PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS
Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl...
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| creator | LINDERS, JOANNES THEODORUS MARIA JAROSKOVA, LIBUSE BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR VAN DER VEKEN, LOUIS JOZEF ELISABETH DIMITROV, VLADIMIR DIMTCHEV NIKIFOROV, THEO TEOFANOV |
| description | Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl Or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.
(ver formula (I)) sus formas N-oxido, sus sales de adicion farmaceuticamente aceptables y sus formas estereoquimicamente isomeras, en donde: N es 1 o 2; L representa un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de alquilo C1-4; alquiloxi C1-3-alquilo C1-4-; hidroxi-alquilo C1-4; hidroxi; alquiloxi C1-3- o fenil-alquilo C1-4; M representa un enlace directo o un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de hidroxi; alquilo C1-4; o alquiloxi C1-4; R1 y R2 representan, cada uno de manera independiente, hidrogeno; halo; ciano; hidroxi; alquilo C1-4 opcionalmente sustituido con halo; alquiloxi C1-4 opcionalmente sustituido con uno, o cuando es posible, con dos o tres sustituyentes seleccionados de hidroxi, Ar1 y halo; o R1 y R2 tomados junto con el anillo fenilo al cual estan unidos forman naftilo o 1,3-benzodioxolilo, en donde dichos naftilo o 1,3-benzodiozolilo estan opcionalmente sustituidos con halo; R3 representa hidrogeno; halo; alquilo C1-4; alquiloxi C1-4-; ciano; o hidroxi; R4 representa hidrogeno; halo; alq |
| format | Patent |
| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_MXPA06012932A</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>MXPA06012932A</sourcerecordid><originalsourceid>FETCH-epo_espacenet_MXPA06012932A3</originalsourceid><addsrcrecordid>eNqNirEKwjAUALs4iPoPoXugSUFwfDVP80CTkITSTKWUOIkW6v9jEQdHp-OOWxejS97bCykyXHJrkIFRzJFD_9PUYi1EajEwCEwI3mAEppPytkshoreklusTzmggICOjqaFofdgWq9twn_Puy01RnjAeNc_Ts8_zNIz5kV_9tXNQ7SshD7WE-q_pDX3YNRY</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS</title><source>esp@cenet</source><creator>LINDERS, JOANNES THEODORUS MARIA ; JAROSKOVA, LIBUSE ; BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR ; VAN DER VEKEN, LOUIS JOZEF ELISABETH ; DIMITROV, VLADIMIR DIMTCHEV ; NIKIFOROV, THEO TEOFANOV</creator><creatorcontrib>LINDERS, JOANNES THEODORUS MARIA ; JAROSKOVA, LIBUSE ; BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR ; VAN DER VEKEN, LOUIS JOZEF ELISABETH ; DIMITROV, VLADIMIR DIMTCHEV ; NIKIFOROV, THEO TEOFANOV</creatorcontrib><description>Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl Or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.
(ver formula (I)) sus formas N-oxido, sus sales de adicion farmaceuticamente aceptables y sus formas estereoquimicamente isomeras, en donde: N es 1 o 2; L representa un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de alquilo C1-4; alquiloxi C1-3-alquilo C1-4-; hidroxi-alquilo C1-4; hidroxi; alquiloxi C1-3- o fenil-alquilo C1-4; M representa un enlace directo o un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de hidroxi; alquilo C1-4; o alquiloxi C1-4; R1 y R2 representan, cada uno de manera independiente, hidrogeno; halo; ciano; hidroxi; alquilo C1-4 opcionalmente sustituido con halo; alquiloxi C1-4 opcionalmente sustituido con uno, o cuando es posible, con dos o tres sustituyentes seleccionados de hidroxi, Ar1 y halo; o R1 y R2 tomados junto con el anillo fenilo al cual estan unidos forman naftilo o 1,3-benzodioxolilo, en donde dichos naftilo o 1,3-benzodiozolilo estan opcionalmente sustituidos con halo; R3 representa hidrogeno; halo; alquilo C1-4; alquiloxi C1-4-; ciano; o hidroxi; R4 representa hidrogeno; halo; alquilo C1-4; alquiloxi C1-4-; ciano; o hidroxi; R5 representa hidrogeno; alquilo C1-4; o Ar2-alquilo C1-4-; R6 representa hidrogeno; halo; alquilo C1-4; o alquiloxi C1-4; Ar1 y Ar2 representan, cada uno de manera independiente, fenilo o naftilo, en donde dichos fenilo y naftilo estan opcionalmente sustituidos con alquilo C1-4; alquiloxi C1-4-; o fenil-alquilo C1-4; para uso como un medicamento.</description><language>eng ; spa</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>2007</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=20070126&DB=EPODOC&CC=MX&NR=PA06012932A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20070126&DB=EPODOC&CC=MX&NR=PA06012932A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>LINDERS, JOANNES THEODORUS MARIA</creatorcontrib><creatorcontrib>JAROSKOVA, LIBUSE</creatorcontrib><creatorcontrib>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</creatorcontrib><creatorcontrib>VAN DER VEKEN, LOUIS JOZEF ELISABETH</creatorcontrib><creatorcontrib>DIMITROV, VLADIMIR DIMTCHEV</creatorcontrib><creatorcontrib>NIKIFOROV, THEO TEOFANOV</creatorcontrib><title>PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS</title><description>Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl Or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.
(ver formula (I)) sus formas N-oxido, sus sales de adicion farmaceuticamente aceptables y sus formas estereoquimicamente isomeras, en donde: N es 1 o 2; L representa un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de alquilo C1-4; alquiloxi C1-3-alquilo C1-4-; hidroxi-alquilo C1-4; hidroxi; alquiloxi C1-3- o fenil-alquilo C1-4; M representa un enlace directo o un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de hidroxi; alquilo C1-4; o alquiloxi C1-4; R1 y R2 representan, cada uno de manera independiente, hidrogeno; halo; ciano; hidroxi; alquilo C1-4 opcionalmente sustituido con halo; alquiloxi C1-4 opcionalmente sustituido con uno, o cuando es posible, con dos o tres sustituyentes seleccionados de hidroxi, Ar1 y halo; o R1 y R2 tomados junto con el anillo fenilo al cual estan unidos forman naftilo o 1,3-benzodioxolilo, en donde dichos naftilo o 1,3-benzodiozolilo estan opcionalmente sustituidos con halo; R3 representa hidrogeno; halo; alquilo C1-4; alquiloxi C1-4-; ciano; o hidroxi; R4 representa hidrogeno; halo; alquilo C1-4; alquiloxi C1-4-; ciano; o hidroxi; R5 representa hidrogeno; alquilo C1-4; o Ar2-alquilo C1-4-; R6 representa hidrogeno; halo; alquilo C1-4; o alquiloxi C1-4; Ar1 y Ar2 representan, cada uno de manera independiente, fenilo o naftilo, en donde dichos fenilo y naftilo estan opcionalmente sustituidos con alquilo C1-4; alquiloxi C1-4-; o fenil-alquilo C1-4; para uso como un medicamento.</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>2007</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNirEKwjAUALs4iPoPoXugSUFwfDVP80CTkITSTKWUOIkW6v9jEQdHp-OOWxejS97bCykyXHJrkIFRzJFD_9PUYi1EajEwCEwI3mAEppPytkshoreklusTzmggICOjqaFofdgWq9twn_Puy01RnjAeNc_Ts8_zNIz5kV_9tXNQ7SshD7WE-q_pDX3YNRY</recordid><startdate>20070126</startdate><enddate>20070126</enddate><creator>LINDERS, JOANNES THEODORUS MARIA</creator><creator>JAROSKOVA, LIBUSE</creator><creator>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</creator><creator>VAN DER VEKEN, LOUIS JOZEF ELISABETH</creator><creator>DIMITROV, VLADIMIR DIMTCHEV</creator><creator>NIKIFOROV, THEO TEOFANOV</creator><scope>EVB</scope></search><sort><creationdate>20070126</creationdate><title>PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS</title><author>LINDERS, JOANNES THEODORUS MARIA ; JAROSKOVA, LIBUSE ; BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR ; VAN DER VEKEN, LOUIS JOZEF ELISABETH ; DIMITROV, VLADIMIR DIMTCHEV ; NIKIFOROV, THEO TEOFANOV</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_MXPA06012932A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; spa</language><creationdate>2007</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>LINDERS, JOANNES THEODORUS MARIA</creatorcontrib><creatorcontrib>JAROSKOVA, LIBUSE</creatorcontrib><creatorcontrib>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</creatorcontrib><creatorcontrib>VAN DER VEKEN, LOUIS JOZEF ELISABETH</creatorcontrib><creatorcontrib>DIMITROV, VLADIMIR DIMTCHEV</creatorcontrib><creatorcontrib>NIKIFOROV, THEO TEOFANOV</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>LINDERS, JOANNES THEODORUS MARIA</au><au>JAROSKOVA, LIBUSE</au><au>BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR</au><au>VAN DER VEKEN, LOUIS JOZEF ELISABETH</au><au>DIMITROV, VLADIMIR DIMTCHEV</au><au>NIKIFOROV, THEO TEOFANOV</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS</title><date>2007-01-26</date><risdate>2007</risdate><abstract>Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl Or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.
(ver formula (I)) sus formas N-oxido, sus sales de adicion farmaceuticamente aceptables y sus formas estereoquimicamente isomeras, en donde: N es 1 o 2; L representa un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de alquilo C1-4; alquiloxi C1-3-alquilo C1-4-; hidroxi-alquilo C1-4; hidroxi; alquiloxi C1-3- o fenil-alquilo C1-4; M representa un enlace directo o un conector alquilo C1-3 opcionalmente sustituido con uno o dos sustituyentes seleccionados de hidroxi; alquilo C1-4; o alquiloxi C1-4; R1 y R2 representan, cada uno de manera independiente, hidrogeno; halo; ciano; hidroxi; alquilo C1-4 opcionalmente sustituido con halo; alquiloxi C1-4 opcionalmente sustituido con uno, o cuando es posible, con dos o tres sustituyentes seleccionados de hidroxi, Ar1 y halo; o R1 y R2 tomados junto con el anillo fenilo al cual estan unidos forman naftilo o 1,3-benzodioxolilo, en donde dichos naftilo o 1,3-benzodiozolilo estan opcionalmente sustituidos con halo; R3 representa hidrogeno; halo; alquilo C1-4; alquiloxi C1-4-; ciano; o hidroxi; R4 representa hidrogeno; halo; alquilo C1-4; alquiloxi C1-4-; ciano; o hidroxi; R5 representa hidrogeno; alquilo C1-4; o Ar2-alquilo C1-4-; R6 representa hidrogeno; halo; alquilo C1-4; o alquiloxi C1-4; Ar1 y Ar2 representan, cada uno de manera independiente, fenilo o naftilo, en donde dichos fenilo y naftilo estan opcionalmente sustituidos con alquilo C1-4; alquiloxi C1-4-; o fenil-alquilo C1-4; para uso como un medicamento.</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 | PYRROLIDIN-2-ONE AND PIPERIDIN-2-ONE DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS |
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