- CASPASE INHIBITOR AND PHARMACEUTICAL COMPOSITION, USE AND THERAPEUTIC METHOD THEREOF
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Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.
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Paragraph 0365; 0366
(2019/04/05)
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- Synthesis of 3-hydroxyindanones via potassium salt of amino acid catalyzed regioselective intramolecular aldolization of ortho-diacylbenzenes
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First organocatalytic intramolecular aldolization of ortho-diacylbenzenes to construct highly functionalized 3-hydroxyindanones is described. In this transformation a high trans-selectivity is achieved by the use of metal salt of amino acid. This method allows an easy access to the strained spirocyclic 3-hydroxyindanones related to a number of natural product frameworks. Synthesis of a new class of indole skeleton substituted by 3-hydroxyindanones added an extra essence to this new protocol.
- Chanda, Tanmoy,Chowdhury, Sushobhan,Anand, Namrata,Koley, Suvajit,Gupta, Ashutosh,Singh, Maya Shankar
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supporting information
p. 981 - 985
(2015/03/04)
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- PYRAZOLE AMIDE DERIVATIVE
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The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.
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Page/Page column 105; 106
(2015/09/28)
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- Enantioselective copper-catalyzed carboetherification of unactivated alkenes
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Chiral saturated oxygen heterocycles are important components of bioactive compounds. Cyclization of alcohols onto pendant alkenes is a direct route to their synthesis, but few catalytic enantioselective methods enabling cyclization onto unactivated alkenes exist. Herein reported is a highly efficient copper-catalyzed cyclization of γ-unsaturated pentenols which terminates in C-C bond formation, a net alkene carboetherification. Both intra- and intermolecular C-C bond formations are demonstrated, thus yielding functionalized chiral tetrahydrofurans as well as fused-ring and bridged-ring oxabicyclic products. Transition-state calculations support a cis-oxycupration stereochemistry-determining step.
- Bovino, Michael T.,Liwosz, Timothy W.,Kendel, Nicole E.,Miller, Yan,Tyminska, Nina,Zurek, Eva,Chemler, Sherry R.
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supporting information
p. 6383 - 6387
(2014/06/24)
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- CYCLOALKYL METHOXYBENZYL PHENYL PYRAN DERIVATIVES AS SODIUM DEPENDENT GLUCOSE CO TRANSPORTER (SGLT2) INHIBITORS
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The invention relates to the cycloalkyl methoxybenzyl phenyl pyran derivatives as Sodium dependent glucose co transporter (SGLT) inhibitors, particularly SGLT2 and method of treating diseases, conditions and/or disorders inhibited by SGLT2 with them, and processes for preparing them.
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Page/Page column 22
(2012/03/26)
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- NOVEL CARBOXAMIDE DERIVATIVES AS HIV INHIBITORS
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The present invention relates to carboxamide derivatives of Formula (I), where B1, B2, X, L, n, R, R1, R2, Z1, Z2, Rx and Ry are as defined in the claims, as compounds and compositions for inhibiting Human Immunodeficiency Virus (HIV) and process for making the compounds.
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Page/Page column 29
(2011/06/19)
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- ABCA-1 ELEVATING COMPOUNDS AND METHODS
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Disclosed are novel compounds of Formula I useful for treating various disease states, in particular, insulin resistance, diabetes, dyslipidemia, coronary artery disease, and inflammation. The compounds of the present invention elevate cellular expression of the ABCA-1 gene as well as increasing the level of ABCA-1 protein, which may result in an increase in HDL levels in the plasma of a mammal, in particular humans.
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- Partial and full agonists of A1 adenosine receptors
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Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.
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- CYCLIC AMIDES AND IMIDES HAVING SELECTIVE ANTAGONIST ACTIVITY AT ALPHA-1D ADRENERGIC RECEPTOR
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Compounds (I) R and R1 independently = H or C1-C4 alkyl or together = (CH2)2-6, n=0 or 1, ...... is a single or a double bond, A=CO or CH2, A1 represents a CO or CH2 or CH, each R3 independently = H or C1-C4 alkyl, B is B1 or B2 (B2); Y=N or CH, R2 = halogen, C1-C4 alkyl or CN, R5 = halogen, C1-C4 alkyl, polyfluoroalkyl or NO2, R6 = H or halogen, m is 1 to 3, Z = O, S, NH or NMe) interact selectively with the alpha 1D subtype of the alpha 1 adrenergic receptor. This selectively makes these compounds useful agents in tissues particularly rich in alpha 1D adrenergic receptors, thus useful in reducing contractility of an unstable urinary bladder, in the treatment and prevention of atherosclerosis as they are inhibitors of noradrenaline-mediated cell proliferation in smooth muscles, and in reducing vascular adrenergic tone. The preparation of these compounds, their enantiomers, diastereoisomers, N-oxides and pharmaceutically acceptable salts, and pharmaceutical compositions containing them are also claimed.
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- Synthesis and X-ray studies of chiral allosteric modifiers of hemoglobin
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This study was designed to investigate the effect of chirality on the allosteric activity of a series of Hb allosteric modifiers. The chiral analogues were based on the lead compound (4), JP7, {1-[4-(((3,5-dimethylanilino)carbonyl)methyl)phenoxy]cyclopentanecarboxylic acid} with different D- and L-amino acids conjugated to the JP7 acid moiety. The D-isomers were the most potent in vitro effectors in Hb solutions as well as with whole blood. In general, this study demonstrated that the chirality of extended amino acid side chains in JP7 conjugates plays an important role in observed degree of allosteric activity. The binding site interactions for four analogues were determined by single crystallographic diffraction studies. Conclusions show that the chiral configuration of some of the D-isomers enable the effectors to bind with a greater number of interactions with the protein residues, D- and L-isomers with equivalent or near equivalent allosteric activity did not show any significant differences or interactions between their amino acid side chains and the protein. The most potent effectors, in vitro, were compounds 15 and 19, D-isomers of leucine and phenylalanine, respectively. Compounds 21, 22, 30, and 32 were more potent in vitro in Hb solutions than JP7.
- Youssef, Amal Mamdouh,Safo, Martin K.,Danso-Danquah, Richmond,Joshi, Gajanan S.,Kister, Jean,Marden, Michael C.,Abraham, Donald J.
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p. 1184 - 1195
(2007/10/03)
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- Steric and electronic effects on the Weiss reaction. Isolation of 1:1 adducts
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The mechanism of the Weiss reaction has been studied with respect to the intermediacy of 4-hydroxycyclopent-2-en-1-ones (1:1 adducts) in this process. Analysis of these experiments provides additional evidence that 4-hydroxycyclopentenones are indeed key intermediates in the Weiss reaction. Based on the reaction of dimethyl 3-oxoglutarate with benzil, pyridil, thenil, furil and phenanthrenequinone, steric effects play the major role in the overall success of this condensation to provide substituted cis-bicyclo[3.3.0]octane-3,7-diones. Moreover a trihydroxyindene [5.6] system (see 26) has been isolated for the first time under the Weiss conditions which provides additional support for the existence of cyclopentenone intermediates in this process.
- Van Ornum, Scott G.,Li, Jin,Kubiak, Greg G.,Cook, James M.
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p. 3471 - 3478
(2007/10/03)
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- Favorski type rearrangement in the lead tetraacetate oxidation of cycloalkanones
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The cycloalkanones (1a-1f) have been converted into their corresponding cycloalkane carboxylates (2a-2f) by a lead(IV) acetate promoted rearrangement in presence of perchloric acid in triethyl orthoformate.
- Mathew, Felix,Myrboh, Bekington
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p. 1097 - 1101
(2007/10/03)
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- Synthesios of Cyclopentane Derivatives by Electrochemical Reduction of 1,5-Dibromopentane Derivatives
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When 1,5-dibromopentane derivatives, which were prepared by CuBr-catalyzed photochemical reaction of 1,3-dibromopropane or its derivatives with electron-deficient olefins, were subjected to electrochemical reduction in THF or DMSO solution, cyclopentane derivatives were obtained.
- Mitani, Michiharu,Takeuchi, Hiroshi,Koyama, Kikuhiko
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p. 2125 - 2126
(2007/10/02)
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- FAVORSKI TYPE REARRANGEMENT IN THE LEAD TETRAACETATE OXIDATION OF ENAMINES PROMOTED BY BORON TRIFLUORIDE
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Favorski type rearrangement has been achieved in the lead tetraacetate oxidation of enamines in the presence of boron trifluoride etherate and alcohol.
- Cekovic, Z.,Bosnjak, J.,Cvetkovic, M
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p. 2675 - 2678
(2007/10/02)
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