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5015639 Substituted benzazepines, their preparation and pharmaceutical compositions containing them
New Patents
xiv
hydroxypropyl methylcellulose for maintaining the prostaglandin in a therapeutically effective without negatively affecting the amount therapeutic activity of the NSAID.
5015639 SUBSTITUTED BENZAZEPINES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Joel Berger, Wei K Chang, Marjori Peters assigned to Schering Corporation Disclosed herein are novel I-substituted-2,3,4, 5-tetrahydro-I-3-benzazepines of the general formula I: See Patent for Chemical Structure I wherein Rl, R2, R3, R4 and R5 are specified substituents. Rl is preferably -X6, -CHR7R8, cycloalkyl, cycloalkenyl, See Patent for Chemical Structure or pyrrolyl where m is 1, R6 represents double bondH, phenyl, substituted phenyl, aralkyl, alkyl, cycloalkyl, haloalkyl or alkoxyalkyl, R7 represents H or alkyl preferably H, R8 represents cycloalkyl, cycloalkenyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl and R9 represents alkyl, aloxy or alkoxyalkyl. R2 preferably represents -H and R3-CH3, and R4 is preferably halogen and R5 is preferably OH, OCO.R9 or -O(CR7)2.OCO.R13 where R7 represents hydrogen, R9 is as defined above and R13 represents alkyl. The compounds of the formula I are indicated as being useful in the treatment of psychoses, depression and pain. Also disclosed are process for the preparation of the novel compounds as well as pharmaceutical , compositions comprising them.
5015646 PHARMACEUTICALLY USEFUL POLYMORPHIC MODIFICATION OF BUSPIRONE Jack C Simms assigned to Bristol-Myers Squibb co Buspirone hydrochloride can exist in two polymorphic forms and the newly discoverd lower
melting form, which is thermodynamically favored at pharmaceutically relevant temperatures, offers advantage in manufacture of buspirone pharmaceutical compositions .
5015654 PHARMACEUTICAL COMPOSITIONS Saa Al-Damluji, London, United Kingdom assigned to National Research Development Corporation A pharmaceutical composition which comprises a mixture of an alpha-2 adrenoceptor antagonist, preferably idazoxan, or a pharmaceutically acceptable salt thereof, and either a catecholamine precursor or carbidopa.
5015656 ORGANIC COMPOUNDS THEIR USE AS PHARMACEUTICALS
AND
Maria I F Fernandez, Terrence Hotten, David E Tupper, Madrid, Spain assigned to Lilly S A; Lilly Industries Limit A pharmaceutical compound of the formula See Patent for Chemical Structure in which Rl, R2 and R3 independently are hydrogen, hydroxy, halo, nitro, amino, C2-5 acylamino, Cl-4 alkyl, CHO, -CH20H, -CH20Cl-4 alkyl, -COOH, COCl-3 alkyl, -CH(OH)Cl-3 alkyl, Cl-4 alkoxy, C2-4 alkenyloxy, Cl-4 alkylthio, Cl-4 alkylsulphinyl, Cl-4 alkylsulphonyl, Nsubstituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or Rl and R2 together form a C3-5 alkylene bridge; provided that at least one of R2 and R3 is Cl-4 alkoxy or C2-4 alkenyloxy; and X is (i) -(CH2)nN(R4)2 where each R4 independently is Cl-4 alkyl, C2-4 alkenyl or optionally substituted C6H5CH2-, and n is I,2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a Cl-3 alkylene chain; and salts and esters thereof.
xiv
hydroxypropyl methylcellulose for maintaining the prostaglandin in a therapeutically effective without negatively affecting the amount therapeutic activity of the NSAID.
5015639 SUBSTITUTED BENZAZEPINES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Joel Berger, Wei K Chang, Marjori Peters assigned to Schering Corporation Disclosed herein are novel I-substituted-2,3,4, 5-tetrahydro-I-3-benzazepines of the general formula I: See Patent for Chemical Structure I wherein Rl, R2, R3, R4 and R5 are specified substituents. Rl is preferably -X6, -CHR7R8, cycloalkyl, cycloalkenyl, See Patent for Chemical Structure or pyrrolyl where m is 1, R6 represents double bondH, phenyl, substituted phenyl, aralkyl, alkyl, cycloalkyl, haloalkyl or alkoxyalkyl, R7 represents H or alkyl preferably H, R8 represents cycloalkyl, cycloalkenyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl and R9 represents alkyl, aloxy or alkoxyalkyl. R2 preferably represents -H and R3-CH3, and R4 is preferably halogen and R5 is preferably OH, OCO.R9 or -O(CR7)2.OCO.R13 where R7 represents hydrogen, R9 is as defined above and R13 represents alkyl. The compounds of the formula I are indicated as being useful in the treatment of psychoses, depression and pain. Also disclosed are process for the preparation of the novel compounds as well as pharmaceutical , compositions comprising them.
5015646 PHARMACEUTICALLY USEFUL POLYMORPHIC MODIFICATION OF BUSPIRONE Jack C Simms assigned to Bristol-Myers Squibb co Buspirone hydrochloride can exist in two polymorphic forms and the newly discoverd lower
melting form, which is thermodynamically favored at pharmaceutically relevant temperatures, offers advantage in manufacture of buspirone pharmaceutical compositions .
5015654 PHARMACEUTICAL COMPOSITIONS Saa Al-Damluji, London, United Kingdom assigned to National Research Development Corporation A pharmaceutical composition which comprises a mixture of an alpha-2 adrenoceptor antagonist, preferably idazoxan, or a pharmaceutically acceptable salt thereof, and either a catecholamine precursor or carbidopa.
5015656 ORGANIC COMPOUNDS THEIR USE AS PHARMACEUTICALS
AND
Maria I F Fernandez, Terrence Hotten, David E Tupper, Madrid, Spain assigned to Lilly S A; Lilly Industries Limit A pharmaceutical compound of the formula See Patent for Chemical Structure in which Rl, R2 and R3 independently are hydrogen, hydroxy, halo, nitro, amino, C2-5 acylamino, Cl-4 alkyl, CHO, -CH20H, -CH20Cl-4 alkyl, -COOH, COCl-3 alkyl, -CH(OH)Cl-3 alkyl, Cl-4 alkoxy, C2-4 alkenyloxy, Cl-4 alkylthio, Cl-4 alkylsulphinyl, Cl-4 alkylsulphonyl, Nsubstituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or Rl and R2 together form a C3-5 alkylene bridge; provided that at least one of R2 and R3 is Cl-4 alkoxy or C2-4 alkenyloxy; and X is (i) -(CH2)nN(R4)2 where each R4 independently is Cl-4 alkyl, C2-4 alkenyl or optionally substituted C6H5CH2-, and n is I,2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a Cl-3 alkylene chain; and salts and esters thereof.