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)
  • Patent number: 4371617
    Abstract: 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: Grant
    Filed: March 18, 1981
    Date of Patent: February 1, 1983
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kentaro Tanaka, Naoki Tsuji, Eiji Kondo, Yoshimi Kawamura
  • Patent number: 4370415
    Abstract: 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: Grant
    Filed: November 7, 1980
    Date of Patent: January 25, 1983
    Assignee: Nippon Oil Company, Ltd.
    Inventors: Ichiro Kojima, Kenji Maruhashi, Yasuo Fujiwara
  • Patent number: 4369252
    Abstract: 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: Grant
    Filed: February 6, 1981
    Date of Patent: January 18, 1983
    Assignee: 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
  • Patent number: 4368203
    Abstract: 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: Grant
    Filed: October 10, 1978
    Date of Patent: January 11, 1983
    Assignee: Sanraku-Ocean Co., Ltd.
    Inventors: Kazuhiko Okamura, Shoji Hirata, Yasushi Okumura, Yasuo Fukagawa, Yasutaka Shimauchi, Tomoyuki Ishikura, Kageaki Kouno, Joseph Lein
  • Patent number: 4368265
    Abstract: 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: Grant
    Filed: February 23, 1981
    Date of Patent: January 11, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chao-Min Liu, Barbara Prosser, John Westley
  • Patent number: 4364866
    Abstract: 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: Grant
    Filed: September 17, 1980
    Date of Patent: December 21, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuko Asai, Kazuo Nakahama, Motowo Izawa
  • Patent number: 4362663
    Abstract: 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: Grant
    Filed: September 17, 1980
    Date of Patent: December 7, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Makoto Kida, Motowo Izawa, Kazuo Nakahama
  • Patent number: 4362665
    Abstract: 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: Grant
    Filed: December 1, 1980
    Date of Patent: December 7, 1982
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kentaro Tanaka, Eiji Kondo, Kouichi Matsumoto, Jun'ichi Shoji, Naoki Tsuji
  • Patent number: 4362814
    Abstract: 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: Grant
    Filed: December 18, 1981
    Date of Patent: December 7, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard B. Sykes, Jerry S. Wells, William L. Parker
  • Patent number: 4361650
    Abstract: 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: Grant
    Filed: August 7, 1981
    Date of Patent: November 30, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuko Asai, Kazuo Nakahama, Motowo Izawa
  • Patent number: 4361649
    Abstract: 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: Grant
    Filed: July 20, 1981
    Date of Patent: November 30, 1982
    Assignee: Pfizer Inc.
    Inventors: Walter D. Celmer, Walter P. Cullen, Riichiro Shibakawa, Junsuke Tone
  • Patent number: 4360462
    Abstract: 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: Grant
    Filed: October 22, 1981
    Date of Patent: November 23, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Eiji Higashide, Mitsuko Asai, Seiichi Tanida
  • Patent number: 4360595
    Abstract: 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: Grant
    Filed: February 20, 1981
    Date of Patent: November 23, 1982
    Assignee: Bristol-Myers Company
    Inventors: David M. Balitz, James A. Bush, Frances A. O'Herron, Donald E. Nettleton, Jr.
  • Patent number: 4356265
    Abstract: 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: Grant
    Filed: November 24, 1980
    Date of Patent: October 26, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kazunori Hatano, Masanari Nakamichi, Shun-ichi Akiyama
  • Patent number: 4356264
    Abstract: 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: Grant
    Filed: April 11, 1980
    Date of Patent: October 26, 1982
    Assignee: International Minerals & Chemical Corp.
    Inventor: Jerome L. Martin
  • Patent number: 4353986
    Abstract: 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: Grant
    Filed: June 22, 1981
    Date of Patent: October 12, 1982
    Assignees: Kyowa Hakko Kogyo Kabushiki Kaisha, Kitasato Kenkyusho
    Inventors: Satoshi Omura, Haruo Tanaka, Itaru Takahashi, Shinzo Ishii, Kazuyuki Mineura, Kunikatsu Shirahata, Masaji Kasai
  • Patent number: 4352934
    Abstract: 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: Grant
    Filed: October 14, 1981
    Date of Patent: October 5, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chao-Min Liu, Homer D. Tresner, John Westley
  • Patent number: 4351769
    Abstract: 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: Grant
    Filed: August 25, 1980
    Date of Patent: September 28, 1982
    Assignee: The Upjohn Company
    Inventors: Howard A. Whaley, John H. Coats
  • Patent number: 4347184
    Abstract: 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: Grant
    Filed: March 25, 1981
    Date of Patent: August 31, 1982
    Assignee: Nippon Oil Company, Ltd.
    Inventors: Ichiro Kojima, Kenji Maruhashi, Yasuo Fujiwara
  • Patent number: 4346171
    Abstract: 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: Grant
    Filed: August 18, 1980
    Date of Patent: August 24, 1982
    Assignee: Sankyo Company, Limited
    Inventors: Yo Takiguchi, Hiroshi Mishima, Shinjiro Yamamoto, Michiya Terao
  • Patent number: 4339535
    Abstract: 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: Grant
    Filed: June 30, 1980
    Date of Patent: July 13, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard B. Sykes, Jerry S. Wells, Wen-Chih Liu
  • Patent number: 4335212
    Abstract: 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: Grant
    Filed: June 17, 1981
    Date of Patent: June 15, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth E. Wilson, August J. Kempf
  • Patent number: 4335211
    Abstract: Disclosed are optically active acylated cephalosporin analogs which are useful as antibacterial agents and methods for preparing such compounds.
    Type: Grant
    Filed: November 13, 1980
    Date of Patent: June 15, 1982
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yukio Hashimoto, Seigo Takasawa, Tadashi Hirata, Ikuo Matsukuma, Shigeo Yoshiie
  • Patent number: 4334022
    Abstract: 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: Grant
    Filed: June 16, 1980
    Date of Patent: June 8, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Suzuki, Hidekazu Sawada, Tsunetomo Asai
  • Patent number: 4332896
    Abstract: 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: Grant
    Filed: April 14, 1980
    Date of Patent: June 1, 1982
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yukio Hashimoto, Kazuo Kimura, Tadashi Hirata, Takehiro Ogasa, Shigeru Kobayashi, Ikuo Matsukuma
  • Patent number: 4331598
    Abstract: 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: Grant
    Filed: September 17, 1980
    Date of Patent: May 25, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Toru Hasegawa, Motowo Izawa, Seiichi Tanida
  • Patent number: 4328335
    Abstract: 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: Grant
    Filed: December 15, 1980
    Date of Patent: May 4, 1982
    Assignee: Merck & Co., Inc.
    Inventor: Helmut H. Mrozik
  • Patent number: 4322348
    Abstract: 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: Grant
    Filed: May 14, 1980
    Date of Patent: March 30, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuko Asai, Motowo Izawa, Seiichi Tanida
  • Patent number: 4316958
    Abstract: 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: Grant
    Filed: February 7, 1980
    Date of Patent: February 23, 1982
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Tadashi Hirata, Yukio Hashimoto, Takehiro Ogasa, Shigeru Kobayashi, Ikuo Matsukuma, Kazuo Kimura
  • Patent number: 4316957
    Abstract: 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: Grant
    Filed: April 4, 1978
    Date of Patent: February 23, 1982
    Assignee: Abbott Laboratories
    Inventors: Takashi Nara, Ryo Okachi, Isao Kawamoto, Tomoyasu Sato, Tetsuo Oka
  • Patent number: 4311643
    Abstract: 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: Grant
    Filed: March 4, 1980
    Date of Patent: January 19, 1982
    Assignee: Gesellschaft fur Biotechnologische Forschung mbH
    Inventors: Volker Koppenhagen, Gerhard Schlingmann, Bernd Dresow, Ortrud Ebelmann
  • Patent number: 4310519
    Abstract: 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: Grant
    Filed: September 8, 1978
    Date of Patent: January 12, 1982
    Assignee: Merck & Co., Inc.
    Inventors: George Albers-Schonberg, Hyman Wallick, Robert E. Ormond, Thomas W. Miller, Richard W. Burg
  • Patent number: 4307016
    Abstract: 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: Grant
    Filed: May 27, 1980
    Date of Patent: December 22, 1981
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuko Asai, Kazuo Nakahama, Motowo Izawa
  • Patent number: 4302541
    Abstract: 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: Grant
    Filed: November 13, 1980
    Date of Patent: November 24, 1981
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Tadashi Hirata, Yukio Hashimoto, Ikuo Matsukuma, Shigeo Yoshiie, Seigo Takasawa
  • Patent number: 4302540
    Abstract: 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: Grant
    Filed: October 24, 1980
    Date of Patent: November 24, 1981
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Tadashi Hirata, Yukio Hashimoto, Takehiro Ogasa, Shigeru Kobayashi, Akira Sato, Kiyoshi Sato, Seigo Takasawa
  • Patent number: 4301248
    Abstract: 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: Grant
    Filed: October 6, 1980
    Date of Patent: November 17, 1981
    Assignee: Bristol-Myers Company
    Inventors: Donald E. Nettleton, Jr., James A. Bush, William T. Bradner
  • Patent number: 4299953
    Abstract: 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: Grant
    Filed: July 29, 1980
    Date of Patent: November 10, 1981
    Assignee: Eli Lilly and Company
    Inventors: Robert L. Hamill, Gene M. Wild
  • Patent number: 4298692
    Abstract: 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: Grant
    Filed: January 17, 1980
    Date of Patent: November 3, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Thomas Schupp, Peter Traxler, Jakob Nuesch
  • Patent number: 4293650
    Abstract: 37,454 RP of the formula: ##STR1## and its non-toxic salts with metals and nitrogen-containing bases possess anti-coccidial activity.
    Type: Grant
    Filed: October 5, 1978
    Date of Patent: October 6, 1981
    Assignee: Rhone-Poulenc Industries
    Inventors: Jean Florent, Jean Lunel, Denise Mancy
  • Patent number: 4292241
    Abstract: 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: Grant
    Filed: January 25, 1980
    Date of Patent: September 29, 1981
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kentaro Tanaka, Jun'ichi Shoji, Yoshimi Kawamura, Teruo Hattori, Eiji Kondo, Kouichi Matsumoto, Tadashi Yoshida, Naoki Tsuji
  • Patent number: 4289760
    Abstract: 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: Grant
    Filed: May 2, 1980
    Date of Patent: September 15, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Helmut H. Mrozik, John G. MacConnell, August J. Kempf
  • Patent number: 4288549
    Abstract: 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: Grant
    Filed: March 3, 1980
    Date of Patent: September 8, 1981
    Assignee: Eli Lilly and Company
    Inventors: LaVerne D. Boeck, Ralph E. Kastner
  • Patent number: 4287302
    Abstract: 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: Grant
    Filed: July 30, 1980
    Date of Patent: September 1, 1981
    Assignee: Eli Lilly and Company
    Inventors: Bernard J. Abbott, David S. Fukuda
  • Patent number: 4285963
    Abstract: 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: Grant
    Filed: August 7, 1980
    Date of Patent: August 25, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Robert T. Goegelman, Vincent P. Gullo
  • Patent number: 4283493
    Abstract: 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: Grant
    Filed: March 10, 1980
    Date of Patent: August 11, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chao-Min Liu, John Westley
  • Patent number: 4282322
    Abstract: 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: Grant
    Filed: August 27, 1979
    Date of Patent: August 4, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Jean S. Kahan, Frederick M. Kahan
  • Patent number: 4277478
    Abstract: 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: Grant
    Filed: May 21, 1979
    Date of Patent: July 7, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Zahner, Hannelore Drautz, Walter Keller
  • Patent number: 4264736
    Abstract: 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: Grant
    Filed: September 26, 1979
    Date of Patent: April 28, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Patrick J. Cassidy, Sheldon B. Zimmerman, Josefino B. Tunac, Sebastian Hernandez
  • Patent number: 4264735
    Abstract: 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: Grant
    Filed: September 10, 1979
    Date of Patent: April 28, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Patrick J. Cassidy, Sheldon B. Zimmerman, Josefino B. Tunac, Sebastian Hernandez
  • Patent number: 4264734
    Abstract: 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: Grant
    Filed: September 11, 1979
    Date of Patent: April 28, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Jean S. Kahan, Frederick M. Kahan