Z Contains A Cyclopentyl Or Cyclopentene Ring Patents (Class 514/530)
-
Patent number: 5739160Abstract: New Cyclopentane- or cyclopentene-beta-aminoacid derivatives and their isomers, acid additional salts and metal salt complexes have strong antimicrobial and broad-spectrum antimycotic acitivity. As antimycotics they are especially active against dermatophyte, and biphasic fungi. The new compounds are also low toxicity antibacterial agents, effective against Gram positive bacteria, including antibiotic-resistant strains. The new Cyclopentane- or cyclopentene-beta-aminoacid derivatives are useful in human or veterinary medicine for combating dermatomycosis or systemic mycosis or local or systemic bacterial infections. In addition, the new compounds can also be used as preservatives, especially for water, foods, or organic materials such as polymers, lubricants, paints, fibers, leather, paper or wood.Type: GrantFiled: September 19, 1994Date of Patent: April 14, 1998Assignee: Bayer AktiengesellschaftInventors: Joachim Mittendorf, Franz Kunisch, Michael Matzke, Hans-Christian Militzer, Rainer Endermann, Karl Georg Metzger, Klaus-Dieter Bremm, Manfred Plempel
-
Patent number: 5739161Abstract: The object of the present invention is to provide a pharmaceutical composition for treatment of hepato.biliary disease reduced in side effect such as diarrhea, which comprises 16,16-difluoro-15-keto-PGs having at least one methyl group or ethyl group on the carbon atom at the 17- or 18-position or adjacent to the terminal methyl group of .omega.-chain as an essential component.Type: GrantFiled: February 12, 1997Date of Patent: April 14, 1998Assignee: R-Tech Ueno, Ltd.Inventor: Ryuji Ueno
-
Patent number: 5728733Abstract: Disclosed is the novel use of N-acyl-N,N',N'-ethylene-diaminetriacetic acids and N-acyl-N,N',N'-(ethylenedioxy) diethylenedinitrilotriacetic acids as active ingredients in preventative as well as therapeutic topical compositions to promote exfoliation and alleviate symptoms of skin conditions caused by abnormal keratinization.Type: GrantFiled: December 10, 1996Date of Patent: March 17, 1998Assignee: Avon Products, Inc.Inventor: Dmitri Ptchelintsev
-
Patent number: 5726205Abstract: This document describes O-acyl-4-phenyl-cycloalkanols of general formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between them denote 5- to 7-membered saturated, monocyclic, heterocyclic rings which may optionally also be interrupted by an oxygen or sulphur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl or alkynyl having up to 17 carbon atoms, and also processes for preparing them, pharmaceutical compositions containing these compounds and the use of these pharmaceutical compositions which intervene in cholesterol biosynthesis.Type: GrantFiled: January 17, 1997Date of Patent: March 10, 1998Assignee: Karl Thomae GmbHInventors: Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
-
Patent number: 5721273Abstract: 9-Halo-13,14-dihydroprostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.Type: GrantFiled: December 15, 1993Date of Patent: February 24, 1998Assignee: Alcon Laboratories, Inc.Inventors: Verney L. Sallee, Louis DeSantis, Jr., Paul W. Zinke, John E. Bishop
-
Patent number: 5719184Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-carboxylate dimers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: June 23, 1997Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
-
Patent number: 5719183Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: June 2, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
-
Patent number: 5719182Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
-
Patent number: 5716985Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 23, 1995Date of Patent: February 10, 1998Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Maria Amparo Lago
-
Patent number: 5700835Abstract: Compositions containing 3-Oxa-D-prostaglandins and methods of their use in treating glaucoma or ocular hypertension are disclosed.Type: GrantFiled: December 22, 1995Date of Patent: December 23, 1997Assignee: Alcon Laboratories, Inc.Inventors: Thomas R. Dean, Mark Hellberg, Verney L. Sallee
-
Patent number: 5698590Abstract: Prostaglandin E.sub.1 ester derivatives of the formula (I): ##STR1## wherein the R' groups are the same as each other and are C4-12 alkyl; or cyclodextrin clathrates thereof, liposome formulations containing them, and pharmaceutical compositions containing them, as active ingredient.The compounds of formula (I) have the effect of increasing blood flow and are useful for the prevention and/or treatment of peripheral circulatory disorder, decubitus, or skin ulcers, or for the maintenance of blood flow.Type: GrantFiled: August 22, 1996Date of Patent: December 16, 1997Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akio Nishiura, Takuya Seko, Ryoji Matsumoto, Shin-ichi Hamano
-
Patent number: 5698598Abstract: The invention relates to the use of EP.sub.2 receptor agonists as potent ocular hypotensives, and are particularly suitable for the management of glaucoma. In particular said compounds are represented by the formulae: ##STR1## wherein the broken line attachment to the cyclopentane ring or the omega chain indicates the .alpha. configuration and the solid line attachment to the cyclopentane ring or the omega chain indicates the .beta. configuration, R is hydrogen or 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.Type: GrantFiled: August 4, 1995Date of Patent: December 16, 1997Assignee: AllerganInventor: David F. Woodward
-
Patent number: 5698733Abstract: Disclosed are 9-deoxyprostaglandins which are useful in the treatment of glaucoma and ocular hypertension. Some of these 9-deoxyprostaglandins are novel. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.Type: GrantFiled: June 7, 1995Date of Patent: December 16, 1997Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, Thomas R. Dean, Paul W. Zinke, Robert D. Selliah, John E. Bishop
-
Patent number: 5696166Abstract: Compositions containing a HETE derivative and methods of use for treating dry eye are disclosed.Type: GrantFiled: October 31, 1995Date of Patent: December 9, 1997Inventors: John M. Yanni, Daniel A. Gamache, Steven T. Miller
-
Patent number: 5688819Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.Type: GrantFiled: February 22, 1996Date of Patent: November 18, 1997Assignee: AllerganInventors: David F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
-
Patent number: 5686487Abstract: A method for treatment of a cataract which comprises administering, to a subject in need of such treatment, a 15-ketoprostaglandin compound in an amount effective in treatment of cataract.Type: GrantFiled: September 6, 1994Date of Patent: November 11, 1997Assignee: R-Tech Ueno Ltd.Inventor: Ryuji Ueno
-
Patent number: 5681850Abstract: The invention describes prostaglandin E1 derivatives as pharmacologically active agents, and pharmaceutical compositions containing these compounds, especially for transcutaneous administration.Type: GrantFiled: October 31, 1995Date of Patent: October 28, 1997Inventors: Jurgen C. Frolich, Herbert Bippi
-
Patent number: 5681964Abstract: Prodrugs containing an active drug molecule linked to a polyethylene glycol group, and a method of use thereof are described. Exemplary soluble ester prodrugs contain naproxen, triamcinolone acetonide, gancyclovir, taxol, cyclosporin, dideoxyinosine, trihydroxy steroids, and flurbiprofen molecules linked to polyethylene glycol (PEG) groups. Pharmaceutical compositions containing these prodrugs, and a method of using these esters for treating disease states or symptoms are also described.Type: GrantFiled: October 5, 1994Date of Patent: October 28, 1997Assignee: University of Kentucky Research FoundationInventors: Paul Ashton, Thomas J. Smith, Peter G. Glavinos, John D. Conklin, Jr., Peter A. Crooks, Robert M. Riggs, Tadeusz Cynkowski, Grazyna Cynkowska
-
Patent number: 5665773Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues for the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic compositions comprising said compounds.Type: GrantFiled: December 18, 1996Date of Patent: September 9, 1997Assignee: Alcon Laboratories, Inc.Inventors: Peter G. Klimko, John E. Bishop, Verney L. Sallee, Paul W. Zinke
-
Patent number: 5661178Abstract: The present invention provides a method of effecting vasodilation, comprising:administering to a warm blooded animal in need of such treatment, an effective amount of a (1,5-inter) aryl prostaglandin derivative represented by the Formula I ##STR1## wherein n is 0 or an integer of from 1 to 6, R is selected from the group of radicals represented by the formulae:CO.sub.2 R', CONR'.sub.2, CH.sub.2 OR' and SO.sub.2 NR'.sub.2'wherein R' is hydrogen or a lower alkyl radical having from one to six carbon atoms; R" is hydrogen or an acyl radical having the formula (CO)R'" wherein R'" is a saturated or unsaturated acyclic hydrocarbon radical having from 1 to about 10 carbon atoms, or --(CH.sub.2).sub.m R"" wherein m is 0 or an integer of from 1 to 6 and R"" is an aliphatic ring having from 3 to 7 carbon atoms or an aryl group, e.g. phenyl, or a heteroaryl group, e.g.Type: GrantFiled: September 1, 1995Date of Patent: August 26, 1997Assignee: AllerganInventors: June Chen, Robert M. Burk, David F. Woodward
-
Patent number: 5656663Abstract: An external skin treatment agent composition containing an active ingredient comprising a prostacyclin, and/or its optical isomer, having the formula (I): ##STR1## (wherein, R.sup.1 is a hydrogen atom, a straight chain or branched alkyl group of C.sub.1 to C.sub.10, or one equivalent of a cation, R.sup.2 is a substitutable C.sub.1 to C.sub.10 straight chain or branched alkyl group or substitutable C.sub.1 to C.sub.10 straight chain or branched alkenyl group or alkinyl group, R.sup.3 is a straight chain alkyl group of C.sub.1 to C.sub.5, and R.sup.4 and R.sup.5 are independently a hydroxyl group or formula: ##STR2## (where, R.sup.6 is a C.sub.1 to C.sub.5 straight chain or branched alkyl group)) and a carrier.Type: GrantFiled: December 28, 1994Date of Patent: August 12, 1997Assignee: Teijin LimitedInventors: Atsuo Hazato, Nobuaki Hanajima, Yuji Makino, Toshiaki Takeda, Tamotsu Koyama, Takehisa Hata, Sumihisa Kimura, Saburo Murata
-
Patent number: 5656635Abstract: The invention relates to the use of alcohol derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are encompassed by the following structure formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched lined indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond; n is 0, or an integer of from 1 to 3; R is hydrogen or a --(CO)R.sub.4 group; R.sub.1, R.sub.2, and R.sub.3 independently are hydroxyl, or --O(CO)R.sub.5 groups, wherein R.sub.4 and R.sub.5 independently stand for saturated or unsaturated acyclic hydrocarbon having from 1 to 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.6 where m is 0-10 and R.sub.6 is an aliphatic, aromatic or heteroaromatic ring, R.sub.7 and R.sub.8 independently are hydrogen or alkyl of 1 to 6 carbon atoms or pharmaceutically acceptable salts thereof.Type: GrantFiled: June 8, 1993Date of Patent: August 12, 1997Assignee: AllerganInventor: Ming Fai Chan
-
Patent number: 5631291Abstract: The invention relates to cyclopentane- and -pentene-.beta.-amino acids, processes for their preparation and their use as medicaments.Type: GrantFiled: November 9, 1994Date of Patent: May 20, 1997Assignee: Bayer AktiengesellschaftInventors: Joachim Mittendorf, Franz Kunisch, Michael Matzke, Hans-Christian Militzer, Rainer Endermann, Karl G. Metzger, Klaus-Dieter Bremm, Manfred Plempel
-
Patent number: 5631287Abstract: The use of polyethoxylated castor oils in prostaglandin compositions greatly enhances the prostaglandin's chemical stability.Type: GrantFiled: December 22, 1994Date of Patent: May 20, 1997Assignee: Alcon Laboratories, Inc.Inventor: L. Wayne Schneider
-
Patent number: 5627208Abstract: 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: June 6, 1995Date of Patent: May 6, 1997Assignee: Pharmacia AktiebolagInventors: Johan W. Stjernschantz, Bahram Resul
-
Patent number: 5627209Abstract: 9-Haloprostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.Type: GrantFiled: October 25, 1995Date of Patent: May 6, 1997Assignee: Alcon Laboratories, Inc.Inventors: Louis DeSantis, Jr., Verney L. Sallee
-
Patent number: 5624956Abstract: Novel urea derivatives and pharmaceutical compositions thereof are provided which inhibit platelet aggregation.Type: GrantFiled: May 24, 1995Date of Patent: April 29, 1997Assignee: The Monsanto CompanyInventors: Foe S. Tjoeng, Mihaly V. Toth, Dudley E. McMackins, Steven P. Adams
-
Patent number: 5616614Abstract: The invention relates to a compound selected from those of general formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable base. Medicinal product which is useful in the treatment of disorders linked to abnormal melatonin activity.Type: GrantFiled: January 25, 1995Date of Patent: April 1, 1997Assignee: Adir ET CompagnieInventors: Said Yous, Daniel Lesieur, Patrick Depreux, B eatrice Guardiola-Lemaitre, G erard Adam, Pierre Renard, Daniel H. Caignard
-
Patent number: 5616607Abstract: Compounds of the general structure ##STR1## are disclosed, wherein X is O, C.sub.n, NH, or S, wherein n is 1, 2, 3 or 4; R1 is OH, CH.sub.3, CH.sub.2 OH, N.sub.3 or CH.sub.2 N.sub.3 ; R3 is H or CH.sub.3 ; R5 is Y-R2, wherein Y is a six-carbon chain optionally containing up to three double or triple bonds or a mixture of double and triple bonds up to a maximum of three; R2 is C.sub.1 -C.sub.10 alkyl OH, C.sub.1 -C.sub.10 alkyl N.sub.3 or COOR4, wherein R4 is H, a branched or unbranched C.sub.1 -C.sub.10 alkyl (including substituted alkyl radicals), cycloalkyl, preferably C.sub.5 or C.sub.6 cycloalkyl, or a five- or six-membered aryl radical (including substituted aryl radicals), i.e. R2 is COOH or an ester of R4; R6 is a seven-carbon chain optionally containing up to three double or triple bonds or a mixture of double and triple bonds up to a maximum of three; and . . . . . . indicates a single, double or triple bond.Type: GrantFiled: March 21, 1995Date of Patent: April 1, 1997Assignee: HSC Research and Development Limited PartnershipInventors: Cecil R. Pace-Asciak, Peter M. Demin
-
Patent number: 5610188Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.Type: GrantFiled: December 30, 1994Date of Patent: March 11, 1997Assignee: University of FloridaInventors: Richard H. Hammer, Nicholas S. Bodor
-
Patent number: 5610182Abstract: A pharmaceutical composition effective for the therapy of cerebral thrombosis, particularly acute cerebral thrombosis, which is in the form of a fat emulsion containing an isocarbacyclin having a specific structure, and a method for the therapy of cerebral thrombosis.Type: GrantFiled: October 3, 1994Date of Patent: March 11, 1997Assignees: Teijin, Limited, Taisho Pharmaceutical Co., Ltd., Yutaka MizushimaInventors: Yutaka Mizushima, Kiyoshi Bannai, Shigeru Nakayana
-
Patent number: 5605931Abstract: Prostaglandins of the PGE type can be administered in a therapeutically effective amount to protect tissue from injury resulting from chemotherapeutic agents by administering the PGE-type prostaglandin prior to administration of the chemotherapeutic agent.Type: GrantFiled: May 11, 1995Date of Patent: February 25, 1997Assignee: Loyola University of ChicagoInventor: Wayne R. Hanson
-
Patent number: 5605922Abstract: 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: December 12, 1995Date of Patent: February 25, 1997Assignee: Alcon Laboratories, Inc.Inventors: Louis DeSantis, Jr., Verney L. Sallee
-
Patent number: 5599837Abstract: The present invention relates to a 15-deoxyprostaglandin derivative of the formula (I): ##STR1## in which ##STR2## is a 5 membered ring which is selected from a group consisting of ##STR3## R.sup.1 is hydrogen or lower alkyl; R.sup.2 is C.sub.6 -C.sub.12 alkyl, C.sub.6 -C.sub.12 alkenyl or C.sub.6 -C.sub.12 alkadienyl;provided that the compound of the following formula is excluded: ##STR4## wherein R' is hydrogen or methyl; or pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical formulation comprising a 15-deoxyprostaglandin derivative as an active ingredient, which is useful as an intraocular pressure reducing agent.Type: GrantFiled: February 28, 1995Date of Patent: February 4, 1997Assignee: Shionogi & Co., Ltd.Inventors: Morio Kishi, Kimio Takahashi, Kenji Kawada, Yasumasa Goh
-
Patent number: 5599838Abstract: A prostaglandin derivative represented by the formula: ##STR1## wherein X is halogen atom R.sup.1 is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, and R.sup.2 is a cycloalkyl group having 3 to 10 carbon atoms, a cycloalkylmethyl group having 4 to 10 carbon atoms or a cycloalkylethyl group having 5 to 12 carbon atoms, or a salt thereof, which has an excellent lowering action of intraocular pressure and improving actions of renal diseases, ischemic heart diseases and heart failure.Type: GrantFiled: February 23, 1996Date of Patent: February 4, 1997Assignees: Taisho Pharmaceutical Co., Ltd., Fumie SatoInventors: Fumie Sato, Takehiro Amano, Kazuya Kameo, Tohru Tanami, Masaru Mutoh, Naoya Ono, Jun Goto
-
Patent number: 5597809Abstract: Methods of treating optic neuritis comprising administering a protective agent which inhibits glutamate-mediated retinal cell damage to a mammal at risk of developing optic neuritis.Type: GrantFiled: June 23, 1994Date of Patent: January 28, 1997Assignee: Massachusetts Eye & Ear InfirmaryInventor: Evan B. Dreyer
-
Patent number: 5591727Abstract: The invention relates to an insecticidal composition which comprises at least one pyrethroid, at least one UV absorbing agent and at least one antioxidant from the group consisting of tocopherol derivatives and citric acid esters. This insecticidal composition can in particular be used as an emulsion or on a powdery carrier for the control of flying and crawling insects such as flies and cockroaches.Type: GrantFiled: February 7, 1995Date of Patent: January 7, 1997Assignees: Perycut-Chemie AG, Franz BencsitsInventor: Franz Bencsits
-
Patent number: 5583158Abstract: A prostaglandin E.sub.1 analogue represented by formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; and X is an oxygen atom and R.sup.2 represents ##STR2## or X is a sulfur atom and R.sup.2 represents ##STR3## The compound has a strong and prolonged inhibitory action for platelet aggregation and is useful for treatment of various thrombotic diseases including peripheral circulatory disturbance.Type: GrantFiled: April 19, 1995Date of Patent: December 10, 1996Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Fumie Sato, Takehiro Amano, Kazuya Kameo, Tohru Tanami, Masaru Mutoh, Naoya Ono, Jun Goto
-
Patent number: 5578640Abstract: Prostaglandins of the PGE type can be administered in a therapeutically effective amount to protect tissue from injury resulting from chemotherapeutic agents by administering the PGE-type prostaglandin prior to administration of the chemotherapeutic agent.Type: GrantFiled: May 11, 1995Date of Patent: November 26, 1996Assignee: Loyola University of ChicagoInventor: Wayne R. Hanson
-
Patent number: 5578643Abstract: Prostaglandins of the PGE type can be administered in a therapeutically effective amount to protect tissue from injury resulting from chemotherapeutic agents by administering the PGE-type prostaglandin prior to administration of the chemotherapeutic agent.Type: GrantFiled: August 4, 1994Date of Patent: November 26, 1996Assignee: Loyola University of ChicagoInventor: Wayne R. Hanson
-
Patent number: 5574066Abstract: A method, compositions and compounds for lowering intraocular pressure involving 15-acyl prostaglandins.Type: GrantFiled: September 21, 1995Date of Patent: November 12, 1996Assignee: AllerganInventors: Ming Fai Chan, David F. Woodward, Charles Gluchowski
-
Patent number: 5571825Abstract: The present invention provides a method of selectively inhibiting prostaglandin G/H synthase-2 that comprises administering to a patient in need of such inhibition an inhibiting amount of a compound having the Formula I, II or III ##STR1## wherein the R groups and heterocycles are defined in the disclosure.Type: GrantFiled: March 31, 1995Date of Patent: November 5, 1996Assignee: Warner-Lambert CompanyInventors: Diane H. Boschelli, David T. Connor, Richard D. Dyer, Sonya S. Khatana, James B. Kramer, William H. Roark
-
Patent number: 5565490Abstract: p-Hydroxyaniline derivatives of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen, or unsubstituted or substituted alkyl;R.sup.2 and R.sup.3 independently of one another are halogen, alkyl, haloalkyl, alkoxy or haloalkoxy;R.sup.4 is unsubstituted or substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or aryl,OR.sup.5 or NR.sup.6 R.sup.7, whereR.sup.5, R.sup.6 are unsubstituted or substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or aryl, andR.sup.7 is hydrogen or alkyl,and their salts, processes for their preparation, compositions containing them and their use for controlling harmful fungi or pests, and also compounds of the formula VI ##STR2## and their salts, processes for their preparation, compositions containing them and their use as intermediates and for controlling pests are described.Type: GrantFiled: November 10, 1994Date of Patent: October 15, 1996Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Karl Eicken, Norbert G otz, Harald Rang, Eberhard Ammermann, Gisela Lorenz
-
Patent number: 5565492Abstract: Disclosed is the use of combinations of F and E series prostaglandins and their respective derivatives and analogues, as well as pharmaceutically acceptable salts and esters thereof in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising said combinations.Type: GrantFiled: December 1, 1994Date of Patent: October 15, 1996Assignee: Alcon Laboratories, Inc.Inventors: Louis M. DeSantis, Verney L. Sallee
-
Patent number: 5554649Abstract: A controlling agent for fabric pest insects characterized by containing, as an active ingredient, a carboxylic acid ester represented by the formula (I): ##STR1## wherein R represents an allyl or propargyl group, Y represents a hydrogen atom or a methyl group, and when Y is a hydrogen atom, X represents an isobutenyl, 2,2-difluorovinyl or 2-chloro-2-fluorovinyl group, and when Y is a methyl group, X represents a methyl group.Type: GrantFiled: December 19, 1994Date of Patent: September 10, 1996Assignee: Sumitomo Chemical Company, Limited.Inventors: Takao Ishiwatari, Kazunori Tsushima
-
Patent number: 5547968Abstract: A method for treatment of ocular hypertension which comprises ocularly administering, to a subject in need of such treatment, an oculo-hypotensively synergistic combination of(a) a 15-ketoprostaglandin or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof, and(b) a carbonate dehydratase inhibitor in an amount effective in treatment of ocular hypertension.Type: GrantFiled: June 7, 1995Date of Patent: August 20, 1996Assignee: R-Tech Ueno, Ltd.Inventor: Ryuji Ueno
-
Patent number: 5545666Abstract: A prostaglandin derivative represented by formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and R.sup.2 represents a cyclohexyl group or a cyclopentylmethyl group. This compound has physiological activities such as platelet aggregation-inhibiting action, renal blood vessel and coronary blood vessel-dilating actions and the like, and is useful for treatment of renal failure and diseases of circulatory organs.Type: GrantFiled: April 19, 1995Date of Patent: August 13, 1996Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Fumie Sato, Takehiro Amano, Kazuya Kameo, Tohru Tanami, Masaru Mutoh, Naoya Ono, Jun Goto
-
Patent number: 5545665Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxycyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.Type: GrantFiled: December 28, 1993Date of Patent: August 13, 1996Assignee: AllerganInventor: Robert M. Burk
-
Patent number: 5534547Abstract: The present invention provides novel prostaglandins D, that is, 13,14-dihydro-15-keto-PGDs, whieh have an excellent sedative and sleep-inducing activity, and so they are useful for tranquilizer and/or soporifics.Type: GrantFiled: September 23, 1994Date of Patent: July 9, 1996Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Ryuji Ueno, Ichie Kato, Tomio Oda
-
Patent number: 5530027Abstract: An external skin treatment agent composition containing an active ingredient comprising of a prostacyclin, and/or its optical isomer, having the formula (I): ##STR1## (wherein, R.sup.1 is a hydrogen atom, a straight chain or branched alkyl group of C.sub.1 to C.sub.10, or one equivalent of cations, R.sup.2 is (CH.sub.2).sub.2 R.sup.21 or a substitutable C.sub.3 to C.sub.10 cycloalkyl group, where R.sup.21 is a substitutable C.sub.1 to C.sub.10 straight chain or branched alkyl group or substitutable C.sub.2 to C.sub.10 straight chain or branched alkenyl group or alkynyl group, and R.sup.3 and R.sup.4 are independently a hydroxyl group or formula ##STR2## (wherein, R.sup.5 is a C.sub.1 to C.sub.5 straight chain or branched alkyl group)) and a carrier.Type: GrantFiled: October 3, 1994Date of Patent: June 25, 1996Assignee: Teijin LimitedInventors: Atsuo Hazato, Nobuaki Hanajima, Yuji Makino, Toshiaki Takeda, Tamotsu Koyama