4388300 clavulanic acid derivatives, a process for their preparation and their use in pharmaceutical...

1
New Patents xi See Patent for Chemical Structure wherein R1 is selected from heterocyclic aromatic and hydro- phobic naturally occuring and modified amino acids in the D- and in the L-form, and from pep- tides, wherein n is an integer of from 1 to 5 and R2 is selected from unsubstituted and sub- stituted phenyl rings, and from heterocyclic rings, as well as to pharmaceutical compositions for preventing sickling of erythrocytes during sickle cell crisis and for desickling of sickle cells of patients afflicted by sickle cell disease, the ac- tive ingredient of which is a compound as defined above. R3 C02H The compounds of the formula (II): See Patent for Chemical Structure (II) wherein R3 and R4 are as defined in relation to formula (I) and R7 is a nitro, cyano, amino or aminomethyl group, are antibacterial agents and beta-lactamase inh- ibitors. Their use and a process for their prepara- tion are described. 4389406 META-PYRAZOLYLAMINO-TETR- AMISOLE ANALOGS AND THEIR USE IN PHARMACEUTICAL COMPOSITIONS Roderick J Dorgan, Richard A Webster, Out- wood, United Kingdom assigned to Beecham Group Limited N N'J"- I, s Compounds of formula (I) in the 1-form See Patentfor Chemical Structure (I) wherein R 1 and R2 are the same or different and each is selected from hydrogen, optionally substituted (C1-7) alkyl, optionally substituted aryl and aromatic heterocyclyl and the dotted line is an optional direct bond, and acid addition salts thereof, are useful in treating worm infections in mammals. Compounds (I) are produced by forming the amide of m-aminotetramisole or by closing the dihydroimidazoline ring. 4388300 CLAVULANIC ACID DER- IVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR USE IN PHARMA- CEUTICAL COMPOSITIONS John B Harbridge, Coulsdon, United Kingdom assigned to Beecham Group Limited 4387102 4-(N-(3', 4'-METHYLENEDIOXY- BENZYLIDENE) -AMINOMETHYL )CYCLOHEXANE-1-CARBOXYLIC ACID AND DERIVATIVES THEREOF AND PHARMA- CEUTICAL COMPOSITION THEREOF Hitoshi Takita, Sakuo Noda, Yutaka Mukaida, Hidetoshi Kobayashi, Tokyo, Japan assigned to Kureha Kagaku Kogyo Kabushiki Kaisha A novel compound of 4-(N-(3',4'-methylen- edioxybenzylidene) aminomethyl) cyclohexane-l-carboxylic acid or a pharma- ceutically acceptable salt or an C1-C4 alkyl ester thereof which has specific pharmacologic act- ivities, a method for preparing thereof and a pharmaceutical composition comprising thereof as an active ingredient are provided. 4387104 N-SUBSTITUTED PYRUVIC ACID HYDRAZONES, PREPARATION THEREOF AND PHARMA- CEUTICAL COMPOSITIONS CONTAINING THEM Ruth Heerdt, Hans P Wolff, Fritz Kaiser, Wolf- gang Schaumann, Hans Kuhnle, Mannheim, Federal Republic Of Germany assigned to Boehringer Mannheim GmbH CH3 / R~B~A~NH~Nm~ C \ COOH

Upload: vankien

Post on 31-Dec-2016

218 views

Category:

Documents


2 download

TRANSCRIPT

Page 1: 4388300 Clavulanic acid derivatives, a process for their preparation and their use in pharmaceutical compositions

New Patents xi

See Patent for Chemical Structure wherein R1 is selected from heterocyclic aromatic and hydro- phobic naturally occuring and modified amino acids in the D- and in the L-form, and from pep- tides, wherein n is an integer of from 1 to 5 and R2 is selected from unsubstituted and sub- stituted phenyl rings, and from heterocyclic rings, as well as to pharmaceutical compositions for preventing sickling of erythrocytes during sickle cell crisis and for desickling of sickle cells of patients afflicted by sickle cell disease, the ac- tive ingredient of which is a compound as defined above.

R3

C02H

The compounds of the formula (II): See Patent for Chemical Structure (II) wherein R3 and R4 are as defined in relation to formula (I) and R7 is a nitro, cyano, amino or aminomethyl group, are antibacterial agents and beta-lactamase inh- ibitors. Their use and a process for their prepara- tion are described.

4389406

META-PYRAZOLYLAMINO-TETR- AMISOLE ANALOGS AND THEIR

USE IN PHARMACEUTICAL COMPOSITIONS

Roderick J Dorgan, Richard A Webster, Out- wood, United Kingdom assigned to Beecham Group Limited

N N'J"- I, s

Compounds of formula (I) in the 1-form See Patent for Chemical Structure (I) wherein R 1 and R2 are the same or different and each is selected from hydrogen, optionally substituted (C1-7) alkyl, optionally substituted aryl and aromatic heterocyclyl and the dotted line is an optional direct bond, and acid addition salts thereof, are useful in treating worm infections in mammals. Compounds (I) are produced by forming the amide of m-aminotetramisole or by closing the dihydroimidazoline ring.

4388300

CLAVULANIC ACID DER- IVATIVES, A PROCESS FOR THEIR PREPARATION AND

THEIR USE IN PHARMA- CEUTICAL COMPOSITIONS

John B Harbridge, Coulsdon, United Kingdom assigned to Beecham Group Limited

4387102

4-(N-(3', 4'-METHYLENEDIOXY- BENZYLIDENE) -AMINOMETHYL )CYCLOHEXANE-1-CARBOXYLIC

ACID AND DERIVATIVES THEREOF AND PHARMA- CEUTICAL COMPOSITION

THEREOF

Hitoshi Takita, Sakuo Noda, Yutaka Mukaida, Hidetoshi Kobayashi, Tokyo, Japan assigned to Kureha Kagaku Kogyo Kabushiki Kaisha

A novel compound of 4-(N-(3',4'-methylen- edioxybenzylidene) aminomethyl) cyclohexane-l-carboxylic acid or a pharma- ceutically acceptable salt or an C1-C4 alkyl ester thereof which has specific pharmacologic act- ivities, a method for preparing thereof and a pharmaceutical composition comprising thereof as an active ingredient are provided.

4387104

N-SUBSTITUTED PYRUVIC ACID HYDRAZONES, PREPARATION

THEREOF AND PHARMA- CEUTICAL COMPOSITIONS

CONTAINING THEM

Ruth Heerdt, Hans P Wolff, Fritz Kaiser, Wolf- gang Schaumann, Hans Kuhnle, Mannheim, Federal Republic Of Germany assigned to Boehringer Mannheim GmbH

CH3 / R ~ B ~ A ~ N H ~ N m ~ C

\ COOH