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17 条记录 (耗时 0.023 秒)

    THIENOPYRANECARBOXAMIDE DERIVATIVES
    1.
    发明授权
    THIENOPYRANECARBOXAMIDE DERIVATIVES 有权
    噻吩并甲酰胺衍生物

    公开(公告)号：EP1200445B1

    公开(公告)日：2003-09-17

    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.

    BENZOPYRAN DERIVATIVES
    2.
    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.

    PIPERAZINE DERIVATIVES AS ALPHA 1A-ADRENERGIC RECEPTOR ANTAGONISTS
    3.
    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。

    1-PHENYLALKYL-PIPERAZINES
    5.
    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
    7.
    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.