MD20160044A2 - Derivaţi de chinolizină substituiţi utili ca inhibitori de integrază a HIV - Google Patents

Derivaţi de chinolizină substituiţi utili ca inhibitori de integrază a HIV Download PDF

Info

Publication number
MD20160044A2
MD20160044A2 MDA20160044A MD20160044A MD20160044A2 MD 20160044 A2 MD20160044 A2 MD 20160044A2 MD A20160044 A MDA20160044 A MD A20160044A MD 20160044 A MD20160044 A MD 20160044A MD 20160044 A2 MD20160044 A2 MD 20160044A2
Authority
MD
Moldova
Prior art keywords
substituted quinolizine
derivatives useful
hiv integrase
integrase inhibitors
quinolizine derivatives
Prior art date
Application number
MDA20160044A
Other languages
English (en)
Russian (ru)
Other versions
MD4794B1 (ro
Inventor
Т Юй
Юнлянь Чжан
Шерман Тим УЭДДЕЛЛ
Эндрю СТЭМФОРД
Джон ВАЙ
Пол Дж. Коулман
Джон М. Сандерс
Рональд ФЕРГЮСОН
Original Assignee
Merck Sharp & Dohme Corp
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
Application filed by Merck Sharp & Dohme Corp filed Critical Merck Sharp & Dohme Corp
Publication of MD20160044A2 publication Critical patent/MD20160044A2/ro
Publication of MD4794B1 publication Critical patent/MD4794B1/ro

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/02—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing not further condensed quinolizine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/03—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/04—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

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

Abstract

Prezenta invenţie se referă la derivaţi de chinolizină substituiţi cu formula (I):(I)şi la sărurile farmaceutic acceptabile sau promedicamentele acestora, în care X, Y, R1, R2, R3,R4, R5, R9 şi R10 au semnificaţiile definite în descrierea invenţiei. Prezenta invenţie se referă, de asemenea, la compoziţii cuprinzând cel puţin un derivat de chinolizină substituit şi la metode de utilizare a derivaţilor de chinolizină substituiţi pentru tratarea sau prevenirea infecţiei cu HIV la un subiect.
MDA20160044A 2013-09-27 2014-09-26 Derivaţi de chinolizină substituiţi utili ca inhibitori de integrază HIV MD4794B1 (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361883463P 2013-09-27 2013-09-27
PCT/US2014/057572 WO2015048363A1 (en) 2013-09-27 2014-09-26 Substituted quinolizine derivatives useful as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
MD20160044A2 true MD20160044A2 (ro) 2016-07-31
MD4794B1 MD4794B1 (ro) 2022-02-28

Family

ID=52744477

Family Applications (1)

Application Number Title Priority Date Filing Date
MDA20160044A MD4794B1 (ro) 2013-09-27 2014-09-26 Derivaţi de chinolizină substituiţi utili ca inhibitori de integrază HIV

Country Status (31)

Country Link
US (2) US9861620B2 (ro)
EP (1) EP3049081B1 (ro)
JP (2) JP6081662B2 (ro)
KR (2) KR102102516B1 (ro)
CN (1) CN105744936B (ro)
AP (1) AP2016009157A0 (ro)
AU (1) AU2014324829B2 (ro)
BR (1) BR112016006651B8 (ro)
CA (1) CA2924829C (ro)
CL (1) CL2016000698A1 (ro)
CR (1) CR20160140A (ro)
DO (1) DOP2016000069A (ro)
EA (1) EA030695B1 (ro)
EC (1) ECSP16016726A (ro)
ES (1) ES2768658T3 (ro)
GT (1) GT201600056A (ro)
HK (1) HK1221648A1 (ro)
IL (1) IL244438B (ro)
MA (1) MA38922A3 (ro)
MD (1) MD4794B1 (ro)
MX (1) MX367057B (ro)
NI (1) NI201600040A (ro)
PE (1) PE20160501A1 (ro)
PH (1) PH12016500553A1 (ro)
SA (1) SA516370826B1 (ro)
SG (1) SG11201602217XA (ro)
SV (1) SV2016005171A (ro)
TN (1) TN2016000090A1 (ro)
UA (1) UA117499C2 (ro)
WO (1) WO2015048363A1 (ro)
ZA (1) ZA201601708B (ro)

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
NO2865735T3 (ro) 2013-07-12 2018-07-21
DK3019503T3 (da) 2013-07-12 2017-11-20 Gilead Sciences Inc Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner
MX367057B (es) * 2013-09-27 2019-08-02 Merck Sharp & Dohme Derivados de quinolizina sustituidos utiles como inhibidores de integrasa del vih.
WO2015089847A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
TWI677489B (zh) 2014-06-20 2019-11-21 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
NO2717902T3 (ro) 2014-06-20 2018-06-23
EP3757105B1 (en) 2014-08-22 2024-07-24 Shionogi & Co., Ltd. Polycyclic pyridone derivative having integrase inhibitory activity
TWI738321B (zh) 2014-12-23 2021-09-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
US10081647B2 (en) 2015-03-26 2018-09-25 Merck Sharp & Dohme Corp. Phosphate substituted quinolizine derivatives useful as HIV integrase inhibitors
TR201905009T4 (tr) 2015-04-02 2019-05-21 Gilead Sciences Inc Polisiklik-karbamoilpiridon bileşikleri ve bunların farmasötik kullanımları.
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
WO2017106071A1 (en) 2015-12-15 2017-06-22 Merck Sharp & Dohme Corp. Spirocyclic quinolizine derivatives useful as hiv integrase inhibitors
US20190216725A1 (en) * 2016-09-21 2019-07-18 Merck Shapr & Dohme Corp. Drug delivery system for the delivery of integrase inhibitors
JOP20190130A1 (ar) 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
WO2018140368A1 (en) 2017-01-26 2018-08-02 Merck Sharp & Dohme Corp. Substituted quinolizine derivatives useful as hiv integrase inhibitors
JP2019016012A (ja) * 2017-07-03 2019-01-31 東芝テック株式会社 プリンタ装置及びプログラム
US11413292B2 (en) 2018-02-15 2022-08-16 Merck, Sharp & Dohme LLC Tricyclic heterocycle compounds useful as HIV integrase inhibitors
US11453669B2 (en) 2018-05-31 2022-09-27 Shionogi & Co., Ltd. Polycyclic pyridone derivative
CA3102063A1 (en) 2018-05-31 2019-12-05 Shionogi & Co., Ltd. Polycyclic carbamoylpyridone derivative
IL286328B1 (en) 2019-03-22 2026-04-01 Gilead Sciences Inc Tricyclic bridging compounds of carbamoylpyridone and their pharmaceutical use
US20200398978A1 (en) 2019-06-20 2020-12-24 Bell Helicopter Textron Inc. Low-drag rotor blade extension
US20220265845A1 (en) 2019-07-31 2022-08-25 Advanced Biodesign Aminothiolester compounds and uses thereof
CN112521386B (zh) * 2019-09-19 2023-05-26 周雨恬 具有抗病毒作用的多环吡啶酮化合物及其药物组合和用途
EP4066839A4 (en) 2019-11-28 2023-12-27 Shionogi & Co., Ltd PROPHYLACTIC AND THERAPEUTIC MEDICINAL PRODUCT FOR HIV INFECTIOUS DISEASES, CHARACTERIZED BY CONTAINING THE COMBINATION OF INTEGRAS INHIBITORS AND ANTI-HIV AGENTS
US12577241B2 (en) 2019-11-28 2026-03-17 Shionogi & Co., Ltd. Polycyclic pyridopyrazine derivative
CR20220418A (es) 2020-02-24 2022-10-10 Gilead Sciences Inc Compuestos tetracíclicos para el tratamiento de infecciones por vih
CA3192145A1 (en) 2020-09-30 2022-04-07 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
JP7591155B2 (ja) 2021-01-19 2024-11-27 ギリアード サイエンシーズ， インコーポレイテッド 置換ピリドトリアジン化合物及びその使用
FR3119314B1 (fr) 2021-01-29 2025-01-10 Advanced Biodesign Nanocapsule lipidique comprenant au moins un composé aminothiolester ou un de ses dérivés pharmaceutiquement acceptable
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
WO2025229179A1 (en) 2024-05-03 2025-11-06 Advanced Biodesign Use of aminothiolester compounds in combination with hypomethylating agents (hma) for the prevention and treatment of cancer

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6630488B1 (en) * 1998-09-21 2003-10-07 Biochem Pharma, Inc. Quinolizinones as integrin inhibitors
GB0110832D0 (en) * 2001-05-03 2001-06-27 Virogen Ltd Antiviral compounds
DK3042894T1 (da) 2001-08-10 2016-11-07 Shionogi & Co Antiviralt middel
DE60209381T2 (de) 2001-10-26 2006-10-05 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase
SI1441734T1 (sl) 2001-10-26 2007-08-31 Angeletti P Ist Richerche Bio Dihidropirimidin karboksamidni inhibitorji HIV-integraze
ES2291642T3 (es) 2002-01-17 2008-03-01 MERCK & CO., INC. Hidroxinaftiridinoncarboxamidas utiles como inhibidores de la integrasa de vih.
US7517532B2 (en) 2002-09-11 2009-04-14 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors
BR0317749A (pt) 2002-12-27 2005-11-22 Angeletti P Ist Richerche Bio Composto, composição farmacêutica, e, uso de um composto
US7135467B2 (en) 2003-01-13 2006-11-14 Bristol-Myers Squibb Company HIV integrase inhibitors
US7037908B2 (en) 2003-04-24 2006-05-02 Bristol-Myers Squibb Company HIV integrase inhibitors
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
JP2006232849A (ja) * 2003-08-13 2006-09-07 Japan Tobacco Inc 含窒素縮合環化合物及びそのｈｉｖインテグラーゼ阻害剤としての利用
AR046938A1 (es) 2003-12-12 2006-01-04 Merck & Co Inc Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
TW200526635A (en) 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
EP1725556A1 (en) * 2004-03-09 2006-11-29 Merck & Co., Inc. Hiv integrase inhibitors
CA2557926A1 (en) 2004-03-09 2005-09-22 Monica Donghi Hiv integrase inhibitors
US7273859B2 (en) 2004-05-12 2007-09-25 Bristol-Myers Squibb Company HIV integrase inhibitors: cyclic pyrimidinone compounds
US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
US7176196B2 (en) 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7173022B2 (en) 2004-05-28 2007-02-06 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7157447B2 (en) 2004-05-28 2007-01-02 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7192948B2 (en) 2004-05-28 2007-03-20 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
WO2006033422A1 (ja) * 2004-09-21 2006-03-30 Japan Tobacco Inc. キノリジノン化合物、およびそのｈｉｖインテグラーゼ阻害剤としての利用
US7745459B2 (en) 2004-09-21 2010-06-29 Japan Tobacco Inc. Quinolizinone compound and use thereof as HIV integrase inhibitor
US20060066414A1 (en) 2004-09-28 2006-03-30 Rockwell Scientific Licensing, Llc Method and apparatus for changing the polarization of a signal
WO2006066414A1 (en) 2004-12-23 2006-06-29 Virochem Pharma Inc. Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase
ATE516026T1 (de) * 2005-02-21 2011-07-15 Shionogi & Co Bicyclisches carbamoylpyridonderivat mit hiv- integrase-hemmender wirkung
AU2006228278C1 (en) 2005-03-31 2011-06-23 Msd Italia S.R.L. HIV integrase inhibitors
PT1874117E (pt) 2005-04-28 2013-10-17 Shionogi & Co Derivado policíclico de carbamoílpiridona possuindo actividade inibidora de hiv-integrasse
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
JP2006342115A (ja) 2005-06-10 2006-12-21 Shionogi & Co Ltd Ｈｉｖインテグラーゼ阻害活性を有する多環性化合物
US7494984B2 (en) 2005-08-31 2009-02-24 Bristol-Myers Squibb Company Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
US7897592B2 (en) 2005-11-15 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
US7902182B2 (en) 2005-11-16 2011-03-08 Bristol-Myers Squibb Company HIV integrase inhibitors
US8039458B2 (en) 2005-11-17 2011-10-18 Bristol-Myers Squibb Company HIV integrase inhibitors
US7897593B2 (en) 2006-05-30 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
US7893055B2 (en) 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
US20120220571A1 (en) * 2009-08-26 2012-08-30 Wai John S Hiv integrase inhibitors
JP5624148B2 (ja) 2009-10-13 2014-11-12 エランコ・アニマル・ヘルス・アイルランド・リミテッド 大環状インテグラーゼ阻害剤
UA105556C2 (uk) 2010-01-27 2014-05-26 Віів Гелскер Компані Комбінація сполук, що містить інгібітори віл інтегрази з іншими терапевтичними агентами
RU2567385C2 (ru) 2010-04-02 2015-11-10 ЯНССЕН Ар ЭНД Ди АЙРЛЭНД Макроциклические ингибиторы интегразы
MX367057B (es) * 2013-09-27 2019-08-02 Merck Sharp & Dohme Derivados de quinolizina sustituidos utiles como inhibidores de integrasa del vih.

Also Published As

Publication number Publication date
HK1221648A1 (zh) 2017-06-09
EA030695B1 (ru) 2018-09-28
ECSP16016726A (es) 2017-08-31
CL2016000698A1 (es) 2016-09-23
JP2017105793A (ja) 2017-06-15
IL244438B (en) 2020-07-30
JP6081662B2 (ja) 2017-02-15
BR112016006651A8 (pt) 2018-01-30
NZ717864A (en) 2021-09-24
PE20160501A1 (es) 2016-05-14
EP3049081A1 (en) 2016-08-03
US20160228419A1 (en) 2016-08-11
UA117499C2 (uk) 2018-08-10
MD4794B1 (ro) 2022-02-28
KR20160061404A (ko) 2016-05-31
BR112016006651B8 (pt) 2021-03-02
JP6550083B2 (ja) 2019-07-24
KR101809392B1 (ko) 2017-12-14
AP2016009157A0 (en) 2016-04-30
EA201690669A8 (ru) 2018-07-31
KR102102516B1 (ko) 2020-04-20
EA201690669A1 (ru) 2016-12-30
JP2016531863A (ja) 2016-10-13
TN2016000090A1 (en) 2017-07-05
PH12016500553B1 (en) 2016-05-23
AU2014324829B2 (en) 2017-09-07
CN105744936B (zh) 2019-07-30
CN105744936A (zh) 2016-07-06
ZA201601708B (en) 2017-06-28
KR20170133521A (ko) 2017-12-05
EP3049081A4 (en) 2017-02-22
CA2924829A1 (en) 2015-04-02
GT201600056A (es) 2017-12-28
US9861620B2 (en) 2018-01-09
IL244438A0 (en) 2016-04-21
US10201533B2 (en) 2019-02-12
DOP2016000069A (es) 2016-07-15
CR20160140A (es) 2016-06-17
MA38922A2 (fr) 2018-10-31
CA2924829C (en) 2019-10-29
ES2768658T3 (es) 2020-06-23
US20180028509A1 (en) 2018-02-01
NI201600040A (es) 2016-06-21
WO2015048363A1 (en) 2015-04-02
MX2016003860A (es) 2016-08-01
AU2014324829A1 (en) 2016-03-24
SV2016005171A (es) 2016-11-21
SG11201602217XA (en) 2016-04-28
PH12016500553A1 (en) 2016-05-23
EP3049081B1 (en) 2019-11-27
MX367057B (es) 2019-08-02
SA516370826B1 (ar) 2020-10-27
MA38922A3 (fr) 2018-11-30
BR112016006651B1 (pt) 2021-01-12
BR112016006651A2 (pt) 2017-08-01

Similar Documents

Publication Publication Date Title
MD4794B1 (ro) Derivaţi de chinolizină substituiţi utili ca inhibitori de integrază HIV
PH12019501198A1 (en) Tetracyclic heterocycle compounds useful as hiv integrase inhibitors
MX2018008095A (es) Compuestos heterociclicos triciclicos condensados como inhibidores de integrasa del vih.
PH12017501326A1 (en) Tgf-� inhibitors
MX2019004578A (es) Oxisteroles y metodos de uso de los mismos.
GEP20186838B (en) 5-phenoxy-3h-pyrimidin-4-one derivatives and their usage as hiv reverse transcriptase inhibitors
PH12018500061A1 (en) Oxysterols and methods of use thereof
PH12018500065B1 (en) Oxysterols and methods of use thereof
CA2875877C (en) Syk inhibitors
PH12015502443A1 (en) 6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
JO3425B1 (ar) مشتقات البابيريدينيل-اندول واستخدامها كعامل متمم لمثبطات b
NZ736709A (en) Benzimidazole and imidazopyridine carboximidamide compounds having activity as inhibitors of indoleamine 2,3-dioxygenase
NZ703064A (en) Inhibitors of hepatitis c virus
DK2997033T3 (da) Kondenserede tricykliske heterocykliske forbindelser som hiv- integrasehæmmere
MX2015012431A (es) Pirrol amida como inhibidores.
EA201790923A1 (ru) Производные бетулина
WO2014172188A3 (en) 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
MX2019006449A (es) Compuestos heterociclicos triciclicos utiles como inhibidores de la integrasa del virus de inmunodeficiencia humana (vih).
MY182353A (en) Novel sulfonimidoylpurinone compounds and derivatives for the treatment and prophylaxis of virus infection
MX2015010611A (es) Nuevos derivados de dihidroquinolin-2-ona como inhibidores de la aldosterona-sintasa (citocromo p450, familia 11, subfamilia b, polipeptido 2 (cyp11b2) o citocromo p450, familia 11, subfamilia b, polipeptido 1 (cyp11b1)).
MD20160111A2 (ro) Derivaţi diheterociclici legaţi de cicloalchil
GEAP201814124A (en) Substituted quinolizine derivatives useful as hiv integrase inhibitors

Legal Events

Date Code Title Description
KA4A Patent for invention lapsed due to non-payment of fees (with right of restoration)