- Synthesis, structure–activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators
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The design, synthesis and SAR studies of novel 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators (NAMs) are presented in this letter. Starting from a HTS hit compound (1, IC50?=?477
- Hirose, Wataru,Kato, Yoshihiro,Yamamoto, Takayoshi,Kassai, Momoe,Takata, Makoto,Hayashi, Shun,Arai, Yukiyo,Imai, Satoki,Yoshida, Kohzo
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p. 3866 - 3869
(2016/08/01)
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- Three coordination polymers of transition metals built using HPPC ligand: Crystal structures and novel topology
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A new pyrazole-carboxylate type ligand, 3-(pyridin-3-yl)-1H-pyrazole-5-carboxylic acid (HPPC) was prepared from 3-acetylpyridine, diethyl oxalate and hydrazine hydrate. By employing this ligand, three new coordination complexes were prepared under solvothermal conditions: {[Ni(PPC)2]·3H2O}n (1), [Ag(PPC)]n (2) and [Cd(PPC)Cl]n (3). Single-crystal X-ray diffraction analyses reveal that 1-3 exhibit three different structural types. Complex 1 displays a 4-connected net with the Schl?fli symbol (44·62) topology, several types of hydrogen bonds connect the 2-D layer to a 3-D structure. Complex 2 is built from [Ag(N2O)] clusters and PPC ligand as 3-connected linker with Schl?fli symbol {36·46·53} without consideration of Ag?Ag interaction. The 2-D networks are also linked to form 3 D framework via Ag?Ag interaction. Complex 3 can be regarded as a (3, 3)-connected net with the Schl?fli symbol {333·433}, which consists of [Cd(N2O2)] clusters and PPC ligand as 3-connected bridge. The layers are further linked by the cholride atoms to generate a 3-D network.
- Zhao, Hong,Chu, Zhao-Jing,Gao, Gui-Yuan,Huang, Huan-Huan,Qu, Zhi-Rong
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p. 143 - 149
(2015/01/09)
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- PYRAZOLE COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF DEGENERATIVE DISEASES AND DISORDERS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful
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Paragraph 0076; 0077; 0080; 0081
(2014/09/29)
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- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-COA DESATURASE
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The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
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Page/Page column 36
(2010/07/04)
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- A facile synthesis of pyrazoles with multi-point structural diversity by 1,3-dipolar cycloaddition
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We describe the synthesis of diverse pyrazoles by 1,3-dipolar cycloaddition of ethyl diazoacetate with various acetylenes in refluxing toluene. The product pyrazoles are useful starting points for preparing a diverse collection of trisubstituted pyrazole
- Cheung, Kwai Ming J.,Reynisson, Jóhannes,McDonald, Edward
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supporting information; experimental part
p. 5915 - 5918
(2010/11/18)
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- Substituted 1-(4-aminophenyl)pyrazoles and their use as anti-inflammatory agents
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1-(4-aminophenyl)pyrazoles optionally substituted on the 3- and 5-positions of the pyrazole ring and on the amino group at the 4-position of the phenyl ring are disclosed and described, which pyrazoles inhibit IL-2 production in T-lymphocytes.
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- Synthesis and structure - Activity relationships of quarternary ammonium cephalosporins with 3-pyrazolylpyridium derivatives
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Cephalosporins with 3-pyazolylpyridinium at C-3 position, which is supposed to exhibit synergic activity of ceftazidime and cefoselis, were synthesized and their antibacterial activity against Gram-positive and Gram-negative was inspected. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Chang, Kwan Young,Kim, Sung Hoon,Nam, Ghilsoo,Seo, Jae Hong,Kim, Joong Hyup,Ha, Deok-Chan
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p. 1211 - 1214
(2007/10/03)
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