AR063625A1 - COMPUESTOS HETEROCICLICOS eTILES COMO AGENTES ANTICANCEROSOS - Google Patents
COMPUESTOS HETEROCICLICOS eTILES COMO AGENTES ANTICANCEROSOSInfo
- Publication number
- AR063625A1 AR063625A1 ARP070104984A ARP070104984A AR063625A1 AR 063625 A1 AR063625 A1 AR 063625A1 AR P070104984 A ARP070104984 A AR P070104984A AR P070104984 A ARP070104984 A AR P070104984A AR 063625 A1 AR063625 A1 AR 063625A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocyclyl
- carbamoyl
- optionally substituted
- carbon
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 31
- -1 cyano, hydroxy Chemical group 0.000 abstract 26
- 229910052757 nitrogen Inorganic materials 0.000 abstract 22
- 125000000623 heterocyclic group Chemical group 0.000 abstract 16
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 9
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 9
- 229910052799 carbon Inorganic materials 0.000 abstract 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 5
- 125000001475 halogen functional group Chemical group 0.000 abstract 5
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 abstract 4
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 abstract 4
- 125000004423 acyloxy group Chemical group 0.000 abstract 4
- 125000005236 alkanoylamino group Chemical group 0.000 abstract 4
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 4
- 125000001589 carboacyl group Chemical group 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 3
- 241001465754 Metazoa Species 0.000 abstract 2
- 230000001093 anti-cancer Effects 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 101000693265 Homo sapiens Sphingosine 1-phosphate receptor 1 Proteins 0.000 abstract 1
- 102100025750 Sphingosine 1-phosphate receptor 1 Human genes 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 abstract 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 abstract 1
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 abstract 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- 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
- C07D235/14—Radicals substituted by nitrogen atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
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- 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
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
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- 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
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- 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
- C07D405/12—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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- 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
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- 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
- C07D413/12—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 chain containing hetero atoms as chain links
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/40—Heterocyclic compounds containing purine ring systems with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Compuestos químicos que poseen actividad antagonista de Edg-1, y que, por consiguiente, son útiles debido a su actividad anticancerosa y por ende en los métodos de tratamiento del cuerpo humano o de animales. También se relaciona con procesos para la elaboración de dichos compuestos químicos, con composiciones farmacéuticas que los contienen y con su uso en la elaboración de medicamentos para la producción de un efecto anticanceroso en un animal de sangre caliente, tal como el hombre. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1) donde el Anillo A es carbociclilo o heterociclilo; en donde si dicho heterociclilo contiene una porción -NH- ese nitrógeno puede estar opcionalmente sustituido por un grupo seleccionado entre R6; R1se selecciona en forma independiente entre halo, nitro, ciano, hidroxi. amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, hidrazinilo, ureido, N,N- di(alquil C1-3)ureido, alcanoilo C1-6, alcanoiloxi C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbarnoilo, alquil C1-6S(O)a en donde a es entre 0 y 2, alcoxicarbonilo C1-6, N- (alquil C1-6)sulfamoilo, N,N-(alquil C1-6)2sulfamoilo, alquilsulfonilamino C1-6, carbociclilo, heterociclilo, en donde R1 puede estar sustituido opcionalmente en un carbono por uno o más R7, y en donde si dicho heterociclilo contiene una porción -NH- ese nitrógeno puede estar opcionalmente sustituido por un grupo seleccionado entre R8; n es 0-5; en donde los valores de R1 pueden ser iguales o diferente; R2 se selecciona entre alquilo C1-6, alquenilo C2-6 o alquinilo C2-6, carbociclilo, y heterociclilo; en donde R2 puede estar sustituido opcionalmente en un carbono por uno o más R9; en donde si dicho heterociclilo contiene una porción NH ese nitrógeno puede estar opcionalmente sustituido por un grupo seleccionado entre R19; R3 se selecciona entre hidrógeno, alquilo C1-6, alquenilo C2-6 o alquinilo C2-6, carbociclilo, heterociclilo; en donde R3 puede estar sustituido opcionalmente en un carbono por uno o más R11; en donde si dicho heterociclilo contiene una porción NH ese nitrógeno puede estar opcionalmente sustituido por un grupo seleccionado entre R20; o, como alternativa. R2 y R3 pueden formar, junto con el carbono al cual están unidos, un anillo carbocíclico C3-6, R4 se selecciona entre alquilo C1-6 o carbociclilo, en donde R4 puede estar sustituido opcionalmente en un carbono por uno o más R10; el Anillo D está fusionado al imidazol de fórmula (1) y es un anillo de 5-7 miembros; en donde si dicho anillo contiene una porción -NH- ese nitrógeno puede estar opcionalmente sustituido por un grupo seleccionado entre R14; R5 es un sustituyente sobre carbono y se selecciona en forma independiente entre halo, nitro, ciano, hidroxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, alcanoiloxi C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)2carbarnoilo, alquil C1-6S(O)a en donde a es entre 0 y 2, alcoxicarbonilo C1-6, heterociclilcarbonilo, N-(alquil C1-6)sulfamoilo, N,N-(alquil C1-6)2sulfamoilo, alquilsulfonilamino C1-6, carbociclilo o heterociclilo, o dos R5 pueden formar junto con los átomos de carbono del anillo D a los cuales están unidos un anillo carbociclilo o heterociclilo de 5 a 8 miembros; en donde R5 puede estar sustituido opcionalmente en un carbono por uno o más R15; y en donde si dicho heterociclilo o anillo heterocíclico contiene una porción -NH- ese nitrógeno puede estar opcionalmente sustituido por un grupo seleccionado entre R16; m es 0-5; en donde los valores de R5 pueden ser iguales o diferentes, R7, R9, R11 y R15 se seleccionan en forma independiente entre halo, nitro, ciano, hidroxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C1-6, alcanoiloxi C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N-(alquil C1- 6)2carbarnoilo, alquil C1-6S(O)a en donde a es entre 0 y 2, alcoxicarbonilo C1-6, N-(alquil C1-6)sulfamoilo, N,N-(alquil C1-6)2sulfamoilo, alquilsulfonilamino C1-6, carbociclilo o heterociclilo, en donde R7, R9, R11 y R15 pueden estar opcionalmente sustituidos sobre carbono en forma independiente por uno o más R17; y en donde si dicho heterociclilo contiene una porción -NH- ese nitrógeno puede estar opcionalmente sustituido por un grupo seleccionado entre R18; R6, R8, R13, R14, R16, R18, R19 y R20 se seleccionan en forma independiente entre alquilo C1-6, alcanoilo C1-6, alquilsulfonilo C1-6, alcoxicarbonilo C1-6, carbamoilo, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)carbamoilo, bencilo, benciloxicarbonilo, benzoilo y fenilsulfonil; R10 se selecciona entre halo, nitro, hidroxi, amino, carboxi, mercapto, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcanoilo C1-6, alcanoiloxi C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1- 6)carbamoilo, N,N-(alquil C1-6)2carbarnoilo, alquil C1-6S(O)a en donde a es entre 0 y 2, alcoxicarbonilo C1-6, N-(alquil C1-6)sulfamoilo, N,N-(alquil C1-6)2sulfamoilo, alquilsulfonilamino C1-6, carbociclilo o heterociclilo, en donde R10 puede estar sustituido opcionalmente en un carbono por uno o más R12; y en donde si dicho heterociclilo contiene una porción -NH- ese nitrógeno pude estar opcionalmente sustituido por un grupo seleccionado entre R13; R12 y R13 se seleccionan entre halo, nitro, ciano, hidroxi, trifluorometoxi, trifluorometilo, amino, carboxi, carbamoilo, mercapto, sulfamoilo, metilo, etilo metoxi, etoxi, acetilo, acetoxi, metilamino, etilamino, dimetilamino, dietilamino, N-metil-N-etilamino, acetilamino, N-metilcarbamoilo, N-etilcarbamoilo, N,N-dimetilcarbamoilo, N,N-dietilcarbamoilo, N-metil-N-etilcarbamoilo, metiltio, etiltio, metilsulfinilo, etilsulfinilo, mesilo, etilsulfonilo, metoxicarbonilo, etoxicarbonilo, N-metilsulfamoilo, N-etilsulfamoilo, N,N- dimetilsulfamoilo, N,N-dietilsulfamoilo o N-metil-N-etilsulfamoilo; o una sal aceptable para uso farmacéutico del mismo; con la salvedad de que el compuesto no sea 4-metil-N-[(1-metil-1H-bencimidazol-2-il)fenilmetil]bencensulfonamida.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US86536406P | 2006-11-10 | 2006-11-10 | |
| US89569907P | 2007-03-19 | 2007-03-19 | |
| US94779507P | 2007-07-03 | 2007-07-03 | |
| US95383807P | 2007-08-03 | 2007-08-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR063625A1 true AR063625A1 (es) | 2009-02-04 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070104984A AR063625A1 (es) | 2006-11-10 | 2007-11-08 | COMPUESTOS HETEROCICLICOS eTILES COMO AGENTES ANTICANCEROSOS |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20100029643A1 (es) |
| EP (1) | EP2094670A1 (es) |
| JP (1) | JP2010509301A (es) |
| KR (1) | KR20090089338A (es) |
| AR (1) | AR063625A1 (es) |
| AU (1) | AU2007319061A1 (es) |
| BR (1) | BRPI0718759A2 (es) |
| CA (1) | CA2668785A1 (es) |
| EC (1) | ECSP099382A (es) |
| IL (1) | IL198658A0 (es) |
| MX (1) | MX2009004906A (es) |
| NO (1) | NO20091703L (es) |
| PE (1) | PE20081492A1 (es) |
| TW (1) | TW200827340A (es) |
| WO (1) | WO2008056150A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009019506A1 (en) * | 2007-08-03 | 2009-02-12 | Astrazeneca Ab | Heterocyclyc sulfonamides having edg-1 antagonistic activity |
| DE102007037579B4 (de) * | 2007-08-09 | 2012-05-16 | Emc Microcollections Gmbh | Neue Benzimidazol-2-yl-alkylamine und ihre Anwendung als mikrobizide Wirkstoffe |
| NZ590285A (en) * | 2008-07-15 | 2012-10-26 | Novartis Ag | Heteroaryl derivatives as dgat1 inhibitors |
| US8288627B2 (en) * | 2009-05-13 | 2012-10-16 | Monsanto Technology Llc | Plants and seeds of hybrid corn variety CH532948 |
| KR101632318B1 (ko) | 2009-11-05 | 2016-06-27 | 재단법인 의약바이오컨버젼스연구단 | 벤조헤테로사이클 유도체 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 암 예방 및 치료용 조성물 |
| ES2786298T3 (es) * | 2011-03-03 | 2020-10-09 | Zalicus Pharmaceuticals Ltd | Inhibidores de benzimidazol del canal de sodio |
| US9051311B2 (en) | 2012-03-09 | 2015-06-09 | Amgen Inc. | Sulfamide sodium channel inhibitors |
| CN112055713A (zh) | 2018-03-01 | 2020-12-08 | 安娜普尔纳生物股份有限公司 | 用于治疗与apj受体活性有关的疾病的化合物和组合物 |
| IL282021B2 (en) * | 2018-10-05 | 2025-04-01 | Annapurna Bio Inc | Compounds and compositions for treating conditions associated with APJ receptor activity |
| US11891374B2 (en) * | 2020-01-17 | 2024-02-06 | Boris Farber | Derivatized benzimidazole compounds, their salts, their complexes, their pharmaceutical compositions and methods for using them for antigeriatric actions |
| CN113461611B (zh) * | 2021-07-08 | 2023-02-28 | 江苏法安德医药科技有限公司 | 一种咪喹莫特中间体的合成方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5128940B2 (ja) * | 2004-06-18 | 2013-01-23 | スリーエム イノベイティブ プロパティズ カンパニー | 置換イミダゾキノリン、イミダゾピリジン、およびイミダゾナフチリジン |
| US8022225B2 (en) * | 2004-08-04 | 2011-09-20 | Taisho Pharmaceutical Co., Ltd | Triazole derivative |
| WO2007112322A2 (en) * | 2006-03-28 | 2007-10-04 | Allergan, Inc. | Indole compounds having sphingosine-1-phosphate (s1p) receptor agonist and/or antagonist biological activity |
| EP2013186A1 (en) * | 2006-04-21 | 2009-01-14 | AstraZeneca AB | Imidazole derivatives for use as edg-1 antagonists |
-
2007
- 2007-11-07 TW TW096142125A patent/TW200827340A/zh unknown
- 2007-11-08 EP EP07824500A patent/EP2094670A1/en not_active Withdrawn
- 2007-11-08 US US12/514,247 patent/US20100029643A1/en not_active Abandoned
- 2007-11-08 WO PCT/GB2007/004267 patent/WO2008056150A1/en not_active Ceased
- 2007-11-08 AU AU2007319061A patent/AU2007319061A1/en not_active Abandoned
- 2007-11-08 JP JP2009535799A patent/JP2010509301A/ja active Pending
- 2007-11-08 AR ARP070104984A patent/AR063625A1/es not_active Application Discontinuation
- 2007-11-08 KR KR1020097010603A patent/KR20090089338A/ko not_active Withdrawn
- 2007-11-08 CA CA002668785A patent/CA2668785A1/en not_active Abandoned
- 2007-11-08 BR BRPI0718759-9A patent/BRPI0718759A2/pt not_active IP Right Cessation
- 2007-11-08 MX MX2009004906A patent/MX2009004906A/es not_active Application Discontinuation
- 2007-11-09 PE PE2007001547A patent/PE20081492A1/es not_active Application Discontinuation
-
2009
- 2009-04-29 NO NO20091703A patent/NO20091703L/no not_active Application Discontinuation
- 2009-05-07 IL IL198658A patent/IL198658A0/en unknown
- 2009-06-03 EC EC2009009382A patent/ECSP099382A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PE20081492A1 (es) | 2008-12-07 |
| EP2094670A1 (en) | 2009-09-02 |
| NO20091703L (no) | 2009-05-29 |
| BRPI0718759A2 (pt) | 2013-12-03 |
| TW200827340A (en) | 2008-07-01 |
| KR20090089338A (ko) | 2009-08-21 |
| JP2010509301A (ja) | 2010-03-25 |
| IL198658A0 (en) | 2010-02-17 |
| US20100029643A1 (en) | 2010-02-04 |
| CA2668785A1 (en) | 2008-05-15 |
| WO2008056150A1 (en) | 2008-05-15 |
| MX2009004906A (es) | 2009-07-09 |
| ECSP099382A (es) | 2009-07-31 |
| AU2007319061A1 (en) | 2008-05-15 |
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