Additional Acyclic Chalcogen Bonded Directly To The Lactone Ring (e.g., Zearalanone, Etc.) Patents (Class 549/270)
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Patent number: 5786490Abstract: 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: GrantFiled: April 10, 1997Date of Patent: July 28, 1998Assignee: The Lubrizol CorporationInventors: Jeffry G. Dietz, Mark R. Baker, Paul E. Adams
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Patent number: 5710174Abstract: 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: GrantFiled: June 7, 1995Date of Patent: January 20, 1998Assignees: Zymo Genetics, Inc., Novo Nordisk A/SInventors: Robert R. West, Teresa Martinez, Hank R. Franklin, Paul D. Bishop, Birgitte R.o slashed.mer Rassing
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Patent number: 5696154Abstract: 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: GrantFiled: June 29, 1994Date of Patent: December 9, 1997Assignees: 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.
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Patent number: 5688924Abstract: 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: GrantFiled: August 13, 1996Date of Patent: November 18, 1997Assignee: PLIVA farmaceutska, kemijska, prehrambena i kozmeticka industrija, d.d.Inventors: Amalija Narandja, Nevenka Lopotar
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Patent number: 5593978Abstract: 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: GrantFiled: December 15, 1993Date of Patent: January 14, 1997Assignee: Mallinckrodt Veterinary, Inc.Inventors: Martin J. Jacobs, Fred J. Hart
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Patent number: 5523418Abstract: 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: GrantFiled: May 4, 1995Date of Patent: June 4, 1996Assignee: Abbott LaboratoriesInventors: Leslie A. Freiberg, Carla Edwards, Richard J. Pariza, Hugh N. Nellans
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Patent number: 5514662Abstract: 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: GrantFiled: November 15, 1993Date of Patent: May 7, 1996Assignee: Laboratoires Mayoly Spindler (S.A.R.L.)Inventor: Michel Seman
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Patent number: 5444174Abstract: 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: GrantFiled: February 25, 1993Date of Patent: August 22, 1995Assignee: Meiji Seika Kaisha, Ltd.Inventors: Keiichi Ajito, Kenichi Kurihara, Tsuneo Ishizuka, Tetsuro Hara, Takayuki Usui, Seiji Shibahara
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Patent number: 5362752Abstract: New cholesterol lowering compounds are formed from the photochemical treatment of zaragozic acid A.Type: GrantFiled: May 17, 1993Date of Patent: November 8, 1994Assignee: Merck & Co., Inc.Inventors: Byron H. Arison, Gregory D. Berger, Leeyuan Huang, John G. MacConnell
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Patent number: 5256689Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents and as inhibitors of squalene synthase.Type: GrantFiled: October 26, 1992Date of Patent: October 26, 1993Assignee: Merck & Co., Inc.Inventor: Yuan-Ching P. Chiang
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Patent number: 5210224Abstract: 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: GrantFiled: July 11, 1990Date of Patent: May 11, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Tatsuhiko Kawai
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Patent number: 5210225Abstract: 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: GrantFiled: May 7, 1992Date of Patent: May 11, 1993Assignee: C.R.C. Compagnia di Ricera Chimica S.p.A.Inventors: Flavio Moimas, Giuliano Clauti
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Patent number: 5183924Abstract: 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: GrantFiled: October 24, 1991Date of Patent: February 2, 1993Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Didier Festal, Jean-Yves Nioche, Denis Descours, Robert Bellemin, Jacques Decerprit
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Patent number: 5137035Abstract: 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: GrantFiled: March 21, 1990Date of Patent: August 11, 1992Assignees: Philip Morris Incorporated, Philip Morris Products Inc.Inventor: Kenneth F. Podraza
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Patent number: 5136056Abstract: 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: GrantFiled: November 16, 1990Date of Patent: August 4, 1992Assignee: C.R.C. Compagnia di Ricerca Chimici S.p.A.Inventors: Flavio Moimas, Giuliano Clauti
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Patent number: 5116960Abstract: 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: GrantFiled: June 9, 1989Date of Patent: May 26, 1992Assignee: Beecham Group p.l.c.Inventors: Michael J. Driver, David T. MacPherson, William S. MacLachlan
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Patent number: 5089521Abstract: 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: GrantFiled: August 3, 1990Date of Patent: February 18, 1992Assignee: Hoechst AktiengesellschaftInventors: Joachim Wink, Susanne Grabley, Gerhard Seibert, Klaus Hutter, Axel Zeeck
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Patent number: 4996229Abstract: 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: GrantFiled: August 31, 1989Date of Patent: February 26, 1991Assignees: University of Hawaii, Eli Lilly and CompanyInventors: Richard E. Moore, Eiichi Furusawa, Ted R. Norton, Gregory M. L. Patterson, Jon S. Mynderse
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Patent number: 4994582Abstract: This invention relates to an antibiotic NK130119 of the formula: ##STR1## which exhibits antifungal, antitumor, vascularizations-inhibitory and insecticidal activities.Type: GrantFiled: January 17, 1990Date of Patent: February 19, 1991Assignee: Nippon Kayaku Kabushiki KaishaInventors: Takaaki Nishikiori, Masanori Yamazaki, Seiichi Saito, Nobuyoshi Shimada, Takashi Kurokawa, Kiyonobu Hirose, Takumi Yamashita, Takashi Harada
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Patent number: 4940726Abstract: 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: GrantFiled: April 26, 1989Date of Patent: July 10, 1990Assignee: Arizona Board of RegentsInventors: George R. Pettit, Sheo B. Singh
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Patent number: 4914206Abstract: 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: GrantFiled: December 15, 1988Date of Patent: April 3, 1990Assignee: Takeda Chemical Industries, LTD.Inventors: Isao Minamida, Naoto Hashimoto
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Patent number: 4914216Abstract: Streptomyces parvullus, DSM 3816, produces on aerobic fermentation new antibiotics which are distinguished by antimicrobial activity even after derivatization.Type: GrantFiled: December 22, 1987Date of Patent: April 3, 1990Assignee: Hoechst AktiengesellschaftInventors: Peter Hammann, Susanne Grabley, Hartmut Voelskow, Burkhard Sachse, Wolfgang Raether, Carlo Giani, Gerhard Seibert
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Patent number: 4873347Abstract: 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: GrantFiled: December 22, 1987Date of Patent: October 10, 1989Assignee: Hoechst AktiengesellschaftInventors: Peter Hammann, Susanne Grabley, Wolfgang Raether, Bernd Ciommer, Heinz Kluge, Burkhard Sachse
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Patent number: 4849447Abstract: 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: GrantFiled: October 13, 1987Date of Patent: July 18, 1989Assignee: Pitman-Moore, Inc.Inventor: Martin J. Jacobs
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Patent number: 4751239Abstract: 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: GrantFiled: June 29, 1987Date of Patent: June 14, 1988Assignee: International Minerals & Chemical Corp.Inventor: Edward B. Hodge
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Patent number: 4703128Abstract: 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: GrantFiled: July 18, 1986Date of Patent: October 27, 1987Assignee: Takahara Shuzo Co., Ltd.Inventors: Teruhiko Beppu, Kazutoh Takesako, Teruya Nakamura, Akira Obayashi
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Patent number: 4608078Abstract: 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: GrantFiled: December 13, 1983Date of Patent: August 26, 1986Assignee: BASF AktiengesellschaftInventors: Rolf-Dieter Acker, Rudolf Karl, Bruno Wuerzer
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Patent number: 4425356Abstract: 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: GrantFiled: November 24, 1981Date of Patent: January 10, 1984Assignee: Takeda Chemical Industries, Ltd.Inventors: Noriaki Narukawa, Keinosuke Takeda, Toshiyuki Yamazaki
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Patent number: 4409392Abstract: 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: GrantFiled: September 3, 1981Date of Patent: October 11, 1983Assignee: International Minerals & Chemical Corp.Inventor: Edward B. Hodge