AR085276A1 - Antagonistas de p2x7r y su uso - Google Patents

Antagonistas de p2x7r y su uso

Info

Publication number
AR085276A1
AR085276A1 ARP120100542A ARP120100542A AR085276A1 AR 085276 A1 AR085276 A1 AR 085276A1 AR P120100542 A ARP120100542 A AR P120100542A AR P120100542 A ARP120100542 A AR P120100542A AR 085276 A1 AR085276 A1 AR 085276A1
Authority
AR
Argentina
Prior art keywords
acetamide
p2x7r
azaindole
indole
halogen
Prior art date
Application number
ARP120100542A
Other languages
English (en)
Inventor
Michael Boes
Original Assignee
Affectis Pharmaceuticals Ag
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 Affectis Pharmaceuticals Ag filed Critical Affectis Pharmaceuticals Ag
Publication of AR085276A1 publication Critical patent/AR085276A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente se refiere a antagonistas de P2X7R que son compuestos de N-indol-3-il-acetamida y N-azaindol-3-il-acetamida, a composiciones farmacéuticas que los comprenden y a su uso para el tratamiento preventivo o terapéutico de enfermedades mediadas por la actividad de P2X7R.Reivindicación 1: Un compuesto de N-indol-3-il-acetamida y N-azaindol-3-il-acetamida representado por la fórmula general (1), en donde, R1 es un resto de fórmula (2) ó (3); R2 es un grupo mono- o bicicloalquilo; R3 está seleccionado del alquilo C1-5 lineal o ramificado que puede estar opcionalmente sustituido con -OH, -CH2-OH, alcoxi C1-5, CN-, CF3, halógeno (es decir, Cl, F, Br o I), piperidino, morfolino, pirrolidino, 5H-tetrazolilpropilo, metilcarbamoilo, dimetilcarbamoilo o etilcarbamoilo, en donde Ra es alquilo C1-5; R4, R5, R6, R7 están seleccionados en cada aparición, de modo independiente, de hidrógeno, halógeno (es decir, Cl, F, Br o I), metilo, metoxi, ciano o trifluorometilo, o, de ser necesario por valencia, puede estar ausente; a, b, c, d, x están seleccionados en cada aparición, de modo independiente, de carbono o nitrógeno; o una de sus sales o solvatos farmacéuticamente aceptables (en donde x debe tener un sustituyente de hidrógeno si es carbono).
ARP120100542A 2011-02-17 2012-02-17 Antagonistas de p2x7r y su uso AR085276A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11154877 2011-02-17
US201161444479P 2011-02-18 2011-02-18

Publications (1)

Publication Number Publication Date
AR085276A1 true AR085276A1 (es) 2013-09-18

Family

ID=45558013

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120100542A AR085276A1 (es) 2011-02-17 2012-02-17 Antagonistas de p2x7r y su uso

Country Status (2)

Country Link
AR (1) AR085276A1 (es)
WO (1) WO2012110190A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103819479B (zh) * 2014-03-10 2017-01-04 东华大学 一种含嘧啶基团刚性共轭大环化合物及其制备方法和应用
TW202043198A (zh) * 2019-01-17 2020-12-01 美商Ｉｆｍ Ｄｕｅ有限公司 用於治療與sting活性相關之病況的化合物及組合物
CN113233958B (zh) * 2021-01-18 2023-09-19 阜阳欣奕华材料科技有限公司 一种2-(反式-4-正丙基环己基)丙烷-1,3-二醇的制备方法

Family Cites Families (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP980096A2 (en) 1997-02-26 1998-12-31 Glaxo Group Ltd Reverse hydroxamate derivatives as matrix metalloprotease inhibitors, metalloprotease inhibitors, and tnf alpha inhibitors
ZA988967B (en) 1997-10-03 2000-04-03 Du Pont Pharm Co Lactam metalloprotease inhibitors.
SE9704544D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
SE9704546D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
SE9704545D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
EP1087937A1 (en) 1998-06-17 2001-04-04 Du Pont Pharmaceuticals Company Cyclic hydroxamic acids as metalloproteinase inhibitors
US6239151B1 (en) 1998-06-26 2001-05-29 Hoffmann-La Roche Inc. Compounds as inhibitor of tumor necrosis factor alpha release
UA59453C2 (uk) 1998-08-12 2003-09-15 Пфайзер Продактс Інк. Похідні гідроксипіпеколат гідроксамової кислоти як інгібітори матричних металопротеїназ
US20040122011A1 (en) 1998-12-23 2004-06-24 Pharmacia Corporation Method of using a COX-2 inhibitor and a TACE inhibitors as a combination therapy
US6225311B1 (en) 1999-01-27 2001-05-01 American Cyanamid Company Acetylenic α-amino acid-based sulfonamide hydroxamic acid tace inhibitors
BR0009651A (pt) 1999-04-09 2002-01-08 Astrazeneca Ab Composto, processo para a preparação de um composto, composição farmacêutica, uso de um composto, e, método para tratar artrite reumatóide e uma doença obstrutiva das vias aéreas
SE9901875D0 (sv) 1999-05-25 1999-05-25 Astra Pharma Prod Novel compounds
SE9904505D0 (sv) 1999-12-09 1999-12-09 Astra Pharma Prod Novel compounds
TWI258462B (en) 1999-12-17 2006-07-21 Astrazeneca Ab Adamantane derivative compounds, process for preparing the same and pharmaceutical composition comprising the same
SE9904652D0 (sv) 1999-12-17 1999-12-17 Astra Pharma Prod Novel Compounds
SE9904738D0 (sv) 1999-12-22 1999-12-22 Astra Pharma Prod Novel compounds
GB0013737D0 (en) 2000-06-07 2000-07-26 Astrazeneca Ab Novel compounds
WO2002018326A1 (fr) 2000-08-31 2002-03-07 Wakunaga Pharmaceutical Co., Ltd. Nouveaux derives d'acide propenohydroxamique
WO2002096426A1 (en) 2001-05-25 2002-12-05 Bristol-Myers Squibb Company Hydantion derivatives as inhibitors of matrix metalloproteinases
WO2003016248A2 (en) 2001-08-17 2003-02-27 Bristol-Myers Squibb Company Patent Department Bicyclic hydroxamates as inhibitors of matrix metalloproteinases and/or tnf-$g(a) converting enzyme (tace)
WO2003024899A2 (en) 2001-09-17 2003-03-27 Bristol-Myers Squibb Company CYCLIC HYDROXAMIC ACIDS AS INHIBITORS OF MATRIX METALLOPROTEINASES AND/OR TNF-α CONVERTING ENZYME (TACE)
WO2003031431A1 (en) 2001-10-09 2003-04-17 Bristol-Myers Squibb Company Cyclic sulfone derivatives as inhibitors of matrix metalloproteinases and/or tnf-$g(a) converting enzyme (tace)
US6884806B2 (en) 2001-10-17 2005-04-26 Bristol-Myers Squibb Company Bicyclic lactam derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
WO2003040103A1 (en) 2001-11-02 2003-05-15 Bristol-Myers Squibb Company β-SULFONE DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEINASES AND/OR TNF-α CONVERTING ENZYME (TACE)
PA8557501A1 (es) 2001-11-12 2003-06-30 Pfizer Prod Inc Benzamida, heteroarilamida y amidas inversas
WO2003042190A1 (en) 2001-11-12 2003-05-22 Pfizer Products Inc. N-alkyl-adamantyl derivatives as p2x7-receptor antagonists
SE0103836D0 (sv) 2001-11-16 2001-11-16 Astrazeneca Ab Novel compounds
WO2003047515A2 (en) 2001-11-30 2003-06-12 The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services P2x7 receptor antagonists
US7294624B2 (en) 2001-12-20 2007-11-13 Bristol Myers Squibb Company Barbituric acid derivatives as inhibitors of TNF-α converting enzyme (TACE) and/or matrix metalloproteinases
CN1617725A (zh) 2001-12-21 2005-05-18 王者制药研究发展有限公司 酪氨酰衍生物及其作为p2x7受体调节剂的用途
US7101883B2 (en) 2002-03-18 2006-09-05 Bristol-Myers Squibb Company Uracil derivatives as inhibitors of TNF-α converting enzyme (TACE) and matrix metalloproteinases
SE0200920D0 (sv) 2002-03-25 2002-03-25 Astrazeneca Ab Novel compounds
GB0216379D0 (en) 2002-07-13 2002-08-21 Astrazeneca Ab Compounds
AU2003261319A1 (en) 2002-08-01 2004-02-23 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme
WO2004033632A2 (en) 2002-10-04 2004-04-22 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme (tace)
EP1558581A4 (en) 2002-10-07 2007-07-25 Bristol Myers Squibb Co DERIVATIVES OF TRIAZOLONE AND TRIAZOLETHIONE
AU2003301903A1 (en) 2002-11-06 2004-06-03 Bristol-Myers Squibb Company Isoxazoline derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme
BR0317844A (pt) 2002-12-31 2005-12-06 Pfizer Prod Inc Inibidores de benzamida do receptor p2x7
PA8591801A1 (es) 2002-12-31 2004-07-26 Pfizer Prod Inc Inhibidores benzamidicos del receptor p2x7.
SE0300480D0 (sv) 2003-02-21 2003-02-21 Astrazeneca Ab Novel compounds
ES2396565T3 (es) 2003-05-12 2013-02-22 Pah Usa 15 Llc Inhibidores benzamida del receptor P2X7
GB0312609D0 (en) 2003-06-02 2003-07-09 Astrazeneca Ab Novel compounds
US7132432B2 (en) 2003-06-05 2006-11-07 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of tumor necrosis factor-alpha converting enzyme (TACE)
GB0324498D0 (en) 2003-07-21 2003-11-26 Aventis Pharma Inc Heterocyclic compounds as P2X7 ion channel blockers
SE0302139D0 (sv) 2003-07-28 2003-07-28 Astrazeneca Ab Novel compounds
SE0302192D0 (sv) 2003-08-08 2003-08-08 Astrazeneca Ab Novel compounds
WO2005019182A1 (en) 2003-08-20 2005-03-03 Bayer Healthcare Ag Pyrazolylmethylbenzamide derivatives as p2xt-receptor antagonists
WO2005039590A1 (en) 2003-10-21 2005-05-06 Inspire Pharmaceuticals, Inc. Non-nucleotide compositions and method for treating pain
MXPA06012595A (es) 2004-04-29 2007-05-09 Abbott Lab Analogos de amino-tetrazoles y metodos de uso.
MXPA06015273A (es) 2004-06-29 2007-03-15 Pfizer Prod Inc Procedimiento para preparar derivados de 5-[4-(2-hidroxi -etil)-3, 5-dioxo-4, 5-dihidro-3h-[1, 2, 4]-triazin -2-il]-benzamida con actividad inhibidora de p2x7 mediante reaccion del derivado no sustituido en posicion 4 de la triazina con un oxirano en
CN1980902A (zh) 2004-06-29 2007-06-13 辉瑞产品有限公司 通过对羟基保护前体去保护而制备5－4－(2－羟基－丙基)－3，5－二氧代－4，5－二氢－3h－[1，2，4]三嗪－2－基－苯甲酰胺衍生物的方法
US7241776B2 (en) 2004-08-02 2007-07-10 Abbott Laboratories Cyanoamidine P2X7 antagonists for the treatment of pain
SA05260265A (ar) 2004-08-30 2005-12-03 استرازينيكا ايه بي مركبات جديدة
SE0402925D0 (sv) 2004-11-30 2004-11-30 Astrazeneca Ab Novel Compounds
DE602005026703D1 (de) 2004-12-24 2011-04-14 Astrazeneca Ab Amidderivate
EP1844003A4 (en) 2005-01-27 2010-09-22 Astrazeneca Ab NEW BIAROMATIC COMPOUNDS AS INHIBITORS OF THE P2X7 RECEPTOR
US20060211739A1 (en) 2005-02-08 2006-09-21 Arturo Perez-Medrano Use of selective P2X7 receptor antagonists
US7402596B2 (en) 2005-03-24 2008-07-22 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
WO2006110516A1 (en) 2005-04-11 2006-10-19 Abbott Laboratories Acylhydrazide p2x7 antagonists and uses thereof
WO2006136004A1 (en) 2005-05-05 2006-12-28 Medicure International Inc. Inhibition of atp-mediated, p2x7 dependent pathways by pyridoxal-5-phosphaste and vitamin b6 related compounds
WO2007016597A2 (en) 2005-07-29 2007-02-08 The Regents Of The University Of California Targeting tnf-alpha converting enzyme (tace)-dependent growth factor shedding in cancer therapy
WO2007025366A1 (en) 2005-08-29 2007-03-08 Irma Bernatchez-Lemaire Use of histogranin and histogranin-like compounds as inhibitors of p2x7 receptor function and as anti-arthritic agents
WO2007028022A2 (en) 2005-09-01 2007-03-08 Renovis, Inc. Novel compounds as p2x7 modulators and uses thereof
JP2009514864A (ja) 2005-11-07 2009-04-09 アボット・ラボラトリーズ Ｐ２ｘ７受容体拮抗薬および使用方法
EP1963275A2 (en) 2005-11-09 2008-09-03 Abbott Laboratories P2x7 receptor antagonists and uses thereof
US20100298285A1 (en) 2006-03-16 2010-11-25 Kelly Michael G Biclycloheteroaryl Compounds as P2x7 Modulators and Uses Thereof
EP2001474B1 (en) 2006-03-16 2016-03-09 Second Genome, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
WO2007109154A2 (en) 2006-03-16 2007-09-27 Renovis, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
TWI464148B (zh) 2006-03-16 2014-12-11 Evotec Us Inc 作為ｐ２ｘ7調節劑之雙環雜芳基化合物與其用途
ES2596532T3 (es) 2006-03-16 2017-01-10 Second Genome, Inc. Compuestos de bicicloheteroarilo como moduladores de P2X7 y usos de los mismos
WO2007109201A2 (en) 2006-03-16 2007-09-27 Renovis, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
JP2009539795A (ja) 2006-06-06 2009-11-19 グラクソ グループ リミテッド 疼痛、炎症および神経変性の治療のためのｐ２ｘ７アンタゴニストとしてのｎ−（フェニルメチル）−２−（１ｈ−ピラゾール−４−イル）アセトアミド誘導体
GB0611154D0 (en) 2006-06-06 2006-07-19 Glaxo Group Ltd Novel receptor antagonists and their methods of use
US20080076924A1 (en) 2006-06-30 2008-03-27 Patrick Betschmann Piperazines as P2X7 antagonists
EA016076B1 (ru) 2006-07-06 2012-01-30 Глэксо Груп Лимитед Замещенные n-фенилметил-5-оксопролин-2-амиды в качестве антагонистов р2х7-рецептора и способы их применения
US20080058309A1 (en) 2006-07-27 2008-03-06 Astrazeneca Ab Novel Compounds 171
BRPI0809930A2 (pt) 2007-04-03 2014-10-07 Glaxo Group Ltd Derivados de carboxamida imidazolidina como moduladores de p2x7
MX2009010523A (es) 2007-04-10 2009-12-15 Lundbeck & Co As H Análogos de amidas heteroarílicas como antagonistas de p2x7.
JP2010523623A (ja) 2007-04-11 2010-07-15 グラクソ グループ リミテッド Ｐ２ｘ７調節因子としてのピラゾール誘導体
US20110046137A1 (en) 2007-05-10 2011-02-24 Glaxo Group Limited Pyrazole Derivatives as P2X7 Modulators
WO2009019503A2 (en) 2007-08-03 2009-02-12 Astrazeneca Ab P2x7 antagonists for use in the treatment of mood disorders
AU2008286946B2 (en) * 2007-08-10 2013-11-21 H. Lundbeck A/S Heteroaryl amide analogues
JP2011500767A (ja) 2007-10-26 2011-01-06 グラクソ グループ リミテッド Ｐ２ｘ７モジュレータとしての４−ベンゾイル−１−置換ピペラジン−２−オン誘導体
PE20091036A1 (es) 2007-11-30 2009-08-15 Astrazeneca Ab Derivado de quinolina como antagonista del receptor p2x7
US20100292295A1 (en) 2007-12-18 2010-11-18 Glaxo Group Limited 5-oxo-3-pyrrolidinecarboxamide derivatives as p2x7 modulators
ES2357682T3 (es) 2008-03-25 2011-04-28 Affectis Pharmaceuticals Ag Antagonistas de p2x7r novedosos y su utilización.
US8431704B2 (en) 2008-04-22 2013-04-30 Janssen Pharmaceutica Nv Quinoline or isoquinoline substituted P2X7 antagonists
MX2011010810A (es) 2009-04-14 2012-01-12 Affectis Pharmaceuticals Ag Nuevos antagonistas de p2x7r y su uso.
GB0907425D0 (en) 2009-04-29 2009-06-10 Glaxo Group Ltd Compounds

Also Published As

Publication number Publication date
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