RU2013148817A - Комбинации соединений-ингибиторов акт и мек и способы их применения - Google Patents
Комбинации соединений-ингибиторов акт и мек и способы их применения Download PDFInfo
- Publication number
- RU2013148817A RU2013148817A RU2013148817/15A RU2013148817A RU2013148817A RU 2013148817 A RU2013148817 A RU 2013148817A RU 2013148817/15 A RU2013148817/15 A RU 2013148817/15A RU 2013148817 A RU2013148817 A RU 2013148817A RU 2013148817 A RU2013148817 A RU 2013148817A
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- RU
- Russia
- Prior art keywords
- combination
- pharmaceutically acceptable
- acceptable salt
- formula
- compound
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract 30
- 229940124647 MEK inhibitor Drugs 0.000 title 1
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 38
- 206010028980 Neoplasm Diseases 0.000 claims abstract 17
- 201000011510 cancer Diseases 0.000 claims abstract 17
- 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 claims abstract 17
- 229960002271 cobimetinib Drugs 0.000 claims abstract 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 13
- 208000035475 disorder Diseases 0.000 claims abstract 10
- 230000003463 hyperproliferative effect Effects 0.000 claims abstract 10
- 230000035772 mutation Effects 0.000 claims abstract 6
- 230000003321 amplification Effects 0.000 claims abstract 4
- 238000003199 nucleic acid amplification method Methods 0.000 claims abstract 4
- 208000029742 colonic neoplasm Diseases 0.000 claims abstract 3
- 201000001441 melanoma Diseases 0.000 claims abstract 3
- 101150029707 ERBB2 gene Proteins 0.000 claims abstract 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims abstract 2
- 208000032612 Glial tumor Diseases 0.000 claims abstract 2
- 206010018338 Glioma Diseases 0.000 claims abstract 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims abstract 2
- 206010027406 Mesothelioma Diseases 0.000 claims abstract 2
- 108091007960 PI3Ks Proteins 0.000 claims abstract 2
- 102000014160 PTEN Phosphohydrolase Human genes 0.000 claims abstract 2
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 claims abstract 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims abstract 2
- 210000000481 breast Anatomy 0.000 claims abstract 2
- 210000001072 colon Anatomy 0.000 claims abstract 2
- 201000010536 head and neck cancer Diseases 0.000 claims abstract 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims abstract 2
- 210000003734 kidney Anatomy 0.000 claims abstract 2
- 210000004072 lung Anatomy 0.000 claims abstract 2
- 210000001672 ovary Anatomy 0.000 claims abstract 2
- 230000002018 overexpression Effects 0.000 claims abstract 2
- 210000000496 pancreas Anatomy 0.000 claims abstract 2
- 230000002265 prevention Effects 0.000 claims abstract 2
- 210000002307 prostate Anatomy 0.000 claims abstract 2
- 201000000498 stomach carcinoma Diseases 0.000 claims abstract 2
- 239000003795 chemical substances by application Substances 0.000 claims 12
- 241000124008 Mammalia Species 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 102000038030 PI3Ks Human genes 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 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
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further 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
- A61K31/495—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (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)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161471038P | 2011-04-01 | 2011-04-01 | |
| US61/471,038 | 2011-04-01 | ||
| PCT/US2012/031716 WO2012135779A1 (en) | 2011-04-01 | 2012-03-30 | Combinations of akt and mek inhibitor compounds, and methods of use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2013148817A true RU2013148817A (ru) | 2015-05-10 |
Family
ID=46931964
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013148817/15A RU2013148817A (ru) | 2011-04-01 | 2012-03-30 | Комбинации соединений-ингибиторов акт и мек и способы их применения |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US9682082B2 (enExample) |
| EP (1) | EP2694073B1 (enExample) |
| JP (1) | JP6147246B2 (enExample) |
| KR (1) | KR20140022053A (enExample) |
| CN (2) | CN110433165A (enExample) |
| AU (1) | AU2012236164A1 (enExample) |
| BR (1) | BR112013025397A2 (enExample) |
| CA (1) | CA2831932A1 (enExample) |
| ES (1) | ES2688809T3 (enExample) |
| IL (1) | IL228643A0 (enExample) |
| MX (1) | MX2013011333A (enExample) |
| PL (1) | PL2694073T3 (enExample) |
| RU (1) | RU2013148817A (enExample) |
| SG (1) | SG194047A1 (enExample) |
| TR (1) | TR201815685T4 (enExample) |
| WO (1) | WO2012135779A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2609767T3 (es) * | 2009-10-12 | 2017-04-24 | F. Hoffmann-La Roche Ag | Combinaciones de un inhibidor de PI3K y un inhibidor de MEK |
| MX2015007054A (es) * | 2012-12-07 | 2016-01-12 | Gen Hospital Corp | Combinaciones de un compuesto inhibidor de pi3k/akt con un compuesto inhibidor de her3/egfr, y métodos de uso. |
| KR102182488B1 (ko) * | 2013-02-25 | 2020-11-24 | 제넨테크, 인크. | 약물 내성 akt 돌연변이체의 검출 및 치료를 위한 방법 및 조성물 |
| WO2015035146A2 (en) * | 2013-09-05 | 2015-03-12 | Memorial Sloan-Kettering Cancer Center | Ddx43 as a biomarker of resistance to mek1/2 inhibitors |
| WO2020131765A1 (en) | 2018-12-19 | 2020-06-25 | Genentech, Inc. | Treatment of breast cancer using combination therapies comprising an akt inhibitor, a taxane, and a pd-l1 inhibitor |
| KR20230048476A (ko) * | 2020-04-03 | 2023-04-11 | 베이진 리미티드 | 암 치료 시에 사용하기 위한 미르다메티닙과 리피라페닙의 공동 투여 |
| US11066358B1 (en) | 2021-02-17 | 2021-07-20 | Warner-Lambert Company Llc | Compositions of essentially pure form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide and uses thereof |
| US11084780B1 (en) | 2021-02-17 | 2021-08-10 | Springworks Therapeutics, Inc. | Crystalline solids of MEK inhibitor N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide and uses thereof |
| WO2024255830A1 (zh) * | 2023-06-14 | 2024-12-19 | 南京正大天晴制药有限公司 | Akt抑制剂在制备预防或治疗卵巢癌药物中的用途 |
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-
2012
- 2012-03-30 TR TR2018/15685T patent/TR201815685T4/tr unknown
- 2012-03-30 MX MX2013011333A patent/MX2013011333A/es not_active Application Discontinuation
- 2012-03-30 KR KR1020137029126A patent/KR20140022053A/ko not_active Withdrawn
- 2012-03-30 JP JP2014502884A patent/JP6147246B2/ja active Active
- 2012-03-30 CA CA2831932A patent/CA2831932A1/en not_active Abandoned
- 2012-03-30 PL PL12764894T patent/PL2694073T3/pl unknown
- 2012-03-30 CN CN201910098566.5A patent/CN110433165A/zh active Pending
- 2012-03-30 RU RU2013148817/15A patent/RU2013148817A/ru not_active Application Discontinuation
- 2012-03-30 WO PCT/US2012/031716 patent/WO2012135779A1/en not_active Ceased
- 2012-03-30 ES ES12764894.7T patent/ES2688809T3/es active Active
- 2012-03-30 EP EP12764894.7A patent/EP2694073B1/en active Active
- 2012-03-30 CN CN201280027030.0A patent/CN103841976A/zh active Pending
- 2012-03-30 BR BR112013025397A patent/BR112013025397A2/pt not_active IP Right Cessation
- 2012-03-30 SG SG2013073739A patent/SG194047A1/en unknown
- 2012-03-30 AU AU2012236164A patent/AU2012236164A1/en not_active Abandoned
- 2012-03-30 US US14/009,320 patent/US9682082B2/en active Active
-
2013
- 2013-09-30 IL IL228643A patent/IL228643A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2688809T3 (es) | 2018-11-07 |
| CN110433165A (zh) | 2019-11-12 |
| WO2012135779A1 (en) | 2012-10-04 |
| TR201815685T4 (tr) | 2018-11-21 |
| CN103841976A (zh) | 2014-06-04 |
| NZ617243A (en) | 2016-02-26 |
| JP6147246B2 (ja) | 2017-06-14 |
| US20140155372A1 (en) | 2014-06-05 |
| EP2694073A4 (en) | 2014-09-03 |
| KR20140022053A (ko) | 2014-02-21 |
| SG194047A1 (en) | 2013-11-29 |
| MX2013011333A (es) | 2014-04-16 |
| IL228643A0 (en) | 2013-12-31 |
| BR112013025397A2 (pt) | 2019-09-24 |
| US9682082B2 (en) | 2017-06-20 |
| JP2014512355A (ja) | 2014-05-22 |
| PL2694073T3 (pl) | 2019-06-28 |
| EP2694073A1 (en) | 2014-02-12 |
| CA2831932A1 (en) | 2012-10-04 |
| AU2012236164A1 (en) | 2013-11-21 |
| EP2694073B1 (en) | 2018-08-08 |
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