Sulfonamides (i.e., Q-(o=)s(=o)-n, Wherein Q Is A Substituent And Wherein Any Substituent Attached To The Nitrogen Will Be Referred To As E) Patents (Class 514/601)
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Patent number: 5668291Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N, R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: June 7, 1995Date of Patent: September 16, 1997Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5663414Abstract: A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.Type: GrantFiled: December 29, 1995Date of Patent: September 2, 1997Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Takashi Hasegawa, Tadanobu Takamura, Kenichi Nomoto, Yoshiharu Daiku, Toshihiko Naito, Sachiyuki Hamano
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Patent number: 5663205Abstract: A pharmaceutical composition for use in glaucoma treatment which contains as an active ingredient 5-[1-hydroxy-2-[2-(2-methoxyphenoxyl)ethylamino]ethyl]-2-methylbenzenesulf onamide of the formula: ##STR1## or its acid salt. This agent is free from side effects and stable and has an excellent intraocular pressure reducing activity at its low concentrations, thus being useful as a pharmaceutical composition for use in glaucoma treatment.Type: GrantFiled: November 15, 1994Date of Patent: September 2, 1997Assignee: Senju Pharmaceutical Co. Ltd.Inventors: Takahiro Ogawa, Takaaki Deguchi, Yoshifumi Ikejiri, Katsuhiro Inada
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Patent number: 5650405Abstract: A method of reducing the severity of toxoplasmosis resulting from infection of a patient with Toxoplasma gondii by administering to a patient in need of such treatment, either after infection or before exposure to infection, a therapeutically effective amount of a compound that is a spiropiperidyl derivative of rifamycin S, wherein the derivative comprises an imidazole ring that includes carbons at positions 3 and 4 of the rifamycin ring, the carbon at position 2 of the imidazole ring also being a ring carbon at position 4 of a piperidine ring system, thereby forming a spiropiperidyl ring system, the spiropiperidyl ring system optionally comprising a lower hydrocarbon substituent on the nitrogen of the piperidine.Type: GrantFiled: June 7, 1995Date of Patent: July 22, 1997Assignee: Palo Alto Medical FoundationInventors: Jack S. Remington, Fausto G. Araujo
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Patent number: 5646135Abstract: The present invention relates to an improved method for controlling coccidiosis in poultry which comprises administering to poultry on shuttle medication an additional medication prior to switching from the starter compound to the grower compound, and continuing the additional medication for a period after the switching.Type: GrantFiled: March 12, 1996Date of Patent: July 8, 1997Assignee: Merck & Co., Inc.Inventors: Tamas Tamas, Dan A. Ostlind
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Patent number: 5637619Abstract: The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat malignant tumors. The agents are especially useful in the treatment of animal and human cancers. Two preferred agents in this class, especially for use in the treatment of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhy drazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs; they are incapable of generating a hydroxyethylating species by the mechanism proposed for the CNUs; and they are capable of chloroethylation or methylation and carbamoylation.Type: GrantFiled: July 5, 1995Date of Patent: June 10, 1997Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh
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Patent number: 5637298Abstract: 2-naphthalenemethanol [Chemical Abstracts registry no. 1592-38-7] produces a high degree of trail-following activity in termites. The attractant 2-naphthalenemethanol and certain derivatives increase bait acceptance by termites, improving the ability of termite baits to kill colonies, allowing lower amounts of toxicant to be used, or both.Type: GrantFiled: June 14, 1996Date of Patent: June 10, 1997Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventor: John C. Stowell
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Patent number: 5631292Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.Type: GrantFiled: June 2, 1995Date of Patent: May 20, 1997Assignee: Bioresearch, Inc.Inventors: Robert J. Kurtz, William D. Fuller
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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
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Patent number: 5567831Abstract: This invention discloses compounds useful as non-steroidal sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R.sub.1 is selected from the group consisting of hydrogen and a lower alkyl group, (b) R.sub.2 is selected from the group consisting of H and a lower alkyl group, (c) m is an integer from 0 to 4, and (d) n is an integer from 5 to 14. R.sub.1 is selected from the group consisting of H and C.sub.1 -C.sub.6 alkyl and R.sub.2 is selected from the group consisting of H and C.sub.1 -C.sub.6 alkyl. The invention also discloses methods of treating a patient prophylactically to provide protection as an estrogen depleting agent for estrogen dependent illnesses and treating a patient therapeutically for estrogen dependent diseases. A method of making the non-steroidal sulfatase inhibitors is also disclosed.Type: GrantFiled: August 16, 1995Date of Patent: October 22, 1996Assignee: Duguesne University of the Holy GhostInventor: Pui-Kai Li
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Patent number: 5563278Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: May 30, 1995Date of Patent: October 8, 1996Assignee: Eli Lilly and CompanyInventors: Sherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
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Patent number: 5559150Abstract: The present invention is directed to novel compounds that are non-peptidic thrombin inhibitors. The compounds have the structure: ##STR1## and pharmaceutically acceptable salts thereof; wherein R.sup.1 is one of alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; and n is from zero to five. The compounds of the invention are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventor: Richard M. Soll
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Patent number: 5541197Abstract: Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.Type: GrantFiled: March 21, 1995Date of Patent: July 30, 1996Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Elizabeth M. Naylor, Ann E. Weber
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Patent number: 5527547Abstract: Improved biocidal composition and method for controlling biofouling and microorganism population levels in recirculating water systems such as cooling towers, swimming pools or spas is disclosed and claimed. The composition comprises a hypochlorite donor and a bromide ion donor in proportions selected to maintain a mole ratio of the sum of all bromine containing species to the sum of all hypohalite species in the recirculating water of about 0.2 to about 20. The method comprises introducing into the recirculating water a mixture or combination of a hypochlorite donor and a bromide ion donor in an amount sufficient to maintain a ratio of the sum of all bromine containing species to the sum of all species in the recirculating water in the range of about 0.2 to about 20.Type: GrantFiled: April 4, 1995Date of Patent: June 18, 1996Assignee: The University of HoustonInventors: Terry V. T. Hight, Jack V. Matson, Lawrence F. Rakestraw, Zhihe Zhang, Thomas C. Kuechler
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Patent number: 5521160Abstract: The present invention is concerned with novel sulfuric acid esters of sugar alcohols and sugar alcohol-like compounds of the formula ##STR1## Also described are methods for the treatment and/or prophylaxis of arteriosclerotic changes in the vascular wall as well as a process for the manufacture of the compounds of formula I and their salts.Type: GrantFiled: January 4, 1995Date of Patent: May 28, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Chucholowski, Jurgen Fingerle, Niggi Iberg, Hans P. Marki, Rita Muller, Michael Pech, Marianne Rouge, Gerard Schmid, Thomas Tschopp, Hans P. Wessel
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Patent number: 5519060Abstract: Methods are provided for using 2-hydroxy-3-aminopropylsulfonamides to mimic peptides and to modulate the chemical and/or biological activity of enzymes, particularly proteolytic enzymes. Also provided are compositions comprising the sulfonamides in admixture with a pharmaceutically acceptable carrier, adjuvant, or vehicle.Type: GrantFiled: January 17, 1995Date of Patent: May 21, 1996Assignee: The Trustees of the University of PennsylvaniaInventors: Paul Sprengeler, Amos B. Smith, III, Ralph F. Hirschmann, Akihisa Yokoyama
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Patent number: 5514717Abstract: Novel 3,4,4-trifluorobutenoic acid derivatives of the formula ##STR1## wherein Q is --(C.dbd.W)--R.sub.2 wherein W is O or S, and R.sub.2 is an aliphatic or aromatic group when W.dbd.O; --OR.sub.50 ; --SR.sub.50 ; or --NR.sub.50 R.sub.60 wherein R.sub.60 is hydrogen or R.sub.50 ; NR.sub.7 R.sub.8 ; a heterocyclic group; phenyl substituted by alkyl; or any agronomically acceptable salt thereof having usefulness as nematocides, insecticides and acaricides.Type: GrantFiled: October 26, 1994Date of Patent: May 7, 1996Assignee: Monsanto CompanyInventors: Dennis P. Phillion, Gopichand Yalamanchili, Peter G. Ruminski
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Patent number: 5491170Abstract: .beta.-Carboxy sulfonyl compounds of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 is hydrogen or alkyl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is --O--, --S--, or --NR.sub.2 --, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.Type: GrantFiled: December 19, 1994Date of Patent: February 13, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5484811Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 B is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexyimethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.Type: GrantFiled: February 23, 1994Date of Patent: January 16, 1996Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5484812Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.Type: GrantFiled: February 28, 1994Date of Patent: January 16, 1996Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5476846Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts, complexes, esters and amides thereof, represented by the formula ##STR1## which is defined herein. Said compounds find application as anti-thrombotic and anti-asthmatic medicines.Type: GrantFiled: November 17, 1994Date of Patent: December 19, 1995Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Claude Lardy, Daniel Guerrier, Gilles Chavernac, Francois Collonges
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Patent number: 5461076Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.Type: GrantFiled: November 30, 1994Date of Patent: October 24, 1995Inventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
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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
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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
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Patent number: 5455262Abstract: Novel mercaptosulfide matrix metalloproteinase inhibitors of the Formula I, ##STR1## wherein: n is 0 or 1;R.sup.1 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH(lower alkyl); andR.sup.2 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH (lower alkyl); orR.sup.1 and R.sup.2 together are --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sup.3 is selected from the group consisting of hydrogen, lower alkyl, aralkyl and heteroaralkyl; andR.sup.4 is selected from the group consisting of hydrogen, lower alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, aralkyl and 2-indolylmethyl; andR.sup.5 is selected from the group consisting of lower alkyl, aralkyl and --CH(R.sup.6)--C(O)NH.sub.2,whereinR.sup.Type: GrantFiled: October 6, 1993Date of Patent: October 3, 1995Assignee: Florida State UniversityInventors: Martin A. Schwartz, Harold Van Wart
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Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5411989Abstract: The invention concerns nitric acid esters of cyclohexanol of formula I ##STR1## in which A signifies a valency bond or a C.sub.1 -C.sub.6 -alkylene chain and B the group --NR.sup.1 --CO--Z, --NR.sup.1 --SO.sub.2 --Z or --CO--NR.sup.2 --Z, whereby R.sup.1 signifies hydrogen or a C.sub.1 -C.sub.6 -alkyl alkyl group R.sup.2 hydrogen, a hydroxyl, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group and Z signifies hydrogen a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group which may optionally be substituted for the case that B is an --NR.sup.1 --CO--Z group, Z can also signify a C.sub.1 -C.sub.6 -alkoxy group.Type: GrantFiled: December 17, 1993Date of Patent: May 2, 1995Assignee: Boehringer Mannheim, GmbHInventors: Helmut Michel, Wolfgang Bartsch
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Patent number: 5409956Abstract: The present invention relates to indan derivatives represented by the formula (1) or pharmaceutically acceptable salts thereof: ##STR1## [wherein R.sup.1 represents C1 to C12 alkyl, benzyl, styryl, naphthyl, optionally substituted phenyl or optionally substituted thienyl; R.sup.2 represents carboxyl, C1 to C4 alkoxycarbonyl, ##STR2## Y represents --(CH.sub.2).sub.p -- (wherein p represents an integer of 0 to 5), --CO--(CH.sub.2).sub.q .about., --CH(OH)--(CH.sub.2).sub.q .about., (wherein q represents an integer of 1 to 4, and the symbol .about. represents a linkage to R.sup.2), oxymethylene or ethylene; and n represents an integer of 1 to 4]. The compounds according to the present invention potently antagonize the action of thromboxane A.sub.2, and therefore useful for the treatment and prevention of diseases caused by thromboxane A.sub.2 such as angiosis, vasospasm, asthma and the like.Type: GrantFiled: August 30, 1993Date of Patent: April 25, 1995Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Kiyoshi Yoshida, Yoshiaki Yamaji, Tadashi Kurimoto, Ryuichi Sato, Motoki Torizuka
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Patent number: 5405871Abstract: Compounds of the formula ##STR1## wherein each of o and p, independently of the other, is 0, 1, 2, 3, 4 or 5, the radicals R.sub.1 being the same or different when o is greater than 1 and the radicals R.sub.2 being the same or different when p is greater than 1;each of R.sub.1 and R.sub.2, independently of the other, is C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, halogen, --NO.sub.2, --OH, C.sub.1 -C.sub.4 alkoxy, halo-C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, halo-C.sub.1 -C.sub.4 alkylthio, --O--S(.dbd.O)--R.sub.6, --O--S(.dbd.O).sub.2 --R.sub.6, phenoxy or --N(R.sub.11)SO.sub.2 R.sub.12 and/or two substituents R.sub.1 and/or two substituents R.sub.2 are, independently of one another, together --Y--Z--Y--;R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or halo-C.sub.1 -C.sub.4 alkyl;R.sub.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, unsubstituted phenyl or naphthyl or mono- or di-substituted phenyl or naphthyl;R.sub.5 is --S--R.sub.7, --S(.dbd.O)--R.sub.7, --S(.dbd.O).Type: GrantFiled: April 6, 1994Date of Patent: April 11, 1995Assignee: Ciba-Geigy CorporationInventors: Roger G. Hall, Alfons Pascual, Odd Kristiansen
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Patent number: 5403853Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: June 13, 1994Date of Patent: April 4, 1995Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane
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Patent number: 5366997Abstract: There are disclosed cardiovascularly active compounds possessing antihypertensive properties, and pharmaceutical compositions containing these agents and a method of treating cardiovascular disorders with the compounds. The active components of the pharmaceutical compositions are compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from straight chain and branched chain alkyl and olefinic groups, which may be unsubstituted or substituted; or R.sub.1 and R.sub.2 together with the nitrogen atom they are bonded to form a heterocyclic group; and R.sub.3 is a pharmaceutically acceptable organic group selected from alkyl and olefinic groups which may be unsubstituted or substituted, acyl, a sulfonyl, sulfinyl, sulfenyl, carbonate, or carbamate derivative; or R.sub.3 is a group of the formula--(CH.sub.2).sub.n ONN(O)NR.sub.1 R.sub.2, wherein n is 2-8, and R.sub.1 and R.sub.2 are as described above. Novel compounds are disclosed wherein at least one of R.sub.1, R.sub.2 and R.sub.Type: GrantFiled: September 23, 1992Date of Patent: November 22, 1994Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Larry K. Keefer, Tambra M. Dunams, Joseph E. Saavedra
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Patent number: 5346887Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, (alpha, alpha) -dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkylamino.Type: GrantFiled: April 23, 1991Date of Patent: September 13, 1994Assignee: Abbott LaboratoriesInventors: Herman H. Stein, Jacob J. Plattner, Steven R. Crowley
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Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5283261Abstract: Nimesulide is effective in the treatment of cataracts.Type: GrantFiled: September 25, 1992Date of Patent: February 1, 1994Assignee: LPB Istituto FarmaceuticoInventor: Filippo Drago
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Patent number: 5227401Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.Type: GrantFiled: October 29, 1991Date of Patent: July 13, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5223535Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.5 and R.sub.8 is independently propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.Type: GrantFiled: October 29, 1991Date of Patent: June 29, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5214068Abstract: Sulfonylhydrazines of the formula RSO.sub.2 N(CH.sub.2 CH.sub.2 X)N(SO.sub.2 CH.sub.3).sub.2, wherein R is an alkyl or an aryl and X is a halogen or OSO.sub.2 Y, wherein Y is an alkyl or an aryl. Such sulfonylhydrazines are useful in treating cancer.Methylating agents of the formula(a) R'SO.sub.2 N(CH.sub.3)N(SO.sub.2 CH.sub.3).sub.2, wherein R' is an alkyl or an aryl and(b) R"SO.sub.2 N(CH.sub.3)N(CH.sub.3)SO.sub.2 R", wherein R" is an alkyl or an aryl.Such methylating agents are useful as antitrypanosomal and anticancer agents.Type: GrantFiled: March 12, 1992Date of Patent: May 25, 1993Assignee: Yale UniversityInventors: Alan C. Sartorelli, Alan A. Divo, Krishnamurthy Shyam, Philip G. Penketh
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Patent number: 5140048Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises; an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine derivatives. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: October 30, 1990Date of Patent: August 18, 1992Assignee: The Rockefeller UniversityInventors: Peter C. Ulrich, Anthony Cerami
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Patent number: 5124343Abstract: The invention relates to carbacyclins of general Formula I ##STR1## wherein R.sub.1 is the residue CH.sub.2 OH or ##STR2## with R.sub.2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl residue, a ##STR3## or heterocyclic residue, or R.sub.1 is the residue ##STR4## with R.sub.3 meaning an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms or the residue R.sub.2, orR.sub.1 is the residue ##STR5## wherein m is the number 1 or 2, X is an oxygen atom or a CH.sub.2 -group,A is a trans--CH.dbd.CH- or --.tbd.C--group,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,n is the number 1, 2, or 3,D is a straight-chain alkylene group of 1-5 carbon atoms,E is a --C.tbd.C---bond or a --CR.sub.6 =CR.sub.7 --group wherein R.sub.6 and R.sub.7 are different from each other and mean a hydrogen atom or an alkyl group of 1-5 carbon atoms or a hydrogen atom or a halogen atom, preferably chlorine,R.sub.Type: GrantFiled: January 6, 1988Date of Patent: June 23, 1992Assignee: Schering AktiengesellschaftInventors: Helmut Vorbrueggen, Hernd Raduechel, Werner Skuballa, Norbert Schwarz, Jorge Casals-Stenzel, Gerda Mannesmann, Michael H. Town
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Patent number: 5116851Abstract: A novel pharmaceutical composition and method is disclosed for the treatment of cardiovascular diseases, e.g. myocardial ischemia and/or arrhythmia. The method and composition include an effective amount of a compound of the formula ##STR1## wherein X, Y, R, R.sub.1, A, A', m, n, p, p' and B are as defined herein.Type: GrantFiled: January 26, 1990Date of Patent: May 26, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: John Krapcho, James L. Bergey, Gary J. Grover
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Patent number: 5036051Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## where A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is Ch.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl methyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-bezyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkyamino.Type: GrantFiled: March 2, 1990Date of Patent: July 30, 1991Assignee: Abbott LaboratoriesInventors: Herman H. Stein, Jacob J. Plattner
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Patent number: 5025034Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.Type: GrantFiled: February 7, 1990Date of Patent: June 18, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5021448Abstract: A method of reducing serum uric acid and/or increasing renal clearance of uric acid in a mammal in need thereof comprising administering to such mammal a uricosuric effective amount of a thromboxane synthetase inhibitor, a thromboxane receptor antagonist, or both in a combined uricosuric effective amount is disclosed. Compositions having one or more of the foregoing in combination with one or more known uricosurics are also set forth.Type: GrantFiled: February 22, 1990Date of Patent: June 4, 1991Assignee: Ciba-Geigy CorporationInventors: Anthony J. Piraino, Steven D. Saris
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Patent number: 4980366Abstract: Novel 4'-hydroxybenzylamine derivatives of the formula ##STR1## pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, succh as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.Type: GrantFiled: March 16, 1989Date of Patent: December 25, 1990Assignee: Warner-Lambert Co.Inventors: Graham Johnson, Michael F. Rafferty
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Patent number: 4971990Abstract: Phenoxyethylamine derivatives represented by the general formula (I): ##STR1## wherein R.sub.1 and R.sub.5 represent lower-alkyl, R.sub.2 and R.sub.3, which may be the same or different, each represents hydrogen or lower-alkyl, or ##STR2## represents a 5- or 6-membered ring system which may include nitrogen, oxygen or sulfur as a ring membered atom, R.sub.4 represents hydrogen or lower-alkyl, and n represents an integer selected from 1 to 3, their optical isomers and pharmacologically-acceptable acid addition salts, which exhibit excellent .alpha..sub.1 -blocking activity, a process for their preparation, pharmaceutical compositions thereof, and a method for the treatment of a subject afflicted with hypertension or dysuria by administrating such a compound, are all disclosed.Type: GrantFiled: January 24, 1989Date of Patent: November 20, 1990Assignee: Hokuriku Pharmaceutical Co., Ltd.Inventors: Yasuo Itoh, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Kazuya Mitani, Shunichiro Sakurai
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Patent number: 4965279Abstract: Novel cyclopropyl aza prostaglandin analogs are disclosed having the formula ##STR1## wherein A can be carbonyl, sulfonyl or a single bond. These compounds are useful, for example, as thromboxane antagonists.Type: GrantFiled: November 18, 1988Date of Patent: October 23, 1990Assignee: E. R. Squibb & Sons, Inc.Inventors: Raj N. Misra, David M. Floyd, Steven E. Hall
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Patent number: 4942161Abstract: The invention relates to the use of beta blockers for the treatment of the progression of infantile axial myopia.Type: GrantFiled: February 24, 1989Date of Patent: July 17, 1990Inventor: Heinfried Tiburtius
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Patent number: 4939133Abstract: The present invention relates to novel N-substituted 2-hydroxybenzamide and N-substituted 2-hydroxy-.alpha.-oxo-benezene acetamide compounds pharmaceutical compositions, and methods of use for therefore for the treatment of diseases in which products having lipoxygenase enzyme activity contribute to the pathological condition. Selected novel intermediates are also the present invention.Type: GrantFiled: October 1, 1985Date of Patent: July 3, 1990Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn, Wiaczeslaw A. Cetenko, Jagadish C. Sircar, Charles F. Schwender, Elizabeth A. Johnson, Roderick J. Sorenson, Paul C. Unangst
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Patent number: 4927807Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is a substituted amino group; or pharmaceutically acceptable salts or esters thereof.Type: GrantFiled: September 8, 1988Date of Patent: May 22, 1990Assignee: Abbott LaboratoriesInventors: Herman H. Stein, Jacob J. Pattner, Steven R. Crowley
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Patent number: 4921696Abstract: A method has been discovered for the control of arthropod pests which comprises treating the pest with an effective amount of selected fluorocarbons.Type: GrantFiled: October 11, 1988Date of Patent: May 1, 1990Assignees: The United States of America as represented by the Secretary of Agriculture, Southern Research Institute, Inc.Inventors: Robert K. Vander Meer, Clifford S. Lofgren, David F. Williams