Arthritis Patents (Class 514/825)
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Patent number: 5470834Abstract: Novel sulfoximine and sulfodiimine matrix metalloproteinase inhibitors of the formula, ##STR1## wherein: R.sup.1 is selected from the group consisting of lower-alkyl, hydroxy lower-alkyl, amino lower-alkyl, carbamoyl lower-alkyl, lower-alkyl carbonyl, lower-alkyoxyalkyl, aralkyl and heteroaralkyl;X is NH or O;R.sup.2 is selected from the group consisting of hydrogen, lower-alkyl and aralkyl;R.sup.3 is selected from the group consisting of hydrogen, lower-alkyl, amino lower-alkyl, guanyl lower-alkyl, aralkyl and heteroaralkyl; andR.sup.4 is selected from the group consisting of lower alkyl, aralkyl and --CH(R.sup.5)--C(O)NH.sub.2,wherein R.sup.5 is selected from the group consisting of hydrogen, lower-alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, hydroxymethyl, 1-hydroxyethyl, mercapto lower-alkyl, and methylthio lower-alkyl;useful for modulating physiological functions or treating diseases and disease conditions associated with matrix metalloproteinase modulation.Type: GrantFiled: October 6, 1993Date of Patent: November 28, 1995Assignee: Florida State UniversityInventors: Martin A. Schwartz, Harold Van Wart
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Patent number: 5468772Abstract: An immunosuppressive compound having the structural formula: ##STR1## is disclosed, along with immunosuppression treatment methods which employ the compound.Type: GrantFiled: March 10, 1993Date of Patent: November 21, 1995Assignee: Pharmagenesis, Inc.Inventors: Ren S. Xu, Tien W. Wiedmann
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Patent number: 5460807Abstract: The oligomers of the present invention are polyureas or polyamides having a number average molecular weight of <10,000. These oligomers are water-soluble, have a rigid backbone with a predictable anion spacing, and are pharmaceutically-acceptable. The oligomers are useful for inhibiting the proliferation of smooth muscle cell.Type: GrantFiled: June 15, 1993Date of Patent: October 24, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Alan D. Cardin, Steven J. Busch, Masayuki Mano
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Patent number: 5459135Abstract: A method for treating mammals suffering from rheumatoid arthritis and other tissue-destructive (chronic inflammatory or other) conditions associated with excess metalloproteinase activity comprising administering to the mammal an amount of a tetracycline that is effectively anti-metalloproteinase, but that is not effectively antimicrobial, and an amount of non-steroidal anti-inflammatory agent which, when combined with the effectively anti-metalloproteinase amount of tetracycline, results in a significant reduction of tissue destruction and/or bone loss.Type: GrantFiled: February 23, 1994Date of Patent: October 17, 1995Assignee: The Research Foundation of State University of New YorkInventors: Lorne M. Golub, Nangavarum S. Ramamurthy, Thomas F. McNamara, Robert A. Greenwald
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Patent number: 5457129Abstract: A novel method of inhibiting production of two important mediators of cellular function, tumor necrosis factor and nitric oxide, and treating a pathophysiological state characterized by an undesirable production or level of tumor necrosis factor or nitric acid. The methods of the present invention employ retinoic acid compounds. The most preferred retinoic acid is all-trans-retinoic acid.Type: GrantFiled: May 17, 1993Date of Patent: October 10, 1995Assignee: Research Development FoundationInventors: Bharat B. Aggarwal, Kapil Mehta
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Patent number: 5456912Abstract: Autoimmune diseases are controlled by the administration of non-methylene interrupted fatty acids of the formula ##STR1## in which R is alkyl or alkenyl. A preferred compound within the scope of this formula is 5,11,14-eicosatrienoic acid.Type: GrantFiled: December 28, 1993Date of Patent: October 10, 1995Assignee: The Regents of the University of CaliforniaInventors: J. Bruce German, M. Eric Gershwin, Alvin Berger
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Patent number: 5455268Abstract: A pharmaceutical composition comprising a compound of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, a saturated or unsaturated aliphatic acyl having 2 to 25 carbon atoms or benzoyl group and R.sup.3 is a hydrogen atom or alkyl group, and a pharmaceutically acceptable carrier is disclosed. Further, a novel compound of the general formula (I) wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, pivaloyl, capryloyl, lauroyl, palmitoyl, stearoyl, linoleoyl, docosahexaenoyl, or benzoyl group, and R.sup.3 is a hydrogen atom or methyl group, is also disclosed.Type: GrantFiled: March 2, 1994Date of Patent: October 3, 1995Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Koju Watanabe, Koichi Niimura, Kiyonori Umekawa
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Patent number: 5455274Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(=NOH)-NH.sub.2 group may be in tautomeric form, and pharmaceutically acceptable salts thereof, in which:R.sub.1 is amino or amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen;R.sub.2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical or hydroxy; or R.sub.2 is hydroxy which is etherified by an aliphatic alcohol, araliphatic alcohol, or aromatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; or R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy;X.sub.1 and X.sub.Type: GrantFiled: December 9, 1992Date of Patent: October 3, 1995Assignee: Ciba-Geigy CorporationInventor: Hongsuk Suh
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Patent number: 5451586Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or (C.sub.1 -C.sub.6)alkyl; R.sup.2 is phenyl, pyridyl, thienyl or furyl, and R.sup.2 may optionally be substituted with from one to three substituents independently selected from (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, chloro, fluoro, bromo, iodo, and trifluoromethyl; R.sup.3 is phenyl, naphthyl, pyridyl, thienyl or furyl, and R.sup.3 may optionally be substituted with from one to three substituents independently selected from (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, chloro, fluoro, bromo, iodo and trifluoromethyl; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.Type: GrantFiled: December 13, 1993Date of Patent: September 19, 1995Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Patent number: 5431924Abstract: A biologically active component of emu oil is disclosed which is useful in pharmaceutical composition for the treatment of inflammation of environmental and systemic origins. Pharmaceutical composition including emu oil and dermal transport enhancing compounds are also disclosed as useful topical anti-inflammatory treatments.Type: GrantFiled: July 16, 1993Date of Patent: July 11, 1995Assignee: Emu Products Western Australia Pty. Ltd.Inventors: Peter Ghosh, Michael Whitehouse, Michael Dawson, Athol G. Turner
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Patent number: 5430051Abstract: A method for the photodynamic therapy of rheumatoid arthritis of mammals, which agent comprises at least one member of fluorescent compounds selected from the group consisting of tetrapyrrole carboxylic acids having at least one carboxyl group, corresponding di- or tetrahydrotetrapyrrole carboxylic acids, and mono-, di- or polyamides of the tetrapyrrole carboxylic acids with amino-mono- or dicarboxylic acids and their salts.Type: GrantFiled: April 19, 1994Date of Patent: July 4, 1995Assignee: Nippon Petrochemicals Company, LimitedInventors: Katsuo Aizawa, Yukari Kuroiwa
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Patent number: 5424332Abstract: A pharmaceutical composition in dosage form for treating psoriasis and psoriatic arthritis includes, essentailly, as active substance (s), a fumaric acid monoalkylester salt having the formula ##STR1## wherein R is a methyl, propyl or isopropyl group, and M.sup.++ is calcium, alone or in combination with at least one of the fumaric acid alkyl ester salts as defined above, M.sup.++ is selected from the group consisting of magnesium, zinc and iron. The combination includes, by weight, 10-250 parts, 0-50 parts magnesium, and 0-50 parts zinc or iron salt of fumaric acid monoalkylester, in an amount of fumaric acid not exceeding 300 mg. per dosage form, in combination with ordinary pharmaceutically compatible solid adjuvants and vehicles.Type: GrantFiled: August 31, 1993Date of Patent: June 13, 1995Inventors: Peter P. Speiser, Rajendra K. Joshi
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Patent number: 5422115Abstract: Methods of treatment of the human or animal body are provided to combat conditions responsive to lithium and/or C.sub.18-22 polyunsaturated fatty acid therapy, including conditions associated with essential lithium deficiency, and also transfer of lipid-enveloped viruses between humans or animals or between cells within a human or animal body. The methods include administration of an effective amount of a lithium salt of a C.sub.18-22 polyunsaturated fatty acid. Devices for combatting transmission of viral diseases including lithium salts of a C.sub.18-22 polyunsaturated fatty acid are also provided.Type: GrantFiled: October 20, 1992Date of Patent: June 6, 1995Assignee: Efamol Holding PLCInventor: David F. Horrobin
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Patent number: 5411743Abstract: Adhesions in synovial capsules are prevented through the administration of liposome intercalated nonsteroidal anti-inflammatory agents.Type: GrantFiled: November 23, 1993Date of Patent: May 2, 1995Assignee: Vestar, Inc.Inventors: Larry J. Moore, Jill Adler-Moore
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Patent number: 5409914Abstract: The present invention provides a pharmaceutical composition of a complex compound having the structure: ##STR1## wherein R.sub.1 and R.sub.1, are the same or different and each is an alkyl group, a phenyl group or a substituted derivative of a phenyl group;wherein R.sub.2 and R.sub.2, are the same or different and each is hydrogen, an unbranched alkyl group, a halide or a group having the structure ##STR2## wherein R is hydrogen, an alkoxide group, an alkyl group, or OH; wherein R.sub.3 and R.sub.3, are the same or different and each is hydrogen or an alkyl group;wherein X and X' are the same or different and each is a water soluble group having weak to intermediate ligand field strength; andQ is a soluble, pharmaceutically acceptable negative ion.Type: GrantFiled: November 1, 1993Date of Patent: April 25, 1995Assignee: Chai-Tech CorporationInventors: Zvi Dori, David Gershon
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Patent number: 5409709Abstract: An ibuprofen-containing antipyretic analgesic preparation blending 0.01-30 parts by weight of acetaminophen based on 1 part by weight of ibuprofen, 0.05-100 parts by weight of magnesium-based antacids based on 1 part by weight of the total amount of ibuprofen and acetaminophen, and/or 0.01-30 parts by weight of at least one sedative selected from bromovalerylurea and allylisopropylacetylurea based on 1 part by weight of ibuprofen.Type: GrantFiled: November 25, 1992Date of Patent: April 25, 1995Assignee: Lion CorporationInventors: Kiyotaka Ozawa, Ryoko Sugita, Kiyo Adachi, Tomiyuki Yanase, Syuichi Ueda, Aya Yamane
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Patent number: 5409932Abstract: The piperazine-substituted pyrroloanthracenes are prepared by reacting either furanoanthracenes with piperazinalkylamines or reacting unsubstituted pyrroloanthracenes first with dihalogenoalkyl compounds and then with appropriately substituted piperazines or by reacting furan derivatives first with piperazinalkylamines and then condensing with anthracenes. The new compounds can be employed as active ingredients in medicaments, in particular in immunomodulators.Type: GrantFiled: December 9, 1993Date of Patent: April 25, 1995Assignee: Bayer AGInventors: Eckhard Schwenner, Gaetan Ladouceur, Hans-Joachim Kabbe, Thomas M. Aune
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Patent number: 5403592Abstract: A composition comprised of at least one surface active phospholipid, hyaluronic acid or a water soluble salt thereof in saline solution for use as a lubricant, in particular, for physiological use such as the lubrication of joints. The composition can be used to reduce the coefficient of kinetic friction between surfaces in contact with each other, particularly load-bearing surfaces.Type: GrantFiled: June 8, 1990Date of Patent: April 4, 1995Assignee: MacNaught Pty LimitedInventor: Brian A. Hills
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Patent number: 5403859Abstract: The invention concerns a heterocyclic derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (1-6C)alkenylene, (3-6C)alkynylene or cyclo-(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X--A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 7 ring atoms, wherein A.sup.2 and A.sup.3 is (1-4C)alkylene and X is oxy;or a pharmaceutically-acceptable salt thereof.These compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: April 29, 1993Date of Patent: April 4, 1995Assignees: Imperial Chemical Industries plc, ICI PharmaInventors: Philip N. Edwards, Jean-Marc M. M. Girodeau
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Patent number: 5401728Abstract: A soybean lecithin based topical liniment and method of making the same is disclosed. The liniment utilizes soybean lecithin as a base and major ingredient and as the emulsifier which is mixed with plant oils, natural menthol, calcium stearate, and magnesium stearate. The soybean lecithin, plant oils, natural menthol, calcium stearate, and magnesium stearate are mixed together in predetermined relative proportions with the amount of soybean lecithin being greater than the sum of the amounts of the plant oils, natural menthol, calcium stearate, and magnesium stearate. The soybean lecithin, plant oils, natural menthol, calcium stearate, and magnesium stearate are added to one another and mixed together in a predetermined sequence to prevent precipitation and provide a homogenous mixture having a viscosity suitable for topical application.Type: GrantFiled: June 9, 1993Date of Patent: March 28, 1995Inventor: John A. Simon
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Patent number: 5399347Abstract: The present invention is directed to a method and pharmaceutical formulations for the treatment of autoimmune arthritis and animal models therefore in mammals, including humans, by the oral, enteral or by-inhalation administration of whole collagen protein or biologically active peptide fragments of collagen.Type: GrantFiled: September 25, 1992Date of Patent: March 21, 1995Assignee: Autoimmune, Inc.Inventors: David E. Trentham, Howard L. Weiner, David A. Hafler
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Patent number: 5397778Abstract: The present invention features saponin containing enteral formulations for treatment of infection and inflammation. These saponin containing formulations are particularly useful in conjunction with oils rich in .omega.3 polyunsaturated fatty acids such as fish oils and flax oil but also show benefits with .omega.6 rich oils such as borage oil, black currant seed oil, canola oil and rapeseed oil. These formulations may also contain a lignan from the sesamin family.Type: GrantFiled: April 15, 1994Date of Patent: March 14, 1995Assignee: New England Deaconess Hospital CorporationInventors: R. Armour Forse, Sambasiva Chavali
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Patent number: 5393775Abstract: A compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and n are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same for treating a mammal afflicted with a disorder connected with peroxydation processes and biosynthesis of eicosanoids.Type: GrantFiled: September 7, 1993Date of Patent: February 28, 1995Assignee: Adir et CompagnieInventors: Guillaume Le Baut, Jean-Paul Babingui, Sylvie Robert-Piessard, Pierre Renard, Daniel-henri Caignard, jean-Francois Renaud de la Faverle, Gerard Adam
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Patent number: 5389617Abstract: A method for treating patients with rheumatoid arthritis comprises administering azaribine to the patient at a dosage level of 10 to 50 mg/kg/day for an initial period of from about 1 to about 3 weeks and then administering azaribine to the patient at dosage levels of at least 50 mg/kg/day and preferably at least 100 mg/kg/day.Type: GrantFiled: November 12, 1993Date of Patent: February 14, 1995Assignee: UR Labs, Inc.Inventor: William Drell
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Patent number: 5384119Abstract: Oligomers of the formula ##STR1## have demonstrated effectiveness in preventing connective tissue damage.Type: GrantFiled: October 29, 1993Date of Patent: January 24, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Michael J. Janusz
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Patent number: 5384134Abstract: There is disclosed a method for treating dermatologic diseases caused by microbial overgrowth or inflammation, such as psoriasis, fungal infections, eczema, dandruff, acne, genital herpes lesions, and leg ulcers. There is further disclosed an antiviral lubricating composition that is effective in preventing the transmission of the HIV virus and other sexually transmitted diseases. There is also disclosed systemic anti-inflammatory compositions and formulations and a method for reducing tissue inflammation in tissues such as the bowel, muscle, bone, tendon and joints (e.g., arthritis).Type: GrantFiled: September 1, 1993Date of Patent: January 24, 1995Assignee: Alcide CorporationInventors: Robert D. Kross, Elliott J. Siff
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Patent number: 5368841Abstract: A method of treating proliferative diseases of the synovial joint using photodynamic therapy. In particular the method of the invention may be used to destroy synovial tissue in inflammatory joint conditions associated with diseases such as rheumatoid arthritis, lupus erythematosus and other rheumatoid variants. A number of methods of delivery are provided, some of which are non invasive.Type: GrantFiled: February 11, 1993Date of Patent: November 29, 1994Assignee: The General Hospital CorporationInventors: Kenneth Trauner, Tayyaba Hasan
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Patent number: 5362732Abstract: A novel class of pharmaceutically active boronated compounds are provided. The boronated compounds include boronated purine and pyrimidine bases and boronated nucleosides, as well as phosphate esters and oligomers thereof. The compounds are boronated at the ring nitrogen of the purine or pyrimidine base, or at a 2', 3' or 5' amino substituent of the nucleoside sugar.Type: GrantFiled: July 7, 1992Date of Patent: November 8, 1994Assignees: University of North Carolina at Chapel Hill, Boron Biologicals, Duke UnversityInventors: Bernard F. Spielvogel, Anup Sood, Iris H. Hall, Barbara R. Shaw, Jeno Tomasz
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Patent number: 5358720Abstract: A regimented therapeutic method for he alleviation of arthritic conditions by orally administering a selective combination of vitamins and minerals in scheduled dosage amounts. The daily scheduled regiment involves the administration of about 25-100 mg of nicotinic acid three times per day, about 200-1000 mg of calcium ascorbate three times a day, and a single dosage form of a copper-free multivitamin with multiminerals to be taken once a day.Type: GrantFiled: October 22, 1993Date of Patent: October 25, 1994Inventors: Richard M. Koppel, Karl Verebey
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Patent number: 5352676Abstract: This invention relates to a method of treating rheumatoid arthritis, which method comprises administering to a mammal a therapeutically effective amount of a compound of formula (I): ##STR1## wherein R1 is unsubstituted or substituted phenyl;R.sub.2 is a morpholinomethyl group;R.sub.3 is hydrogen;R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.a is hydrogen; andR.sub.b is a group --(A).sub.m --R.sub.5 wherein m is zero or 1, A is a C.sub.1 -C.sub.6 alkylene chain and R.sub.5 is unsubstituted or substituted phenyl;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 1, 1993Date of Patent: October 4, 1994Assignee: Farmitalia Carlo Erba SrlInventors: Gianfederico Doria, Anna M. Isetta, Rinaldo Ferreccio, Mario Ferrari, Maria C. Fornasiero, Domenico Trizio
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Patent number: 5348729Abstract: The present invention is directed to a method for testing the susceptibility of a mammal to inflammatory diseases which comprises the steps of:administering to a mammal a compound selected from the group consisting of Type 1 mineralocorticoid receptor antagonists, opiate antagonists, estrogen antagonists or mixed estrogen agonists/antagonists, progesterone agonists; or a combination of an estrogen antagonist with one or a combination of a Type I glucocorticoid receptor antagonist, a Type II glucocorticoid agonist or a progesterone agonist which is effective in stimulating the hypothalamic-pituitary-adrenal (HPA) axis; andmeasuring the level of at least one hormone secreted by the hypothalamus, pituitary or adrenal glands of said mammal.The present invention is also directed to methods of treating inflammatory diseases.Type: GrantFiled: May 5, 1992Date of Patent: September 20, 1994Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Esther M. Sternberg, Philip W. Gold, Samuel W. Page
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Patent number: 5342615Abstract: Interleukin-1.alpha. (IL-1-.alpha.) and derivatives, and their pharmaceutical compositions for use in treating arthritis or inflammation.Type: GrantFiled: July 30, 1990Date of Patent: August 30, 1994Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Satoru Nakai, Yoshikatsu Hirai
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Patent number: 5342614Abstract: Interleukin-1.beta. (IL-1.beta.) and derivatives, and their pharmaceutical compositions for use in treating arthritis or inflammation.Type: GrantFiled: March 26, 1990Date of Patent: August 30, 1994Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Satoru Nakai, Yoshikatsu Hirai
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Patent number: 5340821Abstract: A composition for treating a Sjoegren syndrome disease is disclosed. The composition comprising derivative of spirooxathiolane-quinuclidine of the following formula (I), ##STR1## wherein Z is .dbd.CR.sup.1 R.sup.2, wherein R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen, alkyl, cyclopentyl, cyclohexyl, aryl, diarylmethylol, or alkyl which may be substituted by one or more aryl groups, or an acid addition salt thereof, or an acid addition salt thereof, as an effective component. Especially effective is an administration of a hydrochloric acid addition salt of 2-methylspiro(1,3-oxathiolane-5,3')quinuclidine.Type: GrantFiled: July 7, 1993Date of Patent: August 23, 1994Assignee: Snow Brand Milk Products Co., Ltd.Inventors: Nobuaki Abe, Yasuyoshi Takeshita
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Patent number: 5334617Abstract: The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products 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 are amino acids and their derivatives which contain an active nitrogen-containing group. Particular agents comprise lysine and mixtures thereof. 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: January 27, 1992Date of Patent: August 2, 1994Assignees: The Rockefeller University, Alteon Inc.Inventors: Peter C. Ulrich, Anthony Cerami
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Patent number: 5322838Abstract: The present invention relates to the use of INHIB in the detection and inhibition of inflammation. INHIB is structurally identical to the C3 .beta.-chain.Type: GrantFiled: October 16, 1991Date of Patent: June 21, 1994Assignee: Brigham & Women's HospitalInventors: David S. Silberstein, Marjorie Minkoff
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Patent number: 5321045Abstract: The invention concerns thiosulphinic acid derivatives, medicaments containing these compounds and their use in medicine. It has been found that thiosulphinic acid derivatives display outstanding inflammation-inhibiting properties. The compounds prove to be especially advantageous in the treatment of PAF-induced inflammatory processes of the bronchial area.Type: GrantFiled: March 14, 1989Date of Patent: June 14, 1994Assignee: Boehringer Mannheim GmbHInventors: Walter Dorsch, Hildebert Wagner
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Patent number: 5321017Abstract: A method for treating mammals suffering from rheumatoid arthritis and other tissue-destructive (chronic inflammatory or other) conditions associated with excess metalloproteinase activity comprising administering to the mammal an amount of a tetracycline that is effectively anti-metalloproteinase, but that is not effectively antimicrobial, and an amount of non-steroidal anti-inflammatory agent which, when combined with the effectively anti-metalloproteinase amount of tetracycline, results in a significant reduction of tissue destruction and/or bone loss.Type: GrantFiled: August 12, 1991Date of Patent: June 14, 1994Assignee: The Research Foundation of State University of New YorkInventors: Lorne M. Golub, Nangavarum S. Ramamurthy, Thomas F. McNamara, Robert A. Greenwald
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Patent number: 5314894Abstract: (S)-(+)-Hydroxychloroquine substantially free of (R)-(-)-hydroxychloroquine, or a pharmaceutically acceptable acid-addition salt thereof and a method of use thereof and a composition containing it for the treatment of malaria, lupus erythematosus or rheumatoid arthritis.Type: GrantFiled: September 15, 1992Date of Patent: May 24, 1994Assignee: Sterling Winthrop Inc.Inventors: Vera J. Stecher, William F. Michne
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Patent number: 5308837Abstract: The present invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of certain 5'-amine substituted adenosine analogs.Type: GrantFiled: November 12, 1992Date of Patent: May 3, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Terry L. Bowlin
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Patent number: 5304549Abstract: Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.Type: GrantFiled: January 21, 1992Date of Patent: April 19, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
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Patent number: 5298494Abstract: Derivatives of simple monosaccharides which exhibit anti-proliferative and/or anti-inflammatory activity and are useful for treating mammals having inflammatory disorders and/or autoimmune disorders. This invention also encompasses pharmaceutical compositions containing these compounds and methods of treating inflammatory and/or autoimmune disorders.Type: GrantFiled: June 30, 1993Date of Patent: March 29, 1994Assignee: Greenwich Pharmaceuticals IncorporatedInventors: Sudershan K. Arora, Roy L. Whistler, Albert V. Thomas
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Patent number: 5298521Abstract: 1,5-Diphenyl-3-pyrazolylalkyl-N-hydroxydithiocarbamates of the general formula: ##STR1## are disclosed to have anti-inflammatory activity in mammals.Type: GrantFiled: August 30, 1993Date of Patent: March 29, 1994Assignee: Ortho Pharmaceutical CorporationInventor: Michael Ferro
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Patent number: 5281623Abstract: Provided are methods of treating inflammation, arthritis and muscular dystrophy and preventing ischemia-induced cell damage employing certain phenol and benzamide compounds.Type: GrantFiled: August 27, 1990Date of Patent: January 25, 1994Assignee: Eli Lilly and CompanyInventors: James A. Clemens, Jill A. Panetta
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Patent number: 5278183Abstract: A pharmaceutical composition for the treatment of autoimmune diseases comprising an effective amount of a compound of formulaA--CH.sub.2 --O--CRR'--COOR"' (I)whereA is the nucleus of 1-benzyl-indazol-3-yl,R and R', the same or different from each other, are H or an alkyl having from 1 to 5 carbon atoms,R"' is H or an alkyl having from 1 to 4 carbon atoms,or, when R"' is H, of a salt thereof with organic or inorganic pharmaceutically acceptable bases.Type: GrantFiled: April 14, 1992Date of Patent: January 11, 1994Assignee: Instituto Ricerca Francesco Angelini S.p.A.Inventor: Bruno Silvestrini
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Patent number: 5273742Abstract: A method for treating a body condition comprising introducing an aqueous solution of a water soluble polyether polyurethane into said body condition.Type: GrantFiled: December 30, 1991Date of Patent: December 28, 1993Assignee: Tyndale Plains-Hunter Ltd.Inventors: Francis E. Gould, Murray H. Reich
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Patent number: 5266564Abstract: There is described the production of a pharmaceutical composition for the eatment of autoimmune diseases, whereby multiple sclerosis is excluded. As active materials, there are thereby used compounds of the general formula I ##STR1## in which R.sub.1 represents alkyl with 12 to 18 carbon atoms, R.sub.2 alkyl with 1 to 8 carbon atoms and R.sub.3 H or alkyl with 1 to 3 carbon atoms.Type: GrantFiled: December 23, 1991Date of Patent: November 30, 1993Assignee: Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften E. V.Inventors: Manuel Modolell, Gerhard Munder
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Patent number: 5262161Abstract: A medicine for skin diseases contains a fermented and condensed extract from the stems of Stevia Rebaudiana Bertoni as an active ingredient. The medicine is prepared by condensing and fermenting an extract from the ripened stems of Stevia Rebaudiana Bertoni by multi-stage condensation followed by fermentation and ripening of the condensed extract. It is effective for various skin diseases and other diseases caused by blood circulation insufficiency.Type: GrantFiled: September 30, 1991Date of Patent: November 16, 1993Assignees: Fumio Dozono, Naohiko SatoInventor: Fumio Dozono
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Patent number: 5260328Abstract: Heteroaryl-3-oxo-propanenitrile derivatives of formula (I) ##STR1## wherein X represents an oxygen atom or a --CH(R.sub.4)--, --O--CH(R.sub.4)--, --S(O).sub.n --CH(R.sub.4)--, --CH(R.sub.4)--O--, --CH(R.sub.4)--S(O).sub.n -- or --CH(R.sub.4)--CH.sub.2 -- group wherein n is 0, 1 or 2; R.sub.1 represents C.sub.1 -C.sub.6 alkyl, pyridyl or unsubstituted or substituted phenyl; R.sub.2, R.sub.3, and R.sub.4 are as herein defined; and Q is hydrogen, carboxy, C.sub.2 -C.sub.7 -alkoxycarbonyl or a --CON(R.sub.a)R.sub.b group, R.sub.a and R.sub.b being as defined herein; and their pharmaceutically acceptable salts are useful in the preparation of pharmaceutical compositions active in the treatment of autoimmune diseases.Type: GrantFiled: November 6, 1992Date of Patent: November 9, 1993Assignee: Farmitalia Carlo Erba SrlInventors: Gianfederico Doria, Anna Maria Isetta, Rinaldo Ferreccio, Mario Ferrari, Maria C. Fornasiero, Domenico Trizio
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Patent number: 5258371Abstract: Provided is a method of treating humans or animals suffering from a condition or disease characterized by excessive collagen destruction, which comprises administering to said human or animal an effective amount of a 12a-deoxytetracycline represented by the following general formula ##STR1## The method is effective in the treatment of various articular diseases characterized by excessive collagen destruction.Type: GrantFiled: May 29, 1992Date of Patent: November 2, 1993Assignee: Kuraray Co., Ltd.Inventors: Lorne M. Golub, Nangavarum S. Ramamurthy, Thomas F. McNamara, Robert A. Greenwald, Tsutomu Kawai, Takashi Hamasaki, Michiya Shimamura, Goro Kobayashi, Tetsuo Takigawa, Hisashi Iwata