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1. 发明申请

WO2007070514A1 HETEROARYL SUBSTITUTED PYRROLO[2,3-B]PYRIDINES AND PYRROLO[2,3-B]PYRIMIDINES AS JANUS KINASE INHIBITORS 审中-公开
标题翻译：异丙基取代的吡咯并[2,3-B]吡啶和吡咯并[2,3-b]吡嗪类作为JANUS激酶抑制剂
公开(公告)号：WO2007070514A1
公开(公告)日：2007-06-21
申请号：PCT/US2006/047369
申请日：2006-12-12
申请人： INCYTE CORPORATION , RODGERS, James D. , SHEPARD, Stacey , MADUSKUIE, Thomas P. , WANG, Haisheng , FALAHATPISHEH, Nikoo , RAFALSKI, Maria , ARVANITIS, Argyrios G. , STORACE, Louis , JALLURI, Ravi Kumar , FRIDMAN, Jordan S. , VADDI, Krishna
发明人： RODGERS, James D. , SHEPARD, Stacey , MADUSKUIE, Thomas P. , WANG, Haisheng , FALAHATPISHEH, Nikoo , RAFALSKI, Maria , ARVANITIS, Argyrios G. , STORACE, Louis , JALLURI, Ravi Kumar , FRIDMAN, Jordan S. , VADDI, Krishna
IPC分类号： C07D471/04 , C07D487/04 , A61K31/395 , A61P17/00 , A61P35/00 , A61P37/00
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines (I) and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译：本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶（I）和杂芳基取代的吡咯并[2,3-b]嘧啶，并且可用于治疗与Janus的活性有关的疾病激酶包括例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

2. 发明申请

WO2004089294A3 COMPOSITIONS, METHODS AND KITS RELATING TO HER-2 CLEAVAGE 审中-公开
公开(公告)号：WO2004089294A3
公开(公告)日：2004-10-21
申请号：PCT/US2004/010278
申请日：2004-04-02
申请人： INCYTE CORPORATION , FRIEDMAN, Steven, M. , SCHERLE, Peggy, A. , LIU, Xiangdong , BURN, Timothy, C. , HUBER, Reid , LIU, Phillip, C., C. , HOLLIS, Gregory, F. , VADDI, Krishna , FRIDMAN, Jordan, S.
发明人： FRIEDMAN, Steven, M. , SCHERLE, Peggy, A. , LIU, Xiangdong , BURN, Timothy, C. , HUBER, Reid , LIU, Phillip, C., C. , HOLLIS, Gregory, F. , VADDI, Krishna , FRIDMAN, Jordan, S.
IPC分类号： A61K39/395 , A61K31/19
摘要： The present invention relates to compositions, methods and kits based on the ADAM-mediated cleavage of Her-2. The present invention also relates to treatments for cancer, and in particular, breast cancer, by modulating the ADAMmediated cleavage of Her-2. Further, the invention relates to compositions, methods and kits based on the surprising synergistic effect between inhibition of Her-2 cleavage by an ADAM and certain cytostatic (e.g., Herceptin) and cytotoxic (e.g., Taxol) compounds in, among other things, inhibiting tumor cell proliferation and inducing cell death. Additionally, the invention relates to novel variants of ADAM15, designated ADAM15 variant I and ADAM 15 variant 2, now identified and isolated.

3. 发明申请

WO2016123603A3 HIGH SURFACE-AREA LYOPHILIZED COMPOSITIONS COMPRISING ARSENIC FOR ORAL ADMINISTRATION IN PATIENTS 审中-公开
标题翻译：包含ARSENIC的高表面积的LYOPHILED组合物用于患者口腔管理
公开(公告)号：WO2016123603A3
公开(公告)日：2016-11-03
申请号：PCT/US2016015917
申请日：2016-02-01
申请人： VADDI KRISHNA , KURUMADDALI KUMAR
发明人： VADDI KRISHNA , KURUMADDALI KUMAR
IPC分类号： A61K33/36 , A61K9/16 , A61K9/48 , A61P35/00 , A61P35/02
CPC分类号： A61K9/19 , A61K9/4858 , A61K33/36 , A61K45/06 , A61K2300/00
摘要： The present invention relates to treating malignancies such as tumors or cancers by orally administering lyophilized compositions comprising arsenic to a subject in such need. Malignancies include various hematological malignancies, such as acute myeloid leukemia (AML) including acute promyelocytic leukemia (APL), myelodysplasia syndrome (MDS), multiple myeloma (MM) and lymphomas and solid tumors including glioblastoma multiforme and breast cancer. Arsenic treatment has shown great promise in the treatment of several cancers but requires daily intravenous (IV) administration. This invention relates to a novel formulation comprising a lyophilized compositions comprising arsenic. As a result, the formulation facilitates a systemic bioavailability comparable to that of intravenous (IV) administration of arsenic trioxide currently practiced. The present invention also relates to a method for lyophilizing the arsenic trioxide, preparing the oral formulation comprising lyophilized compositions comprising arsenic, and a method for treating a subject with malignancies using the oral formulation.
摘要翻译：本发明涉及通过在需要时向受试者口服施用包含砷的冻干组合物来治疗诸如肿瘤或癌症的恶性肿瘤。恶性肿瘤包括各种血液恶性肿瘤，如包括急性早幼粒细胞白血病（APL），骨髓增生异常综合征（MDS），多发性骨髓瘤（MM）和淋巴瘤的急性骨髓性白血病（AML）和包括多形性成胶质细胞瘤和乳腺癌的实体瘤。砷治疗在治疗几种癌症方面表现出巨大的希望，但需要每日静脉内（IV）给药。本发明涉及包含含砷的冻干组合物的新型制剂。结果，该制剂促进了与目前实施的三氧化二砷的静脉内（IV）给药相当的全身生物利用度。本发明还涉及一种用于冻干三氧化二砷的方法，制备包含砷的冻干组合物的口服制剂，以及使用口服制剂治疗恶性肿瘤患者的方法。

4. 发明申请

WO2007143600A3 SHEDDASE INHIBITORS COMBINED WITH CD30-BINDING IMMUNOTHERAPEUTICS FOR THE TREATMENT OF CD30 POSITIVE DISEASES 审中-公开
标题翻译：与CD30结合免疫治疗联合治疗CD30阳性疾病的SHEDDASE抑制剂
公开(公告)号：WO2007143600A3
公开(公告)日：2008-02-14
申请号：PCT/US2007070304
申请日：2007-06-04
申请人： INCYTE CORP , FRIEDMAN STEVEN M , NEWTON ROBERT C , SCHERLE PEGGY A , VADDI KRISHNA
发明人： FRIEDMAN STEVEN M , NEWTON ROBERT C , SCHERLE PEGGY A , VADDI KRISHNA
IPC分类号： A61K31/495 , A61K31/397 , A61K31/40 , A61K31/404 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/55 , A61K39/395 , A61P35/00 , A61P35/02
CPC分类号： C07K16/2878 , A61K31/397 , A61K31/40 , A61K31/404 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/55 , A61K39/395 , A61K2039/505 , A61K2300/00
摘要： The present invention is directed to pharmaceutical methods for the treatment of CD30 positive diseases, such as Hodgkin's disease, by administration of a combination of at least one sheddase inhibitor and at least one anti-CD30 immunotherapeutic.
摘要翻译：本发明涉及通过施用至少一种脱落酶抑制剂和至少一种抗CD30免疫治疗剂的组合来治疗CD30阳性疾病如霍奇金病的药物方法。

5. 发明申请

WO2016123603A2 HIGH SURFACE-AREA LYOPHILIZED COMPOSITIONS COMPRISING ARSENIC FOR ORAL ADMINISTRATION IN PATIENTS 审中-公开
标题翻译：包含砷在口腔给药中的高表面积冻干组合物
公开(公告)号：WO2016123603A2
公开(公告)日：2016-08-04
申请号：PCT/US2016/015917
申请日：2016-02-01
申请人： VADDI, Krishna , KURUMADDALI, Kumar
发明人： VADDI, Krishna , KURUMADDALI, Kumar
IPC分类号： A61K33/36 , A61K9/48 , A61K9/16 , A61P35/00 , A61P35/02
CPC分类号： A61K9/19 , A61K9/4858 , A61K33/36 , A61K45/06 , A61K2300/00
摘要： The present invention relates to treating malignancies such as tumors or cancers by orally administering lyophilized compositions comprising arsenic to a subject in such need. Malignancies include various hematological malignancies, such as acute myeloid leukemia (AML) including acute promyelocytic leukemia (APL), myelodysplasia syndrome (MDS), multiple myeloma (MM) and lymphomas and solid tumors including glioblastoma multiforme and breast cancer. Arsenic treatment has shown great promise in the treatment of several cancers but requires daily intravenous (IV) administration. This invention relates to a novel formulation comprising a lyophilized compositions comprising arsenic. As a result, the formulation facilitates a systemic bioavailability comparable to that of intravenous (IV) administration of arsenic trioxide currently practiced. The present invention also relates to a method for lyophilizing the arsenic trioxide, preparing the oral formulation comprising lyophilized compositions comprising arsenic, and a method for treating a subject with malignancies using the oral formulation.
摘要翻译：本发明涉及通过向需要的受试者口服施用包含砷的冻干组合物来治疗恶性肿瘤如肿瘤或癌症。恶性肿瘤包括各种血液恶性肿瘤，例如包括急性早幼粒细胞白血病（APL），骨髓增生异常综合征（MDS），多发性骨髓瘤（MM）和淋巴瘤的急性骨髓性白血病（AML）和包括多形性成胶质细胞瘤和乳腺癌的实体瘤。砷治疗在治疗多种癌症方面显示出巨大的前景，但需要每日静脉（IV）给药。本发明涉及包含含有砷的冻干组合物的新制剂。结果，该制剂有利于与目前实施的静脉内（IV）施用三氧化二砷相当的全身生物利用度。本发明还涉及冻干三氧化二砷的方法，制备包含含砷冻干组合物的口服制剂，以及使用该口服制剂治疗患有恶性肿瘤的受试者的方法。

6. 发明申请

WO2007143600A2 SHEDDASE INHIBITORS COMBINED WITH CD30-BINDING IMMUNOTHERAPEUTICS FOR THE TREATMENT OF CD30 POSITIVE DISEASES 审中-公开
标题翻译：与CD30结合免疫治疗联合治疗CD30阳性疾病的SHEDDASE抑制剂
公开(公告)号：WO2007143600A2
公开(公告)日：2007-12-13
申请号：PCT/US2007/070304
申请日：2007-06-04
申请人： INCYTE CORPORATION , FRIEDMAN, Steven M. , NEWTON, Robert C. , SCHERLE, Peggy A. , VADDI, Krishna
发明人： FRIEDMAN, Steven M. , NEWTON, Robert C. , SCHERLE, Peggy A. , VADDI, Krishna
IPC分类号： A61K31/495 , A61K31/438 , A61K31/445 , A61K31/44 , A61K31/397 , A61K31/40 , A61K31/55 , A61K31/404 , A61K39/395 , A61P35/00 , A61P35/02
CPC分类号： C07K16/2878 , A61K31/397 , A61K31/40 , A61K31/404 , A61K31/438 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/55 , A61K39/395 , A61K2039/505 , A61K2300/00
摘要： The present invention is directed to pharmaceutical methods for the treatment of CD30 positive diseases, such as Hodgkin's disease, by administration of a combination of at least one sheddase inhibitor and at least one anti-CD30 immunotherapeutic.
摘要翻译：本发明涉及通过施用至少一种脱落酶抑制剂和至少一种抗CD30免疫治疗剂的组合来治疗CD30阳性疾病如霍奇金病的药物方法。

7. 发明申请

WO2007038215A1 TETRACYCLIC INHIBITORS OF JANUS KINASES 审中-公开
标题翻译： JANK KINASES的四氯化碳抑制剂
公开(公告)号：WO2007038215A1
公开(公告)日：2007-04-05
申请号：PCT/US2006/036872
申请日：2006-09-21
申请人： INCYTE CORPORATION , ARVANITIS, Argyrios G. , RODGERS, James D. , COMBS, Andrew P. , SPARKS, Richard B. , ROBINSON, Darius J. , FRIDMAN, Jordan S , VADDI, Krishna
发明人： ARVANITIS, Argyrios G. , RODGERS, James D. , COMBS, Andrew P. , SPARKS, Richard B. , ROBINSON, Darius J. , FRIDMAN, Jordan S , VADDI, Krishna
IPC分类号： C07D487/14 , C07D487/22 , A61K31/407
CPC分类号： C07D471/14 , C07D471/22 , C07D487/14 , C07D487/22
摘要： The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译：本发明提供调节Janus激酶活性的化合物，并且可用于治疗与Janus激酶活性相关的疾病，包括例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

8. 发明申请

WO2004089294A2 COMPOSITIONS, METHODS AND KITS RELATING TO HER-2 CLEAVAGE 审中-公开
标题翻译：组合物，方法和与2-CLEAVAGE相关的试剂盒
公开(公告)号：WO2004089294A2
公开(公告)日：2004-10-21
申请号：PCT/US2004010278
申请日：2004-04-02
申请人： INCYTE CORP , FRIEDMAN STEVEN M , SCHERLE PEGGY A , LIU XIANGDONG , BURN TIMOTHY C , HUBER REID , LIU PHILLIP C C , HOLLIS GREGORY F , VADDI KRISHNA , FRIDMAN JORDAN S
发明人： FRIEDMAN STEVEN M , SCHERLE PEGGY A , LIU XIANGDONG , BURN TIMOTHY C , HUBER REID , LIU PHILLIP C C , HOLLIS GREGORY F , VADDI KRISHNA , FRIDMAN JORDAN S
IPC分类号： A61K20060101 , A61K31/19 , A61K39/395 , A61K
CPC分类号： A61K31/19 , A61K31/395
摘要： The present invention relates to compositions, methods and kits based on the ADAM-mediated cleavage of Her-2. The present invention also relates to treatments for cancer, and in particular, breast cancer, by modulating the ADAMmediated cleavage of Her-2. Further, the invention relates to compositions, methods and kits based on the surprising synergistic effect between inhibition of Her-2 cleavage by an ADAM and certain cytostatic (e.g., Herceptin) and cytotoxic (e.g., Taxol) compounds in, among other things, inhibiting tumor cell proliferation and inducing cell death. Additionally, the invention relates to novel variants of ADAM15, designated ADAM15 variant I and ADAM 15 variant 2, now identified and isolated.
摘要翻译：本发明涉及基于ADAM介导的Her-2切割的组合物，方法和试剂盒。本发明还涉及通过调节ADAM介导的Her-2切割来治疗癌症，特别是乳腺癌。此外，本发明涉及基于由ADAM抑制Her-2切割和某些细胞抑制（例如赫赛汀）和细胞毒性（例如紫杉醇）化合物之间令人惊讶的协同效应的组合物，方法和试剂盒，其中除其他外，抑制肿瘤细胞增殖和诱导细胞死亡。另外，本发明涉及现在鉴定和分离的ADAM15的新型变体，称为ADAM15变体I和ADAM 15变体2。

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