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1.
公开(公告)号:WO2021214315A1
公开(公告)日:2021-10-28
申请号:PCT/EP2021/060719
申请日:2021-04-23
申请人: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES , WOMEN & INFANTS HOSPITAL OF RHODE ISLAND , SCIENTIAM PHARMA
发明人: MABONDZO, Aloïse , GUYOT, Anne-Cécile , PRUVOST, Alain , COSTA, Narciso , GALONS, Hervé , OUMATA, Nassima , STONESTREET, Barbara , DISDIER, Clémence
IPC分类号: C07D473/04 , C07D473/16 , C07D473/18 , A61P25/00 , A61K31/52 , A61K31/522
摘要: The present invention relates to a compound of formula (I), for use in the treatment of non-traumatic acquired brain injury, in which M represents a NR1R2 group, an OR1 group or a SR1 group, A represents a NR4R5 group, an OR10 group or a hydrogen atom, R3 is a (C1-C6)alkyl group, a (C1-C6)cycloalkyl group, an aryl group, a -CH2-aryl group, a CH2-(C1-C6)cycloalkyl group or a -CH2-heteroaryl group, and its addition salts with pharmaceutically acceptable acids. The present invention further relates to a compound of formula (I) wherein R5 is a (C1-C8)alkyl group or a (C1-C6)cycloalkyl group, said alkyl and cycloalkyl group being substituted with one, two or three -OCORa group(s).
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公开(公告)号:WO2021208459A1
公开(公告)日:2021-10-21
申请号:PCT/CN2020/134260
申请日:2020-12-07
申请人: 深圳大学 , 深圳市康居正医药科技有限公司
IPC分类号: C07D473/18 , C07D519/00 , C07F9/6584 , C07F9/6561 , C07K7/06 , C07K5/023 , A61P35/00 , A61P37/04 , A61P31/12 , A61K31/52 , A61K31/551 , A61K31/5377 , A61K31/675 , A61K38/07 , A61K38/08
摘要: 一系列新型的Toll样受体7的小分子免疫激动剂,如式I所示。还提供了所述免疫激动剂用于激活和扩增免疫细胞和淋巴细胞、制备免疫调节药物、免疫抗肿瘤小分子和免疫抗肿瘤大分子药物的用途。
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公开(公告)号:WO2021198239A1
公开(公告)日:2021-10-07
申请号:PCT/EP2021/058268
申请日:2021-03-30
IPC分类号: C07D473/18 , C07D519/00 , G01N33/58 , G01N2500/10 , G01N33/582
摘要: The invention relates to a compound of formula I: wherein - A is present or absent; - X1, X2, X3 and X4 are, independently from each other, an alkyl; - Y1, Y2, Y3 and Y4 are independently from each other a C1-C10 alkyl, - Z1, Z2, Z3 and Z4 are independently from each other a C1-C5 linear alkyl; - R1 is a group allowing to carry out bioorthogonal reactions; and - R2 is group comprising a N.
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公开(公告)号:WO2021182491A1
公开(公告)日:2021-09-16
申请号:PCT/JP2021/009406
申请日:2021-03-10
申请人: キッセイ薬品工業株式会社
IPC分类号: C07D473/18 , A61K31/522 , A61P1/04
摘要: 原薬としては、良好な物性を有する結晶が好ましい。しかしながら、いかなる結晶形が原薬として最も優れているかは、化合物ごとに異なる。一般的に、良好な物性を有する原薬の結晶形を予想することは困難であり、各化合物について、種々の検討が求められる。したがって、本発明は、新規化合物について、原薬として良好な物性を有する結晶を提供することを課題とする。 本発明は、炎症性腸疾患の治療に有用な下記式(I)で表される化合物の結晶に関する。
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5.
公开(公告)号:WO2020198367A1
公开(公告)日:2020-10-01
申请号:PCT/US2020/024727
申请日:2020-03-25
IPC分类号: C07D473/16 , C07D473/18 , A61K31/52 , A61K31/5377 , A61P7/06
摘要: Provided herein are compounds of Formula (I). The compounds described herein are useful in treating a disease associated with the expression of endogenous embryonic/fetal globin (e.g., γ globin) in erythrocytes (e.g., treating β -thalassemia and/or sickle cell disease through at least the induction of the globin gene expression in erythrocytes), and/or anemia (β-thalassemia and/or sickle cell anemia). The compounds described herein are useful in treating, delaying, and/or preventing the adverse effects of β-thalassemia and/or sickle cell disease, inducing γ globin production, and/or inducing the expression of embryonic/fetal globin genes in a subject, cell, tissue, or biological sample. Also provided in the present disclosure are pharmaceutical compositions, kits, and methods of using the compounds for inducing γ globin production described herein and for treating any of the target diseases described herein.
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公开(公告)号:WO2020124688A1
公开(公告)日:2020-06-25
申请号:PCT/CN2019/000193
申请日:2019-10-10
申请人: 中国科学院大连化学物理研究所
IPC分类号: C09K11/06 , C07D221/14 , C07D473/18 , G01N21/64 , C07K1/13
摘要: 本发明提供了一种全光谱高亮度、高稳定性荧光染料,该染料由4-酰胺基取代萘酰亚胺类染料、双烷氧基取代的萘酰亚胺类荧光染料、双氨基取代萘酰亚胺类荧光染料、9,10-双氨基取代苝酰亚胺、六元环并罗丹明类染料、五元环并罗丹明类染料、硅基罗丹明类染料中的一种或几种按任意比混合。相比于目前的商业染料,本发明的荧光染料光稳定性更高,半峰宽更窄(25nm),对pH、极性、温度等多种外界环境均保持不敏感性。通过Click基团、蛋白标签、药物分子等活性基团的引入,得到的功能化荧光分子具有很高的生物相容性,能够对活细胞及活体进行快速、特异性染色。此外,由于光稳定性及荧光亮度的提升,该系列染料实现了Storm,STED、SIM等多种模式下的超分辨荧光成像。
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公开(公告)号:WO2020121123A3
公开(公告)日:2020-06-18
申请号:PCT/IB2019/060431
申请日:2019-12-04
发明人: ZHONG, Minghong , WANG, Guangyi
IPC分类号: C07D239/47 , C07D239/54 , C07D473/18 , C07D473/34 , C07D487/04 , C07F9/09 , C07F9/24 , A61P31/12 , A61P31/20 , A61K31/513 , A61K31/519 , A61K31/52 , A61K31/6615 , A61K31/664 , A61K31/685
摘要: Described herein are cyclopentyl nucleoside analogs of Formula (I), pharmaceutical compositions that include one or more cyclopentyl nucleoside analogs and methods of using the same to treat HBV, HDV and/or HIV. (I)
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公开(公告)号:WO2019172835A1
公开(公告)日:2019-09-12
申请号:PCT/SE2019/050209
申请日:2019-03-08
申请人: MEDIVIR AKTIEBOLAG
发明人: KLASSON, Björn , ÖBERG, Fredrik
IPC分类号: C07F9/6561 , A61K31/675 , A61P35/00 , C07F9/6512 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/685 , C07D239/36 , C07D239/54 , C07D473/16 , C07D473/18 , C07D473/30 , C07D473/34
摘要: The invention provides a compound of formula (I) wherein B is a nucleobase; U is O or S; R x is -OC(=O)R y , -OC(=O)CH(R y )NH 2 , -OCH 2 OC(=O)R y ; R y is optionally substituted alkyl or alkenyl or the side chain of a natural or unnatural amino acid R 1 is H, or optionally substituted phenyl, benzyl, naphthyl, pyridyl or indolyl, or R x and R 1 together define a bond thus forming a cyclic phosphate; R 2 and R 2' together define the side chain of a natural or unnatural amino acid; R 3 is optionally substituted alkyl, cycloalkyl, phenyl or benzyl; and pharmaceutically acceptable salts and compositions thereof which are useful in the treatment of cancer, especially leukemias.
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9.
公开(公告)号:WO2019035971A1
公开(公告)日:2019-02-21
申请号:PCT/US2018/000246
申请日:2018-08-16
IPC分类号: C07D473/18 , A61K31/522 , A61P37/04
摘要: Compounds having a structure according to formula (I) or (II) where R 1 , R 2 , R 3 , R 4 , Ar and X 1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
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10.
公开(公告)号:WO2019035970A1
公开(公告)日:2019-02-21
申请号:PCT/US2018/000245
申请日:2018-08-16
IPC分类号: C07D473/18 , A61K31/522 , A61P37/04
摘要: Compounds having a structure according to formula (I) or (II), where R 1 , R 2 , and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
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