Gen. Pharmac. Vol. 17, No. 3, p p . i - v i i i , 1986 Pergamon Press Ltd. Printed in Great Br i ta in

NEW PATENTS

This Section contains abstracts and, where appropriate, illustrations of recently issued United States patents and published patent applications filed from over 30 countries under the Patent Cooperation Treaty. This information was obtained from recent additions to the Pergamon PATSEARCH" online database in accordance with interest profiles developed by the Editors. Further information about Pergamon PATSEARCH" can be obtained from Pergamon InfoLine Inc., 1340 Old Chain Bridge Road, McLean, Virginia 22101 U.S.A.

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4551132 ." R' ~c,,.:,.~-v "~ \

P H A R M A C E U T I C A L L Y ~ /x ACCEPTABLE SILICON RUBBER .if-c.=N--N A N--~C,,..:,,.I A N D T H E R A P E U T I C A L SET A N D

THE USE THEREOF FOR .'" ~-' ."R~ SURGICAL E M B O L I Z A T I O N

Emi Pasztor, Laszlo Nagy Jozsef Lazar, nee Becker Katalin Pallosy, Budapest, Hungary

A silicon rubber embolization agent used in general as well as cerebral vascular surgery having a component A which is composed of: a linear, low viscosity polysiloxane selected from the group consisting of dialkyl, alkylaryl, alkenylalkyl, and diarylpolysiloxanes having reactive functional groups selected from the group consisting of hydroxyl, acyloxyl, alkoxyl and amino; a low viscosity cyclic dia- lkylpolysiloxane having the formula (R2SiO)4, wherein R is alkyl; a pharmaceutically ac- ceptable iodo-containing organosilicium; or a non-metallic, organic X-ray contrast material, and a component B which is a therapeutically ac- ceptable cross-linking catalyst.

4551450

RIFAMYCIN H Y D R A Z O N E S , P H A R M A C E U T I C A L

C O M P O S I T I O N S C O N T A I N I N G T H E M AND THEIR USE

Peter Traxler, Sch Switzerlana assigned to Ciba- Geigy Corporation

CIt)CO C|l.l CII~ CH3

¢'.,o. I ° l ° ~ ' c . ~ 1t3 INH

I 'L' "T Y 0 C CO 0

I [Ri f S] CH3

c.~co oH3 c.3 cm

c.,o,

1t3C [NH

i 5' ' Y T O ~ C ..... CO OH

[ [Rif SV 1 C t h

Novel hydrazones derived from 3- formylrifamycin S or SV as the aldehydo compo- nent and a bi- or tri-cyclic N-aminopiperazine as the hydrazino component and having the for- mula See Patent for Chemical Structure (I) in which R1, R2, R3, R4, R5 and R6, indepen- dently of one another, each represents a hydro-

ii N e w P a t e n t s

gen atom or C1-4-alkyl, m and n, independently of one another, each represents an integer from 0 to 5, X represents C1-5-alkylidene, benzylidene or C1-4-alkoxymethylene, Y represents C1-5- alkylidene, C1-4-alkoxymethylene, oxy, thio or optionally substituted imino of the formula - N(R)- wherein R represents hydrogen, C1-4- alkyl, C3-5-alkenyl, C3-12-cycloalkyl or phenyl, or X and Y together represent 1,2-cycloalkylene or o-phenylene each of which can be substituted by from one to three C1-4-alkyl radicals, and Rif represents a radical of rifamycin S or SV that is bonded in the 3-position by the free valency, are distinguished by a high and long-lasting anti- tuberculotic activity. They are manufactured in conventional manner, for example by condensa- tion of their components.

4551462

EBURNANE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL

COMPOSITIONS CONTAINING THEM

Csaba Szantay, SzaboLajos , Gyorgy Kalaus, Janos Sapi, Eva Palosi, Bel Kiss, Elemer Ezer, Gyorgy Hajos, Budapest, Hungary assigned to Richter Gedeon Vegyeszeti Gyar Rt

tl N

( I ) .

can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the invention.

4551465

PIPERIDINE DERIVATIVES AND PHARMACEUTICAL

COMPOSITIONS CONTAINING THEM

Edit Toth, Jozsef Torley, Eva Palosi, Szabolcs Szeberenyi, Laszlo Szporny, Sandor Gorog, Ist- van Hajdu, Budapest, Hungary assigned to Richter Gedeon Vegyeszeti Gyar Rt

Ri

The invention relates to new piperidine derivatives of the formula (I) See Patent for Chemical Structure (I) wherein R1 is halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms; and R2 is hydrogen or alkyl having from one to 4 carbon atoms, and acid addition and quaternary ammonium salts thereof. According to another aspect of the invention there are pro- vided processes for the preparation of these com- pounds. The compounds of the formula (I) are pharmacologically active. In particular, they in- hibit the microsomal monooxigenase enzyme system of the liver. Pharmaceutical composi- tions containing them as active ingredient are also within the scope of the invention.

4551468

The invention relates to racemic or optically ac- tive eburnane derivatives of the formula (I), See Patent for Chemical Structure (I) wherein R represents an alkyl group having 1 to 6 carbon atoms, A stands for hydroxyl and Y is hydrogen, or A and Y together form an oxo group, and the configuration of the hydrogen in the 3-position and of R is alpha, alpha and/or beta, beta or al- pha, beta and/or beta, alpha, and acid addition salts thereof. The new compounds possess valuable pharmaceutical properties, thus their certain representatives show antiallergic activity, while others are potent antidepressive, gastric secretion inhibiting and anticonvulsive agents. The compounds of the formula (I) and pharma- ceutically acceptable acid addition salts thereof

HETEROCYCLIC THROMBOXANE SYNTHETASE

INHIBITORS AND PHARMACEUTICAL

COMPOSITIONS CONTAINING THEM

Peter E Cross, Roger P Dickinson, Geoffrey N Thomas, Canterbury, United Kingdom assigned to Pfizer Inc

R i

R Y

(I)