ES2068646T3 - Derivados de ciclopropenona. - Google Patents

Derivados de ciclopropenona.

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Publication number
ES2068646T3
ES2068646T3 ES92110674T ES92110674T ES2068646T3 ES 2068646 T3 ES2068646 T3 ES 2068646T3 ES 92110674 T ES92110674 T ES 92110674T ES 92110674 T ES92110674 T ES 92110674T ES 2068646 T3 ES2068646 T3 ES 2068646T3
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Spain
Prior art keywords
cathepsin
cyclopropenone
amyotrophy
calpain
transference
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Expired - Lifetime
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ES92110674T
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English (en)
Inventor
Ryoichi Ando
Yasuhiro Morinaka
Chizuko Takahashi
Yoshikuni Tamao
Akirhiro Tobe
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Mitsubishi Kasei Corp
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Mitsubishi Kasei Corp
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Publication of ES2068646T3 publication Critical patent/ES2068646T3/es
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    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/76—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C235/78—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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    • C07C271/54—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
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    • C—CHEMISTRY; METALLURGY
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/36—Sulfur atoms
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
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    • 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
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    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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
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    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
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    • C07K5/06—Dipeptides
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    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
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    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
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    • C07K5/06052—Val-amino acid
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    • A—HUMAN NECESSITIES
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    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
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    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
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    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/18—Systems containing only non-condensed rings with a ring being at least seven-membered

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Abstract

SE PRESENTA UN NUEVO DERIVADO DE LA CICLOPROPENONA (I) QUE POSEE UNA POTENTE ACTIVIDAD INHIBITORIA CONTRA UNA PROTEASA DE TIOL TAL COMO PAPAINA, CATEPSINA B, CATEPSINA H, CATEPSINA L, CALPAINA O SIMILAR CON EXCELENTES PROPIEDADES DE ABSORBENCIA ORAL, TRANSFERENCIA EN EL TEJIDO Y PERMEABILIDAD A LA MEMBRANA CELULAR, Y QUE SON CLINICAMENTE UTILES EN EL TRATAMIENTO DE VARIAS ENFERMEDADES TALES COMO LA DISTROFIA MUSCULAR, LA AMIOTROFIA, ETC. TAMBIEN SE SUMINISTRA UN PROCESO PARA PRODUCIR EL COMPUESTO (I) ASI COMO COMPOSICIONES FARMACEUTICAS QUE LO CONTIENEN.
ES92110674T 1991-06-25 1992-06-25 Derivados de ciclopropenona. Expired - Lifetime ES2068646T3 (es)

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JP15350091 1991-06-25
JP27790491 1991-10-24
JP34149791 1991-12-24
JP14602492A JP3228347B2 (ja) 1991-06-25 1992-06-05 シクロプロペノン誘導体

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ES2068646T3 true ES2068646T3 (es) 1995-04-16

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CA (1) CA2072416C (es)
DE (1) DE69200901T2 (es)
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US5395958A (en) * 1992-09-30 1995-03-07 Mitsubishi Kasei Corporation Cyclopropene derivatives
US5501969A (en) 1994-03-08 1996-03-26 Human Genome Sciences, Inc. Human osteoclast-derived cathepsin
WO1998018485A1 (en) 1996-10-31 1998-05-07 Alcon Laboratories, Inc. The use of calpain inhibitors to treat ocular neural pathology
WO2002010768A2 (en) * 2000-07-31 2002-02-07 The Regents Of The University Of California Model for alzheimer's disease and other neurodegenerative diseases
WO2003062192A1 (en) 2002-01-17 2003-07-31 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
JPWO2006078056A1 (ja) * 2005-01-19 2008-06-19 国立大学法人大阪大学 筋衛星細胞賦活薬
US20070203073A1 (en) * 2005-06-22 2007-08-30 Diamond Scott L SARS and Ebola inhibitors and use thereof, and methods for their discovery
CN101227908A (zh) * 2005-07-22 2008-07-23 宝洁公司 用于减少药源性心律失常发生的组合物
WO2007047205A2 (en) * 2005-10-11 2007-04-26 Amano Enzyme Usa Co., Ltd. Enzyme inhibitors of pai-1
GB2528227A (en) * 2014-03-14 2016-01-20 Medical Res Council Cyclopropene amino acids and methods
WO2024018245A1 (en) 2022-07-22 2024-01-25 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of calpain inhibitors for the treatment of the diabetic kidney disease

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JPS58126879A (ja) * 1982-01-25 1983-07-28 Nippon Chemiphar Co Ltd 光学活性なピペラジン誘導体ならびに心筋梗塞の予防および治療剤
JPS6276A (ja) * 1985-03-26 1987-01-06 Toyo Jozo Co Ltd 酵素阻害性新規物質
US5055451A (en) * 1986-12-22 1991-10-08 Syntex Inc. Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
DE4001087A1 (de) * 1989-01-26 1990-08-02 Sandoz Ag Verwendung von (alpha)-aminofluoroketonen zur behandlung von cardiovaskulaeren stoerungen und erhoehtem blutdruck
JPH02218610A (ja) * 1989-02-21 1990-08-31 Toyo Jozo Co Ltd 骨疾患の予防および治療剤
JP2701932B2 (ja) * 1989-04-10 1998-01-21 サントリー株式会社 タンパク質分解酵素阻害剤
CA2021660A1 (en) * 1989-07-26 1991-01-27 Philippe Bey Peptidase inhibitors
DD294176A5 (de) * 1990-05-11 1991-09-26 Martin-Luther-Universitaet Halle Wittenberg,De Neue inhibitoren zur hemmung der katalytischen aktivitaet von prolinspezifischen und anderen proteolytischen enzymen und verfahren zu ihrer herstellung

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CA2072416C (en) 2006-03-21
CA2072416A1 (en) 1992-12-26
ATE115554T1 (de) 1994-12-15
US5416117A (en) 1995-05-16
DE69200901T2 (de) 1995-06-01
KR930000468A (ko) 1993-01-15
DK0520427T3 (da) 1995-02-20
DE69200901D1 (de) 1995-01-26
KR100254930B1 (ko) 2000-05-01
JPH05230004A (ja) 1993-09-07
EP0520427A1 (en) 1992-12-30
US5328909A (en) 1994-07-12
JP3228347B2 (ja) 2001-11-12
EP0520427B1 (en) 1994-12-14

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