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1. 发明申请

US20140294865A1 AMATOXIN-CONJUGATES WITH IMPROVED LINKAGES 审中-公开
标题翻译：具有改进的链接的AMATOXIN-CONJUGATE
公开(公告)号：US20140294865A1
公开(公告)日：2014-10-02
申请号：US14004183
申请日：2012-03-09
申请人： Werner Simon , Christian Lutz , Christoph Muller , Jan Anderl
发明人： Werner Simon , Christian Lutz , Christoph Muller , Jan Anderl
IPC分类号： A61K47/48 , A61K38/12
CPC分类号： A61K47/6813 , A61K38/12 , A61K47/61 , A61K47/64 , A61K47/66 , A61K47/6831 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K47/6891
摘要： The invention relates to tumor therapy. In one aspect, the present invention relates to conjugates of an amatoxin and a target-binding moiety, e.g. an antibody, connected by certain linkages, which are useful in the treatment of cancer. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates.
摘要翻译：本发明涉及肿瘤治疗。在一个方面，本发明涉及阿莫地辛和靶结合部分的缀合物，例如，通过某些连接连接的抗体，其可用于治疗癌症。在另一方面，本发明涉及包含这种缀合物的药物组合物。

2. 发明申请

US20180185509A1 AMATOXIN-CONJUGATES WITH IMPROVED LINKAGES 审中-公开
公开(公告)号：US20180185509A1
公开(公告)日：2018-07-05
申请号：US15728170
申请日：2017-10-09
申请人： Werner Simon , Christian Lutz , Christoph Müller , Jan Anderl
发明人： Werner Simon , Christian Lutz , Christoph Müller , Jan Anderl
IPC分类号： A61K47/68 , A61K38/12 , A61K47/64 , A61K47/61 , A61K47/66
CPC分类号： A61K47/6813 , A61K38/12 , A61K47/61 , A61K47/64 , A61K47/66 , A61K47/6831 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K47/6891
摘要： The present disclosure relates to tumour therapy. In one aspect, the present disclosure relates to conjugates of an amatoxin and a target-binding moiety, e.g. an antibody, connected by certain linkages, which are useful in the treatment of cancer. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates.

3. 发明申请

US20130259880A1 Amatoxin-Conjugates with Improved Linkers 有权
标题翻译：具有改进连接子的Am毒素缀合物
公开(公告)号：US20130259880A1
公开(公告)日：2013-10-03
申请号：US13876829
申请日：2011-09-29
申请人： Jan Anderl , Werner Simon , Christoph Mueller
发明人： Jan Anderl , Werner Simon , Christoph Mueller
IPC分类号： C07K16/30
CPC分类号： C07K16/30 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855
摘要： The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of an amatoxin and a target-binding moiety, e.g. an antibody, connected by a linker comprising a urea moiety, which are useful in the treatment of cancer. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates.
摘要翻译：本发明涉及肿瘤治疗。在一个方面，本发明涉及阿莫地辛和靶结合部分的缀合物，例如，通过包含尿素部分的接头连接的抗体，其可用于治疗癌症。在另一方面，本发明涉及包含这种缀合物的药物组合物。

4. 发明授权

US09399681B2 Amatoxin-conjugates with improved linkers 有权
标题翻译：具有改良接头的氨氧化还原偶联物
公开(公告)号：US09399681B2
公开(公告)日：2016-07-26
申请号：US13876829
申请日：2011-09-29
申请人： Jan Anderl , Werner Simon , Christoph Mueller
发明人： Jan Anderl , Werner Simon , Christoph Mueller
IPC分类号： A61K47/48 , C07K16/30
CPC分类号： C07K16/30 , A61K47/6811 , A61K47/6849 , A61K47/6851 , A61K47/6855
摘要： The invention relates to tumor therapy. In one aspect, the present invention relates to conjugates of an amatoxin and a target-binding moiety, e.g. an antibody, connected by a linker comprising a urea moiety, which are useful in the treatment of cancer. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates.
摘要翻译：本发明涉及肿瘤治疗。在一个方面，本发明涉及阿莫地辛和靶结合部分的缀合物，例如，通过包含尿素部分的接头连接的抗体，其可用于治疗癌症。在另一方面，本发明涉及包含这种缀合物的药物组合物。

5. 发明申请

US20120100161A1 Amatoxin-Armed Therapeutic Cell Surface Binding Components Designed for Tumour Therapy 有权
标题翻译：用于肿瘤治疗的Amatoxin-Armed治疗细胞表面结合组分
公开(公告)号：US20120100161A1
公开(公告)日：2012-04-26
申请号：US13263287
申请日：2010-04-08
申请人： Heinz Faulstich , Gerhard Moldenhauer , Werner Simon , Jan Anderl , Christoph Müller
发明人： Heinz Faulstich , Gerhard Moldenhauer , Werner Simon , Jan Anderl , Christoph Müller
IPC分类号： A61K39/395 , C07K16/30 , C07K16/40 , C07K16/18 , A61P35/00 , A61P37/06 , A61P35/02 , A61P3/10 , A61P7/06 , A61P17/06 , A61P19/02 , A61P1/16 , A61P29/00 , A61P25/18 , A61P9/00 , C07K16/00
CPC分类号： A61K47/48492 , A61K47/6831 , A61K47/6849 , A61K47/6851 , A61K47/6855 , C07K16/30 , C07K16/32 , C07K2317/24 , C07K2317/56 , C07K2317/73 , C07K2317/92
摘要： The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of a toxin and a target-binding moiety, e.g. an antibody, which are useful in the treatment of cancer. In particular, the toxin is an amatoxin, and the target-binding moiety is preferably directed against tumour-associated antigens. In particular, the amatoxin is conjugated to the antibody by linker moieties. In particular the linker moieties are covalently bound to functional groups located in positions of the amatoxin proved as preferred positions for the attachment of linkers with respect to optimum antitumor activity. In a further aspect the invention relates to pharmaceutical compositions comprising such target-binding moiety toxin conjugates and to the use of such target-binding moiety toxin conjugates for the preparation of such pharmaceutical compositions. The target-binding moiety toxin conjugates and pharmaceutical compositions of the invention are useful for the treatment of cancer.
摘要翻译：本发明涉及肿瘤治疗。在一个方面，本发明涉及毒素和靶结合部分的缀合物，例如，抗体，其可用于治疗癌症。特别地，毒素是一种amatoxin，靶结合部分优选针对肿瘤相关抗原。特别地，通过接头部分将该amatoxin与抗体结合。特别地，连接体部分共价结合到位于氨苄西毒素位置的官能团，其被证明作为关于最佳抗肿瘤活性的连接子的优选位置。在另一方面，本发明涉及包含这种靶结合部分毒素缀合物的药物组合物以及这种靶结合部分毒素缀合物用于制备这种药物组合物的用途。靶结合部分毒素缀合物和本发明的药物组合物可用于治疗癌症。

6. 发明授权

US09233173B2 Amatoxin-armed therapeutic cell surface binding components designed for tumour therapy 有权
标题翻译：设计用于肿瘤治疗的阿片剂药物治疗细胞表面结合组分
公开(公告)号：US09233173B2
公开(公告)日：2016-01-12
申请号：US13263287
申请日：2010-04-08
申请人： Heinz Faulstich , Gerhard Moldenhauer , Werner Simon , Jan Anderl , Christoph Müller
发明人： Heinz Faulstich , Gerhard Moldenhauer , Werner Simon , Jan Anderl , Christoph Müller
IPC分类号： A61K47/48 , C07K16/30 , A61K39/395 , A61K39/00
CPC分类号： A61K47/48492 , A61K47/6831 , A61K47/6849 , A61K47/6851 , A61K47/6855 , C07K16/30 , C07K16/32 , C07K2317/24 , C07K2317/56 , C07K2317/73 , C07K2317/92
摘要： The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of a toxin and a target-binding moiety, e.g. an antibody, which are useful in the treatment of cancer. In particular, the toxin is an amatoxin, and the target-binding moiety is preferably directed against tumour-associated antigens. In particular, the amatoxin is conjugated to the antibody by linker moieties. In particular the linker moieties are covalently bound to functional groups located in positions of the amatoxin proved as preferred positions for the attachment of linkers with respect to optimum antitumor activity. In a further aspect the invention relates to pharmaceutical compositions comprising such target-binding moiety toxin conjugates and to the use of such target-binding moiety toxin conjugates for the preparation of such pharmaceutical compositions. The target-binding moiety toxin conjugates and pharmaceutical compositions of the invention are useful for the treatment of cancer.
摘要翻译：本发明涉及肿瘤治疗。在一个方面，本发明涉及毒素和靶结合部分的缀合物，例如，抗体，其可用于治疗癌症。特别地，毒素是一种amatoxin，靶结合部分优选针对肿瘤相关抗原。特别地，通过接头部分将该amatoxin与抗体结合。特别地，连接体部分共价结合到位于氨苄西毒素位置的官能团，其被证明作为关于最佳抗肿瘤活性的连接子的优选位置。在另一方面，本发明涉及包含这种靶结合部分毒素缀合物的药物组合物以及这种靶结合部分毒素缀合物用于制备这种药物组合物的用途。靶结合部分毒素缀合物和本发明的药物组合物可用于治疗癌症。

7. 发明授权

US07459462B2 Fredericamycin derivatives 失效
标题翻译：弗雷德霉素衍生物
公开(公告)号：US07459462B2
公开(公告)日：2008-12-02
申请号：US10511411
申请日：2003-03-28
申请人： Werner Simon , Ulrich Abel
发明人： Werner Simon , Ulrich Abel
IPC分类号： A61K31/473 , C07D221/20
CPC分类号： C07D221/20 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04
摘要： The invention relates to novel fredericamycin derivatives, to medicaments containing these derivatives or salts thereof, and to the use of fredericamycin derivatives for treating diseases, particularly tumor diseases.
摘要翻译：本发明涉及新型的fredericamycin衍生物，含有这些衍生物或其盐的药物，以及使用fredericamycin衍生物治疗疾病，特别是肿瘤疾病。

8. 发明授权

US07253297B2 Astaxanthin esters 有权
标题翻译：虾青素酯
公开(公告)号：US07253297B2
公开(公告)日：2007-08-07
申请号：US10503696
申请日：2003-01-29
申请人： Arnold Gloor , Werner Simon
发明人： Arnold Gloor , Werner Simon
IPC分类号： C07C69/56 , C07C229/06 , C07C69/34 , A23L1/30
CPC分类号： C07C403/24 , A23K20/174 , A23K20/179 , A23K50/80 , A23L5/44 , Y02A40/818
摘要： Astaxanthin derivatives of the general formula (I) wherein R is in each case group —NH—CH(R1)—COOR2, —OR3 or —(Y)n-Z and R1, R2, R3, Y, Z and n are significances given in detail in the description, are novel compounds with improved stability during extrusion at the elevated temperatures as required in feed manufacture and during the storage of the manufactured feed and which accordingly are useful as pigmenting carotinoids for feed for aquatic animals. The derivatives are produced by reacting astaxanthin with the pertinent acid RCOOH as such or as its acid chloride RCOC1 or acid anhydride (RCO)2O, or, in the cases where R signifies a group —NH—CH(R1)—COOR2, with the appropriate N-carbonyl-amino acid ester of the formula OCNCH(R1)COOR2. The invention also concerns a formulation containing such an astaxanthin derivative as the pigmenting carotenoid for use in a feed for aquatic animals, a process for producing such a formulation by dissolving the astaxanthin derivative in a plant or vegetable oil or fat, or in an organic solvent, or in a mixture of both a plant or vegetable oil or fat and an organic solvent, emulsifying the solution with an aqueous solution of a protective colloid, at least partially removing the solvent and water to afford a concentrated emulsion, and spray-drying the concentrated emulsion to finally produce a formulation suitable for incorporation in a feed for aquatic animals, and a feed for aquatic animals containing such a pigmenting carotenoid.
摘要翻译：其中R在每种情况基团-NH-CH（R 1） - COOR 2， - 或 - 3）中的通式（I）的虾青素衍生物，或者 - （Y）n -Z和R 1，R 2，R 3，Y， Z和n是在说明书中详细给出的意义，是在饲料生产和饲料生产过程中所需要的高温挤出时具有改进的稳定性的新型化合物，因此其可用作水生动物饲料的着色类胡萝卜素。衍生物通过使虾青素与相应的酸RCOOH本身反应或作为其酰氯RCOC1或酸酐（RCO）2 O 2反应而产生，或者在R表示基团-NH-CH （R 1） - COOR 2与适当的式OCNCH（R 1）H的N-羰基 - 氨基酸酯反应 > 2 。本发明还涉及含有这样的虾青素衍生物作为水生动物饲料中着色的类胡萝卜素的制剂，通过将虾青素衍生物溶解在植物油或植物油或脂肪中或在有机溶剂中制备这种制剂的方法，或在植物油或植物油或脂肪与有机溶剂的混合物中，用保护胶体的水溶液乳化溶液，至少部分除去溶剂和水，得到浓缩乳液，并喷雾干燥最终产生适于掺入水生动物饲料的制剂，以及含有这种着色类胡萝卜素的水生动物饲料。

9. 发明申请

US20080318942A1 Fredericamycin Derivatives 审中-公开
标题翻译：弗雷德里霉素衍生物
公开(公告)号：US20080318942A1
公开(公告)日：2008-12-25
申请号：US12065108
申请日：2006-09-01
申请人： Werner Simon , Rajendra-Prasad Maskey , Hans-Falk Rasser , Bernd Sontag , Peter Eckard , Iris- Grun-Wollny , Friedrich Hansske , Bjorn Friedrich Lindemann
发明人： Werner Simon , Rajendra-Prasad Maskey , Hans-Falk Rasser , Bernd Sontag , Peter Eckard , Iris- Grun-Wollny , Friedrich Hansske , Bjorn Friedrich Lindemann
IPC分类号： A61K31/5377 , C07D221/20 , A61K31/438 , A61P33/00 , A61P17/00 , A61P37/02 , A61P35/00 , C07D295/00
CPC分类号： C07D221/20 , C07D409/12
摘要： The invention relates to new fredericamycin derivatives, to pharmaceutical drugs containing them or their salts, and to the use of the fredericamycin derivatives for the treatment of diseases, especially tumor diseases.
摘要翻译：本发明涉及新的fredericamycin衍生物，含有它们或其盐的药物，以及使用fredericamycin衍生物用于治疗疾病，特别是肿瘤疾病。

10. 发明申请

US20050096477A1 Astaxanthin esters 有权
标题翻译：虾青素酯
公开(公告)号：US20050096477A1
公开(公告)日：2005-05-05
申请号：US10503696
申请日：2003-01-29
申请人： Arnold Gloor , Werner Simon
发明人： Arnold Gloor , Werner Simon
IPC分类号： A23K1/16 , A23K1/18 , A23L1/275 , A23L1/30 , C07C271/34 , C07C403/02 , C07C403/24 , C07D213/80 , C07D307/68 , C07D333/22 , C07D333/24 , C09B61/00
CPC分类号： C07C403/24 , A23K20/174 , A23K20/179 , A23K50/80 , A23L5/44 , Y02A40/818
摘要： Astaxanthin derivatives of the general formula (I) wherein R is in each case group —NH—CH(R1)—COOR2, —OR3 or —(Y)n-Z and R1, R2, R3, Y, Z and n are significances given in detail in the description, are novel compounds with improved stability during extrusion at the elevated temperatures as required in feed manufacture and during the storage of the manufactured feed and which accordingly are useful as pigmenting carotinoids for feed for aquatic animals. The derivatives are produced by reacting astaxanthin with the pertinent acid RCOOH as such or as its acid chloride RCOCl or acid anhydride (RCO)2O, or, in the cases where R signifies a group —NH—CH(R1)—COOR2, with the appropriate N-carbonyl-amino acid ester of the formula OCNCH(R1)COOR2. The invention also concerns a formulation containing such an astaxanthin derivative as the pigmenting carotenoid for use in a feed for aquatic animals, a process for producing such a formulation by dissolving the astaxanthin derivative in a plant or vegetable oil or fat, or in an organic solvent, or in a mixture of both a plant or vegetable oil or fat and an organic solvent, emulsifying the solution with an aqueous solution of a protective colloid, at least partially removing the solvent and water to afford a concentrated emulsion, and spray-drying the concentrated emulsion to finally produce a formulation suitable for incorporation in a feed for aquatic animals, and a feed for aquatic animals containing such a pigmenting carotenoid.
摘要翻译：其中R在每种情况基团-NH-CH（R 1） - COOR 2， - 或 - 3）中的通式（I）的虾青素衍生物，或者 - （Y）n -Z和R 1，R 2，R 3，Y， Z和n是在说明书中详细给出的意义，是在饲料生产和饲料生产过程中所需要的高温挤出时具有改进的稳定性的新型化合物，因此其可用作水生动物饲料的着色类胡萝卜素。衍生物通过使虾青素与相应的酸RCOOH本身反应或作为其酰氯RCOCl或酸酐（RCO）2 O 2反应而产生，或者在R表示基团-NH-CH （R 1） - COOR 2与适当的式OCNCH（R 1）H的N-羰基 - 氨基酸酯反应 > 2 。本发明还涉及含有这样的虾青素衍生物作为水生动物饲料中着色的类胡萝卜素的制剂，通过将虾青素衍生物溶解在植物油或植物油或脂肪中或在有机溶剂中制备这种制剂的方法，或在植物油或植物油或脂肪与有机溶剂的混合物中，用保护胶体的水溶液乳化溶液，至少部分除去溶剂和水，得到浓缩乳液，并喷雾干燥最终产生适于掺入水生动物饲料的制剂，以及含有这种着色类胡萝卜素的水生动物饲料。

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