Polycyclo Ring System Patents (Class 514/577)
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Patent number: 6365625Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.Type: GrantFiled: September 17, 1999Date of Patent: April 2, 2002Assignee: Procept, Inc.Inventors: Shyam K. Singh, Raymond J. Patch, Peter V. Pallai, Edith A. Neidhardt, Gerard P. Palace, Kevin J. Willis, Theresa M. Sampo, Kevin W. McDonald, Zhan Shi
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Publication number: 20020035068Abstract: Anticonvulsant derivatives useful in treating autism.Type: ApplicationFiled: January 18, 2000Publication date: March 21, 2002Inventor: Daniel P. Van Kammen
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Publication number: 20010005760Abstract: The naphthyloxyacetic acid derivatives of the formula (I) 1Type: ApplicationFiled: January 22, 2001Publication date: June 28, 2001Inventors: Yuuki Nagao, Kazuhiko Torisu, Nobuyuki Hamanaka
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Patent number: 6248749Abstract: The invention concerns tye use of a inhibitor of retinoic acid as sole ingredient in a pharmaceutical or cosmetic composition comprising administering effective amount of the composition to treat sensitive skin or skin damage induced by UV radiation.Type: GrantFiled: September 4, 1998Date of Patent: June 19, 2001Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Michel Demarchez, André Jomard
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Patent number: 6210686Abstract: Yeast-derived fiber has been demonstrated, as described herein, to effectively improve the serum lipid profile in humans, when provided as a dietary supplement, without some of the disadvantages known to accompany dietary supplementation with oat fiber or psyllium fiber. Described herein are dietary supplements comprising yeast fiber, e.g., &bgr;-glucan or glucomannan, and further comprising folic acid or a salt thereof, vitamin B6, vitamin B12, and vitamin E. The dietary supplements of the invention can further comprise fats, carbohydrates and proteins, for example, and other ingredients added to formulate a food product. Such food products can be in the form, for example, of solid or semi-solid foods, such as food bars, pudding, or spreads. By including folate and vitamin B6, the dietary supplement provides a second benefit of suppressing the level of homocysteine in the blood.Type: GrantFiled: December 18, 1998Date of Patent: April 3, 2001Assignee: Beth Israel Deaconess Medical CenterInventors: Stacey J. Bell, R. Armour Forse, Bruce R. Bistrian
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Patent number: 6121322Abstract: The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I.The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.Type: GrantFiled: November 24, 1998Date of Patent: September 19, 2000Assignee: Boehringer Mannheim GmbHInventors: Joachim Dickhaut, Walter-Gunar Friebe, Frank Grams, Rainer Haag, Herbert Leinert
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Patent number: 6121320Abstract: A method of treating leukemia which includes administering an effective amount of composition comprising suramin and a biological response modifier, wherein the suramin and the biological response modifier show synergistic or additive anti-leukemic activity. A pharmaceutical composition is also disclosed.Type: GrantFiled: February 26, 1998Date of Patent: September 19, 2000Assignee: The University of Kentucky Research FoundationInventor: Michael A. Doukas
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Patent number: 6075050Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.Type: GrantFiled: June 6, 1995Date of Patent: June 13, 2000Assignee: Procept, Inc.Inventors: Shyam K. Singh, Raymond J. Patch, Peter V. Pallai, Edith A. Neidhardt, Gerard P. Palace, Kevin J. Willis, Theresa M. Sampo, Kevin W. McDonald, Zhan Shi
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Patent number: 6063797Abstract: The use of a combination of an alpha RAR receptor-specific agonist ligand and a gamma RAR receptor-specific antagonist ligand to reduce the rate of apoptosis is disclosed.Type: GrantFiled: July 15, 1998Date of Patent: May 16, 2000Assignee: C.I.R.D. GaldermaInventors: Laszlo Fesus, Zsuzsa Szondy, Uwe Reichert
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Patent number: 5958972Abstract: Tricyclic compounds are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.Type: GrantFiled: May 20, 1997Date of Patent: September 28, 1999Assignee: Warner-Lambert CompanyInventors: Donald Hupe, Linda Lea Johnson, Joseph Armand Picard, Andrew David White, Qi-Zhuang Ye
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Patent number: 5891905Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.Type: GrantFiled: April 14, 1997Date of Patent: April 6, 1999Assignee: Mars, IncorporatedInventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
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Patent number: 5861385Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.Type: GrantFiled: August 8, 1995Date of Patent: January 19, 1999Assignee: Bayer AktiengesellschaftInventors: Rolf Angerbauer, Peter Fey, Walter Hubsch, Thomas Philipps, deceased, Hilmar Bischoff, Hans-Peter Krause, Jorg Petersen von Gehr, Delf Schmidt
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Patent number: 5849727Abstract: This invention relates to a new and improved pharmaceutical composition and method for delivery of therapeutic or bioactive agents. The methods and composition of the invention can be used with several therapeutic or bioactive agents and can achieve site-specific delivery of a therapeutic or biologically-active substance. This can allow for lower doses and for improved efficacy with drugs, particularly agents such as oligonucleotides which are plagued with problems in achieving therapeutic levels at targeted sites.Type: GrantFiled: June 28, 1996Date of Patent: December 15, 1998Assignee: Board of Regents of the University of NebraskaInventors: Thomas R. Porter, Patrick L. Iversen
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Patent number: 5776888Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: February 7, 1997Date of Patent: July 7, 1998Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Eric Wang, Donald J. Sarubbi, Harry Leipold
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Patent number: 5750577Abstract: Novel medicinally-useful compounds are provided herein. These compounds include isomeric cyclic tetramers of formaldehyde and 1-naphthol, and the derivatives or analogues of such cyclic tetramers, and linear oligomers of chromotropic acid, or its derivatives or analogues with naphthalene.Type: GrantFiled: December 5, 1996Date of Patent: May 12, 1998Assignee: Seabright Corporation LimitedInventor: Paris Georghiou
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Patent number: 5698595Abstract: Application of a compound having at least one sulfonic acid functional group which is at least partially non-neutralized, in a cosmetic or dermatological composition, to the skin is useful for treating intrinsic ageing of the skin.Type: GrantFiled: December 19, 1996Date of Patent: December 16, 1997Assignee: L'OrealInventors: Jean Paul Boelle, Jean-Pierre Laugier, Serge Forestier
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Patent number: 5690967Abstract: Compositions for improved topical delivery of lactic acid comprising lactic acid and an amphoteric or pseudoamphoteric agent.Type: GrantFiled: June 7, 1995Date of Patent: November 25, 1997Assignee: Tristrata Technology, Inc.Inventors: Ruey J. Yu, Eugene J. Van Scott
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Patent number: 5684035Abstract: The invention is directed to a method of killing or inhibiting the growth of the malaria-causing pathogen Plasmodium falciparum by exposing the pathogen to an effective amount of a preparation comprising a compound selected from the group consisting of:a) a compound of formula I: ##STR1## where ##STR2## b) a compound of formula II; ##STR3## where each R' is --H or each R' is --OH; and c) a compound of formula III; ##STR4## where R" is --NH.sub.2, --H, or --SO.sub.3 M, and where M is H, Na, or K.Type: GrantFiled: July 17, 1996Date of Patent: November 4, 1997Inventor: Govind J. Kapadia
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Patent number: 5677343Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalene-sulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.Type: GrantFiled: June 6, 1995Date of Patent: October 14, 1997Assignee: Procept, Inc.Inventors: Shyam K. Singh, Raymond J. Patch, Peter V. Pallai, Edith A. Neidhardt, Gerard P. Palace, Kevin J. Willis, Theresa M. Sampo, Kevin W. McDonald, Zhan Shi
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Patent number: 5650167Abstract: Disclosed is a method of inhibiting hepatitis B infection by administering a therapeutically effective amount of a compound having the formula (Formula 1): ##STR1## wherein R1 is selected from the group consisting of H, lower alkanoyl, lower arylalkylacyl, arylacyl, and C-1-linked saccharide, and R2 is separately selected from the group consisting of H, lower alkyl, lower arylalkyl, aryl, and C-1-linked saccharide. The compounds may also be used to treat other conditions, such as inflammatory bowel disease, autoimmune diseases, transplant rejection, septic shock, and for protection against irradiation damage. Novel celastrol derivatives are also disclosed.Type: GrantFiled: November 16, 1995Date of Patent: July 22, 1997Assignee: DAWA IncorporatedInventor: Anthony C. Allison
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Patent number: 5639773Abstract: This invention relates to an ocular hypotensive agent which comprises a compound represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen or an optionally substituted hydrocarbon residue that may be bound via a hetero atom; R.sup.2 represents hydrogen or a hydrocarbon residue that may have a substituent; R.sup.3 represents a group capable of forming an anion or a group capable of changing thereto; X is a covalent bond between the 2 benzene rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n represents 1 or 2; ring A is a benzene ring having 1 or 2 optional substituents in addition to the group represented by COOR.sup.2, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 1, 1994Date of Patent: June 17, 1997Assignees: Senju Pharmaceutical Co., Ltd., Takeda Chemical Industries, Ltd.Inventors: Keiji Kubo, Takahiro Ogawa, Takaaki Deguchi
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Patent number: 5614559Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalene-sulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.Type: GrantFiled: May 19, 1994Date of Patent: March 25, 1997Assignee: Procept Inc.Inventors: Shyam K. Singh, Raymond J. Patch, Peter V. Pallai, Edith A. Neidhardt, Gerard P. Palace, Kevin J. Willis, Theresa M. Sampo, Kevin W. McDonald, Zhan Shi
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Patent number: 5580857Abstract: The use of active gibberellins for the preparation of a pharmaceutical composition for the treatment of prostatitis. The method results in a decrease in prostate mass.Type: GrantFiled: January 24, 1994Date of Patent: December 3, 1996Inventor: Per Oden
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Patent number: 5563129Abstract: There are disclosed novel hydroquinone derivatives of the formula: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments.Type: GrantFiled: April 24, 1995Date of Patent: October 8, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirotomo Masuya, Masayoshi Yamaoka
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Patent number: 5550145Abstract: An antimicrobial composition comprising an antimicrobially effective amount of a combination of: A) a monoglyceride of lauric acid, a monoglyceride of monomyristic acid or a mixture of these monoglycerides, and B) at least one chemical substance selected from the following groups: i) local anesthetics of the amide type; ii) carbamide, iii) antibacterial substances in the form of steroid antibiotics, imidazole derivatives or nitroimidazole derivatives, and iv) diols with 3-6 carbon atoms, and C) optionally, a conventional physiologically acceptable carrier and/or physiologically acceptable additives. A process for the preparation of this composition by heating (A) to the transition temperature of the lipid, adding (B), and optionally (C), and cooling the mixture to form a solid lipid crystal composition. Use of the composition for the preparation of a dermatological preparation for combatting bacteria and fungi or as a preservative additive in a cosmetic product, a food product, or a medical product.Type: GrantFiled: September 27, 1994Date of Patent: August 27, 1996Assignee: Bioglan ABInventors: Karin Olund, Lena-Karin L utz, Rickard Bryland, .ANG.ke Lindahl
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Patent number: 5514710Abstract: The invention describes the synthesis and use of photoactivated (or caged) fluorescent dyes. Upon illumination at less than about 400 nm the caged dyes release highly fluorescent, water soluble hydroxypyrenesulfonic acid dyes according to the following equation: ##STR1## X, Y, and Z are independently sulfonic acid, a sulfonic acid salt, a hydroxyl group, or hydrogen, with at least one of X, Y, and Z being a sulfonic acid or sulfonic acid salt. LINK is either an ether linkage or a carbonate linkage. BLOCK is a caging group whose photolysis results in liberation of a free hydroxypyrenesulfonic acid dye.The caged fluorescent dyes are useful for application in aqueous solutions, including fluids of biological origin. The caged dyes of the present invention are especially useful for flow tagging velocimetry.Type: GrantFiled: January 11, 1994Date of Patent: May 7, 1996Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Kyle R. Gee
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Patent number: 5491134Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: A is a bond or --OCH.sub.2 --, where the oxygen is linked to R.sup.1 ;B is --CH.sub.2 -- or when R.sup.3 is hydrogen, B may be --CH.sub.2 O-- where the oxygen is linked to the phenyl ring;R.sup.1 is an aryl group;R.sup.2 is hydrogen or lower alkyl;R.sup.3 is hydrogen; or R.sup.2 and R.sup.3 together form the group --CH.sub.2 CH.sub.2 --; andR.sup.4 is --SO.sub.3 H, --P(O.sub.2 H)R.sup.5, --P(O.sub.2 R.sup.5')R.sup.5, --PO.sub.3 H.sub.2, --PO.sub.3 HR.sup.5' or --PO.sub.3 (R.sup.5').sub.2 where R.sup.5 and R.sup.5' are independently lower alkyl. These compounds are beta.sub.3 adrenergic receptor agonists and are useful, for example, in the treatment of diabetes, obesity, achalasia, and gastrointestinal diseases.Type: GrantFiled: September 16, 1994Date of Patent: February 13, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, Arvind Mathur
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Patent number: 5489612Abstract: Calixarene derivatives, their synthesis and use as chloride channel blockers are described. Preferred calixarene derivatives are of the formula: ##STR1## wherein R is an acidic group or salt thereof, such as SO.sub.3 X or R.sup.1 SO.sub.3 X where X is H or Na, and R.sup.1 is ##STR2## where m=1-2, and R.sup.3 and R.sup.4 the same or different is each H or a C.sub.1-4 alkyl, or a nitrogen-containing group of the formula ##STR3## or A, wherein R.sup.5 is a C.sub.1-4 alkyl, R.sup.6 is a C.sub.1-4 alkyl and A is ##STR4## where R.sup.7 and R.sup.8, the same or different each is H or a C.sub.1-4 alkyl, and R.sup.9 and R.sup.10, the same or different, each is H or a C.sub.1-4 alkyl; R' is H or a C.sub.1-4 alkyl; and n is an integer of 4-8, preferably 4, 6 or 8.Type: GrantFiled: January 7, 1994Date of Patent: February 6, 1996Assignee: The University of Alabama at Birmingham Research FoundationInventors: Jerry L. Atwood, Robert J. Bridges, Ravindra K. Juneja, Ashvani K. Singh
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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: 5453444Abstract: The present invention relates to methods for treating cachexia in a patient and inhibiting IL-6 bioactivity. This is accomplished by administering to a patient an effective amount of a sulfate-containing compound, for example, suramin, a derivative of suramin, Pentosan polysulfate, or Dextran sulfate. The present invention is also effective in combating IL-6 related diseases.Type: GrantFiled: October 6, 1994Date of Patent: September 26, 1995Assignee: Otsuka Pharmaceutical Co., Ltd.Inventor: Gideon Strassmann
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Patent number: 5424063Abstract: The narrow poly- or mono-dispersed oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a recurring unit of from 3 to 50. These oligomers are water-soluble, preferably have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geometry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The narrow poly- or mono-dispersed oligomers are useful for the treatment and/or diagnosis of AIDS and/or ARC or HSV.Type: GrantFiled: January 9, 1992Date of Patent: June 13, 1995Assignees: The Dow Chemical Company, Merrell Dow Pharmaceuticals, Inc.Inventors: Alan D. Cardin, William A. Fordyce, Michael J. Mullins, Thomas A. Chamberlin, Michael J. Fazio
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Patent number: 5312837Abstract: A method for inhibiting cell infection by an enveloped virus, by administering to an infection site, a therapeutically effective amount of a macrocyclic compound composed of aryl ring subunits connected one to another by ring-attached bridge linkages, and containing sulfonic acid-derived substituents carried on non-bridge atoms of the subunits.Type: GrantFiled: November 13, 1991Date of Patent: May 17, 1994Assignee: Genelabs Technologies, Inc.Inventors: Kou M. Hwang, You M. Qi, Su-Ying Liu
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Patent number: 5281628Abstract: 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.Type: GrantFiled: October 4, 1991Date of Patent: January 25, 1994Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
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Patent number: 5196452Abstract: A compound and method for inhibiting cell infection by an enveloped virus. The compound is a macrocyclic chromotropic acid derivative which can be substituted at a variety of naphthalene ring and bridge positions. The compound may be administered parenterally, orally, or topically for treating infection by enveloped viruses.Type: GrantFiled: January 29, 1991Date of Patent: March 23, 1993Assignee: Genelabs IncorporatedInventors: Kou M. Hwang, You M. Qi, Su-Ying Liu
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Patent number: 5166173Abstract: A method of inhibiting cell infection by herpes simplex virus-1 or -2. The method includes contacting the virus with a macrocyclic chromotropic acid compound, in an amount effective to inhibit cell infectivity of the virus.Type: GrantFiled: January 29, 1991Date of Patent: November 24, 1992Assignee: Genelabs IncorporatedInventors: Kou M. Hwang, You M. Qi, Su-Ying Liu
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Patent number: 5081152Abstract: A series of new azulene analogues are disclosed, which are represented by the following formula: ##STR1## wherein: R.sub.1 is --COOH, --COOR.sub.4 (R.sub.4 represents a lower alkyl), --CH.dbd.CH--COOH, --CH.sub.2 --COOH or --SO.sub.3 H;R.sub.2 is a hydrogen atom or lower-alkyl group;R.sub.3 is a hydrogen atom, a lower alkyl or benzyl group;A is --SO.sub.2 --, ##STR2## (R.sub.5 represents a lower alkyl); B is a phenyl, a lower alkylphenyl, a lower alkoxyphenyl, nitrophenyl, trifluoroalkylphenyl, mono-or di-halogenated-phenyl, naphthyl or tetrahydroaphthyl group;Y is an alkylene or alkenylene group.The compounds of the present invention are useful as thromboxane A.sub.2 and prostagrandin endoperoxide receptor antagonists.Type: GrantFiled: June 26, 1990Date of Patent: January 14, 1992Assignee: Kotobuki Seiyaku Co., Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Masayuki Yokota, Shuuichi Wakabayashi, Hiromi Hayashi, Rei Koyama, Masafumi Yasunami
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Patent number: 4988731Abstract: This invention concerns certain diethyl- or dipropylacetic acid salts of sodium valproate which have physiological properties similar to those of valproic acid or sodium valproate but show highly superior stability characteristics.Type: GrantFiled: November 9, 1987Date of Patent: January 29, 1991Assignee: Abbott LaboratoriesInventor: Edwin M. Meade
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4923893Abstract: External preparations consisting essentially of about 0.1% to about 5% of tocopherol acetate and/or about 0.05% to about 0.3% of glycyrrhetinic acid, about 1% to about 15% of a methacrylic acid-ethyl acrylate copolymer, and about 0.2% to about 3% of a thickening agent in an alcoholic solvent, wherein said copolymer is characterized by that the monomer ratio of ethyl acrylate to methacrylic acid is within a range from 75/25 to 95/5, with residual monomer being 50 ppm or less and with practically no surfactants.Type: GrantFiled: November 4, 1988Date of Patent: May 8, 1990Assignee: Shionogi & Co., Ltd.Inventors: Izumi Saitoh, Shigeru Kido, Yoshio Doi, Shohei Egawa
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Patent number: 4873262Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: December 15, 1987Date of Patent: October 10, 1989Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4806558Abstract: Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of dermatological disorders.Type: GrantFiled: September 20, 1985Date of Patent: February 21, 1989Assignee: BASF AktiengesellschaftInventors: Hans-Heiner Wuest, Fritz-Frieder Frickel, Axel Nuerrenbach
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Patent number: 4803221Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is an anthracene or substituted anthracene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: February 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4771076Abstract: This invention relates to novel [(2-substituted 1,2-dihydro-1-oxo-1H-inden-5-yl)oxy]alkanesulfonic acids and salts thereof. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, the neurological problems caused by AIDS, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions, and elevated intracranial pressure.Type: GrantFiled: June 1, 1987Date of Patent: September 13, 1988Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Adolph M. Pietruszkiewicz
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Patent number: 4737521Abstract: A method of stimulating the immune response of a patient which comprises administering to a patient in need thereof an immunostimulating effective amount of 8,8'-[carbonylbis]imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene) carbonylimino]]bis-1,3,5-naphthalenetrisulphonic acid hexasodium salt.Type: GrantFiled: May 27, 1986Date of Patent: April 12, 1988Assignee: Bayer AktiengesellschaftInventors: Klaus G. Stunkel, Rudi Grutzmann
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Patent number: 4719236Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid additon salts thereof; wherein Ar is a perylene or substituted perylene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl; R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: October 17, 1984Date of Patent: January 12, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4613611Abstract: A method of treating diabetes mellitus using arylglyoxals which are known compounds.Type: GrantFiled: October 14, 1983Date of Patent: September 23, 1986Assignee: American Cyanamid CompanyInventors: Middleton B. Floyd, Jr., Jo A. Goidl
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Patent number: 4591604Abstract: A method of inhibiting the complement system using multisulfonated naphthalene ureas.Type: GrantFiled: August 27, 1984Date of Patent: May 27, 1986Assignee: American Cyanamid CompanyInventors: Ransom B. Conrow, Seymour Bernstein
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Patent number: 4565694Abstract: The invention relates to contraceptive vaginal tablets as well as to a process for preparing them. The tablets of the invention have the following composition:0.2 to 3 parts by weight of boric acid,10 to 20 parts by weight of tartaric acid,1 to 2 parts by weight of vitamin K.sub.3 -sodium bisulfite adduct,0.8 to 1.2 parts by weight of polyvinyl pyrrolidone,2 to 5 parts by weight of magnesium stearate,8 to 12 parts by weight of carboxymethyl cellulose,8 to 12 parts by weight of lactose and50 to 65 parts by weight of microcrystalline cellulose.The vaginal tablets contain preferably 5 to 10 mg of vitamin K.sub.3 -sodium bisulfite adduct and have a total weight of 500 mg.The tablets of the invention are prepared preferably in such way that the boric acid, the tartaric acid and the vitamin K.sub.Type: GrantFiled: June 7, 1984Date of Patent: January 21, 1986Inventors: Andras Kovacs, Rudolf Szebeni, Bela Koszegi