Polycyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/366)
  • Patent number: 6127387
    Abstract: The application concerns a method of identifying compounds that can be used to inhibit undesired human CD4.sup.+ T cell immune responses by identifying compounds that block the interaction of CD4 and class II MHC gene products and a method of treatment which comprises administering such an identified compound. The compounds that inhibit undesired human CD4.sup.+ T cell immune responses can be used to treat disease such as multiple sclerosis and to prevent graft rejection and graft versus host disease. More specifically, the application concerns compounds having molecular weights between about 500 and 150 that bind to the GFCC'C" portion of the D1 domain of human CD4 lymphocyte cell surface antigen.
    Type: Grant
    Filed: December 9, 1997
    Date of Patent: October 3, 2000
    Assignee: Thomas Jefferson University
    Inventors: Ziwei Huang, Robert Korngold
  • Patent number: 6124331
    Abstract: This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: September 26, 2000
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Mohammad R. Marzabadi, Wai C. Wong, Stewart A. Noble
  • Patent number: 6124277
    Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.
    Type: Grant
    Filed: March 11, 1999
    Date of Patent: September 26, 2000
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 6107318
    Abstract: A compound of Formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, wherein n is an integer between 2 and 6 and R.sub.1 is a methyl group or a group ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, methoxy, methylsulfonyl, or one of R.sub.2, R.sub.3 and R.sub.4 together with another one of the three substituents forms a --O--CH.sub.2 --O-- bridge. The asterisk marks an asymmetric carbon atom.
    Type: Grant
    Filed: December 6, 1999
    Date of Patent: August 22, 2000
    Assignee: Zambon Group S.p.A.
    Inventors: Felice Pocchiari, Claudio Masotto, Paolo Cavalleri, Stefania Montanari, Francesco Santangelo
  • Patent number: 6090833
    Abstract: Polycyclic dihydrothiazoles, processes for their preparation, and their pharmaceutical uses are provided. Preferred compounds are represented by the formula I ##STR1## wherein the radicals may have various meanings. The compounds are particularly useful as anorectics.
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: July 18, 2000
    Assignee: Aventis Pharma Deutschand GmbH
    Inventors: Gerhard Jaehne, Heiner Glombik, Karl Geisen, Martin Bickel
  • Patent number: 6080771
    Abstract: DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents CO(CR.sup.4A R.sup.4B).sub.n1 (O(CH.sub.2).sub.p1).sub.n2 OR.sup.5 {wherein n1 represents an integer of 1 or 2; R.sup.4A and R.sup.4B are the same or different, and each represents hydrogen or lower alkyl; p1 and n2 each represents an integer of 1 to 10; and R.sup.
    Type: Grant
    Filed: August 13, 1998
    Date of Patent: June 27, 2000
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yutaka Kanda, Hitoshi Arai, Hiroyuki Yamaguchi, Tadashi Ashizawa, Shun-ichi Ikeda, Chikara Murakata, Tatsuya Tamaoki
  • Patent number: 6066658
    Abstract: A compound represented by the formula: ##STR1## wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R.sup.1 represents an optionally substituted hydrocarbon group; R.sup.2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: May 23, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Yasuma, Tsuneo Oda, Masatoshi Hazama, Shigehisa Taketomi
  • Patent number: 6057318
    Abstract: The invention relates to compounds of formula: ##STR1## in which: A is selected from O or S; B is selected from C or N;Z.sub.1 is selected from C.sub.1 -C.sub.4 alkylene or phenylene;Z.sub.2 is C.sub.1 -C.sub.4 alkylene; W is NR.sub.1 R.sub.2, in which R.sub.1 is selected from H or C.sub.1 -C.sub.4 alkyl and R.sub.2 is selected from H, C.sub.1 -C.sub.4 alkyl, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2 in which Q.sub.1 and Q.sub.2 are independently selected from H or C.sub.1 -C.sub.4 alkyl, SO.sub.2 Q.sub.3 or COQ.sub.3 in which Q.sub.3 is C.sub.1 -C.sub.4 alkyl, COOQ.sub.4 in which Q.sub.4 is selected from C.sub.1 -C.sub.4 alkyl or benzyl, or R.sub.1 and R.sub.2 taken together with N form a saturated heterocycle, or W is selected from C.sub.1 -C.sub.4 alkoxy or thioalkoxy, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2, pyridyl, imidazolyl or COOQ.sub.5 in which Q.sub.5 is C.sub.1 -C.sub.5 alkyl; R.sub.3 is not present when B is N, or is H, C.sub.1 -C.sub.8 alkyl or halogen; Ar.sub.
    Type: Grant
    Filed: May 20, 1998
    Date of Patent: May 2, 2000
    Assignee: Sanofi
    Inventors: Andre Bernat, Jean-Marc Herbert, Gerard Valette
  • Patent number: 6040451
    Abstract: This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: March 21, 2000
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Yoon T. Jeon, Charles Gluchowski
  • Patent number: 5990111
    Abstract: This invention relates to the use of aldose reductase inhibitors in the treatment, prevention or reversal of diabetic cardiomyopathy in a human subject.
    Type: Grant
    Filed: May 1, 1998
    Date of Patent: November 23, 1999
    Assignee: Pfizer Inc.
    Inventor: Brian F. Johnson
  • Patent number: 5981558
    Abstract: DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4, or the like; R.sup.2 represents hydrogen or COR.sup.6 ; R.sup.3 represents --CH.sub.2 OCOR.sup.7, phthalimidomethyl, or the like; and W represents oxygen or NR.sup.8 (wherein R.sup.8 represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, substituted or unsubstituted arylsulfonylamino, or lower alkoxycarbonylamino).
    Type: Grant
    Filed: August 13, 1998
    Date of Patent: November 9, 1999
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hitoshi Arai, Yutaka Kanda, Hiroyuki Yamaguchi, Tadashi Ashizawa, Chikara Murakata, Shun-ichi Ikeda, Tatsuya Tamaoki
  • Patent number: 5955485
    Abstract: The present invention is concerned with the method of using a 2,3-dihydro-imidazo?2,1-b!benzothiazole derivative for the manufacture of a medicament for the therapeutic or prophylactic treatment of humans suffering from ageing of, or degenerative diseases of the nervous and vascular system which are associated with oxidative stress.
    Type: Grant
    Filed: August 12, 1997
    Date of Patent: September 21, 1999
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marc Joris De Brabander, Anne Simone Josephine Lesage, Josepha Eduarda Maria Francisca Leysen
  • Patent number: 5955484
    Abstract: Plant-protecting active ingredient mixtures having synergistically enhanced action, wherein component I is a compound having plant-immunising action of formula I ##STR1## wherein Z is CN, COOH or a salt thereof, CO--OC.sub.1 -C.sub.4 alkyl or CO--SC.sub.1 -C.sub.4 alkyl;and wherein component II is a compound selected from the groupA) 4-?3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)acryloyl!morpholine ("dimethomorph");B) 5-methyl-1,2,4-triazolo?3,4-b!?1,3!benzothiazole ("tricyclazole"); andC) 3-allyloxy-1,2-benzothiazole-1,1-dioxide ("probenazole").
    Type: Grant
    Filed: April 28, 1998
    Date of Patent: September 21, 1999
    Assignee: Novartis Finance Corporation
    Inventor: Wilhelm Ruess
  • Patent number: 5952354
    Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.
    Type: Grant
    Filed: July 21, 1993
    Date of Patent: September 14, 1999
    Assignee: American Home Products Corporation
    Inventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
  • Patent number: 5948804
    Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: September 5, 1997
    Date of Patent: September 7, 1999
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Yoon T. Jeon, Charles Gluchowski
  • Patent number: 5925657
    Abstract: Disclosed herein are methods for reducing or preventing cytokine production associated with an inflammatory response, involving administering to a mammal a therapeutically-effective amount of a thiazolidinedione PPAR.gamma. agonist.
    Type: Grant
    Filed: June 18, 1997
    Date of Patent: July 20, 1999
    Assignee: The General Hospital Corporation
    Inventors: Brian Seed, Chengyu Jiang
  • Patent number: 5919799
    Abstract: An imidazothiazole compound having the formula (A): ##STR1## wherein R.sub.1 is a phenyl or napthyl which may have a substituent, R.sub.2 is an acyl, and the two bonds at dotted line portions may or may not exist simultaneously, or a pharmacologically acceptable salt thereof and an agent for overcoming resistance to an anti-neoplastic agent or an enhancer for the effect of an anti-neoplastic agent comprising said compound or a pharmacologically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: September 9, 1997
    Date of Patent: July 6, 1999
    Assignee: Nikken Chemicals Co., Ltd.
    Inventors: Shigeyuki Tasaka, Akira Kiue
  • Patent number: 5866595
    Abstract: According to the present invention, compounds selected from the thiozole class of organic molecules are employed as antagonists for receptor-operated ion channels (ROICs) useful in the treatment of a variety of disease states in which ROICs are implicated. ROICs of particular interest are receptor-operated calcium channels (ROCCs). Compounds of particular interest with respect to the subject invention are compounds of the thiazolidinedione class of organic molecules, more particularly ciglitazone. Disease states in which particular utility is expected include vasculoproliferative diseases such as atherosclerosis, restenosis following angioplasty, and other conditions in which PDGF is known to play a role. The utility of the present invention with respect to further studies on the operation of ROICs and ROCCs and their role in disease will be apparent to those of skill in the art.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: February 2, 1999
    Assignee: The Regents of The University of California
    Inventors: Harrihar A. Pershadsingh, Theodore W. Kurtz
  • Patent number: 5861424
    Abstract: A pharmaceutical composition for treatment of cancer in a mammal comprising:(A) a therapeutically effective amount of at least one compound selected from the group consisting of compounds represented by the General Formulas (1) to (6) ##STR1## wherein X.sub.1 is O, S, Se, or >N--R.sub.14, ##STR2## X.sub.2 is O, S, Se, >N--R.sub.15, X.sub.3 is O, S, Se, ##STR3## X.sub.4 is >N--R.sub.19, or Y.sub.1 is O, S, Se, or >N--R.sub.18 ;Z.sub.1 represents an atomic group necessary to form a saturated or unsaturated 5- or 6-membered ring which may be substituted or may have another ring fused therewith;Z.sub.2 is a naphthalene ring, an anthracene ring or a phenanthrene ring which may be substituted; in combination with(B) a pharmaceutically acceptable carrier or diluent; and a method for treatment of cancer comprising administering the above pharmaceutical composition to a host afflicted with cancer.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 19, 1999
    Assignees: Dana Farber Cancer Institute, Fuji Photo Film Co., Ltd.
    Inventors: Lan Bo Chen, Tadao Shishido
  • Patent number: 5852014
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 22, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5834499
    Abstract: A 5-HT.sub.3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms;one of L.sub.1 or L.sub.
    Type: Grant
    Filed: August 26, 1996
    Date of Patent: November 10, 1998
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Iwaoka, Hideki Anan, Naoki Imanishi, Kenichi Kazuta, Hiroyuki Koshio, Takeshi Suzuki, Hirotsune Itahana, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta
  • Patent number: 5705498
    Abstract: Compounds of formula (I): ##STR1## wherein X.sup.g is O, S, SO, SO.sub.2, CH.sub.2, CH, N or NR wherein R is hydrogen or C.sub.1-6 alkyl;A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms;R.sub.1.sup.g and R.sub.2.sup.g are hydrogen or C.sub.1-6 alkyl;R.sub.3.sup.g is hydrogen, halo, C.sub.1-6 alkyl, amino, nitro or C.sub.1-6 alkoxy;R.sub.4.sup.g is hydrogen, halo, C.sub.1-6 alkyl or C.sub.1-6 alkoxy,Y is O or NH, or CO--Y together are a heterocyclic bioisostere;Z is of sub-formula: ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; and n.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R.sub.7 wherein R.sub.7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R.sub.7 is C.sub.2-7 alkoxycarbonyl or secondary or tertiary hydroxy substituted C.sub.1-6 alkyl; andR.sub.6 is hydrogen or C.
    Type: Grant
    Filed: May 4, 1995
    Date of Patent: January 6, 1998
    Assignee: SmithKline Beecham plc.
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5705509
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
    Type: Grant
    Filed: July 28, 1995
    Date of Patent: January 6, 1998
    Assignee: SmithKline Beecham plc
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman
  • Patent number: 5698574
    Abstract: The present invention relates to 5-membered heteroaryl-oxazolidinones, to processes for their preparation and to their use as medicaments, in particular as antibacterial medicaments.
    Type: Grant
    Filed: July 17, 1995
    Date of Patent: December 16, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Riedl, Dieter Habich, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus Dieter Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
  • Patent number: 5686459
    Abstract: Novel dioxopyrrolo-pyrrole derivatives of the formula ##STR1## as well as hydrates or solvates thereof, which inhibit thrombin-induced or Factor Xa-induced platelet aggregation and fibrinogen clotting in blood plasma. The derivatives can be manufactured from the corresponding maleimides which are N-substituted by .alpha.-amino carboxylic acids of the formula HN(R.sup.2)CH(R.sup.4)COOH, or functional derivatives thereof; and ketones or aldehydes of the formula R.sup.5 C(O)R.sup.6.
    Type: Grant
    Filed: February 26, 1996
    Date of Patent: November 11, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Francois Diederich, Ulrike Obst, Sabine Wallbaum, Lutz Weber
  • Patent number: 5677321
    Abstract: This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: February 29, 1996
    Date of Patent: October 14, 1997
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Yoon T. Jeon, Charles Gluchowski
  • Patent number: 5670530
    Abstract: An anti-cancer composition comprising a rhodacyanine compound and cyclodextrin or derivative thereof, wherein said rhodacyanine compound is selected from the group consisting of compounds represented by the following Formula (I), the cation moiety of which has a log P value of 4.5-12: ##STR1## wherein X.sub.1 and X.sub.2, which may be the same or different, each represents O, S, Se, ##STR2## Y.sub.1 represents O, S, Se, or ##STR3## R.sub.1 and R.sub.3, which may be the same or different, each represents an alkyl group;R.sub.2 represents an alkyl group, an aryl group or a heterocyclic group;Z.sub.1 and Z.sub.2, which may be the same or different, each represents an atomic group necessary to form a 5- or 6-membered ring;L.sub.1, L.sub.2 and L.sub.3, which may be the same or different, each represents a methine group or nitrogen atom and L.sub.1 and R.sub.3 may combine and form a 5- or 6-membered ring;R.sub.4 and R.sub.5, which may be the same or different, each represents an alkyl group;R.sub.6 and R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 23, 1997
    Assignees: Fuji Photo Film Co., Ltd., Dana Farber Cancer Institute
    Inventors: Lan Bo Chen, Tadao Shishido
  • Patent number: 5643926
    Abstract: Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.
    Type: Grant
    Filed: January 19, 1994
    Date of Patent: July 1, 1997
    Assignee: Eli Lilly and Company
    Inventors: Raymond F. Brown, J. Jeffry Howbert, Karen L. Lobb, David A. Neel, Jon K. Reel, Beverley Greenwood
  • Patent number: 5637603
    Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control of parasites in vertebrate animals.
    Type: Grant
    Filed: April 25, 1995
    Date of Patent: June 10, 1997
    Assignee: Eli Lilly and Company
    Inventor: David I. Wickiser
  • Patent number: 5618831
    Abstract: A pharmaceutical composition for treatment of cancer in an animal comprising:(A) a therapeutically effective amount of at least one compound selected from the group consisting of compounds represented by the General Formula (I). ##STR1## wherein Z.sub.1 and Z.sub.2, which may be the same or different, each represents an atomic group necessary to form a 5- or 6-membered ring;R.sub.1, R.sub.2 and R.sub.3, which may be the same or different, each represents an alkyl group or an aryl group;L.sub.1 and L.sub.2 each represents a methine group or a substituted methine group;X represents a pharmaceutically acceptable anion;k represents a number necessary for electrical charge balance;n represents 0 or 1; and(B) a pharmaceutically acceptable carrier or diluent.
    Type: Grant
    Filed: May 16, 1994
    Date of Patent: April 8, 1997
    Assignees: Fuji Photo Film Co., Ltd., Dana Farber Cancer Institute
    Inventors: Tadao Shishido, Masayuki Kawakami, Akihiko Ikegawa, Toshinao Ukai, Keizo Koya, Lan B. Chen
  • Patent number: 5604224
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: February 18, 1997
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5599825
    Abstract: There are provided methine compounds having the following structure and their analogs, with a high solubility and are usefull as an active ingredient for pharmaceutical composition for treatment of cancer: ##STR1##
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: February 4, 1997
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Noriaki Tatsuta, Akihiko Okegawa, Masayuki Kawakami, Keizo Koya
  • Patent number: 5585091
    Abstract: Compounds which, per molecule, contain at least 2 benzazolyl groups are outstandingly suitable as UV absorbers for sunscreen compositions.
    Type: Grant
    Filed: February 22, 1995
    Date of Patent: December 17, 1996
    Assignee: Haarmann & Reimer GmbH
    Inventors: Ralf Pelzer, Roland Langner, Horst Surburg, Horst Sommer, Alfred Krempel, Rudolf Hopp
  • Patent number: 5569655
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: October 29, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5565479
    Abstract: Condensed thiazole derivatives useful as 5-HT.sub.3 receptor agonists are provided and can be represented by the following formula (I) or a pharmaceutically acceptable salt thereof, a process for the production thereof and a pharmaceutical composition thereof: ##STR1## wherein R, A, L.sub.1, L.sub.2, L, and R.sup.1 -R.sup.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: October 15, 1996
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Iwaoka, Hiroyuki Koshio, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta
  • Patent number: 5556855
    Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomic form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: September 17, 1996
    Assignee: Pharmacia AB
    Inventors: Hubert Agback, Leif Ahrgren, Thomas Berglindh, Martin Haraldsson, G oran Smedeg.ang.rd, Lars-Inge Olsson
  • Patent number: 5512564
    Abstract: The present invention concerns thiazolo- 2,3-a!pyrrole and oxazolo- 1,2-a!pyrrole derivatives of formula I ##STR1## in which HET represents a heterocyclic ring with 3-7 ring atoms which can be substituted by one, two or three residues R.sup.1 which can be the same or different,Y represents an oxygen or sulphur atom, or a SO or SO.sub.2 group,X can be an oxygen or sulphur atom,R denotes an aliphatic residue with 1-9 C-atoms which can be substituted by phenyl or denotes a phenyl ring or a carbocyclic ring with 7-15 C atoms or a heterocyclic ring system each having 5 or 6 ring atoms,in which the aforementioned phenyl rings, carbocyclic rings or heterocyclic ring system can be substituted once or several times, if desired, and R1-R5 denote hydrogen or an aliphatic residue, as well as their tautomers, enantiomers, diastereomers and physiologically tolerated salts.
    Type: Grant
    Filed: March 4, 1994
    Date of Patent: April 30, 1996
    Assignee: Boehringer Mannheim GmbH
    Inventors: Harald Zilch, Herbert Leinert, Alfred Mertens
  • Patent number: 5506243
    Abstract: Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: April 9, 1996
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Ryoichi Ando, Toshiro Sakaki, Chizuko Takahashi, Yoshiyuki Fujimura
  • Patent number: 5449681
    Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control of parasites in vertebrate animals.
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: September 12, 1995
    Assignee: Eli Lilly and Company
    Inventor: David I. Wickiser
  • Patent number: 5418248
    Abstract: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydroxy group, a C.sub.1 -C.sub.4 alkoxy group or an amino group of general formula --NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 each represent, independently of each other, a hydrogen atom, a straight or branched C.sub.1 -C.sub.4 alkyl group, an allyl group or a methoxyethyl group, or alternatively --NR.sub.4 R.sub.5 represents a heterocycle containing 3 to 6 carbon atoms,Y represents a thienyl group optionally substituted by an alkyl group, andX represents a hydrogen or halogen atom,are useful as anticonvulsants and auxiolytics.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: May 23, 1995
    Assignee: Synthelabo
    Inventors: Mireille Sevrin, Claude Morel, Michel Mangane, Pascal George
  • Patent number: 5397794
    Abstract: The present invention concerns the use of compounds of the general formula I ##STR1## for the preparation of medicaments for the treatment of viral or retroviral infections, whereby R signifies a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical with 1-7 carbon atoms, which can possibly be substituted by phenyl, or a phenyl ring which can possibly be substituted one or more times by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, hydroxyl, trifluoromethyl, methylsulphonyl or halogen, such as fluorine, chlorine or bromine, n stands for the numbers 0, 1 or 2, as well as of their pharmacologically compatible salts or tautomers.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: March 14, 1995
    Assignee: Boehringer Mannheim GmbH
    Inventors: Harald Zilch, Alfred Mertens, Herbert Leinert, Ulrike Leser, Bernhard Konig, Hans Seidel
  • Patent number: 5378706
    Abstract: The invention relates to thiazole derivatives corresponding to the general formula: ##STR1## in which: - R.sub.1 and R.sub.2 each independently represent hydrogen; a C.sub.1 -C.sub.4 alkyl group; a phenyl group or a phenyl group monosubstituted or polysubstituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy, nitro or hydroxyl group; or one of the groups R.sub.1 and R.sub.2 denotes hydrogen and the other represents a naphthyl group; a benzyl group; an .alpha.,.alpha.-dimethyl-benzyl group; a cyclohexyl group; a biphenyl group; a thienyl group or an adamantyl group; or alternatively R.sub.1 and R.sub.2, taken together, represent a group; ##STR2## in which the phenyl group is bonded to the 4-position of the thiazole and the group (CH.sub.2).sub.m to the 5-position, m represents an integer equal to 2 or 3 and R.sub.5 denotes hydrogen or a nitro group, R.sub.3 is H or an alkyl group and R.sub.4 is notably an alkyl substituted by an amino group, a pyrrolidino, or a pydridino group.
    Type: Grant
    Filed: May 28, 1993
    Date of Patent: January 3, 1995
    Assignee: Sanofi
    Inventors: Kathleen Biziere, Dominique Olliero, Paul Worms
  • Patent number: 5314889
    Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: May 24, 1994
    Assignee: Elf Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
  • Patent number: 5294629
    Abstract: A novel benzothiazole or benzimidazole derivative represented by formula (I) ##STR1## wherein X represents a sulfur atom or a NH group; R.sup.1 represents a hydrogen atom, a lower alkoxy group, a chlorine atom, a bromine atom or an iodine atom; R.sup.2 represents a hydrogen atom a substituted or unsubstituted lower alkyl group, a vinyl group, an aryl group or an acyl group; m is an integer of 1, 2 or 3; and n is an integer of 0, 1 or 2, which shows an excellent acid secretion suppressing effect and gastric mucosa protecting effect, and an antiulcer agent containing the same as an active ingredient.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: March 15, 1994
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Tomoya Machinami, Kazue Yasufuku, Seiji Shibahara, Fumiya Hirano, Yasukatsu Yuda, Motohiro Nishio, Yuji Matsuhashi, Takashi Tsuruoka, Kiyoaki Katano, Shigeharu Inoye
  • Patent number: 5217987
    Abstract: Mazindol and other nonreinforcing dopamine uptake inhibitors are effective to lessen craving for abused substances.
    Type: Grant
    Filed: February 5, 1990
    Date of Patent: June 8, 1993
    Inventor: Stephen P. Berger
  • Patent number: 5217984
    Abstract: 1-Phenyl substituted-1H,3H-thiazole [3,4-a] benzimidazoles are prepared by reaction of o.phenilendiamine with a substituted benzaldehyde and with 2-mercaptoacetic acid. The new compounds are antiviral products.
    Type: Grant
    Filed: July 25, 1991
    Date of Patent: June 8, 1993
    Inventors: Pietro Monforte, Anna M. Monforte, Maria Zappala, Giovanni Romeo, Silvana Grasso, Alba Chimirri
  • Patent number: 5032590
    Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.
    Type: Grant
    Filed: March 8, 1990
    Date of Patent: July 16, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
  • Patent number: 5007953
    Abstract: Methods of using comminuted Alder bark as a stimulator of seed germination and growth media comprising comminuted Alder bark are disclosed. Also disclosed are seed treatment dusts comprising an active ingredient, a diluent material and comminuted Alder bark and methods of using these dusts. The active ingredients include fungicides, insecticides and other pesticides. The diluent materials used include clays and talcs.
    Type: Grant
    Filed: December 22, 1988
    Date of Patent: April 16, 1991
    Assignee: Snake River Chemicals, Inc.
    Inventor: Charles C. Chollet
  • Patent number: 4981864
    Abstract: The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## or R.sub.1 is a 5 or 6 membered heterocycle or when X is a valency bond R.sub.1 is also H, OH, mercapto, amino, alkyl, alkenyl, alkynyl, haloalkyl, alkylthio, formylaminoalkyl, pyridylcarbonylamino, cycloalkyl, or cycloalkenyl, alkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl or hydroxyalkyl of claim 1 or 2 for the preparation of pharmaceutical compositions with an erythrocyte aggregation inhibition action useful, for example, in states of shock or circulatory disturbance.
    Type: Grant
    Filed: November 30, 1988
    Date of Patent: January 1, 1991
    Assignee: Boehringer Mannehim GmbH
    Inventors: Wolfgang von der Saal, Alfred Mertens, Jens-Peter Hoelck, Erwin Boehm, Ulrich Martin
  • Patent number: 4978671
    Abstract: The invention relates to novel thieno-(3',4'-4,5)imidazo(2,1-b)thiazole derivatives of the formula ##STR1## in which R.sub.1 denotes hydrogen, halogen or CF.sub.3 andR.sub.2 denotes hydrogen or C.sub.1 -C.sub.4 alkyl and, in the case in which R.sub.2 denotes hydrogen, their pharmaceutically utilizable salts, a process for the preparation of these compounds and their use for the treatment of cancer or rheumatoid arthritis caused by a defective immune system.
    Type: Grant
    Filed: August 30, 1989
    Date of Patent: December 18, 1990
    Assignee: Chemisch Pharmazeutische Forschungsgesellschaft m.b.H.
    Inventors: Dieter Binder, Franz Rovenszky, Hubert P. Ferber