BR112013025128A2 - derivados de pirrol como moduladores de receptor de acetilcolina nicotínico para uso no tratamento de distúrbios neurodegenenerativos tal como doença de alzheimer e doença de parkinson - Google Patents

derivados de pirrol como moduladores de receptor de acetilcolina nicotínico para uso no tratamento de distúrbios neurodegenenerativos tal como doença de alzheimer e doença de parkinson

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Publication number
BR112013025128A2
BR112013025128A2 BR112013025128A BR112013025128A BR112013025128A2 BR 112013025128 A2 BR112013025128 A2 BR 112013025128A2 BR 112013025128 A BR112013025128 A BR 112013025128A BR 112013025128 A BR112013025128 A BR 112013025128A BR 112013025128 A2 BR112013025128 A2 BR 112013025128A2
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BR
Brazil
Prior art keywords
disease
alzheimer
acetylcholine receptor
nicotinic acetylcholine
parkinson
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Application number
BR112013025128A
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English (en)
Inventor
Ramchandra Tilekar Ajay
Jana Gourhari
Popat Karche Navnath
Sinha Neelima
Kumar Kamboj Rajender
P Palle Venkata
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Lupin Ltd
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Publication date
Application filed by Lupin Ltd filed Critical Lupin Ltd
Publication of BR112013025128A2 publication Critical patent/BR112013025128A2/pt

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Abstract

derivados de pirrol como moduladores de receptor de acetilcolina nicotínico para uso no tratamento de distúrbios neurodegenenerativos tal como doença de alzheimer e doença de parkinson é revelado um composto da fórmula i: em que "a" e r^ 1^ a r^ 5^ são conforme descrito no presente documento, como um modulador de receptores nicotínicos de acetilcolina, particulamente o subtipo <244>7, em um sujeito que precisa do mesmo, assim como análogos, pró-fármacos, análogos isitopicamente substituídos, metabólitos, sais farmaceuticamente aceitáveis, polimorfos, solvatos, isômeros, claratos e cocristais dos mesmos, para uso seja sozinho ou em combinações com outros medicamentos adequados e composições farmacêuticas que contém tais compostos e análogos. um processo de preparação dos compostos e os usos pretendidos dos mesmos em terapia, particularmente na profilaxia e na terapia de distúrbios tais como doença de alzheimer, deficiência cognitiva leve, demência senil e semelhantes também são revelados.
BR112013025128A 2011-03-31 2012-03-27 derivados de pirrol como moduladores de receptor de acetilcolina nicotínico para uso no tratamento de distúrbios neurodegenenerativos tal como doença de alzheimer e doença de parkinson BR112013025128A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN458KO2011 2011-03-31
PCT/IB2012/051451 WO2012131576A1 (en) 2011-03-31 2012-03-27 Pyrrole derivatives as nicotinic acetylcholine receptor modulators for use in the treatment of neurodegenerative disorders such as alzheimer's and parkinson's disease

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BR112013025128A2 true BR112013025128A2 (pt) 2017-02-14

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US (1) US9187420B2 (pt)
EP (1) EP2691368A1 (pt)
JP (2) JP2014509641A (pt)
KR (1) KR20140025395A (pt)
CN (1) CN103443075A (pt)
AU (1) AU2012235779B2 (pt)
BR (1) BR112013025128A2 (pt)
CA (1) CA2829860A1 (pt)
MX (1) MX344696B (pt)
SG (1) SG193387A1 (pt)
WO (1) WO2012131576A1 (pt)
ZA (1) ZA201306833B (pt)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA34957B1 (fr) 2011-02-23 2014-03-01 Lupin Ltd Derives heteroaryle a titre modulateurs des nachr alpha 7
US9187420B2 (en) * 2011-03-31 2015-11-17 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
US9388196B2 (en) 2012-03-06 2016-07-12 Lupin Limited Thiazole derivatives as alpha 7 nAChR modulators
WO2014072957A1 (en) 2012-11-12 2014-05-15 Lupin Limited Thiazole derivatives as alpha 7 nachr modulators
US9617211B2 (en) 2013-01-16 2017-04-11 Lupin Limited Pyrrole derivatives as alpha 7 nAChR modulators
WO2014141091A1 (en) 2013-03-13 2014-09-18 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
CA2913987A1 (en) 2013-06-17 2014-12-24 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
JP6612874B2 (ja) 2014-12-16 2019-11-27 アクソファント サイエンシーズ ゲーエムベーハー α７−ニコチン性アセチルコリン受容体のアゴニストとしてのジェミナル置換キヌクリジンアミド化合物
MX2017016231A (es) 2015-06-10 2018-11-29 Axovant Sciences Gmbh Compuestos de aminobencisoxazol como agonistas de receptores a7-nicotínicos de acetilcolina.
US10428062B2 (en) 2015-08-12 2019-10-01 Axovant Sciences Gmbh Geminal substituted aminobenzisoxazole compounds as agonists of α7-nicotinic acetylcholine receptors
JP6927734B2 (ja) 2017-04-18 2021-09-01 株式会社ミツトヨ 駆動ステージ装置の駆動制御方法

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4501728A (en) 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
US5019369A (en) 1984-10-22 1991-05-28 Vestar, Inc. Method of targeting tumors in humans
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
US5908858A (en) * 1996-04-05 1999-06-01 Sankyo Company, Limited 1,2-diphenylpyrrole derivatives, their preparation and their therapeutic uses
US6372777B1 (en) * 1999-12-23 2002-04-16 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
TW200420573A (en) 2002-09-26 2004-10-16 Rib X Pharmaceuticals Inc Bifunctional heterocyclic compounds and methods of making and using same
RU2006131454A (ru) 2004-03-29 2008-05-10 Ньюросерч А/С (DK) Новые производные мочевины и их медицинское применение
US20060142349A1 (en) 2004-12-23 2006-06-29 Pfizer Inc Methods of modulating the activities of alpha-7 nicotinic acetylcholine receptor
DE602006016926D1 (de) 2005-02-16 2010-10-28 Neurosearch As Neue diazabicyclische arylderivate und medizinische verwendung dafür
EP1928859A1 (en) * 2005-06-17 2008-06-11 Carex SA Pyrazole derivates as cannabinoid receptor modulators
WO2007031440A2 (en) 2005-09-13 2007-03-22 Janssen Pharmaceutica N.V. 2-aniline-4-aryl substituted thiazole derivatives
EP1987029B1 (en) 2006-02-16 2010-01-13 Neurosearch A/S Enantiopure quinuclidinyloxy pyridazines and their use as nicotinic acetylcholine receptor ligands
JO3019B1 (ar) 2006-04-19 2016-09-05 Janssen Pharmaceutica Nv ثلاثي مستبدل 4،2،1-ثلاثي زولات
US7741364B2 (en) 2006-06-27 2010-06-22 Abbott Laboratories Pyrrole derivatives and their methods of use
US7683084B2 (en) 2006-06-27 2010-03-23 Abbott Laboratories Thiazoline and oxazoline derivatives and their methods of use
EP2168959A1 (en) 2007-06-19 2010-03-31 Kyorin Pharmaceutical Co., Ltd. Pyridazinone derivative and pde inhibitor containing the same as active ingredient
EP2185529A1 (en) 2007-08-08 2010-05-19 NeuroSearch AS Novel 1,2,3-triazole derivatives useful as modulators of nicotinic acetylcholine receptors
CN101821246B (zh) 2007-10-04 2013-05-01 弗·哈夫曼-拉罗切有限公司 四唑取代的芳基酰胺衍生物及其用途
AU2008307195B2 (en) 2007-10-04 2012-11-22 F. Hoffmann-La Roche Ag Cyclopropyl aryl amide derivatives and uses thereof
JO2784B1 (en) 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 5,3,1 - Triazole substitute derivative
KR101564303B1 (ko) 2008-03-19 2015-11-06 얀센 파마슈티카 엔.브이. 니코틴성 아세틸콜린 수용체 조절제로서의 삼치환된 1,2,4-트리아졸
US7786171B2 (en) 2008-04-04 2010-08-31 Abbott Laboratories Amide derivatives as positive allosteric modulators and methods of use thereof
EP2279183B1 (en) 2008-04-17 2012-08-08 Proximagen Limited Indoles as modulators of nicoticic acetylcholine receptor subtype alpha-7
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.
EP2387575B1 (en) 2009-01-15 2013-09-04 Anvyl, LLC Alpha7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof
WO2010130768A1 (en) 2009-05-14 2010-11-18 Neurosearch A/S Novel 1,4-diaza-bicyclo[3.2.1]octane derivatives useful as nicotinic acetylcholine receptor modulators
JO3250B1 (ar) 2009-09-22 2018-09-16 Novartis Ag إستعمال منشطات مستقبل نيكوتينيك أسيتيل كولين ألفا 7
JO3078B1 (ar) 2009-11-27 2017-03-15 Janssen Pharmaceutica Nv مورفولينوثيازولات بصفتها منظمات الوستيرية نوع الفا 7 موجبة
MX344701B (es) * 2011-02-03 2017-01-03 Lupin Ltd Derivados de pirrol como moduladores de nachr alfa 7.
US9187420B2 (en) * 2011-03-31 2015-11-17 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

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AU2012235779B2 (en) 2017-03-02
ZA201306833B (en) 2015-04-29
MX344696B (es) 2017-01-03
SG193387A1 (en) 2013-10-30
JP2014509641A (ja) 2014-04-21
EP2691368A1 (en) 2014-02-05
CN103443075A (zh) 2013-12-11
JP2017081986A (ja) 2017-05-18
KR20140025395A (ko) 2014-03-04
CA2829860A1 (en) 2012-10-04
US20140018327A1 (en) 2014-01-16
WO2012131576A1 (en) 2012-10-04
AU2012235779A1 (en) 2013-10-03
NZ615583A (en) 2015-09-25
US9187420B2 (en) 2015-11-17

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