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CO5261559A1 - Antagonistas de neurokinina selectivos - Google Patents

Antagonistas de neurokinina selectivos

Info

Publication number
CO5261559A1
CO5261559A1 CO00095391A CO00095391A CO5261559A1 CO 5261559 A1 CO5261559 A1 CO 5261559A1 CO 00095391 A CO00095391 A CO 00095391A CO 00095391 A CO00095391 A CO 00095391A CO 5261559 A1 CO5261559 A1 CO 5261559A1
Authority
CO
Colombia
Prior art keywords
alkyl
mfi
jpeg
cycloalkyl
heteroaryl
Prior art date
Application number
CO00095391A
Other languages
English (en)
Inventor
Neng-Yang Shin
Shue Ho-Jane
Gregory Adam Reichard
Paliwal Sunil
David J Blythin
John J Piwinski
Xiao Dong
Chen Xiao
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of CO5261559A1 publication Critical patent/CO5261559A1/es

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    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/10—Oxygen or sulfur atoms
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Abstract

Se describe un compuesto representado por la fórmula estructural <EMI FILE="00095391_1" ID="1" IMF=JPEG >o su sal farmacéuticamente aceptable, en donde Ar1 y Ar2 son heteroarilo optativamente sustituido o fenilo optativamente sustituido; X1 es O-, -S-, -SO-, -SO2-, -NR12-, NCOR12 -o- NR12SO2R15-; <EMI FILE="00095391_2" ID="2" IMF=JPEG >Se seleccionan entre el grupo que consiste en <EMI FILE="00095391_3" ID="3" IMF=JPEG > X2 es -O -, -S -o -NR5-; Y es =O, =S o =NR11; Y1 es H, alquilo C1-C6, -NR17R13, -SCH3, R19-aril(CH2)n6-, R19-heteroaril-(CH2)n6-, -(CH2)n6- heterocicloalquil, -(C1-C3)alquil-NH-C(O)O(C1-C6)alquilo o -NHC(O)R15; R5 es H o -(CH2)n1-G, en donde n1 es 0-5, G es H, -CF3, -CHF2, -CH2F, OH, -O-(alquilo C1-C6), -SO2R13, -O-(cicloalquilo C3-C8), -NR13R14, -SO2NR13R14, -NR13SO2R15, -NR13COR12, -NR12(CONR13R14), -CONR13R14, -COOR12, cicloalquilo C3-C8, R19-arilo, R19-heteroarilo, y siempre y cuando n1 = 0, G no es H; R1, R2, R3 y R7 son H, alquilo, cicloalquilo, -CHF2, -CH2F o -CF3; o R1 y R2, junto con el carbono al cual están unidos, forman un anillo alquileno; o R1 y R2 juntos son =O; R6 es R7 o -OH; y las variables restantes son como se definieron en la memoria descriptiva, también se describen métodos para el tratamiento de enfermedades susceptibles de tratamiento con antagonistas de neurokinina con dichos compuestos, y composiciones farmacéuticas que comprenden a dichos compuestos. También se describen composiciones farmacéuticas que comprenden una cantidad efectiva de un compuesto de acuerdo con la reivindicación 1, por lo menos un portador farmacéuticamente aceptable, y en combinación con una cantidad efectiva de un inhibidor de la recaptación de serotonina selectivo.
CO00095391A 1999-12-17 2000-12-14 Antagonistas de neurokinina selectivos CO5261559A1 (es)

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Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2291538T3 (es) * 2001-11-13 2008-03-01 Schering Corporation Antagonistas de nk1.
PE20030762A1 (es) * 2001-12-18 2003-09-05 Schering Corp Compuestos heterociclicos como antagonistas nk1
DK1501808T3 (da) 2002-04-26 2008-10-13 Lilly Co Eli Tachykininreceptor-antagonister
PT1501809E (pt) * 2002-04-26 2008-03-18 Lilly Co Eli Derivados de triazole como antagonistas de receptores de taquiquinina
US7041682B2 (en) * 2002-07-03 2006-05-09 Schering Corporation NK1 antagonists
GB0308968D0 (en) * 2003-04-17 2003-05-28 Glaxo Group Ltd Medicaments
US7592348B2 (en) * 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
FR2873373B1 (fr) * 2004-07-23 2006-09-08 Sanofi Synthelabo Derives de 4-arylmorpholin-3-one, leur preparation et leur application en therapeutique
WO2008090114A1 (en) 2007-01-24 2008-07-31 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-)
US8835426B2 (en) 2007-02-26 2014-09-16 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11β-hydroxysteroid dehydrogenase 1
AR066191A1 (es) 2007-03-22 2009-08-05 Schering Corp Proceso e intermediarios para la sintesis de compuestos 8- [ ( 1- (3,5- bis- ( trifluorometil) fenil) - etoxi ) - metil]- 8 fenil - 1,7- diaza - espiro (4, 5) decan -2 ona
CL2008002199A1 (es) 2007-07-26 2009-10-23 Vitae Pharmaceuticals Inc Compuestos derivados de 1,3-oxazin-2-ona; composicion farmaceutica que comprende a dichos compuestos; y uso para tratar una enfermedad asociada con la actividad de la 11beta-hidroxiesteroide deshidrogenasa tipo 1 (11beta-hsd1) tales como dislipidemia, hiperlipidemia, hipertension, obesidad y enfermedad cardiovascular, entre otras.
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
CA2708303A1 (en) 2007-12-11 2009-06-18 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
TW200934490A (en) 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
US8592409B2 (en) 2008-01-24 2013-11-26 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11β-hydroxysteroid dehydrogenase 1
EP2252598A2 (en) 2008-02-11 2010-11-24 Vitae Pharmaceuticals, Inc. 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2715290A1 (en) 2008-02-15 2009-08-20 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
TW200946520A (en) 2008-05-01 2009-11-16 Vitae Pharmaceuticals Inc Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5538365B2 (ja) 2008-05-01 2014-07-02 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
US8242111B2 (en) 2008-05-01 2012-08-14 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1
EP2291371B1 (en) 2008-05-01 2015-06-10 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CN104327062A (zh) 2008-07-25 2015-02-04 贝林格尔·英格海姆国际有限公司 11β-羟基类固醇脱氢酶1的环状抑制剂
EP2324017B1 (en) 2008-07-25 2014-12-31 Boehringer Ingelheim International GmbH INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1
CA2729993A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
CN104496988B (zh) 2008-09-05 2017-04-12 欧科生医股份有限公司 用于合成8‑[{1‑(3,5‑双‑(三氟甲基)苯基)‑乙氧基}‑甲基]‑8‑苯基‑1,7‑二氮杂‑螺[4.5]癸‑2‑酮化合物的方法和中间体
US8637505B2 (en) 2009-02-04 2014-01-28 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8680093B2 (en) 2009-04-30 2014-03-25 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8927539B2 (en) 2009-06-11 2015-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 based on the 1,3-oxazinan-2-one structure
US8883778B2 (en) 2009-07-01 2014-11-11 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1
RU2017145628A (ru) 2009-08-14 2019-02-19 ОПКО Хельс, Инк. Композиции антагонистов нейрокинина-1 для внутривенного введения
EP2496589B1 (en) 2009-11-05 2014-03-05 Boehringer Ingelheim International GmbH Novel chiral phosphorus ligands
US8648192B2 (en) 2010-05-26 2014-02-11 Boehringer Ingelheim International Gmbh 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
US8933072B2 (en) 2010-06-16 2015-01-13 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
EP2585444B1 (en) 2010-06-25 2014-10-22 Boehringer Ingelheim International GmbH Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders
CA2813671A1 (en) 2010-11-02 2012-05-10 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
US20180360040A1 (en) * 2015-12-03 2018-12-20 Syngenta Participations Ag Pesticidal compounds and their uses
EP3822268A1 (en) 2019-11-15 2021-05-19 Bayer Aktiengesellschaft Substituted hydantoinamides as adamts7 antagonists
EP3822265A1 (en) 2019-11-15 2021-05-19 Bayer AG Substituted hydantoinamides as adamts7 antagonists

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994010165A1 (en) * 1992-10-28 1994-05-11 Merck Sharp & Dohme Limited 4-arylmethyloxymethyl piperidines as tachykinin antagonists
GB9601680D0 (en) * 1996-01-27 1996-03-27 Pfizer Ltd Therapeutic agents

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