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4333948 Pharmaceutical formulations containing prostaglandin
i
New Patents 4333944
/"-"~ IO~"~ \
/
R2
8-HALO-6-PHENYL-4H.S-TRIAZOLO (3,4-C) THIENO 1,4-DIAZEPIN.1-ONES
R~
4-Phenoxypiperidines of the general formula wherein R i denotes a hydrogen atom, an alkyl group with 1 to 5 carbon atoms, an alkenyl group with 3 to 5 carbon atoms, a cycloalkylmethyl group with 3 to 7 carbon atoms in the cycloalkyl part or a phenylalkyl group with 1 to 3 carbon atoms in the alkyl part, R2 denotes a hydrogen atom, a nitro group, an amino group or an acylamino group and R3 denotes a phenyl group or a benzyl group, and their N-oxides and their acid-addition salts are new compounds. They have an antiptotic and analgesic action and arc suitable lbr the treatment of depressions and painful conditions. Processes for the preparation of the new compounds arc provided.
K Weber, A Langbein, E Lchr, K Boke, F J Kuhn, Gaulgesheim, West Germany assigned to Boehringer Ingelheim GmbH
4333945
THIAZOLINE AND IMIDAZOLINE DERIVATIVES USEFUL AS MINOR TRANQUILIZERS E Ringwald, Riehen, Switzerland assigned to Sandoz Ltd This invention provides a new tranquillizing use of thiazoline and imidazoline derivatives and novel pharmaceutical compositions for such use.
4333946 4333943
BLOCKING HISTAMINE H2RECEPTORS WITH IMIDAZOLYLALKYL GUANIDINE DERIVATIVES
ETHYL 3-(3-1NDOLYL)-3.(5TETRAZOLYL) PROPIONATE COMPOUNDS USED AS ANTIHYPERTENSIVE AGENTS E Kurchacova, M E Safdy, assigned to Miles Laboratories lnc
N ~N I
J
N,~NH
G J Durant, C R Ganellin, G R Owen, R C Young, Welwyn Garden City, United Kingdom assigned to Smith Kline & French Laboratories Limited
0
CH--CH2--C--O--CH2CH
1
I
N H
Disclosed are novel ethyl 3-(3-indolyl)-3(5-tetrazolyl) propionate compounds characterized by the tbrmula wherein X is H or mcthoxy and Y is H, CI or methoxy. These compounds are useful as antihypertensive agents.
The compounds are novel N-substituted-N'heterocyclic alkylthioureas, guanidines and l-nitro-2,2-diaminoethylene compounds which are histamine H2-antagonists.
4333948
PHARMACEUTICAL FORMULATIONS CONTAINING PROSTAGLANDIN K U Weithmann. Eppstein, West Germany assigned to Hoechst Aktiengesellschaft
New Patents What are disclosed are: a substance, obtained from blood serum and having a molecular weight below 2000, which is suitable for stabilizing prostaglandins, especially those of the A, E, F, or I type; methods for preparing such a stabilizing substance from blood serum; pharmaceutical preparations containing a prostaglandin or prostaglandin derivative together with such a stabilizing substance; and methods for stabilizing a pharmaceutical preparation containing a prostaglandin or prostaglandin derivative.
vii bromo, amino or trifiuoromethyl; n is 0-3 and m is 0-2, and the pharmaceutically acceptable salts thereof. The compounds exhibit muscle relaxant activity, and are also useful as anti-inflammatory agents.
4333952 GROWTH PROMOTORS FOR RUMINANTS B G McDonald, Mosspark, United Kingdom assigned to Beecham Group Limited
4333951 2-AMINO-6-BIPHENYLACETIC ACIDS
RI-~X_Y_R
2
D A Walsh, assigned to A H Robins Company lnc
(R2)~l~ ~
Compounds of formula (I) wherein: RI is hydrogen, halogen or C1-4 alkoxy; X is oxygen; NR3 in which R3 is hydrogen, CI-4 alkyl, or -Y-R2; -C double bondO; or -CHOH; Y is -CH2-CHOH, and when X is
CH2COOR
(R'),.--~._ L V -NH2 Novel 2-amino-6-biphenylacetic acids, esters, and metal salts are provided of the formula wherein R represents hydrogen or lower alkyl, RI represents fluoro, chloro, bromo, lower-alkyl or amino; R2 represents lower-alkyl, lower-alkoxy, fluoro, chloro,
-C double bondO it may also be -CH double bondCH-; and R2 is C1-4 alkyl, one carbon atom of which is di- or tri-halogenated; or salts thereof, are useful in promoting growth of ruminants. Processes for their production, veterinary formulations and treatments are described.
For information about PATSEARCHTM and VIDEO PATSEARCHTM: Pergamon International Pergamon lnfoLine Pergamon Press Intbrmation Corporation Limited Canada Ltd 1340 Old Chain Bridge Road 12 Vandy Street McLean, Virginia 22101 lamdon EC2A 2DE USA England Telephone (703) 442-0900 Telephone: (01) 377 4650 Telex: 90-1811 Telex: 8814614 Patent Section Editors: Pergamon Press, Inc. Maxwell House Fairview Park Elmsford, New York 10523
150 Consumers Road Suite 104 Willowdale, Ontario Canada M2J I P9 Telephone: (416) 497-8337 Telex: 065-25460
Pergamon Press Ltd. Headington Hill Hall Oxford OX3 0BW England
New Patents 4333944
/"-"~ IO~"~ \
/
R2
8-HALO-6-PHENYL-4H.S-TRIAZOLO (3,4-C) THIENO 1,4-DIAZEPIN.1-ONES
R~
4-Phenoxypiperidines of the general formula wherein R i denotes a hydrogen atom, an alkyl group with 1 to 5 carbon atoms, an alkenyl group with 3 to 5 carbon atoms, a cycloalkylmethyl group with 3 to 7 carbon atoms in the cycloalkyl part or a phenylalkyl group with 1 to 3 carbon atoms in the alkyl part, R2 denotes a hydrogen atom, a nitro group, an amino group or an acylamino group and R3 denotes a phenyl group or a benzyl group, and their N-oxides and their acid-addition salts are new compounds. They have an antiptotic and analgesic action and arc suitable lbr the treatment of depressions and painful conditions. Processes for the preparation of the new compounds arc provided.
K Weber, A Langbein, E Lchr, K Boke, F J Kuhn, Gaulgesheim, West Germany assigned to Boehringer Ingelheim GmbH
4333945
THIAZOLINE AND IMIDAZOLINE DERIVATIVES USEFUL AS MINOR TRANQUILIZERS E Ringwald, Riehen, Switzerland assigned to Sandoz Ltd This invention provides a new tranquillizing use of thiazoline and imidazoline derivatives and novel pharmaceutical compositions for such use.
4333946 4333943
BLOCKING HISTAMINE H2RECEPTORS WITH IMIDAZOLYLALKYL GUANIDINE DERIVATIVES
ETHYL 3-(3-1NDOLYL)-3.(5TETRAZOLYL) PROPIONATE COMPOUNDS USED AS ANTIHYPERTENSIVE AGENTS E Kurchacova, M E Safdy, assigned to Miles Laboratories lnc
N ~N I
J
N,~NH
G J Durant, C R Ganellin, G R Owen, R C Young, Welwyn Garden City, United Kingdom assigned to Smith Kline & French Laboratories Limited
0
CH--CH2--C--O--CH2CH
1
I
N H
Disclosed are novel ethyl 3-(3-indolyl)-3(5-tetrazolyl) propionate compounds characterized by the tbrmula wherein X is H or mcthoxy and Y is H, CI or methoxy. These compounds are useful as antihypertensive agents.
The compounds are novel N-substituted-N'heterocyclic alkylthioureas, guanidines and l-nitro-2,2-diaminoethylene compounds which are histamine H2-antagonists.
4333948
PHARMACEUTICAL FORMULATIONS CONTAINING PROSTAGLANDIN K U Weithmann. Eppstein, West Germany assigned to Hoechst Aktiengesellschaft
New Patents What are disclosed are: a substance, obtained from blood serum and having a molecular weight below 2000, which is suitable for stabilizing prostaglandins, especially those of the A, E, F, or I type; methods for preparing such a stabilizing substance from blood serum; pharmaceutical preparations containing a prostaglandin or prostaglandin derivative together with such a stabilizing substance; and methods for stabilizing a pharmaceutical preparation containing a prostaglandin or prostaglandin derivative.
vii bromo, amino or trifiuoromethyl; n is 0-3 and m is 0-2, and the pharmaceutically acceptable salts thereof. The compounds exhibit muscle relaxant activity, and are also useful as anti-inflammatory agents.
4333952 GROWTH PROMOTORS FOR RUMINANTS B G McDonald, Mosspark, United Kingdom assigned to Beecham Group Limited
4333951 2-AMINO-6-BIPHENYLACETIC ACIDS
RI-~X_Y_R
2
D A Walsh, assigned to A H Robins Company lnc
(R2)~l~ ~
Compounds of formula (I) wherein: RI is hydrogen, halogen or C1-4 alkoxy; X is oxygen; NR3 in which R3 is hydrogen, CI-4 alkyl, or -Y-R2; -C double bondO; or -CHOH; Y is -CH2-CHOH, and when X is
CH2COOR
(R'),.--~._ L V -NH2 Novel 2-amino-6-biphenylacetic acids, esters, and metal salts are provided of the formula wherein R represents hydrogen or lower alkyl, RI represents fluoro, chloro, bromo, lower-alkyl or amino; R2 represents lower-alkyl, lower-alkoxy, fluoro, chloro,
-C double bondO it may also be -CH double bondCH-; and R2 is C1-4 alkyl, one carbon atom of which is di- or tri-halogenated; or salts thereof, are useful in promoting growth of ruminants. Processes for their production, veterinary formulations and treatments are described.
For information about PATSEARCHTM and VIDEO PATSEARCHTM: Pergamon International Pergamon lnfoLine Pergamon Press Intbrmation Corporation Limited Canada Ltd 1340 Old Chain Bridge Road 12 Vandy Street McLean, Virginia 22101 lamdon EC2A 2DE USA England Telephone (703) 442-0900 Telephone: (01) 377 4650 Telex: 90-1811 Telex: 8814614 Patent Section Editors: Pergamon Press, Inc. Maxwell House Fairview Park Elmsford, New York 10523
150 Consumers Road Suite 104 Willowdale, Ontario Canada M2J I P9 Telephone: (416) 497-8337 Telex: 065-25460
Pergamon Press Ltd. Headington Hill Hall Oxford OX3 0BW England