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PE20140703A1 - Derivados de heteroarilo como moduladores de nachr alfa 7 - Google Patents

Derivados de heteroarilo como moduladores de nachr alfa 7

Info

Publication number
PE20140703A1
PE20140703A1 PE2013001969A PE2013001969A PE20140703A1 PE 20140703 A1 PE20140703 A1 PE 20140703A1 PE 2013001969 A PE2013001969 A PE 2013001969A PE 2013001969 A PE2013001969 A PE 2013001969A PE 20140703 A1 PE20140703 A1 PE 20140703A1
Authority
PE
Peru
Prior art keywords
nitro
optionally substituted
cyane
halogen
alkyl optionally
Prior art date
Application number
PE2013001969A
Other languages
English (en)
Inventor
Neelima Sinha
Gourhari Jana
Sachchidanand Sachchidanand
Sanjay Parlhad Kurhade
Navnath Popat Karche
Anil Kashiram Hajare
Ajay Ramchandra Tilekar
Venkata P Palle
Rajender Kumar Kamboj
Original Assignee
Lupin Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45873193&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20140703(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Lupin Ltd filed Critical Lupin Ltd
Publication of PE20140703A1 publication Critical patent/PE20140703A1/es

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    • 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
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    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
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  • Pyrrole Compounds (AREA)

Abstract

REFERIDA A UN COMPUESTO HETEROARILO DE FORMULA (I), DONDE Z ES S, O Y N(Ra); Ra ES H, ALQUILO C1-C20 OPCIONALMENTE SUSTITUIDO CON O, HALOGENO, NITRO, ENTRE OTROS, ALQUENILO C1-C6 OPCIONALMENTE SUSTITUIDO CON HALOGENO, O, NITRO, CIANO, ENTRE OTROS; R1 ES ARILO OPCIONALMENTE SUSTITUIDO CON HALOGENO, NITRO, CIANO, ENTRE OTROS, HETEROARILO OPCIONALMENTE SUSTITUIDO CON NITRO, OXO, HALOGENO, ENTRE OTROS; R2 ES H, ALQUILO C1-C20 OPCIONALMENTE SUSTITUIDO HALOGENO, NITRO, CIANO, ENTRE OTROS; R3 ES ALQUILO C1-C20 OPCIONALMENTE SUSTITUIDO CON NITRO, OXO, CIANO, ENTRE OTROS; m ES 0 A 3; R4 ES HALOGENO, CIANO, ALQUILO OPCIONALMENTE SUSTITUIDO CON OXO, CIANO, NITRO, ENTRE OTROS; R5 Y R6 SON H, R7aC(=O), ALQUILO C1-C20 OPCIONALMENTE SUSTITUIDO CON NITRO, OXO, CIANO, ENTRE OTROS; R7a ES ALQUILO C1-C20 OPCIONALMENTE SUSTITUIDO CON NITRO, OXO, CIANO, ENTRE OTROS, ALQUENILO C1-C6 OPCIONALMENTE SUSTITUIDO CON HALOGENO, O, NITRO, CIANO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-(5-(4-CLOROFENILO)-4-METIL-2-PROPIONILOTIOFEN-3-ILO)BENCENO SULFONAMIDA, 4-(5-(3-CLOROFENILO)-4-METIL-2-PROPIONILOTIOFEN-3-ILO)BENCENO SULFONAMIDA, 4-(4-METIL-2-PROPIONILO-5-(4-TOLILO)TIOFEN-3-ILO)BENCENO SULFONAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE RECEPTORES DE ACETILCOLINA NICOTINICA DEL SUBTIPO ALFA7 (nAChR ALFA 7) Y SON UTILES EN EL TRATAMIENTO DE ALZHEIMER, DETERIORO COGNITIVO LEVE, DEMENCIA SENIL, ENTRE OTROS
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Families Citing this family (16)

* 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
SG11201405239WA (en) 2012-03-06 2014-09-26 Lupin Ltd Thiazole derivatives as alpha 7 nachr modulators
ES2913753T3 (es) * 2012-09-28 2022-06-06 Takeda Pharmaceuticals Co Forma cristalina de 1-(4-1-(2,6-difluorobencil)-5-dimetilaminometil-3-(6-metoxipiridazin-3-il)-2,4-dioxo-1,2,3,4-tetrahidrotieno(2,3-d)-pirimidin-6il)fenil)-3-metoxiurea
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
AU2014229300A1 (en) * 2013-03-13 2015-06-11 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
US9504680B2 (en) * 2013-06-17 2016-11-29 Lupin Limited Pyrrole derivatives as alpha 7 nAChR modulators
EP3233087B1 (en) 2014-12-16 2019-10-02 Axovant Sciences GmbH Geminal substituted quinuclidine amide compounds as agonists of alpha-7 nicotinic acetylcholine receptors
JP2018516973A (ja) 2015-06-10 2018-06-28 フォーラム・ファーマシューティカルズ・インコーポレイテッドForum Pharmaceuticals Inc. 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アミノベンゾイソオキサゾール化合物
WO2017027600A1 (en) 2015-08-12 2017-02-16 Forum Pharmaceuticals, Inc. GEMINAL SUBSTITUTED AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF α7-NICOTINIC ACETYLCHOLINE RECEPTORS
SG11201808220VA (en) * 2016-03-22 2018-10-30 Merck Sharp & Dohme Allosteric modulators of nicotinic acetylcholine receptors
JP2021527064A (ja) * 2018-06-07 2021-10-11 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン Prc1阻害剤及びそれを用いた治療方法
AR115698A1 (es) * 2018-07-05 2021-02-17 Bayer Ag Tieniloxazolonas y análogos de las mismas
KR102829826B1 (ko) 2019-07-03 2025-07-04 바이엘 악티엔게젤샤프트 살미생물제로서의 치환된 티오펜 카르복스아미드 및 그의 유도체
EP4285723A3 (en) 2019-12-20 2024-03-27 Bayer Aktiengesellschaft Substituted thiophene carboxamides, thiophene carboxylic acids and derivatives thereof

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3953596A (en) 1973-06-14 1976-04-27 Ici United States Inc. 8-Oxa-3-azabicyclo(3.2.1)octane analgesic compositions and method of alleviating pain in animals
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
US5608082A (en) 1994-07-28 1997-03-04 Agouron Pharmaceuticals, Inc. Compounds useful as antiproliferative agents and GARFT inhibitors
WO1999014194A1 (en) 1997-09-12 1999-03-25 Merck Frosst Canada & Co. 2,3,5-trisubstituted pyridines as inhibitors of cyclooxygenase-2
JP2004506734A (ja) * 2000-08-21 2004-03-04 ファルマシア・アンド・アップジョン・カンパニー 疾患治療用のキヌクリド置換ヘテロアリール部分
TWI262917B (en) 2002-02-01 2006-10-01 Dainippon Sumitomo Pharma Co 2-Furancarboxylic hydrazides and pharmaceutical compositions containing the same
US7202367B2 (en) 2002-05-31 2007-04-10 Rhodia Chimie Process for arylating or vinylating or alkynating a nucleophilic compound
SE0201938D0 (sv) 2002-06-20 2002-06-20 Astrazeneca Ab New process
DE10244810A1 (de) 2002-09-26 2004-04-08 Bayer Ag Neue Morpholin-überbrückte Indazolderivate
US7129235B2 (en) 2003-07-11 2006-10-31 Abbott Laboratories Amides useful for treating pain
US7442805B2 (en) 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
GB0403038D0 (en) 2004-02-11 2004-03-17 Novartis Ag Organic compounds
EP1732883A1 (en) 2004-03-29 2006-12-20 Neurosearch A/S Novel urea derivatives and their medical use
ITTO20040264A1 (it) 2004-04-28 2004-07-28 Rotta Res Lab Spa Nuovi derivati pirrolici ad attivita' angiotensina-ii antagonista
EP1790640A4 (en) 2004-09-09 2009-07-29 Chugai Pharmaceutical Co Ltd NEW IMIDAZOLIDINE DERIVATIVE AND APPLICATION THEREOF
US20060142349A1 (en) 2004-12-23 2006-06-29 Pfizer Inc Methods of modulating the activities of alpha-7 nicotinic acetylcholine receptor
ATE481407T1 (de) 2005-02-16 2010-10-15 Neurosearch As Neue diazabicyclische arylderivate und medizinische verwendung dafür
FR2885616B1 (fr) 2005-05-12 2007-06-22 Servier Lab Nouveaux derives de phenylpyridinylpiperazine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2007001225A1 (en) * 2005-06-29 2007-01-04 Astrazeneca Thiophene-2-carboxamide derivatives as alpha 7 nicotinic receptor modulators.
CA2617788A1 (en) 2005-08-04 2007-02-15 Apogee Biotechnology Corporation Sphingosine kinase inhibitors and methods of their use
CA2617394C (en) 2005-09-13 2014-06-03 Janssen Pharmaceutica N.V. 2-aniline-4-aryl substituted thiazole derivatives
WO2007092751A2 (en) 2006-02-03 2007-08-16 Eli Lilly And Company Compounds and methods for modulating fx-receptors
ATE455114T1 (de) 2006-02-16 2010-01-15 Neurosearch As Enantiomerenreine chinuclidinyloxy-pyridazine und ihre verwendung als nikotin-acetylcholin- rezeptorliganden
JO3019B1 (ar) 2006-04-19 2016-09-05 Janssen Pharmaceutica Nv ثلاثي مستبدل 4،2،1-ثلاثي زولات
CA2647601A1 (en) 2006-06-27 2008-01-03 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
AU2007318058A1 (en) 2006-11-02 2008-05-15 Merck Sharp & Dohme Corp. Heterocyclyl-substituted anti-hypercholesterolemic compounds
US20080287479A1 (en) 2006-12-20 2008-11-20 Pfizer Inc Inhibitors of serine palmitoyltransferase
US8110588B2 (en) 2007-08-08 2012-02-07 Neurosearch A/S 1,2,3-triazole derivatives useful as modulators of nicotinic acetylcholine receptors
GB0718735D0 (en) 2007-09-25 2007-11-07 Prolysis Ltd Antibacterial agents
EP2205573B1 (en) 2007-10-04 2013-10-23 F. Hoffmann-La Roche AG Tetrazole-substituted aryl amide derivatives and uses thereof
MX2010003155A (es) 2007-10-04 2010-04-01 Hoffmann La Roche Derivados de ciclopropil aril amida y uso de los mismos.
JO2784B1 (en) 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 5,3,1 - Triazole substitute derivative
AR070936A1 (es) 2008-03-19 2010-05-12 Janssen Pharmaceutica Nv 1,2,4 -triazoles trisustituidos
US7786171B2 (en) 2008-04-04 2010-08-31 Abbott Laboratories Amide derivatives as positive allosteric modulators and methods of use thereof
CN102066357B (zh) 2008-04-17 2014-04-09 葛兰素集团有限公司 作为烟碱型乙酰胆碱受体亚型α71的调节剂的吲哚衍生物
AU2009245715B2 (en) 2008-05-09 2014-01-09 Janssen Pharmaceutica Nv Trisubstituted pyrazoles as acetylcholine receptor modulators
WO2010083444A1 (en) 2009-01-15 2010-07-22 Anvyl, Llc Alpha7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof
WO2010120854A1 (en) 2009-04-15 2010-10-21 Glaxosmithkline Llc Chemical compounds
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
JP5865397B2 (ja) * 2011-02-03 2016-02-17 ルピン・リミテッドLupin Limited α7nAChRのモジュレータとして使用されるピロール誘導体
MA34957B1 (fr) 2011-02-23 2014-03-01 Lupin Ltd Derives heteroaryle a titre modulateurs des nachr alpha 7
SG193387A1 (en) 2011-03-31 2013-10-30 Lupin Ltd 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

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