Ring Oxygen In The Additional Hetero Ring Patents (Class 546/281.7)
  • Patent number: 6596737
    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: February 2, 2001
    Date of Patent: July 22, 2003
    Assignee: FSU Research Foundation, Inc.
    Inventors: Robert A. Holton, Weishuo Fang
  • Publication number: 20030125559
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Application
    Filed: April 26, 2002
    Publication date: July 3, 2003
    Applicant: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Publication number: 20030125362
    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: March 14, 2001
    Publication date: July 3, 2003
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, Dong Fang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin
  • Publication number: 20030114493
    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: Application
    Filed: February 2, 2001
    Publication date: June 19, 2003
    Inventor: Robert A. Holton
  • Patent number: 6576643
    Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 17, 2001
    Date of Patent: June 10, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: William E. Bondinell, William H. Miller, Dirk Heerding, James M. Samanen
  • Publication number: 20030105330
    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: February 1, 2002
    Publication date: June 5, 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
  • Patent number: 6566375
    Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.
    Type: Grant
    Filed: April 26, 2001
    Date of Patent: May 20, 2003
    Assignee: Wyeth
    Inventor: Thomas J. Commons
  • Publication number: 20030083497
    Abstract: New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them.
    Type: Application
    Filed: March 13, 2002
    Publication date: May 1, 2003
    Applicant: Aventis Pharma, S.A.
    Inventors: Herve Bouchard, Jean-Dominique Bourzat, Alain Commercon
  • Publication number: 20030073205
    Abstract: Recombinant Myxococcus host cells can be used to produce polyketides, including epothilone and epothilone analogs that can be purified from the fermentation broth and crystallized.
    Type: Application
    Filed: September 19, 2001
    Publication date: April 17, 2003
    Inventors: Robert L. Arslanian, Gary Ashley, Scott Frykman, Bryan Julien, Leonard Katz, Chaitan Khosla, Janice Lau, Peter J. Licari, Rika Regentin, Daniel Santi, Li Tang
  • Publication number: 20030069277
    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: April 30, 2002
    Publication date: April 10, 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: 20030060638
    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: Application
    Filed: February 6, 2002
    Publication date: March 27, 2003
    Applicant: Florida State University Research Foundation Inc.
    Inventor: Robert A. Holton
  • Publication number: 20030045531
    Abstract: Taxane derivatives having a 3′ butenyl substituted C13 side chain.
    Type: Application
    Filed: March 29, 2002
    Publication date: March 6, 2003
    Applicant: Florida State University
    Inventors: Robert A. Holton, Ki-Byung Chai, Hossain Nadizadeh
  • Publication number: 20030040437
    Abstract: 1
    Type: Application
    Filed: June 22, 2001
    Publication date: February 27, 2003
    Inventors: Andrew Edmunds, Christoph Luthy, Karl Seckinger, Alain De Mesmaeker, Walter Kunz, Jurgen Schaetzer
  • Patent number: 6521643
    Abstract: A compound of formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NOS(nitric oxide synthasey)-mediated diseases such as adult respiratory distress syndrome, myocarditis, synovitis, septic shock, insulin-ependent diabetes mellitus, ulcerative colitis, cerebral infarction, rheumatoid arthritis, osteoarthritis, osteoporosis, systemic lupus erythematosus, rejection by organ transplantation, asthma, pain, ulcer, and the like in human being and animals.
    Type: Grant
    Filed: August 17, 2001
    Date of Patent: February 18, 2003
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaki Tomishima, Kazuhiko Take
  • Patent number: 6514996
    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 C
    Type: Grant
    Filed: November 19, 1997
    Date of Patent: February 4, 2003
    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
  • Publication number: 20030022903
    Abstract: Heterocyclic aromatic amides (HAA) according to Formula 1
    Type: Application
    Filed: December 13, 2001
    Publication date: January 30, 2003
    Inventors: Michael J. Ricks, William H. Dent, 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
  • Publication number: 20030022902
    Abstract: Heterocyclic aromatic amides (HAA) according to Formula I: 1
    Type: Application
    Filed: December 13, 2001
    Publication date: January 30, 2003
    Inventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, 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
  • Publication number: 20030018052
    Abstract: Heterocyclic aromatic amides (HAA) according to Formula 1
    Type: Application
    Filed: December 13, 2001
    Publication date: January 23, 2003
    Inventors: Michael J. Ricks, William H. Dent, 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
  • Patent number: 6509362
    Abstract: The present invention relates to the compounds of formula (I) in which X, R1, R2 and R3 are as defined in claim 1. These compounds are cholesteryl acyl transferase (ACAT) inhibitors.
    Type: Grant
    Filed: November 1, 2001
    Date of Patent: January 21, 2003
    Assignee: Merck Patent Gesellschaft mit Beschraenkter Haftung
    Inventors: Diedier Festal, Jean Yves Nioche, Guy Augert, Jacques Deserprit
  • Publication number: 20020198382
    Abstract: The invention relates to novel arylalkyl- or aryloxyalkyl-substituted oxiranecarboxyclic acids of the general formula I 1
    Type: Application
    Filed: June 18, 2002
    Publication date: December 26, 2002
    Inventor: Horst P.O. Wolf
  • Patent number: 6495568
    Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di
    Type: Grant
    Filed: October 12, 2001
    Date of Patent: December 17, 2002
    Assignee: Warner-Lambert Company
    Inventors: Kevin Neil Dack, Gavin Alistair Whitlock
  • Publication number: 20020177578
    Abstract: Heterocyclic aromatic amides (HAA) according to Formula I: 1
    Type: Application
    Filed: December 13, 2001
    Publication date: November 28, 2002
    Inventors: Michael J. Ricks, William H. Dent, 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
  • Publication number: 20020156285
    Abstract: Compounds of formula 1 1
    Type: Application
    Filed: January 31, 2002
    Publication date: October 24, 2002
    Inventors: Walter Kunz, Kurt Nebel
  • Publication number: 20020147335
    Abstract: Taxane derivatives having an alkyl substituted C13 side chain.
    Type: Application
    Filed: April 29, 2002
    Publication date: October 10, 2002
    Applicant: Florida State University
    Inventors: Robert A. Holton, Ki-Byung Chai, Hamid Idmoumaz, Hossain Nadizadeh, Yukio Suzuki
  • Publication number: 20020143178
    Abstract: This invention is to provide a novel taxol derivative useful as an antitumor compound having respective substituent groups, represented by the following formula (I) which can be orally administered.
    Type: Application
    Filed: March 6, 2002
    Publication date: October 3, 2002
    Applicant: DAIICHI PHARMACEUTICAL CO., LTD.
    Inventors: Tsunehiko Soga, Kouichi Uoto, Yasuyuki Takeda
  • Patent number: 6451845
    Abstract: This invention provides compounds of Formula I having the structure wherein R1 and R2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy; R3 and R4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, perfluoroalkoxy of 1-6 carbon atoms, alkanoyloxy of 2-7 carbon atoms, perfluoroalkanoyloxy of 2-7 carbon atoms, arylalkoxy of 7-15 carbon atoms, aryloxy of 6-12 carbon atoms, aroyloxy of 6-12 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, nitrile, nitro, amino, —NHSO2CF3, carbamoyl, carbo
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: September 17, 2002
    Assignee: Wyeth
    Inventors: Paul J. Dollings, Robert E. McDevitt, Folake O. Adebayo
  • Publication number: 20020128471
    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 8, 2002
    Publication date: September 12, 2002
    Inventors: Gary Ashley, Brian Metcalf
  • Publication number: 20020091274
    Abstract: Taxane derivatives having an amino substituted C13 side chain.
    Type: Application
    Filed: February 25, 2002
    Publication date: July 11, 2002
    Applicant: Florida State University
    Inventors: Robert A. Holton, Hossain Nadizadeh, Kasthuri Rengan, Chunlin Tao
  • Publication number: 20020091264
    Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: 1
    Type: Application
    Filed: December 17, 2001
    Publication date: July 11, 2002
    Applicant: SmithKline Beecham Corporation
    Inventors: William E. Bondinell, William H. Miller, Dirk Heerding, James M. Samanen
  • Publication number: 20020091131
    Abstract: Novel epoxysuccinamide derivatives represented by the general formula (1) or physiologically acceptable salts thereof, which are useful particularly as remedies for bone diseases and arthritis, wherein R1 and R3 are each hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; R2 is alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a hetericyclic-alkyl group; X is —O— or —NR4— (wherein R4 is hydrogen, alkyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; Y1 is OR5, SR6, or NR7R8 (wherein each of R5, R6 and R7 is hydrogen, alkyl, aryl, aralkyl, acyl, a heterocyclic group, or a heterocyclic-alkyl group, and R8 is the same as defined for R4); and Y2 is hydrogen or alkyl, or alternatively Y1 and Y2 can be combined to form ═O, ═S, ═N—R9, or ═N—OR10 (wherein each of R9 and R10 is the same as defined for R4), provided that each of the alkyl, aryl and heterocyclic groups defined fo
    Type: Application
    Filed: January 8, 2002
    Publication date: July 11, 2002
    Inventors: Yutaka Nomura, Toshihiro Takahashi, Yasushi Yoshino, Koichiro Nishioka
  • Publication number: 20020077341
    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: February 2, 2001
    Publication date: June 20, 2002
    Inventors: Robert A. Holton, Weishuo Fang
  • Patent number: 6407268
    Abstract: 4-Benzoylpyrazoles of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR10, —OCOR10, —OSO2R10, —S(O)nR10, —SO2OR10, —SO2NR3R10, —NR10SO2R10 or —NR10COR; Q is a pyrazole of the formula II,  which is attached in position 4 and, Substituted 4-benzoylpyralozoles.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: June 18, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Stefan Engel, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Guido Mayer, Martina Otten, Joachim Rheinheimer, Oliver Wagner, Matthias Witschel, Ulf Misslitz, Helmut Walter
  • Publication number: 20020068755
    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: Application
    Filed: February 2, 2001
    Publication date: June 6, 2002
    Inventor: Robert A. Holton
  • Publication number: 20020065305
    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: Application
    Filed: February 2, 2001
    Publication date: May 30, 2002
    Inventor: Robert A. Holton
  • Patent number: 6395738
    Abstract: The present invention relates to benzofuran derivatives represented by following general formula (I): wherein R1 represents lower alkyl, R2 represents hydrogen or substituted or unsubstituted lower alkyl, R3, R4, R5 and R6 independently represent hydrogen or lower alkyl, X represents CH2 or C═O, and Y represents CH2 or NH, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 29, 2000
    Date of Patent: May 28, 2002
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Tohru Matsuzaki, Haruhiko Manabe
  • Publication number: 20020058817
    Abstract: The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
    Type: Application
    Filed: March 1, 2001
    Publication date: May 16, 2002
    Inventors: Samuel J. Danishefsky, Shawn J. Stachel, Chul Bom Lee, Mark D. Chappell, Zhicai Wu
  • Patent number: 6387931
    Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di
    Type: Grant
    Filed: October 12, 2001
    Date of Patent: May 14, 2002
    Assignee: Pfizer INC
    Inventors: Kevin Neil Dack, Gavin Alistair Whitlock
  • Patent number: 6387908
    Abstract: Epoxysuccinamide derivatives of the formula (1): wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or aralkyl; R2 is alkyl, alkenyl, alkynyl, aryl, or aralkyl; R3 is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl; X is —O— or —NR4— (R4 is hydrogen, alkyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl); Y1 is OR5, SR6, or NR7R8; and Y2 is hydrogen or alkyl. The compounds are useful as remedies for bone diseases and arthritis.
    Type: Grant
    Filed: May 5, 2000
    Date of Patent: May 14, 2002
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Yutaka Nomura, Toshihiro Takahashi, Yasushi Yoshino, Koichiro Nishioka
  • Publication number: 20020045750
    Abstract: The present invention concerns a new general process for asymetric hemisynthesis of harringtonines and their analogs, that are alcaloïds used in chimiotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and fonctionalization are entirely preformed.
    Type: Application
    Filed: March 27, 2001
    Publication date: April 18, 2002
    Inventors: Jean-Pierre Robin, Julie Blanchard, Sylvie Cavoleau, Ludovic Chauviat, Sandra Charbonnel, Robert Dhal, Gilles Dujardin, Florence Fournier, Chrystelle Gilet, Laurent Girodier, Laurence Mevelec, Sandrine Poutot, Sylvie Rouaud
  • Publication number: 20020015804
    Abstract: There can be provided a liquid crystalline compound expressed by the general formula (1): 1
    Type: Application
    Filed: July 22, 1999
    Publication date: February 7, 2002
    Inventors: YASUHIRO HASEBA, SHUICHI MATSUI, KAZUTOSHI MIYAZAWA, NORIHISA HACHIYA, ETSUO NAKAGAWA
  • Publication number: 20020013346
    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: February 2, 2001
    Publication date: January 31, 2002
    Inventor: Robert A. Holton
  • Patent number: 6340676
    Abstract: This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R2)W, —C(CH3)2CO2R3, 5-thiazolidine-2,4-dione, —CH(R4)CH2CO2R3, —COR3, or —PO3(R3)2; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, —CH2(1H-imidazol-4-yl), —CH2(3-1H-indolyl), —CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), —CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or —CH2(3-pyridyl); W is —CO R3, —CONH2, —CONHOH, —CN, CONH(CH2)2CN, 5-tetrazole, or —PO3(R3)2; R3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: January 22, 2002
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Zenan Li
  • Patent number: 6333349
    Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: December 25, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
  • Publication number: 20010051640
    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: Application
    Filed: February 2, 2001
    Publication date: December 13, 2001
    Inventor: Robert A. Holton
  • Publication number: 20010051639
    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: Application
    Filed: February 2, 2001
    Publication date: December 13, 2001
    Inventor: Robert A. Holton
  • Patent number: 6316630
    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: Grant
    Filed: June 6, 2000
    Date of Patent: November 13, 2001
    Assignee: Sloan Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin
  • Patent number: 6288235
    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: April 11, 2000
    Date of Patent: September 11, 2001
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Wenying Chai, William V. Murray
  • Publication number: 20010014689
    Abstract: The present invention relates to 2-aminopyridine derivatives of the formula I: 1
    Type: Application
    Filed: February 8, 2001
    Publication date: August 16, 2001
    Inventor: John A. Lowe
  • Patent number: 6271384
    Abstract: Onium salts of taxo-diterpenoid-Cn,2-O-aza-arenes form water soluble self-assembling nanostructures above a critical aggregation concentration. The onium salt of aza-arene includes a delocalized charge which renders derivatized taxo-diterpenoids amphoteric, enhances their solubility in water, and promotes self-assembly of water soluble nanostructures, e.g., helical fibular structures and spherical micellular structures. These same onium salts of taxo-diterpenoid-Cn,2-O-aza-arenes are employed as water soluble prodrugs. For example, taxol-2′-methylpyridinium tosylate (MPT) is characterized by an elevated aqueous solubility, rapid activation by serum protein, good stability in most other aqueous solutions, formation of a protein:taxol intermediate and good retention within the circulatory system. The toxicity of the activated form is comparable or greater than underivatized taxol. Furthermore, taxol-2′-MPT can be synthesized by a simple one step reaction between taxol and 2-fluoro-1-MPT.
    Type: Grant
    Filed: April 13, 1998
    Date of Patent: August 7, 2001
    Assignee: The Scripps Research Institute
    Inventors: K. C. Nicolaou, Wolfgang Wrasidlo, Rodney K. Guy, Emmanuel Pitsinos
  • Patent number: RE38117
    Abstract: Described herein are novel trioxane dimers of structure which possess antiproliferative and antitumor activities.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: May 6, 2003
    Assignees: Hauser, Inc., Johns Hopkins
    Inventors: Qun Y. Zheng, Christopher Murray, Randall J. Daughenbaugh, Poonsakdi Ploypradith, Gary H. Posner