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1. 发明授权

US5594106A Inhibitors of TNF-.alpha. secretion 失效
公开(公告)号：US5594106A
公开(公告)日：1997-01-14
申请号：US292547
申请日：1994-08-18
申请人： Roy A. Black , Jeffrey N. Fitzner , Paul R. Sleath
发明人： Roy A. Black , Jeffrey N. Fitzner , Paul R. Sleath
IPC分类号： A61K38/00 , C07C259/06 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/072 , A61K31/00
CPC分类号： C07K5/06095 , C07C259/06 , C07K5/0202 , C07K5/06034 , C07K5/06078 , C07K5/06086 , A61K38/00
摘要： Compounds and methods are disclosed that are useful in inhibiting the TNF-.alpha. converting enzyme (TACE) responsible for cleavage of TNF-.alpha. precursor to provide biologically active TNF-.alpha.. The compounds employed in the invention are peptidyl derivatives having active groups capable of inhibiting TACE such as, hydroxamates, thiols, phosphoryls and carboxyls.

2. 发明授权

US5629285A Inhibitors of TNF-.alpha. secretion 失效
标题翻译： TNF-α分泌抑制剂
公开(公告)号：US5629285A
公开(公告)日：1997-05-13
申请号：US651363
申请日：1996-05-22
申请人： Roy A. Black , Jeffrey N. Fitzner , Paul R. Sleath
发明人： Roy A. Black , Jeffrey N. Fitzner , Paul R. Sleath
IPC分类号： A61K38/00 , C07C259/06 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/072 , A61K31/215 , A61K31/66 , A61K38/16
CPC分类号： C07K5/06095 , C07C259/06 , C07K5/0202 , C07K5/06034 , C07K5/06078 , C07K5/06086 , A61K38/00
摘要： Compounds and methods are disclosed that are useful in inhibiting the TNF-.alpha. converting enzyme (TACE) responsible for cleavage of TNF-.alpha. precursor to provide biologically active TNF-.alpha.. The compounds employed in the invention are peptidyl derivatives having active groups capable of inhibiting TACE such as, hydroxamates, thiols, phosphoryls and carboxyls.
摘要翻译：公开了可用于抑制负责TNF-α前体切割以提供生物活性TNF-α的TNF-α转化酶（TACE）的化合物和方法。本发明中使用的化合物是具有能够抑制TACE的活性基团的肽基衍生物，例如异羟肟酸盐，硫醇，磷酰基和羧基。

3. 发明授权

US5112953A Radiolabeled proteins for diagnostic or therapeutic use 失效
标题翻译：放射性蛋白质用于诊断或治疗用途
公开(公告)号：US5112953A
公开(公告)日：1992-05-12
申请号：US457480
申请日：1989-12-29
申请人： Linda M. Gustavson , Ananthachari Srinivasan , Sudhakar Kasina , John M. Reno , Jeffrey N. Fitzner , David S. Jones
发明人： Linda M. Gustavson , Ananthachari Srinivasan , Sudhakar Kasina , John M. Reno , Jeffrey N. Fitzner , David S. Jones
IPC分类号： A61K51/00 , A61K38/00 , A61K47/48 , A61K51/10 , A61P35/00 , C07D207/46 , C07D309/08 , C07K1/107 , C07K5/06 , C07K5/08 , C07K5/083 , C07K14/00 , C07K14/52 , C07K14/575 , C07K16/00 , C09K3/00 , G01N33/534 , G01N33/577
CPC分类号： C07K5/0606 , A61K47/48707 , A61K51/1093 , C07D207/46 , C07D309/08 , C07K5/0806 , A61K38/00
摘要： Chelating compounds of specified structure are useful for radiolabeling targeting molecules such as antibodies. Cleavable linkers connect the radionuclide metal chelates to the antibodies. The radiolabeled antibodies have improved biodistribution properties, including reduced localization within the intestines and kidneys.
摘要翻译：特定结构的螯合化合物可用于放射性标记靶向分子如抗体。可切割接头将放射性核素金属螯合物连接到抗体上。放射标记的抗体具有改善的生物分布特性，包括减少肠和肾内的定位。

4. 发明授权

US5089249A Conjugates for bone imaging and bone cancer therapy 失效
标题翻译：骨骼成像和骨癌治疗结合
公开(公告)号：US5089249A
公开(公告)日：1992-02-18
申请号：US207686
申请日：1988-06-16
申请人： Alan R. Fritzberg , Jean-Luc E. Vanderheyden , Sudhakar Kasina , Jeffrey N. Fitzner
发明人： Alan R. Fritzberg , Jean-Luc E. Vanderheyden , Sudhakar Kasina , Jeffrey N. Fitzner
IPC分类号： A61K51/00 , A61K51/04 , A61P35/00 , C07F1/08 , C07F1/12 , C07F9/38 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0497 , C07F9/3873 , A61K2121/00 , A61K2123/00
摘要： The present invention provides conjugates formed from calcified tissues targeting agents and radiolabeled compounds. One such conjugate comprises a chelate and a targeting agent that is capable of associating with calcified tissue, wherein the chelate contains at least one nitrogen atom or at least one sulfur atom or combinations thereof as the donor atoms.Another aspect of the invention provides methods for using the conjugates for diagnostic and therapeutic purposes, including those related to bone cancer.
摘要翻译：本发明提供由钙化组织靶向剂和放射性标记化合物形成的缀合物。一种这样的缀合物包括能够与钙化组织结合的螯合物和靶向剂，其中螯合物含有至少一个氮原子或至少一个硫原子或其组合作为供体原子。本发明的另一方面提供了用于诊断和治疗目的的缀合物的方法，包括与骨癌相关的那些。

5. 发明授权

US5202109A Conjugates for bone imaging and bone cancer therapy 失效
标题翻译：用于骨成像和骨癌治疗的共轭体
公开(公告)号：US5202109A
公开(公告)日：1993-04-13
申请号：US643578
申请日：1991-01-31
申请人： Alan R. Fritzberg , Jean-Luc E. Vanderheyden , Sudhakar Kasina , Jeffrey N. Fitzner
发明人： Alan R. Fritzberg , Jean-Luc E. Vanderheyden , Sudhakar Kasina , Jeffrey N. Fitzner
IPC分类号： A61K51/04 , C07F9/38 , C07F13/00
CPC分类号： C07F9/3873 , A61K51/0497 , C07F13/005 , A61K2121/00 , A61K2123/00
摘要： The present invention provides conjugates formed from calcified tissues targeting agents and radiolabeled compounds. One such conjugate comprises a chelate and a targeting agent that is capable of associating with calcified tissue, wherein the chelate contains at least one nitrogen atom or at least one sulfur atom or combinations thereof as the donor atoms.Another aspect of the invention provides method for using the conjugates for diagnostic and therapeutic purposes, including those related to bone cancer.
摘要翻译：本发明提供由钙化组织靶向剂和放射性标记化合物形成的缀合物。一种这样的缀合物包括能够与钙化组织结合的螯合物和靶向剂，其中螯合物含有至少一个氮原子或至少一个硫原子或其组合作为供体原子。本发明的另一方面提供了用于诊断和治疗目的的缀合物的方法，包括与骨癌相关的那些。

6. 发明授权

US5017693A Methods for introducing a sulfhydryl amino or hydroxyl groups to a compound 失效
标题翻译：将巯基氨基或羟基引入化合物的方法
公开(公告)号：US5017693A
公开(公告)日：1991-05-21
申请号：US454295
申请日：1989-12-19
申请人： Mark D. Hylarides , Ananthachari Srinivasan , Jeffrey N. Fitzner , Vivekananda M. Vrudhula
发明人： Mark D. Hylarides , Ananthachari Srinivasan , Jeffrey N. Fitzner , Vivekananda M. Vrudhula
IPC分类号： A61K47/48
CPC分类号： A61K47/48715 , A61K2121/00 , A61K2123/00
摘要： The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of target cell an agent free of its targeting molecular carrier. A diagnostically therapeutically effective dose of a cleavable conjugate is administered to a warm-blooded animal such as man.Another aspect of the invention provides methods for isolating a compound. The compound binds covalently to a solid phase which has been derivatized with the linkers described above and is released in native form by a variety of mild conditions.An additional aspect of the invention provides methods for introducing into a compound a free sulfhydryl, amino, or hydroxyl group by use of reagents structurally related to the linkers described above. Preferred uses of the method are to add a free amino or a free sulfhydryl group to a protein, such as an antibody, or a drug.
摘要翻译：本发明提供了可切割的缀合物，其接头含有在多种温和条件下可裂解的不稳定键，包括弱酸性。由于试剂可以直接与接头键合，所以裂解可导致天然试剂的释放。本发明还提供了用于产生可切割缀合物的方法。优选的试剂包括药物，毒素，生物反应调节剂，放射性诊断化合物，放射治疗化合物及其衍生物。本发明中使用的靶向分子可以是完整分子，其片段或其功能等同物。在特别优选的实施方案中，靶向分子是针对人类中与肿瘤相关抗原的单克隆抗体。本发明还提供了向靶细胞的细胞质递送不含靶向分子载体的试剂的方法。将可切割缀合物的诊断治疗有效剂量施用于温血动物如人。本发明的另一方面提供了分离化合物的方法。该化合物共价结合到已经用上述接头衍生化的固相，并且通过各种温和条件以天然形式释放。本发明的另一方面提供了通过使用与上述接头结构相关的试剂将化合物引入游离巯基，氨基或羟基的方法。该方法的优选用途是将游离氨基或游离巯基添加到蛋白质例如抗体或药物中。

7. 发明授权

US5563250A Cleavable conjugates for the delivery and release of agents in native form 失效
标题翻译：用于以天然形式递送和释放试剂的可切割共轭物
公开(公告)号：US5563250A
公开(公告)日：1996-10-08
申请号：US242702
申请日：1994-05-13
申请人： Mark D. Hylarides , Ananthachari Srinivasan , Jeffrey N. Fitzner , Vivekananda M. Vrudhula
发明人： Mark D. Hylarides , Ananthachari Srinivasan , Jeffrey N. Fitzner , Vivekananda M. Vrudhula
IPC分类号： A61K47/48 , A61K51/04 , A61K51/10 , C07H15/04 , C07H15/12 , C07H15/18 , C07H15/252 , C07K1/107 , C07H3/02 , C07D207/04 , C07D295/04 , C07D307/12 , C07D307/14 , C07D333/00 , C07H5/02 , C07H5/04
CPC分类号： A61K51/0491 , A61K47/48338 , A61K47/48715 , A61K51/1093 , C07H15/04 , C07H15/12 , C07H15/18 , C07H15/252 , C07K1/1077 , A61K2121/00 , A61K2123/00
摘要： The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier. A diagnostically/therapeutically effective dose of a cleavable conjugate is administered to a warm-blooded animal such as man.
摘要翻译：本发明提供了可切割的缀合物，其接头含有在多种温和条件下可裂解的不稳定键，包括弱酸性。由于试剂可以直接与接头键合，所以裂解可导致天然试剂的释放。本发明还提供了用于产生可切割缀合物的方法。优选的试剂包括药物，毒素，生物反应调节剂，放射性诊断化合物，放射治疗化合物及其衍生物。本发明中使用的靶向分子可以是完整分子，其片段或其功能等同物。在特别优选的实施方案中，靶向分子是针对人类中与肿瘤相关抗原的单克隆抗体。本发明还提供了向靶细胞的细胞质递送不含其靶向分子载体的试剂的方法。将可切割缀合物的诊断/治疗有效剂量施用于温血动物如人。

8. 发明授权

US5175257A Radiolabeled proteins for diagnostic or therapeutic use 失效
标题翻译：用于诊断或治疗用途的放射性标记蛋白
公开(公告)号：US5175257A
公开(公告)日：1992-12-29
申请号：US641158
申请日：1991-01-14
申请人： Sudhakar Kasina , Ananthachari Srinivasan , John M. Reno , Linda M. Gustavson , Jeffrey N. Fitzner , David S. Jones
发明人： Sudhakar Kasina , Ananthachari Srinivasan , John M. Reno , Linda M. Gustavson , Jeffrey N. Fitzner , David S. Jones
IPC分类号： A61K38/00 , A61K47/48 , A61K51/10 , C07D207/46 , C07D309/08 , C07K5/06 , C07K5/083
CPC分类号： C07K5/0606 , A61K47/48707 , A61K51/1093 , C07D207/46 , C07D309/08 , C07K5/0806 , A61K38/00
摘要： Chelating compounds of specified N.sub.2 S.sub.2 N.sub.3 S derived structure are useful for radiolabeling targeting molecules such as antibodies. Cleavable ester orthioester linkers connect the radionuclide metal chelates to the antibodies. The radiolabeled antibodies have improved biodistribution properties, including reduced localization within the intestines and kidneys.
摘要翻译：指定的N2S2 N3S衍生结构的螯合化合物可用于放射性标记靶向分子如抗体。可裂解的酯或硫酯连接体将放射性核素金属螯合物连接到抗体上。放射标记的抗体具有改善的生物分布特性，包括减少肠和肾内的定位。

9. 发明授权

US5141648A Methods for isolating compounds using cleavable linker bound matrices 失效
标题翻译：使用可切割连接子结合的基质分离化合物的方法
公开(公告)号：US5141648A
公开(公告)日：1992-08-25
申请号：US678535
申请日：1991-03-29
申请人： Mark D. Hylarides , Ananthachari Srinivasan , Jeffrey N. Fitzner , Vivekananda M. Vrudhula
发明人： Mark D. Hylarides , Ananthachari Srinivasan , Jeffrey N. Fitzner , Vivekananda M. Vrudhula
IPC分类号： A61K47/48 , A61K51/04 , A61K51/10 , C07H15/04 , C07H15/12 , C07H15/18 , C07H15/252 , C07K1/107
CPC分类号： A61K51/0491 , A61K47/48338 , A61K47/48715 , A61K51/1093 , C07H15/04 , C07H15/12 , C07H15/18 , C07H15/252 , C07K1/1077 , A61K2121/00 , A61K2123/00 , Y10S435/815 , Y10S436/824 , Y10S530/811 , Y10S530/816
摘要： The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier. A diagnostically/therapeutically effective dose of a cleavable conjugate is administered to a warm-blooded animal such as man.Another aspect of the invention provides methods for isolating a compound. The compound binds covalently to a solid phase which has been derivatized with the linkers described above and is released in native form by a variety of mild conditions.An additional aspect of the invention provides methods for introducing into a compound a free sulfhydryl, amino, or hydroxyl group by use of reagents structurally related to the linkers described above. Preferred uses of the method are to add a free amino or a free sulfhydryl group to a protein, such as an antibody, or a drug.
摘要翻译：本发明提供了可切割的缀合物，其接头含有在多种温和条件下可裂解的不稳定键，包括弱酸性。由于试剂可以直接与接头键合，所以裂解可导致天然试剂的释放。本发明还提供了用于产生可切割缀合物的方法。优选的试剂包括药物，毒素，生物反应调节剂，放射性诊断化合物，放射治疗化合物及其衍生物。本发明中使用的靶向分子可以是完整分子，其片段或其功能等同物。在特别优选的实施方案中，靶向分子是针对人类中与肿瘤相关抗原的单克隆抗体。本发明还提供了向靶细胞的细胞质递送不含其靶向分子载体的试剂的方法。将可切割缀合物的诊断/治疗有效剂量施用于温血动物如人。本发明的另一方面提供了分离化合物的方法。该化合物共价结合到已经用上述接头衍生化的固相，并且通过各种温和条件以天然形式释放。本发明的另一方面提供了通过使用与上述接头结构相关的试剂将化合物引入游离巯基，氨基或羟基的方法。该方法的优选用途是将游离氨基或游离巯基添加到蛋白质例如抗体或药物中。

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