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    AMORPHOUS LERCANIDIPINE HYDROCHLORIDE
    1.
    发明公开
    AMORPHOUS LERCANIDIPINE HYDROCHLORIDE 审中-公开
    非晶态盐酸大戟胺

    公开(公告)号：EP1856051A1

    公开(公告)日：2007-11-21

    申请号：EP06723128.2

    申请日：2006-02-24

    申请人： Recordati Ireland Limited ,  RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a.

    发明人： LEONARDI, Amedeo ,  MOTTA, Gianni ,  BERLATI, Fabio

    IPC分类号： C07D211/90 ,  A61K31/435 ,  A61P9/12

    摘要： The invention provides a substantially pure amorphous lercanidipine hydrochloride having a purity of at least 95% pure, preferably at least about 97% pure, more preferably at least about 99% pure, and still more preferably at least about 99.5% pure. The invention further relates to methods of preparing substantially pure amorphous lercanidipine, as well as methods of providing rapid relief from hypertension by administering the substantially pure amorphous lercanidipine hydrochloride of the present invention to a patient in need of such treatment.

    摘要翻译： 本发明提供纯度至少95％，优选至少约97％纯，更优选至少约99％纯，并且还更优选至少约99.5％纯度的基本上纯的无定形乐卡地平盐酸盐。 本发明进一步提供了制备基本上纯的无定形乐卡地平的方法以及含有基本上纯的无定形乐卡地平的药物组合物。

    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
    5.
    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.

    LERCANIDIPINE CAPSULES
    9.
    发明公开
    LERCANIDIPINE CAPSULES 审中-公开
    乐卡地平胶囊

    公开(公告)号：EP1807059A1

    公开(公告)日：2007-07-18

    申请号：EP05794809.3

    申请日：2005-10-05

    申请人： Recordati Ireland Limited ,  RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a.

    发明人： LEONARDI, Amedeo ,  BERLATI, Fabio ,  PONTELLO, Lino

    IPC分类号： A61K9/48 ,  A61K31/4422

    CPC分类号： A61K31/455 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/4422

    摘要： A modified release pharmaceutical composition comprises lercanidipine dissolved in a waxy substance comprising a polyalcohol fatty acid ester, the solution being contained within a pharmaceutically acceptable capsule. Preferably the polyalcohol fatty acid ester is a polyethylene glycol ester, a polypropylene glycol ester, a fatty acid glyceride or a mixture of two or more thereof. Most preferably, the polyalcohol fatty acid ester is a mixture of mono-, di- and triglycerides and polyethylene glycol mono- and diesters. Oral administration of the modified release pharmaceutical compositions to a patient has been shown to result in a mean lercanidipine plasma concentration of greater than 0.5 ng/ml for 24 hours after administration.

    LERCANIDIPINE SALTS
    10.
    发明公开
    LERCANIDIPINE SALTS 有权

    公开(公告)号：EP1799644A1

    公开(公告)日：2007-06-27

    申请号：EP05776228.8

    申请日：2005-08-22

    申请人： Recordati Ireland Limited ,  RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a.

    发明人： LEONARDI, Amedeo ,  MOTTA, Gianni ,  VON RAUMER, Markus

    IPC分类号： C07D211/90 ,  A61K31/4422 ,  A61P9/12

    CPC分类号： C07D211/90

    摘要： The invention relates to new addition salts comprising lercanidipine and an acid counterion selected from the group consisting of: (i) inorganic acids, (ii) sulphonic acids, (iii) monocarboxylic acids, (iv) dicarboxylic acids, (v) tricarboxylic acids, and (vi) aromatic sulphonimides, with the proviso that said acid counterion is not hydrochloric acid. In particular, both amorphous and crystalline salts of lercanidipine with benzenesulphonic and naphthalene- 1,5-disulphonic acids are disclosed, as are amorphous salts of lercanidipine with several other acid counterions.

    摘要翻译： （i）无机酸，（ii）磺酸，（iii）一元羧酸，（iv）二元羧酸，（v）三元羧酸， 和（vi）芳族磺酰亚胺，条件是所述酸抗衡离子不是盐酸。 具体而言，公开了苯基磺酸和萘-1,5-二磺酸的乐卡地平的无定形盐和结晶盐，以及具有几种其他酸抗衡离子的乐卡地平的无定形盐。