TR201802179T4 - Sodyum (2r,5s,13ar)-7,9-diokso-10-((2,4,6- trifluorobenzil)karbamoil)-2,3,4,5,7,9,13,13a-oktahidro-2,5- metanopirido[1?,2':4,5]pirazino[2,l-b][l,3]oksazepin-8-olat. - Google Patents

Sodyum (2r,5s,13ar)-7,9-diokso-10-((2,4,6- trifluorobenzil)karbamoil)-2,3,4,5,7,9,13,13a-oktahidro-2,5- metanopirido[1?,2':4,5]pirazino[2,l-b][l,3]oksazepin-8-olat. Download PDF

Info

Publication number
TR201802179T4
TR201802179T4 TR2018/02179T TR201802179T TR201802179T4 TR 201802179 T4 TR201802179 T4 TR 201802179T4 TR 2018/02179 T TR2018/02179 T TR 2018/02179T TR 201802179 T TR201802179 T TR 201802179T TR 201802179 T4 TR201802179 T4 TR 201802179T4
Authority
TR
Turkey
Prior art keywords
methanopyrido
oxazepin
trifluorobenzyl
olate
pyrazino
Prior art date
Application number
TR2018/02179T
Other languages
English (en)
Turkish (tr)
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=TR201802179(T4) "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 TR201802179T4 publication Critical patent/TR201802179T4/tr

Links

Classifications

    • 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
    • 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
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
TR2018/02179T 2014-06-20 2015-06-19 Sodyum (2r,5s,13ar)-7,9-diokso-10-((2,4,6- trifluorobenzil)karbamoil)-2,3,4,5,7,9,13,13a-oktahidro-2,5- metanopirido[1?,2':4,5]pirazino[2,l-b][l,3]oksazepin-8-olat. TR201802179T4 (tr)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
TR201802179T4 true TR201802179T4 (tr) 2018-03-21

Family

ID=53674269

Family Applications (1)

Application Number Title Priority Date Filing Date
TR2018/02179T TR201802179T4 (tr) 2014-06-20 2015-06-19 Sodyum (2r,5s,13ar)-7,9-diokso-10-((2,4,6- trifluorobenzil)karbamoil)-2,3,4,5,7,9,13,13a-oktahidro-2,5- metanopirido[1?,2':4,5]pirazino[2,l-b][l,3]oksazepin-8-olat.

Country Status (45)

Country Link
US (3) US20170197985A1 (show.php)
EP (3) EP4523758A3 (show.php)
JP (4) JP6334007B2 (show.php)
KR (1) KR101899803B1 (show.php)
CN (2) CN106459085B (show.php)
AP (1) AP2016009591A0 (show.php)
AR (1) AR100903A1 (show.php)
AU (2) AU2015276860B2 (show.php)
BR (2) BR112016029605B1 (show.php)
CA (1) CA2950307C (show.php)
CL (1) CL2016003249A1 (show.php)
CR (1) CR20160589A (show.php)
CU (1) CU24478B1 (show.php)
CY (1) CY1120025T1 (show.php)
DK (1) DK3157932T3 (show.php)
DO (1) DOP2016000327A (show.php)
EA (2) EA030967B1 (show.php)
EC (1) ECSP16095566A (show.php)
ES (2) ES3010114T3 (show.php)
HR (1) HRP20180455T1 (show.php)
HU (1) HUE036928T2 (show.php)
IL (1) IL249161B (show.php)
LT (1) LT3157932T (show.php)
MA (2) MA40239B1 (show.php)
MD (2) MD20180037A2 (show.php)
ME (1) ME03037B (show.php)
MX (2) MX369555B (show.php)
MY (1) MY186696A (show.php)
NO (1) NO2717902T3 (show.php)
NZ (1) NZ727155A (show.php)
PE (1) PE20170150A1 (show.php)
PH (1) PH12016502499B1 (show.php)
PL (2) PL3321270T3 (show.php)
PT (1) PT3157932T (show.php)
RS (1) RS56950B1 (show.php)
SG (1) SG11201610211QA (show.php)
SI (1) SI3157932T1 (show.php)
SM (1) SMT201800053T1 (show.php)
SV (1) SV2016005339A (show.php)
TR (1) TR201802179T4 (show.php)
TW (2) TWI731354B (show.php)
UA (1) UA118480C2 (show.php)
UY (1) UY36177A (show.php)
WO (1) WO2015196116A1 (show.php)
ZA (1) ZA201608744B (show.php)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013361401C1 (en) 2012-12-21 2018-08-09 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
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
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
PE20180411A1 (es) * 2015-06-30 2018-03-01 Gilead Sciences Inc Formulaciones farmaceuticas que comprenden tenofovir y emtricitabina
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
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
EP3506902A4 (en) * 2016-08-31 2020-04-22 VIIV Healthcare Company COMBINATIONS AND USES AND TREATMENTS THEREOF
US20180085387A1 (en) * 2016-09-27 2018-03-29 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
MX2020008360A (es) * 2018-02-09 2020-09-25 Sandoz Ag Forma cristalina de bictegravir sodico.
EP3784676A1 (en) 2018-04-26 2021-03-03 Mylan Laboratories Ltd. Polymorphic forms of bictegravir and its sodium salt
WO2020003151A1 (en) 2018-06-28 2020-01-02 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
US20210393631A1 (en) * 2018-09-19 2021-12-23 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
WO2020161744A1 (en) 2019-02-07 2020-08-13 Cipla Limited Novel polymorphs of integrase inhibitor
PL3938047T3 (pl) 2019-03-22 2022-11-07 Gilead Sciences, Inc. Zmostkowane tricykliczne związki karbamoilopirydonowe i ich zastosowanie farmaceutyczne
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
CR20220418A (es) 2020-02-24 2022-10-10 Gilead Sciences Inc Compuestos tetracíclicos para el tratamiento de infecciones por vih
CN115605493A (zh) 2020-03-20 2023-01-13 吉利德科学公司(Us) 4′-c-取代的-2-卤代-2′-脱氧腺苷核苷的前药及其制备和使用方法
WO2021236944A1 (en) 2020-05-21 2021-11-25 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
US12421235B2 (en) 2020-09-30 2025-09-23 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
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
US20220144923A1 (en) 2020-11-11 2022-05-12 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
PL4196479T3 (pl) 2021-01-19 2024-03-18 Gilead Sciences, Inc. Podstawione związki pirydotriazynowe i ich zastosowania
US12187740B2 (en) * 2021-04-19 2025-01-07 Honour Lab Limited Polymorphic forms of bictegravir potassium
EP4440701A1 (en) 2021-12-03 2024-10-09 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
TW202446773A (zh) * 2022-04-06 2024-12-01 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
TWI867601B (zh) 2022-07-01 2024-12-21 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
WO2024044477A1 (en) 2022-08-26 2024-02-29 Gilead Sciences, Inc. Dosing and scheduling regimen for broadly neutralizing antibodies
US20240226130A1 (en) 2022-10-04 2024-07-11 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
TW202448483A (zh) 2023-05-31 2024-12-16 美商基利科學股份有限公司 用於hiv之治療性化合物
CN121219281A (zh) 2023-05-31 2025-12-26 吉利德科学公司 用于治疗hiv的化合物的固体形式
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
WO2025080863A1 (en) * 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
US20250120989A1 (en) * 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
US20250127801A1 (en) * 2023-10-11 2025-04-24 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
WO2025184452A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
US20250333424A1 (en) 2024-03-01 2025-10-30 Gilead Sciences, Inc. Antiviral compounds
US20250296932A1 (en) 2024-03-01 2025-09-25 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
US6703396B1 (en) 1990-02-01 2004-03-09 Emory University Method of resolution and antiviral activity of 1,3-oxathiolane nuclesoside enantiomers
US5204466A (en) 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
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
DE69926148D1 (en) 1998-11-09 2005-08-18 Black James Foundation Gastrin und cholecystokinin rezeptor ligande
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
RU2225860C2 (ru) 1998-12-25 2004-03-20 Шионоги & Ко., Лтд. Ароматические гетероциклические соединения, обладающие активностью в отношении вич-интегразы
WO2001095905A1 (fr) 2000-06-14 2001-12-20 Shionogi & Co., Ltd. Inhibiteur d'enzymes possedant deux ions metal divalents en tant que centres actifs
CN101513402B (zh) 2001-08-10 2012-03-21 盐野义制药株式会社 抗病毒药
CN1564685A (zh) 2001-10-03 2005-01-12 Ucb公司 吡咯烷酮衍生物
DK1441735T3 (da) 2001-10-26 2006-06-12 Angeletti P Ist Richerche Bio N-substituerede hydroxypyrimidinon-carboxamid-inhibitorer af HIV-integrase
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
US7517532B2 (en) 2002-09-11 2009-04-14 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors
SI1564210T1 (sl) 2002-11-20 2010-01-29 Japan Tobacco Inc 4-oksokinolinske spojine in njihova uporaba kot inhibitorji HIV integraze
NZ540728A (en) 2003-01-14 2008-08-29 Gilead Sciences Inc Compositions and methods for combination antiviral therapy
EP1628685B1 (en) 2003-04-25 2010-12-08 Gilead Sciences, Inc. Antiviral phosphonate analogs
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
JP2007519735A (ja) 2004-01-30 2007-07-19 メルク エンド カムパニー インコーポレーテッド Hivインテグラーゼ阻害剤として有用であるn−ベンジル−3,4−ジヒドロキシピリジン−2−カルボキサミド及びn−ベンジル−2,3−ジヒドロキシピリジン−4−カルボキサミド化合物
JP2007528396A (ja) 2004-03-09 2007-10-11 メルク エンド カムパニー インコーポレーテッド Hivインテグラーゼ阻害薬
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
US7531554B2 (en) 2004-05-20 2009-05-12 Japan Tobacco Inc. 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
EP2332538A1 (en) 2004-05-21 2011-06-15 Japan Tobacco, Inc. Combinations comprising a 4-isoquinolone derivative and anti-HIV agents
WO2006110157A2 (en) 2004-07-27 2006-10-19 Gilead Sciences, Inc. Nucleoside phosphonate conjugates as anti hiv agents
WO2006030807A1 (ja) 2004-09-15 2006-03-23 Shionogi & Co., Ltd. Hivインテグラーゼ阻害活性を有するカルバモイルピリドン誘導体
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
ATE516026T1 (de) 2005-02-21 2011-07-15 Shionogi & Co Bicyclisches carbamoylpyridonderivat mit hiv- integrase-hemmender wirkung
EP3187225B1 (en) * 2005-04-28 2022-01-05 VIIV Healthcare Company Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity
UA96568C2 (en) * 2005-04-28 2011-11-25 Глаксосмиткляйн Ллк Polycyclic carbamoyl pyridone derivative as hiv-integrase inhibitor
EP1888581A2 (en) 2005-05-16 2008-02-20 Gilead Sciences, Inc. Hiv-integrase inhibitor compounds
WO2007014352A2 (en) 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of hiv
KR20080064182A (ko) 2005-10-27 2008-07-08 시오노기세야쿠 가부시키가이샤 Hiv 인테그라아제 억제활성을 가지는 다환성카르바모일피리돈 유도체
SG170795A1 (en) 2005-12-30 2011-05-30 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
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
BRPI0708685B8 (pt) 2006-03-06 2021-05-25 Japan Tobacco Inc composto de 4-oxoquinolina, seu uso e método para produção dos mesmos
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
CA2661943C (en) 2006-09-12 2015-11-03 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
WO2008048538A1 (en) 2006-10-18 2008-04-24 Merck & Co., Inc. Hiv integrase inhibitors
LT2487163T (lt) 2007-02-23 2016-10-25 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
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
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
NZ585226A (en) 2007-11-16 2012-08-31 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
WO2010011819A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
WO2010011815A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
KR101700267B1 (ko) 2008-07-25 2017-01-26 비이브 헬쓰케어 컴퍼니 화합물
WO2010011816A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
US8217034B2 (en) 2008-07-25 2012-07-10 Shionogi & Co., Ltd. Chemical compounds
WO2010011818A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
PT3617194T (pt) 2008-12-11 2023-11-27 Shionogi & Co Processos e intermediários para inibidores carbamoilpiridona da integrase do vih
CA2744019C (en) 2008-12-11 2017-03-14 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
EP2412708A4 (en) 2009-03-26 2014-07-23 Shionogi & Co 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
PT2444400T (pt) 2009-06-15 2018-06-06 Shionogi & Co Derivado de carbamoilpiridona policíclico substituído
KR101280198B1 (ko) 2009-09-02 2013-06-28 이화여자대학교 산학협력단 피라졸 유도체, 이의 제조방법 및 이를 포함하는 골다공증 예방 및 치료용 조성물
PT3494972T (pt) 2010-01-27 2024-02-12 Viiv Healthcare Co Combinações de dolutegravir e lamivudina para o tratamento de infeção pelo hiv
EP2540720B1 (en) 2010-02-26 2015-04-15 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
WO2011139637A1 (en) 2010-05-03 2011-11-10 Philadelphia Health & Education Corporation Small-molecule modulators of hiv-1 capsid stability and methods thereof
NZ604716A (en) 2010-07-02 2014-12-24 Gilead Sciences Inc 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds
PH12013500011A1 (en) 2010-07-02 2013-02-18 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
WO2012018065A1 (ja) 2010-08-05 2012-02-09 塩野義製薬株式会社 Hivインテグラーゼ阻害活性を有する化合物の製造方法
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
JP5918848B2 (ja) 2011-04-21 2016-05-18 ギリアード サイエンシーズ, インコーポレイテッド ベンゾチアゾール化合物およびその薬学的使用
WO2012151361A1 (en) 2011-05-03 2012-11-08 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
US9540343B2 (en) 2011-07-06 2017-01-10 Gilead Sciences, Inc. Compounds for the treatment of HIV
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
EP2774928B1 (en) 2011-10-12 2017-08-30 Shionogi & Co., Ltd. Polycyclic pyridone derivative having integrase-inhibiting 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
WO2013091096A1 (en) 2011-12-20 2013-06-27 Boehringer Ingelheim International Gmbh Condensed triclyclic compounds as inhibitors of hiv replication
US8987250B2 (en) 2012-04-20 2015-03-24 Gilead Sciences, Inc. Therapeutic compounds
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
EP2877469A4 (en) 2012-07-25 2016-04-06 Merck Sharp & Dohme SUBSTITUTED NAPHTHYRIDEINDION DERIVATIVES AS HIV INTEGRASE INHIBITORS
EA026089B1 (ru) 2012-08-03 2017-02-28 Джилид Сайэнс, Инк. Способ и промежуточные соединения для получения ингибиторов интегразы
US9657009B2 (en) 2012-11-08 2017-05-23 Bristol-Myers Squibb Company Heteroaryl substituted pyridyl compounds useful as kinase modulators
KR20150093819A (ko) 2012-12-14 2015-08-18 글락소스미스클라인 엘엘씨 약제 조성물
WO2014099586A1 (en) 2012-12-17 2014-06-26 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
AU2013361401C1 (en) 2012-12-21 2018-08-09 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
US20160000721A1 (en) 2012-12-21 2016-01-07 Merck Sharp & Dohme Corp. Gastro-retentive formulations
US20140221355A1 (en) 2012-12-21 2014-08-07 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
EP2940019B1 (en) 2012-12-27 2018-03-28 Japan Tobacco Inc. SUBSTITUTED SPIROPYRIDO[1,2-a]PYRAZINE DERIVATIVE AND MEDICINAL USE THEREOF AS HIV INTEGRASE INHIBITOR
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
UA117499C2 (uk) 2013-09-27 2018-08-10 Мерк Шарп Енд Доум Корп. Заміщені похідні хінолізину, які можна використовувати як інгібітори інтегрази віл
WO2015089847A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
EP3096763B1 (en) 2014-01-21 2019-12-25 Laurus Labs Limited Novel 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
NO2717902T3 (show.php) * 2014-06-20 2018-06-23
TWI677489B (zh) 2014-06-20 2019-11-21 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
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
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

Also Published As

Publication number Publication date
RS56950B1 (sr) 2018-05-31
PH12016502499B1 (en) 2019-10-25
ME03037B (me) 2018-10-20
MD4584C1 (ro) 2019-02-28
BR112016029605B1 (pt) 2022-10-11
US20170197985A1 (en) 2017-07-13
ES2660862T3 (es) 2018-03-26
IL249161A0 (en) 2017-01-31
JP2018162246A (ja) 2018-10-18
CN110563747A (zh) 2019-12-13
UA118480C2 (uk) 2019-01-25
ES3010114T3 (en) 2025-04-01
KR101899803B1 (ko) 2018-09-20
ECSP16095566A (es) 2017-01-31
SG11201610211QA (en) 2017-01-27
WO2015196116A1 (en) 2015-12-23
AP2016009591A0 (en) 2016-11-30
AU2018203175B2 (en) 2020-01-02
PH12016502499A1 (en) 2017-03-22
MA40239B1 (fr) 2018-05-31
CU24478B1 (es) 2020-03-04
MX383272B (es) 2025-03-13
CA2950307C (en) 2019-01-08
EP4523758A3 (en) 2025-05-14
MX2016016059A (es) 2017-05-03
HRP20180455T1 (hr) 2018-05-04
EP3321270B1 (en) 2024-12-04
SV2016005339A (es) 2017-03-20
JP2020097593A (ja) 2020-06-25
TW201613937A (en) 2016-04-16
CN106459085B (zh) 2019-07-30
CU20160187A7 (es) 2017-04-05
MA40239A (fr) 2018-01-09
EA030967B1 (ru) 2018-10-31
AR100903A1 (es) 2016-11-09
EA201692414A1 (ru) 2017-06-30
MD4584B1 (ro) 2018-07-31
MA44221A (fr) 2018-12-26
SMT201800053T1 (it) 2018-03-08
ZA201608744B (en) 2023-04-26
HUE036928T2 (hu) 2018-08-28
DOP2016000327A (es) 2017-01-15
JP2022095640A (ja) 2022-06-28
CA2950307A1 (en) 2015-12-23
BR112016029605A8 (pt) 2021-07-20
PL3321270T3 (pl) 2025-03-24
JP6334007B2 (ja) 2018-05-30
EP3157932A1 (en) 2017-04-26
NO2717902T3 (show.php) 2018-06-23
CN106459085A (zh) 2017-02-22
PL3157932T3 (pl) 2018-05-30
AU2015276860B2 (en) 2018-05-31
US10385067B2 (en) 2019-08-20
KR20170016985A (ko) 2017-02-14
TW202014422A (zh) 2020-04-16
US20180065986A1 (en) 2018-03-08
TWI731354B (zh) 2021-06-21
JP2017518356A (ja) 2017-07-06
PT3157932T (pt) 2018-02-21
MX2019013380A (es) 2020-02-20
EA201891464A1 (ru) 2019-03-29
CY1120025T1 (el) 2018-12-12
TWI673274B (zh) 2019-10-01
BR112016029605A2 (pt) 2017-08-22
DK3157932T3 (en) 2018-03-05
AU2018203175A1 (en) 2018-05-24
AU2015276860A1 (en) 2016-12-22
EP3157932B1 (en) 2018-01-10
US20160016973A1 (en) 2016-01-21
MD20180037A2 (ro) 2018-07-31
MX369555B (es) 2019-11-12
MY186696A (en) 2021-08-10
IL249161B (en) 2021-03-25
EP4523758A2 (en) 2025-03-19
PE20170150A1 (es) 2017-04-07
CR20160589A (es) 2017-02-24
EP3321270A1 (en) 2018-05-16
NZ727155A (en) 2022-02-25
CL2016003249A1 (es) 2017-07-14
LT3157932T (lt) 2018-02-26
US9708342B2 (en) 2017-07-18
BR122021025861B1 (pt) 2023-01-24
EP3321270C0 (en) 2024-12-04
UY36177A (es) 2016-01-08
MD20170006A2 (ro) 2017-06-30
SI3157932T1 (en) 2018-06-29

Similar Documents

Publication Publication Date Title
TR201802179T4 (tr) Sodyum (2r,5s,13ar)-7,9-diokso-10-((2,4,6- trifluorobenzil)karbamoil)-2,3,4,5,7,9,13,13a-oktahidro-2,5- metanopirido[1?,2':4,5]pirazino[2,l-b][l,3]oksazepin-8-olat.
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