EA201792187A1 - Производные азахиназолин карбоксамида - Google Patents

Производные азахиназолин карбоксамида

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Publication number
EA201792187A1
EA201792187A1 EA201792187A EA201792187A EA201792187A1 EA 201792187 A1 EA201792187 A1 EA 201792187A1 EA 201792187 A EA201792187 A EA 201792187A EA 201792187 A EA201792187 A EA 201792187A EA 201792187 A1 EA201792187 A1 EA 201792187A1
Authority
EA
Eurasian Patent Office
Prior art keywords
carboxamide
derivatives
azazhinazolin
azahinazoline
novel
Prior art date
Application number
EA201792187A
Other languages
English (en)
Other versions
EA033655B1 (ru
Inventor
Бейярд Р. Хак
Руокси Лань
Джастин Потник
Лизбет Селест Дизелм
Марк У. Джр. Кронин
Константин Неагу
Сяолин Чэнь
Рок Буавен
Тереса Л. Джонсон
Андреас Гоутопоулос
Original Assignee
Мерк Патент Гмбх
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 Патент Гмбх filed Critical Мерк Патент Гмбх
Publication of EA201792187A1 publication Critical patent/EA201792187A1/ru
Publication of EA033655B1 publication Critical patent/EA033655B1/ru

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    • 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/08—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 condensed with carbocyclic rings or ring systems
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Новые производные азахиназолин карбоксамида формулы (I)где W, W, W, W, R, R, Rи m имеют значения, определенные выше, представляют собой p70S6K ингибитор и могут применяться, в частности, для лечения гиперпролиферативных нарушений.
EA201792187A 2012-11-29 2013-11-27 Производные азахиназолин карбоксамида EA033655B1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261731075P 2012-11-29 2012-11-29

Publications (2)

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EA201792187A1 true EA201792187A1 (ru) 2018-02-28
EA033655B1 EA033655B1 (ru) 2019-11-13

Family

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EA201792187A EA033655B1 (ru) 2012-11-29 2013-11-27 Производные азахиназолин карбоксамида
EA201500573A EA029144B1 (ru) 2012-11-29 2013-11-27 Производные азахиназолин карбоксамида

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Country Status (19)

Country Link
US (3) US9440968B2 (ru)
EP (1) EP2925747B1 (ru)
JP (1) JP6290917B2 (ru)
KR (1) KR20150090044A (ru)
CN (1) CN105793254B (ru)
AU (1) AU2013352261B2 (ru)
BR (1) BR112015011974A8 (ru)
CA (1) CA2887539C (ru)
CL (1) CL2015001187A1 (ru)
EA (2) EA033655B1 (ru)
ES (1) ES2821102T3 (ru)
IL (2) IL239054B (ru)
MX (1) MX2015006516A (ru)
NZ (1) NZ706418A (ru)
PE (1) PE20151782A1 (ru)
PH (2) PH12015500712B1 (ru)
SG (2) SG11201502503RA (ru)
UA (1) UA115154C2 (ru)
WO (1) WO2014085528A1 (ru)

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CA2887539C (en) * 2012-11-29 2021-10-26 Merck Patent Gmbh Azaquinazoline carboxamide derivatives
AU2016329513B2 (en) 2015-10-02 2020-09-03 Sentinel Oncology Limited 2-Aminoquinazoline derivatives as p70S6 kinase inhibitors
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
CN114630825A (zh) 2019-11-01 2022-06-14 先正达农作物保护股份公司 杀有害生物活性的稠合二环杂芳香族化合物
CA3221180A1 (en) 2021-06-24 2022-12-29 Syngenta Crop Protection Ag 2-[3-[1 [(quinazolin-4-yl)amino]ethyl]pyrazin-2-yl]thiazole-5-carbonitrile derivatives and similar compounds as pesticides
WO2023247360A1 (en) 2022-06-21 2023-12-28 Syngenta Crop Protection Ag Pesticidally active fused bicyclic heteroaromatic compounds
CN117304182A (zh) * 2022-06-22 2023-12-29 上海海和药物研究开发股份有限公司 一类具有嘧啶并六元环结构的化合物、包含其的药物组合物及其应用

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UA110113C2 (xx) * 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
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CA2887539C (en) * 2012-11-29 2021-10-26 Merck Patent Gmbh Azaquinazoline carboxamide derivatives

Also Published As

Publication number Publication date
PH12016502534A1 (en) 2017-11-20
EA029144B1 (ru) 2018-02-28
BR112015011974A8 (pt) 2019-10-08
PH12016502534B1 (en) 2017-11-20
SG11201502503RA (en) 2015-04-29
CN105793254A (zh) 2016-07-20
EP2925747A1 (en) 2015-10-07
WO2014085528A1 (en) 2014-06-05
US20180237402A1 (en) 2018-08-23
PE20151782A1 (es) 2015-12-02
CA2887539C (en) 2021-10-26
US20160340323A1 (en) 2016-11-24
US10233160B2 (en) 2019-03-19
EA033655B1 (ru) 2019-11-13
EA201500573A1 (ru) 2016-02-29
KR20150090044A (ko) 2015-08-05
US9981925B2 (en) 2018-05-29
MX2015006516A (es) 2015-08-14
IL239054A0 (en) 2015-07-30
US9440968B2 (en) 2016-09-13
EP2925747B1 (en) 2020-06-24
IL256646B (en) 2020-03-31
NZ706418A (en) 2019-09-27
CL2015001187A1 (es) 2015-08-28
AU2013352261A1 (en) 2015-04-23
US20150259339A1 (en) 2015-09-17
PH12015500712A1 (en) 2015-05-18
PH12015500712B1 (en) 2015-05-18
JP2016501229A (ja) 2016-01-18
CN105793254B (zh) 2020-10-23
IL239054B (en) 2021-04-29
JP6290917B2 (ja) 2018-03-07
SG10201800741QA (en) 2018-03-28
IL256646A (en) 2018-02-28
AU2013352261B2 (en) 2018-05-10
BR112015011974A2 (pt) 2017-07-11
CA2887539A1 (en) 2014-06-05
ES2821102T3 (es) 2021-04-23
UA115154C2 (uk) 2017-09-25

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