PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF

A pyrazole derivative represented by the general formula (I) [wherein R1 is H, optionally substituted C1-6 alkyl, etc.; either of Q and T is the group of the formula (II) or the formula (III) and the other is optionally substituted C1-6 alkyl, etc.; R2 is H, halogeno, OH, optionally substituted C1-6...

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description A pyrazole derivative represented by the general formula (I) [wherein R1 is H, optionally substituted C1-6 alkyl, etc.; either of Q and T is the group of the formula (II) or the formula (III) and the other is optionally substituted C1-6 alkyl, etc.; R2 is H, halogeno, OH, optionally substituted C1-6 alkyl, etc.; X is a single bond, O, or S; Y is optionally substituted C1-6 alkylene, etc.; Z is -RB, -CORC, etc. (RB is optionally substituted C1-6 alkyl, etc.; and RC is optionally substituted C1-6 alkyl, etc.); R4 is H, optionally substituted C1-6 alkyl, etc.; and R3, R5, and R6 each is H, halogeno, etc.], a pharmacologically acceptable salt of the derivative, or a prodrug of either. They have excellent human SGLT1 inhibitory activity and are useful as a preventive or therapeutic agent for diseases attributable to hyperglycemia such as diabetes, impaired glucose tolerance, fasting blood sugar abnormality, complications of diabetes, and obesity and for diseases attributable to an increased blood galactose level such as galactosemia. Un derivado de pirazol, representado por la formula general (I): [donde R1 es H, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; uno de Q y T es el grupo de la formula (II): o de la formula (III):y el otro es alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; R2 es H, halogeno, OH, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc. ; X es una ligadura simple, O o S; Y es alquileno de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; Z es -RB, -CORC, etc. (RB es alquilo 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; y RC es alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.); R4 es H, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; y cada uno de R3, R5 y R6 es H, halogeno, etc.]; una sal del derivado aceptable para uso farmaceutico, o un profarmaco de cualquiera de estos. Tienen excelente actividad inhibidora de SGLT1 humano y son utiles como un agente de prevencion o terapeutico para enfermedades atribuibles a hiperglicemia, tales como: diabetes, tolerancia danada a la glucosa, anormalidad de azucar en la sangre en ayunas, complicaciones de diabetes y obesidad; y para enfermedades atribuibles a un nivel incrementado de galactosa en la sangre, tal como galactosemia.
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They have excellent human SGLT1 inhibitory activity and are useful as a preventive or therapeutic agent for diseases attributable to hyperglycemia such as diabetes, impaired glucose tolerance, fasting blood sugar abnormality, complications of diabetes, and obesity and for diseases attributable to an increased blood galactose level such as galactosemia. Un derivado de pirazol, representado por la formula general (I): [donde R1 es H, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; uno de Q y T es el grupo de la formula (II): o de la formula (III):y el otro es alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; R2 es H, halogeno, OH, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc. ; X es una ligadura simple, O o S; Y es alquileno de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; Z es -RB, -CORC, etc. (RB es alquilo 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; y RC es alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.); R4 es H, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; y cada uno de R3, R5 y R6 es H, halogeno, etc.]; una sal del derivado aceptable para uso farmaceutico, o un profarmaco de cualquiera de estos. Tienen excelente actividad inhibidora de SGLT1 humano y son utiles como un agente de prevencion o terapeutico para enfermedades atribuibles a hiperglicemia, tales como: diabetes, tolerancia danada a la glucosa, anormalidad de azucar en la sangre en ayunas, complicaciones de diabetes y obesidad; y para enfermedades atribuibles a un nivel incrementado de galactosa en la sangre, tal como galactosemia.</description><edition>7</edition><language>eng ; spa</language><subject>CHEMISTRY ; DERIVATIVES THEREOF ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; NUCLEIC ACIDS ; NUCLEOSIDES ; NUCLEOTIDES ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS ; SUGARS</subject><creationdate>2005</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=20050603&amp;DB=EPODOC&amp;CC=MX&amp;NR=PA05002129A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76290</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20050603&amp;DB=EPODOC&amp;CC=MX&amp;NR=PA05002129A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>TOMAE, MASAKI</creatorcontrib><title>PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF</title><description>A pyrazole derivative represented by the general formula (I) [wherein R1 is H, optionally substituted C1-6 alkyl, etc.; either of Q and T is the group of the formula (II) or the formula (III) and the other is optionally substituted C1-6 alkyl, etc.; R2 is H, halogeno, OH, optionally substituted C1-6 alkyl, etc.; X is a single bond, O, or S; Y is optionally substituted C1-6 alkylene, etc.; Z is -RB, -CORC, etc. (RB is optionally substituted C1-6 alkyl, etc.; and RC is optionally substituted C1-6 alkyl, etc.); R4 is H, optionally substituted C1-6 alkyl, etc.; and R3, R5, and R6 each is H, halogeno, etc.], a pharmacologically acceptable salt of the derivative, or a prodrug of either. They have excellent human SGLT1 inhibitory activity and are useful as a preventive or therapeutic agent for diseases attributable to hyperglycemia such as diabetes, impaired glucose tolerance, fasting blood sugar abnormality, complications of diabetes, and obesity and for diseases attributable to an increased blood galactose level such as galactosemia. Un derivado de pirazol, representado por la formula general (I): [donde R1 es H, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; uno de Q y T es el grupo de la formula (II): o de la formula (III):y el otro es alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; R2 es H, halogeno, OH, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc. ; X es una ligadura simple, O o S; Y es alquileno de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; Z es -RB, -CORC, etc. (RB es alquilo 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; y RC es alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.); R4 es H, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; y cada uno de R3, R5 y R6 es H, halogeno, etc.]; una sal del derivado aceptable para uso farmaceutico, o un profarmaco de cualquiera de estos. Tienen excelente actividad inhibidora de SGLT1 humano y son utiles como un agente de prevencion o terapeutico para enfermedades atribuibles a hiperglicemia, tales como: diabetes, tolerancia danada a la glucosa, anormalidad de azucar en la sangre en ayunas, complicaciones de diabetes y obesidad; y para enfermedades atribuibles a un nivel incrementado de galactosa en la sangre, tal como galactosemia.</description><subject>CHEMISTRY</subject><subject>DERIVATIVES THEREOF</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>NUCLEIC ACIDS</subject><subject>NUCLEOSIDES</subject><subject>NUCLEOTIDES</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><subject>SUGARS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2005</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjD0LwkAQRNNYiPofFusIUbGwXO42ZiH3wd0lqE0Iclaigdj71zWSwtJqhnmPmSYve3J4NiWBJMc1Bq7Jp6BIsmCNJQijrPEc2OhP1wFZsz5AKAg8KvpVK0_D7sjkKaCWwDqQGzgGgtw4sM7ISny_RnGeTK7trY-LMWfJMqcgilXsHk3su_YS7_HZqKPFbJdlm_Vmj9u_pDfO2TzM</recordid><startdate>20050603</startdate><enddate>20050603</enddate><creator>TOMAE, MASAKI</creator><scope>EVB</scope></search><sort><creationdate>20050603</creationdate><title>PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF</title><author>TOMAE, MASAKI</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_MXPA05002129A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; spa</language><creationdate>2005</creationdate><topic>CHEMISTRY</topic><topic>DERIVATIVES THEREOF</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>NUCLEIC ACIDS</topic><topic>NUCLEOSIDES</topic><topic>NUCLEOTIDES</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><topic>SUGARS</topic><toplevel>online_resources</toplevel><creatorcontrib>TOMAE, MASAKI</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>TOMAE, MASAKI</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF</title><date>2005-06-03</date><risdate>2005</risdate><abstract>A pyrazole derivative represented by the general formula (I) [wherein R1 is H, optionally substituted C1-6 alkyl, etc.; either of Q and T is the group of the formula (II) or the formula (III) and the other is optionally substituted C1-6 alkyl, etc.; R2 is H, halogeno, OH, optionally substituted C1-6 alkyl, etc.; X is a single bond, O, or S; Y is optionally substituted C1-6 alkylene, etc.; Z is -RB, -CORC, etc. (RB is optionally substituted C1-6 alkyl, etc.; and RC is optionally substituted C1-6 alkyl, etc.); R4 is H, optionally substituted C1-6 alkyl, etc.; and R3, R5, and R6 each is H, halogeno, etc.], a pharmacologically acceptable salt of the derivative, or a prodrug of either. They have excellent human SGLT1 inhibitory activity and are useful as a preventive or therapeutic agent for diseases attributable to hyperglycemia such as diabetes, impaired glucose tolerance, fasting blood sugar abnormality, complications of diabetes, and obesity and for diseases attributable to an increased blood galactose level such as galactosemia. Un derivado de pirazol, representado por la formula general (I): [donde R1 es H, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; uno de Q y T es el grupo de la formula (II): o de la formula (III):y el otro es alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; R2 es H, halogeno, OH, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc. ; X es una ligadura simple, O o S; Y es alquileno de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; Z es -RB, -CORC, etc. (RB es alquilo 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; y RC es alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.); R4 es H, alquilo de 1 a 6 atomos de carbono, opcionalmente sustituido, etc.; y cada uno de R3, R5 y R6 es H, halogeno, etc.]; una sal del derivado aceptable para uso farmaceutico, o un profarmaco de cualquiera de estos. Tienen excelente actividad inhibidora de SGLT1 humano y son utiles como un agente de prevencion o terapeutico para enfermedades atribuibles a hiperglicemia, tales como: diabetes, tolerancia danada a la glucosa, anormalidad de azucar en la sangre en ayunas, complicaciones de diabetes y obesidad; y para enfermedades atribuibles a un nivel incrementado de galactosa en la sangre, tal como galactosemia.</abstract><edition>7</edition><oa>free_for_read</oa></addata></record>
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language eng ; spa
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subjects CHEMISTRY
DERIVATIVES THEREOF
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SUGARS
title PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF
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