AR035580A1 - Compuestos inhibidores de ifata, compuestos intermediarios, procedimientos de preparacion y su uso en la preparacion de medicamentos - Google Patents

Compuestos inhibidores de ifata, compuestos intermediarios, procedimientos de preparacion y su uso en la preparacion de medicamentos

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Publication number
AR035580A1
AR035580A1 ARP010103900A ARP010103900A AR035580A1 AR 035580 A1 AR035580 A1 AR 035580A1 AR P010103900 A ARP010103900 A AR P010103900A AR P010103900 A ARP010103900 A AR P010103900A AR 035580 A1 AR035580 A1 AR 035580A1
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AR
Argentina
Prior art keywords
bond
halo
nr11r12
aryl
alkyl
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ARP010103900A
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English (en)
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Pfizer
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Publication date
Priority claimed from GB0020346A external-priority patent/GB0020346D0/en
Priority claimed from GB0027409A external-priority patent/GB0027409D0/en
Priority claimed from GB0029556A external-priority patent/GB0029556D0/en
Application filed by Pfizer filed Critical Pfizer
Publication of AR035580A1 publication Critical patent/AR035580A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
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    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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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    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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

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  • Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
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Abstract

Compuestos de fórmula (1) donde X es N o CH, n es 0 a 3; R1 es: (a)alquilo C1-6 de cadena lineal o ramificada, (b) alquenilo C1-6 de cadena lineal o ramificada, (c) alquinilo C1-6 de cadena lineal o ramificada, (d) heterociclo, (e) heterociclo aromático, (f) arilo, (g) hidrógeno; estando los citados grupos (a), (b) y (c) opcionalmente sustituidos adicionalmente con: cicloalquilo C3-7, arilo, heterociclo aromático, heterociclo, OR11, NR11R12, S(O)pR11, OC(O)R11, CO2R11, CONR11R12, SO2NR11R12, halo y NHSO2R11, pudiendo estar R1 unido en cualquier posición en el anillo de imidazol; R2 y R3 se seleccionan cada uno independientemente de hidrógeno, alquilo C1-6, opcionalmente sustituido adicionalmente con OR11, halo; o pudiendo estar R2 y R3 unidos para formar un enlace, siendo el citado enlace alquileno C2-6; R4 es hidrógeno, alquilo C1-6, opcionalmente sustituido adicionalmente con cicloalquilo C3-7, arilo, OR11, halo y R11; o pudiendo estar R4 y R10 unidos para formar un enlace, siendo dicho enlace alquileno C1-4, opcionalmente sustituido adicionalmente con OR11, halo y R11; R5 y R6 se seleccionan de: hidrógeno, arilo, alquilo C1-6, estando el citado alquilo opcionalmente sustituido adicionalmente con cicloalquilo C3-7, heterociclo aromático, heterociclo, arilo, OR11, R11 y halo; o pudiendo estar R10 y cualquiera de R5 y R6 unidos para formar un enlace, siendo el citado enlace un alquileno C1-3, opcionalmente sustituido adicionalmente con OR11, halo, R11 y arilo; o pudiendo estar R5 y R6 unidos para formar un enlace, siendo el citado enlace alquileno C2-6; R7 y R8 se seleccionan independientemente de: hidrógeno, alquilo C1-6 opcionalmente sustituido adicionalmente con OR11, halo, arilo y R11; o pudiendo estar R7 y R8 unidos para formar un enlace, siendo el citado enlace alquileno C2-6; R9 y R10 se seleccionan independientemente de: hidrógeno, C(NR11)NR11R12, alquilo C1-6, estando el citado alquilo opcionalmente sustituido con OR11, halo, arilo y R11; o pudiendo estar R9 y R10 unidos para formar un enlace, siendo el citado enlace alquileno C2-6; R11 y R12 se seleccionan cada uno independientemente de hidrógeno o alquilo C1-6; o cuando forman un resto NR11R12, R11 y R12 pueden estar también unidos para formar un enlace, siendo el citado enlace alquileno C2-6; p es 0, 1 o 2; en la que: arilo se define como un carbociclo aromático de 6 a 14 miembros, opcionalmente sustituido adicionalmente con R11, halo, OR11, NR11R12, NR11CO2R12, CO2R11, NR11SO2R12, CN, haloalquilo, O(haloalquilo), S(O)pR11, OC(O)R11, SO2NR11R12, C(O)NR11R12; heterociclo aromático se define como un anillo de 5 a 7 miembros que contiene de 1 a 3 heteroátomos, seleccionado cada uno independientemente de O, S y N, estando el citado grupo heterociclo opcionalmente sustituido con OR11, NR11R12, CO2R11, NR11CO2R12, R11, halo, CN, haloalquilo, O(haloalquilo), S(O)pR11, OC(O)R11, NR11SO2R12, SO2NR11R12, C(O)NR11R12; se define heterociclo como un anillo de 3 a 8 miembros que contiene de 1 a 3 heteroátomos seleccionados cada uno independientemente de O, S y N, estando el citado anillo saturado o parcialmente saturado, estando el citado grupo heterociclo opcionalmente sustituido adicionalmente con OR11, NR11R12, CO2R11, NR11CO2R12, R11, halo, CN, haloalquilo, O(haloalquilo), S(O)pR11, OC(O)R11, NR11SO2R12, SO2NR11R12, C(O)NR11R12; o una sal, solvato o profármaco farmacéuticamente aceptable de éstos. Estos compuestos son una clase de inhibidores de IFATa. Dichos compuestos son adecuados para uso en el tratamiento de afecciones tales como trombosis, arteriosclerosis, adherencias, cicatrices dérmicas, cáncer, afecciones fibróticas, enfermedades inflamatorias y aquellas afecciones que se benefician del mantenimiento o la potenciación de los niveles de bradiquinina en el cuerpo. Se describen también compuestos intermediarios, procedimientos de preparación y su uso en la preparación de medicamentos.
ARP010103900A 2000-08-17 2001-08-15 Compuestos inhibidores de ifata, compuestos intermediarios, procedimientos de preparacion y su uso en la preparacion de medicamentos AR035580A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0020346A GB0020346D0 (en) 2000-08-17 2000-08-17 Pharmaceuticals
GB0027409A GB0027409D0 (en) 2000-11-09 2000-11-09 Pharmaceuticals
GB0029556A GB0029556D0 (en) 2000-12-04 2000-12-04 Pharmaceuticals

Publications (1)

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AR035580A1 true AR035580A1 (es) 2004-06-16

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ARP010103900A AR035580A1 (es) 2000-08-17 2001-08-15 Compuestos inhibidores de ifata, compuestos intermediarios, procedimientos de preparacion y su uso en la preparacion de medicamentos

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EP (1) EP1311488B1 (es)
JP (2) JP4119746B2 (es)
KR (1) KR20030022412A (es)
CN (1) CN1443173A (es)
AP (1) AP1375A (es)
AR (1) AR035580A1 (es)
AT (1) ATE447557T1 (es)
AU (1) AU2001276605A1 (es)
BG (1) BG107330A (es)
BR (1) BR0113289A (es)
CA (1) CA2419633C (es)
CY (1) CY1109693T1 (es)
CZ (1) CZ2003388A3 (es)
DE (1) DE60140368D1 (es)
DK (1) DK1311488T3 (es)
DO (1) DOP2001000233A (es)
EA (1) EA005532B1 (es)
EE (1) EE200300070A (es)
ES (1) ES2334101T3 (es)
HR (1) HRP20030103A2 (es)
HU (1) HUP0303763A3 (es)
IL (1) IL153225A0 (es)
IS (1) IS6638A (es)
MA (1) MA26940A1 (es)
MX (1) MXPA03001425A (es)
NO (1) NO20030706L (es)
NZ (1) NZ522823A (es)
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PA (1) PA8525401A1 (es)
PE (1) PE20020352A1 (es)
PL (1) PL361054A1 (es)
PT (1) PT1311488E (es)
SI (1) SI1311488T1 (es)
SK (1) SK1732003A3 (es)
SV (1) SV2002000602A (es)
TN (1) TNSN01126A1 (es)
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WO (1) WO2002014285A1 (es)

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WO2013039202A1 (ja) * 2011-09-15 2013-03-21 第一三共株式会社 新規アクリル酸誘導体
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EP3359528B1 (en) 2015-10-07 2022-01-12 Mitobridge, Inc. Ppar agonists, compounds, pharmaceutical compositions, and methods of use thereof
FR3046793B1 (fr) * 2016-01-14 2018-01-05 Les Laboratoires Servier Nouveaux derives de phosphinanes et azaphosphinanes, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JPWO2017170460A1 (ja) * 2016-03-29 2019-02-07 第一三共株式会社 炎症性腸疾患治療剤
WO2017180818A1 (en) 2016-04-13 2017-10-19 Mitobridge, Inc. Ppar agonists, compounds, pharmaceutical compositions, and methods of use thereof
CN113943255B (zh) * 2020-07-17 2024-08-06 深圳信立泰药业股份有限公司 一种手性3-(4-环丙基-2,5-二氧杂咪唑啉-4-基)丙酸的制备方法

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