AR065891A1 - Derivados de piridina y pirimidina como antagonistas del mglur2 - Google Patents

Derivados de piridina y pirimidina como antagonistas del mglur2

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Publication number
AR065891A1
AR065891A1 ARP080101333A ARP080101333A AR065891A1 AR 065891 A1 AR065891 A1 AR 065891A1 AR P080101333 A ARP080101333 A AR P080101333A AR P080101333 A ARP080101333 A AR P080101333A AR 065891 A1 AR065891 A1 AR 065891A1
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AR
Argentina
Prior art keywords
alkyl
optionally substituted
group
hydroxy
alkoxy
Prior art date
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ARP080101333A
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English (en)
Inventor
Thomas Woltering
Juergen Wichmann
Silvia Gatti Mcarthur
Original Assignee
Hoffmann La Roche
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR065891A1 publication Critical patent/AR065891A1/es

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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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • 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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    • A61P13/00Drugs for disorders of the urinary system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/16Anti-Parkinson drugs
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
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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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Otolaryngology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

La presente está relacionada con los compuestos de formula (1), un proceso para la elaboracion de los mismos, su utilizacion para la preparacion de medicamentos para el tratamiento de trastornos del SNC y composiciones farmacéuticas que loscontienen. Reivindicacion 1: Un compuesto de formula (1) en el que uno de entre X o Y es N y el otro es CH, o ambos X e Y son N; Q es S, O, -CH=N- o -N=CH-; A es arilo o un heteroarilo de 5 o 6 miembros cada uno de los cuales está opcionalmentesustituido por alquilo C1-6; B es un arilo opcionalmente sustituido o un heteroarilo de 5 o 6 miembros opcionalmente sustituido, en el que los sustituyentes están seleccionados de entre el grupo que consiste en: halo, nitro, alquilo C1-6opcionalmente sustituido por hidroxi, NRaRb, en el que Ra y Rb son independientemente H, alquilo C1-6 o -(CO)-alquilo C1-6, -S-alquilo C1-6, -(SO2)-OH, -(SO2)-alquilo C1-6, -(SO2)-NRcRd, en el que Rc y Rd son independientemente: H, alquilo C1-6opcionalmente sustituido por hidroxi, haloalquilo C1-6, alcoxi C1-6, -(CO)alquilo C1-6 opcionalmente sustituido por alcoxi C1-6, -(CH2CH2O)nCHRe, en el que Re es H o CH2OH y n es 1, 2, 3, 4, 5, 6, 7, 8, 9 o 10, -(CH2)m-arilo, en el que m es 1 o 2 yel arilo está opcionalmente sustituido por halo o alcoxi C1-6, -(CH2)p-cicloalquilo C3-6, en el que p es 0 o 1, heterocicloalquilo de 5 o 6 miembros, -(SO2)-NRfRg, en el que Rf y Rg junto al átomo de nitrogeno al que están unidos, forman un anilloheterocicloalquilo de 4, 5 o 6 miembros que contiene opcionalmente otro heteroátomo seleccionado de entre nitrogeno, oxígeno, azufre o un grupo XO2, en el que dicho anillo heterocicloalquilo de 4, 5 o 6 miembros está opcionalmente sustituido por unsustituyente seleccionado de entre el grupo que consiste en: hidroxi, alquilo C1-6, alcoxi C1-6 que está opcionalmente sustituido por hidroxi y heteroariloxi de 5 o 6 miembros, NHSO2-alquilo C1-6, NHSO2-NRhRi en el que Rh y Ri son independientementeH, alquilo C1-6, -(CO)O-alquilo C1-6, o Rh y Ri junto al átomo de nitrogeno al que están unidos, forman un anillo heterocicloalquilo de 4, 5 o 6 miembros que contiene opcionalmente otro heteroátomo seleccionado de entre nitrogeno, oxígeno o azufre,en el que dicho anillo heterocicloalquilo de 4, 5 o 6 miembros está opcionalmente sustituido por alquilo C1-6, R1 es H, halogeno, alquilo C1-6 opcionalmente sustituido por hidroxi, alcoxi C1-6, haloalquilo C1-6, cicloalquilo C3-6; R2 se seleccionade entre el grupo que consiste en: ciano, halogeno, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alquilo C1-6 y cicloalquilo C3-6; o es NRjRk en el que Rj y Rk se seleccionan independientemente de entre el grupo que consiste en: H, cicloalquiloC3-8, arilo, heteroarilo que posee de 5 a 12 átomos en el anillo y alquilo C1-6 que está opcionalmente sustituido por uno o más sustituyente(s) seleccionados de entre el grupo que consiste en halogeno, hidroxi, cicloalquilo C3-8, arilo, heteroariloque posee de 5 a 12 átomos en el anillo y -NRlRm, en el que Rl y Rm son independientemente seleccionados de entre el grupo que consiste en H y alquilo C1-6; o Rl y Rm pueden formar, junto al átomo de nitrogeno al que están unidos, un grupoheterocíclico opcionalmente sustituido que comprende de 5 a 12 átomos en el anillo que contiene opcionalmente otro heteroátomo seleccionado de entre nitrogeno, oxígeno o azufre, en el que dicho grupo heterocíclico está opcionalmente sustituido poruno, dos, tres, cuatro o cinco sustituyentes seleccionados de entre el grupo que consiste en halogeno, hidroxi, alquilo C1-6 y haloalquilo C1-6; así como las sales farmacéuticamente aceptables de los mismos.
ARP080101333A 2007-04-02 2008-03-31 Derivados de piridina y pirimidina como antagonistas del mglur2 AR065891A1 (es)

Applications Claiming Priority (1)

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EP07105429 2007-04-02

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AR065891A1 true AR065891A1 (es) 2009-07-08

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US (2) US8012986B2 (es)
EP (1) EP2142527B1 (es)
JP (1) JP5303544B2 (es)
KR (1) KR101143152B1 (es)
CN (1) CN101641346B (es)
AR (1) AR065891A1 (es)
AT (1) ATE493400T1 (es)
AU (1) AU2008233956B2 (es)
BR (1) BRPI0809971A2 (es)
CA (1) CA2681733A1 (es)
CL (1) CL2008000936A1 (es)
DE (1) DE602008004236D1 (es)
IL (1) IL200780A (es)
MX (1) MX2009010505A (es)
PE (1) PE20090103A1 (es)
TW (1) TW200845999A (es)
WO (1) WO2008119689A1 (es)

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EA201001129A1 (ru) * 2008-01-11 2011-02-28 Новартис Аг Пиримидины в качестве ингибиторов киназы
US20130137865A1 (en) 2010-08-11 2013-05-30 Taisho Pharmaceutical Co., Ltd. Heteroaryl-pyrazole derivative
JP2014062047A (ja) * 2011-01-21 2014-04-10 Taisho Pharmaceutical Co Ltd ピラゾール誘導体
WO2013041652A1 (en) * 2011-09-21 2013-03-28 Cellzome Limited Morpholino substituted urea or carbamate derivatives as mtor inhibitors
CA3132120C (en) * 2012-02-08 2023-10-24 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
SG11201503192XA (en) 2012-10-23 2015-06-29 Hoffmann La Roche Mglu2/3 antagonists for the treatment of autistic disorders
KR20160143853A (ko) 2014-04-23 2016-12-14 에프. 호프만-라 로슈 아게 지적 장애의 치료를 위한 mglu2/3 길항제
JP6552061B2 (ja) * 2014-06-10 2019-07-31 サンフォード−バーンハム メディカル リサーチ インスティテュート 代謝型グルタミン酸受容体の負のアロステリックモジュレーター(nams)とその使用
IL264446B1 (en) 2016-07-29 2024-05-01 Pgi Drug Discovery Llc Compounds and compositions and their use
JP2019523279A (ja) 2016-07-29 2019-08-22 サノビオン ファーマシューティカルズ インクSunovion Pharmaceuticals Inc. 化合物および組成物ならびにそれらの使用
CN111183138A (zh) 2017-08-02 2020-05-19 赛诺维信制药公司 异色满化合物以及用途
CN112334457A (zh) * 2018-06-22 2021-02-05 拜耳公司 制备三环化合物的方法
AU2020236225A1 (en) 2019-03-14 2021-09-16 Sunovion Pharmaceuticals Inc. Salts of a isochromanyl compound and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof

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MXPA03007513A (es) 2001-02-21 2004-07-30 Nps Pharma Inc Compuestos heteropoliciclicos y su uso como antagonistas del receptor metabotropico de glutamato.
EP1613614A2 (en) 2003-04-03 2006-01-11 Merck & Co., Inc. Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5
US7393959B2 (en) * 2003-04-04 2008-07-01 Merck & Co. Inc. Di-aryl substituted pyrrole modulators of metabotropic glutamate receptor-5
US7442797B2 (en) * 2003-11-04 2008-10-28 Takasago International Corporation Platinum complex and light emitting device
US20060173048A1 (en) 2005-02-03 2006-08-03 Mcarthur Silvia G Imidazole derivatives
EP2001849B1 (en) 2006-03-29 2014-11-26 F. Hoffmann-La Roche AG Pyridine and pyrimidine derivatives as mglur2 antagonists
US20070236568A1 (en) 2006-04-11 2007-10-11 Metke Anthony R Method and system for communicating incident scene information

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US8012986B2 (en) 2011-09-06
AU2008233956B2 (en) 2013-05-02
JP5303544B2 (ja) 2013-10-02
CN101641346A (zh) 2010-02-03
MX2009010505A (es) 2009-10-19
JP2010524852A (ja) 2010-07-22
WO2008119689A1 (en) 2008-10-09
US20080280924A1 (en) 2008-11-13
CN101641346B (zh) 2013-11-06
EP2142527A1 (en) 2010-01-13
ATE493400T1 (de) 2011-01-15
DE602008004236D1 (de) 2011-02-10
EP2142527B1 (en) 2010-12-29
KR101143152B1 (ko) 2012-05-08
CA2681733A1 (en) 2008-10-09
AU2008233956A1 (en) 2008-10-09
KR20090117902A (ko) 2009-11-13
TW200845999A (en) 2008-12-01
BRPI0809971A2 (pt) 2014-10-07
IL200780A0 (en) 2010-05-17
US8415380B2 (en) 2013-04-09
PE20090103A1 (es) 2009-02-13
IL200780A (en) 2013-01-31
US20110263615A1 (en) 2011-10-27
CL2008000936A1 (es) 2008-10-03

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