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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- Prior art keywords
- combination
- pharmaceutically acceptable
- acceptable salt
- formula
- compound
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- 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 (https=) |
| EP (1) | EP2694073B1 (https=) |
| JP (1) | JP6147246B2 (https=) |
| KR (1) | KR20140022053A (https=) |
| CN (2) | CN103841976A (https=) |
| AU (1) | AU2012236164A1 (https=) |
| BR (1) | BR112013025397A2 (https=) |
| CA (1) | CA2831932A1 (https=) |
| ES (1) | ES2688809T3 (https=) |
| IL (1) | IL228643A0 (https=) |
| MX (1) | MX2013011333A (https=) |
| PL (1) | PL2694073T3 (https=) |
| RU (1) | RU2013148817A (https=) |
| SG (1) | SG194047A1 (https=) |
| TR (1) | TR201815685T4 (https=) |
| WO (1) | WO2012135779A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2776944A1 (en) * | 2009-10-12 | 2011-05-12 | F. Hoffmann-La Roche Ag | Combinations of a pi3k inhibitor and a mek inhibitor |
| JP2016502974A (ja) * | 2012-12-07 | 2016-02-01 | ザ ジェネラル ホスピタル コーポレイション | Ｐｉ３ｋ／ａｋｔ阻害剤化合物とｈｅｒ３／ｅｇｆｒ阻害剤化合物との組み合わせ及び高増殖性疾患の治療におけるその使用 |
| EP2959014B1 (en) * | 2013-02-25 | 2019-11-13 | Genentech, Inc. | Methods and compositions for detecting and treating drug resistant akt mutant |
| WO2015035146A2 (en) * | 2013-09-05 | 2015-03-12 | Memorial Sloan-Kettering Cancer Center | Ddx43 as a biomarker of resistance to mek1/2 inhibitors |
| TWI719765B (zh) | 2018-12-19 | 2021-02-21 | 美商建南德克公司 | 使用包含akt抑制劑、紫杉烷及pd-l1抑制劑之組合療法之乳癌治療 |
| AU2021246141A1 (en) * | 2020-04-03 | 2022-12-01 | Beigene, Ltd. | Co-administration of mirdametinib and lifirafenib for use in treating cancers |
| 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 RU RU2013148817/15A patent/RU2013148817A/ru not_active Application Discontinuation
- 2012-03-30 KR KR1020137029126A patent/KR20140022053A/ko not_active Withdrawn
- 2012-03-30 CN CN201280027030.0A patent/CN103841976A/zh active Pending
- 2012-03-30 CN CN201910098566.5A patent/CN110433165A/zh active Pending
- 2012-03-30 SG SG2013073739A patent/SG194047A1/en unknown
- 2012-03-30 ES ES12764894.7T patent/ES2688809T3/es active Active
- 2012-03-30 AU AU2012236164A patent/AU2012236164A1/en not_active Abandoned
- 2012-03-30 MX MX2013011333A patent/MX2013011333A/es not_active Application Discontinuation
- 2012-03-30 WO PCT/US2012/031716 patent/WO2012135779A1/en not_active Ceased
- 2012-03-30 CA CA2831932A patent/CA2831932A1/en not_active Abandoned
- 2012-03-30 BR BR112013025397A patent/BR112013025397A2/pt not_active IP Right Cessation
- 2012-03-30 TR TR2018/15685T patent/TR201815685T4/tr unknown
- 2012-03-30 JP JP2014502884A patent/JP6147246B2/ja active Active
- 2012-03-30 EP EP12764894.7A patent/EP2694073B1/en active Active
- 2012-03-30 US US14/009,320 patent/US9682082B2/en active Active
- 2012-03-30 PL PL12764894T patent/PL2694073T3/pl unknown
-
2013
- 2013-09-30 IL IL228643A patent/IL228643A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2014512355A (ja) | 2014-05-22 |
| EP2694073A4 (en) | 2014-09-03 |
| SG194047A1 (en) | 2013-11-29 |
| AU2012236164A1 (en) | 2013-11-21 |
| CN103841976A (zh) | 2014-06-04 |
| US9682082B2 (en) | 2017-06-20 |
| ES2688809T3 (es) | 2018-11-07 |
| WO2012135779A1 (en) | 2012-10-04 |
| CN110433165A (zh) | 2019-11-12 |
| NZ617243A (en) | 2016-02-26 |
| IL228643A0 (en) | 2013-12-31 |
| EP2694073A1 (en) | 2014-02-12 |
| MX2013011333A (es) | 2014-04-16 |
| KR20140022053A (ko) | 2014-02-21 |
| EP2694073B1 (en) | 2018-08-08 |
| JP6147246B2 (ja) | 2017-06-14 |
| TR201815685T4 (tr) | 2018-11-21 |
| US20140155372A1 (en) | 2014-06-05 |
| CA2831932A1 (en) | 2012-10-04 |
| BR112013025397A2 (pt) | 2019-09-24 |
| PL2694073T3 (pl) | 2019-06-28 |
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