9-position Substituted Patents (Class 514/180)
  • Patent number: 5173483
    Abstract: 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: Grant
    Filed: September 5, 1990
    Date of Patent: December 22, 1992
    Assignee: Roussel Uclaf
    Inventor: J. A. Grandadam
  • Patent number: 5166145
    Abstract: A dosage form is disclosed comprising an antiemetic and antinausea drug for treating vomiting and nausea.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: November 24, 1992
    Assignee: Alza Corporation
    Inventors: Francisco Jao, Hoa I. Huynh, Patrick S. L. Wong
  • Patent number: 5166200
    Abstract: 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: Grant
    Filed: April 11, 1991
    Date of Patent: November 24, 1992
    Assignee: Snow Brand Milk Products Company, Limited
    Inventors: Nobuaki Fujise, Yasushi Yamashita, Hiroaki Takaoka, Nobuyoshi Honda, Makoto Yoshihama
  • Patent number: 5124392
    Abstract: 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: Grant
    Filed: May 31, 1990
    Date of Patent: June 23, 1992
    Assignee: Alcon Laboratories, Inc.
    Inventors: Stella M. Robertson, Herman M. Kunkle, Jr.
  • Patent number: 5120723
    Abstract: 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: Grant
    Filed: May 10, 1990
    Date of Patent: June 9, 1992
    Assignee: University of Southern California
    Inventors: Kelvin W. Gee, Michael B. Bolger
  • Patent number: 5116829
    Abstract: 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: Grant
    Filed: April 10, 1991
    Date of Patent: May 26, 1992
    Assignee: Kao Corporation
    Inventors: Kimihiko Hori, Yasuto Suzuki, Tomoki Morioka, Shigeru Moriwaki, Osamu Hirota, Shuichi Tsuchiya
  • Patent number: 5112620
    Abstract: 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: Grant
    Filed: September 20, 1990
    Date of Patent: May 12, 1992
    Assignee: Mikkur, Inc.
    Inventors: Michael A. Repka, Thomas G. Gerding
  • Patent number: 5095010
    Abstract: Combination products containing an antigestagen, a glucocorticoid and a prostaglandin are suitable for combined use in inducing labor or terminating pregnancy.
    Type: Grant
    Filed: November 13, 1990
    Date of Patent: March 10, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Walter Elger, Sybille Beier
  • Patent number: 5082835
    Abstract: 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: Grant
    Filed: March 9, 1990
    Date of Patent: January 21, 1992
    Assignee: 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: 5063222
    Abstract: 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: Grant
    Filed: April 13, 1990
    Date of Patent: November 5, 1991
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Teruo Komoto, Junji Okawa, Yoichiro Ogawa, Susumu Sato, Naokata Taido, Tadayuki Kuraishi
  • Patent number: 5061700
    Abstract: 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: Grant
    Filed: November 16, 1989
    Date of Patent: October 29, 1991
    Assignee: Gordon Jay Dow
    Inventors: Gordon J. Dow, Debra A. Dow
  • Patent number: 5047419
    Abstract: 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: Grant
    Filed: October 24, 1988
    Date of Patent: September 10, 1991
    Assignee: Eastman Kodak Company
    Inventors: Michael R. Detty, Stephen K. Powers
  • Patent number: 5043165
    Abstract: 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: Grant
    Filed: December 14, 1988
    Date of Patent: August 27, 1991
    Assignee: Liposome Technology, Inc.
    Inventor: Ramachandran Radhakrishnan
  • Patent number: 5028600
    Abstract: 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: Grant
    Filed: February 28, 1989
    Date of Patent: July 2, 1991
    Assignee: KabiVitrum AB
    Inventor: Roland I. Jeppsson
  • Patent number: 5026693
    Abstract: 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: Grant
    Filed: May 21, 1990
    Date of Patent: June 25, 1991
    Assignee: Hovione Inter Ltd.
    Inventors: Ivan Villax, William Heggie, Philip R. Page
  • Patent number: 5023251
    Abstract: 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: Grant
    Filed: October 31, 1989
    Date of Patent: June 11, 1991
    Assignee: Beiersdorf AG
    Inventors: Henning Sattler, Bodo Asmussen
  • Patent number: 5019569
    Abstract: 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: Grant
    Filed: August 31, 1989
    Date of Patent: May 28, 1991
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Albert M. Kligman, James A. Mezick, Robert J. Capetola
  • Patent number: 4985418
    Abstract: Use of fluticasone propionate in the treatment of bowel diseases when administered by the oral, stomal or rectal routes.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: January 15, 1991
    Assignee: Glaxo Group Limited
    Inventor: David A. Richards
  • Patent number: 4970206
    Abstract: The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.
    Type: Grant
    Filed: May 8, 1989
    Date of Patent: November 13, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Takeru Higuchi
  • Patent number: 4939135
    Abstract: 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: Grant
    Filed: October 3, 1988
    Date of Patent: July 3, 1990
    Assignee: Alcon Laboratories, Inc.
    Inventors: Stella M. Robertson, Herman M. Kunkle, Jr., Michael E. Stern
  • Patent number: 4918065
    Abstract: 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: Grant
    Filed: October 17, 1988
    Date of Patent: April 17, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Wolfgang Stindl, Ingfried Zimmerman, Renate Reckers, Hans Wendt, Rainold Arndt
  • Patent number: 4913852
    Abstract: 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: Grant
    Filed: February 24, 1988
    Date of Patent: April 3, 1990
    Inventors: Catherine Milioni, Constantin Efthyimiopoulos, Bernard Koch, Louis Jung, Jean Jung
  • Patent number: 4910192
    Abstract: 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: Grant
    Filed: December 4, 1987
    Date of Patent: March 20, 1990
    Assignee: SRI International
    Inventors: Mitchell A. Avery, Masato Tanabe, Dennis Yasuda, George Detre
  • Patent number: 4904649
    Abstract: 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: Grant
    Filed: March 27, 1987
    Date of Patent: February 27, 1990
    Assignee: New England Medical Center Hospitals, Inc.
    Inventor: Bernard Schwartz
  • Patent number: 4889847
    Abstract: The present invention is directed to the topical administration of a retinoid-containing pharmaceutical composition for the prevention of glucocorticoid-induced skin atrophy.
    Type: Grant
    Filed: November 3, 1986
    Date of Patent: December 26, 1989
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Albert M. Kligman, James A. Mezick, Robert J. Capetola
  • Patent number: 4879274
    Abstract: 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: Grant
    Filed: September 12, 1986
    Date of Patent: November 7, 1989
    Assignee: Kao Corporation
    Inventors: Tetsuro Kamiya, Shuichi Tsuchiya, Kenji Hara
  • Patent number: 4876250
    Abstract: 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: Grant
    Filed: October 31, 1988
    Date of Patent: October 24, 1989
    Assignee: Alcon Laboratories, Inc.
    Inventor: Abbot F. Clark
  • Patent number: 4870066
    Abstract: 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: Grant
    Filed: August 11, 1986
    Date of Patent: September 26, 1989
    Assignee: The University of Kentucky Research Foundation
    Inventors: Lee A. Edgerton, Bruce T. Eckerle
  • Patent number: 4868168
    Abstract: 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: Grant
    Filed: November 13, 1987
    Date of Patent: September 19, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard L. O'Laughlin, Andrea Panaggio, Sailesh A. Varia
  • Patent number: 4868170
    Abstract: 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: Grant
    Filed: November 13, 1987
    Date of Patent: September 19, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Marilia M. Faustino, Sailesh A. Varia, Abu T. M. Serajuddin
  • Patent number: 4868169
    Abstract: 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: Grant
    Filed: November 13, 1987
    Date of Patent: September 19, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard L. O'Laughlin, Andrea Panaggio, Sailesh A. Varia
  • Patent number: 4866051
    Abstract: 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: Grant
    Filed: January 30, 1985
    Date of Patent: September 12, 1989
    Assignee: Glaxo Group Limited
    Inventors: John H. Hunt, John M. Padfield
  • Patent number: 4866049
    Abstract: 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: Grant
    Filed: August 10, 1987
    Date of Patent: September 12, 1989
    Assignee: Spectra Pharmaceutical Services, Inc.
    Inventors: A. Edward Maumenee, Richard L. Giovanoni
  • Patent number: 4866050
    Abstract: 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: Grant
    Filed: April 27, 1988
    Date of Patent: September 12, 1989
    Inventor: Daniel Ben-Amoz
  • Patent number: 4835142
    Abstract: 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: Grant
    Filed: February 4, 1988
    Date of Patent: May 30, 1989
    Assignee: Teijin Limited
    Inventors: Yoshiki Suzuki, Hiroshi Ikura
  • Patent number: 4804656
    Abstract: 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: Grant
    Filed: April 3, 1986
    Date of Patent: February 14, 1989
    Assignee: Aktiebolaget Draco
    Inventors: Paul H. Andersson, Per T. Andersson, Bengt I. Axelsson, Bror A. Thalen, Jan W. Trofast
  • Patent number: 4775529
    Abstract: An improved lotion formulation for the topical administration of corticosteroids in a hydro-alcoholic base containing propylene glycol.
    Type: Grant
    Filed: May 21, 1987
    Date of Patent: October 4, 1988
    Assignee: Schering Corporation
    Inventors: Joel A. Sequeira, Farah J. Munayyer, Rebecca Galeos
  • Patent number: 4771042
    Abstract: 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: Grant
    Filed: January 24, 1986
    Date of Patent: September 13, 1988
    Assignee: The Upjohn Company
    Inventors: John M. Braughler, Edward D. Hall, John M. McCall, Wendell Wierenga, Judah Folkman
  • Patent number: 4710495
    Abstract: 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: Grant
    Filed: April 8, 1985
    Date of Patent: December 1, 1987
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventor: Nicholas S. Bodor
  • Patent number: 4705783
    Abstract: 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: Grant
    Filed: June 25, 1985
    Date of Patent: November 10, 1987
    Assignee: SRI International
    Inventors: David F. Crowe, Masato Tanabe, Richard Peters
  • Patent number: 4701451
    Abstract: 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: Grant
    Filed: October 29, 1985
    Date of Patent: October 20, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert, Michael Toepert, Hans Wendt
  • Patent number: 4701450
    Abstract: 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: Grant
    Filed: March 18, 1985
    Date of Patent: October 20, 1987
    Assignee: Akzo N.V.
    Inventors: Jan Kelder, Hermanus A. M. Verheul
  • Patent number: 4693999
    Abstract: 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: Grant
    Filed: July 3, 1985
    Date of Patent: September 15, 1987
    Assignee: Aktiebolaget Draco
    Inventors: Bengt I. Axelsson, Ralph L. Brattsand, Carl M. O. Dahlback, Leif A. Kallstrom, Jan W. Trofast
  • Patent number: 4686214
    Abstract: 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: Grant
    Filed: October 30, 1985
    Date of Patent: August 11, 1987
    Assignee: Alcon Laboratories, Inc.
    Inventor: John J. Boltralik
  • Patent number: 4634696
    Abstract: 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: Grant
    Filed: July 30, 1985
    Date of Patent: January 6, 1987
    Assignee: Roussel Uclaf
    Inventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert
  • Patent number: 4619922
    Abstract: 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: Grant
    Filed: January 2, 1985
    Date of Patent: October 28, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Henry Laurent, Helmut Hofmeister, Michael Topert
  • Patent number: 4619921
    Abstract: 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: Grant
    Filed: April 20, 1984
    Date of Patent: October 28, 1986
    Assignee: Ciba-Geigy Corporation
    Inventors: Jaroslav Kalvoda, Georg Anner
  • Patent number: 4607028
    Abstract: 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: Grant
    Filed: August 9, 1984
    Date of Patent: August 19, 1986
    Assignee: Ciba-Geigy Corporation
    Inventor: Julius Schmidlin
  • Patent number: 4605648
    Abstract: 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: Grant
    Filed: August 15, 1985
    Date of Patent: August 12, 1986
    Inventor: E. Pendleton Price
  • Patent number: RE34136
    Abstract: 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: Grant
    Filed: November 9, 1989
    Date of Patent: December 1, 1992
    Assignee: SRI International
    Inventors: David F. Crowe, Masato Tanabe, Richard Peters