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US 8,618,169 B2Granted
Derivatives of N-phenylanthranilic acid and 2-benzimidazolone as potassium channel and/or neuron activity modulators
AssigneeRamot at Tel-Aviv University Ltd.
InventorsBernard Attali, Asher Peretz
Life of this patent
Estimating the term…
Abstract
Compounds, compositions and methods are provided which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing cortical and/or peripheral neuron activity are disclosed. Novel derivatives of N-phenylanthranilic acid are also disclosed.
Claims7
A pharmaceutical composition comprising, as an active ingredient, a compound having the general Formula I:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- Z is an A-G(═K)—X—Y group,
- and wherein:
- A is alkyl or absent;
- G is C;
- K is selected from the group consisting of O and S;
- X is NRb;
- and
- Y is selected from the group consisting of an unsubstituted hydroxyalkyl, and a substituted or unsubstituted polyalkylene glycol residue,
- R1 is selected from the group consisting of hydrogen, alkyl, cycloalkyl or aryl;
- each of R2, R3, R4, R5, R6, R7, R8, R9 and R10 is independently selected from the group consisting of hydrogen, alkyl, hydroxyalkyl, trihaloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, halo, hydroxy, alkoxy, aryloxy, thiohydroxy, thioalkoxy, thioaryloxy, sulfinyl, sulfonyl, cyano, nitro, amino and —NR15R16, or, alternatively, at least two of R2, R3, R4, R5 and R6, of R7, R8, R9 and R10 and/or of R11, R12, R13, and R14 form a five- or six-membered aromatic, heteroaromatic, alicyclic or heteroalicyclic ring;
- R15 and R16 are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, carbonyl and sulfonyl, or, alternatively R15 and R16 form a five- or six-member heteroalicyclic ring;
- and
- each of Ra, Rb and Rc is independently selected from the group consisting of hydrogen, alkyl, cycloalkyl and aryl,
- wherein when Y is a polyalkylene glycol residue, said polyalkylene glycol residue does not include a —ONO2 group or an antioxidant residue, and a pharmaceutically acceptable carrier,
- the composition being packaged in a packaging material and identified in print, in or on said packaging material, for use in increasing a current amplitude of a voltage-dependent potassium channel which comprises a KCNQ2 channel and/or a KCNQ3 channel and/or a KCNQ2/3 channel, said increasing said current amplitude comprising administering the pharmaceutical composition to a subject in need thereof.
14 more elements
A pharmaceutical composition comprising, as an active ingredient, a compound having the general Formula I:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- Z is an A-G(═K)—X—Y group,
- and wherein:
- A is alkyl or absent;
- G is C;
- K is selected from the group consisting of O and S;
- X is NRb;
- and
- Y is selected from the group consisting of an unsubstituted hydroxyalkyl, and a substituted or unsubstituted polyalkylene glycol residue,
- R1 is selected from the group consisting of hydrogen, alkyl, cycloalkyl or aryl;
- each of R2, R3, R4, R5, R6, R7, R8, R9 and R10 is independently selected from the group consisting of hydrogen, alkyl, hydroxyalkyl, trihaloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, halo, hydroxy, alkoxy, aryloxy, thiohydroxy, thioalkoxy, thioaryloxy, sulfinyl, sulfonyl, cyano, nitro, amino and —NR15R16, or, alternatively, at least two of R2, R3, R4, R5 and R6, of R7, R8, R9 and R10 and/or of R11, R12, R13 and R14 form a five- or six-membered aromatic, heteroaromatic, alicyclic or heteroalicyclic ring;
- R15 and R16 are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, carbonyl and sulfonyl, or, alternatively R15 and R16 form a five- or six-member heteroalicyclic ring;
- and
- each of Ra, Rb and Rc is independently selected from the group consisting of hydrogen, alkyl, cycloalkyl and aryl,
- wherein when Y is a polyalkylene glycol residue, said polyalkylene glycol residue does not include a —ONO2 group or an antioxidant residue, and a pharmaceutically acceptable carrier,
- the composition being packaged in a packaging material and identified in print, in or on said packaging material, for use in treating schizophrenia.
14 more elements
Dependencies are inferred from the claim text.