Chalcogen Attached Indirectly To The Bicyclo Ring System By Acyclic Nonionic Bonding Patents (Class 548/509)
  • Patent number: 7173129
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: February 6, 2007
    Assignee: Athero Genics, Inc.
    Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
  • Patent number: 7138418
    Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: November 21, 2006
    Assignee: Amgen, Inc.
    Inventors: John Flygare, Julio C. Medina, Bei Shan, David L. Clark, Terry J. Rosen
  • Patent number: 7109231
    Abstract: A novel class of tricyclic compounds of the following formula (I): (formula I); is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shock
    Type: Grant
    Filed: July 29, 2002
    Date of Patent: September 19, 2006
    Assignee: Eli Lilly and Company
    Inventors: Michael Dean Kinnick, Edward David Mihelich, John Michael Morin, Jr., Daniel Jon Sall, Jason Scott Sawyer
  • Patent number: 7087750
    Abstract: The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.
    Type: Grant
    Filed: October 22, 2001
    Date of Patent: August 8, 2006
    Assignee: Biovitrum AB
    Inventors: Patrizia Caldirola, Björn M. Nilsson, Gary Johansson
  • Patent number: 7057052
    Abstract: Pyrrolylquinones and indolylquinones useful for treating diseases such as neurodegenerative disease, viral infections and proliferative disease are described, along with methods of making such compounds and pharmaceutical formulations containing such compounds.
    Type: Grant
    Filed: September 26, 2002
    Date of Patent: June 6, 2006
    Assignee: Duke University
    Inventors: Michael C. Pirrung, Johannes Rudolph
  • Patent number: 6962929
    Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: November 8, 2005
    Assignee: Tularik Inc.
    Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
  • Patent number: 6924304
    Abstract: Compounds having formula (I) inhibit cellular proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: August 2, 2005
    Assignee: Abbott Laboratories
    Inventors: Qun Li, Hing Sham, Keith W. Woods, Beth A. Steiner, Stephen L. Gwaltney, II, Kenneth J. Barr, Hovis M. Imade, Saul Rosenberg
  • Patent number: 6867200
    Abstract: The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: March 15, 2005
    Assignee: Axys Pharmaceuticals, Inc.
    Inventors: Darin A. Allen, Jason M. Hataye, Witold N. Hruzewicz, Aleksandr Kolesnikov, Richard L. Mackman, Roopa Rai, Spencer R. Jeffrey, Erik J. Verner, Wendy B. Young, William Dvorak Shrader
  • Patent number: 6852711
    Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
    Type: Grant
    Filed: November 19, 2002
    Date of Patent: February 8, 2005
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Michael James Lovdahl, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
  • Patent number: 6825352
    Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.
    Type: Grant
    Filed: August 30, 2002
    Date of Patent: November 30, 2004
    Assignee: Wyeth
    Inventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan
  • Publication number: 20040214869
    Abstract: This invention provides compounds of Formula I having the structure 1
    Type: Application
    Filed: May 11, 2004
    Publication date: October 28, 2004
    Applicant: Wyeth
    Inventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
  • Patent number: 6770638
    Abstract: Pharmaceutical composite compositions comprising tetrahydroindolones linked to arylpiperazines and derivatives thereof are disclosed. Specifically, composite compositions useful in treating anti-psychotic disorders are disclosed. The composite compositions disclosed herein can effectively ameliorate symptoms and treat psychotic disorders without causing a decrease in cognitive function. Generally, the composite compounds consist of two moieties, moiety A and B in which a tetrahydroindolone comprises a moiety A linked through a linker L to a moiety B, where B is an arylpiperazinyl moiety. The composite compound provides anti-psychotic actively by interaction with GABA, seratoninne and dopamine receptors. The composite molecules with the combined activities will provide treat psychiatric and neurological diseases without cognitive impairment.
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: August 3, 2004
    Assignee: Spectrum Pharmaceuticals, Inc.
    Inventors: David B. Fick, Mark M. Foreman, Alvin J. Glasky, David R. Helton
  • Publication number: 20040110951
    Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands.
    Type: Application
    Filed: July 11, 2003
    Publication date: June 10, 2004
    Inventor: Yuan-Ching P. Chiang
  • Patent number: 6743810
    Abstract: Indol-3-yl derivatives of the general formula I in which A, B, X, R1, R2, R3, R4, R5, n and m are as defined in patent claim 1, and their physiologically acceptable salts or solvates are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumours, osteoporosis, rheumatic arthritis, macular degenerative disease, diabetic retinopathy, infections and restenosis after angioplasty or in pathological processes maintained or propagated by angiogenesis.
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: June 1, 2004
    Assignee: Merck Patent GmbH
    Inventors: Matthias Wiesner, Simon Goodman, Rudolf Gottschlich
  • Patent number: 6727237
    Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.
    Type: Grant
    Filed: October 25, 2002
    Date of Patent: April 27, 2004
    Inventors: Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanadan E. Velu
  • Publication number: 20040029948
    Abstract: A class of novel indole is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
    Type: Application
    Filed: July 30, 2003
    Publication date: February 12, 2004
    Inventors: Richard Waltz Harper, Ho-Shen Lin, Michael Enrico Richett
  • Publication number: 20040029913
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: February 24, 2003
    Publication date: February 12, 2004
    Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
  • Publication number: 20040006231
    Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.
    Type: Application
    Filed: April 11, 2003
    Publication date: January 8, 2004
    Inventors: Robert Lee Bosch, Richard Joseph McCabe, Thomas Norman Nanninga, Robert Joseph Stahl
  • Publication number: 20040006104
    Abstract: The invention provides novel compounds selected from the group consisting of: 1
    Type: Application
    Filed: February 18, 2003
    Publication date: January 8, 2004
    Applicant: The Procter & Gamble Company
    Inventors: Rodney Dean Bush, Paul Mitchell Hershberger, Judith Anne Young, Bhavani Kasibhatla
  • Patent number: 6673787
    Abstract: The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an indole compound represented by the following formula (I), its pharmacologically acceptable salt or hydrates thereof. In the formula, R1 represents hydrogen atom, a halogen atom or cyano group; R2 and R3 are the same as or different from and each represents hydrogen atom, a C1-C4 lower alkyl group or a halogen atom; R4 represents hydrogen atom or a C1-C4 lower alkyl group; and the ring A represents cyanophenyl group, aminosulfonylphenyl group, aminopyridyl group, aminopyrimidyl group, a halopyridyl group or cyanothiophenyl group, provided that the case where all of R1, R2 and R3 are hydrogen atoms, where both R2 and R3 are hydrogen atoms or where the ring A is aminosulfonyl group and both R1 and R2 are halogen atoms is excluded.
    Type: Grant
    Filed: March 18, 2002
    Date of Patent: January 6, 2004
    Assignee: Eisai Co., Ltd.
    Inventors: Toru Haneda, Akihiko Tsuruoka, Junichi Kamata, Tadashi Okabe, Keiko Takahashi, Kazumasa Nara, Shinichi Hamaoka, Norihiro Ueda, Takashi Owa, Toshiaki Wakabayashi, Yasuhiro Funahashi, Taro Semba, Naoko Hata, Yuji Yamamoto, Yoichi Ozawa, Noako Tsukahara
  • Publication number: 20030191175
    Abstract: A class of novel acylsulfonaimide substituted indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shock.
    Type: Application
    Filed: March 21, 2003
    Publication date: October 9, 2003
    Inventors: Edward David Mihelich, Michael LeRoy Phillips, Alan M. Warshawsky
  • Patent number: 6620947
    Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.
    Type: Grant
    Filed: August 26, 2002
    Date of Patent: September 16, 2003
    Assignee: Alcon, Inc.
    Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
  • Publication number: 20030158405
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: November 22, 2002
    Publication date: August 21, 2003
    Applicant: Wyeth
    Inventors: John C. McKew, Steve Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
  • Publication number: 20030088100
    Abstract: A process for producing an optically active propargyl alcohol represented by the following formula (4): 1
    Type: Application
    Filed: September 3, 2002
    Publication date: May 8, 2003
    Applicant: Sumika Fine Chemicals Co., Ltd.
    Inventor: Erick M. Carreira
  • Publication number: 20030040533
    Abstract: Compounds of formula (I): 1
    Type: Application
    Filed: August 2, 2002
    Publication date: February 27, 2003
    Inventors: Daniel Lesieur, Elodie Blanc-Delmas, Said Yous, Patrick Depreux, Gerald Guillaumet, Catherine Dacquet, Nigel Levens, Jean Albert Boutin, Caroline Bennejean, Pierre Renard
  • Patent number: 6503938
    Abstract: 2-phenylindoles are described, as well as a process for making them, pharmaceutical preparations that contain them, methods of using them as pharmaceutical agents.
    Type: Grant
    Filed: May 26, 2000
    Date of Patent: January 7, 2003
    Assignee: Schering Aktiengesellschaft
    Inventors: Erwin Von Angerer, Christian Biberger, Martin Schneider
  • Patent number: 6500853
    Abstract: This invention concerns compounds and pharmaceutical compositions useful for treating or preventing inflammatory conditions in a mammal, the methods comprising administration of novel pharmaceutically useful compounds of the general formulae: or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined in the specification.
    Type: Grant
    Filed: October 11, 2000
    Date of Patent: December 31, 2002
    Assignee: Genetics Institute, LLC
    Inventors: Jasbir S. Seehra, John C. McKew, Frank Lovering, Jean E. Bemis, YiBin Xiang, Lihren Chen, John L. Knopf
  • Patent number: 6500852
    Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.
    Type: Grant
    Filed: July 14, 2000
    Date of Patent: December 31, 2002
    Assignee: University of Alabama Research Foundation
    Inventors: Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanandan E. Velu
  • Patent number: 6495546
    Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.
    Type: Grant
    Filed: November 22, 2000
    Date of Patent: December 17, 2002
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • Patent number: 6482860
    Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: July 18, 1997
    Date of Patent: November 19, 2002
    Assignee: Tularik Inc.
    Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
  • Publication number: 20020165251
    Abstract: The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): 1
    Type: Application
    Filed: October 22, 2001
    Publication date: November 7, 2002
    Inventors: Patrizia Caldirola, Bjorn M. Nilsson, Gary Johansson
  • Publication number: 20020161021
    Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.
    Type: Application
    Filed: June 11, 2002
    Publication date: October 31, 2002
    Inventors: Robert Lee Bosch, Richard Joseph McCabe, Thomas Norman Nanninga, Robert Joseph Stahl
  • Patent number: 6469043
    Abstract: The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an indole compound represented by the following formula (I), its pharmacologically acceptable salt or hydrates thereof. In the formula, R1 represents hydrogen atom, a halogen atom or cyano group; R2 and R3 are the same as or different from and each represents hydrogen atom, a C1˜C4 lower alkyl group or a halogen atom; R4 represents hydrogen atom or a C1˜C4 lower alkyl group; and the ring A represents cyanophenyl group, aminosulfonylphenyl group, aminopyridyl group, aminopyrimidyl group, a halopyridyl group or cyanothiophenyl group, provided that the case where all of R1, R2 and R3 are hydrogen atoms, where both R2 and R3 are hydrogen atoms or where the ring A is aminosulfonyl group and both R1 and R2 are halogen atoms is excluded.
    Type: Grant
    Filed: September 28, 2000
    Date of Patent: October 22, 2002
    Assignee: Eisai Co., Ltd.
    Inventors: Toru Haneda, Akihiko Tsuruoka, Junichi Kamata, Tadashi Okabe, Keiko Takahashi, Kazumasa Nara, Shinichi Hamaoka, Norihiro Ueda, Takashi Owa, Toshiaki Wakabayashi, Yasuhiro Funahashi, Taro Semba, Naoko Hata, Yuji Yamamoto, Yoichi Ozawa, Noako Tsukahara
  • Patent number: 6448243
    Abstract: A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, R4 and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3.) The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.
    Type: Grant
    Filed: August 11, 1999
    Date of Patent: September 10, 2002
    Assignee: Eisai Co., Ltd.
    Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
  • Patent number: 6414008
    Abstract: New disubstituted bicyclic heterocycles of general formula Ra—A—Het—B—Ar—E  (I) Compounds of general formula I, wherein E is an RbNH—C(═NH)— group, have valuable pharmacological properties, particularly a thrombin-inhibiting effect and the effect of prolonging thrombin time, and those wherein E is a cyano group, are valuable intermediates for preparing the other compounds of general formula I.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: July 2, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Norbert Hauel, Henning Priepke, Uwe Ries, Jean Marie Stassen, Wolfgang Wienen
  • Patent number: 6365584
    Abstract: Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesulphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethlylaminoethyl)-benzylsulfonylamino]-benzimidazole; and, 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(3-diethylaminopropyl)-benzenesulphonylamino]-benzimidazole.
    Type: Grant
    Filed: September 21, 2000
    Date of Patent: April 2, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Ralf Anderskewitz, Christine Braun, Hans Briem, Bernd Disse, Christoph Hoenke, Hans Michael Jennewein, Georg Speck
  • Publication number: 20020015938
    Abstract: The invention relates to a method of simultaneous high-throughput preformulation quantification of potential drug candidates, where an aliquot of a mixture of solutions containing different compounds is injected into a high pressure liquid chromatograph. The concentration of each compound can be determined by high pressure liquid chromatographic analysis, and correlated to a physico-chemical property of the compound.
    Type: Application
    Filed: October 29, 1998
    Publication date: February 7, 2002
    Inventor: NARMADA SHENOY
  • Patent number: 6323235
    Abstract: Novel compounds having strong TXA2 receptor antagonist activities and PGI2 receptor agonist activities, which are effective for therapy and prevention of diseases related to TXA2, are disclosed. The compound of the present invention is represented by the following formula (I). (wherein the meanings of the symbols in the formula are as described in the specification).
    Type: Grant
    Filed: January 13, 2000
    Date of Patent: November 27, 2001
    Inventors: Atsushi Ohtake, Kazuhiro Hoshi, Shunji Tsukamoto, Takahiro Takeda, Naohiro Yamada, Kazuhisa Matsumoto, Michihiro Ohno, Kiyotaka Ohno
  • Publication number: 20010021719
    Abstract: The present invention relates to new 2-Phenyl-1-[(2-Aminoethoxy)-Benzyl]-Indole compounds which are usefuil as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utiig these compounds, which have the general structures below: 1
    Type: Application
    Filed: February 8, 2001
    Publication date: September 13, 2001
    Inventors: Chris P. Miller, Michael D. Collini, Bach D. Tran, Arthur A. Santilli
  • Patent number: 6277833
    Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.
    Type: Grant
    Filed: September 24, 1998
    Date of Patent: August 21, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Peter Fey, Walter Hübsch, Thomas Philipps, Hilmar Bischoff, Hans-Peter Krause, Jörg Petersen von Gehr, Delf Schmidt
  • Patent number: 6245761
    Abstract: This invention provides a series of substituted indoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides the novel substituted indoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these substituted indoles.
    Type: Grant
    Filed: August 29, 1996
    Date of Patent: June 12, 2001
    Assignee: Eli Lilly and Company
    Inventors: Thomas C. Britton, Robert F. Bruns, Jr., Donald R. Gehlert, Philip A. Hipskind, Karen L. Lobb, James A. Nixon, Paul L. Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis M. Zimmerman
  • Patent number: 6242637
    Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: June 5, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 6214790
    Abstract: The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: April 10, 2001
    Assignee: Mayo Foundation for Medical Education And Research
    Inventors: Elliott Richelson, Bernadette Marie Cusack, Yuan-Ping Pang, Daniel J. McCormick, Abdul Fauq, Beth Marie Tyler, Mona Boules
  • Patent number: 6147082
    Abstract: The invention relates to a novel class of compounds that have structures related to certain naturally occurring or synthetic chalcones. The invention also relates to pharmaceutical compositions comprising the compounds and methods for treating certain disorders using the pharmaceutical compositions. The invention further relates to process for synthesizing the novel class of compounds.
    Type: Grant
    Filed: December 8, 1999
    Date of Patent: November 14, 2000
    Inventors: Ezio Bombardelli, Piero Valenti
  • Patent number: 6133305
    Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.
    Type: Grant
    Filed: September 25, 1998
    Date of Patent: October 17, 2000
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Patent number: 6121308
    Abstract: Novel disubstituted bicyclic heterocycles, of which the following are exemplary:(a) 1-methyl-2-[(4-amidinophenyl)-oxymethyl]-5-[N-(hydroxycarbonylmethyl)-quin oline-8-sulphonylamino]-benzimidazole,(b) 1-methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(N-(hydroxycarbonylmethyl)-ami nocarbonylmethyl)-quinoline-8-sulphonylamino]-benzimidazole,(c) 1-methyl-2-[N-(4-amidinophenyl)-aminomethyl]-5-[N-(hydroxycarbonylmethyl)- quinoline-8-sulphonylamino]-benzimidazole and(d) 1-methyl-2-[N-(4-amidinophenyl)-aminomethyl]-5-[N-(hydroxycarbonylmethyl)- quinoline-8-sulphonylamino]-indole.These are useful for the treatment of thrombotic disease.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: September 19, 2000
    Assignee: Boehringer Ingelheim KG
    Inventors: Norbert Hauel, Uwe Ries, Henning Priepke, Gerhard Mihm, Wolfgang Wienen, Jean Marie Stassen, Klaus Binder, Rainer Zimmermann
  • Patent number: 6110957
    Abstract: The present invention relates to novel synthetic methods for the preparation of indolylquinones. The methods of the present invention are directed to synthetic reactions involving indoles and halo-quinones in solvent and in the presence of a metal carbonate. The invention also relates to bis- and mono-indolylquinones of high purity and pharmaceutical compositions containing the same.
    Type: Grant
    Filed: May 5, 1998
    Date of Patent: August 29, 2000
    Assignee: Sugen, Inc.
    Inventors: Peng C. Tang, G. Davis Harris, Jr.
  • Patent number: 6090839
    Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
  • Patent number: 5994546
    Abstract: Disclosed are 4-(N,N-dialkylamino)aniline compounds having a 4-N substituent which is a polyethyleneoxy group and which forms a condensed ring with benzene ring, such as aniline compounds having the following structure, a processing composition containing such a compound and a method for forming a color image with the processing solution. The aniline compound is useful as a color developing agent capable of having a low fog density and sufficient yellow and cyan image densities and suitable for the rapid process.
    Type: Grant
    Filed: February 11, 1998
    Date of Patent: November 30, 1999
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Keizo Kimura, Shigeo Hirano, Hiroshi Kawamoto
  • Patent number: 5972982
    Abstract: Heteroaryl-substituted deoxy glycerols represented by the general Formulas Ia, Ib and Ic: ##STR1## wherein: X is oxygen (--O--) or sulfur (--S--); R is substituted or unsubstituted straight or branched chain C.sub.1-30 alkyl or alkenyl, provided that a double bond of the alkenyl does not originate at the carbon atom bound to the X substituent; Het is a 5- to 9-membered heteroaryl mono- or bicyclic ring system having no more than 1 carbonyl carbon in the ring system, with 1 to 4 nitrogen atoms as the sole heteroatoms, one of which nitrogens is bonded to the glycero carbon; and Y is hydroxyl (--OH) or thiol (--SH), pharmaceutical compositions containing the same, and methods of using the compounds, are disclosed. The compounds exhibit antiviral and antibacterial activities.
    Type: Grant
    Filed: October 7, 1997
    Date of Patent: October 26, 1999
    Assignee: Clarion Pharmaceuticals Inc.
    Inventors: Haridasan K. Nair, Andrew C. Peterson, Friedrich Paltauf, Albin Hermetter, Rudolf Franzmair