Materials and methods for the treatment of hypertension and angina
AssigneeARYx Therapeutics, Inc.
InventorsPascal Druzgala, Peter G. Milner, Jürg Pfister, Xiaoming Zhang
Life of this patent
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Abstract
The subject invention provides useful and novel calcium channel blockers based upon mibefradil. The subject invention also provides methods for synthesizing the compounds of the invention. The invention also provides methods for the control or prevention of hypertension, angina pectoris, ischemia, arrhythmias, and cardiac insufficiency in a patient by administering a compound, or composition, of the invention to an individual in need of such treatment.
Claims14
A calcium channel blocker compound having the following structure:
- R4=
- wherein:
- X=a bond, (CH2)n, O, S, or O(CH2)n,
- R=C1-6 alkyl, optionally substituted with OH or NH2;
- R2=F or COOR5,
- wherein R5 is C1-6 alkyl, optionally substituted with OH or NH2;
- R3=CH3 or (CH2)n—COOR6,
- wherein R6 is C1-6 alkyl, optionally substituted with OH or NH2;
- R7=O, NH, or NR9,
- R8=optionally substituted aryl or heterocycle,
- R9=C1-6 alkyl,
- R10=O, S, SO, SO2, NH, NR12 or N(CH2)m COOR13,
- R11=aryl or heterocyclyl optionally substituted with (CH2)n COOR14,
- R12=C1-6 alkyl, optionally substituted with OH or NH2,
- R13=C1-6 alkyl, optionally substituted with OH or NH2,
- R14=C1-6 alkyl, optionally substituted with OH or NH2,
- R15=(CH2)n COOR16,
- R16=C1-6 alkyl, optionally substituted with OH or NH2,
- R17=not present or COOR18 wherein R18 is C1-6 alkyl, optionally substituted with OH or NH2, and
- wherein n=1-6 and m=O or 1.
A calcium channel blocker compound having a formula selected from the group consisting of:
- X=bond, CH2, or OCH2
- R=lower alkyl optionally substituted with OH or NH2;
- R=lower alkyl optionally substituted with OH or NH2;
- n=1 to 3
- R=lower alkyl optionally substituted with OH or NH2;
- n=1 to 3
- R=lower alkyl optionally substituted with OH or NH2;
- R=lower alkyl optionally substituted with OH or NH2.
A pharmaceutical composition comprising a calcium channel blocker compound having the following structure:
- wherein:
- X=a bond, (CH2)n, O, S, or O(CH2)n,
- R1=C1-6 alkyl, optionally substituted with OH or NH2;
- R2=F or COOR5,
- wherein R5 is C1-6 alkyl, optionally substituted with OH or NH2;
- R3=CH3 or (CH2)n—COOR6,
- wherein R6 is C1-6 alkyl, optionally substituted with OH or NH2;
- R4=
- R7=O, NH, or NR9,
- R8=optionally substituted aryl or heterocycle,
- R9=C1-6 alkyl,
- R10=O, S, SO, SO2, NH, NR12 or N(CH2)m COOR13,
- R11=aryl or heterocyclyl optionally substituted with (CH2)n COOR14,
- R12=C1-6 alkyl, optionally substituted with OH or NH2,
- R13=C1-6 alkyl, optionally substituted with OH or NH2,
- R14=C1-6 alkyl, optionally substituted with OH or NE2,
- R15=(CH2)n COOR16,
- R16=C1-6 alkyl, optionally substituted with OH or NH2,
- R17=not present or COOR18 wherein R18 is C1-6 alkyl, optionally substituted with OH or NH2, and
- wherein n=1-6 and m=O or 1.
A pharmaceutical composition comprising a calcium channel blocker compound having a formula selected from the group consisting of:
- X=bond, CH2, or OCH2
- R=lower alkyl optionally substituted with OH or NH2;
- R=lower alkyl optionally substituted with OH or NH2;
- n=1 to 3
- R=lower alkyl optionally substituted with OH or NH2;
- n=1 to 3
- R=lower alkyl optionally substituted with OH or NH2;
- R=lower alkyl optionally substituted with OH or NH2.
Dependencies are inferred from the claim text.