177759-46-5Relevant academic research and scientific papers
COMPOSITIONS FOR THE TREATMENT OF PULMONARY FIBROSIS
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, (2018/02/28)
The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.
Palladium catalyzed α-arylation of methyl isobutyrate and isobutyronitrile: an efficient synthesis of 2,5-disubstituted benzyl alcohol and amine intermediates
Shetty, Rupa,Moffett, Kristofer K.
, p. 8021 - 8024 (2007/10/03)
Several 2,5-disubstituted benzyl alcohols containing a functionalized t-butyl moiety were synthesized via palladium catalyzed α-arylation of methyl isobutyrate and butyronitrile on synthetically useful scales. The resulting benzyl alcohols could then be further elaborated to benzyl amines or other desirable intermediates.
Identification of novel pyrazole acid antagonists for the EP1 receptor
McKeown, Stephen C.,Hall, Adrian,Giblin, Gerard M.P.,Lorthioir, Olivier,Blunt, Richard,Lewell, Xiao Q.,Wilson, Richard J.,Brown, Susan H.,Chowdhury, Anita,Coleman, Tanya,Watson, Stephen P.,Chessell, Iain P.,Pipe, Adrian,Clayton, Nick,Goldsmith, Paul
, p. 4767 - 4771 (2007/10/03)
The discovery, synthesis and structure-activity relationship (SAR) of a novel series of EP1 receptor antagonists is described. Pyrazole acid 4, identified from a chemical array, had desirable physicochemical properties, an excellent in vitro microsomal inhibition and cytochrome P450 (CYP450) profile and good exposure levels in blood. This compound had an ED50 of 1.3 mg/kg in a rat pain model. A range of more potent analogues in the in vitro assay was identified using efficient array chemistry. These EP1 antagonists have potential as agents in the treatment of PGE2 mediated pain.
HETEROCYCLYL COMPOUNDS
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Page/Page column 31, (2010/02/11)
Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein W, X, Y, Z, R1, R2a, R2b, and Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
Compounds for the treatment of ischemia
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Page 63, (2010/02/08)
A3 agonists, methods of using such A3 agonists and pharmaceutical compositions containing such A3 agonists. The A3 agonists are useful for the reduction of tissue damage resulting from tissue ischemia or hypoxia
Aromatic amine compounds that antagonize the pain enhancing effects of prostaglandins
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, (2008/06/13)
PCT No. PCT/GB96/01443 Sec. 371 Date Dec. 16, 1997 Sec. 102(e) Date Dec. 16, 1997 PCT Filed Jun. 17, 1996 PCT Pub. No. WO97/00864 PCT Pub. Date Jan. 9, 1997Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds
Aromatic compounds and pharmaceutical compositions containing them
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, (2008/06/13)
The invention relates to compounds of formula I and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof and processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
ORTHO SUBSTITUTED AROMATIC COMPOUNDS USEFUL AS ANTAGONISTS OF THE PAIN ENHANCING EFFECTS OF E-TYPE PROSTAGLANDINS
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, (2008/06/13)
The invention relates to compounds of the formula (I): STR1 wherein A, B and D are various ring systems such as phenyl, R. sup.1 includes carboxy, R 3 is hydrogen or C 1-4 alkyl and Z is a linking group such as--(CH(R 5)) m--wherein m is 2, 3 or 4, and R 5 includes hydrogen and methyl; and pharmaceutically acceptable salts and in vivo hydrolysable esters or amides thereof, processes for preparing these compounds, pharmaceutical compositions comprising them, and their use in the treatment of pain.
Aromatic amino ethers as pain relieving agents
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, (2008/06/13)
The present invention relates to compounds of formula (I), STR1 wherein A is an optionally substituted phenyl naphthyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidyl, thienyl, thiazolyl, oxazolyl, thiadiazolyl having at least two adjacent ring carbon atoms or a bicyclic ring system, provided that the --CH(R3)N(R2)B--R1 and --OCH(R4 --)--D linking groups arm positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the --OCHR4 -- linking group (and therefore in the 3-position relative to the --CHR3 NR2 -- linking group) is not substituted; B is an optionally substituted ring system; D is an optionally substituted ring system; R1 is a variety of group as defined in the description; R2 is hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, phenylC1-3 alkyl or 5- or 6-membered heteroarylC1-3 alkyl; R3 is hydrogen or C1-4 alkyl; R4 is hydrogen or C1-4 alkyl; and N-oxides of NR2 where chemically possible; and S-oxides of sulphur containing rings were chemically possible; and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof. Process for their preparation, intermediates in theirpreparation, their use as therapeutic agents and pharmaceutical compositions containing them.
