51135-96-7Relevant articles and documents
COMPOUNDS FOR TREATMENT OF INFLAMMATORY DISEASES
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, (2016/10/27)
The present invention refers to relates to compound for treating inflammatory diseases, said formula I compounds represented, such as, a pharmaceutically acceptable salts, or their, or a hydrate thereof is characterized in that the, polymerized. According to the present invention, interacting with-path 5-LOX a compound or interference, in particular 5- oh height[...]width it recovers sourly, in sacrifice, which display inhibitory effects can be provides compounds having. (by machine translation)
Synthesis and SAR of thieno[3,2-b]pyridinyl urea derivatives as urotensin-II receptor antagonists
Lim, Chae Jo,Oh, Seung Ae,Lee, Byung Ho,Oh, Kwang-Seok,Yi, Kyu Yang
, p. 5832 - 5835 (2015/01/08)
The preparation and SAR profile of thieno[3,2-b]pyridinyl urea derivatives as novel and potent urotensin-II receptor antagonists are described. An activity optimization study, probing the effects of substituents on thieno[3,2-b]pyridinyl core and benzyl group of the piperidinyl moiety, led to the identification of p-fluorobenzyl substituted thieno[3,2-b]pyridinyl urea 6n as a highly potent UT antagonist with an IC50 value of 13 nM. Although 6n displays good metabolic stability and low hERG binding activity, it has an unacceptable oral bioavailability.
ACETYLENE DERIVATIVES AS STEAROYL COA DESATURASE INHIBITORS
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Page/Page column 60, (2008/12/05)
The present invention provides Stearoyl CoA Desaturase (SCD) inhibitors, hi particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase 1 (SCD 1) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase (SCD) inhibitors.
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin- 1-yl)propyl)indoles gives selective human 5-HT(1D) receptor ligands with improved pharmacokinetic profiles
Van Niel, Monique B.,Collins, Ian,Beer, Margaret S.,Broughton, Howard B.,Cheng, Susan K. F.,Goodacre, Simon C.,Heald, Anne,Locker, Karen L.,MacLeod, Angus M.,Morrison, Denise,Moyes, Christopher R.,O'Connor, Desmond,Pike, Andrew,Rowley, Michael,Russell, Michael G. N.,Sohal, Baibinder,Stanton, Josephine A.,Thomas, Steven,Verrier, Hugh,Watt, Alan P.,Castro, José L.
, p. 2087 - 2104 (2007/10/03)
It has previously been reported that a 3-(3-(piperazin-1- yl)propyl)indole series of 5-HT(1D) receptor ligands have pharmacokinetic advantages over the corresponding 3-(3-(piperidin-1-yl)propyl)indole series and that the reduced pK(a) of the piperazines compared to the piperidines may be one possible explanation for these differences. To investigate this proposal we have developed versatile synthetic strategies for the incorporation of fluorine into these ligands, producing novel series of 4- fluoropiperidines, 3-fluoro-4-aminopiperidines, and both piperazine and piperidine derivatives with one or two fluorines in the propyl linker. Ligands were identified which maintained high affinity and selectivity for the 5-HT(1D) receptor and showed agonist efficacy in vitro. The incorporation of fluorine was found to significantly reduce the pK(a) of the compounds, and this reduction of basicity was shown to have a dramatic, beneficial influence on oral absorption, although the effect on oral bioavailability could not always be accurately predicted.
Inhibitors of farnesyl-protein transferase
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, (2008/06/13)
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.
Neuroleptic 2-piperidinoalkyl-1,4-benzodioxans
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, (2008/06/13)
2-Piperidinoalkyl-1,4-benzodioxans, e.g. those of the formula STR1 and acid addition salts thereof are neuroleptic agents.
2-Piperidinoalkyl-1,4-benzodioxans
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, (2008/06/13)
2-Piperidinoalkyl-1,4-benzodioxans, e.g. those of the formula STR1 AND ACID ADDITION SALTS THEREOF ARE NEUROLEPTIC AGENTS.
2-Piperidinoalkyl-1,4-benzodioxans
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, (2008/06/13)
2-Piperidinoalkyl-1,4 benzodioxans, e.g. those of the formula STR1 AND ACID ADDITION SALTS THEREOF ARE NEUROLEPTIC AGENTS.