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Pharmaceutical composition
x
New Patents
Antibiotics M43B and M43C, new glycopeptide antibiotics of the vancomycin class, are produced by Nocardia orientalis NRRL 2452. M43B and M43C have antibacterial activity.
4548925 ANTIBIOTIC M43A, PHARMACEUTICAL COMPOSITION AND METHOD OF USE
4550107 CONDENSED DIAZEPINONES, THEIR COMPOSITIONS AND METHODS OF USE AS PHARMACEUTICALS Wolfhard Engel, Gunte Trummlitz, Wolfgang Eberlein, Gerhard Mihm, Gunther Schmidt, Rudolf Hammer, Antonio Giachetti, Biberach, Federal Republic Of Germany assigned to Dr Karl Thomae GmbH H I
Harvey M Higgins, Kurt E Merkel, Mack H McCormick assigned to Eli Lilly and Company
N--C
//
O
_@x ?B
OH
N I
Cm-O I
A]
OH H3C • \
I
/ CH3
N
CH
CONH2
I
I
CH2u ,, O
CH2u
(
~
-AI~N/RI
O Z
/ILN~ R
N
R2
R CH3
R4
CI R3 "-.,.O~~
HOCH2~
tOH
H3C
O
R5
~NHH
Antibiotic M43A, a new glycopeptide antibiotic of the vancomycin class, is produced by Nocardia orientalis strains NRRL 2450 and NRRL 2452. M43A has excellent antibacterial activity comparable to that of vancomycin.
4548950 PHARMACEUTICAL COMPOSITION Lily Baxendale, Siegfrie Gottfried, Arkley, United Kingdom assigned to Biorex Laboratories Limited The present invention provides a pharmaceutical composition in the form of a watercontaining cream which contains at least one glycyrrhetinic acid derivative (as hereinbefore defined), together with at least one non-toxic, water-soluble salt of zinc, calcium and/or magnesium as stabilizer.
Disclosed are novel condensed diazepinones of formula I See Patent for Chemical Structure wherein B is a fused ring selected from See Patent for Chemical Structure X is -CH- or, when B is ortho-phenylene, X can also be nitrogen; AI is C1-C2 alkylene; A2 is C1-C2 when it is in the 2position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3- or 4-position; R1 is C1-C3 alkyl; R2 is C1-C7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C3-C7 cycloalkyl, optionally hydroxy substituted, or C3-C7 cycloalkylmethyl; or R1 and R2 can, together with the nitrogen therebetween, be a 4- to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N-CH3; R3 is hydrogen, chlorine, or methyl; R4 is hydrogen or C1-C4 alkyl, R5 is hydrogen, chlorine or C1-C4 alkyl; and Z is a single bond, oxygen, methylene or 1,2-ethylene; and NR1 R2-N oxides and nontoxic, pharmaceutically acceptable addition salts thereof. Also disclosed are pyrrolobenzodiazepinone intermediates, pharmaceutical compositions containing the condensed diazepinones and methods of using them to treat cardiovascular disorders, particularly bradycardia and bradyarrhythmia.
New Patents
Antibiotics M43B and M43C, new glycopeptide antibiotics of the vancomycin class, are produced by Nocardia orientalis NRRL 2452. M43B and M43C have antibacterial activity.
4548925 ANTIBIOTIC M43A, PHARMACEUTICAL COMPOSITION AND METHOD OF USE
4550107 CONDENSED DIAZEPINONES, THEIR COMPOSITIONS AND METHODS OF USE AS PHARMACEUTICALS Wolfhard Engel, Gunte Trummlitz, Wolfgang Eberlein, Gerhard Mihm, Gunther Schmidt, Rudolf Hammer, Antonio Giachetti, Biberach, Federal Republic Of Germany assigned to Dr Karl Thomae GmbH H I
Harvey M Higgins, Kurt E Merkel, Mack H McCormick assigned to Eli Lilly and Company
N--C
//
O
_@x ?B
OH
N I
Cm-O I
A]
OH H3C • \
I
/ CH3
N
CH
CONH2
I
I
CH2u ,, O
CH2u
(
~
-AI~N/RI
O Z
/ILN~ R
N
R2
R CH3
R4
CI R3 "-.,.O~~
HOCH2~
tOH
H3C
O
R5
~NHH
Antibiotic M43A, a new glycopeptide antibiotic of the vancomycin class, is produced by Nocardia orientalis strains NRRL 2450 and NRRL 2452. M43A has excellent antibacterial activity comparable to that of vancomycin.
4548950 PHARMACEUTICAL COMPOSITION Lily Baxendale, Siegfrie Gottfried, Arkley, United Kingdom assigned to Biorex Laboratories Limited The present invention provides a pharmaceutical composition in the form of a watercontaining cream which contains at least one glycyrrhetinic acid derivative (as hereinbefore defined), together with at least one non-toxic, water-soluble salt of zinc, calcium and/or magnesium as stabilizer.
Disclosed are novel condensed diazepinones of formula I See Patent for Chemical Structure wherein B is a fused ring selected from See Patent for Chemical Structure X is -CH- or, when B is ortho-phenylene, X can also be nitrogen; AI is C1-C2 alkylene; A2 is C1-C2 when it is in the 2position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3- or 4-position; R1 is C1-C3 alkyl; R2 is C1-C7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C3-C7 cycloalkyl, optionally hydroxy substituted, or C3-C7 cycloalkylmethyl; or R1 and R2 can, together with the nitrogen therebetween, be a 4- to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N-CH3; R3 is hydrogen, chlorine, or methyl; R4 is hydrogen or C1-C4 alkyl, R5 is hydrogen, chlorine or C1-C4 alkyl; and Z is a single bond, oxygen, methylene or 1,2-ethylene; and NR1 R2-N oxides and nontoxic, pharmaceutically acceptable addition salts thereof. Also disclosed are pyrrolobenzodiazepinone intermediates, pharmaceutical compositions containing the condensed diazepinones and methods of using them to treat cardiovascular disorders, particularly bradycardia and bradyarrhythmia.