- SnCl2/EtOH-mediated Synthesis of Novel 4-Ethoxy-and 4-Chloroindazoles Bearing Sulfonamide Moieties
-
The treatment of N-alkyl-5-nitroindazole with stannous chloride in ethanol, aftercoupling of the obtained amines with arylsulfonyl chloride in pyridine, gave the new 4-ethoxy-and 4-chloroindazoles bearing sulfonamide in moderate to good yields. Chlorinati
- Chicha, Hakima,Bouissane, Latifa,El Ammari, Lahcen,Saadi, Mohamed,Baltas, Michel,El Mostapha, Rakib
-
-
Read Online
- Discovery of 1-(1H-indazol-4-yl)-3-((1-phenyl-1H-pyrazol-5-yl)methyl) ureas as potent and thermoneutral TRPV1 antagonists
-
A series of 1-indazol-3-(1-phenylpyrazol-5-yl)methyl ureas were investigated as hTRPV1 antagonists. The structure–activity relationship study was conducted systematically for both the indazole A-region and the 3-trifluoromethyl/t-butyl pyrazole C-region to optimize the antagonism toward the activation by capsaicin. Among them, the antagonists 26, 50 and 51 displayed highly potent antagonism with Ki(CAP) = 0.4–0.5 nM. Further, in vivo studies in mice indicated that these derivatives both antagonized capsaicin induced hypothermia, consistent with their in vitro activity, and themselves did not induce hyperthermia. In the formalin model, 51 showed anti-nociceptive activity in a dose-dependent manner.
- Kang, Jin Mi,Kwon, Sun Ok,Ann, Jihyae,Blumberg, Peter M.,Ha, Heejin,Yoo, Young Dong,Frank-Foltyn, Robert,Lesch, Bernhard,Bahrenberg, Gregor,Stockhausen, Hannelore,Christoph, Thomas,Lee, Jeewoo
-
-
- An Alternative Indazole Synthesis for Merestinib
-
A new synthesis of a key indazole-containing building block for the MET kinase inhibitor merestinib was designed and demonstrated. Crucial to the successful construction of the challenging indazole is an SNAr reaction, which forges the heterocy
- Lu, Yu,Cole, Kevin P.,Fennell, Jared W.,Maloney, Todd D.,Mitchell, David,Subbiah, Ramesh,Ramadas, Balakumar
-
p. 409 - 419
(2018/03/22)
-
- HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
-
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.
- -
-
Paragraph 000407
(2016/05/02)
-
- THIENO[3,2-D]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES
-
Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases.
- -
-
Paragraph 0662; 0663; 0664
(2015/01/06)
-
- THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES
-
Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases
- -
-
Page/Page column 95
(2013/07/19)
-
- CONDENSED HETEROCYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
-
The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I) wherein R1, A, B, D, E, G, Q, Ar, n, m, and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
- -
-
Page/Page column 97
(2010/04/03)
-
- 4'-AMINO CYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
-
The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): formula (I) wherein Cy is selected from formula (Il) and wherein R1, R2, R3, Q, G, Ar, m, n and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
- -
-
Page/Page column 115
(2010/04/06)
-
- 3' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
-
The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein Q, R1, R4, m and Ar are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
- -
-
Page/Page column 132
(2009/04/25)
-
- An expedient, regioselective synthesis of novel 2-alkylamino- and 2-alkylthiothiazolo[5,4-e]- and -[4,5-g]indazoles and their anticancer potential
-
Several novel 2-alkylamino- and 2-alkylthiothiazolo[5,4-e]- and -[4,5-g]indazoles and their 6-alkyl and 8-alkyl derivatives have been synthesised in high overall yields starting from 5-nitro and 6-nitroindazoles in a three-step route involving the regioselective cyclisation of thioureidoindazoles and indazolyl dithiocarbamates as the key steps. Some assorted thiazoloindazoles have been screened for anticancer properties, which demonstrated the anticancer potential of at least one product, justifying its further follow-up.
- Chakrabarty, Manas,Kundu, Taraknath,Arima, Shiho,Harigaya, Yoshihiro
-
p. 6711 - 6723
(2008/12/20)
-
- INDAZOLE OXAZOLIDINONES AS ANTIBACTERIAL AGENTS
-
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein: W is C(=O)NHR1, C(=S)NHR1, or CH2het; Y is H, or CF; R1 is H, C16alkyl, or OC1-6/s
- -
-
Page/Page column 19
(2010/11/28)
-
- Reduction of nitroindazoles: Preparation of new amino and chloroamino derivatives
-
The synthesis of chloroaminoindazoles by the reduction of the nitro group of indazoles using stannous chloride in alcoholic acid solution is reported. Using catalytic hydrogenation with palladium the expected reduction to amino-indazoles occur.{A figure is presented}. Indazole Nitro Reduction Chlorination Aminochloroindazole Heterocycle.
- Miloudi, Abdellah,El Abed, Douniazed,Boyer, Gerard,Galy, Jean-Pierre
-
p. 2595 - 2605
(2008/02/04)
-
- N-ALKYNYL-2- (SUBSTITUTED ARYLOXY) ALKYLTHIOAMIDE DERIVATIVES AS FUNGICIDES
-
Fungicidal compounds of the general formula (1), wherein Ar is a group of the formula (A), (B1), (B2) or (C), or Ar is a 5- or 6-linked group of the formula (D1) or (D2); and R1, R2, R3, R4, R5, n, A1, A2, A3, A4, A5, Ka, Kb, L, M, V, W, X,Y and Z have the definitions given in claim 1.
- -
-
Page 106-107
(2010/02/09)
-
- Synthesis of Pyrazoloacridin-9(10H)-ones
-
Eight pyrazoloacridin-9(10H)-ones were prepared in a three step procedure from 5- and 6-nitroindazoles.Palladium catalysed hydrogenation of nitroindazoles afforded the corresponding 5- and 6-aminoindazoles.These, in turn, reacted with o-chlorobenzoic acid under the conditions of the Ullman reaction to give anthranilic acids.Cyclisation of these acids by means of sulfuric acid led to the title compounds.If phosphoryl chloride was used, instead of sulfuric acid, a 9-chloroacridine derivative was obtained.All the compounds were characterised by 1H NMR spectroscopy.
- Boyer, Gerard,Galy, Jean-Pierre,Faure, Robert,Elguero, Jose,Barbe, Jacques
-
p. 2601 - 2615
(2007/10/02)
-