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German Therapy Congress and Pharmaceutical Exhibition.

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CONFERENCE REPORTS
German Therapy Congress and Pharmaceutical Exhibition
Karlsruhe (Germany), August 27 to September 2, 1961
The meeting named 13th Therapeutic Week dealt among
other subjects with geriatric psychotherapy, liver, gallbladder,
cardiovascular and circulatory disorders, the significance of
toxic foci, the intricacy of active vaccination, also with
problems of social medicine and occupational diseases,
physical therapy and traffic safety.
Approximately 230 drug firms participated in the pharmaceutical exhibition. Only a few of the new natural products
and the especially interesting synthetic compounds are presented in this report. The great number of combination products - although they are very valuable for therapeutic
purposes - are not considered here.
Disorders of the blood supply of the heart muscle, i.e.
coronary disorders are among the most frequent causes of
death in our times. The firm Woelm-Labaz GmbH. developed
Amplivix which is 2-ethyl-3-(3’,5’-diiodo-4‘-hydroxybenzoy1)benzofuran (I).
IV is prepared by N-acylation of 6-aminopenicillanic acid
with phenoxypropionic acid and is practically non-toxic.
Used as the potassium salt in the form of tablets, it is resorbed in the intestinal tract because of its good water
solubility and high stability towards acids. Its effective
spectrum corresponds to that of the older penicillins.
Yxinm, active ingredient: 2-(1’,2’,3’,4’-tetrahydro-l’-naphthy1)imidazoline hydrochloride (V), 5 % in isotonic solution,
is a new ophthalmological drug of Pfizer GmbH. It is
recommended for the treatment of conjunctivitis.
V
@
Farbenfabriken Bayer and Schering AG have developed
independently of each other a new sulfadiazine derivative.
Both firms are introducing the product simultaneously as
It is 5-methoxysulfadiazine(VI) and is marketed in
Durenat @.
tablet and liquid form.
It was shown in many pharmacological and clinical tests that
this substance is a specific coronary vasodilator and thus
increases the oxygen supply of the heart muscle. The particular advantage of this product compared to the nitrites is its
long-lasting effect.
E. Merck recommends Nasivin for the decongestion of the
inflamed mucosa of the nose and the sinuses and for the
topical treatment of conjunctivitis. The product is 2-(4‘-tbutyl-2’,6’-dimethyl-3’-hydroxybenzyl)-2-imidazolinehydrochloride (11).
@
CH3
I1
The almost white crystals melt at 30OoC. and are easily
soluble in water and alcohol. The strongly vasoconstricting
preparation does not cause undesirable side-effects.
The long search for a fully active physiological depot-form
of vitamin B12 has been brought to a close by E. Merck with
the introduction of Aquo-Cytobion@.This is the aquocobalamin acetate (111) designated as vitamin Biza or Bl2b in the
co+
The manufacturers stress that extensive investigations proved
its especially long-lasting, intensive effect and its broader
spectrum towards gram negative bacteria as compared to
penicillin.
The Nordmark-Werke GmbH. also offer a new type of
sulfonamide. Sulfuno is 2-(p-aminobenzenesulfonamido)4,5-dimethyl-oxazole (VII); m.p. 193-194 OC.
N---C-CH,
H ~ N - ~ - S ~ ~ - N IIH - CI1
’ I=‘
I
v1
I
literature. It is injected intravenously or intramuscularly.
The neutral cyanocobalamin used up to now has the disadvantage of being eliminated relatively rapidly from the body.
The depotaction of the new preparation is supposed to be
due to a firmer tie with the negatively charged serum and tissue proteins and this results in delayed elimination.
mzer GmbH. markets in Germany a synthetically modified
penicillin designated as “Pen-200‘‘ whose main advantage is
that it can be administered orally (IV).
\=/
\of-c
H3
VII
Aside from its excellent tolerance the favorable midway
position of the drug between the short-term classic sulfonamides with rapid elimination and the repository sulfonamides with delayed resorption and excretion is stressed.
Because of accumulation in the gall bladder the preparation
is especially indicated for disorders of the gall bladder and
the bile duct of the liver.
With Primobolan and Primobolan-Depot, Schering AG put
an anabolic steroid for the enhancement of protein build-up
onto the market. 1-Methyl-A1-androstenolone acetate or
enanthate (VIII) exert a strong anabolic effect without having other undesirable hormonal properties.
VIII
The nitrogen balance becomes positive during therapy; an
additional 22 g. of protein per day are built up by the organism without increasing protein intake.
Farbwerke Hoechst introduced Delmeson a skin-specific
synthetic steroid. 21-Deoxy-6-methyl-9-fluoroprednisolone
@,
Angew. Chem. internat. Edit. 1 VoL 1 (1962)I No. 1
55
(IX) combined with the antibiotic neomycin is especially
suitable for the treatment of inflammatory and allergic
eczemas.
CH3
As a further development of the well-known carcinostatic
drug E 39 Farbenfabriken Bayer have contributed Trenimon to medicine. It consists of 2,3,5-tris(ethylene-imino)benzoquinone-(l,4) (XIII)
@
0
IX
CH3
Squibb recommends its new preparation Omca@ 4-(3-[2(trifluoromethyl) 10 phenothiazinyl] - propyl} -1- piperazineethanol dihydrochloride to influence the complicated vegetative dystonia. The drug is claimed not only to suppress the
peripheral symptoms but also the usually present central
focus in the brain.
A new type of diuretic is produced by C. F. Boehringer u.
Soehne GmbH., Mannheim. Aldactone@belongs to the class
of spironolactones and is 3’-(3-0~0-7a-acetylthio-l7~-hydroxy-A4-androsten-l7cr-yl)propionicacid y-lactone (X); m.p.
200 OC.; [a13 -34 in CHC13.
- -
r-,=
which crystallizes in small purple needles; m.p. 161.6 to
162.5OC.; somewhat soluble in water. The substance is
characterized by a very strong cytostatic effect and was used
successfully in extensive experiments in the treatment of
chronic leukemia, lymphogranulomatosis, and lymphosarcoma.
The attraction of psychopharmacologic agents has not
decreased in the pharmaceutical industry. This is demonstrated by the large number of new preparations. Taractan@
of Hoffmann-La Roche AG. and Truxal@of Troponwerke
have the trans-isomer of 2-chloro-9-(3’-dimethylaminopropy1idene)thiaxanthene (XIV) as active component.
0
‘CH3
XIV
This practically non-toxic substance is an antagonist of the
adrenal hormone aldosterone and inhibits the reabsorption of
sodium by the kidney which is governed by aldosterone. This
results in higher excretion of salt and water.
Chemische Werke Dr. R. Reiss contribute the non-barbiturate, short-term anesthetic Estil CB for intravenous administration. 2-Methoxy-4-allylphenoxyaceticacid N,N-diethylamide (XI) is a eugenol derivative.
/CHz--CH3
0 -CHz-C-N
I
lCHz-CH3
&-CH=CHz
XI
It is an almost odorless oil; b.p. 140-142°C./0.001 mm. Hg;
ng = 1.5300). Its 5 % aqueous solution is used for anesthesia.
Contrary to the usual short-term anesthetics the new preparation is characterized by a stimulation of the respiratory
activity and a short recovery time after anesthesia.
The active component of a chemotherapeutic agent of the
aromatic diamidine series is 4,4-(hexamethy1enedioxy)dibenzamidine bis(P-hydroxyethanesulfonate). It has been
introduced on the market by Upha GmbH. as Hexomedin@
and is to be used for the treatment of dermatological disorders caused by bacteria or fungi.
An oral medication for fungus infections of the skin, hair and
nails is offered by Imperial Chemical Industries, Ltd. The
active component of Fulcin is the antibiotic griseofulvin (XII)
Marplan@,another drug in this field by Hoffmann-La Roche,
(XV).
is l-benzyl-2-(5-methyl-3-isoxazolylcarbonyl)hydrazine
o= C--NH--NH-cH2--//N- :C
I
\=/’
1
HC\\/o
c;
I
CHI
xv
It is supposed to be effective against any kind of depression.
Tremaril@ of Dr. A. Wander GmbH. consists of 4-(1’methylpiperidyl-3’-methyl)thiaxanthenehydrochloride and is
recommended against Parkison’s disease.
Rohm and Haas GmbH. produce Jatroneural@which con10-[3-(l-methyl-4-piperazinyl)-propyl]-2-trifluorometains
thylphenothiazine dihydrochloride (XVI).
XVI
Masmoran of Roerig Pharmazeutika (Division of Pfizer
GmbH.) is the pamoate of l-(p-~hlorobenzhydry1)-4-[2-(2hydroxyethoxy)ethyl]diethylenediamine (XVII). A pamoate
is a salt with 2,2’-dihydroxy-l,l’-dinaphthylmethane-3,3’dicarboxylic acid (XVIII).
@
OCH3
I
Cl
XI1
which is obtained from the filtrates of cultures of Penicillium
Captagon
griseofulvum. The antimycotic. effect is attributed to an infiltration of the substance into the keratin layers.
7-[2’-(l”-methyl-2”-phenylethylamino)ethyl]theophylline hy-
56
@
of Chemiewerk Homburg which consists of
drochloride also belongs in this category.
Angew. Chem. internat. Edit. / Vol. I (1962) / No. 1
NH2
I
H
1
CHzOH
I
C
4
CHzNHz
H-C-
1
I?Hz
c-c’
I
XIX
1
NH2
CHaOH
1
OH
Indications for all these medications are fear, states of tension
and excitation, psychic and physical exhaustion, climatic
distress, etc. These are only a few of the recommendations.
Parke-Davis enlarges the therapeutic possibilities with a new
effective oral antibiotic. Humatin is paromomycin (XIX)
which is obtained from the culture filtrates of Streptomyces
rimosus forma paromomycinus. This active component consists of D-glucosamine, desoxystreptamine, D-ribose, and a
diaminohexose, which are linked together according to formula XIX.
The antibiotic is not resorbed from the intestine and has
well-defined bactericidal and amebicidal activity.
[VB 535/VB 1 IE]
German Society for Mineral Oil Science and Coal Chemistry
Goslar (Germany), September 27-29,
F r o m the papers:
Utilization of Hydrogen Cyanide from
Coke Oven Gas
W. Grimme and E. Ruschenburg, Homberg (Germany)
Through hydrogen sulfide wet-washing of coke oven gases,
gas concentrates (called “foul gases” or “choke damp”) are
obtained. These contain 70-80 % by VOI. H2S, 5-7 % by vol.
HCN, 10-15 % by vol. CO;! and about 5 % by vol. of other
coke oven gas components. The hydrogen cyanide contained
in such gases may be converted at normal pressures directly
and continuously, that is, without previous separation from
the other gases, to acetone cyanohydrin if the alkali, e.g.
KCN or KOH, which catalyzes the reaction between HCN
and acetone is introduced as a dilute aqueous solution into
the washing towers near the plate at which the acetone
contains the greatest amount of HCN. By maintaining a
water content in the acetone of at least 5 % by vol., the
dissolution of HzS and C02 in the acetone is minimized. This
in turn reduces the formation of, for example, KHCO3 or
KHS. Thus, only a small amount of alkali is needed and the
alkali remains catalytically active.
After the separation of excess acetone from the reaction
mixture at normal pressure, water is removed at reduced
pressure. The acetone cyanohydrin is then obtained by
rectification at reduced pressure in a purity which makes it
suitable for use in the preparation of methacrylic acid derivatives, e.g. methacrylic ester.
Because of the economic utilization of the hydrogen cyanide
in the foul gas, as much of the hydrogen cyanide as possible
can be transferred from the coke oven gas into the foul gas,
thus preventing the hazardous contamination of waste waters
and air with hydrocyanic acid. The process is already in use
in a commercial plant.
1961
The reaction rate is approximately proportional to the COpartial pressure; the apparent activation energy is 12 kcal/mole at 75 atm. and decreases to 7 kcal/mole at 200 atm. The
average molecular weight of the products increases with
pressure and decreases with increasing temperature. Up to
95 % of the CO used can be converted into condensed
products. As for gaseous hydrocarbons, only small amounts
of CH4 are formed.
Cold Hydrogenation of CpFractions in Liquid Phase
W. Kronig, Leverkusen (Germany)
Propylene, produced by pyrolysis, contains methylacetylene
and allene which are troublesome in further processing. The
removal of these impurities by selective gas-phase hydrogenation has disadvantages. A process has been worked out in
which the C3-fraction is selectively hydrogenated in large
quantities in the liquid phase (or, to be exact, in the trickle
phase) between 10 and 20 ‘C. over fixed, palladium-containing catalyst. The undesirable components are completely removed without any loss of propylene. This process, called
“cold hydrogenation”, has proven itself in a commercial
plant; after more than one year of operation, the activity of
the catalyst has not yet diminished. Cold hydrogenation may
also be used to advantage for other hydrocarbon fractions.
On the Allcenylation of Aromatics
K. E. Moller, Miilheim/Ruhr (Germany)
At 60 to 65 “C. benzene may be alkenylated with butadiene
in the presence of 95 % phosphoric acid giving approximately
a 60 % yield (based on butadiene) of an isomeric mixture of
phenylbutenes having the following composition :
Synthesis of High Melting Paraffins from Carbon
86.4 % tram- 1-phenylbutene-(2)
Monoxide a n d Water with Suspended Ruthenium
8.0 % cis-1-phenylbutene-(2)
H . Koibei, K. K. Bhattacharyya and W. Miiller,
Berlin (Germany)
When metallic ruthenium is suspended in water and carbon
monoxide is passed through the suspension at pressures above
50 atm. and temperatures between 150 and 26OoC., straight
chain paraffins having melting points up to 131 “C., corresponding to molecular weights of up to about 7000, are
formed according to the equation
3 CO
+ H z 0 + -CHz- + 2 CO, ( A H
=
-58.4 kcal/mole).
In this process, the water serves simultaneously as reactant,
suspension medium, heat transfer medium and direct cooling
medium.
Angew. Chem. internat. Edit. / Vol. I (1962) / No. I
5.5 ”/. 3-phenylb11tene-fl)
0.1 % 4-~henylbutene-(l)
The formation of these four isomers may be explained by 1,4and 1,2-addition of benzene to butadiene. Isomerization of
the hydrocarbons formed primarily, for example to l-phenylbutene-(I), does not take place under the reaction conditions.
The alkenylation of toluene or of the xylenes leads to the
corresponding 0-and p-substitution products.
In the conversion of styrene or a-methylstgrene, ring closure
occurs with the formation of a vinylindane system which is
variously substituted depending on the reaction partners
which include isoprene in addition to butadiene. For example,
57
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