AR100903A1 - (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

Info

Publication number
AR100903A1
AR100903A1 ARP150101953A ARP150101953A AR100903A1 AR 100903 A1 AR100903 A1 AR 100903A1 AR P150101953 A ARP150101953 A AR P150101953A AR P150101953 A ARP150101953 A AR P150101953A AR 100903 A1 AR100903 A1 AR 100903A1
Authority
AR
Argentina
Prior art keywords
oxazepin
dioxo
trifluorobencil
metanopirido
octahidro
Prior art date
Application number
ARP150101953A
Other languages
English (en)
Inventor
Zia Vahid
Chen Irene
A Carra Ernest
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=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR100903(A1) "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 AR100903A1 publication Critical patent/AR100903A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/537—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente solicitud se relaciona con (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 Forma I. Reivindicación 1: Un compuesto de la fórmula (1).
ARP150101953A 2014-06-20 2015-06-18 (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 AR100903A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
AR100903A1 true AR100903A1 (es) 2016-11-09

Family

ID=53674269

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150101953A AR100903A1 (es) 2014-06-20 2015-06-18 (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

Country Status (44)

Country Link
US (3) US20170197985A1 (es)
EP (2) EP3157932B1 (es)
JP (4) JP6334007B2 (es)
KR (1) KR101899803B1 (es)
CN (2) CN106459085B (es)
AP (1) AP2016009591A0 (es)
AR (1) AR100903A1 (es)
AU (2) AU2015276860B2 (es)
BR (2) BR122021025861B1 (es)
CA (1) CA2950307C (es)
CL (1) CL2016003249A1 (es)
CR (1) CR20160589A (es)
CU (1) CU24478B1 (es)
CY (1) CY1120025T1 (es)
DK (1) DK3157932T3 (es)
DO (1) DOP2016000327A (es)
EA (2) EA030967B1 (es)
EC (1) ECSP16095566A (es)
ES (1) ES2660862T3 (es)
HR (1) HRP20180455T1 (es)
HU (1) HUE036928T2 (es)
IL (1) IL249161B (es)
LT (1) LT3157932T (es)
MA (2) MA40239B1 (es)
MD (2) MD4584C1 (es)
ME (1) ME03037B (es)
MX (2) MX369555B (es)
MY (1) MY186696A (es)
NO (1) NO2717902T3 (es)
NZ (1) NZ727155A (es)
PE (1) PE20170150A1 (es)
PH (1) PH12016502499B1 (es)
PL (1) PL3157932T3 (es)
PT (1) PT3157932T (es)
RS (1) RS56950B1 (es)
SG (1) SG11201610211QA (es)
SI (1) SI3157932T1 (es)
SV (1) SV2016005339A (es)
TR (1) TR201802179T4 (es)
TW (2) TWI731354B (es)
UA (1) UA118480C2 (es)
UY (1) UY36177A (es)
WO (1) WO2015196116A1 (es)
ZA (1) ZA201608744B (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2893843C (en) 2012-12-21 2018-09-04 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
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
NO2717902T3 (es) * 2014-06-20 2018-06-23
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
PT4070788T (pt) * 2015-06-30 2023-06-06 Gilead Sciences Inc Formulações farmacêuticas
CN113546052A (zh) * 2015-11-09 2021-10-26 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
EP3506902A4 (en) * 2016-08-31 2020-04-22 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
CN111699190A (zh) * 2018-02-09 2020-09-22 桑多斯股份公司 比卡格韦钠的晶形
US11466031B2 (en) 2018-04-26 2022-10-11 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
WO2020161744A1 (en) 2019-02-07 2020-08-13 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
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
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
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
CN116437958A (zh) 2020-11-11 2023-07-14 吉利德科学公司 鉴定对采用gp120 CD4结合位点导向的抗体的疗法敏感的HIV患者的方法
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
US11613546B2 (en) 2021-01-19 2023-03-28 Gilead Sciences, Inc. Substituted pyridotriazine compounds and uses thereof
US20240208995A1 (en) * 2021-04-19 2024-06-27 Honour Lab Limited Polymorphic forms of bictegravir potassium
KR20240113832A (ko) 2021-12-03 2024-07-23 길리애드 사이언시즈, 인코포레이티드 Hiv 바이러스 감염 치료용 화합물
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
US20240083984A1 (en) 2022-08-26 2024-03-14 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
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
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
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
AU1403099A (en) 1997-11-14 1999-06-07 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
CZ20012160A3 (cs) 1998-12-25 2001-10-17 Shionogi & Co., Ltd. Heteroaromatické deriváty s inhibiční aktivitou proti HIV integráze
WO2001095905A1 (en) 2000-06-14 2001-12-20 Shionogi & Co., Ltd. Inhibitor for enzyme having two divalent metal ions as active centers
ES2587564T1 (es) 2001-08-10 2016-10-25 Shionogi & Co., Ltd. Agente antiviral
US20050004180A1 (en) 2001-10-03 2005-01-06 ZOU Dong Pyrrolidinone derivatives
PT1441735E (pt) 2001-10-26 2006-06-30 Istituto Di Ricerche Di B Mo P Inibidores de integrase do hiv a base de hidroxipirimidinona carboxamida n-substituida
AU2003248872A1 (en) 2002-07-09 2004-01-23 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
WO2004046115A1 (ja) 2002-11-20 2004-06-03 Japan Tobacco Inc. ４−オキソキノリン化合物及びそのｈｉｖインテグラーゼ阻害剤としての利用
WO2004064846A1 (en) 2003-01-14 2004-08-05 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
MXPA05011297A (es) 2003-04-25 2006-05-25 Gilead Sciences Inc Analogos antivirales de fosfonato.
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
WO2005074513A2 (en) 2004-01-30 2005-08-18 Merck & Co., Inc. 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
EP1755586A2 (en) 2004-04-29 2007-02-28 The Regents of the University of California Hydroxypyridinone, hydroxypyridinethione, pyrone, and thiopyrone metalloprotein inhibitors
JP4824673B2 (ja) 2004-05-07 2011-11-30 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｉｖインテグラーゼ阻害剤
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
EP2332538A1 (en) 2004-05-21 2011-06-15 Japan Tobacco, Inc. Combinations comprising a 4-isoquinolone derivative and anti-HIV agents
UA88313C2 (ru) 2004-07-27 2009-10-12 Гилиад Сайенсиз, Инк. Фосфонатные аналоги соединений ингибиторов вич
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
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
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
DK3187225T3 (da) 2005-04-28 2022-02-28 Viiv Healthcare Co Polycyklisk carbamoylpyridonderivat med hiv-integrasehæmmende aktivitet
US20070072831A1 (en) 2005-05-16 2007-03-29 Gilead Sciences, Inc. Integrase inhibitor compounds
AU2006272521A1 (en) 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of HIV
EA200801144A1 (ru) 2005-10-27 2008-10-30 Сионоги Энд Ко., Лтд. Полициклическое карбамоилпиридоновое производное, обладающее ингибиторной активностью в отношении интегразы вич
KR20160074018A (ko) 2005-12-30 2016-06-27 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
JP2009525261A (ja) 2006-02-01 2009-07-09 日本たばこ産業株式会社 レトロウイルス感染症の治療のための、６−（３−クロロ−２−フルオロベンジル）−１−［（２ｓ）−１−ヒドロキシ−３−メチルブタン−２−イル］−７−メトキシ−４−オキソ−１，４−ジヒドロキノリン−３−カルボン酸またはその塩の使用
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
CA2645119C (en) 2006-03-06 2012-01-24 Japan Tobacco Inc. Method for producing 4-oxoquinoline compound
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.
NZ575542A (en) 2006-09-12 2012-03-30 Gilead Sciences Inc Process and intermediates for preparing 4-oxoquinolone integrase inhibitors
AU2007313293A1 (en) 2006-10-18 2008-04-24 Merck & Co., Inc. HIV integrase inhibitors
SG183059A1 (en) 2007-02-23 2012-08-30 Gilead Sciences Inc Modulators of pharmacokinetic properties of therapeutics
US20080280945A1 (en) 2007-05-09 2008-11-13 Sachin Lohani Crystalline forms of an HIV integrase inhibitor
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
WO2009006199A1 (en) 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
US20090258939A1 (en) 2007-07-31 2009-10-15 Wendye Robbins 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
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
WO2010011818A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
EP2330902B1 (en) 2008-07-25 2012-11-14 GlaxoSmithKline LLC Chemical compounds
WO2010011812A1 (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
KR101772610B1 (ko) 2008-07-25 2017-09-12 비이브 헬쓰케어 컴퍼니 화합물
WO2010068262A1 (en) 2008-12-11 2010-06-17 Glaxosmithkline Llc Processes and intermediates for carbamoylpyridone hiv integrase inhibitors
MX351942B (es) 2008-12-11 2017-11-03 Shionogi & Co Sintesis de inhibidores de integrasa de vih de carbamoil-piridona e intermediarios.
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
TR201808501T4 (tr) 2009-06-15 2018-07-23 Shionogi & Co Sübstitüe polisiklik karbamoilpiridon türevi.
KR101280198B1 (ko) 2009-09-02 2013-06-28 이화여자대학교 산학협력단 피라졸 유도체, 이의 제조방법 및 이를 포함하는 골다공증 예방 및 치료용 조성물
US20120295898A1 (en) 2010-01-27 2012-11-22 Mark Richard Underwood Antiviral Therapy
RU2012140961A (ru) 2010-02-26 2014-04-10 Джапан Тобакко Инк. ПРОИЗВОДНОЕ 1,3,4,8-ТЕТРАГИДРО-2Н-ПИРИДО[1,2-a]ПИРАЗИНА И ЕГО ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНИБИТОРА ИНТЕГРАЗЫ ВИЧ
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
NZ604598A (en) 2010-07-02 2014-12-24 Gilead Sciences Inc Naphth-2-ylacetic acid derivatives to treat aids
TWI458711B (zh) 2010-07-02 2014-11-01 Gilead Sciences Inc 治療性化合物
US20130210809A1 (en) 2010-07-14 2013-08-15 Christelle Boléa Novel 2-amino-4-pyrazolyl-thiazole derivatives and their use as allosteric modulators of metabotropic glutamate receptors
CN106046022B (zh) 2010-08-05 2018-06-19 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
WO2012039414A1 (ja) 2010-09-24 2012-03-29 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のプロドラッグ
WO2012106534A2 (en) 2011-02-02 2012-08-09 The Regents Of The University Of California Hiv integrase inhibitors
WO2012145728A1 (en) 2011-04-21 2012-10-26 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
AU2012278976B2 (en) 2011-07-06 2017-05-11 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
EP2742051B1 (en) * 2011-09-14 2016-10-12 Mapi Pharma Limited Amorpous form of the dolutegravir sodium salt
WO2013054862A1 (ja) 2011-10-12 2013-04-18 塩野義製薬株式会社 インテグラーゼ阻害活性を有する多環性ピリドン誘導体
EP2804864B1 (en) 2011-12-12 2017-09-06 Bayer Intellectual Property GmbH Amino-substituted imidazopyridazines
EP2794613B1 (en) 2011-12-20 2017-03-29 Boehringer Ingelheim International GmbH Condensed triclyclic compounds as inhibitors of hiv replication
TWI480271B (zh) 2012-04-20 2015-04-11 Gilead Sciences Inc 醫療性化合物
WO2014008636A1 (en) 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Macrocyclic compounds as hiv integrase inhibitors
US20150166520A1 (en) 2012-07-20 2015-06-18 Merck Sharp & Dohme Corp. Amido-substituted pyrimidinone derivatives useful for the treatment of hiv infection
EP2877469A4 (en) 2012-07-25 2016-04-06 Merck Sharp & Dohme SUBSTITUTED NAPHTHYRIDINEDIONE DERIVATIVES AS INHIBITORS OF HIV INTEGRASE
EA026089B1 (ru) 2012-08-03 2017-02-28 Джилид Сайэнс, Инк. Способ и промежуточные соединения для получения ингибиторов интегразы
BR112015009850A2 (pt) 2012-11-08 2017-07-11 Bristol Myers Squibb Co compostos de piridila substituídos por heteroarila úteis como moduladores de quinase
EA201590862A1 (ru) 2012-12-14 2016-05-31 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Фармацевтические композиции
WO2014099586A1 (en) 2012-12-17 2014-06-26 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
US20140221355A1 (en) 2012-12-21 2014-08-07 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
CA2893843C (en) 2012-12-21 2018-09-04 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
EP2934482A4 (en) 2012-12-21 2016-07-20 Merck Sharp & Dohme ADMINISTRATIVE FORMULATIONS
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
US9951079B2 (en) 2013-06-13 2018-04-24 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
US9861620B2 (en) 2013-09-27 2018-01-09 Merck Sharp & Dohme Corp. 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
IN2014CH00247A (es) 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
NO2717902T3 (es) * 2014-06-20 2018-06-23
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
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
CN113546052A (zh) 2015-11-09 2021-10-26 吉利德科学公司 治疗人免疫缺陷病毒的治疗组合物

Also Published As

Publication number Publication date
CL2016003249A1 (es) 2017-07-14
US20170197985A1 (en) 2017-07-13
UA118480C2 (uk) 2019-01-25
ECSP16095566A (es) 2017-01-31
AU2015276860B2 (en) 2018-05-31
MX2016016059A (es) 2017-05-03
BR112016029605A8 (pt) 2021-07-20
CA2950307C (en) 2019-01-08
EP3321270A1 (en) 2018-05-16
MX2019013380A (es) 2020-02-20
SV2016005339A (es) 2017-03-20
US10385067B2 (en) 2019-08-20
DOP2016000327A (es) 2017-01-15
JP2022095640A (ja) 2022-06-28
MA44221A (fr) 2018-12-26
IL249161B (en) 2021-03-25
MY186696A (en) 2021-08-10
TW201613937A (en) 2016-04-16
EA201891464A1 (ru) 2019-03-29
EP3157932A1 (en) 2017-04-26
JP2017518356A (ja) 2017-07-06
PE20170150A1 (es) 2017-04-07
BR122021025861B1 (pt) 2023-01-24
MD4584B1 (ro) 2018-07-31
CR20160589A (es) 2017-02-24
US20160016973A1 (en) 2016-01-21
ZA201608744B (en) 2023-04-26
JP2018162246A (ja) 2018-10-18
MA40239B1 (fr) 2018-05-31
CN106459085A (zh) 2017-02-22
EP3157932B1 (en) 2018-01-10
HRP20180455T1 (hr) 2018-05-04
CN106459085B (zh) 2019-07-30
CY1120025T1 (el) 2018-12-12
PL3157932T3 (pl) 2018-05-30
NO2717902T3 (es) 2018-06-23
UY36177A (es) 2016-01-08
CU20160187A7 (es) 2017-04-05
TR201802179T4 (tr) 2018-03-21
AP2016009591A0 (en) 2016-11-30
AU2018203175A1 (en) 2018-05-24
JP2020097593A (ja) 2020-06-25
LT3157932T (lt) 2018-02-26
CN110563747A (zh) 2019-12-13
ME03037B (me) 2018-10-20
TWI673274B (zh) 2019-10-01
PH12016502499A1 (en) 2017-03-22
AU2015276860A1 (en) 2016-12-22
TWI731354B (zh) 2021-06-21
EA030967B1 (ru) 2018-10-31
SG11201610211QA (en) 2017-01-27
MD20170006A2 (ro) 2017-06-30
SI3157932T1 (en) 2018-06-29
MD20180037A2 (ro) 2018-07-31
CU24478B1 (es) 2020-03-04
US9708342B2 (en) 2017-07-18
MD4584C1 (ro) 2019-02-28
PH12016502499B1 (en) 2017-03-22
KR20170016985A (ko) 2017-02-14
TW202014422A (zh) 2020-04-16
AU2018203175B2 (en) 2020-01-02
PT3157932T (pt) 2018-02-21
BR112016029605A2 (pt) 2017-08-22
RS56950B1 (sr) 2018-05-31
CA2950307A1 (en) 2015-12-23
MA40239A (fr) 2018-01-09
HUE036928T2 (hu) 2018-08-28
IL249161A0 (en) 2017-01-31
EA201692414A1 (ru) 2017-06-30
MX369555B (es) 2019-11-12
ES2660862T3 (es) 2018-03-26
JP6334007B2 (ja) 2018-05-30
WO2015196116A1 (en) 2015-12-23
KR101899803B1 (ko) 2018-09-20
BR112016029605B1 (pt) 2022-10-11
NZ727155A (en) 2022-02-25
US20180065986A1 (en) 2018-03-08
DK3157932T3 (en) 2018-03-05

Similar Documents

Publication Publication Date Title
AR100903A1 (es) (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
EA201692219A1 (ru) Способы получения противовирусных соединений
UY34844A (es) Formas sólidas de un compuesto antiviral
CR20160450A (es) Anticuerpos multiespecificos
UY34591A (es) Compuestos de imidazopirrolidinona
PL3564244T3 (pl) Krystaliczne postacie (2r,5s,13ar)-8-hydroksy-7,9-diokso-n-(2,4,6-trifluorobenzylo)-2,3,4,5,7,9,13,13a-oktahydro-2,5-metanopirydo[1’,2’:4,5]pirazyno[2,1-b][1,3]oksazepino-10-karboksyamidu
UY34778A (es) ?COMPUESTOS DE HEXAHIDROPIRANO[3,4-d][1,3]TIAZIN-2-AMINA HETEROCÍCLICOS SUSTITUÍDOS?.
UY34302A (es) COMPUESTOS DE HEXAHIDROPIRANO[3,4-d][1,3]TIAZIN-2- AMINA
UY36737A (es) 3-amino-1,5,6,7-tetrahidro-4h-indol-4-onas
EA201790939A1 (ru) ТРИАЗОЛО[4,5-d]ПИРИМИДИНЫ В КАЧЕСТВЕ АГОНИСТОВ КАННАБИНОИДНЫХ РЕЦЕПТОРОВ ТИПА 2
CL2015002358A1 (es) Compuestos bicíclicos.
UY36284A (es) Método para la preparación de imidazopiridazinas sustituidas
UA96860U (xx) Похідні [1,2,4]триазоло[4,3-а]піразину
UA86107U (ru) Пиперазиния 1-н-бутилтеобромин-8-илтиоацетат, который проявляет диуретическое действие
CL2012000503A1 (es) Compuestos agroquimicos derivados de pteridinas.
WO2014113427A3 (en) Irciniastatin analogues

Legal Events

Date Code Title Description
FG Grant, registration