188396-20-5Relevant academic research and scientific papers
PYRROLO AND PYRAZOLOPYRIMIDINES AS UBIQUITIN-SPECIFIC PROTEASE 7 INHIBITORS
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Paragraph 2190; 2192, (2016/08/03)
The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where m, n, X1, X2, R1-R5, R5′ and R6 are described herein.
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4 (3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Mai,Sbardella,Artico,Ragno,Massa,Novellino,Greco,Lavecchia,Musiu,La Colla,Murgioni,La Colla,Loddo
, p. 2544 - 2554 (2007/10/03)
5-Alkyl-2-(alkylthio)-6-(2,6-difluorobenzyl)-3,4-dihydropyrimidin-4(3H)-ones (S-DABOs 2) have been recently described as a new class of human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase (RT) inhibitors (NNRTIs) active at nan
ARYL PYRIMIDINE DERIVATIVES
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, (2008/06/13)
The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT 2B-antagonists. The invention is also directed to formulations and methods for treatment.
ARYL PYRIMIDINE DERIVATIVES
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, (2008/06/13)
The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT 2B-antagonists.
ARYL PYRIMIDINE DERIVATIVES AND USES THEREOF
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, (2008/06/13)
The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT 2B-antagonists. The 5-HT 2B antagonist is a compound of the formula: STR1 wherein: R. sup.1 is hydrogen, alkyl, lower alkoxy, hydroxyalkyl, cycloalkyl, cycloalkyl lower alkyl, alkenyl, lower thioalkoxy, halo, fluoroalkyl,--NR 6 R. sup.7,--CO 2 R 8,--O(CH 2) n R 9, or lower alkyl optionally substituted with hydroxy, alkoxy, halo, or aryl; in which n is 1, 2, or 3;R 6 and R 7 are hydrogen or lower alkyl; R 8 is hydrogen or lower alkyl; andR 9 is hydrogen, lower alkyl, hydroxy, hydroxy lower alkyl, lower alkenyl, or lower alkoxy;R. sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, or lower fluoroalkyl; R 3 is optionally substituted aryl other than pyridyl, thienyl, or furanyl;R 4 is hydrogen, lower alkyl, cycloalkyl, alkenyl, acyl, amino, amido, aryl,--(CH 2) m NR. sup.10 R 11, or lower alkyl optionally substituted by amino, monosubstituted amino, disubstituted amino, hydroxy, carboxy, aryl, lower alkoxy, amido, alkoxy carbonyl, tetrahydrofuran-2-yl, hydroxyalkoxy, or sulfonamido;in whichR 10 and R. sup.11 are hydrogen or lower alkyl; andR 5 is hydrogen or lower alkyl; provided that: (i) when R 3 is naphthyl, indol-1-yl, or 2,3-dihydroindol-1-yl, and R 2, R 4 and R 5 are all hydrogen, R. sup.1 is not methyl; (ii) when R 3 is phenyl or naphthyl, R 1 is not--NR 6 R 7 ;(iii) when R 3 is phenyl, R 2 is not lower alkoxy, and R 1 and R 2 are not halo;(iv) when R 3 is phenyl and R 1 is H, R 2 is not methyl; and (v) when R 3 is 1,2,3,4-tetrahydroquinolinyl, R 4 and R. sup.5 are hydrogen;or a pharmaceutically acceptable salt or N-oxide thereof.
Studies on the active conformation of NK1 antagonist CGP 49823. Part 1. Synthesis of conformationally restricted analogs
Veenstra, Siem J.,Hauser, Kathleen,Betschart, Claudia
, p. 347 - 350 (2007/10/03)
Five conformationally restricted analogs of CGP 49823 have been synthesized. Comparison of their in vitro activities indicates an active conformation of CGP 49823 in which the two aromatic rings of the benzyl and the benzoyl groups are in proximity of each other.
