ES2613538T3 - Derivados de arilamida como bloqueadores de TTX-S - Google Patents

Derivados de arilamida como bloqueadores de TTX-S Download PDF

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ES2613538T3
ES2613538T3 ES11834032T ES11834032T ES2613538T3 ES 2613538 T3 ES2613538 T3 ES 2613538T3 ES 11834032 T ES11834032 T ES 11834032T ES 11834032 T ES11834032 T ES 11834032T ES 2613538 T3 ES2613538 T3 ES 2613538T3
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independently selected
alkyl
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Tatsuya Yamagishi
Kiyoshi Kawamura
Yoshimasa Arano
Mikio Morita
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Raqualia Pharma Inc
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Abstract

Un compuesto de la siguiente fórmula (II)**Fórmula** en la que R1 se selecciona independientemente entre el grupo que consiste en -CF3, -CHF2, -OCF3, - OCHF2, -OCH2CHF2, -OCH2CF3, -OCF2CHF2, -OCF2CF3, -OCH2CH2CF3, - OCH(CH3)CF3, -OCH2C(CH3)F2, -OCH2CF2CHF2, - OCH2CF2CF3, -OCH2CH2OCH2CF3, - NHCH2CF3, -SCF3, -SCH2CF3, -CH2CF3, 10 -CH2CH2CF3, -CH2OCH2CF3 y - OCH2CH2OCF3; R2 se selecciona independientemente entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) hidroxilo, (4) -On-alquilo C1-6, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (5) -On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (6) - On-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (7) -On-fenilo o -On-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (8) -On-grupo heterocíclico, donde el grupo heterocíclico está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (9) -(C>=O)-NR7R8, (10) -NR7R8, (11) -S(O)2-NR7R8, (12) -NR7- S(O)2R8, (13) -S(O)t-R7, donde t es 0, 1 o 2, (14) - NR7(C>=O)R8, (15) -CN y (16) -NO2; en la que n es 0 o 1, cuando n es 0, está presente un enlace químico en el lugar de -On-; p es 1, 2, 3 o 4; cuando p es dos o más de dos, R2 puede ser igual o diferente; R3 y R4 son independientemente hidrógeno o alquilo C1-6 que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo y -O-alquilo C1-6, ni R3 ni R4 son alquilo C1-6 al mismo tiempo. R5 se selecciona entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) hidroxilo, (4) -(C>=O)m-Ol-alquilo C1-6, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (5) -Ol-perfluoroalquilo (C1-3), (6) -(C>=O)m-Ol-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (7) -(C>=O)m-Ol-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (8) - (C>=O)m-Ol-fenilo o -(C>=O)m-Ol-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (9) -(C>=O)m-Ol-grupo heterocíclico, donde el grupo heterocíclico está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (10) -(C>=O)-NR7R8, (11) -NR7R8, (12) -S(O)2-NR7R8, (13) -S(O)t-R7, donde t es 0, 1 o 2, (14) -CO2H, (15) -CN y (16) -NO2; en la que I es 0 o 1 y m es 0 o 1; cuando I es 0 o m es 0, está presente un enlace químico en el lugar de -Ol- o -(C>=O)m- y cuando I es 0 y m es 0, está presente un enlace químico en el lugar de - (C>=O)m-Ol-; R6 se selecciona independientemente entre el grupo que consiste en: (1) hidrógeno, (2) hidroxilo, (3) halógeno, (4) -alquilo C1-6, (5) -cicloalquilo C3-6, (6) - O-alquilo C1-6, (7) - O(C>=O)-alquilo C1-6, (8) -NH-alquilo C1-6, (9) fenilo, (10) grupo heterocíclico y (11) -CN; R7 y R8 son independientemente hidrógeno, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-7 o arilo, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, alquilo C1-6 y -O-alquilo C1-6; o R7 forman un anillo de 4 a 7 miembros con R8 que puede contener un átomo de nitrógeno, un átomo de oxígeno, un átomo de azufre o un doble enlace, en la que el anillo de 4 a 7 miembros está opcionalmente sustituido con 1 a 6 sustituyentes seleccionados independientemente entre el grupo que consiste en: (1) hidrógeno, (2) hidroxilo, (3) halógeno, (4) alquilo C1-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (5) cicloalquilo C3-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (6) -O-alquilo C1-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, y (7) -Ocicloalquilo C3-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6; X es un átomo de nitrógeno o un átomo de carbono; Z es un átomo de nitrógeno o un átomo de carbono; Y es hidrógeno o alquilo C1-6; R9 se selecciona independientemente entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) -On-alquilo C1-6, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (4) - On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5 y (5) -Onalquenilo C2-4, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5; en la que n es 0 o 1, cuando n es 0, está presente un enlace químico en el lugar de -On-; q es 1, 2 o 3; cuando q es dos o más de dos, R9 puede ser igual o diferente; R10 es independientemente hidrógeno, alquilo C1-6, alquenilo C2-6 o cicloalquilo C3-7, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, alquilo C1-6, -O-alquilo C1-6, -cicloalquilo C3-7 y -O-cicloalquilo C3-7; o una sal farmacéuticamente aceptable del mismo.
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Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2613538T3 (es) * 2010-10-18 2017-05-24 Raqualia Pharma Inc Derivados de arilamida como bloqueadores de TTX-S
CN103796997A (zh) * 2011-09-12 2014-05-14 霍夫曼-拉罗奇有限公司 5-环烷基-或5-杂环基-烟酰胺
RU2646754C2 (ru) 2012-04-25 2018-03-07 Раквалиа Фарма Инк. Производные пирролопиридинона в качестве ttx-s блокаторов
BR112014026399B1 (pt) * 2012-04-25 2022-11-01 Raqualia Pharma Inc Composto de fórmula (ii), composição farmacêutica, uso e processo para preparar uma composição farmacêutica
US9944634B2 (en) * 2012-10-31 2018-04-17 Raqualia Pharma Inc. Pyrazolopyridine derivatives as TTX-S blockers
WO2015119998A1 (en) * 2014-02-06 2015-08-13 Abbvie, Inc. 6-heteroaryloxy- and 6-aryloxy-quinoline-2-carboxamides and uses thereof
WO2017062804A1 (en) 2015-10-07 2017-04-13 The Arizona Board Of Regents On Behalf Of The University Of Arizona Crmp2 sumoylation inhibitors and uses thereof
TW202246215A (zh) 2015-12-18 2022-12-01 美商亞德利克斯公司 作為非全身ｔｇｒ５促效劑之經取代之４－苯基吡啶化合物
KR20180094923A (ko) * 2015-12-24 2018-08-24 교와 핫꼬 기린 가부시키가이샤 α, β 불포화 아미드 화합물
CN106083813A (zh) * 2016-06-13 2016-11-09 太原理工大学 一种三唑‑喹啉类化合物的合成方法
WO2018110669A1 (en) 2016-12-15 2018-06-21 Ono Pharmaceutical Co., Ltd. Activator of trek (twik related k+ channels) channels
US20200039930A1 (en) 2017-03-21 2020-02-06 AbbVie Deutschland GmbH & Co. KG Proline amide compounds and their azetidine analogues carrying a specifically substituted benzyl radical
WO2018235851A1 (en) * 2017-06-20 2018-12-27 Raqualia Pharma Inc. AMIDE DERIVATIVES AS NAV1.7 AND NAV1.8 BLOCKERS
WO2019045035A1 (en) * 2017-08-31 2019-03-07 Raqualia Pharma Inc. BIARYLOXY DERIVATIVES AS TTX-S BLOCKERS
IL310857A (en) 2018-04-25 2024-04-01 Bayer Ag Heteroaryl-triazole and heteroaryl-tetrazole compounds as pesticides
RU2761824C2 (ru) * 2018-08-03 2021-12-13 Закрытое Акционерное Общество "Биокад" Ингибиторы CDK8/19
SG11202104326TA (en) * 2018-11-02 2021-05-28 Merck Sharp & Dohme 2-amino-n-heteroaryl-nicotinamides as nav1.8 inhibitors
US20220185815A1 (en) 2019-03-06 2022-06-16 Daiichi Sankyo Company, Limited Pyrrolopyrazole derivative
AR119009A1 (es) * 2019-05-29 2021-11-17 Syngenta Crop Protection Ag Derivados de alcoxipiridina y alcoxipirimidina microbicidas
GB201908453D0 (en) * 2019-06-12 2019-07-24 Enterprise Therapeutics Ltd Compounds for treating respiratory disease
IL293592A (en) * 2019-12-06 2022-08-01 Vertex Pharma Transduced tetrahydrofurans as sodium channel modulators
KR20240024935A (ko) 2021-06-18 2024-02-26 알리고스 테라퓨틱스 인코포레이티드 Pd-l1을 표적화하기 위한 방법 및 조성물
WO2024059207A2 (en) * 2022-09-15 2024-03-21 Vanderbilt University Pyrazoloether analogs as mglu5 negative allosteric modulators and methods of making and using the same

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0725853A (ja) 1993-07-14 1995-01-27 Ishihara Sangyo Kaisha Ltd アミド系化合物又はその塩、それらの製造方法及びそれらを含有する有害動物防除剤
GB9919588D0 (en) * 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
RU2003110962A (ru) 2000-09-18 2004-10-20 Е.И.Дюпон де Немур энд Компани (US) Пиридиниламиды и имиды для использования в качестве фунгицидов
CN1688546A (zh) * 2000-09-18 2005-10-26 纳幕尔杜邦公司 用作杀真菌剂的吡啶酰胺类和吡啶酰亚胺类
DE60235114D1 (de) * 2001-11-01 2010-03-04 Icagen Inc Pyrazolamide zur anwendung in der behandlung von schmerz
TW200306159A (en) 2002-03-19 2003-11-16 Du Pont Bicyclic fused pyridinyl amides and advantageous compositions thereof for use as fungicides
TW200407075A (en) 2002-03-19 2004-05-16 Du Pont Pyridinyl amides and advantageous compositions thereof for use as fungicides
TW200306782A (en) * 2002-03-19 2003-12-01 Du Pont Pyridinyl amides and advantageous compositions thereof for use as fungicides
JP4706482B2 (ja) * 2004-01-13 2011-06-22 株式会社クレハ ２，６−ジクロロイソニコチン酸ピリジルメチル誘導体、その製造方法および農園芸用病害防除剤
GT200500013A (es) 2004-01-23 2005-08-10 Amidas herbicidas
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
US7507748B2 (en) * 2004-07-22 2009-03-24 Amgen Inc. Substituted aryl-amine derivatives and methods of use
US20070155738A1 (en) * 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
JP2007186435A (ja) 2006-01-12 2007-07-26 Astellas Pharma Inc ニコチンアミド誘導体
EP1995241B1 (en) 2007-03-23 2010-03-17 ICAgen, Inc. Inhibitors of ion channels
AU2008247102B2 (en) * 2007-05-03 2011-11-24 Pfizer Limited 2 -pyridine carboxamide derivatives as sodium channel modulators
CA2703915C (en) * 2007-10-31 2015-02-24 Merck Sharp & Dohme Corp. P2x3 receptor antagonists for treatment of pain
CN102036981B (zh) * 2008-03-18 2015-04-08 默沙东公司 取代的4-羟基嘧啶-5-甲酰胺
TW201000446A (en) 2008-05-30 2010-01-01 Astrazeneca Ab New compounds useful in pain therapy
WO2009156484A2 (en) 2008-06-27 2009-12-30 Novartis Ag Organic compounds
WO2010035166A1 (en) * 2008-09-23 2010-04-01 Pfizer Limited Benzamide derivatives
JP5592388B2 (ja) 2008-10-31 2014-09-17 メルク・シャープ・アンド・ドーム・コーポレーション 疼痛治療用のｐ２ｘ３受容体アンタゴニスト技術分野
EP2435407B1 (en) * 2009-05-29 2019-12-25 RaQualia Pharma Inc. Aryl substituted carboxamide derivatives as calcium or sodium channel blockers
US8809380B2 (en) * 2009-08-04 2014-08-19 Raqualia Pharma Inc. Picolinamide derivatives as TTX-S blockers
ES2613538T3 (es) * 2010-10-18 2017-05-24 Raqualia Pharma Inc Derivados de arilamida como bloqueadores de TTX-S

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