- p-diaminobenzene derivative as potassium channel regulator, preparation method and medical applications thereof
-
The invention relates to a p-diaminobenzene derivative as a potassium channel regulator, a preparation method and medical applications thereof, and specifically discloses a compound represented by a general formula A or a pharmaceutically acceptable salt
- -
-
Paragraph 0197-0201
(2019/12/09)
-
- Catalyst-Controlled Regiodivergent Dehydrogenative Heck Reaction of 4-Arylthiophene/Furan-3-Carboxylates
-
A catalyst-controlled regiodivergent dehydrogenative Heck reaction of 4-arylthiophene/furan-3-carboxylates has been realized. Use of a palladium catalyst led to the C-5 alkenylation through electronic palladation, while a ruthenium catalyst favored the C-2 alkenylation with the assistance of a directing group. This reaction exhibited good to excellent regioselectivities. (Figure presented.).
- Gao, Shang,Wu, Zijun,Wu, Fei,Lin, Aijun,Yao, Hequan
-
supporting information
p. 4129 - 4135
(2016/12/30)
-
- PIPERIDINYLOXY LACTONE OREXIN RECEPTOR ANTAGONISTS
-
The present invention is directed to piperidinyloxy lactone compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyloxy lactone compounds described herein in the potential treatment or preventi
- -
-
Page/Page column 51; 52
(2015/07/07)
-
- Efficient synthesis of novel glutamate homologues and investigation of their affinity and selectivity profile at ionotropic glutamate receptors
-
A convenient synthesis of four new enantiomerically pure acidic amino acids is reported and their affinity at ionotropic glutamate receptors was determined. The new compounds are higher homologues of glutamic acid in which the molecular complexity has bee
- Pinto, Andrea,Tamborini, Lucia,Mastronardi, Federica,Ettari, Roberta,Romano, Diego,Nielsen, Birgitte,De Micheli, Carlo,Conti, Paola
-
supporting information
p. 1980 - 1982
(2014/04/17)
-
- Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells
-
A novel family of potent dual inhibitors of CK2 and the Pim kinases was discovered by modifying the scaffolds of tricyclic Pim inhibitors. Several analogs were active at single digit nanomolar IC50 values against CK2 and the Pim isoforms Pim-1
- Pierre, Fabrice,Regan, Collin F.,Chevrel, Marie-Claire,Siddiqui-Jain, Adam,MacAlino, Diwata,Streiner, Nicole,Drygin, Denis,Haddach, Mustapha,O'Brien, Sean E.,Rice, William G.,Ryckman, David M.
-
scheme or table
p. 3327 - 3331
(2012/06/18)
-
- 1-(2-PHENOXYMETHYLHETEROARYL)PIPERIDINE AND PIPERAZINE COMPOUNDS
-
The invention relates to compounds of formula I: where X, HAr, a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
- -
-
Page/Page column 35-36
(2011/10/10)
-
- CONDENSED QUINOLINES AS PROTEIN KINASE MODULATORS
-
The invention relates in part to molecules of formula (I) having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the inv
- -
-
Page/Page column 61
(2011/04/14)
-
- Thieno[3,4-c]quinoline-4-yl-amines - Synthesis and investigation of activity against malaria
-
The 4-aryl derivative 3, obtained by Suzuki cross coupling of the methyl 4-bromothiophene-3-carboxylate (2) with 2-nitrophenylboronic acid cyclizes under reductive conditions pH-dependant to yield the tricyclic hydroxamic acid 4 or the lactam 5. The chlorothieno[3,4-c]quinoline 6 was formed by reaction of the lactam 5 with P,P-dichlorophenylphosphinoxide. The amines 7-14 were synthesized from the chloroimine 6. Compounds 7a,b, 8, 9, 10b, 11, 12 and 14a, b were tested for in vitro antimalarial activity using the chloroquine sensitive 3D7 and the chloroquine resistant Plasmodium falciparum strain Dd2. The highest activity were shown by 10b with IC50 values of 130 nM and 50 nM, respectively and by 11 with IC50 values of 190 nM and 44 nM, respectively.
- Goerlitzer,Gabriel,Jomaa,Wiesner
-
p. 901 - 907
(2007/10/03)
-
- Synthesis of thiophenecarboxamides, thieno[3,4-c]pyridin-4(5H)-ones and thieno[3,4-d]pyrimidin-4(3H)-ones and preliminary evaluation as inhibitors of poly(ADP-ribose)polymerase (PARP)
-
Inhibitors of poly(ADP-ribose)polymerase (PARP) inhibit repair of damaged DNA and thus potentiate radiotherapy and chemotherapy of cancer. Treatment of 3-cyanothiophene with potassium nitrate and concentrated sulphuric acid gave 5-nitrothiophene-3-carboxamide. 4-Nitrothiophene-2-carboxamide and 5-nitrothiophene-2-carboxamide were formed similarly from 2-cyanothiophene. Reduction with tin(II) chloride gave the corresponding aminothiophenecarboxamide salts which were isolated via their N-Cbz derivatives. Lithiation of 3,4-dibromothiophene at -116°C and quenching with alkyl chloroformates gave 4-bromothiophene-3-carboxylates, which were hydrolysed to 4-bromothiophene-3-carboxylic acid. Hurtley reactions with the enolates of pentane-2,4-dione and of 1-phenylbutane-1,3-dione, followed by acyl cleavage, led to 4-(2-oxopropyl)thiophene-3-carboxylic acid and 4-phenacylthiophene-3-carboxylic acid, respectively. Condensation with ammonia in acetic acid gave 6-methyl- and 6-phenyl-thieno[3,4-c]pyridin-4-ones, which were selectively nitrated at the 1- and 7-positions or were dinitrated. Ethyl 4-acetamido- and 4-benzamido-thiophene-3-carboxylates were cyclised to 2-methyl- and 2-phenyl-thieno[3,4-d][1,3]oxazin-4-ones, respectively. Ring-opening with ammonia and recyclisation led to 2-substituted thieno[3,4-d]pyrimidin-4-ones. The aminothiophenecarboxamides are analogues of 3-aminobenzamide, a selective inhibitor of poly(ADP-ribose)polymerase (PARP); the thienopyridinones and the thienopyrimidinones are analogues of isoquinolin-1-ones and quinazolin-4-ones, respectively, which inhibit this enzyme. In preliminary assays, several thienopyridinones and thienopyrimidinones showed potent inhibitory activity against PARP. Copyright (C) 1999 Published by Elsevier Science Ltd.
- Shinkwin, Anne E.,Whish, William J. D.,Threadgill, Michael D.
-
p. 297 - 308
(2007/10/03)
-
- Synthesis and antitumour activity of new derivatives of flavone-8- acetic acid (FAA). Part 31): 2-Heteroaryl derivatives
-
A range of 14 derivatives of flavone-8-acetic acid (FAA) with a heterocyclic substituent in place of the 2-phenyl group have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. Some of the compounds, notably 2c,d and s, showed significant in vivo activity and these require further studies in order to evaluate their potential for development.
- Aitken, R. Alan,Bibby, Michael C.,Bielefeldt, Florian,Double, John A.,Laws, Andrea L.,Mathieu, Anne-Laure,Ritchie, Robert B.,Wilson, David W. J.
-
p. 405 - 411
(2007/10/03)
-
- THE BEHAVIOUR OF VICINAL ALKYL AMINOTHIOPHENECARBOXYLATES IN THE SANDMEYER AND SCHIEMANN REACTIONS
-
The diazotization of vicinal alkyl aminothiophenecarboxylates has been studied. 3-Amino compounds gave clear diazonium salts which yielded the expected halo derivatives in the Sandmeyer and Schiemann conditions.However, 2-amino compounds yielded self-coupling products.
- Corral, Carlos,Lasso, Ana,Lissavetzky, Jaime,Alvarez-Insua, Alberto Sanchez,Valdeolmillos, Ana M.
-
p. 1431 - 1435
(2007/10/02)
-