PT3157932T - (2r,5s,13ar)-7,9-dioxo-10-((2,4,6-trifluorobenzil)-carbamoil)-2,3,4,5,7,9,13,13a-octa-hidro-2,5-metanopirido[ 1',2':4,5]pirazino[2,1-b]oxazepin-8-olato de sódio - Google Patents

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

Info

Publication number
PT3157932T
PT3157932T PT157390634T PT15739063T PT3157932T PT 3157932 T PT3157932 T PT 3157932T PT 157390634 T PT157390634 T PT 157390634T PT 15739063 T PT15739063 T PT 15739063T PT 3157932 T PT3157932 T PT 3157932T
Authority
PT
Portugal
Prior art keywords
methanopyrido
oxazepin
trifluorobenzyl
olate
pyrazino
Prior art date
Application number
PT157390634T
Other languages
English (en)
Inventor
A Carra Ernest
Chen Irene
Zia Vahid
Original Assignee
Gilead Sciences Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53674269&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PT3157932(T) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of PT3157932T publication Critical patent/PT3157932T/pt

Links

Classifications

    • 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
    • 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
    • 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
    • AHUMAN NECESSITIES
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D498/14Ortho-condensed systems
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
PT157390634T 2014-06-20 2015-06-19 (2r,5s,13ar)-7,9-dioxo-10-((2,4,6-trifluorobenzil)-carbamoil)-2,3,4,5,7,9,13,13a-octa-hidro-2,5-metanopirido[ 1',2':4,5]pirazino[2,1-b]oxazepin-8-olato de sódio PT3157932T (pt)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462015245P 2014-06-20 2014-06-20

Publications (1)

Publication Number Publication Date
PT3157932T true PT3157932T (pt) 2018-02-21

Family

ID=53674269

Family Applications (1)

Application Number Title Priority Date Filing Date
PT157390634T PT3157932T (pt) 2014-06-20 2015-06-19 (2r,5s,13ar)-7,9-dioxo-10-((2,4,6-trifluorobenzil)-carbamoil)-2,3,4,5,7,9,13,13a-octa-hidro-2,5-metanopirido[ 1',2':4,5]pirazino[2,1-b]oxazepin-8-olato de sódio

Country Status (44)

Country Link
US (3) US9708342B2 (pt)
EP (2) EP3157932B1 (pt)
JP (4) JP6334007B2 (pt)
KR (1) KR101899803B1 (pt)
CN (2) CN110563747A (pt)
AP (1) AP2016009591A0 (pt)
AR (1) AR100903A1 (pt)
AU (2) AU2015276860B2 (pt)
BR (2) BR122021025861B1 (pt)
CA (1) CA2950307C (pt)
CL (1) CL2016003249A1 (pt)
CR (1) CR20160589A (pt)
CU (1) CU24478B1 (pt)
CY (1) CY1120025T1 (pt)
DK (1) DK3157932T3 (pt)
DO (1) DOP2016000327A (pt)
EA (2) EA030967B1 (pt)
EC (1) ECSP16095566A (pt)
ES (1) ES2660862T3 (pt)
HR (1) HRP20180455T1 (pt)
HU (1) HUE036928T2 (pt)
IL (1) IL249161B (pt)
LT (1) LT3157932T (pt)
MA (2) MA40239B1 (pt)
MD (2) MD4584C1 (pt)
ME (1) ME03037B (pt)
MX (2) MX369555B (pt)
MY (1) MY186696A (pt)
NO (1) NO2717902T3 (pt)
NZ (1) NZ727155A (pt)
PE (1) PE20170150A1 (pt)
PH (1) PH12016502499A1 (pt)
PL (1) PL3157932T3 (pt)
PT (1) PT3157932T (pt)
RS (1) RS56950B1 (pt)
SG (1) SG11201610211QA (pt)
SI (1) SI3157932T1 (pt)
SV (1) SV2016005339A (pt)
TR (1) TR201802179T4 (pt)
TW (2) TWI673274B (pt)
UA (1) UA118480C2 (pt)
UY (1) UY36177A (pt)
WO (1) WO2015196116A1 (pt)
ZA (1) ZA201608744B (pt)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2926068T3 (es) 2012-12-21 2022-10-21 Gilead Sciences Inc Compuestos de carbamoilpiridona policíclicos y su uso farmacéutico
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
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 (pt) 2014-06-20 2018-06-23
WO2017004244A1 (en) * 2015-06-30 2017-01-05 Gilead Sciences, Inc. Pharmaceutical formulations comprising tenofovir and emtricitabine
SG11201802983TA (en) * 2015-11-09 2018-05-30 Gilead Sciences Inc Therapeutic compositions for treatment of human immunodeficiency virus
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
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
US20190183901A1 (en) * 2016-08-31 2019-06-20 Viiv Healthcare Company Combinations and uses and treatments thereof
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
CA3088596A1 (en) 2018-02-09 2019-08-15 Sandoz Ag Crystalline form of bictegravir sodium
CA3098274A1 (en) 2018-04-26 2019-10-31 Mylan Laboratories Limited 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
EP3852761A1 (en) * 2018-09-19 2021-07-28 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
US20220144851A1 (en) 2019-02-07 2022-05-12 Cipla Limited Novel polymorphs of integrase inhibitor
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
JP2023518433A (ja) 2020-03-20 2023-05-01 ギリアード サイエンシーズ, インコーポレイテッド 4’-c-置換-2-ハロ-2’-デオキシアデノシンヌクレオシドのプロドラッグ並びにその製造法及び使用法
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
TW202406932A (zh) 2020-10-22 2024-02-16 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
KR20230107288A (ko) 2020-11-11 2023-07-14 길리애드 사이언시즈, 인코포레이티드 gp120 CD4 결합 부위-지향 항체를 이용한 요법에 감수성인 HIV 환자를 식별하는 방법
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
CR20230315A (es) 2021-01-19 2023-09-01 Gilead Sciences Inc Compuestos de piridotriazina sustituidos y usos de estos
WO2022224120A1 (en) * 2021-04-19 2022-10-27 Honour Lab Limited Polymorphic forms of bictegravir potassium
WO2023102523A1 (en) 2021-12-03 2023-06-08 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
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
WO2024006982A1 (en) 2022-07-01 2024-01-04 Gilead Sciences, Inc. Therapeutic compounds useful for the prophylactic or therapeutic treatment of an hiv virus infection
WO2024044477A1 (en) 2022-08-26 2024-02-29 Gilead Sciences, Inc. Dosing and scheduling regimen for broadly neutralizing antibodies
WO2024076915A1 (en) 2022-10-04 2024-04-11 Gilead Sciences, Inc. 4'-thionucleoside analogues and their pharmaceutical use

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
US5914331A (en) 1990-02-01 1999-06-22 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
CA2346108A1 (en) 1998-11-09 2000-05-18 James Black Foundation Limited 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
CZ20012160A3 (cs) 1998-12-25 2001-10-17 Shionogi & Co., Ltd. Heteroaromatické deriváty s inhibiční aktivitou proti HIV integráze
EP1297834A4 (en) 2000-06-14 2007-05-09 Shionogi & Co ENZYME INHIBITOR HAVING TWO DIVALENT METAL IONS AS ACTIVE CENTERS
DK3042894T1 (da) 2001-08-10 2016-11-07 Shionogi & Co Antiviralt middel
CZ2004442A3 (cs) 2001-10-03 2005-03-16 Ucb, S.A. Pyrrolidinonové deriváty
CN102219750B (zh) 2001-10-26 2013-05-29 P.安杰莱蒂分子生物学研究所 关于hiv整合酶的n-取代的羟基嘧啶酮甲酰胺抑制剂
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
CA2498111A1 (en) 2002-09-11 2004-03-25 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
CA2470365C (en) 2002-11-20 2011-05-17 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
ATE398455T1 (de) 2003-01-14 2008-07-15 Gilead Sciences Inc Zusammensetzungen und verfahren zur antiviralen kombinationstherapie
EA014685B1 (ru) 2003-04-25 2010-12-30 Джилид Сайэнс, Инк. Фосфонатсодержащие антивирусные соединения (варианты) и фармацевтическая композиция на их основе
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
AU2005211349A1 (en) 2004-01-30 2005-08-18 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. N-benzyl-3,4-dihyroxypyridine-2-carboxamide and N-benzyl-2,3-dihydroxypyridine-4-carboxamide compounds useful as HIV integrase inhibitors
US7619086B2 (en) 2004-03-09 2009-11-17 Merck & Co., Inc. HIV integrase inhibitors
WO2005110399A2 (en) 2004-04-29 2005-11-24 The Regents Of The University Of California Zinc-binding groups for metalloprotein inhibitors
WO2006028523A2 (en) 2004-04-29 2006-03-16 THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, SAN DIEGO USDC Technology Transfer Office Hydroxypyridinone, hydroxypyridinethione, pyrone, and thiopyrone metalloprotein inhibitors
US7538112B2 (en) 2004-05-07 2009-05-26 Merck & Co., Inc. HIV integrase inhibitors
US7273859B2 (en) 2004-05-12 2007-09-25 Bristol-Myers Squibb Company HIV integrase inhibitors: cyclic pyrimidinone compounds
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
JP4629104B2 (ja) 2004-05-21 2011-02-09 日本たばこ産業株式会社 4−オキソキノリン誘導体および抗hiv剤を含む併用剤
UA88313C2 (ru) 2004-07-27 2009-10-12 Гилиад Сайенсиз, Инк. Фосфонатные аналоги соединений ингибиторов вич
EP1790638B1 (en) 2004-09-15 2013-04-03 Shionogi Co., Ltd. Carbamoylpyridone derivative having hiv integrase inhibitory activity
JP2006118669A (ja) 2004-10-25 2006-05-11 Sanoh Industrial Co Ltd 樹脂チューブ
CA2634499A1 (en) 2004-12-23 2006-06-29 Virochem Pharma Inc. Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase
ATE516026T1 (de) 2005-02-21 2011-07-15 Shionogi & Co Bicyclisches carbamoylpyridonderivat mit hiv- integrase-hemmender wirkung
UA96568C2 (en) * 2005-04-28 2011-11-25 Глаксосмиткляйн Ллк Polycyclic carbamoyl pyridone derivative as hiv-integrase inhibitor
ES2567197T3 (es) * 2005-04-28 2016-04-20 Viiv Healthcare Company Derivado de carbamoilpiridona policíclico que tiene actividad inhibidora de la integrasa del VIH
AR057023A1 (es) 2005-05-16 2007-11-14 Gilead Sciences Inc Compuestos heterociclicos con propiedades inhibidoras de hiv-integrasa
EP1906971A2 (en) 2005-07-27 2008-04-09 Gilead Sciences, Inc. Antiviral compounds
AU2006307101A1 (en) 2005-10-27 2007-05-03 Shionogi & Co., Ltd. Polycyclic carbamoylpyridone derivative having inhibitory activity on HIV integrase
EP2308490A1 (en) 2005-12-30 2011-04-13 Gilead Sciences, Inc. Methods for improving the pharmacokinetics of hiv integrase inhibitors
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
CN101437801B (zh) 2006-03-06 2013-02-06 日本烟草产业株式会社 制备4-氧代喹啉化合物的方法
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
AU2007275805A1 (en) 2006-07-19 2008-01-24 University Of Georgia Research Foundation, Inc. Pyridinone diketo acids: Inhibitors of HIV replication in combination therapy
TWI411602B (zh) 2006-09-12 2013-10-11 Gilead Sciences Inc 製造整合酶抑制劑的方法及彼所用的中間物
WO2008048538A1 (en) 2006-10-18 2008-04-24 Merck & Co., Inc. Hiv integrase inhibitors
LT2487166T (lt) 2007-02-23 2016-11-10 Gilead Sciences, Inc. Terapinių agentų farmakokinetinių savybių moduliatoriai
US20080280945A1 (en) 2007-05-09 2008-11-13 Sachin Lohani Crystalline forms of an HIV integrase inhibitor
JP5547066B2 (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 治療用組成物およびその使用
WO2009006203A1 (en) 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
WO2009018320A1 (en) 2007-07-31 2009-02-05 Limerick Biopharma, Inc. Pyrone analog compositions and methods
AR068403A1 (es) 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa
EP2220046B1 (en) 2007-11-16 2014-06-18 Gilead Sciences, Inc. 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
US20100272811A1 (en) 2008-07-23 2010-10-28 Alkermes,Inc. Complex of trospium and pharmaceutical compositions thereof
WO2010011815A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
KR101695807B1 (ko) 2008-07-25 2017-01-13 비이브 헬쓰케어 컴퍼니 화합물
ES2449752T3 (es) 2008-07-25 2014-03-21 Viiv Healthcare Company Proceso para la preparación de un derivado de pirido[1,2-a]pirrolo[1',2':3,4]imidazo[1,2-d]piracin-8-carboxamida
PT2320908E (pt) 2008-07-25 2014-03-06 Shionogi & Co Pró-fármacos de dolutegravir
WO2010011819A1 (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
ES2964383T3 (es) 2008-12-11 2024-04-05 Viiv Healthcare Co Procesos e intermedios para inhibidores de la integrasa del VIH de carbamoilpiridona
MX2011006241A (es) 2008-12-11 2011-06-28 Shionogi & Co Sintesis de inhibidores de integrasa de vih de carbamoil-piridona e intermediarios.
JP5697163B2 (ja) 2009-03-26 2015-04-08 塩野義製薬株式会社 置換された3−ヒドロキシ−4−ピリドン誘導体
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
WO2010147068A1 (ja) 2009-06-15 2010-12-23 塩野義製薬株式会社 置換された多環性カルバモイルピリドン誘導体
WO2011028044A2 (ko) 2009-09-02 2011-03-10 이화여자대학교 산학협력단 피라졸 유도체, 이의 제조방법 및 이를 포함하는 골다공증 예방 및 치료용 조성물
KR20170078868A (ko) 2010-01-27 2017-07-07 비이브 헬쓰케어 컴퍼니 항바이러스 치료
JP5765965B2 (ja) 2010-02-26 2015-08-19 日本たばこ産業株式会社 1,3,4,8−テトラヒドロ−2H−ピリド[1,2−a]ピラジン誘導体及びそのHIVインテグラーゼ阻害剤としての利用
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
WO2011139637A1 (en) 2010-05-03 2011-11-10 Philadelphia Health & Education Corporation Small-molecule modulators of hiv-1 capsid stability and methods thereof
BR112013000043A2 (pt) 2010-07-02 2019-09-24 Gilead Sciences Inc derivados de ácido naft-2-ilacético para tratar aids
NZ604716A (en) 2010-07-02 2014-12-24 Gilead Sciences Inc 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds
EP2595986A2 (en) 2010-07-14 2013-05-29 Addex Pharma SA Novel 2-amino-4-pyrazolyl-thiazole derivatives and their use as allosteric modulators of metabotropic glutamate receptors
CN103154004B (zh) 2010-08-05 2016-07-06 盐野义制药株式会社 具有hiv整合酶抑制活性的化合物的制造方法
MX2013003139A (es) 2010-09-24 2013-06-18 Shionogi & Co Profarmaco de derivado de carbamoilpiridona policiclica substituida.
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
WO2012151361A1 (en) 2011-05-03 2012-11-08 Concert Pharmaceuticals Inc. Carbamoylpyridone derivatives
WO2012151567A1 (en) 2011-05-05 2012-11-08 St. Jude Children's Research Hospital Pyrimidinone compounds and methods for preventing and treating influenza
US9121496B2 (en) 2011-06-29 2015-09-01 Arvinmeritor Technology, Llc Drive axle system and a method of control
JP6205354B2 (ja) 2011-07-06 2017-09-27 ギリアード サイエンシーズ, インコーポレイテッド Hivの処置のための化合物
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
US9200009B2 (en) 2011-10-12 2015-12-01 Shionogi & Co., Ltd. Polycyclic pyridone derivative having integrase inhibitory activity
JP6147761B2 (ja) 2011-12-12 2017-06-14 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH アミノ置換イミダゾピリダジン
US9399645B2 (en) 2011-12-20 2016-07-26 Boehringer Ingelheim International Gmbh Inhibitors of HIV replication
ES2571479T3 (es) 2012-04-20 2016-05-25 Gilead Sciences Inc Derivados del ácido benzotiazol-6-il acético y su uso para tratar una infección por VIH
WO2014008636A1 (en) 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Macrocyclic compounds as hiv integrase inhibitors
EP2875024A4 (en) 2012-07-20 2015-12-23 Merck Sharp & Dohme HIV TREATMENT WITH AMIDOSUBSTITUTED PYRIMIDINONE DERIVATIVES
US20150218164A1 (en) 2012-07-25 2015-08-06 Merck Sharp & Dohme Corp. Substituted naphthyridinedione derivatives as hiv integrase inhibitors
ES2608860T3 (es) 2012-08-03 2017-04-17 Gilead Sciences, Inc. Proceso e intermedios para preparar inhibidores de la integrasa
SG11201503397YA (en) 2012-11-08 2015-05-28 Bristol Myers Squibb Co Heteroaryl substituted pyridyl compounds useful as kinase modulators
SG10201704467SA (en) 2012-12-14 2017-06-29 Glaxosmithkline Llc Pharmaceutical compositions
US9714243B2 (en) 2012-12-17 2017-07-25 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as HIV integrase inhibitors
WO2014100077A1 (en) 2012-12-21 2014-06-26 Merck Sharp & Dohme Corp. Gastro-retentive formulations
ES2926068T3 (es) 2012-12-21 2022-10-21 Gilead Sciences Inc Compuestos de carbamoilpiridona policíclicos y su uso farmacéutico
US20140221355A1 (en) 2012-12-21 2014-08-07 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
US20140221378A1 (en) 2012-12-27 2014-08-07 Japan Tobacco Inc. SUBSTITUTED SPIROPYRIDO[1,2-a]PYRAZINE DERIVATIVE AND PHARMACEUTICAL USE OF SAME AS HIV INTEGRASE INHIBITOR
WO2014200880A1 (en) 2013-06-13 2014-12-18 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
AP2016009157A0 (en) 2013-09-27 2016-04-30 Merck Sharp & Dohme Substituted quinolizine derivatives useful as hiv integrase inhibitors
WO2015089847A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
US9856271B2 (en) 2014-01-21 2018-01-02 Laurus Labs Limited Process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof
WO2015138933A1 (en) 2014-03-13 2015-09-17 Assia Chemical Industries Ltd. Solid state forms of dolutegravir sodium
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
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 (pt) * 2014-06-20 2018-06-23
SG11201802983TA (en) 2015-11-09 2018-05-30 Gilead Sciences Inc Therapeutic compositions for treatment of human immunodeficiency virus

Also Published As

Publication number Publication date
RS56950B1 (sr) 2018-05-31
EA201891464A1 (ru) 2019-03-29
MX2019013380A (es) 2020-02-20
AU2018203175A1 (en) 2018-05-24
WO2015196116A1 (en) 2015-12-23
SG11201610211QA (en) 2017-01-27
PE20170150A1 (es) 2017-04-07
MA40239A (fr) 2018-01-09
JP2022095640A (ja) 2022-06-28
MD20170006A2 (ro) 2017-06-30
SI3157932T1 (en) 2018-06-29
NZ727155A (en) 2022-02-25
MD4584C1 (ro) 2019-02-28
TWI731354B (zh) 2021-06-21
JP6334007B2 (ja) 2018-05-30
ECSP16095566A (es) 2017-01-31
MA40239B1 (fr) 2018-05-31
TW202014422A (zh) 2020-04-16
HRP20180455T1 (hr) 2018-05-04
MD20180037A2 (ro) 2018-07-31
BR112016029605A8 (pt) 2021-07-20
MX2016016059A (es) 2017-05-03
US20170197985A1 (en) 2017-07-13
AR100903A1 (es) 2016-11-09
EA201692414A1 (ru) 2017-06-30
CY1120025T1 (el) 2018-12-12
AU2015276860B2 (en) 2018-05-31
DK3157932T3 (en) 2018-03-05
CA2950307C (en) 2019-01-08
TW201613937A (en) 2016-04-16
PH12016502499B1 (en) 2017-03-22
IL249161B (en) 2021-03-25
MY186696A (en) 2021-08-10
CU20160187A7 (es) 2017-04-05
KR20170016985A (ko) 2017-02-14
US9708342B2 (en) 2017-07-18
BR122021025861B1 (pt) 2023-01-24
MD4584B1 (ro) 2018-07-31
EP3157932B1 (en) 2018-01-10
CU24478B1 (es) 2020-03-04
JP2017518356A (ja) 2017-07-06
JP2020097593A (ja) 2020-06-25
IL249161A0 (en) 2017-01-31
MA44221A (fr) 2018-12-26
PL3157932T3 (pl) 2018-05-30
US20160016973A1 (en) 2016-01-21
UA118480C2 (uk) 2019-01-25
CN106459085B (zh) 2019-07-30
US20180065986A1 (en) 2018-03-08
NO2717902T3 (pt) 2018-06-23
HUE036928T2 (hu) 2018-08-28
ES2660862T3 (es) 2018-03-26
TR201802179T4 (tr) 2018-03-21
BR112016029605A2 (pt) 2017-08-22
TWI673274B (zh) 2019-10-01
EA030967B1 (ru) 2018-10-31
ME03037B (me) 2018-10-20
EP3321270A1 (en) 2018-05-16
CR20160589A (es) 2017-02-24
MX369555B (es) 2019-11-12
AU2018203175B2 (en) 2020-01-02
AP2016009591A0 (en) 2016-11-30
UY36177A (es) 2016-01-08
US10385067B2 (en) 2019-08-20
ZA201608744B (en) 2023-04-26
CN110563747A (zh) 2019-12-13
SV2016005339A (es) 2017-03-20
JP2018162246A (ja) 2018-10-18
KR101899803B1 (ko) 2018-09-20
EP3157932A1 (en) 2017-04-26
PH12016502499A1 (en) 2017-03-22
BR112016029605B1 (pt) 2022-10-11
DOP2016000327A (es) 2017-01-15
CN106459085A (zh) 2017-02-22
CA2950307A1 (en) 2015-12-23
AU2015276860A1 (en) 2016-12-22
CL2016003249A1 (es) 2017-07-14
LT3157932T (lt) 2018-02-26

Similar Documents

Publication Publication Date Title
ZA201608744B (en) 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
EP3564244C0 (en) CRYSTAL 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
HK1259623A1 (zh) 作爲irak4調節劑的吡唑並[1,5a]嘧啶衍生物
ZA201605666B (en) Pyrazolo[1,5-a]pyrimidines as antiviral compounds
PT3129374T (pt) (5,6-dihidro)pirimido[4,5-e] indolizinas
AU2015900153A0 (en) Improved Finger Ring, tick-tweezers.