Additional Polycyclo Heterocyclic Ring System Containing Patents (Class 548/159)
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Patent number: 6174907Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N—R4; R1 and R2 independently represent hydrogen, a halogen atom, alkyl group or other; R3 and R4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.Type: GrantFiled: September 30, 1999Date of Patent: January 16, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Aoki, Kazuhiro Aikawa
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6136848Abstract: This invention relates to a flavone derivative represented by the formula (1) or a salt thereof, and also to a medicine containing the same. ##STR1## wherein A represents H, halogen, phenyl, naphthyl, a group of the formula (2) in which X is H or halogen, B is --CH.dbd.CH--, --CH.dbd.N--, --N(R.sup.7)-- (R.sup.7 : lower alkyl or alkoxyalkyl), --O-- or --S--; W represents a single bond, --CH.sub.2 O-- or --CH.dbd.CH--; at least one of R.sup.1 to R.sup.4 represents --COOH, --CN, alkyloxycarbonyl, tetrazolyl or --CONHR.sup.8 (R.sup.8 : H, lower alkyl or phenylsulfonyl), the remainder thereof individually represent H, halogen, --OH, lower alkyl or lower alkoxyl; R.sup.5 represents H, --OH, lower alkoxyl, --O(CH.sub.2).sub.m NR.sup.9 R.sup.10 (R.sup.9,R.sup.10 : H or lower alkyl, or coupled together with the adjacent N to form a phthalimido group; m: 1-5), or a group of the formula (3) (n: 1-5, l: 2-3; and R.sup.6 represents H, halogen, lower alkyl or lower alkoxyl.Type: GrantFiled: October 2, 1997Date of Patent: October 24, 2000Assignee: Kowa Co., Ltd.Inventors: Maria Elizabeth Zwaagstra, Mingqiang Zhang, Henk Timmerman, Masahiro Tamura, Yasushi Wada
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Patent number: 6130217Abstract: This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and multidrug resistant forms of malaria, tuberculosis, leishmania and amoebic dysentery to chemotherapeutants. The compounds and their pharmaceutically acceptable salts are also inhibitors of the active drug transport capability of P-glycoprotein which is encoded by the human MDR1 gene, as well as of certain other related ATP-binding-cassette transporters from eukaryotic and prokaryotic organisms (e.g., pfmdr from Plasmodium falciprum, and murine mdr1 and mdr3 gene products).Type: GrantFiled: September 20, 1995Date of Patent: October 10, 2000Assignee: Pfizer IncInventors: Lee Daniel Arnold, Jotham Wadsworth Coe, Takushi Kaneko, Mikel Paul Moyer
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Patent number: 6127395Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: August 3, 1999Date of Patent: October 3, 2000Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Charles A. Blum
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Patent number: 6114540Abstract: The invention provides spiro[pyrrolidine-2,3'-oxindole] compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, .alpha.-amino acids, and dipolarophiles (e.g., trans-chalcones, acrylate esters, or vinyl oxindoles).Type: GrantFiled: September 8, 1998Date of Patent: September 5, 2000Assignee: ArQule, Inc.Inventors: Demosthenes Fokas, David L. Coffen, William J. Ryan
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Patent number: 6110963Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein A is C or N;B is O, S, N, or CH.dbd.CH;E is ##STR2## or --X--D; D is ##STR3## or alkyl of 1-12 carbon atoms; X is CO, CH(OH), CH.sub.2, or --CH--S-2-benzothiazole;Y is hydrogen, alkyl of 1-6 carbon atoms, or halogen;Z is O, S, or N;R is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, or trifluoromethyl;R.sup.1 is alkyl of 1-12 carbon atoms, aryl of 6-10 carbon atoms, aralkyl of 7-15 carbon atoms, halogen, Het-alkyl wherein the alkyl moiety contains 1-6 carbon atoms, or aryl mono-, di- or tri-substituted with a substituent selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, trifluoromethyl, and alkoxy of 1-6 carbon atoms;Het is ##STR4## G is O, S, or N; and the remaining variables are as defined in claim 1, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: August 29, 2000Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 6077864Abstract: A compound of the formula ##STR1## wherein n, X, Y and Ar are as defined herein, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: June 17, 1999Date of Patent: June 20, 2000Assignee: Pfizer Inc.Inventors: Laurence Edward Burgess, James Patrick Rizzi
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Patent number: 6069156Abstract: Compounds of the formula (I): ##STR1## and their pharmaceutically acceptable compositions are useful in inhibiting the activity of cyclic guanosine 3',5'-monophosphate phosphodiesterase.Type: GrantFiled: December 10, 1997Date of Patent: May 30, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Kozo Sawada, Akio Kuroda, Kazuhiko Ohne, Atsushi Nomoto, Naomi Hosogai, Yoshimitsu Nakajima, Akira Nagashima, Keizo Sogabe, Kouichi Tamura, Masakazu Kobayashi
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Patent number: 6040327Abstract: A compound of formula (I): ##STR1## wherein: R.sub.1 represents halogen or a different group as defined in the description,Ra and Rb, which mnay be identical or different, represent hydrogen, alkyl, or hydroxy,X represents oxygen or sulphur or NR, R being H or alkyl,R.sub.2 represents optionally-substituted aryl,R'.sub.2 represents hydrogen or optionally-substituted aryl,its isomers and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same, are useful as inhibitors of interleukin 1.beta..Type: GrantFiled: July 22, 1998Date of Patent: March 21, 2000Assignee: Adir Et CompagnieInventors: Guillaume De Nanteuil, Bernard Portevin, Jacqueline Bonnet, Armel Fradin
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Patent number: 6037473Abstract: The invention relates to N-substituted benzazoles, processes for their preparation and their use as UV absorbers.Type: GrantFiled: April 23, 1999Date of Patent: March 14, 2000Assignee: Haarmann & Reimer GmbHInventors: Erich Dilk, Roland Langner, William Johncock
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Patent number: 6030619Abstract: Molecular mimetics of unique epitopes of Neisseria meningitidis serogroup B ("MenB") are disclosed. Compositions containing such molecular mimetics can be used to prevent MenB or E. coli K1 disease without the risk of evoking autoantibody responses.Type: GrantFiled: August 26, 1998Date of Patent: February 29, 2000Assignee: Chiron CorporationInventors: Dan M. Granoff, Gregory R. Moe
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Patent number: 6004536Abstract: 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: GrantFiled: August 14, 1996Date of Patent: December 21, 1999Assignee: Molecular Probes, Inc.Inventors: Wai-Yee Leung, Richard P. Haugland, Fei Mao
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Patent number: 5998451Abstract: Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.Type: GrantFiled: May 6, 1991Date of Patent: December 7, 1999Assignee: Pfizer IncInventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr.
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Patent number: 5998456Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R.sup.4 ; R.sup.1 and R.sup.2 independently represent hydrogen, a halogen atom, alkyl group or other; R.sup.1 and R.sup.4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C.sub.2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.Type: GrantFiled: January 16, 1998Date of Patent: December 7, 1999Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Aoki, Kazuhiro Aikawa
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Patent number: 5955607Abstract: Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly efficacious substances for producing medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.Type: GrantFiled: September 25, 1998Date of Patent: September 21, 1999Assignee: Hoechst Marion Roussel DeutschlandInventors: Joachim Brendel, Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann
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Patent number: 5942535Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 24, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5939415Abstract: The present invention relates to heterocyclic compounds with the formula ##STR1## in which R.sup.1 to R.sup.7, B, a, and X have the meanings indicated in the specification. These compounds can be used for the treatment of diseases of the rheumatic variety and for the prevention of allergically-induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 17, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5892033Abstract: Disclosed is a metal chelate dye which is composed of a metal ion and a ligand that is a methine dye having 2 or more bonding positions capable of coordinate bond to the metal ion at the bonding position. A thermal transfer recording material, an ink used for an ink jet image recording process and a color toner for electrostatic image recording process are also disclosed.Type: GrantFiled: September 4, 1996Date of Patent: April 6, 1999Assignee: Konica CorporationInventors: Tawara Komamura, Akira Onishi, Tatsuo Tanaka, Yoriko Nakayama, Mari Honda, Norio Miura
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Patent number: 5886014Abstract: Compounds of formula (I): ##STR1## ?wherein: X represents an optionally substituted benzimidazole group; Y represents an oxygen or sulfur atom; Z represents a 2,4-dioxothiazolidin-5-ylidenylmethyl, 2,4-dioxothiazolidin-5-ylmethyl, 2,4-dioxooxazolidin-5-ylmethyl, 3,5-dioxooxadiazolidin-2-ylmethyl or N-hydroxyureidomethlyl group; R represents hydrogen, alkyl, alkoxy, halogen, hydroxy, nitro, amino or aralkyl; and m is an integer from 1 to 5!; have valuable activity for the treatment and/or prophylaxis of a variety of disorders, including one or more of: hyperlipemia, hyperglycemia, obesity, impaired glucose tolerance (IGT), insulin resistance and diabetic complications.Type: GrantFiled: May 31, 1996Date of Patent: March 23, 1999Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Kunio Wada, Minoru Oguchi, Hiroaki Yanagisawa, Koichi Fujimoto, Toshihiko Fujiwara, Hiroyoshi Horikoshi, Takao Yoshioka
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Patent number: 5866594Abstract: An object of the invention is to provide an indole-2-carboxylic acid ester derivative which shows a selectively high fungicidal effect on fungicide-resistant fungi. The indole-2-carboxylic acid ester derivative of the invention is a compound represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom, a hydroxy group, a C.sub.1-4 acyl group, a C.sub.1-4 acyloxy group, a C.sub.1-4 alkoxy group, a (C.sub.1-4 alkoxycarbonyl)oxy group, a phenoxycarbonyl group or a C.sub.1-4 alkoxycarbonyl group, R.sup.2 is a C.sub.1-4 alkyl group, R.sup.3 is a hydrogen atom, a C.sub.1-4 alkyl group, a C.sub.2-4 alkenyl group, a phenyl group, a cyano group, a carbamoyl group or the like, R.sup.4 and R.sup.5 are the same or different and each represents C.sub.1-4 alkyl group or a halogen atom.Type: GrantFiled: April 4, 1997Date of Patent: February 2, 1999Assignee: Otsuka Kagaku Kabushiki KaishaInventors: Yasuhiro Endo, Kan Manabe, Yoshinori Endo, Tomozo Komura, Kazumi Sagayama, Kunio Yamaguchi
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Patent number: 5856478Abstract: The invention relates to new anellated (oxa) hydantoins, and herbicidal compositions containing same. The invention also relates to methods for controlling noxious plants using the anellated (oxa) hydantoins of the invention.Type: GrantFiled: November 19, 1996Date of Patent: January 5, 1999Assignee: Degussa AktiengesellschaftInventors: Matthias Schafer, Helmut Baier, Karlheinz Drauz, Hans-Peter Krimmer, Sabine Landmann
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Patent number: 5847156Abstract: 1,4-Diketopyrrolopyrroles of the formula ##STR1## in which A and B independently of one another are a group of the formula ##STR2## R.sub.1 is a long-chain radical containing a reactive group capable of polymerization, and R.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR3## or R.sub.1. The novel diketopyrrolopyrroles are suitable for preparing coloured polymers with unexpectedly advantageous colour effects.Type: GrantFiled: January 29, 1997Date of Patent: December 8, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Sameer Hosam Eldin, Abul Iqbal
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Symmetrical bis-heteroarylmethoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis
Patent number: 5843968Abstract: Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d) --NR.sup.6 SO.sub.2 R.sup.Type: GrantFiled: October 27, 1997Date of Patent: December 1, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Pramila Bhatia, Teodozyj Kolasa, Andrew O. Stewart, David E. Gunn, Richard A. Craig -
Patent number: 5840721Abstract: The present invention relates to polysubsituted imidazole having formula 1 ##STR1## These compounds are useful for restoring the sensitivity of multidrug resistant cells to cancer chemotherapeutic agents.Type: GrantFiled: October 16, 1997Date of Patent: November 24, 1998Assignee: Ontogen CorporationInventors: Adnan M. M. Mjalli, Chengzhi Zhang
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Patent number: 5837702Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.Type: GrantFiled: August 30, 1994Date of Patent: November 17, 1998Assignee: Bristol-Myers Squibb Co.Inventors: George C. Rovnyak, Karnail S. Atwal, Dinos P. Santafianos, Charles Z. Ding
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Patent number: 5821256Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.Type: GrantFiled: August 15, 1996Date of Patent: October 13, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus J. Schmitges, Maria Christadler
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Patent number: 5807866Abstract: A process for producing a compound of the formu5la ##STR1## comprising the step of reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## to form a compound of the formula ##STR4## wherein R.sup.2a is selected from the groups recited above for R.sup.2, or R.sup.2a --X-- is a protected hydroxyl group, and Z is a group of formula --Y--R.sub.5 recited above, or a group that can be converted into a group of said formula --Y--R.sup.5. Intermediates of formula IV and composition containing substantially optically pure enantiomers of Formula (I) are included within the scope of the invention.Type: GrantFiled: November 19, 1996Date of Patent: September 15, 1998Assignees: The University of East Anglia, Eli Lilly and CompanyInventors: Nicholas James Bach, Stephen Richard Baker, Jeremy Gilmore, Russell Andrew Lewthwaite, Alexander McKillop, Jason Scott Sawyer, George Richard Stephenson, Michael William John Urquhart
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Patent number: 5786487Abstract: The present invention relates to pyrrolopyrrole derivatives of the formula (I) ##STR1## wherein A and B are identical or different aryl radicals, and DPP is a diaryldiketopyrrolopyrrole radical; which diketopyrrolopyrrole derivative is substituted by from 0 to 6 moles of --SO.sub.3 M per mole of the pyrrolopyrrole derivative; wherein M is hydrogen or a metal or ammonium cation. The pyrrolopyrrole derivatives of formula I are useful as rheology-improving agents for pigment dispersions.Type: GrantFiled: September 26, 1997Date of Patent: July 28, 1998Assignee: Ciba Specialty Chemicals CorporationInventor: Shivakumar B. Hendi
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Patent number: 5783586Abstract: Compounds having the formula: ##STR1## wherein W.sup.1 and W.sup.2 are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted naphthyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is selected from thienyl, furyl, phenyl, naphthyl, benzo?b!thienyl, alkyl, hydroxyl, and hydrogen; Y an alkylene of one to six carbon atoms; and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.4, (c) --NR.sup.5 R.sup.6, (d)--NR.sup.4 SO.sub.2 R.sup.7 (e)--NH--Tetrazolyl, and (f) glycinyl; inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.Type: GrantFiled: October 1, 1996Date of Patent: July 21, 1998Assignee: Abbott LaboratoriesInventors: Teodozyj Kolasa, Clint D. W. Brooks, David E. Gunn
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Patent number: 5756740Abstract: A process for the preparation of photographic binary sensitizing dyes, which comprise two separate, nonconjugated chromophores, one of which has the capability of adsorbing to a silver halide grain surface, the other of which is substantially non-adsorbing to silver halide. The process comprises reacting two dye compounds in a solvent in the presence of a 2-halo-1-alkylpyridinium salt and a 4-dialkylaminopyridine.Type: GrantFiled: April 8, 1992Date of Patent: May 26, 1998Assignee: Eastman Kodak CompanyInventors: Lal Chand Vishwakarma, Chin Hsin Chen
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Patent number: 5753660Abstract: Selected sulfonylalkanoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: November 13, 1996Date of Patent: May 19, 1998Assignee: G. D. Searle & Co.Inventors: James A. Sikorski, Daniel P. Getman, Gary A. DeCrescenzo, Balekudru Devadas, John N. Freskos, Hwang-Fun Lu, Joseph J. McDonald
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Patent number: 5750558Abstract: Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.Type: GrantFiled: June 6, 1996Date of Patent: May 12, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Teodozyj Kolasa, Wendy Lee, Andrew O. Stewart
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Patent number: 5712225Abstract: The present invention relates to oxa(di)azabicyclic and thia(di)azabicyclic compounds, a method for their preparation and their use as herbicides.Type: GrantFiled: February 28, 1996Date of Patent: January 27, 1998Assignees: E. I. du Pont de Nemours and Company, Degussa AktiengesellschaftInventors: Wonpyo Hong, Matthias Schafer, Thomas Martin Stevenson
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Patent number: 5708188Abstract: The invention relates to mixed crystals of 1,4-diketopyrrolo?3,4-c!pyrroles, consisting of 1 mol each of two different compounds of formulae ##STR1## as well as single-phase solid solutions of two different compounds of formulae I and II, wherein the diketopyrrolopyrrole having the smaller geometrical constitution is present in an amount of 53 to 70 mol %. A and B are as defined in claim 1. The novel mixed crystals as well as the novel solid solutions are admirably suited for pigmenting organic material of high molecular weight.Type: GrantFiled: September 28, 1995Date of Patent: January 13, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, Abul Iqbal, Bernhard Medinger, Olof Wallquist
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Patent number: 5698364Abstract: Dye-donor element for thermal dye transfer comprising at least one magenta dye having extremely low side absorption in the blue and red regions of the spectrum, said dye corresponding to the general formula (I) : ##STR1## wherein R.sup.1 is H, (cyclo)alkyl, or aryl; X represents the atoms completing a heterocycle; Z is an electron-withdrawing group; Y is an electron-withdrawing group or --N(R.sup.2)R.sup.3 ; R.sup.2 and R.sup.3 together represent the atoms completing a heterocycle; or R.sup.2 and R.sup.3 together represent .dbd.C(R.sup.4)R.sup.5, or each of R.sup.2 and R.sup.3 represents (same or different) (cyclo) alkyl, aryl, or an electron-withdrawing group; each of R.sup.4 and R.sup.5 (same or different) represents H, (cyclo)alkyl, aryl, a heterocycle, SO.sub.2 R.sup.6, COR.sup.6, CSR.sup.6, POR.sup.6 R.sup.7, OR.sup.8, NR.sup.8 R.sup.9, SR.sup.8, or R.sup.4 and R.sup.5 together represent the atoms completing an aliphatic ring or a heterocycle, each of R.sup.6 and R.sup.Type: GrantFiled: June 6, 1995Date of Patent: December 16, 1997Assignee: Agfa-Gevaert, N.V.Inventors: Wilhelmus Janssens, Luc Vanmaele
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Patent number: 5675023Abstract: The present invention relates to a chromone derivative and an aldose reductase inhibitor comprising said compound as efective component, which is represented by the following formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent a lower alkyl group, etc., R.sub.3 represents an oxygen atom, a sulfur atom, etc., R.sub.7 represents a phenyl group substituted or not substituted, etc., and R represents a hydrogen atom or a lower alkoxy group. The present compounds exhibit superior inhititory action on aldose reductase and are useful for the treatment of various complications of diseases in diabetes, such as cataract, retinopathy, keratopathy, nephropathy, and neuropathy.Type: GrantFiled: June 6, 1995Date of Patent: October 7, 1997Assignee: Tsumura & Co.Inventors: Yasushi Igarashi, Takuji Yamaguchi, Yoshimitsu Ogawa, Mika Tomita, Hiroko Hayashi, Toshitsugu Sato, Kunio Hosaka
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Patent number: 5667764Abstract: Compounds are provided having the capability of binding therapeutically active substances to lipid containing bio-compatible particles, such as cells or viruses. These compounds include a bio-affecting moiety, comprising a therapeutically active substance, which is linked via a linking moiety to at least one hydrocarbon substituent selected so that the compounds is sufficiently non-polar to impart lipid binding capability to the compound. Thus, compounds of the invention are useful for site-selective delivery of therapeutic agents, and retention thereof at the selected site.Methods are provided for using various compounds of the invention in treatment of diseases or other pathological conditions. For example, methods are provided for treatment of: (1) post-angioplasty restenosis; (2) rheumatoid arthritis; (3) tumor cell proliferation, particularly tumor cells associated with ovarian cancer; and (4) psoriasis.Type: GrantFiled: May 15, 1992Date of Patent: September 16, 1997Assignee: Zynaxis, Inc.Inventors: Gregory A. Kopia, Paul K. Horan, Brian D. Gray, David E. Troutner, Katharine A. Muirhead, Kamleshkumar A. Sheth, Chia-En Lin, Zhizhou Yu, Bruce D. Jensen, Sue Ellen Slezak
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Patent number: 5668148Abstract: Compounds that specifically bind to the human alpha1a adrenergic receptor, including compounds effective to reduce symptoms of benign prostatic hypertrophy include compounds of formula: ##STR1## wherein: Ar1 and Ar2 can be independantly aromatic, heteroaromatic, or condensed heteroaromatic unsubstituted or substituted with amino, alkoxy, sulfonamido, alkyl, heteroalkyl, halo;m is 0 or 1;n is 0, 1, or 2;het is an aromatic or nonaromatic heterocyclic ring, substituted with alkyl, halo, or alkoxy substituents; andX is a branched or straight chain aliphatic or halogen substituent.Type: GrantFiled: April 20, 1995Date of Patent: September 16, 1997Assignee: Merck & Co., Inc.Inventors: Linda S. Payne, Steven D. Young, Mary Jo L. Zaborowski
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Patent number: 5663171Abstract: The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.1a, R.sub.2a, R.sub.3, R.sub.3a, R.sub.4, R.sub.5, R.sub.6, A, W, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: March 3, 1995Date of Patent: September 2, 1997Assignee: Merck & Co., Inc.Inventors: Meng Hsin Chen, Gregori J. Morriello, Ravi Nargund, Arthur A. Patchett, Lihu Yang
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Patent number: 5654296Abstract: The compound ##STR1## wherein ring A represents a benzene ring;Ar represents an aromatic group;R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group;m represents an integer of 1 to 6;n represents an integer of 2 to 3;- - - - - represents a single bond or a double bond;X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where - - - - - is a single bond or .dbd.N-- where - - - - - is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.Type: GrantFiled: December 6, 1996Date of Patent: August 5, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato, Yasuo Nagai
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Patent number: 5646290Abstract: Novel thiozolylisoindolenine dyestuffs of the formula (I) ##STR1## have been found in which A represents N or a cyanomethylene radical,B represents a radical of the formula C(CN)COOR.sub.5 or N--R.sub.6and the remaining substituents have the meanings given in the description. The invention also relates to mixtures thereof, a process for their preparation and their use for dyeing hydrophobic synthetic materials.Type: GrantFiled: May 18, 1995Date of Patent: July 8, 1997Assignee: Bayer AktiengesellschaftInventors: Manfred Lorenz, Klaus Wilfried Wanken
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Patent number: 5641789Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts and prodrugs thereof, wherein X.sup.1, Ar, X, Y.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.5 and n are defined below, which are inhibitors of the production of leukotrienes and/or blockers of leukotriene receptors, methods for preparing said compounds and intermediates useful in the preparation thereof, pharmaceutical compositions thereof methods of treatment therewith. The compounds of the above formula are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related diseases in mammals.Type: GrantFiled: March 31, 1995Date of Patent: June 24, 1997Assignee: Pfizer Inc.Inventor: Anthony Marfat
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Patent number: 5616725Abstract: Pyrrolo[3,4-c]pyrroles of formula ##STR1## wherein D and E are each independently of the other a group of formula ##STR2## The symbols Q, R.sub.8, R.sub.9, R.sub.10, R.sub.11, X, Y, Z, m and n are as defined in claim 1.These pyrrolo[3,4-c]pyrroles are distinguished by outstanding solid state fluorescence in the UV range as well as by the ease with which they can be converted to pyrrolopyrrole pigments even in the substrate in which they are incorporated.Type: GrantFiled: October 11, 1995Date of Patent: April 1, 1997Assignee: Ciba-Geigy CorporationInventors: John S. Zambounis, Zhimin Hao, Abul Iqbal
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Patent number: 5616729Abstract: Triggerable dioxetanes with a fluorescent substituent bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are carbon containing groups and wherein one of R.sub.1, R.sub.2 and R.sub.3 is a tethered fluorescent substitutent. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.Type: GrantFiled: December 27, 1988Date of Patent: April 1, 1997Assignee: Board of Governors of Wayne State UniversityInventors: Arthur P. Schaap, Hashem Akhavan-Tafti
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Patent number: 5607939Abstract: The compound ##STR1## wherein ring A represents a benzene ring; Ar represents an aromatic group; R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group; m represents an integer of 1 to 6; n represents an integer of 2 to 3; ----- represents a single bond or a double bond; X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where ----- is a single bond or .dbd.N-- where ----- is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.Type: GrantFiled: April 25, 1995Date of Patent: March 4, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato, Yasuo Nagai
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Patent number: 5599825Abstract: 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: GrantFiled: April 12, 1995Date of Patent: February 4, 1997Assignee: Fuji Photo Film Co., Ltd.Inventors: Noriaki Tatsuta, Akihiko Okegawa, Masayuki Kawakami, Keizo Koya
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Patent number: 5587112Abstract: A new class of proton transfer, benzazole, fluorescent compounds is composed of a 2-benzazolyl moiety covalently bonded to an aromatic fused ring heterocyclic moiety. The 2-benzazolyl moiety may be a 2-benzoxazolyl, 2-benzothiazolyl, or 2-benzimidazolyl. The aromatic fused ring heterocyclic moiety may be a 3-dibenzofuranyl or 3-dibenzothiophenyl each substituted at the 2 position with a proton donating group, or a 2-carbazolyl substituted at the 3 position with a proton donating group. The proton donating group may be hydroxy, sulfonamido, carbonamido, and the like, and preferably is hydroxy. The fluors are soluble in organic matrix materials such as solvents, monomers, resins, polymers, and the like. The UV-excited fluors emit short-lived fluorescence at .gtoreq.520 nm and may be used in the manufacture of fluorescent coatings, objects, scintillators, light sources and the like.Type: GrantFiled: September 2, 1994Date of Patent: December 24, 1996Assignee: Philadelphia College of Pharmacy and ScienceInventors: Joel M. Kauffman, Peter T. Litak
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Patent number: 5576443Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, X.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from a set consisting of aryl, substituted aryl, and a heterocyclic ring of a type present in photographic emulsions;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together can represent atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.Type: GrantFiled: March 30, 1995Date of Patent: November 19, 1996Assignee: Sterling Diagnostic Imaging, Inc.Inventors: Dietrich M. Fabricius, Gregory C. Weed
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Patent number: 5565488Abstract: The inventive Oxalylamino-benzofuran- and benzothienyl-derivatives are prepared by reacting the appropriate amino substituted benzofuranes and benzothiophenes with oxalic acid derivatives. The inventive compounds are suitable for the prevention and treatment of acute and chronic inflammatory processes, particularly of the airways.Type: GrantFiled: May 23, 1995Date of Patent: October 15, 1996Assignee: Bayer AktiengesellschaftInventors: Gabriele Braunlich, Rudiger Fischer, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Wendy J. McDonald-Gibson, Mary F. Fitzgerald