WO2019070167A8 - Ингибиторы рецептора эпидермального фактора роста - Google Patents

Ингибиторы рецептора эпидермального фактора роста Download PDF

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Publication number
WO2019070167A8
WO2019070167A8 PCT/RU2018/050122 RU2018050122W WO2019070167A8 WO 2019070167 A8 WO2019070167 A8 WO 2019070167A8 RU 2018050122 W RU2018050122 W RU 2018050122W WO 2019070167 A8 WO2019070167 A8 WO 2019070167A8
Authority
WO
WIPO (PCT)
Prior art keywords
growth factor
factor receptor
epidermal growth
receptor inhibitors
egfr
Prior art date
Application number
PCT/RU2018/050122
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English (en)
French (fr)
Other versions
WO2019070167A1 (ru
Inventor
Кирилл Вадимович ЗАВЬЯЛОВ
Светлана Леонидовна ГОРБУНОВА
Артем Евгеньевич ШЕХОВЦОВ
Мария Андреевна КАСАТКИНА
Дарья Дмитриевна БЕКЕТОВА
Наталья Владимировна КОЖЕМЯКИНА
Кирилл Игоревич КУЛИШ
Елена Александровна МАКСИМЕНКО
Марина Викторовна МЕЛЕШИНА
Ольга Анатольевна МЕЛЬЧАЕВА
Алексей Леонидович МИНДИЧ
Дмитрий Валентинович МОРОЗОВ
Александра Владимировна ПОПКОВА
Илья Алексеевич СМЕТАНИН
Сергей Александрович СИЛОНОВ
Ярославна Александровна СОЛДАТОВА
Георгий Викторович ЯКОБСОН
Original Assignee
Закрытое Акционерное Общество "Биокад"
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
Priority claimed from RU2017135686A external-priority patent/RU2017135686A/ru
Priority claimed from RU2018134159A external-priority patent/RU2786524C2/ru
Priority to CA3078602A priority Critical patent/CA3078602A1/en
Priority to BR112020006805-5A priority patent/BR112020006805A2/pt
Priority to KR1020207012890A priority patent/KR20200067856A/ko
Priority to CN201880078961.0A priority patent/CN111511727A/zh
Priority to JP2020519708A priority patent/JP2020536113A/ja
Priority to MX2020004025A priority patent/MX2020004025A/es
Priority to EA202090877A priority patent/EA202090877A1/ru
Priority to EP18864310.0A priority patent/EP3693365A4/en
Application filed by Закрытое Акционерное Общество "Биокад" filed Critical Закрытое Акционерное Общество "Биокад"
Priority to JOP/2020/0079A priority patent/JOP20200079A1/ar
Priority to US16/753,847 priority patent/US20200339544A1/en
Priority to MA49606A priority patent/MA49606B1/fr
Priority to AU2018346119A priority patent/AU2018346119A1/en
Publication of WO2019070167A1 publication Critical patent/WO2019070167A1/ru
Publication of WO2019070167A8 publication Critical patent/WO2019070167A8/ru
Priority to CONC2020/0004201A priority patent/CO2020004201A2/es
Priority to PH12020550228A priority patent/PH12020550228A1/en
Priority to ZA2020/02041A priority patent/ZA202002041B/en

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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further 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
    • A61K31/435—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
    • 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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/535—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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

Abstract

Настоящая группа изобретений относится к новым соединениям формулы (I), их солям, сольватам или стереоизомерам, а также к фармацевтической композиции, способу ингибирования биологической активности рецептора эпидермального фактора роста (EFGR), способу лечения заболеваний или нарушений, опосредованных активностью EFGR, и применении заявляемых соединений или указанной композиции для лечения заболевания или нарушения, опосредованного активностью EFGR.
PCT/RU2018/050122 2017-10-06 2018-10-05 Ингибиторы рецептора эпидермального фактора роста WO2019070167A1 (ru)

Priority Applications (15)

Application Number Priority Date Filing Date Title
MA49606A MA49606B1 (fr) 2017-10-06 2018-10-05 Inhibiteurs du récepteur de facteur de croissance épidermique
AU2018346119A AU2018346119A1 (en) 2017-10-06 2018-10-05 Epidermal growth factor receptor inhibitors
JOP/2020/0079A JOP20200079A1 (ar) 2017-10-06 2018-10-05 مثبطات مستقبل عامل نمو البشرة
KR1020207012890A KR20200067856A (ko) 2017-10-06 2018-10-05 상피 성장 인자 수용체 저해제
CN201880078961.0A CN111511727A (zh) 2017-10-06 2018-10-05 表皮生长因子受体抑制剂
JP2020519708A JP2020536113A (ja) 2017-10-06 2018-10-05 上皮成長因子受容体阻害剤
MX2020004025A MX2020004025A (es) 2017-10-06 2018-10-05 Inhibidor del receptor del factor de crecimiento epidermico.
EA202090877A EA202090877A1 (ru) 2018-09-28 2018-10-05 Ингибиторы рецептора эпидермального фактора роста
EP18864310.0A EP3693365A4 (en) 2017-10-06 2018-10-05 EPIDERMAL GROWTH FACTOR RECEPTOR INHIBITORS
CA3078602A CA3078602A1 (en) 2017-10-06 2018-10-05 Epidermal growth factor receptor inhibitors
BR112020006805-5A BR112020006805A2 (pt) 2017-10-06 2018-10-05 inibidor do receptor de fator de crescimento epidérmico
US16/753,847 US20200339544A1 (en) 2017-10-06 2018-10-05 Epidermal growth factor receptor inhibitors
CONC2020/0004201A CO2020004201A2 (es) 2017-10-06 2020-04-03 Inhibidor del receptor del factor de crecimiento epidérmico
PH12020550228A PH12020550228A1 (en) 2017-10-06 2020-04-06 Epidermal growth factor receptor inhibitors
ZA2020/02041A ZA202002041B (en) 2017-10-06 2020-05-04 Epidermal growth factor receptor inhibitors

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
RU2017135686A RU2017135686A (ru) 2017-10-06 2017-10-06 Ингибиторы рецептора эпидермального фактора роста
RU2017135686 2017-10-06
RU2018134159A RU2786524C2 (ru) 2018-09-28 Ингибиторы рецептора эпидермального фактора роста
RU2018134159 2018-09-28

Publications (2)

Publication Number Publication Date
WO2019070167A1 WO2019070167A1 (ru) 2019-04-11
WO2019070167A8 true WO2019070167A8 (ru) 2019-05-16

Family

ID=65995204

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU2018/050122 WO2019070167A1 (ru) 2017-10-06 2018-10-05 Ингибиторы рецептора эпидермального фактора роста

Country Status (17)

Country Link
US (1) US20200339544A1 (ru)
EP (1) EP3693365A4 (ru)
JP (1) JP2020536113A (ru)
KR (1) KR20200067856A (ru)
CN (1) CN111511727A (ru)
AU (1) AU2018346119A1 (ru)
BR (1) BR112020006805A2 (ru)
CA (1) CA3078602A1 (ru)
CL (1) CL2020000933A1 (ru)
CO (1) CO2020004201A2 (ru)
JO (1) JOP20200079A1 (ru)
MX (1) MX2020004025A (ru)
PH (1) PH12020550228A1 (ru)
TW (1) TWI702205B (ru)
UY (1) UY37921A (ru)
WO (1) WO2019070167A1 (ru)
ZA (1) ZA202002041B (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112513029B (zh) * 2019-06-21 2023-10-24 上海翰森生物医药科技有限公司 含氮芳基磷氧化物类衍生物、其制备方法和应用
CA3201333A1 (en) 2020-11-11 2022-05-19 Bayer Aktiengesellschaft N-[2-({4-[3-(anilino)-4-oxo-4,5,6,7-tetrahydro-1h-pyrrolo[3,2-c]pyridin-2-yl]pyridin-3-yl)oxy)ethyl]prop-2-enamide derivatives and similar compounds as egfr inhibitors for the treatment of cancer
WO2023213882A1 (en) 2022-05-04 2023-11-09 Bayer Aktiengesellschaft Irreversible mutegfr inhibitors
WO2024028316A1 (en) 2022-08-02 2024-02-08 Bayer Aktiengesellschaft 1h-pyrrolo[3,2-b]pyridine derivatives as irreversible inhibitors of mutant egfr for the treatment of cancer

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GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
KR19990082463A (ko) 1996-02-13 1999-11-25 돈 리사 로얄 혈관 내피 성장 인자 억제제로서의 퀴나졸린유도체
WO1997032856A1 (en) 1996-03-05 1997-09-12 Zeneca Limited 4-anilinoquinazoline derivatives
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
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EP1289952A1 (en) 2000-05-31 2003-03-12 AstraZeneca AB Indole derivatives with vascular damaging activity
SK52003A3 (en) 2000-07-07 2003-07-01 Angiogene Pharm Ltd Colchinol derivatives as angiogenesis inhibitors, method for their preparation and pharmaceutical composition comprising the same
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US20110207736A1 (en) * 2009-12-23 2011-08-25 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
WO2011140338A1 (en) * 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CN104140418B (zh) * 2014-08-15 2016-08-24 常州润诺生物科技有限公司 2-(2，4，5-取代苯胺)嘧啶衍生物及其用途
CN111171000B (zh) * 2014-10-11 2023-09-01 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用

Also Published As

Publication number Publication date
TW201922709A (zh) 2019-06-16
BR112020006805A2 (pt) 2020-10-06
CN111511727A (zh) 2020-08-07
CO2020004201A2 (es) 2020-04-24
CA3078602A1 (en) 2019-04-11
PH12020550228A1 (en) 2021-02-08
ZA202002041B (en) 2022-11-30
TWI702205B (zh) 2020-08-21
EP3693365A1 (en) 2020-08-12
JOP20200079A1 (ar) 2020-04-30
AU2018346119A1 (en) 2020-05-14
UY37921A (es) 2019-04-30
US20200339544A1 (en) 2020-10-29
JP2020536113A (ja) 2020-12-10
MX2020004025A (es) 2020-08-13
KR20200067856A (ko) 2020-06-12
WO2019070167A1 (ru) 2019-04-11
CL2020000933A1 (es) 2020-10-16
EP3693365A4 (en) 2021-05-05

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