Thiazolyl-dihydro indazoles
Tricyclic thiazole derivatives (I) are new. Tricyclic thiazole derivatives of formula (I) and their salts, isomers, hydrates and solvates are new: A : aromatic ring; Y, Z : C, N, S; j : 1-3; k : 0 or 1; R a>H, COR 8>, NR 9>R 10>, NO 2, OR 8>, SR 11>, SOR 11>, SO 2R 11>, amino...
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| creator | BREITFELDER, STEFFEN REITHER, CHARLOTTE SIMON, OLIVER SCHWEIFER, NORBERT STEURER, STEFFEN IMPAGNATIELLO, MARIA HILBERG, FRANK KRIST, BERND SCHOOP, ANDREAS GRAUERT, MATTHIAS HOENKE, CHRISTOPH WEYER-CZERNILOFSKY, ULRIKE KLEIN, CHRISTIAN BRANDL, TRIXI STEEGMAIER, MARTIN GMACHL, MICHAEL MAIER, UDO SCHEUERER, STEFAN MCCONNELL, DARRYL BRUECKNER, RALPH HOFFMANN, MATTHIAS BETZEMEIER, BODO ZOEPHEL, ANDREAS GERSTBERGER, THOMAS KESSLER, DIRK WAIZENEGGER, IRENE |
| description | Tricyclic thiazole derivatives (I) are new. Tricyclic thiazole derivatives of formula (I) and their salts, isomers, hydrates and solvates are new: A : aromatic ring; Y, Z : C, N, S; j : 1-3; k : 0 or 1; R a>H, COR 8>, NR 9>R 10>, NO 2, OR 8>, SR 11>, SOR 11>, SO 2R 11>, amino(1-6C)alkylcarbonylamino, or optionally substituted 1-6C (halo)alkyl, 2-6C alkenyl, 3-8C cycloalkyl, 3-8C cycloalkenyl, (hetero)aryl, 7-11C aralkyl, Spiro, Het or aryloxymethyl; R 8>1-6C alkyl, 3-6C cycloalkyl, NH 2 or (hetero)aryl, optionally substituted with halo or 1-4C alkyl; R 9>H, COOR 12>, CONR 12> or 1-6C alkyl, optionally substituted with COOH, di(1-6C alkyl)amino or Het, optionally substituted with 1-6C alkyl; or Het optionally substituted with 1-4C alkyl; R 10>H, 1-6C alkyl, 1-6C alkylcarbonyl or 2-6C alkynyl; R 11>1-6C alkyl optionally substituted with di(1-4C alkyl)amino; R b>R 4>, OR 4>, CH 2OR 4>, COR 4>, COOR 4>, CONR 4>R 5>, NR 4>R 5>, NR 5>COR 4>, NR 5>COOR 4>, NR 5>CONR 4>R 5>, NR 5>SOR 4> or NR 5>SO 2R 4>; R 4>, R 5>H, 1-6C (halo)alkyl, 1-6C hydroxyalkyl, 2-6C alkenyl, 2-6C alkynyl, 7-11C aralkyl, (2-4C alkenyl)(hetero)aryl, (2-4C alkynyl)(hetero)aryl, optionally substituted with tri(1-4C alkyl)silyl; or (hetero)aryl or Het optionally substituted with 1-4C alkyl; or R 4>+R 5>5-7-membered ring comprising C and optionally an O, N or S; R c>NHR 6> or NH-CO-B-R 7>; B : bond, 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl; R 6>H or 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-6C cycloalkyl, 3-6C cycloalkenyl, Het or (hetero)aryl optionally substituted with R 61>; R 61>halo, CF 3, OH, CN, OMe, 1-4C alkylsulfonyl; R 7>H, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-6C cycloalkyl, NR 71>R 72>, OR 72>, SR 72>, heteroaryl, Het, optionally substituted with 1-4C alkynyl or CONH 2; R 71>H, 1-6C alkyl, (CH 2) 2-4R 711> or butoxycarbonyl; R 72>H, 1-6C alkyl, optionally substituted with OH; R 711>NR 7111>R 7112>, Het, 1-imidazolyl or 2-(N-ethylpyrrolidine); R 7111>, R 7112>H or 1-6C alkyl; and provided that R a> is not H or Me when Y is N, Z is N, j is 2, k is 0, R b> is H or R c> is NHCONHEt. Spiro, Het and R 12> are not defined. [Image] ACTIVITY : Antiinflammatory; Antiallergic; Dermatological; Antipsoriatic; Antiseborrheic; Ophthalmological; Antiulcer; Hepatotropic; Neuroprotective; Antirheumatic; Antiarthritic; Osteopathic; Nephrotropic. MECHANISM OF ACTION : PI3 kinase (PI3K) inhibitor. In a PI3Kgamma inhibition assay, 2-acetylamino-4,5-dihydro-8-phenyl-8H-pyrazolo[4,5-g]benzothiazole (Ib |
| format | Patent |
| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_ZA200701653B</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>ZA200701653B</sourcerecordid><originalsourceid>FETCH-epo_espacenet_ZA200701653B3</originalsourceid><addsrcrecordid>eNrjZJAOychMrMrPqczRTcnMqEwpylfIzEsBiaQW8zCwpiXmFKfyQmluBkU31xBnD93Ugvz41OKCxOTUvNSS-ChHIwMDcwNDM1NjJ2Ni1AAAoCoj0Q</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>Thiazolyl-dihydro indazoles</title><source>esp@cenet</source><creator>BREITFELDER, STEFFEN ; REITHER, CHARLOTTE ; SIMON, OLIVER ; SCHWEIFER, NORBERT ; STEURER, STEFFEN ; IMPAGNATIELLO, MARIA ; HILBERG, FRANK ; KRIST, BERND ; SCHOOP, ANDREAS ; GRAUERT, MATTHIAS ; HOENKE, CHRISTOPH ; WEYER-CZERNILOFSKY, ULRIKE ; KLEIN, CHRISTIAN ; BRANDL, TRIXI ; STEEGMAIER, MARTIN ; GMACHL, MICHAEL ; MAIER, UDO ; SCHEUERER, STEFAN ; MCCONNELL, DARRYL ; BRUECKNER, RALPH ; HOFFMANN, MATTHIAS ; BETZEMEIER, BODO ; ZOEPHEL, ANDREAS ; GERSTBERGER, THOMAS ; KESSLER, DIRK ; WAIZENEGGER, IRENE</creator><creatorcontrib>BREITFELDER, STEFFEN ; REITHER, CHARLOTTE ; SIMON, OLIVER ; SCHWEIFER, NORBERT ; STEURER, STEFFEN ; IMPAGNATIELLO, MARIA ; HILBERG, FRANK ; KRIST, BERND ; SCHOOP, ANDREAS ; GRAUERT, MATTHIAS ; HOENKE, CHRISTOPH ; WEYER-CZERNILOFSKY, ULRIKE ; KLEIN, CHRISTIAN ; BRANDL, TRIXI ; STEEGMAIER, MARTIN ; GMACHL, MICHAEL ; MAIER, UDO ; SCHEUERER, STEFAN ; MCCONNELL, DARRYL ; BRUECKNER, RALPH ; HOFFMANN, MATTHIAS ; BETZEMEIER, BODO ; ZOEPHEL, ANDREAS ; GERSTBERGER, THOMAS ; KESSLER, DIRK ; WAIZENEGGER, IRENE</creatorcontrib><description>Tricyclic thiazole derivatives (I) are new. Tricyclic thiazole derivatives of formula (I) and their salts, isomers, hydrates and solvates are new: A : aromatic ring; Y, Z : C, N, S; j : 1-3; k : 0 or 1; R a>H, COR 8>, NR 9>R 10>, NO 2, OR 8>, SR 11>, SOR 11>, SO 2R 11>, amino(1-6C)alkylcarbonylamino, or optionally substituted 1-6C (halo)alkyl, 2-6C alkenyl, 3-8C cycloalkyl, 3-8C cycloalkenyl, (hetero)aryl, 7-11C aralkyl, Spiro, Het or aryloxymethyl; R 8>1-6C alkyl, 3-6C cycloalkyl, NH 2 or (hetero)aryl, optionally substituted with halo or 1-4C alkyl; R 9>H, COOR 12>, CONR 12> or 1-6C alkyl, optionally substituted with COOH, di(1-6C alkyl)amino or Het, optionally substituted with 1-6C alkyl; or Het optionally substituted with 1-4C alkyl; R 10>H, 1-6C alkyl, 1-6C alkylcarbonyl or 2-6C alkynyl; R 11>1-6C alkyl optionally substituted with di(1-4C alkyl)amino; R b>R 4>, OR 4>, CH 2OR 4>, COR 4>, COOR 4>, CONR 4>R 5>, NR 4>R 5>, NR 5>COR 4>, NR 5>COOR 4>, NR 5>CONR 4>R 5>, NR 5>SOR 4> or NR 5>SO 2R 4>; R 4>, R 5>H, 1-6C (halo)alkyl, 1-6C hydroxyalkyl, 2-6C alkenyl, 2-6C alkynyl, 7-11C aralkyl, (2-4C alkenyl)(hetero)aryl, (2-4C alkynyl)(hetero)aryl, optionally substituted with tri(1-4C alkyl)silyl; or (hetero)aryl or Het optionally substituted with 1-4C alkyl; or R 4>+R 5>5-7-membered ring comprising C and optionally an O, N or S; R c>NHR 6> or NH-CO-B-R 7>; B : bond, 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl; R 6>H or 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-6C cycloalkyl, 3-6C cycloalkenyl, Het or (hetero)aryl optionally substituted with R 61>; R 61>halo, CF 3, OH, CN, OMe, 1-4C alkylsulfonyl; R 7>H, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-6C cycloalkyl, NR 71>R 72>, OR 72>, SR 72>, heteroaryl, Het, optionally substituted with 1-4C alkynyl or CONH 2; R 71>H, 1-6C alkyl, (CH 2) 2-4R 711> or butoxycarbonyl; R 72>H, 1-6C alkyl, optionally substituted with OH; R 711>NR 7111>R 7112>, Het, 1-imidazolyl or 2-(N-ethylpyrrolidine); R 7111>, R 7112>H or 1-6C alkyl; and provided that R a> is not H or Me when Y is N, Z is N, j is 2, k is 0, R b> is H or R c> is NHCONHEt. Spiro, Het and R 12> are not defined. [Image] ACTIVITY : Antiinflammatory; Antiallergic; Dermatological; Antipsoriatic; Antiseborrheic; Ophthalmological; Antiulcer; Hepatotropic; Neuroprotective; Antirheumatic; Antiarthritic; Osteopathic; Nephrotropic. MECHANISM OF ACTION : PI3 kinase (PI3K) inhibitor. In a PI3Kgamma inhibition assay, 2-acetylamino-4,5-dihydro-8-phenyl-8H-pyrazolo[4,5-g]benzothiazole (Ib) had IC 50 values of 800 nM.</description><language>eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2008</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&date=20080730&DB=EPODOC&CC=ZA&NR=200701653B$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25544,76293</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20080730&DB=EPODOC&CC=ZA&NR=200701653B$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>BREITFELDER, STEFFEN</creatorcontrib><creatorcontrib>REITHER, CHARLOTTE</creatorcontrib><creatorcontrib>SIMON, OLIVER</creatorcontrib><creatorcontrib>SCHWEIFER, NORBERT</creatorcontrib><creatorcontrib>STEURER, STEFFEN</creatorcontrib><creatorcontrib>IMPAGNATIELLO, MARIA</creatorcontrib><creatorcontrib>HILBERG, FRANK</creatorcontrib><creatorcontrib>KRIST, BERND</creatorcontrib><creatorcontrib>SCHOOP, ANDREAS</creatorcontrib><creatorcontrib>GRAUERT, MATTHIAS</creatorcontrib><creatorcontrib>HOENKE, CHRISTOPH</creatorcontrib><creatorcontrib>WEYER-CZERNILOFSKY, ULRIKE</creatorcontrib><creatorcontrib>KLEIN, CHRISTIAN</creatorcontrib><creatorcontrib>BRANDL, TRIXI</creatorcontrib><creatorcontrib>STEEGMAIER, MARTIN</creatorcontrib><creatorcontrib>GMACHL, MICHAEL</creatorcontrib><creatorcontrib>MAIER, UDO</creatorcontrib><creatorcontrib>SCHEUERER, STEFAN</creatorcontrib><creatorcontrib>MCCONNELL, DARRYL</creatorcontrib><creatorcontrib>BRUECKNER, RALPH</creatorcontrib><creatorcontrib>HOFFMANN, MATTHIAS</creatorcontrib><creatorcontrib>BETZEMEIER, BODO</creatorcontrib><creatorcontrib>ZOEPHEL, ANDREAS</creatorcontrib><creatorcontrib>GERSTBERGER, THOMAS</creatorcontrib><creatorcontrib>KESSLER, DIRK</creatorcontrib><creatorcontrib>WAIZENEGGER, IRENE</creatorcontrib><title>Thiazolyl-dihydro indazoles</title><description>Tricyclic thiazole derivatives (I) are new. Tricyclic thiazole derivatives of formula (I) and their salts, isomers, hydrates and solvates are new: A : aromatic ring; Y, Z : C, N, S; j : 1-3; k : 0 or 1; R a>H, COR 8>, NR 9>R 10>, NO 2, OR 8>, SR 11>, SOR 11>, SO 2R 11>, amino(1-6C)alkylcarbonylamino, or optionally substituted 1-6C (halo)alkyl, 2-6C alkenyl, 3-8C cycloalkyl, 3-8C cycloalkenyl, (hetero)aryl, 7-11C aralkyl, Spiro, Het or aryloxymethyl; R 8>1-6C alkyl, 3-6C cycloalkyl, NH 2 or (hetero)aryl, optionally substituted with halo or 1-4C alkyl; R 9>H, COOR 12>, CONR 12> or 1-6C alkyl, optionally substituted with COOH, di(1-6C alkyl)amino or Het, optionally substituted with 1-6C alkyl; or Het optionally substituted with 1-4C alkyl; R 10>H, 1-6C alkyl, 1-6C alkylcarbonyl or 2-6C alkynyl; R 11>1-6C alkyl optionally substituted with di(1-4C alkyl)amino; R b>R 4>, OR 4>, CH 2OR 4>, COR 4>, COOR 4>, CONR 4>R 5>, NR 4>R 5>, NR 5>COR 4>, NR 5>COOR 4>, NR 5>CONR 4>R 5>, NR 5>SOR 4> or NR 5>SO 2R 4>; R 4>, R 5>H, 1-6C (halo)alkyl, 1-6C hydroxyalkyl, 2-6C alkenyl, 2-6C alkynyl, 7-11C aralkyl, (2-4C alkenyl)(hetero)aryl, (2-4C alkynyl)(hetero)aryl, optionally substituted with tri(1-4C alkyl)silyl; or (hetero)aryl or Het optionally substituted with 1-4C alkyl; or R 4>+R 5>5-7-membered ring comprising C and optionally an O, N or S; R c>NHR 6> or NH-CO-B-R 7>; B : bond, 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl; R 6>H or 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-6C cycloalkyl, 3-6C cycloalkenyl, Het or (hetero)aryl optionally substituted with R 61>; R 61>halo, CF 3, OH, CN, OMe, 1-4C alkylsulfonyl; R 7>H, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-6C cycloalkyl, NR 71>R 72>, OR 72>, SR 72>, heteroaryl, Het, optionally substituted with 1-4C alkynyl or CONH 2; R 71>H, 1-6C alkyl, (CH 2) 2-4R 711> or butoxycarbonyl; R 72>H, 1-6C alkyl, optionally substituted with OH; R 711>NR 7111>R 7112>, Het, 1-imidazolyl or 2-(N-ethylpyrrolidine); R 7111>, R 7112>H or 1-6C alkyl; and provided that R a> is not H or Me when Y is N, Z is N, j is 2, k is 0, R b> is H or R c> is NHCONHEt. Spiro, Het and R 12> are not defined. [Image] ACTIVITY : Antiinflammatory; Antiallergic; Dermatological; Antipsoriatic; Antiseborrheic; Ophthalmological; Antiulcer; Hepatotropic; Neuroprotective; Antirheumatic; Antiarthritic; Osteopathic; Nephrotropic. MECHANISM OF ACTION : PI3 kinase (PI3K) inhibitor. In a PI3Kgamma inhibition assay, 2-acetylamino-4,5-dihydro-8-phenyl-8H-pyrazolo[4,5-g]benzothiazole (Ib) had IC 50 values of 800 nM.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2008</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZJAOychMrMrPqczRTcnMqEwpylfIzEsBiaQW8zCwpiXmFKfyQmluBkU31xBnD93Ugvz41OKCxOTUvNSS-ChHIwMDcwNDM1NjJ2Ni1AAAoCoj0Q</recordid><startdate>20080730</startdate><enddate>20080730</enddate><creator>BREITFELDER, STEFFEN</creator><creator>REITHER, CHARLOTTE</creator><creator>SIMON, OLIVER</creator><creator>SCHWEIFER, NORBERT</creator><creator>STEURER, STEFFEN</creator><creator>IMPAGNATIELLO, MARIA</creator><creator>HILBERG, FRANK</creator><creator>KRIST, BERND</creator><creator>SCHOOP, ANDREAS</creator><creator>GRAUERT, MATTHIAS</creator><creator>HOENKE, CHRISTOPH</creator><creator>WEYER-CZERNILOFSKY, ULRIKE</creator><creator>KLEIN, CHRISTIAN</creator><creator>BRANDL, TRIXI</creator><creator>STEEGMAIER, MARTIN</creator><creator>GMACHL, MICHAEL</creator><creator>MAIER, UDO</creator><creator>SCHEUERER, STEFAN</creator><creator>MCCONNELL, DARRYL</creator><creator>BRUECKNER, RALPH</creator><creator>HOFFMANN, MATTHIAS</creator><creator>BETZEMEIER, BODO</creator><creator>ZOEPHEL, ANDREAS</creator><creator>GERSTBERGER, THOMAS</creator><creator>KESSLER, DIRK</creator><creator>WAIZENEGGER, IRENE</creator><scope>EVB</scope></search><sort><creationdate>20080730</creationdate><title>Thiazolyl-dihydro indazoles</title><author>BREITFELDER, STEFFEN ; REITHER, CHARLOTTE ; SIMON, OLIVER ; SCHWEIFER, NORBERT ; STEURER, STEFFEN ; IMPAGNATIELLO, MARIA ; HILBERG, FRANK ; KRIST, BERND ; SCHOOP, ANDREAS ; GRAUERT, MATTHIAS ; HOENKE, CHRISTOPH ; WEYER-CZERNILOFSKY, ULRIKE ; KLEIN, CHRISTIAN ; BRANDL, TRIXI ; STEEGMAIER, MARTIN ; GMACHL, MICHAEL ; MAIER, UDO ; SCHEUERER, STEFAN ; MCCONNELL, DARRYL ; BRUECKNER, RALPH ; HOFFMANN, MATTHIAS ; BETZEMEIER, BODO ; ZOEPHEL, ANDREAS ; GERSTBERGER, THOMAS ; KESSLER, DIRK ; WAIZENEGGER, IRENE</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_ZA200701653B3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2008</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>BREITFELDER, STEFFEN</creatorcontrib><creatorcontrib>REITHER, CHARLOTTE</creatorcontrib><creatorcontrib>SIMON, OLIVER</creatorcontrib><creatorcontrib>SCHWEIFER, NORBERT</creatorcontrib><creatorcontrib>STEURER, STEFFEN</creatorcontrib><creatorcontrib>IMPAGNATIELLO, MARIA</creatorcontrib><creatorcontrib>HILBERG, FRANK</creatorcontrib><creatorcontrib>KRIST, BERND</creatorcontrib><creatorcontrib>SCHOOP, ANDREAS</creatorcontrib><creatorcontrib>GRAUERT, MATTHIAS</creatorcontrib><creatorcontrib>HOENKE, CHRISTOPH</creatorcontrib><creatorcontrib>WEYER-CZERNILOFSKY, ULRIKE</creatorcontrib><creatorcontrib>KLEIN, CHRISTIAN</creatorcontrib><creatorcontrib>BRANDL, TRIXI</creatorcontrib><creatorcontrib>STEEGMAIER, MARTIN</creatorcontrib><creatorcontrib>GMACHL, MICHAEL</creatorcontrib><creatorcontrib>MAIER, UDO</creatorcontrib><creatorcontrib>SCHEUERER, STEFAN</creatorcontrib><creatorcontrib>MCCONNELL, DARRYL</creatorcontrib><creatorcontrib>BRUECKNER, RALPH</creatorcontrib><creatorcontrib>HOFFMANN, MATTHIAS</creatorcontrib><creatorcontrib>BETZEMEIER, BODO</creatorcontrib><creatorcontrib>ZOEPHEL, ANDREAS</creatorcontrib><creatorcontrib>GERSTBERGER, THOMAS</creatorcontrib><creatorcontrib>KESSLER, DIRK</creatorcontrib><creatorcontrib>WAIZENEGGER, IRENE</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>BREITFELDER, STEFFEN</au><au>REITHER, CHARLOTTE</au><au>SIMON, OLIVER</au><au>SCHWEIFER, NORBERT</au><au>STEURER, STEFFEN</au><au>IMPAGNATIELLO, MARIA</au><au>HILBERG, FRANK</au><au>KRIST, BERND</au><au>SCHOOP, ANDREAS</au><au>GRAUERT, MATTHIAS</au><au>HOENKE, CHRISTOPH</au><au>WEYER-CZERNILOFSKY, ULRIKE</au><au>KLEIN, CHRISTIAN</au><au>BRANDL, TRIXI</au><au>STEEGMAIER, MARTIN</au><au>GMACHL, MICHAEL</au><au>MAIER, UDO</au><au>SCHEUERER, STEFAN</au><au>MCCONNELL, DARRYL</au><au>BRUECKNER, RALPH</au><au>HOFFMANN, MATTHIAS</au><au>BETZEMEIER, BODO</au><au>ZOEPHEL, ANDREAS</au><au>GERSTBERGER, THOMAS</au><au>KESSLER, DIRK</au><au>WAIZENEGGER, IRENE</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Thiazolyl-dihydro indazoles</title><date>2008-07-30</date><risdate>2008</risdate><abstract>Tricyclic thiazole derivatives (I) are new. Tricyclic thiazole derivatives of formula (I) and their salts, isomers, hydrates and solvates are new: A : aromatic ring; Y, Z : C, N, S; j : 1-3; k : 0 or 1; R a>H, COR 8>, NR 9>R 10>, NO 2, OR 8>, SR 11>, SOR 11>, SO 2R 11>, amino(1-6C)alkylcarbonylamino, or optionally substituted 1-6C (halo)alkyl, 2-6C alkenyl, 3-8C cycloalkyl, 3-8C cycloalkenyl, (hetero)aryl, 7-11C aralkyl, Spiro, Het or aryloxymethyl; R 8>1-6C alkyl, 3-6C cycloalkyl, NH 2 or (hetero)aryl, optionally substituted with halo or 1-4C alkyl; R 9>H, COOR 12>, CONR 12> or 1-6C alkyl, optionally substituted with COOH, di(1-6C alkyl)amino or Het, optionally substituted with 1-6C alkyl; or Het optionally substituted with 1-4C alkyl; R 10>H, 1-6C alkyl, 1-6C alkylcarbonyl or 2-6C alkynyl; R 11>1-6C alkyl optionally substituted with di(1-4C alkyl)amino; R b>R 4>, OR 4>, CH 2OR 4>, COR 4>, COOR 4>, CONR 4>R 5>, NR 4>R 5>, NR 5>COR 4>, NR 5>COOR 4>, NR 5>CONR 4>R 5>, NR 5>SOR 4> or NR 5>SO 2R 4>; R 4>, R 5>H, 1-6C (halo)alkyl, 1-6C hydroxyalkyl, 2-6C alkenyl, 2-6C alkynyl, 7-11C aralkyl, (2-4C alkenyl)(hetero)aryl, (2-4C alkynyl)(hetero)aryl, optionally substituted with tri(1-4C alkyl)silyl; or (hetero)aryl or Het optionally substituted with 1-4C alkyl; or R 4>+R 5>5-7-membered ring comprising C and optionally an O, N or S; R c>NHR 6> or NH-CO-B-R 7>; B : bond, 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl; R 6>H or 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-6C cycloalkyl, 3-6C cycloalkenyl, Het or (hetero)aryl optionally substituted with R 61>; R 61>halo, CF 3, OH, CN, OMe, 1-4C alkylsulfonyl; R 7>H, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 3-6C cycloalkyl, NR 71>R 72>, OR 72>, SR 72>, heteroaryl, Het, optionally substituted with 1-4C alkynyl or CONH 2; R 71>H, 1-6C alkyl, (CH 2) 2-4R 711> or butoxycarbonyl; R 72>H, 1-6C alkyl, optionally substituted with OH; R 711>NR 7111>R 7112>, Het, 1-imidazolyl or 2-(N-ethylpyrrolidine); R 7111>, R 7112>H or 1-6C alkyl; and provided that R a> is not H or Me when Y is N, Z is N, j is 2, k is 0, R b> is H or R c> is NHCONHEt. Spiro, Het and R 12> are not defined. [Image] ACTIVITY : Antiinflammatory; Antiallergic; Dermatological; Antipsoriatic; Antiseborrheic; Ophthalmological; Antiulcer; Hepatotropic; Neuroprotective; Antirheumatic; Antiarthritic; Osteopathic; Nephrotropic. MECHANISM OF ACTION : PI3 kinase (PI3K) inhibitor. In a PI3Kgamma inhibition assay, 2-acetylamino-4,5-dihydro-8-phenyl-8H-pyrazolo[4,5-g]benzothiazole (Ib) had IC 50 values of 800 nM.</abstract><oa>free_for_read</oa></addata></record> |
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| subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
| title | Thiazolyl-dihydro indazoles |
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