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AR076373A1 - N-pirazolil carboxamidas como inhibidores de canales de calcio - Google Patents

N-pirazolil carboxamidas como inhibidores de canales de calcio

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Publication number
AR076373A1
AR076373A1 ARP100101334A ARP100101334A AR076373A1 AR 076373 A1 AR076373 A1 AR 076373A1 AR P100101334 A ARP100101334 A AR P100101334A AR P100101334 A ARP100101334 A AR P100101334A AR 076373 A1 AR076373 A1 AR 076373A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
halogen
formula
alkoxy
Prior art date
Application number
ARP100101334A
Other languages
English (en)
Original Assignee
Glaxo Group 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
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR076373A1 publication Critical patent/AR076373A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/02—Nasal agents, e.g. decongestants
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    • A—HUMAN NECESSITIES
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Abstract

Se refiere a compuestos de amida, a procedimientos para su preparacion, a composiciones farmacéuticas que contienen estos compuestos y a su uso en el tratamiento de trastornos, afecciones o trastornos tales como trastornos alérgicos, trastornos inflamatorios y trastornos del sistema inmune. Reivindicacion 1: Un compuesto de formula (1) o un profármaco del mismo en la que Ra es un grupo de formula (2) en la que R1a es alquilo C1-6, CF3, OCF3, alcoxi C1-6 o R1a es un grupo L1-Z1 en el que L1 es O, CH2, OCH2 o CH2O y Z1 es cicloalquilo C3-7 o arilo; o Ra es un grupo de formula (3) en la que R2a es halogeno, alquilo C1-6, CF3 u OCH2Ph; y R3a es halogeno, alquilo C1-6, alcoxi C1-6, hidroxi, cicloalquilo C3-7, CO2alquiIo C1-4 o R3a es un grupo L2-Z2 en el que L2 es O, CH2 u O(CH2)n en el que n es un numero entero de 1-7; y Z2 es hidroxi, metoxi, CO2alquilo C1-4, cicloalquilo C3-7, arilo o heteroarilo; o Ra es un grupo de formula (4) en la que R4a es halogeno, alquilo C1-6, alcoxi C1-6, CF3 u OCH2Ph; y R5a es halogeno, alquilo C1-6, hidroxi, alcoxi C1-6 opcionalmente sustituido con metoxi, o R5a es un grupo L3-Z3 en el que L3 es un enlace sencillo, O, CH2, OCH2 o CH2O y Z3 es cicloalquilo C3-7, arilo o heteroarilo; Ra es un grupo de formula (5) en la que R6a es CI, Br, alquilo C1-6 o CF3; y R7a es halogeno, alquilo C1-6, CF3, OCF3, OCHF2, alcoxi C1-6 o R7a es un grupo L4-Z4 en el que L4 es OCH2 y Z4 es cicloalquilo C3-7; Rb es un grupo de formula (6) en la que Y es CH o N, R1b es halogeno, alquilo C1-6 o CF3; R2b es H, halogeno, alquilo C1-6 o alcoxi C1-6 o una sal del mismo sujeto a la condicion de que no sea un compuesto seleccionado entre 2,6-Difluoro-N-{1-[(2-metilfenil)metil]-1H-pirazol-3-il}benzamida; 2-Fluoro-N-{1-[(2-metilfenil)metil]-1H-pirazol-3-iI}benzamida; 2,6-Dicloro-N-{1-[(2-metilfenil)metil]-1H-pirazol-3-il}benzamida; 2-Metil-N-{1-[(2-metilfenil]-1H-pirazol-3-il}benzamida; y 2-Bromo-N-[1-{(2,5-diclorofenil)metil]-1H-pirazol-3-iI}benzamida.
ARP100101334A 2009-04-24 2010-04-22 N-pirazolil carboxamidas como inhibidores de canales de calcio AR076373A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17228509P 2009-04-24 2009-04-24
US29580110P 2010-01-18 2010-01-18

Publications (1)

Publication Number Publication Date
AR076373A1 true AR076373A1 (es) 2011-06-08

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ARP100101334A AR076373A1 (es) 2009-04-24 2010-04-22 N-pirazolil carboxamidas como inhibidores de canales de calcio

Country Status (7)

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US (2) US8399436B2 (es)
EP (1) EP2421835A1 (es)
JP (1) JP2012524755A (es)
AR (1) AR076373A1 (es)
TW (1) TW201103892A (es)
UY (1) UY32571A (es)
WO (1) WO2010122089A1 (es)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10703722B2 (en) 2010-04-27 2020-07-07 Calcimedica, Inc. Compounds that modulate intracellular calcium
EP2563759B1 (en) 2010-04-27 2022-04-06 Calcimedica, Inc. Compounds that modulate intracellular calcium
HUE029570T2 (en) 2010-04-27 2017-03-28 Calcimedica Inc Intracellular calcium modifying compounds
US9079891B2 (en) 2010-08-27 2015-07-14 Calcimedica, Inc. Compounds that modulate intracellular calcium
JP2013544794A (ja) 2010-10-21 2013-12-19 グラクソ グループ リミテッド アレルギー性障害、炎症性障害及び免疫障害に作用するピラゾール化合物
ES2532213T3 (es) * 2010-10-21 2015-03-25 Glaxo Group Limited Compuestos de pirazol que actúan contra afecciones alérgicas, inmunitarias e inflamatorias
US20120316182A1 (en) 2011-06-10 2012-12-13 Calcimedica, Inc. Compounds that modulate intracellular calcium
US9856240B2 (en) 2011-10-19 2018-01-02 Calcimedica, Inc. Compounds that modulate intracellular calcium
US9512116B2 (en) 2012-10-12 2016-12-06 Calcimedica, Inc. Compounds that modulate intracellular calcium
EP2738172A1 (en) 2012-11-28 2014-06-04 Almirall, S.A. New bicyclic compounds as crac channel modulators
BR112015016394A2 (pt) 2013-01-10 2017-07-11 Gruenenthal Gmbh carboxamidas ii baseadas em pirazolil como inibidoras do canal crac
US9206136B2 (en) 2013-01-10 2015-12-08 Grünenthal GmbH Pyrazolyl-based carboxamides I
EP2848615A1 (en) 2013-07-03 2015-03-18 Almirall, S.A. New pyrazole derivatives as CRAC channel modulators
WO2015090579A1 (en) * 2013-12-18 2015-06-25 Grünenthal GmbH Pyrazolyl-based carboxamides iv
SG11201606351VA (en) 2014-02-03 2016-09-29 Quadriga Biosciences Inc Beta-substituted beta-amino acids and analogs as chemotherapeutic agents
EP3102194A1 (en) 2014-02-03 2016-12-14 Quadriga Biosciences, Inc. Beta-substituted gamma-amino acids and analogs as chemotherapeutic agents
UA121548C2 (uk) 2014-06-03 2020-06-25 Ідорсія Фармасьютікалз Лтд Піразольні сполуки та їх застосування як блокаторів кальцієвих каналів t-типу
WO2015197187A1 (en) 2014-06-24 2015-12-30 Grünenthal GmbH Pyrazolyl-based carboxamides v
AU2016224993B2 (en) 2015-02-27 2019-11-21 Calcimedica, Inc. Pancreatitis treatment
CN107847548B (zh) 2015-05-18 2022-06-14 贝思以色列女会吏医学中心公司 P物质、肥大细胞脱颗粒抑制剂和周围神经病
US9783487B2 (en) 2015-08-03 2017-10-10 Quadriga Biosciences, Inc. Beta-substituted beta-amino acids and analogs as chemotherapeutic agents and uses thereof
DK3331525T3 (da) 2015-08-07 2020-12-14 Calcimedica Inc Anvendelse af CRAC-kanal-inhibitorer til behandling af slagtilfælde og traumatisk hjerneskade
ITUA20164199A1 (it) 2016-06-08 2017-12-08 Univ Degli Studi Del Piemonte Orientale Amedeo Avogadro Modulatori di soce compisizioni e relativi usi
LT3554490T (lt) 2016-12-16 2022-04-25 Idorsia Pharmaceuticals Ltd Farmacinis derinys, apimantis t tipo kalcio kanalo blokatorių
KR102608490B1 (ko) 2017-02-06 2023-11-30 이도르시아 파마슈티컬스 리미티드 1-아릴-1-트리플루오로메틸시클로프로판의 신규 합성 방법
DE102017010165A1 (de) 2017-11-02 2019-05-02 Friedrich-Schiller-Universität Jena Selbstheilende Polymere und deren Verwendung
BR112021004893A2 (pt) 2018-09-14 2021-06-01 Rhizen Pharmaceuticals A G composições compreendendo um inibidor de crac e um corticosteroide e métodos de uso dos mesmos
US12522589B2 (en) 2020-11-13 2026-01-13 Calcimedica, Inc. Synthesis of CRAC channel inhibitors
CN117098756A (zh) * 2021-02-25 2023-11-21 辰欣药业股份有限公司 一种环丙基取代的苯并呋喃类化合物的晶型及其制备方法

Family Cites Families (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
GB9127376D0 (en) 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
EP0633776B1 (en) 1992-04-02 2001-05-09 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
EP0689424B1 (en) 1993-03-17 1998-10-14 Minnesota Mining And Manufacturing Company Aerosol formulation containing an ester-, amide-, or mercaptoester-derived dispersing aid
DK0765308T3 (da) 1994-06-15 2000-09-11 Wellcome Found Enzyminhibitorer
MY117948A (en) 1997-01-13 2004-08-30 Glaxo Group Ltd Nitride oxide synthase inhibitors.
US6126919A (en) 1997-02-07 2000-10-03 3M Innovative Properties Company Biocompatible compounds for pharmaceutical drug delivery systems
DE19723722A1 (de) 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
JP4385414B2 (ja) * 1997-10-13 2009-12-16 アステラス製薬株式会社 アミド若しくはアミン誘導体
AU751139B2 (en) 1997-10-13 2002-08-08 Astellas Pharma Inc. Amide derivative
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
US6255303B1 (en) 1998-03-14 2001-07-03 Byk Gulden Lomberg Chemische Fabrik Gmbh Phthalazinone PDE III/IV inhibitors
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
EP1175422A2 (en) 1999-05-04 2002-01-30 Ligand Pharmaceuticals Incorporated Tetracyclic progesterone receptor modulator compounds and methods
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
CO5180649A1 (es) 1999-09-01 2002-07-30 Abbott Lab Antagonistas de los receptores de los glucocorticoides para el tratamiento de la diabetes para el tratamiento de la diabetes
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
ATE416184T1 (de) 2000-08-05 2008-12-15 Glaxo Group Ltd 17.beta.-carbothioat 17.alpha.- arylkarbonyloxyloxy androstanderivate als anti- phlogistische medikamente
BR0114323A (pt) 2000-09-29 2003-07-01 Glaxo Group Ltd Composto ou um seu sal ou solvato farmaceuticamente aceitável, composição farmacêutica, uso do composto ou de um seu sal ou solvato farmaceuticamente aceitável, método de tratamento ou profilaxia de doenças inflamatórias, e, processo para preparar o composto
GB0031179D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6484903B2 (en) 2001-01-09 2002-11-26 Riverwood International Corporation Carton with an improved dispensing feature in combination with a unique handle
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
ES2288543T3 (es) 2001-03-08 2008-01-16 Glaxo Group Limited Agonistas de beta-adrenorreceptores.
JP4143413B2 (ja) 2001-03-22 2008-09-03 グラクソ グループ リミテッド β２−アドレナリン受容体アゴニストとしてのホルムアニリド誘導体
WO2002088167A1 (en) 2001-04-30 2002-11-07 Glaxo Group Limited Anti-inflammatory 17.beta.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.alpha
EP1395604B1 (en) 2001-06-12 2008-06-25 Glaxo Group Limited Novel anti inflammatory 17.alpha.-heterocyclic-esters of 17.beta.-carbothioate androstane derivatives
PL393155A1 (pl) 2001-09-14 2011-03-28 Glaxo Group Limited Pochodne fenetanoloaminy do leczenia chorób układu oddechowego
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
DE60309829T2 (de) 2002-01-14 2007-09-13 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Glucocorticoidmimetika, verfahren zu ihrer herstellung, diese enthaltende pharmazeutische formulierungen und ihre verwendungen
US6831093B2 (en) 2002-01-22 2004-12-14 The Regents Of The University Of California Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
JP2005521717A (ja) 2002-03-26 2005-07-21 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用
KR101022977B1 (ko) 2002-03-26 2011-03-18 베링거 인겔하임 파마슈티칼즈, 인코포레이티드 글루코코르티코이드 모사체, 이의 제조방법, 약제학적조성물 및 이의 용도
DE10215316C1 (de) 2002-04-02 2003-12-18 Schering Ag Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer
US7282591B2 (en) 2002-04-11 2007-10-16 Merck & Co., Inc. 1h-benzo{f}indazol-5-yl derivatives as selective glucocorticoid receptor modulators
JP2005523920A (ja) 2002-04-25 2005-08-11 グラクソ　グループ　リミテッド フェネタノールアミン誘導体
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EP1521733B1 (en) 2002-07-08 2014-08-20 Pfizer Products Inc. Modulators of the glucocorticoid receptor
PL375442A1 (en) 2002-07-18 2005-11-28 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
AU2003259747A1 (en) 2002-08-21 2004-03-11 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
WO2004024728A2 (en) 2002-09-16 2004-03-25 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compounds, and their use as phosphodiesterase inhibitors
CA2499150A1 (en) 2002-09-20 2004-04-01 Merck & Co., Inc. Octahydro-2-h-naphtho[1,2-f] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
EP1554264B1 (en) 2002-10-22 2007-08-08 Glaxo Group Limited Medicinal arylethanolamine compounds
BR0315720A (pt) 2002-10-28 2005-09-06 Glaxo Group Ltd Composto, método para a profilaxia ou tratamento de uma condição clìnica em um mamìmefero, formulação farmacêutica, combinação, uso de um composto, processo para a preparação de um composto, e, intermediário
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
JP4641526B2 (ja) 2003-11-03 2011-03-02 グラクソ グループ リミテッド 流体分配デバイス
WO2006000398A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited 2,3-benzoxazin derivatives as non-steroidal glucocorticoid receptor modulators
WO2006000401A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited Substituted oxazines as glucocorticoid receptor modulators
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
ES2367515T3 (es) 2004-10-19 2011-11-04 F. Hoffmann-La Roche Ag Derivados de quinolina.
EA200801909A1 (ru) 2004-12-23 2009-06-30 Глэксо Груп Лимитед Соединения пиридина для лечения заболеваний, опосредованных действием простагландина
US20090124588A1 (en) 2005-01-10 2009-05-14 Glaxo Group Limited Androstane 17-Alpha-Carbonate for Use in the Treatment of Inflammatory and Allergic Conditions
ATE517908T1 (de) 2005-01-10 2011-08-15 Glaxo Group Ltd Androstan-17-alpha-carbonat-derivate zur verwendung bei der behandlung allergischer und entzündlicher zustände
US8802721B2 (en) * 2005-01-25 2014-08-12 Synta Pharmaceuticals Corp. Thiophene compounds for inflammation and immune-related uses
HU0500126D0 (en) 2005-01-26 2005-04-28 Sanofi Aventis New compounds and process for their preparation
US8093281B2 (en) 2005-04-14 2012-01-10 Glaxo Group Limited Indazoles as glucocorticoid receptor ligands
DE102005000046A1 (de) * 2005-04-28 2006-11-02 Voith Patent Gmbh Maschine zur Herstellung einer Faserstoffbahn
GB0513297D0 (en) 2005-06-29 2005-08-03 Glaxo Group Ltd Novel compounds
GB0522880D0 (en) 2005-11-09 2005-12-21 Glaxo Group Ltd Novel compounds
US8389567B2 (en) * 2007-12-12 2013-03-05 Calcimedica, Inc. Compounds that modulate intracellular calcium

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US20120053150A1 (en) 2012-03-01
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US20100273744A1 (en) 2010-10-28
US8399436B2 (en) 2013-03-19
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WO2010122089A1 (en) 2010-10-28

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