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Antibiotics M43B and M43C, pharmaceutical composition and method of use
New Patents
4547500 ERGOT PEPTIDE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Georg Bolliger, Peter Stutz, Binningen, Switzerland assigned to Sandoz Ltd A 2-methyl-8 (R) or (S) ergot peptide alkaloid in free base form or in pharmaceutically acceptable acid addition salt form is a useful anti-Parkinson agent, prolactin secretion inhibitor, antidepressant, vigilance-increasing agent, and antimigraine agent.
4547508 1-PHENYLISOQUINOLINE DERIVATIVES, PHARMACEUTICAL PRODUCTS CONTAINING THESE COMPOUNDS AND THEIR USE Elmar Konz, Hansjorg Kruse, Kelkheim, Federal Republic Of Germany assigned to Hoechst Aktiengesellschaft
~,~ ~
(R2)n
( R 3 ) m ~ A 1-Phenylisoquinoline derivatives of the general formula I See Patent for Chemical Structure I and a process for their preparation are described. They act on the central nervous system, in particular as antidepressants.
ix
Pharmaceutical benzoic acid is prepared from raw benzoic acid made of oxidation of toluene with an oxygen containing gas, the process is characterized in that the oxidation reaction product is contacted with at least I m3 per kg of benzoic acid of a gas with a critical temperature lower than 435 K by passing this gas through the oxidation reaction product at a flow rate of at least 1 m3 per hour per kg of benzoic acid at a temperature of 340-600 K. and a pressure of at least 3 MPa. The pharmaceutical benzoic acid is separated from the mixture by cooling it to 315370 K. at a pressure of 3-300 MPa.
4548601 PREPACKAGED, INJECTABLE PHARMACEUTICAL AND HYPODERMIC NEEDLE COMBINATION Banning Lary is
ta ~4 P tl .s
i* ii .12 '-13
A prepackaged, injectable pharmaceutical hypodermic needle has semi-rigid outer container, supported within which is a substantially non-resiliant inner container containing a premeasured dose of the pharmaceutical. A cannula extending through and fixed with respect to the outer container is adapted to pierce the inner container for injection of the pharmaceutical upon manual collapsing or squeezing of the outer container. Air flow openings in the outer container permit the flow of air into the cavity between the inner and outer containers upon manual release during successive manual compression or squeezing operations, thereby obviating the possibility of negative air pressure being exerted upon the inner container.
4547587 4548924 PROCESS FOR THE PREPARATION OF PHARMACEUTICAL BENZOIC ACID Ludovicus A L Kleintjens, Hubertus M J Grooten, Stein, Netherlands assigned to Stamicarbon B V
ANTIBIOTICS M43B AND M43C, PHARMACEUTICAL COMPOSITION AND METHOD OF USE Karl H Michel assigned to Eli Lilly and Company
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.
4547500 ERGOT PEPTIDE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Georg Bolliger, Peter Stutz, Binningen, Switzerland assigned to Sandoz Ltd A 2-methyl-8 (R) or (S) ergot peptide alkaloid in free base form or in pharmaceutically acceptable acid addition salt form is a useful anti-Parkinson agent, prolactin secretion inhibitor, antidepressant, vigilance-increasing agent, and antimigraine agent.
4547508 1-PHENYLISOQUINOLINE DERIVATIVES, PHARMACEUTICAL PRODUCTS CONTAINING THESE COMPOUNDS AND THEIR USE Elmar Konz, Hansjorg Kruse, Kelkheim, Federal Republic Of Germany assigned to Hoechst Aktiengesellschaft
~,~ ~
(R2)n
( R 3 ) m ~ A 1-Phenylisoquinoline derivatives of the general formula I See Patent for Chemical Structure I and a process for their preparation are described. They act on the central nervous system, in particular as antidepressants.
ix
Pharmaceutical benzoic acid is prepared from raw benzoic acid made of oxidation of toluene with an oxygen containing gas, the process is characterized in that the oxidation reaction product is contacted with at least I m3 per kg of benzoic acid of a gas with a critical temperature lower than 435 K by passing this gas through the oxidation reaction product at a flow rate of at least 1 m3 per hour per kg of benzoic acid at a temperature of 340-600 K. and a pressure of at least 3 MPa. The pharmaceutical benzoic acid is separated from the mixture by cooling it to 315370 K. at a pressure of 3-300 MPa.
4548601 PREPACKAGED, INJECTABLE PHARMACEUTICAL AND HYPODERMIC NEEDLE COMBINATION Banning Lary is
ta ~4 P tl .s
i* ii .12 '-13
A prepackaged, injectable pharmaceutical hypodermic needle has semi-rigid outer container, supported within which is a substantially non-resiliant inner container containing a premeasured dose of the pharmaceutical. A cannula extending through and fixed with respect to the outer container is adapted to pierce the inner container for injection of the pharmaceutical upon manual collapsing or squeezing of the outer container. Air flow openings in the outer container permit the flow of air into the cavity between the inner and outer containers upon manual release during successive manual compression or squeezing operations, thereby obviating the possibility of negative air pressure being exerted upon the inner container.
4547587 4548924 PROCESS FOR THE PREPARATION OF PHARMACEUTICAL BENZOIC ACID Ludovicus A L Kleintjens, Hubertus M J Grooten, Stein, Netherlands assigned to Stamicarbon B V
ANTIBIOTICS M43B AND M43C, PHARMACEUTICAL COMPOSITION AND METHOD OF USE Karl H Michel assigned to Eli Lilly and Company
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.