Abstract: A compound of the formula: ##STR1## wherein X is a member selected from the group consisting of hydrogen, alkyl of from 1 to 3 carbon atoms, inclusive, chlorine or bromine; Y is a member selected from the group consisting of hydrogen, chlorine or bromine and R is a member selected from the group consisting of hydrogen or lower alkyl of from 1 to 3 carbon atoms.The compounds can be applied to seeds, plants, animals, objects, or places for preventing damage due to fungi. General methods for preparing the active compounds, compositions and methods of use are shown.
Abstract: Novel antibiotic U-36,699 which has been identified as the .alpha.-methylene derivative of pentalenolactone. Antibiotic U-36,699 has the following structural formula ##STR1## This antibiotic is produced in a chemical process using pentalenolactone (also known as antibiotic P.A. 132), as the starting material. Antibiotic U-36,699 is active against Staphylococus aureua, Sarcina lutea, Mycobacterium phlei, Mycobacterium avium, Saccharomyces cerevisiae, and Penicillium oxalicum. Thus, antibiotic U-36,699 can be used in various environments to eradicate or control such fungi and bacteria. Further, antibiotic U-36,699 inhibits P 388 leukemia cells in laboratory mice. Thus, this antibiotic can be used to treat laboratory mice harboring P 388 leukemia cells.
Abstract: This invention relates to a process for stimulating the growth of mammalian hair comprising the application to mammalian skin of a compound of the formula: ##STR1## wherein R.sub.1 is a moiety selected from the group consisting of moieties of the formula ##STR2## wherein R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl, and lower cycloalkyl, and taken together R.sub.3 and R.sub.4 may be a heterocyclic moiety selected from the group consisting of aziridinyl, azetidinyl, pyrrolidinyl, piperidino, hexahydroazepinyl, heptamethylenimino, octamethylenimino, morpholino, and 4-lower-alkylpiperazinyl, each of said heterocyclic moieties having attached as substituents on the carbon atoms 0-3 lower alkyl groups, hydroxy or alkoxy wherein R.sub.
Abstract: Disclosed are degradation products of the antibiotics rubradirin and rubradirin B and processes for their preparation. Some of these products have antibacterial activity, and, thus, can be used in various environments to inhibit susceptible bacteria. Also, some of these products can be used as intermediates to make useful antibacterials.
Abstract: Novel antibiotic 354 (U-54,703) producible in a fermentation under controlled conditions using the new microorganism Streptomyces puniceus subsp. doliceus, NRRL 11160. This antibiotic is active against Gram-negative bacteria, for example, Pseudomonas and Proteus species. Thus, antibiotic 354 can be used in various environments to eradicate or control such bacteria.
Type:
Grant
Filed:
September 19, 1977
Date of Patent:
January 23, 1979
Assignee:
The Upjohn Company
Inventors:
Clarence De Boer, Lester A. Dolak, Durey H. Peterson
Abstract: A process for the therapeutic and prophylactic treatment of allergy by the systemic administration of a compound of the formula: ##STR1## wherein Y is lower alkyl of 1 to 8 carbon atoms, cyclopropyl, ethinyl, --CF.sub.3, --F, --Cl, --OCH.sub.3, --OCHF.sub.3, --OCH.sub.2 OCH.sub.3, --SCH.sub.3, --SCHF.sub.2, --SCH.sub.2 OCH.sub.3, acetyl; R.sub.1 and R.sub.2 are H, CH.sub.3, CHF.sub.2, or taken together are .dbd.CH.sub.2 or .dbd.CF.sub.2 ; and X is hydrogen, lower alkyl of 1 to 8 carbon atoms or a pharmacologically acceptable cation in association with a pharmaceutical carrier.
Abstract: New antiobiotic U-53,946 produced by the controlled fermentation of the new microorganism Paecilomyces abruptus sp. nov., NRRL 11110. This antibiotic is active against Gram-positive bacteria, for example, Sarcina lutea, Staphylococcus aureus, Bacillus subtilis, Mycobacterium avium, and Streptococcus pyrogenes, and the yeast Saccharomyces pastorianus. Accordingly, they can be used in various environments to eradicate or control these microorganisms.
Abstract: Bioconversion of the antibiotic steffimycinone to the antibiotic steffimycinol. Steffimycinol is active against various microorganisms, for example, Bacillus subtilis, Mycobacterium avium and Streptococcus pyogenes. Steffimycinol is converted to 7-deoxysteffimycinol by a microaerophilic Aeromonas hydrophila fermentation. 7-Deoxysteffimycinol is active against Sarcina lutea, Bacillus cereus, and B. subtilis. Thus, these antibiotics can be used to inhibit the growth of the above microorganisms in various environments.
Type:
Grant
Filed:
November 16, 1977
Date of Patent:
September 26, 1978
Assignee:
The Upjohn Company
Inventors:
Vincent P. Marshall, David W. Elrod, James M. Koert, Elizabeth A. Reisender, Paul F. Wiley
Abstract: Novel compounds of the formula: ##STR1## wherein R.sub.1 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, CH.sub.2 -alkenyl wherein alkenyl is from 2 to 4 carbon atoms, inclusive, cycloalkyl of from 3 to 6 carbon atoms, inclusive, cycloalkylmethyl of from 3 to 6 carbon atoms, inclusive; R.sub.2 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen at the same time; Y is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, halogen, trifluoromethyl, hydroxy, alkanoyloxy from 2 to 5 carbon atoms, inclusive, alkoxy of from 1 to 4 carbon atoms, inclusive, cycloalkyloxy of from 3 to 6 carbon atoms, inclusive, benzyloxy; m is an integer 0, 1, 2; R.sub.5 is a variable consisting of hydrogen and alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.3 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.
Abstract: A process for inhibiting platelet aggregation by the addition of a member selected from the group consisting of a compound of the formula: ##STR1## wherein Y is lower alkyl of 1 to 8 carbon atoms, cyclopropyl, ethinyl, -CF.sub.3, -F, -Cl, -OCH.sub.3, -OCHF.sub.3, -OCH.sub.2 OCH.sub.3, -SCH.sub.3, -SCHF.sub.2, -SCH.sub.2 OCH.sub.3, acetyl; R.sub.1 and R.sub.2 are H, CH.sub.3, CHF.sub.2, or taken together are .dbd.CH.sub.2 or .dbd.CF.sub.2 ; and X is hydrogen, lower alkyl of 1 to 8 carbon atoms or a pharmacologically acceptable cation, to in vivo and in vitro platelet systems. In vitro systems include whole blood as kept in blood banks, whole blood as used in heart-lung machines, and platelet rich concentrates. In vivo systems include human or animal bodies. The process provides a means for treating hemorrhage due to thrombocytopenia which in turn is caused by irradiation, cancer chemotherapy, or immunosuppressants as well as hemophilia due to congenital defects.
Abstract: Antibiotic rubradirin B producible by the controlled fermentation of the known microorganism Streptomyces achromogenes var. rubradiris, NRRL 3061. This antibiotic and its base-addition salts are active against various microorganisms, for example, Staphylococcus aureus, Streptococcus hemolyticus, Sarcina lutea, and Mycobacterium avium. Accordingly, they can be used in various environments to eradicate or control such microorganisms.
Type:
Grant
Filed:
April 15, 1977
Date of Patent:
August 15, 1978
Assignee:
The Upjohn Company
Inventors:
Herman Hoeksema, Fritz Reusser, Donald R. Wait
Abstract: Bioconversion of the antibiotic steffimycinone to the antibiotic steffimycinol. Steffimycinol is active against various microorganisms, for example, Bacillus subtilis, Mycobacterium avium and Streptococcus pyogenes. Steffimycinol is converted to 7-deoxysteffimycinol by a microaerophilic Aeromonas hydrophila fermentation. 7-Deoxysteffimycinol is active against Sarcina lutea, Bacillus cereus, and B. subtilis. Thus, these antibiotics can be used to inhibit the growth of the above microorganisms in various environments.
Type:
Grant
Filed:
November 16, 1977
Date of Patent:
August 15, 1978
Assignee:
The Upjohn Company
Inventors:
Vincent P. Marshall, David W. Elrod, James M. Koert, Elizabeth A. Reisender, Paul F. Wiley
Abstract: Antibiotic rubradirin C producible by the controlled fermentation of the known microorganism Streptomyces achromogenes var. rubradiris, NRRL 3061. This antibiotic and its base-addition salts are active against Streptococcus pyogenes and Bacillus cereus. Accordingly, they can be used in various environments to eradicate or control such microorganisms. SuBACKGROUND OF THE INVENTIONAntibiotic rubradirin, and a microbiological process for its preparation, are disclosed in U.S. Pat. No. 3,335,057. Rubradirin B is disclosed in U.S. application Ser. No. 787,833, filed Apr. 15, 1977. Degradation products of rubradirin and rubradirin B, and processes for their preparation are disclosed in U.S. application Ser. No. 793,785, filed May 5, 1977.BRIEF SUMMARY OF THE INVENTIONThe novel antibiotic of the invention, rubradirin C, is obtained by culturing Streptomyces achromogenes var. rubradiris, NRRL 3061, in an aqueous nutrient medium under aerobic conditions. The fermentation conditions disclosed in U.S. Pat. No.
Abstract: Novel compounds prepared by microbial transformation using novel mutants to selectively degrade steroids with or without 17-alkyl side chains of from 2 to 10 carbon atoms, inclusive. These compounds can be used as intermediates to make useful steroids.
Abstract: Novel microbial transformation process to selectively convert steroids with or without 17-alkyl side chains of from 2 to 10 carbon atoms, inclusive, to 3a.alpha.-H-4.alpha.-?3'-propanol!-7a.beta.-methylhexahydro-1,5-indaned ione hemiketal having the following structure: ##STR1## This compound can be used as an intermediate to make useful 19-nor steroids.
Abstract: Microbiological process for preparing the known antibiotics, antibiotic A-396-1 and L-dihydrophenylalanine, by use of the new microorganism Streptomyces lemensis, NRRL 8170 using controlled fermentation conditions. These antibiotics are active against Gram-positive and Gram-negative bacteria. Accordingly, they can be used in various environments to eradicate or control such bacteria.
Type:
Grant
Filed:
March 9, 1977
Date of Patent:
May 23, 1978
Assignee:
The Upjohn Company
Inventors:
Alexander D. Argoudelis, LeRoy E. Johnson
Abstract: Antibiotics steffimycinol and 7-deoxysteffimycinol produced by reduction of the antibiotic steffimycinone. Steffimycinol is active against various microorganisms, for example, Bacillus subtilis, Mycobacterium avium and Streptococcus pyogenes; 7-deoxysteffimycinol is active against Sarcina lutea, Bacillus cereus, and B. subtilis. Thus, these antibiotics can be used to inhibit the growth of the above microorganisms in various environments.
Abstract: Novel antibiotics, 7-O-alkylnogarols, prepared by acidic alcoholysis of nogamycin, which are active against various microorganisms, for example, Bacillus subtilis and Lactobacillus casei. Thus, they can be used to inhibit the growth of the above microorganisms in various environments.
Abstract: This invention relates to novel compounds of the formula: ##STR1## wherein X is H, methoxy, bromine or chloro; R.sub.1 is hydrogen or hydroxy, acyloxy wherein acyl is 2 to 8 carbon atoms, R.sub.2 is hydrogen, hydroxy, methyl, fluoro or chloro; and R.sub.1 and R.sub.2 taken together can be ##STR2## R.sub.3 is hydrogen, methyl, chloro, or fluoro; R.sub.4 is hydrogen, chloro or fluoro; R.sub.5 is oxygen, .beta.-hydroxy or .beta.-chloro, with the proviso that when R.sub.5 is .beta.-chloro then R.sub.4 must be chloro.The compounds have a photocleavable group (R) which is removable by irradiation. The compounds have reduced activity in the uncleaved state and provide a therapeutically active compound upon irradiation at the site of irradiation.