Author
Abraham Thomas
Bio: Abraham Thomas is an academic researcher from North Eastern Hill University. The author has contributed to research in topics: TRPA & RAR-related orphan receptor gamma. The author has an hindex of 18, co-authored 94 publications receiving 920 citations.
Topics: TRPA, RAR-related orphan receptor gamma, Ketene, Aryl, TRPV
Papers published on a yearly basis
Papers
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Patent•
26 Jul 2005
TL;DR: In this paper, the present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: (I) wherein Y is -S(O)m, -CH2-, CHF, or -CF2; m is 0, 1, or 2; X is a bond, C1-C5 alkyl (eg, -Ch2-), or -C(C(=0)-; the dotted line [----] in the carbocyclic ring represents an optional double bond
Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: (I) wherein Y is -S(O)m, -CH2-, CHF, or -CF2; m is 0, 1, or 2; X is a bond, C1-C5 alkyl (eg, -CH2-), or -C(=0)-; the dotted line [----] in the carbocyclic ring represents an optional double bond; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted heterocyclylalkyl, substituted or unsubstituted heteroarylalkyl, CN, -COOR3, CONR3R4, -OR3, -NR3R4, or NR3COR3; R2 is hydrogen, cyano, COOH, or an isostere of a carboxylic acid (such as SO3H, CONOH, B(OH)2, PO3R3R4, SO2NR3R4, tetrazole, -COOR3, -CONR3R4, NR3COR4, or -COOCOR3)
63 citations
Patent•
03 Sep 2003
TL;DR: In this article, the present invention relates to novel heterocyclic compounds that inhibit phosphodiesterase type 4 (PDE 4), which are useful for treating inflammatory conditions, diseases of the central nervous systems and insulin resistant diabetes.
Abstract: The present invention relates to novel heterocyclic compounds that inhibit phosphodiesterase type 4 (PDE 4). The compounds are useful for treating inflammatory conditions, diseases of the central nervous systems and insulin resistant diabetes.
53 citations
Patent•
29 Aug 2013
TL;DR: The present disclosure is directed to compounds of Formula (I), and pharmaceutically acceptable salts thereof, as modulator of retinoid-related orphan receptor gamma t (ROR ϒ t) as discussed by the authors.
Abstract: The present disclosure is directed to compounds of Formula (I), and pharmaceutically acceptable salts thereof, as modulator of retinoid-related orphan receptor gamma t (ROR ϒ t) These compounds prevent, inhibit, or suppress the action of ROR ϒ t and are therefore useful in the treatment of ROR ϒ t mediated disease, disorder, syndrome or condition such as pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, neurodegenerative diseases or cancer
46 citations
TL;DR: In this paper, cyclocondensation of 3-aminopyrazole and 3-amino-5-methylthio-4-phenylpyrazole with α-oxoketene dithioacetals derived from acyclic active methylene ketones was found to be equally successful for the synthesis of 7-styryl, 7-(4-aryl-1,3-butadienyl) and 7-(6-aryl)-1, 3,5-hexatrienyl) pyrazolopyrimidines.
40 citations
TL;DR: In this paper, a variety of mono-and disubstituted phenols are alkylated with propargyl bromide to give phenyl 2-propynyl ethers, which were further coupled with aryl iodides under Sonogashira reaction conditions to give 3-phenoxy-1-aryl-1propyne derivatives.
37 citations
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TL;DR: This review is focused on the analysis of current data on new methods of alkenylation of arenes and heteroarenes with alkynes by transition metal catalyzed reactions, Bronsted/Lewis acid promoted transformations, and others.
Abstract: This review is focused on the analysis of current data on new methods of alkenylation of arenes and heteroarenes with alkynes by transition metal catalyzed reactions, Bronsted/Lewis acid promoted transformations, and others. The synthetic potential, scope, limitations, and mechanistic problems of the alkenylation reactions are discussed. The insertion of an alkenyl group into aromatic and heteroaromatic rings by inter- or intramolecular ways provides a synthetic route to derivatives of styrene, stilbene, chalcone, cinnamic acid, various fused carbo- and heterocycles, etc.
322 citations
317 citations
TL;DR: The promise and challenges of developing TRP channel antagonists as a new generation of pain therapeutics are discussed.
265 citations
TL;DR: The "necessary nitrogen atom" is shown to be a versatile high-impact design element for multiparameter optimization, wherein ≥10, 100, or 1000-fold improvement in a variety of key pharmacological parameters can be realized.
Abstract: There is a continued desire in biomedical research to reduce the number and duration of design cycles required to optimize lead compounds into high-quality chemical probes or safe and efficacious drug candidates. The insightful application of impactful molecular design elements is one approach toward achieving this goal. The replacement of a CH group with a N atom in aromatic and heteroaromatic ring systems can have many important effects on molecular and physicochemical properties and intra- and intermolecular interactions that can translate to improved pharmacological profiles. In this Perspective, the “necessary nitrogen atom” is shown to be a versatile high-impact design element for multiparameter optimization, wherein ≥10-, 100-, or 1000-fold improvement in a variety of key pharmacological parameters can be realized.
171 citations