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1. 发明申请

WO2015200078A8 FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES 审中-公开
公开(公告)号：WO2015200078A8
公开(公告)日：2015-12-30
申请号：PCT/US2015/036328
申请日：2015-06-18
申请人： NOVARTIS AG , BARNES, David Weninger , YAMADA, Ken , IBEBUNJO, Chikwendu , DUTTAROY, Alokesh , KIRMAN, Louise Clare , BRUCE, Alexandra Marshall , USERA, Aimee Richardson , ZECRI, Frederic , YUAN, Jun , LOU, Changgang , KANTER, Aaron , BOSE, Avirup
发明人： BARNES, David Weninger , YAMADA, Ken , IBEBUNJO, Chikwendu , DUTTAROY, Alokesh , KIRMAN, Louise Clare , BRUCE, Alexandra Marshall , USERA, Aimee Richardson , ZECRI, Frederic , YUAN, Jun , LOU, Changgang , KANTER, Aaron , BOSE, Avirup
IPC分类号： A61K47/48 , A61P3/00 , C07K14/475
摘要： The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R 1 , R 2 , R 3 , R 4 , Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

2. 发明申请

WO2016088059A1 METHODS AND COMPOSITIONS USING KLOTHO VARIANT POLYPEPTIDES 审中-公开
标题翻译：方法和组合使用KLOTHO变种多糖
公开(公告)号：WO2016088059A1
公开(公告)日：2016-06-09
申请号：PCT/IB2015/059294
申请日：2015-12-02
申请人： NOVARTIS AG , GUO, Donglin , IBEBUNJO, Chikwendu
发明人： GUO, Donglin , IBEBUNJO, Chikwendu
IPC分类号： C07K14/50 , C12N9/24 , A61K38/00 , C12N15/62
CPC分类号： C07K14/50 , A61K38/00 , C07K2319/00 , C07K2319/30 , C12N9/2402 , C12N15/62 , C12Y302/01031
摘要： The present disclosure is directed to compositions and methods related to an alpha sKlotho variant or fragment, in which 1 to up to about 20 amino acids have been deleted from the C- terminus, optionally also having mutations at V563 and/or K795. The present disclosure also pertains to an alpha sKlotho polypeptide variant or fragment, having mutations at V563 and/or K795, wherein the polypeptide variant or fragment is full-length, or optionally 1 to up to about 20 amino acids have been deleted from the C-terminus. The present disclosure also pertains to fusion polypeptides comprising: (a) an alpha sKlotho, in which 1 to up to about 20 amino acids have been deleted from the C-terminus, optionally also having mutations at V563 and/or K795; (b) a linker; and (c) FGF23, optionally having a mutation at R179, C206 and/or C244, or (c) serum albumin.
摘要翻译：本公开涉及与αsKlotho变体或片段相关的组合物和方法，其中从C末端删除1至多至20个氨基酸，任选地也在V563和/或K795处具有突变。本公开还涉及在V563和/或K795具有突变的αsKlotho多肽变体或片段，其中多肽变体或片段是全长的，或任选的1至多至20个氨基酸已经从C - 末端。本公开还涉及融合多肽，其包含：（a）其中从C末端缺失1至多至多20个氨基酸的αsKlotho，任选地也在V563和/或K795处具有突变; （b）连接体; 和（c）FGF23，任选在R179，C206和/或C244处具有突变，或（c）血清白蛋白。

3. 发明申请

WO2006116269A2 ANTIBODIES TO MYOSTATIN 审中-公开
标题翻译：肌营养素抗体
公开(公告)号：WO2006116269A2
公开(公告)日：2006-11-02
申请号：PCT/US2006/015407
申请日：2006-04-24
申请人： PFIZER INC. , AMGEN FREMONT INC. , CHIN, Eva, Rose , IBEBUNJO, Chikwendu , KRASNEY, Philip, Albert , YIE, Junming , ZACHWIEJA, Joseph , GREEN, Larry
发明人： CHIN, Eva, Rose , IBEBUNJO, Chikwendu , KRASNEY, Philip, Albert , YIE, Junming , ZACHWIEJA, Joseph , GREEN, Larry
IPC分类号： A61K39/00 , C07K16/28
CPC分类号： C07K16/22 , A61K2039/505 , C07K2317/21 , C07K2317/33 , C07K2317/34 , C07K2317/56 , C07K2317/76
摘要： The present invention relates to antibodies including human antibodies and antigen-binding portions thereof that bind to myostatin, and that function to inhibit myostatin. The invention also relates to human anti-myostatin antibodies and antigen-binding portions thereof. The invention also relates to antibodies that are chimeric, bispecific, derivatized, single chain antibodies or portions of fusion proteins. The invention also relates to isolated heavy and light chain immunoglobulins derived from human anti-myostatin antibodies and nucleic acid molecules encoding such immunoglobulins. The present invention also relates to methods of making human anti-myostatin antibodies, compositions comprising these antibodies and methods of using the antibodies and compositions for diagnosis and treatment. The invention also provides gene therapy methods using nucleic acid molecules encoding the heavy and/or light immunoglobulin molecules that comprise the human anti-myostatin antibodies. The invention also relates to transgenic animals or plants comprising nucleic acid molecules of the present invention.
摘要翻译：本发明涉及包含人抗体及其与肌生成抑制素结合的抗原结合部分的抗体，其功能是抑制肌生成抑制素。本发明还涉及人抗肌生成抑制素抗体及其抗原结合部分。本发明还涉及嵌合，双特异性，衍生的单链抗体或融合蛋白的部分的抗体。本发明还涉及衍生自人抗肌生成抑制素抗体的分离的重链和轻链免疫球蛋白和编码这种免疫球蛋白的核酸分子。本发明还涉及制备人抗肌生成抑制素抗体的方法，包含这些抗体的组合物和使用该抗体和组合物进行诊断和治疗的方法。本发明还提供了使用编码包含人抗肌生成抑制素抗体的重和/或轻免疫球蛋白分子的核酸分子的基因治疗方法。本发明还涉及包含本发明的核酸分子的转基因动物或植物。

4. 发明申请

WO2017141208A1 TGFBETA 2 ANTIBODIES 审中-公开
标题翻译： TGFBETA 2抗体
公开(公告)号：WO2017141208A1
公开(公告)日：2017-08-24
申请号：PCT/IB2017/050917
申请日：2017-02-17
申请人： NOVARTIS AG
发明人： IBEBUNJO, Chikwendu , JACOBI, Carsten , MEYER, Angelika , SCHAADT, Eveline , TRENDELENBURG, Anne-Ulrike , VLADIMIROVNA MITINA, Olga
IPC分类号： C07K16/22 , A61K39/395
CPC分类号： C07K16/22 , A61K2039/505 , C07K2317/33 , C07K2317/34 , C07K2317/55 , C07K2317/76 , C07K2317/92
摘要： This invention is in the field of anti-transforming growth factor beta 2 (TGF-β2) antibodies. In particular, the invention provides human monoclonal antibodies that bind the human TGF-β2 isoform preferentially over the human TGF-β1 or TGF-β3 isoforms.
摘要翻译：本发明属于抗转化生长因子β2（TGF-β2）抗体领域。具体而言，本发明提供优先于人TGF-β1或TGF-β3同种型结合人TGF-β2同种型的人单克隆抗体。

5. 发明公开

EP3157571A1 FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES 有权
标题翻译：达赖喇嘛在德累斯顿的VENBIOMOLEKÜLEN
公开(公告)号：EP3157571A1
公开(公告)日：2017-04-26
申请号：EP15732508.5
申请日：2015-06-18
申请人： Novartis AG
发明人： BARNES, David Weninger , YAMADA, Ken , IBEBUNJO, Chikwendu , DUTTAROY, Alokesh , KIRMAN, Louise Clare , BRUCE, Alexandra Marshall , USERA, Aimee Richardson , ZECRI, Frederic , YUAN, Jun , LOU, Changgang , KANTER, Aaron , BOSE, Avirup
IPC分类号： A61K47/50 , A61P3/00 , C07K14/475
CPC分类号： A61K47/48038 , A61K38/08 , A61K38/164 , A61K38/1709 , A61K38/1825 , A61K38/1841 , A61K38/2221 , A61K45/06 , A61K47/542 , C07C55/02 , C07C55/22 , C07C57/02 , C07C57/18 , C07C59/245 , C12N15/113 , C12N2310/14 , C12N2310/351
摘要： The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供了一种缀合物，其包含通过接头与脂肪酸连接的生物分子，其中脂肪酸具有下列式A1，A2或A3：其中R1，R2，R3，R4，Ak，n，m和p如本文所定义。本发明还涉及制备本发明缀合物如GDF15缀合物的方法及其治疗用途，例如治疗或预防代谢紊乱或疾病，2型糖尿病，肥胖症，胰腺炎，血脂异常，酒精和非酒精性脂肪肝疾病/脂肪性肝炎和其他进行性肝病，胰岛素抵抗，高胰岛素血症，葡萄糖不耐受，高血糖症，代谢综合征，高血压，心血管疾病，动脉粥样硬化，外周动脉疾病，中风，心力衰竭，冠心病，糖尿病并发症（包括但不限于慢性肾脏疾病），神经病，胃轻瘫等代谢紊乱。本发明还提供药理活性剂和药物组合物的组合。

6. 发明公开

EP3988170A1 FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES 审中-公开
公开(公告)号：EP3988170A1
公开(公告)日：2022-04-27
申请号：EP21206196.4
申请日：2015-06-18
申请人： Novartis AG
发明人： BARNES, David Weninger , YAMADA, Ken , IBEBUNJO, Chikwendu , DUTTAROY, Alokesh , KIRMAN, Louise Clare , BRUCE, Alexandra Marshall , USERA, Aimee Richardson , ZECRI, Frederic , YUAN, Jun , LOU, Changgang , KANTER, Aaron , BOSE, Avirup
IPC分类号： A61P1/00 , A61P3/00 , A61P5/48 , A61P9/00 , A61P25/18
摘要： The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formula A1:

wherein R 1 , R 2 , R 3 , n and m are defined herein. The invention also relates to uses of the fatty acids in providing said conjuage. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

7. 发明公开

EP3416982A1 TGFBETA 2 ANTIBODIES 审中-公开
公开(公告)号：EP3416982A1
公开(公告)日：2018-12-26
申请号：EP17707960.5
申请日：2017-02-17
申请人： Novartis AG
发明人： IBEBUNJO, Chikwendu , JACOBI, Carsten , MEYER, Angelika , SCHAADT, Eveline , TRENDELENBURG, Anne-Ulrike , VLADIMIROVNA MITINA, Olga
IPC分类号： C07K16/22 , A61K39/395
CPC分类号： C07K16/22 , A61K2039/505 , C07K2317/33 , C07K2317/34 , C07K2317/55 , C07K2317/76 , C07K2317/92
摘要： This invention is in the field of anti-transforming growth factor beta 2 (TGF-β2) antibodies. In particular, the invention provides human monoclonal antibodies that bind the human TGF-β2 isoform preferentially over the human TGF-β1 or TGF-β3 isoforms.

8. 发明公开

EP3227319A1 METHODS AND COMPOSITIONS USING KLOTHO VARIANT POLYPEPTIDES 有权
标题翻译：使用KLOTHO变体多肽的方法和组合物
公开(公告)号：EP3227319A1
公开(公告)日：2017-10-11
申请号：EP15816527.4
申请日：2015-12-02
申请人： Novartis AG
发明人： GUO, Donglin , IBEBUNJO, Chikwendu
IPC分类号： C07K14/50 , C12N9/24 , A61K38/00 , C12N15/62
CPC分类号： C07K14/50 , A61K38/00 , C07K2319/00 , C07K2319/30 , C12N9/2402 , C12N15/62 , C12Y302/01031
摘要： The present disclosure is directed to compositions and methods related to an alpha sKlotho variant or fragment, in which 1 to up to about 20 amino acids have been deleted from the C-terminus, optionally also having mutations at V563 and/or K795. The present disclosure also pertains to an alpha sKlotho polypeptide variant or fragment, having mutations at V563 and/or K795, wherein the polypeptide variant or fragment is full-length, or optionally 1 to up to about 20 amino acids have been deleted from the C-terminus. The present disclosure also pertains to fusion polypeptides comprising: (a) an alpha sKlotho, in which 1 to up to about 20 amino acids have been deleted from the C-terminus, optionally also having mutations at V563 and/or K795; (b) a linker; and (c) FGF23, optionally having a mutation at R179, C206 and/or C244, or (c) serum albumin.
摘要翻译：本公开涉及与α突变变体或片段有关的组合物和方法，其中1至多达约20个氨基酸已从C末端缺失，任选还在V563和/或K795处具有突变。本公开还涉及一种阿尔法的sKlotho多肽变体或片段，其具有在V563和/或K795，其中所述多肽变体或片段是全长，或任选1至至多约20个氨基酸已经被从C删除突变 - 末端。本公开还涉及融合多肽，其包含：（a）α突变体，其中1至高达约20个氨基酸已从C末端缺失，任选地还在V563和/或K795处具有突变; （b）连接子; 和（c）FGF23，任选地在R179，C206和/或C244处具有突变，或（c）血清白蛋白。

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