The Six-membered Hetero Rings Are Bonded Directly To Each Other Patents (Class 514/334)
  • Patent number: 5616317
    Abstract: 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: Grant
    Filed: June 14, 1995
    Date of Patent: April 1, 1997
    Assignees: Sagami Chemical Research Center, K.multidot.I Chemical Industry Co., Ltd.
    Inventors: Yu Nagase, Takao Aoyagi, Tomoko Akimoto, Kazunori Tanaka, Kouichi Iwabuchi, Yoshihiro Konagai
  • Patent number: 5610169
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: March 11, 1997
    Assignee: The Green Cross Corporation
    Inventors: Toru Iwao, Kenichi Hirai, Nobuo Kondoh, Koichi Yamanouchi, Kazumasa Yokoyama
  • Patent number: 5602110
    Abstract: 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: Grant
    Filed: January 26, 1995
    Date of Patent: February 11, 1997
    Assignee: Case Western Reserve University
    Inventors: Mitchell L. Drumm, Thomas J. Kelley
  • Patent number: 5602257
    Abstract: 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: Grant
    Filed: September 9, 1994
    Date of Patent: February 11, 1997
    Assignee: University of Florida Research Foundation
    Inventors: John A. Zoltewicz, Michael P. Cruskie
  • Patent number: 5585389
    Abstract: 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: Grant
    Filed: April 28, 1995
    Date of Patent: December 17, 1996
    Assignee: American Cyanamid Company
    Inventors: Joseph A. Furch, David G. Kuhn, David A. Hunt
  • Patent number: 5530001
    Abstract: 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: Grant
    Filed: February 24, 1995
    Date of Patent: June 25, 1996
    Assignee: The Green Cross Corporation
    Inventors: 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
  • Patent number: 5516785
    Abstract: Method of using anabaseine, and DMAB-anabaseine for stimulating brain cholinergic transmission and a method of making anabaseine.
    Type: Grant
    Filed: October 21, 1993
    Date of Patent: May 14, 1996
    Assignee: University of Florida Research Foundation, Incorporated
    Inventors: John A. Zoltewicz, William R. Kem, Edwin M. Meyer
  • Patent number: 5462951
    Abstract: 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: Grant
    Filed: September 3, 1993
    Date of Patent: October 31, 1995
    Assignee: The Green Cross Corporation
    Inventors: Toru Iwao, Kenichi Hirai, Nobuo Kondoh, Koichi Yamanouchi, Kazumasa Yokoyama
  • Patent number: 5446014
    Abstract: 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: Grant
    Filed: July 26, 1991
    Date of Patent: August 29, 1995
    Assignee: Rhone-Poulenc Chimie
    Inventors: Jean-Luc Schuppiser, Magali Knipper
  • Patent number: 5424323
    Abstract: 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: Grant
    Filed: March 23, 1994
    Date of Patent: June 13, 1995
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5424301
    Abstract: 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: Grant
    Filed: February 1, 1993
    Date of Patent: June 13, 1995
    Assignee: Warner-Lambert Company
    Inventors: Hua-Pin Huang, Scott C. Wootton, Thomas N. Julian, Galen W. Radebaugh, Mahdi B. Fawzi
  • Patent number: 5407949
    Abstract: 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: Grant
    Filed: March 23, 1994
    Date of Patent: April 18, 1995
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5354761
    Abstract: 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: Grant
    Filed: June 1, 1993
    Date of Patent: October 11, 1994
    Assignee: Ciba-Geigy Corp.
    Inventors: Jaroslav Stanek, Giorgio Caravatti, Hans-Georg Capraro, Jorg Frei
  • Patent number: 5346899
    Abstract: Substituted pyridine compounds of formula I ##STR1## and plant-tolerated acid addition salts and metal salt complexes thereof, and fungicides containing these compounds.
    Type: Grant
    Filed: September 1, 1993
    Date of Patent: September 13, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Mueller, Karl Eicken, Albrecht Harreus, Hartmann Koenig, Costin Rentzea, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5344838
    Abstract: 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: Grant
    Filed: December 8, 1993
    Date of Patent: September 6, 1994
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5338737
    Abstract: 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: Grant
    Filed: February 12, 1993
    Date of Patent: August 16, 1994
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Catherine R. Kostlan
  • Patent number: 5338748
    Abstract: 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: Grant
    Filed: December 9, 1993
    Date of Patent: August 16, 1994
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5300526
    Abstract: 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: Grant
    Filed: November 20, 1991
    Date of Patent: April 5, 1994
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Constantin A. Rebeiz, John A. Juvik, Carole C. Rebeiz
  • Patent number: 5260323
    Abstract: 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: Grant
    Filed: November 19, 1992
    Date of Patent: November 9, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall
  • Patent number: 5204357
    Abstract: 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: Grant
    Filed: February 14, 1989
    Date of Patent: April 20, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
  • Patent number: 5200427
    Abstract: 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: Grant
    Filed: January 9, 1989
    Date of Patent: April 6, 1993
    Assignee: The Board of Trustees of the Univ. of Illinois
    Inventors: Constantin A. Rebeiz, John A. Juvik, Carole C. Rebeiz
  • Patent number: 5120734
    Abstract: 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: Grant
    Filed: November 13, 1990
    Date of Patent: June 9, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alexander Klausener, Gerd Kleefeld, Dieter Berg, Stefan Dutzmann, Gerd Hanssler
  • Patent number: 5120747
    Abstract: 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: Grant
    Filed: May 1, 1990
    Date of Patent: June 9, 1992
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Michael Fray, Kenneth Richardson, John Steele
  • Patent number: 5120748
    Abstract: 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: Grant
    Filed: June 28, 1991
    Date of Patent: June 9, 1992
    Assignee: Warner-Lambert Company
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Lawrence D. Wise
  • Patent number: 5064842
    Abstract: 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: Grant
    Filed: June 25, 1990
    Date of Patent: November 12, 1991
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, Terence J. Ward, Albert Opalko
  • Patent number: 5055471
    Abstract: 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: Grant
    Filed: November 15, 1989
    Date of Patent: October 8, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: Paul J. de Fraine, Anne Martin
  • Patent number: 5047414
    Abstract: 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: Grant
    Filed: December 21, 1990
    Date of Patent: September 10, 1991
    Assignee: Boehringer Biochemia Robin S.p.A.
    Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Sergio Tognella
  • Patent number: 5021404
    Abstract: 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: Grant
    Filed: April 20, 1988
    Date of Patent: June 4, 1991
    Assignee: The Children's Medical Center Corporation
    Inventors: Judah Folkman, Donald Ingber
  • Patent number: 5013736
    Abstract: 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: Grant
    Filed: December 26, 1989
    Date of Patent: May 7, 1991
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Michiko Nagahara, Chikara Ieda, Mitsuo Mimura, Katsuhiro Uchida, Soichiro Sato, Makoto Okumura
  • Patent number: 5008275
    Abstract: 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: Grant
    Filed: February 8, 1990
    Date of Patent: April 16, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alexander Klausener, Gerd Kleefeld, Dieter Berg, Stefan Dutzmann, Gerd Hanbler
  • Patent number: 5001137
    Abstract: 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: Grant
    Filed: September 14, 1989
    Date of Patent: March 19, 1991
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
  • Patent number: 4999362
    Abstract: 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: Grant
    Filed: April 4, 1989
    Date of Patent: March 12, 1991
    Assignee: Boehringer Biochemia Robin S.p.A.
    Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Sergio Tognella
  • Patent number: 4997837
    Abstract: 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: Grant
    Filed: October 6, 1989
    Date of Patent: March 5, 1991
    Assignee: Warner-Lambert Company
    Inventors: Alexander W. Chucholowski, Mark W. Creswell, Bruce D. Roth, Drago R. Sliskovic
  • Patent number: 4963564
    Abstract: 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: Grant
    Filed: August 10, 1988
    Date of Patent: October 16, 1990
    Assignee: Glaxo Group Ltd.
    Inventors: Ian F. Skidmore, Alan Naylor, Harry Finch, Lawrence H. C. Lunts, Ian B. Campbell
  • Patent number: 4957930
    Abstract: Dihydropyridines having unsaturated side chains are disclosed. The compounds are useful anti-ischemic and antihypertensive agents.
    Type: Grant
    Filed: April 20, 1988
    Date of Patent: September 18, 1990
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross
  • Patent number: 4935430
    Abstract: 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: Grant
    Filed: September 29, 1988
    Date of Patent: June 19, 1990
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
  • Patent number: 4925852
    Abstract: 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: Grant
    Filed: July 8, 1988
    Date of Patent: May 15, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Kurt Kesseler, Gerhard Beck, Wilhelm Bartmann, Ernold Granzer
  • Patent number: 4912118
    Abstract: 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 deficien
    Type: Grant
    Filed: December 22, 1986
    Date of Patent: March 27, 1990
    Assignee: National Research Development Corporation
    Inventors: Robert C. Hider, George Kontoghiorghes, Jack Silver, Michael A. Stockham
  • Patent number: 4910195
    Abstract: 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: Grant
    Filed: October 29, 1987
    Date of Patent: March 20, 1990
    Assignee: Green Cross Corporation
    Inventors: Atsuyuki Ashimori, Taizo Ono, Yoshihisa Inoue, Chikara Fukaya, Kazumasa Yokoyama
  • Patent number: 4900750
    Abstract: 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: Grant
    Filed: August 3, 1987
    Date of Patent: February 13, 1990
    Assignee: John Wyeth & Brother, Limited
    Inventors: John L. Archibald, Terence J. Ward, Albert Opalko
  • Patent number: 4900749
    Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: February 13, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventors: Saichi Matsumoto, Masami Doteuchi, Takuji Mizui, Kentaro Hirai
  • Patent number: 4886819
    Abstract: 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: Grant
    Filed: August 20, 1987
    Date of Patent: December 12, 1989
    Assignee: The Green Cross Corporation
    Inventors: Atsuyuki Ashimori, Taizo Ono, Yoshihisa Inoue, Chikara Fukaya, Kazumasa Yokoyama
  • Patent number: 4868181
    Abstract: 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: Grant
    Filed: June 30, 1987
    Date of Patent: September 19, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Alexander L. Johnson, Philip Ma, Petrus B. M. W. M. Timmermans, Ruth R. Wexler
  • Patent number: 4851413
    Abstract: 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: Grant
    Filed: January 16, 1987
    Date of Patent: July 25, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shinji Terao, Kohei Nishikawa
  • Patent number: 4847273
    Abstract: 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: Grant
    Filed: June 5, 1986
    Date of Patent: July 11, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jaunin, Henri Ramuz
  • Patent number: 4818766
    Abstract: 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: Grant
    Filed: July 20, 1987
    Date of Patent: April 4, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Franz Ostermayer, Markus Zimmermann
  • Patent number: 4806361
    Abstract: 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: Grant
    Filed: May 24, 1985
    Date of Patent: February 21, 1989
    Assignee: Sterling Drug Inc.
    Inventors: Paul J. Harrison, John R. Langridge, Christopher J. Potter
  • Patent number: 4798840
    Abstract: 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: Grant
    Filed: December 4, 1986
    Date of Patent: January 17, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Egbert Wehinger, Horst Meyer, Andreas Knorr, Stanislav Kazda
  • Patent number: 4791123
    Abstract: 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: Grant
    Filed: January 22, 1987
    Date of Patent: December 13, 1988
    Assignee: Schering Akt.
    Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
  • Patent number: 4786641
    Abstract: 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: Grant
    Filed: August 20, 1987
    Date of Patent: November 22, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Hans-Jurgen Ahr, Walter Puls, Hilmar Bischoff, Dieter Petzinna, Klaus Schlossmann, Joachim Bender