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公开(公告)号:US20070093646A1
公开(公告)日:2007-04-26
申请号:US10557188
申请日:2004-05-25
申请人: Tiina Salminen , Tomi Airenne , Mark Johnson , Heidi Kidron , Yvonne Nymalm-Rejstrom , Annu Soderholm , David Smith , Marjo Pihlavisto , Lenita Viitanen , Olli Pentikainen , Tommi Nyronen
发明人: Tiina Salminen , Tomi Airenne , Mark Johnson , Heidi Kidron , Yvonne Nymalm-Rejstrom , Annu Soderholm , David Smith , Marjo Pihlavisto , Lenita Viitanen , Olli Pentikainen , Tommi Nyronen
IPC分类号: C07K14/705 , G06F19/00
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.
摘要翻译: 本发明涉及结晶血管粘附蛋白-1(VAP-1),特别涉及使用结晶人VAP-1的结构信息用于配体和/或抑制剂鉴定,设计和生产以及筛选测定法 用于检测相同。 本发明还涉及通过根据本发明的测定法鉴定的抑制剂。
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公开(公告)号:US20110021760A1
公开(公告)日:2011-01-27
申请号:US12350844
申请日:2009-01-08
申请人: Tiina SALMINEN , Tomi Airenne , Mark Johnson , Heidi Kidron , Yvonne Nymalm-Rejstrom , Annu Sõderholm , David Smith , Marjo Pihlavisto , Lenita Viitanen , Olli Pentikãinen , Tommi Nyrônen
发明人: Tiina SALMINEN , Tomi Airenne , Mark Johnson , Heidi Kidron , Yvonne Nymalm-Rejstrom , Annu Sõderholm , David Smith , Marjo Pihlavisto , Lenita Viitanen , Olli Pentikãinen , Tommi Nyrônen
IPC分类号: C07K14/00 , C07C243/14 , C07C243/22 , G06T17/00
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 detections of same. The invention further relates to inhibitors identified by the assays according to the present invention.
摘要翻译: 本发明涉及结晶血管粘附蛋白-1(VAP-1),特别涉及使用结晶人VAP-1的结构信息用于配体和/或抑制剂鉴定,设计和生产以及筛选测定法 用于检测相同。 本发明还涉及通过根据本发明的测定法鉴定的抑制剂。
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公开(公告)号:US07499847B2
公开(公告)日:2009-03-03
申请号:US10557188
申请日:2004-05-25
申请人: Tiina Salminen , Tomi Airenne , Mark Johnson , Heidi Kidron , Yvonne Nymalm-Rejström , Annu Söderholm , David Smith , Marjo Pihlavisto , Lenita Viitanen , Olli Pentikäinen , Tommi Nyrönen
发明人: Tiina Salminen , Tomi Airenne , Mark Johnson , Heidi Kidron , Yvonne Nymalm-Rejström , Annu Söderholm , David Smith , Marjo Pihlavisto , Lenita Viitanen , Olli Pentikäinen , Tommi Nyrönen
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.
摘要翻译: 本发明涉及结晶血管粘附蛋白-1(VAP-1),特别涉及使用结晶人VAP-1的结构信息用于配体和/或抑制剂鉴定,设计和生产以及筛选测定法 用于检测相同。 本发明还涉及通过根据本发明的测定法鉴定的抑制剂。
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公开(公告)号:US20080255169A1
公开(公告)日:2008-10-16
申请号:US10593186
申请日:2004-07-12
申请人: David Smith , Anne Marjamaki , Marika Ojala , Marjo Pihlavisto , Jyrki Heino , Jarmo Kapyla , Olli Pentikainen , Tommi Nyronen , Mark Johnson , Mikko Huhtala
发明人: David Smith , Anne Marjamaki , Marika Ojala , Marjo Pihlavisto , Jyrki Heino , Jarmo Kapyla , Olli Pentikainen , Tommi Nyronen , Mark Johnson , Mikko Huhtala
IPC分类号: A61K31/18 , C07C311/21 , C07D209/88 , C07D333/34 , C07D239/42 , C07D277/62 , C07D209/08 , C07D207/335 , C07D263/54 , C07D213/52 , A61K31/505 , A61K31/44 , A61K31/428 , A61K31/421 , A61K31/4164 , A61K31/404
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 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).
摘要翻译: 本发明涉及式(I)的磺酰胺衍生物,其中R C是任选取代的含有一个或多个N原子的4-元杂环或R C C 与其连接的苯环连同苯并二恶唑基,或R 1是-NR 1 R 2,R A 具有式R B的基团是氢或烷基。 本发明还涉及式(I)的衍生物作为胶原受体整联蛋白的抑制剂的用途和制备式(I)的磺酰胺的方法。
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公开(公告)号:US20090023735A1
公开(公告)日:2009-01-22
申请号:US12066950
申请日:2006-09-15
申请人: Jyrki Heino , Mark Johnson , Jarmo Kapyla , Anne Marjamaki , Tommi Nyronen , Marika Ojala , Olli Pentikainen , Marjo Pihlavisto , Liisa Nissinen
发明人: Jyrki Heino , Mark Johnson , Jarmo Kapyla , Anne Marjamaki , Tommi Nyronen , Marika Ojala , Olli Pentikainen , Marjo Pihlavisto , Liisa Nissinen
IPC分类号: A61K31/18 , A61P7/02 , A61P29/00 , A61P35/00 , C07D261/08 , C07C311/21 , A61K31/4164 , A61K31/44 , C07D295/10 , C07D233/61 , C07D213/52 , A61K31/5377 , A61K31/42
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).
摘要翻译: 本发明涉及式(I)的磺酰胺衍生物,其中RC选自二烷基氨基,NO 2,CN,氨基羰基,单烷基氨基羰基,二烷基氨基羰基,烷酰基,恶唑-2-基,恶唑基氨基羰基,芳基,芳酰基,芳基-CH (OH) - ,芳基氨基羰基,呋喃基,其中芳基,芳酰基和呋喃基部分可以被取代,胍基 - (CH 2)z N(R') - ,Het-(CH 2)z N(R') - ,Het-CO-N (R') - ,Het-CH(OH) - 和Het-CO-,其中Het是含有一个或多个N,S和O的杂原子的任选取代的4-6元杂环,R'是氢或 烷基,z为整数1〜5; RA是权利要求中定义的式(A),(B),(C)或(D)的基团; 并且RB是氢,烷基,烷酰基,羟基烷基,烷氧基烷基,烷氧基羰基,烷氧基羰基烷基,氨基烷基,单或二烷基氨基烷基或Het-烷基,其中Het如上所定义。 本发明还涉及式(I)的衍生物作为胶原受体整合蛋白的抑制剂的用途和制备式(II)的磺酰胺的方法。
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公开(公告)号:US20080197641A1
公开(公告)日:2008-08-21
申请号:US12067160
申请日:2006-08-17
申请人: Jyrki Heino , Mark Johnson , Jarmo Kapyla , Arne Marjamaki , Tommi Nyronen , Marika Ojala , Olli Pentikainen , Marjo Pihlavisto , Liisa Nissinen
发明人: Jyrki Heino , Mark Johnson , Jarmo Kapyla , Arne Marjamaki , Tommi Nyronen , Marika Ojala , Olli Pentikainen , Marjo Pihlavisto , Liisa Nissinen
IPC分类号: E05C19/06
CPC分类号: B64D29/06 , E05B63/0004 , E05C3/14 , F02K1/766 , Y10S292/04 , Y10S292/15 , Y10T292/0894 , Y10T292/0895 , Y10T292/0902 , Y10T292/54
摘要: The invention concerns a catching device (1) between a first structure (2) and a second structure (3), characterized in that it comprises at least one bolt (5) linked to the first structure and mounted in opposition to at least one elastic return means (9) tending to bring it back to a retracted position, a stop means (10) corresponding to the second structure being adapted to maintain it in a taut state when the latter is proximate the first structure, such that when the first structure is rapidly spaced apart from the second structure, each bolt is engaged with at least one corresponding retaining means (4) so as to limit the relative spacing and, when the first structure is slowly spaced apart from the second structure, each bolt and corresponding retaining means remain separated, thereby allowing complete opening between the first structure and the second structure.
摘要翻译: 本发明涉及一种在第一结构(2)和第二结构(3)之间的捕获装置(1),其特征在于,其包括至少一个连接到第一结构的螺栓(5),并且与至少一个弹性 返回装置(9)倾向于将其返回到缩回位置,对应于第二结构的停止装置(10)适于在后者靠近第一结构时将其保持在拉紧状态,使得当第一结构 与第二结构快速间隔开,每个螺栓与至少一个对应的保持装置(4)接合,以便限制相对间隔,并且当第一结构与第二结构缓慢间隔开时,每个螺栓和对应的保持 装置保持分离,从而允许在第一结构和第二结构之间完全打开。
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公开(公告)号:US20080255028A1
公开(公告)日:2008-10-16
申请号:US12066955
申请日:2004-09-15
申请人: Jyrki Heino , Mark Johnson , Jarmo Kapyla , Anne Marjamaki , Tommi Nyronen , Marika Ojala , Olli Pentikainen , Liisa Nissinen
发明人: Jyrki Heino , Mark Johnson , Jarmo Kapyla , Anne Marjamaki , Tommi Nyronen , Marika Ojala , Olli Pentikainen , Liisa Nissinen
CPC分类号: C07C311/21 , C07C311/53 , C07K14/705 , G01N33/6803 , G01N2333/7055 , G16H50/50 , Y02A90/26
摘要: The present invention relates to a refined and detailed molecular model of the α2⊕1 integrin I-domain, especially the MIDAS and to the use of such a model for designing novel integrin modulators, especially α2β1 integrin modulators. The present invention further relates to novel α2β1 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
摘要翻译: 本发明涉及α2⊕1整合素I结构域,特别是MIDAS的精制和详细的分子模型,以及使用这种模型来设计新的整联蛋白调节剂,特别是α2β1整合素调节剂。 本发明还涉及具有治疗潜力的新型α2β1I结构域调节剂。 本发明还涉及与胶原受体,四环聚酮化合物和磺酰胺相互作用的小分子调节剂的特定家族。 本发明还涉及这种调节剂用于制造用于血栓形成,炎症和/或癌症的药物的用途
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公开(公告)号:US20090286713A9
公开(公告)日:2009-11-19
申请号:US12066955
申请日:2006-09-15
申请人: Jyrki Heino , Mark Johnson , Jarmo Kapyla , Anne Marjamaki , Tommi Nyronen , Marika Ojala , Olli Pentikainen , Liisa Nissinen
发明人: Jyrki Heino , Mark Johnson , Jarmo Kapyla , Anne Marjamaki , Tommi Nyronen , Marika Ojala , Olli Pentikainen , Liisa Nissinen
CPC分类号: C07C311/21 , C07C311/53 , C07K14/705 , G01N33/6803 , G01N2333/7055 , G16H50/50 , Y02A90/26
摘要: The present invention relates to a refined and detailed molecular model of the α2⊕1 integrin I-domain, especially the MIDAS and to the use of such a model for designing novel integrin modulators, especially α2β1 integrin modulators. The present invention further relates to novel α2β1 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
摘要翻译: 本发明涉及α2⊕1整合素I结构域,特别是MIDAS的精制和详细的分子模型,以及使用这种模型来设计新的整联蛋白调节剂,特别是α2β1整合素调节剂。 本发明还涉及具有治疗潜力的新型α2β1I结构域调节剂。 本发明还涉及与胶原受体,四环聚酮化合物和磺酰胺相互作用的小分子调节剂的特定家族。 本发明还涉及这种调节剂用于制造用于血栓形成,炎症和/或癌症的药物的用途
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公开(公告)号:US07465739B2
公开(公告)日:2008-12-16
申请号:US10861907
申请日:2004-06-07
申请人: Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Pentikaeinen , Tommi Nyroenen , Tiina Salminen , Mark Johnson , Pekka Lehtovuori
发明人: Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Pentikaeinen , Tommi Nyroenen , Tiina Salminen , Mark Johnson , Pekka Lehtovuori
IPC分类号: A01N43/54 , A61K31/505 , C07D471/00 , C07D487/00
CPC分类号: C07D495/04 , A61K31/519
摘要: Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17β-hydroxysteroid dehydrogenase enzymes.
摘要翻译: 噻吩并嘧啶酮化合物及其在治疗中的用途,特别是用于治疗和/或预防类固醇激素依赖性疾病或病症,例如类固醇激素依赖性疾病或需要抑制17β-羟类固醇脱氢酶的病症。
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公开(公告)号:US20050176742A1
公开(公告)日:2005-08-11
申请号:US11011744
申请日:2004-12-15
申请人: Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Pentikaeinen , Tommi Nyroenen , Tiina Salminen , Mark Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
发明人: Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Pentikaeinen , Tommi Nyroenen , Tiina Salminen , Mark Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
IPC分类号: A61K31/519 , C07D495/04 , C07D498/02
CPC分类号: C07D495/04 , A61K31/519
摘要: Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17β-hydroxysteroid dehydrogenase enzymes.
摘要翻译: 噻吩并嘧啶酮化合物及其在治疗中的用途,特别是用于治疗和/或预防类固醇激素依赖性疾病或病症,例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶的病症。
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