AR052342A1 - Derivados sustituidos de triazolona,tetrazolona e imidazolona con actividad selectiva antagonista de alfa2c-adenoreceptores - Google Patents

Derivados sustituidos de triazolona,tetrazolona e imidazolona con actividad selectiva antagonista de alfa2c-adenoreceptores

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Publication number
AR052342A1
AR052342A1 ARP050105336A ARP050105336A AR052342A1 AR 052342 A1 AR052342 A1 AR 052342A1 AR P050105336 A ARP050105336 A AR P050105336A AR P050105336 A ARP050105336 A AR P050105336A AR 052342 A1 AR052342 A1 AR 052342A1
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Argentina
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radical
alkyl
group
disorders
aryl
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ARP050105336A
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English (en)
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Janssen Pharmaceutica Nv
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Publication of AR052342A1 publication Critical patent/AR052342A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/66—Heterocyclic 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 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
    • C07D233/70—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/12—Oxygen or sulfur atoms
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • C07D403/10—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 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
    • C07D405/14—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

Abstract

La presente se refiere a la prevencion y/o tratamiento de trastornos del sistema nerviosos central, trastornos del humor, trastornos de ansiedad, trastornos relacionados con el estrés asociados con depresion y/o ansiedad, trastornos cognitivos, trastornos de la personalidad, trastornos esquizoafectivos, enfermedad de Parkinson, demencia de tipo Alzheimer, afecciones de dolor cronico, enfermedades neurodegenerativas, trastornos de adiccion, trastornos del humor y disfuncion sexual. Composiciones farmacéuticas que los contienen, métodos de preparacion y usos. Reivindicacion 1: Un compuesto de acuerdo con la formula (1) general, una sl de adicion con ácido o base aceptable para uso farmacéutico del mismo, una forma estereoquímicamente isomérica del mismo, una forma N-oxido del mismo o una sal de amonio cuaternaria del mismo, donde: Z1 y Z2 son cada uno en forma independiente uno del otro son CH o N; XA y XB son cada uno en forma independiente uno del otro son un enlace covalente o un radical alquilo C1-4, donde una unidad -CH2- bivalente puede reemplazarse por una unidad fenilo bivalente y/o donde uno o más átomos de hidrogeno en cada porcion XA y XB puede reemplazarse por un radical seleccionado del grupo de halo, ciano, hidroxi, amino, oxo y formilo; YA e YB son cada uno en forma independiente uno del otro son un radical seleccionado del grupo de t-butilo, NR1R2 y Pir; R1 y R2 son cada uno en forma independiente uno del otro son un radical seleccionado del grupo de hidrogeno; alquilo; arilo; ariloxi; Het; -NRaRb, donde Ra y Rb son cada uno en forma independiente son hidrogeno, alquilo, arilo o arilalquilo; y alquilo sustituido con uno o más radicales seleccionados del grupo de arilo, ariloxi, Het y -NRaRb, donde Ra y Rb son cada uno en forma independiente se seleccionan del grupo de hidrogeno, alquilo, arilo y arilalquilo; Pir es un radical seleccionado del grupo de pirrolilo; pirazolilo; imidazolilo; piridinilo; pirimidinilo; pirazinilo; piridazinilo; pirrolidinilo; imidazolidinilo; pirrazolidinilo, piperidinilo, diazepino, morfolinilo, tiomorfolinilo, piperazinilo, imidazolidinilo, 2H-pirrolilo, pirrolinilo, imidazolinilo, pirrazolinilo, 1,2,3,4-tetrahidro- isoquinolinilo, 7,9-diaza-biciclo[4,2,2]dec-3-enilo e isoindolilo; donde cada radical Pir puede estar sustituido en forma opcional con uno o más radicales seleccionados del grupo de hidroxi; oxo; alquilo; alquilcarbonilo; alquilsulfonilo; alquiloxicarbonilo; ariloxialquilo; mono-arilaminoalquilo; arilo; arilalquilo; arilalquenilo; pirrolidinilo; furilalquilo sustituido en forma opcional con 1 o 2 radicales alquilo; benzofurilalquilo; 2,3-dihidro-benzo[1,4]dioxilalquilo; quinolinilalquilo; benzotienilalquilo e indolilalquilo, sustituido en forma opcional con halo; Het es un radical heterocíclico monocíclico seleccionado del grupo de pirrolilo, pirazolilo; imidazolilo; piridinilo; pirimidinilo; pirazinilo; piridazinilo; pirrolidinilo; imidazolidinilo; pirrazolidinilo, piperidinilo, diazepino, morfolinilo, tiomorfolinilo, piperazinilo, imidazolidinilo, 2H-pirrolilo, pirrolinilo, imidazolinilo, pirrazolinilo, furanilo, tienilo, oxazolilo, isoxazolilo, tiazolilo, tiadiazolilo, isotiazolilo, dioxolilo, ditianilo, tetrahidrofurilo, triazolilo y triazinilo; o un radical heterocíclico bicíclico seleccionado del grupo que quinolinilo, isoquinolinilo, 1,2,3,4-tetrahidro-isoquinolinilo, quinoxalinilo, indolilo, isoindolilo, bencimidazolilo, benzoxazolilo, bencisoxazolilo, benzotiazolilo, bencisotiazolilo, benzofuranilo, benzotienilo, benzopiperidinilo, cromenilo e imidazo[1,2-a] piridinilo; donde cada radical Het está sustituido opcionalmente con alquilo; o dos restos adyacentes X e Y pueden fusionarse para formar el radical bivalente 1,2,3,4-tetrahidro-isoquinolinilo, sustituido en forma opcional con hidrogeno, alquilo, arilo, arilalquilo, alquilcarbonilo, alquilsulfonilo y pirrolidinilalquilo; arilo es naftalenilo o fenilo, cada uno sustituido en forma opcional con 1, 2 o 3 sustituyentes, cada uno independientemente uno del otro, seleccionados del grupo de halo, ciano, hidroxi, amino, alquilamino, alquiloxialquilamino, oxo, carboxi, nitro, tio, formilo y alquiloxi; alquilo es un radical hidrocarbonado saturado de cadena recta o ramificada C1-6; o es un radical hidrocarbonado (cicloalquilo) saturado cíclico C3-7; o es un radical hidrocarbonado saturado cíclico C3-7 unidos a un radical hidrocarbonado saturado de cadena recta o ramificada C1-6; cada radical puede estar sustituido en forma opcional en uno o más átomos de carbono con uno o más radicales seleccionados del grupo de halo, ciano, hidroxi, amino, oxo, carboxi, nitro, tio y formilo; y alquenilo es un radical alquilo como se definio con anterioridad que tiene además uno o más dobles enlaces.
ARP050105336A 2004-12-21 2005-12-19 Derivados sustituidos de triazolona,tetrazolona e imidazolona con actividad selectiva antagonista de alfa2c-adenoreceptores AR052342A1 (es)

Applications Claiming Priority (2)

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EP04106817 2004-12-21
EP05104873 2005-06-03

Publications (1)

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AR052342A1 true AR052342A1 (es) 2007-03-14

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Country Status (15)

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US (1) US20100029620A1 (es)
EP (1) EP1831185A1 (es)
JP (1) JP2008524312A (es)
KR (1) KR20070090941A (es)
AR (1) AR052342A1 (es)
AU (1) AU2005318188A1 (es)
BR (1) BRPI0516380A (es)
CA (1) CA2588028A1 (es)
EA (1) EA011514B1 (es)
IL (1) IL184048A0 (es)
MX (1) MX2007007472A (es)
NO (1) NO20073760L (es)
PA (1) PA8657301A1 (es)
TW (1) TW200635906A (es)
WO (1) WO2006067139A1 (es)

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WO2008083124A1 (en) 2006-12-28 2008-07-10 Rigel Pharmaceuticals, Inc. N-substituted-heterocycloalkyloxybenzamide compounds and methods of use
CA2798330A1 (en) 2010-05-05 2011-11-10 Infinity Pharmaceuticals, Inc. Tetrazolones as inhibitors of fatty acid synthase
SI2623499T1 (sl) * 2010-10-01 2015-10-30 Taisho Pharmaceutical Co., Ltd. Derivat 1,2,4-triazolona
FR2976287B1 (fr) 2011-06-09 2013-07-05 Pf Medicament Derives benzoquinolizidines, leur procede de preparation et leurs applications en therapeutique
WO2013062027A1 (ja) * 2011-10-27 2013-05-02 大正製薬株式会社 アゾール誘導体
BR112014028991A2 (pt) 2012-05-22 2017-06-27 Autifony Therapeutics Ltd triazóis como inibidores de kv3
WO2014198592A1 (en) * 2013-06-11 2014-12-18 F. Hoffmann-La Roche Ag Novel tetrazolone derivatives
JP2016523918A (ja) 2013-06-27 2016-08-12 シーダーズ−サイナイ メディカル センター 神経変性状態の予防および治療のためのアドレナリン受容体拮抗薬
BR112019000569A2 (pt) 2016-07-12 2019-04-24 Bayer Cropscience Aktiengesellschaft compostos bicíclicos como pesticidas
WO2019089066A1 (en) * 2017-11-06 2019-05-09 Acelot, Inc. SMALL MOLECULE DRUGS AND RELATED METHODS FOR TREATMENT OF DISEASES RELATED TO Aβ42 OLIGOMER FORMATION

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NO20073760L (no) 2007-07-19
MX2007007472A (es) 2007-07-20
PA8657301A1 (es) 2007-01-17
AU2005318188A1 (en) 2006-06-29
JP2008524312A (ja) 2008-07-10
US20100029620A1 (en) 2010-02-04
KR20070090941A (ko) 2007-09-06
IL184048A0 (en) 2007-10-31
BRPI0516380A (pt) 2008-09-02
TW200635906A (en) 2006-10-16
WO2006067139A1 (en) 2006-06-29
EP1831185A1 (en) 2007-09-12
EA200701345A1 (ru) 2007-10-26
EA011514B1 (ru) 2009-04-28
CA2588028A1 (en) 2006-06-29

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