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

    • 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
    • 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
    • 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)
  • 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)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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) US9708342B2 (enExample)
EP (3) EP4523758A3 (enExample)
JP (4) JP6334007B2 (enExample)
KR (1) KR101899803B1 (enExample)
CN (2) CN110563747A (enExample)
AP (1) AP2016009591A0 (enExample)
AR (1) AR100903A1 (enExample)
AU (2) AU2015276860B2 (enExample)
BR (2) BR122021025861B1 (enExample)
CA (1) CA2950307C (enExample)
CL (1) CL2016003249A1 (enExample)
CR (1) CR20160589A (enExample)
CU (1) CU24478B1 (enExample)
CY (1) CY1120025T1 (enExample)
DK (1) DK3157932T3 (enExample)
DO (1) DOP2016000327A (enExample)
EA (2) EA030967B1 (enExample)
EC (1) ECSP16095566A (enExample)
ES (2) ES3010114T3 (enExample)
HR (1) HRP20180455T1 (enExample)
HU (1) HUE036928T2 (enExample)
IL (1) IL249161B (enExample)
LT (1) LT3157932T (enExample)
MA (2) MA40239B1 (enExample)
MD (2) MD4584C1 (enExample)
ME (1) ME03037B (enExample)
MX (2) MX383272B (enExample)
MY (1) MY186696A (enExample)
NO (1) NO2717902T3 (enExample)
NZ (1) NZ727155A (enExample)
PE (1) PE20170150A1 (enExample)
PH (1) PH12016502499B1 (enExample)
PL (2) PL3321270T3 (enExample)
PT (1) PT3157932T (enExample)
RS (1) RS56950B1 (enExample)
SG (1) SG11201610211QA (enExample)
SI (1) SI3157932T1 (enExample)
SM (1) SMT201800053T1 (enExample)
SV (1) SV2016005339A (enExample)
TR (1) TR201802179T4 (enExample)
TW (2) TWI673274B (enExample)
UA (1) UA118480C2 (enExample)
UY (1) UY36177A (enExample)
WO (1) WO2015196116A1 (enExample)
ZA (1) ZA201608744B (enExample)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA030003B1 (ru) 2012-12-21 2018-06-29 Джилид Сайэнс, Инк. Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции
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
NO2717902T3 (enExample) * 2014-06-20 2018-06-23
EP4233846B1 (en) * 2015-06-30 2024-12-04 Gilead Sciences, Inc. Pharmaceutical formulations
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
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
ES2916405T3 (es) 2018-02-09 2022-06-30 Sandoz Ag Forma cristalina de bictegravir sódico
WO2019207602A1 (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
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
KR20240151256A (ko) 2019-03-22 2024-10-17 길리애드 사이언시즈, 인코포레이티드 가교된 트리시클릭 카르바모일피리돈 화합물 및 그의 제약 용도
US12486286B2 (en) 2019-06-18 2025-12-02 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
EP4110783A1 (en) 2020-02-24 2023-01-04 Gilead Sciences, Inc. Tetracyclic compounds for treating hiv infection
KR102987126B1 (ko) 2020-03-20 2026-07-07 길리애드 사이언시즈, 인코포레이티드 4'-c-치환된-2-할로-2'-데옥시아데노신 뉴클레오시드의 프로드러그 및 이의 제조 및 사용 방법
EP4153181B1 (en) 2020-05-21 2026-07-29 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
CN116390924B (zh) 2020-09-30 2025-11-07 吉利德科学公司 桥连三环氨基甲酰基吡啶酮化合物及其用途
TWI815194B (zh) 2020-10-22 2023-09-11 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
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
CR20260070A (es) 2021-01-19 2026-04-24 Gilead Sciences Inc COMPUESTOS DE PIRIDOTRIAZINA SUSTITUIDOS Y USOS DE ESTOS (Divisional 2023-0315)
WO2022224120A1 (en) * 2021-04-19 2022-10-27 Honour Lab Limited Polymorphic forms of bictegravir potassium
AU2022403012B2 (en) 2021-12-03 2026-02-12 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
TWI856796B (zh) 2022-04-06 2024-09-21 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
US20240034724A1 (en) 2022-07-01 2024-02-01 Gilead Sciences, Inc. Therapeutic compounds useful for the prophylactic or therapeutic treatment of an hiv virus infection
CN119768183A (zh) 2022-08-26 2025-04-04 吉利德科学公司 用于广泛中和抗体的给药和安排方案
WO2024076915A1 (en) 2022-10-04 2024-04-11 Gilead Sciences, Inc. 4'-thionucleoside analogues and their pharmaceutical use
EP4698174A1 (en) 2023-04-19 2026-02-25 Gilead Sciences, Inc. Dosing regimen of capsid inhibitor
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
WO2024249573A1 (en) 2023-05-31 2024-12-05 Gilead Sciences, Inc. Solid forms of compounds useful in the treatment of hiv
CN122295099A (zh) 2023-07-28 2026-06-26 吉利德科学公司 用于治疗和预防hiv的来那卡帕韦的每周方案
AU2023462614A1 (en) 2023-08-23 2026-03-19 Gilead Sciences, Inc. Dosing regimen of hiv capsid inhibitor
IL327206A (en) 2023-10-11 2026-05-01 Gilead Sciences Inc Bridged tricyclic carbamoylpyridone compounds and their uses
KR20260093341A (ko) 2023-10-11 2026-06-19 길리애드 사이언시즈, 인코포레이티드 가교 트리시클릭 카르바모일피리돈 화합물 및 이의 용도
AU2024360779A1 (en) 2023-10-11 2026-04-16 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
WO2025184447A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
US20250333424A1 (en) 2024-03-01 2025-10-30 Gilead Sciences, Inc. Antiviral compounds
WO2025184452A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
WO2025260028A1 (en) 2024-06-14 2025-12-18 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
WO2026076265A1 (en) 2024-10-03 2026-04-09 Gilead Sciences, Inc. Combination therapy comprising bridged tricyclic carbamoylpyridone compounds and p-glycoprotein 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
DE3900736A1 (de) 1989-01-12 1990-07-26 Hoechst Ag Positiv arbeitendes strahlungsempfindliches gemisch enthaltend einen mehrfunktionellen (alpha)-diazo-(beta)-ketoester, verfahren zu dessen herstellung und strahlungsempfindliches aufzeichnungsmaterial enthaltend dieses gemisch
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
US6642245B1 (en) 1990-02-01 2003-11-04 Emory University Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
DE4014649A1 (de) 1990-05-08 1991-11-14 Hoechst Ag Neue mehrfunktionelle verbindungen mit (alpha)-diazo-ss-ketoester- und sulfonsaeureester-einheiten, verfahren zu ihrer herstellung und deren verwendung
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
US5922695A (en) 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
SE9702772D0 (sv) 1997-07-22 1997-07-22 Astra Pharma Prod Novel compounds
US5935946A (en) 1997-07-25 1999-08-10 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
WO1999025345A1 (en) 1997-11-14 1999-05-27 Merck & Co., Inc. Alpha-1a adrenergic receptor antagonists
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
BR9916583A (pt) 1998-12-25 2001-09-25 Shionogi & Co Derivados heteroaromáticos tendo uma atividade inibitória contra integrase de hiv
EP1297834A4 (en) 2000-06-14 2007-05-09 Shionogi & Co ENZYME INHIBITOR HAVING TWO DIVALENT METAL IONS AS ACTIVE CENTERS
ATE530520T1 (de) 2001-08-10 2011-11-15 Shionogi & Co Antivirales mittel
NZ532018A (en) 2001-10-03 2004-12-24 Ucb S Pyrrolidinone derivatives
DE122009000048I1 (de) 2001-10-26 2010-04-08 Angeletti P Ist Richerche Bio N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase
WO2004004657A2 (en) 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Hiv integrase inhibitors
WO2004024078A2 (en) 2002-09-11 2004-03-25 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
US7176220B2 (en) 2002-11-20 2007-02-13 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as pharmaceutical agent
PT1583542E (pt) 2003-01-14 2008-09-17 Gilead Sciences Inc Composições e métodos para terapia de combinação antiviral
SG182849A1 (en) 2003-04-25 2012-08-30 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
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
EP1725535A4 (en) 2004-03-09 2009-11-25 Merck & Co Inc HIV integrase
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
WO2005110399A2 (en) 2004-04-29 2005-11-24 The Regents Of The University Of California Zinc-binding groups for metalloprotein inhibitors
ES2529038T3 (es) 2004-05-07 2015-02-16 Merck Sharp & Dohme Corp. Inhibidores de la integrasa de VIH
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
US8633219B2 (en) 2004-05-21 2014-01-21 Japan Tobacco Inc. Combination therapy
PT2258376T (pt) 2004-07-27 2019-05-31 Gilead Sciences Inc Análogos fosfonatados de compostos inibidores do vih
JP4953297B2 (ja) 2004-09-15 2012-06-13 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
WO2006088173A1 (ja) 2005-02-21 2006-08-24 Shionogi & Co., Ltd. Hivインテグラーゼ阻害活性を有する2環性カルバモイルピリドン誘導体
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
TW200800988A (en) 2005-10-27 2008-01-01 Shionogi & Amp Co Ltd Polycyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
US20070219243A1 (en) 2005-12-30 2007-09-20 Kearney Brian P Method 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
EP1978960A4 (en) 2006-02-01 2009-12-02 Japan Tobacco Inc USE OF 6- (3-CHLORO-2-FLUORBENZYL) -1 - [(2S) -1-HYDROXY-3-METHYLBUTAN-2-YL [-7-METHOXY-4-OXO-1,4-DIHYDROCHINOLINE-3- CARBOXYLIC ACID OR SALT THEREOF FOR THE TREATMENT OF 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
JP4669040B2 (ja) 2006-03-06 2011-04-13 日本たばこ産業株式会社 4−オキソキノリン化合物の製造方法
US7893055B2 (en) 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
CA2657034A1 (en) 2006-07-19 2008-01-24 University Of Georgia Research Foundation, Inc. Pyridinone diketo acids: inhibitors of hiv replication in combination therapy
ES2536923T3 (es) 2006-09-12 2015-05-29 Gilead Sciences, Inc. Proceso e intermedios para preparar inhibidores de la integrasa del VIH
CA2665538A1 (en) 2006-10-18 2008-04-24 Merck & Co., Inc. Hiv integrase inhibitors
PT3150586T (pt) 2007-02-23 2020-03-31 Gilead Sciences Inc Moduladores de propriedades farmacocinéticas de agentes terapêuticos
US20080280945A1 (en) 2007-05-09 2008-11-13 Sachin Lohani Crystalline forms of an HIV integrase inhibitor
SG182229A1 (en) 2007-06-29 2012-07-30 Gilead Sciences Inc Therapeutic compositions and the use thereof
WO2009006203A1 (en) 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
EP2182801A4 (en) 2007-07-31 2011-04-13 Limerick Biopharma Inc PYRONANALOGUE COMPOSITIONS AND CORRESPONDING METHODS
AR068403A1 (es) 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa
US8354429B2 (en) 2007-11-16 2013-01-15 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
WO2010011813A1 (en) 2008-07-23 2010-01-28 Alkermes, Inc. Complex of trospium and pharmaceutical compositions thereof
EP2660239B1 (en) 2008-07-25 2016-11-23 VIIV Healthcare Company Chemical compounds as synthetic intermediates
WO2010011819A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
ES2395705T3 (es) 2008-07-25 2013-02-14 Glaxosmithkline Llc Compuestos químicos
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
WO2010011818A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
EP3617194B1 (en) 2008-12-11 2023-11-08 VIIV Healthcare Company Processes and intermediates for carbamoylpyridone hiv integrase inhibitors
SG171308A1 (en) 2008-12-11 2011-07-28 Shionogi & Co Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
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
US8835461B2 (en) 2009-03-26 2014-09-16 Shionogi & Co., Ltd. Substituted 3-hydroxy-4-pyridone derivative
US8338441B2 (en) 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
JP5737691B2 (ja) 2009-06-15 2015-06-17 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
US8637674B2 (en) 2009-09-02 2014-01-28 Ewha University-Industry Collaboration Foundation Pyrazole derivatives, preparation method thereof, and composition for prevention and treatment of osteoporosis containing same
EP3351249A1 (en) 2010-01-27 2018-07-25 VIIV Healthcare Company Antiviral therapy
CN102858771A (zh) 2010-02-26 2013-01-02 日本烟草产业株式会社 1,3,4,8-四氢-2H-吡啶并[1,2-a]吡嗪衍生物及其作为HIV整合酶抑制剂的用途
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
CN103140474A (zh) 2010-07-02 2013-06-05 吉里德科学公司 治疗aids的萘-2-基乙酸衍生物
EP2588455B1 (en) 2010-07-02 2018-04-04 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
SMT202100268T1 (it) 2010-08-05 2021-07-12 Shionogi & Co Metodo per produrre composti aventi attività di inibizione di integrasi di hiv.
LT2620436T (lt) 2010-09-24 2018-08-10 Shionogi & Co., Ltd. Pakeistojo policiklinio karbamoilpiridono darinio provaistas
WO2012106534A2 (en) 2011-02-02 2012-08-09 The Regents Of The University Of California Hiv integrase inhibitors
MX2013012266A (es) 2011-04-21 2013-11-22 Gilead Sciences Inc Compuestos de benzotiazol y su uso farmaceutico.
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
CA2840095A1 (en) 2011-07-06 2013-01-10 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
PL2742051T3 (pl) 2011-09-14 2017-06-30 Mapi Pharma Limited Amorficzna postać soli sodowej dolutegrawiru
AU2012321762A1 (en) 2011-10-12 2014-04-17 Shionogi & Co., Ltd. Polycyclic pyridone derivative having integrase-inhibiting activity
US9643974B2 (en) 2011-12-12 2017-05-09 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines
JP6144698B2 (ja) 2011-12-20 2017-06-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Hiv複製の阻害剤としての縮合三環式化合物
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
US20150166520A1 (en) 2012-07-20 2015-06-18 Merck Sharp & Dohme Corp. Amido-substituted pyrimidinone derivatives useful for the treatment of hiv infection
US20150218164A1 (en) 2012-07-25 2015-08-06 Merck Sharp & Dohme Corp. Substituted naphthyridinedione derivatives as hiv integrase inhibitors
EP2880017B1 (en) 2012-08-03 2016-10-05 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
AU2013341200A1 (en) 2012-11-08 2015-07-02 Bristol-Myers Squibb Company Heteroaryl substituted pyridyl compounds useful as kinase modulators
CN104902905A (zh) 2012-12-14 2015-09-09 葛兰素史克有限责任公司 药物组合物
EP2931730B1 (en) 2012-12-17 2019-08-07 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
US20140221355A1 (en) 2012-12-21 2014-08-07 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
EA030003B1 (ru) 2012-12-21 2018-06-29 Джилид Сайэнс, Инк. Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции
HK1214817A1 (en) 2012-12-27 2016-08-05 Japan Tobacco Inc. Substituted spiropyrido[1,2-a]pyrazine derivative and medicinal use thereof as hiv integrase inhibitor
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
CA2924829C (en) 2013-09-27 2019-10-29 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
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
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
NO2717902T3 (enExample) * 2014-06-20 2018-06-23
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
AU2018203175B2 (en) 2020-01-02
MY186696A (en) 2021-08-10
IL249161B (en) 2021-03-25
MD20170006A2 (ro) 2017-06-30
SI3157932T1 (en) 2018-06-29
SMT201800053T1 (it) 2018-03-08
JP2017518356A (ja) 2017-07-06
US10385067B2 (en) 2019-08-20
CU20160187A7 (es) 2017-04-05
CN106459085B (zh) 2019-07-30
AP2016009591A0 (en) 2016-11-30
CL2016003249A1 (es) 2017-07-14
EP4523758A2 (en) 2025-03-19
ZA201608744B (en) 2023-04-26
PE20170150A1 (es) 2017-04-07
EP3321270B1 (en) 2024-12-04
BR112016029605B1 (pt) 2022-10-11
EP3157932B1 (en) 2018-01-10
US9708342B2 (en) 2017-07-18
AU2015276860B2 (en) 2018-05-31
HUE036928T2 (hu) 2018-08-28
CA2950307A1 (en) 2015-12-23
PH12016502499B1 (en) 2019-10-25
MX383272B (es) 2025-03-13
CY1120025T1 (el) 2018-12-12
SV2016005339A (es) 2017-03-20
CR20160589A (es) 2017-02-24
CU24478B1 (es) 2020-03-04
PH12016502499A1 (en) 2017-03-22
CN110563747A (zh) 2019-12-13
EA201891464A1 (ru) 2019-03-29
EP3321270C0 (en) 2024-12-04
AU2018203175A1 (en) 2018-05-24
ECSP16095566A (es) 2017-01-31
MA40239A (fr) 2018-01-09
MX369555B (es) 2019-11-12
DOP2016000327A (es) 2017-01-15
JP6334007B2 (ja) 2018-05-30
EP3157932A1 (en) 2017-04-26
ME03037B (me) 2018-10-20
LT3157932T (lt) 2018-02-26
UA118480C2 (uk) 2019-01-25
EP3321270A1 (en) 2018-05-16
MX2016016059A (es) 2017-05-03
PL3157932T3 (pl) 2018-05-30
EA201692414A1 (ru) 2017-06-30
KR20170016985A (ko) 2017-02-14
NZ727155A (en) 2022-02-25
PL3321270T3 (pl) 2025-03-24
MD4584B1 (ro) 2018-07-31
WO2015196116A1 (en) 2015-12-23
EP4523758A3 (en) 2025-05-14
DK3157932T3 (en) 2018-03-05
US20180065986A1 (en) 2018-03-08
RS56950B1 (sr) 2018-05-31
TWI731354B (zh) 2021-06-21
ES2660862T3 (es) 2018-03-26
UY36177A (es) 2016-01-08
BR122021025861B1 (pt) 2023-01-24
CN106459085A (zh) 2017-02-22
US20170197985A1 (en) 2017-07-13
JP2022095640A (ja) 2022-06-28
BR112016029605A2 (pt) 2017-08-22
MA44221A (fr) 2018-12-26
MD4584C1 (ro) 2019-02-28
HRP20180455T1 (hr) 2018-05-04
TW202014422A (zh) 2020-04-16
NO2717902T3 (enExample) 2018-06-23
PT3157932T (pt) 2018-02-21
MX2019013380A (es) 2020-02-20
BR112016029605A8 (pt) 2021-07-20
MA40239B1 (fr) 2018-05-31
JP2018162246A (ja) 2018-10-18
IL249161A0 (en) 2017-01-31
SG11201610211QA (en) 2017-01-27
AU2015276860A1 (en) 2016-12-22
ES3010114T3 (en) 2025-04-01
JP2020097593A (ja) 2020-06-25
CA2950307C (en) 2019-01-08
TWI673274B (zh) 2019-10-01
MD20180037A2 (ro) 2018-07-31
KR101899803B1 (ko) 2018-09-20
US20160016973A1 (en) 2016-01-21
AR100903A1 (es) 2016-11-09
EA030967B1 (ru) 2018-10-31
TW201613937A (en) 2016-04-16

Similar Documents

Publication Publication Date Title
UA118480C2 (uk) (2R,5S,13aR)-7,9-ДІОКСО-10-((2,4,6-ТРИФТОРБЕНЗИЛ)КАРБАМОЇЛ)-2,3,4,5,7,9,13,13a-ОКТАГІДРО-2,5-МЕТАНОПІРИДО[1',2':4,5]ПІРАЗИНО[2,1-b][1,3]ОКСАЗЕПІН-8-ОЛАТ НАТРІЮ
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
CL2016001973A1 (es) Derivados de nucleosido sustituidos con 4' -difluorometilo como inhibidores de la replicación de arn de la influenza.
HK1235402A1 (en) 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