Inflammation, Skin Patents (Class 514/886)

Cross-Reference Art Collections

Topical treatment (Class 514/887)
  • Patent number: 5262161
    Abstract: 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: Grant
    Filed: September 30, 1991
    Date of Patent: November 16, 1993
    Assignees: Fumio Dozono, Naohiko Sato
    Inventor: Fumio Dozono
  • Patent number: 5260341
    Abstract: A product for treating bovine mastitis and bovine metritis includes mixture of diacetyl and acetoin. The diacetyl and acetoin is produced by fermentation of milk and is then distilled and concentrated. The concentrated mixture of diacetyl and acetoin is infused into the udder cistern of a cow when treating mastitis, and is infused into the uterus of a cow when treating metritis.
    Type: Grant
    Filed: July 14, 1992
    Date of Patent: November 9, 1993
    Assignee: Agro-K Corporation Inc.
    Inventor: A. H. J. Rajamannan
  • Patent number: 5258391
    Abstract: Therapeutic as well as preventative measures to improve the cosmetic conditions or to alleviate the symptoms of dermatologic disorders with phenyl alpha acyloxyalkanoic acids and derivatives is disclosed. The cosmetic conditions and dermatologic disorders in humans in which the compounds may be useful include brittle or soft nails; abnormally thin skin, mucous membranes or wound; friction blisters; brittle hairs; pruritus; acne; and diseased nails, skin or mucous membranes due to natural or unnatural causes including but not limited to in flammations or infections. The phenyl alpha acyloxyalkanoic acids and derivatives include, for example, diphenyl alpha acetoxyacetic acid, phenyl alpha acetoxyacetic acid, phenyl alpha methyl alpha acetoxyacetic acid and phenyl alpha acetoxypropanoic acid. The compositions containing the active ingredients are also useful for treatment of skin, nails and hair conditions or disorders in domestic animals.
    Type: Grant
    Filed: December 20, 1990
    Date of Patent: November 2, 1993
    Inventors: Eugene J. Van Scott, Ruey J. Yu
  • Patent number: 5256647
    Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## wherein X may represent sulfur or two hydrogen atoms; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-18 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen, in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.
    Type: Grant
    Filed: November 13, 1990
    Date of Patent: October 26, 1993
    Assignee: Whitby Research, Inc.
    Inventors: Gevork Minaskanian, James V. Peck, Eric L. Nelson
  • Patent number: 5256403
    Abstract: Solubilized melanin based compositions supply melanin to skin, scalp and/or hair. The compositions consist of melanin, as an active ingredient, and a substance to solubilize the melanin blended together in a vehicle suitable for topical application. A melanin-based composition applied to the skin provides photoprotection of the human epidermis from exposure to ultraviolet rays. A melanin-based composition applied to wounds in the skin accelerates healing of the wounds. A melanin-based composition applied to the hair and scalp strengthens the hair.
    Type: Grant
    Filed: January 8, 1991
    Date of Patent: October 26, 1993
    Inventor: Frances C. Gaskin
  • Patent number: 5250301
    Abstract: A liquid internal medicine contains only an extract from stems of natural Stevia plants. The medicine is particularly effective for curing disorders of the digestive organs. The medicine contains a liquid obtained by fermenting a concentrate of an extract from Stevia stems, and is administered to patients as is or after dilution. As the medicine contains only the natural component, it is free of any side effects when applied to patients.
    Type: Grant
    Filed: January 28, 1992
    Date of Patent: October 5, 1993
    Assignees: Fumio Dozono, Naohiko Sato
    Inventor: Fumio Dozono
  • Patent number: 5250300
    Abstract: A liquid internal medicine for domestic animals contains only an extract from stems of natural Stevia plants. The medicine is effective for curing disorders of the digestive organs of domestic animals and for improving the physical constitution of domestic animals to further result in improvement of meat quality, milk quality and hair gloss of domestic animals and promotion of the estrous cycle and their establishment of the menstrual function. The medicine contains a liquid obtained by fermenting a concentrate of an extract from Stevia stems, and is administered to domestic animals as is or after dilution. As the medicine contains only the natural component, it is free of any side effects when applied to domestic animals.
    Type: Grant
    Filed: January 28, 1992
    Date of Patent: October 5, 1993
    Assignees: Fumio Dozono, Naohiko Sato
    Inventor: Fumio Dozono
  • Patent number: 5246964
    Abstract: A method of treatment of inflammatory diseases which comprises administering, to a subject in need of such treatment, an anti-inflammatory effective amount of a polyoxyethylenesorbitan mono-higher-fatty acid ester.
    Type: Grant
    Filed: July 8, 1991
    Date of Patent: September 21, 1993
    Assignee: K.K. Ueno Seiyaku Oyo Kenkyujo
    Inventor: Ryuji Ueno
  • Patent number: 5244917
    Abstract: This invention relates to substituted naphthofurans as anti-inflammatory and anti-allergic agents, pharmaceutical compositions containing them, processes for their preparation, and their use as anti-inflammatory and anti-allergic agents. The naphthofurans are of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 is CN or COOR.sup.9 ;R.sup.2 and R.sup.8 independently are H, C.sub.1 -C.sub.4 alkyl, COR.sup.9 or COR.sup.10 ;R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are independently H, C.sub.1 -C.sub.4 alkyl, halogen, phenyl, CF.sub.3 or OR.sup.9 ;R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, or COR.sup.9 ; andR.sup.9 and R.sup.10 are independently C.sub.1 -C.sub.4 alkyl, halogen or aryl.
    Type: Grant
    Filed: June 2, 1992
    Date of Patent: September 14, 1993
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Joseph J. Petraitis, Donald J. P. Pinto
  • Patent number: 5244899
    Abstract: The compounds of this invention are azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.
    Type: Grant
    Filed: July 29, 1992
    Date of Patent: September 14, 1993
    Assignee: G. D. Searle and Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5238965
    Abstract: The subject invention relates to methods for regulating wrinkles in mammalian skin comprising topical application of a lysophosphatidic acid compound having the structure: ##STR1## or a cyclic derivative thereof having the structure: ##STR2## or a pharmaceutically acceptable salt thereof, wherein --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 12 to about 23 carbon atoms; each --X-- is independently --O-- or --S--; and --Y-- is --O-- or --CH.sub.2 --.
    Type: Grant
    Filed: May 31, 1991
    Date of Patent: August 24, 1993
    Assignee: The Procter & Gamble Company
    Inventors: Gary A. Piazza, Adam W. Mazur
  • Patent number: 5229421
    Abstract: This invention encompasses compounds and pharmaceutical compositions comprising a pharmaceutical carrier and an effective lipoxygenase inhibiting amount of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different members of the group consisting of 1,1-dimethylethyl, halo, phenyl and substituted phenyl wherein the substituents are selected from the group consisting of halo, hydroxy, lower alkyl and lower alkoxy, Alk is straight or branched chain lower alkylene; and R.sub.3 is lower alkoxycarbonylloweralkyl.
    Type: Grant
    Filed: September 18, 1992
    Date of Patent: July 20, 1993
    Assignee: G. D. Searle & Co.
    Inventor: Richard A. Mueller
  • Patent number: 5223539
    Abstract: The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Z can be: ##STR2## wherein R.sup.3 is alkyl having 1 to 6 carbon atoms and, when n is greater than 1, each R.sup.3 can be the same or different; and n is an integer from 1 to 3;R.sup.1 and R.sup.2 can each independently be hydrogen, straight or branched chain alkyl, or cycloalkyl having 3 to 8 carbon atoms which can optionally be substituted at one or more positions by alkyl of 1 to 6 carbon atoms; X is oxygen, sulfur, NR.sup.4, wherein R.sup.4 is hydrogen or alkyl having 1 to 4 carbon atoms, C.dbd.O, CHOH, or CH.sub.2 ; Y is hydrogen, alkoxy, halogen, alkyl, or hydroxy; and m is an integer from 0 to 3. The compounds are antagonists of platlet-activating factor (PAF).
    Type: Grant
    Filed: November 21, 1991
    Date of Patent: June 29, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Roger A. Nosal, Michael A. Stealey, Richard M. Weiser
  • Patent number: 5215979
    Abstract: The invention refers to compounds having activity against inflammatory, allergic, and dermatological conditions. The compounds are characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula R.sub.1 is selected from a straight or branched hydrocarbon chain having 1-4 carbon atoms.The invention also refers to processes for the preparation of these compounds, pharmaceutical preparations containing one of the compounds and a method for the treatment of inflammatory, allergic, muscoskeletal and dermatological conditions.
    Type: Grant
    Filed: October 16, 1991
    Date of Patent: June 1, 1993
    Assignee: Aktiebolaget Draco
    Inventors: Paul H. Andersson, Per T. Andersson, Bengt I. Axelsson, Ralph L. Brattsand, Bror A. Thalen, Jan W. Trofast
  • Patent number: 5214069
    Abstract: The invention concerns a compound of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;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; wherein R.sup.2 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl; and whereinR.sup.3 is hydroxy-(1-4C)alkyl, mercapto-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, (3-4C)alkenyloxy-(1-4C)alkyl, (3-4C)alkynyloxy-(1-4C)alkyl, (1-4C)alkoxy-(2-4C)alkoxy-(1-4C)alkyl, (1-4C)alkylthio-(1-4C)alkyl, (1-4C)alkylsulphinyl-(1-4C)alkyl, (1-4C)alkylsulphonyl-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, (2-4C)alkanoyl-(1-4C)alkyl, (2-4C)alkanoyloxy-(1-4C)alkyl or cyano-(1-4C)alkyl; or R.sup.
    Type: Grant
    Filed: January 23, 1992
    Date of Patent: May 25, 1993
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventor: Jean-Marc M. M. Girodeau
  • Patent number: 5214070
    Abstract: The invention concerns a diaryl ether cycloalkane of the formula I, or a pharmaceutically-acceptable salt thereof, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl; X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is (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 (3-6C)alkylene group which defines an optionally substituted ring having 4 to 7 ring atoms.The invention also concerns processes for the manufacture of a diaryl ether cycloalkane of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said cycloalkane. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
    Type: Grant
    Filed: August 21, 1991
    Date of Patent: May 25, 1993
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Thomas G. C. Bird, Philip N. Edwards
  • Patent number: 5209920
    Abstract: Inbred Lewis (LEW/N) female rats develop an arthritis in response to Group A streptococcal cell wall peptidoglycanpolysaccharide (SCW) which mimics human rheumatoid arthritis. Histocompatible Fischer (F344/N) rats, on the other hand, do not develop arthritis in response to the same SCW stimulus. To evaluate this difference in inflammatory reactivity between the two strains, the function of the hypothalamic-pituitary-adrenal axis and its ability to modulate the development of the inflammatory response was studied. It has been found that, in contrast to F344/N rats, LEW/N rats had markedly impaired plasma ACTH and corticosterone responses to SCW, recombinant human Interleukin-1 alpha (IL-1 alpha), the serotonin agonist, quipazine, and synthetic rat corticotropin-releasing hormone (CRH). In addition, LEW/N rats compared to F344/N rats had smaller adrenal glands and larger thymuses. Treatment of LEW/N rats with replacement doses of dexamethasone decreased the severity of their SCW-induced arthritis.
    Type: Grant
    Filed: September 25, 1989
    Date of Patent: May 11, 1993
    Assignee: The United States of America as represented by the United States Department of Health and Human Services
    Inventors: Esther M. Sternberg, Ronald L. Wilder, Philip W. Gold, George P. Chrousos
  • Patent number: 5210073
    Abstract: A composition and method for the treatment of inflammation, rheumatism, autoimmune disease, ischemic damage of organs, drug toxicity and arteriosclerosis comprising human ADF is disclosed.
    Type: Grant
    Filed: September 28, 1990
    Date of Patent: May 11, 1993
    Assignees: Ajinomoto Co., Inc., Junji Yodoi
    Inventors: Junji Yodoi, Atsushi Uchida, Yutaka Tagaya, Akira Mitsui, Tadashi Hirakawa
  • Patent number: 5208031
    Abstract: This invention relates to the use of zinc salts as anti-viral agents in sexual lubricants. A zinc salt which releases divalent zinc ions in an aqueous carrier fluid is provided in a sexual lubricant formulation which is spread on the genitals before sexual intercourse. The mixture is non-irritating, and the zinc ions serve as an anti-viral agent to reduce the risk of contracting genital herpes if a sexual partner is infected. These lubricants may also reduce the risk of infection by other sexually transmitted viral diseases, such as hepatitis, papilloma viruses, and AIDS. A preferred lubricant formulation comprises water, a thickening or suspending agent, a lubricating agent, and a suitable zinc salt. Salts which have been tested and shown to be non-irritating during sexual intercourse include zinc acetate, zinc propionate, and zinc gluconate. Other zinc salts have also been identified which are soluble in water and have low pK values, which indicates a high rate of zinc ion release.
    Type: Grant
    Filed: July 29, 1991
    Date of Patent: May 4, 1993
    Inventor: Patrick D. Kelly
  • Patent number: 5208012
    Abstract: An anti-inflammatory cosmetic composition having a large effect of absorbing and shielding all of UV-A, UV-B and UV-C, small degeneration with the passage of time even upon absorption of light, small influence upon the skin, not lowered effect of absorbing light and high stability for heat is provided. This anti-inflammatory cosmetic composition comprises 0.1 to 20% by weight of a hydroxyaryl-s-triazine compound represented by the following structural formula in a cosmetically acceptable oil carrier: ##STR1## wherein R.sub.1 and R.sub.2 represent, same or different, hydrogen atoms, chlorine atoms, hydroxyl groups, alkoxy groups of 1 to 18 carbon atoms, aryloxy groups of 6 to 8 carbon atoms or mono- or dialkylamino groups containing 1 to 4 carbon atoms and R.sub.3 and R.sub.4 represent, same or different, hydrogen atoms, chlorine atoms, alkyl groups of 1 to 8 carbon atoms, methoxy groups or ethoxy groups.
    Type: Grant
    Filed: July 31, 1991
    Date of Patent: May 4, 1993
    Assignee: Daikyo Gomu Seiko Ltd.
    Inventors: Mirihiro Sudo, Tomoyasu Muraki, Eiji Kawachi, Yasushi Kawachi
  • Patent number: 5208015
    Abstract: The certain imidazoles have been found to exhibit anti-inflammatory as well as antifungal activity.
    Type: Grant
    Filed: July 23, 1991
    Date of Patent: May 4, 1993
    Assignee: Bristol-Myers Squibb Company
    Inventors: Hemanshu S. Shah, Cheng-Der Yu, John Gibson
  • Patent number: 5202118
    Abstract: Wound healing compositions comprising IL-1.alpha. and IL-1.beta. proteins in a physiologically acceptable hydrophilic vehicle are used to promote wound healing.
    Type: Grant
    Filed: May 6, 1991
    Date of Patent: April 13, 1993
    Assignee: Immunex Corporation
    Inventors: Steven Gillis, Cindy A. Jacobs
  • Patent number: 5202321
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, psoriasis, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: June 13, 1991
    Date of Patent: April 13, 1993
    Assignee: Merck Frosst Canada, Inc.
    Inventors: John H. Hutchinson, Yves Girard, Rejean Fortin, Dwight MacDonald, John Scheigetz, Daniel Delorme, Michel Therien, Pierre Hamel
  • Patent number: 5190916
    Abstract: A treating agent such as a wound therapeutic agent, inflammation therapeutic agent, hair growth agent and hair tonic, and a cosmetic, comprising as an effective component ovomacroglobulin are disclosed. They can act on the skin, a scalp or hairs to exhibit excellent wound curing promotion effect, hair growth promotion effect, and skin or hair protective effect.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: March 2, 1993
    Assignees: Japan Immuno Research Laboratories Co., Ltd., Otsuka Pharmaceutical Co., Ltd.
    Inventor: Masakazu Adachi
  • Patent number: 5187150
    Abstract: The pharmaceutical composition is intended in particular for the sustained and controlled release of an effective dose of a medicinal substance. It comprises, as a carrier for the medicinal substance, a biodegradable polymer or copolymer or a mixture of biodegradable polymers and/or copolymers derived from a dicarboxylic acid selected from the acids of the Krebs cycle, and from an aliphatic diol containing 4 carbon atoms or from cyclohexane-1,4-dimethanol.
    Type: Grant
    Filed: March 29, 1990
    Date of Patent: February 16, 1993
    Assignee: Debiopharm S.A.
    Inventors: Peter Speiser, Urs Schleuniger, Piero Orsolini, Frederic Heimgartner
  • Patent number: 5178873
    Abstract: A method of inhibiting phospholipase A2 in the control of inflammation, wherein delta-6,9,12,15-octadecatetraenoic acid (stearidonic acid) and/or delta-8,11,14,17-eicosatetraenoic acid is administered alone or in a pharmaceutically acceptable diluent or carrier.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: January 12, 1993
    Assignee: Efamol Holdings PLC
    Inventors: David F. Horrobin, Michael J. Finnen
  • Patent number: 5175000
    Abstract: A pharmaceutical composition of a free amine benzophenanthridine alkaloid and a pharmaceutically acceptable carrier is disclosed. The composition is an antibacterial and antifungal agent.
    Type: Grant
    Filed: May 6, 1991
    Date of Patent: December 29, 1992
    Assignee: Vipont Pharmaceutical, Inc.
    Inventors: Kenneth C. Godowski, Ronald J. Harkrader, Richard L. Dunn, Arthur J. Tipton
  • Patent number: 5175321
    Abstract: An amide derivative represented by the following general formula (I) or (II): ##STR1## (wherein R.sup.1 and R.sup.2 represent each a straight-chain or branched, saturated or unsaturated hydrocarbon group provided that one of them carries 26 to 39 carbon atoms while the other carries 9 to 39 carbon atoms); or ##STR2## (wherein R.sup.3 represents a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 10 to 40 carbon atoms; R.sup.4 represents a straight-chain or branched hydrocarbon group carrying 3 to 39 carbon atoms; and R.sup.5 represents a dydrogen atom, a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 10 to 40 carbon atoms or an acyl group);and a dermatologic preparation containing the same.
    Type: Grant
    Filed: May 18, 1990
    Date of Patent: December 29, 1992
    Assignee: KAO Corporation
    Inventors: Yukihiro Ohashi, Mituo Suda, Shinji Yano, Akira Kawamata, Minehiro Okuda, Genji Imokawa
  • Patent number: 5165932
    Abstract: The invention relates to therapeutical compositions on medical herb basis for the treatment of psoriasis and the preparation of the same. A further object of the invention in the use of medical herbs as listed below in the treatment of psoriasis, rheumatism and asthmatic dyspnoea. The medical herbs used in the invention are as follows:Allium sativum /garlic/,Urtica dioica /common nettle/,Chelidonium majus /milkweed/,Veronica officinalis /veronica/,Calendula officinalis /calendula or marigold/,Achillea herba /millefolium/ /yarrow/,Fumaria officinalis /fumitory, earth-gall/.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: November 24, 1992
    Assignee: Unipharma Co., Ltd.
    Inventor: Ferenc Horvath
  • Patent number: 5166137
    Abstract: A family of compounds effective in inhibiting interleukin-1 (IL-1) production, interleukin-6 (IL-6), tumor necrosis factor (TNF) production, and the production of other leukocyte derived cytokines is comprised of oligomers and polymers of .alpha.1-4 linked L-guluronic acid residues which may be administered to a human or mammal in an amount sufficient to inhibit the production effect of leukocyte-derived cytokines. The inhibition of IL-1, IL-6 and TNF, and other cytokines in mammals is implicated in alleviation of a wide variety of disease conditions.
    Type: Grant
    Filed: March 27, 1991
    Date of Patent: November 24, 1992
    Assignees: Nobipols Forskningsstiftelse, Protan Biopolymer A/S
    Inventors: Marit Otterlei, Terje Espevik, Gudmund Skjak-Braek, Olav Smidsrod
  • Patent number: 5160736
    Abstract: A composition for preventing or treating hypertriglyceridemia containing purple laver as an active ingredient is disclosed. A neutral fat level in blood can be reduced by ingesting the composition in a daily diet.
    Type: Grant
    Filed: January 15, 1991
    Date of Patent: November 3, 1992
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventor: Shuhachi Kiriyama
  • Patent number: 5157053
    Abstract: The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; x is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group-consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, aszabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino, The compounds are useful as anti-inflammatory and anti-allergy agents.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: October 20, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5155096
    Abstract: The invention relates to a method for potentiation of a therapeutic agent, the method comprising the steps of administering an effective dose of insulin to induce to hypoglycemia; administering a pre-determined dose of a therapeutic agent; and administering a pre-determined dose of glucose sufficient to substantially neutralize the hypoglycemia. As an adjuvant system, the instant invention constitutes the combination of a quantity of insulin in the range of one to four units per 10 kilograms of body weight; a pre-determined quantity of the therapeutic agent; and glucose in the form of a hypertonic solution between about 5% and about 50% glucose, the volume of the solution being in the range of about 10 cubic centimeters to about 100 cubic centimeters. The inventive method is known as Insulin Potentiation Therapy (IPT).
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: October 13, 1992
    Inventors: Donato P. Garcia y Bellon, Donato P. Garcia, Jr., Steven G. Ayre
  • Patent number: 5151534
    Abstract: Compounds corresponding to the formula: ##STR1## wherein A represents --(CH.sub.2).sub.2 or --(C.tbd.C)--;n is equal to 0, 1 or 2;R represents hydroxyl, alkoxy having the formula --OR.sub.1, or amino having the formula ##STR2## R.sub.1 represents alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or aralkyl;R.sub.2 and R.sub.3 represent hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or benzyl;R.sub.2 and R.sub.3 form, with the nitrogen atom, a heterocyclic ring.Application of these compounds in pharmacy and cosmetics.
    Type: Grant
    Filed: May 10, 1989
    Date of Patent: September 29, 1992
    Assignee: Centre International de Recherches Dermatologiques (CIRD)
    Inventors: Braham Shroot, Christopher Hensby, Jean Maignan, Gerard Lang, Michel Colin
  • Patent number: 5151425
    Abstract: According to the invention, it has been found that plant cytokinins are effective in treating inflammation in mammals, such as humans. The plant cytokinins are effective to treat the inflammation, to accelerate healing of lesions, and to provide substantially immediate relief of pain, itching, and other immunological responses resulting from inflammation. The plant cytokinin is administered to the mammal in a suitable pharmaceutical preparation.Particular plant cytokinins which have been tested include trans-zeatin (trans-6-(4-hydroxy-3-methyl(but-2-enyl)-aminopurine)), 6-benzyl-adenine (6-benzylaminopurine), and kinetin (6-furfurylaminopurine).A composition for topical use in accordance with the method comprises an effective amount of the plant cytokinin in a carrier suitable for topical application to the human skin, for example, hydrophilic ointment, isopropyl alcohol, or a powder formulation.
    Type: Grant
    Filed: June 20, 1991
    Date of Patent: September 29, 1992
    Inventor: LeaLand L. Clark
  • Patent number: 5141951
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is alkyl, alkoxy, alkylthio, alkylamino, aryl, aryloxy, arylthio, arylamino, aralkyl, aralkoxy, aralkylthio or aralkylamino,R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, mercapto, nitro or amino or have the meanings given for R.sub.1, andX is --NH.sub.2, --NH--OH, --N(R.sub.4)OH, --NH--NH.sub.2 or --NH--N.dbd.C(R.sub.4)R.sub.5, whereinR.sub.4 and R.sub.5 are each alkyl,in free form or pharmaceutically acceptable salt form, have pharmaceutical utility, in particular in the treatment or prophylaxis of asthma, or in the treatment of inflammation or psoriasis.
    Type: Grant
    Filed: November 27, 1991
    Date of Patent: August 25, 1992
    Assignee: Sandoz Ltd.
    Inventor: Hans-Jurg Wuthrich
  • Patent number: 5134161
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy,R.sup.2 is the same as R.sup.1, or R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl,R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;both X groups are the same and X is either --C(O)OR.sup.4 or --C(O)NR.sup.5 R.sup.6, whereinR.sup.4 is alkyl, phenyl or benzyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl, cycloalkyl or phenyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo.
    Type: Grant
    Filed: April 15, 1988
    Date of Patent: July 28, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Michael C. Venuti, John M. Young
  • Patent number: 5126331
    Abstract: Compositions for topical use containing as active ingredients depolymerized deoxyribonucleic acids can be used for the reduction of the unaesthetisms of the face skin, due to the couperose. Said compositions can be advantageously used also to locally reduce, in the lower limbs, the skin unaesthetisms (dilated capillaries, oedemas, tumefactions), resulting from a situation of an extended physical stress acting on the above-mentioned legs.
    Type: Grant
    Filed: August 16, 1990
    Date of Patent: June 30, 1992
    Assignee: Crinos Industria Farmacobiologica S.p.A.
    Inventor: Giovanni Gazzani
  • Patent number: 5126135
    Abstract: The present invention relates to a dermatological composition composed for cosmetics or medicines for external application to skin and to oral or nasal mucous-membrane. This composition can be applied in particular in the cosmetic or pharmaceutical field, especially in the dermatological cases to regenerate and to revitalize damaged cells by equilibrating electrochemical ion gradients across cell membrane and also by osmotic pressure on the inner face of the cell membrane. A composition based on a water phase in accordence with present invention comprises dextran, glucose, mutan lentinan, NaCl, KCl, and CaCl.sub.2, which are dissolved in the aqueous phase.
    Type: Grant
    Filed: June 18, 1991
    Date of Patent: June 30, 1992
    Assignee: Japan Fine Chemical Co., Ltd.
    Inventors: Hajime Yamada, Akira Yamada
  • Patent number: 5124320
    Abstract: An external analgesic lotion containing active ingredients of camphor and menthol to relieve pain in muscles, joints, or viscera distal at the site of application by stimulating cutaneous sensory receptors and a method of making such lotion and being made from camphor and menthol crystals.
    Type: Grant
    Filed: February 13, 1991
    Date of Patent: June 23, 1992
    Inventors: Jeffery W. Ivy, Curtis E. Payne
  • Patent number: 5124334
    Abstract: The invention relates to benylalcohol phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylalcohol phospholipase A.sub.2 inhibitor.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: June 23, 1992
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventor: Wendell W. Wilkerson
  • Patent number: 5110831
    Abstract: The present invention relates to vinylogous hydroxamic acids, processes for their manufacture, pharmaceutical preparations containing them, and their use in the treatment of various disorders.
    Type: Grant
    Filed: November 30, 1990
    Date of Patent: May 5, 1992
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Ronald L. Magolda, Stephen W. Wright
  • Patent number: 5099068
    Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, wherein AR represents the group ##STR2## where Q.sup.1 represents a straight or branched C.sub.1-3 alkylene group, ##STR3## where Q.sup.2 represents a group R.sup.3 CO--, R.sup.3 NHCO--, R.sup.3 R.sup.4 NSO.sub.2 --, or R.sup.5 SO.sub.2 --, where R.sup.3 and R.sup.4 each represent a hydrogen atom or a C.sub.1-3 alkyl group, and R.sup.5 represents a C.sub.1-3 alkyl group, ##STR4## R represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sup.1 and R.sup.
    Type: Grant
    Filed: December 5, 1990
    Date of Patent: March 24, 1992
    Assignee: Glaxo Group Limited
    Inventors: William L. Mitchell, Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, David Hartley
  • Patent number: 5091182
    Abstract: A dispensing unit for a ketorolac topical gel formulation is disclosed, wherein the dispensing unit comprises a ketorolac topical gel formulation and a gas-impermeable multi-layered container wherein the container is comprised of a polyolefin inner layer and a metal foil outer layer.
    Type: Grant
    Filed: July 23, 1990
    Date of Patent: February 25, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John T. H. Ong, Jean S. Fujiki, Wei-Cheng Liaw
  • Patent number: 5087638
    Abstract: Benzofuran derivatives, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation. The compounds are also useful as analgesics and as cytoprotective agents.
    Type: Grant
    Filed: June 28, 1989
    Date of Patent: February 11, 1992
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Patrice C. Belanger, John Scheigetz, Joshua Rokach
  • Patent number: 5086050
    Abstract: Salts of azelastine with acetic acid, gluconic acid, lactic acid or malic acid.
    Type: Grant
    Filed: February 8, 1991
    Date of Patent: February 4, 1992
    Assignee: Asta Pharma AG
    Inventors: Helmut Hettche, Reinhard Muckenschnabel, Gerhard Scheffler, Ilona Fleischhauer, Wolfgang Morick
  • Patent number: 5084481
    Abstract: Pharmaceutical compositions and their preparation which contain dihydrolipoic acid or its pharmaceutically acceptable salts as active substance. The pharmaceutical compositions have a cytoprotective effect and are suitable for combatting pain and inflammatory disorders.
    Type: Grant
    Filed: February 8, 1990
    Date of Patent: January 28, 1992
    Assignee: Asta Pharma Aktiengesellschaft
    Inventors: Heinz Ulrich, Carl-Heinrich Weischer, Jurgen Engel, Helmut Hettche
  • Patent number: 5071876
    Abstract: The compounds of this invention are anilides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is hydrogen or lower alkyl; and R.sub.4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.
    Type: Grant
    Filed: July 27, 1990
    Date of Patent: December 10, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5061720
    Abstract: Disclosed are novel substituted 4-thiazolidinone derivatives having cyclooxygenase and 5-lipoxygenase inhibiting properties and which are topical antiinflammatory agents for inflammed conditions of the skin having the formula: ##STR1## wherein R is hydrogen or loweralkyl; R.sup.1 is loweralkyl or aryl; X is --(CH.sub.2)-aryl, --O--(CH.sub.2).sub.0-3 -aryl, --C(O)(CH.sub.2).sub.0-3 -aryl, --CH(OH)--(CH.sub.2).sub.0-3 -aryl or 3,4 ##STR2## (to form naphthyl ring); aryl is phenyl, substituted phenyl, or 2,3 or 4 pyridyl; W is oxygen; Q is -(alk.sup.1).sub.0-1 --(O).sub.0-1 --(B).sub.0-1 --(alk.sup.2).sub.0-1 --[C(O)Z].sub.0-1 ; B is ##STR3## Z is OR.sup.3 or NR.sup.4 R.sup.5 where R.sup.3 is hydrogen, loweralkyl, or a pharmaceutically acceptable metal cation, R.sup.4 and R.sup.5 are hydrogen or loweralkyl; alk.sup.1 and alk.sup.
    Type: Grant
    Filed: September 13, 1989
    Date of Patent: October 29, 1991
    Assignee: A. H. Robins Company, Inc.
    Inventors: David A. Walsh, Ibrahim M. Uwaydah
  • Patent number: 5061491
    Abstract: A medicinal agent for treatment of mastitis in animals and humans which includes a mixture of a decoction of a mixture of the following medicinal herbs in equal parts by weight and an ammonia solution infusion which is a mixture of the same medicinal herbs in equal parts by weight, wherein the medicinal herbs include Matricaria chamomilla L., flores Calendulae officinalis L., Urtica dioica L., Erythreae centaurium Raf. L., gemmae Betula pendula Roth, Plantago major L., gammae Pinus sylvestris L., Origanum vulgare L., Salvia officinalis Hoffm., Archangelica officinalis Hoffm., Taraxacum officinale Web., folium Tussilaginis farfarae L., Sanguisorba officinalis L., Valeriana officinalis L., Menthae piperitae L., Thymus vulgaris L., and Bidens tripartita L. The decoction and infusion are mixed in a ratio to adjust the Ph of the mixture to not below 7.4. Also disclosed is a method of treating mastitis using the medicinal agent described above.
    Type: Grant
    Filed: July 21, 1989
    Date of Patent: October 29, 1991
    Inventor: Alexandr M. Deryabin