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The present invention relates to the gamma-Polymorph of (R)-N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide, methods for its preparation, medicaments comprising this compound as well as their use for the preparation of a medicament for the treatment of humans and animals.

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Diarylimidazolecarboxamides and diaryltriazolecarboxamides related to SR141716 were synthesized and tested for binding to the human CB1 receptor. Suitably substituted imidazoles are comparably potent to the clinical candidate, whereas the analogous triazoles are less so due to the absence of an additional substituent on the azole ring.

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N,N’,N”-Trimethoxyborazines (-BX-NOMe-)3 (1: X = Cl, 2: X = OMe) are obtained from MeON(SiMe3)2 and Cl2BX.With NaOCMe3 or LiCMe3 1 gives the derivatives 3 (X = OCMe3) and 4 (X = CMe3), respectively.Reaction of PhBCl2 with MeON(SiMe3)2 leads to the 1,2,4,3,5-oxadiazadiborolane derivative 5.With 2 equivalents of Me2BBr Me2BON(SiMe3)BMe2 (6) is obtained.The N,N’,N”-tris(amino)borazine (-BOMe-NNMe2-)3 (13) is made from Me2NN(SnMe3)2 and Cl2BOMe. 2 and 13 readily give condensed products.

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Disclosed are a preparation method for a kinase inhibitor and a use thereof. The kinase inhibitor is a compound represented by formula (I) wherein the groups are defined as described in the description. The compound of formula (I) has a kinase inhibitory activity and therefore can be used for the preparation of medicines for treating kinase activity-related diseases.

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A new series of 3-allylthio-6-(mono or disubstituted) aminopyridazines was synthesized by reacting 3-allylthio-6-chloropyridazine with several amines to develop new anticancer agents. These new compounds showed antiproliferative activities against lung cancer (A549), hepatoblastoma (Hep3b), prostate cancer (PC3), colon cancer (SW480) and cervical cancer (HeLa) cells in MTT assays, and could be promising candidates for chemotherapy of carcinomas. Compound 5 (3-allylthio-6-homopiperidinylaminopyridazine) showed higher potencies than 5-FU for inhibiting the growth of these cell lines. This suggests the potential anticancer activity of compound 5.

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In our ongoing program aimed at deeply investigating the endocannabinoid system (ES), a set of new alkyl-resorcinol derivatives was prepared focusing on the nature and the importance of the carboxamide functionality. Binding studies on CB1 and CB2 receptors, monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) showed that some of the newly developed compounds behaved as very potent cannabinoid receptor ligands (Ki in the nanomolar range) while, however, none of them was able to inhibit MAGL and/or FAAH. Derivative 11 was a potent CB1 and CB2 ligand, with Ki values similar to WIN 55,212, exhibiting a CB 1 and CB2 agonist profile in vitro. In the formalin test of peripheral acute and inflammatory pain in mice, this compound showed a weak and delayed antinociceptive effect against the second phase of the nocifensive response, exhibiting, interestingly, a quite potent transient receptor potential ankyrin type-1 (TRPA1) channel agonist activity. Moreover, derivative 14, characterized by lower affinity but higher CB2 selectivity than 11, proved to behave as a weak CB2 competitive inverse agonist.

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The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them

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The remarkable cytostatic activity of 1-substituted indazolols 2a, b, condensed indazolinones 4a-c and indoxyl derivatives 5a, b against HeLa cells is reported.Three different approaches to the synthesis of indazolophthalazinone 4a, representing alternatives to those previously reported, were studied.Several compounds related to the mentioned indazolols and indazolinones were obtained and their cytostatic activity against HeLa cells was tested.Among them we can mention the tetracyclic SO2 analogue 14 and the condensed pyridine derivative 18, the tricyclic pyrazolophthalazinone 22 and the bicyclic pyrazolodiazepinone 25, which were prepared by taking advantage of the reactivity of heterocyclic spiro aminimides. – Key Words: Indazolols / Indazolinones / Indoxyls / Cytostatic agents / HeLa cells

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2213-43-6, molcular formula is C5H12N2, introducing its new discovery. COA of Formula: C5H12N2

Salts of 1,5-diarylpyrazole-3-carboxamides and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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Hydroalumination of 1-aza-but-1-en-ynes 1 provides facile access to propargylamines 4 by reduction of the C=N bonds or alternatively to 1-aza-buta-1,3-dienes 6 by reduction of the triple bond. The chemoselectivity depends not only on the steric properties of both the hydroalumination agent (di-iso-butylaluminum (DIBAL-H, iBu2AlH) versus di-tert-butylaluminum hydride (tBu2AlH)) and the substrates but also on the reaction temperatures. In several cases, initial aluminum species of 5-aluminazole type 5 could be isolated and characterized by X-ray diffraction, indicating an “anti-Michael” addition of the hydride to the triple bond. Aqueous workup of those species led to 1-azabutadiene derivatives 6. High-level DFT calculations indicate that the observed chemoselectivity is only compatible with a dimeric nature of the hydroaluminating agent. Using such a dimer, the imine reduction corresponds to the kinetically controlled pathway, whereas the triple bond reduction leads to the thermodynamically much more stable 5-aluminazoles, 5.

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