TW201726683A - 作為ｈｉｖ整合酶抑制劑之稠合三環雜環化合物 - Google Patents

作為ｈｉｖ整合酶抑制劑之稠合三環雜環化合物 Download PDF

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Publication number
TW201726683A
TW201726683A TW105142826A TW105142826A TW201726683A TW 201726683 A TW201726683 A TW 201726683A TW 105142826 A TW105142826 A TW 105142826A TW 105142826 A TW105142826 A TW 105142826A TW 201726683 A TW201726683 A TW 201726683A
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Taiwan
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group
int
alkyl
formula
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TW105142826A
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于濤
雪曼 Ｔ 偉德爾
湯瑪士 Ｈ 葛拉翰
張永璉
約翰 Ａ 麥克考利
安德魯 W 史丹佛
蔡嘉強
齊志奇
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默沙東藥廠
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    • 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
    • C07D471/16—Peri-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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic 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
    • A61K31/495—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
    • A61K31/33—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
    • A61K31/5365—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 ortho- or peri-condensed with heterocyclic 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
    • A61K31/63—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
    • A61K31/683—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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (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)
TW105142826A 2015-12-31 2016-12-22 作為ｈｉｖ整合酶抑制劑之稠合三環雜環化合物 TW201726683A (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2015/100106 WO2017113288A1 (en) 2015-12-31 2015-12-31 Fused tricyclic heterocyclic compounds as hiv integrase inhibitors

Publications (1)

Publication Number Publication Date
TW201726683A true TW201726683A (zh) 2017-08-01

Family

ID=57799839

Family Applications (1)

Application Number Title Priority Date Filing Date
TW105142826A TW201726683A (zh) 2015-12-31 2016-12-22 作為ｈｉｖ整合酶抑制劑之稠合三環雜環化合物

Country Status (15)

Country Link
US (4) US20170190701A1 (enExample)
EP (1) EP3397639B1 (enExample)
JP (1) JP2019500387A (enExample)
KR (1) KR20180095833A (enExample)
CN (1) CN108473494A (enExample)
AR (1) AR107170A1 (enExample)
AU (1) AU2016381072B2 (enExample)
BR (1) BR112018013251A2 (enExample)
CA (1) CA3008018A1 (enExample)
JO (1) JO3811B1 (enExample)
MA (1) MA43528A (enExample)
MX (1) MX2018008095A (enExample)
RU (1) RU2740187C2 (enExample)
TW (1) TW201726683A (enExample)
WO (2) WO2017113288A1 (enExample)

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US10081647B2 (en) * 2015-03-26 2018-09-25 Merck Sharp & Dohme Corp. Phosphate substituted quinolizine derivatives useful as HIV 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)
WO2018102634A1 (en) 2016-12-02 2018-06-07 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as hiv integrase inhibitors
WO2019209667A1 (en) * 2018-04-27 2019-10-31 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as hiv integrase inhibitors
EP3805221A4 (en) 2018-05-31 2022-01-05 Shionogi & Co., Ltd POLYCYCLIC PYRIDONE DERIVATIVE
CR20230571A (es) 2018-05-31 2024-01-22 Shionogi & Co DERIVADO POLICÍCLICO DE CARBAMOILPIRIDONA (divisional 2020-0644)
US11884683B2 (en) 2018-06-05 2024-01-30 Merck Sharp & Dohme Llc Tricyclic heterocycle compounds useful as HIV integrase inhibitors
EP4751717A3 (en) * 2018-10-22 2026-08-05 Board of Regents of the University of Nebraska Antiviral prodrugs and nanoformulations thereof
KR20240151256A (ko) 2019-03-22 2024-10-17 길리애드 사이언시즈, 인코포레이티드 가교된 트리시클릭 카르바모일피리돈 화합물 및 그의 제약 용도
US20200398978A1 (en) 2019-06-20 2020-12-24 Bell Helicopter Textron Inc. Low-drag rotor blade extension
US12564595B2 (en) 2019-11-28 2026-03-03 Shionogi & Co., Ltd. Prophylactic and therapeutic pharmaceutical agent for HIV infectious diseases characterized by comprising combination of integrase inhibitor and anti-HIV agent
WO2021107065A1 (ja) 2019-11-28 2021-06-03 塩野義製薬株式会社 多環性ピリドピラジン誘導体
EP4110783A1 (en) * 2020-02-24 2023-01-04 Gilead Sciences, Inc. Tetracyclic compounds for treating hiv infection
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
CR20260070A (es) 2021-01-19 2026-04-24 Gilead Sciences Inc COMPUESTOS DE PIRIDOTRIAZINA SUSTITUIDOS Y USOS DE ESTOS (Divisional 2023-0315)
US11958864B2 (en) * 2021-02-16 2024-04-16 Merck Sharp & Dohme Llc Tetracyclic heterocycle compounds useful as HIV integrase inhibitors
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

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SI2997033T1 (en) * 2013-05-17 2018-04-30 Merck Sharp & Dohme Corp. FUZYCLE TRICYCLE HETEROCYCLIC COMPOUNDS AS HIV INTEGRATED INHIBITORS

Also Published As

Publication number Publication date
RU2018127728A (ru) 2020-02-03
RU2018127728A3 (enExample) 2020-02-14
AU2016381072B2 (en) 2020-11-26
AU2016381072A1 (en) 2018-05-31
AR107170A1 (es) 2018-03-28
US20170190701A1 (en) 2017-07-06
MA43528A (fr) 2018-11-07
US20180099967A1 (en) 2018-04-12
BR112018013251A2 (pt) 2018-12-04
US20210040096A1 (en) 2021-02-11
US20190322666A1 (en) 2019-10-24
EP3397639B1 (en) 2022-02-23
WO2017113288A1 (en) 2017-07-06
KR20180095833A (ko) 2018-08-28
WO2017116928A1 (en) 2017-07-06
CA3008018A1 (en) 2017-07-06
MX2018008095A (es) 2018-08-23
JO3811B1 (ar) 2021-01-31
EP3397639A1 (en) 2018-11-07
JP2019500387A (ja) 2019-01-10
CN108473494A (zh) 2018-08-31
RU2740187C2 (ru) 2021-01-12

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