PE20020064A1 - Derivados nitrilo beta-aminoacidos como inhibidores de cistein proteasas - Google Patents

Derivados nitrilo beta-aminoacidos como inhibidores de cistein proteasas

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Publication number
PE20020064A1
PE20020064A1 PE2001000541A PE2001000541A PE20020064A1 PE 20020064 A1 PE20020064 A1 PE 20020064A1 PE 2001000541 A PE2001000541 A PE 2001000541A PE 2001000541 A PE2001000541 A PE 2001000541A PE 20020064 A1 PE20020064 A1 PE 20020064A1
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PE
Peru
Prior art keywords
alkyl
cistein
proteases
beta
amino acid
Prior art date
Application number
PE2001000541A
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English (en)
Inventor
Tobias Gabriel
Sarmiento Rosa Maria Rodriguez
Michael Pech
Original Assignee
Hoffmann La Roche
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20020064A1 publication Critical patent/PE20020064A1/es

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    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/20Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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    • C07C255/44Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
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Abstract

SE REFIERE A DERIVADOS DE NITRILO BETA-AMINOACIDOS DE FORMULA I DONDE R1 ES H, ARILO, CORa, SO2Rb; Ra ES ALQUILO, ALCOXILO, CICLOALQUILO, ENTRE OTROS; Rb ES ARILO, ARIL-ALQUILO, HETEROARILO; R2, R3, R4 SON H, ALQUILO; R5 ES H, ALQUILO, CICLOALQUILO, ARILO; n ES 1-2. SON COMPUESTOS PREFERIDOS ESTER BENCILICO DEL ACIDO (1R,2R)-(2-{(S)-[CIANO-(3-HIDROXI-FENIL)-METIL]-CARBAMOIL}-CICLOHEXIL)CARBAMICO; [2-(CIANOMETIL-CARBAMOIL)-CICLOHEXIL]AMIDA DEL ACIDO CIS-5-METOXI-BENZOFURAN-2-CARBOXILICO, ENTRE OTROS; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS PUEDEN SER UTILES PARA EL TRATAMIENTO DE ENFERMEDADES QUE SE ASOCIAN CON CISTEIN PROTEASAS COMO OSTEOPOROSIS, ANGINA DE PECHO INESTABLE, RUPTURA DE LA PLACA ATEROSCLEROTICA
PE2001000541A 2000-06-14 2001-06-08 Derivados nitrilo beta-aminoacidos como inhibidores de cistein proteasas PE20020064A1 (es)

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EP00112577 2000-06-14

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EP (1) EP1294679B1 (es)
JP (1) JP3872427B2 (es)
KR (1) KR20030029057A (es)
CN (1) CN1324006C (es)
AR (1) AR031594A1 (es)
AT (1) ATE304997T1 (es)
AU (2) AU6605601A (es)
BR (1) BR0111733A (es)
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DE (1) DE60113533T2 (es)
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NZ (1) NZ522587A (es)
PE (1) PE20020064A1 (es)
PL (1) PL359811A1 (es)
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WO (1) WO2001096285A1 (es)
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RU2286339C2 (ru) * 2001-09-13 2006-10-27 Ф.Хоффманн-Ля Рош Аг Производные 1,2-диаминопентана как антагонисты рецептора ccr-3 и фармацевтическая композиция на их основе
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US6759428B2 (en) * 2001-12-04 2004-07-06 Roche Palo Alto Llc Indole nitriles
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WO2005000793A1 (ja) * 2003-06-26 2005-01-06 Taisho Pharmaceutical Co., Ltd. 2位置換シクロアルキルカルボン酸誘導体
JP4690319B2 (ja) * 2003-06-30 2011-06-01 メルク フロスト カナダ リミテツド カテプシンシステインプロテアーゼ阻害剤
WO2006076797A1 (en) * 2005-01-19 2006-07-27 Merck Frosst Canada Ltd. Cathepsin k inhibitors and atherosclerosis
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EP2240491B1 (en) 2008-01-09 2015-07-15 Amura Therapeutics Limited TETRAHYDROFURO(2,3-b)PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEINASES
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CN105646362B (zh) 2011-07-26 2019-07-05 赛诺菲 3-杂芳酰基氨基-丙酸衍生物及其作为药物的用途
CN103086923B (zh) * 2013-01-21 2014-04-23 吉林大学 肼腈类组织蛋白酶k抑制剂及其在治疗骨质疏松症方面的应用
CN105593230B (zh) * 2013-10-08 2018-07-06 默沙东公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
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RU2245871C2 (ru) 2005-02-10
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YU90802A (sh) 2006-05-25
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US6462076B2 (en) 2002-10-08
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ATE304997T1 (de) 2005-10-15
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EP1294679A1 (en) 2003-03-26
HK1057539A1 (en) 2004-04-08
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