The Six-membered Hetero Rings Are Bonded Directly To Each Other Patents (Class 514/334)
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Patent number: 5616317Abstract: A polycationic microbicidal and algaecidal agent containing as an active ingredient a polymer comprising repeating units represented by the formula (I) and having a number average molecular weight of at least 1,000, and a microbicidal and algaecidal method using the polymer: ##STR1## (wherein A is a single bond, an oxygen atom, a phenylene group, a dioxyethylene group or a tetramethyldisiloxane group, X.sub.1.sup.- and X.sub.2.sup.- may be the same or different and are counter anions in quaternary salts, p and q may be the same or different and are integers of from 1 to 6, and m is an integer of from 1 to 6, provided that A, X.sub.1.sup.-, X.sub.2.sup.-, p, q and m may be the same or optionally different for every repeating unit).Type: GrantFiled: June 14, 1995Date of Patent: April 1, 1997Assignees: Sagami Chemical Research Center, K.multidot.I Chemical Industry Co., Ltd.Inventors: Yu Nagase, Takao Aoyagi, Tomoko Akimoto, Kazunori Tanaka, Kouichi Iwabuchi, Yoshihiro Konagai
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Patent number: 5610169Abstract: The orally administrable pharmaceutical compositions containing a slightly water-soluble drug, characterized by improved stability and improved absorption of the drug from digestive tract into blood. The use of the compositions of the present invention enables decrease of the dose amount of a slightly water-soluble drug, which eventually leads to alleviation of pains and side effects on the part of patients.Type: GrantFiled: June 7, 1995Date of Patent: March 11, 1997Assignee: The Green Cross CorporationInventors: Toru Iwao, Kenichi Hirai, Nobuo Kondoh, Koichi Yamanouchi, Kazumasa Yokoyama
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Patent number: 5602110Abstract: A method and composition for treating cystic fibrosis comprising administering to a patient a first component, a second component, and preferably a third component. The first component is an inhibitor which is specific for a cGMP-inhibited type III cAMP phosphodiesterase, preferably milrinone or amrinone; the second component is an adenylate cyclase activator, preferably forskolin, isoproterenol or albuterol; the third component is cAMP or a cAMP analog which activates protein kinase A.Type: GrantFiled: January 26, 1995Date of Patent: February 11, 1997Assignee: Case Western Reserve UniversityInventors: Mitchell L. Drumm, Thomas J. Kelley
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Patent number: 5602257Abstract: A novel synthesis of anabaseine using an animal nicotinoyl piperidone salt having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are lower alkyl, or R.sub.1 and R.sub.2 forms a morpholine or piperidine ring and the metal is a group I alkaline metal.Type: GrantFiled: September 9, 1994Date of Patent: February 11, 1997Assignee: University of Florida Research FoundationInventors: John A. Zoltewicz, Michael P. Cruskie
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Patent number: 5585389Abstract: There are provided substituted acid amide, arylhydrazone compounds (amidrazones) of formula I ##STR1## the use thereof for the control of insect and acarid pests and methods and compositions for the protection of crops from the damage and loss caused by said pests.Type: GrantFiled: April 28, 1995Date of Patent: December 17, 1996Assignee: American Cyanamid CompanyInventors: Joseph A. Furch, David G. Kuhn, David A. Hunt
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Patent number: 5530001Abstract: A novel pharmaceutical use of a dihydropyridine derivative of the formula (I) ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and each is an alkyl or the like; R.sub.4 is a hydrogen atom or the like; R.sub.5 is nitro, a halogenated alkyl, cyano or the like; X is a vinylene or an azomethine; A is an alkylene; and B is --N(R.sub.6) (R.sub.7) or a group of the formula ##STR2## wherein R.sub.6 and R.sub.7 are the same or different and each is an alkyl, an aralkyl, an aryl or the like; R.sub.8 and Ar are aryl or the like; and n is 0, 1 or 2, or an acid addition salt thereof for promoting PGI.sub.2 production, and for the treatment and prevention of hyperlipemia, arteriosclerosis and cerebral diseases.Type: GrantFiled: February 24, 1995Date of Patent: June 25, 1996Assignee: The Green Cross CorporationInventors: Masahide Nakajima, Norifumi Nakamura, Feng Wang, Koichi Yamanouchi, Kazutaka Hayashi, Hideaki Kido, Yoshiji Kubo, Minori Okita, Takeshi Uchida, Masahiro Watanabe, Katsumi Yamanaga, Hiroshi Shinyama, Toru Kawamura, Yuji Narita
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Patent number: 5516785Abstract: Method of using anabaseine, and DMAB-anabaseine for stimulating brain cholinergic transmission and a method of making anabaseine.Type: GrantFiled: October 21, 1993Date of Patent: May 14, 1996Assignee: University of Florida Research Foundation, IncorporatedInventors: John A. Zoltewicz, William R. Kem, Edwin M. Meyer
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Patent number: 5462951Abstract: The orally administrable pharmaceutical compositions containing a slightly water-soluble drug, characterized by improved stability and improved absorption of the drug from digestive tract into blood. The use of the compositions of the present invention enables decrease of the dose amount of a slightly water-soluble drug, which eventually leads to alleviation of pains and side effects on the part of patients.Type: GrantFiled: September 3, 1993Date of Patent: October 31, 1995Assignee: The Green Cross CorporationInventors: Toru Iwao, Kenichi Hirai, Nobuo Kondoh, Koichi Yamanouchi, Kazumasa Yokoyama
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Patent number: 5446014Abstract: Precipitate-free aqueous compositions, well adapted as agricultural chemicals, e.g., crop protectants, are comprised of at least one water soluble cationic organic compound, e.g., a pesticidally active quaternary ammonium compound, and a thickening amount of a xanthan gum having an intrinsic viscosity of less than 3,500 cm.sup.3 /g.Type: GrantFiled: July 26, 1991Date of Patent: August 29, 1995Assignee: Rhone-Poulenc ChimieInventors: Jean-Luc Schuppiser, Magali Knipper
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Patent number: 5424323Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.Type: GrantFiled: March 23, 1994Date of Patent: June 13, 1995Assignee: Cetylite Industries, Inc.Inventors: Stanley L. Wachman, Sidney Karlan
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Patent number: 5424301Abstract: Solid compositions of certain cholinergic compounds are stabilized in starch. Especially compositions of corn starch combined or mixed with the 0-substituted-1,2,5,6-tetrahydro-3-pyridine oxime ether, CI-979 HCl, a cognition activator, have been found stable in a heated environment of up to 60.degree. C. over 17 days such that no losses were detected by HPLC analysis. A solid peroral pharmaceutical formulation for the treatment of cognitive disorders is based on the bicomponent composition of active ingredient and stabilizer using appropriate amounts of other excipients or components known in the formulation art.Type: GrantFiled: February 1, 1993Date of Patent: June 13, 1995Assignee: Warner-Lambert CompanyInventors: Hua-Pin Huang, Scott C. Wootton, Thomas N. Julian, Galen W. Radebaugh, Mahdi B. Fawzi
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Patent number: 5407949Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.Type: GrantFiled: March 23, 1994Date of Patent: April 18, 1995Assignee: Cetylite Industries, Inc.Inventors: Stanley L. Wachman, Sidney Karlan
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Patent number: 5354761Abstract: Compounds of formula I ##STR1## wherein Y, Z, S, S', m, n and R.sub.1 -R.sub.4 are as defined in the description, have valuable pharmaceutical properties and are effective especially against protozoal infections. They are prepared in a manner known per se.Type: GrantFiled: June 1, 1993Date of Patent: October 11, 1994Assignee: Ciba-Geigy Corp.Inventors: Jaroslav Stanek, Giorgio Caravatti, Hans-Georg Capraro, Jorg Frei
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Patent number: 5346899Abstract: Substituted pyridine compounds of formula I ##STR1## and plant-tolerated acid addition salts and metal salt complexes thereof, and fungicides containing these compounds.Type: GrantFiled: September 1, 1993Date of Patent: September 13, 1994Assignee: BASF AktiengesellschaftInventors: Thomas Mueller, Karl Eicken, Albrecht Harreus, Hartmann Koenig, Costin Rentzea, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5344838Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.Type: GrantFiled: December 8, 1993Date of Patent: September 6, 1994Assignee: Cetylite Industries, Inc.Inventors: Stanley L. Wachman, Sidney Karlan
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Patent number: 5338737Abstract: Novel heterocyclic methyl derivatives of biphenyl oxadiazoles and thiadiazoles are described, as well as methods for the preparation of said derivatives and pharmaceutical compositions of the same, which are useful as antagonists of the angiotensin II enzyme and thus useful in treating hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.Type: GrantFiled: February 12, 1993Date of Patent: August 16, 1994Assignee: Warner-Lambert CompanyInventors: David T. Connor, Catherine R. Kostlan
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Patent number: 5338748Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.Type: GrantFiled: December 9, 1993Date of Patent: August 16, 1994Assignee: Cetylite Industries, Inc.Inventors: Stanley L. Wachman, Sidney Karlan
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Patent number: 5300526Abstract: Insecticidal compositions comprising one or more compounds selected from the group consisting of delta-aminolevulinic acid, inducers of delta aminolevulinic acid, and enhancers of delta-aminolevulinic acid conversion to photodynamic tetrapyrroles; and methods of making and using same.Type: GrantFiled: November 20, 1991Date of Patent: April 5, 1994Assignee: The Board of Trustees of the University of IllinoisInventors: Constantin A. Rebeiz, John A. Juvik, Carole C. Rebeiz
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Patent number: 5260323Abstract: 2,4- and 2,5-substituted pyridine-N-oxides are provided which are effective as fibrosuppressives and immunosuppressives. Said compounds are also suitable for the treatment of disorders of the metabolism of collagen and collagen-like substances or the biosynthesis of Clq.Type: GrantFiled: November 19, 1992Date of Patent: November 9, 1993Assignee: Hoechst AktiengesellschaftInventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall
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Patent number: 5204357Abstract: The invention relates to compounds of the formula I ##STR1## in which A represents a substituted thio-, sulfinyl- or sulfonyl-alkanoyl radical or a four- to eleven-membered heterocycle, B is an amino acid residue, R.sup.1 denotes hydrogen (substituted) alkyl, (substituted)cycloalkyl or aryl, R.sup.2 represents hydrogen, (substituted)alkyl or aryl, R.sup.3 denotes a radical of the formula --(CH.sub.2).sub.q --(X).sub.r --(CH.sub.2).sub.s --R.sup.6 with X denoting CF.sub.2, CO or CHR.sup.8, R.sup.6 denoting a (substituted)heteroaromatic, R.sup.8 denoting alkyl, alkoxy, alkylthio, alkylamino, hydroxyl, azide or halogen, q and s denoting 1 to 4, and r denoting 0 or 1, and R.sup.9 is hydrogen, (substituted)alkyl, alkanoyl, cycloalkanoyl, (substituted) aroyl or (substituted)aryl, and to the salts thereof. In addition, processes for the preparation of these compounds, and the use thereof as renin inhibitors are described.Type: GrantFiled: February 14, 1989Date of Patent: April 20, 1993Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
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Patent number: 5200427Abstract: Insecticidal compositions comprising one or more compounds selected from the group consisting of delta-aminolevulinic acid, inducers of delta aminolevulinic acid, and enhancers of delta-aminolevulinic acid conversion to photodynamic tetrapyrroles; and methods of making and using same.Type: GrantFiled: January 9, 1989Date of Patent: April 6, 1993Assignee: The Board of Trustees of the Univ. of IllinoisInventors: Constantin A. Rebeiz, John A. Juvik, Carole C. Rebeiz
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Patent number: 5120734Abstract: Fungicidal acetic acid esters of the formula ##STR1## in which A.sup.1 is an optionally substituted phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, thienyl, furanyl, pyrrolyl, thiazolyl, pyrazolyl, oxazolyl, phenoxy, phenylacetylenyl or phenylethylenyl radical, andA.sup.2 and A.sup.3 each is a lower alkyl radical.Type: GrantFiled: November 13, 1990Date of Patent: June 9, 1992Assignee: Bayer AktiengesellschaftInventors: Alexander Klausener, Gerd Kleefeld, Dieter Berg, Stefan Dutzmann, Gerd Hanssler
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Patent number: 5120747Abstract: Platelet activating factor antagonists of formula (I): ##STR1## wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl(C.sub.1 -C.sub.4)alkoxy, fluoro(C.sub.1 -C.sub.4)alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring;R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C.sub.1 -C.sub.4 alkyl)piperazinyl or N-(C.sub.2 -C.sub.4 alkanoyl)-piperazinyl group;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl and R.sup.1 is CN, C.sub.3 -C.sub.7 cycloalkyl, aryl, heteroaryl or a C.sub.1 -C.sub.4 alkyl group substituted by one or more substituents selected from C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, aryl or heteroaryl;Z is selected from C.sub.1 -C.sub.6 alkoxy, aryl(C.sub.1 -C.sub.Type: GrantFiled: May 1, 1990Date of Patent: June 9, 1992Assignee: Pfizer Inc.Inventors: Kelvin Cooper, Michael Fray, Kenneth Richardson, John Steele
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Patent number: 5120748Abstract: Substituted 1,2,3,6-tetrahydropyridines are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: June 28, 1991Date of Patent: June 9, 1992Assignee: Warner-Lambert CompanyInventors: Bradley W. Caprathe, Juan C. Jaen, Lawrence D. Wise
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Patent number: 5064842Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein:.alpha. and .beta. together represent a bond and additionally when B is an electron withdrawing group .alpha. can also represent OH and .beta. can represent hydrogen;Ar is an optionally substituted aryl or heteroaryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optioanlly substituted aryl or heteroaryl;A represents a group of formula --XR.sup.3 wherein X is a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q -- in which formula: Y represents --O--, --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 R.sup.6, R.sup.7 and R.sup.Type: GrantFiled: June 25, 1990Date of Patent: November 12, 1991Assignee: John Wyeth & Brother LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5047414Abstract: Compounds of formula I, and pharmaceutical compositions containing compounds of formula I ##STR1## wherein: R.sub.1 is:(a) COCH.sub.3, COC.sub.6 H.sub.5, CN or NO.sub.2 ;(b) COORa wherein Ra is hydrogen, or optionally substituted C.sub.1 -C.sub.6 straight or branched alkyl;R.sub.2 is optionally substituted phenyl; pentafluorophenyl; .alpha.- or .beta.-naphthyl; a five- or six-membered heterocyclic ring; .alpha.-benzo[2,3-b]-1,4-dioxan-.alpha.-yl; or .alpha.-benzofuroxanyl;R.sub.3 is COORa;P is hydrogen, --(CH.sub.2).sub.p --W, or C.sub.1 -C.sub.8 linear or branched alkyl;N--P.sub.1 is the residue of a primary or secondary amino group wherein P.sub.1 is hydrogen, C.sub.1 -C.sub.6 lower linear or branched alkyl group, or --(CH.sub.2).sub.p --W; and P, taken together with P.sub.1 and the nitrogen atom to which P.sub.1 is linked, may form a pyrrolidine or a piperidine ring; W is hydroxymethyl, formyloxymethyl, CO.sub.2 R wherein R is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: December 21, 1990Date of Patent: September 10, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Sergio Tognella
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Patent number: 5021404Abstract: Angiostatic compounds are potentiated by collagen matrix metabolism modulators including:a) proline analogs which inhibit proline hydroxylation when substituted for proline in collagen;b) inhibitors of proline hydroxylase;c) inhibitors of collagen cross-linking; andd) all trans-retinoic acid.In methods and therapeutic compositions for inhibiting angiogenesis in a mammal, the collagen matrix modulator is administered with an angiostatic steroid or with heparin (including angiostatic heparin fragments of six or more sugar units, and synthetic fragments).Type: GrantFiled: April 20, 1988Date of Patent: June 4, 1991Assignee: The Children's Medical Center CorporationInventors: Judah Folkman, Donald Ingber
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Patent number: 5013736Abstract: An azaazulene derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond or double bond; when the bond C N is single bond, R.sup.2 is 5-tetrazolyl group, R.sup.3 is taken together with carbon atom to form carbonyl group at the 2-position, and R.sup.4 is hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, a lower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl group having a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, a diphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring with the general formula: ##STR2## in which W is single bond or carbonyl group, oxygen atom, sulfur atom or --CH.dbd.CH--, n is an integer of 1 to 6, and R.sup.1', R.sup.2' and R.sup.Type: GrantFiled: December 26, 1989Date of Patent: May 7, 1991Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Michiko Nagahara, Chikara Ieda, Mitsuo Mimura, Katsuhiro Uchida, Soichiro Sato, Makoto Okumura
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Patent number: 5008275Abstract: Fungicidal pyridyl-substituted acrylic esters of the formula ##STR1## in which R.sup.1 represents alkyl or represents optionally substituted aralkyl,R.sup.2 represents dialkylamino or represents a radical --Z--R.sup.3,X represents oxygen or sulphur or represents a radical ##STR2## Py represents optionally substituted pyridyl, where R.sup.3 represents alkyl or represents optionally substituted aralkyl,R.sup.4 represents hydrogen, alkyl or alkanoyl or represents in each case optionally substituted aralkyl or aryl andZ represents oxygen or sulphur, their geometric isomers and isomer mixtures.Type: GrantFiled: February 8, 1990Date of Patent: April 16, 1991Assignee: Bayer AktiengesellschaftInventors: Alexander Klausener, Gerd Kleefeld, Dieter Berg, Stefan Dutzmann, Gerd Hanbler
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Patent number: 5001137Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.Type: GrantFiled: September 14, 1989Date of Patent: March 19, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
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Patent number: 4999362Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an alkoxycarbonyl group, acetyl, benzoyl, cyano, nitro or aminocarbonyl;R.sub.2 is an optionally substituted aryl or hetaryl group;R.sub.3 is an alkoxycarbonyl group;.phi. is a thio residue such as alkylthio, cycloalkylthio, arylthio, heteroarylthio, aminoalkylthio,are described.Compounds I are useful in human therapy as antihypertensive, antiulcer, antithrombotic, antiischaemic agents.Type: GrantFiled: April 4, 1989Date of Patent: March 12, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Sergio Tognella
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Patent number: 4997837Abstract: Certain trans-6-[[(substituted)pyridin-3-yl]-alkyl- and alkenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.Type: GrantFiled: October 6, 1989Date of Patent: March 5, 1991Assignee: Warner-Lambert CompanyInventors: Alexander W. Chucholowski, Mark W. Creswell, Bruce D. Roth, Drago R. Sliskovic
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Patent number: 4963564Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, wherein Z represents the group ##STR2## (wherein Q.sup.1 represents a straight or branched C.sub.1-3 alkylene group), ##STR3## (where Q.sup.2 represents a group R.sup.5 CO--, R.sup.5 NHCO--, R.sup.5 R.sup.6 NSO.sub.2 -- or R.sup.7 SO.sub.2 --, where R.sup.5 and R.sup.6 each represent a hydrogen atom or a C.sub.1-3 alkyl group, and R.sup.7 represents a C.sub.1-3 alkyl group), or ##STR4## X represents a bond, or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain, and Y represents a bond, or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain with the proviso that the sum total of carbon atoms in the chains X and Y is not more than 10;R represents a hydrogen atom or C.sub.1-3 alkyl group;R.sup.1 and R.sup.2 each represent a hydrogen atom or a C.sub.1-3 alkyl group; with the proviso that the sum total of carbon atoms in R.sup.1 and R.sup.Type: GrantFiled: August 10, 1988Date of Patent: October 16, 1990Assignee: Glaxo Group Ltd.Inventors: Ian F. Skidmore, Alan Naylor, Harry Finch, Lawrence H. C. Lunts, Ian B. Campbell
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Patent number: 4957930Abstract: Dihydropyridines having unsaturated side chains are disclosed. The compounds are useful anti-ischemic and antihypertensive agents.Type: GrantFiled: April 20, 1988Date of Patent: September 18, 1990Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross
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Patent number: 4935430Abstract: Platelet activating factor antagonists of formula (I): ##STR1## wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl (C.sub.1 -C.sub.4) alkoxy, fluoro (C.sub.1 -C.sub.4) alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring;R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C.sub.1 -C.sub.4 alkyl) piperazinyl or N-(C.sub.2 -C.sub.4 alkanoyl)-piperazinyl group;orR.sup.2 is H or C.sub.1 -C.sub.4 alkyl and R.sup.1 is CN, C.sub.3 -C.sub.7 cycloalkyl, aryl, heteroaryl or a C.sub.1 -C.sub.4 alkyl group substituted by one or more substituents selected from C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, aryl or heteroaryl;Z is selected from C.sub.1 -C.sub.6 alkoxy, aryl (C.sub.1 -C.sub.Type: GrantFiled: September 29, 1988Date of Patent: June 19, 1990Assignee: Pfizer Inc.Inventors: Kelvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
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Patent number: 4925852Abstract: 3-Demethylmevalonic acid derivatives of the formula I (.delta.-lactone) and II (corresponding dihydroxy carboxylic acid derivative) ##STR1## in which A--B, Z, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the indicated meanings, a process for the preparation of these compounds, their use as medicaments, and pharmaceutical products, are described. In addition, new intermediates for the preparation of the compounds of the formula I and formula II are described.Type: GrantFiled: July 8, 1988Date of Patent: May 15, 1990Assignee: Hoechst AktiengesellschaftInventors: Kurt Kesseler, Gerhard Beck, Wilhelm Bartmann, Ernold Granzer
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Patent number: 4912118Abstract: Compounds in which two or more rings, being a 3-hydroxpypyrid-2-one, 3-hydroypyrid-4-one or 1-hydropyrid-2-one, are linked are of value in the treatment of patients having a toxic concentration of a metal, particularly iron, in the body while the iron complexes of such compounds are of value in the treatment of iron deficienType: GrantFiled: December 22, 1986Date of Patent: March 27, 1990Assignee: National Research Development CorporationInventors: Robert C. Hider, George Kontoghiorghes, Jack Silver, Michael A. Stockham
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Patent number: 4910195Abstract: Dihydropyridine derivatives represented by formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.6, which may be the same or different, each represents an alkyl group, a cycloalkyl group or an alkoxyalkyl group; R.sub.4 and R.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a nitro group, a halogenated alkyl group, an alkylsulfonyl group, a halogenated alkoxy group, an alkylsulfinyl group, an alkyl group, a cycloalkyl group, an alkxoy group, a cyano group, an alkoxycarbonyl group or an alkylthio group (provided that R.sub.4 and R.sub.5 are not hydrogen atoms at the same time); X represents a vinylene group or an azomethine group; A and B are each an alkylene group or an alkenylene group; R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, an aryl group, or a heterocyclic group (provided that R.sub.7 and R.sub.Type: GrantFiled: October 29, 1987Date of Patent: March 20, 1990Assignee: Green Cross CorporationInventors: Atsuyuki Ashimori, Taizo Ono, Yoshihisa Inoue, Chikara Fukaya, Kazumasa Yokoyama
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Patent number: 4900750Abstract: This invention concerns compounds of formula ##STR1## or salts thereof, wherein: Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl, aralkyl, or aryl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A and B independently represent a group of formula --XR.sup.3 whereinX is a group of formula --(CHR.sup.6).sub.p Y(CHR.sup.7).sub.q --whereinY represents --O--, --S--, --NR.sup.8 -- or a direct bond; p and q each represent 0, 1 or 2 providing that p and q do not both represent O when Y is a direct bond; and R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or alkyl; and R.sup.Type: GrantFiled: August 3, 1987Date of Patent: February 13, 1990Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 4900749Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.Type: GrantFiled: March 10, 1986Date of Patent: February 13, 1990Assignee: Shionogi & Co., Ltd.Inventors: Saichi Matsumoto, Masami Doteuchi, Takuji Mizui, Kentaro Hirai
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Patent number: 4886819Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, A, B are defined as in the specification and nontoxic acid-addition salts thereof, have an excellent calcium blocking action (Ca-antagonist), and antihypertensive action, a platelet aggregation-inhibiting action, a phosphodiesterase-inhibiting action and the like, and thus are useful as a medicine, such as a coronary vasocilator, a cerebral hyperkinemic, antihypertensive, thrombosis-preventing or -treating agents, phosphodiesterase-inhibitor or the like. Pharmaceutical compositions and methods of use are also disclosed.Type: GrantFiled: August 20, 1987Date of Patent: December 12, 1989Assignee: The Green Cross CorporationInventors: Atsuyuki Ashimori, Taizo Ono, Yoshihisa Inoue, Chikara Fukaya, Kazumasa Yokoyama
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Patent number: 4868181Abstract: 1,4-Dihydropyridine derivatives which combine both calcium agonist and alpha.sub.1 -antagonist activity are useful in treating congestive heart failure. These derivatives are compounds having the formula: ##STR1## wherein Ar, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined in the specification.Type: GrantFiled: June 30, 1987Date of Patent: September 19, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Alexander L. Johnson, Philip Ma, Petrus B. M. W. M. Timmermans, Ruth R. Wexler
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Patent number: 4851413Abstract: Quinone derivatives represented by the general formula ##STR1## (wherein, R.sup.1 and R.sup.2, the same or different, refer to a hydrogen atom, methyl or methoxymethyl group, or R.sup.1 and R.sup.2 bind together to form --CH.dbd.CH--CH.dbd.CH--; R.sup.3 is a hydrogen atom or methyl group; R.sup.4 is a nitrogen-containing heterocyclic group which may be substituted; R.sup.Type: GrantFiled: January 16, 1987Date of Patent: July 25, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Shinji Terao, Kohei Nishikawa
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Patent number: 4847273Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols R and R.sup.1 to R.sup.6 have the significance given in claim 1, have a pronounced calcium-antagonist activity and can accordingly be used as medicaments, especially in the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.Type: GrantFiled: June 5, 1986Date of Patent: July 11, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jaunin, Henri Ramuz
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Patent number: 4818766Abstract: The invention relates to novel 1,4-dihydropyridine-3-carboxylic acid phenoxyaliphatylphenyleneoxyalkyl esters of the formula ##STR1## in which Ac represents an acyl group, X represents oxy or optionally substituted imino, A represents a divalent aliphatic hydrocarbon radical interrupted by a group --X.sub.1 --Ph--X.sub.2 -- in which at least one of the radicals X.sub.1 and X.sub.2 represents oxy and a radical X.sub.1 or X.sub.2 that is other than oxy represents a direct bond, and Ph represents an optionally substituted phenylene radical, and R represents an optionally substituted phenyl, pyridyl or 1-oxidopyridyl, (1,3-dioxa)indanyl or benzofurazanyl radical, R.sub.1 represents an optionally substituted phenyl or indolyl radical, R.sub.2 represents an aliphatic hydrocarbon radical and R.sub.3 represents an aliphatic radical, cyano or amino, and acid addition salts thereof.Type: GrantFiled: July 20, 1987Date of Patent: April 4, 1989Assignee: Ciba-Geigy CorporationInventors: Franz Ostermayer, Markus Zimmermann
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Patent number: 4806361Abstract: Sustained-release compositions for oral administration comprising medicament-coated nonpareils surrounded by a sustaining coating of at least three admixed polymers afford exceptionally good plasma levels of the medicament.Type: GrantFiled: May 24, 1985Date of Patent: February 21, 1989Assignee: Sterling Drug Inc.Inventors: Paul J. Harrison, John R. Langridge, Christopher J. Potter
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Patent number: 4798840Abstract: Hypotensive long-acting 1,4-dihydropyridines of the formula ##STR1## in which R.sup.1 is phenyl or heterocyclic,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the usual definitions in such compounds,R.sup.6 represents hydrogen or a lower alkyl radical or the trifluoromethyl group,R.sup.7 and R.sup.8 each denote a hydrogen atom or a fluorine atom,n.gtoreq.1 andm.gtoreq.0, and the sum of n and m must be a least 4, andX represents a single bond, an oxygen atom or the group --N(alkyl)--O.sub.2 S--,or pharmacologically acceptable acid addition salts thereof.Type: GrantFiled: December 4, 1986Date of Patent: January 17, 1989Assignee: Bayer AktiengesellschaftInventors: Egbert Wehinger, Horst Meyer, Andreas Knorr, Stanislav Kazda
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Patent number: 4791123Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: January 22, 1987Date of Patent: December 13, 1988Assignee: Schering Akt.Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
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Patent number: 4786641Abstract: Blood-sugar-lowering dihydropyridines of the formula ##STR1## in which R.sup.1 represents phenyl, naphthyl, thienyl, pyridyl, chromenyl or thiochromenyl, it being possible for the radicals mentioned each to carry up to 2 identical or different substituents from the series comprising halogen, alkyl, alkoxy and alkylthio with in each case up to 6 carbon atoms, fluoroalkyl and fluoroalkoxy with in each case up to 3 carbon atoms and 3 fluorine atoms, nitro and cyano,R.sup.2 represents straight-chain, branched or cyclic alkyl which has up to 8 carbon atoms, can be interrupted in the alkyl chain by an oxygen or a sulphur atom and can be substituted by halogen, phenyl, cyano, hydroxyl, amino, alkylamino or dialkylamino with in each case up to 3 carbon atoms per alkyl group or by N-benzylmethylamino,R.sup.Type: GrantFiled: August 20, 1987Date of Patent: November 22, 1988Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Hans-Jurgen Ahr, Walter Puls, Hilmar Bischoff, Dieter Petzinna, Klaus Schlossmann, Joachim Bender