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1. 发明申请

US20080300237A1 Pharmaceutically Active Diazepanes 审中-公开
标题翻译：药用活性二氮杂环庚烷
公开(公告)号：US20080300237A1
公开(公告)日：2008-12-04
申请号：US11911876
申请日：2006-04-19
申请人： Berndt Oberhauser , Dieter Scholz
发明人： Berndt Oberhauser , Dieter Scholz
IPC分类号： A61K31/551 , C07D243/08
CPC分类号： C07D405/12 , C07D243/08 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Leukocyte Function-Associated Antigen One (LFA-1) is a cell adhesion molecule selectively expressed on leukocytes, and plays a major role in the activation and trafficking of T lymphocytes in the tissue at sites of inflammation. In the last decade a large body of preclinical data has accumulated to establish the importance of LFA-1 as a biological target, 10 particularly in chronic, T-cell driven inflammatory conditions. The present invention provides pharmaceutically active 1,4-diazepan-2-ones of formula I useful for the treatment of conditions related to LFA-1 activity.
摘要翻译：白细胞功能相关抗原一（LFA-1）是在白细胞上选择性表达的细胞粘附分子，在炎症部位组织中T淋巴细胞的活化和运输中起主要作用。在过去十年中，积累了大量临床前数据，以确定LFA-1作为生物靶标的重要性，特别是在慢性，T细胞驱动的炎症病症中。本发明提供可用于治疗与LFA-1活性相关的病症的式I的药学活性的1,4-二氮杂环庚烷-2-酮。

2. 发明授权

US6011136A Cyclopeptolides 失效
标题翻译：环磷酰胺
公开(公告)号：US6011136A
公开(公告)日：2000-01-04
申请号：US68915
申请日：1998-06-25
申请人： Michael Morris Dreyfuss , Theodor Fehr , Carolyn Ann Foster , Dieter Geyl , Berndt Oberhauser
发明人： Michael Morris Dreyfuss , Theodor Fehr , Carolyn Ann Foster , Dieter Geyl , Berndt Oberhauser
IPC分类号： C12P21/02 , A61K31/00 , A61K38/00 , A61K38/12 , A61K38/15 , A61P3/00 , A61P3/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08 , C07K1/02 , C07K7/64 , C07K11/02 , C12N1/14 , C12P21/04 , C12R1/645 , A61K38/08 , C07K5/12
CPC分类号： C12R1/645 , C07K11/02 , A61K38/00
摘要： Cyclopeptolides of formula (I), wherein A, B, R.sub.1 Leu, Leu, C, X and Y are as defined, are inhibitors of adhesion molecule, expression and inhibitors of TNF release and are thus useful for treatment of inflammatory and other diseases which involve increased levels of adhesion molecule expression and/or are mediated by TNF. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 05123 Sec。 371日期：1998年6月25日第 102（e）1998年6月25日PCT PCT 1996年11月11日PCT公布。第WO97 / 19104号公报日期：1997年5月29日其中A，B，R1Leu，Leu，C，X和Y如上定义的式（I）的环磷酰哌啶是粘附分子，TNF和释放抑制剂的抑制剂，因此可用于治疗炎症和涉及增加粘附分子表达水平和/或由TNF介导的其它疾病。

3. 发明授权

US07419976B2 Diazepanes derivatives useful as IFA inhibitors 失效
标题翻译：二氮杂衍生物可用作IFA抑制剂
公开(公告)号：US07419976B2
公开(公告)日：2008-09-02
申请号：US10541183
申请日：2004-01-22
申请人： Berndt Oberhauser , Josef G Meingassner
发明人： Berndt Oberhauser , Josef G Meingassner
IPC分类号： C07D403/06 , C07D403/14 , A61K31/5513 , A61P37/08
CPC分类号： C07D401/06 , C07D243/08 , C07D401/14 , C07D405/06
摘要： Pharmaceutically active diazepanes, e.g. useful for treating disorders or diseases mediated by LFA-1/ICAM-1, LFA-1/ICAM-2, LFA-1/ICAM-3 or LFA-1/JAM-1 interactions.
摘要翻译：药用活性二氮杂可用于治疗由LFA-1 / ICAM-1，LFA-1 / ICAM-2，LFA-1 / ICAM-3或LFA-1 / JAM-1相互作用介导的疾病或疾病。

4. 发明申请

US20060148780A1 Diazepanes derivatives useful as ifa inhibitors 失效
标题翻译：作为ifa抑制剂有用的二氮杂环庚烷衍生物
公开(公告)号：US20060148780A1
公开(公告)日：2006-07-06
申请号：US10541183
申请日：2004-01-22
申请人： Berndt Oberhauser , Josef Meingassner
发明人： Berndt Oberhauser , Josef Meingassner
IPC分类号： A61K31/551 , C07D405/02
CPC分类号： C07D401/06 , C07D243/08 , C07D401/14 , C07D405/06
摘要： Pharmaceutically active diazepanes, e.g. useful for treating disorders or diseases mediated by LFA-1/ICAM-1, LFA-1/ICAM-2, LFA-1/ICAM-3 or LFA-1/JAM-1 interactions.
摘要翻译：药用活性二氮杂可用于治疗由LFA-1 / ICAM-1，LFA-1 / ICAM-2，LFA-1 / ICAM-3或LFA-1 / JAM-1相互作用介导的疾病或疾病。

5. 发明授权

US06274322B1 Composition for introducing nucleic acid complexes into higher eucaryotic cells 有权
标题翻译：用于将核酸复合物引入高级真核细胞的组合物
公开(公告)号：US06274322B1
公开(公告)日：2001-08-14
申请号：US09465646
申请日：1999-12-16
申请人： David T. Curiel , Max L. Birnstiel , Matthew Cotten , Ernst Wagner , Kurt Zatloukal , Christian Plank , Berndt Oberhauser , Walter G. M. Schmidt
发明人： David T. Curiel , Max L. Birnstiel , Matthew Cotten , Ernst Wagner , Kurt Zatloukal , Christian Plank , Berndt Oberhauser , Walter G. M. Schmidt
IPC分类号： C12Q168
CPC分类号： C12N15/87 , A61K38/00 , A61K47/50 , A61K47/6901 , A61K48/00 , C07K14/005 , C07K14/56 , C07K14/775 , C07K14/79 , C07K16/00 , C07K16/2803 , C07K2317/77 , C07K2319/00 , C12N7/00 , C12N2710/10251 , C12N2710/10261 , C12N2710/10322 , C12N2710/10351 , C12N2710/10361 , C12N2710/10363 , C12N2740/11022 , C12N2740/15022 , C12N2740/16022 , C12N2740/16122 , C12N2760/16122 , C12N2770/32722 , C12N2770/32761 , Y10T436/143333
摘要： A composition for the transfection of higher eucaryotic cells, comprising complexes of nucleic acid, a substance having an affinity for nucleic acid and optionally an internalizing factor, contains an endosomolytic agent, e.g. a virus or virus component, which may be conjugated. The endosomolytic agent, which is optionally part of the nucleic acid complex, is internalized into the cells together with the complex and releases the contents of the endosomes into the cytoplasm, thereby increasing the gene transfer capacity. Pharmaceutical preparations, transfection kits and methods for introducing nucleic acid into higher eucaryotic cells by treating the cells with the composition are also disclosed.
摘要翻译：用于转染高等真核细胞的组合物，其包含核酸复合物，对核酸和任选的内在因子具有亲和力的物质，含有内体细胞溶解剂可以结合的病毒或病毒组分。任选地是核酸复合物的一部分的内体细胞溶解剂与复合物一起被内化到细胞中，并将内体的内容物释放到细胞质中，从而增加基因转移能力。还公开了药物制剂，转染试剂盒和通过用组合物处理细胞将核酸引入高级真核细胞的方法。

6. 发明授权

US6013627A Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US6013627A
公开(公告)日：2000-01-11
申请号：US776440
申请日：1997-01-24
申请人： Michael Morris Dreyfuss , Carolyn Ann Foster , Hans-Ulrich Naegeli , Berndt Oberhauser
发明人： Michael Morris Dreyfuss , Carolyn Ann Foster , Hans-Ulrich Naegeli , Berndt Oberhauser
IPC分类号： C07K7/06 , A61K8/00 , A61K8/64 , A61K38/00 , A61K38/15 , A61P7/02 , A61P11/00 , A61P17/00 , A61P25/00 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/08 , A61Q19/00 , C07K7/64 , C07K11/02 , C12N1/14 , C12P21/04 , C12R1/645 , A61K38/12 , C07K5/00 , C07K7/00
CPC分类号： C12R1/645 , C07K11/02 , A61K38/00
摘要： Cyclopeptolides of formula I ##STR1## wherein A, B, R, Leu, Leu, C, X and Y are as defined, are inhibitors of adhesion molecule expression and are thus useful for treatment of inflammatory and other diseases which involve increased levels of adhesion molecule expression.
摘要翻译： PCT No.PCT / EP95 / 02966 Sec。 371日期1997年1月24日 102（e）日期1997年1月24日PCT提交1995年7月26日PCT公布。出版物WO96 / 03430 日期1996年2月8日其中A，B，R，Leu，Leu，C，X和Y如上定义的式I的环磷酰哌啶是粘附分子表达的抑制剂，因此可用于治疗炎症和其它涉及增加水平的疾病的粘附分子表达。

7. 发明授权

US08119617B2 aSMase inhibitors 失效
标题翻译： aSMase抑制剂
公开(公告)号：US08119617B2
公开(公告)日：2012-02-21
申请号：US12438437
申请日：2007-08-21
申请人： Karl Baumann , Andreas Billich , Berndt Oberhauser
发明人： Karl Baumann , Andreas Billich , Berndt Oberhauser
IPC分类号： A61K31/66 , C07F9/02 , C07C233/00
CPC分类号： C07D285/10 , C07F9/3882
摘要： The present invention relates to compounds of formula wherein the residues have various meanings and their use as pharmaceuticals.
摘要翻译：本发明涉及式的化合物，其中残基具有各种含义及其作为药物的用途。

8. 发明申请

US20090170914A1 Cermide Kinase Modulation 审中-公开
标题翻译：金属激酶调制
公开(公告)号：US20090170914A1
公开(公告)日：2009-07-02
申请号：US12295375
申请日：2007-03-28
申请人： Frederic Bornancin , Berndt Oberhauser
发明人： Frederic Bornancin , Berndt Oberhauser
IPC分类号： A61K31/423 , C07D277/82
CPC分类号： C07D277/82
摘要： A compound of formula (I) wherein R1 is a straight chain, branched or cyclic aliphatic, aromatic or heterocyclyl group comprising at least 8 carbon atoms, e.g. 8 to 22, R2 is a straight chain, branched or cyclic aliphatic, aromatic or heterocyclic group comprising from 1 to 12 carbon atoms, and ring A is heterocycyl, fused with the phenyl ring to which ring A is attached comprising 5 or 6 ring members, and 1 to 4 heteroatoms selected from N, S, O; wherein certain compounds are excluded by proviso and the use of such compounds without proviso as pharmaceuticals in disorders which are mediated by ceramide kinase.
摘要翻译：式（I）的化合物，其中R 1是包含至少8个碳原子的直链，支链或环状脂族，芳族或杂环基，例如 8至22中，R 2是包含1至12个碳原子的直链，支链或环状脂族，芳族或杂环基团，并且环A是杂环基，与环A连接的苯环稠合，包含5或6个环成员和1至4个选自N，S，O的杂原子; 其中某些化合物被排除在条件之外，并且在没有附带条件下使用这些化合物作为由神经酰胺激酶介导的病症中的药物。

9. 发明授权

US6077663A Composition for introducing nucleic acid complexes into higher eucaryotic cells 失效
标题翻译：用于将核酸复合物引入高级真核细胞的组合物
公开(公告)号：US6077663A
公开(公告)日：2000-06-20
申请号：US449754
申请日：1995-05-25
申请人： David T. Curiel , Max L. Birnstiel , Matthew Cotten , Ernst Wagner , Kurt Zatloukal , Christian Plank , Berndt Oberhauser , Walter G.M. Schmidt
发明人： David T. Curiel , Max L. Birnstiel , Matthew Cotten , Ernst Wagner , Kurt Zatloukal , Christian Plank , Berndt Oberhauser , Walter G.M. Schmidt
IPC分类号： C12N15/09 , A61K35/76 , A61K38/00 , A61K38/21 , A61K38/36 , A61K39/44 , A61K47/48 , A61K48/00 , A61P31/12 , A61P35/00 , C07K14/005 , C07K14/075 , C07K14/095 , C07K14/11 , C07K14/15 , C07K14/16 , C07K14/56 , C07K14/775 , C07K14/79 , C07K16/00 , C07K16/28 , C12N5/10 , C12N7/04 , C12N15/34 , C12N15/41 , C12N15/44 , C12N15/87 , G01N33/00 , C12Q1/68
CPC分类号： C12N15/87 , A61K47/48 , A61K47/48776 , A61K48/00 , C07K14/005 , C07K14/56 , C07K14/775 , C07K14/79 , C07K16/00 , C07K16/2803 , C12N7/00 , A61K38/00 , C07K2317/77 , C07K2319/00 , C12N2710/10251 , C12N2710/10261 , C12N2710/10322 , C12N2710/10351 , C12N2710/10361 , C12N2710/10363 , C12N2740/11022 , C12N2740/15022 , C12N2740/16022 , C12N2740/16122 , C12N2760/16122 , C12N2770/32722 , C12N2770/32761 , Y10T436/143333
摘要： A composition for the transfection of higher eucaryotic cells, comprising complexes of nucleic acid, a substance having an affinity for nucleic acid and optionally an internalizing factor, contains an endosomolytic agent, e.g. a virus or virus component, which may be conjugated. The endosomolytic agent, which is optionally part of the nucleic acid complex, is internalized into the cells together with the complex and releases the contents of the endosomes into the cytoplasm, thereby increasing the gene transfer capacity. Pharmaceutical preparations, transfection kits and methods for introducing nucleic acid into higher eucaryotic cells by treating the cells with the composition are also disclosed.
摘要翻译：用于转染高等真核细胞的组合物，其包含核酸复合物，对核酸和任选的内在因子具有亲和力的物质，含有内体细胞溶解剂可以结合的病毒或病毒组分。任选地是核酸复合物的一部分的内体细胞溶解剂与复合物一起被内化到细胞中，并将内体的内容物释放到细胞质中，从而增加基因转移能力。还公开了药物制剂，转染试剂盒和通过用组合物处理细胞将核酸引入高级真核细胞的方法。

10. 发明授权

US6022735A Composition for introducing nucleic acid complexes into higher eucaryotic cells 失效
公开(公告)号：US6022735A
公开(公告)日：2000-02-08
申请号：US449741
申请日：1995-05-25
申请人： David T. Curiel , Max L. Birnstiel , Matthew Cotten , Ernst Wagner , Kurt Zatloukal , Christian Plank , Berndt Oberhauser , Walter G. M. Schmidt
发明人： David T. Curiel , Max L. Birnstiel , Matthew Cotten , Ernst Wagner , Kurt Zatloukal , Christian Plank , Berndt Oberhauser , Walter G. M. Schmidt
IPC分类号： C12N15/09 , A61K35/76 , A61K38/00 , A61K38/21 , A61K38/36 , A61K39/44 , A61K47/48 , A61K48/00 , A61P31/12 , A61P35/00 , C07K14/005 , C07K14/075 , C07K14/095 , C07K14/11 , C07K14/15 , C07K14/16 , C07K14/56 , C07K14/775 , C07K14/79 , C07K16/00 , C07K16/28 , C12N5/10 , C12N7/04 , C12N15/34 , C12N15/41 , C12N15/44 , C12N15/87 , G01N33/00 , C12N15/63 , C07H21/04 , C12N15/00 , C12Q1/70
CPC分类号： C12N15/87 , A61K47/48 , A61K47/48776 , A61K48/00 , C07K14/005 , C07K14/56 , C07K14/775 , C07K14/79 , C07K16/00 , C07K16/2803 , C12N7/00 , A61K38/00 , C07K2317/77 , C07K2319/00 , C12N2710/10251 , C12N2710/10261 , C12N2710/10322 , C12N2710/10351 , C12N2710/10361 , C12N2710/10363 , C12N2740/11022 , C12N2740/15022 , C12N2740/16022 , C12N2740/16122 , C12N2760/16122 , C12N2770/32722 , C12N2770/32761 , Y10T436/143333
摘要： A composition for the transfection of higher eucaryotic cells, comprising complexes of nucleic acid, a substance having an affinity for nucleic acid and optionally an internalizing factor, contains an endosomolytic agent, e.g. a virus or virus component, which may be conjugated. The endosomolytic agent, which is optionally part of the nucleic acid complex, is internalized into the cells together with the complex and releases the contents of the endosomes into the cytoplasm, thereby increasing the gene transfer capacity. Pharmaceutical preparations, transfection kits and methods for introducing nucleic acid into higher eucaryotic cells by treating the cells with the composition are also disclosed.

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