Both Rings Which Form The Spiro Are Hetero Rings Patents (Class 549/343)
  • Publication number: 20150004545
    Abstract: A photoresist composition containing (A) a polymer having a structural unit (I) that includes an acid-labile group, and (I) a compound represented by the following formula (1). In the following formula (1), R1, R2, R3 and R represent a hydrogen atom or a monovalent organic group having 1 to 20 carbon atoms. X represents a single bond, an oxygen atom or —NRa—. Ra represents a hydrogen atom, a hydroxy group or a monovalent organic group having 1 to 20 carbon atoms, and optionally taken together represents a ring structure by binding with R each other. A? represents —SO3? or —CO2?. M+ represents a monovalent onium cation.
    Type: Application
    Filed: September 19, 2014
    Publication date: January 1, 2015
    Applicant: JSR CORPORATION
    Inventors: Hayato NAMAI, Norihiko IKEDA, Takanori KAWAKAMI
  • Patent number: 8916717
    Abstract: The invention relates to dioxaspiroketal derivatives of formula (I): wherein R, is selected from the group consisting of H, straight or branched chain C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, cycloalkyl, heterocyclyl, phenyl, optionally para-, meta- or ortho-substituted with 0 to 3 substituent selected from halogen, —CN, —NH2, —OH, —NO2, COOR2, wherein R2 is selected from H and C1-C6 alkyl, n is 1 or 2, X is O or S, R1 is selected from H, OH, halogen, C1-C6 alkyl, C1-C6 alkoxy, COOR3, wherein R3 is selected from H and C1-C6 alkyl, or physiologically acceptable salts thereof, process for preparation thereof, their uses in medical field, in particular as anti-tumor medicaments.
    Type: Grant
    Filed: May 10, 2007
    Date of Patent: December 23, 2014
    Assignee: Consiglio Nazionale Delle Ricerche
    Inventors: Antonella DeMico, Andrea Cottarelli, Mariapia Fuggetta, Giulia Lanzilli, Maria Tricarico
  • Publication number: 20140371285
    Abstract: Salinomycin analogs and pharmaceutically acceptable compositions containing salinomycin analogs. Dosage forms and kits comprising salinomycin analogs and pharmaceutically acceptable compositions containing salinomycin analogs. Methods of using salinomycin analogs, pharmaceutically acceptable compositions, dosage forms, and kits for the treatment of proliferative diseases, e.g.
    Type: Application
    Filed: January 7, 2013
    Publication date: December 18, 2014
    Inventors: Kevin Sprott, Michael Lewis, Hyeongwook Choi, Frank Fang, Mingde Shan, Tsvetelina I. Lazarova, Lin Li, M. Arshad Siddiqui, Robin Larouche-Gauthier, Alexandre Lemire
  • Patent number: 8822528
    Abstract: This invention relates to novel polyether ionophores, formulations comprising same, and to methods of making and using these compounds and formulations for the treatment and/or prevention of parasitic infection in animals and humans. These compounds exhibit improved safety profiles and/or efficacies as compared to parent compounds.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: September 2, 2014
    Assignees: Merial Limited, Universite Claude Bernard Lyon 1, Centre National de la Recherche Scientifique (CNRS)
    Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
  • Publication number: 20140171498
    Abstract: This invention relates to diterpenes of general formula (1) belonging to labdane class, isolated from Leucas stelligera, being useful for prevention, treatment, inhibition or controlling growth and proliferation of mycobacterial activity in mammals. The invention further discloses process for isolation of the fractions containing the same.
    Type: Application
    Filed: August 6, 2012
    Publication date: June 19, 2014
    Applicant: Council of Scientific & Indusrtial Reasearch
    Inventors: Swati Joshi, Roshan Rajan Kulkarni, Ketaki Dilip Shurpali, Sampa Sarkar, Dhiman Sarkar
  • Patent number: 8574607
    Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: November 5, 2013
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
  • Publication number: 20130177950
    Abstract: A bacterium belonging to the genus Streptomyces having an ability to produce reveromycin A or a synthetic intermediate thereof, the bacterium being modified so as to increase expression of revQ gene coding for the amino acid sequence of SEQ ID NO: 36 or an amino acid sequence having an identity of not less than 80% to SEQ ID NO: 36 as compared with a parent strain, thereby the above-mentioned production ability is increased as compared with the parent strain.
    Type: Application
    Filed: August 30, 2011
    Publication date: July 11, 2013
    Applicant: RIKEN
    Inventors: Hiroyuki Osada, Shunji Takahashi, Makoto Kawatani, Yoshiyuki Sakaki, Atsushi Toyoda
  • Publication number: 20130041106
    Abstract: Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.
    Type: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Inventors: Erin E. Carlson, Darci Trader, Antoinette Odendaal
  • Patent number: 8350062
    Abstract: The present invention provides bistramide analogs useful for treating various types of cancer.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: January 8, 2013
    Assignee: The University of Chicago
    Inventors: Sergey A. Kozmin, Syed Rizvi
  • Publication number: 20120128722
    Abstract: This invention relates to novel polyether ionophores, formulations comprising same, and to methods of making and using these compounds and formulations for the treatment and/or prevention of parasitic infection in animals and humans. These compounds exhibit improved safety profiles and/or efficacies as compared to parent compounds.
    Type: Application
    Filed: November 16, 2011
    Publication date: May 24, 2012
    Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
  • Patent number: 8048496
    Abstract: The purpose the invention is to provide a polymerizable liquid crystal compound which has an excellent solubility with other compounds, a high homeotropic property, and a spirobiindan-backbone, and a liquid crystal composition comprising this compound. The purpose is attained with a polymerizable liquid crystal compound represented by Formula (1). A polymer which is excellent in many characteristics can be obtained from this compound and a formed body having optical anisotropy, produced from this polymer can be obtained. In Formula (1), G is a single bond or oxygen; R is hydrogen, methyl (Me) or a group represented by Formula (a), wherein at least two of R are groups represented by Formula (a); P is a polymerizable group represented by any of Formula (P1) to Formula (P8). In Formula (a), a desirable A is 1,4-cyclohexylene or 1,4-phenylene; Z is a bonding group; m is an integer of 0 to 3; X0 is a single bond or alkylene; Z0 is a single bond, —O—, —OCO—, or —OCOO—; X is a single bond or alkylene.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: November 1, 2011
    Assignee: JNC Corporation
    Inventors: Maiko Itoh, Yoshiharu Hirai, Junichi Inagaki, Daisuke Ootsuki
  • Publication number: 20110082303
    Abstract: Improved process for the isolation of laidlomycin from a fermentation broth includes increasing the pH of the fermentation broth and centrifuging the pH adjusted fermentation broth, resulting in an aqueous layer and a wet solid layer containing laidlomycin. After the aqueous layer is removed, the wet solid layer containing laidlomycin is dried. The process provides an efficient and high yielding method.
    Type: Application
    Filed: September 22, 2010
    Publication date: April 7, 2011
    Applicant: Alpharma Inc.
    Inventor: Robert Sheridan
  • Publication number: 20100227919
    Abstract: The invention relates to dioxaspiroketal derivatives of formula (I): wherein R, is selected from the group consisting of H, straight or branched chain C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, cycloalkyl, heterocyclyl, phenyl, optionally para-, meta- or ortho-substituted with 0 to 3 substituent selected from halogen, —CN, —NH2, —OH, —NO2, COOR2, wherein R2 is selected from H and C1-C6 alkyl, n is 1 or 2, X is O or S, R1 is selected from H, OH, halogen, C1-C6 alkyl, C1-C6 alkoxy, COOR3, wherein R3 is selected from H and C1-C6 alkyl, or physiologically acceptable salts thereof, process for preparation thereof, their uses in medical field, in particular as anti-tumour medicaments.
    Type: Application
    Filed: May 10, 2007
    Publication date: September 9, 2010
    Inventors: Antonella DeMico, Andrea Cottarelli, Mariapia Fuggetta, Giulia Lanzilli, Maria Tricarico
  • Publication number: 20100217019
    Abstract: The present invention provides a novel bistramide analog useful for treating various types of cancer.
    Type: Application
    Filed: February 17, 2010
    Publication date: August 26, 2010
    Inventors: Sergey A. Kozmin, Syed Rizvi
  • Publication number: 20080153901
    Abstract: The invention relates to a pharmaceutical composition, especially a dermatological composition, containing, in a physiologically acceptable medium, at least one compound of the avermectin family, and benzoyl peroxide, and also to its use for the manufacture of a medicament for treating skin conditions, especially rosacea.
    Type: Application
    Filed: December 10, 2007
    Publication date: June 26, 2008
    Applicant: GALDERMA S.A.
    Inventors: Alexandre Kaoukhov, Colette Pernin
  • Patent number: 7323577
    Abstract: A novel process for efficiently and easily producing a compound represented by the formula: wherein ring A is a benzene ring that may be optionally further substituted in addition to the group represented by W, or a salt thereof; which comprises reacting a compound represented by the formula: wherein R1 and R2 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, Y is a halogen atom, ring A is a benzene ring that may be optionally further substituted in addition to the group represented by Y and ring B is an optionally substituted benzene ring, or a salt thereof, with a compound represented by the formula: WH wherein W is wherein ring C is an optionally substituted benzene ring, ring D is an optionally substituted 5- to 7-membered nitrogen-containing heterocyclic ring, R3 is a hydrogen atom, an aliphatic hydrocarbon group containing an aromatic group or an acyl group, and R4 is a hydrogen atom, an opt
    Type: Grant
    Filed: February 22, 2006
    Date of Patent: January 29, 2008
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Hiroyuki Tawada, Makoto Yamashita, Yujiro Ono
  • Patent number: 7169940
    Abstract: NST 400 compounds consisting of a unit for partial coordination of Ca2+ ions (CPCU). The NST 400 compounds are optionally conjugated to another pharmaceutically active compound. The compounds and conjugates can be used for affinity filters and for binding negative charged phospholipids. The compounds and conjugates can also be used for treating diseases involving changes of cell membrane asymmetry.
    Type: Grant
    Filed: October 31, 2000
    Date of Patent: January 30, 2007
    Assignee: NST Neurosurvival Technologies Ltd.
    Inventor: Ilan Ziv
  • Patent number: 6512003
    Abstract: Novel tubulin binding compounds (SPIKETS) having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel SP binding pocket on tubulin, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: January 28, 2003
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Chen Mao, He Huang
  • Patent number: 6335364
    Abstract: Novel tubulin binding compounds (SPIKETS) having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel SP binding pocket on tubulin, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: January 1, 2002
    Assignee: Parker Hughes Institute
    Inventors: Faith M. Uckun, Chen Mao, He Huang
  • Patent number: 6310091
    Abstract: A novel antifungal compound, “CAY-1”, was isolated from the dried fruit of Capsicum frutescens (cayenne pepper), purified to homogeneity, and characterized as a novel sterol glycoside (a saponin) with a molecular mass of 1243.35 Da. CAY-1 demonstrates antifungal activity against a large variety of fungal organisms associated with diseases in plants, animals and humans including, but not limited to, Aspergillus flavus, A. fumigatus, A. parasiticus, A. niger, Pneumocystis carnii and Candida albicans, but has minimal toxic effects on mammalian cells.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: October 30, 2001
    Assignees: The United States of America as represented by the Secretary of Agriculture, Mycologics, Inc.
    Inventors: Anthony J. De Lucca, II, John M. Bland, Craig B. Vigo, Claude P. Selitrennikoff
  • Patent number: 6166034
    Abstract: Novel spiro piperdine derivatives of formula (I), in which P.sup.1, P.sup.2, R.sup.1, R.sup.2, R.sup.2 ', R.sup.3, m, A, E, G, X, Y, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 have the meanings defined in claim 1 are described, as well as their use for preparing medicaments which have 5HT1D receptor antagonist activity.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: December 26, 2000
    Assignee: SmithKline Beecham p. l. c
    Inventor: Francis David King
  • Patent number: 6147076
    Abstract: The present invention provides a compound having the structure: ##STR1## wherein R.sub.1 R.sub.6 and R.sub.7 are independently hydrogen, OH, NH.sub.2, SH, halogen, C.sub.1 -C.sub.9 linear or branched chain alkyl, alkylmercapto, alkylamino, dialkylamino, alkoxy, phenyl, etc.; wherein R.sub.0 and R.sub.2 are independently hydrogen, OH, linear or branched chain alkyl, --CR.sub.3 R.sub.3 --CH(O)CH.sub.2, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.3, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.2 OH, --CR.sub.3 R.sub.3 --CH(OH)R.sub.4 or --CR.sub.3 R.sub.3 --CH.dbd.CHR.sub.4 ; wherein R.sub.3 and R.sub.4 are independently hydrogen, halogen, C.sub.1 -C.sub.9 linear or branched chain alkyl, phenyl, etc.; wherein R.sub.5 is hydrogen, C.sub.1 -C.sub.9 linear or branched chain alkyl, phenyl, etc.; and wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.9 linear or branched chain acyl, benzoyl, etc.; with the proviso that (a) when R.sub.2 is --CR.sub.3 R.sub.3 --CH(O)CH.sub.2, --CR.sub.3 R.sub.3 --CH.sub.2 CH.sub.3, --CR.sub.3 R.sub.3 --CH.
    Type: Grant
    Filed: November 15, 1996
    Date of Patent: November 14, 2000
    Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New York
    Inventors: Samuel J. Danishefsky, Kristopher Depew, Stephen P. Marsden, William Bornmann, Ting Chao Chou, Andrej Zatorski
  • Patent number: 6121274
    Abstract: The invention concerns componuds of formula (I), in which R1, R2, R3 and R4 have the meanings given in the description. The compounds are novel, effective PDE-inhibitors.
    Type: Grant
    Filed: April 4, 1997
    Date of Patent: September 19, 2000
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventors: Wolf-Rudiger Ulrich, Ulrich Thibaut
  • Patent number: 5874592
    Abstract: The present invention relates to a novel compound EI-2128-1 having IL-1 production inhibitory activity which is represented by formula (I): ##STR1##
    Type: Grant
    Filed: November 12, 1997
    Date of Patent: February 23, 1999
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Takeo Tanaka, Fumito Koizumi, Tsutomu Agatsuma, Hidemasa Kondo, Yutaka Saitoh, Katsuhiko Ando, Yuzuru Matsuda
  • Patent number: 5693524
    Abstract: Actinomadura roseorufa mutants characterized by the ability to produce by fermentation UK-61,689, an acidic polycyclic ether anticoccidial antibiotic previously available only by selective acid hydrolysis of UK-58,852; and Actinomadura roseorufa having the identifying characteristics of ATCC 53,666, ATCC 53,665, ATCC 53,664 and ATCC 53,674.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 2, 1997
    Assignee: Pfizer Inc.
    Inventor: Edward J. Tynan, III
  • Patent number: 5646308
    Abstract: Benzopyran derivatives represented by formula (I): ##STR1## wherein X represents .dbd.O, .dbd.S, .dbd.N--Z, etc. (Z represents a lower alkyl group, etc.); Y represents a substituted amino group, an alkoxy group, an alkylthio group, etc., and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 each represents a hydrogen atom, a lower alkyl group, etc, are disclosed. The benzopyran derivative exhibit K.sup.+ channel opening activities and are widely applicable as antiasthmatics, antiepileptics, and the like.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: July 8, 1997
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroshi Koga, Hiroyuki Nabata
  • Patent number: 5494931
    Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 55080. This novel antibiotic is useful as an anticoccidial in poultry, in the prevention and treatment of swine dysentery and as a growth promotant in cattle and swine.
    Type: Grant
    Filed: December 6, 1994
    Date of Patent: February 27, 1996
    Assignee: Pfizer Inc.
    Inventors: Walter P. Cullen, John P. Dirlam, Hiroshi Maeda, Junsuke Tone
  • Patent number: 5432193
    Abstract: This invention relates to antibiotic LL-D37187.alpha. derived from the microorganism Streptomyces which is useful as an antibacterial agent.
    Type: Grant
    Filed: May 14, 1993
    Date of Patent: July 11, 1995
    Assignee: American Cyanamid Company
    Inventors: Guy T. Carter, Gerhard Schlingmann, David P. Labeda, Joseph J. Goodman
  • Patent number: 5328929
    Abstract: A black Spongia sp. in the Porifera class Demospongiae has been found to contain two new and exceptionally active cell (human cancer) growth inhibitors named spongistatin 2 and spongistatin 3. A bright colored Southwest Indian Ocean sponge Spirastrella spinispirulifera has also been found to contain related human cancer cell growth inhibitors named spongistatin 4 and spongistatin 6. A method of treating human cancer cells with spongistatin 1, spongistatin 2, spongistatin 3, spongistatin 4 and spongistatin 6 is also disclosed. The approximate mean GI.sub.50 of the disclosed compounds in the NCI cell line panel is about 10.sup.-10 .mu.g/ml.
    Type: Grant
    Filed: July 2, 1993
    Date of Patent: July 12, 1994
    Assignee: Arizona Board of Regents
    Inventors: George R. Pettit, Zbigniew A. Cichacz, Cherry L. Herald
  • Patent number: 5322854
    Abstract: A novel antibiotic Reveromycin A represented by the following formula: ##STR1## and a process for preparing said antibiotic which comprises the steps of cultivating a strain which belongs to genus Streptomyces and produces the antibiotic Reveromycin A, and recovering the antibiotic Reveromycin A from the culture product are provided. The antibiotic is useful for its anti-leukemia and antifungal activities.
    Type: Grant
    Filed: February 6, 1992
    Date of Patent: June 21, 1994
    Assignees: Rikagaku Kenkyusho, Snow Brand Milk Products Co., Ltd.
    Inventors: Kiyoshi Isono, Hiroyuki Osada, Hidetoshi Takahashi, Gosei Kawanishi
  • Patent number: 5298524
    Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 53764. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, and as a growth promotant in cattle and swine.
    Type: Grant
    Filed: March 27, 1992
    Date of Patent: March 29, 1994
    Assignee: Pfizer Inc.
    Inventors: John P. Dirlam, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
  • Patent number: 5217993
    Abstract: The present invention is directed to a class of novel C-25-monohydrazine derivatives, and C-25, C-26-bishydrazine derivatives, of the polyether monensin. The derivatives are useful in animal husbandry.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: June 8, 1993
    Assignee: Eli Lilly and Company
    Inventor: George O. P. O'Doherty
  • Patent number: 5215981
    Abstract: In this invention, a new microbial strain which is a strain of Actinomycetes and belongs to the genus Actinomadura, namely Actinomadura sp. MI215-NF3 strain is cultured, and MI215-NF3 substance, a novel antibiotic classifiable as a polyether antibiotic, is recovered from the resultant culture. MI215-NF3 substance and its salts obtained according to this invention are useful for therapeutic treatment of chicken coccidiosis and also have useful antibacterial activities against certain species of bacteria.
    Type: Grant
    Filed: July 1, 1991
    Date of Patent: June 1, 1993
    Assignees: Hokko Chemical Industry Co., Ltd., Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Tomio Takeuchi, Yoshikazu Takahashi, Masa Hamada, Hiroshi Naganawa, Kiyoshi Sato
  • Patent number: 5206263
    Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Streptomyces hygroscopicus ATCC 53626. This novel antibiotic is useful as an anticoccidial in chickens and as a growth promotant in cattle and swine.
    Type: Grant
    Filed: December 5, 1989
    Date of Patent: April 27, 1993
    Assignee: Pfizer Inc.
    Inventors: John P. Dirlam, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
  • Patent number: 5180665
    Abstract: The present invention relates to a method for quantitatively assaying the presence of DSP toxins such as okadaic acid and dinophysistoxin-1 in marine samples. The method comprises the steps of preparing a marine extract, fractionating the prepared marine extract and selecting the extract fraction containing the toxin to be assayed. Once the desired extract fraction has been selected, a labelled substrate for protein phosphatase and at least one protein phosphatase are added to the extract in an assay. The amount of toxin present is quantitatively measured by the ability of the extract fraction to inhibit catalysis, mainly dephosphorylation, of the labelled substrate by protein phosphatases, such as phosphatase-1 (PP1) or phosphatase-2A (PP2A). Preferably, the method of the present invention is used to assay the presence of okadaic acid in marine organisms such as mussels, oysters, scallops, phytoplankton and the like.
    Type: Grant
    Filed: November 21, 1990
    Date of Patent: January 19, 1993
    Assignee: Her Majesty the Queen in right of Canada, as represented by The National Research Council of Canada
    Inventor: Charles Holmes
  • Patent number: 5102906
    Abstract: Catechol derivatives which relate to the production of nerve growth factor in particular tissues of brain are disclosed.Methods for the synthesis, data on the physiological activity, and data on the toxicity of these derivatives as well as examples of preparation for their administration are also disclosed.The disclosed derivatives provide preventive and remedial effect for regressive disorders in the central nervous system including senile dementia of Alzheimer type.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: April 7, 1992
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Shigenobu Nakayama, Fumiaki Ikeda
  • Patent number: 5096905
    Abstract: The invention relates to elaiophylin derivatives of the formulae (I), (I'), (III) and (III') ##STR1## in which the C.dbd.C double bonds in the 2,3 and 4,5 position may also be hydrogenated and in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings indicated. The invention furthermore relates to a process for the preparation of these elaiophylin derivatives, and the use thereof as pharmaceuticals, in particular as anthelmintic pharmaceuticals.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: March 17, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Kretzschmar, Peter Hammann, Dieter Duwel, Gerhard Wohner, Rudiger Marquardt, Klaus Kuhlein
  • Patent number: 5095127
    Abstract: A new acidic polycyclic antibiotic UK-61,689 has the formula: ##STR1## or a pharmaceutically acceptable cationic salt thereof. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis and swine dysentery as well as being effective in promotion of growth and/or improving efficiency of feed utilization in swine and ruminants.
    Type: Grant
    Filed: December 17, 1990
    Date of Patent: March 10, 1992
    Assignee: Pfizer Inc.
    Inventors: Alexander C. Goudie, Nigel D. A. Walshe
  • Patent number: 5064855
    Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Streptomyces sp. ATCC 53862. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, and as a growth promotant in cattle and swine.
    Type: Grant
    Filed: January 28, 1991
    Date of Patent: November 12, 1991
    Assignee: Pfizer Inc.
    Inventors: Walter P. Cullen, James R. Hauske, Gloria J. Kostek, Hiroshi Maeda, Junsuke Tone
  • Patent number: 5064856
    Abstract: Compound of formulae (I) and (II) are HMG-CoA synthase inhibitors and exhibit antifungal activity.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: November 12, 1991
    Assignee: Merck & Co., Inc.
    Inventors: George M. Garrity, Robert Giacobbe, Michael D. Greenspan, Otto D. Hensens, Henry Joshua, Maria T. D. Matas, Isabel Martin, James A. Milligan, Sagrario M. del Val, Walter Rozdilsky, Janet C. Onishi, Jerrold M. Liesch
  • Patent number: 5043353
    Abstract: New polyether antibiotic A80789, its acyl ester, alkyl ester, and alkyl ether derivatives, and salts thereof, are useful as antibacterial and anticoccidial agents and increase feed-utilization efficiency in animals. Methods of making A80789 by culture of Streptomyces hygroscopicus NRRL 18513, and combinations of the A80789 compounds with nicarbazin, 4,4'-dinitrocarbanilide, certain napthalenamine and benzenamine compounds and are also provided.
    Type: Grant
    Filed: October 10, 1989
    Date of Patent: August 27, 1991
    Assignee: Eli Lilly and Company
    Inventors: Raymond C. Yao, Robert L. Hamill
  • Patent number: 5011845
    Abstract: Compounds of the formula ##STR1## wherein R.sup.5 represents C.sub.1 to C.sub.6 -alkyl or the group--(CH.sub.2).sub.n --Z--(CH.sub.2).sub.m --Ar wherein Z represents O, S or --CH.sub.2 --and Ar is phenyl, optionally substituted by one or two groups selected from the group consisting of hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.2, CF.sub.3, CN, R.sup.6 -S(O).sub.x, R.sup.7 --CO--,(R.sup.8 R.sup.9)NCO-and phenyl, wherein x is 0, 1 or 2, and each R.sup.6, R.sup.7, R.sup.8 and R.sup.9 is independently C.sub.1 to C.sub.6 alkyl or two adjacent groups on Ar may form together an additional fused benzenoid ring; n and m independently represent integers of from 1 to 8; and ring Q represents one of the rings Q.sub.1, Q.sub.2, Q.sub.3 or Q.sub.4 below: ##STR2## X is N or C--R.sup.1 ; Y is N or C--R.sup.4 ;W represents O or S;each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently selected from hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.
    Type: Grant
    Filed: June 13, 1990
    Date of Patent: April 30, 1991
    Assignee: Schering Corporation
    Inventors: David J. Blythin, Ho-Jane Shue, Ashit K. Ganguly
  • Patent number: 4977280
    Abstract: The present invention relates to conjugates in which a monovalent carboxylic ionophore is associated by means of a covalent bond with a macromolecule chosen from antibodies, fragments of antibodies, proteins such as peptide hormones or human proteins, and peptide ligands. It also relates to the activated ionophores.These conjugates are suitable as immunotoxin potentiators.
    Type: Grant
    Filed: December 27, 1989
    Date of Patent: December 11, 1990
    Assignee: Sanofi
    Inventors: Franz Jansen, Pierre Gros
  • Patent number: 4929638
    Abstract: Antiparasitic milbemycin derivatives having at the C.25 position a substituted 2-propenyl group --C(CH.sub.3).dbd.CH--R.sup.2 wherein R.sup.2 is a C.sub.3 -C.sub.8 alkyl, alkenyl or alkynyl group which may optionally contain an oxygen or sulphur atom as part of the chain, or a C.sub.3 -C.sub.8 cycloalkyl or cycloalkenyl group, or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may optionally be substituted by one or more alkyl groups or halogen atoms; and process for their preparation.
    Type: Grant
    Filed: May 25, 1989
    Date of Patent: May 29, 1990
    Assignee: Pfizer Inc.
    Inventors: Christopher Dutton, David Perry
  • Patent number: 4820758
    Abstract: This invention pertains to a new method for killing and controlling worms (Helminths), new formulations for killing and controlling worms in animals, new chemical compounds, and a new synthesis of northern hemisphere intermediates for the synthesis of milbemycin and avermectin macrolides.
    Type: Grant
    Filed: May 6, 1987
    Date of Patent: April 11, 1989
    Assignee: The Upjohn Company
    Inventor: Stephen J. Nelson
  • Patent number: 4804680
    Abstract: A new acidic polycyclic antibiotic UK-61,689 has the formula: ##STR1## or a pharmaceutically acceptable cationic salt thereof. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis and swine dysentery as well as being effective in promotion of growth and/or improving efficiency of feed utilization in swine and ruminants.
    Type: Grant
    Filed: July 21, 1987
    Date of Patent: February 14, 1989
    Assignee: Pfizer Inc.
    Inventors: Alexander C. Goudie, Nigel D. A. Walshe
  • Patent number: 4707493
    Abstract: Antibiotic 19-epi-dianemycin, process for its preparation by fermenting a new strain of Streptomyces hygroscopicus, and isolation from the fermentation broth; and its use as an anticoccidial agent and antibacterial agent against gram-positive bacteria.
    Type: Grant
    Filed: November 17, 1986
    Date of Patent: November 17, 1987
    Assignee: Pfizer Inc.
    Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, John C. Ruddock, Junsuke Tone
  • Patent number: 4686297
    Abstract: This invention pertains to a new method for killing and controlling worms (Helminths), new formulations for killing and controlling worms in animals, new chemical compounds, and a new synthesis of northern hemisphere intermediates for the synthesis of milbemycin and avermectin macrolides.
    Type: Grant
    Filed: July 22, 1985
    Date of Patent: August 11, 1987
    Assignee: The Upjohn Company
    Inventor: Stephen J. Nelson
  • Patent number: 4680419
    Abstract: This invention pertains to a new method for killing and controlling worms (Helminths), new formulations for killing and controlling worms in animals, new chemical compounds, and a new synthesis of northern hemisphere intermediates for the synthesis of milbemycin and avermectin macrolides.
    Type: Grant
    Filed: July 22, 1985
    Date of Patent: July 14, 1987
    Assignee: The Upjohn Company
    Inventor: Stephen J. Nelson
  • Patent number: 4625041
    Abstract: A new acidic polycyclic ether antibiotic, CP-63,517, having the formula: ##STR1## and cationic salts thereof produced by submerged aerobic propagation of Streptomyces endus subsp. aureus, ATCC-39574, a new strain of microorganism isolated from a soil sample in Japan, a process for producing this antibiotic and methods for its use to improve feed utilization, promote growth of cattle and swine and to control coccidiosis.
    Type: Grant
    Filed: August 29, 1985
    Date of Patent: November 25, 1986
    Assignee: Pfizer Inc.
    Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone