Containing At Least Two Hetero Rings Bridged Or Fused Among Themselves Or Bridged Or Fused With A Common Carbocyclic Ring System, (e.g., Rifamycin, Etc.) Patents (Class 435/119)
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Patent number: 4371617Abstract: A new process for preparing thienamycin, a known antibiotic useful as a medicament and veterinary drug, characterized by cultivating Streptomyces penemifaciens sp. nov. in a suitable medium and recovering thienamycin from the fermentation broth.Type: GrantFiled: March 18, 1981Date of Patent: February 1, 1983Assignee: Shionogi & Co., Ltd.Inventors: Kentaro Tanaka, Naoki Tsuji, Eiji Kondo, Yoshimi Kawamura
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Patent number: 4370415Abstract: A process for producing uroporphyrin III, which comprises cultivating a uroporphyrin III-producing microorganism of the genus Arthrobacter in a culture medium containing a carbon source, a nitrogen source and a mineral, and recovering uroporphyrin III from the culture broth.Type: GrantFiled: November 7, 1980Date of Patent: January 25, 1983Assignee: Nippon Oil Company, Ltd.Inventors: Ichiro Kojima, Kenji Maruhashi, Yasuo Fujiwara
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Patent number: 4369252Abstract: The invention relates to a new process for the preparation of ergot alkaloids, primarily ergocornine and .beta.-ergocryptine, by subjecting a Claviceps purpurea strain to fermentation under aerobic conditions in a culture medium which contains carbon and nitrogen sources, mineral salts and optionally other additives, too. According to the invention a Claviceps purpurea variant strain deposited under No. MNG 00186 is applied as alkaloid-producing strain.Type: GrantFiled: February 6, 1981Date of Patent: January 18, 1983Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Geza Wack, Janos Kiss, Zsuzsa Lengyel nee Szemenyei, Lajos Nagy, Eva Udvardy Nagy nee Cserey Pechany, Karoly Zalai, Erzsebet Zsoka nee Somkuti
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Patent number: 4368203Abstract: A novel antibiotic substance of the formula ##STR1## wherein R.sub.1 is CH.sub.3 and R.sub.2 is --CH.sub.2 --CH.sub.2 -- or R.sub.1 is H and R.sub.2 is --CH.dbd.CH--; and R.sub.3 represents hydrogen, lower alkyl or triphenylmethyl,and including the salts of the compound of formula (I) wherein R.sub.3 is hydrogen, said antibiotic substance having strong antibiotic activity and .beta.-lactamase inhibiting effect, and a method for producing the same by aerobic cultivation of Streptomyces A271.Type: GrantFiled: October 10, 1978Date of Patent: January 11, 1983Assignee: Sanraku-Ocean Co., Ltd.Inventors: Kazuhiko Okamura, Shoji Hirata, Yasushi Okumura, Yasuo Fukagawa, Yasutaka Shimauchi, Tomoyuki Ishikura, Kageaki Kouno, Joseph Lein
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Patent number: 4368265Abstract: Antibiotic X-14868A having the following chemical structure ##STR1## and the pharmaceutically acceptable salts thereof is presented. Also presented is a fermentative method of producing the above antibiotic.Antibiotic X-14868A exhibits anticoccidiostatic activity.Type: GrantFiled: February 23, 1981Date of Patent: January 11, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Chao-Min Liu, Barbara Prosser, John Westley
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Patent number: 4364866Abstract: Antibiotic C-15003 PHO of the formula: ##STR1## wherein R.sub.1 is H, hydroxyl, alkanoyloxy, alkenylcarbonyloxy or arylcarbonyloxy; R.sub.2 is H, hydroxyl or alkanoyloxy; R.sub.3 is H or alkanoyloxy is produced by introducing a hydroxyl group into 15-position of a maytansinoid compound, and, if desired, thus obtained compound is subjected to deacylation or acylation.Antibiotic C-15003 PHO is useful as antiprotozoal or antitumor agent.Type: GrantFiled: September 17, 1980Date of Patent: December 21, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuko Asai, Kazuo Nakahama, Motowo Izawa
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Patent number: 4362663Abstract: Antibiotic C-15003 PND of the formula: ##STR1## wherein R is H or alkanoyl containing not more than 5 carbon atoms is produced by contacting a maytansinoid compound with a culture broth, inclusive of a processed matter derived therefrom, of a microorganism belonging to one of the genera Streptomyces and Chainia which is able to transform said maytansinoid compound into Antibiotic C-15003 PND.Antibiotic C-15003 PND is useful as antitumor, antifungal or antiprotozoal agent.Type: GrantFiled: September 17, 1980Date of Patent: December 7, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Makoto Kida, Motowo Izawa, Kazuo Nakahama
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Patent number: 4362665Abstract: A new antibiotic having .beta.-lactamase inhibitory activity, PA-39504-X.sub.1 of the formula: ##STR1## being useful as a medicament and a veterinary drug for inhibiting the growth of gram-positive and gram-negative pathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces argenteolus PA-39504 or Streptomyces tokunonensis PA-31088 in a suitable medium and recovering PA-39504-X.sub.1 from the cultured broth.Type: GrantFiled: December 1, 1980Date of Patent: December 7, 1982Assignee: Shionogi & Co., Ltd.Inventors: Kentaro Tanaka, Eiji Kondo, Kouichi Matsumoto, Jun'ichi Shoji, Naoki Tsuji
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Patent number: 4362814Abstract: Culturing aerobically Serratia sp. SC 11,482 A.T.C.C. No. 39006 in a culture medium containing assimilable carbon and nitrogen sources yields 1-carba-2-penem-3-carboxylic acid.Type: GrantFiled: December 18, 1981Date of Patent: December 7, 1982Assignee: E. R. Squibb & Sons, Inc.Inventors: Richard B. Sykes, Jerry S. Wells, William L. Parker
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Patent number: 4361650Abstract: Novel demethylmaytansinoids representable by the formula: ##STR1## (wherein X is Cl or H; R.sub.1 is H or acyl group) are produced from maytansinoids by means of enzymic transformation. The demethylmaytansinoids are useful as antifungal, antiprotozoal or antitumor agents.Type: GrantFiled: August 7, 1981Date of Patent: November 30, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuko Asai, Kazuo Nakahama, Motowo Izawa
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Patent number: 4361649Abstract: A new acidic polycyclic ether antibiotic has the formula: ##STR1## and can be prepared by the submerged aerobic propagation in aqueous nutrient media of Streptomyces halstedii ATCC 31812. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis, swine dysentery and theileriosis as well as being effective in promotion of growth in poultry and ruminants.Type: GrantFiled: July 20, 1981Date of Patent: November 30, 1982Assignee: Pfizer Inc.Inventors: Walter D. Celmer, Walter P. Cullen, Riichiro Shibakawa, Junsuke Tone
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Patent number: 4360462Abstract: A novel Antibiotic C-15003 is produced by cultivating a microorganism of the genus Nocardia.The Antibiotic C-15003 is useful as an antifungal agent or an antiprotozoan agent.Type: GrantFiled: October 22, 1981Date of Patent: November 23, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Eiji Higashide, Mitsuko Asai, Seiichi Tanida
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Patent number: 4360595Abstract: A polycyclic antitumor antibiotic designated herein as anandimycin is produced by fermentation of Streptomyces anandii subsp. araffinosus strain C-22,437 (ATCC 31431). Anandimycin possesses antibacterial activity and inhibits the growth of tumors in experimental animals.Type: GrantFiled: February 20, 1981Date of Patent: November 23, 1982Assignee: Bristol-Myers CompanyInventors: David M. Balitz, James A. Bush, Frances A. O'Herron, Donald E. Nettleton, Jr.
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Patent number: 4356265Abstract: Antibiotic C-15003 P-3 is specifically produced by cultivating a microorganism belonging to the genus Nocardia in a culture medium to which isobutyl aldehyde, isobutyl alcohol or a fatty acid ester of isobutyl alcohol is added.The Antibiotic C-15003 P-3 is useful as an antifungal, antiprotozoan or antitumor agent.Type: GrantFiled: November 24, 1980Date of Patent: October 26, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Kazunori Hatano, Masanari Nakamichi, Shun-ichi Akiyama
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Patent number: 4356264Abstract: Zinc complexes of mononitrogen-containing divalent pyrrole ether antibiotics are provided. Such complexes act as coccidiostats and growth-promoting agents when administered to poultry and act as active agents for improving cardiovascular function in animals.Zinc complexes of the type disclosed can be prepared by adding soluble zinc salt to a fermentation beer containing the mononitrogen-containing pyrrole ether antibiotic to thereby form an insoluble, recoverable biomass containing the desired zinc antibiotic complex.Type: GrantFiled: April 11, 1980Date of Patent: October 26, 1982Assignee: International Minerals & Chemical Corp.Inventor: Jerome L. Martin
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Patent number: 4353986Abstract: The present invention teaches a new antibiotic nanaomycin E represented by the formula: ##STR1## Nanaomycin E is active against Gram-positive bacteria, Trichophyton and Mycoplasma and may be used as antibacterial and therapeutic agents for humans and animals. Nanaomycin E is also a useful starting material for the preparation of nanaomycin A which latter nanaomycin has the highest activity among the various nanaomycin-type compounds. Nanaomycin E is produced by fermentation of a microorganism belonging to the genus Streptomyces and capable of producing nanaomycin E, especially Streptomyces rosa variant notoensis (FERM-P 2209; ATCC 31135) and recovering the same from the fermented liquor.Type: GrantFiled: June 22, 1981Date of Patent: October 12, 1982Assignees: Kyowa Hakko Kogyo Kabushiki Kaisha, Kitasato KenkyushoInventors: Satoshi Omura, Haruo Tanaka, Itaru Takahashi, Shinzo Ishii, Kazuyuki Mineura, Kunikatsu Shirahata, Masaji Kasai
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Patent number: 4352934Abstract: There is presented an antibiotic compound of the formula ##STR1## and the pharmaceutically acceptable salts and esters thereof. The compound exhibits activity as an anti-swine dysentery agent and an antimicrobial agent.Also presented is a fermentation process to produce the compound of formula I.Type: GrantFiled: October 14, 1981Date of Patent: October 5, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Chao-Min Liu, Homer D. Tresner, John Westley
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Patent number: 4351769Abstract: Novel antibiotic U-61,732 producible in a fermentation under controlled conditions using a biologically pure culture of the microorganism Saccharopolyspora hirsuta strain 367, NRRL 12045. This antibiotic is active against gram-positive bacteria, for example, Staphylococcus aureus. Also disclosed are the 11-acyl esters of U-61,732. Thus, these compounds can be used in various environments to eradicate or control such bacteria.Type: GrantFiled: August 25, 1980Date of Patent: September 28, 1982Assignee: The Upjohn CompanyInventors: Howard A. Whaley, John H. Coats
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Patent number: 4347184Abstract: A process for separating and recovering coproporphyrin and uroporphyrin from a culture broth containing them, which comprises(1) adjusting the pH of the liquid phase of a cultured broth containing coproporphyrin and uroporphyrin to a range of 2.5 to 4 to form a solid precipitate containing coproporphyrin and uroporphyrin and collecting the precipitate,(2) preparing an aqueous alkaline solution of the solid precipitate obtained in step (1), adjusting the pH of the solution to a range of more than 4 but not over 6, to form a solid precipitate containing coproporphyrin, and collecting the precipitate, and(3) adjusting the pH of the residue left after collection of the precipitate in step (2) to a range of 1 to 4 to form a solid precipitate containing uroporphyrin and collecting the precipitate.The active porphyrin components thus obtained have physiological activity in regulating various organisms of the body, such as, for example, improving the function of the liver.Type: GrantFiled: March 25, 1981Date of Patent: August 31, 1982Assignee: Nippon Oil Company, Ltd.Inventors: Ichiro Kojima, Kenji Maruhashi, Yasuo Fujiwara
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Patent number: 4346171Abstract: A new compound, named "Compound B-41D", has the formula: ##STR1## and can be prepared by cultivating a microorganism of the genus Streptomyces, especially Streptomyces strain B-41-146. Compound B-41D has valuable acaricidal and anthelmintic activities.Type: GrantFiled: August 18, 1980Date of Patent: August 24, 1982Assignee: Sankyo Company, LimitedInventors: Yo Takiguchi, Hiroshi Mishima, Shinjiro Yamamoto, Michiya Terao
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Patent number: 4339535Abstract: Cultivation of a strain of the microorganism Nocardia sp. 11,340, which has been deposited in the American Type Culture Collection as A.T.C.C. No. 31531, yields a novel antibiotic substance EM 4940, having activity against a range of gram-positive and gram-negative bacteria, yeasts, fungi, acholeplasma, and the protozoan Trichomonas vaginalis.Type: GrantFiled: June 30, 1980Date of Patent: July 13, 1982Assignee: E. R. Squibb & Sons, Inc.Inventors: Richard B. Sykes, Jerry S. Wells, Wen-Chih Liu
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Patent number: 4335212Abstract: Disclosed is a fermentation process for preparing and isolating the antibiotic, (5R,6S,8S)-3-(2-aminoethylthio)-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2. 0]hept-2-ene-2-carboxylic acid in substantially pure form.Type: GrantFiled: June 17, 1981Date of Patent: June 15, 1982Assignee: Merck & Co., Inc.Inventors: Kenneth E. Wilson, August J. Kempf
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Patent number: 4335211Abstract: Disclosed are optically active acylated cephalosporin analogs which are useful as antibacterial agents and methods for preparing such compounds.Type: GrantFiled: November 13, 1980Date of Patent: June 15, 1982Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yukio Hashimoto, Seigo Takasawa, Tadashi Hirata, Ikuo Matsukuma, Shigeo Yoshiie
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Patent number: 4334022Abstract: A method for producing mildiomycin in a commercial quantity and at low cost by cultivating a mildiomycin-producing microorganism belonging to Actinomycetes in a culture medium containing an N-methyl compound in an amount of at least 3 mM to have mildiomycin elaborated and accumulated in the culture broth.Type: GrantFiled: June 16, 1980Date of Patent: June 8, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Suzuki, Hidekazu Sawada, Tsunetomo Asai
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Patent number: 4332896Abstract: Optically active cephalosporin analogs are produced by an optically selective acylation reaction. The reaction is carried out in the presence of a microbial enzyme which catalyzes the selective optical acylation. The products thus obtained are useful as antibacterial agents.Type: GrantFiled: April 14, 1980Date of Patent: June 1, 1982Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yukio Hashimoto, Kazuo Kimura, Tadashi Hirata, Takehiro Ogasa, Shigeru Kobayashi, Ikuo Matsukuma
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Patent number: 4331598Abstract: Novel antibiotic C-15003 PHM, which is produced by cultivating a microorganism belonging to the genus Nocardia and being capable of producing antibiotic C-15003 PHM, and novel C-15003 PHM acylate, which is produced by subjecting C-15003 PHM thus obtained to acylation reaction with an acylating agent, have antiprotozoan and antitumor activities.Type: GrantFiled: September 17, 1980Date of Patent: May 25, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Toru Hasegawa, Motowo Izawa, Seiichi Tanida
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Patent number: 4328335Abstract: The C-076 compounds are a series of four pairs of macrolides in which the members of each pair are homologous. The instant processes convert the C-076 A2 and B2 compounds isolated from a fermentation broth into the biologically preferred B1 and A1 compounds or into the dihydro derivatives thereof.Type: GrantFiled: December 15, 1980Date of Patent: May 4, 1982Assignee: Merck & Co., Inc.Inventor: Helmut H. Mrozik
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Patent number: 4322348Abstract: Novel Antibiotic C-15003PND, which has the formula: ##STR1## wherein R represents hydrogen, --CO--CH.sub.3, --CO--CH.sub.2 --CH.sub.3, ##STR2## is produced by cultivating a microorganism of the genus Nocardia. The Antibiotic C-15003PND wherein R is acetyl, propionyl, isobutyryl or isovaleryl is useful for an antifungal, antiprotozoal or antitumor agent and Antibiotic C-15003PND wherein R is hydrogen is useful for an intermediate thereof.Type: GrantFiled: May 14, 1980Date of Patent: March 30, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuko Asai, Motowo Izawa, Seiichi Tanida
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Patent number: 4316958Abstract: Optically active cephalosporin analogs are produced by optically selective deacylation of an optically inactive acylated analog. The compounds are useful as intermediates in the preparation of optically active acylated antimicrobial agents.Type: GrantFiled: February 7, 1980Date of Patent: February 23, 1982Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tadashi Hirata, Yukio Hashimoto, Takehiro Ogasa, Shigeru Kobayashi, Ikuo Matsukuma, Kazuo Kimura
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Patent number: 4316957Abstract: The antibacterial compounds 7-deazaadenosine and 7-deazinosine are produced by fermentation of a new microorganism of the genus Micromonospora. At least one of the active substances is isolated from the culture medium.Type: GrantFiled: April 4, 1978Date of Patent: February 23, 1982Assignee: Abbott LaboratoriesInventors: Takashi Nara, Ryo Okachi, Isao Kawamoto, Tomoyasu Sato, Tetsuo Oka
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Patent number: 4311643Abstract: A process for producing red metal corrinoids comprising reacting yellow metal-free corrinoids having main absorptions .lambda..sub.max of 480 and 290 nm, in a liquid medium, with complex-forming metal ions to give yellow metal corrinoids, and alkalizing said metal corrinoids by treatment with an alkali.Type: GrantFiled: March 4, 1980Date of Patent: January 19, 1982Assignee: Gesellschaft fur Biotechnologische Forschung mbHInventors: Volker Koppenhagen, Gerhard Schlingmann, Bernd Dresow, Ortrud Ebelmann
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Patent number: 4310519Abstract: Novel compounds are produced by the fermentation of a nutrient medium with the previously undescribed microorganism Streptomyces avermitilis. They may be isolated by solvent extraction and chromatographic fractionation techniques. The compounds, which are described generically as C-076 have significant parasiticidal activity. The compounds may be included in compositions for the oral or parenteral administration to animals for the treatment of parasitic infections.Type: GrantFiled: September 8, 1978Date of Patent: January 12, 1982Assignee: Merck & Co., Inc.Inventors: George Albers-Schonberg, Hyman Wallick, Robert E. Ormond, Thomas W. Miller, Richard W. Burg
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Patent number: 4307016Abstract: Novel demethylmaytansinoids representable by the formula: ##STR1## [wherein X is Cl or H; R.sub.1 is H or acyl group] are produced from maytansinoids by means of enzymic transformation. The demethylmaytansinoids are useful as antifungal, antiprotozoal or antitumor agents.Type: GrantFiled: May 27, 1980Date of Patent: December 22, 1981Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuko Asai, Kazuo Nakahama, Motowo Izawa
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Patent number: 4302541Abstract: Optically active cephalosporin analogs are produced by optically selective deacylation of an optically inactive acylated analog. The compounds are useful as intermediates in the preparation of optically active acylated antimicrobial agents.Type: GrantFiled: November 13, 1980Date of Patent: November 24, 1981Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tadashi Hirata, Yukio Hashimoto, Ikuo Matsukuma, Shigeo Yoshiie, Seigo Takasawa
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Patent number: 4302540Abstract: Disclosed are optically active cephalosporin analogs which are produced by optically selective deacylation of an optically inactive acylated analog. The compounds are useful as intermediates in the preparation of optically active acylated antimicrobial agents.Type: GrantFiled: October 24, 1980Date of Patent: November 24, 1981Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tadashi Hirata, Yukio Hashimoto, Takehiro Ogasa, Shigeru Kobayashi, Akira Sato, Kiyoshi Sato, Seigo Takasawa
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Patent number: 4301248Abstract: A known antibiotic substance designated herein as rachelmycin is produced by fermentation of Streptomyces sp. strain C-329, variant 70 (ATCC 31128) or Streptomyces anandii subsp. arraffinosus strain C-22, 437 (ATCC 31431). Rachelmycin exhibits both antibiotic and antitumor properties.Type: GrantFiled: October 6, 1980Date of Patent: November 17, 1981Assignee: Bristol-Myers CompanyInventors: Donald E. Nettleton, Jr., James A. Bush, William T. Bradner
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Patent number: 4299953Abstract: Mycarosyltylactone (5-O-mycarosyl-20-dihydro-20,23-dideoxytylonolide) which has the formula: ##STR1## 3,4'-diacyl ester derivatives of mycarosyltylactone wherein each of said esters is an ester of a monocarboxylic acid or a hemi-ester of a dicarboxylic acid, each of 1 to 18 carbon atoms, and the corresponding 3-acyl ester derivatives of tylactone, are useful intermediates in the preparation of macrolide antibiotics. New methods for making tylactone and the 3-acyl ester derivatives of tylactone are provided.Type: GrantFiled: July 29, 1980Date of Patent: November 10, 1981Assignee: Eli Lilly and CompanyInventors: Robert L. Hamill, Gene M. Wild
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Patent number: 4298692Abstract: New antibiotically active compounds having the basic structure of rifamycin S, namely 3-hydroxyrifamycin S (formula A: X.dbd.>C.dbd.O; R.sup.1 .dbd.OH; R.sup.2 .dbd.H), 3,31-dihydroxyrifamycin S (formula A: X.dbd.>C.dbd.O; R.sup.1 .dbd.R.sup.2 .dbd.OH) and 1-desoxy-1-oxarifamycin S (formula A: X.dbd.--O--; R.sup.1 .dbd.R.sup.2 .dbd.H) ##STR1## are formed by cultivating, under aerobic conditions, a strain of Nocardia mediterranei which is derived from Streptomyces mediterranei ATCC 13 685 as the parent strain and is characterized by the ability to produce at least one of the mentioned compounds. The recombinant strain Nocardia mediterranei DSM 1415 has proved suitable. The mentioned rifamycin S analogues have analogous antibiotic properties to this but have a wider range of action, especially against gram-negative bacteria.Type: GrantFiled: January 17, 1980Date of Patent: November 3, 1981Assignee: Ciba-Geigy CorporationInventors: Thomas Schupp, Peter Traxler, Jakob Nuesch
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Patent number: 4293650Abstract: 37,454 RP of the formula: ##STR1## and its non-toxic salts with metals and nitrogen-containing bases possess anti-coccidial activity.Type: GrantFiled: October 5, 1978Date of Patent: October 6, 1981Assignee: Rhone-Poulenc IndustriesInventors: Jean Florent, Jean Lunel, Denise Mancy
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Patent number: 4292241Abstract: A new antibiotic having .beta.-lactamase inhibitory activity, PA-31088-IV, being useful as a medicament and a veterinary drug for inhibiting the growth of gram-positive and gram-negative phathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces tokunonensis sp. nov. in a suitable medium and recovering PA-31088-IV from the cultured broth.Type: GrantFiled: January 25, 1980Date of Patent: September 29, 1981Assignee: Shionogi & Co., Ltd.Inventors: Kentaro Tanaka, Jun'ichi Shoji, Yoshimi Kawamura, Teruo Hattori, Eiji Kondo, Kouichi Matsumoto, Tadashi Yoshida, Naoki Tsuji
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Patent number: 4289760Abstract: Derivatives of C-076 compounds are described in which the C-076 molecule, a series of macrolides, has the 23-hydroxy group thereof oxidized to the 23-keto group. The 23-keto compounds are prepared by selectively oxidizing the suitably protected 23-hydroxy compound using such oxidizing agents as pyridinium dichromate, chromic acid-dimethyl pyrazole, chromic acid, chromic acid-acetic acid, and the like. Alternatively, selective oxidation of the unprotected 23-hydroxy compound may be accomplished by placing the compound in soil. Further reaction of the oxidized C-076 compounds is also possible. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal, and acaricidal activity. Compositions containing the described C-076 derivatives as the active ingredient thereof are also disclosed.Type: GrantFiled: May 2, 1980Date of Patent: September 15, 1981Assignee: Merck & Co., Inc.Inventors: Helmut H. Mrozik, John G. MacConnell, August J. Kempf
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Patent number: 4288549Abstract: The microorganism Aspergillus nidulans var. roseus NRRL 11440 and the method of producing the A-30912 antibiotics by submerged aerobic fermentation of this microorganism to give the A-42355 antibiotic complex. A-30912 factors A, B, D, and H are separated from the A-42355 complex by chromatography. The A-42355 complex and A-30912 factors A, B, D, and H are antifungal agents.Type: GrantFiled: March 3, 1980Date of Patent: September 8, 1981Assignee: Eli Lilly and CompanyInventors: LaVerne D. Boeck, Ralph E. Kastner
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Patent number: 4287302Abstract: Cultivation of Streptomyces chartreusis NRRL 11407 in the presence of antibiotic A23187 methyl ester produces 16-hydroxy A23187 methyl ester, 16-hydroxy-N-demethyl A23187 methyl ester, and N-demethyl A23187 methyl ester. Hydrolysis of the products affords the corresponding free acids which form dimeric complexes with divalent cations.Type: GrantFiled: July 30, 1980Date of Patent: September 1, 1981Assignee: Eli Lilly and CompanyInventors: Bernard J. Abbott, David S. Fukuda
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Patent number: 4285963Abstract: There are disclosed certain new derivatives of C-076 compounds which have been isolated from the fermentation broth that produced the original C-076 compounds. The compounds retain the C-076 16-membered cyclic backbone, however, the groups attached thereto are considerably modified from the original C-076 compounds. The new compounds have been found to retain the biological activity of the parent C-076 compounds. The compounds are thus potent antiparasitic agents and compositions and methods for such uses are also disclosed.Type: GrantFiled: August 7, 1980Date of Patent: August 25, 1981Assignee: Merck & Co., Inc.Inventors: Byron H. Arison, Robert T. Goegelman, Vincent P. Gullo
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Patent number: 4283493Abstract: A compound of the formula ##STR1## and its pharmaceutically acceptable salts are disclosed. The compound exhibits antibacterial activity, antimalarial activity, has activity as a growth promotant for ruminants and as an agent in the treatment of swine dysentery. Also provided is a process to produce the novel compound.Type: GrantFiled: March 10, 1980Date of Patent: August 11, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Chao-Min Liu, John Westley
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Patent number: 4282322Abstract: This invention relates to two new antibiotics, desacetyl 890A.sub.1 and desacetyl 890A.sub.3, active against both gram-positive and gram-negative bacteria, which are produced by treating 890A.sub.1 and 890A.sub.3, respectively, with an N-acetylthienamycin amidohydrolase produced by a soil microorganism isolated by enrichment techniques. This invention also relates to the process whereby N-acetylated structures of the thienamycin class of antibiotics such as N-acetyl thienamycin can be enzymatically deacetylated.Type: GrantFiled: August 27, 1979Date of Patent: August 4, 1981Assignee: Merck & Co., Inc.Inventors: Jean S. Kahan, Frederick M. Kahan
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Patent number: 4277478Abstract: The invention relates to the new antibiotic Lysolipin including two components X and I, and derivatives thereof. Lysolipin is formed when the strain Streptomyces violaceoniger (Waksman et Curtis) Waksman et Henrici Tu 96, which strain has been deposited under the reference NRRL 8097 at the Northern Regional Laboratory, U.S. Department of Agriculture, Peoria, Illinois, is cultured in a nutrient medium. The structural formulae of the 2 components are ##STR1## Lysolipin I and X and their derivatives have antibacterial activity and are effective against yeast - like fungi, such as Candida albicans. Their antibiotic action probably depends on an inhibition of the cell wall synthesis.Type: GrantFiled: May 21, 1979Date of Patent: July 7, 1981Assignee: Ciba-Geigy CorporationInventors: Hans Zahner, Hannelore Drautz, Walter Keller
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Patent number: 4264736Abstract: The antibiotic MSD 890A.sub.10 and pharmaceutically acceptable salts thereof (hereinafter referred to as antibiotic 890A.sub.10) is active against both gram-positive and gram-negative bacteria. The antibiotic is produced by growing species of Streptomyces on suitable fermentation media.Type: GrantFiled: September 26, 1979Date of Patent: April 28, 1981Assignee: Merck & Co., Inc.Inventors: Patrick J. Cassidy, Sheldon B. Zimmerman, Josefino B. Tunac, Sebastian Hernandez
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Patent number: 4264735Abstract: The antibiotic MSD 890A.sub.9 and pharmaceutically acceptable salts thereof (hereinafter referred to as antibiotic 890A.sub.9) is active against both gram-positive and gram-negative bacteria. The antibiotic is produced by growing species of Streptomyces on suitable fermentation media.Type: GrantFiled: September 10, 1979Date of Patent: April 28, 1981Assignee: Merck & Co., Inc.Inventors: Patrick J. Cassidy, Sheldon B. Zimmerman, Josefino B. Tunac, Sebastian Hernandez
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Patent number: 4264734Abstract: This invention relates to the new antibiotic, desacetyl 890A.sub.10, active against both gram-positive and gram-negative bacteria, which is produced by treating 890A.sub.10 with an N-acetyl-890A.sub.10 amidohydrolase produced by a soil microorganism isolated by enrichment techniques. This invention also relates to the process by which 890A.sub.10 is enzymatically deacetylated.Type: GrantFiled: September 11, 1979Date of Patent: April 28, 1981Assignee: Merck & Co., Inc.Inventors: Jean S. Kahan, Frederick M. Kahan