925418-83-3Relevant academic research and scientific papers
HETEROCYCLIC DERIVATIVES AS M3 MUSCARINIC RECEPTORS
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Page/Page column 56, (2008/12/08)
This invention relates to M3 antagonists of formula (I) wherein R2, R4, R5, R6, W, V, A, D, X, t, u and v are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment of diseases where enhanced M3 receptor activation is implicated.
OXAZOLE AND THIAZOLE DERIVATIVES AND THEIR USES
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Page/Page column 20-21, (2008/12/08)
A quaternary ammonium compound of formula (I) having M3 receptor antagonist activity; a composition comprising such a compound; the use of such a compound in therapy (such as asthma or COPD); and a method of treating a patient with such a compound.
OXAZOLE AND THIAZOLE DERIVATIVES AND THEIR USES 2
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Page/Page column 44, (2008/12/08)
Compounds of formula (I): wherein A, X, R1, R2, R3, R4, R5, R6 and R8 are as defined in the Specification are useful in the treatment of diseases where enhanced M3 receptor activ
NAPADISYLATE SALT OF A MUSCARINIC M3 ANTAGONIST
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Page/Page column 21, (2008/12/08)
The invention provides [2-((R)-Cyclohexyl-hydroxy-phenyl-methyl)-oxazol-5-ylmethyl]- dimethyl-(3-phenoxy-propyl)-ammonium napadisylate, pharmaceutical compositions containing it, and its use in therapy.
COMBINATION OF A MUSCARINIC RECEPTOR ANTAGONIST AND A BETA-2-ADRENOCEPTOR AGONIST
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Page/Page column 32-33, (2008/12/08)
The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist selected, and a second active ingredient which is a β2-adrenoceptor agonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.
CHEMICAL COMPOUNDS
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Page/Page column 69-70, (2008/06/13)
The present invention provides compounds of formula (Ia): wherein A, X, and R1-R8 are as defined herein, such compounds having utility in the treatment of diseases where M3 and beta2 receptors are implicated, such as respiritory tract diseases; compositions comprising such compounds; uses of such compounds in therapy (such as asthma or COPD); and methods of treating a patient with such compounds.
AZOLE AND THIAZOLE DERIVATIVES AND THEIR USE
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Page/Page column 43-44, (2010/11/25)
Compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiritory tract diseases: wherein (i) R1 is C1-C6-alkyl or hydrogen; and R2 is hydrogen or a group -R7, -Z-Y-R7, -Z-NR9R10; -Z-CO-NR9R10, -Z-NR9-[AE11]C(O)O-R7, or -Z-C(O)-R7; and R3 is a lone pair, or C1C6-alkyl; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a lone pair or a group -R7, -Z-Y-R7, -Z-NR9R10, -Z-CO-NR9R10, -Z-NR9-[AE12]C(O)O-R7; or; -Z-C(O)-R7; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group -Y-R7, -Z-Y-R7, -Z-NR9R10; -Z-CO-NR9R10; -Z-NR9-[AE13]C(O)O-R7; or; -Z-C(O)-R7; and R3 is a lone pair, or C1-C6-aIkyl; R4 and R5 are independently selected from the group consisting of aryl, arytfused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl; R6 is -OH, C1-C6-alkyl, C1-C6-alkoxy, hydroxy-C1-C6-alkyl, nitrile, a group CONR82 or a hydrogen atom; A is an oxygen or a sulfur atom; X is an alkylene, alkenylene or alkynylene group; R7 is an C1-C6-alkyl, aryl, aryl-fused-cycloalkyl, aryl-ffused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group; R8 is C1-C6-alkyl or a hydrogen atom; Z is a C1-C16-alkylene, C2-C16-alkenylene or C2-C16-alkynylene group; Y is a bond or oxygen atom; R9 and R10 are independently a hydrogen atom, C1-C6-alkyl, aryl, aryl-fused-heterocycloalkyl, aryl-fused-cycloalkyl, heteroaryl, aryl(C1-C6-alkyl)-, or heteroaryl(C1-C6-alkyl)- group; or R9 and R10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 48 atoms, optionally containing a further nitrogen or oxygen atom.
