EA201300186A1 - Бициклические азагетероциклические карбоксамиды - Google Patents

Бициклические азагетероциклические карбоксамиды

Info

Publication number
EA201300186A1
EA201300186A1 EA201300186A EA201300186A EA201300186A1 EA 201300186 A1 EA201300186 A1 EA 201300186A1 EA 201300186 A EA201300186 A EA 201300186A EA 201300186 A EA201300186 A EA 201300186A EA 201300186 A1 EA201300186 A1 EA 201300186A1
Authority
EA
Eurasian Patent Office
Prior art keywords
bicyclic
carbosamides
azageterocyclic
preparation
accordance
Prior art date
Application number
EA201300186A
Other languages
English (en)
Other versions
EA023132B1 (ru
Inventor
Бейард Р. Хак
Константин Неагу
Рейнальдо С. Джонс
Лизбет Селест Деселм
Юфан Сяо
Сриниваса Р. Карра
Руокси Лань
Игорь Мочалкин
Аманда Э. Саттон
Томас Э. Ричардсон
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 EA201300186A1 publication Critical patent/EA201300186A1/ru
Publication of EA023132B1 publication Critical patent/EA023132B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • 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
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (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)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Изобретение обеспечивает новые соединения бициклических азагетероциклических карбоксамидов в соответствии с указанной ниже формулой (I), их получение и применение для лечения гиперпролиферативных заболеваний, таких как злокачественное новообразование
EA201300186A 2010-07-29 2011-07-01 Бициклические азагетероциклические карбоксамиды EA023132B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36896410P 2010-07-29 2010-07-29
PCT/EP2011/003272 WO2012013282A1 (en) 2010-07-29 2011-07-01 Bicyclic azaheterocyclic carboxamides as inhibitors of the kinase p70s6k

Publications (2)

Publication Number Publication Date
EA201300186A1 true EA201300186A1 (ru) 2013-12-30
EA023132B1 EA023132B1 (ru) 2016-04-29

Family

ID=44532723

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201300186A EA023132B1 (ru) 2010-07-29 2011-07-01 Бициклические азагетероциклические карбоксамиды

Country Status (19)

Country Link
US (1) US8710044B2 (ru)
EP (1) EP2598492B1 (ru)
JP (1) JP5894157B2 (ru)
KR (1) KR101852644B1 (ru)
CN (1) CN103003250B (ru)
AR (1) AR082414A1 (ru)
AU (1) AU2011285247B2 (ru)
BR (1) BR112013002090A2 (ru)
CA (1) CA2806610C (ru)
CL (1) CL2013000263A1 (ru)
EA (1) EA023132B1 (ru)
ES (1) ES2557383T3 (ru)
HK (1) HK1183302A1 (ru)
IL (1) IL224072A (ru)
MX (1) MX2013001054A (ru)
NZ (1) NZ604379A (ru)
SG (1) SG187166A1 (ru)
UA (1) UA110113C2 (ru)
WO (1) WO2012013282A1 (ru)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
MX2012012204A (es) 2010-04-22 2012-12-05 Vertex Pharma Proceso para producir compuestos de cicloalquilcarboxamido-indol.
SG186199A1 (en) * 2010-07-29 2013-01-30 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
WO2012069146A1 (en) * 2010-11-24 2012-05-31 Merck Patent Gmbh Quinazoline carboxamide azetidines
ES2646759T3 (es) 2011-09-12 2017-12-15 Merck Patent Gmbh Derivados de aminopirimidina para uso como moduladores de la actividad de la quinasa
SI2755965T1 (sl) 2011-09-12 2017-12-29 Merck Patent Gmbh Novi imidazolni amidi kot modulatorji kinazne aktivnosti
AR093512A1 (es) 2012-11-16 2015-06-10 Merck Patent Gmbh Derivados heterociclicos como moduladores de la actividad de cinasas
AU2013344549B2 (en) 2012-11-16 2018-03-08 Xiaoling Chen Novel imidazol-piperidinyl derivatives as modulators of kinase activity
BR112015011974A8 (pt) 2012-11-29 2019-10-08 Merck Patent Gmbh derivados de azaquinazolina carboxamida, seus usos e processo para sua produção, medicamento e composição farmacêutica
BR112015021324A2 (pt) 2013-03-11 2017-07-18 Merck Patent Gmbh derivados de 6-[4-(1h-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de atividade de quinase
CN103232401B (zh) * 2013-04-12 2015-11-04 浙江工业大学 一种4-芳硫基喹唑啉类化合物的合成方法
CN103254141B (zh) * 2013-04-26 2016-02-24 浙江工业大学 4-[4-(2-二丙氨基乙酰氨基)苯胺基]-6-取代喹唑啉类化合物及制备和应用
EP3125935B1 (en) 2014-04-03 2019-10-23 Merck Patent GmbH Combinations of cancer therapeutics
CN110840847B (zh) 2014-04-15 2022-07-29 沃泰克斯药物股份有限公司 用于治疗囊性纤维化跨膜传导调节因子介导的疾病的药物组合物
CN116322773A (zh) * 2020-04-21 2023-06-23 马萨诸塞大学 用于治疗年龄相关性黄斑变性的方法和组合物
CA3201799A1 (en) 2020-11-16 2022-05-19 Merck Patent Gmbh Kinase inhibitor combinations for cancer treatment
WO2023039068A1 (en) * 2021-09-08 2023-03-16 Neubase Therapeutics, Inc. Compositions and methods for synthesis of peptide nucleic acid intermediates

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9613021D0 (en) * 1996-06-21 1996-08-28 Pharmacia Spa Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors
AR016817A1 (es) * 1997-08-14 2001-08-01 Smithkline Beecham Plc Derivados de fenilurea o feniltiourea, procedimiento para su preparacion, coleccion de compuestos, compuestos intermediarios, composicion farmaceutica,metodo de tratamiento y uso de dichos compuestos para la manufactura de un medicamento
DE60144322D1 (de) * 2000-04-27 2011-05-12 Astellas Pharma Inc Kondensierte heteroarylderivate
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
WO2004014873A1 (ja) * 2002-08-09 2004-02-19 Kyorin Pharmaceutical Co., Ltd. 4-置換キナゾリン-8-カルボン酸アミド誘導体とその薬理上許容される付加塩
AU2003252315A1 (en) * 2002-08-09 2004-02-25 Kyorin Pharmaceutical Co., Ltd. 4-substituted-quinoline-8-carboxylic amide derivatives and pharmacologically acceptable addition salts thereof
JP2006522124A (ja) 2003-04-03 2006-09-28 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼのインヒビターとして有用な組成物
JP2007507531A (ja) 2003-09-30 2007-03-29 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
AU2004283751B2 (en) 2003-10-24 2011-05-19 Exelixis, Inc. p70S6 kinase modulators and method of use
EP1687305B1 (en) 2003-11-21 2008-07-09 Novartis AG 1h-imidazoquinoline derivatives as protein kinase inhibitors
EP1694331B8 (en) 2003-12-09 2010-02-24 THE GOVERNMENT OF THE UNITED STATES OF AMERICA as represented by THE SECRETARY of the DEPARTMENT OF HEALTH AND HUMAN SERVICES Methods for suppressing an immune response or treating a proliferating disorder
AU2005249380C1 (en) 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
CA2569404A1 (en) 2004-06-04 2005-12-22 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof
WO2006071819A1 (en) 2004-12-28 2006-07-06 Exelixis, Inc. [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
US8343953B2 (en) 2005-06-22 2013-01-01 Astex Therapeutics Limited Pharmaceutical compounds
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
CA2751886C (en) * 2009-02-11 2017-08-29 Merck Patent Gmbh Novel amino azaheterocyclic carboxamides

Also Published As

Publication number Publication date
EP2598492B1 (en) 2015-10-28
EP2598492A1 (en) 2013-06-05
JP2013532668A (ja) 2013-08-19
US20130137677A1 (en) 2013-05-30
KR20130096714A (ko) 2013-08-30
SG187166A1 (en) 2013-02-28
NZ604379A (en) 2015-01-30
US8710044B2 (en) 2014-04-29
AU2011285247B2 (en) 2016-08-04
HK1183302A1 (zh) 2013-12-20
WO2012013282A8 (en) 2012-03-29
CA2806610A1 (en) 2012-02-02
AU2011285247A1 (en) 2013-03-14
EA023132B1 (ru) 2016-04-29
AR082414A1 (es) 2012-12-05
IL224072A0 (en) 2013-03-05
JP5894157B2 (ja) 2016-03-23
CN103003250B (zh) 2016-02-17
CA2806610C (en) 2018-08-28
WO2012013282A1 (en) 2012-02-02
MX2013001054A (es) 2013-02-21
ES2557383T3 (es) 2016-01-25
CL2013000263A1 (es) 2013-09-06
CN103003250A (zh) 2013-03-27
IL224072A (en) 2016-02-29
KR101852644B1 (ko) 2018-04-26
BR112013002090A2 (pt) 2016-05-24
UA110113C2 (xx) 2015-11-25

Similar Documents

Publication Publication Date Title
EA201300186A1 (ru) Бициклические азагетероциклические карбоксамиды
EA201101182A1 (ru) Новые аминоазагетероциклические карбоксамиды
EA201200218A1 (ru) Новые бициклические соединения мочевины
EA201300610A1 (ru) Хиназолинкарбоксамидазетидины
EA201200247A1 (ru) Новые азагетероциклические соединения
EA201291143A1 (ru) Пиразолилхиназолиновые ингибиторы киназы
EA201290909A1 (ru) Химические соединения
EA201500314A1 (ru) Лекарственные формы энзалутамида
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
EA201400339A1 (ru) Новые имидазоламины в качестве модуляторов киназной активности
EA201391106A1 (ru) Новые гетероциклические производные
CR20130045A (es) Compuestos terapéuticos
EA201270722A1 (ru) Формы рифаксимина и их применение
EA201370018A1 (ru) Составы рифаксимина и их применение
EA201692166A1 (ru) Гетероциклические ингибиторы глютаминазы
EA201270257A1 (ru) Производные n1-сульфонил-5-фторпиримидинона
EA201590281A1 (ru) Новые гетероарильные и гетероциклические соединения, их композиции и способы
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
EA201391285A1 (ru) Производные тетрагидрохинолина, полезные в качестве ингибиторов бромодомена
EA201201670A1 (ru) Циклический амин-азагетероциклический карбоксамид
EA201390682A1 (ru) Спирооксиндольные антагонисты mdm2
EA201100296A1 (ru) Новые фениламино-изоникотинамидные соединения
EA201270808A1 (ru) Новые формы рифаксимина и их применение
MX348451B (es) Derivados de n-[(1h-pirazol-1-il)aril]-1h-indol o 1h-indazol-3-carboxamida, su preparación y su uso como antagonistas p2y12.
EA201401062A1 (ru) Бициклические пиразиноновые производные

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU