257876-04-3Relevant academic research and scientific papers
NOVEL COMPOUNDS, SYNTHESIS METHOD THEREOF AND USE OF SAME IN MEDICINE AND IN COSMETICS
-
Paragraph 0275, (2018/01/04)
Novel compounds, synthesis methods and use of the same in medicine and in cosmetics are disclosed. Also disclosed, are novel compounds and ligands that modulate RARs.
Zinc Coordination Polymers Containing Isomeric Forms of p-(Thiazolyl)benzoic Acid: Blue-Emitting Materials with a Solvatochromic Response to Water
Staderini, Samuele,Tuci, Giulia,Luconi, Lapo,Müller, Philipp,Kaskel, Stefan,Eychmüller, Alexander,Eichler, Franziska,Giambastiani, Giuliano,Rossin, Andrea
, p. 4909 - 4918 (2017/11/21)
Two coordination polymers of assorted dimensionality (1D, 2D) have been prepared, namely [Zn3(L2Th)4(OH)2·2(HL2Th)]∞ (1) and [Zn(L5Th)(OAc)]∞ (2), starting from ZnII salts and the isomeric forms of the organic linker p-(thiazolyl)benzoic acid: p-(2-thiazolyl)benzoic acid (HL2Th) and p-(5-thiazolyl)benzoic acid (HL5Th). The isomers have been prepared ad hoc, following straightforward Pd-catalyzed C–C coupling reaction protocols. In 1, the deprotonated ligand is coordinated through its carboxylate group only, with dangling thiazole groups. The –COO– units are bridging adjacent metal centers, thus creating a 1D chain. The Zn3 cluster is made of one six-coordinate (Oh) and two four-coordinate (Td) ZnII ions; triple-bridging μ3-OH groups are balancing the overall positive charge. The structure of 2 is instead made of Zn2(carboxylate)4 “paddle-wheel” dimers as the constituting inorganic node. The octahedral metal coordination sphere includes two μ-(κ-COO) benzoate spacers, two μ-(κ-COO) acetate ions, the thiazole N atoms coming from adjacent building blocks, and a weak Zn···Zn axial interaction. The resulting final assembly is two-dimensional (2D), where p-(5-thiazolyl)benzoate adopts a genuine μ-[κ(COO):κ(N)] bridging coordination mode. The luminescent properties of both polymers have been analyzed in the solid state; they feature ligand-centered emissions at λ = 434 nm (1) and λ = 427 nm (2). These electronic transitions fall in the visible region, giving the samples a characteristic blue color under an ordinary UV lamp (excitation at λ = 254 nm). The theoretical analysis of the electronic features of the ligands and related molecular orbitals reveals that the observed transitions are mainly of π→π* nature, involving π orbitals delocalized on both aromatic cycles. A significant (reversible) blueshift of the emission maximum of ca. 60 nm, from the visible to the UV region, has been observed for 1 when suspended in water.
Preparation method of (5-halogenothiazole-2-yl) benzoic acid compounds
-
Paragraph 0024; 0025, (2017/07/12)
The invention discloses a preparation method of (5-halogenothiazole-2-yl) benzoic acid compounds. The method comprises the steps of firstly synthesizing thiazole benzoate compounds by taking 2-bromine thiazole as a raw material, then halogenating and hydr
A trifluorinated thiazoline scaffold leading to pro-apoptotic agents targeting prohibitins
Pérez-Perarnau, Alba,Preciado, Sara,Palmeri, Claudia Mariela,Moncunill-Massaguer, Cristina,Iglesias-Serret, Daniel,González-Gironès, Diana M.,Miguel, Miriam,Karasawa, Satoki,Sakamoto, Satoshi,Cosialls, Ana M.,Rubio-Pati?o, Camila,Saura-Esteller, José,Ram?n, Rosario,Caja, Laia,Fabregat, Isabel,Pons, Gabriel,Handa, Hiroshi,Albericio, Fernando,Gil, Joan,Lavilla, Rodolfo
supporting information, p. 10150 - 10154 (2015/03/31)
A new class of small molecules, with an unprecedented trifluorothiazoline scaffold, were synthesized and their pro-apoptotic activity was evaluated. With an EC50 in the low micromolar range, these compounds proved to be potent inducers of apopt
Cobalt-catalyzed C-SMe bond activation of heteroaromatic thioethers
Begouin, Jeanne-Marie,Rivard, Michael,Gosmini, Corinne
supporting information; experimental part, p. 5972 - 5974 (2010/11/02)
Cobalt-catalyzed activation of methylthio-substituted N-heterocycles facilitates either cross-coupling reactions with aryl- or benzylzinc compounds or synthesis of the corresponding zinc compounds.
Imidazolylsulfonates: Electrophilic partners in cross-coupling reactions
Albaneze-Walker, Jennifer,Raju, Ravinder,Vance, Jennifer A.,Goodman, Andrew J.,Reeder, Michael R.,Liao, Jing,Maust, Mathew T.,Irish, Patrick A.,Espino, Peter,Andrews, David R.
supporting information; experimental part, p. 1463 - 1466 (2009/08/07)
Aryl imidazolylsulfonates participate as electrophilic coupling partners in palladium-mediated cross-coupling reactions. The aryl imidazolylsulfonates display good stability while maintaining good reactivity in a variety of palladium-catalyzed coupling reactions. Imidazolylsulfonates are a practical and economic alternative to triflates.
PIPERAZINE AND PIPERIDINE BIARYL DERIVATIVES
-
Page/Page column 74-75, (2010/11/28)
This invention relates to piperazine and piperidine biaryl compounds of Formula (I) or a pharmaceutically acceptable prodrug, salt, polymorph, solvate, enantiomer, diastereomer, racemate, mixture of stereoisomers thereof, or derivative thereof; and to processes for preparing the compounds or pharmaceutical compositions containing the same. The compounds and pharmaceutical compositions of the present invention are provided for use in the treatment of HIV infection and/or AIDS.
FIBROSIS INHIBITOR
-
, (2008/06/13)
Medicament being useful as a fibrosis inhibitor for organs or tissues, which comprises a compound of the formula (I): wherein Ring Z is optionally substituted pyrrole ring, etc.; W2 is -CO-, -SO2-, optionally substituted C1-C4 alkylene, etc.; Ar2 is optionally substituted aryl, etc.; W1 and Ar1 mean the following (1) and (2):(1) W1 is optionally substituted C1-C4 alkylene, etc.; Ar1 is optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms:(2) W1 is optionally substituted C2-C5 alkylene, optionally substituted C2-C5 alkenylene, etc.; and Ar1 is aryl or monocyclic heteroaryl, which is substituted by carboxyl, alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof.
Pyrrole derivatives
-
, (2008/06/13)
Pyrrole derivatives represented by the following formula: wherein Ring Z is an optionally substituted pyrrole ring, etc.; W2 is —CO—, —SO2—, an optionally substituted C1-C4 alkylene, etc.; Ar2 is an optionally substituted aryl, etc.; W2 and Ar1 mean the following (1) and (2): (1) W1 is an optionally substituted C1-C4 alkylene, etc.; Ar1 is an optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is an optionally substituted C2-C5 alkylene, an optionally substituted C2-C5 alkenylene, etc.; and Ar1 is an aryl or monocyclic heteroaryl, which are substituted by carboxyl, an alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof These compounds are useful as medicaments such as a fibrosis inhibitor for organs or tissues.
COMPOUNDS AND METHODS
-
, (2008/06/13)
This invention relates to substituted heteroanilide compounds which are modulators, agonists or antagonists, of the CCR5 receptior. In addition, this invention relates to the treatment and prevention of disease states mediatd by CCR5.
