Additional Chalcogen Attached Directly Or Indirectly To The Lactone Ring By Nonionic Bonding Patents (Class 549/271)
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Publication number: 20090312316Abstract: The present invention relates to derivatives of borrelidin that are useful in medicine, e.g. in the treatment of cancer or B-cell malignancies, or other diseases in which angiogenesis contributes to the pathology including ophthalmic disorders such as diabetic retinopathy as well as age related macular degeneration (AMD), corneal neovascularisation and retinopathy or prematurity. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies and other diseases in which angiogenesis is implicated in the pathogenic process.Type: ApplicationFiled: May 17, 2007Publication date: December 17, 2009Inventors: Barrie Wilkinson, Steven Moss, Ming Zhang
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Patent number: 7626043Abstract: The subject invention provides novel biologically active compounds that have utility for use in inhibiting cellular proliferation. Pharmaceutical compositions comprising these compounds are also provided. In a specific embodiment, the compounds and compositions of the subject invention can be used in the treatment of cancer.Type: GrantFiled: August 6, 2007Date of Patent: December 1, 2009Assignee: Florida Atlantic University Board of TrusteesInventors: Amy E. Wright, John K. Reed, Jill Roberts, Ross E. Longley
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Patent number: 7619100Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: GrantFiled: October 29, 2007Date of Patent: November 17, 2009Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.Inventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20090263552Abstract: A method of using organic compounds and providing slow release flavoring in or for food products wherein flavor precursors are added to flavor compositions and/or food products and release flavor compounds upon consumption of the food products, and novel flavor precursor compounds. The flavor precursors can be prepared from mono- and/or diglycerides and lactone flavor compounds.Type: ApplicationFiled: July 25, 2007Publication date: October 22, 2009Inventor: Willi Grab
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Patent number: 7576204Abstract: A compound represented by the following general formula (I): (I) wherein R7 and R21 are the same or different and each represents optionally substituted C2-22 alkoxy, etc.; a pharmaceutically acceptable salt thereof or hydrates of the same. The compound (1) inhibits angiogenesis and inhibits the production of VEGF particularly under hypoxic conditions, which makes it useful as a remedy for solid cancer.Type: GrantFiled: July 31, 2003Date of Patent: August 18, 2009Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.Inventors: Mitsuo Nagai, Masashi Yoshida, Toshio Tsuchida
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Patent number: 7569576Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.Type: GrantFiled: January 12, 2006Date of Patent: August 4, 2009Assignee: XenoPort, Inc.Inventors: Mark A Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
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Publication number: 20090192215Abstract: The present invention concerns groups of compounds derived from tunicates of the Synoicum species, as well as to pharmaceutical compositions comprising these compounds, and uses thereof. Extracts from tunicates show selective toxicity against several different cancer cell lines in the NCI 60 cell line panel. These compounds are useful in the effective treatment of cancers, particularly malignant melanomas, colon cancer, and renal cancer cell lines.Type: ApplicationFiled: September 18, 2006Publication date: July 30, 2009Applicants: University of South Florida, UAB Research FoundationInventors: Bill Baker, Thushara Diyabalanage, James B. McClintock, Charles D. Amsler
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Patent number: 7550503Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: GrantFiled: June 23, 2006Date of Patent: June 23, 2009Assignees: Eisai R& D Management Co., Ltd., Merican CorporationInventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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ANALOGS OF DICODERMOLIDE AND DICTYOSTATIN-1, INTERMEDIATES THEREFOR AND METHODS OF SYNTHESIS THEREOF
Publication number: 20090036691Abstract: A compound of the following structure: wherein R1 is H, an alkyl group, an aryl group, an alkenyl group, an alkynyl group, or a halogen atom; R2 is H, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; Ra, Rb and Rc are independently an alkyl group or an aryl group; Rd is an alkyl group, an aryl group, an alkoxylalkyl group, —RiSiRaRbRc or a benzyl group, wherein Ri is an alkylene group; Re is an alkyl group, an allyl group, a benzyl group, an aryl group, an alkoxy group, or —NRgRh, wherein Rg and Rh are independently H, an alkyl group or an aryl group; R3 is (CH2)n where n is and integer in the range of 0 to 5, —CH2CH(CH3)—, —CH?CH—, —CH?C(CH3)—, or —C?C—; R4 , wherein y1 and y2 are 1 and y3, y4 and y5 are independently 0 or 1, Rk1, Rk2, Rk3, Rk4 and Rk5 are independently H, CH3, or OR2a, and Rs1, Rs2, Rs3, and Rs4 are independently H or CH3, wherein R2a is H, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; and R5 isType: ApplicationFiled: September 23, 2008Publication date: February 5, 2009Inventors: DENNIS P. CURRAN, YOUSEUNG SHIN, NAKYEN CHOY, BILLY W. DAY, RAGHAVAN BALACHANDRAN, CHARITHA MADIRAJU, TIFFANY TURNER -
Publication number: 20080275059Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: ApplicationFiled: October 29, 2007Publication date: November 6, 2008Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20080255146Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.Type: ApplicationFiled: October 29, 2007Publication date: October 16, 2008Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20080188651Abstract: Dictyostatin and its analogs show great promise as new anticancer agents. The present invention provides dictyostatin analogs, synthetic intermediates for the synthesis of dictyostatin analogs, and synthetic methods for the synthesis of such analogs and intermediates.Type: ApplicationFiled: January 2, 2008Publication date: August 7, 2008Inventors: Dennis P. Curran, Youseung Shin, Jean-Hugues Fournier, John Mancuso, Billy W. Day, Arndt Bruckner, Yoshikazu Fukui
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Publication number: 20080146545Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.Type: ApplicationFiled: August 10, 2007Publication date: June 19, 2008Inventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
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Patent number: 7378508Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.Type: GrantFiled: July 31, 2007Date of Patent: May 27, 2008Assignee: Optimer Pharmaceuticals, Inc.Inventors: Yu-Hung Chiu, Tessie Mary Che, Alex Romero, Yoshi Ichikawa, Youe-Kong Shue
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Patent number: 7358275Abstract: Novel derivatives of prostaglandin compounds of the F-series (PGF), specifically macrocyclic internal 1,15-lactones of fluprostenol and related PGF analogs, such as cloprostenol or latanoprost. The novel analogs can be formulated into ophthalmic solutions and topically applied for the treatment of the increased intraocular pressure caused by glaucoma and the reduction of ocular hypertension.Type: GrantFiled: February 14, 2006Date of Patent: April 15, 2008Assignee: Cayman Chemical CompanyInventors: Kirk M. Maxey, Michelle L. Stanton
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Patent number: 7321046Abstract: Dictyostatin and its analogs show great promise as new anticancer agents. The present invention provides dictyostatin analogs, synthetic intermediates for the synthesis of dictyostatin analogs, and synthetic methods for the synthesis of such analogs and intermediates.Type: GrantFiled: May 27, 2005Date of Patent: January 22, 2008Assignee: University of PittsburghInventors: Dennis P. Curran, Youseung Shin, Jean-Hugues Fournier, John Mancuso, Billy W. Day, Arndt Bruckner, Yoshikazu Fukui
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Patent number: 7238816Abstract: The invention comprises a novel process for the preparation of an epothilone derivative of formula I: wherein R1 and R2 independently from each other represent hydrogen or protecting groups and R3 is methyl or trifluoromethyl, which are useful precursors in the synthesis of the desoxyepothilone derivatives of the formula IV: wherein R3 is methyl or trifluoromethyl. The desoxepothilones of formula IV inhibit the growth of tumor cells and are therefore promising candidates for novel anticancer agents.Type: GrantFiled: April 7, 2006Date of Patent: July 3, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Puentener, Michelangelo Scalone
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Patent number: 7214705Abstract: The invention provides a compound of formula (I) and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 30, 2003Date of Patent: May 8, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Jacobus Alphonsus Josephus Van Dun, Walter Boudewijn Leopold Wouters, Michel Marie François Janicot, Ursula Maria Mocek, Jodi Ann Laakso
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Patent number: 7151116Abstract: The invention provides novel apoptosis-inducing compounds that include isolated, purified isoapoptolidin, and selectively functionalized isoapoptolidin derivatives and stereoisomers thereof; selectively functionalized apoptolidin derivatives and stereoisomers thereof; and deglycosylated isoapoptolidin and selectively functionalized derivatives and stereoisomers thereof. The isoapoptolidin, apoptolidin, and deglycosylated isoapoptolidin derivatives may be functionalized by substituting any or all of the methoxyl or hydroxyl groups of the parent molecule. Pharmaceutical compositions and methods for using the compounds are also provided.Type: GrantFiled: January 13, 2004Date of Patent: December 19, 2006Assignee: Board of Trustees of The Leland Stanford Junior UniversityInventors: Paul A. Wender, Orion D. Jankowski, Elie A. Tabet
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Patent number: 7105684Abstract: An object of the present invention is to provide a novel monomer compound having a lactone structure which gives polymers having more excellent feature as resist material, etc. The present invention relates to a compound represented by the following formula [1]: wherein R1 and R2 are an alkyl group; R3 and R4 are each independently hydrogen atom or an alkyl group; R5 is hydrogen atom, acryloyl group or methacryloyl group; and X is a methylene group which may have an alkyl group or an ethylene group which may have an alkyl group. The present invention provides a compound having a lactone structure which gives a polymer having more excellent feature particularly as a resist material and also provides a hydroxy lactone being useful as a material, etc. therefor.Type: GrantFiled: July 26, 2004Date of Patent: September 12, 2006Assignee: Takasago International CorporationInventors: Tomoya Sawaki, Hiroyuki Kenmochi, Yoji Hori
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Patent number: 7026351Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.Type: GrantFiled: March 20, 2003Date of Patent: April 11, 2006Assignee: Xenoport, Inc.Inventors: Mark A Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
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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: 6989450Abstract: The present invention relates to methods for use in producing epothilones and analogs and derivatives thereof. A general method according to the present invention broadly comprises performing an aldol condensation of a first compound with a second compound thereby to form a third compound selected from the formulas: and stereoisomers thereof, and performing a macrolactonization of the third compound. The present invention also provides chemical compounds, and methods for producing such chemical compounds, that are useful in producing epothilones and analogs and derivatives thereof.Type: GrantFiled: October 15, 2001Date of Patent: January 24, 2006Assignee: The University of MississippiInventor: Mitchell A. Avery
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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: 6965034Abstract: 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: GrantFiled: December 23, 2002Date of Patent: November 15, 2005Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: 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: 6946482Abstract: Motilide compounds having the formula (I), wherein R1, R2, R3, and R4 are as defined herein, and methods for their preparation and use in the treatment of diseases or conditions characterized by impaired gastric motility.Type: GrantFiled: August 26, 2003Date of Patent: September 20, 2005Assignee: Kosan Biosciences, Inc.Inventors: Daniel V. Santi, Brian Metcalf, Christopher Carreras, Yaoquan Liu, Robert McDaniel, Eduardo J. Rodriguez
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Patent number: 6936402Abstract: Disclosed herein is a novel norbornene, acrylate or methacrylate monomer as a photoresist monomer containing an oxepan-2-one group. Further disclosed are photoresist compositions comprising a polymer prepared from the monomer, methods for preparing the photoresist compositions, and methods for forming photoresist patterns using the photoresist compositions.Type: GrantFiled: February 24, 2004Date of Patent: August 30, 2005Assignee: Korea Advanced Institute Science & TechnologyInventors: Jin-Baek Kim, Tae-Hwan Oh, Jae-Hak Choi, Jae-Jun Lee
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Patent number: 6919464Abstract: Macrolide compounds produced by synthetic modification of factors produced by NRRL 30141 have insecticidal and acaricidal activity and are useful intermediates for preparing additional insecticidal and acaricidal compoundsType: GrantFiled: March 21, 2002Date of Patent: July 19, 2005Assignee: Dow AgroSciences LLCInventors: Gary D. Crouse, Donald R. Hahn, Paul R. Graupner, Jeffrey R. Gilbert, Paul Lewer, Jesse L. Balcer
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Patent number: 6855831Abstract: The present invention relates to a process for the preparation of compounds of formula I: wherein the substituents are as defined in claim 1, by conversion of a compound of formula II: reaction of that compound with a compound of formula IV: X—C(O)—Q??(IV), wherein X is a leaving group, to form a compound of formula V: and treatment of that compound in the presence of a base with catalytic amounts of cyanide ions.Type: GrantFiled: April 8, 2003Date of Patent: February 15, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Hermann Schneider, Christoph Lüthy, Andrew Edmunds
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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: 6710189Abstract: A polyketide, or an antibiotic which is obtainable from the polyketide by a method comprising treating the polyketide with a culture medium conditioned by Saccharopolyspora erythraea, selected from the group consisting of:Type: GrantFiled: June 28, 2002Date of Patent: March 23, 2004Assignees: Stanford University, Brown UniversityInventors: Chaitan Khosla, Rembert Pieper, Guanglin Luo, David E. Cane, Camilla Kao, Gary Ashley
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Patent number: 6706740Abstract: Heterocyclic aromatic amides (HAA) according to Formula I: wherein X1-X4, M, Z, and A are herein defined. The invention also encompasses hydrates, salts and complexes thereof. These compounds are useful as antifungal agents.Type: GrantFiled: December 13, 2001Date of Patent: March 16, 2004Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Matthew J. Henry, Jenifer L. Adamski Butz, Robert P. Gajewski
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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: 6667338Abstract: Compounds of formula (I) and formula (II) or therapeutically acceptable salts or prodrugs thereof are useful as antibacterial agents. Methods to make the compounds, compositions containing the compounds, and methods of treatment using the compounds are also disclosed.Type: GrantFiled: January 16, 2002Date of Patent: December 23, 2003Assignee: Abbott LaboratoriesInventors: Zhenkun Ma, Ly Tam Phan, Suoming Zhang, Stevan W. Djuric
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Patent number: 6660448Abstract: The invention provides a polymer comprising recurring units containing bridged aliphatic rings in the backbone and having a hydroxyl, acyloxy or alkoxylcarbonyloxy group as well as a lactone structure bonded through a spacer, the polymer having a weight average molecular weight of 1,000-500,000. A resist composition comprising the polymer as a base resin is sensitive to high-energy radiation, has excellent sensitivity, resolution, and etching resistance, and lends itself to micropatterning with electron beams or deep-UV.Type: GrantFiled: November 8, 2001Date of Patent: December 9, 2003Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Seiichiro Tachibana, Mutsuo Nakashima, Tsunehiro Nishi, Takeshi Kinsho, Koji Hasegawa, Takeru Watanabe, Jun Hatakeyama
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Patent number: 6656961Abstract: 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: March 14, 2001Date of Patent: December 2, 2003Assignee: 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: 6610736Abstract: The invention relates to novel epothilone derivatives of general formula (I), wherein R8 means a halogen atom, especially a fluorine or chlorine atom, and the remaining substituents have the meanings given in the description. The novel compounds are suitable for producing medicaments.Type: GrantFiled: December 7, 2001Date of Patent: August 26, 2003Assignee: Schering AGInventors: Ulrich Klar, Werner Skuballa, Bernd Buchmann, Wolfgang Schwede, Michael Schirner
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Patent number: 6559322Abstract: The present invention provides a new biocatalyst whole cell system for converting cyclic ketones such as cyclopentanone/cyclohexanone to the corresponding lactones such as valerolactone/caprolactone. Another novel aspect of the present invention is that biocatalyst fungus Fusarium oxysporum f.sp. ciceri NCIM 1282 species has been found to be an efficient biocatalyst system for any biotransformation for the first time.Type: GrantFiled: December 21, 2001Date of Patent: May 6, 2003Assignee: Council of Scientific and Industrial ResearchInventors: Deendayal Mandal, Absar Ahmad, Mohammed Islam Khan, Rajiv Kumar
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Patent number: 6500961Abstract: Lactone compounds of formula (1) are useful as monomers to form base resins for use in chemically amplified resist compositions adapted for micropatterning lithography. R1 is H or C1-6 alkyl, R2 is H or an acyl or alkoxycarbonyl group of 1-15 carbon atoms which may be substituted with halogen atoms, Z is a divalent C1-15 organic group which forms a lactone ring with the carbonyloxy group, k is 0 or 1, and m is an integer from 0 to 5.Type: GrantFiled: May 31, 2001Date of Patent: December 31, 2002Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Takeshi Kinsho, Koji Hasegawa, Takeru Watanabe, Tsunehiro Nishi, Mutsuo Nakashima, Seiichiro Tachibana, Jun Hatakeyama
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Patent number: 6437151Abstract: Erythromycins, particularly ones with novel C-13 substituents R1 (e.g. C3-C6 cycloalkyl or cycloalkenyl groups) are prepared by fermenting suitable organisms in the presence of R1CO2H. A preferred organism is Saccharopolyspora erythraea preferably containing an integrated plasmid capable of directing synthesis of desired compounds.Type: GrantFiled: June 29, 2001Date of Patent: August 20, 2002Assignees: Biotica Technology Limited, Pfizer Inc.Inventors: Peter Francis Leadlay, James Staunton, Jesus Cortes, Michael Stephen Pacey
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Patent number: 6399789Abstract: A multiple-plasmid system for heterologous expression of polyketides facilitates combinatorial biosynthesis. The method can be extended to any modular polyketide synthase (PKS) or non-ribosomal peptide synthase (NRPS) and has the potential to produce thousands of novel natural products, including ones derived from further modification of the PKS or NRPS products by tailoring enzymes.Type: GrantFiled: April 12, 2000Date of Patent: June 4, 2002Assignee: Kosan Biosciences, Inc.Inventors: Daniel V. Santi, Qun Xue, Gary Ashley
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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: 6355660Abstract: A compound having the following formula: wherein R3 and M are defined herein, and processes therewith.Type: GrantFiled: August 4, 2000Date of Patent: March 12, 2002Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, III, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Matthew J. Henry, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison, Jenifer L. Adamski Butz
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Patent number: 6320045Abstract: The invention as claimed is directed to a process for making an epothilone having the following structures from ones having an oxiranyl moiety, by reacting a compound having the latter structure with a metal or metal-assisted reagent. Said metal or metal-assisted reagent is selected from the group consisting of a) reactive metallocenes; b) [N2C(CO2Me)2, cat Rh2,(OAC)4]; c) [N2C(CO2Me)2, cat[(n-C7H15CO2)2 Rh]2]; d) [Zn—Cu, EtOH]; e) [Mg(Hg), MgBr]; f) Cr; g) [FeCl3, n-BuLi]; h) [TiCl3, LiAlH4]; i) [TiCl4, Zn]; j) [WCl6, LiAlH4,]; k) [NbCl5, NaAlH4]; l) [VCl3,Zn] and m) [WCl6, n-BuLi].Type: GrantFiled: May 21, 1999Date of Patent: November 20, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Soong-Hoon Kim, James A. Johnson
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Publication number: 20010031880Abstract: The present invention relates to a stereospecific process to produce aziridinyl epothilones from oxiranyl epothilones and the intermediates derived therein.Type: ApplicationFiled: March 17, 2000Publication date: October 18, 2001Inventors: Robert M. Borzilleri, Soong-Hoon Kim, Alicia Regueiro-Ren, Gregory D. Vite
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Patent number: 6291684Abstract: The present invention relates to a stereospecific process to produce aziridinyl epothilones from oxiranyl epothilones and the intermediates derived therein.Type: GrantFiled: March 17, 2000Date of Patent: September 18, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Soong-Hoon Kim, Alicia Regueiro-Ren, Gregory D. Vite
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Patent number: 6270768Abstract: This invention relates to methods of preparing compounds of Formula 1: and to pharmaceutically acceptable salts and solvates thereof, and to methods for preparing same. The compounds of Formula 1 are antibacterial agents that may be used to treat various bacterial and protozoal infections, and may also be used to treat cancer. The invention also relates to pharmaceutical compositions comprising the compounds of Formula 1, and to methods of treating sbacterial and protozoal infections by administering compounds of Formula 1.Type: GrantFiled: January 26, 2000Date of Patent: August 7, 2001Assignee: Pfizer IncInventors: Thomas N. O'Connell, Brook K. Morse, Hamish Alastair Irvine McArthur, John Philip Dirlam
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Patent number: RE39991Abstract: A compound having the following formula: wherein R3 and M are defined herein, and processes therewith.Type: GrantFiled: August 22, 2003Date of Patent: January 1, 2008Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, III, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamad M. Niyaz, Irene M. Morrison, Matthew J. Henry, Jenifer L. Adamski Butz, Robert P. Gajewski