89938-07-8Relevant academic research and scientific papers
HEPATITIS B VIRAL ASSEMBLY EFFECTORS
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Paragraph 00116, (2015/05/05)
Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Paragraph 0511-0512, (2014/01/08)
The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 48-49, (2012/09/11)
The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 44, (2012/09/11)
The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 18, (2012/09/11)
The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists
Ho, Koc-Kan,Auld, Douglas S.,Bohnstedt, Adolph C.,Conti, Paolo,Dokter, Wim,Erickson, Shawn,Feng, Daming,Inglese, Jim,Kingsbury, Celia,Kultgen, Steven G.,Liu, Rong-Qiang,Masterson, Christopher M.,Ohlmeyer, Michael,Rong, Yajing,Rooseboom, Martijn,Roughton, Andrew,Samama, Philippe,Smit, Martin-Jan,Son, Ellen,van der Louw, Jaap,Vogel, Gerard,Webb, Maria,Wijkmans, Jac,You, Ming
, p. 2724 - 2728 (2007/10/03)
An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the o
Pyrimidine derivatives as IL-8 receptor antagonists
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Page 29-30, (2010/02/06)
Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl. A representative example is:
Pyrimidine derivatives and processes for the preparation thereof
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, (2008/06/13)
The present invention relates to novel pyrimidine derivatives of the formulae (I-1) and (I-2) and pharmaceutically acceptable salts thereof which possess an excellent anti-secretory activity, pharmaceutical compositions containing same as an active ingredient, their novel intermediates, and processes for the preparation thereof: STR1 wherein: R4 and R5, which may be the same or different, are independently hydrogen or a C1 -C3 alkyl group, or jointly form a cyclopentyl or cyclohexyl ring; A is a group of formula(II): STR2 wherein R1 and R2 are, independently of each other, hydrogen or a C1 -C3 alkyl group, and R3 is hydrogen, a C1 -C3 alkyl group or a halogen; and B is 1-(substituted)-1,2,3,4-tetrahydroisoquinolin-2-yl of formula (III-1) or 7-(substituted)-4,5,6,7-tetrahydrothieno?2,3-c!pyridin-6-yl of formula (III-2) STR3 wherein R6 is hydrogen or a C1 -C3 alkyl group.
2,4-Diamino-5-benzylpyrimidines as Antibacterial Agents. 4. 6-Substituted Trimethoprim Derivatives from Phenolic Mannich Inetrmediates. Application to the Synthesis of Trimethoprim and 3,5-Dialkylbenzyl Analogues
Roth, Barbara,Aig, Edward,Lane, Kenneth,Rauckman, Barbara S.
, p. 535 - 541 (2007/10/02)
The preparation of a wide variety of 6-substituted trimethoprim analogues was readily accomplished by the reaction of 2,4-diamino-6-substituted-pyrimidines with 2,6-dimethoxy-4-phenol at 120-160 deg C.The less reactive 2,6-dialkyl-4-phenols reacted successfully with 2,4-diamino-6-(alkylthio)pyrimidines to give 5-(substituted benzyl)pyrimidines.The phenolic groups of the products were alkylated in high yield when a nonreactive 6-substituent was present in the pyrimidine ring. 6-(Alkylthio) groups were easily removed with Raney nickel.Trimethoprim was thus obtained in high yield from its 6-(methylthio) counterpart.The 6-substituted trimethoprim analogues all had low activity as inhibitors of Escherichia coli dihydrofolate reductase and as antibacterial agents.
