RU2749043C2 - Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич - Google Patents

Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич Download PDF

Info

Publication number
RU2749043C2
RU2749043C2 RU2019116590A RU2019116590A RU2749043C2 RU 2749043 C2 RU2749043 C2 RU 2749043C2 RU 2019116590 A RU2019116590 A RU 2019116590A RU 2019116590 A RU2019116590 A RU 2019116590A RU 2749043 C2 RU2749043 C2 RU 2749043C2
Authority
RU
Russia
Prior art keywords
int
mmol
enantiomer
compound
mixture
Prior art date
Application number
RU2019116590A
Other languages
English (en)
Russian (ru)
Other versions
RU2019116590A3 (enExample
RU2019116590A (ru
Inventor
Томас Х. ГРЭХЭМ
Тао Юй
Шерман Т. УОДДЕЛЛ
Джон А. МАККОЛИ
Original Assignee
Мерк Шарп И Доум Корп.
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 Мерк Шарп И Доум Корп. filed Critical Мерк Шарп И Доум Корп.
Publication of RU2019116590A publication Critical patent/RU2019116590A/ru
Publication of RU2019116590A3 publication Critical patent/RU2019116590A3/ru
Application granted granted Critical
Publication of RU2749043C2 publication Critical patent/RU2749043C2/ru

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
    • C07D498/16—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
    • A61K31/53—Heterocyclic 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
    • 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
    • A61K31/33—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
    • A61K31/5395—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 having two or more nitrogen atoms in the same ring, e.g. oxadiazines
    • 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
    • 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
    • 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
    • C07D491/22—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 four or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
RU2019116590A 2016-12-02 2017-12-01 Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич RU2749043C2 (ru)

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 (3)

Publication Number Publication Date
RU2019116590A RU2019116590A (ru) 2021-01-11
RU2019116590A3 RU2019116590A3 (enExample) 2021-01-26
RU2749043C2 true RU2749043C2 (ru) 2021-06-03

Family

ID=62242756

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2019116590A RU2749043C2 (ru) 2016-12-02 2017-12-01 Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич

Country Status (11)

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

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11202011386QA (en) 2018-05-31 2020-12-30 Shionogi & Co Polycyclic pyridone derivative
IL313474A (en) 2018-05-31 2024-08-01 Shionogi & Co Polycyclic carbamoylpyridone derivative
WO2019236396A1 (en) 2018-06-05 2019-12-12 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as hiv integrase inhibitors
HUE059677T2 (hu) 2019-03-22 2022-12-28 Gilead Sciences Inc Áthidalt triciklusos karbamoilpiridon-vegyületek és ezek gyógyszerészeti alkalmazása
CR20220418A (es) 2020-02-24 2022-10-10 Gilead Sciences Inc Compuestos tetracíclicos para el tratamiento de infecciones por vih
CN112047945B (zh) * 2020-09-10 2021-11-12 浙江大学 螺环吡啶酮衍生物及应用
JP7691494B2 (ja) 2020-09-30 2025-06-11 ギリアード サイエンシーズ， インコーポレイテッド 架橋三環式カルバモイルピリドン化合物及びその使用
LT4196479T (lt) 2021-01-19 2023-12-11 Gilead Sciences, Inc. Pakeistieji piridotriazino junginiai ir jų panaudojimo būdai
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA200801144A1 (ru) * 2005-10-27 2008-10-30 Сионоги Энд Ко., Лтд. Полициклическое карбамоилпиридоновое производное, обладающее ингибиторной активностью в отношении интегразы вич
WO2014099586A1 (en) * 2012-12-17 2014-06-26 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
WO2014200880A1 (en) * 2013-06-13 2014-12-18 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
WO2016191239A1 (en) * 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE15187654T1 (de) 2001-08-10 2016-12-01 Shionogi & Co., Ltd Antivirales Mittel
US7169780B2 (en) 2001-10-26 2007-01-30 Istitute Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
AU2002334205B2 (en) 2001-10-26 2007-07-05 Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
US7279487B2 (en) 2002-01-17 2007-10-09 Merck & Co., Inc. Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors
EP1509537B9 (en) 2002-04-26 2007-11-14 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such
AU2003292436B2 (en) 2002-12-27 2009-07-30 Msd Italia S.R.L. Tetrahydro-4H-pyrido[1,2-A]pyrimidines and related compounds useful as HIV integrase inhibitors
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
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
US7176196B2 (en) 2004-05-28 2007-02-13 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
EP1866313A1 (en) 2005-03-31 2007-12-19 Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. Hiv integrase inhibitors
KR101580310B1 (ko) 2005-04-28 2016-01-04 비이브 헬쓰케어 컴퍼니 Ｈｉｖ 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체
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
CA2777664C (en) 2009-10-13 2014-06-10 Johannes Wilhelmus J. Thuring Macrocyclic integrase inhibitors
CN102958935B (zh) 2010-04-02 2015-12-09 爱尔兰詹森科学公司 大环整合酶抑制剂
EP2986291B1 (en) * 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof 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
WO2017113288A1 (en) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA200801144A1 (ru) * 2005-10-27 2008-10-30 Сионоги Энд Ко., Лтд. Полициклическое карбамоилпиридоновое производное, обладающее ингибиторной активностью в отношении интегразы вич
US20120208998A1 (en) * 2005-10-27 2012-08-16 Hiroshi Yoshida Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity
WO2014099586A1 (en) * 2012-12-17 2014-06-26 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
WO2014200880A1 (en) * 2013-06-13 2014-12-18 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
WO2016191239A1 (en) * 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
T. Kawasuji et al. "Carbamoyl Pyridone HIV-1 Integrase Inhibitors. 2. Bi- and Tricyclic Derivatives Result in Superior Antiviralang Pharmacokinetic Profiles" Journal of Medicinal Chemistry, vol. 56, 2013, 1124-1135. *

Also Published As

Publication number Publication date
RU2019116590A3 (enExample) 2021-01-26
BR112019011074B1 (pt) 2021-01-19
EP3548031A1 (en) 2019-10-09
BR112019011074A2 (pt) 2019-08-20
EP3548031A4 (en) 2020-06-03
CN110062627A (zh) 2019-07-26
AU2017367714A1 (en) 2019-05-16
US10934312B2 (en) 2021-03-02
RU2019116590A (ru) 2021-01-11
KR20190086017A (ko) 2019-07-19
WO2018102634A1 (en) 2018-06-07
EP3548031B1 (en) 2023-07-19
MX2019006449A (es) 2019-09-10
JP2020500866A (ja) 2020-01-16
AU2017367714B2 (en) 2020-11-12
MX384729B (es) 2025-03-14
CA3042314A1 (en) 2018-06-07
US20200017524A1 (en) 2020-01-16

Similar Documents

Publication Publication Date Title
RU2749043C2 (ru) Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич
EP3008044B1 (en) Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
EP3083641B1 (en) Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
EP3229805B1 (en) Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
US10233193B2 (en) Fused tricyclic heterocyclic compounds useful for treating HIV infection
RU2740187C2 (ru) Слитые трициклические гетероциклические соединения в качестве ингибиторов интегразы вич
EP3330272B1 (en) Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
EP3377065B1 (en) Spirocyclic pyridotriazine derivatives useful as hiv integrase inhibitors
US10081647B2 (en) Phosphate substituted quinolizine derivatives useful as HIV integrase inhibitors
KR102345924B1 (ko) Hiv 인테그라제 억제제로서 유용한 테트라시클릭 헤테로사이클 화합물
EP3801543B1 (en) Tricyclic heterocycle compounds useful as hiv integrase inhibitors
EP3229804A1 (en) Spirocyclic heterocycle compounds useful as hiv integrase inhibitors