- IMMUNOCONJUGATES TARGETING HER2
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The invention provides an immunoconjugate of formula (I) or (II). Antibody-adjuvant immunoconjugates of the invention, comprising an antibody construct that has an antigen binding domain that binds human epidermal growth factor receptor 2 ("HER2") linked to one or more adjuvants, demonstrate superior pharmacological properties over conventional antibody conjugates. The invention further provides compositions comprising and methods of treating cancer with the immunoconjugate.
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Paragraph 0366-0367
(2020/10/09)
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- MACROMOLECULE-SUPPORTED TLR AGONISTS
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The invention provides a macromolecule-supported compound of formula (I) or (II). Macromolecule-supported compounds of the invention, comprising macromolecular support linked to one or more TLR agonists, are recognized by TLRs (e.g., TLR7 and/or TLR8) with high affinity providing utility in therapeutics, diagnostics, and chemical assays. The invention further provides compositions comprising and methods of treating cancer with the macromolecule- supported compounds.
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Paragraph 0264-0265
(2020/10/09)
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- IMMUNOCONJUGATES TARGETING PD-L1
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The invention provides an immunoconjugate of formula (I) or (II). Antibody-adjuvant immunoconjugates of the invention, comprising an antibody construct that has an antigen binding domain that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants, demonstrate superior pharmacological properties over conventional antibody conjugates. The invention further provides compositions comprising and methods of treating cancer with the immunoconjugate.
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Paragraph 0299; 0300
(2020/10/09)
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- IMMUNOCONJUGATES TARGETING CEA
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The invention provides an immunoconjugate of formula (I) or (II). Antibody-adjuvant immunoconjugates of the invention, comprising an antibody construct that has an antigen binding domain that binds carcinoembryonic antigen ("CEA") linked to one or more adjuvants, demonstrate superior pharmacological properties over conventional antibody conjugates. The invention further provides compositions comprising and methods of treating cancer with the immunoconjugate.
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Paragraph 0287-0288
(2020/10/09)
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- IMMUNOCONJUGATES
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The invention provides an immunoconjugate comprising (a) an antibody construct comprising (i) an antigen binding domain and (ii) an Fc domain and (b) 1-8 adjuvant cores, wherein each adjuvant core is covalently bonded to the antibody construct via a linker, wherein each adjuvant core comprises a 2-amino nitrogen moiety with a pendant nitrogen atom and a point of attachment of the linker to the adjuvant core, and wherein the distance between the pendant nitrogen atom and the point of attachment of the linker is greater than about 5 ?. The invention also provides methods for treating cancer with the immunoconjugates.
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Paragraph 0375; 0376
(2019/12/04)
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- NLRP3 MODULATORS
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The present invention provides compounds of Formula (I): wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subjec
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Paragraph 111-113
(2019/11/12)
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- Topsentin derivatives as well as preparation and application thereof in resistance to plant viruses and germs
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The invention relates to Topsentin derivatives I as well as preparation and application thereof in resistance to plant viruses and germs. The Topsentin derivatives I show especially excellent anti-plant virus activity, can well inhibit tobacco mosaic viruses (TMV), and also show good anti-plant germ activity, and details of referred content of substituent groups in a general formula see the specification. (The general formula is described in the specification).
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- Discovery of Topsentin Alkaloids and Their Derivatives as Novel Antiviral and Anti-phytopathogenic Fungus Agents
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Topsentin alkaloids and their derivatives were designed, synthesized, and characterized on the basis of NMR and mass spectroscopy. The antiviral activities against tobacco mosaic virus (TMV) and anti-phytopathogenic fungus activities of these alkaloids were evaluated for the first time. Alkaloids 1c, 1e, 2b, and 2d displayed significantly higher antiviral activities against TMV than Ribavirin, emerging as new lead compounds for anti-TMV research. Further fungicidal activity tests against 14 kinds of phytopathogenic fungi revealed that these alkaloids displayed broad-spectrum fungicidal activities. Topsentin derivative 2d with 4-5 mg/kg EC50 values against Sclerotinia sclerotiorum (Lib.), Rhizoctonia solani (Kuhn), and Botrytis cinerea (Pers.) emerged as a new lead compound for fungicidal research. Current studies provide support for the application of topsentin alkaloids as novel agrochemicals.
- Ji, Xiaofei,Wang, Ziwen,Dong, Ji,Liu, Yuxiu,Lu, Aidang,Wang, Qingmin
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p. 9143 - 9151
(2016/12/16)
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- Rhodium-catalyzed enantioselective 1,2-addition of arylboronic acids to heteroaryl α-ketoesters for synthesis of heteroaromatic α-hydroxy esters
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The first example of catalytic asymmetric 1,2-addition of arylboronic acids to heteroaryl α-ketoesters has been developed for the highly efficient and enantioselective synthesis of quaternary carbon-containing heteroaromatic α-hydroxy esters. The reaction works well with a variety of α-ketoesters including 3-indoleglyoxylates, 3-benzofuranglyoxylates and 3-benzothiopheneglyoxylates under very mild conditions, affording the corresponding products in moderate to good yields with high enantiomeric excesses (up to 97%).
- Wang, Hui,Zhu, Ting-Shun,Xu, Ming-Hua
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p. 9158 - 9164,7
(2012/12/12)
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- Rhodium-catalyzed enantioselective 1,2-addition of arylboronic acids to heteroaryl α-ketoesters for synthesis of heteroaromatic α-hydroxy esters
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The first example of catalytic asymmetric 1,2-addition of arylboronic acids to heteroaryl α-ketoesters has been developed for the highly efficient and enantioselective synthesis of quaternary carbon-containing heteroaromatic α-hydroxy esters. The reaction works well with a variety of α-ketoesters including 3-indoleglyoxylates, 3-benzofuranglyoxylates and 3-benzothiopheneglyoxylates under very mild conditions, affording the corresponding products in moderate to good yields with high enantiomeric excesses (up to 97%).
- Wang, Hui,Zhu, Ting-Shun,Xu, Ming-Hua
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p. 9158 - 9164
(2013/01/15)
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