2987-06-6Relevant academic research and scientific papers
CYCLIC CYANOENONE DERIVATIVES AS MODULATORS OF KEAP1
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, (2022/01/24)
The present invention relates to cyclic cyanoenone derivatives of Formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R1, R2, R3, R4 and m are as defined herein. The present invention also relates to pharmaceutical compositions comprising the cyclic cyanoenone derivatives of Formula (I) and to their use in therapy.
EMULSION WITH IMPROVED BIOABSORPTION COMPOSITION COMPRISING CATIONIC POLYESTER COPOLYMER AND HYDROPHOBIC DRUG AND METHOD FOR PREPARING THE SAME
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, (2019/01/12)
The present invention relates to an emulsion composition with an improved bioabsorption rate containing a cationic polyester-based copolymer, and a poorly soluble drug. The emulsion composition comprises: a cationic polyester-based copolymer including a c
Hydrogen Borrowing Catalysis with Secondary Alcohols: A New Route for the Generation of β-Branched Carbonyl Compounds
Akhtar, Wasim M.,Cheong, Choon Boon,Frost, James R.,Christensen, Kirsten E.,Stevenson, Neil G.,Donohoe, Timothy J.
, p. 2577 - 2580 (2017/03/01)
A hydrogen borrowing reaction employing secondary alcohols and Ph? (Me5C6) ketones to give β-branched carbonyl products is described (21 examples). This new C-C bond forming process requires low loadings of [Cp?IrCl2]2, relatively low temperatures, and up to 2.0 equiv of the secondary alcohol. Substrate-induced diastereoselectivity was observed, and this represents the first example of a diastereoselective enolate hydrogen borrowing alkylation. By utilizing the Ph? group, the β-branched products could be straightforwardly cleaved to the corresponding esters or amides using a retro-Friedel-Crafts reaction. Finally, this protocol was applied to the synthesis of fragrance compound (±)-3-methyl-5-phenylpentanol.
Development of Phenyl Cyclohexylcarboxamides as a Novel Class of Hsp90 C-terminal Inhibitors
Garg, Gaurav,Forsberg, Leah K.,Zhao, Huiping,Blagg, Brian S. J.
, p. 16574 - 16585 (2017/11/13)
Inhibition of the heat shock protein 90 (Hsp90) C-terminus represents a promising therapeutic strategy for the treatment of cancer. Novobiocin, a coumarin antibiotic, was the first Hsp90 C-terminal inhibitor identified, however, it manifested poor anti-proliferative activity (SKBr3, IC50≈700 μm). Subsequent structure–activity relationship (SAR) studies on novobiocin led to development of several analogues that exhibited improved anti-proliferative activity against several cancer cell lines. Recent studies demonstrate that the biphenyl core could be used in lieu of the coumarin ring system, which resulted in more efficacious analogues. In continuation of previous efforts, the work described herein has identified the phenyl cyclohexyl core as a novel scaffold for Hsp90 C-terminal inhibition. Structure–activity relationship (SAR) studies on this scaffold led to the development of compounds that manifest mid-nanomolar activity against SKBr3 and MCF-7 breast cancer cell lines through Hsp90 inhibition.
AMINOACYLINDAZOLE IMMUNOMODULATORS FOR TREATMENT OF AUTOIMMUNE DISEASES
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, (2017/12/29)
2-Acylindazole compounds of formula I or formula II are disclosed. These compounds inhibit Coagulation Factor XIIa. They are useful to treat autoimmune diseases.
COMPOUNDS USEFUL AS KINASE INHIBITORS
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Paragraph 00226; 00287; 00288, (2017/07/14)
This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK).The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.
FeCl3·6H2O/acetaldehyde, a versatile system for the deprotection of ketals and acetals via a transacetalization process
Schiavo, Lucie,Jeanmart, Lo?c,Lanners, Steve,Choppin, Sabine,Hanquet, Gilles
, p. 1421 - 1424 (2017/02/23)
Mild and efficient catalytic deprotection of ketals/acetals mediated by FeCl3·6H2O/acetaldehyde has been described in this paper. The versatility and high chemoselectivity of the iron(iii)/aldehyde system are demonstrated by a large scope of examples. Deprotected ketones/aldehydes are nearly quantitatively isolated after filtration over a pad of silica gel followed by evaporation of volatile by-products.
Stereoelectronic Model to Explain Highly Stereoselective Reactions of Seven-Membered-Ring Oxocarbenium-Ion Intermediates
Beaver, Matthew G.,Buscagan, Trixia M.,Lavinda, Olga,Woerpel
, p. 1816 - 1819 (2016/02/03)
Nucleophilic attack on seven-membered-ring oxocarbenium ions is generally highly stereoselective. The preferred mode of nucleophilic attack forms the product in a conformation that minimizes transannular interactions, thus leading to different stereoselectivity as compared to that of reactions involving six-membered-ring oxocarbenium ions.
A 5-hydrocarbyloxy-2-oxo-cyclohexyl amide compound and its preparation method and application
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Paragraph 0026; 0029; 0030; 0032, (2016/10/31)
The invention belongs to the technical field of agricultural chemistry, and particularly relates to a 5-oxyl-2-oxocyclohexylsulfonamide compound as well as a preparation method and application thereof. The preparation method comprises the following steps:
PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS
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, (2015/10/05)
The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
