Abstract: A process is described for the preparation of a compound of formula (IX) from 4-hydroxybutyl 3-pyridyl ketone. The compound of formula (IX) is an intermediate useful in the preparation of (1R,2R)-2-(3-pyridyl)-N-alkyl-tetrahydro-2H-thiopyran-2-carbothioamide 1-oxides which possess useful pharmaceutical properties, for example anti-hypertensive properties.

Abstract: An improved method for producing natamycin by fermentation is disclosed.

Abstract: The present invention relates to a method of enzymatic polymerization and/or modification of lignin or lignin containing materials. The invention also relates to the use of this method in the manufacture of wood composites or wood laminates.

Abstract: A brandykinin antagonist of the formula:X(BKA).sub.nwherein BKA is the peptide chain of a bradykinin antagonist peptide, X is a linking group and n is a whole number greater than 1. The BKA substituents may be the same or different. Monomeric antagonists of the formula X(BKA) are also disclosed. Also disclosed are bradykinin antagonists of the formula:(Y)(X)(BKA)where X and BKA have the meanings indicated above and Y is the peptide chain of an antagonist or agonist for a non-bradykinin receptor.

Abstract: A bradykinin antagonist of the formula:X(BKA).sub.nwherein BKA is the peptide chain of a bradykinin antagonist peptide, X is a linking group and n is a whole number greater than 1. The BKA substituents may be the same or different. Monomeric antagonists of the formula X(BKA) are also disclosed. Also disclosed are bradykinin antagonists of the formula:(Y)(X)(BKA)where X and BKA have the meanings indicated above and Y is the peptide chain of an antagonist or agonist for a non-bradykinin receptor.

Abstract: Biotransformation products of a fermentation with culture MA7074 are potent HIV protease inhibitors. These products are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: The invention relates to compounds of the following general formula I ##STR1## especially the compound of formula Ia referred to as thiangazole ##STR2## their pharmaceutically acceptable acid addition salts, processes for their preparation and therapeutic compositions and compositions that can be used in crop-protection.

Abstract: The present invention provides a heterodimeric compound possessing bradykinin and neurokinin receptor antagonist activities useful in the treatment of asthma and other inflammatory diseases especially those involving the airway or pulmonary system. The present invention is also useful in the treatment of pain and inflammation.

Abstract: A compound of formula (I) is obtainable by the cultivation of a microorganism from the genus Streptomyces, such as Streptomyces NCIMB 40515. In the presence of rapamycin, and recovery thereof from the culture medium. The compound, and pharmaceutical compositions containing it, is useful as an immunomodulatory agent, as an anticancer agent, or in the treatment of microbial infections in animals including humans.

Abstract: The present invention is directed to a process for producing frenolicin B. The process comprises fermenting a broth so as to produce frenolicin, said broth having a microorganism capable of producing frenolicin. The frenolicin is then converted in the broth under anaerobic conditions to deoxyfrenolicin. The deoxyfrenolicin is converted to frenolicin B.

Abstract: The compound of formula (I) is useful as an antifungal and immunosuppressive agent.

Abstract: A compound of formula ##STR1## in which X is hydrogen or a group of formula --SO.sub.2 NH.sub.2 is reduced to the trans (4S,6S) form of the corresponding alcohol by an enzyme reduction system.

Abstract: The present invention concerns a process for the production of pilocarpine, in which root formation is induced from part of a plant of the genus Pilocarpus, the said roots are cultivated in vitro in a culture medium and pilocarpine is isolated from the roots and/or the medium.

Abstract: A novel process comprises reducing a benzazepine or benzothiazepine at the 3-position in d-cis configuration by treatment with reductase-supplying microorganisms or enzymes derived therefrom. The process can be catalyzed in a single stage by growing microbial cultures or in a two-stage fermentation/transformation by resting cell-suspensions. The enzymes derived from the microorganisms can be used in free state or immobilized form. The microorganisms and enzymes catalyzes the specific reduction with 90 to 99% conversion efficiency to 99% or greater optical purity of the desired enantiomer.

Abstract: The active component of the pharmaceutical composition of the present invention is a compound which has been isolated from the controlled aerobic fermentation of a marine microorganism, Agrobacterium sp. PH-103. The pharmaceutical compositions of the present invention, useful for post surgical graft tolerance, are thus directed to compositions comprising a pharmaceutically acceptable carrier, diluent or excipient, and an effective amount of the compound having the formula: ##STR1## This compound, known as Sesbanimide, is an alkaloid that has been previously been isolated from seeds and reported to be useful as an antitumor drug. Prior to the present invention however, this compound had not been isolated from any fermentation broth nor had it been determined to have immunomodulatory activity.

Abstract: A DNA fragment containing a caffeine demethylase gene produced by a microorganism belonging to the genus Pseudomonas and capable of assimilating caffeine and a process for producing a 3-methyl-7-alkylxanthine comprising cultivating a novel bacterium strain of the genus Pseudomonas having been transformed with a recombinant DNA having integrated therein the above-mentioned DNA fragment in a nutrient culture medium containing a 1,3-dimethyl-7-alkylxanthine to produce a 3-methyl-7-alkylxanthine in the culture and recovering the produced 3-methyl-7-alkylxanthine from the culture are disclosed, as well as a process for producing 3-methyl-7-propylxanthine, comprising cultivating a microorganism capable of converting 1,3-dimethyl-7-propylxanthine to 3-methyl-7-propylxanthine or a mutant thereof in a nutrient culture medium containing 1,3-dimethyl-7-propylxanthine, to produce 3-methyl-7-propylxanthine in the culture and recovering the produced 3-methyl-7-propylxanthine from the culture.

Abstract: An enzymatic process employing pancreatin or choelsterol esterase for resolution of racemates of 4-aryl-2-oxo-pyrrolidine-3-carboxylic acid esters of general formula I ##STR1## in which X represents a carbon-carbon bond or an oxygen atom,R.sub.1 means a hydrocarbon radical optionally substituted by hydroxy groups, oxo groups and/or halogen atoms and/or interrupted by nitrogen atoms with at most 16 carbon atoms,R.sub.2 symbolizes an alkyl group with up to 4 carbon atoms andR.sub.3 represents an alkyl group with at most 6 carbon atoms is described.

Abstract: A biotransformation process for the production of an intermediate used in the chemical synthesis of an antibiotic compound.

Abstract: Granules containing salinomycin are prepared that are free-flowing, dust-free, and have unrestricted bioavailability of salinomycin. The granules are produced by fermenting a culture broth with a salinomycin producing microorganism to a residual fat content of about 24 to 30% by dry weight broth, adding to the fermented broth a cellulose ether and an anticaking agent, and spray drying the broth while adding a flow auxiliary to produce granules containing 10 to 26% by weight salinomycin. The granules also contain, based on the weight of the broth being fermented, 30 to 40% anticaking agent and flow auxiliary in a ratio of 3:1 to 9:1 and 0.5 to 2% cellulose ether. The anticaking agent is preferably a calcium carbonate such as chalk or a silica of natural origin such as diatomaceous earth, talc, or kaolin. The flow auxiliary is preferably a synthetic or precipitated silica.

Abstract: This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases, infectious diseases, and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to a use thereof.

Abstract: There is disclosed a process for preparing indigo which comprises bringing an indigo-producing bacteria belonging to genus Acinetobacter or treated products thereof into contact with an aqueous solution containing at least indole to have indigo formed and accumulated in the aqueous solution; and collecting indigo from the aqueous solution.

Abstract: A compound of the formula ##STR1## is a novel immunosuppressant agent prepared by fermenting Steptomyces braeaensis subsp. pulcherrimus, ATCC 55150, or another compound of the formula I producing strain and extracting the compound of the formula I from the fermentation medium. The compound is useful in treating transplant rejection and autoimmune diseases.

Abstract: The present invention provides a process for the stereoselective reduction of phenylalkyl ketones to their corresponding (S)-hydroxy compounds. The process utilizes the novel microorganism Microbacterium MB 5614 to effectuate the chiral reduction. The present invention also provides said novel Microbacterium, which has been deposited with the ATCC and assigned the accession number ATCC 55557.

Abstract: The invention concerns a method for the colorimetric determination of an analyte by means of enzymatic oxidation with a PQQ-dependent dehydrogenase in the presence of an electron acceptor from the group of the electron-rich aromatic nitroso compounds by enzymatic reduction of the nitroso compound to an imino compound and detection of the imino compound by color formation. In addition the invention concerns a corresponding agent containing a PQQ-dependent dehydrogenase, an electon-rich aromatic nitroso compound as well as, if desired, a detection reagent for imino compounds. The invention in addition concerns novel nitrosoamino compounds which form colored quinone diimines on reduction as well as their use for the colorimetric enzymatic determination of an analyte.

Abstract: There is disclosed a novel microbial bioconversion process for the synthesis of a trans-hydroxy sulfone intermediate, which is the precursor to topical carbonic anhydrase inhibitors (TCAI's). TCAI's are effective in the treatment of glaucoma and ocular hypertension. The bioconversion process is carried out in the presence of the microorganism Rhodotorula rubra, or Rhodotorula piliminae and results in a trans-hydroxy sulfone which exhibits a diastereomeric excess of greater than 95%.

Abstract: The present invention provides a process for producing oxazopyrroloquinolines which comprises culturing microorganisms to produce pyrroloquinolinequinone and adding .alpha.-amino acids or monomethylamine to the resulting culture broth which contains the pyrroloquinolinequinone and from which cells of microorganisms are not separated, thereby to convert the pyrroloquinolinequinone to the corresponding oxazopyrroloquinolines. The thus obtained oxazopyrroloquinolines include novel compounds. The present invention further provides aldose reductase inhibitors, diabetic combined disease curing agents, immunopotentiating agents and liver disease inhibiting agents which contain as active ingredient these oxazopyrroloquinolines having excellent physiological activity.

Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 55080. This novel antibiotic is useful as an anticoccidial in poultry, in the prevention and treatment of swine dysentery and as a growth promotant in cattle and swine.

Abstract: A new FR901451 substance which is produced by culturing a FR901451 substance-producing strain of the genus Flexibacter in a nutrient medium, this new substance possessing a human leukocyte elastase-inhibiting activity.

Abstract: The present invention relates to a novel antibacterial compound obtainable from the genus Alteromonas and which shares structural similarity with the pseudomonic acids.

Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 53764. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, and as a growth promotant in cattle and swine.

Abstract: A process is described for selectively preparing a compound of the formula ##STR1## wherein: R.sup.1 is halogen;R.sup.2 is halogen, alkyl, cycloalkyl, aryl or ##STR2## and R.sup.3 hydrogen, alkyl, cycloalkyl, aryl, ##STR3## wherein the process comprises treating the associated ketone with an oxido-reductase or a microorganism comprising an oxidoreductase. Compounds prepared by this process are useful antipsychotic agents or useful intermediates therefor.

Abstract: Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation product the compound 3-[2-(benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2-(1H)-pyridinone . This product is useful in the prevention or treatment of infection by HIV and the treatment of AIDS.

Abstract: Novel macrocyclic lactone antibacterials isolated from a culture containing the microorganism S. aerocolongenes sub sp. antibiotica SCC 1886, ATTC 55003 and their use for treating and/or preventing antibacterial infections, especially Chlamydia infections are disclosed.

Abstract: A microorganism for selective production of a specific compound of avermectin having one or more of the following properties:specific accumulation of avermectin compound "a",effective incorporation of isoleucine or its keto acid (3-methyl-2-oxovaleric acid) into avermectin molecule, andmarkedly suppressed incorporation of valine or its keto acid (2-oxoisovaleric acid) into avermectin molecule.

Abstract: Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation products the 5-(1-hydroxy)ethyl pyridinone analog as well as the 5-(1-hydroxy)ethyl pyridyl and the 5-(2-hydroxy)ethyl pyridyl derivatives.

Abstract: Pyrrolo-quinoline quinone (PQQ) is microbiologically produced by culturing a bacterium in a medium containing methanol, methylamine or a mixture thereof as a carbon source and recovering PQQ from the culture medium. The bacteria are strains of Methylobacterium, Ancylobacter, Hyphomicrobium, Xanthobacter, Thiobacillus, Microcyclus and Achromobacter.

Abstract: Several classes of water immiscible lipophilic phases effect the transfer of crystalline orange precursor pigments produced by Monascus species in an aqueous culture medium from the aqueous to the lipophilic phase without solubilizing a major portion of the pigment. Liquid vegetable and mineral oils are two such classes. This phenomenon permits high recovery of pigment in a simple and convenient manner, and also permits development of a batch recycle and a continuous fermentation process for pigment production.

Abstract: Described is a process for producing an immunosuppressant, "demethimmunomycin" (L-683,7411) a C-31 demethylated analog of L-683,590 under fermentation conditions utilizing the microorganism, Actinoplanacete sp, (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Abstract: A novel antitumor substance BE-13793C or a pharmaceutically acceptable salt thereof, which is represented by the following formula: ##STR1## an anticancer agent comprising the novel substance or a pharmaceutically acceptable salt thereof, a method of producing the novel substance and a microorganism Streptoverticillium FERM P-10489, capable of producing the novel substance are disclosed.

Abstract: Improved processes for producing a polyether antibiotic compound represented by A82810 comprising: (1) cultivating Actinomadura fibrosa sp. nov. NRRL 18348 or Actinomadura sp. NRRL 18880, (2) feeding acid hydrolyzed casein at a rate from about 2.50-7.50 gm/L/day, (3) feeding glucose at a rate from about 2.50-7.50 gm/L/day, and (4) feeding propionate at a rate from about 0.50-1.5 gm/L/day to the appropriate culture medium during fermentation, are provided.

Abstract: Described is a new process for producing the immunosuppressant, L-683,742, a C-31 demethylated, derivative of L-683,590 (FK-520), produced under fermentation conditions utilizing the new mutant microorganism, Streptomyces hygroscopicus subsp. ascomyceticus (Merck Culture Collection MA 6646) ATCC No. 53855, being a blocked mutant of Streptomyces hygroscopicus subsp. ascomyceticus (MA 6475) ATCC No. 14891. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Abstract: Described is a process for producing a new immunosuppressant, L-682,992, a C-13, C-31 demethylated ring-rearranged analog of L-679,934, under novel fermentation conditions utilizing the microorganism, Actinoplanacete Sp., (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Abstract: Synthesis of semi-synthetic monobactamic or .beta.-Lactamic antibiotics by using derivatives stabilized by various methods of penicillin G acylase from various microbial sources according to a thermodynamically controlled strategy in monophase water/cosolvent organic apolar systems, wherein the concentration of the cosolvent varies between 30% and 90%, the temperature between -10.degree. C. and 50.degree. C., the pH between 4.5 and 8.5, with concentrations of the antibiotic nucleus between 0.5 an 875 mM and acyl donor between 0.2 mM and 1M, with a relationship antibiotic ring/activated or free acyl donor, using a buffer between 0 and 1M. Application to the pharmaceutical industry.

Abstract: The present invention concerns a novel process for the microbiological manufacture of L-ascorbic acid from L-gulono-gamma-lactone, a process for preparing the enzyme being responsible for the microbiological oxidation of L-gulono-gamma-lactone, and said enzyme as a homogeneous protein, which is a L-gulono-gamma-lactone dehydrogenase.

Abstract: New polyether antibiotic A80789, its acyl ester, alkyl ester, and alkyl ether derivatives, and salts thereof, are useful as antibacterial and anticoccidial agents and increase feed-utilization efficiency in animals. Methods of making A80789 by culture of Streptomyces hygroscopicus NRRL 18513, and combinations of the A80789 compounds with nicarbazin, 4,4'-dinitrocarbanilide, certain napthalenamine and benzenamine compounds and are also provided.

Abstract: A microbiological process for the oxidation of methyl groups in aromatic 5- or 6-member ring heterocycles to the corresponding carboxylic acid. The heterocycle serves as the substrate and exhibits no substituent on the carbon atoms adjacent to the methyl groups to be oxidized. The reaction of the heterocycle takes place by means of microorganisms of the genus Pseudomonas utilizing toluene, xylene, or cymene. The enzymes of the microorganisms been previously induced.

Abstract: A natamycin producing Streptomyces species ferments to produce natamycin. A spore suspension of the Streptomyces species is propagated in a predetermined medium to obtain a quantity of Streptomyces cells. The Streptomyces cells ferment in a predetermined production medium having a controlled pH to produce a recoverable amount of natamycin.

Abstract: Described is a process for producing a new FK-506 antagonist agent, a C-21 hydroxylated analog of FR-900520 under novel fermentation conditions utilizing the novel microorganism, Streptomyces hygroscopicus (Merck Culture Collection MA 6832) ATCC No. 55166. The macrolide antagonist is useful in preventing and/or counteracting accidental or inadvertent FK-506 overdosage in an FK-506 therapeutic program designed to prevent autoimmune diseases or human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

Abstract: Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6963) ATCC No. 55230. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

Abstract: A novel antitumor substance BE-13793C or a pharmaceutically acceptable salt thereof, which is represented by the following formula: ##STR1## an anticancer agent comprising the novel substance or a pharmaceutically acceptable salt thereof, a method of producing the novel substance and a microorganism capable of producing the novel substance are disclosed.