- NOVEL DIHYDROPYRIDOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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A compound according to Formula I: wherein R1, LA, GA, R2a, R2b, R3, R4, R5, and R6 are as described herein. The present invention relates to novel compound
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Paragraph 00291
(2016/01/12)
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- Biaryl cannabinoid mimetics-Synthesis and structure-activity relationship
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Synthesis, in vitro biological evaluation, and structure-activity relationships of a biaryl cannabinoid mimetic 2 are reported. Variations in the substitution pattern yielded a number of agonists with low nanomolar affinity. Replacing the phenol group by
- Worm, Karin,Zhou, Q. Jean,Stabley, Gabriel J.,DeHaven, Robert N.,Dolle, Roland E.
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p. 3652 - 3656
(2008/02/05)
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- Phenyl derivatives and methods of use
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Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.
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Page/Page column 26
(2010/10/20)
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- 1,2-AZOLE DERIVATIVES WITH HYPOGLYCEMIC AND HYPOLIPIDEMIC ACTIVITY
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A compound represented by the formula (1) wherein ring A is a ring optionally having 1 to 3 substituents; ring B is a 1,2-azole ring which may further have 1 to 3 substituents; Xa, Xb and Xc are the same or different and each is a bond, - O -, - S - and the like; Ya is a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; Yb and Yc are the same or different and each is a bond or a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; ring C is a monocyclic aromatic ring which may further have 1 to 3 substituents; and R represents -OR4 (R4 is hydrogen atom or optionally substituted hydrocarbon group) and the like, or a salt thereof or a prodrug thereof is useful as an agent for the prophylaxis or treatment of diabetes and the like.
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- A Cannabinoid Derived Prototypical Analgesic
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The synthesis and analgesic testing of 3-cyclohexanol (1) are described.Prior (SAR) studies led us to conclude that the pyran ring of 9-nor-9β-hydroxyhexahydrocannabinol (HHC) was not necessary for the expression of biological activity in this series of cannabinoids.Analysis of models and the use of molecular mechanics calculations suggested that a simpler compound, such as 1, would possess the biological activity of HHC.Compound 1 was prepared in nine steps from acetonitrile (2).Biological testing in five models of pain shows that compound 1 and morphine are equally potent as analgesics and demonstrates that the pyran ring of HHC is not necessary for biological activity.Further simplification of 1 was pursued by the synthesis of 4--2-pentanol (17), but this derivative exhibits significantly reduced analgesic activity.
- Melvin, Lawrence S.,Johnson, M. Ross,Harbert, Charles A.,Milne, George M.,Weissman, Albert
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- 3-[2-Hydroxy-4-(substituted)phenyl]-cycloalkanol analgesic agents
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Cycloalkanones, cycloalkanols and unsaturated analogs thereof, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl which can have an oxygen atom as part of the alkyl chain, their use for pharmacological and medicinal purposes, intermediates therefor and processes for their preparation.
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- Hydroxyalkyl and oxoalkyl substituted phenols as analgesics and sedatives
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Compounds useful for pharmacological and medicinal purposes having the formulae STR1 wherein R is H, C1 -C5 alkanoyl; R1 is H, benzyl, C1 -C5 alkanoyl, P(O)(OH)2, --CO(CH2)2
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- 3-[2-Hydroxy-4-(substituted)-phenyl]azacycloalkanes and derivatives thereof as analgesic agents and intermediates therefor
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Azacycloalkanes, and derivatives thereof, including unsaturated analogs, each of which has at the 3-position a 2-hydroxy-4-substituted phenyl group wherein the 4-position substituent is alkyl which can have an oxygen atom as part of the chain, or aralkyl
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