Abstract: Human urokinase is produced using recombinant DNA techniques. The invention disclosed thus enables the production of urokinase free of contaminants with which it is ordinarily associated in its native cellular environment. Methods, expression vehicles and various host cells useful in its production are also disclosed.

Abstract: Described are methods and means for the construction and microbial expression of quasi-synthetic genes arising from the combination of organic synthesis and enzymatic reverse transcription from messenger RNA sequences incomplete from the standpoint of the desired protein product. Preferred products of expression lack bio-inactivating leader sequences common in eukaryotic expression products but problematic with regard to microbial cleavage to yield bioactive material. Illustrative is a preferred embodiment in which a gene coding for human growth hormone (useful in, e.g., treatment of hypopituitary dwarfism) is constructed and expressed.

Abstract: The specification discloses:1. Recombinant microbial cloning vehicles comprising heterologous DNA coding for the expression of mammalian hormone (e.g., somatostatin) and other polypeptides, including plasmids suited for the transformation of bacterial hosts. The latter incorporate a regulon homologous to the host in its untransformed state, in reading phase with the structural gene for the heterologous DNA;2. Cloning vehicles coding for the microbial expression of a protein variously comprising (a) a polypeptide hapten and additional protein sufficient in size to confer immunogenicity on the product of expression, which may find use in raising antibodies to the hapten for assay use or in the manufacture of vaccines; and (b) a desired polypeptide product and additional protein from which the desired product may be cleaved; and3. Methods of preparing synthetic structural genes coding for the expression of mammalian polypeptides in microbial cloning systems.

Abstract: Oxazoles which are substituted in the 2,4 or 5-position with an N-substituted-acylamino group have anti-allergic activity. Methods of making such compounds, pharmaceutical compositions containing the active compounds of the invention and methods of treating asthma utilizing such compounds are provided.

Abstract: Cardiac arrhythmia is treated orally or parenterally with diarylalkylamines and diarylalkenylamines.

Abstract: An N-perfluoroacyl-L-.alpha.-amino acid is converted to the corresponding acid halide which is useful as a resolving agent for the resolution of racemic amines.

Abstract: Reaction of 3-hydroxy cephalosporins with alkylfluorosulfonates in the presence of a base provides 3-alkoxy cephalosporins which are useful as intermediates for cephalosporin antibiotic preparation.

Abstract: Imino chlorides of 6-aminopenicillanic esters and 7-aminocephalosporanic esters are reacted at a temperature between -80.degree. and -25.degree. C. with a strong base such as an alkali metal amide of a secondary amine and the generated anion is halogenated to provide the corresponding 6- or 7-halo-N(.alpha.-haloalkylidene) or N(.alpha.-halo-.alpha.-arylmethylidene)-6-aminopenicillanic or 7-aminocephalosporanic esters, respectively. The 6-halopenicillins and 7-halocephalosporins are converted to 6-methoxypenicillins and 7-methoxycephalosporins.

Abstract: 3,3-Dialkyl-1-(substituted-phenyl)triazene-1-oxides and N-phenylazo heterocyclic compounds having anti-inflammatory properties.

Abstract: 3-Aryl-triazene-1-oxides are useful for treating inflammatory diseases.

Abstract: 6-Acylamino-6-alkylthiopenicillanic or 7-acylamino-7-alkylthiocephalosporanic acids or esters are reacted at a temperature between -80.degree. and -25.degree.C. with one equivalent of halogen to provide an intermediate halosulfonium halide which is reacted with a C.sub.1 -C.sub.4 alkyl amine, a C.sub.1 -C.sub.4 dialkylamine or ammonia in an appropriate solvent. The ester group is removed to provide the 6-aminopenicillanic or 7-aminocephalosporanic acid.

Abstract: A process for preparing new compounds which are N- and O-acylates of pyrazofurin comprises first selective mono-N-acylation under non-basic conditions in an organic solvent. The mono-N-acylate so formed is further acylated under mild basic conditions to provide a tetra-acylated or penta-acylated pyrazofurin derivative, depending upon the duration of reaction. Mild solvolysis of either a tetra-acylate or a penta-acylate provides a tri-acylated pyrazofurin derivative. In the presence of a strong base, the mono-N-acylate is further acylated to provide different tetra-acylates or penta-acylates of pyrazofurin, again depending upon the duration of reaction. Pyrazofurin acylates are useful as antiviral, antipsoriatic, and antifungal agents, as well as intermediates for new C-nucleosides.

Abstract: 7-Acylamino and 7-amino-3-carboxy-3-cephem-4-carboxylic acids and derivatives thereof, which are useful as antibiotics or as intermediates in preparing antibiotic substances, are prepared by an NBS oxidation of acetal derivatives of 3-formyl cephalosporins.

Abstract: Acyloxymethyl esters of 7-D-mandelamido-3-(1-methyl-1,2,3,4-tetrazole-5-thiomethyl)-3-cephem-4-car boxylic acid are orally active broad spectrum antibiotics.