CU24478B1 - (2r,5s,13ar)-7,9-dioxo-10-((2,4,6-trifluorobencil)carbamoil)-2,3,4,5,7,9,13, 13a-octahidro-2,5-metanopirido[1',2':4,5]pirazino[2,1-b][1,3]oxazepin-8-olato de sodio - Google Patents

(2r,5s,13ar)-7,9-dioxo-10-((2,4,6-trifluorobencil)carbamoil)-2,3,4,5,7,9,13, 13a-octahidro-2,5-metanopirido[1',2':4,5]pirazino[2,1-b][1,3]oxazepin-8-olato de sodio

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Publication number
CU24478B1
CU24478B1 CU2016000187A CU20160187A CU24478B1 CU 24478 B1 CU24478 B1 CU 24478B1 CU 2016000187 A CU2016000187 A CU 2016000187A CU 20160187 A CU20160187 A CU 20160187A CU 24478 B1 CU24478 B1 CU 24478B1
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CU
Cuba
Prior art keywords
methanopyrido
oxazepin
trifluorobenzyl
octahydro
dioxo
Prior art date
Application number
CU2016000187A
Other languages
English (en)
Spanish (es)
Other versions
CU20160187A7 (es
Inventor
Ernest A Carra
Irene Chen
Vahid Zia
Original Assignee
Gilead Sciences Inc
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Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of CU20160187A7 publication Critical patent/CU20160187A7/es
Publication of CU24478B1 publication Critical patent/CU24478B1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/683Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/683Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CU2016000187A 2014-06-20 2015-06-19 (2r,5s,13ar)-7,9-dioxo-10-((2,4,6-trifluorobencil)carbamoil)-2,3,4,5,7,9,13, 13a-octahidro-2,5-metanopirido[1',2':4,5]pirazino[2,1-b][1,3]oxazepin-8-olato de sodio CU24478B1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462015245P 2014-06-20 2014-06-20
PCT/US2015/036757 WO2015196116A1 (en) 2014-06-20 2015-06-19 Sodium (2r, 5s, 13ar) -7, 9-dioxo-10- ( (2,4,6-trifluorobenzyl) carbamoyl) -2, 3, 4, 5, 7, 9, 13, 13a-octahydro-2, 5-methanopyrido [1',2' : 4.5] pyrazino [2, 1-b] oxazepin-8-olate

Publications (2)

Publication Number Publication Date
CU20160187A7 CU20160187A7 (es) 2017-04-05
CU24478B1 true CU24478B1 (es) 2020-03-04

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CU2016000187A CU24478B1 (es) 2014-06-20 2015-06-19 (2r,5s,13ar)-7,9-dioxo-10-((2,4,6-trifluorobencil)carbamoil)-2,3,4,5,7,9,13, 13a-octahidro-2,5-metanopirido[1',2':4,5]pirazino[2,1-b][1,3]oxazepin-8-olato de sodio

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Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3067358T1 (sl) 2012-12-21 2019-12-31 Gilead Sciences, Inc. Policiklične spojine karbamoilpiridona in njihova farmacevtska uporaba
NO2717902T3 (show.php) * 2014-06-20 2018-06-23
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
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
MX2017016806A (es) * 2015-06-30 2018-05-07 Gilead Sciences Inc Formulaciones farmaceuticas que comprenden tenofovir y emtricitabina.
CN108348473B (zh) 2015-11-09 2021-06-18 吉利德科学公司 治疗人免疫缺陷病毒的治疗组合物
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
JP2019528304A (ja) * 2016-08-31 2019-10-10 ヴィーブ ヘルスケア カンパニー 組み合わせ並びにその使用及び治療
EP3518935A1 (en) * 2016-09-27 2019-08-07 Gilead Sciences, Inc. Therapeutic compositions for treatment of human immunodeficiency virus
CN107445994A (zh) * 2017-05-31 2017-12-08 北京阜康仁生物制药科技有限公司 替诺福韦艾拉酚胺半富马酸盐新晶型
DK3749673T3 (da) * 2018-02-09 2022-06-20 Sandoz Ag Krystallinsk form af bictegravir-natrium
EP3784676A1 (en) 2018-04-26 2021-03-03 Mylan Laboratories Ltd. Polymorphic forms of bictegravir and its sodium salt
US11623933B2 (en) 2018-06-28 2023-04-11 Honour Lab Limited Process for the preparation of sodium (2R,5S,13AR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl) carbamoyl)-2,3,4,5,7,9,13,13A-octahydro-2,5-Methanopyrido[1 ′,2′:4,5]pyrazino[2,1 -b] [1,3] oxazepin-8-olate and its polymorphic form
AU2019344929B2 (en) * 2018-09-19 2023-03-30 Gilead Sciences, Inc. Integrase inhibitors for the prevention of HIV
EP3653629A1 (en) 2018-11-16 2020-05-20 Sandoz AG Acid addition salts of an integrase strand transfer inhibitor
US12195480B2 (en) 2019-02-07 2025-01-14 Cipla Limited Polymorphs of integrase inhibitor
WO2020197991A1 (en) 2019-03-22 2020-10-01 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
WO2020255004A1 (en) * 2019-06-18 2020-12-24 Laurus Labs Limited Process and polymorphic forms of bictegravir and its pharmaceutically acceptable salts or co-crystals thereof
CN111978333B (zh) * 2019-09-30 2021-06-18 常州制药厂有限公司 Bictegravir钠盐的晶型A、制备方法及用途
BR112022015771A2 (pt) 2020-02-24 2022-10-11 Gilead Sciences Inc Compostos tetracíclicos para tratar a infecção por hiv
TW202421168A (zh) 2020-03-20 2024-06-01 美商基利科學股份有限公司 4’-c-經取代-2-鹵基-2’-去氧腺苷核苷之前藥及其製造與使用方法
EP4153181A1 (en) 2020-05-21 2023-03-29 Gilead Sciences, Inc. Pharmaceutical compositions comprising bictegravir
CN113698420A (zh) * 2020-05-22 2021-11-26 上海迪赛诺生物医药有限公司 比克替拉韦钠的新晶型及其制备方法
TW202222798A (zh) 2020-09-30 2022-06-16 美商基利科學股份有限公司 橋接三環胺甲醯基吡啶酮化合物及其用途
TWI815194B (zh) 2020-10-22 2023-09-11 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
WO2022103758A1 (en) 2020-11-11 2022-05-19 Gilead Sciences, Inc. METHODS OF IDENTIFYING HIV PATIENTS SENSITIVE TO THERAPY WITH gp120 CD4 BINDING SITE-DIRECTED ANTIBODIES
CN112409380A (zh) * 2020-12-10 2021-02-26 上海迪赛诺生物医药有限公司 比克替拉韦钠的新晶型的制备方法及其应用
CA3202957A1 (en) 2021-01-19 2022-07-28 Hang CHU Substituted pyridotriazine compounds and uses thereof
WO2022224120A1 (en) * 2021-04-19 2022-10-27 Honour Lab Limited Polymorphic forms of bictegravir potassium
CN118369316A (zh) 2021-12-03 2024-07-19 吉利德科学公司 Hiv病毒感染的治疗性化合物
TWI843506B (zh) 2022-04-06 2024-05-21 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
WO2023248240A1 (en) 2022-06-21 2023-12-28 Mylan Laboratories Limited Polymorphic forms of bictegravir sodium
TW202434566A (zh) 2022-07-01 2024-09-01 美商基利科學股份有限公司 可用於hiv病毒感染之疾病預防性或治療性治療的治療性化合物
AU2023330037A1 (en) 2022-08-26 2025-03-06 Gilead Sciences, Inc. Dosing and scheduling regimen for broadly neutralizing antibodies
EP4598934A1 (en) 2022-10-04 2025-08-13 Gilead Sciences, Inc. 4'-thionucleoside analogues and their pharmaceutical use
AR132464A1 (es) 2023-04-19 2025-07-02 Gilead Sciences Inc Régimen de dosificación de inhibidor de la cápside
WO2024249592A1 (en) 2023-05-31 2024-12-05 Gilead Sciences, Inc. Quinazolinyl-indazole derivatives as therapeutic compounds for hiv
TW202504592A (zh) 2023-05-31 2025-02-01 美商基利科學股份有限公司 固體形式
WO2025029247A1 (en) 2023-07-28 2025-02-06 Gilead Sciences, Inc. Weekly regimen of lenacapavir for the treatment and prevention of hiv
WO2025042394A1 (en) 2023-08-23 2025-02-27 Gilead Sciences, Inc. Dosing regimen of hiv capsid inhibitor
WO2025080850A1 (en) * 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
US20250122219A1 (en) * 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
TW202515549A (zh) 2023-10-11 2025-04-16 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
US20250333424A1 (en) 2024-03-01 2025-10-30 Gilead Sciences, Inc. Antiviral compounds
US20250289822A1 (en) 2024-03-01 2025-09-18 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
WO2025184447A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
WO2025260028A1 (en) 2024-06-14 2025-12-18 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors

Family Cites Families (121)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE788516A (fr) 1971-09-10 1973-03-07 Lonza Ag Procede de fabrication d'esters alcoxyacetylacetiques
GB1528382A (en) 1974-12-26 1978-10-11 Teijin Ltd Cyclopentene diols and acyl esters thereof and processes for their preparation
DE2658401A1 (de) 1976-12-23 1978-07-06 Merck Patent Gmbh Cyclopentan-1-amine, verfahren zu ihrer herstellung und diese verbindungen enthaltende mittel
US4575694A (en) 1984-03-05 1986-03-11 Allied Corporation Coaxial connector
DE3900735A1 (de) 1989-01-12 1990-07-26 Hoechst Ag Neue mehrfunktionelle (alpha)-diazo-(beta)-ketoester, verfahren zu ihrer herstellung und deren verwendung
US5204466A (en) 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
US6703396B1 (en) 1990-02-01 2004-03-09 Emory University Method of resolution and antiviral activity of 1,3-oxathiolane nuclesoside enantiomers
US6642245B1 (en) 1990-02-01 2003-11-04 Emory University Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
DE4014649A1 (de) 1990-05-08 1991-11-14 Hoechst Ag Neue mehrfunktionelle verbindungen mit (alpha)-diazo-ss-ketoester- und sulfonsaeureester-einheiten, verfahren zu ihrer herstellung und deren verwendung
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
US5922695A (en) 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
SE9702772D0 (sv) 1997-07-22 1997-07-22 Astra Pharma Prod Novel compounds
US5935946A (en) 1997-07-25 1999-08-10 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
WO1999025345A1 (en) 1997-11-14 1999-05-27 Merck & Co., Inc. Alpha-1a adrenergic receptor antagonists
PL347591A1 (en) 1998-11-09 2002-04-08 Gastrin and cholecystokinin receptor ligands
GB2345058A (en) 1998-12-01 2000-06-28 Cerebrus Pharm Ltd Hydroxypyridone compounds useful in the treatment of oxidative damage to the central nervous system
PL348596A1 (en) 1998-12-25 2002-06-03 Shionogi & Co Aromatic heterocycle compounds having hiv integrase inhibiting activities
US20040039060A1 (en) 2000-06-14 2004-02-26 Ryuichi Kiyama Inhibitor for enzyme having two divalent metal ions as active centers
DK2266958T1 (da) 2001-08-10 2016-04-04 Shionogi & Co Antiviralt middel
HUP0402503A2 (hu) 2001-10-03 2005-03-29 Ucb, S.A. Pirrolidinonszármazékok és a vegyületeket tartalmazó gyógyászati készítmények
SI1441735T1 (sl) 2001-10-26 2006-06-30 Angeletti P Ist Richerche Bio N-substituirani hidroksipirimidinon-karboksamidniinhibitorji HIV-integraze
WO2004004657A2 (en) 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Hiv integrase inhibitors
EP1549315A4 (en) 2002-09-11 2007-05-23 Merck & Co Inc DIHYDROXYPYRIDOPYRAZINE-1,6-DION COMPOUNDS AS HIV INTEGRASE INHIBITORS
BRPI0306214B1 (pt) 2002-11-20 2017-08-08 Japan Tobacco Inc. 4-oxoquinoline compound and use of this as a hiv integrase inhibitor
AU2004206821C1 (en) 2003-01-14 2009-10-01 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
DK1628685T3 (da) 2003-04-25 2011-03-21 Gilead Sciences Inc Antivirale phosphonatanaloge
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
TW200528440A (en) 2003-10-31 2005-09-01 Fujisawa Pharmaceutical Co 2-cyanopyrrolidinecarboxamide compound
EP1713773A4 (en) 2004-01-30 2009-09-23 Merck & Co Inc N-BENZYL-3,4-DIHYDROXYPYRIDINE-2-CARBOXYLIC AMID AND N-BENZYL-2,3-DIHYDROXYPYRIDINE-4-CARBOXYLIC AMIDE COMPOUNDS SUITABLE AS INHIBITORS OF THE HIV INTEGRASE
AU2005220767A1 (en) 2004-03-09 2005-09-22 Merck & Co., Inc. HIV integrase inhibitors
EP1755586A2 (en) 2004-04-29 2007-02-28 The Regents of the University of California Hydroxypyridinone, hydroxypyridinethione, pyrone, and thiopyrone metalloprotein inhibitors
WO2005110399A2 (en) 2004-04-29 2005-11-24 The Regents Of The University Of California Zinc-binding groups for metalloprotein inhibitors
CN1964975B (zh) 2004-05-07 2011-11-30 默沙东公司 Hiv整合酶抑制剂
US7273859B2 (en) 2004-05-12 2007-09-25 Bristol-Myers Squibb Company HIV integrase inhibitors: cyclic pyrimidinone compounds
WO2005113509A1 (en) 2004-05-20 2005-12-01 Japan Tobacco Inc. Novel 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
MY134672A (en) 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
EP3287130A1 (en) 2004-05-21 2018-02-28 Japan Tobacco Inc. Combinations comprising a 4-isoquinolone derivative and protease inhibitors
AU2005330489B2 (en) 2004-07-27 2011-08-25 Gilead Sciences, Inc. Nucleoside phosphonate conjugates as anti HIV agents
US7550463B2 (en) 2004-09-15 2009-06-23 Shionogi & Co., Ltd. Carbamoylpyridone derivatives having inhibitory activity against HIV integrase
JP2006118669A (ja) 2004-10-25 2006-05-11 Sanoh Industrial Co Ltd 樹脂チューブ
WO2006066414A1 (en) 2004-12-23 2006-06-29 Virochem Pharma Inc. Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase
US7858788B2 (en) 2005-02-21 2010-12-28 Shionogi & Co., Ltd. Bicyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
CN101212903B (zh) * 2005-04-28 2013-07-24 史密丝克莱恩比彻姆公司 具有hiv整合酶抑制活性的多环氨基甲酰基吡啶酮衍生物
PL3372281T3 (pl) * 2005-04-28 2021-12-27 Viiv Healthcare Company Policykliczne pochodne karbamoilopirydonu o aktywności inhibitorowej wobec integrazy HIV
WO2006125048A2 (en) 2005-05-16 2006-11-23 Gilead Sciences, Inc. Hiv-integrase inhibitor compounds
EP1906971A2 (en) 2005-07-27 2008-04-09 Gilead Sciences, Inc. Antiviral compounds
BRPI0617842A2 (pt) 2005-10-27 2011-08-09 Shionogi & Co composto ou um sal farmaceuticamente aceitável ou um solvato do mesmo, e, composição farmacêutica
KR101524165B1 (ko) 2005-12-30 2015-06-01 길리애드 사이언시즈, 인코포레이티드 Hiv 인테그라제 억제제의 약동학을 개선하기 위한 방법
US7601844B2 (en) 2006-01-27 2009-10-13 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
US20090018162A1 (en) 2006-02-01 2009-01-15 Yuji Matsuzaki Use of 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or salt thereof for treating retrovirus infection
WO2007102499A1 (ja) 2006-03-06 2007-09-13 Japan Tobacco Inc. 4-オキソキノリン化合物の製造方法
ES2531190T3 (es) 2006-03-06 2015-03-11 Japan Tobacco Inc Método para producir un compuesto de 4-oxoquinolina
US7893055B2 (en) 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
MX2009000661A (es) 2006-07-19 2009-03-27 Univ Georgia Res Found Piridinon-diceto-acidos: inhibidores de replicacion de vih en terapia de combinacion.
HRP20090213B1 (hr) 2006-09-12 2016-12-02 Gilead Sciences, Inc. Postupak i međuprodukti u pripravi inhibitora integraze
EP2084160A1 (en) 2006-10-18 2009-08-05 Merck & Co., Inc. Hiv integrase inhibitors
ES2779826T3 (es) 2007-02-23 2020-08-20 Gilead Sciences Inc Moduladores de propiedades farmacocinéticas de agentes terapéuticos
US20080280945A1 (en) 2007-05-09 2008-11-13 Sachin Lohani Crystalline forms of an HIV integrase inhibitor
CN101686972B (zh) 2007-06-29 2013-08-14 吉里德科学公司 治疗用组合物和方法
CN103356622A (zh) 2007-06-29 2013-10-23 吉里德科学公司 治疗用组合物及其用途
EP2182801A4 (en) 2007-07-31 2011-04-13 Limerick Biopharma Inc COMPOSITIONS OF PYRONE ANALOGS AND METHODS
AR068403A1 (es) 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa
WO2009062285A1 (en) 2007-11-16 2009-05-22 Boehringer Ingelheim International Gmbh Inhibitors of human immunodeficiency virus replication
GB0803019D0 (en) 2008-02-19 2008-03-26 Btg Int Ltd Fluorinated compounds
US8129398B2 (en) 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2010011813A1 (en) 2008-07-23 2010-01-28 Alkermes, Inc. Complex of trospium and pharmaceutical compositions thereof
PL2320908T3 (pl) 2008-07-25 2014-06-30 Viiv Healthcare Co Proleki dolutegrawiru
WO2010011816A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
WO2010011818A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
WO2010011819A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
KR101772610B1 (ko) 2008-07-25 2017-09-12 비이브 헬쓰케어 컴퍼니 화합물
WO2010011815A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
JP5572168B2 (ja) 2008-12-11 2014-08-13 ビーブ・ヘルスケア・カンパニー カルバモイルピリドンhivインテグラーゼ阻害剤の製造方法および中間体
US8624023B2 (en) 2008-12-11 2014-01-07 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates
US8835461B2 (en) 2009-03-26 2014-09-16 Shionogi & Co., Ltd. Substituted 3-hydroxy-4-pyridone derivative
TWI518084B (zh) 2009-03-26 2016-01-21 鹽野義製藥股份有限公司 哌喃酮與吡啶酮衍生物之製造方法
US8338441B2 (en) 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
PL2444400T3 (pl) 2009-06-15 2018-08-31 Shionogi & Co., Ltd. Podstawiona policykliczna pochodna karbamoilopirydonowa
US8637674B2 (en) 2009-09-02 2014-01-28 Ewha University-Industry Collaboration Foundation Pyrazole derivatives, preparation method thereof, and composition for prevention and treatment of osteoporosis containing same
EA032868B1 (ru) 2010-01-27 2019-07-31 Вайв Хелткер Компани Комбинация для лечения вич-инфекции
NZ601847A (en) 2010-02-26 2014-03-28 Japan Tobacco Inc 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor
TWI582097B (zh) 2010-03-23 2017-05-11 Viiv醫療保健公司 製備胺甲醯吡啶酮衍生物及中間體之方法
US20130165489A1 (en) 2010-05-03 2013-06-27 The Trustees Of The University Of Pennsylvania Small Molecule Modulators of HIV-1 Capsid Stability and Methods Thereof
SG186821A1 (en) 2010-07-02 2013-02-28 Gilead Sciences Inc 2 -quinolinyl- acetic acid derivatives as hiv antiviral compounds
EP2588450B1 (en) 2010-07-02 2017-05-24 Gilead Sciences, Inc. Napht-2-ylacetic acid derivatives to treat aids
WO2012009009A2 (en) 2010-07-14 2012-01-19 Addex Pharma S.A. Novel 2-amino-4-pyrazolyl-thiazole derivatives and their use as allosteric modulators of metabotropic glutamate receptors
DK3456721T3 (da) 2010-08-05 2021-04-26 Shionogi & Co Fremgangsmåde til at fremstille forbindelser som har hiv-integrase-inhiberende aktivitet.
US8987441B2 (en) 2010-09-24 2015-03-24 Shionogi & Co., Ltd. Substituted polycyclic carbamoyl pyridone derivative prodrug
WO2012106534A2 (en) 2011-02-02 2012-08-09 The Regents Of The University Of California Hiv integrase inhibitors
SG194512A1 (en) 2011-04-21 2013-12-30 Gilead Sciences Inc Benzothiazole compounds and their pharmaceutical use
US20140213553A1 (en) 2011-05-03 2014-07-31 Concert Pharmaceuticals Inc. Carbamoylpyridone derivatives
US9328075B2 (en) 2011-05-05 2016-05-03 St. Jude Children's Research Hospital Pyrimidinone compounds and methods for treating influenza
US9121496B2 (en) 2011-06-29 2015-09-01 Arvinmeritor Technology, Llc Drive axle system and a method of control
ES2553449T3 (es) 2011-07-06 2015-12-09 Gilead Sciences, Inc. Compuestos para el tratamiento de VIH
CN102863512B (zh) 2011-07-07 2016-04-20 上海泓博智源医药技术有限公司 抗病毒化合物
ES2613180T3 (es) * 2011-09-14 2017-05-23 Mapi Pharma Limited Forma amorfa de la sal sódica dolutegravir
RU2014113230A (ru) 2011-10-12 2015-11-20 Шионоги Энд Ко., Лтд. Полициклическое производное пиридона, обладающее ингибирующей активностью в отношении интегразы
EP2804864B1 (en) 2011-12-12 2017-09-06 Bayer Intellectual Property GmbH Amino-substituted imidazopyridazines
US9399645B2 (en) 2011-12-20 2016-07-26 Boehringer Ingelheim International Gmbh Inhibitors of HIV replication
CA2850881C (en) 2012-04-20 2021-02-16 Gilead Sciences, Inc. Benzothiazol-6-yl acetic acid derivatives and their use for treating an hiv infection
WO2014008636A1 (en) 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Macrocyclic compounds as hiv integrase inhibitors
WO2014014933A1 (en) 2012-07-20 2014-01-23 Merck Sharp & Dohme Corp. Hiv treatment with amido-substituted pyrimidinone derivatives
WO2014018449A1 (en) 2012-07-25 2014-01-30 Merck Sharp & Dohme Corp. Substituted naphthyridinedione derivatives as hiv integrase inhibitors
AU2013296289B2 (en) 2012-08-03 2017-10-05 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
CA2890983A1 (en) 2012-11-08 2014-05-15 Bristol-Myers Squibb Company Heteroaryl substituted pyridyl compounds useful as kinase modulators
KR20150093819A (ko) 2012-12-14 2015-08-18 글락소스미스클라인 엘엘씨 약제 조성물
EP2931730B1 (en) 2012-12-17 2019-08-07 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
US20160000721A1 (en) 2012-12-21 2016-01-07 Merck Sharp & Dohme Corp. Gastro-retentive formulations
SI3067358T1 (sl) 2012-12-21 2019-12-31 Gilead Sciences, Inc. Policiklične spojine karbamoilpiridona in njihova farmacevtska uporaba
US20140221355A1 (en) 2012-12-21 2014-08-07 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
AR094311A1 (es) 2012-12-27 2015-07-22 Japan Tobacco Inc Derivados de tetrahidroespiro-ciclopropil-pirido[1,2-a]pirazina inhibidores de la integrasa del hiv
EP3008044B1 (en) 2013-06-13 2018-11-21 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
WO2015039348A1 (en) 2013-09-23 2015-03-26 Merck Sharp & Dohme Corp. Tetracyclic heterocycle compounds useful as hiv integrase inhibitors
HK1221648A1 (zh) 2013-09-27 2017-06-09 Merck Sharp & Dohme Corp. 用作hiv整合酶抑制劑的取代喹嗪衍生物
WO2015089847A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
IN2014CH00247A (show.php) 2014-01-21 2015-08-14 Laurus Labs Private Ltd
WO2015138933A1 (en) 2014-03-13 2015-09-17 Assia Chemical Industries Ltd. Solid state forms of dolutegravir sodium
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 (show.php) 2014-06-20 2018-06-23
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
CN108348473B (zh) 2015-11-09 2021-06-18 吉利德科学公司 治疗人免疫缺陷病毒的治疗组合物

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