195503-40-3Relevant academic research and scientific papers
Expansion of substrate scope for nitroxyl radical/copper-catalyzed aerobic oxidation of primary alcohols: A guideline for catalyst selection
Iwabuchi, Yoshiharu,Nagasawa, Shota,Sasaki, Ryota,Sasano, Yusuke,Yamaichi, Aoto
, p. 488 - 497 (2021/05/27)
Four distinctive sets of optimum nitroxyl radical/copper salt/additive catalyst combinations have been identified for accommodating the aerobic oxidation of various types of primary alcohols to their corresponding aldehydes. Interestingly, less nucleophilic catalysts exhibited higher catalytic activities for the oxidation of particular primary allylic and propargylic alcohols to give α,β-unsaturated aldehydes that function as competent Michael acceptors. The optimum conditions identified herein were successful in the oxidation of various types of primary alcohols, including unprotected amino alcohols and divalent-sulfur-containing alcohols in good-to-high yields. Moreover, N-protected alaninol, an inefficient substrate in the nitroxyl radical/ copper-catalyzed aerobic oxidation, was oxidized in good yield. On the basis of the optimization results, a guideline for catalyst selection has been established.
SULFONYL-SUBSTITUTED BICYCLIC COMPOUND WHICH ACTS AS ROR INHIBITOR
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Paragraph 0595; 0596, (2020/08/16)
Provided is a sulfonyl-substituted bicyclic compound (A) which acts as a RORγ inhibitor, said compound has good RORγ inhibitory activity and is expected to be used for treating diseases mediated by a RORγ receptor in mammals.
IMIDAZOPIPERAZINONE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
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Paragraph 0751; 0752, (2019/10/20)
The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
COMPOUNDS AS BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS
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Paragraph 257; 258, (2018/07/31)
Provided are certain Bcl-2 inhibitors, pharmaceutical compositions thereof, and methods of use thereof.
Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors
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Page/Page column 131; 132, (2016/09/13)
The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
HETEROCYCLIC PROTEIN KINASE INHIBITORS
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Paragraph 00299; 00300, (2013/03/26)
The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists
Kiyoi, Takao,Adam, Julia M.,Clark, John K.,Davies, Keneth,Easson, Anna-Marie,Edwards, Darren,Feilden, Helen,Fields, Ruth,Francis, Stuart,Jeremiah, Fiona,McArthur, Duncan,Morrison, Angus J.,Prosser, Alan,Ratcliffe, Paul D.,Schulz, Jurgen,Wishart, Grant,Baker, James,Campbell, Robert,Cottney, Jean E.,Deehan, Maureen,Epemolu, Ola,Evans, Louise
scheme or table, p. 1748 - 1753 (2011/05/05)
Novel 3-(1H-indol-3-yl)-1,2,4-oxadiazoles and -thiadiazoles were synthesized and found to be potent CB1 cannabinoid receptor agonists. The oral bioavailability of these compounds could be dramatically improved by optimization studies of the side chains attached to the indole and oxadiazole cores, leading to identification of a CB1 receptor agonist with good oral activity in a range of preclinical models of antinociception and antihyperalgesia.
HETEROCYCLIC COMPOUND
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Page/Page column 49, (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
Propylphosphonic anhydride (T3P): A remarkably efficient reagent for the one-pot transformation of aromatic, heteroaromatic, and aliphatic aldehydes to nitriles
Augustine, John Kallikat,Atta, Rajendra Nath,Ramappa, Balakrishna Kolathur,Boodappa, Chandrakantha
experimental part, p. 3378 - 3382 (2010/03/03)
Propylphosphonic anhydride has been demonstrated to be an efficient reagent for the transformation of aromatic, heteroaromatic, and aliphatic aldehydes to respective nitriles in excellent yields. This procedure offers simple and one-pot access to nitriles and highlights the synthetic utility of T3P as a versatile reagent in organic chemistry. Georg Thieme Verlag Stuttgart - New York.
BENZIMIDAZOLE DERIVATIVES USEFUL IN TREATMENT OF VALLINOID RECE TOR TRPVL RELATED DISORDERS
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Page/Page column 55, (2008/06/13)
The claimed invention provides benzimidazole derivatives antagonists of VRl, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds of Formula I may be used in the treatment of osteoarthritis,
