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
-
- 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)
- Manufacturing & Machinery (AREA)
- Ceramic Engineering (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Materials Engineering (AREA)
- Inorganic Chemistry (AREA)
- Structural Engineering (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (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 (OSRAM) |
| EP (1) | EP1663210B1 (OSRAM) |
| JP (1) | JP5026076B2 (OSRAM) |
| KR (1) | KR20060121853A (OSRAM) |
| CN (1) | CN1874768A (OSRAM) |
| AR (1) | AR045738A1 (OSRAM) |
| AU (1) | AU2004270166A1 (OSRAM) |
| BR (1) | BRPI0413152A (OSRAM) |
| CA (1) | CA2537098A1 (OSRAM) |
| ES (1) | ES2628959T3 (OSRAM) |
| IL (1) | IL173935A (OSRAM) |
| IS (1) | IS8384A (OSRAM) |
| MX (1) | MXPA06002268A (OSRAM) |
| NO (1) | NO20061432L (OSRAM) |
| RU (1) | RU2006109600A (OSRAM) |
| TW (1) | TW200524879A (OSRAM) |
| WO (1) | WO2005023251A1 (OSRAM) |
| ZA (1) | ZA200602588B (OSRAM) |
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2478374C (en) * | 2002-03-13 | 2009-01-06 | Eli M. Wallace | N3 alkylated benzimidazole derivatives as mek inhibitors |
| WO2005009975A2 (en) | 2003-07-24 | 2005-02-03 | Warner-Lambert Company Llc | Benzimidazole derivatives as mek inhibitors |
| US7538120B2 (en) * | 2003-09-03 | 2009-05-26 | Array Biopharma Inc. | Method of treating inflammatory diseases |
| US7144907B2 (en) * | 2003-09-03 | 2006-12-05 | Array Biopharma Inc. | Heterocyclic inhibitors of MEK and methods of use thereof |
| US7517994B2 (en) * | 2003-11-19 | 2009-04-14 | Array Biopharma Inc. | Heterocyclic inhibitors of MEK and methods of use thereof |
| JP4869075B2 (ja) * | 2003-11-19 | 2012-02-01 | アレイ バイオファーマ、インコーポレイテッド | Mekの複素環阻害剤及びその使用方法 |
| US7732616B2 (en) * | 2003-11-19 | 2010-06-08 | Array Biopharma Inc. | Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof |
| BRPI0416852A (pt) * | 2003-11-21 | 2007-02-27 | Array Biopharma Inc | inibidores da quinase akt |
| RU2500673C2 (ru) * | 2005-05-18 | 2013-12-10 | Астразенека Аб | Гетероциклические ингибиторы мек и способы их применения |
| EP1934174B1 (en) * | 2005-10-07 | 2011-04-06 | Exelixis, Inc. | Azetidines as mek inhibitors for the treatment of proliferative diseases |
| PL2090575T3 (pl) | 2005-11-15 | 2011-09-30 | Array Biopharma Inc | Sposoby i związki pośrednie do otrzymywania pochodnych N4-fenylo-chinazolino-4-aminy |
| 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 |
| RU2418790C3 (ru) * | 2005-12-21 | 2022-03-14 | Астразенека Аб | Новая гидросульфатная соль |
| TWI405756B (zh) | 2005-12-21 | 2013-08-21 | Array Biopharma Inc | 新穎硫酸氫鹽 |
| GB0601962D0 (en) | 2006-01-31 | 2006-03-15 | Ucb Sa | Therapeutic agents |
| WO2008006025A1 (en) | 2006-07-06 | 2008-01-10 | Array Biopharma Inc. | Dihydrofuro pyrimidines as akt protein kinase inhibitors |
| PL2049500T3 (pl) * | 2006-07-06 | 2012-02-29 | Array Biopharma Inc | Cyklopenta[d]pirymidyny jako inhibitory kinaz białkowych AKT |
| US8063050B2 (en) * | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| WO2008006039A1 (en) | 2006-07-06 | 2008-01-10 | Array Biopharma Inc. | Dihydrothieno pyrimidines as akt protein kinase inhibitors |
| US8492378B2 (en) | 2006-08-03 | 2013-07-23 | Takeda Pharmaceutical Company Limited | GSK-3β inhibitor |
| ATE511509T1 (de) | 2006-11-30 | 2011-06-15 | Genentech Inc | Azaindolylverbindungen und anwendungsverfahren |
| JP5311673B2 (ja) * | 2006-12-14 | 2013-10-09 | エグゼリクシス, インコーポレイテッド | Mek阻害剤の使用方法 |
| EP2404907B1 (en) * | 2007-07-05 | 2015-01-14 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| BRPI0813999A2 (pt) | 2007-07-05 | 2019-10-01 | Array Biopharma Inc | ciclopentanos de pirimidil como inibidores de akt proteína cinase |
| 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 |
| JP2010536723A (ja) * | 2007-08-16 | 2010-12-02 | エフ.ホフマン−ラ ロシュ アーゲー | 置換ヒダントイン |
| WO2009064675A1 (en) | 2007-11-12 | 2009-05-22 | Takeda Pharmaceutical Company Limited | Mapk/erk kinase inhibitors |
| US20100004247A1 (en) * | 2007-12-12 | 2010-01-07 | Astrazeneca Ab | Combination comprising a mek inhibitor and an aurora kinase inhibitor 188 |
| WO2009080523A1 (en) | 2007-12-20 | 2009-07-02 | F. Hoffmann-La Roche Ag | Substituted hydantoins as mek kinase inhibitors |
| AU2009204019B2 (en) * | 2008-01-09 | 2014-02-20 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentane as AKT protein kinase inhibitor |
| KR101624753B1 (ko) * | 2008-01-09 | 2016-05-26 | 어레이 바이오파마 인크. | Akt 단백질 키나제 저해물질로서의 수산화된 피리미딜 시클로펜탄 |
| EP2240494B1 (en) | 2008-01-21 | 2016-03-30 | UCB Biopharma SPRL | Thieno-pyridine derivatives as mek inhibitors |
| GB0811304D0 (en) | 2008-06-19 | 2008-07-30 | Ucb Pharma Sa | Therapeutic agents |
| KR20110028651A (ko) * | 2008-07-11 | 2011-03-21 | 노파르티스 아게 | (a) 포스포이노시타이드 3-키나제 억제제 및 (b) ras/raf/mek 경로의 조절제의 조합물 |
| WO2010051933A2 (en) | 2008-11-10 | 2010-05-14 | Bayer Schering Pharma Aktiengesellschaft | Substituted sulphonamido phenoxybenzamides |
| PE20121816A1 (es) * | 2009-10-12 | 2013-01-02 | Hoffmann La Roche | Combinaciones de un inhibidor de pi3k y un inhibidor de mek |
| US8962606B2 (en) | 2009-10-21 | 2015-02-24 | Bayer Intellectual Property Gmbh | Substituted benzosulphonamides |
| CA2777071A1 (en) | 2009-10-21 | 2011-04-28 | Bayer Pharma Aktiengesellschaft | Substituted halophenoxybenzamide derivatives |
| CA2777430A1 (en) | 2009-10-21 | 2011-04-28 | Bayer Pharma Aktiengesellschaft | Substituted benzosulphonamides |
| US20150141380A1 (en) | 2010-08-05 | 2015-05-21 | Case Western Reserve University | Inhibitors of erk for developmental disorders of neuronal connectivity |
| PE20140192A1 (es) | 2010-10-06 | 2014-02-24 | Glaxosmithkline Llc | Derivados de bencimidazol como inhibidores de cinasa pi3 |
| US9045429B2 (en) | 2010-10-29 | 2015-06-02 | Bayer Intellectual Property Gmbh | Substituted phenoxypyridines |
| 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 |
| HUE024504T2 (en) | 2010-12-23 | 2016-01-28 | Sanofi Sa | Pyrimidine derivatives, a process for their preparation and their use in medicine |
| BR112013025397A2 (pt) | 2011-04-01 | 2019-09-24 | Deepak Sampath | combinação de um composto, composto de fórmula i ou um sal farmaceuticamente aceitável do mesmo, uso, kit, produto, método para tratamento de um distúrbio hiperproliferativo e método para tratamento de uma doença ou afecção modulada por quinase akt em um mamífero |
| CA2831922C (en) | 2011-04-01 | 2019-12-31 | Genentech, Inc. | Combinations of akt inhibitor compounds and vemurafenib, and methods of use |
| ES2597052T3 (es) | 2011-05-25 | 2017-01-13 | Université Paris Descartes | Inhibidores de ERK para su uso en el tratamiento de atrofia muscular espinal |
| WO2013066483A1 (en) | 2011-08-31 | 2013-05-10 | Novartis Ag | Synergistic combinations of pi3k- and mek-inhibitors |
| CN103204827B (zh) | 2012-01-17 | 2014-12-03 | 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二唑化合物及其制备方法和用途 |
| EP2834237B1 (en) | 2012-03-14 | 2018-06-06 | Lupin Limited | Heterocyclyl compounds as mek inhibitors |
| AR091876A1 (es) * | 2012-07-26 | 2015-03-04 | Novartis Ag | Combinaciones farmaceuticas para el tratamiento de enfermedades proliferativas |
| HRP20180670T1 (hr) | 2012-10-12 | 2018-07-13 | Exelixis Inc. | Novi postupak dobivanja spojeva namijenjenih upotrebi u liječenju raka |
| AR099630A1 (es) | 2012-10-19 | 2016-08-10 | Novartis Ag | Preparación de un inhibidor de mek y formulación que lo comprende |
| WO2014097125A1 (en) * | 2012-12-20 | 2014-06-26 | Novartis Ag | Pharmaceutical combination comprising binimetinib |
| PT2976106T (pt) | 2013-03-21 | 2021-05-26 | Array Biopharma Inc | Terapia de combinação que compreende um inibidor de b-raf e um segundo inibidor |
| 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 |
| MX387795B (es) * | 2016-06-03 | 2025-03-19 | Array Biopharma Inc | Combinaciones farmaceuticas. |
| 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 |
| JP6974618B2 (ja) * | 2017-12-07 | 2021-12-01 | ハルビン チェンバオ ファーマシューティカル カンパニー リミテッド | Fgfr及びvegfr阻害剤としての化合物の塩形態、結晶形およびその製造方法 |
| ES3007082T3 (en) | 2018-09-18 | 2025-03-19 | Hoffmann La Roche | Quinazoline derivatives as antitumor agents |
| BR112021011894A2 (pt) | 2018-12-21 | 2021-09-08 | Daiichi Sankyo Company, Limited | Composição farmacêutica |
| 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 |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| 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 |
| WO2022251193A1 (en) | 2021-05-27 | 2022-12-01 | 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 |
| WO2023283425A1 (en) | 2021-07-09 | 2023-01-12 | Plexium, Inc. | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
| JP2024539212A (ja) | 2021-10-20 | 2024-10-28 | エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト | キナゾリン誘導体の結晶形態、調製、組成物およびその使用 |
| 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 |
| 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 |
| JP2002509536A (ja) | 1997-07-01 | 2002-03-26 | ワーナー−ランバート・カンパニー | 2−(4−ブロモ又は4−ヨードフェニルアミノ)安息香酸誘導体及びmek阻害物質としてのそれらの使用 |
| JP2002511092A (ja) | 1997-07-01 | 2002-04-09 | ワーナー−ランバート・コンパニー | 4−ブロモまたは4−ヨードフェニルアミノベンズヒドロキサム酸誘導体およびそのmek阻害剤としての使用 |
| 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 |
| 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 |
| CA2350234A1 (en) | 1999-01-07 | 2000-07-13 | Alexander James Bridges | Treatment of asthma with mek inhibitors |
| EP1140067A1 (en) | 1999-01-07 | 2001-10-10 | Warner-Lambert Company | Antiviral method using mek inhibitors |
| BR9916857A (pt) | 1999-01-13 | 2001-12-04 | Warner Lambert Co | 4 heteroaril diarilaminas |
| 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 |
| IL144214A0 (en) | 1999-01-13 | 2002-05-23 | Warner Lambert Co | Benzoheterocycles and their use as mek inhibitors |
| AP2001002225A0 (en) * | 1999-01-13 | 2001-09-30 | Warner Lambert Co | 1-heterocycle substituted diarylamines. |
| ATE311363T1 (de) | 1999-01-13 | 2005-12-15 | Warner Lambert Co | Sulfohydroxamsäure and sulfohydroxamate und ihre verwendung als mek-inhibitoren |
| EP1144371B1 (en) | 1999-01-13 | 2005-11-09 | Warner-Lambert Company Llc | Benzenesulphonamide derivatives and their use as mek inhibitors |
| GB9910577D0 (en) | 1999-05-08 | 1999-07-07 | Zeneca Ltd | Chemical compounds |
| CN1358094A (zh) | 1999-07-16 | 2002-07-10 | 沃尼尔·朗伯公司 | 用mek抑制剂治疗慢性疼痛的方法 |
| HUP0202381A3 (en) | 1999-07-16 | 2004-12-28 | Warner Lambert Co | 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 |
| AU5786000A (en) | 1999-07-16 | 2001-02-05 | Warner-Lambert Company | Method for treating chronic pain using mek inhibitors |
| JP2003504401A (ja) | 1999-07-16 | 2003-02-04 | ワーナー−ランバート・カンパニー | Mek阻害剤を用いる慢性疼痛の治療方法 |
| US7001905B2 (en) * | 2000-03-15 | 2006-02-21 | Warner-Lambert Company | Substituted diarylamines as MEK inhibitors |
| BR0109188A (pt) | 2000-03-15 | 2003-03-18 | Warner Lambert Co | Diarilaminas 5-amida substituìdas como inibidores de mex |
| IL153817A0 (en) | 2000-07-19 | 2003-07-31 | Warner Lambert Co | Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids |
| MXPA03001654A (es) | 2000-08-25 | 2004-09-10 | Warner Lambert Co | Proceso para la elaboracion del acido n-aril-antranilico y sus derivados. |
| 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 |
| CA2478534A1 (en) * | 2002-03-13 | 2003-09-25 | Array Biopharma, Inc. | N3 alkylated benzimidazole derivatives as mek inhibitors |
| CA2478374C (en) * | 2002-03-13 | 2009-01-06 | Eli M. Wallace | N3 alkylated benzimidazole derivatives as mek inhibitors |
| WO2005009975A2 (en) * | 2003-07-24 | 2005-02-03 | Warner-Lambert Company Llc | Benzimidazole derivatives as mek inhibitors |
-
2003
- 2003-08-29 US US10/652,733 patent/US7235537B2/en not_active Expired - Lifetime
-
2004
- 2004-08-20 AU AU2004270166A patent/AU2004270166A1/en not_active Abandoned
- 2004-08-20 ZA ZA200602588A patent/ZA200602588B/en unknown
- 2004-08-20 CA CA002537098A patent/CA2537098A1/en not_active Abandoned
- 2004-08-20 KR KR1020067004187A patent/KR20060121853A/ko not_active Withdrawn
- 2004-08-20 MX MXPA06002268A patent/MXPA06002268A/es unknown
- 2004-08-20 EP EP04781809.1A patent/EP1663210B1/en not_active Expired - Lifetime
- 2004-08-20 CN CNA2004800323322A patent/CN1874768A/zh active Pending
- 2004-08-20 JP JP2006524761A patent/JP5026076B2/ja not_active Expired - Lifetime
- 2004-08-20 RU RU2006109600/04A patent/RU2006109600A/ru not_active Application Discontinuation
- 2004-08-20 WO PCT/US2004/027199 patent/WO2005023251A1/en not_active Ceased
- 2004-08-20 ES ES04781809.1T patent/ES2628959T3/es not_active Expired - Lifetime
- 2004-08-20 TW TW093125125A patent/TW200524879A/zh unknown
- 2004-08-20 BR BRPI0413152-5A patent/BRPI0413152A/pt not_active Application Discontinuation
- 2004-08-27 AR ARP040103103A patent/AR045738A1/es not_active Application Discontinuation
-
2006
- 2006-02-26 IL IL173935A patent/IL173935A/en active IP Right Grant
- 2006-03-29 NO NO20061432A patent/NO20061432L/no not_active Application Discontinuation
- 2006-03-29 IS IS8384A patent/IS8384A/is unknown
-
2007
- 2007-06-14 US US11/762,897 patent/US7842816B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| WO2005023251A1 (en) | 2005-03-17 |
| ES2628959T3 (es) | 2017-08-04 |
| AU2004270166A1 (en) | 2005-03-17 |
| RU2006109600A (ru) | 2007-10-10 |
| EP1663210A1 (en) | 2006-06-07 |
| IL173935A (en) | 2015-08-31 |
| CN1874768A (zh) | 2006-12-06 |
| CA2537098A1 (en) | 2005-03-17 |
| KR20060121853A (ko) | 2006-11-29 |
| US20070299063A1 (en) | 2007-12-27 |
| US7235537B2 (en) | 2007-06-26 |
| IL173935A0 (en) | 2006-07-05 |
| BRPI0413152A (pt) | 2006-10-03 |
| JP2007504139A (ja) | 2007-03-01 |
| US20040116710A1 (en) | 2004-06-17 |
| US7842816B2 (en) | 2010-11-30 |
| IS8384A (is) | 2006-03-29 |
| NO20061432L (no) | 2006-08-25 |
| EP1663210B1 (en) | 2017-04-19 |
| EP1663210A4 (en) | 2009-04-22 |
| JP5026076B2 (ja) | 2012-09-12 |
| TW200524879A (en) | 2005-08-01 |
| ZA200602588B (en) | 2008-07-30 |
| MXPA06002268A (es) | 2006-05-31 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR045738A1 (es) | Derivados de bencimidazol n3 alquilados como inhibidores de mek | |
| AR038971A1 (es) | Derivados de bencimidazol n3 alquilado como inhibidores de mek | |
| AR119698A2 (es) | Compuesto amida n-urea sustituida derivado de aminoácido | |
| AR038881A1 (es) | Compuestos que modulan la actividad de ppar, composicion farmaceutica que los contiene y un procedimiento para la preparcion de aquellos | |
| AR051403A1 (es) | Derivados de purina, purinona y deazapurina como inhibidores de la actividad de la protein quinasa; metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la elaboracion de un medicamento para el tratamiento de enfermedades mediadas por la protein quinasa a y b. | |
| AR076460A1 (es) | Antagonistas del receptor cxcr3 | |
| AR038972A1 (es) | Derivados de bencimidazol n3 alquilado como inhibidores de mek | |
| AR083367A1 (es) | Compuestos de tipo quinazolinona como antagonistas de crth | |
| AR033379A1 (es) | Compuestos de difenilurea, procedimiento para su preparacion y composiciones farmaceuticas que los contienen | |
| AR044402A1 (es) | Compuestos heterociclicos y su uso como inmunodepresores. composiciones farmaceuticas que los contienen. | |
| AR039673A1 (es) | Derivados de heteroarilamida benzocondensada de tienopiridinas utiles como agentes terapeuticos, composiciones farmaceuticas que incluyen a los mismos y metodos para su aplicacion | |
| AR038883A1 (es) | Compuestos que modulan la actividad de ppar, composicion farmaceutica que los contiene y un metodo para prepararlos | |
| CL2020001343A1 (es) | Nuevos profármacos de catecolamina para uso en el tratamiento de la enfermedad de parkinson. | |
| AR044134A1 (es) | Derivados de quinuclidina, metodo de preparacion y composiciones farmaceuticas. | |
| AR085004A1 (es) | Inhibidores selectivos de glicosidasas y usos de los mismos | |
| AR072227A1 (es) | Derivados de triazinona sustituidos | |
| BRPI0619823A8 (pt) | compostos que são inibidores de erk | |
| CL2019002919A1 (es) | Compuestos inhibidores vmat2 y composiciones relacionadas. | |
| AR046272A1 (es) | Inhibidores de dipeptidil peptidasa iv | |
| BR112015015812A2 (pt) | derivados de pirimidina fundidos a pirido ou pirrolo como inibidores de autotaxina para tratamento de dor | |
| AR043199A1 (es) | Componentes heterociclicos utiles para el tratamiento de enfermedades inflamatorias y alergicas, proceso para su operacion y composicion farmaceutica que contiene dichos componentes | |
| AR046081A1 (es) | Inhibidores heterociclicos de mek y uso de los mismos | |
| CL2014003181A1 (es) | Compuestos derivados de benzamidas n- sustituidas o piridinamidas n-sustituidas; composicion farmaceutica que los comprende; metodo de tratamiento; y su uso para el tratamiento de enfermedades o trastornos seleccionados de dolor, depresion y enfermedades cardiovasculares, respiratorias o psiquiatricas o combinaciones de estas. | |
| UY28144A1 (es) | Agentes terapéuticos | |
| AR069510A1 (es) | Arilo y heteroarilo imidazo[1,5-a]pirazinas fusionadas como inhibidores de la fosfodiesterasa 10 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal | ||
| FA | Abandonment or withdrawal | ||
| FB | Suspension of granting procedure |