发明名称 SUBSTITUTED ACYLPIPERAZINE DERIVATIVES
摘要 THE INVENTION RELATES TO COMPOUNDS OF FORMULA WHEREIN Ar IS SUBSTITUTED ARYL OR UNSUBSTITUTED OR SUBSTITUTED 6-MEMBERED HETEROARYL, CONTAINING ONE, TWO OR THREE NITROGEN ATOMS, AND WHEREIN THE ARYL AND THE HETEROARYL GROUPS MAY BE SUBSTITUTED BY ONE OR MORE SUBSTITUENTS SELECTED FROM THE GROUP CONSISTING OF HYDROXY, HALOGEN, CN, (C1-C6)-ALKYL, (C₁-C6)-ALKYL SUBSTITUTED BY HALOGEN, (C₁-C6)-ALKOXY, (C₁-C6)-ALKOXY SUBSTITUTED BY HALOGEN, NR7R8, C(O)R9 OR SO₂R10; R¹ IS HYDROGEN OR (C₁-C6)-ALKYL; R² IS HALOGEN, (C₁-C6)-ALKYL, (C₁-C6)-ALKENYL, WHEREIN A HYDROGEN ATOM MAY BE REPLACED BY CN, C(O)-R9 OR (C₁-C6)-ALKYL, OR IS (C₂-C6)ALKYNYL, (C₁-C6)-ALKYL SUBSTITUTED BY HALOGEN, -(CH₂)n-(C₃-C7)CYCLOALKYL, -(CH₂)n-HETEROCYCLOALKYL, -C(O)-R9, -(CH₂)n-ARYL OR -(CH₂)n-5 OR -6-MEMBERED HETEROARYL CONTAINING ONE, TWO OR THREE HETEROATOMS, SELECTED FROM THE GROUP CONSISTING OF OXYGEN, SULPHUR OR NITROGEN WHEREIN ARYL, CYCLOALKYL, HETEROCYCLOALKYL AND HETEROARYL ARE UNSUBSTITUTED OR SUBSTITUTED BY ONE OR MORE SUBSTITUENTS SELECTED FROM THE GROUP CONSISTING OF HYDROXY, HALOGEN, (C₁-C6)-ALKYL, (C₁-C6)-ALKYL SUBSTITUTED BY HALOGEN OR (C₁-C6)-ALKOXY; R³, R⁴ AND R6 INDEPENDENTLY FROM EACH OTHER ARE HYDROGEN, HYDROXY, HALOGEN, (C₁-C6)-ALKYL OR (C₁-C6)-ALKOXY; R5 IS NO₂, CN, C(O)R9, SO₂ R10 OR NR11 R12; R7 AND R8 INDEPENDENTLY FROM EACH OTHER ARE HYDROGEN OR (C₁-C6)-ALKYL; R9 IS (C₁-C6)-ALKYL, (C₃-C6)-CYCLOALKYL, (C₁-C6)-ALKOXY OR NR7 R8; R10 IS (C₁-C6)-ALKYL, (C₃-C6)-CYCLOALKYL OR NR7 R8; R11 AND R12 INDEPENDENTLY FROM EACH OTHER ARE HYDROGEN, OR FORM TOGETHER WITH THE N-ATOM TO WHICH THEY ARE ATTACHED A 5-MEMBERED HETEROARYL GROUP; n IS 0, 1 OR 2;AND TO PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF FOR THE TREATMENT OF PSYCHOSES, PAIN, NEURODEGENERATIVE DISFUNCTION IN MEMORY AND LEARNING, SCHIZOPHRENIA, DEMENTIA AND OTHER DISEASES IN WHICH COGNITIVE PROCESSES ARE IMPAIRED, SUCH AS ATTENTION DEFICIT DISORDERS OR ALZHEIMER'S DISEASE.
申请公布号 MY140470(A) 申请公布日期 2009.12.31
申请号 MYPI20043602 申请日期 2004.09.06
申请人 F. HOFFMANN-LA ROCHE AG 发明人 DANIELA ALBERATI-GIANI;SYNESE JOLIDON;ROBERT NARQUIZIAN;MATTHIAS HEINRICH NETTEKOVEN;ROGER DAVID NORCROSS;EMMANUEL PINARD;HENRI STALDER
分类号 A61K31/495;A61K31/496;A61P25/28;C07D213/56;C07D213/69;C07D213/74;C07D233/54;C07D239/26;C07D239/42;C07D241/12;C07D251/42;C07D251/48;C07D257/04;C07D263/32;C07D277/30;C07D295/16;C07D295/185;C07D309/04;C07D309/20;C07D333/24;C07D409/12 主分类号 A61K31/495
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