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 заболеванийInfo
- 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
Links
- 239000012824 ERK inhibitor Substances 0.000 title abstract 2
- 229940124647 MEK inhibitor Drugs 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 230000003463 hyperproliferative effect Effects 0.000 title abstract 2
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title 1
- RZUOCXOYPYGSKL-GOSISDBHSA-N 1-[(1s)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]pyridin-2-one Chemical compound CN1N=CC=C1NC1=NC=CC(C2=CC(=O)N([C@H](CO)C=3C=C(F)C(Cl)=CC=3)C=C2)=N1 RZUOCXOYPYGSKL-GOSISDBHSA-N 0.000 abstract 1
- RFWVETIZUQEJEF-UHFFFAOYSA-N GDC-0623 Chemical compound OCCONC(=O)C=1C=CC2=CN=CN2C=1NC1=CC=C(I)C=C1F RFWVETIZUQEJEF-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- BSMCAPRUBJMWDF-KRWDZBQOSA-N cobimetinib Chemical compound C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F BSMCAPRUBJMWDF-KRWDZBQOSA-N 0.000 abstract 1
- 229960002271 cobimetinib Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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.
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 (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2820009T3 (en) * | 2012-03-01 | 2018-04-16 | Array Biopharma Inc | Serine / threonine kinase inhibitors |
| CN106029672B (zh) | 2013-12-06 | 2019-03-29 | 基因泰克公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| 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 |
| WO2017080980A1 (en) | 2015-11-09 | 2017-05-18 | Astrazeneca Ab | Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer |
| LT3374359T (lt) | 2015-11-09 | 2020-03-25 | Astrazeneca Ab | Dihidroimidazopirazinono deriniai, tinkami panaudoti vėžio gydymui |
| 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 |
| KR20180134347A (ko) | 2016-04-15 | 2018-12-18 | 제넨테크, 인크. | 암의 진단 및 치료 방법 |
| AU2017316618A1 (en) | 2016-08-23 | 2019-02-07 | Genentech, Inc. | Combination therapy for the treatment of pancreatic cancer |
| DK3425390T3 (da) * | 2016-11-25 | 2021-02-15 | Genuv Inc | Sammensætning til fremme af differentiering og beskyttelse af neurale stamceller og fremgangsmåde til induktion af neural regenerering ved anvendelse heraf |
| 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 |
| KR102811888B1 (ko) | 2017-09-08 | 2025-05-27 | 에프. 호프만-라 로슈 아게 | 암의 진단 및 치료 방법 |
| EP3684364A4 (en) | 2017-09-18 | 2021-06-02 | Goldfinch Bio, Inc. | PYRIDAZINONE AND METHOD OF USE THEREOF |
| US11395823B2 (en) | 2018-01-09 | 2022-07-26 | Duke University | Topical administration of MEK inhibiting agents for the treatment of skin disorders |
| EP3752200A1 (en) | 2018-02-13 | 2020-12-23 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| US12377063B2 (en) * | 2019-07-11 | 2025-08-05 | Emory University | Combination therapies for managing cancer |
| KR102695469B1 (ko) * | 2021-07-23 | 2024-08-14 | 차의과학대학교 산학협력단 | 2,4-디아미노피리미딘을 포함하는 암의 예방 또는 치료용 조성물 |
| CN118001281B (zh) * | 2023-12-11 | 2025-10-17 | 中国科学院深圳先进技术研究院 | 一种治疗或预防甲基苯丙胺成瘾的药物及应用 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1934174T1 (sl) | 2005-10-07 | 2011-08-31 | Exelixis Inc | Inhibitorji MEK in postopki za njihovo uporabo |
| ES2528797T3 (es) | 2006-08-21 | 2015-02-12 | Genentech, Inc. | Compuestos de aza-benzotiofenilo y métodos de uso |
| AU2007286808B2 (en) | 2006-08-21 | 2012-12-06 | Genentech, Inc. | Aza-benzofuranyl compounds and methods of use |
| PE20081354A1 (es) | 2006-11-30 | 2008-11-14 | Genentech Inc | Compuestos de azaindolilo como inhibidores de mek |
| PL2101759T3 (pl) | 2006-12-14 | 2019-05-31 | Exelixis Inc | Sposoby stosowania inhibitorów MEK |
| JP5580735B2 (ja) | 2007-06-12 | 2014-08-27 | ジェネンテック, インコーポレイテッド | N−置換アザインドール類及び使用方法 |
| US8293763B2 (en) | 2007-12-19 | 2012-10-23 | Genentech, Inc. | 8-anilinoimidazopyridines and their use as anti-cancer and/or anti-inflammatory agents |
| JP5421925B2 (ja) * | 2007-12-19 | 2014-02-19 | ジェネンテック, インコーポレイテッド | 5−アニリノイミダゾピリジン及び使用の方法 |
| CA2708176A1 (en) | 2007-12-21 | 2009-07-02 | Genentech, Inc. | Azaindolizines and methods of use |
| ES2426096T3 (es) | 2008-07-01 | 2013-10-21 | Genentech, Inc. | Derivados de isoindolona como inhibidores de la quinasa MEK y métodos de utilización |
| US8841462B2 (en) | 2008-07-01 | 2014-09-23 | Robert A. Heald | Bicyclic heterocycles as MEK kinase inhibitors |
| US20120214828A1 (en) | 2009-08-24 | 2012-08-23 | Georgia Hatzivassiliou | Determining sensitivity of cells to b-raf inhibitor treatment by detecting kras mutation and rtk expression levels |
| CA2776944A1 (en) | 2009-10-12 | 2011-05-12 | F. Hoffmann-La Roche Ag | Combinations of a pi3k inhibitor and a mek inhibitor |
| PT2643322T (pt) | 2010-11-23 | 2017-11-13 | Abbvie Inc | Sais e formas cristalinas de um agente indutor de apoptose |
| EP2681215B1 (en) | 2011-02-28 | 2015-04-22 | Array Biopharma, Inc. | Serine/threonine kinase inhibitors |
| WO2012145503A1 (en) | 2011-04-21 | 2012-10-26 | Novartis Ag | Pharmaceutical combinations |
| US9187462B2 (en) | 2011-08-04 | 2015-11-17 | Array Biopharma Inc. | Substituted quinazolines as serine/threonine kinase inhibitors |
| DK2820009T3 (en) | 2012-03-01 | 2018-04-16 | Array Biopharma Inc | Serine / threonine kinase inhibitors |
| 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. |
| KR20190057421A (ko) | 2012-08-17 | 2019-05-28 | 에프. 호프만-라 로슈 아게 | 코비메티닙 및 베무라피닙을 투여함을 포함하는 흑색종의 조합 치료법 |
| TW201408658A (zh) | 2012-08-27 | 2014-03-01 | Array Biopharma Inc | 絲胺酸/酥胺酸激酶抑制劑 |
| KR102204520B1 (ko) | 2012-10-12 | 2021-01-20 | 엑셀리시스, 인코포레이티드 | 암의 치료에 사용하기 위한 화합물의 신규 제조 방법 |
| MX2015004615A (es) | 2012-10-16 | 2015-07-17 | Hoffmann La Roche | Inhibidores de serina/treonina cinasa. |
| CN106029672B (zh) | 2013-12-06 | 2019-03-29 | 基因泰克公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| 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 |
| BR112016015235A2 (pt) | 2013-12-30 | 2017-08-08 | Genentech Inc | Composto, composição farmacêutica, método de inibição da atividade da proteína quinase erk e método de tratamento |
| EP3129025B1 (en) | 2014-04-09 | 2019-05-15 | Genentech, Inc. | Process for the manufacturing of medicaments |
-
2014
- 2014-08-29 US US14/473,311 patent/US9532987B2/en not_active Expired - Fee Related
- 2014-09-04 TW TW103130648A patent/TW201605477A/zh unknown
- 2014-09-04 HK HK16106100.6A patent/HK1218072A1/zh unknown
- 2014-09-04 WO PCT/EP2014/068776 patent/WO2015032840A1/en not_active Ceased
- 2014-09-04 CN CN201480048950.XA patent/CN105517548B/zh not_active Expired - Fee Related
- 2014-09-04 JP JP2016539537A patent/JP2016531139A/ja not_active Withdrawn
- 2014-09-04 MX MX2016002857A patent/MX370417B/es active IP Right Grant
- 2014-09-04 MA MA38827A patent/MA38827A1/fr unknown
- 2014-09-04 PE PE2016000076A patent/PE20160529A1/es unknown
- 2014-09-04 EA EA201690513A patent/EA034872B1/ru not_active IP Right Cessation
- 2014-09-04 AU AU2014317119A patent/AU2014317119B2/en not_active Expired - Fee Related
- 2014-09-04 CA CA2916619A patent/CA2916619A1/en not_active Abandoned
- 2014-09-04 SG SG11201600989VA patent/SG11201600989VA/en unknown
- 2014-09-04 EP EP14761328.5A patent/EP3041471A1/en not_active Withdrawn
- 2014-09-04 UA UAA201603616A patent/UA120423C2/uk unknown
- 2014-09-04 AR ARP140103309A patent/AR097556A1/es unknown
- 2014-09-04 KR KR1020167005716A patent/KR20160048807A/ko not_active Ceased
-
2015
- 2015-12-21 IL IL243251A patent/IL243251B/en not_active IP Right Cessation
-
2016
- 2016-01-06 ZA ZA2016/00091A patent/ZA201600091B/en unknown
- 2016-01-08 CL CL2016000042A patent/CL2016000042A1/es unknown
- 2016-02-09 PH PH12016500270A patent/PH12016500270A1/en unknown
-
2018
- 2018-10-03 JP JP2018188348A patent/JP2019031517A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2014317119A1 (en) | 2016-03-03 |
| KR20160048807A (ko) | 2016-05-04 |
| PH12016500270A1 (en) | 2016-05-16 |
| SG11201600989VA (en) | 2016-03-30 |
| JP2016531139A (ja) | 2016-10-06 |
| ZA201600091B (en) | 2017-04-26 |
| EP3041471A1 (en) | 2016-07-13 |
| MX370417B (es) | 2019-12-10 |
| US9532987B2 (en) | 2017-01-03 |
| EA034872B1 (ru) | 2020-03-31 |
| CN105517548A (zh) | 2016-04-20 |
| WO2015032840A1 (en) | 2015-03-12 |
| CN105517548B (zh) | 2020-01-21 |
| IL243251B (en) | 2019-02-28 |
| CL2016000042A1 (es) | 2016-08-05 |
| TW201605477A (zh) | 2016-02-16 |
| MX2016002857A (es) | 2016-06-22 |
| US20150111869A1 (en) | 2015-04-23 |
| JP2019031517A (ja) | 2019-02-28 |
| CA2916619A1 (en) | 2015-03-12 |
| AR097556A1 (es) | 2016-03-23 |
| AU2014317119B2 (en) | 2019-12-05 |
| UA120423C2 (uk) | 2019-12-10 |
| PE20160529A1 (es) | 2016-05-21 |
| HK1218072A1 (zh) | 2017-02-03 |
| MA38827A1 (fr) | 2017-10-31 |
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