Muscarine antagonists
AssigneeMerck & Co., Inc.
InventorsWayne J. Thompson, Michael F. Sugrue, Richard W. Ransom, Pierre J. Mallorga, Ian M. Bell, Anthony M. Smith
Life of this patent
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Abstract
Compounds, 1,3-dihydro-1-{1-piperidin-4-yl!piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).
Claims9
A compound of structural formula I;
- ##STR130## wherein;
- C is carbon;
- H is hydrogen;
- N is nitrogen;
- O is oxygen;
- S is sulfur;
- P is phosphorus;
- X and Y are independently N or CH;
- Z is N;
- J is NB or CB.sub.2 ;
- K is NB, CB.sub.2, O, carbonyl, thiocarbonyl, sulfonyl, phosphonyl, NBCO, NBCO.sub.2, NBCB.sub.2, COCB.sub.2, CONB, CO.sub.2, CO.sub.2 B, NB.sub.2, NBCONB.sub.2, CB.sub.2 COCB.sub.2, CB.sub.2 CONB, NBCOCB.sub.2 or OB;
- m and o are 0, 1 or 2;
- k is 1 or 2;
- B is H, Me, Et, Pr, iPr, CH.sub.2 OH, CO.sub.2 Me, CO.sub.2 Et, CH.sub.2 CH.sub.2 OH, CONH.sub.2, OH, NH.sub.2, NHMe, OMe, OEt, CONHMe or CONMe.sub.2 ;
- Q is phenyl or heterocycle ring unsubstituted or substituted with Me, Et, Pr, Bu, hydroxyl, alkoxy, F, Cl, Br, I alkylsulfonyl, phenyl or heterocyclic;
- and
- D,E,F and G are chosen from:
- ______________________________________ DEFG ______________________________________ SCRCR CRSCR CRCRCRCR CRCRS OCRCR CROCR and CRCRO ______________________________________
- wherein:
- R is H, small alkyl, branched alkyl, halo, alkoxy, OH, amino, dialkylamino or alkylamino.
A method for the treatment or prevention of abnormal increase in eye axial length in an animal in need thereof, which comprises the step of ocularly administering to said animal a pharmacologically effective amount of a muscarinic pharmacological agent known to be selective for m1, m2 and m4 receptors, but less active at m3 receptors.
A composition useful for the treatment or prevention of abnormal increase in eye axial length in an animal in need thereof, which comprises a pharmacologically effective amount of a muscarinic pharmacological agent, known to be selective for m1, m2 and m4 receptors, but less active at m3 receptors, in a carrier or diluent buffered to a pH suitable for ocular administration.
Dependencies are inferred from the claim text.