BRPI0606110A2 - compostos de arilamina substituìdos e seu uso como 5 - ht6 moduladores - Google Patents

compostos de arilamina substituìdos e seu uso como 5 - ht6 moduladores

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Publication number
BRPI0606110A2
BRPI0606110A2 BRPI0606110-9A BRPI0606110A BRPI0606110A2 BR PI0606110 A2 BRPI0606110 A2 BR PI0606110A2 BR PI0606110 A BRPI0606110 A BR PI0606110A BR PI0606110 A2 BRPI0606110 A2 BR PI0606110A2
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Brazil
Prior art keywords
substituted
alkyl
heteroaryl
aryl
hydrogen
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BRPI0606110-9A
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English (en)
Inventor
Oren Becker
Srinivasa Rao Cheruku
Yael Marantz
Silvia Noiman
Merav Fichman
Hanoch Senderowitz
Sharon Shacham
Ashis Saha
Pini Orbach
Mercedes Lobera
Rosa E Melendez
Anurag Sharadendu
Laurence Wu
Xiang Y Yu
Dale S Dhanoa
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Epix Delaware Inc
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Application filed by Epix Delaware Inc filed Critical Epix Delaware Inc
Publication of BRPI0606110A2 publication Critical patent/BRPI0606110A2/pt

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    • 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
    • C07D295/12—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 substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—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 substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • 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
    • C07D295/06—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 substituted by halogen atoms or nitro radicals
    • C07D295/073—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 substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • 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
    • C07D207/10—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 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
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • 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
    • C07D211/36—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 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
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    • 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
    • C07D295/14—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 substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—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 substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
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  • Chemical & Material Sciences (AREA)
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  • Neurology (AREA)
  • Biomedical Technology (AREA)
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  • Cardiology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)

Abstract

COMPOSTOS DE ARILAMINA SUBSTITUìDOS E SEU USO COMO 5-HT6 MODULADORES. A invenção refere-se a antagonistas de 5-HT6 receptores. São descritos novos compostos de arilamina tendo a fórmula: e sais e/ou ésteres dos mesmos farmaçeuticamente aceitáveis, em que - n é 0,1, 2, 3, ou 4; - A, quando presente é um grupo alquila inferior; - R~ 1~ é hidrogênio ou alquila ou arila substituído ou não-substituído; - R~ 2~ é hidrogênio; halo; nitro; ciano; alçóxi inferior; ácido de sal de carboxilato ou éster de aíquila do mesmo; uma sulfona; haloalquila ou haloalcóxi; acetaldeido; carboxamida; carbomila; alcoxiaminocarbonila; ou arilalquilamino substituído; - R~ 3 e R~ 4~ são de modo independente hidrogênio, substituído ou não-substituído alquila, arila, alquilarila, heteroarila ou alquilheteroarila, ou, tomados juntos, R~ 3~ e R~ 4~ formam um grupo substituido ou não-substituído arila; alquilarila, heteroarila ou alquilheteroarila; - B, quando presente, é alquila inferior; e - X e Y são de modo independente O ou N; e o uso destes compostos e suas composições farmacêuticas, por exemplo, no tratamento, modulação e/ou prevenção de condições fisiológicas associadas com a ação da serotonina, tais como no tratamento da obesidade, e de distúrbios relacionados com obesidade, por exemplo, doença cardiovascular, doença digestiva, doença respiratória, câncer e diabetes tipo II; e distúrbios psicológicos tais como esquizofrenia.
BRPI0606110-9A 2005-01-25 2006-01-25 compostos de arilamina substituìdos e seu uso como 5 - ht6 moduladores BRPI0606110A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US64695705P 2005-01-25 2005-01-25
US70185305P 2005-07-22 2005-07-22
PCT/US2006/002718 WO2006081332A1 (en) 2005-01-25 2006-01-25 Substituted arylamine compounds and their use as 5-ht6 modulators

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BRPI0606110A2 true BRPI0606110A2 (pt) 2009-06-02

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BRPI0606110-9A BRPI0606110A2 (pt) 2005-01-25 2006-01-25 compostos de arilamina substituìdos e seu uso como 5 - ht6 moduladores

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US (2) US7968538B2 (pt)
EP (1) EP1856075A1 (pt)
JP (2) JP5186219B2 (pt)
KR (1) KR20070097590A (pt)
AU (1) AU2006209216A1 (pt)
BR (1) BRPI0606110A2 (pt)
CA (1) CA2595607C (pt)
IL (1) IL184705A0 (pt)
MA (1) MA29429B1 (pt)
MX (1) MX2007008279A (pt)
NO (1) NO20074324L (pt)
NZ (1) NZ556761A (pt)
RU (1) RU2440996C2 (pt)
WO (1) WO2006081332A1 (pt)

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EP1856075A1 (en) 2007-11-21
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RU2440996C2 (ru) 2012-01-27
RU2007132161A (ru) 2009-03-10
NO20074324L (no) 2007-10-25
US20120115850A1 (en) 2012-05-10
AU2006209216A1 (en) 2006-08-03
US20060205737A1 (en) 2006-09-14
CA2595607C (en) 2014-07-15
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