Abstract: This invention relates to a novel .alpha.-amino.alpha.-(p-acyloxyphenyl)acetamidopenicillanic acid which is useful as an antibacterial agent, and also to a novel process for the production of 6-D-(-).alpha.-amino-.alpha.-(p-hydroxyphenylacetamido)penicillanic acid (also known as amoxycillin).BACKGROUND OF THE INVENTION1. Field of the InventionThe chemical compound of the present invention is an antibacterial agent of the class commonly called penicillins.2. Description of the Prior ArtU.S. Pat. No. 2,985,648 relates to .alpha.-aminobenzylpenicillins and discloses a general formula for such penicillins which includes, inter alia, lower alkanoyloxy substituents on the benzene ring. This document does not give any more specific details of compounds so substituted, and no specific examples are given of their preparation. The document indicates that the .alpha.-aminobenzylpenicillins exist in various optical forms and specific examples are given of the preparation of both D- and L- forms.U.S. Pat. No.

Abstract: This invention provides a new chemical named bestatin which inhibits aminopeptidase B, leucine aminopeptidase and bleomycin hydrolase, enhances the antitumor effect of bleomycin, has the chemical name [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine and has the following structure: ##STR1## and also provides a process for the production thereof which comprises cultivating a strain of streptomyces which produces bestatin in a nutrient medium under aerobic conditions until substantial activity inhibitory to aminopeptidase B is imparted to said cultured medium and then recovering said bestatin from said cultured medium. A preferred strain is Streptomyces olivoreticuli FERM-P No. 2590 (A.T.C.C. 31159).

Abstract: There are disclosed two new antibiotics formerly denominated MC916-A and MC916-B and now called neothramycin A and neothramycin B which are potent inhibitors of the growth of leukemia cells, e.g. Leukema L-1210 cells in mice. They are produced by controlled fermentation of Streptomyces FERM-P 2452 (A.T.C.C. 31123).

Abstract: Compounds having the formula ##STR1## (the meanings of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are indicated hereinafter) exhibit suppressive activity to various immune responses and can be employed in the therapy of immunological diseases, especially autoimmune diseases.

Abstract: This invention provides a new chemical named bestatin which inhibits aminopeptidase B, leucine aminopeptidase and bleomycin hydrolase, enhances the antitumor effect of bleomycin, has the chemical name [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine and has the following structure: ##STR1## and also provides a process for the production thereof which comprises cultivating a strain of streptomyces which produces bestatin in a nutrient medium under aerobic conditions until substantial activity inhibitory to aminopeptidase B is imparted to said cultured medium and then recovering said bestatin from said cultured medium. A preferred strain is Streptomyces olivoreticuli FERM-P No. 2590 (A.T.C.C. 31159).

Abstract: Compounds of the formula ##STR1## wherein A is hydrogen, hydroxy, methyl or methoxy,R.sup.1 is hydrogen, sodium or potassium,R.sup.2 is carboxyl or an aliphatic, aromatic or heterocyclic radical to which there is also attached a strongly acidic group in the form of its sodium or potassium salt, andR.sup.3 is 1,2,3-triazol-5-yl, such group being unsubstituted or substituted with one or two lower alkyl groups of one to four carbon atoms are prepared by reacting the appropriate aldehyde with the corresponding amphoteric cephalosporin.

Abstract: Compounds having the general formula ##STR1## (the meanings of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are indicated hereinafter) and the pharmaceutically acceptable salts and esters thereof exhibit strong activities in inhibiting histidine decarboxylase and xanthine oxidase and are useful for treating elevated histamine and uric acid levels.

Abstract: The title compounds, which can casually be called 1-oxapenicillins, are produced by total synthesis. Thus 1-oxabenzylpenicillin is produced either by phenylacetylation of 2,2-dimethyl-3R-carboxy-6S-amino-1-oxa-4-aza-5R-bicyclo[3,2,0]heptan-7-one or by hydrolysis and rearrangement of 2-benzyl-6-(1'-methoxycarbonyl-2'-methylprop-1'-enyl)-1-oxa-3,6-diaza-4S, 5R-bicyclo[3,2,0]hept-2-en-7-one.

Abstract: This invention relates to a process for the preparation of coformycin, 3-(.beta.-D-ribofuranosyl)-6,7,8-trihydroimidazo[4,5-d][1,3]diazepin-8(R)- ol, through a synthetic route from a new derivative of 9.beta.-D-ribofuranosyl-purine and other synthetic intermediates involved in the process and their preparation.

Abstract: This invention relates to certain novel .alpha.-amino- or .alpha.-formyl-.alpha.-(p-acyloxyphenyl)acetamidocephalosporanic acids which are useful as antibacterial agents.

Abstract: There is disclosed a new antibiotic called calvatic acid having the structure p-carboxyphenyl-azoxycarbonitrile and processes for its production by fermentation and processes for its recovery and purification. This substance is effective in inhibiting the growth of Gram-positive bacteria and carcinoma.

Abstract: The specification discloses a process for preparing methoxymethyl D-6-(2,2-dimethyl-5-oxo-4-phenyl-1-imidazolidinyl)penicillanate and the use of this compound as a well absorbed antibacterial agent and also as an intermediate in the preparation of other antibiotic derivatives of 6-aminopenicillanic acid such as hetacillin. The methoxymethyl ester of ampicillin is also disclosed.

Abstract: A new antitumor agent named macracidmycin, which is a macromolecular peptide and inhibits the growth of various tumor cells and experimental animal tumors such as Ehrlich ascites carcinoma and Sarcoma 180 is produced by the fermentation of a microorganism belonging to the genus Streptomyces which has been designated Streptomyces atrofaciens (M590-G2 and A.T.C.C. 31104); it is recovered from the broth by conventional methods for recovering antibiotics.

Abstract: New antitumor agents named aclacinomycins A and B, which are anthracycline glycosides and inhibit the growth of various microorganisms e.g., Staphylococcus aureus, Micrococcus flavus, Corynebacterium bovis and inhibit the growth of animal tumors such as leukemia L1210 and P388 and lymphoma 6C3HED in mice and hepatomas in rats are produced by the fermentation of a microorganism belonging to the genus Streptomyces which has been designated Streptomyces galilaeus (MA144-M1 and A.T.C.C. 31133); they are recovered from the broth by conventional methods for recovering antibiotics.

Abstract: 7-(D-.alpha.-Hydroxy-2-arylacetamido)-3-(tetrazolo-[4,5-b]pyridazin-6-ylthi omethyl)-3-cephem-4-carboxylic acids and their nontoxic, pharmaceutically acceptable salts are valuable as antibacterial agents and are particularly valuable as therapeutic agents in poultry and animals, including man, in the treatment of infectious diseases caused by many Gram-positive and Gram-negative bacteria.

Abstract: Improved yields of 7-[D-.alpha.-amino-.alpha.-(4-hydroxy- and 3-chloro-4-hydroxy-phenyl)acetamido]-3-methyl-3-cephem-4-carboxylic acids are obtained by acylating 7-aminodesacetoxycephalosporanic acid with the mixed anhydride (from ethyl chloroformate) of the ring-substituted 2-phenylglycine when the latter's .alpha.-amino group has been blocked by reaction with a .beta.-keto compound such as methyl acetoacetate. Improved purification processes include the use of dimethylformamide and acetonitrile solvates and solvates and bis-anthraquinone-1,5-disulfonic acid salts.

Abstract: Chlorinated esters of anhydrobenzylpenicillin are reacted with alumina or silica gel to produce fused oxazoline azetidinones. One product may be named methyl 2-(3-benzyl-7-oxo-4-oxa-2,6-diazabicyclo[3,2,0]hept-2-en-6-yl)-3-methylbut -2-enoate or 2-benzyl-6-(1'-methoxycarbonyl-2'-methylprop-1'-enyl)-1-oxa-3,6-diaza-4S,5 R-bicyclo[3,2,0]hept-2-en-7-one.

Abstract: There is disclosed a new antibiotic called calvatic acid having the structure p-carboxyphenyl-azoxycarbonitrile and processes for its production by fermentation and processes for its recovery and purification. This substance is effective in inhibiting the growth of Gram-positive bacteria and carcinoma.

Abstract: In the production of amoxicillin by acylation of silylated 6-aminopenicillanic acid with the appropriate acid chloride hydrochloride the efficiency of the process and the purity of the product are increased by a new recovery process consisting of isolation from the acylation reaction mixture of solid amoxicillin hydrochloride which is then easily converted to amoxicillin trihydrate.

Abstract: This invention relates to the novel compounds 3',5,7-trihydroxy-4',6-dimethoxy-isoflavone, 3',5,7-trihydroxy-4',8-dimethoxy-isoflavone and 3',7-dihydroxy-4',6,8-trimethoxy-isoflavone which are powerful inhibitors of catechol-O-methyl transferase (COMT) and to their production by fermentation of Actinomyces roseolus.