AR045738A1 - Derivados de bencimidazol n3 alquilados como inhibidores de mek - Google Patents
Derivados de bencimidazol n3 alquilados como inhibidores de mekInfo
- Publication number
- AR045738A1 AR045738A1 ARP040103103A ARP040103103A AR045738A1 AR 045738 A1 AR045738 A1 AR 045738A1 AR P040103103 A ARP040103103 A AR P040103103A AR P040103103 A ARP040103103 A AR P040103103A AR 045738 A1 AR045738 A1 AR 045738A1
- Authority
- AR
- Argentina
- Prior art keywords
- aryl
- heteroaryl
- heterocyclyl
- nr3r4
- alkyl
- Prior art date
Links
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 23
- 125000001072 heteroaryl group Chemical group 0.000 abstract 22
- 125000003118 aryl group Chemical group 0.000 abstract 21
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 15
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 13
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 13
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 12
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 10
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 abstract 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 10
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 10
- 125000000304 alkynyl group Chemical group 0.000 abstract 9
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 9
- 150000002367 halogens Chemical class 0.000 abstract 9
- 125000003342 alkenyl group Chemical group 0.000 abstract 8
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000004043 oxo group Chemical group O=* 0.000 abstract 5
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 3
- 125000004429 atom Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 241000124008 Mammalia Species 0.000 abstract 2
- 125000002837 carbocyclic group Chemical group 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 229910019142 PO4 Inorganic materials 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 125000000539 amino acid group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- BNGCVNHMPJGSOA-UHFFFAOYSA-N azidophosphonic acid Chemical compound OP(O)(=O)N=[N+]=[N-] BNGCVNHMPJGSOA-UHFFFAOYSA-N 0.000 abstract 1
- PSHRANCNVXNITH-UHFFFAOYSA-N dimethylamino acetate Chemical compound CN(C)OC(C)=O PSHRANCNVXNITH-UHFFFAOYSA-N 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 abstract 1
- 239000010452 phosphate Substances 0.000 abstract 1
- 125000005541 phosphonamide group Chemical group 0.000 abstract 1
- 150000003014 phosphoric acid esters Chemical class 0.000 abstract 1
- -1 phosphorylmethyloxycarbonyl Chemical group 0.000 abstract 1
- 229920001184 polypeptide Polymers 0.000 abstract 1
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
- C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
- C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
- C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
- C04B35/632—Organic additives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic 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
- C07D403/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic 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
- C07D403/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic 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
- C07D403/12—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6503—Five-membered rings
- C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
- C07F9/65068—Five-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Molecular Biology (AREA)
- Ceramic Engineering (AREA)
- Manufacturing & Machinery (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Inorganic Chemistry (AREA)
- Materials Engineering (AREA)
- Structural Engineering (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/652,733 US7235537B2 (en) | 2002-03-13 | 2003-08-29 | N3 alkylated benzimidazole derivatives as MEK inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045738A1 true AR045738A1 (es) | 2005-11-09 |
Family
ID=34273411
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040103103A AR045738A1 (es) | 2003-08-29 | 2004-08-27 | Derivados de bencimidazol n3 alquilados como inhibidores de mek |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US7235537B2 (enExample) |
| EP (1) | EP1663210B1 (enExample) |
| JP (1) | JP5026076B2 (enExample) |
| KR (1) | KR20060121853A (enExample) |
| CN (1) | CN1874768A (enExample) |
| AR (1) | AR045738A1 (enExample) |
| AU (1) | AU2004270166A1 (enExample) |
| BR (1) | BRPI0413152A (enExample) |
| CA (1) | CA2537098A1 (enExample) |
| ES (1) | ES2628959T3 (enExample) |
| IL (1) | IL173935A (enExample) |
| IS (1) | IS8384A (enExample) |
| MX (1) | MXPA06002268A (enExample) |
| NO (1) | NO20061432L (enExample) |
| RU (1) | RU2006109600A (enExample) |
| TW (1) | TW200524879A (enExample) |
| WO (1) | WO2005023251A1 (enExample) |
| ZA (1) | ZA200602588B (enExample) |
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL230179B1 (pl) * | 2002-03-13 | 2018-09-28 | Array Biopharma Inc | N3 Alkilowane pochodne benzoimidazolu, kompozycja je zawierająca oraz ich zastosowanie do wytwarzania leku do leczenia zaburzeń hiperproliferacyjnych |
| CA2532067C (en) | 2003-07-24 | 2010-12-21 | Stephen Douglas Barrett | N-methyle-substituted benzamidazoles |
| US7144907B2 (en) * | 2003-09-03 | 2006-12-05 | Array Biopharma Inc. | Heterocyclic inhibitors of MEK and methods of use thereof |
| US7538120B2 (en) * | 2003-09-03 | 2009-05-26 | Array Biopharma Inc. | Method of treating inflammatory diseases |
| US7517994B2 (en) * | 2003-11-19 | 2009-04-14 | Array Biopharma Inc. | Heterocyclic inhibitors of MEK and methods of use thereof |
| US7732616B2 (en) * | 2003-11-19 | 2010-06-08 | Array Biopharma Inc. | Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof |
| CN1905873A (zh) * | 2003-11-19 | 2007-01-31 | 阵列生物制药公司 | Mek的杂环抑制剂及其使用方法 |
| US20050130954A1 (en) * | 2003-11-21 | 2005-06-16 | Mitchell Ian S. | AKT protein kinase inhibitors |
| TW201238952A (en) * | 2005-05-18 | 2012-10-01 | Array Biopharma Inc | Heterocyclic inhibitors of MEK and methods of use thereof |
| EA032466B1 (ru) | 2005-10-07 | 2019-05-31 | Экселиксис, Инк. | Способы получения ингибиторов mek |
| ES2364901T3 (es) | 2005-11-15 | 2011-09-16 | Array Biopharma, Inc. | Procesos e intermedios para la preparación de derivados de n4-fenil-quinazolin-4-amina. |
| CN101341132A (zh) * | 2005-12-21 | 2009-01-07 | 阿斯利康(瑞典)有限公司 | 作为mek抑制剂用于治疗癌症的6-(4-溴-2-氯-苯基氨基)-7-氟-n-(2-羟基乙氧基)-3-甲基-3h-苯并咪唑-5-甲酰胺的甲苯磺酸盐 |
| TWI405756B (zh) * | 2005-12-21 | 2013-08-21 | Array Biopharma Inc | 新穎硫酸氫鹽 |
| RU2418790C3 (ru) * | 2005-12-21 | 2022-03-14 | Астразенека Аб | Новая гидросульфатная соль |
| GB0601962D0 (en) | 2006-01-31 | 2006-03-15 | Ucb Sa | Therapeutic agents |
| US8329701B2 (en) | 2006-07-06 | 2012-12-11 | Array Biopharma Inc. | Dihydrofuro pyrimidines as AKT protein kinase inhibitors |
| US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| EP2054418B1 (en) | 2006-07-06 | 2011-11-09 | Array Biopharma Inc. | Dihydrothieno pyrimidines as akt protein kinase inhibitors |
| JP5268904B2 (ja) | 2006-07-06 | 2013-08-21 | アレイ バイオファーマ、インコーポレイテッド | Aktプロテインキナーゼ阻害剤としてのシクロペンタ[d]ピリミジン |
| US8492378B2 (en) | 2006-08-03 | 2013-07-23 | Takeda Pharmaceutical Company Limited | GSK-3β inhibitor |
| WO2008067481A1 (en) | 2006-11-30 | 2008-06-05 | Genentech, Inc. | Aza-indolyl compounds and methods of use |
| CN111643496A (zh) * | 2006-12-14 | 2020-09-11 | 埃克塞利希斯股份有限公司 | 使用mek抑制剂的方法 |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| AU2008272832B2 (en) * | 2007-07-05 | 2014-02-20 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| KR20150089099A (ko) | 2007-07-05 | 2015-08-04 | 어레이 바이오파마 인크. | Akt 단백질 키나제 억제제로서의 피리미딜 시클로펜탄 |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| GB0714384D0 (en) | 2007-07-23 | 2007-09-05 | Ucb Pharma Sa | theraputic agents |
| CA2695956A1 (en) | 2007-08-16 | 2009-02-19 | F. Hoffmann-La Roche Ag | Substituted hydantoins |
| ES2456966T3 (es) | 2007-11-12 | 2014-04-24 | Takeda Pharmaceutical Company Limited | Inhibidores de MAPK/ERK cinasa |
| JP2011506420A (ja) * | 2007-12-12 | 2011-03-03 | アストラゼネカ アクチボラグ | Mek阻害剤及びオーロラキナーゼ阻害剤188を含んでなる組合せ |
| AU2008341680A1 (en) | 2007-12-20 | 2009-07-02 | F. Hoffmann-La Roche Ag | Substituted hydantoins as MEK kinase inhibitors |
| CN101932564B (zh) * | 2008-01-09 | 2012-12-26 | 阵列生物制药公司 | 作为akt蛋白激酶抑制剂的羟基化嘧啶基环戊烷类 |
| ES2401685T3 (es) * | 2008-01-09 | 2013-04-23 | Array Biopharma, Inc. | Pirimidil ciclopentano hidroxilado como inhibidor de la proteína quinasa AKT |
| WO2009093008A1 (en) | 2008-01-21 | 2009-07-30 | Ucb Pharma S.A. | Thieno-pyridine derivatives as mek inhibitors |
| GB0811304D0 (en) | 2008-06-19 | 2008-07-30 | Ucb Pharma Sa | Therapeutic agents |
| US20110105521A1 (en) | 2008-07-11 | 2011-05-05 | Novartis Ag | Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of ras/raf/mek pathway |
| JP5746630B2 (ja) | 2008-11-10 | 2015-07-08 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | 置換スルホンアミドフェノキシベンズアミド |
| MA33974B1 (fr) * | 2009-10-12 | 2013-02-01 | Hoffmann La Roche | Combinaisons d'un inhibiteur de pi3k et d'un inhibiteur de mek |
| WO2011047796A1 (en) | 2009-10-21 | 2011-04-28 | Bayer Schering Pharma Aktiengesellschaft | Substituted halophenoxybenzamide derivatives |
| US8962606B2 (en) | 2009-10-21 | 2015-02-24 | Bayer Intellectual Property Gmbh | Substituted benzosulphonamides |
| US20120269803A1 (en) | 2009-10-21 | 2012-10-25 | Bayer Intellectual Property Gmbh | Substituted benzosulphonamides |
| US20150141380A1 (en) | 2010-08-05 | 2015-05-21 | Case Western Reserve University | Inhibitors of erk for developmental disorders of neuronal connectivity |
| CA2812608C (en) | 2010-10-06 | 2020-07-14 | Glaxosmithkline Llc | Benzimidazole derivatives as pi3 kinase inhibitors |
| CN103282351A (zh) | 2010-10-29 | 2013-09-04 | 拜耳知识产权有限责任公司 | 取代的苯氧基吡啶 |
| CN102020651B (zh) | 2010-11-02 | 2012-07-18 | 北京赛林泰医药技术有限公司 | 6-芳基氨基吡啶酮甲酰胺mek抑制剂 |
| EP2655375B1 (fr) | 2010-12-23 | 2014-12-03 | Sanofi | Derives de pyrimidinone, leur preparation et leur utilisation pharmaceutique |
| AU2012236164A1 (en) | 2011-04-01 | 2013-11-21 | Genentech, Inc. | Combinations of AKT and MEK inhibitor compounds, and methods of use |
| JP6239497B2 (ja) | 2011-04-01 | 2017-11-29 | ジェネンテック, インコーポレイテッド | Akt阻害剤化合物及びアビラテロンの組み合わせ、及び使用方法 |
| ES2597052T3 (es) | 2011-05-25 | 2017-01-13 | Université Paris Descartes | Inhibidores de ERK para su uso en el tratamiento de atrofia muscular espinal |
| KR20140072028A (ko) * | 2011-08-31 | 2014-06-12 | 노파르티스 아게 | Pi3k- 및 mek-억제제의 상승작용적 조합물 |
| CN103204825B (zh) | 2012-01-17 | 2015-03-04 | 上海科州药物研发有限公司 | 作为蛋白激酶抑制剂的苯并噻唑化合物及其制备方法和用途 |
| CU24335B1 (es) | 2012-03-14 | 2018-04-03 | Lupin Ltd | Piridopirimidinas sustituidas como inhibidores de la quinasa mek y útiles para el tratamiento del cáncer |
| AR091876A1 (es) * | 2012-07-26 | 2015-03-04 | Novartis Ag | Combinaciones farmaceuticas para el tratamiento de enfermedades proliferativas |
| SI2909188T1 (en) | 2012-10-12 | 2018-07-31 | Exelixis, Inc. | A novel process for the manufacture of compounds for use in the treatment of cancer |
| SMT202400044T1 (it) | 2012-10-19 | 2024-03-13 | Array Biopharma Inc | Formulazione comprendente un inibitore di mek |
| US9867825B2 (en) * | 2012-12-20 | 2018-01-16 | Novartis Ag | Pharmaceutical combination comprising binimetinib |
| AU2014233805B2 (en) * | 2013-03-21 | 2018-10-18 | Array Biopharma Inc. | Combination therapy comprising a B-Raf inhibitor and a second inhibitor |
| WO2015038704A1 (en) | 2013-09-11 | 2015-03-19 | The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone | Compositions for preparing cardiomyocytes |
| WO2016009306A1 (en) | 2014-07-15 | 2016-01-21 | Lupin Limited | Heterocyclyl compounds as mek inhibitors |
| CN105384754B (zh) * | 2014-09-02 | 2018-04-20 | 上海科州药物研发有限公司 | 作为蛋白激酶抑制剂的杂环类化合物及其制备方法和用途 |
| WO2016035008A1 (en) | 2014-09-04 | 2016-03-10 | Lupin Limited | Pyridopyrimidine derivatives as mek inhibitors |
| CN105566225A (zh) * | 2015-02-16 | 2016-05-11 | 苏州晶云药物科技有限公司 | 一种口服丝裂原活化蛋白激酶抑制剂的晶型及其制备方法 |
| WO2017033113A1 (en) | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
| JP6805336B2 (ja) * | 2016-06-03 | 2020-12-23 | アレイ バイオファーマ、インコーポレイテッド | 薬学的組み合わせ |
| CN109438362B (zh) * | 2017-11-14 | 2020-07-21 | 深圳市塔吉瑞生物医药有限公司 | 一种取代的苯并咪唑化合物及包含该化合物的组合物 |
| ES2989088T3 (es) * | 2017-12-07 | 2024-11-25 | Harbin Zhenbao Pharmaceutical Co Ltd | Forma de sal y forma de cristal que sirven como compuestos inhibidores de FGFR y VEGFR, y método de preparación de las mismas |
| PT4360713T (pt) | 2018-09-18 | 2025-01-07 | Hoffmann La Roche | Derivados de quinazolina enquanto agentes antitumorais |
| KR20210107069A (ko) | 2018-12-21 | 2021-08-31 | 다이이찌 산쿄 가부시키가이샤 | 항체-약물 컨쥬게이트와 키나아제 저해제의 조합 |
| US11447482B1 (en) | 2019-02-14 | 2022-09-20 | KUDA Therapeutics, Inc. | Imidazopyridine and oxazolopyridine derivatives and analogs thereof, methods of preparation thereof, methods of HIF-2A pathway inhibition, and induction of ferroptosis |
| MX2021009863A (es) | 2019-03-21 | 2021-11-12 | Onxeo | Una molecula dbait en combinacion con inhibidor de quinasa para el tratamiento del cancer. |
| WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN115322105A (zh) * | 2021-05-11 | 2022-11-11 | 江苏润安制药有限公司 | 一种合成艾拉莫德关键中间体的方法 |
| EP4346826A4 (en) | 2021-05-27 | 2025-04-30 | Mirati Therapeutics, Inc. | COMBINATION THERAPIES |
| CN115490640B (zh) * | 2021-06-17 | 2024-11-26 | 深圳市塔吉瑞生物医药有限公司 | 取代的苯并咪唑类化合物及包含该化合物的组合物及其用途 |
| KR20240035820A (ko) | 2021-07-09 | 2024-03-18 | 플렉시움 인코포레이티드 | Ikzf2를 조절하는 아릴 화합물 및 약학 조성물 |
| PE20242106A1 (es) | 2021-10-20 | 2024-10-28 | Hoffmann La Roche | Formas cristalinas de derivados de quinazolina, preparacion, composicion y uso de estas |
| CN116135839A (zh) * | 2021-11-18 | 2023-05-19 | 江苏润安制药有限公司 | 一种阿齐沙坦关键中间体的制备方法 |
| WO2025073765A1 (en) | 2023-10-03 | 2025-04-10 | Institut National de la Santé et de la Recherche Médicale | Methods of prognosis and treatment of patients suffering from melanoma |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5750545A (en) | 1993-07-23 | 1998-05-12 | The Green Cross Corporation | Triazole derivative and pharmaceutical use thereof |
| US5525625A (en) * | 1995-01-24 | 1996-06-11 | Warner-Lambert Company | 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders |
| UA73073C2 (uk) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| DE69836378T2 (de) | 1997-07-01 | 2007-10-11 | Warner-Lambert Co. Llc | Benzoesäure- und Benzamid-Derivate von Anthranilsäure und ihre Anwendung als MEK-Inhibitoren |
| US6506798B1 (en) * | 1997-07-01 | 2003-01-14 | Warner-Lambert Company | 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors |
| US6821963B2 (en) * | 1997-07-01 | 2004-11-23 | Warner-Lambert Company | 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors |
| US6310060B1 (en) | 1998-06-24 | 2001-10-30 | Warner-Lambert Company | 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors |
| BR9810366A (pt) | 1997-07-01 | 2000-08-29 | Warner Lambert Co | Derivados de ácido 4-bromo ou 4-iodo fenilamino benzidroxîmico e seu uso como inibidores de mek |
| WO2000040237A1 (en) | 1999-01-07 | 2000-07-13 | Warner-Lambert Company | Antiviral method using mek inhibitors |
| AU2483000A (en) | 1999-01-07 | 2000-07-24 | Warner-Lambert Company | Treatment of asthma with mek inhibitors |
| CA2348236A1 (en) | 1999-01-13 | 2000-07-20 | Stephen Douglas Barrett | 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors |
| BR9916857A (pt) | 1999-01-13 | 2001-12-04 | Warner Lambert Co | 4 heteroaril diarilaminas |
| BR9916885A (pt) | 1999-01-13 | 2001-11-20 | Warner Lambert Co | Derivados de benzeno-sulfonamida e seu uso comoinibidores da mek |
| BR9916896A (pt) | 1999-01-13 | 2001-11-20 | Warner Lambert Co | Diaril aminas substituìdas com 1-heterociclo |
| CA2349467A1 (en) | 1999-01-13 | 2000-07-20 | Warner-Lambert Company | Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors |
| EE200100373A (et) * | 1999-01-13 | 2002-10-15 | Warner-Lambert Company | Bensoheterotsüklid ja nende kasutamine MEK inhibiitoritena |
| GB9910577D0 (en) | 1999-05-08 | 1999-07-07 | Zeneca Ltd | Chemical compounds |
| TR200200204T2 (tr) | 1999-07-16 | 2002-11-21 | Warner-Lambert Company | MEK inhibitörleri kullanılarak kronik ağrının tedavi edilmesi. |
| EP1202726A2 (en) | 1999-07-16 | 2002-05-08 | Warner-Lambert Company Llc | Method for treating chronic pain using mek inhibitors |
| US7030119B1 (en) | 1999-07-16 | 2006-04-18 | Warner-Lambert Company | Method for treating chronic pain using MEK inhibitors |
| DK1202724T3 (da) | 1999-07-16 | 2004-01-26 | Warner Lambert Co | Fremgangsmåde til behandling af kronisk smerte under anvendelse af mek-inhibitorer |
| CA2377092A1 (en) | 1999-07-16 | 2001-01-25 | Warner-Lambert Company | Method for treating chronic pain using mek inhibitors |
| CA2403017A1 (en) | 2000-03-15 | 2001-09-20 | Warner-Lambert Company | 5-amide substituted diarylamines as mex inhibitors |
| US7001905B2 (en) | 2000-03-15 | 2006-02-21 | Warner-Lambert Company | Substituted diarylamines as MEK inhibitors |
| HU230251B1 (hu) | 2000-07-19 | 2015-11-30 | Warner-Lambert Co. | 4-Jód-fenil-amino-benzhidroxámsav-észter-származékok és ezeket tartalmazó gyógyászati készítmények |
| CN1458921A (zh) | 2000-08-25 | 2003-11-26 | 沃尼尔·朗伯有限责任公司 | N-芳基邻氨基苯甲酸和它们的衍生物的制备方法 |
| AU2002210714A1 (en) | 2000-11-02 | 2002-06-11 | Astrazeneca Ab | Substituted quinolines as antitumor agents |
| US20040039208A1 (en) | 2001-07-20 | 2004-02-26 | Chen Michael Huai Gu | Process for making n-aryl-anthranilic acids and their derivatives |
| PL230179B1 (pl) * | 2002-03-13 | 2018-09-28 | Array Biopharma Inc | N3 Alkilowane pochodne benzoimidazolu, kompozycja je zawierająca oraz ich zastosowanie do wytwarzania leku do leczenia zaburzeń hiperproliferacyjnych |
| US20030216460A1 (en) * | 2002-03-13 | 2003-11-20 | Wallace Eli M. | N3 alkylated benzimidazole derivatives as MEK inhibitors |
| CA2532067C (en) * | 2003-07-24 | 2010-12-21 | Stephen Douglas Barrett | N-methyle-substituted benzamidazoles |
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2004
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- 2004-08-20 JP JP2006524761A patent/JP5026076B2/ja not_active Expired - Lifetime
- 2004-08-20 CN CNA2004800323322A patent/CN1874768A/zh active Pending
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- 2004-08-20 EP EP04781809.1A patent/EP1663210B1/en not_active Expired - Lifetime
- 2004-08-20 KR KR1020067004187A patent/KR20060121853A/ko not_active Withdrawn
- 2004-08-20 BR BRPI0413152-5A patent/BRPI0413152A/pt not_active Application Discontinuation
- 2004-08-20 ES ES04781809.1T patent/ES2628959T3/es not_active Expired - Lifetime
- 2004-08-20 AU AU2004270166A patent/AU2004270166A1/en not_active Abandoned
- 2004-08-20 WO PCT/US2004/027199 patent/WO2005023251A1/en not_active Ceased
- 2004-08-20 RU RU2006109600/04A patent/RU2006109600A/ru not_active Application Discontinuation
- 2004-08-27 AR ARP040103103A patent/AR045738A1/es not_active Application Discontinuation
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- 2006-02-26 IL IL173935A patent/IL173935A/en active IP Right Grant
- 2006-03-29 IS IS8384A patent/IS8384A/is unknown
- 2006-03-29 NO NO20061432A patent/NO20061432L/no not_active Application Discontinuation
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| CA2537098A1 (en) | 2005-03-17 |
| US20070299063A1 (en) | 2007-12-27 |
| US20040116710A1 (en) | 2004-06-17 |
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| BRPI0413152A (pt) | 2006-10-03 |
| IL173935A0 (en) | 2006-07-05 |
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| CN1874768A (zh) | 2006-12-06 |
| NO20061432L (no) | 2006-08-25 |
| EP1663210B1 (en) | 2017-04-19 |
| EP1663210A1 (en) | 2006-06-07 |
| IL173935A (en) | 2015-08-31 |
| JP5026076B2 (ja) | 2012-09-12 |
| JP2007504139A (ja) | 2007-03-01 |
| MXPA06002268A (es) | 2006-05-31 |
| TW200524879A (en) | 2005-08-01 |
| ZA200602588B (en) | 2008-07-30 |
| KR20060121853A (ko) | 2006-11-29 |
| AU2004270166A1 (en) | 2005-03-17 |
| EP1663210A4 (en) | 2009-04-22 |
| RU2006109600A (ru) | 2007-10-10 |
| IS8384A (is) | 2006-03-29 |
| US7235537B2 (en) | 2007-06-26 |
| WO2005023251A1 (en) | 2005-03-17 |
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