EA201201496A1 - Способ ингибирования интегразы вич, способ улучшения фармакокинетики 6-(3-хлор-2-фторбензил)-1-[(2s)-1-гидрокси-3-метилбутан-2-ил]-7-метокси-4-оксо-1,4-дигидрохинолин-3-карбоновой кислоты (варианты), набор, фармацевтическая композиция (варианты) и антиретровирусный агент (варианты) - Google Patents
Способ ингибирования интегразы вич, способ улучшения фармакокинетики 6-(3-хлор-2-фторбензил)-1-[(2s)-1-гидрокси-3-метилбутан-2-ил]-7-метокси-4-оксо-1,4-дигидрохинолин-3-карбоновой кислоты (варианты), набор, фармацевтическая композиция (варианты) и антиретровирусный агент (варианты)Info
- Publication number
- EA201201496A1 EA201201496A1 EA201201496A EA201201496A EA201201496A1 EA 201201496 A1 EA201201496 A1 EA 201201496A1 EA 201201496 A EA201201496 A EA 201201496A EA 201201496 A EA201201496 A EA 201201496A EA 201201496 A1 EA201201496 A1 EA 201201496A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- options
- hiv integrase
- dihydrochinolin
- methylbutan
- fluorobenzyl
- Prior art date
Links
- 108010002459 HIV Integrase Proteins 0.000 title abstract 2
- -1 3-chloro-2-fluorobenzyl Chemical group 0.000 title 1
- 229940124522 antiretrovirals Drugs 0.000 title 1
- 239000003903 antiretrovirus agent Substances 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229940099797 HIV integrase inhibitor Drugs 0.000 abstract 1
- 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 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 235000013305 food Nutrition 0.000 abstract 1
- 239000003084 hiv integrase inhibitor Substances 0.000 abstract 1
- 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 abstract 1
- 229960000311 ritonavir Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4704—2-Quinolinones, e.g. carbostyril
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75503905P | 2005-12-30 | 2005-12-30 | |
| US75663106P | 2006-01-06 | 2006-01-06 | |
| US76390106P | 2006-02-01 | 2006-02-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA201201496A1 true EA201201496A1 (ru) | 2013-07-30 |
Family
ID=38016698
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201201496A EA201201496A1 (ru) | 2005-12-30 | 2006-12-29 | Способ ингибирования интегразы вич, способ улучшения фармакокинетики 6-(3-хлор-2-фторбензил)-1-[(2s)-1-гидрокси-3-метилбутан-2-ил]-7-метокси-4-оксо-1,4-дигидрохинолин-3-карбоновой кислоты (варианты), набор, фармацевтическая композиция (варианты) и антиретровирусный агент (варианты) |
| EA200801619A EA018544B1 (ru) | 2005-12-30 | 2006-12-29 | Способ лечения ретровирусной инфекции |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200801619A EA018544B1 (ru) | 2005-12-30 | 2006-12-29 | Способ лечения ретровирусной инфекции |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20070219243A1 (https=) |
| EP (2) | EP2308490A1 (https=) |
| JP (1) | JP4676536B2 (https=) |
| KR (3) | KR101524165B1 (https=) |
| CN (1) | CN104069108A (https=) |
| AP (1) | AP2702A (https=) |
| AU (1) | AU2006332664B2 (https=) |
| BR (1) | BRPI0620865A2 (https=) |
| CA (2) | CA2847871C (https=) |
| EA (2) | EA201201496A1 (https=) |
| HR (1) | HRP20080313A2 (https=) |
| IL (1) | IL192208A (https=) |
| NO (1) | NO20083333L (https=) |
| NZ (1) | NZ569576A (https=) |
| SG (2) | SG170795A1 (https=) |
| WO (1) | WO2007079260A1 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090233964A1 (en) * | 2005-12-30 | 2009-09-17 | Gilead Sciences, Inc. | Methods for improving the pharmacokinetics of hiv integrase inhibitors |
| PL3150586T3 (pl) | 2007-02-23 | 2020-06-01 | Gilead Sciences, Inc. | Modulatory farmakokinetycznych właściwości środków terapeutycznych |
| WO2009006199A1 (en) * | 2007-06-29 | 2009-01-08 | Gilead Sciences, Inc. | Therapeutic compositions and the use thereof |
| AR067184A1 (es) * | 2007-06-29 | 2009-09-30 | Gilead Sciences Inc | Uso de 6-(3-cloro-2-fluorbencil)-1-[(2s)-1-hidroxi-3-metilbutan-2-il]-7-metoxi-4-oxo-1,4-dihidroquinolina-3-carboxilico. composicion farmaceutica |
| US20110117193A1 (en) * | 2008-01-17 | 2011-05-19 | Duquesne University Of The Holy Spirit | Antiretroviral drug formulations for treatment of children exposed to hiv/aids |
| PE20121524A1 (es) | 2010-01-27 | 2012-12-03 | Viiv Healthcare Co | Combinaciones de compuestos que comprenden inhibidores de la integrasa de vih y otros agentes terapeuticos |
| WO2013109354A2 (en) * | 2011-12-07 | 2013-07-25 | Texas Southern University | Etravirine formulations and uses thereof |
| EA030003B1 (ru) | 2012-12-21 | 2018-06-29 | Джилид Сайэнс, Инк. | Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции |
| SI3019503T1 (sl) | 2013-07-12 | 2017-11-30 | Gilead Sciences, Inc. | Policiklične karbamoilpiridonske spojine in njihova uporaba za zdravljenje HIV infekcij |
| NO2865735T3 (https=) | 2013-07-12 | 2018-07-21 | ||
| 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 |
| NO2717902T3 (https=) | 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 |
| DK3236972T3 (en) | 2014-12-26 | 2021-10-04 | Univ Emory | Antivirale N4-hydroxycytidin-derivativer |
| JP6402259B2 (ja) | 2015-04-02 | 2018-10-10 | ギリアード サイエンシーズ， インコーポレイテッド | 多環式カルバモイルピリドン化合物およびそれらの薬学的使用 |
| SG11201802983TA (en) | 2015-11-09 | 2018-05-30 | Gilead Sciences Inc | Therapeutic compositions for treatment of human immunodeficiency virus |
| JP6804790B1 (ja) | 2017-12-07 | 2020-12-23 | エモリー ユニバーシティー | Ｎ４−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5354866A (en) * | 1989-05-23 | 1994-10-11 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5552558A (en) * | 1989-05-23 | 1996-09-03 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| EP1302468B1 (en) | 1992-12-29 | 2008-12-17 | Abbott Laboratories | Processes and intermediates for manufacturing retroviral protease inhibiting compounds |
| US5567823A (en) | 1995-06-06 | 1996-10-22 | Abbott Laboratories | Process for the preparation of an HIV protease inhibiting compound |
| US6037157A (en) | 1995-06-29 | 2000-03-14 | Abbott Laboratories | Method for improving pharmacokinetics |
| ATE332132T1 (de) * | 1999-06-04 | 2006-07-15 | Abbott Lab | Verbesserte arzneizubereitungen enthaltend ritonavir |
| US6541515B2 (en) * | 2000-08-09 | 2003-04-01 | Merck & Co., Inc. | HIV integrase inhibitors |
| US6407128B1 (en) * | 2001-12-03 | 2002-06-18 | Elan Pharmaceuticals, Inc. | Method for increasing the bioavailability of metaxalone |
| TWI286476B (en) * | 2001-12-12 | 2007-09-11 | Tibotec Pharm Ltd | Combination of cytochrome P450 dependent protease inhibitors |
| US20040157804A1 (en) | 2002-10-16 | 2004-08-12 | Gilead Sciences, Inc. | Pre-organized tricyclic integrase inhibitor compounds |
| EP2161258A3 (en) | 2002-11-20 | 2010-04-07 | Japan Tabacco Inc. | 4-oxoquinoline compound and use thereof as hiv integrase inhibitor |
| JP3567162B1 (ja) * | 2002-11-20 | 2004-09-22 | 日本たばこ産業株式会社 | 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 |
| BRPI0407052A (pt) * | 2003-01-27 | 2006-01-17 | Pfizer | Inibidores da hiv-integrase, composições farmacêuticas, e métodos para sua utilização |
| US7812016B2 (en) * | 2003-05-13 | 2010-10-12 | Smithkline Beecham Corporation | Naphthyridine integrase inhibitors |
| MY134672A (en) | 2004-05-20 | 2007-12-31 | Japan Tobacco Inc | Stable crystal of 4-oxoquinoline compound |
| WO2005113509A1 (en) * | 2004-05-20 | 2005-12-01 | Japan Tobacco Inc. | Novel 4-oxoquinoline compound and use thereof as hiv integrase inhibitor |
| EP3287130A1 (en) * | 2004-05-21 | 2018-02-28 | Japan Tobacco Inc. | Combinations comprising a 4-isoquinolone derivative and protease inhibitors |
| NZ563361A (en) * | 2005-06-02 | 2011-02-25 | Schering Corp | HCV protease inhibitors in combination with food |
| US20090233964A1 (en) * | 2005-12-30 | 2009-09-17 | Gilead Sciences, Inc. | Methods for improving the pharmacokinetics of hiv integrase inhibitors |
| EA022099B1 (ru) * | 2006-09-12 | 2015-11-30 | Джилид Сайэнс, Инк. | Способы и интермедиаты для получения ингибиторов интегразы |
| WO2009006199A1 (en) * | 2007-06-29 | 2009-01-08 | Gilead Sciences, Inc. | Therapeutic compositions and the use thereof |
| AR067184A1 (es) * | 2007-06-29 | 2009-09-30 | Gilead Sciences Inc | Uso de 6-(3-cloro-2-fluorbencil)-1-[(2s)-1-hidroxi-3-metilbutan-2-il]-7-metoxi-4-oxo-1,4-dihidroquinolina-3-carboxilico. composicion farmaceutica |
| AR068403A1 (es) * | 2007-09-11 | 2009-11-18 | Gilead Sciences Inc | Proceso e intermediarios para la preparacion de inhibidores de integrasa |
-
2006
- 2006-12-29 JP JP2008548784A patent/JP4676536B2/ja active Active
- 2006-12-29 KR KR1020087018651A patent/KR101524165B1/ko active Active
- 2006-12-29 HR HR20080313A patent/HRP20080313A2/xx not_active Application Discontinuation
- 2006-12-29 KR KR1020167016288A patent/KR20160074018A/ko not_active Ceased
- 2006-12-29 US US11/647,858 patent/US20070219243A1/en not_active Abandoned
- 2006-12-29 SG SG201102227-4A patent/SG170795A1/en unknown
- 2006-12-29 WO PCT/US2006/049668 patent/WO2007079260A1/en not_active Ceased
- 2006-12-29 EA EA201201496A patent/EA201201496A1/ru unknown
- 2006-12-29 BR BRPI0620865-7A patent/BRPI0620865A2/pt not_active IP Right Cessation
- 2006-12-29 SG SG201102229-0A patent/SG170796A1/en unknown
- 2006-12-29 NZ NZ569576A patent/NZ569576A/en unknown
- 2006-12-29 CN CN201410249622.8A patent/CN104069108A/zh active Pending
- 2006-12-29 AU AU2006332664A patent/AU2006332664B2/en active Active
- 2006-12-29 EP EP20100193364 patent/EP2308490A1/en not_active Withdrawn
- 2006-12-29 CA CA2847871A patent/CA2847871C/en active Active
- 2006-12-29 KR KR1020147014797A patent/KR20140082858A/ko not_active Ceased
- 2006-12-29 EP EP06848393A patent/EP1976517A1/en not_active Withdrawn
- 2006-12-29 EA EA200801619A patent/EA018544B1/ru unknown
- 2006-12-29 AP AP2008004522A patent/AP2702A/xx active
- 2006-12-29 CA CA2635468A patent/CA2635468C/en active Active
-
2008
- 2008-06-16 IL IL192208A patent/IL192208A/en active IP Right Grant
- 2008-07-29 NO NO20083333A patent/NO20083333L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2007079260A9 (en) | 2007-08-30 |
| EP2308490A1 (en) | 2011-04-13 |
| JP4676536B2 (ja) | 2011-04-27 |
| IL192208A0 (en) | 2009-02-11 |
| US20070219243A1 (en) | 2007-09-20 |
| AU2006332664A1 (en) | 2007-07-12 |
| KR101524165B1 (ko) | 2015-06-01 |
| CA2847871A1 (en) | 2007-07-12 |
| EP1976517A1 (en) | 2008-10-08 |
| CA2635468C (en) | 2016-08-09 |
| AP2008004522A0 (en) | 2008-06-30 |
| CN104069108A (zh) | 2014-10-01 |
| JP2009525265A (ja) | 2009-07-09 |
| CA2635468A1 (en) | 2007-07-12 |
| KR20160074018A (ko) | 2016-06-27 |
| BRPI0620865A2 (pt) | 2011-11-29 |
| CA2847871C (en) | 2016-07-26 |
| EA200801619A1 (ru) | 2008-10-30 |
| IL192208A (en) | 2013-10-31 |
| SG170796A1 (en) | 2011-05-30 |
| EA018544B1 (ru) | 2013-08-30 |
| KR20140082858A (ko) | 2014-07-02 |
| NZ569576A (en) | 2011-09-30 |
| SG170795A1 (en) | 2011-05-30 |
| HRP20080313A2 (en) | 2008-11-30 |
| WO2007079260A1 (en) | 2007-07-12 |
| AU2006332664B2 (en) | 2013-03-14 |
| AP2702A (en) | 2013-07-23 |
| KR20080081358A (ko) | 2008-09-09 |
| NO20083333L (no) | 2008-09-29 |
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