Z Contains A Cyclopentyl Or Cyclopentene Ring Patents (Class 514/530)
  • Patent number: 5516796
    Abstract: Thiosubstituted prostaglandin derivatives and related compounds having the general structure ##STR1## useful as intraocular pressure reducing agents; pharmaceutical compositions containing such compounds; and methods of treatment using such compositions are disclosed.
    Type: Grant
    Filed: March 24, 1994
    Date of Patent: May 14, 1996
    Assignee: Kabi Pharmacia AB
    Inventors: Johan W. Stjernschantz, Bahram Resul, Laszlo Z. Bito
  • Patent number: 5514712
    Abstract: The present invention relates to the use of oils of chaulmoogra and derivatives thereof, particularly in the form of esters or salts, for preparing a cosmetic or pharmaceutical, particularly dermatological composition, intended for harmonizing the pigmentation of the skin. It concerns in particular a process for harmonizing tanning.
    Type: Grant
    Filed: June 14, 1994
    Date of Patent: May 7, 1996
    Assignee: Shiseido International France
    Inventor: Jacques LeClere
  • Patent number: 5510384
    Abstract: A method of treating damaged human tissues, especially mucosal and epithelial tissues, comprising topically administering to the damaged tissues a composition having an effective amount of misoprostol. The treatment is particularly effective against periodontal disease and oral ulcers caused by radiation therapy and chemotherapy.
    Type: Grant
    Filed: May 5, 1994
    Date of Patent: April 23, 1996
    Inventors: Rex N. McKee, Frank A. Wingrove
  • Patent number: 5510382
    Abstract: The invention is related to the field of treating gastric and duodenal disorders and more specifically to the use of certain 13,14-dihydro-prostaglandin E derivatives, especially of PGE.sub.2, which are modified to contain a ring structure in the omega chain. The invention relates also to pharmaceutical compositions containing an active amount of these derivatives.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: April 23, 1996
    Assignee: Pharmacia AB
    Inventors: Johan Stjernschantz, Bahram Resul
  • Patent number: 5510383
    Abstract: Disclosed is the use of cloprostenol, fluprostenol, and their pharmaceutically acceptable salts and esters for the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic compositions comprising said compounds.
    Type: Grant
    Filed: August 3, 1993
    Date of Patent: April 23, 1996
    Assignee: Alcon Laboratories, Inc.
    Inventors: John E. Bishop, Louis DeSantis, Jr., Verney L. Sallee
  • Patent number: 5510381
    Abstract: The present invention is a novel therapeutic use of gabapentin, its derivatives, and the pharmaceutical salts thereof. The compounds are useful in the treatment of mania in all its various forms whether acute or chronic, single or recurrent, and whether or not it is associated with depression. The invention further includes the treatment of bipolar disorder.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: April 23, 1996
    Assignee: Warner-Lambert Company
    Inventor: Atul C. Pande
  • Patent number: 5504111
    Abstract: This invention relates to methods for treating Adult Respiratory Distress Syndrome (ARDS) which involves the administration of 2,3-alkylcarbonyloxybenzoic acid and salts thereof wherein the alkyl group has 2-18 carbon atoms.
    Type: Grant
    Filed: December 30, 1994
    Date of Patent: April 2, 1996
    Assignee: Medichem Research, Inc.
    Inventors: Michael T. Flavin, Deanna J. Nelson, Julian F. Borgia, deceased, Gary Jesmok
  • Patent number: 5486540
    Abstract: The present invention provides therapeutic agents comprising cyclopentane heptane or heptenoic acid, 2 arylalkyl or arylalkenyl and derivatives thereof, wherein the carboxylic acid of the parent compound is converted to a hydroxyl or ester group. These therapeutic agents are potent ocular hypotensives as well as having other therapeutic uses.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: January 23, 1996
    Assignee: Allergan, Inc.
    Inventor: Steven W. Andrews
  • Patent number: 5480900
    Abstract: Combinations of at least one clonidine derivative and at least one prostaglandin are used to treat glaucoma and ocular hypertension without some of the side effects typically associated with topical administration of prostaglandins.
    Type: Grant
    Filed: April 10, 1995
    Date of Patent: January 2, 1996
    Assignee: Alcon Laboratories, Inc.
    Inventors: Louis DeSantis, Jr., Verney L. Sallee
  • Patent number: 5476872
    Abstract: Compounds of the formula ##STR1## where the hatched lines indicate alpha (.alpha.) configuration, a solid triangle is used to indicate beta (.beta.) configuration, lines on both sides of a double bond indicate cis (Z) configuration, and lines on opposite sides of the double bond indicate trans (E) configuration; R.sub.1 is alkyl of 1-10 carbons, C.sub.1 -C.sub.10 alkylphenyl, phenyl-C.sub.1 -C.sub.10 alkyl, or alkenyl of 2 to 10 carbons and having 1 to 3 double bonds; R.sub.2 is Z--OR.sub.3, Z--OCOR.sub.3, Z--OCONHR.sub.3, Z--OCOOR.sub.3, Z--NR.sub.4 R.sub.5, Z--NR.sub.4 COR.sub.3, Z--NR.sub.4 SO.sub.2 R.sub.3, Z--COOR.sub.3, Z--CONR.sub.4 R.sub.5, Z--CHO; Z is (CH.sub.2).sub.n where n is 1-6, or Z is an alkenyl group having 2 to 6 carbons and 1 or 2 double bonds, R.sub.3 is H, alkyl of 1-6 carbons, alkenyl of 2 to 6 carbons or phenyl, R.sub.4 and R.sub.5 independently are H or alkyl of 1 to 6 carbons, have ocular hypotensive activity.
    Type: Grant
    Filed: October 18, 1993
    Date of Patent: December 19, 1995
    Assignee: Allergan, Inc.
    Inventors: Michael E. Garst, Elizabeth T. Syage, Michael B. Roof, David F. Woodward, Ming Fai Chan
  • Patent number: 5472970
    Abstract: Allylaminoesters of the formula (I): ##STR1## in which: R.sub.1 is H or low-molecular-weight alkyl,R.sub.2 is low-molecular-weight alkyl, cycloalkyl, or low-molecular-weight phenylcycloalkyl, pyridyl or phenyl, low-molecular-weight phenylalkyl, low-molecular-weight diphenylalkyl, low-molecular-weight phenylalkenyl, in which the phenyl cycle may be mono-, di- or trisubstituted by chlorine atoms, low-molecular-weight alkyl radicals, low-molecular-weight alkoxy, or trifluoromethyl, acetamide or acetyloxy radicals, their racemic forms, their (S) enantiomers and their addition salts. Also, antiallergic drugs containing the same.
    Type: Grant
    Filed: September 19, 1994
    Date of Patent: December 5, 1995
    Assignee: Institut de Recherche Jouveinal S.A.
    Inventors: Alain P. Calvet, Agnes G. Grouhel, Jean-Louis Junien
  • Patent number: 5468778
    Abstract: Intraocular pressure is lowered in the eye of a mammal by administration of a pharmaceutical composition containing as active ingredient a compound of the formula ##STR1## where the dotted line represents a bond or the absence of a bond, wavy lines connected to the olefinic bond represent cis or trans configuration about the olefinic bond; R.sub.1 represents H, or CO-R.sub.3 where R.sub.3 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group; R.sub.2 represents H or lower alkyl of 1 to 6 carbons, and n is an integer between 0 and 8.
    Type: Grant
    Filed: September 24, 1992
    Date of Patent: November 21, 1995
    Assignee: Allergan, Inc.
    Inventors: Michael E. Garst, Robert M. Burk, Ming F. Chan, Michael B. Roof
  • Patent number: 5464868
    Abstract: The invention describes prostaglandin E1 derivatives as pharmacologically active agents, and pharmaceutical compositions containing these compounds, especially for transcutaneous administration.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: November 7, 1995
    Inventors: Jurgen C. Frolich, Herbert Bippi
  • Patent number: 5462968
    Abstract: The invention relates to (.+-.) trans-2-[-4(1-hydroxyhexyl) phenyl]-5-oxocyclopentaneheptanoic acid, and ester and unsaturated derivatives thereof, prostaglandin derivatives. More particularly, the present invention concerns compounds of the formula I ##STR1## wherein the wavy bonds indicate that .alpha. or .beta. configuration, the dashed bond represents either a single or double bond, which double bond may be a cis or trans double bond and R is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.1 wherein m is 0-10, and R.sub.1 is an aliphatic ring having from about 3 to about 7 carbon atoms, or an aryl or heteroaryl ring having from about 4 to about 10 carbon atoms and wherein the heteroatom is selected from the group consisting of N, O and S. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
    Type: Grant
    Filed: January 19, 1994
    Date of Patent: October 31, 1995
    Assignee: Allergan, Inc.
    Inventor: David F. Woodward
  • Patent number: 5457131
    Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.
    Type: Grant
    Filed: August 18, 1994
    Date of Patent: October 10, 1995
    Assignee: Allergan, Inc.
    Inventor: Steven W. Andrews
  • Patent number: 5455273
    Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: October 3, 1995
    Assignee: Karl Thomae GmbH
    Inventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
  • Patent number: 5451607
    Abstract: There are disclosed hydrazone derivatives of the general formula [I]: ##STR1## wherein R.sup.1 is halogen, etc.; R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.5 is C.sub.1 -C.sub.6 alkyl, etc.; R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; A is (CH.sub.2).sub.t, O, S(O).sub.n, etc.; a is an integer of 1 to 4; n is an integer of 0 to 2; and t is an integer of 1 to 3; as well as production processes therefor, insecticides and/or acaricides containing the same as an active ingredient and intermediate compounds thereof.
    Type: Grant
    Filed: April 19, 1993
    Date of Patent: September 19, 1995
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Toshiaki Taki, Hirosi Kisida, Shigeru Saito, Shinji Isayama
  • Patent number: 5449691
    Abstract: A method for inducing the production of interleukin 2 in a warm blooded animal by administering an effective amount of a compound of the formula (I) ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.
    Type: Grant
    Filed: June 24, 1993
    Date of Patent: September 12, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: William N. Washburn, Lee H. Latimer, Barbara B. Lussier, Carl R. Illig, Alexander L. Weis
  • Patent number: 5446041
    Abstract: Disclosed is an intraocular pressure reducing method and composition wherein 11-acyl prostaglandins are contained in a pharmaceutically acceptable excipient for topical application to the surface of the eye.
    Type: Grant
    Filed: October 10, 1990
    Date of Patent: August 29, 1995
    Assignee: Allergan, Inc.
    Inventors: Ming F. Chan, David F. Woodward
  • Patent number: 5434180
    Abstract: The present invention relates to new polycyclic aromatic derivatives, to processes for their preparation and to their use in therapeutic and cosmetic formulations.
    Type: Grant
    Filed: March 27, 1992
    Date of Patent: July 18, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (CIRD Galderma)
    Inventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 5432174
    Abstract: A method for the treatment of ocular hypertension which comprises administering, to a subject in need of such treatment,(a) a .beta.-adrenergic blocker at the enhancement phase of aqueous humor production, and(b) a prostanoic acid compound at the suppression phase of aqueous humor production, andin an amount effective in treatment of ocular hypertension.
    Type: Grant
    Filed: December 7, 1993
    Date of Patent: July 11, 1995
    Assignee: R-Tech Ueno, Ltd.
    Inventors: Ryuji Ueno, Sachiko Kuno
  • Patent number: 5428062
    Abstract: The novel 13,14-dihydro-15-keto prostaglandins E of the invention have remarkable preventive effects against ulcers. Further, the novel 13,14-dihydro-15-keto-prostaglandins E of the invention have an advatage that they have none of side effects which prostaglandin E intrinsically has, or can remarakably reduce such effects of the prostaglandin E.Therefore, the novel 13,14-dihydro-15-keto prostaglandins E of the invention are effective for animal and human use for treatment and prevention of ulcers, such as duodenal ulcer and gastric ulcer.
    Type: Grant
    Filed: April 28, 1993
    Date of Patent: June 27, 1995
    Assignee: K.K. Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuzo Ueno, Ryuji Ueno, Ichie Kato, Tomio Oda
  • Patent number: 5426115
    Abstract: A method of treatment for improving encephalic function which comprises administering, to a subject in need of such treatment, a 15-keto-prostaglandin compound in an amount effective for improvement of encephalic function.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: June 20, 1995
    Assignee: Kabushikikaisha Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuji Ueno, Hiroyoshi Osama, Tomio Oda
  • Patent number: 5422369
    Abstract: This invention relates a method for topical treatment of glaucoma or ocular hypertension by administration of an effective intraocular pressure reducing amont of a prostaglandin derivative of PGA, PGB, PGE and PGF, in which the omega chain contains a ring structure. The invention further relates to compositions comprising said prostaglandin derivatives in an ophthalmologically compatible carrier.
    Type: Grant
    Filed: February 25, 1994
    Date of Patent: June 6, 1995
    Assignee: Kabi Pharmacia AB
    Inventors: Johan W. Stjernschantz, Bahram Resul
  • Patent number: 5422368
    Abstract: The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in which the omega chain contains a ring structure, in an ophthalmologically compatible carrier. The invention further relates to the preparation of said compositions and their use for treatment of glaucoma or ocular hypertension.
    Type: Grant
    Filed: December 8, 1992
    Date of Patent: June 6, 1995
    Assignee: Kabi Pharmacia AB
    Inventors: Johan W. Stjernschantz, Bahram Resul
  • Patent number: 5414016
    Abstract: Leukotriene-B.sub.4 derivatives of formula I ##STR1## are described, in which R.sup.1 means CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sup.5, CONR.sup.6 R.sup.7, orR.sup.1 together with R.sup.2 means a carbonyl group,R.sup.4 symbolizes H, C.sub.1 -C.sub.10 alkyl optionally substituted, C.sub.3 -C.sub.10 cycloalkyl, C.sub.6 -C.sub.10 aryl radical optionally substituted, or a 5-6-membered aromatic heterocyclic ring,A symbolizes a trans, trans-CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group,B symbolizes a C.sub.1 -C.sub.10 alkylene group, which optionally can be substituted by fluorine or the group ##STR2## D can mean a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sup.6 or together withB can also mean a direct bond, their salts with physiologically compatible bases and their cyclodextrin clathrates.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: May 9, 1995
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5414014
    Abstract: The present invention provides methods of using compositions containing local anesthetic compounds for facilitating the removal of sucking arthropods from the skin of a mammal; for reducing inflammation associated with a bite of a sucking arthropod; for limiting infection from a sucking arthropod; and for enhancing the facilitated removal of sucking arthropods from the skin of a mammal.
    Type: Grant
    Filed: April 8, 1993
    Date of Patent: May 9, 1995
    Assignee: Innova Biomed, Inc.
    Inventors: Linda H. Schneider, Randall B. Murphy
  • Patent number: 5411987
    Abstract: Combating fungi with substituted amine acid derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, halogenoalkinyl, cycloalkyl or cycloalkenyl,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and represent hydrogen, cycloalkyl or alkyl, orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring, andR.sup.6 represents hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, unsubstituted or substituted phenylalkyl, unsubstituted or substituted phenyl or unsubstituted or substituted cycloalkyl, or represents unsubstituted or substituted heterocyclyl or heterocyclylalkyl,orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a heterocyclyl radical, which can contain further hetero atoms.
    Type: Grant
    Filed: February 25, 1993
    Date of Patent: May 2, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Detlef Wollweber, Thomas Seitz, Wilhelm Brandes
  • Patent number: 5405846
    Abstract: A method for treatment of ocular hypertension which comprises ocularly administering, to a subject in need of such treatment, an ocular-hypertension synergistic combination of(a) a 15-deoxy-prostaglandin compound, and(b) a .beta.-adrenergic blocker in an amount effective in treatment of ocular hypertension.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: April 11, 1995
    Assignee: R-Tech Ueno, Ltd.
    Inventor: Ryuji Ueno
  • Patent number: 5405870
    Abstract: Compounds of formula (Ic): ##STR1## having valuable platelet-aggregation inhibitory activities useful for the prophylaxis and treatment of such diseases as thrombosis and pharmaceutical compositions containing said compounds.
    Type: Grant
    Filed: November 4, 1993
    Date of Patent: April 11, 1995
    Assignee: Sankyo Company, Limited
    Inventors: Kazuo Koyama, Shigeo Amemiya, Koichi Kojima, Shinsaku Kobayashi
  • Patent number: 5399588
    Abstract: The compounds of this invention which have the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, halogen, C.sub.1 -C.sub.8 alkoxy, or trifluoromethyl;R.sup.3 is --OH or --NHCO.sub.2 CH.sub.3 ;X is --CH.sub.2 -- or --OCH.sub.2 --;n is 1 or 2;or a pharmaceutically acceptable salt thereof,are useful in treating or inhibiting the long-term complications of diabetes such as diabetic retinopathy, nephropathy and neuropathy through the inhibition of the enzyme aldose reductase. Aldose reductase inhibitors have been shown to prevent the biochemical, functional and morphological changes induced by hyperglycemia.
    Type: Grant
    Filed: December 14, 1993
    Date of Patent: March 21, 1995
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Patent number: 5393764
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: February 28, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5389619
    Abstract: Compounds of the formula I ##STR1## where n, W, X, Y, Z, R.sup.1, R.sup.2, and R.sup.3 are as defined herein exhibit fungicidal, insecticidal, and acaracidal activity.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: February 14, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5387608
    Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.
    Type: Grant
    Filed: August 17, 1993
    Date of Patent: February 7, 1995
    Assignee: Allergan, Inc.
    Inventor: Steven W. Andrews
  • Patent number: 5387607
    Abstract: O-Benzyloxime ethers of the formula I ##STR1## where X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: February 7, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
  • Patent number: 5385931
    Abstract: The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I ##STR1## in which: R represents a straight-chain or branched lower alkyl radical having 1 to 9 C;a phenyl radical which is unsubstituted or substituted by one or more groups:straight-chain or branched lower alkyl having 1 to 4 C, halogeno, alkoxy, nitro, amino, dialkylamino or CF.sub.3 ;a substituted or unsubstituted naphthalene;a thiophenyl radical;R.sub.1 represents a hydrogen or a straight-chain or branched lower alkyl or a benzyl;R.sub.2 represents a hydrogen, a straight-chain or branched lower alkyl group, a substituted or unsubstituted phenyl group or an aralkyl group;R.sub.3 represents a hydrogen or a straight-chain or branched lower alkyl (1 to 6 C);--X-- represents a divalent functional radical chosen from the following: --CH.sub.2 --; ##STR2## where R.sub.
    Type: Grant
    Filed: December 28, 1990
    Date of Patent: January 31, 1995
    Assignee: Pierre Fabre Medicament
    Inventors: Dennis Bigg, Alain Duflos, Jean-Pierre Rieu
  • Patent number: 5380709
    Abstract: The novel 13, 14-dihydro-15-keto prostaglandins E of the invention have remarkable preventive effects against ulcers. Further, the novel 13,14-dihydro-15-keto prostaglandins E of the invention have an advatage that they have none of side effects which prostaglandin E intrinsically has, or can remarakably reduce such effects of the prostaglandin E. Therefore, the novel 13, 14-dihydro-15-keto prostaglandins E of the invention are effective for animal and human use for treatment and prevention of ulcers, such as duodenal ulcer and gastric ulcer.
    Type: Grant
    Filed: April 28, 1993
    Date of Patent: January 10, 1995
    Assignee: K.K. Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuzo Ueno, Ryuji Ueno, Ichie Kato, Tomio Oda
  • Patent number: 5376683
    Abstract: The invention relates to .DELTA..sup.8 - and .DELTA..sup.9 -prostaglandin derivatives of formula I, ##STR1## in which means the radicals or , R.sup.1 means ##STR2## COOR.sup.4 or CONHR.sup.5, R.sup.2 and R.sup.3 respectively mean a hydrogen atom or a hydroxy group, and the OH group can be respectively in alpha- or beta- position,means a CH.sub.2 group, an O or S atom,W means hydrogen, --OR.sup.6, halogen, --CN--, --NO.sub.2, trifluoromethyl or COOR.sup.6, and if R.sup.4 means hydrogen, their salts with physiologically compatible bases, the alpha-, beta- or gamma- cyclodextrin clathrates, as well as the compounds of formula I encapsulated with liposomes, process for their production and their pharmaceutical use.
    Type: Grant
    Filed: November 25, 1992
    Date of Patent: December 27, 1994
    Assignee: Schering Aktiengesellschaft
    Inventors: Ulrich Klar, Hartmut Rehwinkel, Helmut Vorbruggen, Karl H. Thierauch, Claus S. Sturzebecher
  • Patent number: 5374654
    Abstract: The invention relates to carbacyclin derivatives of Formula I ##STR1## wherein the various substituents are defined herein, including, inter alia,if R.sub.2 is a hydrogen atom, their salts with physiologically compatible bases, their cyclodextrin clathrates, and their use as medicinal agents.
    Type: Grant
    Filed: April 21, 1993
    Date of Patent: December 20, 1994
    Assignee: Schering Aktiengesellschaft
    Inventors: Helmut Vorbruggen, Ulrich Klar, Bob Nieuweboer, Claus-Steffen Sturzebecher
  • Patent number: 5364883
    Abstract: 16(S)-Isocarbacyclins have been found to the useful in the treatment of liver and kidney diseases.
    Type: Grant
    Filed: May 3, 1993
    Date of Patent: November 15, 1994
    Assignee: Teijin Limited
    Inventors: Kiyoshi Bannai, Toshio Tanaka, Yoshinori Kato, Tamotsu Koyama, Satoshi Asano, Akira Ohtsu, Seizi Kurozumi, Makoto Ogawa, Yoshio Mori
  • Patent number: 5362751
    Abstract: The present invention provides a tracheobronchodilator comprising 15-keto-PGEs, reduced in stimuli against bronchi and other side effects.
    Type: Grant
    Filed: June 17, 1993
    Date of Patent: November 8, 1994
    Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuzo Ueno, Ryuji Ueno, Tomio Oda
  • Patent number: 5356931
    Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.
    Type: Grant
    Filed: January 4, 1993
    Date of Patent: October 18, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
  • Patent number: 5356621
    Abstract: A method of attracting flies of the Muscidae or Muscinae families comprising providing in a locus where the flies exist a fly attractant composition which contains as an active ingredient a composition extracted from a bamboo with an extractive solvent such as water or C.sub.1 -C.sub.4 alcohol.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: October 18, 1994
    Assignee: Sankyo Company, Limited
    Inventors: Yuichiro Tabaru, Akio Saito
  • Patent number: 5324746
    Abstract: A method of treating damaged human tissues, especially mucosal and epithelial tissues, comprising topically administering to the damaged tissues a composition having an effective amount of misoprostol. The treatment is particularly effective against periodontal disease.
    Type: Grant
    Filed: February 12, 1993
    Date of Patent: June 28, 1994
    Inventors: Rex N. McKee, Frank A. Wingrove
  • Patent number: 5321128
    Abstract: This invention relates a method for topical treatment of glaucoma or ocular hypertension by administration of an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGE and PGF, in which the omega chain contains a ring structure. The invention further relates to compositions comprising said prostaglandin derivatives in an ophthalmologically compatible carrier.
    Type: Grant
    Filed: December 8, 1992
    Date of Patent: June 14, 1994
    Assignee: Kabi Pharmacia AB
    Inventors: Johan W. Stjernschantz, Bahram Resul
  • Patent number: 5317032
    Abstract: The present invention relates to cathartics comprising 15-keto-16-halogen-PGs as an essential ingredient without substantive side-effects; the catharic effect is thought mainly caused by an enteropooling effect.
    Type: Grant
    Filed: December 30, 1992
    Date of Patent: May 31, 1994
    Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuzo Ueno, Ryuji Ueno, Sachiko Kuno, Tomio Oda
  • Patent number: 5317021
    Abstract: Amino acid compounds of the formula: ##STR1## wherein the various symbols are as hereinafter described, which have inhibiting effect on enkephalinase.
    Type: Grant
    Filed: November 4, 1992
    Date of Patent: May 31, 1994
    Assignee: ONO Pharmaceutical Co., Ltd.
    Inventors: Masanori Kawamura, Yoshinobu Arai, Hideki Aishita
  • Patent number: 5316766
    Abstract: The combination of a fibrinolytic and a prostacyclin analogue is very useful for thrombosis treatment, especially to avoid subsequent rethrombosis.
    Type: Grant
    Filed: February 6, 1990
    Date of Patent: May 31, 1994
    Assignee: Schering Aktiengesellschaft
    Inventors: Berthold Baldus, Bernhard Maass, Bernd Muller, Werner Witt
  • Patent number: RE34756
    Abstract: Amethod for inducing decrease in potassium ion concentration in the blood which comprises administering, to a subject having an increased potassium ion concentration in the blood, a prostanoic acid derivative in an amount effective in inducing decrease in potassium ion concentration in the blood wherein said concentration is increased or for improving extracorporeal excretion of potassium ion in the blood which comprises administering, to a subject having an increased potassium ion concentration in the blood, a prostanoic acid derivative in an amount effective in improving extracorporeal excretion of potassium ion concentration is increased.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: October 11, 1994
    Assignee: Kabushikikaisha Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuji Ueno, Hiroyoshi Osama
  • Patent number: RE34878
    Abstract: A compound of D-phenylalanine derivative for hypoglycemic use, represented by the general formula ##STR1## R.sup.1 is selected from hydrogen, alkyl of 1 to 5 carbon atoms, aryl of 6 to 12 carbon atoms, aralkyl of 6 to 12 carbon atoms, ##STR2## --CH.sub.2 CO.sub.2 R.sup.3, --CH(CH.sub.3)--OCO--R.sup.3, and --CH.sub.2 --OCO--C(CH.sub.3).sub.3 ; R.sup.2 is selected from groups comprising aryl of 6 to 12 carbon atoms, a hetero six-membered ring, a hetero five-membered ring, cycloalkyl, or cycloalkenyl, any of which groups may have one or more substituents; and R.sup.3 is selected from hydrogen and alkyl of 1 to 5 carbon atoms; the salts thereof, and precursors which can be converted thereto in the human or animal body.Some of the compounds are novel per se.
    Type: Grant
    Filed: November 23, 1993
    Date of Patent: March 14, 1995
    Assignee: Ajinomoto Co., Inc.
    Inventors: Shigeshi Toyoshima, Yoshiko Seto, Hisashi Shinkai, Koji Toi, Izumi Kamashiro