公开(公告)号：WO2015069587A9

公开(公告)日：2015-12-17

申请号：PCT/US2014063624

申请日：2014-11-03

申请人： MERCK SHARP & DOHME ,  COLLETTI STEVEN L ,  TUCKER THOMAS J ,  TELLERS DAVID M ,  KIM BOYOUNG ,  BURKE ROB ,  CALATI KATHLEEN B ,  STANTON MATTHEW G ,  PARMAR RUBINA G ,  AARONSON JEFFREY G ,  WANG WEIMIN

发明人： COLLETTI STEVEN L ,  TUCKER THOMAS J ,  TELLERS DAVID M ,  KIM BOYOUNG ,  BURKE ROB ,  CALATI KATHLEEN B ,  STANTON MATTHEW G ,  PARMAR RUBINA G ,  AARONSON JEFFREY G ,  WANG WEIMIN

IPC分类号： C07K16/00 ,  A61K38/14

CPC分类号： C07K19/00 ,  A61K38/14 ,  C07K2319/00 ,  C07K2319/01 ,  C12N15/113 ,  C12N15/62 ,  C12N2310/14 ,  C12N2310/3513

公开(公告)号：WO2015069587A2

公开(公告)日：2015-05-14

申请号：PCT/US2014/063624

申请日：2014-11-03

申请人： MERCK SHARP & DOHME CORP. ,  COLLETTI, Steven, L. ,  TUCKER, Thomas, J. ,  TELLERS, David, M. ,  KIM, Boyoung ,  BURKE, Rob ,  CALATI, Kathleen, B. ,  STANTON, Matthew, G. ,  PARMAR, Rubina, G. ,  AARONSON, Jeffrey, G. ,  WANG, Weimin

发明人： COLLETTI, Steven, L. ,  TUCKER, Thomas, J. ,  TELLERS, David, M. ,  KIM, Boyoung ,  BURKE, Rob ,  CALATI, Kathleen, B. ,  STANTON, Matthew, G. ,  PARMAR, Rubina, G. ,  AARONSON, Jeffrey, G. ,  WANG, Weimin

IPC分类号： A61K38/14

CPC分类号： C07K19/00 ,  A61K38/14 ,  C07K2319/00 ,  C07K2319/01 ,  C12N15/113 ,  C12N15/62 ,  C12N2310/14 ,  C12N2310/3513

摘要： Disclosed herein is a peptide containing conjugate comprising (P) c -(L) d -(G) e , wherein P is a peptide and each occurance of P is independently selected from Table 2; L is an optional linker and each occurance of L, if present, is independently selected from Table 3; G is a targeting ligand and each occurance of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. The conjugate can be administered to a subject either alone or in combination with a composition comprising R-(L) a -(G) b , wherein R is an oligonucleotide as defined herein, to inhibit expression of a gene of the subject.

摘要翻译： 本文公开了含有（P） - （ - ） - （L） - （G）e

公开(公告)号：WO2015069586A9

公开(公告)日：2015-05-14

申请号：PCT/US2014/063621

申请日：2014-11-03

申请人： MERCK SHARP & DOHME CORP. ,  COLLETTI, Steven, L. ,  TUCKER, Thomas, J. ,  TELLERS, David, M. ,  KIM, Boyoung ,  BURKE, Rob ,  CALATI, Kathleen, B. ,  STANTON, Matthew, G. ,  PARMAR, Rubina, G. ,  AARONSON, Jeffrey, G. ,  WANG, Weimin

发明人： COLLETTI, Steven, L. ,  TUCKER, Thomas, J. ,  TELLERS, David, M. ,  KIM, Boyoung ,  BURKE, Rob ,  CALATI, Kathleen, B. ,  STANTON, Matthew, G. ,  PARMAR, Rubina, G. ,  AARONSON, Jeffrey, G. ,  WANG, Weimin

IPC分类号： A61K48/00

公开(公告)号：WO2015069586A2

公开(公告)日：2015-05-14

申请号：PCT/US2014063621

申请日：2014-11-03

申请人： MERCK SHARP & DOHME ,  COLLETTI STEVEN L ,  TUCKER THOMAS J ,  TELLERS DAVID M ,  KIM BOYOUNG ,  BURKE ROB ,  CALATI KATHLEEN B ,  STANTON MATTHEW G ,  PARMAR RUBINA G ,  AARONSON JEFFREY G ,  WANG WEIMIN

发明人： COLLETTI STEVEN L ,  TUCKER THOMAS J ,  TELLERS DAVID M ,  KIM BOYOUNG ,  BURKE ROB ,  CALATI KATHLEEN B ,  STANTON MATTHEW G ,  PARMAR RUBINA G ,  AARONSON JEFFREY G ,  WANG WEIMIN

IPC分类号： A61K48/00

CPC分类号： A61K31/7125 ,  A61K31/713 ,  A61K38/10 ,  A61K38/16 ,  C07K2319/10 ,  C12N15/111 ,  C12N15/113 ,  C12N15/87 ,  C12N2310/14 ,  C12N2310/351 ,  C12N2320/31

摘要： Disclosed herein is a method for inhibiting expression of a gene of a subject comprising administering (1) a composition comprising R-(L)a-(G)b; wherein R is an oligonucleotide selected from the group consisting of DNA, RNA, siRNA, and microRNA; L is a linker and each occurance of L is independently selected from Table 3; G is a targeting ligand and each occurance of G is independently selected from Table 4; each of a and b is independently 0, 1, 2, 3 or 4; and (2) a composition comprising (P)c-(L)d-(G)e; wherein P is a peptide and each occurance of P is independently selected from Table 2; L is a linker and each occurance of L is independently selected from Table 3; G is a targeting ligand and each occurance of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. Compositions in (1) and (2) can be co-administered or sequentially administered.

摘要翻译： 本文公开了一种抑制受试者基因表达的方法，包括给予（1）包含R-（L）a-（G）b; 其中R是选自DNA，RNA，siRNA和微小RNA的寡核苷酸; L是连接体，L的每个出现独立地选自表3; G是靶向配体，G的每个出现独立地选自表4; a和b各自独立地为0,1,2,3或4; 和（2）包含（P）c-（L）d-（G）e的组合物; 其中P是肽，并且每个出现的P独立地选自表2; L是连接体，L的每个出现独立地选自表3; G是靶向配体，G的每个出现独立地选自表4; d为0,1,2,3,4,5或6; c和e中的每一个独立地为1,2,3,4,5或6.（1）和（2）中的组合物可以共同施用或依次施用。