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AR050194A1 - Analogos de biaril piperazinil-piridina sustituidos - Google Patents

Analogos de biaril piperazinil-piridina sustituidos

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Publication number
AR050194A1
AR050194A1 ARP050103213A ARP050103213A AR050194A1 AR 050194 A1 AR050194 A1 AR 050194A1 AR P050103213 A ARP050103213 A AR P050103213A AR P050103213 A ARP050103213 A AR P050103213A AR 050194 A1 AR050194 A1 AR 050194A1
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Argentina
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alkyl
mono
independently selected
halogen
amino
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ARP050103213A
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Neurogen Corp
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    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/08Bronchodilators
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
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    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
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    • 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
    • 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
    • C07D401/14Heterocyclic 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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    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Urology & Nephrology (AREA)
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  • Rheumatology (AREA)
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  • Obesity (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Tales compuestos son ligantes que pueden utilizarse para modular la actividad de un receptor específico in vivo o in vitro, y que son particularmente utiles en el tratamiento de cuadros asociados con la activacion patologica de los receptores en seres humanos, animales domésticos y ganado. También se proporcionan las composiciones farmacéuticas y los métodos para usar dichos compuestos en el tratamiento de esos desordenes, así como métodos para usar dichos ligantes para estudios de localizacion de receptores. Reivindicacion 1: Un compuesto de la formula (1), o una sal farmacéuticamente aceptables del mismo, en donde: Ar2 es fenilo o un heterociclo aromático de 6 miembros, cada uno de los cuales está sustituido con desde 0 a 4 sustituyentes independientemente elegidos de R2; X, Y y Z son independientemente CRx o N, de tal modo que por lo menos uno de X, Y y Z es N; D, K, J y F son independientemente N, CH o carbono sustituido con un sustituyente representado por R1 o R10; Rx es elegido independientemente en cada caso entre hidrogeno, halogeno, alquilo C1-4, amino, ciano y mono- o di-(alquilC1-4)amino; R1 representa desde 0 a 3 sustituyentes elegidos independientemente entre: a) halogeno, ciano y nitro; b) grupos de la formula -Q-M-Ry; y c) grupos que se toman en forma conjunta con R10 para formar un anillo heterocíclico o carbocíclico de 5 a 7 miembros fusionados que está sustituido con desde 0 a 4 sustituyentes elegidos independientemente entre halogeno, ciano, nitro y grupos de la formula -Q-M-Ry; R10 representa un sustituyente elegido entre: a) grupos de la formula -Q-M-Ry; y b) grupos que se toman en forma conjunta con un R1 para formar un anillo heterocíclico o carbocíclico de 5 a 7 miembros opcionalmente sustituidos, fusionados; de tal modo que R10 no es hidroxi, amino ni un grupo no sustituido elegido entre: alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alquilC2-6éter, alcanoilo C2-6, alcanona C3-6, haloalquilo C1-6, haloalcoxi C1-6, mono- o di-(alquil C1-6)amino, alquilC1-6-sulfonilo, mono- o di-(alquil C1-6)aminosulfonilo o mono- o di-(alquil C1-6)aminocarbonilo; cada Q es independientemente elegido entre alquileno C0-4; cada M está independientemente ausente o seleccionado entre 0, C(=O), OC(=O), C(=O)O, O-C(=O)O, S(O)m, N(Rz), C(=O)N(Rz), C(=NH)N(Rz), N(Rz)C(=O), N(Rz)C(=NH), N(Rz)S(O)m, S(O)mN(Rz) y N[S(O)mN(Rz)]S(O)m; en donde m es independientemente seleccionado en cada caso entre 0, 1 y 2; y Rz es independientemente seleccionado en cada caso entre hidrogeno, alquilo C1-8 y grupos que se toman junto con Ry para formar un heterociclo de 4 a 7 miembros opcionalmente sustituido; y cada Ry es independientemente hidrogeno, haloalquilo C1-8, alquilo C1-8, carbocicloC3-8alquiloC0-4, heterociclo de 4 a 7 miembros)alquiloC0-4, o se toma en forma conjunta con Rz para formar un heterociclo de 4 a 7 miembros en donde cada alquilo, carbociclo y heterociclo está sustituido con desde 0 a 4 sustituyentes independientemente seleccionados entre hidroxi, halogeno, amino, ciano, nitro, oxo, -COOH, aminocarbonilo, aminosulfonilo, alquilo C1-6, cicloalquilo C3-7, alquiloC2-6éter, alcanoilo C1-6, alquilC1-6-sulfonilo, alcoxi C1-8, alquiltio C1-8, mono- y di-(alquil C1-6)aminocarbonilo, mono- y di-(alquil C1-6)aminosulfonilo, mono- y di(alquil C1-6)amino y fenilo; de tal modo que Ry no es hidrogeno si Q es alquilo C0 y si M está ausente; cada R2 es: a) independientemente elegido entre i) hidroxi, amino, ciano, halogeno, -COOH, aminosulfonilo, nitro y aminocarbonilo; y ii) alquilo C1-6, cicloalquilC3-8alquiloC0-4, haloalquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilC2-6éter, alcanoilo C2-6, alcoxiC1-6-carbonilo, alcanoiloxi C2-6, alcanona C3- 6, mono- y di-(alquil C1-6)aminoalquilC0-6, (heterociclo de 4 a 7 miembros)alquiloC0-4, alquilC1-6-sulfonilo, mono- y di-(alquil C1-6)aminosulfonilo, y mono- y di-(alquil C1-6)aminocarbonilo, cada uno de los cuales está sustituido con desde 0 a 4 sustituyentes independientemente elegidos entre halogeno, hidroxi, ciano, amino, aminocarbonilo, aminosulfonilo, -COOH y oxo; o b) tomado junto con un R2 adyacente para formar un grupo heterocíclico o carbocíclico de 5 a 13 miembros fusionados que está sustituido con desde 0 a 3 sustituyentes independientemente elegidos entre halogeno, oxo y alquilo C1-6; R3 está seleccionado entre: i) hidrogeno y halogeno; ii) alquilo C1-6, cicloalquilC3-8alquiloC0-2, haloalquilo C1-6 y fenialquilo C0-2; y iii) grupos de la formula (2), en donde: L es alquileno C0-6 o alquileno C1-6 que está tomado junto con R5, R6 o R7 para formar un heterociclo de 4 a 7 miembros; W es O, CO, S, SO o SO2; R5 y R6 están: a) independientemente elegidos entre hidrogeno, alquilo C1-12, alquenilo C2-12, cicloalquilC3-8alquiloC0-4, alcanoilo C2-6, alquilC1-6-sulfonilo, fenilalquilo C0-6, (heterociclo de 4 a 7 miembros)alquiloC0-6 y grupos que están unidos a L para formar un heterociclo de 4 a 7 miembros; o b) unidos para formar un heterociclo de 4 a 12 miembros; y R7 es hidrogeno, alquilo C1-12, alquenilo C2-12, cicloalquilC3-8alquiloC1-4, alcanoilo C2-6, fenilalquilo C0-6, (heterociclo de 4 a 7 miembros)alquilo C0-6 o un grupo que está unido a L para formar un heterociclo de 4 a7 miembros; en donde cada uno de ii) y iii) está opcionalmente sustituido con desde 0 a 4 sustituyentes independientemente elegidos entre: a) halogeno, hidroxi, amino, ciano, nitro, -COOH, aminosulfonilo, aminocarbonilo y oxo; y b) alquilo C1-6, cicloalquilC3-8alquiloC0-2, haloalquilo C1-6, alcoxi C1-6, alcanoilo C1-6, alcoxiC1-6-carbonilo, alcanoilC2-6-amino, mono- y di-(alquilC1-6)aminoalquiloC0-4, alquilC1-6sulfonilo, mono- y di-(alquil C1-6)aminosulfonilo, mono- y di- (alquilC1-6)aminocarbonilalquiloC0-4, fenilalquilo C0-4 y (heterociclo de 4 a 7 miembros)alquiloC0-4, cada uno de los cuales está sustituido con desde 0 a 4 sustituyentes secundarios independientemente elegidos entre halogeno, hidroxi, ciano, oxo, imino, alquilo C1-4, alcoxi C1-4 y haloalquilo C1-4; y R4 representa desde 0 a 2 sustituyentes elegidos independientemente entre alquilo C1-3, haloalquilo C1-3 y oxo.
ARP050103213A 2004-08-13 2005-08-02 Analogos de biaril piperazinil-piridina sustituidos AR050194A1 (es)

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US60172104P 2004-08-13 2004-08-13
US64179605P 2005-01-05 2005-01-05

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US (2) US7662830B2 (es)
EP (1) EP1786800B1 (es)
JP (1) JP4955554B2 (es)
KR (1) KR20070046924A (es)
CN (1) CN101014587B (es)
AR (1) AR050194A1 (es)
BR (1) BRPI0514319A (es)
CA (1) CA2577301C (es)
CR (1) CR8992A (es)
EC (1) ECSP077318A (es)
HN (1) HN2007006799A (es)
IL (1) IL181040A0 (es)
MA (1) MA28857B1 (es)
MX (1) MX2007001696A (es)
MY (1) MY145822A (es)
NI (1) NI200700040A (es)
NO (1) NO20071243L (es)
NZ (1) NZ553388A (es)
PE (1) PE20060620A1 (es)
RU (1) RU2413726C2 (es)
SG (1) SG157399A1 (es)
TW (1) TW200605889A (es)
WO (1) WO2006026135A2 (es)
ZA (1) ZA200701530B (es)

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US8334382B2 (en) 2012-12-18
EP1786800A4 (en) 2009-05-06
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CR8992A (es) 2007-08-14
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US20060122394A1 (en) 2006-06-08
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CA2577301C (en) 2014-05-27
US20110003813A1 (en) 2011-01-06
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