AR079205A1 - Morfolinotiazoles como moduladores alostericos positivos alfa 7 - Google Patents

Morfolinotiazoles como moduladores alostericos positivos alfa 7

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Publication number
AR079205A1
AR079205A1 ARP100104379A ARP100104379A AR079205A1 AR 079205 A1 AR079205 A1 AR 079205A1 AR P100104379 A ARP100104379 A AR P100104379A AR P100104379 A ARP100104379 A AR P100104379A AR 079205 A1 AR079205 A1 AR 079205A1
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AR
Argentina
Prior art keywords
alkyl
substituted
cycloalkyl
alkyloxy
trifluoromethyl
Prior art date
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ARP100104379A
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English (en)
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Janssen Pharmaceutica Nv
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Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR079205A1 publication Critical patent/AR079205A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
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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
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/04Antibacterial agents
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    • CCHEMISTRY; METALLURGY
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Psychology (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente se refiere a derivados morfolinotiazol y sus sales farmacéuticamente aceptables, procesos para prepararlos, composiciones farmacéuticas que los contienen y sus usos en terapia. La solicitud en particular se refiere a moduladores alostéricos positivos de receptores acetilcolina nicotínicos, dichos moduladores alostéricos positivos que tengan la capacidad de aumentar la eficacia de agonistas del receptor nicotínico. Reivindicacion 1: Un compuesto que tiene la formula (1) o un isomero estereoquímico del mismo, donde R1 es alquilo C1-6, alquilo C1-6 sustituido con 1, 2 o 3 sustituyentes halogeno, alquilo C1-6 sustituido con 1 grupo ciano, alquilo C1-6 sustituido con 1 grupo heteroarilo, cicloalquilo C3-6, cicloalquilo C3-6 sustituido con 1, 2, 3 o 4 grupos metilo, cicloalquilo C3-6 sustituido con 1 grupo hidroxi, cicloalquilo C3-6-alquilo C1-6, alquiloxi C1-6-alquilo C1-6, halo alquiloxi C1-4-alquilo C1-6, tetrahidrofurilo, arilo, heteroarilo, pirrolidinilo, pirrolidinilo sustituido con 1 grupo alquilo C1-4, o tetrahidrofurilo sustituido con 1, 2 o 3 sustituyentes seleccionados de metilo y oxo; arilo es 2,2-difluoro-1,3-benzodioxolil; fenilo; o fenilo sustituido con 1, 2 o 3 sustituyentes seleccionados de halogeno, trifluorometilo, trifluorometoxi, ciano, alquilo C1-6, alquiloxi C1-4, y aminosulfonilo; heteroarilo es un radical heterocíclico aromático mono o bicíclico que contiene por lo menos un heteroátomo seleccionado de N, O y S, opcionalmente sustituido con 1, 2 o de ser posible con 3 sustituyentes seleccionados de alquilo C1-4, alquiloxi C1-4, cicloalquilo C3-6, y trifluorometilo; R2 y R3 son de manera independiente H, alquilo C1-4 o trifluorometilo; o R2 y R3 se toman juntos para formar 1,2-etanodiilo o 1,3-propanodiil; Ar es un resto de formula (2) o (3); R4 y R5 son de manera independiente H, alquilo C1-4, trifluorometilo, cicloalquilo C3-6 o alquiloxi C1-4; o una sal de adicion ácida del mismo, o un solvato del mismo.
ARP100104379A 2009-11-27 2010-11-26 Morfolinotiazoles como moduladores alostericos positivos alfa 7 AR079205A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09177347 2009-11-27

Publications (1)

Publication Number Publication Date
AR079205A1 true AR079205A1 (es) 2012-01-04

Family

ID=42010343

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104379A AR079205A1 (es) 2009-11-27 2010-11-26 Morfolinotiazoles como moduladores alostericos positivos alfa 7

Country Status (25)

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US (1) US8637510B2 (es)
EP (1) EP2504333B1 (es)
JP (1) JP5636434B2 (es)
KR (1) KR101749953B1 (es)
CN (1) CN102639530B (es)
AR (1) AR079205A1 (es)
AU (1) AU2010323175B2 (es)
BR (1) BR112012012657A2 (es)
CA (1) CA2780218C (es)
CL (1) CL2012001366A1 (es)
CO (1) CO6531464A2 (es)
DK (1) DK2504333T3 (es)
EA (1) EA020275B1 (es)
ES (1) ES2549917T3 (es)
IL (1) IL219926A0 (es)
JO (1) JO3078B1 (es)
MX (1) MX349585B (es)
MY (1) MY160728A (es)
NZ (1) NZ600138A (es)
PL (1) PL2504333T3 (es)
SG (1) SG181054A1 (es)
TW (1) TWI473803B (es)
UA (1) UA106636C2 (es)
WO (1) WO2011064288A1 (es)
ZA (1) ZA201203856B (es)

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DE10164139A1 (de) 2001-12-27 2003-07-10 Bayer Ag 2-Heteroarylcarbonsäureamide
ES2424023T3 (es) * 2007-10-18 2013-09-26 Janssen Pharmaceutica N.V. 1,2,4-triazoles trisustituidos
JO2784B1 (en) * 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 5,3,1 - Triazole substitute derivative
CA2714662C (en) * 2008-03-19 2016-05-10 Janssen Pharmaceutica Nv Trisubstituted 1,2,4-triazoles as nicotinic acetylcholine receptor modulators
CL2009001125A1 (es) * 2008-05-09 2011-02-11 Janssen Pharmaceutica Nv Compuestos derivados de pirazol trisustituido, moduladores alostericos positivos de los receptores ach nicotinicos; composicion farmaceutica que los comprende; proceso de preparacion de la composicion; y su uso en el tratamiento de enfermedades de snc o inflamatorias.
KR20180101641A (ko) 2010-05-17 2018-09-12 포럼 파마슈티칼즈 인크. (R)-7-클로로-N-(퀴누클리딘-3-일)벤조[b]티오펜-2-카르복사미드 히드로클로리드 모노히드레이트의 결정질 형태
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
MX344701B (es) 2011-02-03 2017-01-03 Lupin Ltd Derivados de pirrol como moduladores de nachr alfa 7.
AP3649A (en) 2011-02-23 2016-03-18 Lupin Ltd Heteroaryl derivatives as alpha7 nachr modulators
CA2829860A1 (en) 2011-03-31 2012-10-04 Lupin Limited Pyrrole derivatives as nicotinic acetylcholine receptor modulators for use in the treatment of neurodegenerative disorders such as alzheimer's and parkinson's disease
EP2729455B1 (en) 2011-07-05 2016-09-14 Lupin Limited Biaryl derivatives as nachr modulators
IN2014MN01756A (es) 2012-03-06 2015-07-03 Lupin Ltd
EP3461481A1 (en) 2012-05-08 2019-04-03 Forum Pharmaceuticals Inc. Methods of maintaining, treating or improving cognitive function
WO2014072957A1 (en) 2012-11-12 2014-05-15 Lupin Limited Thiazole derivatives as alpha 7 nachr modulators
WO2014111839A1 (en) 2013-01-16 2014-07-24 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
JP2016512225A (ja) 2013-03-13 2016-04-25 ルピン・リミテッドLupin Limited アルファー7nachrモジュレータとしてのピロール誘導体
TW201446243A (zh) 2013-06-03 2014-12-16 Lupin Ltd 4-(5-(4-氯苯基)-2-(2-環丙基乙醯基)-1,4-二甲基-1氫-吡咯-3-基)苯磺醯胺作為α7尼古丁乙醯膽鹼受體調節劑
EP3010899A1 (en) 2013-06-17 2016-04-27 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
HRP20221497T1 (hr) 2016-08-19 2023-02-17 The University Of Bristol Derivati citizina za liječenje ovisnosti
EP3856180A1 (en) * 2018-09-24 2021-08-04 Astrazeneca AB Azd0328 dosage regime for treating cognitive impairment
US20220347166A1 (en) * 2019-10-21 2022-11-03 Cambridge Cognition Limited Schizophrenic Disorder Treatment using Combination Therapy
CN115317480B (zh) * 2022-09-01 2023-05-16 新乡医学院 N-(3-甲基-5-异噻唑基)-2-氧代-3-(2h)-苯并噁唑乙酰胺的药物应用

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US6479510B2 (en) * 2000-08-18 2002-11-12 Pharmacia & Upjohn Company Quinuclidine-substituted aryl compounds for treatment of disease
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BRPI0609464A2 (pt) 2005-05-23 2010-04-13 Japan Tobacco Inc composto de pirazol e agente terapêutico para diabetes compreendendo o mesmo
EA015034B1 (ru) * 2005-09-13 2011-04-29 Янссен Фармацевтика Н.В. 2-анилин-4-арилзамещенные тиазольные производные
CN101374810A (zh) * 2006-01-18 2009-02-25 锡耶纳生物技术股份公司 α7烟碱型乙酰胆碱受体的调节剂及其治疗用途
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MX2016002975A (es) 2013-09-09 2016-10-21 Melinta Therapeutics Inc Compuestos antimicrobianos y métodos de fabricación y utilización de los mismos.

Also Published As

Publication number Publication date
NZ600138A (en) 2013-05-31
CN102639530A (zh) 2012-08-15
TW201127836A (en) 2011-08-16
CL2012001366A1 (es) 2012-10-05
US20120238561A1 (en) 2012-09-20
JP2013512218A (ja) 2013-04-11
CN102639530B (zh) 2014-08-06
PL2504333T3 (pl) 2015-12-31
JP5636434B2 (ja) 2014-12-03
EA201290394A1 (ru) 2012-10-30
TWI473803B (zh) 2015-02-21
MY160728A (en) 2017-03-15
US8637510B2 (en) 2014-01-28
HK1171449A1 (en) 2013-03-28
SG181054A1 (en) 2012-07-30
AU2010323175B2 (en) 2014-06-26
KR20120102083A (ko) 2012-09-17
ES2549917T3 (es) 2015-11-03
ZA201203856B (en) 2015-01-28
CO6531464A2 (es) 2012-09-28
JO3078B1 (ar) 2017-03-15
CA2780218C (en) 2018-10-16
CA2780218A1 (en) 2011-06-03
EA020275B1 (ru) 2014-09-30
BR112012012657A2 (pt) 2016-07-12
EP2504333B1 (en) 2015-07-15
IL219926A0 (en) 2012-07-31
WO2011064288A1 (en) 2011-06-03
AU2010323175A1 (en) 2012-05-10
KR101749953B1 (ko) 2017-06-22
MX2012006082A (es) 2012-06-19
EP2504333A1 (en) 2012-10-03
UA106636C2 (uk) 2014-09-25
MX349585B (es) 2017-08-03
DK2504333T3 (en) 2015-10-19

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