EA201500573A1 - Производные азахиназолин карбоксамида - Google Patents

Производные азахиназолин карбоксамида

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Publication number
EA201500573A1
EA201500573A1 EA201500573A EA201500573A EA201500573A1 EA 201500573 A1 EA201500573 A1 EA 201500573A1 EA 201500573 A EA201500573 A EA 201500573A EA 201500573 A EA201500573 A EA 201500573A EA 201500573 A1 EA201500573 A1 EA 201500573A1
Authority
EA
Eurasian Patent Office
Prior art keywords
carboxamide
derivatives
azazhinazolin
azahinazoline
novel
Prior art date
Application number
EA201500573A
Other languages
English (en)
Other versions
EA029144B1 (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 EA201500573A1 publication Critical patent/EA201500573A1/ru
Publication of EA029144B1 publication Critical patent/EA029144B1/ru

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    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D253/00Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/08Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (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.
EA201500573A 2012-11-29 2013-11-27 Производные азахиназолин карбоксамида EA029144B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261731075P 2012-11-29 2012-11-29
PCT/US2013/072141 WO2014085528A1 (en) 2012-11-29 2013-11-27 Azaquinazoline carboxamide derivatives

Publications (2)

Publication Number Publication Date
EA201500573A1 true EA201500573A1 (ru) 2016-02-29
EA029144B1 EA029144B1 (ru) 2018-02-28

Family

ID=49759613

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201792187A EA033655B1 (ru) 2012-11-29 2013-11-27 Производные азахиназолин карбоксамида
EA201500573A EA029144B1 (ru) 2012-11-29 2013-11-27 Производные азахиназолин карбоксамида

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA201792187A EA033655B1 (ru) 2012-11-29 2013-11-27 Производные азахиназолин карбоксамида

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) PH12015500712A1 (ru)
SG (2) SG11201502503RA (ru)
UA (1) UA115154C2 (ru)
WO (1) WO2014085528A1 (ru)

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EA033655B1 (ru) * 2012-11-29 2019-11-13 Merck Patent Gmbh Производные азахиназолин карбоксамида
KR20180061318A (ko) 2015-10-02 2018-06-07 센티넬 온콜로지 리미티드 P70s6 키나제 억제제로서의 2-아미노퀴나졸린 유도체
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
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
IL291996A (en) 2019-11-01 2022-06-01 Syngenta Crop Protection Ag Fused heteroaromatic bicyclic compounds are active as pesticides
EP4359408A1 (en) 2021-06-24 2024-05-01 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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IL112249A (en) * 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL129825A0 (en) 1996-11-27 2000-02-29 Pfizer Fused bicyclic pyrimidine derivatives
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
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CA2522595A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
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EA033655B1 (ru) * 2012-11-29 2019-11-13 Merck Patent Gmbh Производные азахиназолин карбоксамида

Also Published As

Publication number Publication date
CN105793254B (zh) 2020-10-23
IL256646B (en) 2020-03-31
US20150259339A1 (en) 2015-09-17
PH12016502534A1 (en) 2017-11-20
EP2925747B1 (en) 2020-06-24
PE20151782A1 (es) 2015-12-02
EA033655B1 (ru) 2019-11-13
IL239054A0 (en) 2015-07-30
PH12016502534B1 (en) 2017-11-20
JP6290917B2 (ja) 2018-03-07
CA2887539A1 (en) 2014-06-05
US20180237402A1 (en) 2018-08-23
CN105793254A (zh) 2016-07-20
CL2015001187A1 (es) 2015-08-28
CA2887539C (en) 2021-10-26
US9440968B2 (en) 2016-09-13
AU2013352261B2 (en) 2018-05-10
PH12015500712B1 (en) 2015-05-18
AU2013352261A1 (en) 2015-04-23
SG11201502503RA (en) 2015-04-29
BR112015011974A8 (pt) 2019-10-08
MX2015006516A (es) 2015-08-14
NZ706418A (en) 2019-09-27
IL256646A (en) 2018-02-28
US10233160B2 (en) 2019-03-19
EP2925747A1 (en) 2015-10-07
US9981925B2 (en) 2018-05-29
UA115154C2 (uk) 2017-09-25
EA029144B1 (ru) 2018-02-28
US20160340323A1 (en) 2016-11-24
KR20150090044A (ko) 2015-08-05
WO2014085528A1 (en) 2014-06-05
SG10201800741QA (en) 2018-03-28
ES2821102T3 (es) 2021-04-23
PH12015500712A1 (en) 2015-05-18
BR112015011974A2 (pt) 2017-07-11
JP2016501229A (ja) 2016-01-18
IL239054B (en) 2021-04-29
EA201792187A1 (ru) 2018-02-28

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