- RAC INHIBITORS
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The present invention relates to compounds that act as pan-Rac inhibitors, compositions including the compounds, and methods of using the compounds. In particular, the compounds are useful for treating certain cancers such as breast cancer.
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Paragraph 0570-0572
(2019/02/13)
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- Hydrotropic polymer-based paclitaxel-loaded self-assembled nanoparticles: Preparation and biological evaluation
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The poor compatibility of carrier materials with drugs is one of the main obstacles in the drug encapsulation of nano-drug delivery system (NDDS), hindering the clinical translation of NDDS. In this study, using paclitaxel (PTX) as the insoluble model drug, we conjugated N,N-diethylniacinamide (DENA), a hydrotropic agent of PTX, to the backbone of poly(l-γ-glutamyl-glutamine) (PGG), a water-soluble polymer, to prepare the "hydrotropic polymer" PGG-DENA to improve its compatibility with PTX. By virtue of the hydrotropic effect of the DENA group, PTX was encapsulated by PGG-DENA to obtain the hydrotropic polymeric nanoparticles (PGG-DENA/PTX NPs). PTX-conjugated poly(l-γ-glutamyl-glutamine) acid (PGG-PTX) NPs previously reported were used as the control in the study. The PGG-DENA/PTX NPs showed a z-average hydrodynamic diameter of about 70 nm, and good long-term stability in PBS solution at 4 °C. The cumulative release rate of PTX from PGG-DENA/PTX NPs reached 79.10% at 96 h, while that of PGG-PTX NPs was 22.96%. PGG-DENA/PTX NPs showed significantly increased in vitro cytotoxicity on NCI-H460 lung cancer cells compared with PGG-PTX NPs. The hemolysis study proved that the PGG-DENA/PTX NPs has good biocompatibility. These results indicated that by introducing the hydrotropic agent DENA, the hydrotropic polymer PGG-DENA becomes an effective carrier material of PTX. This study provides a solution to increase the compatibility of carrier materials with insoluble drugs, and also may provide an effective way to develop a series of personalized carrier materials suitable for different insoluble drugs.
- Gao, Lipeng,Gao, Liefang,Fan, Mingxue,Li, Qilong,Jin, Jiyu,Wang, Jing,Lu, Weiyue,Yu, Lei,Yan, Zhiqiang,Wang, Yiting
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p. 33248 - 33256
(2017/07/12)
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- HETEROARYLCARBOXAMIDE DERIVATIVES AS PLASMA KALLIKREIN INHIBITORS
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The present invention relates to compounds of general formula I, wherein D1 to D3, A, R1, R2, Y and n are defined as in claim 1, which have valuable pharmacological properties, in particular are inhibitors of pl
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Page/Page column 48; 58
(2017/05/21)
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- HETEROARYLCARBOXAMIDE DERIVATIVES AS PLASMA KALLIKREIN INHIBITORS
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The present invention relates to compounds of general formula (I), wherein D 1 to D 3, -A-, n, R 1, R 2, Y 1, L and y2 are defined as in claim 1, which have valuable pharmacological propert
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Page/Page column 53; 63
(2017/06/01)
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- SYNTHESIS OF TRITHIOCARBONATES AND ALLYL SULFIDES AND THEIR APPLICATION INTO ADVANCES IN COVALENT ADAPTABLE NETWORKS
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Monomers having a C-B-A-B-C structure are disclosed, where A is a core of either trithiocarbonate and allyl sulfide, where B are linker units, and where C are end units. The end units may comprise acrylates, methacrylates, alcohol(s), amine(s), and alkyne
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Paragraph 0099
(2014/10/16)
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- Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. Separation of the antithrombotic effect and bleeding for candidate drug AZD1283
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Synthesis and structure-activity relationships of ethyl 6-aminonicotinate acyl sulfonamides, which are potent antagonists of the P2Y12 receptor, are presented. Shifting from 5-chlorothienyl to benzyl sulfonamides significantly increased the pot
- Bach, Peter,Antonsson, Thomas,Bylund, Ruth,Bj?rkman, Jan-Arne,?sterlund, Krister,Giordanetto, Fabrizio,Van Giezen,Andersen, S?ren M.,Zachrisson, Helen,Zetterberg, Fredrik
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p. 7015 - 7024
(2013/10/01)
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- NEW PYRIDINE ANALOGUES
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The present invention relates to certain new pyridin analogues of Formula ( I ), to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
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Page/Page column 165
(2008/06/13)
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