Abstract: A process for the preparation of five-membered or six-membered ring lactams from aliphatic .alpha.,.omega.-dinitriles has been developed. In the process an aliphatic .alpha.,.omega.-dinitrile is first converted to an ammonium salt of an .omega.-nitrilecarboxylic acid in aqueous solution using a catalyst having an aliphatic nitrilase (EC 3.5.5.7) activity, or a combination of nitrile hydratase (EC 4.2.1.84) and amidase (EC 3.5.1.4) activities. The aimnonium salt of the .omega.-nitrilecarboxylic acid is then converted directly to the corresponding lactam by hydrogenation in aqueous solution, without isolation of the intermediate .omega.-nitrilecarboxylic acid or .omega.-monocarboxylic acid. When the aliphatic .alpha.,.omega.-dinitrile is also unsymmetrically substituted at the .alpha.-carbon atom, the nitrilase produces the .omega.-nitrilecarboxylic acid ammonium salt resulting from hydrolysis of the .omega.

Abstract: Asymmetric bioreduction of a ketone substrate with yeast produces the corresponding (R)-alcohol of structure: ##STR1## a key intermediate in the synthesis of a .beta..sub.

Abstract: Compositions comprising novel di-nitrogen heterocycle compounds containing at least one N-meta-substituted alkaryl group are prepared. The compounds of the present invention are useful as antibacterial and as other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents.

Abstract: A process for the preparation of five-membered or six-membered ring lactams from aliphatic .alpha.,.omega.-dinitriles has been developed. In the process an aliphatic .alpha.,.omega.-dinitrile is first converted to an ammonium salt of an .omega.-nitrile-carboxylic acid in aqueous solution using a catalyst having an aliphatic nitrilase (EC 3.5.5.7) activity, or a combination of nitrile hydratase (EC 4.2.1.84) and amidase (EC 3.5.1.4) activities. The ammonium salt of the .omega.-nitrilecarboxylic acid is then converted directly to the corresponding lactam by hydrogenation in aqueous solution, without isolation of the intermediate .omega.-nitrilecarboxylic acid or .omega.-aminocarboxylic acid. When the aliphatic .alpha.,.omega.-dinitrile is also unsymmetrically substituted at the .alpha.-carbon atom, the nitrilase produces the .omega.-nitrilecarboxylic acid ammonium salt resulting from hydrolysis of the .omega.

Abstract: Compound 9 is prepared by a 9-step ##STR1## process in an overall yield of about 35% from 3-acetylpyridine. Compound 10 is prepared by a seven-step ##STR2## process in an overall yield of about 30% from 3-acetyl pyridine. These compounds are key intermediates in the synthesis of Compound 11, an important .beta.-3 agonist useful in the treatment of obesity and diabetes.

Abstract: A compound of formula (II), either as a single enantiomer or in an enantiomerically enriched form ##STR1## wherein: ##STR2## and ##STR3## (wherein N in the benzimidazole moiety of Het.sub.2 means that one of the carbon atoms substituted by any one of R.sub.6 to R.sub.9 optionally may be exchanged for an unsubstituted nitrogen atom; R.sub.1, R.sub.2 and R.sub.3 are the same or different and selected from hydrogen, alkyl, alkoxy optionally substituted by fluorine, alkylthio, alkoxyalkoxy, dialkylamino, piperidino, morpholino, halogen, phenylalkyl, phenylakoxy; R.sub.4 and R.sub.4, are the same or different and selected from hydrogen, alkyl, aralkyl; R.sub.5 is hydrogen, halogen, trifluoromethyl, alkyl, alkoxy; R.sub.6 -R.sub.9 are the same or different and selected from hydrogen, alkyl, alkoxy, halogen, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, oxazolyl, trifluoroalkyl or adjacent groups R.sub.6 -R.sub.

Abstract: Microorganisms of interest are capable of utilizing .alpha.-imino carboxamides, in the form of the racemate or of its optically active isomers, of the general formula ##STR1## wherein A together with --NH-- and --CH-- is an optionally substituted 5- or 6-membered saturated heterocyclic ring, as sole nitrogen source, and converting (RS)-.alpha.-imino carboxamides of Formula I into an S-.alpha.-imino carboxylic acid of the general formula ##STR2## These microorganisms are useful also for biconversion of an (RS)-.alpha.-imino carboxamide of Formula I into an S-.alpha.-imino carboxylic acid.

Abstract: A process for producting vitamin B.sub.6 comprises cultivating a microorganism belonging to the genus Rhizobium and being capable of producing vitamin B.sub.6 in a culture medium under aerobic conditions, and separating the resulting vitamin B.sub.6 from the fermentation broth. As well as containing assimilable carbon sources, digestible nitrogen sources, inorganic salts and other nutrients necessary for the growth of the microorganism, the culture medium preferably additionally contains pyruvate, D-glyceraldehyde, glycolaldehyde, glycine, 1-deoxy-D-threo-pentulose, 4-hydroxy-L-threonine or a mixture thereof. This process affords high yields of vitamin B.sub.6, a vitamin essential for the nutrition of animals, plants and microorganisms and useful as a medicine and in foodstuffs.

Abstract: A method for producing a 3-hydroxy nitrogen-containing six-membered cyclic compound is provided. Namely, microbial cells of a microorganism and/or a preparation obtained from the microbial cells is allowed to act on a nicotinic acid derivative or a 2-pyrazinecarboxylic acid derivative represented by the following general formula: ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different, representing hydrogen atom, halogen atom, hydroxyl group, amino group, carboxyl group, cyano group, oxime group, or alkyl group having a number of carbon atom or atoms of 1 to 5 respectively, and A represents carbon atom or nitrogen atom, the microbial cells and/or the preparation obtained from the microbial cells having an ability to perform hydroxylation of the nicotinic acid derivative or the 2-pyrazinecarboxylic acid derivative accompanied by decarboxylation of carboxyl group.

Abstract: Disclosed are 1,4-dihydropyridine derivatives represented by the general formula (I) and salts thereof, as well as optical active 1,4-dihydropyridine derivatives represented by the general formula (II) and salts thereof which are obtained from the derivative by biochemical reactions using microorganisms or enzymes and useful as preventive and therapeutic agents for ischemic heart diseases and hypertension. ##STR1## (wherein x and Y are H, NO.sub.2, CN, halogen; R.sup.1 and R.sup.2 are H, CHO, substituted alkylcarbonyl, crotonyl, cinnamoyl, alkoxycarbonyl, aryloxycarbonyl, benzyloxycarbonyl, carboxybenzoyl, or R.sup.1 and R.sup.2 taken together represent phthaloyl; n is an integer of 1 to 3).

Abstract: A process for the biotechnological preparation of alcohols, aldehydes and carboxylic acids by oxidation of compounds of the formula R.sup.1 --C(CH.sub.3).dbd.CR.sup.2 R.sup.3, where R.sup.1, R.sup.2 and R.sup.3 have the meanings indicated in the description, with the aid of microorganisms is described.

Abstract: An enzyme is provided which has acylase activity capable of hydrolyzing N-acetyl-(R,S)-pipecolic acid stereoselectively to give (S)-pipecolic acid, wherein this activity is greater than that on N-acetyl-S-proline, at pH 7.5, 25.degree. C., and substrate concentration 20 g/l, in 75 mM Tris buffer. The enzyme is obtainable from the species of Alcaligenes denitrificans deposited as NCIMB 40587. A microorganism having therein the enzyme also is provided, as is a process for preparing (S)-pipecolic acid comprising contacting a mixture of enantiomers of an N-acyl-pipe colic acid with the enzyme or microorganism.

Abstract: Novel lactams and processes for the preparation of chiral compounds having utility as intermediates in the synthesis of compounds with Central Nervous System stimulant activity.

Abstract: A method for manufacturing S-3-(4'-tert-butyl)-phenyl-2-methyl propylamines having the structure I ##STR1## where NR.sub.1 R.sub.

Abstract: A process for preparing nicotinamide, wherein, in the first stage, 2-methyl-1,5-diaminopentane is catalytically converted into 3-picoline, then the 3-picoline is converted via an ammonoxidation into 3-cyanopyridine and, finally, the 3-cyanopyridine is converted microbiologically into the nicotinamide.

Abstract: A microbiological process for the preparation of a heteroaromatic carboxylic acid or one of its physiologically tolerated salts of the formulae I or II: ##STR1## wherein R.sub.1 and R.sub.2 are identical or different and each denotes a hydrogen or halogen atom, and X denotes a nitrogen atom or CH--, from a heteroaromatic nitrile of the formulae III or IV, respectively: ##STR2## First, a microorganism, Alcaligenes faecalis (DSM 6335), is cultured in the presence of an inducer, 2-cyanopyridine, and a carbon source such as a dicarboxylic acid, a tricarboxylic acid or a carbohydrate. Substrate III or IV is then reacted with the cultured microorganism. The biotransformation is carried out under anaerobic conditions for compounds of the formula I, and under aerobic conditions for compounds of the formula II.

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: Enantiomeric glutarimides such as aminoglutethimide and rogletimide are prepared by cyclisation of a corresponding ester-nitrile which is a good substrate for biotransformation with an enantiospecific esterase.

Abstract: (4R)-3-(Substituted aminoalkyl)oxycarbonyl-1,4-dihydro-2,6-dimethyl-4-(nitrophenyl)pyridine-5- carboxylic acids can be prepared efficiently, by reacting bis(substituted aminoalkyl) 1,4-dihydro-2,6-dimethyl-4-(nitrophenyl)pyridine-3,5-dicarboxylates with a microorganism capable of asymmetric hydrolysis and belonging to the genus Streptomyces, the genus Paecilomyces, the genus Botryodioplodia, the genus Alternaria or the genus Helminthosporium, or a treated product thereof. The compounds are extremely useful as important intermediates for preparation of pharmaceuticals useful for the prevention and treatment of angina pectoris, hypertension, etc.

Abstract: This invention relates to the enantioselective biologically-catalyzed hydrolysis of certain racemic nitriles to the corresponding R- or S-amides, chemically or biologically-catalyzed hydrolysis of the amides to the corresponding R- or S-acids in a batch process or in a continuous process that employs racemization and recycling of enantiomeric nitrile intermediates, the racemic nitriles being selected from the group, A--C(R.sup.1)(R.sup.2)CN, wherein A, R.sup.1 and R.sup.2 are as defined in the text, as well as certain biological materials employed to catalyze the process.

Abstract: A morphinone reductase enzyme and related process provide for the preparation of hydromorphone from morphinone and hydrocodone from neopinone or codeinone. The enzyme has no significant activity with compounds of similar ring structure, has a molecular weight of approximately 81 kilodaltons and is composed of two identical subunits. The enzyme uses NADH as a cofactor and displays no significant enzymatic activity in the reverse direction.

Abstract: A new and practical method for synthesizing heterocyclic polyhydroxylated alkaloids using enzymatic aldol condensation and catalytic intramolecular reductive amination is disclosed.

Abstract: The present invention provides a process for production of amide compounds, which includes converting a nitrile compound into its corresponding amide compound by hydrating the nitrile compound in the presence of a cultured broth of bacterial cells, intact bacterial cells, disrupted bacterial cells or enzymes contained therein, or immobilized preparations obtainable by immobilizing intact bacterial cells, disrupted bacterial cells or enzymes contained therein, the bacterial cells being those of a biologically pure culture of a thermophilic microorganism having hydration activity to convert a nitrile compound into its corresponding amide compound, such as Bacillus smithii SC-J05-1 (FERM BP-4935).

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: 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: Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides a phthalyl amidase, a method for producing it by culturing the natural organism from which the activity was identified, and methods for using the phthalyl amidase to remove the phthalyl moiety from phthalyl-containing amides. The enzyme is isolated from Xanthobacter agilis.

Abstract: The microbiological process for the production of hydroxy-heterocyclic carboxylic acid of formula ##STR1## wherein R.sub.1 means a hydrogen or a halogen atom and X means a nitrogen atom or a CR.sub.2 function, wherein R.sub.2 means a hydrogen or halogen atom, starting from the corresponding heterocyclic carboxylic acid. The process is performed so that an aerobic biomass which utilizes nicotinic acid, is cultivated in a molar ratio of nicotinic acid to mineral acid of 1 to 8. The ratio is assured over the entire cultivation phase. The the hydroxylation of the corresponding heterocyclic carboxylic acid of the general formula ##STR2## wherein R.sub.1 and X have the above-mentioned meanings, is performed with the biomass. Under these conditions, strain Pseudomonas acidovorans DSM 7205, strain Pseudomonas acidovorans DSM 7203, strain Alcaligenes faecalis DSM 7204 and strain Arthrobacter crystallopoietes DSM 7202 are concentrated in the cultivation phase.

Abstract: DNA molecules encoding a modified tryptophan synthase beta subunit are disclosed. When expressed in a recombinant host microorganism, these polypeptide analogs enable significant levels of intracellular indole production and accumulation. In the presence of an aromatic dioxygenase enzyme, the indole so produced can be converted to indoxyl, which upon exposure to air oxidizes to indigo.

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: 6-Hydroxy nitrogen-containing 6-membered ring compounds of the following general formula (II): ##STR1## wherein R.sup.1 represents carboxy group, carbamoyl group, cyano group, formyl group, C.sub.1 -C.sub.5 hydroxyalkyl group, C.sub.2 -C.sub.6 alkoxycarbonyl group, carboxyvinyl group, carboxymethyl group or oxime group, R.sup.2 represents hydrogen atom or carboxy group, and A represents carbon atom or nitrogen atom, can be prepared by reacting a nitrogen-containing 6-membered ring compounds of the following general formula (I): ##STR2## wherein R.sup.1, R.sup.2 and A are as defined in the general formula (II) above, with a microorganism or physico-chemically treated microorganism in an aqueous medium. Efficiency of the above reaction can be raised by conducting the reaction in the presence of phenazine methosulfate.

Abstract: A process for reducing a phenylalkyl ketone to the corresponding (S)-hydroxy derivative is disclosed. The process comprises contacting the phenylalkyl ketone with Mucor hiemalis IFO 5834 and recovering the (S)-hydroxy derivative.

Abstract: There is disclosed a process for production of amide compounds which includes converting a nitrile compound into an amide compound using a cultured broth of bacterial cells, or bacterial cells or materials obtainable by treating bacterial cells, the bacterial cells being cells of a microorganism Agrobacterium radiobacter FERM BP-3843, having activity to convert nitrile compounds into corresponding amide compounds.

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: DNA molecules encoding a modified tryptophan synthase beta subunit are disclosed. When expressed in a recombinant host microorganism, these polypeptide analogs enable significant levels of intracellular indole production and accumulation. In the presence of an aromatic dioxygenase enzyme, the indole so produced can be converted to indoxyl, which upon exposure to air oxidizes to indigo.

Abstract: A new microbiological process for the production of hydroxy-nitrogen-heterocyclic-carboxylic acids or their soluble salts of the general formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom, a halogen atom or a C.sub.1 -C.sub.4 alkyl group and X is a nitrogen atom or a CR.sub.3 function, wherein R.sub.3 is a hydrogen atom or a halogen atom, starting from the corresponding nitrogen-heterocyclic-carboxylic acids, as well as new microorganisms suitable for use in the process.

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: A microbiological process for the production of 5-hydroxypyrazinecarboxylic acid and/or its salts with microorganisms of the strain Agrobacterium sp. DSM 6336 or descendants thereof or mutants thereof, utilizing 3-cyanopyridine.

Abstract: The present invention discloses the preparation of R-configured trialkylsilylethynyl .alpha.-alcohols from similarly substituted .alpha.-ketones, and vice versa, catalyzed by the alcohol dehydrogenase of Lactobacillus kefir, ATCC No. 35411. Also disclosed is the acceptance or transfer of a hydride ion from or to the pro-R face of NADPH or NADP, respectively, as catalyzed by that enzyme.

Abstract: Trans-4-hydroxy-L-proline is produced microbially, especially by the cultivation of a microorganism of the genus Clonostachys, Gliocladium or Nectria.

Abstract: 10'-Desmethoxystreptonigrin, obtainable by cultivation of a strain of Streptomyces albus, A.T.C.C. No. 55161, and salts, esters and amides thereof. The novel compounds have antitumor and antibiotic activity.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or a hydrocarbon residue which may be substituted; R.sup.2 is oxo or hydrogen plus hydroxy which may be acylated; R.sup.3 is hydrogen or hydroxy which may be acylated; at least one of the dotted lines represents a single bond, or a salt thereof, produced from Penicillum thomii has potent RA-89 muscarinic receptor blocking activity and is of value as therapeutic agent for parkinsonism, ulcer, etc. or as mydriatics.

Abstract: A new microbiological process for the production of hydroxy-nitrogen-heterocyclic-carboxylic acids or their soluble salts of the general formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom, a halogen atom or a C.sub.1 -C.sub.4 alkyl group and X is a nitrogen atom or a CR.sub.3 function, wherein R.sub.3 is a hydrogen atom or a halogen atom, starting from the corresponding nitrogen-heterocyclic-carboxylic acids, as well as new microorganisms suitable for use in the process.

Abstract: A microbiological process for terminal hydroxylation of ethyl groups on aromatic 5- or 6-member ring heterocycles. The hydroxylation is performed with microorganisms which:(a) contain the genes of a Pseudomonas OCT plasmid which form an active alkane monooxygenase, and(b) form no active chromosomal or plasmid-coded alcohol dehydrogenase.

Abstract: Two enzymes, one an acetylmorphine carboxyesterase (AMCE), the other a morphine dehydrogenase (MDH), have been isolated from bacteria. The AMCE degrades heroin to morphine and the MDH oxidises morphine to morphinone, with the aid of a cofactor. These reactions are used in detection of heroin (using the two reactions coupled together) or morphine. The enzymes can be incorporated in sensors for this purpose.

Abstract: Microorganisms which are capable of growing with 2,5-dimethylpyrazine as the sole carbon, nitrogen and energy source. These microorganisms hydroxylate heterocycles of general formula: ##STR1## to heterocycles of general formula: ##STR2## The latter compounds are accumulated in the growth medium.

Abstract: Intermediates and a process for their preparation are disclosed which are useful for the preparation of a renin inhibiting compound of the formula: ##STR1## wherein R is a nitrogen-containing heterocycle which is bonded via a nitrogen atom to the sulfonyl group, R.sub.6 is hydrogen, alkoxy, halogen or loweralkyl, R.sub.7 is loweralkyl having 2 to 7 carbon atoms, and R.sub.8 is loweralkyl, cycloalkyl, or aryl or a pharmaceutically acceptable acid addition salt thereof.

Abstract: A microbiological process for the production of 5-hydroxypyrazinecarboxylic acid and/or its salts with microorganisms using nicotinic acid and/or its salts.

Abstract: A microbiological process for the production of 6-hydroxypicolinic acid starting from picolinic acid and/or its salts. The concentration of picolinic acid and/or its salts is selected so that the 6-hydroxypicolinic acid is not further metabolized. The process is performed either by microorganisms of genus Pseudomonas, Bacillus, Alcaligenes, Aerococcus, or Rhodotorula, or with biomass using picolinic acid, which grow with picolinic acid as the sole carbon, nitrogen and energy source.

Abstract: Microorganisms, which are capable of growing with pyrazine as the sole carbon, nitrogen and energy source. These microorganisms hydroxylate pyrazine derivatives of general formula: ##STR1## to hydroxylated pyrazine derivatives of general formula: ##STR2## and the latter are accumulated in the growth medium.

Abstract: A microbiological process for the production of 6-hydroxynicotinic acid starting from 3-cyanopyridine. For this process, new microorganisms are used, which are capable of growing with 3-cyanopyridine as the sole carbon, nitrogen and energy source and of biotransforming it as substrate in 6-hydroxynicotinic acid.