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AR058405A1 - Amidas inhibidoras de leucotrieno a4 hidrolasa - Google Patents

Amidas inhibidoras de leucotrieno a4 hidrolasa

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Publication number
AR058405A1
AR058405A1 ARP060105807A ARP060105807A AR058405A1 AR 058405 A1 AR058405 A1 AR 058405A1 AR P060105807 A ARP060105807 A AR P060105807A AR P060105807 A ARP060105807 A AR P060105807A AR 058405 A1 AR058405 A1 AR 058405A1
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AR
Argentina
Prior art keywords
optionally substituted
heterocyclyl
linear
attached
branched
Prior art date
Application number
ARP060105807A
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English (en)
Inventor
Thomas Kirkland
William Guilford
Monica Kochanny
David Vogel
David Davey
Ming Chen
David R Light
Arwed Cleve
Emmanuel Claret
Seock-Kyu Khim
John Parkinson
Amy Liang
Guo Ping Wei
Hong Ye
Bin Ye
Original Assignee
Schering Ag
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Publication date
Application filed by Schering Ag filed Critical Schering Ag
Publication of AR058405A1 publication Critical patent/AR058405A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/40—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/42—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/46—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups containing any of the groups, X being a hetero atom, Y being any atom, e.g. acylureas
    • C07C275/58—Y being a hetero atom
    • C07C275/62—Y being a nitrogen atom, e.g. biuret
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/09—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton the carbon skeleton being further substituted by at least two halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

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  • Heart & Thoracic Surgery (AREA)
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Estos compuestos son amidas inhibidoras de leucotrieno A4 hidrolasa y que son por lo tanto utiles en el tratamiento de trastornos inflamatorios. Composiciones farmacéuticas que comprenden estos compuestos. Reivindicacion 1: Un compuesto de formula (1), donde R es i) el grupo de formula (2) o ii) el grupo de formula (3), o iii) un heteroarilo opcionalmente sustituido; n1, n2, y n3 son en forma independiente entre sí entre 0 y 2; r es entre 0 y 4; q es entre 0 y 2; R1a, R1b, R1c, R1d y R1e se seleccionan en forma independiente entre sí entre hidrogeno, -R14-OR11, -R14-C(=O)OR11, -R14-C(=O)R11, alquilo, halo, haloalquilo, ciano, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroarilalquilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, o heterociclilalquilo opcionalmente sustituido; o R1a y R1d, junto con los átomos de carbono a los cuales están unidos, forman un heteroarilo opcionalmente sustituido o heterociclilo opcionalmente sustituido; R1v, R1w, R1x, R1y y R1z son en forma independiente entre sí hidrogeno o fluoro; R2 es hidrogeno, -R13-OR11, -R13- N(R11)R12, -R14-C(=O)OR11, -R14-C(=O)N(R11)R12, alquilo, haloalquilo, haloalquenilo, haloalquinilo, hidroxialquilo, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroarilalquilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, o heterociclilalquilo opcionalmente sustituido; o R2 y R7, junto con los átomos de nitrogeno a los cuales están unidos, forman un N-heterociclilo opcionalmente sustituido de entre 5 y 7 miembros; o R2 y R7, junto con los átomos de nitrogeno a los cuales están unidos y uno de R5a, R5b y R5c, forman un N-heterociclilo en puente opcionalmente sustituido de entre 6 y 10 miembros; o R2 y R5a, junto con el nitrogeno y el carbono al cual están unidos, forman un N-heterociclilo opcionalmente sustituido de entre 5 y 7 miembros o un N-heterociclilo en puente opcionalmente sustituido de entre 6 y 10 miembros; o R2 y R5b, junto con el nitrogeno y el carbono al cual están unidos, forman un N-heterociclilo opcionalmente sustituido de entre 5 y 7 miembros; o R2 y R5c, junto con el nitrogeno y el carbono al cual están unidos, forman un N- heterociclilo opcionalmente sustituido de entre 5 y 7 miembros; o R2 y R8, junto con el nitrogeno al cual están unidos, forman un N-heterociclilo opcionalmente sustituido o un N-heteroarilo opcionalmente sustituido; R3 es un enlace directo, -O-, - R13-O-, -O-R13-, -O-R13-O-, una cadena alquileno lineal o ramificada opcionalmente sustituida, una cadena alquenileno lineal o ramificada opcionalmente sustituida, o una cadena alquinileno lineal o ramificada opcionalmente sustituida; R4a, R4b y R4c son en forma independiente entre sí un enlace directo o una cadena alquileno lineal o ramificada opcionalmente sustituida, una cadena alquenileno lineal o ramificada opcionalmente sustituida, o una cadena alquinileno lineal o ramificada opcionalmente sustituida; cada R5a, R5b, R5c, R6a, R6b y R6c es en forma independiente hidrogeno, alquilo, haloalquilo, hidroxialquilo, aralquilo opcionalmente sustituido o -R14-C(=O)OR11; o R5a y R5b, junto con los átomos de carbono a los cuales están unidos, forman un cicloalquilo opcionalmente sustituido de entre 3 y 7 miembros; o R5b y R6b, junto con el carbono al cual están unidos, forman un cicloalquilo opcionalmente sustituido de entre 3 y 7 miembros; o R5a y R6a juntos, R5b y R6b juntos, o R5c y R6c juntos pueden formar un oxo; R7 es hidrogeno, -R13-OR11, -R14-C(=O)R11, -R14-C(=O)OR11, -R14-C(=O)-R14-N(R11)R12, -R13-N(R11)C(=O)N(R11)R12, alquilo, haloalquilo, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilalquilo opcionalmente sustituido, o heterociclilalquilo opcionalmente sustituido; o R7 y R5a, junto con el nitrogeno y el carbono al cual están unidos, forman un N-heterociclilo opcionalmente sustituido de entre 5 y 7 miembros; o R7 y R5b, junto con el nitrogeno y el carbono al cual están unidos, forman un N-heterociclilo opcionalmente sustituido de entre 5 y 7 miembros; o R7 y R5c, junto con el nitrogeno y el carbono al cual están unidos, forman un N-heterociclilo opcionalmente sustituido de entre 5 y 7 miembros o un N-heterociclilo en puente opcionalmente sustituido de entre 6 y 10 miembros; R8 es hidrogeno, alquilo, haloalquilo, haloalquenilo, haloalquinilo, hidroxialquilo, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroarilalquilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, heterociclilalquilo opcionalmente sustituido, -R13-OR10, -R13-O-R14-C(=O)OR10, -R13-C(=O)R10, -R13-C(=O)OR10, R13-C(=O)-R14-C(=O)OR10, -R13-C(=O)-R13-N(R10)R11, -R13-C(O)-R14-S(=O)tN(R10)R11 (donde t es 1 o 2), o -R14-S(=O)pR10 (donde p es 0, 1 o 2); o R8 es aralquilo opcionalmente sustituido con uno o más .sustituyentes seleccionados entre el grupo que consiste en halo, nitro, ciano, heteroarilo opcionalmente sustituido, hidroxiiminoalquilo, -R13- OR10, -R13-C(=O)R10, -R13-C(=O)OR10, -R13-C(=O)-R13-N(R10)R11, -R13-C(=O)N(R10)-R14-N(R10)R11, -R13-S(=O)tN(R10)R11 (donde t es 1 o 2), -R13-N(R10)R11, -R13-N(R10)C(=O)R10, -R13-N(R10)C(=O)-R13-N(R10)R11, -R13-N(R10)-R13-C(=O)OR10, -R13-N(R10)C(=O)- R14-s(=o)tN(R10)R11 (donde t es 1 o 2), -R13-N(R10)C(=O)-R13-N(R10)C(=O)R10, -R13-N(R10)C(=O)-R13-N(R10)-R14-N(R10)R11, -R13-N(R10)S(=O)tN(R10)R11 (donde t es 1 o 2) , y -R13-O-R14-C(=O)OR10; cada R9 es en forma independiente -O-R10, alquilo, hidroxialquilo, halo, haloalquilo, arilo o aralquilo; cada R10 y R11 es en forma independiente hidrogeno, alquilo, haloalquilo, hidroxialquilo, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroarilalquilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, o heterociclilalquilo opcionalmente sustituido; o R10 y R11, junto con el nitrogeno al cual están unidos, forman un N-heterociclilo opcionalmente sustituido o un N- heteroarilo opcionalmente sustituido; R12 es una cadena alquileno lineal o ramificada opcionalmente sustituida, una cadena alquenileno lineal o ramificada opcionalmente sustituida, o una cadena alquinileno lineal o ramificada opcionalmente sustituida; R12a es una cadena alquileno lineal o ramificada opcionalmente sustituida, una cadena alquenileno lineal o ramificada opcionalmente sustituida, o una cadena alquinileno lineal o ramificada opcionalmente sustituida; cada R13 es en forma independiente un enlace directo, una cadena alquileno lineal o ramificada opcionalmente sustituida, una cadena alquenileno lineal o ramificada opcionalmente sustituida, o una cadena alquinileno lineal o ramificada opcionalmente sustituida; y cada R14 es en forma independiente una cadena alquileno lineal o ramificada opcionalmente sustituida, una cadena alquenileno lineal o ramificada opcionalmente sustituida, o una cadena alquinileno lineal o ramificada opcionalmente sustituida; como estereoisomero aislado o como mezcla de estereoisomeros; o una sal, solvato, polimorfo, clatrato, ion de amonio, N-oxido o prodroga aceptable para uso farmacéutico del mismo.
ARP060105807A 2005-12-29 2006-12-27 Amidas inhibidoras de leucotrieno a4 hidrolasa AR058405A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US75573205P 2005-12-29 2005-12-29
US83548906P 2006-08-04 2006-08-04

Publications (1)

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AR058405A1 true AR058405A1 (es) 2008-01-30

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DK1976828T3 (en) 2005-12-29 2017-03-06 Celtaxsys Inc DIAMINE DERIVATIVES AS INhibitors of Leukotriene A4 HYDROLASE
KR20150127245A (ko) * 2013-03-14 2015-11-16 켈탁시스, 인코퍼레이티드 류코트라이엔 a4 가수분해효소의 저해제
MX2021006326A (es) * 2015-09-17 2022-12-16 Inhibidores de pcna.
MX391259B (es) 2015-10-14 2025-03-21 X Therma Inc Composiciones y métodos para reducir la formación de cristales de hielo.
AU2017371353B2 (en) 2016-12-09 2022-02-03 Celltaxis, Llc Monamine and monoamine derivatives as inhibitors of leukotriene A4 hydrolase
AU2017371362A1 (en) * 2016-12-09 2019-07-25 Celltaxis, Llc Pendant amines and derivatives as inhibitors of leukotriene A4 hydrolase
JP7386815B2 (ja) 2018-05-31 2023-11-27 セルタクシー、エルエルシー 呼吸器疾患患者の肺増悪を軽減する方法
WO2022152852A1 (en) * 2021-01-15 2022-07-21 Glaxosmithkline Intellectual Property Development Limited Antagonists of mrgx2
CN115215760B (zh) * 2021-04-19 2023-10-17 四川大学华西医院 一种含芳基的季铵盐衍生物及其在制备局部麻醉药物中的用途
KR102854346B1 (ko) * 2023-02-02 2025-09-04 한국원자력의학원 아릴-피페리딘 유도체를 포함하는 암 질환 예방 또는 치료용 조성물

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US6573264B1 (en) * 2000-10-23 2003-06-03 Cv Therapeutics, Inc. Heteroaryl alkyl piperazine derivatives
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US20040147502A1 (en) * 2002-12-17 2004-07-29 Bisacchi Gregory S. Beta lactam compounds and their use as inhibitors of tryptase
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PE20070850A1 (es) 2007-10-19
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US20070155727A1 (en) 2007-07-05
WO2007079003A3 (en) 2009-08-27

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