Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To Ring Carbon Of The Five-membered Hetero Ring By An Acyclic Carbon Or Acyclic Carbon Chain (e.g., Indole-3-acetic Acid, Etc.) Patents (Class 548/494)
  • Patent number: 6069164
    Abstract: A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed methods relate to the administration of melatonin at times determined with relation to the time of dim light endogenous melatonin onset. Embodiments capable of alleviating the effects of jet lag, winter depression and shiftwork sleep disturbance are provided.
    Type: Grant
    Filed: January 6, 1997
    Date of Patent: May 30, 2000
    Assignee: Oregon Health Sciences University
    Inventors: Alfred J. Lewy, Robert L. Sack
  • Patent number: 6046138
    Abstract: An indole derivative having the formula (I) or (II) and root formation inducing agents wherein these indole derivatives are an effective ingredient: ##STR1## wherein, R does not exist or represents a C.sub.1 to C.sub.4 alkylene group.
    Type: Grant
    Filed: March 10, 1998
    Date of Patent: April 4, 2000
    Assignee: Shiseido Company, Ltd.
    Inventors: Mineyuki Yokoyama, Shoko Yamaguchi, Seiichi Yoshida, Okihiko Sakamoto, Kiyotaka Kojima
  • Patent number: 6017945
    Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R.sup.1 and R.sup.2 are optional substituents and independently represent C.sub.1-6 alkyl, C.sub.2-6 alkenyl [optionally substituted by CO.sub.2 H or CO.sub.2 (C.sub.1-6 alkyl)], C.sub.2-6 alkynyl, halogen, C.sub.1-3 perfluoroalkyl, (CH.sub.2).sub.m Ar.sup.1, (CH.sub.2).sub.m Het.sup.1, (CH.sub.2).sub.m CONR.sup.7 R.sup.8, (CH.sub.2).sub.m CO.sub.2 R.sup.8, O(CH.sub.2).sub.q CO.sub.2 R.sup.8, (CH.sub.2).sub.m COR.sup.8, (CH.sub.2).sub.m OR.sup.8, O(CH.sub.2).sub.p OR.sup.8, (CH.sub.2).sub.m NR.sup.7 R.sup.8, CO.sub.2 (CH.sub.2).sub.q NR.sup.7 R.sup.8, (CH.sub.2).sub.m CN, S(O).sub.n R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, CONH(CH.sub.2).sub.m Ar.sup.1 or CONH(CH.sub.2).sub.m Het.sup.1 ; R.sup.3 represents H, C.sub.1-6, alkyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, SO.sub.2 R.sup.10, SO.sub.2 NR.sup.9 R.sup.10, (CH.sub.2).sub.m COR.sup.10, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, (CH.sub.2).sub.m CONR.sup.9 R.sup.10, (CH.sub.2).sub.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: January 25, 2000
    Assignee: Pfizer Inc.
    Inventors: David James Rawson, Kevin Neil Dack, Roger Peter Dickinson, Kim James
  • Patent number: 6015830
    Abstract: Antibacterial compounds for Ralstonia solanacearum having substantially (S)-3-(3-indolyl) butanoic acid of a specified structure or its salt as active component can selectively inhibit the growth of Ralstonia solanacearum and suppress bacterial wilt dependably even if used at relatively lower concentration.
    Type: Grant
    Filed: January 13, 1999
    Date of Patent: January 18, 2000
    Assignee: Kagome Kabushiki Kaisha
    Inventors: Kazuhiko Matsuda, Hideyoshi Toyoda, Satoshi Harada
  • Patent number: 6004536
    Abstract: The present invention relates to a family of cyanine dyes possessing lipophilic alkyl chains and either one or more reactive functional groups, bromo or chloro, or phenyl, sulfophenyl or polysulfophenyl substituents or combinations thereof. The dyes of the invention are useful for staining membranes in cells or isolated from cells, and are well-retained therein. Additionally, the reactive dyes of the invention are useful for preparing dye-conjugates, thereby conferring the membrane staining ability of the subject dye onto the resulting dye-conjugate.
    Type: Grant
    Filed: August 14, 1996
    Date of Patent: December 21, 1999
    Assignee: Molecular Probes, Inc.
    Inventors: Wai-Yee Leung, Richard P. Haugland, Fei Mao
  • Patent number: 5981569
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: November 9, 1999
    Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem, Sugen, Inc.
    Inventors: Harald App, Gerald M. McMahon, Peng Cho Tang, Aviv Gazit, Alexander Levitzki
  • Patent number: 5955492
    Abstract: This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: September 24, 1998
    Date of Patent: September 21, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Scott K. Thompson, Stacie M. Halbert, Katherine L. Widdowson
  • Patent number: 5952355
    Abstract: The present invention relates to propenone derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or YR.sup.5 (wherein Y represents S or O; and R.sup.5 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a substituted or unsubstituted cyclic ether residue); R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, or substituted or unsubstituted aralkyl, or alternatively R.sup.2 and R.sup.3 are combined to form substituted or unsubstituted methylene or ethylene; R.sup.4 represents hydrogen, hydroxy, lower alkyl, substituted or unsubstituted aralkyl, lower alkoxy, substituted or unsubstituted aralkyloxy, or halogen; and X represents substituted or unsubstituted indolyl; or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 26, 1996
    Date of Patent: September 14, 1999
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Shun-Ichi Ikeda, Uichiro Kimura, Tadashi Ashizawa, Katsushige Gomi, Hiromitsu Saito, Masaji Kasai, Junji Kanazawa, Kimihito Sasaki, Etsuko Nukui, Masami Okabe, Soichiro Sato
  • Patent number: 5942544
    Abstract: The present application describes m-amidino phenyl analogs of formula I: ##STR1## wherein D can be amidino and E can be phenyl, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: February 19, 1997
    Date of Patent: August 24, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Thomas Peter Maduskuie, Jr., Joseph Cacciola, John Matthew Fevig, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
  • Patent number: 5936097
    Abstract: Novel products of formula (I): ##STR1## preparation thereof and pharmaceutical compositions containing said products are disclosed. In formula (I), R is a group of formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z, where X.sub.1 is a simple bond or O or S, n is 0 or 1 and n is 0, 1 or 2, the CH.sub.2 groups being optionally substituted by carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, amino, alkylamino or dialkylamino, and Z is carboxy, COOR.sub.4, where R.sub.4 is alkyl, or CON(R.sub.5)(R.sub.6), where R.sub.5 hydrogen or alkyl and R.sub.6 is hydrogen or optionally substituted alkyl, or else R.sub.5 is hydrogen or alkyl and R.sub.6 is hydroxy, optionally substituted alkoxy or amino, or PO(OR.sub.7).sub.2, where R.sub.7 is hydrogen or alkyl; or a group --NH--CO--T where T is hydrogen or optionally substituted alkyl; or else a group (a); R.sub.1 and R.sub.2 are hydrogen or halogen or optionally substituted alkyloxy or alkyl, or else R.sub.1 and R.sub.
    Type: Grant
    Filed: July 23, 1998
    Date of Patent: August 10, 1999
    Assignee: Rhone-Poulenc Rorer, S.A.
    Inventors: Alain Commer.cedilla.on, Alain Le Brun, Patrick Mailliet, Jean-Fran.cedilla.ois Peyronel, Fabienne Sounigo-Thompson, Alain Truchon, Martine Zucco
  • Patent number: 5919943
    Abstract: A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: December 16, 1997
    Date of Patent: July 6, 1999
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
  • Patent number: 5919810
    Abstract: A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: May 14, 1997
    Date of Patent: July 6, 1999
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
  • Patent number: 5886191
    Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.
    Type: Grant
    Filed: August 18, 1997
    Date of Patent: March 23, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
  • Patent number: 5877202
    Abstract: The present invention relates to novel indole derivatives useful in down-regulating estrogen receptor expression. Also included are methods for the treatment of neoplasms or of controlling the growth of a neoplasm in a patient afflicted with a neoplastic disease, especially estrogen-dependent neoplasms such as those associated with breast, ovarian and cervical tissue. Another embodiment of the present invention is a method of prophylactically treating a patient at risk of developing a neoplastic disease state. Also provided is a method for treating autoimmune diseases. Also included are pharmaceutical compositions of the novel indole derivatives.
    Type: Grant
    Filed: January 31, 1996
    Date of Patent: March 2, 1999
    Inventors: Alan J. Bitonti, Ian A. McDonald, Francesco G. Salituro, Jeffrey P. Whitten, Esa T. Jarvi, Paul S. Wright
  • Patent number: 5869691
    Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: February 9, 1999
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Stephen Richard Baker, Jesus Ezquerra Carrera, Carlos Lamas Peteira, Concepcion Pedregal Tercero
  • Patent number: 5854277
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: December 29, 1998
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, William Harrison Bullock, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, Jill Elizabeth Wood, David Ross Brittelli
  • Patent number: 5847135
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: December 8, 1998
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
  • Patent number: 5840726
    Abstract: The present invention relates to substituted piperazinone derivatives (compounds of formula (1)) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis. The present invention also relates to intermediates useful in the preparation of compounds of formula (1).
    Type: Grant
    Filed: June 19, 1997
    Date of Patent: November 24, 1998
    Assignee: Hoechst Marion Roussel Inc.
    Inventors: Timothy P. Burkholder, Elizabeth M. Kudlacz, Tieu-Binh Le
  • Patent number: 5811552
    Abstract: A novel cyclobutenedione derivative prepared in accordance with the following reaction formula, a process for the preparation thereof, and a nonlinear optical element comprising such a derivative are provided: ##STR1## wherein R.sup.1 and R.sup.2 each represents an alkyl group, an alkenyl group or an alkynyl group; R.sup.3 and R.sup.4 each represents a hydrogen atom, an alkyl group, an alkenyl group or an alkynyl group; and C.sup.* represents an asymmetric carbon atom, with the proviso that R.sup.1, R.sup.2 and the nitrogen atom to which they are connected may form a cyclic structure larger than 3-membered ring, R.sup.1 and R.sup.3, and R.sup.2 and R.sup.4 each may be connected to each other to form a methylene chain --(CH.sub.2).sub.n -, and the hydrogen atoms in R.sup.1 and R.sup.2 may be substituted by halogen atom, alkyloxy group or cyano group.
    Type: Grant
    Filed: April 14, 1995
    Date of Patent: September 22, 1998
    Assignee: Fuji Xerox Co., Ltd.
    Inventors: Yasunari Nishikata, Lyong Sun Pu
  • Patent number: 5804593
    Abstract: A compound of formula I or pharmaceutical acceptable salts thereof, ##STR1## wherein R.sub.1 is isopropyl, 2-methylbut-2yl, phenyl, benzyl, or 1H-indol-3ylmethyl; R.sub.2 is n-octyl, phenyl, or phenyl substituted with methoxy, fluoro, or bromo, are matrix metalloproteinase inhibitors.
    Type: Grant
    Filed: October 20, 1997
    Date of Patent: September 8, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Martha A. Warpehoski, Mark Allen Mitchell, Eric Jon Jacobsen
  • Patent number: 5786488
    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: November 5, 1997
    Date of Patent: July 28, 1998
    Assignee: Sugen, Inc.
    Inventors: Peng C. Tang, G. Davis Harris
  • Patent number: 5780498
    Abstract: The present invention provides novel compounds represented by the general formula I: ##STR1## wherein R.sub.1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl;R.sub.2 is hydrogen, a straight or branched lower alkyl, a cycloalkyl, or a cycloalkyl-lower alkyl;R.sub.3 and R.sub.3 ' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; orR.sub.3 and R.sub.3 ' together form a ring structure;R.sub.3 " is hydrogen, lower alkyl or an aryl; orR.sub.2 and R.sub.3 " together form a lower alkylene group --(CH.sub.2).sub.n -- wherein n is an integer of 1, 2 or 3; orR.sub.2 and R.sub.3 " together form a group represented by the formula: --(CH.sub.2).sub.p --Ar-- or --Ar--(CH.sub.2).sub.p --, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene;C(.dbd.X) is C(.dbd.
    Type: Grant
    Filed: April 30, 1996
    Date of Patent: July 14, 1998
    Assignee: Ciba-Geigy Japan Limited
    Inventors: Hideyuki Saika, Toshiki Murata, Thomas Pitterna, Thomas Fruh, Lene D. Svensson, Yoshihiro Urade, Takaki Yamamura, Toshikazu Okada
  • Patent number: 5741804
    Abstract: This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: April 21, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Richard McCulloch Keenan, William Henry Miller
  • Patent number: 5733923
    Abstract: A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: March 28, 1997
    Date of Patent: March 31, 1998
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
  • Patent number: 5733648
    Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: March 31, 1998
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
  • Patent number: 5719144
    Abstract: Fibrinogen receptor antagonists having the formula ##STR1## where L is L is (CH.sub.2).sub.p, where p is 1 or 2; and Z is --CR.sup.1 .dbd.CR.sup.
    Type: Grant
    Filed: February 22, 1995
    Date of Patent: February 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John H. Hutchinson, Wasyl Halczenko
  • Patent number: 5696148
    Abstract: The present invention relates to therapeutically active indole compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system related to the metabotropic glutamate receptor system.
    Type: Grant
    Filed: November 18, 1996
    Date of Patent: December 9, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Jane Marie Lundbech, Anders Kanstrup
  • Patent number: 5677329
    Abstract: Methods of inhibiting cell proliferation in a patient suffering from such disorder comprising the use of a styryl-substituted heteroaryl compound wherein the heteroaryl group is a monocyclic ring with 1 or 2 heteroatoms, or a bicyclic ring with 1 to about 4 heteroatoms, said compound optionally substituted or polysubstituted, with the proviso that when said ring is polysubstituted, the substituents do not have a common point of attachment to said ring, and those compounds wherein no substituent on the heteroaryl group is a carboxy group or an ester group, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: October 14, 1997
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals, Inc.
    Inventors: Alfred P. Spada, Paul E. Persons, Alexander Levitzki, Chaim Gilon, Aviv Gazit
  • Patent number: 5654440
    Abstract: An optically active (+)-4,4,4-trifluoro-3-(indole-3-)butyric acid is produced by a method which consists essentially of causing 2,2,2-trifluoroethanol to react on a racemic modification 4,4,4-trifluoro-3-(indole-3-)butyric acid thereby forming a reaction solution containing the trifluoroethyl ester of the butyric acid, causing an enzyme having an esterase activity to act on the reaction solution thereby forming an optically active (+)-4,4,4-trifluoro-3-(indole-3-)butyric acid, and thereafter separating the reaction product from the reaction solution.
    Type: Grant
    Filed: March 15, 1996
    Date of Patent: August 5, 1997
    Assignee: Agency of Industrial Science & Technology, Ministry of International Trade & Industry
    Inventors: Katsuya Kato, Shozo Fujii, Masato Katayama, Hiroshi Kimoto
  • Patent number: 5654326
    Abstract: A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
  • Patent number: 5622983
    Abstract: Novel unnatural dipeptoids of .alpha.-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, colorectal tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents, antiulcer agents, antidepressant agents, and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol, cocaine, caffeine, or opiods. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: April 22, 1997
    Assignee: Warner-Lambert Company
    Inventors: David C. Horwell, Martyn C. Pritchard, Edward Roberts, Reginald S. Richardson, Julian Aranda
  • Patent number: 5607960
    Abstract: The present invention relates to 3,5-disubstituted indole compounds which are selective agonists which act on 5-hdroxytryptamine receptors useful in the treatment of migraine.
    Type: Grant
    Filed: October 20, 1995
    Date of Patent: March 4, 1997
    Assignee: Pfizer Inc.
    Inventor: Martin J. Wythes
  • Patent number: 5604253
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: February 18, 1997
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Cheuk K. Lau, Cameron Black, Daniel Guay, Jacques Y. Gauthier, Yves LeBlanc, Patrick Roy, Yves Ducharme, Pierre Hamel
  • Patent number: 5597845
    Abstract: The present invention relates to novel substituted alkyldiamine derivatives and pharmaceutically acceptable salts thereof which are useful tachykinin antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions including asthma, cough, and bronchitis.
    Type: Grant
    Filed: June 20, 1994
    Date of Patent: January 28, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Timothy P. Burkholder, Elizabeth M. Kudlacz, Tieu-Binh Le
  • Patent number: 5591768
    Abstract: A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed methods relate to the administration of melatonin at times determined with relation to the time of dim light endogenous melatonin onset. Embodiments capable of alleviating the effects of jet lag, winter depression and shift-work sleep disturbance are provided.
    Type: Grant
    Filed: August 24, 1993
    Date of Patent: January 7, 1997
    Assignee: State of Oregan, Acting by and Through the Oregon State Board of Higher Education on Behalf of the Oregon Health Sciences University
    Inventors: Alfred J. Lewy, Robert L. Sack
  • Patent number: 5578634
    Abstract: A class of novel 1H-indole-3-acetic acid hydrazides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids (e.g., arachidonic acid) for treatment of conditions such as septic shock.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: November 26, 1996
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
  • Patent number: 5578552
    Abstract: An agent for increasing the sugar content and/or decreasing the acid content of plant fruits has as a substantial main component thereof a fluorine-containing .beta.-indolebutyric acid compound represented by the general formula ##STR1## (wherein Y stands for one member selected from the class consisting of hydroxyl group, alkoxy group, amino group, and alkyl amino group and R.sup.1 and R.sup.2 independently stand for one member selected from the class consisting of hydrogen atom, halogen atom, alkyl group, alkoxy group, aryl group, nitro group, amino group, and alkyl amino group). A method for producing ripe fruits having a high sugar content and/or a low acid content by causing the fluorine-containing .beta.-indolebutyric acid compound mentioned above to adhere to unripe fruits on plants and plants bearing fruits and subsequently allowing the fruits to mature.
    Type: Grant
    Filed: November 9, 1994
    Date of Patent: November 26, 1996
    Assignees: Agency of Industrial Science and Technology,, Ministry of International Trade and Industry
    Inventors: Masato Katayama, Shozo Fujii, Hiroshi Kimoto, Katsuya Kato
  • Patent number: 5569768
    Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: October 29, 1996
    Assignee: Eli Lilly and Company
    Inventors: Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
  • Patent number: 5554642
    Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description,its optical isomers and its addition salts thereof with a pharmaceuticaliy-accepable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: September 10, 1996
    Assignee: Adir et Compagnie
    Inventors: Michel Langlois, Pierre Renard, G erard Adam
  • Patent number: 5519136
    Abstract: A radiation-sensitive compound has the general formula ##STR1## wherein A represents the ring members required to complete a 5- or 6-membered heterocyclic ring which may optionally be fused to an optionally substituted aromatic nucleus,B represents H, acryl, aroyl, heterocyclyl carbonyl or ##STR2## R represents an optionally substituted alkyl group, E and G, which may be the same or different, each represents H or CH.sub.p X.sub.3-p,J and K, which may be the same or different, each represents an aryl or heterocyclic group, which may optionally include a substitutent additional to E or G,X represents Cl or Br, andm, n and p, which may be the same or different, each represents an integer equal to 0, 1 or 2.The compound can be used to form radiation sensitive compositions for the production of radiation sensitive plates in lithographic printing plate manufacture.
    Type: Grant
    Filed: May 22, 1992
    Date of Patent: May 21, 1996
    Inventor: John R. Wade
  • Patent number: 5510368
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating inflammation and, in particular, cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of inflammation and, in particular, cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: April 23, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Cheuk K. Lau, Cameron Black, Michel Belley
  • Patent number: 5510538
    Abstract: A process for the selective oxidation of a primary or secondary alcohol to an aldehyde or ketone and for the oxidation of a 1,2-diol to an .alpha.-ketol or .alpha.-diketone, which comprises contacting the alcohol or 1,2-diol with o-iodoxybenzoic acid. This process is suited for selective oxidation of alcohols containing easily oxidizable groups, such as amino or thioether groups and easily oxidizable heterocycles.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: April 23, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Marco Frigerio, Simona Sputore, Marco Santagostino
  • Patent number: 5496844
    Abstract: The present invention provides indole derivatives of the general formula: ##STR1## The indole derivatives of the invention have potent antiestrogen activity and are useful as drugs for the treatment of estrogen-dependent diseases, such as anovulatory infertility, prostatic hypertrophy, osteoporosis, breast cancer, endometrial cancer and melanoma.
    Type: Grant
    Filed: November 8, 1994
    Date of Patent: March 5, 1996
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Masatoshi Inai, Tadanao Shibutani, Jun Kanaya, Masako Moritake, Akie Tanaka
  • Patent number: 5496794
    Abstract: A substituted fluorine-containing .beta.-indolebutyric acid compound represented by the formula: ##STR1## wherein Y stands for one member selected from the group consisting of hydroxyl group, alkoxy group, amino group, and alkylamino group, at least one of R.sup.1 and R.sup.2 stands for one member selected from the group consisting of halogen atom, alkyl group, alkoxy group, aryl group, nitro group, amino group, and alkylamino group, and the remaining one, if any, for a hydrogen atom, a plant growth regulating agent having as a substantial main component thereof the substituted fluorine-containing .beta.-indolebutyric acid compound, and a method for regulating the length of roots sprouting from plant seeds and the length of hypocotyls by causing adhesion of the substituted fluorine-containing .beta.-indolebutyric acid compound to the plant seeds.
    Type: Grant
    Filed: October 28, 1994
    Date of Patent: March 5, 1996
    Assignees: Agency of Industrial Science & Technology, Ministry of International Trade & Industry
    Inventors: Masato Katayama, Shozo Fujii, Hiroshi Kimoto, Katsuya Kato
  • Patent number: 5455262
    Abstract: Novel mercaptosulfide matrix metalloproteinase inhibitors of the Formula I, ##STR1## wherein: n is 0 or 1;R.sup.1 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH(lower alkyl); andR.sup.2 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH (lower alkyl); orR.sup.1 and R.sup.2 together are --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sup.3 is selected from the group consisting of hydrogen, lower alkyl, aralkyl and heteroaralkyl; andR.sup.4 is selected from the group consisting of hydrogen, lower alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, aralkyl and 2-indolylmethyl; andR.sup.5 is selected from the group consisting of lower alkyl, aralkyl and --CH(R.sup.6)--C(O)NH.sub.2,whereinR.sup.
    Type: Grant
    Filed: October 6, 1993
    Date of Patent: October 3, 1995
    Assignee: Florida State University
    Inventors: Martin A. Schwartz, Harold Van Wart
  • Patent number: 5451605
    Abstract: Compounds of the formula ##STR1## where R.sub.1 -R.sub.5 are hydrogen, lower alkyl of 1-6 carbons, or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.
    Type: Grant
    Filed: December 30, 1993
    Date of Patent: September 19, 1995
    Assignee: Allergan, Inc.
    Inventors: Roshantha A. Chandraratna, Richard L. Beard
  • Patent number: 5403851
    Abstract: This invention relates to novel substituted tryptamine and phenalkylamine and related compounds, pharmaceutical compositions thereof and methods of using said compounds and compositions for a number of pharmaceutical indications including (but not limited to): 1. central nervous system and psychiatric disorders (e.g., sleep disorders, epilepsy and other convulsive disorders, anxiety, psychiatric diseases, neurodegenerative diseases, fever); 2. chronobiological-based disorders (e.g., jet lag, delayed sleep syndrome, shift-work, seasonal affective disorder); 3. endocrine indications (e.g., contraception and infertility, precocious puberty, premenstrual syndrome, hyperprolactinemia, growth hormone deficiency); 4. cancer and other proliferative diseases; 5. immune system disorders and conditions associated with senescence; 6. ophthalmological diseases; 7. animal breeding (e.g., regulation of fertility, puberty, pelage color).
    Type: Grant
    Filed: April 5, 1994
    Date of Patent: April 4, 1995
    Assignee: Interneuron Pharmaceuticals, Inc.
    Inventors: Kay J. D'Orlando, Kenneth W. Locke, Emile M. Bellott, Richard L. Gabriel, Michael D. Nohrden, Yesh P. Sachdeva, Salah A. Zahr, Emile Al-Farhan, Subramaniam Krishnananthan
  • Patent number: 5401438
    Abstract: Disclosed is a novel UV light absorbing compound which can preferably be employed in the art of colored molding plastics, resin films, heat-sensitive transfer materials, liquid crystal display materials, color photographs and the like, and method for producing thereof. The UV light absorbing compound is characterized by the general formula: ##STR1## wherein R.sup.1 represents linear or branched alkyl or aralkyl group, and R.sup.2 represents --CN or --COOR.sup.3, wherein R.sup.3 represents substituted or unsubstituted alkyl or aralkyl group.
    Type: Grant
    Filed: December 20, 1993
    Date of Patent: March 28, 1995
    Assignee: Orient Chemical Industries, Ltd.
    Inventor: Masahiro Otsuka
  • Patent number: 5354772
    Abstract: Compounds of the formula ##STR1## wherein one of R and R.sub.o is ##STR2## and the other is primary or secondary C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-6 cycloalkyl or phenyl-(CH.sub.2).sub.m --,whereinR.sub.4 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy,R.sub.5 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy,R.sub.5a is hydrogen, C.sub.1-2 alkyl, C.sub.1-2 alkoxy, fluoro or chloro, andm is 1, 2 or 3, with the provisos that both R.sub.5 and R.sub.5a must be hydrogen when R.sub.4 is hydrogen, R.sub.5a must be hydrogen when R.sub.5 is hydrogen, not more than one of R.sub.4 and R.sub.5 is trifluoromethyl, not more than one of R.sub.4 and R.sub.5 is phenoxy, and not more than one of R.sub.4 and R.sub.5 is benzyloxy,R.sub.2 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.3-6 cycloalkyl, C.sub.
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: October 11, 1994
    Assignee: Sandoz Pharm. Corp.
    Inventor: Faizulla G. Kathawala
  • Patent number: 5332755
    Abstract: Indole derivative for leucotriene antagonism of the formula ##STR1## wherein groups A, B, D, E, F and G are as described in the specification.
    Type: Grant
    Filed: January 13, 1992
    Date of Patent: July 26, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: John E. Butler, Nigel J. Cuthbert