Additional Acyclic Chalcogen Bonded Directly To The Lactone Ring (e.g., Zearalanone, Etc.) Patents (Class 549/270)
  • Patent number: 5786490
    Abstract: A process for preparing compounds useful as intermediates used for preparing lubricant and fuel additives. The intermediates include the products prepared by the process and dilactones.
    Type: Grant
    Filed: April 10, 1997
    Date of Patent: July 28, 1998
    Assignee: The Lubrizol Corporation
    Inventors: Jeffry G. Dietz, Mark R. Baker, Paul E. Adams
  • Patent number: 5710174
    Abstract: A compound that is useful for inhibiting FXIIIa catalysis of fibrin cross-linking, and related pharmaceutical compositions and methods, are disclosed. The compound and compositions may be advantageously used to enhance fibrinolysis and resolution of blood clots.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 20, 1998
    Assignees: Zymo Genetics, Inc., Novo Nordisk A/S
    Inventors: Robert R. West, Teresa Martinez, Hank R. Franklin, Paul D. Bishop, Birgitte R.o slashed.mer Rassing
  • Patent number: 5696154
    Abstract: Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.
    Type: Grant
    Filed: June 29, 1994
    Date of Patent: December 9, 1997
    Assignees: The United States of America as represented by the Department of Health and Human Services, Starks Associates, Inc.
    Inventors: Louis Malspeis, B. Rao Vishnuvajjala, Jeffrey G. Supko, Charles Theodore Kane, Jr.
  • Patent number: 5688924
    Abstract: The invention relates to derivatives of 12,13-epoxy-tylosin, the novel seynthetic antibiotics from tylosin group and the methods of their preparation. According to this invention hydrogenation followed by oximation of 12,13-epoxy-tylosin derivatives yields the following tylosin derivatives: 10,11-dihydro-12,13-epoxy, respectively 10,11-dihydro-12,13-epoxy oxime.Direct oximation of 12,13-epoxy tylosin derivative gives 12,13-epoxy oxime derivatives of tylosin.
    Type: Grant
    Filed: August 13, 1996
    Date of Patent: November 18, 1997
    Assignee: PLIVA farmaceutska, kemijska, prehrambena i kozmeticka industrija, d.d.
    Inventors: Amalija Narandja, Nevenka Lopotar
  • Patent number: 5593978
    Abstract: A method for promoting growth in fish comprising administering a low level dosage amount of zearalanol to fish. The zearalanol may be conveniently administered to the fish via a novel fish feed formulation comprising a conventional feed mixture supplemented with a relatively low dosage amount of zearalanol ranging from 1 to 20 parts per million (ppm) zearalanol in the feed. In another embodiment, the zearalanol may be administered to the fish in the form of a novel complex of zearalanol and a cyclodextrin compound which further enhances the growth process.
    Type: Grant
    Filed: December 15, 1993
    Date of Patent: January 14, 1997
    Assignee: Mallinckrodt Veterinary, Inc.
    Inventors: Martin J. Jacobs, Fred J. Hart
  • Patent number: 5523418
    Abstract: Macrocylic lactam compounds of formula (i) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the invention, as well as compositions containing the same and methods for their use in stimulating contractile motion of the gastrointestinal tract.
    Type: Grant
    Filed: May 4, 1995
    Date of Patent: June 4, 1996
    Assignee: Abbott Laboratories
    Inventors: Leslie A. Freiberg, Carla Edwards, Richard J. Pariza, Hugh N. Nellans
  • Patent number: 5514662
    Abstract: The invention is directed toward the use of amphotericin B and derivatives thereof as inhibitors of serine-proteases and for applying these inhibitors for the production of medicinal products intended for the treatment of infection by the human immunodeficiency virus (HIV).
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: May 7, 1996
    Assignee: Laboratoires Mayoly Spindler (S.A.R.L.)
    Inventor: Michel Seman
  • Patent number: 5444174
    Abstract: 16-membered macrolide compounds wherein both of hydroxyl groups at the 3"- and 4"-positions form ether bonds together with two alkyl groups which are either the same or different from each other is useful as an antibacterial agent. The macrolide compounds represented by formula (I) are prepared by chemically modifying midecamycin A.sub.3 to obtain a synthesis intermediate of the formula (II), which is further chemically modified.
    Type: Grant
    Filed: February 25, 1993
    Date of Patent: August 22, 1995
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Keiichi Ajito, Kenichi Kurihara, Tsuneo Ishizuka, Tetsuro Hara, Takayuki Usui, Seiji Shibahara
  • Patent number: 5362752
    Abstract: New cholesterol lowering compounds are formed from the photochemical treatment of zaragozic acid A.
    Type: Grant
    Filed: May 17, 1993
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Gregory D. Berger, Leeyuan Huang, John G. MacConnell
  • Patent number: 5256689
    Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents and as inhibitors of squalene synthase.
    Type: Grant
    Filed: October 26, 1992
    Date of Patent: October 26, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Yuan-Ching P. Chiang
  • Patent number: 5210224
    Abstract: A process for preparing a lankacidine carbamate derivative of the formula ##STR1## or a salt thereof, by the reaction of a lankacidine 8-substituted carbonate with an amine, wherein R.sub.1 is a hydroxy group or an alkanoyloxy group; and R.sub.2 and R.sub.3 are each a hydrogen atom, an optionally substituted lower alkyl group, a cycloalkyl group or a phenyl group; or R.sub.2 and R.sub.3 together with an adjacent nitrogen atom to which they bond form an optionally substituted heterocyclic group.
    Type: Grant
    Filed: July 11, 1990
    Date of Patent: May 11, 1993
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Akio Miyake, Tatsuhiko Kawai
  • Patent number: 5210225
    Abstract: A process for producing high purity .alpha.-zeranol from a zeralenone containing surface fermentation product is described. One feature of the process entails fractional crystallization from an aqueous acetonitrile solvent of high purity .alpha.-zeranol from a solution containing a mixture of 50 to 60 parts by weight .alpha.-zeranol and 40 to 50 parts by weight .beta.-zeranol.
    Type: Grant
    Filed: May 7, 1992
    Date of Patent: May 11, 1993
    Assignee: C.R.C. Compagnia di Ricera Chimica S.p.A.
    Inventors: Flavio Moimas, Giuliano Clauti
  • Patent number: 5183924
    Abstract: Derivatives of benzocycloalkenyldihydroxyalkanoic acids, inhibitors of HMG CoA reductase, antagonists of thromboxane A.sub.2 receptors and antifungals, denoted by the formula I ##STR1## in which X=CH.sub.2, O or S; R.sub.1 and R.sub.2, identical or different, =H, C.sub.1-3 alkyl or together form a --(CH.sub.2).sub.n -- chain (n=4,5) optionally substituted symmetrically by one or two C.sub.1-3 alkyl radicals.R.sub.3 and R.sub.4, identical or different, =H, CF.sub.3, halogen (Cl, F, Br), C.sub.1-5 N,N-dialkylamino, C.sub.1-4 alkyl, C.sub.1-5 -alkoxy, C.sub.1-3 alkylthio, or phenyl optionally substituted by at most substituents which may be identical or different and may denote C.sub.1-3 alkyl or C.sub.1-3 alkoxy radicals or halogens (F, Cl), it being understood that when one of R.sub.3 and R.sub.4 denotes the radicals: CF.sub.3, N,N-dialkylamino, C.sub.6 H.sub.5 or substituted phenyl, it is present at the vertices 3', R' or 5' according to formula 1 and the other denotes a hydrogen atom.R.sub.5 and R.sub.
    Type: Grant
    Filed: October 24, 1991
    Date of Patent: February 2, 1993
    Assignee: Lipha, Lyonnaise Industrielle Pharmaceutique
    Inventors: Didier Festal, Jean-Yves Nioche, Denis Descours, Robert Bellemin, Jacques Decerprit
  • Patent number: 5137035
    Abstract: This invention provides a process for the production of novel smoking compositions which contain a benzofuranone flavorant additive, and further provides novel benzofuranone compounds as illustrated by the cis 6-phenyl-3a, 4,5,7a-tetrahydro-2(3H)-benzofuranone: ##STR1## Under normal cigarette smoking conditions, the benzofuranone additive in an invention smoking composition enhances the flavor and aroma of the mainstream and sidestream smoke.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: August 11, 1992
    Assignees: Philip Morris Incorporated, Philip Morris Products Inc.
    Inventor: Kenneth F. Podraza
  • Patent number: 5136056
    Abstract: A process for producing high purity .alpha.-zeranol from a zeralenone containing surface fermentation product is described. One feature of the process entails fractional crystallization from an aqueous acetonitrile solvent of high purity .alpha.-zeranol from a solution containing a mixture of 50 to 60 parts by weight .alpha.-zeranol and 40 to 50 parts by weight .beta.-zeranol.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: August 4, 1992
    Assignee: C.R.C. Compagnia di Ricerca Chimici S.p.A.
    Inventors: Flavio Moimas, Giuliano Clauti
  • Patent number: 5116960
    Abstract: Compounds of formula (I) or salts thereof: ##STR1## wherein: each R.sub.1 is independently hydrogen or a silyl protecting group; R.sub.2 is a carboxylic acid or derivative thereof; a ketone or aldehyde function; hydroxymethyl in which the hydroxyl function is optionally silylated, or substituted by hydroxy C.sub.1-4 alkyl, alkoxy C.sub.1-4 alkyl, alkoxycarbonyl C.sub.1-4 alkyl, hydroxycarbonyl C.sub.1-4 alkyl, alkyl, alkanoyl, or optionally substituted aryl or aroyl; one of X and Y is hydrogen, and the other is a sugar residue; hydroxy; optionally substituted C.sub.1-6 alkoxy or C.sub.3-8 cycloalkoxy; alkanoyloxy; thioalkanoyloxy; sulphonyloxy; halogen; or optionally substituted aryloxy, aralkyloxy or aroyloxy; or X and Y together with the carbon atom to which they are bonded are a carbonyl group or derivative thereof, are provided; their use as chemical intermediates and in the treatment of fungal infections is described.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: May 26, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Michael J. Driver, David T. MacPherson, William S. MacLachlan
  • Patent number: 5089521
    Abstract: New 10-membered ring lactones, a process for the preparation thereof, and the use thereof.It is possible with the aid of Penicillium strains to prepare new 10-membered ring lactones having a pharmacological action.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: February 18, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Joachim Wink, Susanne Grabley, Gerhard Seibert, Klaus Hutter, Axel Zeeck
  • Patent number: 4996229
    Abstract: Scytophycins A, B, C, D and E, an aldehyde and alcohol derivative of scytophycin B and the specified alkanoyl and benzoyl esters of scytophycins A, B, C, D and E and the B derivatives (scytophycin compounds) are novel antineoplastic and antifungal agents. Antifungal compositions containing a scytophycin compound and methods of inhibiting fungi, especially plant pathogenic fungi, using these compositions are included. A method for producing the scytophycin complex, comprising scytophycins A, B, C, D and E, using a new strain of the blue-green alga Scytonema pseudohofmanni, and a biologically purified culture of the alga are also provided.
    Type: Grant
    Filed: August 31, 1989
    Date of Patent: February 26, 1991
    Assignees: University of Hawaii, Eli Lilly and Company
    Inventors: Richard E. Moore, Eiichi Furusawa, Ted R. Norton, Gregory M. L. Patterson, Jon S. Mynderse
  • Patent number: 4994582
    Abstract: This invention relates to an antibiotic NK130119 of the formula: ##STR1## which exhibits antifungal, antitumor, vascularizations-inhibitory and insecticidal activities.
    Type: Grant
    Filed: January 17, 1990
    Date of Patent: February 19, 1991
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Takaaki Nishikiori, Masanori Yamazaki, Seiichi Saito, Nobuyoshi Shimada, Takashi Kurokawa, Kiyonobu Hirose, Takumi Yamashita, Takashi Harada
  • Patent number: 4940726
    Abstract: The isolation and elucidation of novel caffrane macrocyclic lactones denominated "Combretastatin D-1" and "Combretastatin D-2", each of which was found to possess unexpected cell growth inhibitory properties.
    Type: Grant
    Filed: April 26, 1989
    Date of Patent: July 10, 1990
    Assignee: Arizona Board of Regents
    Inventors: George R. Pettit, Sheo B. Singh
  • Patent number: 4914206
    Abstract: The present invention provides lankacidin derivatives of the formula ##STR1## and procedures for the production thereof. The lankacidin derivatives [1] show excellent antimicrobial activities and thus can be used for prophylaxis and treatment of infectious disease in animals.
    Type: Grant
    Filed: December 15, 1988
    Date of Patent: April 3, 1990
    Assignee: Takeda Chemical Industries, LTD.
    Inventors: Isao Minamida, Naoto Hashimoto
  • Patent number: 4914216
    Abstract: Streptomyces parvullus, DSM 3816, produces on aerobic fermentation new antibiotics which are distinguished by antimicrobial activity even after derivatization.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: April 3, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Peter Hammann, Susanne Grabley, Hartmut Voelskow, Burkhard Sachse, Wolfgang Raether, Carlo Giani, Gerhard Seibert
  • Patent number: 4873347
    Abstract: It is possible to prepare the demalonyl compound of macrolide lactones by hydrolysis in the presence of a base without a retro-aldol cleavage occurring.
    Type: Grant
    Filed: December 22, 1987
    Date of Patent: October 10, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Peter Hammann, Susanne Grabley, Wolfgang Raether, Bernd Ciommer, Heinz Kluge, Burkhard Sachse
  • Patent number: 4849447
    Abstract: Compounds having the formula: ##STR1## wherein R.sub.1 is hydrogen, or an alkyl from about 1 to about 3 carbon atoms; R.sub.2 is hydrogen, or an alkyl from about 1 to about 18 carbon atoms; R.sub.3 is keto, or hydroxyl; and R.sub.4 is hydrogen, an alkyl from about 1 to about 4 carbon atoms, hydroxyl, or amino are synthesized and administered to animals as anabolic agents.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: July 18, 1989
    Assignee: Pitman-Moore, Inc.
    Inventor: Martin J. Jacobs
  • Patent number: 4751239
    Abstract: 6' carbonate esters of zearalanol and its derivatives are used to promote growth in ruminants. The compounds have the structural formula: ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are H, X, or COX, where X is an alkyl group having from 1-6 carbon atoms; and R is an alkyl group or a Br or Cl substituted alkyl group having from 1-12 carbon atoms.
    Type: Grant
    Filed: June 29, 1987
    Date of Patent: June 14, 1988
    Assignee: International Minerals & Chemical Corp.
    Inventor: Edward B. Hodge
  • Patent number: 4703128
    Abstract: The feature of the present invention is a process for preparing compounds represented by general formula (Ia) described below: ##STR1## wherein X.sub.1, X.sub.2, X.sub.3, R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are as defined in formula (I) and R.sub.10 represents a lower alkyl group, or acid salts thereof, which process is characterized by using the guanidylfungins (II) as raw materials, reacting these guanidylfungins with alcohols (III) in the presence of an acid catalyst, and then hydrolyzing the malonic acid monoester (IV).
    Type: Grant
    Filed: July 18, 1986
    Date of Patent: October 27, 1987
    Assignee: Takahara Shuzo Co., Ltd.
    Inventors: Teruhiko Beppu, Kazutoh Takesako, Teruya Nakamura, Akira Obayashi
  • Patent number: 4608078
    Abstract: Brefeldin A derivatives of the formula ##STR1## where R is alkyl, unsubstituted or substituted alkanoyl, unsubstituted or substituted aralkyl, unsubstituted or substituted benzoyl, a radical of the formula (R.sup.1 O).sub.2 P(O)-- or a radical R.sup.2 R.sup.3 R.sup.4 Si, and the use of brefeldin A and brefeldin A derivatives of the formula I for combatting unwanted plant growth.
    Type: Grant
    Filed: December 13, 1983
    Date of Patent: August 26, 1986
    Assignee: BASF Aktiengesellschaft
    Inventors: Rolf-Dieter Acker, Rudolf Karl, Bruno Wuerzer
  • Patent number: 4425356
    Abstract: Compound of the formula: ##STR1## wherein R.sup.1 is .dbd.O or ##STR2## and R.sup.2 and R.sup.3 are each hydrogen or carboxylic acid-derived acyl, are effective for prophylaxis or treatment of swine dysentery or for increase of swine productivity.
    Type: Grant
    Filed: November 24, 1981
    Date of Patent: January 10, 1984
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Noriaki Narukawa, Keinosuke Takeda, Toshiyuki Yamazaki
  • Patent number: 4409392
    Abstract: Novel compositions of matter comprising the 6' esters of zearalanol which have utility as growth promoting agents in meat-producing animals, particularly ruminants. The compositions include: zearalanol 6'-butyrate; zearalanol 6'-decanoate; zearalanol 6'-hexanoate; zearalanol 6'-laurate; zearalanol 6'-trichloroacetate; and zearalanol 6'-trifluoroacetate.
    Type: Grant
    Filed: September 3, 1981
    Date of Patent: October 11, 1983
    Assignee: International Minerals & Chemical Corp.
    Inventor: Edward B. Hodge