AR039778A1 - Moduladores alostericos positivos del receptor nicotinico de la acetilcolina - Google Patents

Moduladores alostericos positivos del receptor nicotinico de la acetilcolina

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AR039778A1
AR039778A1 ARP030101491A ARP030101491A AR039778A1 AR 039778 A1 AR039778 A1 AR 039778A1 AR P030101491 A ARP030101491 A AR P030101491A AR P030101491 A ARP030101491 A AR P030101491A AR 039778 A1 AR039778 A1 AR 039778A1
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Argentina
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substituted
heterocycloalkyl
alkyl
alkynyl
alkenyl
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Upjohn Co
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Abstract

Reivindicación 1: Un compuesto de fórmula (1) en donde X es O ó S; A es un resto de fórmula (2), donde cada WA-1, WA-2, WA-3,WA-4 y WA-5 es independientemente N o CRA, siempre y cuando no más de cuatro de los grupos, WA-1, WA-2, WA-3, WA-4 o WA-5 sean simultáneamente N; cada RA es independientemente H, halógeno, alquilo, haloalquilo, alquilo sustituido, alquenilo, haloalquenilo, alquenilo sustituido, alquinilo, haloalquinilo, alquinilo sustituido, heterocicloalquilo, haloheterocicloalquilo, heterocicloalquilo sustituido, cicloalquilo, halocicloalquilo, cicloalquilo sustituido, arilo, -N3, -SCN-, -CN, -NO2, -OR7, -SR8, -S(O)R8, -S(O)2R8, -N(R9)2, -C(O)R10, -C(O)OR7, -C(O)N(R9)2, -NR9C(O)R10, -C(R10)=NOR7, S(O)2N(R9)2, -NR9S(O)2R8, -N(R9)C(O)N(R9)2, siempre y cuando al menos un RA sea distinto de H, o cuando dos grupos RA se hallan en átomos de C adyacentes, los dos RA pueden combinarse para formar un anillo de 5 a 8 miembros fusionado al anillo de 6 miembros, en donde el anillo de 5 a 8 miembros es saturado o insaturado y contiene hasta 2 heteroátomos seleccionados entre -O-, -S-, -N(RA-2)-o -N= y además está sustituido, donde la valencia lo permita, en el anillo de 5 a 8 miembros con un máximo de 2 sustituyentes seleccionados independientemente del grupo RA-1; cada RA-1 es independientemente H, F, Cl, Br, I, alquilo, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, haloalquilo, haloalquenilo, haloalquinilo, halocicloalquilo, haloheterocicloalquilo, alquilo sustituido, alquenilo sustituido, alquinilo sustituido, cicloalquilo sustituido, heterocicloalquilo sustituido, -CN, -NO2, -OR7, -SR8, -S(O)2R8, -S(O)R8, -OS(O)2R8, -N(R9)2, -C(O)R10, -C(S)R10, -C(O)2R7, -C(O)N(R9)2, -NR9C(O)R10, -S(O)2N(R9)2, -NR9S(O)2R8, -N(R9)C(O)N(R9)2 o arilo; RA-2 es H, alquilo, haloalquilo, alquilo sustituido, alquenilo, haloalquenilo, alquenilo sustituido, alquinilo, haloalquinilo, alquinilo sustituido, cicloalquilo, halocicloalquilo, cicloalquilo sustituido, heterocicloalquilo, haloheterocicloalquilo, heterocicloalquilo sustituido o arilo; B es un anillo aromático de 5 o 6 miembros que contiene hasta 4 heteroátomos seleccionados entre O, -N(RB-3)-, =N-, o -S-, en donde B es un resto seleccionado del grupo de fórmulas (3), en donde B1 es N o C; B2, B3, B4 y B5 son independientemente N, O, S, C, siempre que, cuando la valencia lo permita, el N pueda tener un tercer enlace a RB-3 y el C pueda tener un cuarto enlace a RB-1; cada RB-1 es independientemente H, halógeno, alquilo, haloalquilo, alquilo sustituido, cicloalquilo, halocicloalquilo, cicloalquilo sustituido, alquenilo, haloalquenilo, alquenilo sustituido, alquinilo, haloalquinilo, alquinilo sustituido, heterocicloalquilo, haloheterocicloalquilo, heterocicloalquilo sustituido, arilo, -CN, -N3, -NO2, -COR10, -CO2R7, -CON(R9)2, -C(R10)=NOR7, -SCN, -OR7, -N(R9)2, -SR8, -SOR8, -SO2R8, -SN(R9)2, -SON(R9)2, -SO2N(R9)2; cuando dos grupos RB-1 se hallan en átomos de C adyacentes, los dos RB-1 pueden combinarse para formar un anillo de 5 a 7 miembros fusionado al anillo de 5 o 6 miembros, para formar un sistema de anillo bicíclico fusionado, en donde el anillo de 5 a 7 miembros es saturado o insaturado y contiene hasta 2 heteroátomos seleccionados entre -O-, -S-, -N(RB-3)-, o -N= y además está sustituido, conforme a la valencia, en el anillo de 5 a 7 miembros con un máximo de 2 sustituyentes seleccionados independientemente del grupo RB-2; cada RB-2 es independientemente H, F, Cl, Br, I, alquilo, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, haloalquilo, haloalquenilo, haloalquinilo, halocicloalquilo, haloheterocicloalquilo, alquilo sustituido, alquenilo sustituido, alquinilo sustituido, cicloalquilo sustituido, heterocicloalquilo sustituido, -CN, -NO2, -OR7, -SR8, -S(O)2R8, -S(O)R8, -OS(O)2R8, -N(R9)2, -C(O)R10, -C(S)R10, -C(O)2R7, -C(O)N(R9)2, -NR9C(O)R10, -S(O)2N(R9)2, -NR9S(O)2R8, -N(R9)C(O)N(R9)2 o arilo; RB-3 es H, alquilo, haloalquilo, alquilo sustituido, alquenilo, haloalquenilo, alquenilo sustituido, alquinilo, haloalquinilo, alquinilo sustituido, cicloalquilo, halocicloalquilo, cicloalquilo sustituido, heterocicloalquilo, haloheterocicloalquilo, heterocicloalquilo sustituido o arilo; cada WB-1, WB-2, WB-3, WB-4 y WB-5 es independientemente N o CRB-1, a condición de que no más de 4 de los grupos WB-1, WB-2, WB-3, WB-4 y WB-5 sean simultáneamente N; R7 es H, alquilo, haloalquilo, alquilo sustituido, alquenilo, haloalquenilo, alquenilo sustituido, alquinilo, haloalquinilo, alquinilo sustituido, cicloalquilo, halocicloalquilo, cicloalquilo sustituido, heterocicloalquilo, haloheterocicloalquilo, heterocicloalquilo sustituido o arilo; R8 es H, alquilo, haloalquilo, alquilo sustituido, alquenilo, haloalquenilo, alquenilo sustituido, alquinilo, haloalquinilo, alquinilo sustituido, cicloalquilo, halocicloalquilo, cicloalquilo sustituido, heterocicloalquilo, haloheterocicloalquilo, heterocicloalquilo sustituido o arilo; cada R9 es independientemente H, alquilo, haloalquilo, alquilo sustituido, alquenilo, haloalquenilo, alquenilo sustituido, alquinilo, haloalquinilo, alquinilo sustituido, cicloalquilo, halocicloalquilo, cicloalquilo sustituido, heterocicloalquilo, haloheterocicloalquilo, heterocicloalquilo sustituido o arilo; R10 es H, alquilo, haloalquilo, alquilo sustituido, alquenilo, haloalquenilo, alquenilo sustituido, alquinilo, haloalquinilo, alquinilo sustituido, cicloalquilo, halocicloalquilo, cicloalquilo sustituido, heterocicloalquilo, haloheterocicloalquilo, heterocicloalquilo sustituido o arilo; o una de sus composiciones farmacéuticas, sales farmacéuticamente aceptables, mezclas racémicas o enantiómeros puros; siempre que cuando B sea tiadiazolilo y A sea fenilo, al menos un RA se seleccione entre grupos diferentes de H, metilo, isopropilo, -NO2, -CF3, metoxi, -OH, -CN o halógeno; y con la condición adicional de que cuando B sea isoxasol-3-ilo sustituido opcionalmente en la posición 4 con trifluorometilo, O-alquilo C1-4, o alquilo sustituido con hidroxi, y A sea fenilo, el fenilo no esté sustituido con alquilo, trifluorometilo o halo en ninguna de las posiciones orto.
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Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050130990A1 (en) * 2001-03-23 2005-06-16 Universite Laval Nicotinic receptor agonists for the treatment of inflammatory diseases
CA2341952A1 (en) 2001-03-23 2002-09-23 Universite Laval Nicotinic receptor agonists for the treatment of inflammatory pulmonary diseases
DE10164139A1 (de) 2001-12-27 2003-07-10 Bayer Ag 2-Heteroarylcarbonsäureamide
US8039459B2 (en) 2004-07-15 2011-10-18 Universite Laval Nicotinic receptor agonists for the treatment of inflammatory diseases
US8557804B2 (en) 2002-03-25 2013-10-15 Universite Laval Nicotinic receptor agonists for the treatment of inflammatory diseases
US20030236287A1 (en) * 2002-05-03 2003-12-25 Piotrowski David W. Positive allosteric modulators of the nicotinic acetylcholine receptor
SI1557411T1 (es) * 2002-07-12 2013-01-31 Astellas Pharma Inc
EA200500783A1 (ru) * 2002-12-11 2005-12-29 ФАРМАЦИЯ ЭНД АПДЖОН КОМПАНИ ЭлЭлСи Комбинация для лечения синдрома дефицита внимания с гиперактивностью
EP1572205A2 (en) * 2002-12-11 2005-09-14 Pharmacia & Upjohn Company LLC Treatment of diseases with combinations of alpha 7 nicotinic acetylcholine receptor agonists and other compounds
JP4613157B2 (ja) 2003-01-14 2011-01-12 サイトキネティクス・インコーポレーテッド 化合物、組成物および方法
US7767670B2 (en) * 2003-11-13 2010-08-03 Ambit Biosciences Corporation Substituted 3-carboxamido isoxazoles as kinase modulators
EP3002283B1 (en) * 2003-12-26 2017-06-14 Kyowa Hakko Kirin Co., Ltd. Thiazole derivatives
DE102004009933A1 (de) * 2004-02-26 2005-09-15 Merck Patent Gmbh Verwendung von Thiadiazolharnstoffderivaten
CA2561639A1 (en) 2004-03-29 2005-10-06 Neurosearch A/S Novel urea derivatives and their medical use
PL1765327T3 (pl) 2004-06-17 2015-01-30 Cytokinetics Inc Związki, kompozycje i sposoby
WO2006012308A1 (en) * 2004-06-25 2006-02-02 Icos Corporation Bisarylurea derivatives useful for inhibiting chk1
US7176222B2 (en) 2004-07-27 2007-02-13 Cytokinetics, Inc. Syntheses of ureas
US20060142349A1 (en) * 2004-12-23 2006-06-29 Pfizer Inc Methods of modulating the activities of alpha-7 nicotinic acetylcholine receptor
US7538223B2 (en) 2005-08-04 2009-05-26 Cytokinetics, Inc. Compounds, compositions and methods
WO2007070683A2 (en) * 2005-12-15 2007-06-21 Cytokinetics, Inc. Certain chemical entities, compositions and methods
US20070208000A1 (en) * 2005-12-15 2007-09-06 Morgan Bradley P Certain chemical entities, compositions and methods
US7825120B2 (en) * 2005-12-15 2010-11-02 Cytokinetics, Inc. Certain substituted ((piperazin-1-ylmethyl)benzyl)ureas
EP1959947A2 (en) * 2005-12-15 2008-08-27 Cytokinetics, Inc. Certain chemical entities, compositions and methods
EP1959962A2 (en) 2005-12-16 2008-08-27 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
US7989455B2 (en) * 2005-12-19 2011-08-02 Cytokinetics, Inc. Compounds, compositions and methods
KR20110007258A (ko) 2006-03-22 2011-01-21 에프. 호프만-라 로슈 아게 11-베타-ｈｓｄ-1로서의 피라졸
WO2008028903A2 (en) * 2006-09-04 2008-03-13 Neurosearch A/S Pharmaceutical combinations of a nicotine receptor modulator and a cognitive enhancer
GB0713686D0 (en) * 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
US20090239901A1 (en) * 2008-03-19 2009-09-24 Merouane Bencherif Method and compositions for treatment of cerebral malaria
WO2009152356A2 (en) * 2008-06-11 2009-12-17 Irm Llc Compounds and compositions useful for the treatment of malaria
TR201807944T4 (tr) 2008-11-19 2018-06-21 Forum Pharmaceuticals Inc (R)-7-kloro-N-(kinüklidin-3-il)benzo[b]tiyofen-2-karboksamit ve bunun farmasötik olarak kabul edilebilir tuzları ile şizofreninin negatif belirtilerinin tedavisi.
JP5808319B2 (ja) * 2009-05-11 2015-11-10 フォルム ファーマシューティカルズ、インコーポレイテッド アセチルコリンエステラーゼ阻害剤と組み合わせた特定のα７ニコチン酸受容体を用いた認知障害の治療
WO2010130063A1 (zh) * 2009-05-12 2010-11-18 Han Mei 具有促进干細胞增殖作用的小分子化合物及其用途
ES2746850T3 (es) 2010-05-17 2020-03-09 Forum Pharmaceuticals Inc Formulaciones farmacéuticas que comprenden formas cristalinas de clorhidrato de (R)-7-cloro-N-(quinuclidin-3-il)benzo(b)tiofeno-2-carboxamida monohidratado
US9296722B2 (en) 2010-05-27 2016-03-29 Ambit Biosciences Corporation Azolyl urea compounds and methods of use thereof
WO2012029994A1 (en) 2010-09-02 2012-03-08 Kyoto University Pharmaceutical composition for prevention and treatment of amyotrophic lateral sclerosis
JP2014114212A (ja) * 2011-03-29 2014-06-26 Dainippon Sumitomo Pharma Co Ltd 新規ベンズイミダゾール誘導体
JP2014166961A (ja) * 2011-06-20 2014-09-11 Dainippon Sumitomo Pharma Co Ltd 新規インダゾール誘導体
AU2012276651A1 (en) 2011-06-30 2014-02-06 Toray Industries, Inc. Antipruritic agent
KR20150000900A (ko) 2012-04-10 2015-01-05 다이닛본 스미토모 세이야꾸 가부시끼가이샤 신규한 1-치환된 인다졸 유도체
MX365776B (es) * 2012-04-20 2019-06-12 Kumiai Chemical Industry Co Derivado de sulfuro de alquil fenilo y agente de control de plagas.
MX358512B (es) 2012-05-08 2018-08-24 Forum Pharmaceuticals Inc Uso de (r)-7cloro-n-(quinuclidin-3-il) benzo[b] tiofeno-2-carboxamida o una sal farmacéuticamente aceptable de la misma para preparar una composición farmacéutica en el tratamiento de una disfunción cognitiva.
CN102875427B (zh) * 2012-09-18 2014-02-19 安徽世华化工有限公司 一种2-甲氧基甲磺酸甲酯的合成方法
WO2014054635A1 (ja) 2012-10-02 2014-04-10 大日本住友製薬株式会社 イミダゾール誘導体
GB201401886D0 (en) 2014-02-04 2014-03-19 Lytix Biopharma As Neurodegenerative therapies
MD20160105A2 (ro) 2014-04-10 2017-03-31 Pfizer Inc. 2-Amino-6-metil-4,4a,5,6-tetrahidropirano[3,4-d][1,3]tiazin-8a(8H)-il-1,3-tiazol-4-il amide
WO2015199208A1 (ja) * 2014-06-27 2015-12-30 味の素株式会社 甘味受容体アンタゴニスト
US10899702B2 (en) 2015-02-07 2021-01-26 University of Pittsburgh—of the Commonwealth System of Higher Education HTRPVI chemical agents
GB201514021D0 (en) 2015-08-07 2015-09-23 Arner Elias Set Jeno Novel Pyridines and their use in the treatment of cancer
US10653681B2 (en) 2016-03-16 2020-05-19 Recurium Ip Holdings, Llc Analgesic compounds
CA3051539A1 (en) 2017-02-07 2018-08-16 Oblique Therapeutics Ab Hydrocarbylsulfonyl-substituted pyridines and their use in the treatment of cancer
MX2019009354A (es) 2017-02-07 2019-09-19 Oblique Therapeutics Ab Piridinas sustituidas con heterociclilsulfonilo y su uso en el tratamiento del cancer.
US11208384B2 (en) 2017-02-07 2021-12-28 Oblique Therapeutics Ab Sulfinylpyridines and their use in the treatment of cancer
AU2018218519B2 (en) 2017-02-07 2021-08-05 Oblique Therapeutics Ab Heteroarylsulfonyl-substituted pyridines and their use in the treatment of cancer
LT3837256T (lt) 2018-08-17 2023-06-12 Novartis Ag Karbamido junginiai ir kompozicijos kaip smarca2 / brm atfazės inhibitoriai

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US165398A (en) * 1875-07-06 Improvement in processes for cleansing gas-retorts
US2199A (en) * 1841-07-29 Improvement in the manufacture of buttons
JPS5031039A (es) * 1973-07-27 1975-03-27
US4062861A (en) * 1973-07-27 1977-12-13 Shionogi & Co., Ltd. 3-Isoxazolylurea derivatives
US3990879A (en) * 1974-12-26 1976-11-09 Eli Lilly And Company Method of controlling aquatic weeds
FR2639636B1 (fr) * 1988-11-30 1994-03-04 Novapharme Nouveaux composes heterocycliques a activite anticonvulsivante, procede de preparation et compositions therapeutiques les contenant
US5185358A (en) * 1991-06-24 1993-02-09 Warner-Lambert Co. 3-heteroatom containing urea and thiourea ACAT inhibitors
US5162360A (en) * 1991-06-24 1992-11-10 Warner-Lambert Company 2-heteroatom containing urea and thiourea ACAT inhibitors
DK41193D0 (da) * 1993-04-07 1993-04-07 Neurosearch As Ionkanalaabnere
EP0809492A4 (en) * 1995-02-17 2007-01-24 Smithkline Beecham Corp IL-8 RECEPTOR ANTAGONISTS
US5814646A (en) * 1995-03-02 1998-09-29 Eli Lilly And Company Inhibitors of amyloid beta-protein production
US5773459A (en) * 1995-06-07 1998-06-30 Sugen, Inc. Urea- and thiourea-type compounds
EP0795328A1 (en) * 1996-03-15 1997-09-17 Pfizer Inc. Use of naphthalene derivatives in treating lung carcinoma
US6262113B1 (en) * 1996-03-20 2001-07-17 Smithkline Beecham Corporation IL-8 receptor antagonists
EP0906273B1 (en) * 1996-05-24 2002-10-16 Neurosearch A/S Phenyl derivatives containing an acidic group, their preparation and their use as chloride channel blockers
SE9603738D0 (sv) * 1996-10-14 1996-10-14 Abb Research Ltd A method for producing a bipolar semiconductor device and a bipolar semiconductor device
US6093742A (en) * 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
US6455566B1 (en) * 1997-09-03 2002-09-24 Wyeth Substituted 1-aryl-3-heteroaryl-thioureas (or isothioureas) as antiatherosclerotic agents
US6262044B1 (en) * 1998-03-12 2001-07-17 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (PTPASES)
US6277870B1 (en) * 1998-05-04 2001-08-21 Astra Ab Use
GB9823873D0 (en) * 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
WO2000035455A1 (en) * 1998-12-15 2000-06-22 Telik, Inc. Heteroaryl-aryl ureas as igf-1 receptor antagonists
UA73492C2 (en) * 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
DE60014603T2 (de) * 1999-03-12 2006-02-16 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Heterocyklischer harnstoff und verwandte verbindungen als entzündungshemmende mittel
UA73543C2 (uk) * 1999-12-07 2005-08-15 Тераванс, Інк. Похідні сечовини, фармацевтична композиція та застосування похідного при приготуванні лікарського засобу для лікування захворювання, яке опосередковується мускариновим рецептором
PL365124A1 (en) * 2000-02-28 2004-12-27 Bayer Aktiengesellschaft Medicament for viral diseases
AR030273A1 (es) * 2000-03-10 2003-08-20 Smithkline Beecham Corp Compuestos de hidroxifenil urea sustituidos con sulfonamidas, composiciones farmaceuticas que los comprenden, y uso de los mismos en la fabricacion de medicamentos para tratar una enfermedad mediada por una quimioquina
US6372795B1 (en) * 2000-06-30 2002-04-16 Unilever Home And Personal Care Usa, A Division Of Conopco, Inc. Cosmetic compositions containing substituted amide derivatives
US6645990B2 (en) * 2000-08-15 2003-11-11 Amgen Inc. Thiazolyl urea compounds and methods of uses
US20020173507A1 (en) * 2000-08-15 2002-11-21 Vincent Santora Urea compounds and methods of uses
US6492385B2 (en) * 2000-08-18 2002-12-10 Pharmacia & Upjohn Company Quinuclidine-substituted heteroaryl moieties for treatment of disease
AU2001282874A1 (en) * 2000-08-18 2002-03-04 Pharmacia And Upjohn Company Quinuclidine-substituted aryl moieties for treatment of disease (nicotinic acetylcholine receptor ligands)
GB0021885D0 (en) * 2000-09-06 2000-10-18 Fujisawa Pharmaceutical Co New use
EP1256578B1 (en) * 2001-05-11 2006-01-11 Pfizer Products Inc. Thiazole derivatives and their use as cdk inhibitors
US20030236287A1 (en) * 2002-05-03 2003-12-25 Piotrowski David W. Positive allosteric modulators of the nicotinic acetylcholine receptor

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