Only Two Ring Oxygens In The Hetero Ring Which Is Not A Polycyclo Ring System (e.g., Dioxolane, Etc.) Patents (Class 514/467)
  • Patent number: 5059623
    Abstract: A substituted cycloalkyl- or heterocyclyl-carboxanilide of the formula (I) ##STR1## in which X stands for an unsubstituted or an alkyl-substituted cycloalkyl or an unsubstituted or an alkyl-substituted heterocyclic,Hal stands for halogen andY.sup.1, Y.sup.2 and Y.sup.3 independently of one another stand for hydrogen, halogen, an unsubstituted or a halogen-substituted alkyl, an unsubstituted or a halogen-substituted alkoxy or an unsubstituted or a halogen-substituted alkylthio. Such substituted cycloalkyl- or heterocyclyl-carboxanilides are useful as fungicides.
    Type: Grant
    Filed: April 5, 1989
    Date of Patent: October 22, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Kruger, Klaus Sasse, Hermann Hagemann, Albrecht Marhold, Wilhelm Brandes
  • Patent number: 5051428
    Abstract: The invention concerns a series of novel 2-amino-monomethoxycyclohexyl amides having analgesic and neuroprotective activity. The compounds bind selectivity to the kappa opioid receptor. Pharmaceutical compositions containing the compounds, methods of using them, and processes for preparing them are also disclosed.
    Type: Grant
    Filed: March 29, 1990
    Date of Patent: September 24, 1991
    Assignee: Warner-Lambert Company
    Inventors: David C. Horwell, David C. Rees
  • Patent number: 5036103
    Abstract: A method of treating or inhibiting cancer cells grown in the pancreas, liver, kiidney, lymph glands, salivery glands, breast, lung and stomach of humans, which comprises administering an effective amount of a sodium salt, potassium salt or calcium salt of 5,6-O-benzylidene-L-ascorbic acid to a human who is suffering from the growth of cancer cells in the body of the patient.
    Type: Grant
    Filed: July 25, 1990
    Date of Patent: July 30, 1991
    Inventor: Matsuyuki Kochi
  • Patent number: 5032610
    Abstract: The use of L-ascorbic acid, or a pharmaceutically acceptable salt thereof, in combination with 5,6-O-benzylidene-L-ascorbic acid, or 5,6-O-benzylidene-L-ascorbic acid deuterated at least at the 1-position of the aldehyde group of the benzylidene moiety, or a pharmaceutically acceptable salt of such acids, results in a synergistically enhanced cytotoxicity on human carcinoma cells.
    Type: Grant
    Filed: November 21, 1988
    Date of Patent: July 16, 1991
    Assignee: Norsk Hydro AS
    Inventors: Bernt Borretzen, Rolf O. Larsen, John M. Dornish, Reidar Oftebro, Erick O. Pettersen
  • Patent number: 5017618
    Abstract: Compounds having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein --X-- is --O--, --CH.sub.2 -- or --; .dbd.Y is .dbd.O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having from 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms; and Ar is the 3-aromatic or heterocyclic residue of a 1-alkylamino-2-propanol having an aromatic or heterocyclic substituent at the 3-position and having .beta.-adrenergic blocking properties; are useful as .beta.-adrenergic blocking agents and are of particular interest in the treatment of glaucoma or for lowering intraocular pressure.
    Type: Grant
    Filed: September 18, 1989
    Date of Patent: May 21, 1991
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 5013734
    Abstract: The esters of phenylalkanoic acid of the formula: ##STR1## wherein R.sup.1 is 4-10 membered, saturated or unsaturated, mono- or bi-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen,(ii) two or three of nitrogen and sulfur in total, or(iii) one or two sulfur;R.sup.2 is hydrogen; orR.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, form 4-7 membered, saturated or unsaturated, mono-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen, or(ii) two or three of nitrogen and oxygen in total,the aforementioned hetero rings, represented by R.sup.1 or formed by R.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, may be substituted by one substituent selected from C1-4 alkyl and C2-5 acyl;R.sup.3 each, independently, is hydrogen or C1-4 alkyl;R.sup.4 is hydrogen, halogen, trihalomethyl, C1-4 alkyl, C1-4 alkoxy, C2-5 acyl, cyano, nitro or nitroxy;R.sup.5 each, independently, is hydrogen, C1-4 alkyl or phenyl; or the two R.sup.
    Type: Grant
    Filed: May 11, 1990
    Date of Patent: May 7, 1991
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Sadahiko Iguchi, Masanori Kawamura, Tsumoru Miyamoto
  • Patent number: 4996231
    Abstract: This invention relates to triyne cyclic carbonates that are useful in the treatment of fungal diseases and hypercholesterolemic conditions.
    Type: Grant
    Filed: August 8, 1989
    Date of Patent: February 26, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, Yuan-Ching P. Chiang, James V. Heck, Michael D. Lewis
  • Patent number: 4988729
    Abstract: Combattting fungi and bacteria with aminomethylheterocyclic compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkenyl, in each case optionally substituted tetrahydronaphthyl, decahydronaphthyl, cycloalkyl or cycloalkenyl, furthermore alkyl which is substituted by cycloalkyl, cycloalkenyl, cycloalkyloxy or cycloalkylthio, where the cyclic radicals may optionally be substituted, furthermore optionally substituted aryl, in addition alkyl which is substituted by aryl, aryloxy, arylthio, arylsulphinyl or arylsulphonyl, or alkenyl which is substituted by aryl, where the aryl radicals may in each case optionally be substituted;R.sup.2 represents hydrogen or methyl,R.sup.
    Type: Grant
    Filed: October 17, 1989
    Date of Patent: January 29, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Joachim Weissmuller, Graham Holmwood, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 4987132
    Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.
    Type: Grant
    Filed: August 16, 1988
    Date of Patent: January 22, 1991
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
  • Patent number: 4985456
    Abstract: (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl 2-(2,6-dichloroanilino)phenylacetate is disclosed as a novel compound possessing strong valuable pharmacological properties accompanied by surprisingly weak side-effects as well as a process for preparing the new compound.
    Type: Grant
    Filed: February 9, 1990
    Date of Patent: January 15, 1991
    Assignees: Mikasa Seiyaku Co., Ltd., Daito Koeki Kabushiki Kaisha
    Inventors: Keisuke Shimizu, Takumi Matsumura, Masato Nakamoto
  • Patent number: 4975444
    Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.
    Type: Grant
    Filed: August 25, 1989
    Date of Patent: December 4, 1990
    Assignee: Pfizer Inc.
    Inventors: John C. Danilewicz, Keith James, Ryszard J. Kobylecki
  • Patent number: 4971981
    Abstract: Novel substituted 1,3-dioxolan and 1,4-dioxan derivatives of formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently of the others represents hydrogen or C.sub.1 -C.sub.4 -alkyl or, if n=1,R.sub.2 and R.sub.4 together represent one of the radicals ##STR2## R.sub.7 represents hydrogen, halogen, methyl, ethyl, C.sub.1 -C.sub.2 -alkyl substituted by 1 to 5 halogen atoms, methoxy, ethoxy or C.sub.1 -C.sub.2 -alkoxy substituted by 1 to 5 halogen atoms;R.sub.8 represents a halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkyl substituted by 1 to 7 halogen atoms, C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -alkoxy substituted by 1 to 7 halogen atoms, or cyano;U represents a grouping --CH.dbd. or --N.dbd.;X represents --O--, --S-- or --N(R.sub.9)--;Y represents --O--, --S--, --S(O)--, --S(O.sub.2)--, --CH.sub.2 --, --CO-- or --N(R.sub.9)--, whereinR.sub.9 represents hydrogen, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: November 20, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Friedrich Karrer
  • Patent number: 4968706
    Abstract: Compounds of formula I ##STR1## wherein Ar is an optionally substituted phenyl ring; B is a single bond, a group --(CH.sub.2 OCH.sub.2).sub.n being n=1 or 2, a 2,4-disubstituted-1,3-dioxolane ring or a 2,4-disubstituted-1,3-thioxolane ring, R is a single bond, an optionally substituted methylene or ethylene group and T is 2-, 3- or 4-pyridyl, an optionally salified or esterified carboxy group or a carboxyamide group. Said compounds are useful in treatment of respiratory diseases.
    Type: Grant
    Filed: August 11, 1988
    Date of Patent: November 6, 1990
    Assignee: Boehringer Mannhein Italia, S.p.A.
    Inventors: Silvano Spinelli, Roberto Di Domenico, Ernesto Menta, Bruno Lumachi, Licia Gallico, Sergio Tognella
  • Patent number: 4962207
    Abstract: The present application discloses novel potassium salts of particular tellurium and selenium compounds which are useful for the stimulation of the production of cytokines.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: October 9, 1990
    Assignee: Bar-Ilan University
    Inventors: Michael Albeck, Benjamin Sredni
  • Patent number: 4960771
    Abstract: Compositions for carrying physiologically active agents through body membranes having the structural formula I: ##STR1## where: R=H, Alkyl group containing from 1-18 carbon atoms, cycloalkyl, aryl, aralkyl, alkoxy, hydroxyalkyl, alkoyloxyalkyl, acyloxyalkyl and alkoxyalkyl;X=O and NR.sub.1, where R.sub.1 is selected from H, alkyl, aralkyl acyl group containing from 1-18 carbon atoms, cycloalkyl, hydroxyalkyl, alkoyloxyalkyl acyloxyalkyl and alkoxyalkyl;Y=O and NR.sub.2, where R.sub.2 is selected from H, alkyl, aralkyl, cycloalkyl, acyl group containing from 1-18 carbon atoms, hydroxyalkyl, alkoyloxyalkyl, acyloxyalkyl and alkoxyalkyl;m=2-4; andn=0-4,are disclosed.
    Type: Grant
    Filed: July 12, 1988
    Date of Patent: October 2, 1990
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4959362
    Abstract: An ascorbic acid derivative of the formula: ##STR1## wherein R.sup.1 is organic residue having molecular weight of from 15 to 700, R.sup.2 is hydrogen or hydroxyl, R.sup.3 is hydrogen, acyl, optionally substituted phosphono or sulfo, and R.sup.3 and hydroxyl or R.sup.2 may form acetal residue or ketal residue, and a salt thereof are provided.The compound [I] and salts thereof have antioxidant activity and excellent prophylactic and improving actions on disorders of circulatory functions, and they are usefule as antioxidant agent for food and as agents of prophylaxis and improvement of circulatory functional disorders.
    Type: Grant
    Filed: September 19, 1988
    Date of Patent: September 25, 1990
    Assignee: Takeda Chemical Industries, Inc.
    Inventors: Shinji Terao, Minoru Hirata
  • Patent number: 4956383
    Abstract: The novel triacetylenic dioxolone antifungal compound of this invention is isolated from the EV-22 complex of this invention which is elaborated by the microorganism Microbispora sp. SCC 1438, ATCC 53620.
    Type: Grant
    Filed: August 25, 1987
    Date of Patent: September 11, 1990
    Assignee: Schering Corporation
    Inventors: Mahesh G. Patel, Ann C. Horan, Joseph A. Marquez, J. Allan Waitz
  • Patent number: 4954520
    Abstract: The present invention relates to compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is alkyl of 5 to 14 carbon atoms, alkenyl of 5 to 14 carbon atoms or alkynyl of 5 to 14 carbon atoms; R.sup.1 is lower alkylene or phenylene; and R.sup.2 is hydrogen, lower alkyl or a pharmaceutically acceptable cation.
    Type: Grant
    Filed: January 19, 1989
    Date of Patent: September 4, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Thomas D. Penning
  • Patent number: 4950669
    Abstract: The growth rate of an animal is stimulated by administering to the animal a growth promoting amount of a compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are each selected from the group consisting of hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms and halogen; X is selected from carbonyl and a ketal group of the formula ##STR2## wherein R.sub.6 and R.sub.7, which can be the same or different, are each selected from hydrogen and alkyl having 1 to 3 carbon atoms; A is a linear or branched alkylene having from 1 to 8 carbon atoms; and R.sub.8 and R.sub.9, which can be the same or different, are each selected from the group consisting of hydrogen, alkyl having 1 to 4 carbon atoms, or 2-hydroxy-alkyl wherein the alkyl group has 2 to 4 carbon atoms, or R.sub.8 and R.sub.
    Type: Grant
    Filed: July 19, 1988
    Date of Patent: August 21, 1990
    Assignee: Cometec s.r.l.
    Inventors: Aldo Garzia, Umberto Bucci
  • Patent number: 4946865
    Abstract: A compound of the formula: ##STR1## wherein X is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group and Y is a hydrogen atom, a halogen atom, a cyano group, a formyl group, an ethylene-dioxymethyl group, a hydroxyl group, a hydroxymethyl group or a group of either one of the formulas: --CH.dbd.N--OR.sup.1, --COOR.sup.2, --CONH--R.sup.2 and --CH(OR.sup.3).sub.2 in which R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group, a C.sub.3 -C.sub.5 alkenyl group, a C.sub.3 -C.sub.5 alkynyl group, a halo(C.sub.3 -C.sub.5)alkynyl group or a C.sub.1 -C.sub.3 alkyl group substituted with a phenyl group or a cyano group, R.sup.2 is a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group, a C.sub.3 -C.sub.5 alkenyl group or a C.sub.3 -C.sub.5 alkynyl group and R.sup.3 is a C.sub.1 -C.sub.
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: August 7, 1990
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junya Takahashi, Shigeko Nakamura
  • Patent number: 4943307
    Abstract: The invention relates to a plant-protective solution containing 2.5 to 40 % by weight of one or more water-insoluble plant-protective ingredient(s) 20 to 71.5 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 10 to 71.5 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 1 to 15 % by weight of commonly used additives such as anionic and/or nonionic surface active agents and macromolecules.The invention also relates to the ready-for-use plant-protective suspension containing 0.2 to 10 % by weight of one or more water-insoluble plant-protective ingredient(s) with a particle size of 0.1 to 50 .mu.m, 0 to 60 % by weight of a fertilizer, 0.2 to 10 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 0.2 to 10 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 0.05 to 2.
    Type: Grant
    Filed: July 15, 1988
    Date of Patent: July 24, 1990
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Tamas Detre, Sandor ngyan, Laszlo Pap, Andras Szego, Zoltan Karadi, Klara Bertus nee Bende, Katalin Marmarosi nee Kellner
  • Patent number: 4940706
    Abstract: The present invention describes novel 2,4-disubstituted 1,3-dioxolanes having the formula I ##STR1## wherein R.sup.1 represents a long chain alkyl group; X is a covalent single bond, a carbonyl group, a carboxyl group, a carbamoyl group or a --O--P(.dbd.O)(O.sup.z)-- group; z is a negative charge (-) when q is zero, or z is an hydrogen atom when q is one; n is an integer from 2 to 10; R.sup.2, R.sup.3 and R.sup.4 are lower alkyl groups, or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents an aromatic cyclic ammonium group or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents a non-aromatic cyclic ammonium group in which two of the groups (R.sup.2, R.sup.3 or R.sup.4) form a non-aromatic ring together with the quaternary nitrogen atom; and A.sup.- is a pharmaceutically acceptable anion. These compounds are in vitro inhibitors of the platelet aggregation induced by the platelet activating factor (PAF) and, thus, useful for the treatment of the diseases in which this substance is involved.
    Type: Grant
    Filed: October 13, 1988
    Date of Patent: July 10, 1990
    Assignee: J. Uriach & Cia, S.A.
    Inventors: Javier Bartroli, Manuel Anquita, Elena Carceller
  • Patent number: 4929739
    Abstract: A novel complex of a class of tellurium and selenium compounds is disclosed, which is based on a complexing agent and the particular compound to be complexed.
    Type: Grant
    Filed: March 24, 1988
    Date of Patent: May 29, 1990
    Assignee: Bar-Ilan University
    Inventors: Benjamin Sredni, Leo Pavliv, Michael Albeck
  • Patent number: 4921844
    Abstract: Novel fungicidal compositions comprising a 25-azasterol composition and a .beta.-ketothiolase inhibitor compound are disclosed.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: May 1, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Janet C. Onishi, Arthur A. Patchett
  • Patent number: 4920109
    Abstract: Method of potentiating antifungal agents with 25-azasterol compound to produce superior antifungal compositions and use of the compositions to control mycotic infections is disclosed.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: April 24, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Janet C. Onishi, Arthur A. Patchett
  • Patent number: 4920106
    Abstract: This invention relates to acetylenic cyclic carbonates that are useful in the treatment of fungal diseases and hypercholesterolemic conditions.
    Type: Grant
    Filed: August 1, 1989
    Date of Patent: April 24, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, Yuan-Ching P. Chiang, James V. Heck, Michael D. Lewis, Shu S. Yang
  • Patent number: 4910220
    Abstract: The present invention relates to pharmaceutical compositions containing thiodioxolane derivatives having an interesting mucolytic activity, and to a process for the preparation of said thiodioxolane derivatives of the general structural formula ##STR1## in which the carbon atom marked with an asterisk indicates a asymmetry center in the molecule,X represents an hydroxy group or --SR" and R" is hydrogen or a suitable acylic radical,R represents hydrogen, a lower alkyl, a lower hydroxy alkyl, or phenyl,R' represents a lower alkyl, a lower hydroxy alkyl, phenyl, --(CH.sub.2).sub.n SR" where n is a whole number between 1 and 3 and R" has the above indicated meaning, with condition that X and R' can never be both type of groups.
    Type: Grant
    Filed: April 20, 1988
    Date of Patent: March 20, 1990
    Assignee: Proter Spa
    Inventor: Piercarlo Braga
  • Patent number: 4898853
    Abstract: This invention relates to acetylenic esters that are useful in the treatment of fungal diseases and hypercholesterolemic conditions.
    Type: Grant
    Filed: August 1, 1989
    Date of Patent: February 6, 1990
    Assignee: Merck & Co. Inc.
    Inventors: James V. Heck, Michael D. Lewis
  • Patent number: 4894391
    Abstract: 5-Cyanoprostacyclins of Formula I ##STR1## wherein A is a --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C-group,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position, D and E together form a direct bond orD is the group ##STR3## a straight-chain, saturated alkylene group of 1-5 carbon atoms, a branched, saturated or a straight-chain, unsaturated alkylene group of 2-5 carbon atoms, any of which can optionally be substituted by fluorine atoms,n is the number 1, 2, or 3,E is oxygen, sulfur, a --C.tbd.C-bond, a direct bond, or a --CR.sub.4 .dbd.CR.sub.5 -group wherein R.sub.4 and R.sub.5 are different and can be a hydrogen atom or an alkyl group of 1-3 carbon atoms,R.sub.2 is an alkyl, cycloalkyl, optionally substituted aryl, or heterocyclic group,R.sub.1 is a free or functionally modified hydroxy group, andR.sub.3 is an acetal residue ##STR4## wherein R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.
    Type: Grant
    Filed: June 25, 1984
    Date of Patent: January 16, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Helmut Dahl, Bernd Raduchel, Helmut Vorbruggen, Olaf Loge
  • Patent number: 4879307
    Abstract: The invention comprises antitumor compounds of the formula: ##STR1## wherein R is an alkyl group of up to 20 carbon atoms.
    Type: Grant
    Filed: August 9, 1988
    Date of Patent: November 7, 1989
    Assignee: Harbor Branch Oceanographic Institution, Inc.
    Inventor: Ashok D. Patil
  • Patent number: 4874780
    Abstract: Deuterated aromatic aldehydes of the formula: ##STR1## where Ar is substituted phenyl, and derivatives thereof represented by the formula: ##STR2## where Ar is substituted or unsubstituted phenyl, and X.sub.1 and X.sub.2 are substituted hetero atoms or together with the carbon to which they are attached from a heterocycle. These compounds are useful as anticancer agents.
    Type: Grant
    Filed: March 11, 1987
    Date of Patent: October 17, 1989
    Assignee: Norsk Hydro a.s.
    Inventors: Bernt Borretzen, Rolf O. Larsen, Erik O. Pettersen, John M. Dornish, Rolf Oftebro
  • Patent number: 4861764
    Abstract: Novel 1,3-dioxolanes (1,3-dioxyacyclopentanes) are provided along with new 1,3-dioxolanes (1,3-dioxacyclopentanes) compositions which are useful in enhancing the absorption of therapeutic agents through the skin of humans and animals. The method for enhancing skin penetration of therapeutic agents using 1,3-dioxacycloalkanes is also described.The preferred compounds are 1,3-dioxolanes (1,3-dioxacyclopentanes) and 1,3-dioxanes (1,3-dioxacyclohexanes). The preferred compounds have the formula: ##STR1## wherein R, R.sub.0, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently selected from hydrogen and C.sub.1 to C.sub.18 aliphatic groups, preferably alkyl, alkenyl, and the halo, hydroxy, carboxy, carboxamide and carboalkoxy substituted forms thereof, with at least one of said R's an alkyl or alkenyl group of C.sub.4 to C.sub.
    Type: Grant
    Filed: November 17, 1986
    Date of Patent: August 29, 1989
    Assignee: Macro Chem. Corp.
    Inventors: Carlos M. Samour, Stefanos Daskalakis
  • Patent number: 4855318
    Abstract: Iodopropargyl ethers of the formula ##STR1## wherein A represents oxygen or a methylene group,R.sup.1 denotes hydrogen or lower alkyl,R.sup.2 and R.sup.3 are identical or different and represent hydrogen, lower alkyl, alkenyl or unsubstituted or halogen-substituted phenyl, or R.sup.2 and R.sup.3 together form a carbocyclic ring with 4 to 7 C atoms,l and m represent 0, 1 or 2,k denotes 0 or 1 andn denotes an integer from 0 to 4, with the proviso that if l is 0, n represents 1, 2, 3 or 4,can be prepared by reaction of the corresponding propargyl ethers with iodinating agents. The iodopropargyl ethers are active compounds in microbicidal agents.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: August 8, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerold Schade, Wilfried Paulus, Hans-Georg Schmitt
  • Patent number: 4847286
    Abstract: Cromoglycic acid derivatives of the general formula ##STR1## wherein R.sup.1 is an .alpha.-, .beta.- or .gamma.-amino acid residue (for ester bonding) whose amino group may optionally be substituted by at least one lower alkyl group, and R.sup.2 and R.sup.3 each independently is a lower alkyloxy-substituted or an unsubstituted lower alkyl group, an 1-alkanoyloxyalkyl group, an 1-alkoxycarbonyloxyalkyl group, a phthalidyl group or a 5-methyl-1,3-dioxol-2-on-4-ylmethyl group; nontoxic salts thereof; and pharmaceutical compositions containing such compounds. Since the compounds have antiallergic activity and are readily absorbable into the blood stream, they are useful as oral antiallergic agents.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: July 11, 1989
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Satoshi Tamaki, Masaru Kitagawa, Hirokazu Tsuda, Susumu Nishizawa, Nobuhara Kakeya, Kazuhiko Kitao
  • Patent number: 4845119
    Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.tbd.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent of each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substitutent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkyl;wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --; andwherein R.sup.9 is alkyl or up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.
    Type: Grant
    Filed: February 18, 1986
    Date of Patent: July 4, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: Leslie R. Hughes, Howard Tucker
  • Patent number: 4826873
    Abstract: Compounds of the general formula ##STR1## wherein R.sub.1 represents hydrogen, an acyl group having 1 to 18 carbon atoms or both R.sub.1 together the group ##STR2## R.sub.2 represents hydrogen or a methyl group, have been isolated in small amounts from the leaves of Clausena lansium. The new compounds are to be used for the production of compositions for the use of the treatment of acute and chronical viral hepatitis, liver intoxication, hypoxia or amnesia.
    Type: Grant
    Filed: January 15, 1987
    Date of Patent: May 2, 1989
    Assignees: Chinese Academy of Medical Sciences, Bayer Aktiengesellschaft
    Inventors: Ming-he Yang, Yan-rong Chen, Geng-tao Liu, Liang Huang
  • Patent number: 4816473
    Abstract: Novel aroyl-substituted benzofuran and benzothiophene acetic and propionic acids are disclosed herein. These compounds are useful as analgesic, anti-inflammatory, and antipyretic agents.
    Type: Grant
    Filed: September 22, 1986
    Date of Patent: March 28, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: James P. Dunn
  • Patent number: 4806566
    Abstract: The invention relates to the tri-yne carbonate of formula I which has activity against gram positive bacteria. Such compound can be produced by isolating it from the fermentation broth of ATCC-53614, ATCC-53615 or ATCC-53616.
    Type: Grant
    Filed: May 26, 1987
    Date of Patent: February 21, 1989
    Assignee: Merck & Co., Inc.
    Inventor: Sheldon B. Zimmerman
  • Patent number: 4806565
    Abstract: The invention relates to a novel tri-yne carbonate of formula I. Such compound can be produced by isolating it from the fermentation broth of ATCC-53614, ATCC-53615 OR ATCC-53616. The tri-yne carbonate has antifungal activity.
    Type: Grant
    Filed: May 26, 1987
    Date of Patent: February 21, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Otto D. Hensens, August J. Kempf, Robert E. Schwartz, Ruth S. Sykes, Carol F. Wichmann, Kenneth E. Wilson, Sheldon B. Zimmerman, Deborah L. Zink
  • Patent number: 4788190
    Abstract: Novel 1,3-dioxolane compounds useful as antifungal and antiallergy agents and represented by the formula ##STR1## wherein Ar is thienyl, pyridyl, biphenyl, phenyl or phenyl substituted by one or more of halo, nitro, cyano, lower alkyl, lower alkoxy or perhalo(lower)alkyl; Y is CH or N;Q is ##STR2## W is --NR.sub.5 --, --O--, --S(O).sub.n --; X is NO.sub.2, NR.sub.6 R.sub.7 or COR.sub.8 ;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl or (C.sub.2 -C.sub.6) alkanoyl; R.sub.6 and R.sub.7 are independently hydrogen, lower alkyl, phenyl or phenyl substituted by one or more of halo, perhalo loweralkyl, (C.sub.2 -C.sub.6)alkanoyl lower alkyl, lower alkoxy or 2-loweralkyl-3-oxo-1,2,4-trirazol-4-yl or R.sub.6 and R.sub.7 taken together with the nitrogen atom in NR.sub.6 R.sub.7 form substituted or unsubstituted heterocyclyl, said heterocyclyl substituents being (C.sub.2 -C.sub.
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: November 29, 1988
    Assignee: Schering Corporation
    Inventors: Anil K. Saksena, Alan B. Cooper, Henry Guzik, Viyoor M. Girijavallabhan, Ashit K. Ganguly
  • Patent number: 4780311
    Abstract: The compounds of the following general structural formula (I) ##STR1## wherein R is hydrogen or a pharmaceutically acceptable salt thereof, are .beta.-ketoacyl-coenzyme A thiolase inhibitors and are useful as antihypercholesterolemic agents for the treatment of disease in which the inhibition of cholesterol biosynthesis would be useful, such as arteriosclerosis, hyperlipidemia and familial hypercholesterolemia.
    Type: Grant
    Filed: May 26, 1987
    Date of Patent: October 25, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Janet Onishi, Michael Greenspan
  • Patent number: 4780479
    Abstract: Derivatives of carbonyl-group containing behavior modifying compounds, in which said carbonyl group has been converted to a photolabile group which regenerates the carbonyl group on exposure to radiation, are of value in various methods for the control of animal, and in particular insect, species.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: October 25, 1988
    Assignee: National Research Development Corporation
    Inventors: John A. Pickett, Ewen D. M. Macaulay
  • Patent number: 4752614
    Abstract: Certain tellurium compounds have been found to have the ability to stimulate the in vivo and in vitro production of cytokines and their receptors. These compounds may be utilized in the treatment of certain tumors, autoimmune diseases, immune diseases and infectious diseases.
    Type: Grant
    Filed: June 3, 1987
    Date of Patent: June 21, 1988
    Assignee: Bar-Ilan University
    Inventors: Michael Albeck, Benjamin Sredni
  • Patent number: 4735959
    Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.
    Type: Grant
    Filed: May 14, 1985
    Date of Patent: April 5, 1988
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
  • Patent number: 4721726
    Abstract: A method for inhibiting the action of enkephalinases in a mammal to thereby elicit an analgesic effect in said mammal is described.Novel compound and compositions useful for accomplishing the method of the invention are also described.
    Type: Grant
    Filed: July 25, 1986
    Date of Patent: January 26, 1988
    Assignee: Schering Corporation
    Inventor: Joel G. Berger
  • Patent number: 4684661
    Abstract: The invention relates to novel homopropargylamines of formula I ##STR1## wherein n is 2 or 3,R.sub.1 is a group of formula IIa, IIb or IIc ##STR2## in which R.sub.6 and R.sub.7 independently are H, halogen, CF.sub.3, lower alkyl or lower alkoxy,s is a number of 3 to 5,X is O, S, OCH.sub.2, SCH.sub.2, CH.sub.2 or NR.sub.8, andR.sub.8 is H or lower alkyl,R.sub.2 is H or lower alkyl, eitherR.sub.3 and R.sub.4, independently, are H or lower alkyl, orR.sub.3 and R.sub.4 together are (CH.sub.2).sub.u, in which u is a number of 3 to 5, andR.sub.5 is H, alkenyl or is a group selected from alkyl, trialkylsilyl, dialkylphenylsilyl, phenyl, phenylalkyl and cycloalkyl, in which alkyl, phenyl and cycloalkyl groups or moieties are unsubstituted or substituted by OH, lower alkyl, lower alkoxy, phenyl or halogen,in free base form or acid addition salt form thereof, their preparation, their chemotherapeutical and agricultural use and to compositions comprising such novel compounds and suitable for such use.
    Type: Grant
    Filed: November 20, 1985
    Date of Patent: August 4, 1987
    Assignee: Sandoz Ltd.
    Inventor: Anton Stuetz
  • Patent number: 4668700
    Abstract: Substituted aminoketals of the formula ##STR1## in which R.sup.1 to R.sup.4 are various organic radicals andR.sup.2 may also be hydrogen,are fungicidally active. Some of the compounds are new.
    Type: Grant
    Filed: July 13, 1984
    Date of Patent: May 26, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kr/a/ mer, Wolf Reiser, Dieter Berg, Wilhelm Brandes, Paul Reinecke
  • Patent number: 4663347
    Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
    Type: Grant
    Filed: April 19, 1985
    Date of Patent: May 5, 1987
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau
  • Patent number: 4657926
    Abstract: Derivatives of carbonyl-group containing behavior modifying compounds, in which said carbonyl group has been converted to a photolabile group which regenerates the carbonyl group on exposure to radiation, are of value in various methods for the control of animal, and in particular insect, species.
    Type: Grant
    Filed: May 14, 1984
    Date of Patent: April 14, 1987
    Assignee: National Research Development Corporation
    Inventors: John A. Pickett, Ewen D. M. Macaulay
  • Patent number: 4654331
    Abstract: The (5-R-2-oxo-1,3-dioxolen-4-yl)methyl moiety: ##STR1## wherein R is loweralkyl of 1-6 carbon atoms, especially methyl or t-butyl; when utilized as an ester on a pharmaceutical having a carboxylic acid functionality, enhances oral absorption of the pharmaceutical. This effect is applicable to a broad range of pharmaceutically active substances, including antibiotics, and antihypertensives as well as other classes of therapeutic agents.
    Type: Grant
    Filed: August 23, 1984
    Date of Patent: March 31, 1987
    Assignee: Merck & Co., Inc.
    Inventor: Burton G. Christensen