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公开(公告)号:US12180264B2
公开(公告)日:2024-12-31
申请号:US17474718
申请日:2021-09-14
Applicant: R-Pharm Overseas, Inc.
Inventor: Yan Lavrovsky , Alexey Repik , Mikhail Samsonov , Sergei Barbashov , Vasily Ignatiev
IPC: C07K14/715 , A61K38/00
Abstract: A therapeutic composition is described that can be used for treating or prevention of diseases association with modulation of activity of human IL-1β. In certain aspects, the disclosed composition is based on engineering of a heterodimeric protein assembly that is capable of binding to human IL-1β and attenuating its function. The heterodimeric protein assembly comprises extracellular portions of human IL1-R1 and of human IL-1RAcP, or their functional fragments. Each, the IL1-R1 portion and the IL-1RAcP portion, is fused to a distinct mutant of Fc portion of the human Ig Gamma-1. The two distinct Fc mutants in the heterodimeric protein assembly are engineered as to favor the heteromeric dimer formation between the two Fc mutants over any homomeric assembly. The therapeutic composition has been formulated for administration into humans and animals.
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公开(公告)号:US20210403534A1
公开(公告)日:2021-12-30
申请号:US17474718
申请日:2021-09-14
Applicant: R-Pharm Overseas, Inc.
Inventor: Yan Lavrovsky , Alexey Repik , Mikhail Samsonov , Sergei BARBASHOV , Vasily IGNATIEV
IPC: C07K14/715
Abstract: A therapeutic composition is described that can be used for treating or prevention of diseases association with modulation of activity of human IL-1β. In certain aspects, the disclosed composition is based on engineering of a heterodimeric protein assembly that is capable of binding to human IL-1β and attenuating its function. The heterodimeric protein assembly comprises extracellular portions of human IL1-R1 and of human IL-1RAcP, or their functional fragments. Each, the IL1-R1 portion and the IL-1RAcP portion, is fused to a distinct mutant of Fc portion of the human Ig Gamma-1. The two distinct Fc mutants in the heterodimeric protein assembly are engineered as to favor the heteromeric dimer formation between the two Fc mutants over any homomeric assembly. The therapeutic composition has been formulated for administration into humans and animals.
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公开(公告)号:US20180179164A1
公开(公告)日:2018-06-28
申请号:US15324658
申请日:2015-06-26
Applicant: R-Pharm Overseas Inc.
Inventor: Alexandre Vasilievich IVACHTCHENKO
IPC: C07D233/86 , C07D491/107 , C07C229/60 , C07D307/24 , C07C227/16 , A61P35/00
Abstract: Novel (R)-stereoisomers of substituted 2-thioxo-imidazolidin-4-ones of formula 1, or spiro analogues thereof, which exhibit androgen receptor antagonist properties. Also provided are variants of a method for producing the same, intermediate compounds for producing compounds of formula 1, and pharmaceutical compositions containing compounds of formula 1 in the form of tablets, capsules, and/or injections. Compounds of formula 1 can be used to produce a medicinal agent suitable for treating cancers, such as prostate cancer and breast cancer. The compounds of formula 1 may have the structure: wherein R1 is OH, NH2, or an OR4 group; R2 and R3 are methyl, or R2 and R3 are a CH2—CH2 group; and R4 is C1-C4 alkyl or cyclopropyl.
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公开(公告)号:US20170226185A1
公开(公告)日:2017-08-10
申请号:US15129412
申请日:2014-03-24
Applicant: R-Pharm Overseas, Inc.
Inventor: Yan Lavrovsky , Ting Xu , Elena Batienko , Anna Krotkova , Vasily Ignatiev , Mikhail Samsonov , Alexey Repik
IPC: C07K14/715
CPC classification number: C07K14/7155 , A61K38/00 , A61K38/1793 , C07K14/715 , C07K2319/30
Abstract: A therapeutic composition is described that can be used for treating or prevention of diseases association with modulation of activity of human IL-1β. In certain aspects, the disclosed invention is based, on engineering of a heterodimeric protein assembly that is capable of binding to human IL-1β and attenuating its function. The heterodimeric protein assembly comprises extracellular portions of human IL1-R1 and of human IL-1RAcP, or their functional fragments. Each, the IL1-R1 portion and the IL-1RAcP portion, is fused to a distinct mutant of Fc portion of the human Ig Gamma-1. The two distinct Fc mutants in the heterodimeric protein assembly are engineered as to favor the heteromeric dimer formation between the two Fc mutants over any homomeric assembly. The therapeutic composition has been formulated for administration into humans and animals.
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公开(公告)号:US20170073391A1
公开(公告)日:2017-03-16
申请号:US15124026
申请日:2014-03-06
Applicant: R-Pharm Overseas, Inc.
Inventor: Yan Lavrovsky , Ting Xu , Irina Kostareva , Shorena Archuadze , Vasily Ignatiev , Mikhail Samsonov , Alexey Repik
IPC: C07K14/705
CPC classification number: C07K14/70578 , A61K38/00 , C07K2319/30 , C07K2319/32
Abstract: A pharmaceutical composition is described that can be used for treating or prevention of diseases association with bone resorption, particularly of a metastatic carcinoma. In certain aspects, the composition is based on a polypeptide which includes the leading 215 amino acids of the human osteoprotegerin followed by the Fc portion of the human IgG1 protein. Pharmaceutical formulations are provided that are suitable for administering the pharmaceutical composition into primates via subcutaneous and intravenous routes.
Abstract translation: 描述了可用于治疗或预防与骨吸收相关的疾病,特别是转移性癌的药物组合物。 在某些方面,组合物是基于多肽,其包括人骨保护素的前导215个氨基酸,随后是人IgG1蛋白的Fc部分。 提供了适于通过皮下和静脉内途径将药物组合物施用于灵长类动物的药物制剂。
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公开(公告)号:US20240307490A1
公开(公告)日:2024-09-19
申请号:US18672826
申请日:2024-05-23
Applicant: R-Pharm Overseas, Inc.
Inventor: Mikhail Samsonov , Alexey Maslyansky , Sergey Grishin , Alexey Repik , Yan Lavrovsky
CPC classification number: A61K38/1793 , A61K9/0019 , A61P9/00 , A61P29/00 , A61P37/06
Abstract: Disclosed invention provides for methods of treating idiopathic recurrent pericarditis (IRP), including a step of administering to a subject in need of treatment a heterodimeric IL-1R1/IL-1RAcP-derived composition at a therapeutically effective dose and an administration interval for a treatment period sufficient to reduce the risk of pericarditis recurrence relative to a control.
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公开(公告)号:US11155600B2
公开(公告)日:2021-10-26
申请号:US15129412
申请日:2014-03-24
Applicant: R-Pharm Overseas, Inc.
Inventor: Yan Lavrovsky , Ting Xu , Elena Batienko , Anna Krotkova , Vasily Ignatiev , Mikhail Samsonov , Alexey Repik
IPC: C07K14/715 , A61K38/17 , A61K38/00
Abstract: A therapeutic composition is described that can be used for treating or prevention of diseases association with modulation of activity of human IL-1β. In certain aspects, the disclosed invention is based, on engineering of a heterodimeric protein assembly that is capable of binding to human IL-1β and attenuating its function. The heterodimeric protein assembly comprises extracellular portions of human IL1-R1 and of human IL-1RAcP, or their functional fragments. Each, the IL1-R1 portion and the IL-1RAcP portion, is fused to a distinct mutant of Fc portion of the human Ig Gamma-1. The two distinct Fc mutants in the heterodimeric protein assembly are engineered as to favor the heteromeric dimer formation between the two Fc mutants over any homomeric assembly. The therapeutic composition has been formulated for administration into humans and animals.
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公开(公告)号:US20210115143A1
公开(公告)日:2021-04-22
申请号:US16606647
申请日:2018-04-18
Applicant: R-PHARM OVERSEAS, INC.
Inventor: Yan LAVROVSKY , Ting XU , Sergei BARBASHOV , Alexey REPIK , Mikhail SAMSONOV , Vasily IGNATIEV , Shorena ARCHUADZE
Abstract: Fully human anti-PD-L1 antibodies and their corresponding applications. Fully human antibodies capable of specifically binding to human PD-L1 were obtained by employing a yeast display library-based screening technique and also by affinity maturation to further improve their affinity for PD-L1. The fully human anti-PD-L1 antibodies show good specificity, affinity and stability. They are capable of enhancing T cell activity by binding to activated T cells, while significantly inhibiting tumor growth, and can be used in the diagnosis and treatment of PD-L1-related cancers and other associated diseases.
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公开(公告)号:US10450278B2
公开(公告)日:2019-10-22
申请号:US15324658
申请日:2015-06-26
Applicant: R-Pharm Overseas Inc.
Inventor: Alexandre Vasilievich Ivachtchenko
IPC: C07D233/86 , C07D491/107 , C07D307/24 , C07C229/60 , C07C227/16 , A61P35/00 , A61K31/4166 , A61K31/4188
Abstract: Novel (R)-stereoisomers of substituted 2-thioxo-imidazolidin-4-ones of formula 1, or spiro analogues thereof, which exhibit androgen receptor antagonist properties. Also provided are variants of a method for producing the same, intermediate compounds for producing compounds of formula 1, and pharmaceutical compositions containing compounds of formula 1 in the form of tablets, capsules, and/or injections. Compounds of formula 1 can be used to produce a medicinal agent suitable for treating cancers, such as prostate cancer and breast cancer. The compounds of formula 1 may have the structure: wherein R1 is OH, NH2, or an OR4 group; R2 and R3 are methyl, or R2 and R3 are a CH2—CH2 group; and R4 is C1-C4 alkyl or cyclopropyl.
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