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21.发明授权Crystal form of lercanidipine hydrochloride for use as an antihypertensive agent 有权盐酸Lercanipidin的晶形用作降压药
公开(公告)号：EP1600441B1
公开(公告)日：2009-12-30
申请号：EP05106264.4
申请日：2002-08-05
IPC分类号： C07D211/90 , A61K31/44 , A61P9/12
CPC分类号： C07D211/90
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公开(公告)号：EP1853562A1
公开(公告)日：2007-11-14
申请号：EP06723129.0
申请日：2006-02-24
IPC分类号： C07D211/90
CPC分类号： C07D211/90
摘要： The invention provides substantially pure lercanidipine free base, having a purity of at least 95 %, preferably at least about 97 %, more preferably at least about 99 %, and still more preferably at least about 99.5 %. The lercanidipine free base of the present invention is formed as an amorphous solid that is easily handled and particularly well suited to the formulation of pharmaceutical compositions.
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23.发明公开
公开(公告)号：EP1432683A1
公开(公告)日：2004-06-30
申请号：EP02762428.7
申请日：2002-08-05
IPC分类号： C07D211/90 , A61K31/44 , A61P9/12
CPC分类号： C07D211/90
摘要： The invention describes novel lercanidipine crude Forms (A) and (B), novel lercanidipine hydrochloride crystalline Forms (I) and (II) obtained form said crude Forms, pharmaceutical, antihypertensive compositions containing as active agent at least one of the lercanidipine hydrochloride crystalline Forms (I) and (II) and methods of use thereof
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24.发明公开
公开(公告)号：EP1423367A1
公开(公告)日：2004-06-02
申请号：EP02767318.5
申请日：2002-08-05
IPC分类号： C07D211/90
CPC分类号： C07D211/90
摘要： The invention describes new solvates of lercanidipine hydrochloride with organic solvents, new crystalline Forms (III) and (IV) of lercanidipine hydrochloride obtained from said solvates by removing solvation solvents, and pharmaceutical compositions containing as active agent at least one of the crystalline Forms (III) and (IV) of lercanidipine hydrochloride.
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公开(公告)号：EP1856051B1
公开(公告)日：2019-11-13
申请号：EP06723128.2
申请日：2006-02-24
发明人： LEONARDI, Amedeo , MOTTA, Gianni , BERLATI, Fabio
IPC分类号： C07D211/90 , A61K31/435 , A61P9/12
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公开(公告)号：EP1858851B1
公开(公告)日：2015-06-24
申请号：EP05817765.0
申请日：2005-10-26
发明人： CHOO, So Mi , HA, Hong Joo , AN, Jung Gi , LEE, Won Jung , LEE, S. G., , BYUN, Young-Seok , MOON, Young Il,
IPC分类号： C07D211/90
CPC分类号： C07D211/90
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公开(公告)号：EP2590985A1
公开(公告)日：2013-05-15
申请号：EP11746494.1
申请日：2011-07-08
发明人： LEONARDI, Amedeo , MOTTA, Gianni , RIVA, Carlo , GUARNERI, Luciano , GRAZIANI, Davide , DE TOMA, Carlo , KARAMFILOVA, Katia Dimitrova
IPC分类号： C07D491/10 , C07D498/10 , A61K31/438 , A61P13/02
CPC分类号： C07D498/10 , C07D491/10
摘要： The invention provides compounds having the general formula (I) wherein X is O or S; R
1 is C, N, O or S; R
1a is CH, CH
2 , N or NH; R
2 is a bond, CH or CH
2 ; m is 1, 2 or 3; n is 1 or 2; when n is 2 or m is 2 or 3, the ring containing R
1 may be fused with a benzene ring; each --- represents a single or double bond provided that one double bond extends from the carbon atom to which R
3 -C≡C- is bonded and that no ring carbon atom bears two double bonds; and R
3 , R
4 and R
5 represent a wide range of substituents. These compounds are selective for the metabotropic mGlu5 receptor. They, their solvates, hydrates, enantiomers, diastereomers, N-oxides and pharmaceutically acceptable salts, and pharmaceutical compositions containing them, can be used to treat diseases or disorders of the lower urinary tract, especially neuromuscular dysfunctions of the lower urinary tract. They may also be useful for the treatment of migraine; for the treatment of gastroesophageal reflux disease (GERD); for the treatment of anxiety disorder; for the treatment of abuse, substance dependence and substance withdrawal disorder; for the treatment of neuropathic pain disorder; and for the treatment of fragile X syndrome disorders.-
公开(公告)号：EP2178858A1
公开(公告)日：2010-04-28
申请号：EP08785292.7
申请日：2008-08-01
发明人： LEONARDI, Amedeo , MOTTA, Gianni , RIVA, Carlo , POGGESI, Elena , GRAZIANI, Davide , LONGHI, Matteo Marco
IPC分类号： C07D401/14 , C07D401/06 , C07D401/04 , C07D417/06 , C07D417/14 , C07D211/70 , C07D409/14 , C07D513/04 , C07D413/14 , C07D407/14 , C07D471/04 , A61K31/4545 , A61P13/02
CPC分类号： C07D401/06 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/04 , C07D513/04
摘要： In Compounds I: Z is a group of the formula, m is 0, 1 or 2; n is 0, 1 or 2; Y is a linking group or is absent; R' is H or OH or is absent; ---- is an optional double bond; and R1, R2 and R3 are selected from a wide range of optionally substituted alkyl, cycloalkyl, aryl and heterocyclic groups. Compounds I are mGlu5 antagonists useful for the treatment of neuromuscular dysfunction of the lower urinary tract, migraine and gastroesophagael reflux disease in mammals. Preferred Compounds I are those having the formula
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29.发明授权USE OF SELECTIVE ANTAGONISTS OF THE ALPHA 1b-ADRENERGIC RECEPTOR FOR IMPROVEMENT OF SEXUAL DYSFUNCTION 有权选择性α肾上腺素能受体拮抗剂对性疾病的治疗用途
公开(公告)号：EP1177190B1
公开(公告)日：2005-11-02
申请号：EP00927199.0
申请日：2000-05-08
IPC分类号： C07D403/04 , C07D407/14 , A61K31/517 , A61P15/10
CPC分类号： C07D403/04 , A61K31/517 , A61K31/519 , A61K31/557 , A61K45/06 , C07D239/95 , C07D405/12 , C07D405/14 , G01N33/9433 , G01N2500/00 , A61K2300/00
摘要： Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the alpha1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.
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30.发明授权
公开(公告)号：EP1432683B1
公开(公告)日：2005-10-19
申请号：EP02762428.7
申请日：2002-08-05
IPC分类号： C07D211/90 , A61K31/44 , A61P9/12
CPC分类号： C07D211/90
摘要： The invention describes novel lercanidipine crude Forms (A) and (B), novel lercanidipine hydrochloride crystalline Forms (I) and (II) obtained form said crude Forms, pharmaceutical, antihypertensive compositions containing as active agent at least one of the lercanidipine hydrochloride crystalline Forms (I) and (II) and methods of use thereof
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