- "TRPV1 VANILLOID RECEPTOR ANTAGONISTS WITH A BICYCLIC PORTION"
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The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active
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Page/Page column 75; 132; 133
(2011/10/13)
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- TRPV1 vanilloid receptor antagonists with a bicyclic portion
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The invention discloses compounds of formula I wherein Y s selected from a group of formula and W, Q, n, R1, R2, R3, U1-U5 have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1. 1.
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Page/Page column 25
(2011/11/01)
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- ALKYL-SUBSTITUTED 3' COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, Ar, m and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 32-33
(2010/02/17)
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- CONDENSED HETEROCYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I) wherein R1, A, B, D, E, G, Q, Ar, n, m, and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 82
(2010/04/03)
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- ACYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, Q, G, Ar, m, and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 57
(2010/03/02)
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- 4'-AMINO CYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): formula (I) wherein Cy is selected from formula (Il) and wherein R1, R2, R3, Q, G, Ar, m, n and p are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 100; 101
(2010/04/06)
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- PYRROLIDINE-SUBSTITUTED AZAINDOLE COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, A, B, D, E, G, Ar, and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 43
(2010/02/17)
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- 3' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein Q, R1, R4, m and Ar are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 118
(2009/04/25)
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- Sensitized lanthanide-ion luminescence with aryl-substituted N-(2-nitrophenyl)acetamide-derived chromophores
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The syntheses of the two tetraazamacrocyclic ligands L1 and L2 bearing a [(methoxy-2-nitrophenyl)amino]carbonyl chromophore, i.e., an N-(methoxy-2-nitrophenyl)acetamide moiety, together with their corresponding lanthanide-ion complexes are described. A combined spectroscopic (UV/VIS, 1H-NMR), structural (X-ray), and theoretical (DFT) investigation revealed that the absorption properties of the chromophores were dictated by the extent of electronic delocalisation, which in turn was determined by the position of the MeO substituent at the aromatic ring. X-Ray crystallographic studies showed that when attached to the macrocycle, both isomeric forms of the N-(methoxy-2-nitrophenyl)acetamide unit can participate in coordination, via the C=O, to an encapsulated potassium cation. Luminescence measurements confirmed that such a binding mode also exists in solution for the corresponding lanthanide complexes (q ca. ≤1), with the para-MeO derivative allowing longer wavelength sensitization (λex 330 nm).
- Andrews, Michael,Ward, Benjamin D.,Laye, Rebecca H.,Kariuki, Benson M.,Pope, Simon J. A.
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scheme or table
p. 2159 - 2172
(2010/03/26)
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- 4' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, R6, B, D, E, G, Q, x and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 41
(2009/01/24)
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- 6' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1—R4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 63
(2008/12/08)
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- Sulfonamide peri-substituted bicyclics for occlusive artery disease
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Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
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Page/Page column 61
(2008/06/13)
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- CARBOXYLIC ACID PERI - SUBSTITUTED BICYCLICS FOR OCCLUSIVE ARTERY DISEASE
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Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.
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Page/Page column 97
(2010/11/08)
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- 4-Piperidinecarboxamide modulators of vanilloid VR1 receptor
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This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals.
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Page/Page column 66; 67
(2010/11/08)
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- Vanilloid receptor ligands and their use in treatments
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Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache,
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Page/Page column 35-36
(2008/06/13)
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- Synthesis and herbicidal activity of 1,4-benzoxazin-3-one sulfonylureas
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A series of 1,4-benzoxazin-3-ones with a sulfonylurea group attached at either the 5 or 8 position have been synthesised and found to show moderate herbicidal activity. Similarly, a series of l,4-benzothiazin-3-ones, including some of the related S-oxides
- Anderson, Janet E.
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p. 131 - 138
(2007/10/03)
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- High-affinity α-aminobutyric acid A/benzodiazepine ligands: Synthesis and structure - Activity relationship studies of a new series of tetracyclic imidazoquinoxalines
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A series of tetracyclic imidazoquinoxaline analogs was developed which constrain the carbonyl group of the partial agonist 3-(5-cyclopropyl-1,2,4- oxadiazol-3-yl)-5-[(dimethylamino)carbonyl]4,5-dihydroimidazo[1,5- a]quinoxaline (2, U-91571) away from the benzene ring. These analogs orient the carbonyl group in the opposite direction of the previously reported full agonist 1-(5-cyclopropyl- 1,2,4-oxadiazol-3-yl)- 12,12a-dihydroimidazo[1,5- a]pyrrolo[2,1-c]quinoxalin- 10(11H)one (3, U-89267). A number of approaches were utilized to form the 'bottom' ring of this tetracyclic ring system including intramolecular cyclizations promoted by Lewis acids or base, as well as metal-carbenoid conditions. The size and substitution pattern of the additional ring was widely varied. Analogs within this series had high affinity for the benzodiazepine receptor on the α-aminobutyric acid A chloride ion channel complex. From TBPS shift and Cl- current assays, the in vitro efficacy of compounds within this class ranged from antagonists to partial agonists with only 18a identified as a full agonist. Additionally, several analogs were quite potent at antagonizing metrazole-induced seizures indicating possible anticonvulsant or anxiolytic activity. Unlike 3, analogs in this series did not have high affinity for the diazepam insensitive α6β2δ2 subtype. These results suggest that either constraining the carbonyl group away from the benzene ring or the greater planarity that results from the additional cyclic structure provides analogs with partial agonist properties and prevents effective interaction with the α6β2δ2 subtype.
- Mickelson, John W.,Jacobsen, E. Jon,Carter, Donald B.,Im, Haesook K.,Im, Wha Bin,Schreur, Peggy J. K. D.,Sethy, Vimala H.,Tang, Andy H.,McGee, James E.,Petke, James D.
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p. 4654 - 4666
(2007/10/03)
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- Herbicidal sulfonamides
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Compounds of the formula and salts thereof, W and W1 being independently O or S; A being a nitrogen-containing heterocyclic ring system, E being O, S(O)mor NR4 where m is 0-2; E1 being CH2, CH2CH2, CH (C1-C4 alkyl), C(C1-C4 alkyl)2 or CH (aryl); R1 and R2 are independently hydrogen, halogen or one of a variety of organic substituents. The compounds are effective herbicides.
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