-o-c-o- Is Part Of A Hetero Ring (e.g., Acetonide, Etc.) Patents (Class 514/174)
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Patent number: 5939409Abstract: Disclosed are processes for preparing the 22R and 22S epimers of the compound ##STR1## The processes involve acetalization, transacetalization, hydrolysis (of an ester) or hydrogenation (of a diene) of an appropriate starting material. Also disclosed are pharmaceutical compositions comprising the compounds produced by the processes and methods of treatment of inflammatory and allergic conditions employing the compounds.Type: GrantFiled: October 7, 1997Date of Patent: August 17, 1999Assignee: Astra AktiebolagInventors: Paul Andersson, Bengt Axelsson, Ralph Brattsand, Arne Thalen
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Patent number: 5929111Abstract: A-seco steroids are disclosed. Methods of use are disclosed for treating ophthalmic pathological neovascularization and controlling intraocular pressure.Type: GrantFiled: December 17, 1997Date of Patent: July 27, 1999Assignee: Alcon Laboratories, Inc.Inventors: Raymond E. Conrow, Abbot F. Clark
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Patent number: 5908833Abstract: Novel compounds which are a glucocorticosteroid (GCS) chemically bound to a sugar, having the general formulaGCS.sup.1 --O--Sugar.sup.1for colon- or ileum-specific delivery of the GCS to inflamed bowel mucosa, as well as processes for their preparation, pharmaceutical preparations containing the compounds and the use of said compounds in therapy.Type: GrantFiled: December 13, 1996Date of Patent: June 1, 1999Assignee: Aktiebolaget AstraInventors: Ralph Lennart Brattsand, Peter Edman, Thomas Hogberg, Stinabritt Nilsson, Bror Arne Thalen, Jan Erik Ulmius
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Patent number: 5902609Abstract: This invention pertains to a composition for controlling wound scar production containing a calcium antagonist and a protein synthesis inhibitor. The method can be used to minimize wound scars, such as hypertrophic wound healing disorders keloids and burn scar contractures in humans or other mammals, particularly those individually prone to excesssive scarring Calcium antagonist treatment can also be used to control diseases associated with excessive scarring. such as cirrhosis of the liver, constructive pericarditis Dupuytren's disease of the hand, plantar fibrosis of the foot, and various other fibromatoses.Type: GrantFiled: October 25, 1996Date of Patent: May 11, 1999Assignee: Massachusetts Institute of TechnologyInventor: Raphael C. Lee
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Patent number: 5888995Abstract: The invention concerns compounds of formula I ##STR1## in which R.sub.1 is hydrogen or a straight or branched hydrocarbon chain; R.sub.2 is hydrogen or a straight or branched hydrocarbon chain; R.sub.3 is acyl; X.sub.1 is hydrogen, fluorine or chlorine; and X.sub.2 is hydrogen, fluorine or chlorine. Also disclosed are processes for preparation of the compounds, pharmaceutical compositions containing them and methods employing the compounds in the treatment of inflammatory and allergic conditions.Type: GrantFiled: June 22, 1995Date of Patent: March 30, 1999Assignee: Astra AktiebolagInventors: Bengt Ingemar Axelsson, Ralph Lennart Brattsand, Leif Arne Kallstrom, Bror Arne Thalen
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Patent number: 5872147Abstract: The subject invention provides a method of treating a symptom associated with chronic obstructive pulmonary disease in a patient suffering from chronic obstructive pulmonary disease which comprises administering a therapeutically effective amount of an oxandrolone to the patient. The subject invention further provides a method of improving functional capacity and/or pulmonary function in a patient suffering from chronic obstructive pulmonary disease which comprises administering a therapeutically effective amount of an oxandrolone to the patient.Type: GrantFiled: December 5, 1997Date of Patent: February 16, 1999Assignee: Bio-Technology General Corp.Inventor: Robert E. Bowen
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Patent number: 5863910Abstract: The present disclosure relates to an oral formulation for treating gastrointestinal inflammation that includes an effective amount of budesonide suspended in an edible oil, typically a vegetable oil. A method for treating gastrointestinal inflammation in mammals is also described and includes orally administering a composition of this invention to a mammal. In one embodiment, an initial dosage is administered daily for about two to four weeks and the dosage is subsequently tapered, generally at about two week intervals, in response to a reduction in symptoms until a minimum dose that controls symptoms is achieved.Type: GrantFiled: October 21, 1997Date of Patent: January 26, 1999Inventors: Joel Bolonick, Alan Stewart
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Patent number: 5855897Abstract: The present invention relates to topical compositions useful in enhancing lipid synthesis in skin comprising an effective amount of cafestol, in combination with a pharmaceutically or cosmetically acceptable carrier. Such compositions are useful in treatment or prevention of dry skin and conditions in which the skin's lipid barrier is defective or damaged.Type: GrantFiled: September 13, 1996Date of Patent: January 5, 1999Assignee: E-L Management Corp.Inventor: Edward Pelle
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Patent number: 5847009Abstract: Methods for preventing or ameliorating the transient adverse physiological response to particulate dispersions (TAPR response) when these dispersions are administered parenterally to a patient. The methods comprise the administration of a prophylactic anti-inflammatory drug prior to administration of the particulate-containing material, and optionally during administration as well. Preferred drugs are cyclooxygenase inhibitors and corticosteroids.Type: GrantFiled: October 15, 1993Date of Patent: December 8, 1998Assignee: Alliance Pharmaceutical Corp.Inventor: David M. Long, Jr.
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Patent number: 5837698Abstract: The present invention relates to a pharmaceutical composition or preparation which comprises hydroxyl containing steroidal hormones and organic nitrite/nitrate or other nitric oxide donating agents.Type: GrantFiled: May 2, 1996Date of Patent: November 17, 1998Assignee: G. D. Searle & Co.Inventors: Foe S. Tjoeng, Mark G. Currie, Mark E. Zupec
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Patent number: 5824669Abstract: Disclosed are (i) compounds of a steroid, a .beta.-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO.sub.2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, .beta.-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO.sub.2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO.sup.+) or nitroxyl (NO.sup.-), or as the neutral species, nitric oxide (NO.circle-solid.) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.Type: GrantFiled: March 22, 1996Date of Patent: October 20, 1998Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Stewart K. Richardson
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Patent number: 5801165Abstract: Compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, and are as defined herein, their use as antiinflammatory, immunosuppressive, and antiallergic agents, pharmaceutical compositions comprising them, and methods for their preparation comprising irradiating compounds of formula II ##STR2## under an inert atmosphere, in the presence or absence of a compound of formula R.sub.3 --S--S(O).sub.m --R.sub.8, where R.sub.7, R.sub.8, and m are as defined herein, and methods for their preparation comprising oxidizing, reducing, halogenating, or alkylating compounds of formula I are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: September 1, 1998Assignee: Rhone-Poulenc Rorer LimitedInventors: Michael John Ashton, Sven Jan-Anders Karlsson, Bernard Yvon Jack Vacher, Michael Thomas Withnall
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Patent number: 5792758Abstract: The present invention discloses novel steroid nitrite ester derivatives, and to their use treating inflammatory diseases.Type: GrantFiled: December 8, 1995Date of Patent: August 11, 1998Assignee: G. D. Searle & Co.Inventors: Foe S. Tjoeng, Mark G. Currie, Mark E. Zupec
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Patent number: 5770589Abstract: In the treatment of age-related macular degeneration, a method for treating an inflammatory response in the macula of the eye by use of a depot injection of a suitable anti-inflammatory agent into the vitreous humour is described. Triamcinolone acetomide (T) is employed which is in crystalline form and is sparingly soluble in the vitreous of the eye, and which does not leave any vision impairing residue in the eye.Type: GrantFiled: September 27, 1996Date of Patent: June 23, 1998Assignee: The University of SydneyInventors: Francis Alfred Billson, Philip Leslie Penfold
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Patent number: 5767113Abstract: In accordance with the present invention, it has been discovered that certain synthetic steroid compounds are capable of inhibiting the efflux pump which is believed to be responsible for multidrug resistance, while at the same time activating glucocorticoid-induced response. Thus, chemotherapy of glucocorticoid sensitive tumors can be enhanced by use of a compound having the dual ability to activate glucocorticoid-induced response and facilitate the accumulation of drug at the target site, with reduced or eliminated competition by the drug efflux system.Type: GrantFiled: May 10, 1995Date of Patent: June 16, 1998Assignee: The Salk Institute For Biological StudiesInventors: Suzanne Bourgeois Cohn, Donald J. Gruol
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Patent number: 5763430Abstract: A method of treating a viral infection includes administering an effective amount of a compound having the following structure: ##STR1## or a pharmaceutically acceptable salt thereof. This compound treats the viral infection by suppressing the growth of a viral target cell. As one specific example, this compound may be used to treat HIV infection.Type: GrantFiled: June 7, 1995Date of Patent: June 9, 1998Assignee: Magainin Pharmaceuticals Inc.Inventor: Michael Zasloff
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Patent number: 5760025Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.Type: GrantFiled: March 31, 1995Date of Patent: June 2, 1998Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Hitoshi Kurata, Koki Ishibashi, Hiroyoshi Horikoshi, Takakazu Hamada
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Patent number: 5733901Abstract: Epimers of the compound having the formula (I) are disclosed, both in their pure form and mixed in any desire mix ratio.Type: GrantFiled: September 29, 1995Date of Patent: March 31, 1998Assignee: BYK Gulden Lomberg Chemische Fabrik GmbHInventor: Beate Gutterer
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11.beta.-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents
Patent number: 5728689Abstract: A method of inducing an antigestagenic effect by the administration of compounds of formula I: ##STR1## wherein, substituents are as defined in the specification.Type: GrantFiled: June 6, 1995Date of Patent: March 17, 1998Assignee: Schering AktiengesellschaftInventors: Arwed Cleve, Cornelius Scheidges, Gunter Neef, Eckhard Ottow, Walter Elger, Sybille Beier -
Patent number: 5723455Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.Type: GrantFiled: March 11, 1997Date of Patent: March 3, 1998Assignee: SRI InternationalInventors: Masato Tanabe, Wan-Ru Chao, Wesley K. M. Chong, David F. Crowe
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Patent number: 5721226Abstract: A method of inhibiting angiogenesis in a patient includes administering to the patient an effective amount of squalamine or a pharmaceutically acceptable salt of squalamine. Alternatively, a compound according to the following Formula (III) (or a pharmaceutically acceptable salt thereof) can be administered: ##STR1## wherein Z.sub.5 is .alpha.-H or .beta.-H; each of the substituents Z.sub.7 is selected from the group of --H, --OH, --SH, --NH.sub.2, --F, --(C.sub.1 -C.sub.3)-alkyl, and --(C.sub.1 -C.sub.3)-alkoxy; and one of the substituents Z.sub.12 is --H and the other is --H or --OH. X' is a polyamine side chain of the formula --X.sub.1 --(CH.sub.2).sub.p --X.sub.2 --(CH.sub.2).sub.q --N(R.sup.II)(R.sup.III), wherein one of X.sub.1 and X.sub.2 is --N(R.sup.IV) and the other is selected from the group of --N(R.sup.V), --O, --S, and --CH.sub.2. R.sup.IV and R.sup.V are each --H or --(C.sub.1 -C.sub.3)-alkyl, p and q are each an integer of from 0 to 5 (but both are not 0). R.sup.II and R.sup.Type: GrantFiled: June 7, 1995Date of Patent: February 24, 1998Assignee: Magainin Pharmaceuticals Inc.Inventors: Leah L. Frye, Michael A. Zasloff, William A. Kinney, Robert Moriarty, Delwood C. Collins
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Patent number: 5721228Abstract: Topical rectal therapeutic composition containing, as the active ingredient, flunisolide and/or one or more ester derivatives of same, in combination with suitable excipients and/or diluents, for the treatment of inflammatory intestinal disorders.Type: GrantFiled: May 17, 1995Date of Patent: February 24, 1998Assignee: Valeas S.p.A. Industria Chimica E FarmaceuticaInventors: Virgilio Bernareggi, Maurizio Fano, Alessandro Gagnoni
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Patent number: 5707981Abstract: A pharmaceutical composition comprises a synergistic combination of about 0.01-0.15% by wt. triamcinolone acetonide and about 0.04-0.3% by wt. halcinonide as active ingredients, in combination with a pharmaceutically acceptable carrier.Type: GrantFiled: June 6, 1995Date of Patent: January 13, 1998Assignee: Psorial, L.L.C.Inventor: Georges Chriki
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Patent number: 5679668Abstract: The invention is a method of controlling fertility in male warm-blooded animals by administering a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 15 carbon atoms or taken together form a saturated heterocycle of 5 to 6 ring members optionally having a second ring heteroatom selected from the group consisting of sulfur, oxygen and nitrogen, R.sub.3 is an .alpha.-alkyl of 1 to 8 carbon atoms, n is an integer from 2 to 15, R.sub.4 is alkyl of 1 to 12 carbon atoms, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of up to 12 carbon atoms and the wavy lines indicate that the 17- and 20- asymmetrical centers are independent of the absolute R and S configurations and their non-toxic, pharmaceutically acceptable acid addition salts.Type: GrantFiled: August 2, 1996Date of Patent: October 21, 1997Assignee: Roussel UclafInventors: Armelle Bonfils, Daniel Philibert
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Patent number: 5674860Abstract: Effective amounts of formoterol and/or a physiologically acceptable salt and/or solvate thereof and budesonide are used in combination for simultaneous, sequential or separate administration by inhalation in the treatment of an inflammatory respiratory disorder, such as asthma.Type: GrantFiled: October 3, 1994Date of Patent: October 7, 1997Assignee: Astra AktiebolagInventors: Christer Carl Gustav Carling, Jan William Trofast
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Patent number: 5674861Abstract: Disclosed are the 22R and 22S epimers of compounds of the formula ##STR1## wherein X.sub.1 represents a fluorine atom, and X.sub.2 represents a hydrogen atom or a fluorine atom. Also disclosed are processes for the preparation of the compounds, pharmaceutical compositions comprising the compounds and methods of treatment of inflammatory and allergic conditions employing the compounds.Type: GrantFiled: August 31, 1993Date of Patent: October 7, 1997Assignee: Astra AktiebolagInventors: Paul Andersson, Bengt Axelsson, Ralph Brattsand, Arne Thalen
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Patent number: 5654293Abstract: The present invention relates to a topical oil-in-water emulsion composition comprising ketoconazole, an acetonide glucocorticosteroid and a dermatologically acceptable carrier, characterized by a pH above 2.5 and below 6, and a method of preparing said composition.Type: GrantFiled: June 14, 1995Date of Patent: August 5, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Marc Karel Jozef Fran.cedilla.ois, Alfons Jeanne Wouters, Gerard Frans Maria Jan Cauwenbergh
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Patent number: 5620966Abstract: The invention relates to a 11,21-bisphenyl-19-norpregnane derivative of formula I ##STR1## wherein R.sub.1 is selected from H, halogen, (1-6C)alkoxy, and NR.sub.5 R.sub.6, R.sub.5 and R.sub.6 being independently hydrogen or (1-6C)alkyl or R.sub.5 and R.sub.6 together are (3-6C)alkylene; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 together are a (1-3C)alkylenedioxy group, optionally substituted by one or more halogen atoms; R.sub.3 is methyl or ethyl; R.sub.4 is selected from C(O)-NR.sub.5 R.sub.6, SO.sub.n -(1-6C)alkyl optionally substituted by one or more halogen atoms, SO.sub.n -(3-6C)cycloalkyl, n being 1 or 2, SO.sub.2 -NR.sub.5 R.sub.6, 2-oxypyrrolidinyl, and NR.sub.5 R.sub.6 ; R.sub.7 is H or (1-6C)alkyl; R.sub.8 is H or carboxy-1-oxo(1-6C)alkyl; and X is selected from (H,OH), O, and NOH; 11 or a pharmaceutically acceptable salt thereof.The compounds of the invention have anti-glucocorticoid activity and can be used in treating or preventing glucocorticoid-dependent diseases.Type: GrantFiled: May 19, 1995Date of Patent: April 15, 1997Assignee: Akzo Nobel N.V.Inventors: Ronald Gebhard, Hendrikus A. A. van der Voort
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Patent number: 5618806Abstract: Invented are 17.alpha. and 17.beta.-substituted acyl-3-carboxy aromatic A ring analogues of steroidal synthetic compounds. Representative of such compounds include the following ##STR1## wherein Z is .alpha. or .beta. ##STR2## in which A is absent or present as a linear or branched, saturated or unsaturated hydrocarbon chain containing from 1-6 carbon atoms and R isa) a linear or branched, saturated or unsaturated hydrocarbon chain containing 1-12 carbon atoms substituted with one or more substituents selected from the group consisting of: --OC.sub.6 -C.sub.12 aryl, --OC.sub.1 -C.sub.4 alkyl, halogen, carboxy and --S(O).sub.n .sup.R.sup.7, where n is 0-2 and R.sup.7 is hydrogen or C.sub.1-4 alkyl;b) C.sub.3 -C.sub.8 nonaromatic, unsaturated or saturated, cycloalkyl, optionally substituted with one or more substituents selected from the group consisting of:--OC.sub.6 -C.sub.12 aryl, --(CH.sub.2).sub.m OH, --OC.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.12 aryl, C.sub.1 -C.sub.Type: GrantFiled: October 28, 1994Date of Patent: April 8, 1997Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy
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Patent number: 5616573Abstract: Glucocorticoids of general formula IR--Val--O--GC (II),are described,in whichO-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action,Val represents a valine radical in the 21-position of the corticoid andR means a hydrogen atom or a hydrocarbon radical with up to 32 carbon atoms that is optionally substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO.sub.2 groups and/or NH groups and their salts.Type: GrantFiled: October 6, 1995Date of Patent: April 1, 1997Assignee: Schering AktiengesellschaftInventors: Hans J. Zentel, Michael Topert, Henry Laurent, Thomas Brumby, Peter Esperling
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Patent number: 5614514Abstract: Compounds of the general formula (I), ##STR1## in which formula the 1,2-position is saturated or is a double bond, R.sub.1 is hydrogen or a straight or branched hydrocarbon chain, R.sub.2 is hydrogen or a straight or branched hydrocarbon chain, R.sub.3 is acyl, X.sub.1 is hydrogen or halogen, X.sub.2 is hydrogen or halogen and provided that 1) R.sub.1 and R.sub.2 are not simultaneously hydrogen, 2) X.sub.1 and X.sub.2 are not simultaneously hydrogen, 3) when the 1,2-position is a double bond, R.sub.1 and R.sub.2 are not simultaneously methyl groups, 4) when the 1,2-position is a double, R.sub.1 is a hydrogen atom and R.sub.2 is a straight or branched hydrocarbon chain having 1-10 carbon atoms R.sub.3 is acyl having 11-20 carbon atoms, processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment of inflammatory and allergic conditions.Type: GrantFiled: August 24, 1993Date of Patent: March 25, 1997Assignee: Aktiebolaget AstraInventors: Bengt Axelsson, Ralph Brattsand, Leif Kallstrom, Arne Thalen
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Patent number: 5599806Abstract: The invention describes hydrazino and hydroxyamino-14.beta.-hydroxyandrostane derivatives having general formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration and A, B, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have the meanings given in the description and their use in the treatment of cardiovascular disorders such as heart failure and hypertension.Type: GrantFiled: May 18, 1995Date of Patent: February 4, 1997Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Giuseppe Bianchi, Patrizia Ferrari, Elena Folpini, Piero Melloni
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Patent number: 5583127Abstract: Disclosed are 17-iminomethylalkenyl and 17-iminoalkyl-14.beta.-hydroxy-5.beta.-androstane derivatives of the formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration or a Z or E configuration; A represents (CH.sub.2).sub.m or --(CH.dbd.CH).sub.n --; m represents an integer number from 1 to 6; n represents an integer number from 1 to 3; R.sup.2 represents hydrogen or hydroxy; R.sup.1 represents hydrogen, C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5, which may be the same or different, represent hydrogen, C.sub.1 -C.sub.4 alkyl or R.sup.4 and R.sup.5 may form, when taken together with the nitrogen atom, a five- or six- membered heterocyclic ring optionally containing one or more heteroatoms selected from oxygen and nitrogen; R.sup.3 represents NHC(.dbd.X)NR.sup.6 R.sup.7 or OR.sup.8 wherein R.sup.6 and R.sup.7, which may be the same or different, represent hydrogen, methyl, or C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.Type: GrantFiled: December 23, 1994Date of Patent: December 10, 1996Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Giuseppe Bianchi, Patrizia Ferrari, Elena Folpini, Piero Melloni
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Patent number: 5569678Abstract: This invention pertains to a method for controlling wound scar production by administering a calcium antagonist, alone or in a combination with or followed by a steroid, to the wound site. The method can be used to minimize wound scars, such as hypertrophic wound healing disorders, keloids and burn scar contractures in humans or other mammals, particularly those individually prone to excesssive scarring.Type: GrantFiled: February 1, 1994Date of Patent: October 29, 1996Assignees: Massachusetts Institute of Technology, Arch Develop.Inventor: Raphael C. Lee
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Patent number: 5536714Abstract: The invention includes compounds of formula (I): ##STR1## in which R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl; and pharmaceutically acceptable salts and esters of the compounds. The compounds have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydro-testosterone.Type: GrantFiled: January 19, 1995Date of Patent: July 16, 1996Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Hitoshi Kurata, Koki Ishibashi, Hiroyoshi Horikoshi, Takakazu Hamada
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Patent number: 5482934Abstract: The present invention relates to compounds of the formula: ##STR1## in which X.sub.1 and X.sub.2 correspond to H or F without distinction; R.sub.1 represents the following radicals: ##STR2## and R.sub.2 represents the radicals ##STR3## in the form of an R epimer, an S epimer, or a stereoisomeric mixture of the R and S epimers in terms of the orientation of the substituents on the carbon atom at position 22, novel intermediates and a method of their preparation by hydrolysis-ketalization, and use of such compounds as drugs and/or therapeutic agents.Type: GrantFiled: July 20, 1994Date of Patent: January 9, 1996Assignee: Especialidades Latinas Medicamentos Universales, S.A. (Elmu, S.A.)Inventors: Jose Calatayud, Jose R. Conde, Manuel Luna
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Patent number: 5420120Abstract: Topically administrable C-21 thioether glucocorticoid steroid derivatives are disclosed as effective anti-inflammatory agents for the treatment of ophthalmic inflammatory disorders. These C-21 thioether derivatives do not cause a significant increase in intraocular pressure as a side effect.Type: GrantFiled: December 17, 1993Date of Patent: May 30, 1995Assignee: Alcon Laboratories, Inc.Inventor: John J. Boltralik
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Patent number: 5382434Abstract: Disclosed are dry pharmaceutical preparations containing potent steroidal medicinal agents in combination with an excipient capable of binding the agent to an extent greater than 80% and a having a demixing potential of less than 10% for said agent. Such excipients include spray-dried polyalcohols, granulated .alpha.-lactose monohydrate, or mixtures thereof. Also disclosed is a process of manufacturing stable tablets containing nearly identical amounts of at least one steroidal medicinal agent present in each tablet in an amount varying from 0.005 to 0.5 percent by weight of the tablet. Also disclosed is a dry mix consisting essentially of 1 to 100 parts, by weight, of at least one medicinal agent uniformly distributed throughout 2000 to 20,000 parts, by weight, of the described excipients. The mixture can be used to make dry dosage forms such as capsules, tablets, powders, and slugged granulates.Type: GrantFiled: March 22, 1994Date of Patent: January 17, 1995Assignee: Akzo N.V.Inventors: Pieter de Haan, M. Deurloo
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Patent number: 5272140Abstract: The invention relates to 11-aryl steroid derivatives, having the structure ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described in the specificationand to processes for their preparation and to pharmaceuticals comprising these compounds.These compounds exhibit a strong anti-progestinic activity and a weak or non-existent anti-glucocorticoid activity.Type: GrantFiled: February 27, 1990Date of Patent: December 21, 1993Assignee: Akzo N.V.Inventor: Hubert J. J. Loozen
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Patent number: 5236906Abstract: A topical therapeutic preparation which contains an adrenocortical hormone and hyaluronic acid, the amount of said adrenocortical hormone being lower than the usual clinical dose of it, is used for combatting a skin disease.Type: GrantFiled: January 3, 1991Date of Patent: August 17, 1993Assignee: Takeda Chemical Industries, Ltd.Inventor: Toshiko Yamamoto
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Patent number: 5183815Abstract: Described are new agents for treating bone disorders associated with a reduction in bone mass and abnormalities in bone resportion or bone formation including osteoporosis. Paget's disease, bone metastases and malignant hypercalcemia. The agents are hydroxyl containing steroidal hormones, having bone resportion antagonist or bone formation stimulatory activity, covalently linked through the hydroxyl group via a bond hydrolyzable in the human body, e.g. carbamate or carbonate, which is further covalently linked to an amino, or hydroxy substituted alkylidene-1,1-bisphosphonate, through the respective amino or hydroxy group. The alkyl bisphosphonate moiety confers bone affinity. The agent acts by delivering the steroidal hormone directly to the bone target site where it is released for bone resorption antagonist or bone formation stimulatory action by hydrolysis of the hydrolyzable covalent bond.Type: GrantFiled: February 19, 1992Date of Patent: February 2, 1993Assignee: Merck & Co., Inc.Inventors: Walfred S. Saari, Gideon A. Rodan, Thorsten E. Fisher, Paul S. Anderson
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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
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Patent number: 5079239Abstract: Novel sterol disulfates have been isolated from the marine sponge Petrosia weinbergii. These compounds, and derivatives thereof, are useful antiviral compounds. One of these compounds is active against the AIDS virus and exhibits immunosuppressive activity.Type: GrantFiled: February 16, 1990Date of Patent: January 7, 1992Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: H. Howard Sun, Sue S. Cross, Frank Koehn, Malika Gunasekera
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Patent number: 5066648Abstract: The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.Type: GrantFiled: September 13, 1990Date of Patent: November 19, 1991Assignee: Merck & Co., Inc.Inventors: Jose Alexander, Takeru Higuchi, deceased
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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
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Patent number: 5053404Abstract: The invention relates to antiinflammatory compounds of the formula (I), ##STR1## wherein A stands for hydrogen or hydroxyl 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;R.sup.1 and R.sup.2, which are the same or different, stand for hydrogen or a C.sub.1-4 alkyl group; or one of R.sup.1 and R.sup.2 is hydrogen and the other is phenyl group; or R.sup.1 and R.sup.2 together form a C.sub.4-5 alkylene group;means 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: October 1, 1991Assignee: 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
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Patent number: 4983595Abstract: A non-stinging aqueous anti-inflammatory steroid formulation suitable for intranasal administration comprises: an anti-inflammatory steroid in an amount between about 0.01% and about 0.05% (w/v); propylene glycol in an amount between about 2% and about 10% (w/v); PEG 400 in an amount between about 10% and about 25% (w/v); polysorbate 20 in an amount between about 1% and about 4% (w/v); an effective amount of a preservative; an effective amount of a stabilizer; an effective amount of an antioxidant; water; and pH buffering agent sufficient to adjust the pH of the resulting solution to between about 3.5 and about 7.Type: GrantFiled: September 20, 1988Date of Patent: January 8, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Eric Benjamin, Shabbir Anik, Ya-Yun T. Lin
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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
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Patent number: 4954491Abstract: The present invention is directed to a method for the treatment of hyperaldosteronism and related disorders which comprises administering to an appropriate patient an appropriate 18-cyanopregnane.Type: GrantFiled: January 27, 1989Date of Patent: September 4, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: J. O'Neal Johnston, Gene W. Holbert
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Patent number: 4933168Abstract: A unique crystalline polymorphic form of flunisolide is disclosed which is stable in aerosols such as Freon.RTM. mixtures and is valuable in the treatment of respiratory diseases, particularly bronchial asthma and allergic rhinitis.Type: GrantFiled: September 14, 1981Date of Patent: June 12, 1990Assignee: Syntex Pharmaceuticals International LimitedInventors: Richard E. Jones, Gisela T. Haringer