Additional Acyclic Chalcogen Bonded Directly To The Lactone Ring (e.g., Zearalanone, Etc.) Patents (Class 549/270)
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Patent number: 9095545Abstract: There is disclosed herein a composition for treating gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers' diarrhea, chronic idiopathic nausea, IBD-associated constipation and diarrhea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinson's disease, MS, Alzheimer's Disease, Motor Neurone Disease or autism, the composition comprising: (i) at least two anti-Clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (ii) at least one anti-Clostridial agent selected from the above combined with an opioid blocking agent.Type: GrantFiled: July 7, 2014Date of Patent: August 4, 2015Inventor: Thomas Julius Borody
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Publication number: 20150018566Abstract: The invention provides combretastatin A-4 like compounds that are modified to have enhanced tubulin binding activity and in some embodiments the ability to promote accumulation in the vasculature undergoing angiogenesis (homing activity). The compounds are based on the combretastatin A-4 skeletal structure having a tubulin-binding pharmacophore comprising two fused rings (A and B rings) in which the B ring is substituted with (a) an aromatic ring structure (C ring) and (b) a second substituent/functional group that comes off the B ring. The aromatic ring structure is typically a six membered ring phenolic or aniline structure, or may also be a fused ring structure such as a substituted or unsubstituted naphthalene.Type: ApplicationFiled: August 27, 2012Publication date: January 15, 2015Inventors: John Jarlath Walsh, Richard Shah, Emmet Martin McCormack, Gillian Joy Hudson, Martina White, Gary Daniel Stack, Brian William Moran, Adrian Coogan, Elaine Carmel Breen
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Patent number: 8674120Abstract: This invention is directed generally to a process for producing Zeranol that eliminates high pressure and high temperature hydrogenations and provides high selectivity for Zeranol at improved yields.Type: GrantFiled: November 3, 2009Date of Patent: March 18, 2014Assignee: Intervet International B.V.Inventors: John Richard Bethell, Gary Robert Reid, Krista Marie Affleck, Tibor Breining
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Patent number: 8513440Abstract: Disclosed are novel analogues of the natural product radicicol A of formulae I, .Ia, pi, Ha, lib and HI, pharmaceutical compositions comprising the compounds. The compounds of the invention are kinase and phosphatase inhibitors and find utility in the treatment or prevention of kinase and phosphatase-mediated disorders. Also provided are uses and methods for the treatment or prevention of kinase- and phosphatase-mediated disorders and synthetic processes for the preparation of the compounds.Type: GrantFiled: June 5, 2008Date of Patent: August 20, 2013Assignees: Universite de Strasbourg, Centre National de la Recherche ScientifiqueInventors: Nicolas Winssinger, Sofia Barluenga
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Publication number: 20130211103Abstract: Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R1-R12 are as defined herein.Type: ApplicationFiled: January 3, 2013Publication date: August 15, 2013Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventor: EISAI R&D MANAGEMENT CO., LTD.
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Publication number: 20130196987Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.Type: ApplicationFiled: October 30, 2012Publication date: August 1, 2013Applicant: EISAI CO., LTD.Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-Andre Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
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Publication number: 20130053434Abstract: The present invention provides new compounds having a kinase inhibitory activity and useful for treating cancer.Type: ApplicationFiled: September 28, 2010Publication date: February 28, 2013Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURGInventors: Nicolas Winssinger, Sofia Barluenga
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Patent number: 8383785Abstract: The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit superior antibacterial properties, particularly against Haemophilus influenzae. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: GrantFiled: May 8, 2009Date of Patent: February 26, 2013Assignee: Enanta Pharmaceuticals, Inc.Inventors: Rajesh Iyengar, Yanchun Wang, Ly Tam Phan, Yat Sun Or
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Publication number: 20130029325Abstract: A method which can isolate plasma cells and plasmablasts efficiently and with high purity, from mammals and birds, without using a cell surface marker is provided. Further disclosed is a fluorescent probe wherein the staining selectivity for the endoplasmic reticulum of cells is higher than the staining selectivity for cell organelles other than the endoplasmic reticulum. Also disclosed is a method for identifying plasma cells and plasmablasts which includes staining cells derived from lymph node tissue or similar by using this probe, and identifying plasma cells and plasmablasts on the basis of the fluorescence intensity from the stained cells. Also disclosed is a fluorescent probe wherein the staining selectivity for cell nuclei is higher than the staining selectivity for cell organelles other than the cell nuclei.Type: ApplicationFiled: March 22, 2011Publication date: January 31, 2013Applicant: NATIONAL UNIVERSITY CORPORATION UNIVERSITY OF TOYAMAInventors: Nobuyuki Kurosawa, Masaharu Isobe
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Patent number: 8350059Abstract: Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R1-R12 are as defined herein.Type: GrantFiled: December 8, 2008Date of Patent: January 8, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Roch Boivin, Silvio A. Campagna, Hong Du, Francis G. Fang, Thomas Horstmann, Charles-Andre Lemelin, Jing Li, Pamela McGuinness, Xiang Niu, Matthew J. Schnaderbeck, Kevin (kuo-ming) Wu, Xiaojie (jeff) Zhu
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Publication number: 20120016137Abstract: This invention is directed generally to a process for producing Zeranol that eliminates high pressure and high temperature hydrogenations and provides high selectivity for Zeranol at improved yields.Type: ApplicationFiled: November 3, 2009Publication date: January 19, 2012Inventors: John Richard Bethell, Gary Robert Reid, Krista Marie Affleck, Tibor Breining
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Patent number: 8071793Abstract: Disclosed are: a novel dinoflagellate alga; and a macrolide compound which can be used as a novel anticancer agent. Specifically disclosed is a macrolide compound produced by a dinoflagellate Amphidinium sp. Strain HYA002 or HYA0024. The macrolide compound has excellent proliferation-inhibiting effect against a human tumor cell and therefore can be used as a novel anticancer agent.Type: GrantFiled: December 19, 2007Date of Patent: December 6, 2011Assignee: National University Corporation Hokkaido UniversityInventors: Masashi Tsuda, Keiko Oguchi, Rie Iwamoto, Yumiko Okamoto
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Publication number: 20110237805Abstract: Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R1-R12 are as defined herein.Type: ApplicationFiled: December 8, 2008Publication date: September 29, 2011Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Roch Boivin, Silvio A. Campagna, Hong Du, Francis G. Fang, Thomas Horstmann, Charles-Andre Lemelin, Jing Li, Pamela Mcguinness, Xiang Niu, Matthew J. Schnaderbeck, Kevin (kuo-ming) Wu, Xiaojie (Jeff) Zhu
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Publication number: 20100324094Abstract: A method for synthesizing anti-leukemic epothilone analogues includes rigidifying a region between the macrolactone ring and the aromatic side-chain. The anti-leukemic compositions are non-naturally occurring epothilone analogue that are rigidified between the macrolactone ring and the aromatic side-chain.Type: ApplicationFiled: March 20, 2008Publication date: December 23, 2010Applicant: The University of ToledoInventors: Viranga Tillekeratne, Richard A. Hudson, Mamoun Alhamadsheh
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Publication number: 20100233279Abstract: Disclosed are novel analogues of the natural product radicicol A of formulae I, .Ia, pi, Ha, lib and HI, pharmaceutical compositions comprising the compounds. The compounds of the invention are kinase and phosphatase inhibitors and find utility in the treatment or prevention of kinase and phosphatase-mediated disorders. Also provided are uses and methods for the treatment or prevention of kinase- and phosphatase-mediated disorders and synthetic processes for the preparation of the compounds.Type: ApplicationFiled: June 5, 2008Publication date: September 16, 2010Inventors: Nicolas Winssinger, Sofia Barluenga
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Patent number: 7745646Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.Type: GrantFiled: July 6, 2007Date of Patent: June 29, 2010Assignee: Kalypsys, Inc.Inventors: Steven Govek, Andrew K. Shiau, Stewart A. Noble, David J. Thomas
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Publication number: 20100121079Abstract: Disclosed are: a novel dinoflagellate alga; and a macrolide compound which can be used as a novel anticancer agent. Specifically disclosed is a macrolide compound produced by a dinoflagellate Amphidinium sp. Strain HYA002 or HYA0024. The macrolide compound has excellent proliferation-inhibiting effect against a human tumor cell and therefore can be used as a novel anticancer agent.Type: ApplicationFiled: December 19, 2007Publication date: May 13, 2010Inventors: Masashi Tsuda, Keiko Oguchi, Rie Iwamoto, Yumiko Okamoto
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Publication number: 20090169540Abstract: The present invention relates to the use of at least one Epac (Exchange Protein directly Activated by cAMP) antagonist for the manufacture of a medicament intended for the prevention or the treatment of pathologies selected from the list comprising cardiac hypertrophy, cardiac arrhythmias, valvulopathies, diastolic dysfunction, chronic heart failure, ischemic heart failure, and myocarditis.Type: ApplicationFiled: March 2, 2006Publication date: July 2, 2009Applicant: INSERM (Institute National De La Sane Et De La Recherche Medicle)Inventors: Frank Lezoualc'h, Eric Morel, Monique Gastineau, Gregoire Vandecasteele
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Patent number: 7470792Abstract: The present invention provides a synthesis for the preparation of epothilone derivatives of formula 9 wherein R1 is methyl, and R2 is an unsubstituted or substituted aryl; an unsubstituted or substituted heteroaryl; or an unsubstituted or substituted heterocyclic radical fused to a benzene nucleus; and salts thereof, and intermediates for the synthesis of a compound of formula 9.Type: GrantFiled: September 12, 2003Date of Patent: December 30, 2008Assignee: Novartis AGInventors: Guido Koch, Olivier Loiseleur
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Patent number: 7381744Abstract: The present invention provides vacuolar-type (H+)-ATPase-inhibiting compounds, compositions thereof, and methods of using them to treat or prevent a condition treatable by the inhibition of a vacuolar-type (H+)-ATPase. The composition of the present invention comprises a compound of the present invention and a carrier. The method of the present invention includes administering a vacuolar-type (H+)-ATPase inhibiting-effective amount of a compound of the present invention.Type: GrantFiled: March 2, 2000Date of Patent: June 3, 2008Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Michael R. Boyd
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Patent number: 7317100Abstract: The present invention relates to C4-demethyl-epothilones or C4-bisnor-epothilones of Formula (I), their pharmaceutical use, pharmaceutical composition containing the same and methods for their preparation.Type: GrantFiled: December 22, 2003Date of Patent: January 8, 2008Assignee: Novartis AGInventors: Donatienne Denni-Dischert, Andreas Floersheimer, Ernst Kuesters, Lukas Oberer, Gottfried Sedelmeier
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Patent number: 7115651Abstract: The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) wherein R0–R4, Z, X, A—B, D—E, G—J, and K—L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.Type: GrantFiled: August 24, 2001Date of Patent: October 3, 2006Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Robert M. Garbaccio, Daniel K. Baeschlin, Shawn J. Stachel, David Solit, Neal Rosen
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Patent number: 7109235Abstract: Laulimalide and epothilone derivatives useful as microtubule stabilizing agents, and in the treatment of cancers are disclosed. Methods of making the compounds and using the compounds as therapeutic agents in treating cancers also are disclosed.Type: GrantFiled: March 5, 2003Date of Patent: September 19, 2006Assignee: The Board of Trustees of the University IllinoisInventor: Arun K. Ghosh
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Patent number: 7105268Abstract: A polymeric compound for photoresist of the invention includes at least one monomer unit represented by following Formula (I): wherein R1, R2, R3, R4 and R5 are the same or different and are each a hydrogen atom or a methyl group; m, p and q each denote an integer of from 0 to 2; and n denotes 0 or 1, where the hydroxyl group and carbonyloxy group extending from a principle chain in the formula are independently combined with either of two carbon atoms on the far-left portion of the rings. By using the polymeric compound for photoresist as a base of a photoresist, the resulting photoresist exhibits well-rounded adhesion to substrates and resistance to etching.Type: GrantFiled: December 11, 2001Date of Patent: September 12, 2006Assignee: Daicel Chemical Industries, Ltd.Inventors: Yoshinori Funaki, Kiyoharu Tsutsumi, Keizo Inoue, Tomoko Adachi
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Patent number: 7094725Abstract: The present invention provides compounds of the formula wherein R is optionally substituted lower alkyl, cycloalkyl or aryl; R? is alkyl or aryl; n is zero or an integer of 1 or 2; or an enantiomer thereof; or an enantiomeric mixture thereof. The compounds of formula (I) are bridged C2-symmetric biphenyldiphosphine analogs and, thus, may be employed as ligands to generate chiral transition metal catalysts which may be applied in a variety of asymmetric reactions. The compounds of the present invention are easily accessible in high diastereomeric and optical purity according to the methods disclosed herein.Type: GrantFiled: July 9, 2004Date of Patent: August 22, 2006Assignee: The Hong Kong Polytechnic UniversityInventors: Albert Sun-Chi Chan, Liqin Qiu
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Patent number: 7026352Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer.Type: GrantFiled: February 1, 2002Date of Patent: April 11, 2006Assignees: Mercian Corporation, Eisai Co., Ltd.Inventors: Yoshiharu Mizui, Takashi Sakai, Satoshi Yamamoto, Keisuke Komeda, Masanori Fujita, Akifumi Okuda, Kumiko Kishi, Jun Niijima, Mitsuo Nagai, Kiyoshi Okamoto, Masao Iwata, Yoshihiko Kotake, Toshimitsu Uenaka, Naoki Asai, Motoko Matsufuji, Tomohiro Sameshima, Naoto Kawamura, Kazuyuki Dobashi, Takashi Nakashima, Masashi Yoshida, Toshio Tsuchida, Susumu Takeda, Tomonari Yamada, Koji Norihisa, Takao Yamori
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Patent number: 6982280Abstract: The present invention relates to epothilon derivatives, processes for their production and their use in the manufacture of medicaments and plant protection agents.Type: GrantFiled: May 7, 1999Date of Patent: January 3, 2006Inventors: Gerhard Hoefle, Thomas Leibold
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Patent number: 6936723Abstract: The present invention provides compounds having improved stability over that of natural benzolactones, and a process for synthesizing these compounds. These compounds exhibit anti-cancer activity and inhibit V-ATPase activity.Type: GrantFiled: March 1, 2004Date of Patent: August 30, 2005Assignee: Board of Regents, The University of Texas SystemInventors: Jef De Brabander, Yusheng Wu
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Patent number: 6872747Abstract: A novel class of decalactones with the general formula (I) and their stereoisomers is disclosed. A method for the synthesis of the decalactones of general formula (I) and the use of the decalactones in pharmaceutical compositions is also described.Type: GrantFiled: May 9, 2002Date of Patent: March 29, 2005Assignee: Biotecmarin GmbHInventors: Gerhard Bringmann, Peter Prokosch, Ru Angelie Edrada, Markus Heubes, Sudarsono, Eckhard Gunter
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Patent number: 6828340Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.Type: GrantFiled: January 28, 2002Date of Patent: December 7, 2004Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dang Fang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin
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Patent number: 6815463Abstract: Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.Type: GrantFiled: February 10, 2003Date of Patent: November 9, 2004Assignee: Kosan Biosciences, Inc.Inventors: Gary Ashley, Brian Metcalf
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Patent number: 6765016Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: GrantFiled: June 5, 2003Date of Patent: July 20, 2004Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ly Tam Phan, Zhigang Chen, Tongzhu Liu, Yat Sun Or
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Patent number: 6710073Abstract: Peripherally administered analogs and derivatives of Brefeldin A are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal tissues.Type: GrantFiled: December 2, 1996Date of Patent: March 23, 2004Assignee: The Regents of the University of CaliforniaInventors: Katumi Sumikawa, Ken-Ichi Ito, James L. McGaugh
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Patent number: 6670389Abstract: Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.Type: GrantFiled: February 8, 2002Date of Patent: December 30, 2003Assignee: Kosan Biosciences, Inc.Inventors: Gary Ashley, Brian Metcalf
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Patent number: 6635662Abstract: Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 {wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR5R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl, and the like; R7 represents hydroxyl, substituted lower alkyl, and the like), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, and the like), and the like} and the like; X represents halogen or is combined together with R4 to represent a single bond; and R4 is combined together with X to represent a single bond, or represents hydrogen, alkanoyl, and the like.Type: GrantFiled: February 26, 2001Date of Patent: October 21, 2003Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
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Patent number: 6617348Abstract: The present invention provides compounds having improved stability over that of natural benzolactones, and a process for synthesizing these compounds. These compounds exhibit anti-cancer activity and inhibit V-ATPase activity.Type: GrantFiled: August 3, 2001Date of Patent: September 9, 2003Assignee: UT Southwestern Medical CenterInventors: Jef Karel De Brabander, Yusheng Wu
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Publication number: 20030069277Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.Type: ApplicationFiled: April 30, 2002Publication date: April 10, 2003Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dongfang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin, Scott Kuduk, Christina Harris, Xiu-Guo Zhang, Joseph R. Bertino
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Patent number: 6528489Abstract: The present invention provides a treatment for mammalian diseases characterized by aberrant cell proliferation. The treatment consists of administering therapeutically active dosages of antibiotic inhibitors such as efrapeptin oligopeptides or mycotoxin derivatives including those comprising a-zearalenol structural motifs resulting in inhibition of cell mitosis.Type: GrantFiled: September 21, 2000Date of Patent: March 4, 2003Assignee: Ergon Pharmaceuticals LLCInventor: Adonia E. Papathanassiu
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Patent number: 6486330Abstract: A 4-oxatricyclo[4.3.1.13,8]undecan-5-one derivative is shown by the following formula (1): wherein R is a hydrogen atom or a (meth)acryloyl group, and carbon atoms constituting a ring may have a substituent in addition to the substituents indicated in the formula. This compound is a novel 4-oxatricyclo[4.3.1.13,8]undecan-5-one derivative having a hydroxyl group or a (meth)acryloyloxy group at the 1-position.Type: GrantFiled: August 28, 2000Date of Patent: November 26, 2002Assignee: Daicel Chemical Industries, Ltd.Inventor: Tatsuya Nakano
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Publication number: 20020045609Abstract: The present invention relates to 16-membered macrocyclic compounds. These compounds are cytotoxic agents and can be used to treat cancer and non-cancer disorders characterized by cellular hyperproliferation.Type: ApplicationFiled: May 15, 2001Publication date: April 18, 2002Inventors: Gary Ashley, Maria Fardis, Daniel Santi
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Patent number: 6369099Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.Type: GrantFiled: April 20, 2000Date of Patent: April 9, 2002Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski
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Patent number: 6362218Abstract: Cytotoxic Michael addition derivatives of brefeldin A are described. Oxidation of thiol addition products of brefeldin A provides the corresponding sulfoxides and sulfones. The sulfoxides exhibited more cytotoxic activity than the corresponding sulfides and sulfones in a variety of human cancer cell lines. Pharmaceutical formulations of the disclosed cytotoxic derivatives are also described.Type: GrantFiled: June 16, 2000Date of Patent: March 26, 2002Assignee: Purdue Research FoundationInventors: Mark S. Cushman, Ankush B. Argade, Rudiger D. Haugwitz, Rajesh Devraj
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Patent number: 6353019Abstract: The present invention provides compound of the formula: wherein R1 and R2 are the same or different and are independently H, C1-C6 straight-chain or branched saturated or unsaturated alkyl, aryl, R6CH2—, R6CO—, or R6SO2—, wherein R6 is H, C1-C6 straight-chain or branched saturated or unsaturated alkyl, or aryl; R3 is H, C1→C6 straight-chain or branched-chain saturated alkyl, aryl, an oxime, or an oxime methyl ether; at least one aromatic ring position is optionally substituted with a substituent selected from the group consisting of halo, nitro, amino, hydroxyl, thio, acyl, C1-C6 alkyl, and cyano; and Z is a contiguous linker comprising a chain of 7-10 atoms (including heteroatoms) which atoms, together with the five atoms beginning with the carbon of the aromatic ring in meta-relationship with OR1 and ending with the carbon directly attached to the alkyl oxygen of the lactone, which carbons are covalently bonded to either end of linker Z, integrally form a 12-15 membeType: GrantFiled: April 10, 2000Date of Patent: March 5, 2002Assignee: United States of America as represented by the Department of Health and Human ServicesInventors: Michael R. Boyd, Tawnya C. McKee, John H. Cardellina, II, John A. Beutler, Karen Erickson, Deborah Galinis, Lewis Pannell
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Publication number: 20010027208Abstract: Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: 1Type: ApplicationFiled: February 26, 2001Publication date: October 4, 2001Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
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Patent number: 6242469Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.Type: GrantFiled: December 3, 1997Date of Patent: June 5, 2001Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dang Fang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin
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Patent number: 6239168Abstract: Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 {wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl; R7 represents hydroxyl, substituted lower alkyl), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, X represents halogen.Type: GrantFiled: February 25, 2000Date of Patent: May 29, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
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Patent number: 6074838Abstract: The present invention provides a bacterial microorganism having the ability to degrade or detoxify zearalenone or derivatives or analogs of zearalenone. The present invention also provides a method for the isolation and utilization of a zearalenone-degradation gene encoding a gene product having the ability to degrade or detoxify zearalenone or derivatives or analogs of zearalenone. In another embodiment, the present invention provides for the generation of transformants into which the zearalenone-degradation gene has been introduced, thereby providing the ability to degrade or detoxify zearalenone or derivatives or analogs of zearalenone to said transformants. The present invention further provides a method for detoxification of plants pre- or post-harvest using microbes having the ability to degrade or detoxify zearalenone or derivatives or analogs of zearalenone. The invention also provides a method for detoxification of plants pre- or post-harvest using the zearalenone-degradation gene.Type: GrantFiled: May 20, 1999Date of Patent: June 13, 2000Assignee: Pioneer Hi-Bred International, Inc.Inventors: Jon Duvick, Tracy A. Rood
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Patent number: 6025350Abstract: This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: July 29, 1998Date of Patent: February 15, 2000Assignee: Pfizer Inc.Inventors: Hiroko Masamune, Wei-Guo Su, Bingwei V. Yang
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Patent number: 5977165Abstract: The present invention relates to radicicol derivatives represented by the following formula (I) or pharmacologically acceptable salts thereof: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert-butyldimethylsilyl; (1) when X represents halogen, Y represents an oxygen atom or R.sup.4 --O--N (wherein R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl); and R.sup.3 represents hydrogen, alkanoyl, alkenoyl or the like; and (2) when X and R.sup.3 are combined with each other to represent a single bond; Y represents R.sup.4B --O--N (wherein R.sup.4B has the same meaning as R.sup.4). The radicicol derivatives of the present invention demonstrate tyrosine kinase inhibition activity and pharmacological activities such as antitumor, antimicrobial or immunosuppression effects.Type: GrantFiled: October 27, 1997Date of Patent: November 2, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tsutomu Agatsuma, Yutaka Saitoh, Yoshinori Yamashita, Tamio Mizukami, Shiro Akinaga, Katsushige Gomi, Kazuhito Akasaka, Isami Takahashi
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Patent number: RE41895Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.Type: GrantFiled: August 11, 2009Date of Patent: October 26, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson