公开(公告)号：US10046020B2

公开(公告)日：2018-08-14

申请号：US15379047

申请日：2016-12-14

申请人： Thomas Luger

发明人： Thomas Luger

IPC分类号： A61K38/00 ,  A61K38/06 ,  A61K39/00 ,  A61K9/06

CPC分类号： A61K38/06 ,  A23L33/175 ,  A23L33/18 ,  A61K9/06 ,  A61K31/198 ,  A61K38/04 ,  A61K38/05 ,  A61K39/001 ,  A61K2039/5154 ,  C07K5/06086 ,  C07K5/0815 ,  C12N2501/86 ,  A61K2300/00

摘要： The present invention relates to the use of compounds selected from the group consisting of Lys-(D)Pro-Thr, N-acyl Lys-(D)Pro-Thr, C-amide Lys-(D)Pro-Thr, and C-esters of Lys-(D)Pro-Thr; or a pharmaceutically acceptable salt of said compound for the treatment of inflammatory disorders. The invention also relates to the use of αMSH for inducing tolerance.

公开(公告)号：US20180051302A1

公开(公告)日：2018-02-22

申请号：US15550472

申请日：2015-06-25

申请人： DALIAN NATIONALITIES UNIVERSITY

发明人： Shubiao ZHANG ,  Yinan ZHAO ,  Shaohui CUI ,  Huiying CHEN ,  Quan ZHOU

IPC分类号： C12N15/88 ,  A61K9/127 ,  C07K4/00 ,  C07K1/06

CPC分类号： C12N15/88 ,  A61K9/1272 ,  A61K47/542 ,  C07K1/06 ,  C07K1/066 ,  C07K4/00 ,  C07K5/06086 ,  C07K5/0815 ,  C07K5/1019

摘要： A bis-alkoxyl amide alkyl cationic peptide lipid has a chemical structure as below: wherein the bis-alkoxyl amide alkyl cationic peptide lipid is dispersed in water to obtain the cationic peptide liposome which are high in stability and uniform in dispersion and have about 120 nm of average grain diameter and Zeta electric potential between 30 and 50 mV. The liposome can effectively compress the plasmids DNA and siRNA, can efficient transfection both in-vitro and in-vivo, and almost does not have toxicity to cells and mice, so that the liposome can be widely applied in gene delivery as a gene vector.

公开(公告)号：US20170260231A1

公开(公告)日：2017-09-14

申请号：US15602709

申请日：2017-05-23

申请人： The Board of Regents of the University of Oklahoma

发明人： Patrick A. McKee ,  Kenneth W. Jackson ,  Victoria J. Christiansen

IPC分类号： C07K5/11 ,  C07K5/072 ,  C07K5/062

CPC分类号： C07K5/1019 ,  A61K38/00 ,  A61K38/1825 ,  A61K38/1858 ,  A61K38/21 ,  A61K38/28 ,  A61K38/30 ,  C07K5/0202 ,  C07K5/06043 ,  C07K5/06069 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/0815 ,  C07K5/0817 ,  C07K5/0819 ,  C07K5/0821 ,  C07K7/06 ,  A61K2300/00

摘要： Inhibitors of fibroblast activation protein alpha (FAP) and Prolyl Oligopeptidase (POP) are disclosed, along with their use in various therapies related to conditions, diseases, and disorders involving abnormal cell proliferation such as malignancies and angiogenesis, and in neural disorders such as Alzheimer's disease. Stalk portions of the inhibitor molecules, and substrates of FAP and POP, are also disclosed and may be used, for example, in screening methods for identifying such inhibitors.

公开(公告)号：US20170224759A1

公开(公告)日：2017-08-10

申请号：US15502060

申请日：2015-08-06

申请人： Georgia State University Research Foundation, Inc.

发明人： Didier MERLIN

IPC分类号： A61K38/06 ,  A61K39/395 ,  A61K45/06

CPC分类号： A61K38/06 ,  A61K31/197 ,  A61K31/655 ,  A61K38/05 ,  A61K39/395 ,  A61K45/06 ,  A61P1/04 ,  A61P35/00 ,  C07K5/06026 ,  C07K5/06052 ,  C07K5/06086 ,  C07K5/06165 ,  C07K5/0815 ,  G01N33/57419 ,  G01N2800/50 ,  A61K2300/00

摘要： The present invention relates to methods of treating a patient who has colorectal cancer and to methods of reducing the likelihood that a patient will develop or experience a recurrence of colorectal cancer. The methods comprise a step of introducing, to the patient, an effective amount of an agent that targets an intestinal H−-coupled di/tripeptide transporter (PepT1). Useful compositions including, for example, the tripeptide KPV, vectors encoding such peptides, and cells (e.g., bacterial cells) including them, are also within the scope of the present invention, as are kits including such compositions.

公开(公告)号：US20170183378A1

公开(公告)日：2017-06-29

申请号：US15397523

申请日：2017-01-03

申请人： Biogen MA Inc.

发明人： Natalia Penner

IPC分类号： C07K5/09 ,  C07K5/068

CPC分类号： C07K5/0815 ,  C07K5/0215 ,  C07K5/0606 ,  C07K5/06086 ,  G01N33/6848 ,  G01N33/94 ,  Y02P20/55

摘要： The present invention provides compounds of Formula (I) and (II): wherein R1, R2, R4, R5, R6, X and n are as defined herein, and wherein R3 is hydrogen or a sulfur protecting group. Compounds of Formula (I) and (II), wherein R3 is hydrogen, may be useful in methods for detecting a reactive metabolite in a sample, e.g., wherein the metabolite is generated from the metabolism of a test compound, and wherein the metabolite and the compound of Formula (I) or (II) react to form a detectable adduct, e.g., detectable by mass spectrometry.

公开(公告)号：US20170182117A1

公开(公告)日：2017-06-29

申请号：US15313833

申请日：2015-05-27

申请人： STEALTH BIOTHERAPEUTICS CORP

发明人： D. Travis Wilson ,  Mark Bamberger ,  Peter Oates

IPC分类号： A61K38/10 ,  A61K31/198 ,  A61K31/205 ,  A61K31/51 ,  A61K31/525 ,  A61K31/455 ,  A61K31/675 ,  A61K31/714 ,  A61K31/519 ,  A61K31/375 ,  A61K31/355 ,  A61K31/385 ,  A61K31/194 ,  A61K38/07 ,  A61K38/08 ,  A61K38/06 ,  A61K38/05 ,  A61K45/06 ,  A61K38/13 ,  A61K31/122

CPC分类号： A61K38/10 ,  A01N1/0226 ,  A61K31/122 ,  A61K31/194 ,  A61K31/198 ,  A61K31/205 ,  A61K31/355 ,  A61K31/375 ,  A61K31/385 ,  A61K31/4415 ,  A61K31/455 ,  A61K31/51 ,  A61K31/519 ,  A61K31/525 ,  A61K31/675 ,  A61K31/714 ,  A61K38/04 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K38/13 ,  A61K45/06 ,  A61K47/645 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0817 ,  C07K5/1008 ,  C07K5/1016 ,  C07K5/1019 ,  C07K5/1024 ,  A61K2300/00

摘要： Disclosed herein are methods and compositions for the treatment and/or prevention of diseases or conditions comprising administration of TSM, and/or naturally or artificially occurring derivatives, analogues, or pharmaceutically acceptable salts thereof, alone or in combination with one or more active agents (e.g., an aromatic-cationic peptide). The present technology provides compositions related to aromatic-cationic peptides linked to TSM and uses of the same. In some embodiments, the aromatic-cationic peptide comprises 2′,6′-dimethyl-Tyr-D-Arg-Phe-Lys-NH2, Phe-D-Arg-Phe-Lys-NH2, or D-Arg-2′,6′-Dmt-Lys-Phe-NH2.

公开(公告)号：US09688722B2

公开(公告)日：2017-06-27

申请号：US14398886

申请日：2013-05-03

申请人： The Board of Regents of the University of Oklahoma

发明人： Patrick A. McKee ,  Kenneth W. Jackson ,  Victoria J. Christiansen

IPC分类号： A61K38/00 ,  A61P35/00 ,  C07K14/515 ,  C07K7/06 ,  A61K38/18 ,  A61K38/21 ,  A61K38/28 ,  A61K38/30 ,  C07K5/09 ,  C07K5/11 ,  C07K5/02 ,  C07K5/093 ,  C07K5/097 ,  C07K5/078 ,  C07K5/072 ,  C07K5/062 ,  C07K5/068

CPC分类号： C07K5/1019 ,  A61K38/00 ,  A61K38/1825 ,  A61K38/1858 ,  A61K38/21 ,  A61K38/28 ,  A61K38/30 ,  C07K5/0202 ,  C07K5/06043 ,  C07K5/06069 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06113 ,  C07K5/06147 ,  C07K5/0815 ,  C07K5/0817 ,  C07K5/0819 ,  C07K5/0821 ,  C07K7/06 ,  A61K2300/00

摘要： Inhibitors of fibroblast activation protein alpha (FAP) and Prolyl Oligopeptidase (POP) are disclosed, along with their use in various therapies related to conditions, diseases, and disorders involving abnormal cell proliferation such as malignancies and angiogenesis, and in neural disorders such as Alzheimer's disease. Stalk portions of the inhibitor molecules, and substrates of FAP and POP, are also disclosed and may be used, for example, in screening methods for identifying such inhibitors.

公开(公告)号：US20170087202A1

公开(公告)日：2017-03-30

申请号：US15379047

申请日：2016-12-14

申请人： Thomas LUGER

发明人： Thomas LUGER

IPC分类号： A61K38/06 ,  A61K9/06 ,  A61K39/00

CPC分类号： A61K38/06 ,  A23L33/175 ,  A23L33/18 ,  A61K9/06 ,  A61K31/198 ,  A61K38/04 ,  A61K38/05 ,  A61K39/001 ,  A61K2039/5154 ,  C07K5/06086 ,  C07K5/0815 ,  C12N2501/86 ,  A61K2300/00

摘要： The present invention relates to the use of compounds selected from the group consisting of Lys-(D)Pro-Thr, N-acyl Lys-(D)Pro-Thr, C-amide Lys-(D)Pro-Thr, and C-esters of Lys-(D)Pro-Thr; or a pharmaceutically acceptable salt of said compound for the treatment of inflammatory disorders. The invention also relates to the use of αMSH for inducing tolerance.

公开(公告)号：US09453048B2

公开(公告)日：2016-09-27

申请号：US14419975

申请日：2013-08-06

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Robert M. Borzilleri ,  Heidi L. Perez ,  Donna D. Wei ,  Kyoung S. Kim

IPC分类号： A61K38/06 ,  C07K5/09 ,  C07D401/12 ,  C07D207/16 ,  C07K5/062 ,  C07K5/083 ,  A61K45/06

CPC分类号： C07K5/0815 ,  A61K38/06 ,  A61K45/06 ,  C07D207/16 ,  C07D401/12 ,  C07K5/06026 ,  C07K5/0806

摘要： There are disclosed compounds of formula (I) that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing said compounds.

公开(公告)号：US20160271270A1

公开(公告)日：2016-09-22

申请号：US15070549

申请日：2016-03-15

申请人： Pfizer Inc.

发明人： Andreas MADERNA ,  Chakrapani SUBRAMANYAM ,  Lawrence N. TUMEY ,  Zecheng CHEN ,  Jeffrey M. CASAVANT

IPC分类号： A61K47/48 ,  C07F9/6561 ,  C07K16/32 ,  C07K5/09 ,  C07B59/00 ,  C07K16/28 ,  C07D519/00 ,  C07K5/062

CPC分类号： C07K16/32 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6807 ,  A61K47/6849 ,  A61K47/6863 ,  A61K47/6865 ,  A61K47/6869 ,  A61K47/6871 ,  C07B59/002 ,  C07B2200/05 ,  C07D495/04 ,  C07D519/00 ,  C07F9/6561 ,  C07K5/06052 ,  C07K5/0815 ,  C07K16/2803 ,  C07K16/2866

摘要： The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula: F1-L1-T-L2-F2 where F1, L1, T, L2 and F2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.

摘要翻译： 其中F1，L1，T，L2和F2如本文所定义，可用于治疗增殖性疾病，其中本发明的二聚体可用作独立药物，抗体 - 药物共轭物（ADC）中的有效载荷和接头有效载体 可用于生产或管理此类ADC的化合物; 以及包含上述二聚体，连接物有效载体和ADC的组合物，以及使用这些二聚体，连接体有效载体和ADC的方法来治疗包括癌症在内的病理状况。