- Novel methylene-linked heterocyclic EP1 receptor antagonists
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We describe the SAR, in terms of heterocyclic replacements, for a series of pyrazole EP1 receptor antagonists. This study led to the identification of several aromatic heterocyclic replacements for the pyrazole in the original compound. Investi
- Hall, Adrian,Bit, Rino A.,Brown, Susan H.,Chowdhury, Anita,Giblin, Gerard M.P.,Hurst, David N.,Kilford, Ian R.,Lewell, Xiao,Naylor, Alan,Scoccitti, Tiziana
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p. 1592 - 1597
(2008/12/22)
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- OXAZOLE AND THIAZOLE COMPOUNDS AND THEIR USE IN THE TREATMENT OF PGE2 MEDIATED DISORDERS
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Compounds of formula (I) or a pharmaceutiically acceptable derivative thereof: wherein X, Z, Y', Y'', R1 ,R2a, R2b, and Rx 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.
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Page/Page column 26; 27
(2010/11/24)
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- Novel phosphorus-containing derivatives
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A compound of the Formula I a prodrug thereof, or the pharmaceutically acceptable salt of the compound or prodrug; wherein X, Y, a, b, c, d, R1, R2, R3, R4, R5, R6 and R7 are as defined above and are useful to treat inflammation and other immune disorders. The present invention also relates to pharmaceutical compositions that include compounds of Formula I and a pharmaceutically acceptable carrier. Moreover, the present invention relates to methods of using the above-described compounds and compositions to treat and prevent diseases and conditions.
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- Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine σ ligands as potential antipsychotic drugs
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Receptor antagonists may be effective antipsychotic drugs that do not induce motor side effects caused by ingestion of classical drugs such as haloperidol. We obtained evidence that 1-(2-dipropylaminoethyl)-4-methoxy- 6H-dibenzo[b,d]pyran hydrochloride 2a had selective affinity for σ receptor over dopamine D2 receptor. This compound was designed to eliminate two bonds of apomorphine 1 to produce structural flexibility for the nitrogen atom and to bridge two benzene rings with a -CH2O- bond to maintain the planar structure. In light of the evidence, N,Y-dipropyl-2-(4-methoxy-3- benzyloxylphenyl)ethylamine hydrochloride 10b was designed. Since compound 10b had eliminated a biphenyl bond of 6H-dibenzo[b,d]pyran derivative 2a, it might be more released from the rigid structure of apomorphine 1 than compound 2a. The chemical modification of compound 10b led to the discovery that N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxyl)phenyl]ethylamine hydrochloride 10g (NE- 100), the best compound among arylalkoxyphenylalkylamine derivatives 3, had a high and selective affinity for σ receptor and had a potent activity in an animal model when the drug was given orally. We report here the design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine derivatives 3.
- Nakazato, Atsuro,Ohta, Kohmei,Sekiguchi, Yoshinori,Okuyama, Shigeru,Chaki, Shigeyuki,Kawashima, Yutaka,Hatayama, Katsuo
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p. 1076 - 1087
(2007/10/03)
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