6309-59-7Relevant academic research and scientific papers
Evaluating the Viability of Successive Ring-Expansions Based on Amino Acid and Hydroxyacid Side-Chain Insertion
Lawer, Aggie,Epton, Ryan G.,Stephens, Thomas C.,Palate, Kleopas Y.,Lodi, Mahendar,Marotte, Emilie,Lamb, Katie J.,Sangha, Jade K.,Lynam, Jason M.,Unsworth, William P.
supporting information, p. 12674 - 12683 (2020/09/17)
The outcome of ring-expansion reactions based on amino/hydroxyacid side-chain insertion is strongly dependent on ring size. This manuscript, which builds upon our previous work on Successive Ring Expansion (SuRE) methods, details efforts to better define the scope and limitations of these reactions on lactam and β-ketoester ring systems with respect to ring size and additional functionality. The synthetic results provide clear guidelines as to which substrate classes are more likely to be successful and are supported by computational results, using a density functional theory (DFT) approach. Calculating the relative Gibbs free energies of the three isomeric species that are formed reversibly during ring expansion enables the viability of new synthetic reactions to be correctly predicted in most cases. The new synthetic and computational results are expected to support the design of new lactam- and β-ketoester-based ring-expansion reactions.
SUBSTITUTED PHENYLOXAZOLIDINONES FOR ANTIMICROBIAL THERAPY
-
Page/Page column 28; 29, (2017/02/09)
The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
-
Paragraph 0777; 0778; 0779, (2015/07/22)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
-
Paragraph 0774, (2015/09/22)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
FUSED TRICYCLIC COMPOUNDS FOR USE AS INHIBITORS OF JANUS KINASES
-
Page/Page column 110, (2013/03/26)
The invention provides novel compounds of formula (I) having the general formula (I) wherein R1, V, W, X, Y and Z are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
1-(DIHYDRONAPHTHALENYL)PYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
-
Page/Page column 59, (2013/10/22)
Provided are 1-(dihydronaphthalenyl)pyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy for the treatment of obesity and diabetes.
HETEROCYCLIC COMPOUND
-
Page/Page column 51-52, (2010/12/30)
The present invention provides to a compound having melanin-concentrating hormone receptor antagonistic action and low toxicity, and useful as a agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound re
Kinase inhibitor compounds
-
Page/Page column 20; 21, (2009/04/24)
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.
NOVEL COMPOUNDS
-
Page/Page column 62, (2009/10/22)
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.
PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
-
Page/Page column 52, (2008/12/07)
The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 /PDE type 7 inhibitors. Compounds disclosed hereinf having the structure of Formula 1: can be useful in the treatment, prevention, inhibiti
