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1. 发明申请

US20080167220A1 METHODS FOR SELECTIVELY INHIBITING JANUS TYROSINE KINASE 3 (JAK3) 失效
标题翻译：用于选择性抑制JANUS TYROSINE KINASE 3（JAK3）的方法
公开(公告)号：US20080167220A1
公开(公告)日：2008-07-10
申请号：US11935147
申请日：2007-11-05
申请人： Robert A. KIRKEN , Barry D. KAHAN , Stanislaw M. STEPKOWSKI , Waldemar PRIEBE , Izabela FOKT , Szymon KOSINSKI
发明人： Robert A. KIRKEN , Barry D. KAHAN , Stanislaw M. STEPKOWSKI , Waldemar PRIEBE , Izabela FOKT , Szymon KOSINSKI
IPC分类号： A61K38/13 , A61K31/132 , A61K31/436 , C12Q1/48 , C12N9/99 , A61P41/00 , A61P35/02
CPC分类号： A61K31/335 , C07C225/12 , G01N33/505 , G01N2333/91215
摘要： Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a derivative or modified compound, is employed which is capable of selectively inhibiting Jak3 while affecting other protein tyrosine kinase activities to a lesser extent or not at all, to provide beneficial effects such as mitigation of transplant rejection and alleviation of allergic responses with fewer side effects than with conventional immunosuppressive agents.
摘要翻译：公开了用于抑制或破坏淋巴或骨髓来源的细胞中的Janus酪氨酸激酶3（Jak3）依赖性功能的方法，特别是用于阻断淋巴细胞（例如T细胞，B细胞）的增殖和功能。使用Mannich碱性化合物或衍生物或修饰化合物，其能够选择性抑制Jak 3，同时在较小程度上或根本不影响其它蛋白酪氨酸激酶活性，以提供有益效果，例如减轻移植排斥反应和缓解的过敏反应与常规免疫抑制剂相比具有较少的副作用。

2. 发明授权

US07928062B2 Methods for selectively inhibiting Janus tyrosine kinase 3 (Jak3) 失效
标题翻译：选择性抑制Janus酪氨酸激酶3（Jak3）的方法
公开(公告)号：US07928062B2
公开(公告)日：2011-04-19
申请号：US11935147
申请日：2007-11-05
申请人： Robert A. Kirken , Barry D. Kahan , Stanislaw M. Stepkowski , Waldemar Priebe , Izabela Fokt , Szymon Kosinski
发明人： Robert A. Kirken , Barry D. Kahan , Stanislaw M. Stepkowski , Waldemar Priebe , Izabela Fokt , Szymon Kosinski
IPC分类号： A61K38/00 , A61K31/12 , A61K31/13 , A01N35/00
CPC分类号： A61K31/335 , C07C225/12 , G01N33/505 , G01N2333/91215
摘要： Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a derivative or modified compound, is employed which is capable of selectively inhibiting Jak3 while affecting other protein tyrosine kinase activities to a lesser extent or not at all, to provide beneficial effects such as mitigation of transplant rejection and alleviation of allergic responses with fewer side effects than with conventional immunosuppressive agents.
摘要翻译：公开了用于抑制或破坏淋巴或骨髓来源的细胞中的Janus酪氨酸激酶3（Jak3）依赖性功能的方法，特别是用于阻断淋巴细胞（例如T细胞，B细胞）的增殖和功能。使用曼尼希碱基化合物或衍生物或修饰化合物，其能够选择性抑制Jak3，同时在较小程度上或根本不影响其它蛋白酪氨酸激酶活性，以提供有益效果，例如减轻移植排斥反应和缓解过敏反应与常规免疫抑制剂相比具有较少的副作用。

3. 发明授权

US6051232A Chimeric MHC class I antigens for inducing allograft tolerance 失效
标题翻译：用于诱导同种异体移植耐受的嵌合MHC I类抗原
公开(公告)号：US6051232A
公开(公告)日：2000-04-18
申请号：US842656
申请日：1997-04-15
申请人： Rafik R. Ghobrial , Stanislaw M. Stepkowski , Barry D. Kahan
发明人： Rafik R. Ghobrial , Stanislaw M. Stepkowski , Barry D. Kahan
IPC分类号： C12N15/09 , A61K35/12 , A61K38/00 , A61K38/17 , A61K39/00 , A61K48/00 , A61P37/06 , C07K14/705 , C07K14/74 , C07K19/00 , C12P21/02 , C12R1/91 , A61K39/385 , C07K14/745
CPC分类号： C07K14/70539 , A61K38/13 , A61K38/00 , C07K2319/00 , Y10S530/868
摘要： Chimeric MHC Class I molecules having a recipient-type N-terminus, a donor-type alpha-1 helical region, and a recipient-type alpha-2 domain induce tolerance to donor grafts when administered to the recipient at time of transplantation.
摘要翻译：具有受体型N末端，供体型α-1螺旋区和受体型α-2结构域的嵌合MHC I类分子在移植时施用于受体时诱导对供体移植物的耐受性。

4. 发明授权

US07365096B2 Methods for selectively inhibiting Janus tyrosine kinase 3 (Jak3) 失效
标题翻译：选择性抑制Janus酪氨酸激酶3（Jak3）的方法
公开(公告)号：US07365096B2
公开(公告)日：2008-04-29
申请号：US10731769
申请日：2003-12-09
申请人： Robert A. Kirken , Barry D. Kahan , Stanislaw M. Stepkowski , Waldemar Priebe , Izabela Fokt , Szymon Kosinski
发明人： Robert A. Kirken , Barry D. Kahan , Stanislaw M. Stepkowski , Waldemar Priebe , Izabela Fokt , Szymon Kosinski
IPC分类号： A61K31/21 , A61K31/13 , A61K31/12 , A61K8/73
CPC分类号： A61K31/335 , C07C225/12 , G01N33/505 , G01N2333/91215
摘要： Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a derivative or modified compound, is employed which is capable of selectively inhibiting Jak3 while affecting other protein tyrosine kinase activities to a lesser extent or not at all, to provide beneficial effects such as mitigation of transplant rejection and alleviation of allergic responses with fewer side effects than with conventional immunosuppressive agents.
摘要翻译：公开了用于抑制或破坏淋巴或骨髓来源的细胞中的Janus酪氨酸激酶3（Jak3）依赖性功能的方法，特别是用于阻断淋巴细胞（例如T细胞，B细胞）的增殖和功能。使用曼尼希碱基化合物或衍生物或修饰化合物，其能够选择性抑制Jak3，同时在较小程度上或根本不影响其它蛋白酪氨酸激酶活性，以提供有益效果，例如减轻移植排斥反应和缓解过敏反应与常规免疫抑制剂相比具有较少的副作用。

5. 发明授权

US06355639B1 Reverse prenyl compounds as immunosuppressants 失效
标题翻译：反式异戊烯基化合物作为免疫抑制剂
公开(公告)号：US06355639B1
公开(公告)日：2002-03-12
申请号：US09463537
申请日：2000-02-16
申请人： Ting-Chao Chou , Joseph R. Bertino , Samuel J. Danishefsky , Barry D. Kahan
发明人： Ting-Chao Chou , Joseph R. Bertino , Samuel J. Danishefsky , Barry D. Kahan
IPC分类号： A61K31495
CPC分类号： A61K31/519
摘要： The present invention provides a method for treating a subject in need of immunosuppression, comprising administering to the subject an effective amount of a compound having structure (I) wherein R1, R6 and R7 are independently hydrogen, OH, NH2, SH, halogen, C1-C9 linear or branched chain alkyl, alkylmercapto, alkylamino, etc.; wherein R0 and R2 are independently hydrogen, OH, C1-C9 linear or branched chain alkyl, —CR3R3—CH(O)CH2, —CR3R3—CH═CHR4, etc.; wherein R3 and R4 are independently hydrogen halogen C1-C9 linear or branched chain alkyl, etc.; wherein R5 is hydrogen, C1-C9 linear or branched chain alkyl, phenyl, alkylphenyl, dialkylphenyl, alkylmercapto, etc.; and wherein R8 is hydrogen, C1-C9 linear or branched chain acyl, benzoyl, alkylbenzoyl, etc. Also provided are methods of treating autoimmune disease and preventing organ graft rejection using N-acetylardeemin and related compounds.
摘要翻译：本发明提供了一种治疗需要免疫抑制的受试者的方法，其包括向所述受试者施用有效量的具有结构（I）的化合物，其中R 1，R 6和R 7独立地是氢，OH，NH 2，SH，卤素，C 1 -C9直链或支链烷基，烷基巯基，烷基氨基等; 其中R 0和R 2独立地是氢，OH，C 1 -C 9直链或支链烷基，-CR 3 R 3 -CH（O）CH 2，-CR 3 R 3 -CH = CHR 4等; 其中R3和R4独立地是氢卤素C1-C9直链或支链烷基等; 其中R5是氢，C1-C9直链或支链烷基，苯基，烷基苯基，二烷基苯基，烷基巯基等; 并且其中R8是氢，C1-C9直链或支链酰基，苯甲酰基，烷基苯甲酰基等。还提供了使用N-乙酰胆碱和相关化合物治疗自身免疫疾病和预防器官移植排斥的方法。

6. 发明授权

US4228236A Process of producing carcinoembryonic antigen 失效
标题翻译：产生癌胚抗原的方法
公开(公告)号：US4228236A
公开(公告)日：1980-10-14
申请号：US906036
申请日：1978-05-15
申请人： Milda M. Jakstys , Baldwin H. Tom , Barry D. Kahan
发明人： Milda M. Jakstys , Baldwin H. Tom , Barry D. Kahan
IPC分类号： A61K39/00 , G01N33/574 , C12K9/00
CPC分类号： G01N33/57473 , A61K39/00
摘要： Carcinoembryonic antigen (CEA) is produced in vitro from the cell lines LS-180 (ATCC No. CL-187), LS-174T (ATCC No. CL-188), and cells derived therefrom. The CEA thus produced can be used as a standard source for radioimmunoassay procedures to determine CEA plasma levels.
摘要翻译：从细胞系LS-180（ATCC号CL-187），LS-174T（ATCC号CL-188）和从其衍生的细胞体外产生癌胚抗原（CEA）。因此产生的CEA可用作放射免疫测定程序的标准来源，以确定CEA血浆水平。

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