- NOVEL THYROMIMETICS
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Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, X1, X2, Q, R1, R2 and n are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
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Page/Page column 101
(2020/09/19)
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- 2-(2-ACRYLOYL-2,6-DIAZASPIRO[3.4]OCTAN-6-YL)-6-(1H-INDAZOL-4-YL)-BENZONITRILE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF G12C MUTANT KRAS PROTEIN FOR INHIBITING TUMOR METASTASIS
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The present invention provides e.g. 2-(2-acryloyl-2,6- diazaspiro[3.4]octan-6-yl)-6-(lH-indazol-4-yl)-benzonitrile and e.g. 2-(2-acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-6-(1H-indazol-4-yl)- benzonitrile derivatives and related compounds of formula (I) as inhibitors of G12C mutant KRAS protein for treating tumor metastasis. The present description discloses exemplary compounds (e.g. pages 53 to 90; table 1; compounds I-1 to I-141), pharmacological data (e.g. page 125 to 128; table 2; example 1) and synthesis thereof (e.g. pages 129 to 143; examples 2 to 7). Exemplary compounds are e.g. 2-(2-acryloyl-2,6- diazaspiro[3.4]octan-6-yl)-6-(5-methyl-1H-indazol-4-yl)-4- morpholinobenzonitrile (example 2; compound I-1) and 6-(2- acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-3-methoxy-2-(5-methyl-1H- indazol-4-yl)-4-morpholinobenzonitrile (example 7; compound I-84).
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Page/Page column 137; 138
(2020/05/28)
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- DERIVATIVES OF SOBETIROME
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Compounds are provided that function as thyromimetics, which compounds have utility for treating diseases such as neurodegenerative disorders. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation. Such compounds have the structure of Formula (I) as shown herein, or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof.
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Page/Page column 39; 40
(2019/09/04)
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- Synthesis and arm dissociation in molecular stars with a spoked wheel core and bottlebrush arms
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Unique star-like polymeric architectures composed of bottlebrush arms and a molecular spoked wheel (MSW) core were prepared by atom transfer radical polymerization (ATRP). A hexahydroxy-functionalized MSW (MSW6-OH) was synthesized and converted into a six-fold ATRP initiator (MSW6-Br). Linear chain arms were grafted from MSW6-Br and subsequently functionalized with ATRP moieties to form six-arm macroinitiators. Grafting of side chains from the macroinitiators yielded four different star-shaped bottlebrushes with varying lengths of arms and side chains, i.e., (450-g-20)6, (450-g-40)6, (300-g-60)6, and (300-g-150)6. Gel permeation chromatography analysis and molecular imaging by atomic force microscopy confirmed the formation of well-defined macromolecules with narrow molecular weight distributions. Upon adsorption to an aqueous substrate, the bottlebrush arms underwent prompt dissociation from the MSW core, followed by scission of covalent bonds in the bottlebrush backbones. The preferential cleavage of the arms is attributed to strong steric repulsion between bottlebrushes at the MSW branching center. Star-shaped macroinitiators may undergo aggregation which can be prevented by sonication.
- Burdyska, Joanna,Li, Yuanchao,Aggarwal, Anant Vikas,H?ger, Sigurd,Sheiko, Sergei S.,Matyjaszewski, Krzysztof
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supporting information
p. 12762 - 12770
(2014/12/10)
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- INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING VLA-4
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The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.
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Page/Page column 75
(2013/08/15)
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- TETRACYCLIC INHIBITORS OF JANUS KINASES
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The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
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Page/Page column 106
(2008/06/13)
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- Novel triarylimidazoles
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Compounds of the general formula (I) are presented and are valuable therapeutics for the treatment of cancer and cancer related diseases.
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Page/Page column 7
(2010/02/11)
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- Simple, short and efficient procedure for the preparation of hydroxyl- and hydroxymethyl-substituted 2,6-dichlorobenzaldehydes
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Hydroxyl- and hydroxymethyl-substituted 2,6-dichlorobenzaldehydes 1-4 have been obtained by lithiation of the corresponding TIPS-protected dichlorophenols or dichlorobenzylic alcohols followed by reaction with DMF and subsequent deprotection of the hydroxy group. Yields are high and formation of regioisomers is not observed.
- Von Hirschheydt, Thomas,Voss, Edgar
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p. 2062 - 2065
(2007/10/03)
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- 2-(2,6-dichlorophenyl)-diarylimidazoles
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The invention is directed to compounds of formula (I), which are valuable therapeutics for the treatment of cancer and related diseases.
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Page/Page column 6
(2010/11/29)
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