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公开(公告)号：US20100222396A1
公开(公告)日：2010-09-02
申请号：US12695462
申请日：2010-01-28
申请人： Dirk BEHNKE , Claudia Betschart , Simona Cotesta , Marc Gerspacher , Samuel Hintermann , Bernard Lucien Roy , Anette Von Matt , Jürgen Wagner
发明人： Dirk BEHNKE , Claudia Betschart , Simona Cotesta , Marc Gerspacher , Samuel Hintermann , Bernard Lucien Roy , Anette Von Matt , Jürgen Wagner
IPC分类号： A61K31/44 , C07D207/30 , A61K31/40 , C07D213/81
CPC分类号： C07C233/78 , C07D207/416 , C07D209/08 , C07D213/81 , C07D215/48 , C07D215/50 , C07D217/26 , C07D233/66 , C07D235/24 , C07D277/56 , C07D307/79 , C07D317/68 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译： 本发明涉及式I化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。
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![DIAZA-SPIRO[5.5]UNDECANES USEFUL AS OREXIN RECEPTOR ANTAGONISTS](/abs-image/US/2013/10/24/US20130281463A1/abs.jpg.150x150.jpg)
2.发明申请DIAZA-SPIRO[5.5]UNDECANES USEFUL AS OREXIN RECEPTOR ANTAGONISTS 审中-公开DIAZA-SPIRO [5.5]有机质作为OREXIN受体拮抗剂公开(公告)号：US20130281463A1
公开(公告)日：2013-10-24
申请号：US13880994
申请日：2011-10-25
申请人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Simona Cotesta , Samuel Hintermann , Silvio Ofner , Chetan Pandit , Bernard Lucien Roy
发明人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Simona Cotesta , Samuel Hintermann , Silvio Ofner , Chetan Pandit , Bernard Lucien Roy
IPC分类号： C07D471/10 , A61K45/06 , A61K31/444 , A61K31/506
CPC分类号： C07D471/10 , A61K31/444 , A61K31/506 , A61K45/06 , C07D519/00
摘要： The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译： 本发明涉及式（I）化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。
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公开(公告)号：US08742106B2
公开(公告)日：2014-06-03
申请号：US13517115
申请日：2010-12-20
申请人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Murali Chebrolu , Simona Cotesta , Samuel Hintermann , Arndt Meyer , Chetan Pandit
发明人： Sangamesh Badiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Murali Chebrolu , Simona Cotesta , Samuel Hintermann , Arndt Meyer , Chetan Pandit
IPC分类号： C07D471/04 , C07D498/04 , C07D519/00
CPC分类号： C07D471/04 , C07D498/04 , C07D519/00
摘要： The invention relates to compound of the formula (I′) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译： 本发明涉及式（I'）的化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。
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公开(公告)号：US20120258973A1
公开(公告)日：2012-10-11
申请号：US13517115
申请日：2010-12-20
申请人： Sangamesh Babiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Murali Chebrolu , Simona Cotesta , Samuel Hintermann , Arndt Meyer , Chetan Pandit
发明人： Sangamesh Babiger , Dirk Behnke , Claudia Betschart , Vinod Chaudhari , Murali Chebrolu , Simona Cotesta , Samuel Hintermann , Arndt Meyer , Chetan Pandit
IPC分类号： A61K31/437 , A61P3/00 , A61P25/30 , A61P25/28 , A61K31/4709 , A61K31/506 , A61K31/497 , C07D519/00 , C07D498/04 , A61K31/444 , A61P25/00 , C07D471/04
CPC分类号： C07D471/04 , C07D498/04 , C07D519/00
摘要： The invention relates to compound of the formula (I′) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译： 本发明涉及式（I'）的化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。
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公开(公告)号：US20090281077A1
公开(公告)日：2009-11-12
申请号：US12440440
申请日：2007-09-07
申请人： Samuel Hintermann , Michele Chiesi
发明人： Samuel Hintermann , Michele Chiesi
IPC分类号： A61K31/554 , C07D281/02 , A61P25/00 , A61P9/00
CPC分类号： C07D281/10
摘要： The invention relates to novel heterocyclic compounds of the formula in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译： 本发明涉及游离碱形式或酸加成盐形式的新颖的式杂环化合物，其制备方法，其用作药物和包含它们的药物。
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公开(公告)号：US07160856B2
公开(公告)日：2007-01-09
申请号：US10205021
申请日：2002-07-25
申请人： Samuel J. Danishefsky , Dalibor Sames , Samuel Hintermann , Xiao Tao Chen , Jacob B. Schwarz , Peter Glunz , Govindaswami Ragupathi , Philip O. Livingston , Scott Kuduk , Lawrence Williams
发明人： Samuel J. Danishefsky , Dalibor Sames , Samuel Hintermann , Xiao Tao Chen , Jacob B. Schwarz , Peter Glunz , Govindaswami Ragupathi , Philip O. Livingston , Scott Kuduk , Lawrence Williams
IPC分类号： A61K38/14 , A61K39/385 , C07K9/00
CPC分类号： C07K14/4727 , A61K38/00 , A61K39/00 , C07K9/001
摘要： The present invention provides novel α-O-linked glycoconjugates such as α-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the α-O-linked glycoconjugates.
摘要翻译： 本发明提供了新的α-O-连接的糖缀合物，例如α-O-连接的糖肽，以及用于合成它们的收敛方法。 通常的制备方法通过上皮肿瘤细胞表面上通常发现的粘蛋白基序的合成来举例说明。 本发明还提供了使用α-O-连接的糖缀合物治疗癌症的组合物和方法。
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公开(公告)号：US07550146B2
公开(公告)日：2009-06-23
申请号：US10898410
申请日：2004-07-23
申请人： Samuel J. Danishefsky , Dalibor Sames , Samuel Hintermann , Peter Glunz , Govindaswami Ragupathi , Philip O. Livingston , Kenneth O. Lloyd , Valery Kudryashov
发明人： Samuel J. Danishefsky , Dalibor Sames , Samuel Hintermann , Peter Glunz , Govindaswami Ragupathi , Philip O. Livingston , Kenneth O. Lloyd , Valery Kudryashov
IPC分类号： A61K38/14 , A61K39/385 , C07K9/00
CPC分类号： C07H5/06
摘要： The present invention provides novel glycoconjugates such as glycopeptides, as well as convergent methods for the synthesis thereof. An exemplary preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the glycoconjugates of the invention.
摘要翻译： 本发明提供了新的糖缀合物，如糖肽，以及其合成方法。 通过合成通常在上皮肿瘤细胞表面上发现的粘蛋白基序来举例说明一个示例性的制备方法。 本发明还提供了使用本发明的糖缀合物治疗癌症的组合物和方法。
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公开(公告)号：US07087756B2
公开(公告)日：2006-08-08
申请号：US10486569
申请日：2002-08-14
IPC分类号： C07D471/02
CPC分类号： C07D498/04
摘要： The invention provides compounds of formula I, wherein X, Y, R1, R2, and R3 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.
摘要翻译： 本发明提供式I化合物，其中X，Y，R 1，R 2和R 3是如说明书中所定义的， 及其制备。 式I的化合物可用作药物。
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公开(公告)号：US20100137340A1
公开(公告)日：2010-06-03
申请号：US12529593
申请日：2008-03-03
IPC分类号： A61K31/519 , C07D487/04 , A61P1/00 , A61P13/00 , A61P25/16 , A61P25/28 , A61P25/00 , A61P25/30
CPC分类号： C07D487/04 , C07D473/30 , C07D498/04 , C07D519/00
摘要： The invention relates to compounds of Formula (I) wherein the substituents are as defined in claim 1; to compositions comprising said compounds and to their use as pharmaceutical agents.
摘要翻译： 本发明涉及式（I）的化合物，其中取代基如权利要求1所定义; 包含所述化合物的组合物和它们作为药剂的用途。
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![Benzo[1,2,5]oxadiazoles and benzol[1,2,5]thiadiazoles useful as histopathological staining agents, imaging agents and biomarkers](/abs-image/US/2006/05/04/US20060093551A1/abs.jpg.150x150.jpg)
10.发明申请Benzo[1,2,5]oxadiazoles and benzol[1,2,5]thiadiazoles useful as histopathological staining agents, imaging agents and biomarkers 失效可用作组织病理学染色剂的苯并[1,2,5]恶二唑和苯并[1,2,5]噻二唑，成像剂和生物标志物公开(公告)号：US20060093551A1
公开(公告)日：2006-05-04
申请号：US10549248
申请日：2004-04-02
IPC分类号： A61K51/00 , C07D417/02 , C07D413/02
CPC分类号： C07D271/12 , A61K47/6813 , C07D285/14
摘要： The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R1 is 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-18F-ethylamino)-thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R2 is NHCH3, NH11CH3, N(CH3)11CH3, N(CH3)2, N(11CH3)2, NH(CH2)nF, NH(CH2)n18F, N(CH3)(CH2)nF, N(CH3)—(CH2)n 18F, O—(CH2)nF, O—(CH2)n 18F, CONH(CH2)nF or CONH(CH2)n18F (n being in each case 2 to 4) and R3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.
摘要翻译： 本发明涉及式（I）的新的苯并[1,2,5]恶二唑和苯并[1,2,5]噻二唑，其中X是O或S，R 1是5-（ 2-（2-氟 - 乙基氨基） - 噻唑-2-基，5-（2-叔丁基乙基氨基） - 噻唑-2-基或式（a）的基团，其中Y是CH或N R 2是NHCH 3，NH 11，CH 3，N（CH 3）3 N（CH 3）2 N，N（11）O，N（CH 3）2 N， NH（CH 2）n，NH（CH 2）2，NH（CH 2）n， / SUB>）N（CH 3）（CH 2）n N（CH 3） F，N（CH 3） - （CH 2 CH 2）n F 18，F（O） CH 2，N 2，CH 2，CH 2，CH 2，CH 2，CH 2， ，CONH（CH 2 CH 2）n F或CONH（CH 2 CH 2）n（n）在每种情况下 2〜4），R 3为羟基，（C 1-4）烷氧基，氢或硝基，为游离碱或酸加成盐形式; 它们的制备，它们在诊断中的用途和含有它们的组合物。
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