公开(公告)号：US20160045526A1

公开(公告)日：2016-02-18

申请号：US14436687

申请日：2013-10-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： Vinay Girijavallabhan ,  Stephane Bogen ,  Weidong Pan ,  Qun Dang ,  Ian Davies

IPC: A61K31/706 ,  A61K31/7056 ,  A61K45/06 ,  C07H7/06

CPC classification number: A61K31/706 ,  A61K31/7056 ,  A61K38/21 ,  A61K45/06 ,  C07D487/04 ,  C07H7/06 ,  A61K2300/00

Abstract: 2′-disubstituted substituted nucleoside derivatives of formula (I) and pharmaceutically acceptable salts thereof are disclosed: (1), wherein A is N3 or NH2 and X, Y, R1, R2, R3, R4, R5 and R18 are as defined herein. Compositions comprising at least one 2′-disubstituted nucleoside derivative, and methods of using the 2′-disubstituted nucleoside derivatives for treating or preventing HCV infection in a patient are disclosed.

Abstract translation: 公开了式（I）的2'-二取代取代的核苷衍生物及其药学上可接受的盐：（1）其中A是N 3或NH 2，X，Y，R 1，R 2，R 3，R 4，R 5和R 18如本文所定义 。 公开了包含至少一种2'-二取代核苷衍生物的组合物，以及使用2'-二取代核苷衍生物治疗或预防患者HCV感染的方法。

公开(公告)号：US09765107B2

公开(公告)日：2017-09-19

申请号：US14899008

申请日：2014-06-16

Applicant: Merck Sharp & Dohme Corp.

Inventor： Stephane Bogen ,  Vinay Girijavallabhan ,  Quang Truong ,  Ping Chen ,  Frank Bennett ,  Angela Kerekes ,  Qun Dang ,  David B. Olsen ,  Ian Davies

IPC: A01N43/04 ,  A61K31/70 ,  C07H19/10 ,  A61K45/06 ,  A61K31/661 ,  C07F9/6558 ,  C07F9/6574 ,  C07H19/11 ,  A61K31/7072 ,  A61K31/7068 ,  A61K31/706 ,  A61K31/7064

CPC classification number: C07H19/10 ,  A61K31/661 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  C07F9/65586 ,  C07F9/65744 ,  C07H19/11 ,  A61K2300/00

Abstract: The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

公开(公告)号：US09457039B2

公开(公告)日：2016-10-04

申请号：US14436687

申请日：2013-10-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： Vinay Girijavallabhan ,  Stephane Bogen ,  Weidong Pan ,  Qun Dang ,  Ian Davies

IPC: C07H19/12 ,  C07H19/23 ,  C07D487/04 ,  A61K31/706 ,  A61K31/53 ,  A61P31/14 ,  A61K45/06 ,  A61K31/7056 ,  A61K38/21 ,  C07H7/06

CPC classification number: A61K31/706 ,  A61K31/7056 ,  A61K38/21 ,  A61K45/06 ,  C07D487/04 ,  C07H7/06 ,  A61K2300/00

Abstract: 2′-disubstituted substituted nucleoside derivatives of formula (I) and pharmaceutically acceptable salts thereof are disclosed: (1), wherein A is N3 or NH2 and X, Y, R1, R2, R3, R4, R5 and R18 are as defined herein. Compositions comprising at least one 2′-disubstituted nucleoside derivative, and methods of using the 2′-disubstituted nucleoside derivatives for treating or preventing HCV infection in a patient are disclosed.

公开(公告)号：US10899788B2

公开(公告)日：2021-01-26

申请号：US16311363

申请日：2017-06-20

Applicant: Stephane Bogen ,  David Dukhan ,  Guillaume Brandt ,  Claire Pierra Rouviere ,  Cyril B. Dousson ,  Francois-Rene Alexandre ,  MERCK SHARP & DOHME CORP. ,  IDENIX PHARMACEUTICALS LLC

Inventor： Stephane Bogen ,  David Dukhan ,  Guillaume Brandt ,  Claire Pierra Rouviere ,  Cyril B. Dousson ,  Francois-Rene Alexandre

IPC: C07H19/11 ,  A61P31/14 ,  C07H19/213 ,  A61K45/06 ,  A61K31/7072 ,  A61K31/7076

Abstract: The present invention relates to Cyclic Phosphate Substituted Nucleoside Compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein in A, B, R1, R2, R3, Q and V are as defined herein. The present invention also relates to compositions comprising a Cyclic Phosphate Substituted Nucleoside Compound, and methods of using the Cyclic Phosphate Substituted Nucleoside Compounds for treating or preventing HCV infection in a patient.

公开(公告)号：US20160122380A1

公开(公告)日：2016-05-05

申请号：US14899008

申请日：2014-06-16

Applicant: Merck Sharp & Dohme Corp.

Inventor： Stephane Bogen ,  Vinay Girijavallabhan ,  Quang Truong ,  Ping Chen ,  Frank Bennett ,  Angela Kerekes ,  Qun Dang ,  David B. Olsen ,  Ian Davies

IPC: C07H19/10 ,  A61K45/06 ,  A61K31/7072

CPC classification number: C07H19/10 ,  A61K31/661 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  C07F9/65586 ,  C07F9/65744 ,  C07H19/11 ,  A61K2300/00

Abstract: The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Abstract translation: 本发明涉及式（I）的环磷酸酯取代的核苷衍生物：（结构）及其药学上可接受的盐，其中B，X，R 1，R 2和R 3如本文所定义，以及使用 用于治疗或预防患者HCV感染的环磷酸酯取代的核苷衍生物。

公开(公告)号：US09242988B2

公开(公告)日：2016-01-26

申请号：US14436697

申请日：2013-10-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： Vinay Girijavallabhan ,  Stephane Bogen ,  Weidong Pan ,  Qun Dang ,  Ian Davies

IPC: C07H19/12 ,  C07H19/23 ,  A61K31/7052 ,  A61P31/14 ,  C07D487/04 ,  A61K38/21 ,  A61K45/06 ,  A61K31/7056 ,  A61K31/706 ,  A61K47/48 ,  C07F9/6561 ,  C07F9/6574

CPC classification number: C07D487/04 ,  A61K31/7056 ,  A61K31/706 ,  A61K38/212 ,  A61K45/06 ,  A61K47/48215 ,  A61K47/60 ,  C07F9/65616 ,  C07F9/65744 ,  A61K2300/00

Abstract: Compounds of Formula (I) are disclosed, wherein R1, R2, R3, R4, R5, and R18 are defined herein. The compounds encompassed by Formula (I) include compounds which are HCV NS5B inhibitors and other compounds which can be metabolized in vivo to HCV NS5B inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 公开了式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5和R 18在本文中定义。 由式（I）包括的化合物包括HCV NS5B抑制剂和可以在体内被代谢为HCV NS5B抑制剂的其它化合物。 该化合物及其药学上可接受的盐可用于预防或治疗HCV的感染以及由HCV引起的疾病发作的预防，治疗或延迟。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。