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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
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
cycloalkyl
alkyloxy
trifluoromethyl
Prior art date
Application number
ARP100104379A
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English (en)
Original Assignee
Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
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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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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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    • 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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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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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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    • 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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    • A61P31/04Antibacterial 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
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  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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)

Country Link
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
JP2011500625A (ja) * 2007-10-18 2011-01-06 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ トリ置換された1,2,4−トリアゾール
JO2784B1 (en) * 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 5,3,1 - Triazole substitute derivative
MY152486A (en) * 2008-03-19 2014-10-15 Janssen Pharmaceutica Nv Trisubstituted 1,2,4 - triazoles as nicotinic acetylcholine receptor modulators
BRPI0912196A2 (pt) * 2008-05-09 2015-10-06 Janssen Pharmaceutica Nv pirazóis trissubstituídos como moduladores do receptor de acetilcolina.
CA2799744C (en) 2010-05-17 2020-01-28 Envivo Pharmaceuticals, Inc. A crystalline form of (r)-7-chloro-n-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
AU2012213086B2 (en) 2011-02-03 2016-05-05 Lupin Limited Pyrrole derivatives used as modulators of alpha7 nAChR
KR20140026378A (ko) 2011-02-23 2014-03-05 루핀 리미티드 알파 7 nachr 조절자로서 헤테로아릴 유도체
AU2012235779B2 (en) 2011-03-31 2017-03-02 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
US8946432B2 (en) 2011-07-05 2015-02-03 Lupin Limited Biaryl derivatives as nAChR modulators
EP2822946A1 (en) * 2012-03-06 2015-01-14 Lupin Limited Thiazole derivatives as alpha 7 nachr modulators
US9585877B2 (en) 2012-05-08 2017-03-07 Forum Pharmaceuticals, Inc. Methods of maintaining, treating or improving cognitive function
US20150299178A1 (en) 2012-11-12 2015-10-22 Lupin Limited Thiazole Derivatives as Alpha 7 NACHR Modulators
EP2945941B1 (en) 2013-01-16 2016-12-07 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
US9617210B2 (en) 2013-03-13 2017-04-11 Lupin Limited Pyrrole derivatives as alpha 7 NACHR modulators
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
WO2014203150A1 (en) 2013-06-17 2014-12-24 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
JP7178538B2 (ja) 2016-08-19 2022-11-28 ザ ユニバーシティ オブ ブリストル 化合物
US20220040158A1 (en) * 2018-09-24 2022-02-10 Astrazeneca Ab Azd0328 dosage regime for treating cognitive impairment
JP7650270B2 (ja) * 2019-10-21 2025-03-24 ケンブリッジ コグニション リミテッド 併用療法を用いた統合失調症性障害の治療
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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WO2002016358A2 (en) * 2000-08-18 2002-02-28 Pharmacia & Upjohn Company Quinuclidine-substituted aryl moieties for treatment of disease (nicotinic acetylcholine receptor ligands)
JP4881725B2 (ja) 2003-04-09 2012-02-22 エクセリクシス, インク. Tie−2モジュレータと使用方法
BRPI0609464A2 (pt) 2005-05-23 2010-04-13 Japan Tobacco Inc composto de pirazol e agente terapêutico para diabetes compreendendo o mesmo
JP5341516B2 (ja) * 2005-09-13 2013-11-13 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 2−アニリン−4−アリール置換チアゾール誘導体
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
JO3019B1 (ar) * 2006-04-19 2016-09-05 Janssen Pharmaceutica Nv ثلاثي مستبدل 4،2،1-ثلاثي زولات
JP2011516598A (ja) * 2008-04-17 2011-05-26 グラクソ グループ リミテッド ニコチン性アセチルコリン受容体サブタイプアルファ−71のモジュレータとしてのインドール
KR20160070066A (ko) 2013-09-09 2016-06-17 멜린타 테라퓨틱스, 인크. 항균 화합물, 및 이의 제조 방법 및 이용 방법

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

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