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5145611 Carboxylic acid derivatives, and pharmaceutical compositions containing them
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alkyl or alkoxy; and n is 0 or 1) or a group of the formula: See Patent for Chemical Structure (wherein R2 is hydrogen or alkyl); Y is a single bond, -NH-, alkylene having 1 or 2 carbon atoms or -CH double bondCH-; and R3 is an optionally substituted hydrocarbon group, or their salts are disclosed. They show strong ACAT inhibitory activities.
5143936 BENZOPYRAN COMPOUND AND ITS PHARMACEUTICAL USE Tsutomu Yamanaka, Toshio Seki, Tohru Nakajima, Osamu Yaoka, Nakatsu, Japan assigned to Yoshitomi Pharmaceutical Industries Ltd A benzopyran compound of the general formula (I) See Patent for Chemical Structure (I) wherein A represents -OR1 or -NH-COR2 (wherein R1 represents hydrogen, a lower alkyl, formyl, an alkanoyl, an aroyl or an aralkyl and R2 represents hydrogen, a lower alkyl, a lower alkoxy, amino, mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyllower alkyl, an aryl or a heteroaryl); R3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyllower alkyl, an aryl or a heteroaryl, or R2 and R3 combinedly together form an alkylene having 1 to 2 carbon atoms; R4 and R5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R6 represents hydroxyl group, formyloxy, an alkanoyloxy, a haloalkanoyloxy, a lower alkoxycarbonyloxy, an aroyloxy, a heteroaroyloxy, carbamoyloxy, a mono- or di-lower alkycarbamoyloxy and R7 represents hydrogen, or R6 and R7 combinedly together form a bond and X and Y are the same or different, and respectively represent hydrogen, halogen, nitro, cyano, a lower alkyl, a lower alkoxy, a halo-lower alkyl, carboxyl, formyl, an alkanoyl, an aroyl, a haloalkanoyl, carbamoyl, a lower alkylsulfinyl, an arylsulfinyl, a lower alkylsulfonyl, an arylsulfonyl, sulfonamido or a mono- or di-lower alkylsulfonamido, or their pharmaceutically acceptable salts and its pharmaceutical use. The compounds of the present invention exhibit remarkable and long lasting antihypertensive ac-
tions and peripheral vascular relaxant actions and therefore are useful as therapeutic medicines for hypertensive. Since they also display selective coronary vasodilating actions and the duration of actions are very long, they are of use as therapeutic medicines for cardiovascular disturbances such as angina pectoris and cardiac insufficiency.
5144011 ACIDITY-SENSITIVE SPACER MOLECULE TO CONTROL THE RELEASE OF PHARMACEUTICALS FROM MOLECULAR CARRIERS Wei C Shen, Hugues J - Ryser assigned to Boston University A method for controlling the release of durgs or other passenger molecules form carrier conjugates, and a class of conjugates that releases drugs when ingested by a cell or subjected to acidic conditions, are disclosed. These conjugates contain a passenger molecule which is attached to a spacer molecule through an acidic bonding group, such as carboxyl, that is in a cis configuration with another acidic group, and a carrier molecule that is bonded to the spacer molecule at another site. When subjected to a mild increase in acidity, such as occurs within a lysosome of a cell, the drug or other passenger molecule is hydrolyzed from the the conjugate and released in unmodified, active form.
5145611 CARBOXYLIC ACID DERIVATIVES, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Hans P Wolff, Ernst-Christian Witte, HansFrieder Kuehnle, Hirschberg Grossachsen, Federal Republic Of Germany assigned to Boehringer Mannheim G m b H Carboxylic acid derivatives of the formula See Patent for Chemical Structure R1 is alkoxy, alkylthio, alkylsulphinyl, alkulsulphonyl, alkylamino, cycloalkyl, or cycloalkoxy or optionally substituted aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or arylamino. R2 is
New Patents
alkyl or alkoxy; and n is 0 or 1) or a group of the formula: See Patent for Chemical Structure (wherein R2 is hydrogen or alkyl); Y is a single bond, -NH-, alkylene having 1 or 2 carbon atoms or -CH double bondCH-; and R3 is an optionally substituted hydrocarbon group, or their salts are disclosed. They show strong ACAT inhibitory activities.
5143936 BENZOPYRAN COMPOUND AND ITS PHARMACEUTICAL USE Tsutomu Yamanaka, Toshio Seki, Tohru Nakajima, Osamu Yaoka, Nakatsu, Japan assigned to Yoshitomi Pharmaceutical Industries Ltd A benzopyran compound of the general formula (I) See Patent for Chemical Structure (I) wherein A represents -OR1 or -NH-COR2 (wherein R1 represents hydrogen, a lower alkyl, formyl, an alkanoyl, an aroyl or an aralkyl and R2 represents hydrogen, a lower alkyl, a lower alkoxy, amino, mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyllower alkyl, an aryl or a heteroaryl); R3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyllower alkyl, an aryl or a heteroaryl, or R2 and R3 combinedly together form an alkylene having 1 to 2 carbon atoms; R4 and R5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R6 represents hydroxyl group, formyloxy, an alkanoyloxy, a haloalkanoyloxy, a lower alkoxycarbonyloxy, an aroyloxy, a heteroaroyloxy, carbamoyloxy, a mono- or di-lower alkycarbamoyloxy and R7 represents hydrogen, or R6 and R7 combinedly together form a bond and X and Y are the same or different, and respectively represent hydrogen, halogen, nitro, cyano, a lower alkyl, a lower alkoxy, a halo-lower alkyl, carboxyl, formyl, an alkanoyl, an aroyl, a haloalkanoyl, carbamoyl, a lower alkylsulfinyl, an arylsulfinyl, a lower alkylsulfonyl, an arylsulfonyl, sulfonamido or a mono- or di-lower alkylsulfonamido, or their pharmaceutically acceptable salts and its pharmaceutical use. The compounds of the present invention exhibit remarkable and long lasting antihypertensive ac-
tions and peripheral vascular relaxant actions and therefore are useful as therapeutic medicines for hypertensive. Since they also display selective coronary vasodilating actions and the duration of actions are very long, they are of use as therapeutic medicines for cardiovascular disturbances such as angina pectoris and cardiac insufficiency.
5144011 ACIDITY-SENSITIVE SPACER MOLECULE TO CONTROL THE RELEASE OF PHARMACEUTICALS FROM MOLECULAR CARRIERS Wei C Shen, Hugues J - Ryser assigned to Boston University A method for controlling the release of durgs or other passenger molecules form carrier conjugates, and a class of conjugates that releases drugs when ingested by a cell or subjected to acidic conditions, are disclosed. These conjugates contain a passenger molecule which is attached to a spacer molecule through an acidic bonding group, such as carboxyl, that is in a cis configuration with another acidic group, and a carrier molecule that is bonded to the spacer molecule at another site. When subjected to a mild increase in acidity, such as occurs within a lysosome of a cell, the drug or other passenger molecule is hydrolyzed from the the conjugate and released in unmodified, active form.
5145611 CARBOXYLIC ACID DERIVATIVES, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Hans P Wolff, Ernst-Christian Witte, HansFrieder Kuehnle, Hirschberg Grossachsen, Federal Republic Of Germany assigned to Boehringer Mannheim G m b H Carboxylic acid derivatives of the formula See Patent for Chemical Structure R1 is alkoxy, alkylthio, alkylsulphinyl, alkulsulphonyl, alkylamino, cycloalkyl, or cycloalkoxy or optionally substituted aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl or arylamino. R2 is