10-05 | 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 |
| NO2865735T3 (enExample) | 2013-07-12 | 2018-07-21 | ||
| ES2859102T3 (es) | 2013-07-12 | 2021-10-01 | Gilead Sciences Inc | Compuestos de carbamoilpiridona policíclica y su uso para el tratamiento de infecciones por VIH |
| 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 |
| NO2717902T3 (enExample) | 2014-06-20 | 2018-06-23 | ||
| 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 |
| 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 |
| JP7381190B2 (ja) | 2014-12-26 | 2023-11-15 | エモリー・ユニバーシテイ | Ｎ４－ヒドロキシシチジン及び誘導体並びにそれに関連する抗ウイルス用途 |
| KR20190057158A (ko) | 2015-04-02 | 2019-05-27 | 길리애드 사이언시즈, 인코포레이티드 | 폴리시클릭-카르바모일피리돈 화합물 및 그의 제약 용도 |
| PT3706762T (pt) | 2017-12-07 | 2024-12-05 | Univ Emory | N4-hidroxicitidina e derivados e utilizações antivirais relacionadas com os mesmos |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5539122A (en) * | 1989-05-23 | 1996-07-23 | Abbott Laboratories | 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 |
| SK2662004A3 (sk) * | 2002-11-20 | 2005-06-02 | Japan Tobacco, Inc. | Zlúčenina s obsahom 4-oxochinolínu a jej použitie ako inhibítora integráz |
| WO2005034001A1 (en) * | 2003-10-09 | 2005-04-14 | Steven Wheeler | Adaptive medical decision support system |
| MY134672A (en) * | 2004-05-20 | 2007-12-31 | Japan Tobacco Inc | Stable crystal of 4-oxoquinoline compound |
| EP1758581A1 (en) * | 2004-05-21 | 2007-03-07 | 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 |
| US20090233964A1 (en) * | 2005-12-30 | 2009-09-17 | Gilead Sciences, Inc. | Methods for improving the pharmacokinetics of hiv integrase inhibitors |
| EP1976517A1 (en) * | 2005-12-30 | 2008-10-08 | 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 |
| PL2049506T5 (pl) * | 2006-07-07 | 2024-09-09 | Gilead Sciences, Inc. | Modulatory farmakokinetycznych właściwości leków |
| WO2008033836A2 (en) * | 2006-09-12 | 2008-03-20 | Gilead Sciences, Inc. | Process and intermediates for preparing integrase inhibitors |
| US20100331331A1 (en) * | 2007-06-29 | 2010-12-30 | Therapeutic Compositons And Use Thereof | 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 |
| MX2010011963A (es) * | 2008-05-02 | 2010-12-06 | Gilead Sciences Inc | Uso de particulas trasportadoras solidas para mejorar la capacidad de procesamiento de un agente farmaceutico. |
| US20110000941A1 (en) * | 2009-07-06 | 2011-01-06 | Volk J Patrick | Apparatus and System for Carrying a Digital Media Player |
-
2008
- 2008-06-26 AR ARP080102760A patent/AR067184A1/es not_active Application Discontinuation
- 2008-06-26 TW TW097123981A patent/TW200916103A/zh unknown
- 2008-06-26 NZ NZ582089A patent/NZ582089A/xx not_active IP Right Cessation
- 2008-06-26 JP JP2010515115A patent/JP5547067B2/ja not_active Expired - Fee Related
- 2008-06-26 CA CA002691736A patent/CA2691736A1/en not_active Abandoned
- 2008-06-26 AU AU2008270634A patent/AU2008270634B2/en not_active Ceased
- 2008-06-26 UA UAA200913904A patent/UA103881C2/ru unknown
- 2008-06-26 EA EA200971096A patent/EA200971096A1/ru unknown
- 2008-06-26 KR KR1020107001984A patent/KR20100028656A/ko not_active Ceased
- 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 SG SG2012046926A patent/SG182228A1/en unknown
- 2008-06-26 AP AP2009005083A patent/AP2490A/xx active
- 2008-06-26 WO PCT/US2008/068351 patent/WO2009006203A1/en not_active Ceased
- 2008-06-26 US US12/666,995 patent/US20110009411A1/en not_active Abandoned
- 2008-06-26 EP EP20080781024 patent/EP2167089A1/en not_active Withdrawn
- 2008-06-26 MX MX2009013828A patent/MX2009013828A/es not_active Application Discontinuation
- 2008-06-26 CN CN2013101948825A patent/CN103356622A/zh active Pending
- 2008-06-26 US US12/147,220 patent/US20090093482A1/en not_active Abandoned
-
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 ZA ZA2010/00468A patent/ZA201000468B/en unknown
- 2010-01-21 EC EC2010009889A patent/ECSP109889A/es 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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