Patents Examined by Edward C. Ward
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Patent number: 5204340Abstract: This invention provides 6-substituted-4-(amino or substituted amino)tetrahydrobenz[c,d]indole serotonin agonists useful in treating a variety of conditions associated with serotonin function.Type: GrantFiled: February 26, 1990Date of Patent: April 20, 1993Assignee: Eli Lilly and CompanyInventors: Michael E. Flaugh, Mark M. Foreman
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Patent number: 5202326Abstract: The invention concerns a heterocyclic ether of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl or (2-4 C)alkanoyl, or optionally substituted benzoyl;R.sup.2 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl; andR.sup.3 is substituted (1-4C)alkyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: November 25, 1991Date of Patent: April 13, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Jean-Marc M. M. Girodeau
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Patent number: 5180737Abstract: Compound of the formula (I):Q.sup.1 Q(CR.sup.2 .dbd.CR.sup.3).sub.a (CR.sup.4 .dbd.CF)(CR.sup.5 .dbd.CR.sup.6).sub.b C(.dbd.O)NHR.sup.1 (1)or a salt thereof, wherein Q.sup.1 is a phenyl ring or a fused bicyclic ring system containing 9 or 10 ring carbon atoms at least one ring being aromatic, or Q.sup.1 is a dihalovinyl group; Q is an alkyl chain containing 1 to 12 carbon atoms and optionally containing one or two oxygen atoms and/or an unsaturated group --CR.sup.7 .dbd.CR.sup.8 --, or --C.dbd.C--, wherein R.sup.7 and R.sup.8 are selected from hydrogen or halo; a is 0 or 1; b is 0 or 1; the sum of a and b is 0 or 1; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and are independently selected from hydrogen, halo and C.sub.1-4 alkyl; R.sup.1 is selected from hydrogen and C.sub.1-6 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy are disclosed which have pesticidal activity.Type: GrantFiled: June 8, 1989Date of Patent: January 19, 1993Assignee: Roussel UclafInventor: Robert J. Blade
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Patent number: 5164371Abstract: The invention provides a series of novel heterocyclic ketones of formula I ##STR1## and pharmaceutically acceptable base-addition salts thereof, in which the values of R.sup.4, L, A, X and Q have the meanings defined in the following specification. The compounds of formula I are inhibitors of human leukocytic elastase. The invention also provides pharmaceutical compositions containing a compound of formula I, or a pharmaceutically acceptable base-addition salt thereof, and processes and intermediates for the manufacture of compounds of formula I.Type: GrantFiled: May 11, 1988Date of Patent: November 17, 1992Assignee: ICI Americas Inc.Inventors: Philip D. Edwards, Joseph J. Lewis, Charles W. Perkins, Diane A. Trainor, Richard A. Wildonger
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Patent number: 5132432Abstract: The invention relates to novel fluorescent dyes based on the following pyrenyloxy sulfonic acid structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is --OCH.sub.2 C(O)OCH.sub.3, --OCH.sub.2 CON(O)H, --OCH.sub.2 CON.sub.3, --OCH.sub.2 CONHNH.sub.2, ##STR2## or --CH.sub.2 CONH(CH.sub.2).sub.n NH.sub.2 where n is an integer from 1 to 10; at least one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is sulfonic acid or alkali salts of sulfonic acid; and all other of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen or a hydroxyl group. The new reagents contain functional groups typically found in biomolecules or polymers. The spectral properties of the fluorescent dyes are sufficiently different in wavelengths and intensity from fluorescein as to permit simultaneous use of both dyes with minimum interference.Type: GrantFiled: September 22, 1989Date of Patent: July 21, 1992Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, James E. Whitaker
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Patent number: 5128345Abstract: Novel indoloquinoline compounds of formula (I), benzo(b)acridines of formula (II) and benzo(c)acridines of formula (III) have carcinostatic activities. The compounds, processes for preparing the compounds via nucleophilic aromatic substitution, and carcinostatic compositions containing the same are disclosed.Type: GrantFiled: March 3, 1989Date of Patent: July 7, 1992Assignee: Mect CorporationInventor: Masatoshi Yamato
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Patent number: 5118670Abstract: Compositions useful in the treatment of inadequate neuronal dopamine release, as well as methods of use therefor. The compositions include drugs, such as thyrotropin-releasing hormone, which result in enhanced release of dopamine and tyrosine or a tyrosine precursor.Type: GrantFiled: December 14, 1988Date of Patent: June 2, 1992Assignee: Massachusetts Institute of TechnologyInventors: Richard J. Wurtman, Ian Acworth, Michael Kreutz, Hendrik Lehnert
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Patent number: 5068334Abstract: This invention relates to pharmaceutical compositions containing quinolin-2,5-diones of formula ##STR1## wherein A, B, R.sup.1 to R.sup.3 and X are defined hereinbelow, some of which are novel, which compounds have valuable pharmacological properties, particularly analgesic antipyretic and/or antiphlogistic effects, to new intermediates and processes for preparing them.Type: GrantFiled: September 27, 1989Date of Patent: November 26, 1991Assignee: Karl Thomae GmbHInventors: Erich Muller, Josef Nickl, deceased, Armin Heckel, Gunther Engelhardt
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Patent number: 5061701Abstract: A compounds of general formula I ##STR1## wherein R.sub.1 is hydrogen or hydroxy, and the hydroxy group at the 7-position can be either in .alpha. or .beta. configuration, are valuable in human therapy. Compounds I can be prepared by fluorination of the suitably protected 6-hydroxy-7-keto-derivatives.Type: GrantFiled: April 9, 1990Date of Patent: October 29, 1991Assignee: Giuliani S.p.A.Inventors: Roberto Pellicciari, Aldo Roda, Giuliano Frigerio
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Patent number: 5055470Abstract: A process for protecting brain cells from ischemia and for treating ischemic and degenerative brain disorders. The process involves systemic administration of BMY 14802 or a pharmaceutically acceptable acid addition salt and/or hydrate.Type: GrantFiled: June 1, 1989Date of Patent: October 8, 1991Assignee: Bristol-Myers Squibb Co.Inventors: Christopher G. Boissard, Duncan P. Taylor, Michael S. Eison
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Patent number: 5053514Abstract: Method for prophylaxis and treatment of heart diseases using a carbostyril derivative of formula: ##STR1## wherein R.sup.1 is H or CN, and R.sup.2 and R.sup.3 are each H, alkyl optionally substituted by OH, cyclocalkyl, alkenyl, phenyl, phenylalkyl having optionally substituents of alkoxyalkoxy, halogen, alkoxy, NO.sub.2, alkyl, CN, alkylthio or alkylsulfinyl on phenyl ring and having optionally OH-substituent on alkyl moiety, phenylsulfonyl having optionally alkoxy substituent on phenyl ring, phenylthioalkyl, phenylsulfinylalkyl having optionally substituents of halogen or alkoxy on phenyl ring, phenoxyalkyl having optionally substituents of halogen or alkoxy on phenyl ring, pyridylalkyl having optionally substituents of halogen or alkoxy on pyridine ring, thienylalkyl, benzoyalkyl, anilinothiocarbonyl, benzoyl, pyridyl, phenylalkenyl, or group of --A--NR.sup.4 R.sup.5 (R.sup.4 and R.sup.Type: GrantFiled: August 9, 1989Date of Patent: October 1, 1991Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Takafumi Fujioka, Shuji Teramoto, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5049588Abstract: A method for the treatment and/or prophylaxis of disorders associated with neuronal degeneration resulting from ischaemic events, in mammals, such as humans, which comprises administering to the mammal in need of such treatment an effective amount of a 5-HTl.sub.A agonist.Type: GrantFiled: May 8, 1989Date of Patent: September 17, 1991Assignee: Beecham Group p.l.c.Inventors: Charles D. Nicholson, Johannes Jukna
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Patent number: 5047552Abstract: Disclosed herein are novel benzopyrans having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of hypertension.Type: GrantFiled: February 7, 1990Date of Patent: September 10, 1991Assignee: American Home Products CorporationInventors: Dominick A. Quagliato, Leslie G. Humber
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Patent number: 5039820Abstract: 4-Amino-6-iodo-1,2,2a,3,4,5-hexahydrobenz[ cd]indoles are useful intermediates to 4-amino-1,3,4,5-tetrahydrobenz [cd]indoles containing aminocarbonyl or alkoxycarbonyl substituents in the 6-position which are useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: February 26, 1990Date of Patent: August 13, 1991Assignee: Eli Lilly and CompanyInventors: Thomas J. Kress, James P. Wepsiec
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Patent number: 5039798Abstract: Provided are novel naphthalocyanine dimer compounds of the general formula:RO--YNc--O--NcY--OR (I)wherein Nc represents a naphthalocyanine moiety, which can be substituted or unsubstituted; Y represents a central hetero atom of the naphthalocyanine moiety; and, OR represents an alkoxide cap bonded to the central hetero atom Y, with the first carbon atom of the alkoxide (OR) capping group being a tertiary carbon. Also provided is a method for preparing the dimer compounds, which method comprises reacting a naphthalocyanine dihalide in solution with a tertiary alcohol and a nucleophile. The process efficiently and reproducibly provides a naphthalocyanine oxo-bridged dimer having terminal alkoxide caps.Type: GrantFiled: March 1, 1990Date of Patent: August 13, 1991Assignee: Hoechst Celanese Corp.Inventor: Robert E. Johnson
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Patent number: 5028708Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## (wherein X represents ##STR2## Y represents C.dbd.O, C.dbd.C(CN).sub.2 or SO.sub.2 ; R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group which may be substituted, an alkoxyl group which may be substituted, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group which may be substituted, --A--R or ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom, an alkyl group which may be substituted, an aryl group which may be substituted or a cyclohexyl group; R.sub.5 and R.sub.6 may be combined to form a ring or may form a ring with a hetero atom; R.sub.7 and R.sub.Type: GrantFiled: April 8, 1988Date of Patent: July 2, 1991Assignee: Sumitomo Chemical Company, LimitedInventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
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Patent number: 5021563Abstract: A metal naphthalocyanine derivative and process for producing said derivative which is represented by the following formula (I): ##STR1## wherein M represents germanium or tin; L and L' each independently represent a halogen, a hydroxyl group, an alkyl group, an alkoxy group or a siloxy group of the formula R.sub.1 R.sub.2 R.sub.3 SiO-- (wherein R.sub.1, R.sub.2 and R.sub.3 each independently represent a hydrogen atom, an alkyl group, an alkoxy group or an aryl group).Type: GrantFiled: October 6, 1989Date of Patent: June 4, 1991Assignees: Hitachi Chemical Company, Ltd., Hitachi, Ltd.Inventors: Shigeru Hayashida, Seiji Tai, Nobuyuki Hayashi, Yasushi Iwakabe, Noriyuki Kinjo, Shunichi Numata
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Patent number: 5015418Abstract: Disclosed is a composition comprising a mixture of acylated diesters of dl-malic acid corresponding to the formula: ##STR1## where P is palmityl and S is stearyl.Type: GrantFiled: December 14, 1989Date of Patent: May 14, 1991Assignee: Haarmann & Reimer Corp.Inventors: Donald F. Hershberger, Richard A. Plunkett
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Patent number: 5011837Abstract: Novel compounds of the formula ##STR1## and tautomers thereof, wherein at least one of R.sub.2, R.sub.3 and R.sub.4 is a strong electron withdrawing group, are disclosed. These compounds possess potassium channel activating activity and, as such, are useful as antihypertensive agents. Advantageously, the compounds of the present invention have shown less cardiac effects than known potassium channel activators.Also disclosed is a process for preparing these and other compounds.Type: GrantFiled: May 8, 1989Date of Patent: April 30, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Karnail Atwal, John R. McCullough, Gary J. Grover
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Patent number: 4997827Abstract: A composition for in vivo inhibition of aromatase in a mammal, which comprises an in vivo inhibitory amount of a compound having the following general formula: ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-20 acyl, in combination with a pharmaceutically acceptable carrier or diluent thereof.Type: GrantFiled: March 9, 1989Date of Patent: March 5, 1991Assignee: Medical Foundation of Buffalo, Inc.Inventor: Yoshio Osawa