TWI673274B - （２Ｒ，５Ｓ，１３ａＲ）－７，９－二側氧基－１０－（（２，４，６－三氟苄基）胺甲醯基）－２，３，４，５，７，９，１３，１３ａ－八氫－２，５－甲橋吡啶並［１’，２’：４，５］吡並［２，１－ｂ］［１，３］氧氮呯－８－醇化鈉 - Google Patents

（２Ｒ，５Ｓ，１３ａＲ）－７，９－二側氧基－１０－（（２，４，６－三氟苄基）胺甲醯基）－２，３，４，５，７，９，１３，１３ａ－八氫－２，５－甲橋吡啶並［１’，２’：４，５］吡並［２，１－ｂ］［１，３］氧氮呯－８－醇化鈉 Download PDF

Info

Publication number
TWI673274B
TWI673274B TW104119604A TW104119604A TWI673274B TW I673274 B TWI673274 B TW I673274B TW 104119604 A TW104119604 A TW 104119604A TW 104119604 A TW104119604 A TW 104119604A TW I673274 B TWI673274 B TW I673274B
Authority
TW
Taiwan
Prior art keywords
hiv
compound
pharmaceutical composition
patent application
octahydro
Prior art date
Application number
TW104119604A
Other languages
English (en)
Chinese (zh)
Other versions
TW201613937A (en
Inventor
恩尼斯特 卡拉
艾琳 陳
凡德 尼爾
Original Assignee
美商基利科學股份有限公司
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=TWI673274(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 美商基利科學股份有限公司 filed Critical 美商基利科學股份有限公司
Publication of TW201613937A publication Critical patent/TW201613937A/zh
Application granted granted Critical
Publication of TWI673274B publication Critical patent/TWI673274B/zh

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)
  • 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)
TW104119604A 2014-06-20 2015-06-17 （２Ｒ，５Ｓ，１３ａＲ）－７，９－二側氧基－１０－（（２，４，６－三氟苄基）胺甲醯基）－２，３，４，５，７，９，１３，１３ａ－八氫－２，５－甲橋吡啶並［１’，２’：４，５］吡並［２，１－ｂ］［１，３］氧氮呯－８－醇化鈉 TWI673274B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462015245P 2014-06-20 2014-06-20
US62/015,245 2014-06-20

Publications (2)

Publication Number Publication Date
TW201613937A TW201613937A (en) 2016-04-16
TWI673274B true TWI673274B (zh) 2019-10-01

Family

ID=53674269

Family Applications (2)

Application Number Title Priority Date Filing Date
TW104119604A TWI673274B (zh) 2014-06-20 2015-06-17 （２Ｒ，５Ｓ，１３ａＲ）－７，９－二側氧基－１０－（（２，４，６－三氟苄基）胺甲醯基）－２，３，４，５，７，９，１３，１３ａ－八氫－２，５－甲橋吡啶並［１’，２’：４，５］吡並［２，１－ｂ］［１，３］氧氮呯－８－醇化鈉
TW108122266A TWI731354B (zh) 2014-06-20 2015-06-17 （２Ｒ，５Ｓ，１３ａＲ）－７，９－二側氧基－１０－（（２，４，６－三氟苄基）胺甲醯基）－２，３，４，５，７，９，１３，１３ａ－八氫－２，５－甲橋吡啶並［１’，２’：４，５］吡𠯤並［２，１－ｂ］［１，３］氧氮呯－８－醇化鈉

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW108122266A TWI731354B (zh) 2014-06-20 2015-06-17 （２Ｒ，５Ｓ，１３ａＲ）－７，９－二側氧基－１０－（（２，４，６－三氟苄基）胺甲醯基）－２，３，４，５，７，９，１３，１３ａ－八氫－２，５－甲橋吡啶並［１’，２’：４，５］吡𠯤並［２，１－ｂ］［１，３］氧氮呯－８－醇化鈉

Country Status (45)

Country Link
US (3) US9708342B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (3) EP3157932B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (4) JP6334007B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (1) KR101899803B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (2) CN106459085B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AP (1) AP2016009591A0 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AR (1) AR100903A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (2) AU2015276860B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (2) BR112016029605B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2950307C (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CL (1) CL2016003249A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CR (1) CR20160589A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CU (1) CU24478B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CY (1) CY1120025T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DK (1) DK3157932T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
DO (1) DOP2016000327A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EA (2) EA030967B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EC (1) ECSP16095566A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ES (2) ES2660862T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HR (1) HRP20180455T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HU (1) HUE036928T2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (1) IL249161B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
LT (1) LT3157932T (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MA (2) MA40239B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MD (2) MD20180037A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ME (1) ME03037B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (2) MX383272B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MY (1) MY186696A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NO (1) NO2717902T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
NZ (1) NZ727155A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PE (1) PE20170150A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PH (1) PH12016502499B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PL (2) PL3157932T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
PT (1) PT3157932T (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
RS (1) RS56950B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SG (1) SG11201610211QA (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SI (1) SI3157932T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SM (1) SMT201800053T1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SV (1) SV2016005339A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
TR (1) TR201802179T4 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
TW (2) TWI673274B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
UA (1) UA118480C2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
UY (1) UY36177A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2015196116A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ZA (1) ZA201608744B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3131094A1 (en) 2012-12-21 2014-06-26 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
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 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) * 2014-06-20 2018-06-23
PT4070787T (pt) * 2015-06-30 2023-05-22 Gilead Sciences Inc Formulações farmacêuticas
EA201890654A1 (ru) * 2015-11-09 2018-10-31 Джилид Сайэнс, Инк. Терапевтические композиции для лечения вируса иммунодефицита человека
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
JP2019528304A (ja) * 2016-08-31 2019-10-10 ヴィーブ ヘルスケア カンパニー 組み合わせ並びにその使用及び治療
EP3518935A1 (en) * 2016-09-27 2019-08-07 Gilead Sciences, Inc. Therapeutic compositions for treatment of human immunodeficiency virus
CN107445994A (zh) * 2017-05-31 2017-12-08 北京阜康仁生物制药科技有限公司 替诺福韦艾拉酚胺半富马酸盐新晶型
SI3749673T1 (sl) * 2018-02-09 2022-07-29 Sandoz Ag Kristalinična oblika biktegravir natrija
US11466031B2 (en) 2018-04-26 2022-10-11 Mylan Laboratories Limited 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
JP7313438B2 (ja) * 2018-09-19 2023-07-24 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖの予防のためのインテグラーゼ阻害剤
EP3653629A1 (en) 2018-11-16 2020-05-20 Sandoz AG Acid addition salts of an integrase strand transfer inhibitor
US12195480B2 (en) 2019-02-07 2025-01-14 Cipla Limited Polymorphs of integrase inhibitor
MX2021011394A (es) 2019-03-22 2021-10-13 Gilead Sciences Inc Compuestos de carbamoilpiridona triciclica puenteada y su uso farmaceutico.
EP3993797A4 (en) * 2019-06-18 2023-10-25 Laurus Labs Limited METHOD AND POLYMORPHOLIC FORMS OF BICTEGRAVIR AND 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
TWI845826B (zh) 2020-03-20 2024-06-21 美商基利科學股份有限公司 4'-c-經取代-2-鹵基-2'-去氧腺苷核苷之前藥及其製造與使用方法
EP4153181A1 (en) 2020-05-21 2023-03-29 Gilead Sciences, Inc. Pharmaceutical compositions comprising bictegravir
CN113698420A (zh) * 2020-05-22 2021-11-26 上海迪赛诺生物医药有限公司 比克替拉韦钠的新晶型及其制备方法
TWI815194B (zh) 2020-10-22 2023-09-11 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
WO2022103758A1 (en) 2020-11-11 2022-05-19 Gilead Sciences, Inc. METHODS OF IDENTIFYING HIV PATIENTS SENSITIVE TO THERAPY WITH gp120 CD4 BINDING SITE-DIRECTED ANTIBODIES
CN112409380A (zh) * 2020-12-10 2021-02-26 上海迪赛诺生物医药有限公司 比克替拉韦钠的新晶型的制备方法及其应用
HRP20231654T2 (hr) 2021-01-19 2025-01-03 Gilead Sciences, Inc. Supstituirani spojevi piridotriazina i njihove uporabe
WO2022224120A1 (en) * 2021-04-19 2022-10-27 Honour Lab Limited Polymorphic forms of bictegravir potassium
KR20240113832A (ko) 2021-12-03 2024-07-23 길리애드 사이언시즈, 인코포레이티드 Hiv 바이러스 감염 치료용 화합물
CN118922419A (zh) * 2022-04-06 2024-11-08 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
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
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
AU2023330037A1 (en) 2022-08-26 2025-03-06 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
WO2024220624A1 (en) 2023-04-19 2024-10-24 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
US20250011352A1 (en) 2023-05-31 2025-01-09 Gilead Sciences, Inc. Solid forms
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
US20250122219A1 (en) * 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
WO2025080850A1 (en) * 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
TW202515549A (zh) * 2023-10-11 2025-04-16 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
WO2025184609A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Antiviral compounds
WO2025184452A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
WO2025184447A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090318421A1 (en) * 2005-04-28 2009-12-24 Brian Alvin Johns Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity

Family Cites Families (120)

* 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
WO2000027823A1 (en) 1998-11-09 2000-05-18 James Black Foundation Limited Gastrin and cholecystokinin receptor ligands
GB2345058A (en) 1998-12-01 2000-06-28 Cerebrus Pharm Ltd Hydroxypyridone compounds useful in the treatment of oxidative damage to the central nervous system
CN1178913C (zh) 1998-12-25 2004-12-08 盐野义制药株式会社 具有hiv整合酶抑制活性的芳族杂环化合物
AU2001262732A1 (en) 2000-06-14 2001-12-24 Shionogi And Co., Ltd. Inhibitor for enzyme having two divalent metal ions as active centers
ATE530520T1 (de) 2001-08-10 2011-11-15 Shionogi & Co Antivirales mittel
HUP0402503A2 (hu) 2001-10-03 2005-03-29 Ucb, S.A. Pirrolidinonszármazékok és a vegyületeket tartalmazó gyógyászati készítmények
IL161337A0 (en) 2001-10-26 2004-09-27 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
EP1549315A4 (en) 2002-09-11 2007-05-23 Merck & Co Inc DIHYDROXYPYRIDOPYRAZINE-1,6-DION COMPOUNDS AS HIV INTEGRASE INHIBITORS
AU2003302029B8 (en) 2002-11-20 2006-08-17 Japan Tobacco Inc. 4-oxoquinoline compound and utilization thereof as HIV integrase inhibitor
CA2512319A1 (en) 2003-01-14 2004-08-05 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
US7429565B2 (en) 2003-04-25 2008-09-30 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
AU2005220767A1 (en) 2004-03-09 2005-09-22 Merck & Co., Inc. HIV integrase inhibitors
WO2006028523A2 (en) 2004-04-29 2006-03-16 THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, SAN DIEGO USDC Technology Transfer Office Hydroxypyridinone, hydroxypyridinethione, pyrone, and thiopyrone metalloprotein inhibitors
WO2005110399A2 (en) 2004-04-29 2005-11-24 The Regents Of The University Of California Zinc-binding groups for metalloprotein inhibitors
WO2005110414A2 (en) 2004-05-07 2005-11-24 Merck & Co., Inc. Hiv integrase inhibitors
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
CN101027062A (zh) 2004-07-27 2007-08-29 吉里德科学公司 Hiv抑制剂化合物的膦酸酯类似物
CN101014572B (zh) 2004-09-15 2011-07-06 盐野义制药株式会社 具有hiv整合酶抑制活性的氨基甲酰基吡啶酮衍生物
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
JP5317257B2 (ja) 2005-02-21 2013-10-16 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２環性カルバモイルピリドン誘導体
UA96568C2 (en) * 2005-04-28 2011-11-25 Глаксосмиткляйн Ллк Polycyclic carbamoyl pyridone derivative as hiv-integrase inhibitor
AR057023A1 (es) 2005-05-16 2007-11-14 Gilead Sciences Inc Compuestos heterociclicos con propiedades inhibidoras de hiv-integrasa
US20080076740A1 (en) 2005-07-27 2008-03-27 Gilead Sciences, Inc. Antiviral compounds
CA2626956A1 (en) 2005-10-27 2007-05-03 Shionogi & Co., Ltd. Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity
JP4676536B2 (ja) 2005-12-30 2011-04-27 ギリアド サイエンシズ， インコーポレイテッド Ｈｉｖインテグラーゼ阻害剤の薬物動態の改善方法
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
EA017861B9 (ru) 2006-03-06 2014-05-30 Джапан Тобакко Инк. Способ получения 4-оксохинолинового соединения
US8420821B2 (en) 2006-03-06 2013-04-16 Japan Tobacco Inc. Process for production of 4-oxoquinoline compound
US7893055B2 (en) 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
US20100092427A1 (en) 2006-07-19 2010-04-15 The University Of Georgia Research Foundation Pyridinone Diketo Acids: Inhibitors of HIV Replication in Combination Therapy
SG174787A1 (en) 2006-09-12 2011-10-28 Gilead Sciences Inc Process and intermediates for preparing integrase inhibitors
CA2665538A1 (en) 2006-10-18 2008-04-24 Merck & Co., Inc. Hiv integrase inhibitors
EP3689353A1 (en) 2007-02-23 2020-08-05 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
EP2167089A1 (en) 2007-06-29 2010-03-31 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
AP2965A (en) 2007-06-29 2014-09-30 Gilead Sciences Inc Therapeutic compositions and the use thereof
WO2009018350A1 (en) 2007-07-31 2009-02-05 Limerick Biopharma, Inc. Pyrone analog compositions and methods
AR068403A1 (es) 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa
EA019259B1 (ru) 2007-11-16 2014-02-28 Джилид Сайенсиз, Инк. Ингибиторы репликации вируса иммунодефицита человека
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
WO2010011818A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
CN102149385B (zh) 2008-07-25 2015-04-01 盐野义制药株式会社 化合物
PT2320908E (pt) 2008-07-25 2014-03-06 Shionogi & Co Pró-fármacos de dolutegravir
WO2010011815A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
EP2465858B1 (en) 2008-07-25 2013-12-25 VIIV Healthcare Company Process for preparing a pyrido[1,2-a]pyrrolo[1',2':3,4]imidazo[1,2-d]pyrazine-8-carboxamide derivative
WO2010011819A1 (en) 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
US8624023B2 (en) 2008-12-11 2014-01-07 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone HIV integrase inhibitors and intermediates
EP3617194B1 (en) 2008-12-11 2023-11-08 VIIV Healthcare Company Processes and intermediates for carbamoylpyridone hiv integrase inhibitors
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
JP5697163B2 (ja) 2009-03-26 2015-04-08 塩野義製薬株式会社 置換された３−ヒドロキシ−４−ピリドン誘導体
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
EA032868B1 (ru) 2010-01-27 2019-07-31 Вайв Хелткер Компани Комбинация для лечения вич-инфекции
MX2012009869A (es) 2010-02-26 2012-09-12 Japan Tobacco Inc Derivado de 1, 3,4, 8-tetrahidro-2h-pirido[1, 2-a]pirazina y sus uso como inhibidor de la integrasa del vih.
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
EA201291300A1 (ru) 2010-07-02 2013-06-28 Джилид Сайэнс, Инк. Производные нафт-2-илуксусной кислоты для лечения спида
KR20130124291A (ko) 2010-07-02 2013-11-13 길리애드 사이언시즈, 인코포레이티드 Ｈｉｖ 항바이러스 화합물로서의 2-퀴놀리닐-아세트산 유도체
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
RS61796B1 (sr) 2010-08-05 2021-06-30 Shionogi & Co Postupak za proizvodnju jedinjenja koja imaju inhibitornu aktivnost u odnosu na hiv integrazu
ES2683153T3 (es) 2010-09-24 2018-09-25 Shionogi & Co., Ltd. Profármaco derivado de carbamoil piridona policíclica sustituida
WO2012106534A2 (en) 2011-02-02 2012-08-09 The Regents Of The University Of California Hiv integrase inhibitors
UA111841C2 (uk) 2011-04-21 2016-06-24 Гіліад Сайєнсіз, Інк. Сполуки бензотіазолу та їх фармацевтичне застосування
US20140213553A1 (en) 2011-05-03 2014-07-31 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
PT2729448E (pt) 2011-07-06 2015-12-02 Gilead Sciences Inc Compostos para o tratamento de vih
CN102863512B (zh) 2011-07-07 2016-04-20 上海泓博智源医药技术有限公司 抗病毒化合物
WO2013038407A1 (en) 2011-09-14 2013-03-21 Mapi Pharma Ltd. Amorphous form of dolutegravir
JP6163428B2 (ja) 2011-10-12 2017-07-12 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
CA2858685A1 (en) 2011-12-12 2013-06-20 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
AU2013249041B2 (en) 2012-04-20 2016-11-03 Gilead Sciences, Inc. Benzothiazol- 6 -yl acetic acid derivatives and their use for treating an HIV infection
WO2014008636A1 (en) 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Macrocyclic compounds as hiv integrase inhibitors
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 NAPHTHYRIDEINDION DERIVATIVES AS HIV INTEGRASE INHIBITORS
PT2880017T (pt) 2012-08-03 2016-12-14 Gilead Sciences Inc Processo e intermediários para preparar inibidores da integrase
JP6204484B2 (ja) 2012-11-08 2017-09-27 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ キナーゼモジュレーターとして有用なヘテロアリール置換ピリジル化合物
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
CA3131094A1 (en) 2012-12-21 2014-06-26 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
US20140221355A1 (en) 2012-12-21 2014-08-07 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
EP2934482A4 (en) 2012-12-21 2016-07-20 Merck Sharp & Dohme ADMINISTRATIVE FORMULATIONS
KR20150102069A (ko) 2012-12-27 2015-09-04 니뽄 다바코 산교 가부시키가이샤 치환된 스피로피리도[1,2-a]피라진 유도체 및 그의 HIV 인테그라제 저해제로서의 의약 용도
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
TN2016000090A1 (en) 2013-09-27 2017-07-05 Merck Sharp & Dohme Substituted quinolizine derivatives useful as hiv integrase inhibitors.
WO2015089847A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
US9856271B2 (en) 2014-01-21 2018-01-02 Laurus Labs Limited Process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof
NO2717902T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) * 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
WO2016102078A1 (en) 2014-12-24 2016-06-30 Ratiopharm Gmbh Solid state forms of dolutegravir sodium
EA201890654A1 (ru) 2015-11-09 2018-10-31 Джилид Сайэнс, Инк. Терапевтические композиции для лечения вируса иммунодефицита человека

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090318421A1 (en) * 2005-04-28 2009-12-24 Brian Alvin Johns Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity

Also Published As

Publication number Publication date
EA030967B1 (ru) 2018-10-31
EP3157932B1 (en) 2018-01-10
MA44221A (fr) 2018-12-26
HRP20180455T1 (hr) 2018-05-04
IL249161A0 (en) 2017-01-31
CU24478B1 (es) 2020-03-04
ME03037B (me) 2018-10-20
CL2016003249A1 (es) 2017-07-14
NO2717902T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2018-06-23
CN106459085A (zh) 2017-02-22
ES2660862T3 (es) 2018-03-26
DK3157932T3 (en) 2018-03-05
BR112016029605B1 (pt) 2022-10-11
ES3010114T3 (en) 2025-04-01
ECSP16095566A (es) 2017-01-31
MY186696A (en) 2021-08-10
EA201891464A1 (ru) 2019-03-29
PL3321270T3 (pl) 2025-03-24
CN106459085B (zh) 2019-07-30
BR112016029605A8 (pt) 2021-07-20
US20180065986A1 (en) 2018-03-08
UY36177A (es) 2016-01-08
HUE036928T2 (hu) 2018-08-28
US20160016973A1 (en) 2016-01-21
MD4584B1 (ro) 2018-07-31
AU2015276860B2 (en) 2018-05-31
RS56950B1 (sr) 2018-05-31
UA118480C2 (uk) 2019-01-25
PT3157932T (pt) 2018-02-21
MD4584C1 (ro) 2019-02-28
PL3157932T3 (pl) 2018-05-30
AU2018203175B2 (en) 2020-01-02
CA2950307A1 (en) 2015-12-23
PH12016502499B1 (en) 2019-10-25
BR112016029605A2 (pt) 2017-08-22
CR20160589A (es) 2017-02-24
ZA201608744B (en) 2023-04-26
CY1120025T1 (el) 2018-12-12
CN110563747A (zh) 2019-12-13
US9708342B2 (en) 2017-07-18
TWI731354B (zh) 2021-06-21
AU2015276860A1 (en) 2016-12-22
JP2022095640A (ja) 2022-06-28
EP3321270A1 (en) 2018-05-16
KR101899803B1 (ko) 2018-09-20
JP2018162246A (ja) 2018-10-18
WO2015196116A1 (en) 2015-12-23
NZ727155A (en) 2022-02-25
CU20160187A7 (es) 2017-04-05
TW201613937A (en) 2016-04-16
EP4523758A3 (en) 2025-05-14
MA40239B1 (fr) 2018-05-31
JP2017518356A (ja) 2017-07-06
CA2950307C (en) 2019-01-08
DOP2016000327A (es) 2017-01-15
US20170197985A1 (en) 2017-07-13
MD20170006A2 (ro) 2017-06-30
SI3157932T1 (en) 2018-06-29
TR201802179T4 (tr) 2018-03-21
JP2020097593A (ja) 2020-06-25
MX2019013380A (es) 2020-02-20
EP3157932A1 (en) 2017-04-26
EA201692414A1 (ru) 2017-06-30
US10385067B2 (en) 2019-08-20
EP3321270C0 (en) 2024-12-04
EP4523758A2 (en) 2025-03-19
MX2016016059A (es) 2017-05-03
MA40239A (fr) 2018-01-09
MX369555B (es) 2019-11-12
PH12016502499A1 (en) 2017-03-22
PE20170150A1 (es) 2017-04-07
MX383272B (es) 2025-03-13
EP3321270B1 (en) 2024-12-04
SG11201610211QA (en) 2017-01-27
AP2016009591A0 (en) 2016-11-30
JP6334007B2 (ja) 2018-05-30
SMT201800053T1 (it) 2018-03-08
SV2016005339A (es) 2017-03-20
KR20170016985A (ko) 2017-02-14
AR100903A1 (es) 2016-11-09
BR122021025861B1 (pt) 2023-01-24
IL249161B (en) 2021-03-25
AU2018203175A1 (en) 2018-05-24
TW202014422A (zh) 2020-04-16
MD20180037A2 (ro) 2018-07-31
LT3157932T (lt) 2018-02-26

Similar Documents

Publication Publication Date Title
TWI673274B (zh) （２Ｒ，５Ｓ，１３ａＲ）－７，９－二側氧基－１０－（（２，４，６－三氟苄基）胺甲醯基）－２，３，４，５，７，９，１３，１３ａ－八氫－２，５－甲橋吡啶並［１’，２’：４，５］吡並［２，１－ｂ］［１，３］氧氮呯－８－醇化鈉
US11202780B2 (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
HK40013745A (en) An anti-hiv compound and crystalline forms thereof
HK1253820A1 (en) Sodium (2r, 5s, 13ar) -7, 9-dioxo-10- ( (2,4,6-trifluorobenzyl) carbamoyl) -2, 3, 4, 5, 7, 9, 13, 13a-octahydro-2, 5-methanopyrido [1',2' : 4.5] pyrazino [2, 1-b] oxazepin-8-olate
HK1232879B (zh) 抗hiv化合物及其晶型
HK1235403B (en) Sodium (2r, 5s, 13ar) -7, 9-dioxo-10- ( (2,4,6-trifluorobenzyl) carbamoyl) -2, 3, 4, 5, 7, 9, 13, 13a-octahydro-2, 5-methanopyrido [1',2' : 4.5]pyrazino [2, 1-b]oxazepin-8-olate
HK1235403A1 (en) Sodium (2r, 5s, 13ar) -7, 9-dioxo-10- ( (2,4,6-trifluorobenzyl) carbamoyl) -2, 3, 4, 5, 7, 9, 13, 13a-octahydro-2, 5-methanopyrido [1',2' : 4.5]pyrazino [2, 1-b]oxazepin-8-olate
HK1232879A1 (en) An anti-hiv compound and crystalline forms thereof
OA18760A (en) Sodium (2R, 5S, 13AR)-7,9-dioxo-10-((2,4,6trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13Aoctrahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1B] oxazepin-8-olate.