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    ISOXAZOLECARBOXAMIDE DERIVATIVES
    1.
    发明授权
    ISOXAZOLECARBOXAMIDE DERIVATIVES 有权
    异唑衍生物作为α1 - 肾上腺素能受体的拮抗剂

    公开(公告)号：EP1226131B1

    公开(公告)日：2003-12-17

    申请号：EP00992436.6

    申请日：2000-10-16

    申请人： RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a. ,  RECORDATI S.A.

    发明人： LEONARDI, Amedeo ,  MOTTA, Gianni ,  RIVA, Carlo ,  POGGESI, Elena

    IPC分类号： C07D261/18 ,  A61K31/42 ,  A61P13/08

    CPC分类号： C07D261/18

    摘要： Isoxazolecarboxamide derivatives (I) (R=alkyl, alkoxy, polyfluoroalkoxy, OH or CF3SO2O; each of R1 and R2 independently =H, halogen, polyfluoroalkoxy or alkoxy; R3 = one or more substituents selected from H, halogen, alkyl, alkoxy, NO2, NH2, NHacyl, CN, alkoxycarbonyl, carboxamido; R4 = H, alkyl or aralkyl; an n is 0, 1 or 2) and their N-oxides and pharmaceutically acceptable salts are endowed with adrenergic antagonist activity and high selectivity toward the αla adrenergic receptor with respect to the 5-HTlA receptor. This activity profile suggests the use of these derivatives in the treatment of obstructive syndromes of the lower urinary tract, including BPH, without side effects associated with hypotensive activity being present.

    1-PHENYLALKYL-PIPERAZINES
    3.
    发明公开
    1-PHENYLALKYL-PIPERAZINES 审中-公开
    1-苯基烷基的哌嗪

    公开(公告)号：EP1549627A1

    公开(公告)日：2005-07-06

    申请号：EP03759960.2

    申请日：2003-06-16

    申请人： Recordati Ireland Limited ,  Recordati Industria Chimica e Farmaceutica S.p.A.

    发明人： LEONARDI, Amadeo ,  MOTTA, Gianni ,  RIVA, Carlo ,  POGGESI, Elena

    IPC分类号： C07D295/08 ,  C07D295/10 ,  C07D319/18 ,  A61K31/495 ,  A61P13/10

    CPC分类号： C07D295/088 ,  C07D295/108 ,  C07D295/155 ,  C07D319/18 ,  C07D405/12 ,  C07D409/12

    摘要： Compounds of formula (I) (R and R1 are a wide range of substituents, Q is CO, CHOH or CHOR2, R2 is alkyl, alkenyl, alkynyl or cycloalkyl group, each of which is optionally substituted, or is alkanoyl, alkanoyoxy, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, aminothiocarbonyl, alkylaminothiocarbonyl or dialkylaminothiocarbonyl, R3 is H, alkyl, -alkenyl, alkynyl, cycloalkyl, aryl or heterocyclic group, each of which is optionally substituted, n is 1 or 2, A is a bond or a methylene or ethylene group and R4 is an aryl or heteroaryl group, either of which is optionally substituted) have affinity for serotoninergic receptors. These compounds and their enantiomers, diastereoisomers, N-piperazine oxides, polymorphs, solvates and pharmaceutically acceptable salts are useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptor activity.

    摘要翻译： 式（I）化合物（R和R 1为宽范围的取代基，Q为CO，CHOH或CHOR 2，R 2为烷基，烯基，炔基或环烷基，其各自任选被取代，或者为烷酰基，烷酰氧基，氨基羰基 烷基氨基羰基，二烷基氨基羰基，氨基硫代羰基，烷基氨基硫代羰基或二烷基氨基硫代羰基，R3是H，烷基， - 链烯基，炔基，环烷基，芳基或杂环基，其各自任选被取代，n为1或2，A为键或亚甲基或 亚乙基和R 4是芳基或杂芳基，其中任一个任选被取代）对血清素能受体具有亲和力。 这些化合物及其对映异构体，非对映异构体，N-哌嗪氧化物，多晶型物，溶剂化物和药学上可接受的盐可用于治疗患有下尿路神经肌肉功能障碍和与5-HT1A受体活性有关的疾病的患者。

    1,4-DISUBSTITUTED PIPERAZINES
    4.
    发明公开
    1,4-DISUBSTITUTED PIPERAZINES 失效
    1,4-DISUBSTITUIERTE PIPERAZINE

    公开(公告)号：EP1000045A1

    公开(公告)日：2000-05-17

    申请号：EP98945130.7

    申请日：1998-07-31

    申请人： RECORDATI S.A.CHEMICAL and PHARMACEUTICAL COMPANY ,  RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a.

    发明人： LEONARDI, Amedeo ,  MOTTA, Gianni ,  RIVA, Carlo ,  GUARNERI, Luciano ,  POGGESI, Elena

    IPC分类号： C07D295/10 ,  A61K31/495

    CPC分类号： C07D213/75

    摘要： Compounds of formula (I) (n = 1 or 2, Het = monocyclic heteroaryl, R = cycloalkyl or monocyclic heteroaryl, R3 = H or lower alkyl, Z = bond, -CH2-, -CH2CH2-, -CH2C(O)-, -CH2CH(OH)-, -O-, -OCH2- or -C(O)-, B = substituted or unsubstituted aryl or heteroaryl) bind to 5HT1A receptors and are therefore useful for the treatment of neuromuscular dysfunctions of the lower urinary tract. The compounds in which Z = bond, B = a substituted phenyl group of formula (a) (R1 = H, halogen, alkoxy, NO2, NH2, NH(acyl), NHSO2(alkyl), R2 = halogen, alkoxy, polyfluoroalkoxy, CN, CONH2; provided that if R1 NH(acyl) or NHSO2(alkyl) then R2 = polyfluoroalkoxy) and the compounds in which Z = -CH2-, -CH2CH2-, -CH2C(O)-, -CH2CH(OH)-, -O-, -OCH2- or -C(O)- are claimed per se; other compounds are claimed for use in preparation of medicaments for treating neuromuscular dysfunctions of the lower urinary tract.

    ISOXAZOLECARBOXAMIDE DERIVATIVES
    5.
    发明公开
    ISOXAZOLECARBOXAMIDE DERIVATIVES 有权
    异唑衍生物作为α1 - 肾上腺素能受体的拮抗剂

    公开(公告)号：EP1226131A2

    公开(公告)日：2002-07-31

    申请号：EP00992436.6

    申请日：2000-10-16

    申请人： RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a. ,  RECORDATI S.A.CHEMICAL and PHARMACEUTICAL COMPANY

    发明人： LEONARDI, Amedeo ,  MOTTA, Gianni ,  RIVA, Carlo ,  POGGESI, Elena

    IPC分类号： C07D261/18 ,  A61K31/42 ,  A61P13/08

    CPC分类号： C07D261/18

    摘要： Isoxazolecarboxamide derivatives (I) (R=alkyl, alkoxy, polyfluoroalkoxy, OH or CF3SO2O; each of R1 and R2 independently =H, halogen, polyfluoroalkoxy or alkoxy; R3 = one or more substituents selected from H, halogen, alkyl, alkoxy, NO2, NH2, NHacyl, CN, alkoxycarbonyl, carboxamido; R4 = H, alkyl or aralkyl; an n is 0, 1 or 2) and their N-oxides and pharmaceutically acceptable salts are endowed with adrenergic antagonist activity and high selectivity toward the αla adrenergic receptor with respect to the 5-HTlA receptor. This activity profile suggests the use of these derivatives in the treatment of obstructive syndromes of the lower urinary tract, including BPH, without side effects associated with hypotensive activity being present.