AR045626A1 - Derivados del bencil- bencimidazolilo - Google Patents
Derivados del bencil- bencimidazoliloInfo
- Publication number
- AR045626A1 AR045626A1 ARP040103244A ARP040103244A AR045626A1 AR 045626 A1 AR045626 A1 AR 045626A1 AR P040103244 A ARP040103244 A AR P040103244A AR P040103244 A ARP040103244 A AR P040103244A AR 045626 A1 AR045626 A1 AR 045626A1
- Authority
- AR
- Argentina
- Prior art keywords
- cooa
- hal
- cooh
- mono
- conh2
- Prior art date
Links
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 4
- -1 benzyl benzimidazolyl Chemical class 0.000 abstract 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 3
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 2
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000000565 sulfonamide group Chemical group 0.000 abstract 2
- 102100022014 Angiopoietin-1 receptor Human genes 0.000 abstract 1
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical group O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 abstract 1
- 108091008794 FGF receptors Proteins 0.000 abstract 1
- 101000753291 Homo sapiens Angiopoietin-1 receptor Proteins 0.000 abstract 1
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 abstract 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 abstract 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 abstract 1
- 108091008605 VEGF receptors Proteins 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 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
- C07D235/24—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Nuevos derivados de bencil-bencimidazolilo como inhibidores de las tirosina quinasas, en especial de TIE-2, VEGFR, PDGFR, FGFR y/o FLT/KDR para el tratamiento de tumores y de enfermedades no cancerosas, según la fórmula (1), en donde R1, R2 son en cada caso, de modo independiente entre sí, R, Hal, CN, NO2, NHR, NR2, NHCOR, NHSO2R, OR, COR, CONHR, SF3, SO3R, SO2R, SO2NR2, SR, COOH, o COOA, en donde dos radicales R2 también pueden ser humanos -O-CH2-O- u -O-CH2-CH2-O-; R es H, A, Ar, Het, (CH2)pAr, o (CH2)pHet; p es 1, 2 ó 3; Ar es fenilo o naftilo insustituido o mono, di o trisustituido con A, Hal, OH, OA, CN, NO2, NH2, NHA, NA2, NHCOA, SCF3, SO2A, COOH, COOA, CONH2, CONHA, CONA2, NHSO2A, SO2NH2, SO2NHA, SO2NA2, CHO o COA, A es alquilo no ramificado, ramificado o cíclico C1-10, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH- y/o también 1-7 átomos de H pueden estar reemplazados por F y/o Cl y en donde A puede estar mono, di o trisustituidos con COOH, OH, COOA' o CONH2; Het es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que está insustituido o mono, di o trisustituido con el oxígeno del carbonilo, Hal, A, -(CH2)n- Ar, -(CH2)n-cicloalquilo, OH, OA, NH2, NHA, NA2, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 y/o S(O)mA; A' puede ser alquilo no ramificado, ramificado o cíclico C1-6; m es 0, 1 ó 2; n es 0, 1, 2, 3 ó 4; Hal es F, Cl, Br o I; r es 0, 1, 2, 3 ó 4; s es 0, 1, 2, 3, 4 ó 5, así como sus derivados, sales, solvatos y estereoisómeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10342503A DE10342503A1 (de) | 2003-09-12 | 2003-09-12 | Benzyl-Benzimidazolylderivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045626A1 true AR045626A1 (es) | 2005-11-02 |
Family
ID=34305752
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040103244A AR045626A1 (es) | 2003-09-12 | 2004-09-10 | Derivados del bencil- bencimidazolilo |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20070066606A1 (es) |
| EP (1) | EP1663988B1 (es) |
| JP (1) | JP4921168B2 (es) |
| AR (1) | AR045626A1 (es) |
| AU (1) | AU2004274118B2 (es) |
| CA (1) | CA2538743C (es) |
| DE (1) | DE10342503A1 (es) |
| WO (1) | WO2005028448A1 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007022947A2 (de) * | 2005-08-21 | 2007-03-01 | Abbott Gmbh & Co. Kg | 5-ring-heteroaromaten-verbindungen und ihre verwendung als bindungspartner für 5-ht5-rezeptoren |
| AU2006311914C1 (en) * | 2005-11-03 | 2013-10-24 | Chembridge Corporation | Heterocyclic compounds as tyrosine kinase modulators |
| US8147828B2 (en) | 2006-04-17 | 2012-04-03 | Ludwig Institute For Cancer Research | Methods and compositions for modulation of blood-neural barrier |
| WO2008153701A1 (en) * | 2007-05-24 | 2008-12-18 | Schering Corporation | Compounds for inhibiting ksp kinesin activity |
| EP2671891A3 (en) | 2008-06-27 | 2014-03-05 | Amgen Inc. | Ang-2 inhibition to treat multiple sclerosis |
| EP2400985A2 (en) | 2009-02-25 | 2012-01-04 | OSI Pharmaceuticals, LLC | Combination of an either an anti-igf-1r antibody or an igf binding protein and a small molecule igf-1r kinase inhibitor |
| EP2401613A2 (en) | 2009-02-27 | 2012-01-04 | OSI Pharmaceuticals, LLC | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| US8642834B2 (en) | 2009-02-27 | 2014-02-04 | OSI Pharmaceuticals, LLC | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| WO2010099138A2 (en) | 2009-02-27 | 2010-09-02 | Osi Pharmaceuticals, Inc. | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| JO2860B1 (en) * | 2009-05-07 | 2015-03-15 | ايلي ليلي اند كومباني | Phenylendazolyl compounds |
| ES2616238T3 (es) * | 2010-10-06 | 2017-06-12 | Glaxosmithkline Llc, Corporation Service Company | Derivados de bencimidazol como inhibidores de PI3 quinasa |
| AU2012220601B2 (en) | 2011-02-24 | 2017-03-09 | Cephalon, Inc. | Vinyl -aryl - sulfones for use in peritoneal carcinomatosis |
| EP2702173A1 (en) | 2011-04-25 | 2014-03-05 | OSI Pharmaceuticals, LLC | Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment |
| WO2013152252A1 (en) | 2012-04-06 | 2013-10-10 | OSI Pharmaceuticals, LLC | Combination anti-cancer therapy |
| AU2014247941C1 (en) | 2013-04-04 | 2019-10-31 | University Of Maryland, Baltimore | Nonsteroidal and steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity |
| WO2014176259A1 (en) | 2013-04-22 | 2014-10-30 | Icahn School Of Medicine At Mount Sinai | Mutations in pdgfrb and notch3 as causes of autosomal dominant infantile myofibromatosis |
| PE20180573A1 (es) * | 2015-07-20 | 2018-04-04 | Genzyme Corp | Inhibidores del receptor del factor estimulador de colonias 1 (csf-1r) |
| JP2024500919A (ja) | 2020-12-23 | 2024-01-10 | ジェンザイム・コーポレーション | 重水素化コロニー刺激因子－１受容体（ｃｓｆ－１ｒ）阻害剤 |
| CN116444544A (zh) * | 2022-01-10 | 2023-07-18 | 中国科学院上海药物研究所 | 苯并咪唑类化合物及其医药用途 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU168095B (es) * | 1973-05-09 | 1976-02-28 | ||
| US4004016A (en) * | 1975-08-11 | 1977-01-18 | E. R. Squibb & Sons, Inc. | Amino-benzimidazole derivatives |
| US5314903A (en) * | 1991-12-03 | 1994-05-24 | Neurosearch A/S | Benzimidazole compounds useful as calcium channel blockers |
| DK154092D0 (da) * | 1992-12-23 | 1992-12-23 | Neurosearch As | Imidazolforbindelser, deres fremstilling og anvendelse |
| US6194447B1 (en) * | 1998-07-02 | 2001-02-27 | Neurosearch A/S | Bis (benzimidazole) derivatives serving as potassium blocking agents |
| WO2000001676A1 (en) * | 1998-07-02 | 2000-01-13 | Neurosearch A/S | Potassium channel blocking agents |
| US6348032B1 (en) * | 1998-11-23 | 2002-02-19 | Cell Pathways, Inc. | Method of inhibiting neoplastic cells with benzimidazole derivatives |
| US20020065296A1 (en) | 1999-01-13 | 2002-05-30 | Bayer Corporation | Heteroaryl ureas containing nitrogen hetero-atoms as p38 kinase inhibitors |
| JP2000281659A (ja) * | 1999-03-30 | 2000-10-10 | Sumitomo Pharmaceut Co Ltd | チオウレア誘導体 |
| EP1189609A4 (en) * | 1999-05-03 | 2002-10-30 | Smithkline Beecham Corp | CXCR-4 RECEPTOR ANTAGONISTS AND THROMBOPOIETIN MIMETIKA |
| US6506769B2 (en) * | 1999-10-06 | 2003-01-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | Heterocyclic compounds useful as inhibitors of tyrosine kinases |
| ES2225231T3 (es) * | 1999-10-06 | 2005-03-16 | Boehringer Ingelheim Pharmaceuticals Inc. | Compuestos heterociclicos, utiles como inhibidores de tirosina quinasas. |
| US7238813B2 (en) * | 2000-11-29 | 2007-07-03 | Smithkline Beecham Corporation | Chemical compounds |
| CA2477505A1 (en) * | 2002-03-01 | 2003-09-12 | Smithkline Beecham Corporation | Diamino-pyrimidines and their use as angiogenesis inhibitors |
-
2003
- 2003-09-12 DE DE10342503A patent/DE10342503A1/de not_active Withdrawn
-
2004
- 2004-08-17 AU AU2004274118A patent/AU2004274118B2/en not_active Ceased
- 2004-08-17 JP JP2006525666A patent/JP4921168B2/ja not_active Expired - Fee Related
- 2004-08-17 US US10/571,587 patent/US20070066606A1/en not_active Abandoned
- 2004-08-17 WO PCT/EP2004/009205 patent/WO2005028448A1/de active Application Filing
- 2004-08-17 CA CA2538743A patent/CA2538743C/en not_active Expired - Fee Related
- 2004-08-17 EP EP04764195.6A patent/EP1663988B1/de not_active Expired - Lifetime
- 2004-09-10 AR ARP040103244A patent/AR045626A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DE10342503A1 (de) | 2005-04-14 |
| EP1663988A1 (de) | 2006-06-07 |
| AU2004274118B2 (en) | 2010-08-12 |
| JP4921168B2 (ja) | 2012-04-25 |
| CA2538743A1 (en) | 2005-03-31 |
| US20070066606A1 (en) | 2007-03-22 |
| EP1663988B1 (de) | 2014-04-16 |
| CA2538743C (en) | 2012-04-24 |
| AU2004274118A1 (en) | 2005-03-31 |
| JP2007505057A (ja) | 2007-03-08 |
| WO2005028448A1 (de) | 2005-03-31 |
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Legal Events
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| FB | Suspension of granting procedure |