2-Aminoethyl Substituted Pyrimidin-2-Ones Cyclopropanes, Pyrazolines, Pyrimidines and Benzothiazepines and Their Uses as Urotensin II and Somatostatin 5 Receptor Ligands
First Claim
Patent Images
1. A compound of formula I, II, III, IV, V or salts thereof, wherein R1 and R3 are independently selected from the group consisting of hydrogen, optionally substituted carbonyl(R), O(R), S(R), N(R)(R″
- ), SO(R), SO2(R), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these group may be branched or unbranched and may be optionally substituted;
R2 and R4, R5 and R6 are independently selected from the group consisting of hydrogen, optionally substituted O(R), S(R), N(R)(R″
), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted;
R7 is absent or selected from the group consisting of hydrogen, optionally substituted O(R), S(R), N(R)(R″
), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted;
R8 is selected from the group consisting of hydrogen, optionally substituted O(R), S(R), N(R)(R″
), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted;
R9 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl;
R10 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl;
R11 is absent or selected from the group consisting of optionally substituted O(R), S(R), N(R)(R″
), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted; and
R and R″
are independently selected from the group consisting of hydrogen, optionally substituted alkyl, alkenyl or alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted.
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Abstract
The present invention provides a combinatorial approach to a library of novel compounds having four diversity points. The compounds provide for the mapping of urotensin II and somatostatin 5 receptors by differential binding of said receptors. The present invention further relates to a method of treating diseases for which modulation of the urotensin II receptor produces a physiologically beneficial response in said disease, such as those associated with CNS function and cardiovascular diseases. The present invention further relates to pharmaceutical compositions comprising these agents for the treatment of these diseases adapted to modulate the urotensin II receptor.
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Citations
33 Claims
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1. A compound of formula I, II, III, IV, V or salts thereof,
wherein R1 and R3 are independently selected from the group consisting of hydrogen, optionally substituted carbonyl(R), O(R), S(R), N(R)(R″ - ), SO(R), SO2(R), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these group may be branched or unbranched and may be optionally substituted;
R2 and R4, R5 and R6 are independently selected from the group consisting of hydrogen, optionally substituted O(R), S(R), N(R)(R″
), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted;R7 is absent or selected from the group consisting of hydrogen, optionally substituted O(R), S(R), N(R)(R″
), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted;R8 is selected from the group consisting of hydrogen, optionally substituted O(R), S(R), N(R)(R″
), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted;R9 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl; R10 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl; R11 is absent or selected from the group consisting of optionally substituted O(R), S(R), N(R)(R″
), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted; andR and R″
are independently selected from the group consisting of hydrogen, optionally substituted alkyl, alkenyl or alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these groups may be branched or unbranched and may be optionally substituted. - View Dependent Claims (6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
- ), SO(R), SO2(R), alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein these group may be branched or unbranched and may be optionally substituted;
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24. A pharmaceutical composition comprising a compound selected from the group consisting of
together with pharmaceutically acceptable excipients and carriers.
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25. (canceled)
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26. (canceled)
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27. A method of treating diseases and disorders for which activation or modulation of the urotensin II receptor produces a physiologically beneficial response in said disease or disorder comprising administering an effective amount of a compound selected from the group consisting of
wherein the activation or modulation of the urotensin II receptor alters the vascular pressure, heart rate or locomotor activity in a mammal.
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30. (canceled)
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31. (canceled)
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Specification
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Current AssigneeAcadia Pharmaceuticals Inc.
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Original AssigneeAcadia Pharmaceuticals Inc.
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InventorsOlsson, Roger
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Application NumberUS10/568,149Publication NumberTime in Patent OfficeDaysField of SearchUS Class Current514/211.90CPC Class CodesA61P 21/00 Drugs for disorders of the ...A61P 21/02 Muscle relaxants, e.g. for ...A61P 21/04 for myasthenia gravisA61P 25/00 Drugs for disorders of the ...A61P 25/02 for peripheral neuropathiesA61P 25/16 Anti-Parkinson drugsA61P 25/18 Antipsychotics, i.e. neurol...A61P 25/20 Hypnotics; SedativesA61P 25/28 for treating neurodegenerat...A61P 31/04 Antibacterial agentsA61P 43/00 Drugs for specific purposes...A61P 9/02 Non-specific cardiovascular...A61P 9/04 Inotropic agents, i.e. stim...A61P 9/12 AntihypertensivesC07C 225/18 the carbon skeleton contain...C07C 2601/02 with a three-membered ringC07D 231/06 having one double bond betw...C07D 239/22 with hetero atoms directly ...C07D 239/26 with only hydrogen atoms, h...C07D 281/10 condensed with one six-memb...
