公开(公告)号：US11180524B2

公开(公告)日：2021-11-23

申请号：US16647236

申请日：2018-09-14

Applicant: Janssen BioPharma, Inc.

Inventor： Sergei Gryaznov ,  Jin Hong ,  Vivek Kumar Rajwanshi ,  Leonid Beigelman

IPC: C07H19/10 ,  C07H19/00 ,  C07H19/20 ,  C07H1/00

Abstract: The present disclosure relates to compounds and compositions containing 5′-phosphoramidite nucleoside monomers of formulae (I) and (II), and methods of making and use, wherein the substituents are as defined in the appended claims.

公开(公告)号：US12077757B2

公开(公告)日：2024-09-03

申请号：US17063080

申请日：2020-10-05

Applicant: Janssen Biopharma, Inc.

Inventor： Sergei Gryaznov ,  Leonid Beigelman ,  Antitsa Dimitrova Stoycheva ,  Saul Martinez Montero ,  Jin Hong ,  Rajendra K. Pandey ,  Vivek Kumar Rajwanshi ,  Lakshmipathi Pandarinathan ,  Yi Jin ,  Bharat Baral

IPC: C07H21/02 ,  A61K31/712 ,  A61K31/7125 ,  A61K47/54 ,  A61P31/20 ,  C12N15/11 ,  C12N15/113

CPC classification number: C12N15/1131 ,  A61K31/712 ,  A61K31/7125 ,  A61K47/549 ,  A61P31/20 ,  C07H21/02 ,  C12N15/111 ,  C12N2310/11 ,  C12N2310/314 ,  C12N2310/3145 ,  C12N2310/315 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/344 ,  C12N2310/351 ,  C12N2320/32 ,  C12N2310/321 ,  C12N2310/3525

Abstract: Modified oligonucleotides comprising modifications at the 2′ and/or 3′ position(s) along with methods of making and use, e.g., against HBV are disclosed.

公开(公告)号：US10793859B2

公开(公告)日：2020-10-06

申请号：US15705137

申请日：2017-09-14

Applicant: Janssen BioPharma, Inc.

Inventor： Sergei Gryaznov ,  Leonid Beigelman ,  Antitsa Dimitrova Stoycheva ,  Saul Martinez Montero ,  Jin Hong ,  Rajendra K. Pandey ,  Vivek Kumar Rajwanshi ,  Lakshmipathi Pandarinathan ,  Yi Jin ,  Bharat Baral

IPC: C07H21/02 ,  C07H21/04 ,  C12N15/113 ,  C12N15/11 ,  A61K31/712 ,  A61K47/54 ,  A61P31/20 ,  A61K31/7125

Abstract: Modified oligonucleotides comprising modifications at the 2′ and/or 3′ positions(s) along with methods of making and use, e.g., against HBV are disclosed.

公开(公告)号：US12030907B2

公开(公告)日：2024-07-09

申请号：US17514168

申请日：2021-10-29

Applicant: Janssen BioPharma, Inc.

Inventor： Sergei Gryaznov ,  Jin Hong ,  Vivek Kumar Rajwanshi ,  Leonid Beigelman

IPC: C07H19/10 ,  C07H1/00 ,  C07H19/20

CPC classification number: C07H19/10 ,  C07H1/00 ,  C07H19/20

Abstract: A method of making a compound represented by Formula (I):




includes a reducing step, a protecting step, and a phosphitylating step, where X is NH; Y is OCF3, —O(CR42)aCR43, —O(CR42)bOCR43, or —O(CR42)b—CR4═CR42; Z is H; B is adenine (A), guanine (G), thymine (T), cytosine (C), uracil (U), 5-methylcytosine (5-me-C), or a protected version of A, G, T, C, U, or 5-me-C; each R1 is independently C1-6 alkyl or cycloalkyl; R2 is CH2CH2CN or C1-6 alkyl; or R1 and R2 together form an optionally substituted C1-6 cycloalkyl; R3 is H or PG; PG is a protecting group; R4 is independently in each instance H or F; a is 1 or 2; and b is 1, 2, or 3.