9-position Substituted Patents (Class 514/180)
-
Patent number: 5173483Abstract: A method of stimulating ovulation in warm-blooded animals comprising administering to warm-blooded animals an ovulation stimulating effective amount of at least one anti-progestomimetic compound.Type: GrantFiled: September 5, 1990Date of Patent: December 22, 1992Assignee: Roussel UclafInventor: J. A. Grandadam
-
Patent number: 5166145Abstract: A dosage form is disclosed comprising an antiemetic and antinausea drug for treating vomiting and nausea.Type: GrantFiled: September 10, 1990Date of Patent: November 24, 1992Assignee: Alza CorporationInventors: Francisco Jao, Hoa I. Huynh, Patrick S. L. Wong
-
Patent number: 5166200Abstract: A remedy for endometriosis comprising, as an active ingredient, 14.alpha.-hydroxy-4-androstene-3,6,17-trione or an ester derivative thereof, can effectively treat endometriosis by the strong aromatase-inhibitory activity without giving serious side effects.Type: GrantFiled: April 11, 1991Date of Patent: November 24, 1992Assignee: Snow Brand Milk Products Company, LimitedInventors: Nobuaki Fujise, Yasushi Yamashita, Hiroaki Takaoka, Nobuyoshi Honda, Makoto Yoshihama
-
Patent number: 5124392Abstract: Methods for preventing and treating corneal haze resulting from exposure of the eye to laser irradiation are disclosed. The methods include administration of compositions of wound healing modulators to the eye. Compositions for use in preventing and treating the corneal haze are also disclosed.Type: GrantFiled: May 31, 1990Date of Patent: June 23, 1992Assignee: Alcon Laboratories, Inc.Inventors: Stella M. Robertson, Herman M. Kunkle, Jr.
-
Patent number: 5120723Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.Type: GrantFiled: May 10, 1990Date of Patent: June 9, 1992Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger
-
Patent number: 5116829Abstract: A 21-substituted steroid compound is disclosed. The compound has a structure of formula (I), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl, lower alkenyl, lower alkoxy, or phenyl group, R.sup.2 is a hydroxyl group or an acyloxy group having 1-6 carbon atoms, R.sup.3 is a hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 may together form a lower alkylidenedioxy group, X.sup.1 and X.sup.2 may be the same or different and individually represents a hydrogen atom or a halogen atom, Y.sup.1 and Y.sup.2 may be the same or different and individually represents a methylene group or a sulfur atom, Z is a sulfur atom or an imino group, the wave line means that the configuration of R.sup.3 may be of either .alpha. or .beta., and dotted line between the 1 and 2 position means that the bond may be the double bond.Type: GrantFiled: April 10, 1991Date of Patent: May 26, 1992Assignee: Kao CorporationInventors: Kimihiko Hori, Yasuto Suzuki, Tomoki Morioka, Shigeru Moriwaki, Osamu Hirota, Shuichi Tsuchiya
-
Patent number: 5112620Abstract: A therapeutic ointment having wet adherent properties and particularly well suited for delivery of medicaments to mucosal surfaces includes a base material comprising from about 3 to 15% by weight of a water soluble salt of a copolymer of methyl vinyl ether and maleic acid or anhydride in a polyethylene glycol ointment. Formulations of the base material with triamcinolone acetonide and lidocaine are particularly efficacious in the treatment of recurrent aphthous ulcers.Type: GrantFiled: September 20, 1990Date of Patent: May 12, 1992Assignee: Mikkur, Inc.Inventors: Michael A. Repka, Thomas G. Gerding
-
Patent number: 5095010Abstract: Combination products containing an antigestagen, a glucocorticoid and a prostaglandin are suitable for combined use in inducing labor or terminating pregnancy.Type: GrantFiled: November 13, 1990Date of Patent: March 10, 1992Assignee: Schering AktiengesellschaftInventors: Walter Elger, Sybille Beier
-
Patent number: 5082835Abstract: The invention relates to antiinflammatory compounds of the formula (I), ##STR1## wherein A stands for hydrogen, hydroxyl or trifluoroacetoxy group;X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;R stands for hydrogen, benzoyl or C.sub.1-8 alkanoyl group; andrepresents a single or double bond between two adjacent carbon atoms,as well as pharmaceutical compositions containing these compounds and a process for their preparation.Type: GrantFiled: March 9, 1990Date of Patent: January 21, 1992Assignee: Richter Gedeon Vegyeszeti Gyar R.T.Inventors: Csaba Molnar, Gyorgy Hajos, Laszlo Szporny, Jozsef Toth, Arpad Kiraly, Anna Boor nee Mezei, Janos Csorgei, Kristina Szekely, Lilla Forgacs, Gyorgy Fekete, Bulcsu Herenyi, Sandor Holly, Jozsef Szunyog
-
Patent number: 5063222Abstract: Steroid derivatives represented by formula (I) are disclosed. ##STR1## wherein R is a hydrogen atom, a halogen atom, a hydroxy group, or a group --OCOR.sub.1, wherein R.sub.1 is a linear or branched alkyl group which may be substituted by a halogen atom or a cycloalkyl group, a cycloalkyl group, or an aryl group. The compounds are useful for curing or alleviating inflammation or rheumatism.Type: GrantFiled: April 13, 1990Date of Patent: November 5, 1991Assignee: SS Pharmaceutical Co., Ltd.Inventors: Teruo Komoto, Junji Okawa, Yoichiro Ogawa, Susumu Sato, Naokata Taido, Tadayuki Kuraishi
-
Patent number: 5061700Abstract: Compositions of matter serving as topical ointment vehicles and comprising a glyceryl acetate, preferably triacetin, and an oleaginous material that can be combined with a medicament, preferably a corticosteriod, are described. The glyceryl acetate component functions as a solvent for the medicament. Additionally, methods of use for treating skin disorders comprising the topical application of a therapeutically effective amount of a medicament in a composition of the invention are detailed.Type: GrantFiled: November 16, 1989Date of Patent: October 29, 1991Assignee: Gordon Jay DowInventors: Gordon J. Dow, Debra A. Dow
-
Patent number: 5047419Abstract: There are disclosed pyrylium salts and a method of using them medicinally in photodynamic therapy for increasing the survival time of animals affected with glioma or mammary carcinoma. The salts are seleno- or telluropyrylium compounds having a singlet oxygen quantum efficiency of at least 0.005 when exposed as described at wavelengths between about 650 and 1000 nanometers.Type: GrantFiled: October 24, 1988Date of Patent: September 10, 1991Assignee: Eastman Kodak CompanyInventors: Michael R. Detty, Stephen K. Powers
-
Patent number: 5043165Abstract: This invention relates to a novel, non-conventional liposome formulation for the sustained release and delivery of steroids. The formulation provides prolonged release of the drug, improved therapeutic ratio, lower toxicity, reduced systemic side effects and is stable for up to three months. The formulation is suitable for sustained delivery of steroid via inhalation, parenteral, intrathecal, intraarticular, topical, ophthalmic, and oral administration.Type: GrantFiled: December 14, 1988Date of Patent: August 27, 1991Assignee: Liposome Technology, Inc.Inventor: Ramachandran Radhakrishnan
-
Patent number: 5028600Abstract: A composition for intravenous administration of 3-alpha-hydroxy-5-beta-pregnan-20-one (pregnanolone), comprising a stable oil-in-water emulsion, capable of being sterilized by autoclaving, of from 0.1 to 1.0 g of pregnanolone.Type: GrantFiled: February 28, 1989Date of Patent: July 2, 1991Assignee: KabiVitrum ABInventor: Roland I. Jeppsson
-
Patent number: 5026693Abstract: Novel esters of 9.alpha.-fluoro- and chloro-corticosteroids of the formula ##STR1## wherein Y is chlorine or OR.sub.1, R.sub.1 and R.sub.2 represent an acyl group of 2-6 carbon atoms or a benzoyl group and where R.sub.1 and R.sub.2 can be the same or different in the same molecule, R.sub.3 is methyl or fluorine in either the .alpha.- or .beta.- orientation, X is chlorine or fluorine, and the C.sub.1 C.sub.2 bond can be saturated or not, especially those compounds of the formula ##STR2## wherein Y and R.sub.2 have the significance given above, are prepared by reacting the respective 9.beta.,11.beta.-epoxy compounds with hydrogen fluoride or chloride.Type: GrantFiled: May 21, 1990Date of Patent: June 25, 1991Assignee: Hovione Inter Ltd.Inventors: Ivan Villax, William Heggie, Philip R. Page
-
Patent number: 5023251Abstract: The invention relates to a cream containing hydrocortisone diester, which contains0.01-0.5% of hydrocortisone diester5-20% of O/W emulsifier based on polyoxyethylene fatty acid esters and fatty alcohols0-10% of stearyl alcohol1-50% of white vaseline0-5% of benzyl alcohol and20-80% of water.Type: GrantFiled: October 31, 1989Date of Patent: June 11, 1991Assignee: Beiersdorf AGInventors: Henning Sattler, Bodo Asmussen
-
Patent number: 5019569Abstract: The present invention is directed to the topical administration of a retinoid-containing pharmaceutical composition for reversing the effects of glucocorticoid-induced skin atrophy.Type: GrantFiled: August 31, 1989Date of Patent: May 28, 1991Assignee: Ortho Pharmaceutical CorporationInventors: Albert M. Kligman, James A. Mezick, Robert J. Capetola
-
Patent number: 4985418Abstract: Use of fluticasone propionate in the treatment of bowel diseases when administered by the oral, stomal or rectal routes.Type: GrantFiled: December 23, 1987Date of Patent: January 15, 1991Assignee: Glaxo Group LimitedInventor: David A. Richards
-
Patent number: 4970206Abstract: The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.Type: GrantFiled: May 8, 1989Date of Patent: November 13, 1990Assignee: Merck & Co., Inc.Inventors: Jose Alexander, Takeru Higuchi
-
Patent number: 4939135Abstract: Methods for preventing and treating corneal haze resulting from exposure of the eye to laser irradiation are disclosed. The methods include administration of compositions of wound healing modulators to the eye. Compositions for use in preventing and treating the corneal haze are also disclosed.Type: GrantFiled: October 3, 1988Date of Patent: July 3, 1990Assignee: Alcon Laboratories, Inc.Inventors: Stella M. Robertson, Herman M. Kunkle, Jr., Michael E. Stern
-
Patent number: 4918065Abstract: A corticoid-containing pharmaceutical preparation adapted for topical application, comprising 0.005-2% by weight of a corticoid having antiinflammatory activity, a fatty phase, an aqueous phase, an emulsifier, a preservative, and, optionally, a fragrant substance, or an additional hydrophilic or lipophilic cosmetically active ingredients, wherein the fatty phase, and the aqueous phase are present in the form of a dispersed mixture of an oil/water emulsifier and a preservative, and a water/oil emulsion containing a water/oil emulsifier, the particle size of the inner phase of the emulsions being 2-50 .mu.m.Type: GrantFiled: October 17, 1988Date of Patent: April 17, 1990Assignee: Schering AktiengesellschaftInventors: Wolfgang Stindl, Ingfried Zimmerman, Renate Reckers, Hans Wendt, Rainold Arndt
-
Patent number: 4913852Abstract: Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of .DELTA.-4-pregnene-3,20-dione or with derivatives of .DELTA.-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields.Type: GrantFiled: February 24, 1988Date of Patent: April 3, 1990Inventors: Catherine Milioni, Constantin Efthyimiopoulos, Bernard Koch, Louis Jung, Jean Jung
-
Patent number: 4910192Abstract: Introduction of a C-12 substituent and especially a .beta. C-12 substituent into glucocorticoids improves their usefulness as topical antiinflammatories by increasing their topical activity relative to their systemic activity, thus reducing systemic side effects such as adrenal suppression.Type: GrantFiled: December 4, 1987Date of Patent: March 20, 1990Assignee: SRI InternationalInventors: Mitchell A. Avery, Masato Tanabe, Dennis Yasuda, George Detre
-
Patent number: 4904649Abstract: A method for treating glaucoma consisting of exposing the eye to a corticosteroid and a beta adrenergic agent to the eye which acts to decrease ocular pressure. Useful adrenergic agents include beta agonists antagonists, including, for example, epinephrine, dipivalyl epinephrine, betaxolol, levobunolol, and timolol. Useful steroids, which are preferably applied topically, include dexamethasone, prednisolone, cortisone, and triamcinolone. The beta adrenergic agent is administered at a concentration between about 10% and 20% of the concentration that the agent is administered in its normal use. The corticosteroid is administered at a concentration between 5% and 10% of the concentration that the corticosteroid is administered in its normal use.Type: GrantFiled: March 27, 1987Date of Patent: February 27, 1990Assignee: New England Medical Center Hospitals, Inc.Inventor: Bernard Schwartz
-
Patent number: 4889847Abstract: The present invention is directed to the topical administration of a retinoid-containing pharmaceutical composition for the prevention of glucocorticoid-induced skin atrophy.Type: GrantFiled: November 3, 1986Date of Patent: December 26, 1989Assignee: Ortho Pharmaceutical CorporationInventors: Albert M. Kligman, James A. Mezick, Robert J. Capetola
-
Patent number: 4879274Abstract: Novel external medications comprise, as essential components, the following three components (A) to (C):(A) an .alpha.-monoglyceryl ether represented by the following formula (I): ##STR1## wherein R means an alkyl or alkenyl group having 10 - 24 carbon atoms; (B) a physiologically active material; and(C) an oily material.The external medications have extremely high skin occlusive properties and significantly-improved absorptivity of phosiologically active materials. Therefore, a smaller amount of the medications compared with the conventional ones can give sufficient pharmacological effects and thus side effects can be reduced. The external medications may contain physiologically active materials such as drugs, growth hormones and the like, which are expected to show pharmacological effects upon their percutaneous absorption.Type: GrantFiled: September 12, 1986Date of Patent: November 7, 1989Assignee: Kao CorporationInventors: Tetsuro Kamiya, Shuichi Tsuchiya, Kenji Hara
-
Patent number: 4876250Abstract: Angiostatic steroids for use in controlling ocular hypertension are disclosed. Pharmaceutical composition of the angiostatic steroids and methods for their use in treating ocular hypertension, including controlling the ocular hypertension associated with primary open angle glaucoma, are disclosed.Type: GrantFiled: October 31, 1988Date of Patent: October 24, 1989Assignee: Alcon Laboratories, Inc.Inventor: Abbot F. Clark
-
Patent number: 4870066Abstract: A method and composition are provided for extending the gestation period of a sow so as to increase the live birth and survival rates of a swine litter without adversely affecting the sow. The method includes the step of administering an effective dosage of estrogen to the sow 21/2-7 days prior to the end of the expected gestation period for the sow. The composition administered includes from 0.5-10 mg of an estrogen selected from a group consisting of estradiol benzoate, estradiol valerate, estrone, estradiol 17.beta. and effective mixtures thereof. The composition is adapted for administration parenterally by including a carrier such as corn oil. A method is also provided for synchronizing farrowing in a herd of swine bred following synchronized weaning so as to shorten the target period during which all the sows of the herd begin farrowing.Type: GrantFiled: August 11, 1986Date of Patent: September 26, 1989Assignee: The University of Kentucky Research FoundationInventors: Lee A. Edgerton, Bruce T. Eckerle
-
Patent number: 4868168Abstract: A steroid ointment formulation which has enhanced physical and chemical stability is formed of 11.beta.,17.alpha.)-17-(ethylthio)-9.alpha.-fluoro-11.beta.-hydroxy-17-(me thylthio)androsta-1,4-dien-3-one (tipredane), and a vehicle containing as major ingredients propylene glycol and water, cetearyl alcohol and ceteareth 20 or other dispersing agent for propylene glycol, together with a sodium or potassium citrate and magnesium hydroxide buffer to impart a neutral or slightly alkaline apparent pH (5 to 9), a non-acidic long chain fatty acid wax to impart proper consistency to the ointment and sodium metabisulfite and butylated hydroxy toluene as antioxidants, together with thickeners, emollients, lubricants and other conventional ointment formulation ingredients.Type: GrantFiled: November 13, 1987Date of Patent: September 19, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Richard L. O'Laughlin, Andrea Panaggio, Sailesh A. Varia
-
Patent number: 4868170Abstract: A steroid lotion formulation which has enhanced physical and chemical stability is formed of (11.beta.,17.alpha.)-17-(ethylthio)-9.alpha.-fluoro-11.beta.-hydroxy-17-(m ethylthio)androsta-1,4-diene-3-one (tipredane), and a vehicle containing as major ingredients polyethylene glycol, propylene glycol and water together with a potassium citrate buffer or tromethamine buffer, and sodium metabisulfite and butylated hydroxytoluene as antioxidants.Type: GrantFiled: November 13, 1987Date of Patent: September 19, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Marilia M. Faustino, Sailesh A. Varia, Abu T. M. Serajuddin
-
Patent number: 4868169Abstract: A steroid cream formulation which has enhanced physical and chemical stability is formed of (11.beta.,17.alpha.)-17-(ethylthio)-9.alpha.-fluoro-11.beta.-hydroxy-17-(m ethylthio)androsta-1,4-dien-3-one (tipredane), and a vehicle containing as major ingredients glyceryl monostearate having an acid value of greater than 4, propylene glycol and water together with a sodium citrate or potassium citrate buffer, a non-acidic long chain fatty acid wax to impart proper consistency, and sodium metabisulfite as an antioxidant, together with emulsifiers, skin conditioners, emollients, lubricants and other conventional cream formulation ingredients.Type: GrantFiled: November 13, 1987Date of Patent: September 19, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Richard L. O'Laughlin, Andrea Panaggio, Sailesh A. Varia
-
Patent number: 4866051Abstract: Beclomethasone dipropionate in the form of its micronised monohydrate substantially free from water other than water of crystallisation. Pharmaceutical compositions containing the compound are also described. The compositions may be in the form of powder inhalation cartridges especially suitable for the treatment and/or prophylaxis of asthma.Type: GrantFiled: January 30, 1985Date of Patent: September 12, 1989Assignee: Glaxo Group LimitedInventors: John H. Hunt, John M. Padfield
-
Patent number: 4866049Abstract: The present invention relates to ophthalmic compositions and their preparation and use. More specifically, the invention relates to ophthalmic compositions useful in the treatment of surface disorders of the eye caused by abnormal precorneal tear film, and most specifically to the compositions for treatment of so-called dry eye conditions.Type: GrantFiled: August 10, 1987Date of Patent: September 12, 1989Assignee: Spectra Pharmaceutical Services, Inc.Inventors: A. Edward Maumenee, Richard L. Giovanoni
-
Patent number: 4866050Abstract: A dexamethasone delivery composition includes dexamethasone disposed in a cellulosic gel, preferably a hydroxycellulose gel. Lidocaine solubilizes the dexamethasone into the gel to provide a dexamethasone composition of increased concentration and enhanced tissue penetration capability. A method for the transdermal delivery of dexamethasone includes the step of applying the dexamethasone gel composition of the invention to the tissue of a patient and applying ultrasound at the site to effect penetration of the dexamethasone.Type: GrantFiled: April 27, 1988Date of Patent: September 12, 1989Inventor: Daniel Ben-Amoz
-
Patent number: 4835142Abstract: A powdery pharmaceutical composition for application to the mucosa of the oral or nasal cavity including: (a) a base selected from the group consisting of lower alkyl ethers of cellulose; (b) a pharmaceutically effective amount of a drug selected from the group consisting of steroid or glycyrrhizic acid type anti-inflammatory agents; and (c) a stabilizer for the drug composed of at least one low irritant solid organic acid selected from the group consisting of saturated higher aliphatic monocarboxylic acids having 12 or more carbon atoms, aliphatic polycarboxylic acid, hydroxy aliphatic polycarboxylic acids, aromatic carboxylic acids, unsaturated lower aliphatic monocarboxylic acids having six or less carbon atoms, and cellulose derivatives having carboxyl group.Type: GrantFiled: February 4, 1988Date of Patent: May 30, 1989Assignee: Teijin LimitedInventors: Yoshiki Suzuki, Hiroshi Ikura
-
Patent number: 4804656Abstract: The invention refers to compounds having anti-inflammatory activity characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula X.sub.1 represents a hydrogen, chlorine, bromine or fluorine atom;X.sub.2 represents a hydrogen, chlorine, bromine or fluorine atom;R.sub.1 represents a .beta.-hydroxy group, a .beta.-chlorine atom or an oxo group;R.sub.2 represents a hydrogen atom, a methylene group or an .alpha.- or .beta.-methyl group;R.sub.3 represents a hydrogen atom or an acyl group of 1 through 8 carbon atoms;R.sub.4 represents a hydrogen atom, a (C.sub.1 -C.sub.5) alkyl group or a phenyl group;R.sub.5 represents a hydrogen atom, a (C.sub.1 -C.sub.5) alkyl group or a phenyl group;Y represents either CR.sub.7 R.sub.8, O, S or NR.sub.9, where R.sub.7, R.sub.8 and R.sub.9 are selected from hydrogen or from straight or branched hydrocarbon chains having 1-8 carbon atoms or from a phenyl group.R.sub.Type: GrantFiled: April 3, 1986Date of Patent: February 14, 1989Assignee: Aktiebolaget DracoInventors: Paul H. Andersson, Per T. Andersson, Bengt I. Axelsson, Bror A. Thalen, Jan W. Trofast
-
Patent number: 4775529Abstract: An improved lotion formulation for the topical administration of corticosteroids in a hydro-alcoholic base containing propylene glycol.Type: GrantFiled: May 21, 1987Date of Patent: October 4, 1988Assignee: Schering CorporationInventors: Joel A. Sequeira, Farah J. Munayyer, Rebecca Galeos
-
Patent number: 4771042Abstract: A method of inhibiting angiogenesis in a warm blooded animal which comprises administering to said animal an anti-angiogenic effective amount of a compound of the formula: ##STR1## wherein the dotted line between positions C-1 and C-2 means the presence or absence of a double bond; the .about.bond at C-6 denotes .alpha. or .beta.;wherein R.sub.1 is CH.sub.3 or --C.sub.2 H.sub.5 ;wherein R.sub.2 is H, and R.sub.3 is in the .alpha.-position and is --OH, --O-alkyl(C.sub.1 -C.sub.12), --OC(.dbd.O)alkyl(C.sub.1 -C.sub.12), --OC(.dbd.O)aryl, --OC(.dbd.O)N(R).sub.2, or --OC(.dbd.O)OR.sub.7, wherein aryl is furyl, thienyl, pyrrolyl, or pyridyl wherein each of said hetero moiety is optionally substituted with one or two (C.sub.1 -C.sub.4)-alkyl groups or aryl is --(CH.sub.2).sub.f -phenyl wherein f is 0 to 2 and wherein the phenyl ring is optionally substituted with one to three groups selected from chlorine, fluorine, bromine, alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), thioalkoxy(C.sub.1 -C.sub.3), Cl.sub.Type: GrantFiled: January 24, 1986Date of Patent: September 13, 1988Assignee: The Upjohn CompanyInventors: John M. Braughler, Edward D. Hall, John M. McCall, Wendell Wierenga, Judah Folkman
-
Patent number: 4710495Abstract: Novel soft steroid anti-inflammatory agents, said agents being esters or thioesters of 17.alpha.-alkoxy-11.beta.-hydroxyandrost-4-en-3-one-17.beta.-carboxylic acids, pharmaceutical compositions containing said agents, novel chemical intermediates useful in the preparation of said agents and methods of administering same to mammals in the treatment of inflammation. Preferred compounds are the haloalkyl esters of 17.alpha.-alkoxy-11.beta.-hydroxyandrost-4-en-3-one-17.beta.-carboxylic acids.Type: GrantFiled: April 8, 1985Date of Patent: December 1, 1987Assignee: Otsuka Pharmaceutical Co., Ltd.Inventor: Nicholas S. Bodor
-
Patent number: 4705783Abstract: 9 alpha, 11 beta and 11 beta-substituted estranes are disclosed which exhibit elevated estrogenic and postcoital contraceptive activities. A process for their manufacture and their use in pharmaceuticals is also disclosed.Type: GrantFiled: June 25, 1985Date of Patent: November 10, 1987Assignee: SRI InternationalInventors: David F. Crowe, Masato Tanabe, Richard Peters
-
Patent number: 4701451Abstract: Compounds of Formula I ##STR1## wherein the bond is a single bond or a double bond,X is hydrogen, fluorine, chlorine, or bromine,R.sub.1 is formyl, alkanoyl or alkoxyalkyl each of which contains 2-8 carbon atoms, or benzoyl, andY is chlorine, hydroxy, formyl, alkanoyloxy of 2-8 carbon atoms, or benzoyloxy,have valuable anti-inflammatory properties.Type: GrantFiled: October 29, 1985Date of Patent: October 20, 1987Assignee: Schering AktiengesellschaftInventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert, Michael Toepert, Hans Wendt
-
Patent number: 4701450Abstract: The invention relates to a group of .DELTA..sup.4 - and .DELTA..sup.5(10) -oestrene derivatives having an alkyl(1-4 C) substituent in position 6 or 7, an oxy substituent in position 17.beta. and optionally an oxo- or oxy-substituent in position 3 and a hydrocarbyl(1-4 C) group in position 17.alpha., for use as immunomodulator. The compounds are in particular suitable for therapeutic use in the treatment of auto-immune diseases.Type: GrantFiled: March 18, 1985Date of Patent: October 20, 1987Assignee: Akzo N.V.Inventors: Jan Kelder, Hermanus A. M. Verheul
-
Patent number: 4693999Abstract: Pharmaceutical composition for administration primarily to the respiratory tract when treating and controlling anti-inflammatory conditions comprising liposomes in combination with a compound of the formula ##STR1## and R.sup.1 is a saturated or unsaturated, straight or branched alkyl group with 11-19 carbon atoms and R is H, --COCH.sub.3, --COC.sub.2 H.sub.5, --CO(CH.sub.2).sub.2 CH.sub.3 or --CO(CH.sub.2).sub.3 CH.sub.3.The invention also refers to the compounds of the formula I per se processes for preparation of these compounds and to a method for the treatment of inflammatory conditions.Type: GrantFiled: July 3, 1985Date of Patent: September 15, 1987Assignee: Aktiebolaget DracoInventors: Bengt I. Axelsson, Ralph L. Brattsand, Carl M. O. Dahlback, Leif A. Kallstrom, Jan W. Trofast
-
Patent number: 4686214Abstract: Anti-inflammatory compounds and a method of treating inflamed ocular tissue utilizing these compounds are described. The steroidal actives are advantageously characterized in that they do not cause any significant increase in intraocular pressure during chronic use.Type: GrantFiled: October 30, 1985Date of Patent: August 11, 1987Assignee: Alcon Laboratories, Inc.Inventor: John J. Boltralik
-
Patent number: 4634696Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.Type: GrantFiled: July 30, 1985Date of Patent: January 6, 1987Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert
-
Patent number: 4619922Abstract: 6.alpha.,16.alpha.-Dimethyl corticoids of general Formula I ##STR1## wherein the bond is a single bond or a double bond,X is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom,R.sub.1 is a formyl group, an alkanoyl group or alkoxyalkyl group of 2-8 carbon atoms, or a benzoyl group, andY is a hydrogen atom, a chlorine atom, a hydroxy group, a formyl group, an alkanoyloxy group of 2-8 carbon atoms, or a benzoyloxy group,are pharmacologically effective compounds.Type: GrantFiled: January 2, 1985Date of Patent: October 28, 1986Assignee: Schering AktiengesellschaftInventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Michael Topert
-
Patent number: 4619921Abstract: Novel 6.alpha.,9.alpha.,21-trihalogeno-11.beta.-hydroxy-16.alpha. or 16.beta.-methyl-17.alpha.-propionyloxy-pregn-4-ene-3,20-dione compounds of the formula ##STR1## in which X represents chlorine or flourine, R represents the group --CH.sub.2 CH--, --CH.dbd.CH-- or --CH.dbd.CCl--, the chlorine atom being in the positon 2 of the steroid numbering, and in which the 16-methyl radical is .alpha.- or .beta.-oriented, are useful pharmaceuticals, especially anti-inflammatory agents for topical administration.Type: GrantFiled: April 20, 1984Date of Patent: October 28, 1986Assignee: Ciba-Geigy CorporationInventors: Jaroslav Kalvoda, Georg Anner
-
Patent number: 4607028Abstract: Novel 17.beta.-methoxycarbonyl derivatives of the androstane series of the formula ##STR1## in which R represents alkyl having from 1 to 4 carbon atoms are distinguished by a high local anti-inflammatory activity without having any systemic side effects. The compounds are manufactured by conventional processes of steroid chemistry.Type: GrantFiled: August 9, 1984Date of Patent: August 19, 1986Assignee: Ciba-Geigy CorporationInventor: Julius Schmidlin
-
Patent number: 4605648Abstract: A method of suppressing the outbreaks of Herpes Simplex virus lesions and related symptoms in humans by administering to an individual who has experienced Herpes Simplex virus outbreaks a therapeutically effective dosage of an androgenic flurosteroid.Type: GrantFiled: August 15, 1985Date of Patent: August 12, 1986Inventor: E. Pendleton Price
-
Patent number: RE34136Abstract: 9 alpha, 11 beta and 11 beta-substituted estranes are disclosed which exhibit elevated estrogenic and postcoital contraceptive activities. A process for their manufacture and their use in pharmaceuticals is also disclosed.Type: GrantFiled: November 9, 1989Date of Patent: December 1, 1992Assignee: SRI InternationalInventors: David F. Crowe, Masato Tanabe, Richard Peters