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    AMORPHOUS LERCANIDIPINE HYDROCHLORIDE
    4.
    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
    6.
    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。

    HETEROCYCLIC MGLU5 ANTAGONISTS
    9.
    发明公开
    HETEROCYCLIC MGLU5 ANTAGONISTS 审中-公开
    杂环的mGlu5拮抗剂

    公开(公告)号：EP2477981A1

    公开(公告)日：2012-07-25

    申请号：EP10759812.0

    申请日：2010-09-14

    申请人： Recordati Ireland Limited

    发明人： LEONARDI, Amedeo ,  MOTTA, Gianni ,  RIVA, Carlo ,  GUARNERI, Luciano ,  GRAZIANI, Davide ,  MARINONI, Fabio ,  BETTINELLI, Ilaria

    IPC分类号： C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4523 ,  A61P13/00

    CPC分类号： C07D405/14 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： Compounds (I) (R
    1 is an optionally substituted C
    1 -C
    13 heteromonocyclic, heterobicyclic or heterotri cyclic group containing from 1 to 5 heteroatoms selected from N, O and S; R
    2 is H, an optionally substituted monocyclic aromatic group, or a C
    1 -C
    5 heteroaromatic group containing from 1 to 4 heteroatoms selected from N, O and S; R
    3 is an optionally substituted C
    1 -C
    13 heteromonocyclic, heterobicyclic or heterotri cyclic group containing from 1 to 5 heteroatoms selected from N, O and S; an optionally substituted mono-, bi- or tricyclic C
    6 -C
    14 aryl group, an optionally substituted C
    3 -C
    6 cycloalkyl group, or an optionally substituted C
    3 -C
    6 cycloalkenyl group; each R
    4 , independently for each position capable of substitution, is H or C
    1 -C
    6 alkyl; R
    5 is H, halogen or C
    1 -C
    6 alkyl; m is 0, 1 or 2; n is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, or 6; and --- is an optional double bond) and their enantiomers, diastereomers, N-oxides and pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful for the treatment of neuromuscular dysfunction of the lower urinary tract and also for the treatment of gastrooesophageal reflux disease; anxiety disorder; abuse, substance dependence and substance withdrawal disorders; neuropathic pain disorder, migraine and fragile X syndrome disorders.

    COMBINATION THERAPY OF LOWER URINARY TRACT DISORDERS WITH 2 LIGANDS AND NSAIDS
    10.
    发明公开
    COMBINATION THERAPY OF LOWER URINARY TRACT DISORDERS WITH 2 LIGANDS AND NSAIDS 有权
    联合治疗与2个配体和非甾体抗炎下尿路疾病

    公开(公告)号：EP2125021A1

    公开(公告)日：2009-12-02

    申请号：EP07857036.3

    申请日：2007-12-21

    申请人： Recordati Ireland Limited

    发明人： LEONARDI, Amedeo ,  GUARNERI, Luciano ,  ANGELICO, Patrizia

    IPC分类号： A61K45/06 ,  A61P13/10

    CPC分类号： A61K45/06 ,  A61K31/197

    摘要： The administration to a mammal of a combination of compounds, at least one of which is an α2δ calcium channel subunit (A2d) ligand and at least one of which is a non-steroidal anti-inflammatory drug (NSAID), provides a surprising and potent inhibition of the micturition reflex, superior to that obtained by treatment with an A2d ligand or NSAID alone. Combinations of A2d ligand and NSAIDs are thus useful for treatment of lower urinary tract disorders and symptoms thereof. Preferred A2d ligands are gabapentin and pregabalin. Preferred NSAIDs are celecoxib, diclofenac, diflunisal, flurbiprofen, naproxen, nimesulide or sulindac.