Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 548/217)
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Patent number: 5180825Abstract: Disclosed in a mitomycin derivative represented by the formula (I): ##STR1## wherein W is a heterocyclic group.Type: GrantFiled: November 13, 1991Date of Patent: January 19, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hitoshi Arai, Motomichi Kono, Masaji Kasai, Katsushige Gomi, Tadashi Ashizawa
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Patent number: 5175298Abstract: The present invention provides processes and intermediates for one preparation of the hydroxy ethylene isostere dipeptide of leu-val which is itself useful in the preparation of renin inhibitory peptides. The process employs certain novel oxazolidenes.Type: GrantFiled: December 11, 1990Date of Patent: December 29, 1992Assignee: The Upjohn CompanyInventor: Peter G. M. Wuts
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Patent number: 5169952Abstract: An efficient process for stereoselective preparation of a medicinally significant hydroxyamide compound of structural formula: ##STR1## comprises the addition of metalated amide enolates to chiral .alpha.-amino metalated epoxides. The hydroxyamide reaction products are useful as inhibitors of the HIV protease or of renin, or as intermediates in the preparation of inhibitors of the HIV protease or renin.Type: GrantFiled: July 2, 1991Date of Patent: December 8, 1992Assignee: Merck & Co., Inc.Inventors: David Askin, Ralph Volante, Michael Wallace, Ichiro Shinkai
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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: 5158964Abstract: A series of novel N-alkyl N-(alkanesulphonamidoheterocyclicmethyl)-4-alkanesulphonamidophenethylamin es have been prepared, including their pharmaceutically acceptable salts and various key novel intermediates therefor. The heterocyclic moiety present in these compounds is a benzo-fused heterocyclic group derived from either benzofuran, benzothiophene, benzoxazole or quinoline, and it is attached to the adjacent methyl group of the molecule by means of the available ring carbon atom which is situated alpha to the hetero atom. These particular compounds are useful in therapy as highly effective anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Preferred member compounds include N-methyl-N-(5 methanesulphonamidobenzofur-2-ylmethyl)-4-methanesulphonamidophenethylamin e and N-methyl-N-(6 methanesulphonamidoquinol-2-ylmethyl)-4-methanesulphonamidophenethylamine. Methods for preparing all these compounds from known starting materials are provided.Type: GrantFiled: July 8, 1991Date of Patent: October 27, 1992Assignee: Pfizer Inc.Inventors: John E. Arrowsmith, Peter E. Cross, Geoffrey N. Thomas
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Patent number: 5153358Abstract: A novel process for the preparation of .alpha.-alkylated .alpha.-amino acids and .alpha.-halogenated .alpha.-amino acids is disclosed. These .alpha.-alkylated .alpha.-amino acids and .alpha.-halogenated .alpha.-amino acids are useful as intermediates for the preparation of enzyme inhibitors (for example, renin inhibitors) and other peptides or amino acid derivatives or analogs.Type: GrantFiled: January 30, 1991Date of Patent: October 6, 1992Assignee: Abbott LaboratoriesInventor: Thomas M. Zydowsky
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Patent number: 5151523Abstract: A process for preparing 2-methylbenzoxazole by cyclizing acetamidophenol with the simultaneous elimination of the water of reaction. The process involves the drying and melting of the acetamidophenol, the cyclization of acetamidophenol to 2-methylbenzoxazole, and the removal of the water of reaction and the 2-methylbenzoxazole from the reaction mixture after the cyclization step by distillation. All the steps are carried out in a dryer.Type: GrantFiled: March 11, 1991Date of Patent: September 29, 1992Assignee: BASF AktiengesellschaftInventors: Manfred Gaeng, Heinz Saukel, Wolfgang Hoffmann, Josef Koenig
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Patent number: 5151424Abstract: [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1H-azepines and pyrrolidines and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.Type: GrantFiled: September 9, 1991Date of Patent: September 29, 1992Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Gaston S. M. Diels, Geert M. E. Pille
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Patent number: 5149764Abstract: Polymer-ceramic networks in which the polymer chain is anchored in a cera network are formed from compounds of the formula ##STR1## where X is R', OR', OH, H, Cl, or Br,X is R', OR', Cl, or Br,R' is an alkyl group having 1 to 8 carbon atoms, andR is selected from the group consisting of phenyl and a phenyl-substituted benzoxazole group,or oligomers thereof. Methods of forming the monomer, oligomer, and polymer are disclosed. Related phthalocyanine polymers are also disclosed.Type: GrantFiled: April 10, 1990Date of Patent: September 22, 1992Assignee: United States of America as represented by the Secretary of the NavyInventors: Kreisler S. Y. Lau, Abraham L. Landis, Thomas K. Dougherty
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Patent number: 5147878Abstract: Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S, --SO--, or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen such as chlorine, bromine or iodine, A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical in which the hydroxy is optionally substituted by a lower alkyl radical, Ar represents a group ##STR2## R.sub.4 denotes hydrogen or an alkyl radical and Cy represents a cyclic group.Type: GrantFiled: April 19, 1990Date of Patent: September 15, 1992Assignee: SanofiInventors: Jean Gubin, Pierre Chatelain
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Patent number: 5136099Abstract: 5-Hydroxy-benzo-(1',2')-cyclodeca-2,7-diyne-1-one and derivatives thereof and related fused ring diyneone macrocyclic compounds are disclosed. The compounds possess DNA-cleaving, antibiotic and tumor growth-inhibiting properties. Methods of making and using the same are also disclosed.Type: GrantFiled: August 1, 1990Date of Patent: August 4, 1992Assignee: Scripps Clinic and Research FoundationInventors: Golfo Skokotas, Kyriacos C. Nicolaou
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Patent number: 5120851Abstract: Water-soluble salts of (+)2-(4-fluorophenyl)-alpha-methyl-5-benzoxazole acetic acid with DL-lysine, D-lysine or L-lysine, suitable for the preparation of medicinal specialities such as syrups, creams, suppositories, aqueous solutions for personal hygiene etc, and their preparation process.The salts are obtained by suspending said acid in an organic solvent soluble or partly soluble in water, adding an equivalent quantity of the lysine and crystallizing the salt obtained.Type: GrantFiled: November 17, 1989Date of Patent: June 9, 1992Assignee: Euroresearch S.r.l.Inventor: Diego Furlan
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Patent number: 5118323Abstract: Novel benzoxazine compounds of the structure ##STR1## wherein X and Y are independently selected from the group hydrogen, alkyl, alkoxyalkyl, aminoalkyl, hydroxyalkyl and hydroxyaminoalkyl, each alkyl moiety having 1 to 6 carbons, and m=1, 2, or 3, have been found suitable as hair dyes.Type: GrantFiled: August 29, 1991Date of Patent: June 2, 1992Assignee: Clairol, Inc.Inventors: Mu-Ill Lim, Nancy A. Botta
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Patent number: 5112825Abstract: Novel pyridazinamines having antirhinoviral activity, compositions containing these compounds as active ingredient, and a method of inhibiting combating or preventing the growth of viruses in warm-blooded animals suffering from diseases caused by these viruses.Type: GrantFiled: April 30, 1990Date of Patent: May 12, 1992Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa
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Patent number: 5105009Abstract: Intermediates of Formula ##STR1## where R is a methylthio, methylsulfoxy, methylsulfonyl or a nitro group; andX1 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl, phenyl or phenylalkyl(1-6C), where the phenyl ring may be substituted by one or two halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; orX1 together with X2 is an oxygen atom or an alkylene having from two to five Carbon atoms; orX1 together with X2 and R4 is a chain of formula ##STR2## where p is 3 or 4 and q is 1 or 2; and X2 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl or phenyl which may be substituted by one or two halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; orX2 together with R4 is ##STR3## where n is 1 or 2; m is 0 or 1; X is hydrogen, halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; andX3 is hydrogen or --CO--R4 where R4 is hydrogen, 1-6 alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl, phenylalkyl(1-6C) or phenyl where the phenyl ring may be substituted by one or two halogen, 1-3 alkyl, 1-3 alkoxy or nitro; andX4 is --OH, fluorine,Type: GrantFiled: February 29, 1988Date of Patent: April 14, 1992Assignee: Zambon S.p.A.Inventors: Giancarlo Jommi, Dario Chiarino
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Patent number: 5104874Abstract: A series of 2-amino-5,6-dimethyl-1,4-benzoquinone derivatives, inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergic and antiinflammatory agents.Type: GrantFiled: December 13, 1990Date of Patent: April 14, 1992Assignee: Pfizer Inc.Inventors: Takafumi Ikeda, Hiroaki Wakabayashi, Masami Nakane
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5102893Abstract: Certain trans-6-[2-(N-heteroaryl-3,5-disubstituted) pyrazol-4-yl)ethyl]- or ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding ring-opened acids, esters and N-oxides derived therefrom which are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hydrolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.Type: GrantFiled: June 19, 1990Date of Patent: April 7, 1992Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Bruce D. Roth, Drago R. Sliskovic
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Patent number: 5099021Abstract: Process for the preparation of pure, unsymmetrically disubstituted ureas of the general formula ##STR1## in which R denotes a phenyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy, aryloxy or trifluoromethyl groups, an oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzoxazolyl or benzothiazolyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy or trifluoromethyl groups and R.sub.1 and R.sub.2 independently of one another denote a hydrogen atom or an alkyl group, where R.sub.1 and R.sub.2 are not simultaneously hydrogen or R.sub.1 and R.sub.2 together denote a butylene or pentylene group, by reaction of an N-alkyl- or N,N-dialkylurea with an unsubstituted or substituted arylamine or a heterocyclic amine in the presence of that amine which is already present in the starting material, the respective N-alkyl- or N,N-dialkylurea.Type: GrantFiled: October 30, 1990Date of Patent: March 24, 1992Assignee: Agrolinz Agrarchemikalien Gesellschaft m.b.H.Inventors: Rudolf H. Worther, Horst Korntner, Egmont Auer, Kurt Thonhofer
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Patent number: 5097034Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.Type: GrantFiled: May 14, 1991Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Udo Eckstein
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Patent number: 5097064Abstract: This invention relates to a process for preparing an optically active 2-arylpropionic acid of general formula (I), by the hydrogenation, in a heterogeneous aqueous-organic medium, of a 2-arylacrylic acid of general formula (II) in the presence of a catalyst consisting of a rhodium derivative and a water-soluble chiral ligand.Type: GrantFiled: August 30, 1990Date of Patent: March 17, 1992Assignee: Rhone-Poulenc SanteInventor: Jean-Michel Grosselin
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Patent number: 5089592Abstract: A biscyclobutarene monomer is prepared comprising two cyclobutarene moieties bridged by a divalent radical having at least one benzoxazole, benzothiazole or benzimidazole linkage. A reactive biscyclobutarene oligomer is also prepared by reacting a cyclobutarene-carboxylic acid, a diaminodihydroxyarene, diaminodithiolarene or tetraaminoarene and either an aromatic diacid or an aromatic diacid chloride. the monomers and reactive oligomers can be polymerized to form polymers exhibiting outstanding thermooxidative stability at high temperatures for prolonged time periods.Type: GrantFiled: May 25, 1989Date of Patent: February 18, 1992Assignee: The Dow Chemical CompanyInventors: Alan K. Schrock, William J. Harris, Norman L. Madison
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Patent number: 5089514Abstract: Certain 3-(phenyl, chroman-2-yl, benzofuran-5-yl, or benzoxazol-5-yl)-2-(hydroxy or mercapto)propionic acid derivatives and analogs are useful as hypoglycemic and hypocholesterolemic agents.Type: GrantFiled: June 14, 1990Date of Patent: February 18, 1992Assignee: Pfizer Inc.Inventor: Bernard Hulin
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Patent number: 5084468Abstract: A novel DC-88A derivative represented by general formula: ##STR1## wherein ##STR2## represents ##STR3## has an excellent antitumor activity and is useful as an antitumor agent.Type: GrantFiled: August 10, 1989Date of Patent: January 28, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hiromitsu Saito, Masaji Kasai, Makoto Morimoto, Eiji Kobayashi, Yoichi Uosaki, Yutaka Kanda, Hiroshi Sano
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Patent number: 5081245Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.Type: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 5081282Abstract: Bicyclo prostaglandin analogues have been prepared.Type: GrantFiled: January 13, 1988Date of Patent: January 14, 1992Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5077309Abstract: Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.Type: GrantFiled: March 28, 1990Date of Patent: December 31, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5064846Abstract: Insecticides of the general formula ##STR1## wherein R.sub.1 is an optionally substituted 5- to 10-member heterocyclic moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety; X is oxygen, sulfur or --NH--; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl, 3-(pyridyloxy)phenalkyl, 3-phenylaminophenalkyl, 3-benzylphenalkyl or 3-benzyloxyphenalkyl moiety; (b) a benzylfuranylmethyl moiety; (c) a 3- or 4-substituted benzyl or tetrafluorobenzyl moiety; (d) 4-phenoxy-2-butyn-2-yl; or (e) 2-methyl-3-phenylbenzyl.Type: GrantFiled: August 24, 1990Date of Patent: November 12, 1991Assignee: ICI Americas Inc.Inventor: Michael D. Broadhurst
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Patent number: 5055387Abstract: Sensitizing dyes for photographic materials are disclosed. The dyes have the formula: ##STR1## R.sub.2 is substituted or unsubstituted alkyl or substituted or unsubstituted aryl, andR.sub.1 and R.sub.3 are each independently substituted or unsubstituted alkyl, at least one of R.sub.1 and R.sub.3 having at least about 5 carbon atoms.Type: GrantFiled: March 13, 1990Date of Patent: October 8, 1991Assignee: Eastman Kodak CompanyInventors: Donald R. Diehl, Michael C. Malec
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5055110Abstract: Novel benzoxazine compounds of the structure ##STR1## wherein X and Y are independently selected from the group hydrogen, alkyl, alkoxyalkyl, aminoalkyl, hydroxyalkyl and hydroxyaminoalkyl, each alkyl moiety having 1 to 6 carbons, and m=1, 2 or 3, have been found suitable as hair dyes.Type: GrantFiled: November 22, 1989Date of Patent: October 8, 1991Assignee: Clairol IncorporatedInventors: Mu-Ill Lim, Nancy A. Botta
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Patent number: 5047554Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: January 31, 1990Date of Patent: September 10, 1991Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 5037842Abstract: A series of 5-(4-[2-substituted benzoxazolylmethoxy]benzyl)oxa- and thiazolidine-2,4-diones as antidiabetic and cholesterol lowering agents.Type: GrantFiled: June 5, 1990Date of Patent: August 6, 1991Assignee: Pfizer Inc.Inventor: Steven W. Goldstein
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Patent number: 5032590Abstract: 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: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 5028733Abstract: Bicyclooctane and bicycloheptane prostaglandin intermediates have been synthesized.Type: GrantFiled: December 12, 1989Date of Patent: July 2, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5026848Abstract: A heteroaryloxyalkylheterocyclic derivative of the Formula I:R--(CH.sub.2).sub.n --O--R.sup.1 Iis provided wherein:R is a non-fused azole moiety;n is 5, 6, 7 or 8; andR.sup.1 is a non-fused or fused substituted azole, azine, furyl or polycyclic hydrocarbon.Type: GrantFiled: March 27, 1989Date of Patent: June 25, 1991Assignee: Synphar Laboratories IncorporatedInventors: Mohsen Daneshtalab, Dai Q. Nguyen, Chan M. Ha, Hiep T. Luu, Laurence M. Tempest, Ronald G. Micetich
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Patent number: 5021438Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.Type: GrantFiled: March 15, 1989Date of Patent: June 4, 1991Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber
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Patent number: 5017707Abstract: Tetraindolylheptamethine ethers and alcohols of the isomeric formulae ##STR1## and ##STR2## and dyestuffs of the formula ##STR3## in which A, B, D and E denote ##STR4## and D'.sup..sym. denotes ##STR5## and the remaining symbols have the meanings given in the description, are used in pressure- and heat-sensitive recording materials.Type: GrantFiled: October 24, 1988Date of Patent: May 21, 1991Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Hubert Psaar, Gert Jabs
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Patent number: 5006660Abstract: The present invention relates to a process for producing an alkoxybenzene compound or an aryloxybenzene compound by reacting a halogenobenzene compound with an alcohol or a phenol compound in the presence of copper or a copper compound, an amine, and a base. According to the disclosure, an alkoxybenzene compound and an aryloxybenzene compound can be produced under moderate conditions in good yield with high selectivity.Type: GrantFiled: June 28, 1989Date of Patent: April 9, 1991Assignee: Fuji Photo Film Co., Ltd.Inventor: Katsuyoshi Yamakawa
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Patent number: 5003077Abstract: Methine dye which contains a cycloheptimidazole nucleus having a substituent at its 1-position thereof and in which the 7-membered ring moiety is substituted by a methine bond having an auxochrome, at the terminal thereof, for forming a conjugated resonance chromophoric group with the 10 .pi. electron series of the nucleus, showing a long absorption with one or a few methine bonds and have high light-stability and solution-stability.Type: GrantFiled: August 7, 1989Date of Patent: March 26, 1991Assignee: Fuji Photo Film Co., Ltd.Inventors: Takanori Hioki, Kazuhiko Matsumoto
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Patent number: 5001129Abstract: The present invention relates to tricyclic carbamates coplying with the formula ##STR1## in which n=0, 1 or 2,p=0 or 1,R.sub.1 represents a hydrogen atom; a group which is alkyl in C.sub.1 -C.sub.4 ; a phenyl group; a group which is alkenyl in C.sub.2 -C.sub.3 ; or a methyl group substituted by a hydroxy group, a group which is alkoxy in C.sub.1 -C.sub.4, an amino group or an N-alkylamino or N,N-dialkylamino group where the alkyl radical is in C.sub.1 -C.sub.4, andR.sub.2 represents a hydrogen atom; a halogen atom; a group which is alkyl in C.sub.1 -C.sub.4, or a group which is alkoxy in C.sub.1 -C.sub.4, and their salts of addition of acid.These compounds are therapeutically useful, notably as antidepressant agents.Type: GrantFiled: December 13, 1988Date of Patent: March 19, 1991Assignee: Delalande S.A.Inventors: Alain J. L. Renaud, Alain R. Schoofs, Jean-Marc M. Guiraudie, Denis M. Brochet
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Patent number: 4999042Abstract: Compounds of the fomrula (I): ##STR1## and sterioisomers thereof, wherein X is halogen, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, alkenyl, alkynyl, aryl, amino, arylazo, heteroarylalkyl, heteroaryloxyalkyl, acylamino nitro, nitride, trifluoromethyl, -OR.sup.1, -SR.sup.1, -CO.sub.2 R.sup.2, -CONR.sup.3 R.sup.4, -COR.sup.5, -CR.sup.6 .dbd.NR.sup.7, -N.dbd.CR8R.sup.9, -SOR.sup.10 or -SO.sub.2 R.sup.11 ; W, Y and Z, which may be the same or different, are any of the atoms or groups listed for X above and, in addition, may be hydrogen atoms; or any two of the groups W, X, Y and Z, in adjacent positions on the phenyl ring, optionally join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; R.sup.1 is alkyl, or cycloalkyl optionally containing a heteroatom in the cycloalkyl ring, alkenyl, acyl, aryl, heteroaryl, aralkyl or heteroarylalkyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.8, R.sup.9, R.sup.10 and R.sup.Type: GrantFiled: December 19, 1989Date of Patent: March 12, 1991Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Christopher R. A. Godfrey, Thomas E. Wiggins
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Patent number: 4996218Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.Type: GrantFiled: August 10, 1988Date of Patent: February 26, 1991Assignee: Glaxo Group LimitedInventor: Lawrence H. C. Lunts
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Patent number: 4992563Abstract: This invention relates to several intermediates useful in preparing thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)-thioxomethyl]hydrazono]ethyl]-1.alpha ., 4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha., 7a.alpha.-4.alpha.,7.alpha.-methano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: February 12, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 4988711Abstract: Inhibiting HMG-CoA reductase, as in treating hyperlipopproteinaemia, lipoproteinaemia and arteriosclerosis, with the new N-substituted N-amino-pyrroles of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2 is an aryl or heteroaryl radical,R.sup.3 is a hydrogen or an organic radical,R.sup.4 and R.sup.5 each independently is hydrogen or an organic radical or, together, they complete a heterocylic ring,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.10 is hydrogen or alkyl, and R.sup.11 is hydrogen, an organic radical or a cation.Type: GrantFiled: April 12, 1989Date of Patent: January 29, 1991Assignee: Bayer AktiengesellschaftInventors: Rolf Angerbauer, Walter Hubsch, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4968681Abstract: 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: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4966828Abstract: Disclosed is a compound of the general formula ##STR1## wherein L=H or CO--(R.sup.1).sub.n (CX.sub.3).sub.m, M=alkylene, alkenylene, Q=S, Se, O, dialkylmethylene, alken-1,2-ylene, 1,2-phenylene or N-R, with M+Q together forming 3 or 4 ring members, R=alkyl, aralkyl or alkoxyalkyl, R.sup.1 is an aromatic group and X=Cl, Br or I, with n=O and m=1 or n=1 and m=1 or 2. The compounds, on exposure, eliminate HX and form free radicals and are therefore highly effective as acid donors and free radical initiators for photochemical processes.Type: GrantFiled: September 13, 1984Date of Patent: October 30, 1990Assignee: Hoechst AktiengesellschaftInventors: Reinhard Doenges, Hans Ruckert, Ulrich Geissler, Hartmut Steppan
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Patent number: 4963576Abstract: The invention relates to dithioacetal compounds having 5-lipoxygenase-inhibiting activity, of the formula: ##STR1## wherein R.sup.1 is lower alkyl, di-(lower)alkylamino, aryl, or heterocyclic group which may have one or more substituents selected from halogen, lower alkyl, lower alkoxy and phenyl,R.sup.2 and R.sup.3 are each lower alkyl, aryl or ar-(lower)alkyl, or R.sup.2 and R.sup.3 are together to form 1,3-dithian ring,R.sup.4 is hydrogen or lower alkoxy, andn is O or an integer 1 to 4 and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 6, 1988Date of Patent: October 16, 1990Assignee: Fujisawa Pharmaceutical Company, Ltd.Inventors: Teruo Oku, Yoshio Kawai, Hiroshi Kayakiri, Kazuyoshi Kuratani, Masashi Hashimoto
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Patent number: 4962202Abstract: New derivatives of penem and pharmaceutically acceptable salt thereof are herein disclosed; these compounds being useful as an antibacterial agent which has an extremely wide antibacterial spectrum, exhibits a high sensitivity to bacteria resistant to conventional penicillins and cephalosporing antibiotics and is excellent in its physico-chemical stability, solubility to water and biological stability, in particular, stability to decomposition by enzyme such as dehydropeptidase I in kidney, .beta.-lactamase; these derivatives of penem being able to be prepared by reacting 2-substituted sulfinyl derivative of penem with a thiol compound and then optionally removing protective group(s) and further alkylating the reaction product or vice versa.Type: GrantFiled: January 11, 1988Date of Patent: October 9, 1990Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Makoto Sato, Makoto Takemura, Kunio Higashi, Tsunehiko Soga, Hiroo Matsumoto, Toshiyuki Nishi
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Patent number: 4957932Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, antiallergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: November 25, 1987Date of Patent: September 18, 1990Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Robert Zamboni