Both Rings Which Form The Spiro Are Hetero Rings Patents (Class 549/343)
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Publication number: 20150004545Abstract: 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: ApplicationFiled: September 19, 2014Publication date: January 1, 2015Applicant: JSR CORPORATIONInventors: Hayato NAMAI, Norihiko IKEDA, Takanori KAWAKAMI
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Patent number: 8916717Abstract: 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: GrantFiled: May 10, 2007Date of Patent: December 23, 2014Assignee: Consiglio Nazionale Delle RicercheInventors: Antonella DeMico, Andrea Cottarelli, Mariapia Fuggetta, Giulia Lanzilli, Maria Tricarico
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Publication number: 20140371285Abstract: 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: ApplicationFiled: January 7, 2013Publication date: December 18, 2014Inventors: Kevin Sprott, Michael Lewis, Hyeongwook Choi, Frank Fang, Mingde Shan, Tsvetelina I. Lazarova, Lin Li, M. Arshad Siddiqui, Robin Larouche-Gauthier, Alexandre Lemire
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Patent number: 8822528Abstract: 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: GrantFiled: November 16, 2011Date of Patent: September 2, 2014Assignees: 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
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Publication number: 20140171498Abstract: 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: ApplicationFiled: August 6, 2012Publication date: June 19, 2014Applicant: Council of Scientific & Indusrtial ReasearchInventors: Swati Joshi, Roshan Rajan Kulkarni, Ketaki Dilip Shurpali, Sampa Sarkar, Dhiman Sarkar
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Patent number: 8574607Abstract: Compounds of the formula (I) useful as pesticides are disclosed, wherein the substituents are as defined in claim 1.Type: GrantFiled: May 21, 2010Date of Patent: November 5, 2013Assignee: Syngenta Crop Protection, Inc.Inventors: Jürgen Harry Schaetzer, Thomas Pitterna, Long Lu, Yaming Wu, Peter Renold, Francesca Perruccio, Jérome Yves Cassayre, Michel Mueglebach
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Publication number: 20130177950Abstract: 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: ApplicationFiled: August 30, 2011Publication date: July 11, 2013Applicant: RIKENInventors: Hiroyuki Osada, Shunji Takahashi, Makoto Kawatani, Yoshiyuki Sakaki, Atsushi Toyoda
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Publication number: 20130041106Abstract: 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: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Inventors: Erin E. Carlson, Darci Trader, Antoinette Odendaal
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Patent number: 8350062Abstract: The present invention provides bistramide analogs useful for treating various types of cancer.Type: GrantFiled: February 17, 2010Date of Patent: January 8, 2013Assignee: The University of ChicagoInventors: Sergey A. Kozmin, Syed Rizvi
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Publication number: 20120128722Abstract: 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: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Jean Delaveau, Emile Vialle, Marc Lemaire, Stephane Pellet-Rostaing, Bruno Andrioletti
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Patent number: 8048496Abstract: 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: GrantFiled: September 25, 2009Date of Patent: November 1, 2011Assignee: JNC CorporationInventors: Maiko Itoh, Yoshiharu Hirai, Junichi Inagaki, Daisuke Ootsuki
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Publication number: 20110082303Abstract: 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: ApplicationFiled: September 22, 2010Publication date: April 7, 2011Applicant: Alpharma Inc.Inventor: Robert Sheridan
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Publication number: 20100227919Abstract: 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: ApplicationFiled: May 10, 2007Publication date: September 9, 2010Inventors: Antonella DeMico, Andrea Cottarelli, Mariapia Fuggetta, Giulia Lanzilli, Maria Tricarico
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Publication number: 20100217019Abstract: The present invention provides a novel bistramide analog useful for treating various types of cancer.Type: ApplicationFiled: February 17, 2010Publication date: August 26, 2010Inventors: Sergey A. Kozmin, Syed Rizvi
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Publication number: 20080153901Abstract: 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: ApplicationFiled: December 10, 2007Publication date: June 26, 2008Applicant: GALDERMA S.A.Inventors: Alexandre Kaoukhov, Colette Pernin
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Patent number: 7323577Abstract: 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 optType: GrantFiled: February 22, 2006Date of Patent: January 29, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Hiroyuki Tawada, Makoto Yamashita, Yujiro Ono
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Patent number: 7169940Abstract: 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: GrantFiled: October 31, 2000Date of Patent: January 30, 2007Assignee: NST Neurosurvival Technologies Ltd.Inventor: Ilan Ziv
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Patent number: 6512003Abstract: 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: GrantFiled: October 9, 2001Date of Patent: January 28, 2003Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Chen Mao, He Huang
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Patent number: 6335364Abstract: 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: GrantFiled: June 29, 1999Date of Patent: January 1, 2002Assignee: Parker Hughes InstituteInventors: Faith M. Uckun, Chen Mao, He Huang
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Patent number: 6310091Abstract: 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: GrantFiled: September 14, 2000Date of Patent: October 30, 2001Assignees: 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
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Patent number: 6166034Abstract: 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: GrantFiled: May 8, 1998Date of Patent: December 26, 2000Assignee: SmithKline Beecham p. l. cInventor: Francis David King
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Patent number: 6147076Abstract: 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: GrantFiled: November 15, 1996Date of Patent: November 14, 2000Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New YorkInventors: Samuel J. Danishefsky, Kristopher Depew, Stephen P. Marsden, William Bornmann, Ting Chao Chou, Andrej Zatorski
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Patent number: 6121274Abstract: 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: GrantFiled: April 4, 1997Date of Patent: September 19, 2000Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventors: Wolf-Rudiger Ulrich, Ulrich Thibaut
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Patent number: 5874592Abstract: 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: GrantFiled: November 12, 1997Date of Patent: February 23, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Takeo Tanaka, Fumito Koizumi, Tsutomu Agatsuma, Hidemasa Kondo, Yutaka Saitoh, Katsuhiko Ando, Yuzuru Matsuda
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Patent number: 5693524Abstract: 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: GrantFiled: June 6, 1995Date of Patent: December 2, 1997Assignee: Pfizer Inc.Inventor: Edward J. Tynan, III
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Patent number: 5646308Abstract: 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: GrantFiled: July 18, 1994Date of Patent: July 8, 1997Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Hiroyuki Nabata
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Patent number: 5494931Abstract: 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: GrantFiled: December 6, 1994Date of Patent: February 27, 1996Assignee: Pfizer Inc.Inventors: Walter P. Cullen, John P. Dirlam, Hiroshi Maeda, Junsuke Tone
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Patent number: 5432193Abstract: This invention relates to antibiotic LL-D37187.alpha. derived from the microorganism Streptomyces which is useful as an antibacterial agent.Type: GrantFiled: May 14, 1993Date of Patent: July 11, 1995Assignee: American Cyanamid CompanyInventors: Guy T. Carter, Gerhard Schlingmann, David P. Labeda, Joseph J. Goodman
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Patent number: 5328929Abstract: 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: GrantFiled: July 2, 1993Date of Patent: July 12, 1994Assignee: Arizona Board of RegentsInventors: George R. Pettit, Zbigniew A. Cichacz, Cherry L. Herald
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Patent number: 5322854Abstract: 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: GrantFiled: February 6, 1992Date of Patent: June 21, 1994Assignees: Rikagaku Kenkyusho, Snow Brand Milk Products Co., Ltd.Inventors: Kiyoshi Isono, Hiroyuki Osada, Hidetoshi Takahashi, Gosei Kawanishi
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Patent number: 5298524Abstract: 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: GrantFiled: March 27, 1992Date of Patent: March 29, 1994Assignee: Pfizer Inc.Inventors: John P. Dirlam, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
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Patent number: 5217993Abstract: 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: GrantFiled: July 20, 1992Date of Patent: June 8, 1993Assignee: Eli Lilly and CompanyInventor: George O. P. O'Doherty
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Patent number: 5215981Abstract: 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: GrantFiled: July 1, 1991Date of Patent: June 1, 1993Assignees: Hokko Chemical Industry Co., Ltd., Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Yoshikazu Takahashi, Masa Hamada, Hiroshi Naganawa, Kiyoshi Sato
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Patent number: 5206263Abstract: 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: GrantFiled: December 5, 1989Date of Patent: April 27, 1993Assignee: Pfizer Inc.Inventors: John P. Dirlam, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
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Patent number: 5180665Abstract: 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: GrantFiled: November 21, 1990Date of Patent: January 19, 1993Assignee: Her Majesty the Queen in right of Canada, as represented by The National Research Council of CanadaInventor: Charles Holmes
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Patent number: 5102906Abstract: 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: GrantFiled: October 31, 1990Date of Patent: April 7, 1992Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Shigenobu Nakayama, Fumiaki Ikeda
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Patent number: 5096905Abstract: 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: GrantFiled: September 14, 1989Date of Patent: March 17, 1992Assignee: Hoechst AktiengesellschaftInventors: Gerhard Kretzschmar, Peter Hammann, Dieter Duwel, Gerhard Wohner, Rudiger Marquardt, Klaus Kuhlein
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Patent number: 5095127Abstract: 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: GrantFiled: December 17, 1990Date of Patent: March 10, 1992Assignee: Pfizer Inc.Inventors: Alexander C. Goudie, Nigel D. A. Walshe
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Patent number: 5064855Abstract: 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: GrantFiled: January 28, 1991Date of Patent: November 12, 1991Assignee: Pfizer Inc.Inventors: Walter P. Cullen, James R. Hauske, Gloria J. Kostek, Hiroshi Maeda, Junsuke Tone
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Patent number: 5064856Abstract: Compound of formulae (I) and (II) are HMG-CoA synthase inhibitors and exhibit antifungal activity.Type: GrantFiled: July 31, 1989Date of Patent: November 12, 1991Assignee: 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
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Patent number: 5043353Abstract: 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: GrantFiled: October 10, 1989Date of Patent: August 27, 1991Assignee: Eli Lilly and CompanyInventors: Raymond C. Yao, Robert L. Hamill
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Patent number: 5011845Abstract: 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: GrantFiled: June 13, 1990Date of Patent: April 30, 1991Assignee: Schering CorporationInventors: David J. Blythin, Ho-Jane Shue, Ashit K. Ganguly
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Patent number: 4977280Abstract: 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: GrantFiled: December 27, 1989Date of Patent: December 11, 1990Assignee: SanofiInventors: Franz Jansen, Pierre Gros
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Patent number: 4929638Abstract: 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: GrantFiled: May 25, 1989Date of Patent: May 29, 1990Assignee: Pfizer Inc.Inventors: Christopher Dutton, David Perry
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Patent number: 4820758Abstract: 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: GrantFiled: May 6, 1987Date of Patent: April 11, 1989Assignee: The Upjohn CompanyInventor: Stephen J. Nelson
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Patent number: 4804680Abstract: 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: GrantFiled: July 21, 1987Date of Patent: February 14, 1989Assignee: Pfizer Inc.Inventors: Alexander C. Goudie, Nigel D. A. Walshe
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Patent number: 4707493Abstract: 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: GrantFiled: November 17, 1986Date of Patent: November 17, 1987Assignee: Pfizer Inc.Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, John C. Ruddock, Junsuke Tone
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Patent number: 4686297Abstract: 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: GrantFiled: July 22, 1985Date of Patent: August 11, 1987Assignee: The Upjohn CompanyInventor: Stephen J. Nelson
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Patent number: 4680419Abstract: 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: GrantFiled: July 22, 1985Date of Patent: July 14, 1987Assignee: The Upjohn CompanyInventor: Stephen J. Nelson
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Patent number: 4625041Abstract: 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: GrantFiled: August 29, 1985Date of Patent: November 25, 1986Assignee: Pfizer Inc.Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone