Hoffmann-la Roche Inc.

Chao-Min Liu

John Westley

Homer D Tresner

Barbara Prosser

Norberto J Palleroni

Theron Hermann

There is presented antibiotic compounds designated as Antibiotics X-14889 A, C and D of the formulas ##STR1## wherein (for X-14889A) R.sub.1 is methyl, R.sub.2 is methyl, R.sub.3 is hydrogen, R.sub.4 is methyl and R.sub.5 is hydrogen or (for X-14889C) R.sub.1 is hydrogen, R.sub.2 is methyl, R.sub.3 is hydrogen, R.sub.4 is methyl and R.sub.5 is CO.sub.2 H or ##STR2## and the pharmaceutically acceptable salts thereof. The compounds exhibit antimicrobial activity and one of the compounds X-14889C also exhibits activity against Treponema hyodysenteriae (in vitro), Plasmodium berghei and as food efficiency enhancers in ruminants. Also presented is a process to produce the above compounds and another known component Antibiotic X-14889B.

Antibiotics X-14889 A,C and D

There are provided antibiotics X-14873 A, G and H of the formulas ##STR1## wherein for X-14873A, R.sub.1 is CO.sub.2 H and R.sub.2 is ##STR2## for X-14873G, R.sub.1 is hydrogen and R.sub.2 is ##STR3## and for X-14873H, R.sub.1 is hydrogen and R.sub.2 is ##STR4## The compounds exhibit antibiotic activity. Also disclosed is a process to produce the above compounds.

Process to produce antibiotics X-14873 A, G and H

The present invention relates to a novel polyether ionophore antibiotic of the formula ##STR1## and its pharmaceutically acceptable salts. The compound of formula I and its salts exhibit activity as an antibacterial agent and as an anticoccidial agent.

Antibiotic X-14934A and a method for its preparation

Treatment of coccidiosis with antibiotic X-14934A

Antibiotics X-14889 A, C and D

The present invention relates to a novel polyether ionophore antibiotic of the formula ##STR1## and its pharmaceutically acceptable salts . . . The compound of formula I and its salts exhibit activity as an antibacterial agent and as an anticoccidial agent.

Antibiotic X-14934A

There is presented an antibiotic compound of the formula ##STR1## and the pharmaceutically acceptable salts and esters thereof. The compound exhibits activity as an anti-swine dysentery agent and an antimicrobial agent. Also presented is a fermentation process to produce the compound of formula I.

Process to produce antibiotic X-14885A

Antibiotics X-14873 A, G and H

Antibiotic X-14868A having the following chemical structure ##STR1## and the pharmaceutically acceptable salts thereof is presented. Also presented is a fermentative method of producing the above antibiotic. Antibiotic X-14868A exhibits anticoccidiostatic activity.

Culturing a strain of nocardia to produce antibiotic X-14868A

Antibiotic X-14885A

Monensin urethane derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen, wherein R.sub.4 is alkyl, aryl, alkylaryl, arylalkyl, haloaryl, nitroaryl, haloarylalkyl, alkoxyaryl, aryloxyaryl, arylcycloalkyl, acylaryl and cycloalkyl; R.sub.2 is methyl or ethyl and R.sub.3 is-CONHR.sub.4 and their pharmaceutically acceptable salts. The compounds exhibit antimicrobial activity and activity as growth promotant agents in ruminants. Further activities for this series of compounds are anticoccidial activity, antihypertensive activity, antimalarial activity and as agents in the treatment of swine dysentery. Also disclosed are a fermentative process and a semisynthetic process for producing the urethane derivatives.

Monensin urethane derivatives produced by streptomyces

A compound of the formula ##STR1## and its pharmaceutically acceptable salts are disclosed. The compound exhibits antibacterial activity, antimalarial activity, has activity as a growth promotant for ruminants and as an agent in the treatment of swine dysentery. Also provided is a process to produce the novel compound.

Process of producing antibiotic X-14766A by a streptomyces

Antibiotic X-14868A, B, C and D

Monensin urethane derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen, wherein R.sub.4 is alkyl, aryl, alkylaryl, arylalkyl, haloaryl, nitroaryl, haloarylalkyl, alkoxyaryl, aryloxyaryl, arylcycloalkyl, acylaryl and cycloalkyl; R.sub.2 is methyl or ethyl and R.sub.3 is --CONHR.sub.4 and their pharmaceutically acceptable salts. The compounds exhibit antimicrobial activity and activity as growth promotant agents in ruminants. Further activities for this series of compounds are anticoccidial activity, antihypertensive activity, antimalarial activity and as agents in the treatment of swine dysentery. Also disclosed are a fermentative process and a semisynthetic process for producing the urethane derivatives.

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Cedar Grove, NJ, United States of America

Chao-Min Liu