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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: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: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: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:US20120196884A1
公开(公告)日:2012-08-02
申请号:US13378503
申请日:2010-06-14
申请人: Jarkko Tapani Koivunen , Jani Korhonen , Anne Marjamäki , Liisa Nissinen , Marjo Pihlavisto , Olli Taneli Pentikäinen
发明人: Jarkko Tapani Koivunen , Jani Korhonen , Anne Marjamäki , Liisa Nissinen , Marjo Pihlavisto , Olli Taneli Pentikäinen
IPC分类号: A61K31/18 , C07D209/42 , A61K31/404 , C07D231/18 , A61K31/415 , C07D409/04 , A61K31/4155 , C07D413/04 , A61K31/422 , A61K31/4436 , C07D401/04 , A61K31/4439 , C07D417/04 , A61K31/427 , A61K31/4245 , C07D333/34 , A61K31/381 , C07D233/84 , A61K31/4164 , C07D409/14 , C07D277/36 , C07D319/18 , A61K31/357 , C07D213/71 , A61K31/4418 , C07D213/54 , A61K31/506 , C07D231/12 , A61K31/4535 , A61P7/02 , A61P29/00 , A61P35/00 , A61P9/00 , A61P1/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P11/06 , A61P37/08 , C07C303/40 , C07C303/38 , C07C311/44 , C07C311/29 , A61K31/277 , C07C311/21
CPC分类号: C07D213/75 , C07C311/21 , C07C311/29 , C07C311/47 , C07D209/08 , C07D213/34 , C07D213/40 , C07D213/71 , C07D213/76 , C07D231/12 , C07D231/18 , C07D231/38 , C07D231/40 , C07D233/84 , C07D277/36 , C07D319/18 , C07D333/34 , C07D401/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
摘要: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially α2β1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I′).
摘要翻译: 本发明涉及一种尿素部分的磺酰胺衍生物。 本发明还涉及衍生物作为胶原受体整合素抑制剂的用途,特别是α2和bgr1整联蛋白抑制剂。 涉及涉及表达胶原受体的细胞和血小板的作用的疾病和医学病症,它们作为药物的用途,例如, 用于治疗血栓形成,炎症,癌症和血管疾病,含有它们的药物组合物及其制备方法。 磺酰胺衍生物具有通式(I)或(I')。
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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:US20140024648A1
公开(公告)日:2014-01-23
申请号:US14003626
申请日:2012-03-06
申请人: Marjo Pihlavisto , David Smith , Auni Juhakoski , Ferenc Fulop , Laszlo Lazar , Istvan Szatmari , Ferenc Miklos , Zsolt Szakonyi , Lorand Kiss , Marta Palko
发明人: Marjo Pihlavisto , David Smith , Auni Juhakoski , Ferenc Fulop , Laszlo Lazar , Istvan Szatmari , Ferenc Miklos , Zsolt Szakonyi , Lorand Kiss , Marta Palko
IPC分类号: C07D237/24 , A61K31/501 , A61K45/06 , A61K31/50 , C07D403/12 , C07D401/04 , C07D405/04 , C07D413/04 , C07D409/04 , C07D403/14 , A61K31/5377 , C07D401/14 , C07D237/16 , C07D405/14 , G01N33/50 , C07D403/04
CPC分类号: C07D237/24 , A61K31/4439 , A61K31/496 , A61K31/50 , A61K31/501 , A61K31/5377 , A61K45/06 , C07C57/15 , C07D237/16 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , G01N33/502
摘要: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I′), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.
摘要翻译: 本发明涉及具有式(I)或(I')的哒嗪酮和吡啶酮化合物及其药学上可接受的盐,水合物和溶剂合物(I),其中R1 / R4和X和X3如权利要求中所定义。 本发明还涉及它们作为含铜胺氧化酶抑制剂的用途。 本发明还涉及上述化合物的制备以及包含一种或多种上述化合物,药学上可接受的盐,水合物或溶剂合物作为活性成分的药物组合物。
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公开(公告)号:US20130195883A1
公开(公告)日:2013-08-01
申请号:US13395029
申请日:2010-09-07
申请人: Christopher Weston , Lee Charles Claridge , David Adam , David Smith , Nina Westerlund , Marjo Pihlavisto , Thua Österman
发明人: Christopher Weston , Lee Charles Claridge , David Adam , David Smith , Nina Westerlund , Marjo Pihlavisto , Thua Österman
IPC分类号: A61K39/395 , A61K31/185 , G01N33/573 , A61K31/137
CPC分类号: A61K39/3955 , A61K31/00 , A61K31/137 , A61K31/185 , A61K2039/505 , C07K16/40 , C07K2317/76 , G01N33/573 , G01N33/6893 , G01N2333/90638 , G01N2800/085
摘要: The present invention relates to inhibitors of VAP-1 and their use as medicaments in treating fibrotic conditions. Furthermore, the present invention relates to a method of diagnosing a fibrotic condition on the basis of elevated level of soluble VAP-1 or SSAO activity in a bodily fluid, and to a kit for use in said diagnostic method.
摘要翻译: 本发明涉及VAP-1抑制剂及其作为药物治疗纤维化病症的用途。 此外,本发明涉及一种基于体液中可溶性VAP-1或SSAO活性水平升高以及用于所述诊断方法的试剂盒诊断纤维化病症的方法。
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公开(公告)号:US09795671B2
公开(公告)日:2017-10-24
申请号:US13395029
申请日:2010-09-07
申请人: Christopher Weston , Lee Charles Claridge , David Adams , David Smith , Nina Westerlund , Max Ole Valdemar Westerlund , Marjo Pihlavisto , Thua Österman , Elina Ainomaija Antikainen
发明人: Christopher Weston , Lee Charles Claridge , David Adams , David Smith , Nina Westerlund , Marjo Pihlavisto , Thua Österman
IPC分类号: A61K39/395 , A61K39/00 , C07K16/00 , C12P21/08 , A61K31/00 , C07K16/40 , G01N33/68 , A61K31/137 , A61K31/185 , G01N33/573
CPC分类号: A61K39/3955 , A61K31/00 , A61K31/137 , A61K31/185 , A61K2039/505 , C07K16/40 , C07K2317/76 , G01N33/573 , G01N33/6893 , G01N2333/90638 , G01N2800/085
摘要: The present invention relates to inhibitors of VAP-1 and their use as medicaments in treating fibrotic conditions. Furthermore, the present invention relates to a method of diagnosing a fibrotic condition on the basis of elevated level of soluble VAP-1 or SSAO activity in a bodily fluid, and to a kit for use in said diagnostic method.
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