Ring Oxygen In The Additional Hetero Ring Patents (Class 546/281.7)
  • Patent number: 6967205
    Abstract: There are provided novel compounds which have both antibacterial and antiparasitic properties, thereby reducing the need for using several compounds in combined antibacterial and antiparasitic treatment of livestock. The present novel compounds are especially well suited for treatment of coccidiosis, and they are represented by general formula (I) wherein R1-R6, X and A are as defined in the specification.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: November 22, 2005
    Assignee: New Pharma Research Sweden AB
    Inventor: Shoaá Abdul-Rahman
  • Patent number: 6927225
    Abstract: The present invention relates to compounds of Formula I: wherein: represents a 6-membered heterocyclic aromatic ring in which X1 is N, and X2, X3 and X4 are CR?; wherein R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORz in which Rz is H or C1-C3 alkyl; and c) A represents (i) C2-C14 alkenyl, or C2-C14 alkynyl, all of which may be branched or unbranched, unsubstituted or substituted with halogen, hydroxy, nitro, aroyl, aryloxy, C1-C8 acyloxy, C1-C6 alkylthio, arylthio, aryl, heteroaryl, heteroarylthio, heteroaryloxy, C1-C6 acyl, C1-C6 haloalkyl, C1-C6 alkoxy or C1-C6 haloalkoxy, and (ii) C3-C14 cycloalkyl, containing 0 heteroatoms and 0-2 unsaturations, substituted with aryloxy, heteroaryloxy, C1-C6 alkylthio, a
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: August 9, 2005
    Assignee: Dow AgroSciences LLC
    Inventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, III, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison
  • Patent number: 6919359
    Abstract: The invention provides compounds of Formula I: Azabicyclo-N(R1)—C(?X)—W??Formula I These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.
    Type: Grant
    Filed: November 6, 2002
    Date of Patent: July 19, 2005
    Assignee: Pfizer Inc
    Inventors: David W. Piotrowski, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, Alice L. Bodnar, Vincent E. Groppi, Jr., Daniel Patrick Walker, Brad A. Acker
  • Patent number: 6916932
    Abstract: A process comprising reacting compound GF-I with a reducing agent to form compound GF-II wherein Y is selected from the group consisting of H, benzyl, substituted benzyl, CH2OC1-8 alkyl, CH2OC3-8 cycloalkyl, allyl, tetrahydropyranyl, tetra-hydrofuranyl, substituted tetrahydropyranyl, substituted tetra-hydrofuranyl, Si(C1-4 alkyl)3, and Si(Ph)x(C1-4 alkyl)3-x where x is equal to 1, 2 or 3; and wherein said process is conducted: (a) in the presence of a reducing agent; (b) in the presence of an aprotic solvent; and (c) under reaction conditions; is provided.
    Type: Grant
    Filed: July 31, 2002
    Date of Patent: July 12, 2005
    Assignee: Dow AgroSciences LLC
    Inventors: Kevin Gerald Meyer, Carl Vincent DeAmicis, Normohamed Mohamed Niyaz, Richard Brewer Rogers, Gina Marie Fitzpatrick
  • Patent number: 6906088
    Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: July 11, 2003
    Date of Patent: June 14, 2005
    Assignee: FSU Research Foundation, Inc.
    Inventors: Robert A. Holton, Weishuo Fang
  • Patent number: 6903219
    Abstract: A process to produce alkyl ethers from UK-2A derivatives is provided. Additionally, alkyl ether derivatives of UK-2A are provided.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: June 7, 2005
    Assignee: Dow AgroSciences LLC
    Inventors: Noormohamed Mohamed Niyaz, Carl Vincent DeAmicis, Richard Brewer Rogers, Kevin Gerald Meyer, William Hunter Dent, III, Peter Biagio Anzeveno
  • Patent number: 6890928
    Abstract: This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
    Type: Grant
    Filed: September 5, 2003
    Date of Patent: May 10, 2005
    Assignee: Pharmacia Corporation
    Inventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffrey N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
  • Patent number: 6878727
    Abstract: Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: April 12, 2005
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Allen J. Borchardt, Michael Paul Goble
  • Patent number: 6872747
    Abstract: 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: Grant
    Filed: May 9, 2002
    Date of Patent: March 29, 2005
    Assignee: Biotecmarin GmbH
    Inventors: Gerhard Bringmann, Peter Prokosch, Ru Angelie Edrada, Markus Heubes, Sudarsono, Eckhard Gunter
  • Patent number: 6872837
    Abstract: Taxanes having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: March 29, 2005
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6861446
    Abstract: Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: November 24, 2003
    Date of Patent: March 1, 2005
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6861390
    Abstract: Derivatives of UK-2A are provided.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: March 1, 2005
    Assignee: Dow AgroSciences LLC
    Inventors: Kevin Gerald Meyer, Richard Brewer Rogers, Noormohamed Mohamed Niyaz, Jenifer Lynn Adamski Butz, Bassam Salim Nader, Chenglin Yao
  • Publication number: 20040260098
    Abstract: 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: Application
    Filed: March 28, 2003
    Publication date: December 23, 2004
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin
  • Publication number: 20040192944
    Abstract: Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C9 substituent other than keto in which the C9 keto substituent of taxol, a taxol analog, baccatin III or 10-desacetyl baccatin III is selectively reduced to the corresponding hydroxy group.
    Type: Application
    Filed: January 27, 2004
    Publication date: September 30, 2004
    Applicant: Florida State University
    Inventors: Robert A. Holton, Carmen Somoza, Yukio Suzuki, Mitsuru Shindo
  • Publication number: 20040192924
    Abstract: Derivatives of UK-2A are provided.
    Type: Application
    Filed: April 23, 2004
    Publication date: September 30, 2004
    Inventors: Kevin Gerald Meyer, Richard Brewer Rogers, Noormohamed Mohamed Niyaz, Jenifer Lynn Adamski Butz, Bassam Salim Nader, Chenglin Yao
  • Publication number: 20040186296
    Abstract: A process to produce alkyl ethers from UK-2A derivatives is provided. Additionally, alkyl ether derivatives of UK-2A are provided.
    Type: Application
    Filed: April 5, 2004
    Publication date: September 23, 2004
    Inventors: Noormohamed Mohamed Niyaz, Carl Vincent DeAmicis, Richard Brewer Rogers, Kevin Gerald Meyer, William Hunter Dent, Peter Biagio Anzeveno
  • Publication number: 20040171838
    Abstract: A process comprising reacting compound GF-I with a reducing agent to form compound GF-II wherein Y is selected from the group consisting of H, benzyl, substituted benzyl, CH2OC1-8 alkyl, CH2OC3-8 cycloalkyl, allyl, tetrahydropyranyl, tetra-hydrofuranyl, substituted tetrahydropyranyl, substituted tetra-hydrofuranyl, Si(C1-4 alkyl)3, and Si(Ph)x(C1-4 alkyl)3-x where x is equal to 1, 2 or 3; and wherein said process is conducted: (a) in the presence of a reducing agent; (b) in the presence of an aprotic solvent; and (c) under reaction conditions; is provided. Additionaly, novel compounds produced therefrom are provided.
    Type: Application
    Filed: January 15, 2004
    Publication date: September 2, 2004
    Inventors: Kevin Gerald Meyer, Carl Vincent DeAmicis, Normohammed Mohamed Niyaz, Richard Brewer Rogers
  • Patent number: 6784137
    Abstract: 4-Aminopicolinic acids having aryl or heteroaryl substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: August 31, 2004
    Assignee: Dow AgroSciences LLC
    Inventors: Terry William Balko, Ann Marie Buysse, Jeffrey Brian Epp, Stephen Craig Fields, Christian Thomas Lowe, Renee Joan Keese, John Sanders Richburg, III, James Melvin Ruiz, Monte Ray Weimer, Renard Antonio Green, Roger Eugene Gast, Kristy Bryan, Nicholas Martin Irvine, William Chi-Leung Lo, William Kirkland Brewster, Jeffery Dale Webster
  • Patent number: 6780879
    Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: August 24, 2004
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Publication number: 20040158073
    Abstract: The present invention relates to an efficient process for preparing derivatives of 1-(pyridinyl)-1,1-dialkoxy-2-aminoethane of the formula (I), with which compounds of the formula (I) can be prepared in high purity and yield and in the form of the free base without isolating the acetylpyridine oxime of the formula (XI) which is a critical product from a safety point of view as a solid.
    Type: Application
    Filed: January 26, 2004
    Publication date: August 12, 2004
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Hans-Wolfram Flemming, Gerhard Korb, Juergen Mueller-Lehar, Walter Weber
  • Publication number: 20040152708
    Abstract: The present invention provides new trans-9,10-dehydroepothilone C and trans-9,10-dehydroepothilone D based derivative compounds, compositions and methods of inhibiting cellular hyperproliferation and/or stabilizing microtubules in vitro and of treatment of hyperproliferative diseases in vivo. Also disclosed are methods of making the compounds.
    Type: Application
    Filed: November 7, 2003
    Publication date: August 5, 2004
    Inventors: Yong Li, Kurt Sundermann, Li Tang, David Myles
  • Publication number: 20040147756
    Abstract: An optically active fluorine-containing compound represented by the following formula (1): 1
    Type: Application
    Filed: November 25, 2003
    Publication date: July 29, 2004
    Inventors: Takuya Miyata, Toshio Naka, Takumi Kagawa
  • Patent number: 6750245
    Abstract: Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10, and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 6, 2002
    Date of Patent: June 15, 2004
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6727239
    Abstract: A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.
    Type: Grant
    Filed: April 2, 2003
    Date of Patent: April 27, 2004
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre-Etienne Chabrier de Lassauniere, Serge Auvin, Jerry Harnett, Dominique Pons, Gérard Ulibarri, Dennis Bigg
  • Publication number: 20040072870
    Abstract: Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell lines. Among the several bioactive analogs, the epothilone B analog with a thiomethyl thiazole ring stands out as the most potent.
    Type: Application
    Filed: August 4, 2003
    Publication date: April 15, 2004
    Applicant: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Andreas Ritzen, Kenji Namoto
  • Patent number: 6720329
    Abstract: The present application describes novel spiro-cyclic &bgr;-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), and/or aggrecanase inhibitors.
    Type: Grant
    Filed: March 12, 2002
    Date of Patent: April 13, 2004
    Assignee: Bristol-Myers Squibb Pharma
    Inventors: Gregory R. Ott, Xiao Tao Chen, Jingwu Duan, Matthew E. Voss
  • Patent number: 6716987
    Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: April 6, 2004
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
  • Patent number: 6710189
    Abstract: 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: Grant
    Filed: June 28, 2002
    Date of Patent: March 23, 2004
    Assignees: Stanford University, Brown University
    Inventors: Chaitan Khosla, Rembert Pieper, Guanglin Luo, David E. Cane, Camilla Kao, Gary Ashley
  • Publication number: 20040053990
    Abstract: Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: 1
    Type: Application
    Filed: July 30, 2003
    Publication date: March 18, 2004
    Applicant: KYOWA HAKKO KOGYO CO., LTD
    Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
  • Publication number: 20040039026
    Abstract: The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV 1
    Type: Application
    Filed: August 23, 2002
    Publication date: February 26, 2004
    Applicant: The Scripps Research Institute
    Inventors: Kyriacos C. Nicoloou, Kenji Namoto, Andreas Ritzen, Mitsuru Shoji, Trond Ulven, Karl-Heinz Altmann
  • Publication number: 20040034230
    Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Application
    Filed: July 11, 2003
    Publication date: February 19, 2004
    Applicant: FSU Research Foundation, Inc.
    Inventors: Robert A. Holton, Weishuo Fang
  • Publication number: 20040029922
    Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-ketoepoxide group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or to stimulate hematopoietic cells ex vivo.
    Type: Application
    Filed: May 21, 2003
    Publication date: February 12, 2004
    Applicant: Beacon Laboratories, Inc.
    Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
  • Patent number: 6689794
    Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: February 10, 2004
    Assignee: Pharmacia Corporation
    Inventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
  • Patent number: 6686503
    Abstract: The invention relates to methods of synthesizing libraries of diverse and complex highly substituted 2,4-dioxopiperidine compounds of the general formula: wherein R1, R2 and R3 are as herein described, novel intermediates useful for synthesizing such 2,4-dioxopiperidine compounds and methods for identifying and isolating the compounds.
    Type: Grant
    Filed: June 13, 2001
    Date of Patent: February 3, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Wenying Chai, William V. Murray
  • Publication number: 20040014979
    Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Application
    Filed: June 25, 2003
    Publication date: January 22, 2004
    Applicant: Florida State University
    Inventor: Robert A. Holton
  • Publication number: 20040014978
    Abstract: 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: Application
    Filed: February 12, 2003
    Publication date: January 22, 2004
    Applicant: Schering AG
    Inventors: Ulrich Klar, Werner Skuballa, Bernd Buchmann, Wolfgang Schwede, Michael Schirner
  • Patent number: 6677330
    Abstract: The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof or hydrates thereof (provided that 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, a pharmaceutically acceptable salt thereof and hydrates thereof are excluded). wherein R1 and R2 represent substituents.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: January 13, 2004
    Assignee: Eisai Co., Ltd.
    Inventors: Yoichi Iimura, Takashi Kosasa, Yoshiharu Yamanishi, Hachiro Sugimoto, Yoshio Takeuchi, Tetsuo Shibata, Emiko Suzuki
  • Patent number: 6664275
    Abstract: Taxanes having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: December 16, 2003
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6660866
    Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: December 9, 2003
    Assignee: PSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Publication number: 20030216571
    Abstract: The present invention is to provide novel tricyclic compounds having leukotriene antagonistic action and represented by the formula: 1
    Type: Application
    Filed: July 31, 2002
    Publication date: November 20, 2003
    Inventors: Yoshiaki Kuroki, Hitoshi Ueno, Tetsushi Katsube, Tetsuo Kawaguchi, Eiji Okanari, Takashi Ikuta
  • Publication number: 20030216354
    Abstract: 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: Application
    Filed: May 9, 2002
    Publication date: November 20, 2003
    Inventors: Gerhard Bringmann, Peter Proksch, Ru Angelie Edrada, Markus Heubes, Sudarsono, Eckhard Gunther
  • Patent number: 6649632
    Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: November 18, 2003
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6646129
    Abstract: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C5-C14 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carboxy, C1-C4 alkoxycarbonyl, di(C1-C4 alkoxy)-phosphinoyloxy, amino, C1-C4 alkoxycarbonylamino or tetrahydropyranyloxy; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.
    Type: Grant
    Filed: February 4, 2002
    Date of Patent: November 11, 2003
    Assignee: Leo Pharmaceutical Products Ltd. A/S
    Inventors: Charlotte Schou Hunneche, Erik Rytter Ottosen
  • Publication number: 20030208080
    Abstract: 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: Application
    Filed: December 23, 2002
    Publication date: November 6, 2003
    Inventors: 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
  • Publication number: 20030203938
    Abstract: The invention relates to epothilone analog represented by the formula I 1
    Type: Application
    Filed: March 11, 2003
    Publication date: October 30, 2003
    Applicant: The Scripps Research Institute
    Inventors: Kyriacos Costa Nicolaou, Nigel Paul King, Maurice Raymond Verschoyle Finlay, Yun He, Frank Roschangar, Dionisios Vourloumis, Hans Vallberg, Antony Bigot
  • Patent number: 6638967
    Abstract: Compounds of Formula I Wherein Z2 is an Oxygen or a Sulfur, Z1 is —CH═CH— and Y is a bond, W1 and W2 are hydrogens and X1 and X2 are various heterocyclic rings are disclosed.
    Type: Grant
    Filed: August 6, 2001
    Date of Patent: October 28, 2003
    Assignee: Ortho-McNeil Phamraceutical, Inc.
    Inventors: Michael Bogenstaetter, Wenying Chai, Annette K. Kwok
  • Patent number: 6635662
    Abstract: 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: Grant
    Filed: February 26, 2001
    Date of Patent: October 21, 2003
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
  • Publication number: 20030195181
    Abstract: Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.
    Type: Application
    Filed: February 10, 2003
    Publication date: October 16, 2003
    Inventors: Gary Ashley, Brian Metcalf
  • Publication number: 20030171596
    Abstract: 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: Application
    Filed: January 28, 2002
    Publication date: September 11, 2003
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dang Fang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin
  • Publication number: 20030144523
    Abstract: This invention relates to the new epothilone derivatives of general formula I, 1
    Type: Application
    Filed: May 3, 2000
    Publication date: July 31, 2003
    Inventors: ULRICH KLAR, WOLFGANG SCHWEDE, WERNER SKUBALLA, BERND BUCHMANN