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)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (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 |
|---|---|---|---|
| EA200801619A EA018544B1 (ru) | 2005-12-30 | 2006-12-29 | Способ лечения ретровирусной инфекции |
| 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) |
Family Applications Before (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 (enExample) |
| EP (2) | EP1976517A1 (enExample) |
| JP (1) | JP4676536B2 (enExample) |
| KR (3) | KR101524165B1 (enExample) |
| CN (1) | CN104069108A (enExample) |
| AP (1) | AP2702A (enExample) |
| AU (1) | AU2006332664B2 (enExample) |
| BR (1) | BRPI0620865A2 (enExample) |
| CA (2) | CA2847871C (enExample) |
| EA (2) | EA018544B1 (enExample) |
| HR (1) | HRP20080313A2 (enExample) |
| IL (1) | IL192208A (enExample) |
| NO (1) | NO20083333L (enExample) |
| NZ (1) | NZ569576A (enExample) |
| SG (2) | SG170795A1 (enExample) |
| WO (1) | WO2007079260A1 (enExample) |
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 |
| LT2487163T (lt) | 2007-02-23 | 2016-10-25 | Gilead Sciences, Inc. | Terapinių agentų farmakokinetinių savybių moduliatoriai |
| EP2167088A1 (en) * | 2007-06-29 | 2010-03-31 | Gilead Sciences, Inc. | Therapeutic compositions and the use thereof |
| JP5547067B2 (ja) * | 2007-06-29 | 2014-07-09 | ギリアード サイエンシーズ， インコーポレイテッド | 治療組成物およびその使用 |
| WO2009092002A1 (en) * | 2008-01-17 | 2009-07-23 | Duquesne University Of The Holy Spirit | Antiretroviral drug formulations for treatment of children exposed to hiv/aids |
| PT3494972T (pt) * | 2010-01-27 | 2024-02-12 | Viiv Healthcare Co | Combinações de dolutegravir e lamivudina para o tratamento de infeção pelo hiv |
| US8703786B2 (en) * | 2011-12-07 | 2014-04-22 | Texas Southern University | Etravirine formulations and uses thereof |
| AU2013361401C1 (en) | 2012-12-21 | 2018-08-09 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| NO2865735T3 (enExample) | 2013-07-12 | 2018-07-21 | ||
| PL3019503T3 (pl) | 2013-07-12 | 2018-01-31 | Gilead Sciences Inc | Policykliczne związki karbamoilopirydonowe i ich zastosowanie do leczenia infekcji hiv |
| 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 (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 |
| TWI738321B (zh) | 2014-12-23 | 2021-09-01 | 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 |
| CN118286245A (zh) | 2014-12-26 | 2024-07-05 | 埃莫里大学 | N4-羟基胞苷和衍生物及与其相关的抗病毒用途 |
| CN110790773A (zh) | 2015-04-02 | 2020-02-14 | 吉利德科学公司 | 多环氨甲酰基吡啶酮化合物及其药物用途 |
| CA2948021C (en) | 2015-11-09 | 2024-06-18 | Gilead Sciences, Inc. | Pharmaceutical formulations of (2r,5s,13 ar)-8hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzy1)-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 |
| US11331331B2 (en) | 2017-12-07 | 2022-05-17 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
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 |
| US5539122A (en) * | 1989-05-23 | 1996-07-23 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| DE674513T1 (de) * | 1992-12-29 | 1996-01-18 | Abbott Lab | Inhibitoren der retroviralen protease. |
| 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 |
| ES2324549T5 (es) * | 1999-06-04 | 2012-10-31 | Abbott Laboratories | Solución farmacéutica que comprende ritonavir, un disolvente (ácido graso de cadena larga) y agua |
| 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 |
| AU2003301439A1 (en) * | 2002-10-16 | 2004-05-04 | Gilead Sciences, Inc. | Pre-organized tricyclic integrase inhibitor compounds |
| SI1564210T1 (sl) * | 2002-11-20 | 2010-01-29 | Japan Tobacco Inc | 4-oksokinolinske spojine in njihova uporaba kot inhibitorji HIV integraze |
| 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 |
| US7531554B2 (en) * | 2004-05-20 | 2009-05-12 | Japan Tobacco Inc. | 4-oxoquinoline compound and use thereof as HIV integrase inhibitor |
| EP2332538A1 (en) | 2004-05-21 | 2011-06-15 | Japan Tobacco, Inc. | Combinations comprising a 4-isoquinolone derivative and anti-HIV agents |
| US8119602B2 (en) * | 2005-06-02 | 2012-02-21 | Schering Corporation | Administration of HCV protease inhibitors in combination with food to improve bioavailability |
| US20090233964A1 (en) * | 2005-12-30 | 2009-09-17 | Gilead Sciences, Inc. | Methods for improving the pharmacokinetics of hiv integrase inhibitors |
| CA2661943C (en) * | 2006-09-12 | 2015-11-03 | Gilead Sciences, Inc. | Process and intermediates for preparing integrase inhibitors |
| JP5547067B2 (ja) * | 2007-06-29 | 2014-07-09 | ギリアード サイエンシーズ， インコーポレイテッド | 治療組成物およびその使用 |
| EP2167088A1 (en) * | 2007-06-29 | 2010-03-31 | 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 |
-
2006
- 2006-12-29 SG SG201102227-4A patent/SG170795A1/en unknown
- 2006-12-29 AP AP2008004522A patent/AP2702A/xx active
- 2006-12-29 CA CA2847871A patent/CA2847871C/en active Active
- 2006-12-29 KR KR1020087018651A patent/KR101524165B1/ko active Active
- 2006-12-29 CN CN201410249622.8A patent/CN104069108A/zh active Pending
- 2006-12-29 AU AU2006332664A patent/AU2006332664B2/en active Active
- 2006-12-29 KR KR1020167016288A patent/KR20160074018A/ko not_active Ceased
- 2006-12-29 SG SG201102229-0A patent/SG170796A1/en unknown
- 2006-12-29 EP EP06848393A patent/EP1976517A1/en not_active Withdrawn
- 2006-12-29 KR KR1020147014797A patent/KR20140082858A/ko not_active Ceased
- 2006-12-29 NZ NZ569576A patent/NZ569576A/en unknown
- 2006-12-29 BR BRPI0620865-7A patent/BRPI0620865A2/pt not_active IP Right Cessation
- 2006-12-29 HR HR20080313A patent/HRP20080313A2/xx not_active Application Discontinuation
- 2006-12-29 EP EP20100193364 patent/EP2308490A1/en not_active Withdrawn
- 2006-12-29 CA CA2635468A patent/CA2635468C/en active Active
- 2006-12-29 US US11/647,858 patent/US20070219243A1/en not_active Abandoned
- 2006-12-29 JP JP2008548784A patent/JP4676536B2/ja active Active
- 2006-12-29 EA EA200801619A patent/EA018544B1/ru unknown
- 2006-12-29 WO PCT/US2006/049668 patent/WO2007079260A1/en not_active Ceased
- 2006-12-29 EA EA201201496A patent/EA201201496A1/ru unknown
-
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 |
|---|---|
| AU2006332664A1 (en) | 2007-07-12 |
| NO20083333L (no) | 2008-09-29 |
| WO2007079260A9 (en) | 2007-08-30 |
| EP1976517A1 (en) | 2008-10-08 |
| HRP20080313A2 (en) | 2008-11-30 |
| CA2847871C (en) | 2016-07-26 |
| JP4676536B2 (ja) | 2011-04-27 |
| CA2635468C (en) | 2016-08-09 |
| IL192208A (en) | 2013-10-31 |
| KR101524165B1 (ko) | 2015-06-01 |
| CA2635468A1 (en) | 2007-07-12 |
| CA2847871A1 (en) | 2007-07-12 |
| WO2007079260A1 (en) | 2007-07-12 |
| SG170796A1 (en) | 2011-05-30 |
| KR20080081358A (ko) | 2008-09-09 |
| US20070219243A1 (en) | 2007-09-20 |
| BRPI0620865A2 (pt) | 2011-11-29 |
| IL192208A0 (en) | 2009-02-11 |
| AU2006332664B2 (en) | 2013-03-14 |
| NZ569576A (en) | 2011-09-30 |
| EP2308490A1 (en) | 2011-04-13 |
| CN104069108A (zh) | 2014-10-01 |
| KR20140082858A (ko) | 2014-07-02 |
| JP2009525265A (ja) | 2009-07-09 |
| AP2702A (en) | 2013-07-23 |
| EA200801619A1 (ru) | 2008-10-30 |
| AP2008004522A0 (en) | 2008-06-30 |
| EA018544B1 (ru) | 2013-08-30 |
| KR20160074018A (ko) | 2016-06-27 |
| SG170795A1 (en) | 2011-05-30 |
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