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54 条记录 (耗时 0.025 秒)

    ISOXAZOLECARBOXAMIDE DERIVATIVES
    31.
    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.

    BENZOPYRAN DERIVATIVES
    32.
    发明授权
    BENZOPYRAN DERIVATIVES 有权
    苯并吡喃衍生物

    公开(公告)号：EP1222183B1

    公开(公告)日：2003-04-23

    申请号：EP00975868.1

    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 ,  SIRONI, Giorgio

    IPC分类号： C07D311/24 ,  A61K31/496 ,  A61P9/00 ,  C07D311/30

    CPC分类号： C07D311/24 ,  C07D311/30

    摘要： Benzopyran derivatives (I) (R = phenyl, alkoxycarbonyl, alkylcarbonyl, CONH2, CONH(alkyl), CON(alkyl)2, CN or alkoxycarbonylamino; R2 = alkyl, alkoxy, polyfluoroalkoxy, OH or CF3SO2O; each of R4 and R5 independently = H, halogen, polyfluoroalkyl, polyfluoroalkoxy, CN or CONH2; n is 0, 1 or 2; but if R = Ph and both of R4 and R5 = H or hologen atoms, then R2 = polyfluoroalkoxy or CF3SO2O) and their N-oxides and pharmaceutically acceptable salts are endowed with adrenergic antagonist activity and, in particular, with high selectivity for the α1-adrenergic receptor as compared to the 5-HT1A receptor. This activity profile suggests the use of these benzopyran derivatives in the treatment of obstructive syndromes of the lower urinary tract, including BPH, without side-effects associated with hypotensive activity.

    ISOXAZOLECARBOXAMIDE DERIVATIVES
    33.
    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.

    THIENOPYRANECARBOXAMIDE DERIVATIVES
    34.
    发明公开
    THIENOPYRANECARBOXAMIDE DERIVATIVES 有权
    噻吩并甲酰胺衍

    公开(公告)号：EP1200445A1

    公开(公告)日：2002-05-02

    申请号：EP00958313.9

    申请日：2000-07-28

    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 ,  TESTA, Rodolfo

    IPC分类号： C07D495/04 ,  A61K31/496 ,  A61P9/00

    CPC分类号： C07D495/04

    摘要： Compounds (I) (R = aryl, cycloalkyl or polyhaloalkyl, R1 = alkyl, alkoxy, polyfluoroalkoxy, hydroxy or trifluoromethanesulphonyloxy, each of R2 and R3 independently = H, halogen, alkoxy or polyfluoroalkoxy, n is 0, 1 or 2) and their N-oxides or pharmaceutically acceptable salts are endowed with enhanced selectivity for the α1 adrenergic receptor and a low activity in lowering blood pressure. This activity profile makes these compounds useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), in lowering intraocular pressure, in the treatment of cardiac arrhythmia and erectile and sexual dysfunction, and in the treatment of lower urinary tract symptoms (LUTS) and neurogenic lower urinary tract dysfunction (NLUTD). Compounds (I) per se, pharmaceutical compositions containing compounds (I) and medical uses of compounds (I) are claimed.

    PIPERAZINE DERIVATIVES AS ALPHA 1A-ADRENERGIC RECEPTOR ANTAGONISTS
    35.
    发明公开
    PIPERAZINE DERIVATIVES AS ALPHA 1A-ADRENERGIC RECEPTOR ANTAGONISTS 失效
    哌嗪类阿司匹林1A-亚硝酸酯抗体拮抗剂

    公开(公告)号：EP0711288A1

    公开(公告)日：1996-05-15

    申请号：EP94925382.0

    申请日：1994-07-22

    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 ,  TESTA, Rodolfo

    IPC分类号： C07D295 ,  A61K31 ,  A61P25 ,  A61P43 ,  C07D261 ,  C07D263 ,  C07D277 ,  C07D307 ,  C07D319 ,  C07D333 ,  C07F9

    CPC分类号： C07D295/088 ,  C07C2601/14 ,  C07D295/13 ,  C07F9/650958

    摘要： There are disclosed compounds of general formula (I). Y is a linking group, chosen from a wide range, but including -COO-, -CH2COO-, -CONH-, -CON(CH3)-, -CH2CONH-, -SO2NH-, -SO2N(CH3)- and -PO(OC2H5)NH-. W is an alkylene chain. A is a substituted phenyl group or a benzofuran or benzodioxan group. R and R1 may have many values, but R is preferably a bulky group. These compounds and their prodrugs, enantiomers, diastereoisomers, N-oxides and pharmaceutically acceptable salts block α1A-adrenergic receptors and are thus useful for the prevention of contractions of the prostate, urethra and lower urinary tract, without affecting blood pressure.

    摘要翻译： 公开了通式（I）的化合物。 Y是从宽范围选择的连接基团，包括-COO - ， - CH 2 COO - ， - CONH - ， - CON（CH 3） - ， - CH 2 CONH - ， - SO 2 NH-， - SO 2 N（CH 3） （OC2H5）NH-。 W是亚烷基链。 A是取代的苯基或苯并呋喃或苯并二恶烷基。 R和R 1可以具有许多值，但R优选为大体积基团。 这些化合物及其前药，对映异构体，非对映异构体，N-氧化物和药学上可接受的盐阻断α1-肾上腺素能受体，因此可用于预防前列腺，尿道和下泌尿道的收缩，而不影响血压。

    HETEROCYCLIC MGLU5 ANTAGONISTS
    36.
    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
    37.
    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.