公开(公告)号：EP2951180A4

公开(公告)日：2016-06-15

申请号：EP14745870

申请日：2014-01-29

申请人： MERCK SHARP & DOHME

发明人： CAMMARANO CAROLYN MICHELE ,  CHRISTOPHER MATTHEW P ,  DINSMORE CHRISTOPHER ,  DOLL RONALD J ,  FRADERA LLINAS FRANCESC XAVIER ,  LI CHAOMIN ,  MACHACEK MICHELLE ,  MARTINEZ MICHELLE ,  NAIR LATHA G ,  PAN WEIDONG ,  REUTERSHAN MICHAEL HALE ,  SHIZUKA MANAMI ,  STEINHUEBEL DIETRICH P ,  SUN BINYUAN ,  THOMPSON CHRISTOPHER FRANCIS ,  TROTTER B WESLEY ,  VOSS MATTHEW ERNST ,  WANG YAOLIN ,  YANG LIPING ,  PANDA JAGANNATH ,  KURISSERY ANTHAPPAN TONY ,  BOGEN STEPHANE L

IPC分类号： C07D473/00 ,  A61K31/52 ,  A61P35/00 ,  C07D473/16 ,  C07D473/30 ,  C07D473/34

CPC分类号： C07D473/00 ,  C07D473/16 ,  C07D473/30 ,  C07D473/34

摘要： The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

摘要翻译： 本发明提供如本文所述的2,6,7,8取代的嘌呤或其药学上可接受的盐。 代表性化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。

公开(公告)号：EP2731434A4

公开(公告)日：2014-12-31

申请号：EP12811164

申请日：2012-07-10

申请人： MERCK SHARP & DOHME

发明人： VERMA VISHAL ,  ARASAPPAN ASHOK ,  NJOROGE F GEORGE ,  GIRI-JAVALLABHAN VINAY ,  BOGEN STEPHANE L ,  DANG QUN ,  OLSEN DAVID B

IPC分类号： A61K31/415 ,  C07H19/04

CPC分类号： C07H19/14 ,  A61K31/7056 ,  A61K31/7064 ,  A61K45/06

公开(公告)号：EP3226690A4

公开(公告)日：2018-06-20

申请号：EP15866280

申请日：2015-12-01

申请人： MERCK SHARP & DOHME

发明人： FISCHER CHRISTIAN ,  BOGEN STEPHANE L ,  CHILDERS MATTHEW L ,  LLINAS FRANCESC XAVIER FRADERA ,  KIM ALEXANDER J ,  LAMPE JOHN W ,  MACHACEK MICHELLE R ,  MCMASTERS DANIEL R ,  PARKER DANN L JR ,  SUN WANYING ,  SCIAMMETTA NUNZIO ,  SHAO PENGCHENG P ,  SLOMAN DAVID L ,  UJJAINWALLA FEROZE ,  HUANG CHUNHUI

IPC分类号： C07D471/04 ,  A01N43/00 ,  A61K31/551 ,  A61K31/5513 ,  A61P35/00 ,  C07D471/14 ,  C07D519/00

CPC分类号： A61K31/5513 ,  A01N43/00 ,  A61K31/551 ,  A61K45/06 ,  A61P35/00 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00 ,  A61K2300/00

摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), (II-ii), (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

公开(公告)号：EP2934535A4

公开(公告)日：2016-06-29

申请号：EP13865881

申请日：2013-12-18

申请人： MERCK SHARP & DOHME

发明人： DINSMORE CHRISTOPHER ,  FRADERA LLINAS FRANCESC XAVIER ,  KUDALE AMIT ASHOKRAO ,  REUTERSHAN MICHAEL HALE ,  THOMPSON CHRISTOPHER FRANCIS ,  YANG LIPING ,  ALTMAN MICHAEL D ,  BOGEN STEPHANE L ,  DOLL RONALD J ,  VOSS MATTHEW E

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D487/04

摘要： The present invention provides substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

公开(公告)号：EP2488028A4

公开(公告)日：2013-05-01

申请号：EP10823840

申请日：2010-10-05

申请人： MERCK SHARP & DOHME

发明人： BOGEN STEPHANE L ,  MA YAO ,  WANG YAOLIN ,  LAHUE BRIAN ROBERT ,  NAIR LATHA G ,  SHIZUKA MANAMI ,  VOSS MATTHEW ERNST ,  KIROVA-SNOVER MARGARITA ,  PAN WEIDONG ,  TIAN YUAN ,  KULKARNI BHEEMASHANKAR A ,  GIBEAU CRAIG R ,  LIU YUAN ,  SCAPIN GIOVANNA ,  RINDGEN DIANE ,  DOLL RONALD J ,  GUZI TIMOTHY J ,  HICKLIN DANNY J ,  NOMEIR AMIN ,  SEIDEL-DUGAN CYNTHIA ,  SHIPPS GERALD W JR ,  MACCOSS MALCOLM

IPC分类号： C07D401/14 ,  C07D409/14

CPC分类号： C07D401/14 ,  C07D409/14

摘要： The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.

公开(公告)号：EP3226689A4

公开(公告)日：2018-06-13

申请号：EP15866163

申请日：2015-12-01

申请人： MERCK SHARP & DOHME

发明人： FISCHER CHRISTIAN ,  BOGEN STEPHANE L ,  CHILDERS MATTHEW L ,  LLINAS FRANCESC XAVIER FRADERA ,  ELLIS J MICHAEL ,  ESPOSITE SARA ,  HOFFMAN DAWN M ,  HUANG CHUNHUI ,  KATTAR SOLOMON ,  KIM ALEXANDER J ,  LAMPE JOHN W ,  MACHACEK MICHELLE R ,  MCMASTERS DANIEL R ,  PARKER DANN L JR ,  REUTERSHAN MICHAEL ,  SCIAMMETTA NUNZIO ,  SHAO PENGCHENG P ,  SLOMAN DAVID L ,  SUN WANYING ,  UJJAINWALLA FEROZE ,  WU ZHICAI

IPC分类号： A61K31/551 ,  A61P35/00 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D519/00

摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

公开(公告)号：EP2919792A4

公开(公告)日：2016-06-01

申请号：EP13854794

申请日：2013-11-14

申请人： MERCK SHARP & DOHME

发明人： BENNETT FRANK ,  HUANG YUHUA ,  WANG LINGYAN ,  BOGEN STEPHANE L ,  KEREKES ANGELA D ,  GIRIJAVALLABHAN VINAY M ,  BUTORA GABOR ,  TRUONG QUANG ,  DAVIES IAN ,  WEBER ANNE E

IPC分类号： C07H19/10 ,  A61K31/7068 ,  A61K45/06 ,  C07H19/06 ,  C07H19/067 ,  C07H19/09 ,  C07H19/11

CPC分类号： C07H19/10 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  C07H19/06 ,  C07H19/067 ,  C07H19/09 ,  C07H19/11

摘要： The present invention relates to 2′-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2′-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

公开(公告)号：EP2793890A4

公开(公告)日：2015-06-03

申请号：EP12860596

申请日：2012-12-17

申请人： MERCK SHARP & DOHME

发明人： MA YAO ,  SHIZUKA MANAMI ,  GUZI TIMOTHY J ,  TIAN YUAN ,  LAHUE BRIAN R ,  WANG YAOLIN ,  SHIPPS GERALD W JR ,  BOGEN STEPHANE L ,  NAIR LATHA G ,  PAN WEIDONG ,  VOSS MATTHEW E ,  KIROVA-SNOVER MARGARITA ,  CLAYTON W BRENT ,  MICCOY MARK A ,  LIU YUAN ,  GIBEAU GRAIG R

IPC分类号： A61K31/497 ,  A61P35/00 ,  C07D409/14 ,  C07D495/04

CPC分类号： C07D495/04 ,  C07D409/14

公开(公告)号：EP2771008A4

公开(公告)日：2015-04-08

申请号：EP12844222

申请日：2012-10-23

申请人： MERCK SHARP & DOHME

发明人： NAIR LATHA G ,  BOGEN STEPHANE L ,  DOLL RONALD J ,  MA YAO ,  TIAN YUAN

IPC分类号： A61K31/497

CPC分类号： C07D498/14 ,  C07D409/14