公开(公告)号：US12030907B2

公开(公告)日：2024-07-09

申请号：US17514168

申请日：2021-10-29

申请人： Janssen BioPharma, Inc.

发明人： Sergei Gryaznov ,  Jin Hong ,  Vivek Kumar Rajwanshi ,  Leonid Beigelman

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

CPC分类号： C07H19/10 ,  C07H1/00 ,  C07H19/20

摘要： 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.

公开(公告)号：US12077757B2

公开(公告)日：2024-09-03

申请号：US17063080

申请日：2020-10-05

申请人： Janssen Biopharma, Inc.

发明人： 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分类号： C07H21/02 ,  A61K31/712 ,  A61K31/7125 ,  A61K47/54 ,  A61P31/20 ,  C12N15/11 ,  C12N15/113

CPC分类号： 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

摘要： 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：US11021444B2

公开(公告)日：2021-06-01

申请号：US16165865

申请日：2018-10-19

申请人： Janssen BioPharma, Inc.

发明人： Guangyi Wang ,  Leonid Beigelman ,  Anh Truong ,  Carmela Napolitano ,  Daniele Andreotti ,  Haiying He ,  Karin Ann Stein

IPC分类号： C07D213/40 ,  A61K45/06 ,  A61K31/4355 ,  A61K31/505 ,  A61K31/427 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4365 ,  A61K31/4439 ,  A61K31/4178 ,  A61K31/4418 ,  A61K31/4436 ,  C07D491/052 ,  C07D207/273 ,  C07D417/12 ,  C07D405/12 ,  C07D401/06 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D409/14 ,  C07D233/64 ,  C07D491/048 ,  C07D401/12 ,  C07D213/65 ,  C07D471/04 ,  C07D239/34 ,  C07D417/04 ,  C07D413/04 ,  C07D401/04 ,  C07D495/14 ,  C07D409/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4709

摘要： Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

公开(公告)号：US20210106604A1

公开(公告)日：2021-04-15

申请号：US17001512

申请日：2020-08-24

申请人： Janssen BioPharma, Inc.

发明人： Lawrence M. Blatt ,  Leonid Beigelman ,  Natalia Dyatkina ,  Julian Alexander Symons ,  David Bernard Smith

IPC分类号： A61K31/7068 ,  A61K31/708 ,  A61K31/7072 ,  A61K31/7076

摘要： Disclosed herein are nucleosides, nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a Filoviridae virus infection with one or more nucleosides and/or nucleotide analogs.

公开(公告)号：US10793859B2

公开(公告)日：2020-10-06

申请号：US15705137

申请日：2017-09-14

申请人： Janssen BioPharma, Inc.

发明人： 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分类号： C07H21/02 ,  C07H21/04 ,  C12N15/113 ,  C12N15/11 ,  A61K31/712 ,  A61K47/54 ,  A61P31/20 ,  A61K31/7125

摘要： 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：US20200030328A1

公开(公告)日：2020-01-30

申请号：US16537396

申请日：2019-08-09

申请人： Janssen BioPharma, Inc.

发明人： Robert Than Hendricks ,  Leonid Beigelman ,  David Bernard Smith ,  Antitsa Dimitrova Stoycheva

IPC分类号： A61K31/5025 ,  C07D487/04 ,  A61K31/13 ,  A61K31/196 ,  A61K31/215 ,  A61K31/351 ,  A61K31/4965 ,  A61K31/5377 ,  A61K31/7056 ,  A61K38/21 ,  C07B59/00

摘要： Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection.

公开(公告)号：US11180524B2

公开(公告)日：2021-11-23

申请号：US16647236

申请日：2018-09-14

申请人： Janssen BioPharma, Inc.

发明人： Sergei Gryaznov ,  Jin Hong ,  Vivek Kumar Rajwanshi ,  Leonid Beigelman

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

摘要： 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：US10980805B2

公开(公告)日：2021-04-20

申请号：US16537396

申请日：2019-08-09

申请人： Janssen BioPharma, Inc.

发明人： Robert Than Hendricks ,  Leonid Beigelman ,  David Bernard Smith ,  Antitsa Dimitrova Stoycheva

IPC分类号： A61K31/5025 ,  C07D487/04 ,  A61K31/13 ,  A61K31/196 ,  A61K31/215 ,  A61K31/351 ,  A61K31/4965 ,  A61K31/5377 ,  A61K31/7056 ,  A61K38/21 ,  C07B59/00

摘要： Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection.

公开(公告)号：USRE48171E1

公开(公告)日：2020-08-25

申请号：US16130971

申请日：2018-09-13

申请人： Janssen BioPharma, Inc.

发明人： Guangyi Wang ,  David Bernard Smith ,  Leonid Beigelman ,  Jerome Deval ,  Marija Prhavc

IPC分类号： C07H19/06 ,  A61K31/708 ,  A61K31/706 ,  C07H19/20 ,  A61K31/7076 ,  C07H19/12 ,  C07H19/207 ,  A61K31/7068 ,  C07H19/16 ,  A61K31/7072 ,  C07H19/10

摘要： Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

公开(公告)号：US10745427B2

公开(公告)日：2020-08-18

申请号：US16090715

申请日：2017-03-09

申请人： Janssen BioPharma, Inc.

发明人： Leonid Beigelman ,  Guangyi Wang ,  Minghong Zhong

IPC分类号： A61K31/683 ,  A61K31/675 ,  C07F9/6561 ,  C07D487/04 ,  A61P31/18 ,  A61P31/20 ,  A61F13/511 ,  A61F13/513 ,  A61F13/512 ,  A61F13/514 ,  A61F13/51

摘要： Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HBV and/or HDV and/or HIV infection with one or more nucleotide analogs.