CN110062627A - 可用作hiv整合酶抑制剂的三环杂环化合物 - Google Patents

可用作hiv整合酶抑制剂的三环杂环化合物 Download PDF

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Publication number
CN110062627A
CN110062627A CN201780074646.6A CN201780074646A CN110062627A CN 110062627 A CN110062627 A CN 110062627A CN 201780074646 A CN201780074646 A CN 201780074646A CN 110062627 A CN110062627 A CN 110062627A
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compound
int
mmol
alkyl
mixture
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CN201780074646.6A
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English (en)
Chinese (zh)
Inventor
T·H·格拉哈姆
余涛
S·T·沃德尔
J·A·麦考利
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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Publication of CN110062627A publication Critical patent/CN110062627A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/16Peri-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5365Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5395Heterocyclic 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 having two or more nitrogen atoms in the same ring, e.g. oxadiazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/22Heterocyclic 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 four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201780074646.6A 2016-12-02 2017-12-01 可用作hiv整合酶抑制剂的三环杂环化合物 Pending CN110062627A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662429376P 2016-12-02 2016-12-02
US62/429,376 2016-12-02
PCT/US2017/064116 WO2018102634A1 (en) 2016-12-02 2017-12-01 Tricyclic heterocycle compounds useful as hiv integrase inhibitors

Publications (1)

Publication Number Publication Date
CN110062627A true CN110062627A (zh) 2019-07-26

Family

ID=62242756

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780074646.6A Pending CN110062627A (zh) 2016-12-02 2017-12-01 可用作hiv整合酶抑制剂的三环杂环化合物

Country Status (11)

Country Link
US (1) US10934312B2 (https=)
EP (1) EP3548031B1 (https=)
JP (1) JP2020500866A (https=)
KR (1) KR20190086017A (https=)
CN (1) CN110062627A (https=)
AU (1) AU2017367714B2 (https=)
BR (1) BR112019011074B1 (https=)
CA (1) CA3042314A1 (https=)
MX (1) MX384729B (https=)
RU (1) RU2749043C2 (https=)
WO (1) WO2018102634A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112047945A (zh) * 2020-09-10 2020-12-08 浙江大学 螺环吡啶酮衍生物及应用

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4257137A3 (en) 2018-05-31 2023-11-01 Shionogi & Co., Ltd Polycyclic carbamoylpyridone derivatives for the treatment of hiv
MA52802A (fr) 2018-05-31 2021-04-14 Shionogi & Co Dérivé de pyridone polycyclique
EP3801543B1 (en) 2018-06-05 2024-09-11 Merck Sharp & Dohme LLC Tricyclic heterocycle compounds useful as hiv integrase inhibitors
MY201239A (en) 2019-03-22 2024-02-13 Gilead Sciences Inc Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
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
PE20221569A1 (es) 2020-02-24 2022-10-06 Gilead Sciences Inc Compuestos tetraciclicos para el tratamiento de infecciones por vih
ES3064867T3 (en) 2020-09-30 2026-04-29 Gilead Sciences Inc Bridged tricyclic carbamoylpyridone compounds for a use in the treatment of hiv
US11613546B2 (en) 2021-01-19 2023-03-28 Gilead Sciences, Inc. Substituted pyridotriazine compounds and uses thereof
TW202446773A (zh) 2022-04-06 2024-12-01 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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014183532A1 (en) * 2013-05-17 2014-11-20 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
US20150329539A1 (en) * 2012-12-17 2015-11-19 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2572030T3 (es) 2001-08-10 2017-07-19 Shionogi & Co., Ltd. Agente antiviral
ATE355064T1 (de) 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
IL161337A0 (en) 2001-10-26 2004-09-27 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
EP1467970B1 (en) 2002-01-17 2007-08-22 Merck & Co., Inc. Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors
WO2003091264A2 (en) 2002-04-26 2003-11-06 Gilead Sciences, Inc. Non nucleoside reverse transcriptase inhibitors
NZ540729A (en) 2002-12-27 2008-03-28 Angeletti P Ist Richerche Bio Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds useful as HIV integrase inhibitors
WO2004062613A2 (en) 2003-01-13 2004-07-29 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
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
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
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
US7176196B2 (en) 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
CA2600832C (en) 2005-03-31 2011-12-13 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors
KR101363875B1 (ko) 2005-04-28 2014-02-21 시오노기세야쿠 가부시키가이샤 Hiv 통합효소 억제 활성을 가지는 다환식카르바모일피리돈 유도체
MX2008005137A (es) * 2005-10-27 2008-09-29 Shionogi & Co Derivado de carbamoilpiridona policiclica que tiene actividad inhibidora en vih integrasa.
US8039458B2 (en) 2005-11-17 2011-10-18 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2007143446A1 (en) 2006-05-30 2007-12-13 Bristol-Myers Squibb Company Spiro-condensed heterotricyclic compounds as hiv integrase inhibitors
US7893055B2 (en) 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
ES2446720T3 (es) 2009-10-13 2014-03-10 Elanco Animal Health Ireland Limited Inhibidores de la integrasa macrocíclica
WO2011121105A1 (en) 2010-04-02 2011-10-06 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
US9493479B2 (en) * 2013-04-16 2016-11-15 Merck Sharp & Dohme Corp. Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors
EP3008044B1 (en) * 2013-06-13 2018-11-21 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
WO2015089847A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
US9975906B2 (en) * 2014-05-16 2018-05-22 Shionogi & Co., Ltd. Tricyclic heterocycle derivatives having HIV replication inhibitory effect
WO2016187788A1 (en) * 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
WO2017113288A1 (en) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150329539A1 (en) * 2012-12-17 2015-11-19 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
WO2014183532A1 (en) * 2013-05-17 2014-11-20 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
TAKASHI KAWASUJI: "Carbamoyl Pyridone HIV‑1 Integrase Inhibitors. 2. Bi- and Tricyclic", 《JOURNAL OF MEDICINAL CHEMISTRY》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112047945A (zh) * 2020-09-10 2020-12-08 浙江大学 螺环吡啶酮衍生物及应用
CN112047945B (zh) * 2020-09-10 2021-11-12 浙江大学 螺环吡啶酮衍生物及应用

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Publication number Publication date
US20200017524A1 (en) 2020-01-16
MX384729B (es) 2025-03-14
RU2749043C2 (ru) 2021-06-03
EP3548031B1 (en) 2023-07-19
EP3548031A4 (en) 2020-06-03
AU2017367714A1 (en) 2019-05-16
MX2019006449A (es) 2019-09-10
BR112019011074A2 (pt) 2019-08-20
AU2017367714B2 (en) 2020-11-12
RU2019116590A (ru) 2021-01-11
BR112019011074B1 (pt) 2021-01-19
JP2020500866A (ja) 2020-01-16
US10934312B2 (en) 2021-03-02
EP3548031A1 (en) 2019-10-09
KR20190086017A (ko) 2019-07-19
CA3042314A1 (en) 2018-06-07
WO2018102634A1 (en) 2018-06-07
RU2019116590A3 (https=) 2021-01-26

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Application publication date: 20190726