Small molecule inhibitors of rotamase enzyme activity

本发明涉及具有FKBP型亲免蛋白亲合性的神经营养性N-乙醛酰基脯氨酰基酯化合物,其制备方法和作为与亲免蛋白有关的酶活性抑制剂,特别是肽基-脯氨酰基异构酶或旋转异构酶活性抑制剂的应用。 This application relates to 3-phenyl-1-prbpyl(2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate. It further relates to a method of preparing such a compound comprising the step of reacting (2S)-1-...

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Hauptverfasser: G.S. HAMILTON, J.P. STEINER
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J.P. STEINER
description 本发明涉及具有FKBP型亲免蛋白亲合性的神经营养性N-乙醛酰基脯氨酰基酯化合物,其制备方法和作为与亲免蛋白有关的酶活性抑制剂,特别是肽基-脯氨酰基异构酶或旋转异构酶活性抑制剂的应用。 This application relates to 3-phenyl-1-prbpyl(2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate. It further relates to a method of preparing such a compound comprising the step of reacting (2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-pyrrolidinecarboxylic acid with 3-phenyl-1-propanol and dicyclohexylcarbodiimide. Finally, the application relates to the intermediate compound (2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-pyrrolidinecarboxylic acid which may be used to produce 3-phenyl-1-propyl(2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate. 3-phenyl-1-propyl (2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate functions as a rotamase enzyme inhibitor and is therefore useful as a component in pharmaceutical compositions, in particular for promoting neuronal growth and regeneration and for treating neurological disorders.
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Finally, the application relates to the intermediate compound (2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-pyrrolidinecarboxylic acid which may be used to produce 3-phenyl-1-propyl(2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate. 3-phenyl-1-propyl (2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate functions as a rotamase enzyme inhibitor and is therefore useful as a component in pharmaceutical compositions, in particular for promoting neuronal growth and regeneration and for treating neurological disorders.</description><edition>7</edition><language>chi ; eng</language><subject>APPARATUS THEREFOR ; BEER ; BIOCHEMISTRY ; CHEMISTRY ; COMPOSITIONS THEREOF ; CULTURE MEDIA ; ENZYMOLOGY ; GENERAL METHODS OF ORGANIC CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; MICROBIOLOGY ; MICROORGANISMS OR ENZYMES ; MUTATION OR GENETIC ENGINEERING ; ORGANIC CHEMISTRY ; PEPTIDES ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS ; SPIRITS ; VINEGAR ; WINE</subject><creationdate>2004</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20041208&amp;DB=EPODOC&amp;CC=CN&amp;NR=1178912C$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76289</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20041208&amp;DB=EPODOC&amp;CC=CN&amp;NR=1178912C$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>G.S. 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HAMILTON</creatorcontrib><creatorcontrib>J.P. STEINER</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>G.S. HAMILTON</au><au>J.P. STEINER</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Small molecule inhibitors of rotamase enzyme activity</title><date>2004-12-08</date><risdate>2004</risdate><abstract>本发明涉及具有FKBP型亲免蛋白亲合性的神经营养性N-乙醛酰基脯氨酰基酯化合物,其制备方法和作为与亲免蛋白有关的酶活性抑制剂,特别是肽基-脯氨酰基异构酶或旋转异构酶活性抑制剂的应用。 This application relates to 3-phenyl-1-prbpyl(2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate. It further relates to a method of preparing such a compound comprising the step of reacting (2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-pyrrolidinecarboxylic acid with 3-phenyl-1-propanol and dicyclohexylcarbodiimide. Finally, the application relates to the intermediate compound (2S)-1-(1,2-dioxo-3,3-dimethylpentyl)-2-pyrrolidinecarboxylic acid which may be used to produce 3-phenyl-1-propyl(2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate. 3-phenyl-1-propyl (2S)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate functions as a rotamase enzyme inhibitor and is therefore useful as a component in pharmaceutical compositions, in particular for promoting neuronal growth and regeneration and for treating neurological disorders.</abstract><edition>7</edition><oa>free_for_read</oa></addata></record>
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language chi ; eng
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subjects APPARATUS THEREFOR
BEER
BIOCHEMISTRY
CHEMISTRY
COMPOSITIONS THEREOF
CULTURE MEDIA
ENZYMOLOGY
GENERAL METHODS OF ORGANIC CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
MICROBIOLOGY
MICROORGANISMS OR ENZYMES
MUTATION OR GENETIC ENGINEERING
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SPIRITS
VINEGAR
WINE
title Small molecule inhibitors of rotamase enzyme activity
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