AR037090A1 - Compuestos pirazolilo sustituidos para el tratamiento de inflamaciones - Google Patents
Compuestos pirazolilo sustituidos para el tratamiento de inflamacionesInfo
- Publication number
- AR037090A1 AR037090A1 ARP020103533A ARP020103533A AR037090A1 AR 037090 A1 AR037090 A1 AR 037090A1 AR P020103533 A ARP020103533 A AR P020103533A AR P020103533 A ARP020103533 A AR P020103533A AR 037090 A1 AR037090 A1 AR 037090A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- heteroaryl
- aryl
- hydride
- Prior art date
Links
- 206010061218 Inflammation Diseases 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 28
- 125000003118 aryl group Chemical group 0.000 abstract 21
- 125000001072 heteroaryl group Chemical group 0.000 abstract 20
- 150000004678 hydrides Chemical class 0.000 abstract 19
- 125000001188 haloalkyl group Chemical group 0.000 abstract 17
- 125000000623 heterocyclic group Chemical group 0.000 abstract 17
- -1 amino Chemical group 0.000 abstract 13
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 12
- 229910052736 halogen Inorganic materials 0.000 abstract 12
- 150000002367 halogens Chemical class 0.000 abstract 12
- 125000003342 alkenyl group Chemical group 0.000 abstract 11
- 125000003545 alkoxy group Chemical group 0.000 abstract 10
- 125000000304 alkynyl group Chemical group 0.000 abstract 9
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 9
- 125000005343 heterocyclic alkyl group Chemical group 0.000 abstract 9
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 8
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 8
- 125000000278 alkyl amino alkyl group Chemical group 0.000 abstract 6
- 125000003282 alkyl amino group Chemical group 0.000 abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 6
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 5
- 125000001691 aryl alkyl amino group Chemical group 0.000 abstract 5
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 5
- 125000005842 heteroatom Chemical group 0.000 abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 abstract 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 4
- 125000002252 acyl group Chemical group 0.000 abstract 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 3
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 101100274896 Arabidopsis thaliana CAMTA5 gene Proteins 0.000 abstract 2
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 2
- 101100477978 Hypocrea jecorina (strain QM6a) sor6 gene Proteins 0.000 abstract 2
- 125000004442 acylamino group Chemical group 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 abstract 2
- 150000002334 glycols Chemical class 0.000 abstract 2
- 230000004054 inflammatory process Effects 0.000 abstract 2
- RAHZWNYVWXNFOC-UHFFFAOYSA-N sulfur dioxide Inorganic materials O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 125000001054 5 membered carbocyclic group Chemical group 0.000 abstract 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 abstract 1
- 101100516563 Caenorhabditis elegans nhr-6 gene Proteins 0.000 abstract 1
- 101100079984 Caenorhabditis elegans nhr-9 gene Proteins 0.000 abstract 1
- 101100134929 Gallus gallus COR9 gene Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-M Thiocyanate anion Chemical compound [S-]C#N ZMZDMBWJUHKJPS-UHFFFAOYSA-M 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000006323 alkenyl amino group Chemical group 0.000 abstract 1
- 125000004422 alkyl sulphonamide group Chemical group 0.000 abstract 1
- 125000006319 alkynyl amino group Chemical group 0.000 abstract 1
- 125000000266 alpha-aminoacyl group Chemical group 0.000 abstract 1
- 125000003368 amide group Chemical group 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 abstract 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N hydrogen thiocyanate Natural products SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 abstract 1
- 150000002540 isothiocyanates Chemical class 0.000 abstract 1
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Chemical group 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004001 thioalkyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 to carbon atoms of the hetero ring
-
- 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
- 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
- C07D405/10—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 aromatic 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
- C07D405/12—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
- 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
- C07D405/14—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 three or more hetero rings
-
- 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
-
- 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
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
-
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un compuesto para tratar el cáncer, la inflamación y trastornos relacionados con la inflamación, por ejemplo la artritis. Reivindicación 1: Un compuesto caracterizado porque responde a la formula (1) donde A es (CH2)m; donde cada CH2 se puede sustituir independientemente con una o más sustituciones seleccionadas del grupo formado por: hidroxi, halógeno, alcoxi, alquilo inferior, amino, aminoalquilo, alquilamino, alquenilo, y alquinilo; m es entre 1 y 4; B es un heterocíclico heteroarilo, arilo, saturado o insaturado de 5 ó 6 miembros donde dicho arilo, heteroarilo, ó heterocíclico se sustituyen opcionalmente con R1, R2, y R12; X se selecciona del grupo formado por: N y C; Y y Z se seleccionan independientemente del grupo formado por: N, CH, CR3, S, y O; R1 se selecciona del grupo formado por: hidruro, halógeno, alquilo, arilo, heteroarilo, alquenilo, alquinilo, haloalquilo, CN, NO2, OR5, OCOOR5, CO2R7, CON(R6)R7, COR6, SR6, SOR6, SO2R6, NR6R7, NR6COR7, NR6CONHR7, NR6SO2R7, NR6SO2NHR7, y SO2N(R6)R7 donde R6 y R7 se pueden tomar juntos para formar un anillo carbocíclico de 3-7 miembros con entre 1 y 3 heteroátomos sustituidos ó insustituidos seleccionados del grupo formado por: S, SO, SO2, O, y NR6; donde dichos alquenilo, alquinilo, alquilo, arilo, heteroarilo ó OR5 son opcionalmente sustituidos con, hidruro, halógeno, alquilo, hidroxialquilo, arilo, heteroarilo, haloalquilo, COCF3, CN, NO2, OR5, OCOOR5, CO2R7, CON(R6)R7, COR6, SR6, SOR6, SO2R6, NR6R7, NR6COR7, NR6CONHR7, NR6SO2R7, NR6SO2NHR7, y SO2N(R6)R7 donde R6 y R7 se pueden tomar juntos para formar un anillo carbocíclico de 3-7 miembros con entre 1 y 3 heteroátomos sustituidos ó insustituidos seleccionados del grupo formado por: S, SO, SO2, O, y NR6; R2 se selecciona del grupo formado por: halógeno, hidruro, hidroxialquilo, alquilo, OR6, CN, NO2, SR6, NHR6, CON(R6)R7, NHCONHR6, CO2H, y haloalquilo; R1 y R2 se pueden tomar juntos para formar un anillo carbocíclico saturado o insaturado de 5 a 7 miembros que contiene opcionalmente entre 0 y 3 heteroátomos seleccionados del grupo formado por N, O, ó S, y donde dicho anillo es opcionalmente sustituido con R1; R3 se selecciona del grupo formado por: amida sustituida ó insustituida, alquilamino, aminoalquilo, CONHR7, NH2, NHCOR6, y CH2NHCOR6 con la condición de que cuando R3 es NH2 ó NHCH3, entonces R1, R2, R4, R11, y R12 no son hidruro; R4 se selecciona del grupo formado por: halógeno, alquilsulfinilo, alquilsulfonilo, ciano, alcoxicarbonilo, alquilo, haloalquilo, hidruro, hidroxialquilo, haloalcoxi, heterocíclico, nitro, acilamino, arilo, heteroarilo, y alquenilo, OR13, SR8, SO2N(R8)R8', NHR9, NHCOR9, NR9COR9, NHCO(OR9), NR9CO(OR9), NR8SO2R10, NHSO2N(R10)R10', NR6CON(R10)R10', COR9, CO2R8, CON(R8)R8', donde R8 y R8' se pueden tomar juntos para formar un anillo carbocíclico de 3-7 miembros con entre 1 y 3 heteroátomos sustituidos ó insustituidos seleccionados entre S, SO, SO2, O, N, y NR6, y donde R10 y R10' se pueden tomar juntos para formar un anillo carbocíclico de 3-7 miembros con entre 1 y 3 heteroátomos sustituidos ó insustituidos seleccionados entre S, SO, SO2, O, N, y NR6 donde dicho arilo, heterocíclico, heteroarilo, ó alquenilo se sustituyen opcionalmente con R9; R5 se selecciona del grupo formado por: hidruro, alquilo, arilo, arilalquilo, heteroarilo, heterocíclicoalquilo, y heteroarilalquilo, donde arilo, alquilo, arilalquilo, heteroarilo, heterocíclicoalquilo, ó heteroarilalquilo se sustituyen opcionalmente con uno o más radicales seleccionados del grupo formado por OR14, N(R14)R14', y glicoles; R6 se selecciona independientemente del grupo formado por: hidruro, arilo, heteroarilo, alquilo inferior, haloalquilo, alquenilo, alquinilo, hidroxialquilo, aminoalquilo, alquilaminoalquilo, alcoxi, alcoxialquilo, heterocíclicoalquilo, y heterocíclico; R7 se selecciona independientemente del grupo formado por: hidruro, arilo, heteroarilo, alquilo inferior, haloalquilo, alquenilo, alquinilo, hidroxialquilo, aminoalquilo, alquilaminoalquilo, alcoxi, alcoxialquilo, heterocíclicoalquilo, y heterocíclico; R8 se selecciona independientemente del grupo formado por: hidruro, arilo, heteroarilo, arilalquilo, heterocíclico, haloalquilo, arilalquilamino, alquilaminoalquilo, dialquilaminoalquilo, alquilo, alquenilo, alquinilo, heteroarilalquilo, y heterocíclicoalquilo; R8' se selecciona independientemente del grupo formado por: hidruro, arilo, heteroarilo, arilalquilo, heterocíclico, haloalquilo, arilalquilamino, alquilaminoalquilo, dialquilaminoalquilo, alquilo, alquenilo, alquinilo, heteroarilalquilo, y heterocíclicoalquilo; R9 se selecciona independientemente del grupo formado por: hidruro, alquilo inferior, arilo, heteroarilo, arilalquilo, heterocíclico, cicloalquilo, heterocíclicoalquilo, haloalquilo, arilalquilamino, amino, aminoalquilo, aminoacilo, nitro, azido, y heteroarilalquilo, donde alquilo, arilo, heteroarilo, aminoalquilo, ó arilalquilo se sustituyen opcionalmente con uno o más radicales seleccionados del grupo formado por: alquilsulfonamida, sulfamilo, alquilo, alquiltio, alquilsulfinilo, alquilsulfonilo, alquilamino, aminoalquilo, alquilaminoalquilo, alcoxi, halógeno, aciloxi, oxi, formilo, haloalquilo, ciano, haloalcoxi, acilo, carboxilo, hidroxi, hidroxialquiloxi, fenoxi, nitro, azido, benciloxi, dialquilaminoacilo, tioalquilo, aminoaciloxi, tiocianato, isotiocianato, alquildioxi, hidroxialquilo, alquilamino, alquiloxicarbonilo, alcoxialquilo, alquenilamino, alquinilamino, alquenilo, alquinilo, dialquilaminoalquiloxi, y heterocíclico opcionalmente sustituido con alquilo, alquilamino, aminoalquilo, hidroxialquilo, y alquilaminoalquilo; R10 se selecciona independientemente del grupo formado por: hidruro, alquilo inferior, heteroarilo, heterocíclico, haloalquilo, arilalquilamino, heteroarilalquilo, arilo, y arilalquilo, donde arilo, heteroarilo, heterocíclico, ó arilalquilo se sustituyen opcionalmente con uno o más radicales seleccionados entre alquilo, alcoxi, halógeno, haloalquilo, ciano, haloalcoxi, acilo, carboxilo, hidroxi, hidroxialquiloxi, fenoxi, benciloxi, dialquilaminoalquiloxi, y heterocíclico; R10' se selecciona independientemente del grupo formado por: hidruro, alquilo inferior, heteroarilo, heterocíclico, haloalquilo, arilalquilamino, heteroarilalquilo, arilo, y arilalquilo, donde arilo, heteroarilo, heterocíclico, ó arilalquilo se sustituyen opcionalmente con uno o más radicales seleccionados entre alquilo, alcoxi, halógeno, haloalquilo, ciano, haloalcoxi, acilo, carboxilo, hidroxi, hidroxialquiloxi, fenoxi, benciloxi, dialquilaminoalquiloxi, y heterocíclico, R11 se selecciona del grupo formado por: hidruro, halógeno, haloalquilo, CN, CO2R5, alquilo inferior, alquenilo inferior, alquinilo inferior, alcoxi, y CONH2; R12 se selecciona del grupo formado por: hidruro, halógeno, alquilo, y alcoxi; R13 se selecciona del grupo formado por: hidruro, alquilo, arilo, arilalquilo, heteroarilo, heterocíclicoalquilo, y heteroarilalquilo, donde arilo, alquilo, arilalquilo, heteroarilo, heterocíclicoalquilo, ó heteroarilalquilo se sustituyen opcionalmente con uno o más radicales seleccionados del grupo formado por OR14, N(R14)R14', y glicoles; R14 se selecciona independientemente del grupo formado por hidruro, y alquilo inferior; y R14' se selecciona independientemente del grupo formado por hidruro, y alquilo inferior; con la condición de que cuando R1 es sulfamilo, entonces R4 no es halógeno, alquiltio, alquilsulfinilo, alquilsulfonilo, ciano, carboxilo, alcoxicarbonilo, amido, N-monoalquilamido, N-monoarilamido, alquilo, N,N-dialquilamido, N-alquil-N-arilamido, haloalquilo, hidruro, hidroxilo, alcoxi, hidroxialquilo, haloalcoxi, sulfamilo, N-alquilsulfamilo, amino, alquilamino, heterocíclico, nitro, y acilamino, y/o cuando R4 es sulfamilo, entonces R1 no es sulfamilo, halógeno, alquilo, alcoxi, hidroxilo y haloalquilo; ó isómeros, vehículos, ésteres, profármacos, sales aceptables para uso farmacéutico del mismo.mismo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32342301P | 2001-09-19 | 2001-09-19 | |
| US37909002P | 2002-05-09 | 2002-05-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR037090A1 true AR037090A1 (es) | 2004-10-20 |
Family
ID=26983952
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020103533A AR037090A1 (es) | 2001-09-19 | 2002-09-19 | Compuestos pirazolilo sustituidos para el tratamiento de inflamaciones |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US6956052B2 (es) |
| EP (1) | EP1444207A2 (es) |
| JP (2) | JP2005506983A (es) |
| AR (1) | AR037090A1 (es) |
| AU (1) | AU2002341729A1 (es) |
| BR (1) | BR0212611A (es) |
| CA (1) | CA2460942A1 (es) |
| MX (1) | MXPA04002667A (es) |
| WO (1) | WO2003024935A2 (es) |
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| JP2006512313A (ja) | 2002-10-31 | 2006-04-13 | アムジェン インコーポレイテッド | 抗炎症剤 |
| WO2005061519A1 (en) * | 2003-12-19 | 2005-07-07 | Takeda San Diego, Inc. | Kinase inhibitors |
| GB0400895D0 (en) * | 2004-01-15 | 2004-02-18 | Smithkline Beecham Corp | Chemical compounds |
| JP2007533753A (ja) * | 2004-04-23 | 2007-11-22 | タケダ サン ディエゴ インコーポレイテッド | インドール誘導体及びキナーゼ阻害剤としてのその使用 |
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| EP1778669A2 (en) * | 2004-08-18 | 2007-05-02 | Takeda San Diego, Inc. | Kinase inhibitors |
| PE20060748A1 (es) | 2004-09-21 | 2006-10-01 | Smithkline Beecham Corp | Derivados de indolcarboxamida como inhibidores de quinasa ikk2 |
| DE602005023333D1 (de) * | 2004-10-15 | 2010-10-14 | Takeda Pharmaceutical | Kinaseinhibitoren |
| KR20080021077A (ko) | 2005-06-30 | 2008-03-06 | 스미스클라인 비참 코포레이션 | 화합물 |
| US8063071B2 (en) | 2007-10-31 | 2011-11-22 | GlaxoSmithKline, LLC | Chemical compounds |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| CA2641441A1 (en) * | 2006-02-09 | 2007-08-23 | Athersys, Inc. | Pyrazoles for the treatment of obesity and other cns disorders |
| GEP20135728B (en) | 2006-10-09 | 2013-01-25 | Takeda Pharmaceuticals Co | Kinase inhibitors |
| EP2223925A1 (en) * | 2006-10-09 | 2010-09-01 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| AR065804A1 (es) | 2007-03-23 | 2009-07-01 | Smithkline Beecham Corp | Compuesto de indol carboxamida, composicion farmaceutica que lo comprende y uso de dicho compuesto para preparar un medicamento |
| US11969501B2 (en) | 2008-04-21 | 2024-04-30 | Dompé Farmaceutici S.P.A. | Auris formulations for treating otic diseases and conditions |
| KR20190026056A (ko) | 2008-04-21 | 2019-03-12 | 오토노미, 인코포레이티드 | 귀 질환 및 병태를 치료하기 위한 귀 조제물 |
| WO2010102968A1 (en) | 2009-03-10 | 2010-09-16 | Glaxo Group Limited | Indole derivatives as ikk2 inhibitors |
| TW201116515A (en) | 2009-07-31 | 2011-05-16 | Organon Nv | Dihydrobenzoindazoles |
| US8830866B2 (en) * | 2009-09-30 | 2014-09-09 | Apple Inc. | Methods and apparatus for solicited activation for protected wireless networking |
| TW201118073A (en) * | 2009-10-30 | 2011-06-01 | Merck Sharp & Dohme | Hexahydrocyclopentyl [F] indazole pyridyl ethanols and derivatives thereof as selective glucocorticoid receptor modulators |
| LT2651902T (lt) | 2010-12-17 | 2018-01-10 | Reata Pharmaceuticals, Inc. | Tricikliniai pirazolil- ir pirimidinilenonai, kaip antioksidantų uždegimo moduliatoriai |
| EP2904119B1 (en) | 2012-10-02 | 2020-06-17 | The General Hospital Corporation d/b/a Massachusetts General Hospital | Methods relating to dna-sensing pathway related conditions |
| US9604316B2 (en) * | 2014-09-23 | 2017-03-28 | Globalfoundries Inc. | Tin-based solder composition with low void characteristic |
| CN106632050B (zh) * | 2015-11-04 | 2019-08-13 | 中国人民解放军第二军医大学 | 苯并吲唑类衍生物及其制备方法、应用 |
| CN105646467B (zh) * | 2016-02-25 | 2018-07-20 | 黄燕鸽 | 一种抗癌化合物奥美替尼及其合成方法 |
| KR20190024983A (ko) | 2016-06-29 | 2019-03-08 | 오토노미, 인코포레이티드 | 트리글리세라이드 귀 제제 및 이의 용도 |
| CN106614663A (zh) * | 2016-12-29 | 2017-05-10 | 新沂市中诺新材料科技有限公司 | 一种新型纳米级吲唑类农药合成方法 |
| US20220380310A1 (en) * | 2019-07-01 | 2022-12-01 | Ligang Qian | P2x7r antagonists |
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| GB8814587D0 (en) | 1988-06-20 | 1988-07-27 | Erba Carlo Spa | Condensed pyrazole 3-oxo-propanenitrile derivatives & process for their preparation |
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| GB8916290D0 (en) | 1989-07-17 | 1989-08-31 | Erba Carlo Spa | Heteroaryl-3-oxo-propanenitrile derivatives useful in stimulating myelopoiesis |
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| US5387693A (en) * | 1991-08-08 | 1995-02-07 | Ortho Pharmaceutical Corporation | Tetrahydroindazole, tetrahydrocyclopentapyrazole, and hexahydrocycloheptapyrazole intermediate compounds |
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| WO1999017769A1 (en) | 1997-10-06 | 1999-04-15 | Basf Aktiengesellschaft | INDENO[1,2-c]-, NAPHTHO[1,2-c]- AND BENZO[6,7]CYCLOHEPTA[1,2-c]PYRAZOLE DERIVATIVES |
| TR200102277T2 (tr) | 1998-11-06 | 2002-01-21 | Basf Aktiengesellschaft Ag. | Üç halkalı (Trisiklik) pirazol türevleri |
| BR0009561A (pt) | 1999-04-06 | 2002-04-16 | Knoll Gmbh | 1,4-didro indeno [1,2-c] pirazóis substituìdos como inbidores de tirosina cinase |
| AU4308300A (en) * | 1999-05-03 | 2000-11-17 | Dr. Reddy's Research Foundation | Pyrazoles having antiinflammatory activity |
| FR2800375B1 (fr) | 1999-11-03 | 2004-07-23 | Sanofi Synthelabo | Derives tricycliques d'acide pyrazolecarboxylique, leur preparation, les compositions pharmaceutiques en contenant |
| GB0003154D0 (en) | 2000-02-12 | 2000-04-05 | Astrazeneca Uk Ltd | Novel compounds |
| EP1142889A1 (en) | 2000-04-03 | 2001-10-10 | Pfizer Products Inc. | Pyrazole derivatives as anti-inflammatory/analgesic agents |
| JP2005506983A (ja) * | 2001-09-19 | 2005-03-10 | ファルマシア・コーポレーション | 炎症の治療のための置換ピラゾリル化合物 |
-
2002
- 2002-09-19 JP JP2003528783A patent/JP2005506983A/ja not_active Ceased
- 2002-09-19 CA CA002460942A patent/CA2460942A1/en not_active Abandoned
- 2002-09-19 AU AU2002341729A patent/AU2002341729A1/en not_active Abandoned
- 2002-09-19 AR ARP020103533A patent/AR037090A1/es unknown
- 2002-09-19 BR BR0212611-7A patent/BR0212611A/pt not_active IP Right Cessation
- 2002-09-19 EP EP02775879A patent/EP1444207A2/en not_active Withdrawn
- 2002-09-19 MX MXPA04002667A patent/MXPA04002667A/es unknown
- 2002-09-19 WO PCT/US2002/029774 patent/WO2003024935A2/en active Application Filing
- 2002-09-19 US US10/247,096 patent/US6956052B2/en not_active Expired - Fee Related
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2005
- 2005-04-25 US US11/113,926 patent/US7186743B2/en not_active Expired - Fee Related
-
2008
- 2008-07-22 JP JP2008188020A patent/JP2009029808A/ja not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CA2460942A1 (en) | 2003-03-27 |
| US6956052B2 (en) | 2005-10-18 |
| US7186743B2 (en) | 2007-03-06 |
| US20050256180A1 (en) | 2005-11-17 |
| WO2003024935A3 (en) | 2003-08-21 |
| US20040110741A1 (en) | 2004-06-10 |
| EP1444207A2 (en) | 2004-08-11 |
| JP2005506983A (ja) | 2005-03-10 |
| AU2002341729A1 (en) | 2003-04-01 |
| JP2009029808A (ja) | 2009-02-12 |
| MXPA04002667A (es) | 2004-06-18 |
| WO2003024935A2 (en) | 2003-03-27 |
| BR0212611A (pt) | 2004-08-17 |
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