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1. 发明授权

EP2986630B1 NOVEL BISPECIFIC BINDING MOLECULES WITH ANTITUMORAL ACTIVITY 失效转让
公开(公告)号：EP2986630B1
公开(公告)日：2018-08-15
申请号：EP14710220.6
申请日：2014-03-06
申请人： Covagen AG
发明人： BULLER, Fabian , WÜLLNER, Ulrich , KLUPSCH, Kristina , ZBINDEN, Irene , SANTIMARIA, Roger , ATTINGER-TOLLER, Isabella , KÖNIG-FRIEDRICH, Susann , BERTSCHINGER, Julian , GRABULOVSKI, Dragan , BRACK, Simon , SILACCI, Michela , WOODS, Richard , HACHEMI, Helen , HENNE, Patricia , VON DER BEY, Ulrike
IPC分类号： C07K14/47 , C07K16/28 , C07K16/46
CPC分类号： C12Y207/10002 , A61K2039/505 , C07K16/2809 , C07K16/2851 , C07K16/2863 , C07K16/32 , C07K2317/31 , C07K2317/73 , C07K2318/20 , C07K2319/33
摘要： The present invention relates to a bispecific binding molecule that specifically binds to (i) CD3 and (ii) a surface target antigen on cancer cells, wherein the binding molecule comprises (a) an antibody specifically binding to CD3, and (b) a Fyn-SH3-derived polypeptide binding to a surface target antigen on cancer cells, wherein said Fyn-SH3-derived polypeptide consists of the amino acid sequence of SEQ ID NO: 1, with the proviso that (i) at least one amino acid within amino acids positions 10 to 19 of SEQ ID NO: 1 is substituted, deleted or added, and (ii) at least one amino acid amino acid within amino acids positions 29 to 36 of SEQ ID NO: 1 is substituted, deleted or added, provided that said polypeptide has at least 85% sequence identity to the amino acid sequence of SEQ ID NO: 1, wherein the determination of identity excludes amino acid positions 12 to 17 and 31 to 34 of SEQ ID NO: 1.

2. 发明公开

EP3347462A1 METHODS, COMPOSITIONS, AND USES OF NOVEL FYN KINASE INHIBITORS 无效
公开(公告)号：EP3347462A1
公开(公告)日：2018-07-18
申请号：EP16845050.0
申请日：2016-09-08
申请人： Lau, Warren C.
发明人： Lau, Warren C.
IPC分类号： C12N9/12 , A61K38/45
CPC分类号： A61K31/497 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/496 , A61K31/4965 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/5377 , C07K2319/23 , C12N9/12 , C12N9/1205 , C12Y207/10002
摘要： The present invention provides methods for inhibiting Fyn kinase, using 5-3-pyridin-2-amine, 6-3-imidazo[1,2-a] pyrazine, 6-3-imidazo[1,2-b] pyridazine, N-(5-imidazo [2,1-b][1,3,4] thiadiazol-2-yl)-amine, 4-3-1H-pyrazolo[3,4-b] pyridine, and N-(3-imidazo [1,2-b] pyridazin-6-yl) amine compounds and methods of treatment, prevention, inhibition or amelioration of diseases and conditions associated with Fyn kinase using such compounds.

3. 发明公开

EP3345597A2 PKC DELTA INHIBITORS FOR USE AS THERAPEUTICS 审中-公开
公开(公告)号：EP3345597A2
公开(公告)日：2018-07-11
申请号：EP17204687.2
申请日：2013-09-19
申请人： Faller & Williams Technology, LLC
发明人： WILLIAMS, Robert M. , FALLER, Douglas V.
IPC分类号： A61K31/407 , C07D487/14 , A61P35/00
CPC分类号： A61K31/403 , A61K9/0019 , A61K31/404 , A61K45/06 , A61P35/00 , C07D209/86 , C07D405/06 , C07D487/14 , C12Y207/10002 , G01N33/5011 , G01N2333/91205
摘要： The invention is directed to compounds that are specific inhibitors of PKC delta, and methods and compositions for the treatment and prevention of cancers and other disorders. Compositions comprising compounds of the invention are used to treat cancers such as, for example, carcinoid and neuroendocrine tumors, malignant melanomas, pancreatic, gastrointestinal and lung cancers. Neuroendocrine tumor cell lines of pulmonary and gastrointestinal origin are surprisingly sensitive to PKC delta inhibition by the compounds of the invention. The invention is further directed to methods, compositions and kits containing compounds of the formulas (Ia), (Ib), (IIa), (IIb), (IIIa), (IIIb), (IVa), (IVb) and (V) as disclosed and described in Figures 11 and 12.

4. 发明公开

EP3277293A1 METHODS FOR IN VITRO PRODUCTION OF PLATELETS AND COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译：用于体外产生血小板和组合物的方法及其用途
公开(公告)号：EP3277293A1
公开(公告)日：2018-02-07
申请号：EP16774027.3
申请日：2016-03-29
申请人： Loh, Jeffrey Thomas
发明人： Loh, Jeffrey Thomas
IPC分类号： A61K35/16 , C12N5/078
CPC分类号： C12N15/85 , A61K9/0019 , A61K35/19 , C07K14/4728 , C07K14/82 , C12N5/0644 , C12N5/0647 , C12N9/12 , C12N15/63 , C12N15/907 , C12N2501/145 , C12N2501/727 , C12N2506/11 , C12N2506/45 , C12N2510/00 , C12N2521/00 , C12Y207/10002
摘要： The present invention encompasses methods for generating JAK2-modified cultured red blood cells (modified cRBCs) expressing a mutant Janus kinase 2 peptide, JAK2-modified cRBCs as a composition of matter, and methods for using the generated JAK2-modified cRBCs.

5. 发明授权

EP2823044B1 MEMBRANE SPAN-KINASE FUSION PROTEIN AND THE USES THEREOF 有权
标题翻译：膜跨度融合蛋白及其用途
公开(公告)号：EP2823044B1
公开(公告)日：2017-12-06
申请号：EP13712165.3
申请日：2013-03-06
申请人： VIB vzw , Universiteit Gent
发明人： TAVERNIER, Jan , LIEVENS, Samuel
IPC分类号： C07K14/705 , C07K14/72 , C12Q1/66 , C12N9/02 , C12N9/12 , C12N15/62 , G01N33/58 , G01N33/74
CPC分类号： C07K14/723 , C07K14/705 , C07K2319/42 , C07K2319/61 , C12N9/0069 , C12N9/12 , C12N15/62 , C12Q1/66 , C12Y207/10002 , G01N33/581 , G01N33/74 , G01N2333/726 , G01N2333/90241 , G01N2333/91205 , G01N2500/02 , G01N2500/10

6. 发明公开

EP3036260A4 BRUTON'S TYROSINE KINASE AS ANTI-CANCER DRUG TARGET 审中-公开
标题翻译： BRUTON-TYROSINKINASE ALSZIELMOLEKÜLFÜRWIRKSTOFFE GEGEN KREBS
公开(公告)号：EP3036260A4
公开(公告)日：2017-04-05
申请号：EP14838754
申请日：2014-08-20
申请人： UNIV NEW YORK STATE RES FOUND
发明人： CONKLIN DOUGLAS S , EIFERT CHERYL , KOURTIDIS ANTONIS , WANG XIANHUI , KOKABEE LEILA
IPC分类号： C07K16/40 , A61K31/519 , A61K31/704 , A61K31/713 , A61K35/00 , A61K45/06 , C12N15/113
CPC分类号： A61K31/713 , A61K31/519 , A61K31/704 , A61K45/06 , C07K16/40 , C12N15/1137 , C12N2310/14 , C12N2310/531 , C12N2320/31 , C12Y207/10002 , A61K2300/00
摘要： Receptor protein kinases (RPTKs) transmit extracellular signals across the plasma membrane to cytosolic proteins, stimulating formation of complexes that regulate key cellular functions. Over half of the known tyrosine kinases are implicated in human cancers and are therefore highly promising drug targets. A large-scale loss-of-function analysis of tyrosine kinases using RNA interference in the clinically relevant Erb-B2 positive, BT474 breast cancer cell line showed that Bruton's tyrosine kinase (BTK), a cytosolic, non-receptor tyrosine kinase that has been extensively studied for its role in B cell development, is required, in altered form, for BT474 breast cancer survival. This alternative form contains an amino-terminal extension that is also present in tumorigenic breast cells at significantly higher levels than in normal breast cells.
摘要翻译：受体蛋白激酶（RPTK）通过质膜将细胞外信号传递到胞质蛋白，刺激调节关键细胞功能的复合物的形成。已知的一半以上酪氨酸激酶涉及人类癌症，因此是非常有希望的药物靶点。在临床相关的Erb-B2阳性，BT474乳腺癌细胞系中使用RNA干扰的酪氨酸激酶的大规模功能丧失功能分析显示，Bruton的酪氨酸激酶（BTK）是一种胞质，非受体酪氨酸激酶广泛研究其在B细胞发育中的作用，以BT474乳腺癌存活的形式需要改变。这种替代形式包含氨基末端延伸，其也以与正常乳腺细胞相比显着更高的水平存在于致瘤性乳腺细胞中。

7. 发明公开

EP2914298A4 INHIBITION OF HISTONE METHYLTRANSFERASE FOR CARDIAC REPROGRAMMING 有权转让
标题翻译： HEMMUNG DER HISTONMETHYLTRANSFERASE ZUR KARDIALEN REPROGRAMMIERUNG
公开(公告)号：EP2914298A4
公开(公告)日：2016-04-20
申请号：EP13850316
申请日：2013-11-04
申请人： UNIV DUKE
发明人： DZAU VICTOR J , MIROTSOU MARIA
IPC分类号： A61K48/00 , A61K31/437 , A61K31/551 , A61K35/34 , A61K45/06 , A61P9/00 , C07D401/14 , C07D487/04 , C12N15/113
CPC分类号： A61K31/551 , A61K31/437 , A61K35/34 , A61K45/06 , C07D401/14 , C07D487/04 , C12N15/1137 , C12N2310/141 , C12N2320/30 , C12Y201/01043 , C12Y201/01125 , C12Y207/10002 , C12Y207/11001
摘要： A method for promoting the reprogramming of a non-cardiomyocytic cell or tissue into cardiomyocytic cell or tissue comprising is carried out by contacting a non-cardiomyocytic cell or tissue with a modulator of histone methyltransferase activity or expression.
摘要翻译：通过使非心肌细胞或组织与组蛋白甲基转移酶活性或表达的调节剂接触，来促进非心肌细胞或组织重编程成心肌细胞或组织的方法。

8. 发明授权

EP1973911B1 AZAINDOLES USEFUL FOR THE TREATMENT OF (INTER ALIA) PROLIFERATIVE, CARDIAC, NEURODEGENERATIVE, AUTOIMMUNE OR INFLAMMATORY DISORDERS 有权
标题翻译： FOR（包括）增殖性，心脏病，神经变性，自身免疫或炎性病症SUITABLE氮杂吲哚于治疗
公开(公告)号：EP1973911B1
公开(公告)日：2016-01-13
申请号：EP07718337.4
申请日：2007-01-17
申请人： Vertex Pharmaceuticals Incorporated
发明人： FARMER, Luc , MARTINEZ-BOTELLA, Gabriel , PIERCE, Albert , SALITURO, Francesco , WANG, Jian , WANNAMAKER, Marion , WANG, Tiansheng
IPC分类号： C07D471/04 , A61K31/506 , A61K31/53 , A61P29/00 , C07D495/10 , A61K31/517 , A61P25/00 , A61P37/00
CPC分类号： A61K31/506 , A61K31/517 , A61K31/53 , A61K31/5377 , A61K45/06 , C07D471/04 , C07D495/10 , C07D519/00 , C12N9/12 , C12Y207/10002

9. 发明公开

EP2941439A1 HUMAN SERUM ALBUMIN BINDING COMPOUNDS AND FUSION PROTEINS THEREOF 无效转让
标题翻译：人参皂甙VARBINDUNGEN UND FUSIONSPROTEINE DARAUS
公开(公告)号：EP2941439A1
公开(公告)日：2015-11-11
申请号：EP13821463.0
申请日：2013-12-18
申请人： Covagen AG
发明人： BULLER, Fabian , WÜLLNER, Ulrich , ZBINDEN, Irene , ATTINGER-TOLLER, Isabella , VON DER BEY, Ulrike , KÖNIG-FRIEDRICH, Susann , BERTSCHINGER, Julian , GRABULOVSKI, Dragan , HENNE, Patricia
IPC分类号： C07K14/765 , C07K14/47 , C12N1/21 , C12N1/15 , C12N5/10
CPC分类号： C12N9/12 , C07K14/47 , C07K14/765 , C07K16/18 , C07K2317/31 , C07K2319/31 , C12Y207/10002
摘要： The present invention relates to a polypeptide binding to human serum albumin and comprising or consisting of an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDY(X 1 )(X 2 )(X 3 )(X 4 )(X 5 )(X 6 )D(X 7 )SFHKGEKFQIL(X 8 )(X 9 )(X 10 )(X 11 )(X 12 )G(X 13 )(X 14 )W(X 15 )(X 1 6 )RSLTTG(X 17 )(X 18 )G(X 19 )IPSNYVAPVDSIQ (SEQ ID NO: 1), wherein (X 1 ) is A, V, I, L, M, G, P, S, T, N, Q, C, R, H, K, D or E; (X 2 ) is R, H, K, A, V, I, L, M, G, P, S, T, N, Q or C; (X 3 ) is R, H, K, S, T, N, Q, C, F, Y, W, A, V, I, L, M, G or P; (X 4 ) is S, T, N, Q, C, A, V, I, L, M, G, P, R, H, K, F, Y, W, D or E; (X 5 ) is S, T, N, Q, C, D, E, F, Y, W, A, V, I, L, M, G, P, R, H or K; (X 6 ) is F, Y, W, A, V, I, L, M, G, P, R, H, K, S, T, N, Q or C; (X 7 ) is A, V, I, L, M, G, P, R, H or K; (X 8 ) is S, T, N, Q, C, D or E; (X 9 ) is S, T, N, Q, C, D, E, A, V, I, L, M, G, P, F, Y or W; (X 10 ) is A, V, I, L, M, G or P; (X 11 ) is F, Y, W, R, H or K; (X 12 ) is S, T, N, Q, C, F, Y or W; (X 13 ) is F, Y, W, R, H, K, S, T, N, Q, C, D, E, A, V, I, L, M, G or P; (X 14 ) is F, Y, W, A, V, I, L, M, G or P; (X 15 ) is D, E, A, V, I, L, M, G or P; (X 16 ) is A, V, I, L, M, G or P; (X 17 ) is D, E, A, V, I, L, M, G, P, R, H or K; (X 18 ) is S, T, N, Q, C, A, V, I, L, M, G or P; (X 19 ) is F, Y, W, S, T, N, Q or C; and (b) an amino acid sequence which is at least 90% identical to the amino acid sequence of (a), wherein the identity determination excludes amino acid positions (X 1 ) to (X 19 ).
摘要翻译：本发明涉及与人血清白蛋白结合的多肽，其包含或选自由以下组成的组的氨基酸序列组成：（a）GVTLFVALYDY（X 1）（X 2）（X 3）（X 4）（X 5）（X 6）D（X 7）SFHKGEKFQIL（X 8）（X 9）（X 10）（X 11）（X 12）G ）RSLTTG（X 17）（X 18）G（X 19）IPSNYVAPVDSIQ（SEQ ID NO：1）其中（X 1）为A，V，I，L，M，G，P，S，T， Q，C，R，H，K，D或E; （X 2）为R，H，K，A，V，I，L，M，G，P，S，T，N，Q或C; （X 3）为R，H，K，S，T，N，Q，C，F，Y，W，A，V，I，L，M，G或P; （X 4）是S，T，N，Q，C，A，V，I，L，M，G，P，R，H，K，F，Y，W，D或E; （X 5）是S，T，N，Q，C，D，E，F，Y，W，A，V，I，L，M，G，P，R，H或K; （X 6）为F，Y，W，A，V，I，L，M，G，P，R，H，K，S，T，N，Q或C; （X 7）为A，V，I，L，M，G，P，R，H或K; （X 8）为S，T，N，Q，C，D或E; （X 9）是S，T，N，Q，C，D，E，A，V，I，L，M，G，P，F，Y或W; （X 10）为A，V，I，L，M，G或P; （X 11）为F，Y，W，R，H或K; （X 12）为S，T，N，Q，C，F，Y或W; （X 13）是F，Y，W，R，H，K，S，T，N，Q，C，D，E，A，V，I，L，M，G或P; （X 14）是F，Y，W，A，V，I，L，M，G或P; （X 15）为D，E，A，V，I，L，M，G或P; （X 16）为A，V，I，L，M，G或P; （X 17）为D，E，A，V，I，L，M，G，P，R，H或K; （X 18）是S，T，N，Q，C，A，V，I，L，M，G或P; （X 19）为F，Y，W，S，T，N，Q或C; 和（b）与（a）的氨基酸序列至少90％相同的氨基酸序列，其中身份确定不包括氨基酸位置（X 1）至（X 19）。

10. 发明公开

EP2897610A2 PKC DELTA INHIBITORS FOR USE AS THERAPEUTICS 有权
标题翻译： PKC-DELTA-INHIBITOREN ZUR VERWENDUNG ALS THERAPEUTIKA
公开(公告)号：EP2897610A2
公开(公告)日：2015-07-29
申请号：EP13839158.6
申请日：2013-09-19
申请人： Faller, Douglas V. , Williams, Robert M.
发明人： Faller, Douglas V. , Williams, Robert M.
IPC分类号： A61K31/407 , C07D487/14
CPC分类号： A61K31/403 , A61K9/0019 , A61K31/404 , A61K45/06 , A61P35/00 , C07D209/86 , C07D405/06 , C07D487/14 , C12Y207/10002 , G01N33/5011 , G01N2333/91205
摘要： The invention is directed to compounds that are specific inhibitors of PKC delta, and methods and compositions for the treatment and prevention of cancers and other disorders. Compositions comprising compounds of the invention are used to treat cancers such as, for example, carcinoid and neuroendocrine tumors, malignant melanomas, pancreatic, gastrointestinal and lung cancers. Neuroendocrine tumor cell lines of pulmonary and gastrointestinal origin are surprisingly sensitive to PKC delta inhibition by the compounds of the invention. The invention is further directed to methods, compositions and kits containing compounds of the formulas (Ia), (IIa), (IIIa), (IVa), and (V) as disclosed and described in FIGS. 11 and 12.
摘要翻译：本发明涉及作为PKCδ特异性抑制剂的化合物，以及用于治疗和预防癌症和其它病症的方法和组合物。包含本发明化合物的组合物用于治疗癌症例如类癌和神经内分泌肿瘤，恶性黑素瘤，胰腺，胃肠道和肺癌。肺和胃肠道起源的神经内分泌肿瘤细胞系对本发明化合物对PKCδ抑制具有惊人的敏感性。本发明进一步涉及包含如图1和2所公开和描述的式（Ia），（IIa），（IIIa），（IVa）和（V）化合物的方法，组合物和试剂盒。 11和12。

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