DICIANOPIRIDINAS ALQUILAMINO-SUSTITUIDAS COMO AGONISTAS DEL RECEPTOR DE ADENOSINA A1 Y A2

La presente solicitud se refiere a nuevas dicianopiridinas 6-alquilamino-sustituidas, a sus profármacos de éster de aminoácido, a procedimientos para su preparación, a su uso para el tratamiento y/o la profilaxis de enfermedades y a su uso para preparar medicamentos para el tratamiento y/o la preven...

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Hauptverfasser: PETER NELL, ALEXANDROS VAKALOPOULOS, FRANK SUSSMEIER, JOERG KELDENICH, URSULA KRENZ, BARBARA ALBRECHTKUPPER, DANIEL MEIBOM, KATJA ZIMMERMANN, HANS-GEORG LERCHEN
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creator PETER NELL
ALEXANDROS VAKALOPOULOS
FRANK SUSSMEIER
JOERG KELDENICH
URSULA KRENZ
BARBARA ALBRECHTKUPPER
DANIEL MEIBOM
KATJA ZIMMERMANN
HANS-GEORG LERCHEN
description La presente solicitud se refiere a nuevas dicianopiridinas 6-alquilamino-sustituidas, a sus profármacos de éster de aminoácido, a procedimientos para su preparación, a su uso para el tratamiento y/o la profilaxis de enfermedades y a su uso para preparar medicamentos para el tratamiento y/o la prevención de trastornos cardiovasculares, tales como hipertension, enfermedad cardiaca coronaria, sindrome coronario agudo, angina de pecho. Alkylamino-substituted dicyanopyridine compounds (I) and their salts, N-oxides, solvates, salts of N-oxide or solvates of N-oxide and salts are new. Alkylamino-substituted dicyanopyridine compounds of formula (I) and their salts, N-oxides, solvates, salts of N-oxide or solvates of N-oxide and salts are new. Either R 1> : H or (1-4C)-alkyl; and R 2> : (1-6C)-alkyl, (2-4C)-alkenyl, (2-4C)-alkynyl or (3-7C)-cycloalkyl, where: (1-6C)-alkyl is optionally substituted by 1-3 F, Cl, CF 3, CF 3O, (1-4C)-alkoxy, (3-7C)-cycloalkyl, (3-7C)-cycloalkoxy, (1-4C)-alkylsulfanyl or (1-4C)-alkylsulfonyl, (2-4C)-alkenyl and (2-4C)-alkynyl is optionally substituted by 1 or 2 F, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy, and (3-7C)-cycloalkyl is optionally substituted by 1 or 2 F, Cl, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy; or R 1>R 2>N : 4-7-membered heterocycle optionally substituted by 1 or 2 F, Cl, oxo, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy; R 3> : H, -C(=O)-C(R 4>)(R 5>)-N(R 7>)(R 6>) (A), -C(=O)-C(R 8>)(R 9>)-N(R 10>)-C(=O)-C(R 11>)(R 12>)-N(R 13>)(R 14>) (B), -C(=O)-C(R 8>)(R 9>)-N(R 10>)-C(=O)-L 1>-N(R 15>)(R 16>) (C), -C(=O)-L 2>-N(R 16>)(R 17>) (D), -C(=O)-L 2>-N(R 19>)-C(=O)-C(R 11>)(R 12>)-N(R 13>)(R 13>) (E) or -C(=O)-L 2>-N(R 19>)-C(=O) -L 1>-N(R 15>)(R 16>) (F); L 1>, L 2> : (2-6C)-alkanediyl; either R 4>, R 8> : H or the side group of a natural amino acid or its homologous or isomer; and R 6>, R 7>, R 13>-R 18> : H or (1-4C)-alkyl; or R 6>R 7>N, R 13>R 14>N, R 15>R 16>N, R 17>R 18>N : a 5- or 6-membered heterocycle optionally substituted by 1 or 2 (1-4C)-alkyl, amino, OH or (1-4C)-alkoxy; or R 7>R 4> : pyrrolidine- or piperidine ring; R 5>, R 9>, R 10>, R 12>, R 19> : H or CH 3; and either R 11> : H or a side group of a natural alpha -amino acid or its homologous or isomer; or R 14>R 11> : pyrrolidine- or piperidine ring. Independent claims are included for: (1) the preparations of (I); and (2) a medicament comprising (I) in combination with one or more further active agent comprising an active agent that modifies fat metabo
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fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_DOP2011000243A</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>DOP2011000243A</sourcerecordid><originalsourceid>FETCH-epo_espacenet_DOP2011000243A3</originalsourceid><addsrcrecordid>eNqNjE0KwjAQRrtxIeodBlwXktYLDEnUgTQT87PoqhSJK9FCvT9m4QFcPd7j49s2oyZF6NhTIE0OI6C9ZbI4kOM25pgoZdK1Kx4Y8MKOYqqqjYVglPGJQxVAbRzH-gAoYQTs9s3mMT_Xcvhx1xzPJqlrW5b3VNZlvpdX-UyafSekFEJ0px77_1Zf8J8yMA</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>DICIANOPIRIDINAS ALQUILAMINO-SUSTITUIDAS COMO AGONISTAS DEL RECEPTOR DE ADENOSINA A1 Y A2</title><source>esp@cenet</source><creator>PETER NELL ; ALEXANDROS VAKALOPOULOS ; FRANK SUSSMEIER ; JOERG KELDENICH ; URSULA KRENZ ; BARBARA ALBRECHTKUPPER ; DANIEL MEIBOM ; KATJA ZIMMERMANN ; HANS-GEORG LERCHEN</creator><creatorcontrib>PETER NELL ; ALEXANDROS VAKALOPOULOS ; FRANK SUSSMEIER ; JOERG KELDENICH ; URSULA KRENZ ; BARBARA ALBRECHTKUPPER ; DANIEL MEIBOM ; KATJA ZIMMERMANN ; HANS-GEORG LERCHEN</creatorcontrib><description>La presente solicitud se refiere a nuevas dicianopiridinas 6-alquilamino-sustituidas, a sus profármacos de éster de aminoácido, a procedimientos para su preparación, a su uso para el tratamiento y/o la profilaxis de enfermedades y a su uso para preparar medicamentos para el tratamiento y/o la prevención de trastornos cardiovasculares, tales como hipertension, enfermedad cardiaca coronaria, sindrome coronario agudo, angina de pecho. Alkylamino-substituted dicyanopyridine compounds (I) and their salts, N-oxides, solvates, salts of N-oxide or solvates of N-oxide and salts are new. Alkylamino-substituted dicyanopyridine compounds of formula (I) and their salts, N-oxides, solvates, salts of N-oxide or solvates of N-oxide and salts are new. Either R 1&gt; : H or (1-4C)-alkyl; and R 2&gt; : (1-6C)-alkyl, (2-4C)-alkenyl, (2-4C)-alkynyl or (3-7C)-cycloalkyl, where: (1-6C)-alkyl is optionally substituted by 1-3 F, Cl, CF 3, CF 3O, (1-4C)-alkoxy, (3-7C)-cycloalkyl, (3-7C)-cycloalkoxy, (1-4C)-alkylsulfanyl or (1-4C)-alkylsulfonyl, (2-4C)-alkenyl and (2-4C)-alkynyl is optionally substituted by 1 or 2 F, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy, and (3-7C)-cycloalkyl is optionally substituted by 1 or 2 F, Cl, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy; or R 1&gt;R 2&gt;N : 4-7-membered heterocycle optionally substituted by 1 or 2 F, Cl, oxo, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy; R 3&gt; : H, -C(=O)-C(R 4&gt;)(R 5&gt;)-N(R 7&gt;)(R 6&gt;) (A), -C(=O)-C(R 8&gt;)(R 9&gt;)-N(R 10&gt;)-C(=O)-C(R 11&gt;)(R 12&gt;)-N(R 13&gt;)(R 14&gt;) (B), -C(=O)-C(R 8&gt;)(R 9&gt;)-N(R 10&gt;)-C(=O)-L 1&gt;-N(R 15&gt;)(R 16&gt;) (C), -C(=O)-L 2&gt;-N(R 16&gt;)(R 17&gt;) (D), -C(=O)-L 2&gt;-N(R 19&gt;)-C(=O)-C(R 11&gt;)(R 12&gt;)-N(R 13&gt;)(R 13&gt;) (E) or -C(=O)-L 2&gt;-N(R 19&gt;)-C(=O) -L 1&gt;-N(R 15&gt;)(R 16&gt;) (F); L 1&gt;, L 2&gt; : (2-6C)-alkanediyl; either R 4&gt;, R 8&gt; : H or the side group of a natural amino acid or its homologous or isomer; and R 6&gt;, R 7&gt;, R 13&gt;-R 18&gt; : H or (1-4C)-alkyl; or R 6&gt;R 7&gt;N, R 13&gt;R 14&gt;N, R 15&gt;R 16&gt;N, R 17&gt;R 18&gt;N : a 5- or 6-membered heterocycle optionally substituted by 1 or 2 (1-4C)-alkyl, amino, OH or (1-4C)-alkoxy; or R 7&gt;R 4&gt; : pyrrolidine- or piperidine ring; R 5&gt;, R 9&gt;, R 10&gt;, R 12&gt;, R 19&gt; : H or CH 3; and either R 11&gt; : H or a side group of a natural alpha -amino acid or its homologous or isomer; or R 14&gt;R 11&gt; : pyrrolidine- or piperidine ring. Independent claims are included for: (1) the preparations of (I); and (2) a medicament comprising (I) in combination with one or more further active agent comprising an active agent that modifies fat metabolism, antidiabetic drug, blood pressure reducing agent and antithrombotic active agent. [Image] ACTIVITY : Muscular-Gen.; Cardiant; Vasotropic; Antianginal; Antidiabetic; Analgesic; Antilipemic; Hypotensive; Antiarrhythmic; Antiinflammatory; Anticoagulant; Thrombolytic; Cerebroprotective; Endocrine-Gen.; Antipsoriatic; Antiseborrheic; Dermatological; Ophthalmological; Vulnerary; Virucide; Cardiovascular-Gen.; Neuroprotective; Nootropic; Antiparkinsonian; Anticonvulsant; Antidepressant; Cytostatic; Antiemetic; Gastrointestinal-Gen.; Antiulcer; Immunosuppressive; Antiarthritic; Antirheumatic; Respiratory-Gen.; Antiasthmatic; CNS-Gen.; Nephrotropic; Anorectic; Antithyroid; Anabolic; Osteopathic; Angiogenesis Modulator. MECHANISM OF ACTION : Adenosine A1 receptor agonist; Adenosine A2b receptor agonist. The ability of (I) to agonize adenosine A1 receptor was tested in Chinese hamster ovary cell line. The results showed that 2-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulfanyl)-6-[(2-fluorethyl)amino]-4-[4-(2-hydroxyethoxy)phenyl]pyridin-3,5-dicarbonitrile exhibited a median effective concentration of 0.05 nM.</description><language>spa</language><subject>HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><creationdate>2017</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=20171015&amp;DB=EPODOC&amp;CC=DO&amp;NR=P2011000243A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,309,782,887,25571,76555</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20171015&amp;DB=EPODOC&amp;CC=DO&amp;NR=P2011000243A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>PETER NELL</creatorcontrib><creatorcontrib>ALEXANDROS VAKALOPOULOS</creatorcontrib><creatorcontrib>FRANK SUSSMEIER</creatorcontrib><creatorcontrib>JOERG KELDENICH</creatorcontrib><creatorcontrib>URSULA KRENZ</creatorcontrib><creatorcontrib>BARBARA ALBRECHTKUPPER</creatorcontrib><creatorcontrib>DANIEL MEIBOM</creatorcontrib><creatorcontrib>KATJA ZIMMERMANN</creatorcontrib><creatorcontrib>HANS-GEORG LERCHEN</creatorcontrib><title>DICIANOPIRIDINAS ALQUILAMINO-SUSTITUIDAS COMO AGONISTAS DEL RECEPTOR DE ADENOSINA A1 Y A2</title><description>La presente solicitud se refiere a nuevas dicianopiridinas 6-alquilamino-sustituidas, a sus profármacos de éster de aminoácido, a procedimientos para su preparación, a su uso para el tratamiento y/o la profilaxis de enfermedades y a su uso para preparar medicamentos para el tratamiento y/o la prevención de trastornos cardiovasculares, tales como hipertension, enfermedad cardiaca coronaria, sindrome coronario agudo, angina de pecho. Alkylamino-substituted dicyanopyridine compounds (I) and their salts, N-oxides, solvates, salts of N-oxide or solvates of N-oxide and salts are new. Alkylamino-substituted dicyanopyridine compounds of formula (I) and their salts, N-oxides, solvates, salts of N-oxide or solvates of N-oxide and salts are new. Either R 1&gt; : H or (1-4C)-alkyl; and R 2&gt; : (1-6C)-alkyl, (2-4C)-alkenyl, (2-4C)-alkynyl or (3-7C)-cycloalkyl, where: (1-6C)-alkyl is optionally substituted by 1-3 F, Cl, CF 3, CF 3O, (1-4C)-alkoxy, (3-7C)-cycloalkyl, (3-7C)-cycloalkoxy, (1-4C)-alkylsulfanyl or (1-4C)-alkylsulfonyl, (2-4C)-alkenyl and (2-4C)-alkynyl is optionally substituted by 1 or 2 F, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy, and (3-7C)-cycloalkyl is optionally substituted by 1 or 2 F, Cl, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy; or R 1&gt;R 2&gt;N : 4-7-membered heterocycle optionally substituted by 1 or 2 F, Cl, oxo, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy; R 3&gt; : H, -C(=O)-C(R 4&gt;)(R 5&gt;)-N(R 7&gt;)(R 6&gt;) (A), -C(=O)-C(R 8&gt;)(R 9&gt;)-N(R 10&gt;)-C(=O)-C(R 11&gt;)(R 12&gt;)-N(R 13&gt;)(R 14&gt;) (B), -C(=O)-C(R 8&gt;)(R 9&gt;)-N(R 10&gt;)-C(=O)-L 1&gt;-N(R 15&gt;)(R 16&gt;) (C), -C(=O)-L 2&gt;-N(R 16&gt;)(R 17&gt;) (D), -C(=O)-L 2&gt;-N(R 19&gt;)-C(=O)-C(R 11&gt;)(R 12&gt;)-N(R 13&gt;)(R 13&gt;) (E) or -C(=O)-L 2&gt;-N(R 19&gt;)-C(=O) -L 1&gt;-N(R 15&gt;)(R 16&gt;) (F); L 1&gt;, L 2&gt; : (2-6C)-alkanediyl; either R 4&gt;, R 8&gt; : H or the side group of a natural amino acid or its homologous or isomer; and R 6&gt;, R 7&gt;, R 13&gt;-R 18&gt; : H or (1-4C)-alkyl; or R 6&gt;R 7&gt;N, R 13&gt;R 14&gt;N, R 15&gt;R 16&gt;N, R 17&gt;R 18&gt;N : a 5- or 6-membered heterocycle optionally substituted by 1 or 2 (1-4C)-alkyl, amino, OH or (1-4C)-alkoxy; or R 7&gt;R 4&gt; : pyrrolidine- or piperidine ring; R 5&gt;, R 9&gt;, R 10&gt;, R 12&gt;, R 19&gt; : H or CH 3; and either R 11&gt; : H or a side group of a natural alpha -amino acid or its homologous or isomer; or R 14&gt;R 11&gt; : pyrrolidine- or piperidine ring. Independent claims are included for: (1) the preparations of (I); and (2) a medicament comprising (I) in combination with one or more further active agent comprising an active agent that modifies fat metabolism, antidiabetic drug, blood pressure reducing agent and antithrombotic active agent. [Image] ACTIVITY : Muscular-Gen.; Cardiant; Vasotropic; Antianginal; Antidiabetic; Analgesic; Antilipemic; Hypotensive; Antiarrhythmic; Antiinflammatory; Anticoagulant; Thrombolytic; Cerebroprotective; Endocrine-Gen.; Antipsoriatic; Antiseborrheic; Dermatological; Ophthalmological; Vulnerary; Virucide; Cardiovascular-Gen.; Neuroprotective; Nootropic; Antiparkinsonian; Anticonvulsant; Antidepressant; Cytostatic; Antiemetic; Gastrointestinal-Gen.; Antiulcer; Immunosuppressive; Antiarthritic; Antirheumatic; Respiratory-Gen.; Antiasthmatic; CNS-Gen.; Nephrotropic; Anorectic; Antithyroid; Anabolic; Osteopathic; Angiogenesis Modulator. MECHANISM OF ACTION : Adenosine A1 receptor agonist; Adenosine A2b receptor agonist. The ability of (I) to agonize adenosine A1 receptor was tested in Chinese hamster ovary cell line. The results showed that 2-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulfanyl)-6-[(2-fluorethyl)amino]-4-[4-(2-hydroxyethoxy)phenyl]pyridin-3,5-dicarbonitrile exhibited a median effective concentration of 0.05 nM.</description><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2017</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjE0KwjAQRrtxIeodBlwXktYLDEnUgTQT87PoqhSJK9FCvT9m4QFcPd7j49s2oyZF6NhTIE0OI6C9ZbI4kOM25pgoZdK1Kx4Y8MKOYqqqjYVglPGJQxVAbRzH-gAoYQTs9s3mMT_Xcvhx1xzPJqlrW5b3VNZlvpdX-UyafSekFEJ0px77_1Zf8J8yMA</recordid><startdate>20171015</startdate><enddate>20171015</enddate><creator>PETER NELL</creator><creator>ALEXANDROS VAKALOPOULOS</creator><creator>FRANK SUSSMEIER</creator><creator>JOERG KELDENICH</creator><creator>URSULA KRENZ</creator><creator>BARBARA ALBRECHTKUPPER</creator><creator>DANIEL MEIBOM</creator><creator>KATJA ZIMMERMANN</creator><creator>HANS-GEORG LERCHEN</creator><scope>EVB</scope></search><sort><creationdate>20171015</creationdate><title>DICIANOPIRIDINAS ALQUILAMINO-SUSTITUIDAS COMO AGONISTAS DEL RECEPTOR DE ADENOSINA A1 Y A2</title><author>PETER NELL ; ALEXANDROS VAKALOPOULOS ; FRANK SUSSMEIER ; JOERG KELDENICH ; URSULA KRENZ ; BARBARA ALBRECHTKUPPER ; DANIEL MEIBOM ; KATJA ZIMMERMANN ; HANS-GEORG LERCHEN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_DOP2011000243A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>spa</language><creationdate>2017</creationdate><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><toplevel>online_resources</toplevel><creatorcontrib>PETER NELL</creatorcontrib><creatorcontrib>ALEXANDROS VAKALOPOULOS</creatorcontrib><creatorcontrib>FRANK SUSSMEIER</creatorcontrib><creatorcontrib>JOERG KELDENICH</creatorcontrib><creatorcontrib>URSULA KRENZ</creatorcontrib><creatorcontrib>BARBARA ALBRECHTKUPPER</creatorcontrib><creatorcontrib>DANIEL MEIBOM</creatorcontrib><creatorcontrib>KATJA ZIMMERMANN</creatorcontrib><creatorcontrib>HANS-GEORG LERCHEN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>PETER NELL</au><au>ALEXANDROS VAKALOPOULOS</au><au>FRANK SUSSMEIER</au><au>JOERG KELDENICH</au><au>URSULA KRENZ</au><au>BARBARA ALBRECHTKUPPER</au><au>DANIEL MEIBOM</au><au>KATJA ZIMMERMANN</au><au>HANS-GEORG LERCHEN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>DICIANOPIRIDINAS ALQUILAMINO-SUSTITUIDAS COMO AGONISTAS DEL RECEPTOR DE ADENOSINA A1 Y A2</title><date>2017-10-15</date><risdate>2017</risdate><abstract>La presente solicitud se refiere a nuevas dicianopiridinas 6-alquilamino-sustituidas, a sus profármacos de éster de aminoácido, a procedimientos para su preparación, a su uso para el tratamiento y/o la profilaxis de enfermedades y a su uso para preparar medicamentos para el tratamiento y/o la prevención de trastornos cardiovasculares, tales como hipertension, enfermedad cardiaca coronaria, sindrome coronario agudo, angina de pecho. Alkylamino-substituted dicyanopyridine compounds (I) and their salts, N-oxides, solvates, salts of N-oxide or solvates of N-oxide and salts are new. Alkylamino-substituted dicyanopyridine compounds of formula (I) and their salts, N-oxides, solvates, salts of N-oxide or solvates of N-oxide and salts are new. Either R 1&gt; : H or (1-4C)-alkyl; and R 2&gt; : (1-6C)-alkyl, (2-4C)-alkenyl, (2-4C)-alkynyl or (3-7C)-cycloalkyl, where: (1-6C)-alkyl is optionally substituted by 1-3 F, Cl, CF 3, CF 3O, (1-4C)-alkoxy, (3-7C)-cycloalkyl, (3-7C)-cycloalkoxy, (1-4C)-alkylsulfanyl or (1-4C)-alkylsulfonyl, (2-4C)-alkenyl and (2-4C)-alkynyl is optionally substituted by 1 or 2 F, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy, and (3-7C)-cycloalkyl is optionally substituted by 1 or 2 F, Cl, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy; or R 1&gt;R 2&gt;N : 4-7-membered heterocycle optionally substituted by 1 or 2 F, Cl, oxo, CF 3, (1-4C)-alkyl, CF 3O or (1-4C)-alkoxy; R 3&gt; : H, -C(=O)-C(R 4&gt;)(R 5&gt;)-N(R 7&gt;)(R 6&gt;) (A), -C(=O)-C(R 8&gt;)(R 9&gt;)-N(R 10&gt;)-C(=O)-C(R 11&gt;)(R 12&gt;)-N(R 13&gt;)(R 14&gt;) (B), -C(=O)-C(R 8&gt;)(R 9&gt;)-N(R 10&gt;)-C(=O)-L 1&gt;-N(R 15&gt;)(R 16&gt;) (C), -C(=O)-L 2&gt;-N(R 16&gt;)(R 17&gt;) (D), -C(=O)-L 2&gt;-N(R 19&gt;)-C(=O)-C(R 11&gt;)(R 12&gt;)-N(R 13&gt;)(R 13&gt;) (E) or -C(=O)-L 2&gt;-N(R 19&gt;)-C(=O) -L 1&gt;-N(R 15&gt;)(R 16&gt;) (F); L 1&gt;, L 2&gt; : (2-6C)-alkanediyl; either R 4&gt;, R 8&gt; : H or the side group of a natural amino acid or its homologous or isomer; and R 6&gt;, R 7&gt;, R 13&gt;-R 18&gt; : H or (1-4C)-alkyl; or R 6&gt;R 7&gt;N, R 13&gt;R 14&gt;N, R 15&gt;R 16&gt;N, R 17&gt;R 18&gt;N : a 5- or 6-membered heterocycle optionally substituted by 1 or 2 (1-4C)-alkyl, amino, OH or (1-4C)-alkoxy; or R 7&gt;R 4&gt; : pyrrolidine- or piperidine ring; R 5&gt;, R 9&gt;, R 10&gt;, R 12&gt;, R 19&gt; : H or CH 3; and either R 11&gt; : H or a side group of a natural alpha -amino acid or its homologous or isomer; or R 14&gt;R 11&gt; : pyrrolidine- or piperidine ring. Independent claims are included for: (1) the preparations of (I); and (2) a medicament comprising (I) in combination with one or more further active agent comprising an active agent that modifies fat metabolism, antidiabetic drug, blood pressure reducing agent and antithrombotic active agent. [Image] ACTIVITY : Muscular-Gen.; Cardiant; Vasotropic; Antianginal; Antidiabetic; Analgesic; Antilipemic; Hypotensive; Antiarrhythmic; Antiinflammatory; Anticoagulant; Thrombolytic; Cerebroprotective; Endocrine-Gen.; Antipsoriatic; Antiseborrheic; Dermatological; Ophthalmological; Vulnerary; Virucide; Cardiovascular-Gen.; Neuroprotective; Nootropic; Antiparkinsonian; Anticonvulsant; Antidepressant; Cytostatic; Antiemetic; Gastrointestinal-Gen.; Antiulcer; Immunosuppressive; Antiarthritic; Antirheumatic; Respiratory-Gen.; Antiasthmatic; CNS-Gen.; Nephrotropic; Anorectic; Antithyroid; Anabolic; Osteopathic; Angiogenesis Modulator. MECHANISM OF ACTION : Adenosine A1 receptor agonist; Adenosine A2b receptor agonist. The ability of (I) to agonize adenosine A1 receptor was tested in Chinese hamster ovary cell line. The results showed that 2-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulfanyl)-6-[(2-fluorethyl)amino]-4-[4-(2-hydroxyethoxy)phenyl]pyridin-3,5-dicarbonitrile exhibited a median effective concentration of 0.05 nM.</abstract><oa>free_for_read</oa></addata></record>
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recordid cdi_epo_espacenet_DOP2011000243A
source esp@cenet
subjects HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
title DICIANOPIRIDINAS ALQUILAMINO-SUSTITUIDAS COMO AGONISTAS DEL RECEPTOR DE ADENOSINA A1 Y A2
url https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-04T08%3A22%3A25IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-epo_EVB&rft_val_fmt=info:ofi/fmt:kev:mtx:patent&rft.genre=patent&rft.au=PETER%20NELL&rft.date=2017-10-15&rft_id=info:doi/&rft_dat=%3Cepo_EVB%3EDOP2011000243A%3C/epo_EVB%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true