Z Contains A Cyclopentyl Or Cyclopentene Ring Patents (Class 514/530)
-
Patent number: 5516796Abstract: 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: GrantFiled: March 24, 1994Date of Patent: May 14, 1996Assignee: Kabi Pharmacia ABInventors: Johan W. Stjernschantz, Bahram Resul, Laszlo Z. Bito
-
Patent number: 5514712Abstract: 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: GrantFiled: June 14, 1994Date of Patent: May 7, 1996Assignee: Shiseido International FranceInventor: Jacques LeClere
-
Patent number: 5510384Abstract: 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: GrantFiled: May 5, 1994Date of Patent: April 23, 1996Inventors: Rex N. McKee, Frank A. Wingrove
-
Patent number: 5510382Abstract: 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: GrantFiled: May 6, 1993Date of Patent: April 23, 1996Assignee: Pharmacia ABInventors: Johan Stjernschantz, Bahram Resul
-
Patent number: 5510383Abstract: 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: GrantFiled: August 3, 1993Date of Patent: April 23, 1996Assignee: Alcon Laboratories, Inc.Inventors: John E. Bishop, Louis DeSantis, Jr., Verney L. Sallee
-
Patent number: 5510381Abstract: 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: GrantFiled: May 15, 1995Date of Patent: April 23, 1996Assignee: Warner-Lambert CompanyInventor: Atul C. Pande
-
Patent number: 5504111Abstract: 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: GrantFiled: December 30, 1994Date of Patent: April 2, 1996Assignee: Medichem Research, Inc.Inventors: Michael T. Flavin, Deanna J. Nelson, Julian F. Borgia, deceased, Gary Jesmok
-
Patent number: 5486540Abstract: 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: GrantFiled: October 28, 1993Date of Patent: January 23, 1996Assignee: Allergan, Inc.Inventor: Steven W. Andrews
-
Patent number: 5480900Abstract: 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: GrantFiled: April 10, 1995Date of Patent: January 2, 1996Assignee: Alcon Laboratories, Inc.Inventors: Louis DeSantis, Jr., Verney L. Sallee
-
Patent number: 5476872Abstract: 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: GrantFiled: October 18, 1993Date of Patent: December 19, 1995Assignee: Allergan, Inc.Inventors: Michael E. Garst, Elizabeth T. Syage, Michael B. Roof, David F. Woodward, Ming Fai Chan
-
Patent number: 5472970Abstract: 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: GrantFiled: September 19, 1994Date of Patent: December 5, 1995Assignee: Institut de Recherche Jouveinal S.A.Inventors: Alain P. Calvet, Agnes G. Grouhel, Jean-Louis Junien
-
Patent number: 5468778Abstract: 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: GrantFiled: September 24, 1992Date of Patent: November 21, 1995Assignee: Allergan, Inc.Inventors: Michael E. Garst, Robert M. Burk, Ming F. Chan, Michael B. Roof
-
Patent number: 5464868Abstract: The invention describes prostaglandin E1 derivatives as pharmacologically active agents, and pharmaceutical compositions containing these compounds, especially for transcutaneous administration.Type: GrantFiled: April 7, 1993Date of Patent: November 7, 1995Inventors: Jurgen C. Frolich, Herbert Bippi
-
Patent number: 5462968Abstract: 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: GrantFiled: January 19, 1994Date of Patent: October 31, 1995Assignee: Allergan, Inc.Inventor: David F. Woodward
-
Patent number: 5457131Abstract: 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: GrantFiled: August 18, 1994Date of Patent: October 10, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
-
Patent number: 5455273Abstract: 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: GrantFiled: November 19, 1993Date of Patent: October 3, 1995Assignee: Karl Thomae GmbHInventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
-
Patent number: 5451607Abstract: 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: GrantFiled: April 19, 1993Date of Patent: September 19, 1995Assignee: Sumitomo Chemical Co., Ltd.Inventors: Toshiaki Taki, Hirosi Kisida, Shigeru Saito, Shinji Isayama
-
Patent number: 5449691Abstract: 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: GrantFiled: June 24, 1993Date of Patent: September 12, 1995Assignee: Sterling Winthrop Inc.Inventors: William N. Washburn, Lee H. Latimer, Barbara B. Lussier, Carl R. Illig, Alexander L. Weis
-
Patent number: 5446041Abstract: 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: GrantFiled: October 10, 1990Date of Patent: August 29, 1995Assignee: Allergan, Inc.Inventors: Ming F. Chan, David F. Woodward
-
Patent number: 5434180Abstract: The present invention relates to new polycyclic aromatic derivatives, to processes for their preparation and to their use in therapeutic and cosmetic formulations.Type: GrantFiled: March 27, 1992Date of Patent: July 18, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (CIRD Galderma)Inventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
-
Patent number: 5432174Abstract: 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: GrantFiled: December 7, 1993Date of Patent: July 11, 1995Assignee: R-Tech Ueno, Ltd.Inventors: Ryuji Ueno, Sachiko Kuno
-
Patent number: 5428062Abstract: 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: GrantFiled: April 28, 1993Date of Patent: June 27, 1995Assignee: K.K. Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Ryuji Ueno, Ichie Kato, Tomio Oda
-
Patent number: 5426115Abstract: 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: GrantFiled: October 29, 1993Date of Patent: June 20, 1995Assignee: Kabushikikaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuji Ueno, Hiroyoshi Osama, Tomio Oda
-
Patent number: 5422369Abstract: 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: GrantFiled: February 25, 1994Date of Patent: June 6, 1995Assignee: Kabi Pharmacia ABInventors: Johan W. Stjernschantz, Bahram Resul
-
Patent number: 5422368Abstract: 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: GrantFiled: December 8, 1992Date of Patent: June 6, 1995Assignee: Kabi Pharmacia ABInventors: Johan W. Stjernschantz, Bahram Resul
-
Patent number: 5414016Abstract: 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: GrantFiled: June 13, 1994Date of Patent: May 9, 1995Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
-
Patent number: 5414014Abstract: 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: GrantFiled: April 8, 1993Date of Patent: May 9, 1995Assignee: Innova Biomed, Inc.Inventors: Linda H. Schneider, Randall B. Murphy
-
Patent number: 5411987Abstract: 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: GrantFiled: February 25, 1993Date of Patent: May 2, 1995Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Thomas Seitz, Wilhelm Brandes
-
Patent number: 5405846Abstract: 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: GrantFiled: September 28, 1993Date of Patent: April 11, 1995Assignee: R-Tech Ueno, Ltd.Inventor: Ryuji Ueno
-
Patent number: 5405870Abstract: 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: GrantFiled: November 4, 1993Date of Patent: April 11, 1995Assignee: Sankyo Company, LimitedInventors: Kazuo Koyama, Shigeo Amemiya, Koichi Kojima, Shinsaku Kobayashi
-
Patent number: 5399588Abstract: 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: GrantFiled: December 14, 1993Date of Patent: March 21, 1995Assignee: American Home Products CorporationInventor: Michael S. Malamas
-
Patent number: 5393764Abstract: 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: GrantFiled: August 25, 1993Date of Patent: February 28, 1995Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
-
Patent number: 5389619Abstract: 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: GrantFiled: March 29, 1993Date of Patent: February 14, 1995Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
-
Patent number: 5387608Abstract: 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: GrantFiled: August 17, 1993Date of Patent: February 7, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
-
Patent number: 5387607Abstract: 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: GrantFiled: December 13, 1993Date of Patent: February 7, 1995Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
-
Patent number: 5385931Abstract: 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: GrantFiled: December 28, 1990Date of Patent: January 31, 1995Assignee: Pierre Fabre MedicamentInventors: Dennis Bigg, Alain Duflos, Jean-Pierre Rieu
-
Patent number: 5380709Abstract: 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: GrantFiled: April 28, 1993Date of Patent: January 10, 1995Assignee: K.K. Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Ryuji Ueno, Ichie Kato, Tomio Oda
-
Patent number: 5376683Abstract: 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: GrantFiled: November 25, 1992Date of Patent: December 27, 1994Assignee: Schering AktiengesellschaftInventors: Ulrich Klar, Hartmut Rehwinkel, Helmut Vorbruggen, Karl H. Thierauch, Claus S. Sturzebecher
-
Patent number: 5374654Abstract: 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: GrantFiled: April 21, 1993Date of Patent: December 20, 1994Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Ulrich Klar, Bob Nieuweboer, Claus-Steffen Sturzebecher
-
Patent number: 5364883Abstract: 16(S)-Isocarbacyclins have been found to the useful in the treatment of liver and kidney diseases.Type: GrantFiled: May 3, 1993Date of Patent: November 15, 1994Assignee: Teijin LimitedInventors: Kiyoshi Bannai, Toshio Tanaka, Yoshinori Kato, Tamotsu Koyama, Satoshi Asano, Akira Ohtsu, Seizi Kurozumi, Makoto Ogawa, Yoshio Mori
-
Patent number: 5362751Abstract: The present invention provides a tracheobronchodilator comprising 15-keto-PGEs, reduced in stimuli against bronchi and other side effects.Type: GrantFiled: June 17, 1993Date of Patent: November 8, 1994Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Ryuji Ueno, Tomio Oda
-
Patent number: 5356931Abstract: 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: GrantFiled: January 4, 1993Date of Patent: October 18, 1994Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
-
Patent number: 5356621Abstract: 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: GrantFiled: February 10, 1993Date of Patent: October 18, 1994Assignee: Sankyo Company, LimitedInventors: Yuichiro Tabaru, Akio Saito
-
Patent number: 5324746Abstract: 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: GrantFiled: February 12, 1993Date of Patent: June 28, 1994Inventors: Rex N. McKee, Frank A. Wingrove
-
Patent number: 5321128Abstract: 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: GrantFiled: December 8, 1992Date of Patent: June 14, 1994Assignee: Kabi Pharmacia ABInventors: Johan W. Stjernschantz, Bahram Resul
-
Patent number: 5317032Abstract: 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: GrantFiled: December 30, 1992Date of Patent: May 31, 1994Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Ryuji Ueno, Sachiko Kuno, Tomio Oda
-
Patent number: 5317021Abstract: Amino acid compounds of the formula: ##STR1## wherein the various symbols are as hereinafter described, which have inhibiting effect on enkephalinase.Type: GrantFiled: November 4, 1992Date of Patent: May 31, 1994Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Masanori Kawamura, Yoshinobu Arai, Hideki Aishita
-
Patent number: 5316766Abstract: The combination of a fibrinolytic and a prostacyclin analogue is very useful for thrombosis treatment, especially to avoid subsequent rethrombosis.Type: GrantFiled: February 6, 1990Date of Patent: May 31, 1994Assignee: Schering AktiengesellschaftInventors: Berthold Baldus, Bernhard Maass, Bernd Muller, Werner Witt
-
Patent number: RE34756Abstract: 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: GrantFiled: September 30, 1992Date of Patent: October 11, 1994Assignee: Kabushikikaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuji Ueno, Hiroyoshi Osama
-
Patent number: RE34878Abstract: 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: GrantFiled: November 23, 1993Date of Patent: March 14, 1995Assignee: Ajinomoto Co., Inc.Inventors: Shigeshi Toyoshima, Yoshiko Seto, Hisashi Shinkai, Koji Toi, Izumi Kamashiro