AR044163A1 - Derivados de pirazol sustituidos, composiciones farmaceuticas que los contienen y compuestos relacionados como antagonistas del receptor de bradiquinina b1 - Google Patents

Derivados de pirazol sustituidos, composiciones farmaceuticas que los contienen y compuestos relacionados como antagonistas del receptor de bradiquinina b1

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AR044163A1
AR044163A1 ARP040101509A ARP040101509A AR044163A1 AR 044163 A1 AR044163 A1 AR 044163A1 AR P040101509 A ARP040101509 A AR P040101509A AR P040101509 A ARP040101509 A AR P040101509A AR 044163 A1 AR044163 A1 AR 044163A1
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Argentina
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substituted
methyl
heteroaryl
heterocyclic
alkyl
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Elan Pharm Inc
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    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D231/16—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
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    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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
    • 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
    • C07D471/08—Bridged systems
    • 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
    • C07D487/08—Bridged systems

Abstract

Compuestos que son antagonistas de los receptores de bradiquinina B1, composiciones farmacéuticas que los contienen y son útiles para tratar enfermedades, o aliviar síntomas adversos asociados con estados patológicos, en mamíferos provocados por el receptor de la bradiquinina B1. Algunos de los compuestos presentan mayor potencia y también se espera que presenten una acción más prolongada. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1) y/o fórmula (2): donde Z se selecciona entre O, S y NH; Q se selecciona entre el grupo formado por -NR4R5, -OH, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, cicloalquilo, cicloalquilo sustituido, heterocíclico, heterocíclico sustituido, alcoxi, alcoxi sustituido, arilo, arilo sustituido, heteroarilo, y heteroarilo sustituido; R1 se selecciona entre el grupo formado por H, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, arilo sustituido, cicloalquilo, cicloalquilo sustituido, heteroarilo, heteroarilo sustituido; heterocíclico y heterocíclico sustituido; R2 y R3 se seleccionan en forma independiente entre el grupo formado por H: alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, arilo sustituido, cicloalquilo, cicloalquilo sustituido, heteroarilo, heteroarilo sustituido; heterocíclico y heterocíclico sustituido; R4 y R5 se seleccionan en forma independiente entre el grupo formado por H, alquilo, alquilo sustituido, alcoxi, alcoxi sustituido, cicloalquilo, cicloalquilo sustituido, heterocíclico, heterocíclico sustituido y donde R4 y R5, junto con el átomo de N al cual están unidos se unen para formar un heterocíclico, un heterocíclico sustituido, un heteroarilo o un grupo heteroarilo sustituido, con la condición de que cuando R4 o R5 es un grupo alquilo sustituido este grupo no es -CHRa-C(O)-NRbRc o -CHRa-C(O)-ORb, donde Ra es la cadena lateral de un aminoácido natural o no natural, y Rb y Rc se seleccionan en forma independiente entre el grupo formado por H, alquilo, alquilo sustituido, arilo, arilo sustituido, heteroarilo o heteroarilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, cicloalquilo, cicloalquilo sustituido, heterocíclico, y heterocíclico sustituido; X se selecciona entre el grupo formado por H, halógeno, alquilo, alquilo sustituido, nitro, ciano, hidroxilo, alcoxi, alcoxi sustituido, carboxi, ésteres carboxílicos, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, amino, amino sustituido, acilamino, aminoacilo, y -C(O)NR7R8 donde R7 y R8 se seleccionan en forma independiente entre el grupo formado por H, alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, heterocíclico y heterocíclico sustituido, o R7 y R8 junto con el átomo de N al cual están unidos formar un heteroarilo, heteroarilo sustituido, heterocíclico, y heterocíclico sustituido, o sus sales aceptables para uso farmacéutico, prodrogas o isómeros; con las siguiente salvedades; A) cuando Z es O; R2 es H; R3 es 5-(2,4-diclorofenil)-imidazol-4-iliden-[2-metil-4-(N-(1-metilsufonilet-2-il)-N-etilamino)fenil]amina; X es H; y R1 es 1-(3-t-butil-4-hidroxifeniloxi)tridec-1-ilo; entonces Q no es etoxi; B) cuando Z es O; R2 es H; R3 es 4-clorofenilo; X es aminoacilo; y R1 es metilo o fenilo; entonces Q no es metilo; C) cuando Z es O; R2 es H; R3 es 4-clorofenilo o 4-metilfenilo; X es ciano; y R1 es metilo; entonces Q no es metilo; D) cuando Z es O; R2 es H; R3 es H; X es H; y R1 es 1-[(1-ciclohexil-2-(furan-3-il)-1H-benzoimidazol-5-il)acilamino]ciclopent-1-ilo; entonces Q no es hidroxi, E) cuando Z es O; R2 es H; R3 es H; X es H; y R1 es 3-isobutoxi-5-isopropoxifenilo o isopropilo; entonces Q no es metoxi; F) cuando Z es O; R2 es H; R3 es metilo; X es H; y R1 es 2-metil-3-acetamidopirazol-5-ilo; entonces Q no es hidroxi o metoxi; G) cuando Z es O; R2 es H; R3 es H; X es isobutoxicarbonilo o n-propoxicarbonilo; y R1 es metilo; entonces Q no es metoxi; H) cuando Z es O; R2 es H; R3 es metilo; X es H; y R1 es 2-(3-trifluorometil-fenoxi)piridin-3-ilo; entonces Q no es etoxi; I) cuando Z es O; R2 es 3-cianobencilo; R3 es metilo; X es H; y R1 es metilo; entonces Q no es isopropilo; J) cuando Z´ es O; R2 es H; R3 es metilo; X es H; y R1 es 1-metil-3-(benciloxicarbonilamino)pirazol-5-ilo; entonces Q no es N,N-dimetilamino-etilamino, metoxi o hidroxi; K) cuando Z´es O; R2 es H; R3 es metilo; X es H; y R1 es 1-metil-3-(N,N-dimetilaminoetilcarbonilamino)pirazol-5-ilo; entonces Q no es N,N-dimetilamino-etilamino; L) cuando Z´es O; R2 es H; R3 es metilo; X es H; y R1 es 1-metil-5-aminopirazol-3-ilo; entonces Q no es N,N-dimetilaminoetilamino o metoxi; M) cuando Z´ es O; R2 es H; R3 es metilo; X es H; y R1 es 1-metil-5-acetamidopirazol-3-il-; entonces Q no es hidroxi o metoxi; N) cuando Z´es O; R2 es H; R3 es metilo; X es H; y R1 es 1-metil-5-(benciloxicarbonilamino)pirazol-3-ilo; entonces Q no es N,N-dimetilaminoetilamino, metoxi o hidroxi; O) cuando Z´es O; R2 es H; R3 es metilo; X es H; y R1 es 1-metil-5-(N,N-dimetilaminoetilcarbonilamino)pirazol-3-ilo; entonces Q no es N,N-dimetilamino-etilamino; P) cuando Z´ es O; R2 es H; R3 es metilo; X es H; y R1 es 1-metil-5-metilcarbonilaminopirazol-3-ilo; entonces Q no es 1-clorometil-5-nitro-2,3-dihidro-1(H)-benzo[e]indol-3-ilo o 1-clorometil-5-amino-2,3-dihidro-1(H)-benzo[e]indol-3-ilo; Q) cuando Z´es O; R2 es H; R3 es fenilo; X es benzotiazol-2-ilo; y R1 es metilo; entonces Q no es etoxi; o R) cuando Q es -NR4R5, -OH, alcoxi o alcoxi sustituido; R1 es arilo sustituido o heteroarilo sustituido, el grupo arilo o heteroarilo no está sustituido con -C(O)NH-W´-C(O)ORb o -C(O)NH-W´-C(O)NRbRc, donde W es arilo, arilo sustituido, heteroarilo o heteroarilo sustituido; y con la salvedad adicional de que el compuesto en la fórmula (1) no es A´) ácido 4-bromo-5-(2-cloro-benzoilamino)-1H-pirazol-3-carboxílico; o B´) (2-dimetilamino-1-metil-etil)-amida del ácido 5-(2-cloro-benzoilamino)-1H-pirazol-3-carboxílico.
ARP040101509A 2003-05-02 2004-05-03 Derivados de pirazol sustituidos, composiciones farmaceuticas que los contienen y compuestos relacionados como antagonistas del receptor de bradiquinina b1 AR044163A1 (es)

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US46769503P 2003-05-02 2003-05-02
US53954604P 2004-01-27 2004-01-27

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US (2) US7417152B2 (es)
EP (1) EP1633348B1 (es)
JP (1) JP2006526015A (es)
AR (1) AR044163A1 (es)
AT (1) ATE410161T1 (es)
CA (1) CA2524269A1 (es)
DE (1) DE602004016992D1 (es)
ES (1) ES2314418T3 (es)
PE (1) PE20050525A1 (es)
TW (1) TW200509910A (es)
WO (1) WO2004098589A1 (es)

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