- Synthesis, molecular docking, dynamic simulation and pharmacological characterization of potent multifunctional agent (dual GPR40-PPARγ agonist) for the treatment of experimental type 2 diabetes
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The current manuscript describes two molecules that were designed against PPARγ and GPR40 receptors. The preparation of the compounds was carried out following a synthetic route of multiple steps. Then, the mRNA expression levels of PPARγ, GLUT4, and GPR4
- Hidalgo-Figueroa, Sergio,Rodríguez-Luévano, Ana,Almanza-Pérez, Julio C.,Giacoman-Martínez, Abraham,Ortiz-Andrade, Rolffy,León-Rivera, Ismael,Navarrete-Vázquez, Gabriel
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- GK and PPAR dual agonist activity aryl urea derivatives
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The invention discloses a novel arylurea derivative, its preparation method, pharmaceutical composition and application. Specifically, the invention relates to an arylurea derivative as shown in the general formula I, its medicinal salt, a preparation met
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Paragraph 0090; 0091
(2016/12/01)
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- Pyrazolo[3,4-c]pyridine derivative
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The invention relates to a pyrazolo[3,4-c]pyridine derivative. The invention relates to a compound represented by a formula (I), a tautomer thereof, an optical isomer thereof or a pharmaceutically acceptable salt thereof, wherein the formula (I) is shown in the description, and Z, X, RNc, RNd, RNe and RNf are defined according to the claim 1. The invention further relates to the pharmaceutical composition contain the compound. The invention further relates to use of the compound or the pharmaceutical composition in preparing a drug for preventing and/or treating a disease which inhibits positive influence of an Xa factor, particularly use in preparing the drug for preventing and/or treating the disease which inhibits positive influence of the Xa factor under the condition of low hemorrhage risk.
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Paragraph 0367; 0368; 0369
(2016/10/08)
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- CONJUGATES AND SMALL MOLECULES WHICH INTERACT WITH THE CD16A RECEPTOR
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The invention is related to medicine, in particular, to oncology and immunology. The novel compounds of the general formula 1 or 2, exhibiting affinity for CD16a receptor have been proposed. There were also proposed novel modified proteins active towards
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Paragraph 0040; 0041
(2015/12/08)
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- HETEROARYL COMPOUNDS AND USES THEREOF
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The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
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Paragraph 0674
(2015/07/02)
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- 2,4-Pyrimidinediamine Compounds and Their Uses
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The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
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Paragraph 0485
(2015/11/10)
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- AZAQUINAZOLINE INHIBITORS OF ATYPICAL PROTEIN KINASE C
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The present invention provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. A compound of formula (I) and its salts have a PKC inhibitory activity, and may be used to treat proliferative disorders.
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Page/Page column 347-348
(2014/04/17)
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- HETEROARYL COMPOUNDS AND USES THEREOF
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The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
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Paragraph 0427; 0429
(2014/07/08)
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- Synthesis, in vitro and in silico studies of a PPARγ and GLUT-4 modulator with hypoglycemic effect
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Compound {4-[({4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy}acetyl)amino]phenoxy}acetic acid (1) was prepared and the in vitro relative expression of PPARγ, GLUT-4 and PPARα, was estimated. Compound 1 showed an increase of 2-fold in the mRNA
- Navarrete-Vzquez, Gabriel,Torres-Gmez, Hctor,Hidalgo-Figueroa, Sergio,Ramrez-Espinosa, Juan Jos,Estrada-Soto, Samuel,Medina-Franco, Jos L.,Len-Rivera, Ismael,Alarcn-Aguilar, Francisco Javier,Almanza-Prez, Julio Csar
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supporting information
p. 4575 - 4579
(2015/02/19)
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- HETEROCYCLIC UREA COMPOUNDS
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The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture
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Page/Page column 62
(2013/07/05)
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- Synthesis and structure of supramolecular compound with ethyl 2-(4-aminophenoxy)acetate based on 18-crown-6
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The title ammonium compound ethyl 2-(4-aminophenoxy)acetate (C 10H13NO3, I) and its crown ether inclusion complex {[(C10H14NO3)·(18-crown-6)] +[PF6]-, II} (
- Wang, Wenxiang,Sun, Suwen,Xiong, Rengen
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p. 1957 - 1961,5
(2020/09/09)
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- Structure-based design of a new series of d-glutamic acid based inhibitors of bacterial UDP-N-acetylmuramoyl-l-alanine: D-glutamate ligase (MurD)
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MurD ligase is one of the key enzymes participating in the intracellular steps of peptidoglycan biosynthesis and constitutes a viable target in the search for novel antibacterial drugs to combat bacterial drug-resistance. We have designed, synthesized, and evaluated a new series of d-glutamic acid-based Escherichia coli MurD inhibitors incorporating the 5-benzylidenethiazolidin-4- one scaffold. The crystal structure of 16 in the MurD active site has provided a good starting point for the design of structurally optimized inhibitors 73-75 endowed with improved MurD inhibitory potency (IC50 between 3 and 7 μM). Inhibitors 74 and 75 showed weak activity against Gram-positive Staphylococcus aureus and Enterococcus faecalis. Compounds 73-75, with IC 50 values in the low micromolar range, represent the most potent d-Glu-based MurD inhibitors reported to date.
- Toma?i?, Tihomir,Zidar, Nace,?ink, Roman,Kova?, Andreja,Blanot, Didier,Contreras-Martel, Carlos,Dessen, Andréa,Müller-Premru, Manica,Zega, Anamarija,Gobec, Stanislav,Kikelj, Danijel,Peterlin Ma?i?, Lucija
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supporting information; experimental part
p. 4600 - 4610
(2011/09/14)
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- Cosmetic and pharmaceutical compositions
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This invention relates to novel compounds that display retinoid like activities, including HB-EGP (Heparin. Binding Epidermal Growth Factor) release from keratinocytes, cell proliferation, and epidermal thickening without the irritation potentials, such as release of interleukin 8 and inhibition of terminal differentiation of keratinocytes. This invention also relates to the use of such a compound for both external and non-external applications.
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Page/Page column 12; 23
(2009/07/17)
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- AMINOPHENYLPROPANOIC ACID DERIVATIVE
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A compound represented by the formula (1): wherein each symbol is as defined in the specification, and a salt thereof and a prodrug thereof unexpectedly have superior GPR40 receptor agonist activity, superior in the properties as a pharmaceutical product such as stability and the like, and can be a safe and useful pharmaceutical agent as a drug for the prophylaxis or treatment of GPR40 receptor related pathology or diseases such as diabetes and the like.
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Page/Page column 52
(2010/11/24)
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- Novel sulfonamide derivatives as inhibitors of histone deacetylase
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Inhibition of the enzyme histone deacetylase (HDAC) is emerging as a novel approach to the treatment of cancer. A series of novel sulfonamide derivatives were synthesized and evaluated for their ability to inhibit human HDAC. Compounds were identified which are potent enzyme inhibitors, with IC 50 values in the low nanomolar range against enzyme obtained from HeLa cell extracts, and with antiproliferative effects in cell culture. Extensive characterization of the structure - activity relationships of this series identified key requirements for activity. These include the direction of the sulfonamide bond and substitution patterns on the central phenyl ring. The alkyl spacer between the aromatic head group and the sulfonamide functionality also influenced the HDAC inhibitory activity. One of these compounds, m11.1, also designated PXD101, has entered clinical trials for solid tumors and haematological malignancies.
- Finn, Paul W.,Bandara, Morwena,Butcher, Chris,Finn, Angela,Hollinshead, Ruth,Khan, Nagma,Law, Norman,Murthy, Sreenivasa,Romero, Rosario,Watkins, Clare,Andrianov, Victor,Bokaldere, Rasma M.,Dikovska, Klara,Gailite, Vija,Loza, Einars,Piskunova, Irina,Starchenkov, Igor,Vorona, Maxim,Kalvinsh, Ivars
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p. 1630 - 1657
(2007/10/03)
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- Bifunctional rhodium intercalator conjugates as mismatch-directing DNA alkylating agents
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A conjugate of a DNA mismatch-specific rhodium intercalator, containing the bulky chrysenediimine ligand, and an aniline mustard has been prepared, and targeting of mismatches in DNA by this conjugate has been examined. The preferential alkylation of mism
- Schatzschneider, Ulrich,Barton, Jacqueline K.
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p. 8630 - 8631
(2007/10/03)
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- Carboxylic acid derivatives, medicaments comprising these compounds, their use and processes for their production
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The present invention relates to carboxylic acid derivatives of the general formula STR1 in which Ra to Rc, A, B, D, E and X1 to X3 are as defined in claim 1, their tautomers, their stereoisomers including their mixtures, and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases, which have useful pharmacological properties, preferably aggregation-inhibiting inhibiting actions, medicaments containing these compounds, their use and processes for their preparation.
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- Quantitative structure-activity analyses of novel hydroxyphenylurea derivatives as antioxidants
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A series of substituted hydroxyphenylureas was synthesized, the chemical structure of which was designed based on structures of natural antioxidants, vitamin E (α-tocopherol) and uric acid. They exhibited high inhibitory activity against lipid peroxidation. In order to gain an insight into the mechanism of the inhibition reaction, we analyzed their structure-activity relationships quantitatively. Electronic and steric effects of substituents on the phenolic hydroxyl group were shown to be of importance in governing the inhibitory potency. An increase in the electron donating property of substituents toward the phenolic hydroxyl group enhanced the antioxidative activity by the stabilization of an electron-deficient radical-type transition state. The steric shielding by ortho-substituents stabilized the phenoxy radicals formed following the transition state. Derivatives having the carboxyl group were only weakly active presumably because of an intermolecular ion-dipole interaction of the phenolic hydroxyl group with the carboxylate anion which could retard the formation of the transition state. Copyright (C) 1998 Elsevier Science Ltd.
- Nakao, Kazuya,Shimizu, Ryo,Kubota, Hitoshi,Yasuhara, Mikiko,Hashimura, Yoshimasa,Suzuki, Toshikazu,Fujita, Toshio,Ohmizu, Hiroshi
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p. 849 - 868
(2007/10/03)
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- CARBOXYLIC ACID COMPOUND HAVING CONDENSED RING, SALT THEREOF AND PHARMACEUTICAL USE THEREOF
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A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases
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