EA201690513A1 - Комбинация ингибитора mek и ингибитора erk для применения в лечении гиперпролиферативных заболеваний - Google Patents

Комбинация ингибитора mek и ингибитора erk для применения в лечении гиперпролиферативных заболеваний

Info

Publication number
EA201690513A1
EA201690513A1 EA201690513A EA201690513A EA201690513A1 EA 201690513 A1 EA201690513 A1 EA 201690513A1 EA 201690513 A EA201690513 A EA 201690513A EA 201690513 A EA201690513 A EA 201690513A EA 201690513 A1 EA201690513 A1 EA 201690513A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitor
treatment
combination
hyperproliferative diseases
erk
Prior art date
Application number
EA201690513A
Other languages
English (en)
Other versions
EA034872B1 (ru
Inventor
Марсия Белвин
Джон Моффэт
Марк Мёрчант
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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 Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of EA201690513A1 publication Critical patent/EA201690513A1/ru
Publication of EA034872B1 publication Critical patent/EA034872B1/ru

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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/495—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
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Abstract

Согласно изобретению предложены комбинации, содержащие ингибитор MEK (такой как GDC-0973 или GDC-0623) или его фармацевтически приемлемую соль и ингибитор ERK (такой как GDC-0994). Данные комбинации являются особенно полезными для лечения гиперпролиферативных расстройств, таких как рак.
EA201690513A 2013-09-05 2014-09-04 Комбинация ингибитора mek кобиметиниба и ингибитора erk (s)-1-(1-(4-хлор-3-фторфенил)-2-гидроксиэтил)-4-(2-((1-метил-1h-пиразол-5-ил)амино)пиримидин-4-ил)пиридин-2(1h)-она для применения в лечении раковых заболеваний EA034872B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361874206P 2013-09-05 2013-09-05
PCT/EP2014/068776 WO2015032840A1 (en) 2013-09-05 2014-09-04 Combination of a mek inhibitor and an erk inhibitor for use in treatment of hyperproliferative diseases

Publications (2)

Publication Number Publication Date
EA201690513A1 true EA201690513A1 (ru) 2016-07-29
EA034872B1 EA034872B1 (ru) 2020-03-31

Family

ID=51492945

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201690513A EA034872B1 (ru) 2013-09-05 2014-09-04 Комбинация ингибитора mek кобиметиниба и ингибитора erk (s)-1-(1-(4-хлор-3-фторфенил)-2-гидроксиэтил)-4-(2-((1-метил-1h-пиразол-5-ил)амино)пиримидин-4-ил)пиридин-2(1h)-она для применения в лечении раковых заболеваний

Country Status (21)

Country Link
US (1) US9532987B2 (ru)
EP (1) EP3041471A1 (ru)
JP (2) JP2016531139A (ru)
KR (1) KR20160048807A (ru)
CN (1) CN105517548B (ru)
AR (1) AR097556A1 (ru)
AU (1) AU2014317119B2 (ru)
CA (1) CA2916619A1 (ru)
CL (1) CL2016000042A1 (ru)
EA (1) EA034872B1 (ru)
HK (1) HK1218072A1 (ru)
IL (1) IL243251B (ru)
MA (1) MA38827A1 (ru)
MX (1) MX370417B (ru)
PE (1) PE20160529A1 (ru)
PH (1) PH12016500270A1 (ru)
SG (1) SG11201600989VA (ru)
TW (1) TW201605477A (ru)
UA (1) UA120423C2 (ru)
WO (1) WO2015032840A1 (ru)
ZA (1) ZA201600091B (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2857649T3 (es) * 2012-03-01 2021-09-29 Array Biopharma Inc Inhibidores de serina/treonina cinasa
KR102359759B1 (ko) 2013-12-06 2022-02-09 제넨테크, 인크. 세린/트레오닌 키나제 저해제
JP6642942B2 (ja) * 2013-12-30 2020-02-12 アレイ バイオファーマ、インコーポレイテッド セリン／トレオニンキナーゼ阻害剤
WO2016162325A1 (en) 2015-04-07 2016-10-13 Astrazeneca Ab Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors
EA038028B1 (ru) 2015-11-09 2021-06-24 Астразенека Аб Производные дигидроимидазопиразинона, применимые в лечении рака
WO2017080980A1 (en) 2015-11-09 2017-05-18 Astrazeneca Ab Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer
CN105330643B (zh) * 2015-12-09 2017-12-05 苏州明锐医药科技有限公司 卡比替尼的制备方法
CN109072311A (zh) * 2016-04-15 2018-12-21 豪夫迈·罗氏有限公司 用于癌症的诊断和治疗方法
AU2017316618A1 (en) * 2016-08-23 2019-02-07 Genentech, Inc. Combination therapy for the treatment of pancreatic cancer
AU2017363804B2 (en) * 2016-11-25 2021-12-23 Genuv Inc. Composition for promoting differentiation of and protecting neural stem cells and method for inducing neural regeneration using same
JP2019019094A (ja) * 2017-07-19 2019-02-07 学校法人福岡大学 変異ｋｒａｓ関連シグナル阻害用組成物
AU2018329925A1 (en) 2017-09-08 2020-03-05 F. Hoffmann-La Roche Ag Diagnostic and therapeutic methods for cancer
WO2019139970A1 (en) * 2018-01-09 2019-07-18 Duke University Topical administration of mek inhibiting agents for the treatment of skin disorders
WO2019158579A1 (en) 2018-02-13 2019-08-22 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
WO2021007499A1 (en) * 2019-07-11 2021-01-14 Emory University Combination therapies for managing cancer

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2006302415B2 (en) 2005-10-07 2012-09-13 Exelixis, Inc. Azetidines as MEK inhibitors for the treatment of proliferative diseases
KR101428116B1 (ko) 2006-08-21 2014-08-07 제넨테크, 인크. 아자-벤조푸라닐 화합물 및 사용 방법
CA2660963A1 (en) 2006-08-21 2008-02-28 Genentech, Inc. Aza-benzothiophenyl compounds and methods of use
ATE511509T1 (de) 2006-11-30 2011-06-15 Genentech Inc Azaindolylverbindungen und anwendungsverfahren
EP2101759B1 (en) 2006-12-14 2018-10-10 Exelixis, Inc. Methods of using mek inhibitors
WO2008157179A2 (en) 2007-06-12 2008-12-24 Genentech, Inc. N-substituted azaindoles and methods of use
CN101945870B (zh) 2007-12-19 2012-10-03 健泰科生物技术公司 5-苯氨基咪唑并吡啶和使用方法
EP2231662B1 (en) 2007-12-19 2011-06-22 Genentech, Inc. 8-anilinoimidazopyridines and their use as anti-cancer and/or anti-inflammatory agents
WO2009082687A1 (en) 2007-12-21 2009-07-02 Genentech, Inc. Azaindolizines and methods of use
BRPI0910200A2 (pt) 2008-07-01 2015-09-29 Genentech Inc composto, composição farmacêutica, método de inibir o crescimento de células anormais ou de tratar um distúrbio hiperproliferativo em um mamífero e método de tratar uma doença inflamatória em um mamífero
CN102137847B (zh) 2008-07-01 2015-06-10 健泰科生物技术公司 作为mek激酶抑制剂的二环杂环
SG10201402917XA (en) 2009-08-24 2014-08-28 Genentech Inc Determining sensitivity of cells to b-raf inhibitor treatment by detecting kras mutation and rtk expression levels
NZ599939A (en) 2009-10-12 2014-02-28 Hoffmann La Roche Combinations of a pi3k inhibitor and a mek inhibitor
SI2643322T1 (en) 2010-11-23 2018-01-31 Abbvie Inc. Salts and crystalline forms of an apoptosis induction agent
MX339873B (es) 2011-02-28 2016-06-15 Genentech Inc Inhibidores de serina/treonina cinasa.
WO2012145503A1 (en) 2011-04-21 2012-10-26 Novartis Ag Pharmaceutical combinations
CN103958502B (zh) 2011-08-04 2016-02-10 阵列生物制药公司 作为丝氨酸/苏氨酸激酶抑制剂的喹唑啉化合物
ES2857649T3 (es) 2012-03-01 2021-09-29 Array Biopharma Inc Inhibidores de serina/treonina cinasa
US20130267517A1 (en) 2012-03-31 2013-10-10 Hoffmann-La Roche Inc. Novel 4-methyl-dihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection
MX2014014308A (es) 2012-05-30 2015-02-12 Hoffmann La Roche Pirrolidino heterociclos.
SG10201913359TA (en) 2012-08-17 2020-02-27 Hoffmann La Roche Combination therapies for melanoma comprising administering cobimetinib and vemurafinib
AR092253A1 (es) 2012-08-27 2015-04-08 Array Biopharma Inc Inhibidores de serina/treonina cinasa
MA38085B1 (fr) 2012-10-12 2018-11-30 Exelixis Inc Nouveau procédé pour la production de composés à utiliser dans le traitement du cancer
EP2909206A1 (en) 2012-10-16 2015-08-26 F. Hoffmann-La Roche AG Serine/threonine kinase inhibitors
KR102359759B1 (ko) 2013-12-06 2022-02-09 제넨테크, 인크. 세린/트레오닌 키나제 저해제
WO2015103133A1 (en) 2013-12-30 2015-07-09 Genentech, Inc. Serine/threonine kinase inhibitors
JP6642942B2 (ja) 2013-12-30 2020-02-12 アレイ バイオファーマ、インコーポレイテッド セリン／トレオニンキナーゼ阻害剤
EP3129025B1 (en) 2014-04-09 2019-05-15 Genentech, Inc. Process for the manufacturing of medicaments

Also Published As

Publication number Publication date
SG11201600989VA (en) 2016-03-30
MX2016002857A (es) 2016-06-22
UA120423C2 (uk) 2019-12-10
PE20160529A1 (es) 2016-05-21
JP2019031517A (ja) 2019-02-28
EP3041471A1 (en) 2016-07-13
MX370417B (es) 2019-12-10
CN105517548A (zh) 2016-04-20
IL243251B (en) 2019-02-28
CN105517548B (zh) 2020-01-21
PH12016500270A1 (en) 2016-05-16
AR097556A1 (es) 2016-03-23
TW201605477A (zh) 2016-02-16
US9532987B2 (en) 2017-01-03
MA38827A1 (fr) 2017-10-31
HK1218072A1 (zh) 2017-02-03
WO2015032840A1 (en) 2015-03-12
US20150111869A1 (en) 2015-04-23
KR20160048807A (ko) 2016-05-04
EA034872B1 (ru) 2020-03-31
ZA201600091B (en) 2017-04-26
AU2014317119B2 (en) 2019-12-05
CL2016000042A1 (es) 2016-08-05
JP2016531139A (ja) 2016-10-06
AU2014317119A1 (en) 2016-03-03
CA2916619A1 (en) 2015-03-12

Similar Documents

Publication Publication Date Title
EA201690513A1 (ru) Комбинация ингибитора mek и ингибитора erk для применения в лечении гиперпролиферативных заболеваний
MX2016013689A (es) Compuestos 4-amino-imidazoquinolina.
EA201792205A1 (ru) Гетероциклические соединения как ингибиторы lsd1
MX2020003702A (es) Ciclopropilaminas como inhibidores de desmetilasa especifica de lisina 1 (lsd1).
EA201791420A1 (ru) Соединения триазолопиримидина и их применения
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
EA201591509A1 (ru) Ингибиторы cdc7
EA201790273A1 (ru) Флагеллиновые композиции и их применение
EA201591764A1 (ru) Варианты тканевого ингибитора металлопротеиназ третьего типа (timp-3), композиции и способы
EA202090291A2 (ru) Производные бипиразола в качестве ингибиторов jak
EP3030323A4 (en) Kdm1a inhibitors for the treatment of disease
TR201901886T4 (tr) DNA-PK inhibitörleri.
EA201500314A1 (ru) Лекарственные формы энзалутамида
EA201590987A1 (ru) Соединения и способы их применения
EA201790785A1 (ru) Производные тетрагидроизохинолина
EA201590997A1 (ru) Соединения и способы их применения
TN2015000519A1 (en) Small molecule inhibitors of fibrosis
MX2018006674A (es) Tratamiento de cancer usando 2-desoxi-2-fluoro-l-fucosa en combinacion con un inhibidor del punto de control.
TR201901348T4 (tr) Metap-2 inhibitörleri olarak pirolidinon türevleri.
EA201690039A1 (ru) Ингибиторы rorc2 и способы их применения
EA201790687A1 (ru) Хинолинкарбоксамиды для применения в лечении множественной миеломы
EA201792571A1 (ru) Терапевтическое применение l-4-хлорокинуренина
EA201692518A2 (ru) Способы улучшения производительности миокарда у пациентов после операции фонтена с применением композиций уденафила
MX2018005987A (es) Compuestos heterociclicos para el tratamiento de enfermedades.
EA201591717A1 (ru) Твердые формы гидрохлорида вемурафениба

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 TJ TM RU