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公开(公告)号:EP1924554A1
公开(公告)日:2008-05-28
申请号:EP06820086.4
申请日:2006-09-15
发明人: HEINO, Jyrki , JOHNSON, Mark , KÄPYLÄ, Jarmo , MARJAMÄKI, Anne , NYRÖNEN, Tommi , OJALA, Marika , PENTIKÄINEN, Olli , PIHLAVISTO, Marjo , NISSINEN, Liisa
IPC分类号: C07C311/21 , C07D233/32 , A61K31/18 , A61K31/4166 , C07D207/34 , C07D213/50 , C07D233/61 , C07D261/08 , C07D261/10 , C07D263/32 , C07D295/13 , C07D295/192 , A61K31/215 , A61K31/27 , A61K31/277 , A61K31/401 , A61K31/417 , A61K31/42 , A61K31/421 , A61K31/4409 , A61K31/5375
CPC分类号: C07C311/21 , C07D207/416 , C07D213/50 , C07D233/38 , C07D261/08 , C07D261/14 , C07D261/18 , C07D263/32 , C07D295/192
摘要: The invention relates to sulphonamide derivatives of formula (I), where Rc is selected from a group consisting of dialkylamino, NO2, CN, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkanoyl, oxazol-2-yl, oxazolylaminocarbonyl, aryl, aroyl, aryl-CH(OH)-, arylaminocarbonyl, furanyl, where the aryl, aroyl and furanyl moieties may be substituted, guanidinyl-(CH2)z-N(R´)-, Het-(CH2)z -N(R')-, Het-CO-N(R')-, Het-CH(OH)- and Het-CO-, where Het is an optionally substituted 4-6-membered heterocyclic ring containing one or more heteroatoms sleeted from N, S and O, R' is hydrogen or alkyl, and z is an integer 1 to 5; RA is a group of formula (A), (B), (C) or (D) as defined in the claims; and RB is hydrogen, alkyl, alkanoyl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminoalkyl, mono- or dialkylaminoalkyl or Het-alkyl, where Het is as defined above; The invention also relates to the use of derivatives of formula (I) as inhibitors for collagen receptor integrins and a process for preparing sulphonamides of formula (II).
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公开(公告)号:EP1633861A1
公开(公告)日:2006-03-15
申请号:EP04734701.8
申请日:2004-05-25
发明人: SALMINEN, Tiina , AIRENNE, Tomi , JOHNSON, Mark , KIDRON, Heidi , NYMALM-REJSTRÖM, Yvonne , SÖDERHOLM, Annu , SMITH, David , PIHLAVISTO, Marjo , VIITANEN, Lenita , PENTIKÄINEN, Olli , NYRÖNEN, Tommi
CPC分类号: C07K14/705 , C07K2299/00
摘要: The present invention relates to crystalline vascular adhesion protein-1 (VAP-1) and in particular to methods for the use of structural information of crystalline human VAP-1 for ligand and/or inhibitor identification, design and production, as well as screening assays for detection of same. The invention further relates to inhibitors identified by the assays according to the present invention.
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公开(公告)号:EP1732884A1
公开(公告)日:2006-12-20
申请号:EP04742190.4
申请日:2004-07-12
发明人: SMITH, David , MARJAMÄKI, Anne , OJALA, Marika , PIHLAVISTO, Marjo , HEINO, Jyrki , KÄPYLÄ, Jarmo , PENTIKÄINEN, Olli , NYRÖNEN, Tommi , JOHNSON, Mark , HUHTALA, Mikko
IPC分类号: C07C317/32 , A61K31/18 , A61P35/00
CPC分类号: C07D239/22 , C07C311/21 , C07C311/29 , C07D207/325 , C07D209/08 , C07D209/48 , C07D209/88 , C07D213/61 , C07D213/82 , C07D231/12 , C07D231/16 , C07D231/42 , C07D233/54 , C07D233/68 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/48 , C07D239/52 , C07D257/04 , C07D263/56 , C07D271/06 , C07D271/08 , C07D275/06 , C07D277/62 , C07D277/64 , C07D277/66 , C07D277/68 , C07D277/74 , C07D285/06 , C07D295/135 , C07D295/30 , C07D303/36 , C07D317/66 , C07D333/34 , C07D403/04 , C07D403/12 , C07D405/04 , C07D409/12 , C07D413/12 , C07D413/14
摘要: The invention relates to sulphonamide derivatives of formula (I), where RC is optionally substituted 4-6-membered heterocyclic ring containing one or more N atoms, or RC forms together with the phenyl ring to which it is attached a benzodioxolyl group, or RC is -NR1R2, RA is a group having the formula (A), (B) or (C) RB is hydrogen or alkyl. The invention also relates to the use of derivatives of formula (I) as inhibitors for collagen receptor integrins and a process for preparing sulphonamides of formula (I).
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公开(公告)号:EP1633861B1
公开(公告)日:2009-11-04
申请号:EP04734701.8
申请日:2004-05-25
发明人: SALMINEN, Tiina , AIRENNE, Tomi , JOHNSON, Mark , KIDRON, Heidi , NYMALM-REJSTRÖM, Yvonne , SÖDERHOLM, Annu , SMITH, David , PIHLAVISTO, Marjo , VIITANEN, Lenita , PENTIKÄINEN, Olli , NYRÖNEN, Tommi
CPC分类号: C07K14/705 , C07K2299/00
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公开(公告)号:EP1931706A1
公开(公告)日:2008-06-18
申请号:EP06794113.8
申请日:2006-09-15
发明人: HEINO, Jyrki , JOHNSON, Mark , KÄPYLÄ, Jarmo , MARJAMÄKI, Anne , NYRÖNEN, Tommi , OJALA, Marika , PENTIKÄINEN, Olli , NISSINEN, Liisa
IPC分类号: C07K14/705 , G01N33/68 , C40B30/02 , A61K31/18 , A61K31/65 , C07C317/32 , C07C49/798 , G06F19/00
CPC分类号: C07C311/21 , C07C311/53 , C07K14/705 , G01N33/6803 , G01N2333/7055 , G06F19/00 , G16H50/50 , Y02A90/26
摘要: The present invention relates to a refined and detailed molecular model of the alpha2⊕1 integrin I-domain, especially the MIDAS and to the use of such a model for designing novel integrin modulators, especially alpha2beta1 integrin modulators. The present invention further relates to novel alpha2beta1 I-domain modulators, which are of therapeutic potential. The present invention further relates to specific families of small molecule modulators interacting with collagen receptors, tetracyclic polyketides and sulfonamides. The present invention further relates to the use of such modulators for the manufacture of medicaments for thrombosis, inflammation and/or cancer
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