21-position Substituted Patents (Class 514/181)
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Patent number: 5646136Abstract: Methods for treating angiogenesis, tumors, and ocular hypertension with steroids are disclosed herein. The steroids have angiostatic activity with reduced glucocorticoid activity.Type: GrantFiled: January 4, 1994Date of Patent: July 8, 1997Assignee: Duke UniversityInventors: Vladimir Petrow, Alan D. Proia
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Patent number: 5637310Abstract: Invented is a Method of Treating Prostatic Adenocarcinoma by employing asteroid 5-.alpha.-reductase inhibiting compound or a combination of steroid 5-.alpha.-reductase inhibiting compounds.Type: GrantFiled: May 30, 1995Date of Patent: June 10, 1997Assignee: SmithKline Beecham CorporationInventor: Randall K. Johnson
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Patent number: 5622942Abstract: A percutaneous absorptive anesthetic is provided, wherein said anesthetic is formed by mixing a base agent of said anesthetic with one or two type of mixtures which has/have been selected from the groups, for example made of glycyrrhizin, glycyrrhetic acid, glycyrrhetic acid derivatives glycyrrhetic acid 3.beta.-monohemisuccinate, glycyrrhetic acid 3.beta.-monohemisuccinate, 18.beta.-olean-12-ene-3.beta., 30-dihemiphthalate, 18.beta.-olean-9, (11)12-diene-3.beta., 30-diol-dihemiphthalate, olean-11,13(18)-diene-3.beta., 30-diol-dihemiphthalate or their pharmaceutically allowable salt.Type: GrantFiled: November 22, 1993Date of Patent: April 22, 1997Assignee: Minophagen Pharmaceutical CompanyInventors: Masahiro Nakano, Motohiro Mishima, Tatsuhiko Kano, Nobuyuki Nagata
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Patent number: 5622944Abstract: Compositions and methods are provided for enhanced transdermal electrotransport of 17-hydroxy sterol compounds, including testosterone. The parent sterols are modified at the 17-hydroxy position by covalent attachment of a charged chemical modifier. The chemical modifier provides the parent sterol with enhanced transport properties and is hydrolyzed under physiological conditions to release the active parent compound.The composition comprises a 17-hydroxy sterol/chemical modifier complex, more generally represented by the formula (sterol--O--)C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+. The portion of the complex derived from the chemical modifier is indicated by "C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ ", where N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ represents a quaternary ammonium group and R.sup.1, R.sup.2, and R.sup.3 are independently selected from the group consisting of lower alkyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroalkyl, and heteroarylalkyl; or R.sup.1 and R.sup.Type: GrantFiled: May 4, 1995Date of Patent: April 22, 1997Assignees: Affymax Technologies N.V., Alza CorporationInventors: Ron L. Hale, Amy T. Lu, Dennis W. Solas, Michel J. N. Cormier
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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: 5591733Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.Type: GrantFiled: August 2, 1993Date of Patent: January 7, 1997Assignee: University of Southern CaliforniaInventors: Michael B. Bolger, Kelvin W. Gee, Nancy C. Lan, Robert H. Purdy, Seid Mirsadeghi, Syed Hasan Tahir, Delia Belelli
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Patent number: 5585366Abstract: A method for reducing the cholesterol level in mammalian blood by administering a water soluble cellulose ether thereto. The cellulose ethers have a viscosity, measured as a 2% aqueous solution at 20.degree. C., of at least about 35 cps. Oral administration is preferred, and, in one embodiment the high viscosity water soluble cellulose ether is hydroxypropyl methylcellulose, contained in a nutritious foodstuff.Type: GrantFiled: May 19, 1995Date of Patent: December 17, 1996Assignee: Regents of the University of MinnesotaInventors: Daniel D. Gallaher, Craig A. Hassel
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Patent number: 5578589Abstract: The invention is drawn to a method for suppressing an immunoresponse in animals by administering an estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R.sup.1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R.sup.2 is acyl, dansyl, or alkyl; R.sup.3, R.sup.4, and R.sup.5 independently are H, oxo, OH, or acyloxy; m is an integer of 1 to 3; and n is an integer of 0 to 3; provided that when n is 0, all of R.sup.3, R.sup.4, and R.sup.5 are not H at the same time, and at least one of R.sup.3, R.sup.4, and R.sup.5 is a group other than H and OH; and further, when n is 2 or 3, the groups R.sup.1 are the same or different.Type: GrantFiled: May 15, 1995Date of Patent: November 26, 1996Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Fumio Tamura, Tsuyoshi Saito, Satoshi Mitsuhashi, Tadahiro Matsudaira, Kiro Asano
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Patent number: 5554601Abstract: A method is provided for conferring neuroprotection on a population of cells using estrogen compounds that have insubstantial sex activity and furthermore, a method is provided that utilizes estrogen compounds in the absence of testosterone for treating neurodegenerative diseases including Alzheimer's disease so as to retard the adverse effects of these disorders, Examples of estrogen compounds that have insubstantial sex activity includes alpha isomers of estrogen compounds such as 17.alpha. estradiol.Type: GrantFiled: October 4, 1994Date of Patent: September 10, 1996Assignee: University of FloridaInventors: James W. Simpkins, Meharvan Singh, Jean Bishop
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Patent number: 5527788Abstract: The invention describes a method and composition for treating obesity or related disorders in animals using an anorectic agent and dehydroepiandrosterone (DHEA). The composition effectively diminishes caloric intake, may alter metabolism, weight gain, or a combination thereof.Type: GrantFiled: January 18, 1994Date of Patent: June 18, 1996Assignee: Louisiana State Univ. Medical Center FoundationInventors: Frank Svec, Johnny Porter
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Patent number: 5506220Abstract: The invention relates to the domain of medicinal chemistry. It concerns more particularly that of the preparation of pharmaceutical compositions for ocular use.A subject of the invention is pharmaceutical compositions for ocular use characterized in that they contain at least one selected compound of steroidal structure in combination with or admixed with a pharmaceutically-acceptable, inert carrier or vehicle.The compositions according to the invention are intended to the treatment of glaucoma.Type: GrantFiled: May 25, 1994Date of Patent: April 9, 1996Assignee: Laboratoire Theramex SAInventor: Gerard Schwadrohn
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Patent number: 5496556Abstract: Invented is a Method of Treating Prostatic Adenocarcinoma by employing asteroid 5-.alpha.-reductase inhibiting compound or a combination of steroid 5-.alpha.-reductase inhibiting compounds.Type: GrantFiled: December 20, 1993Date of Patent: March 5, 1996Assignee: Smithkline Beecham CorporationInventor: Randall K. Johnson
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Patent number: 5486511Abstract: This invention is directed to 4-amino-17.beta.-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17.beta.-(cyclopropylylamino)androst-4-en-3-one and related compounds, a process for their synthesis, a pharmaceutical composition having C.sub.17-20 lyase and 5.alpha.-reductase inhibitory activity, the use of the present compounds as C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and also to a method for using such compounds in the treatment of androgen and/or estrogen dependent disorders, including bengin prostatic hyperplasia, breast cancer and prostatic cancer. The 4-amino compounds are prepared by the reaction of the appropriate 4,5-epoxide with sodium azide in an inert solvent in the presence of a catalytic amount of strong acid under appropriate reaction conditions. Alternatively, the 4-amino compounds are prepared by first nitration and then reduction of the appropriate steroid under appropriate reaction conditions.Type: GrantFiled: May 2, 1994Date of Patent: January 23, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Cynthia A. Gates, Michael R. Angelastro, Timothy T. Curran, J. O'Neal Johnston
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Patent number: 5426102Abstract: Novel compounds of the general formula I ##STR1## and the pharmacologically tolerable addition salts thereof with acids are described, in which eitherIa) R.sup.11 represents a hydrogen atom in the .beta.-configuration and each of R.sup.12 and R.sup.13 represents a hydrogen atom, orIb) R.sup.11 represents a hydrogen atom in the .beta.-configuration and R.sup.12 and R.sup.13 together represent a second bond, orIc) R.sup.11 and R.sup.12 together represent a second bond and R.sup.13 represents a hydrogen atom, orId) R.sup.11 represents a hydrogen atom in the .alpha.-configuration and R.sup.12 and R.sup.13 together represent a second bond,and in Ia), Ib), Ic) or Id)X represents an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 represents a hydrogen atom or a methyl group,R.sup.2 represents a hydroxy group, a C.sub.1 -C.sub.10 -alkoxy group or a C.sub.1 -C.sub.10 -acyloxy group, andR.sup.3 and R.sup.Type: GrantFiled: June 22, 1993Date of Patent: June 20, 1995Assignee: Schering AktiengesellschaftInventors: Wolfgang Schwede, Eckhard Ottow, Gunter Neef, Arwed Cleve, Krzysztof Chwalisz, Horst Michna
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Patent number: 5401509Abstract: 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: July 25, 1994Date of Patent: March 28, 1995Assignee: Alcon Laboratories, Inc.Inventors: Stella M. Robertson, Herman M. Kunkle, Jr.
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Patent number: 5376652Abstract: A method for preventing or reducing restenosis wherein a 27-hydroxycholesterol or a 25,26 and/or 27-aminocholesterol, or a sterol 27-hydroxylase stimulant is administered in a restenosis preventing and/or reducing amount.Type: GrantFiled: November 30, 1993Date of Patent: December 27, 1994Assignee: New York University Medical CenterInventor: Norman B. Javitt
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Patent number: 5371078Abstract: Angiostatic steroids for use in controlling ocular hypertension are disclosed. Pharmaceutical compositions 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. In addition, the combination of the compounds with glucocorticoids for the prevention of elevated IOP during the treatment of inflammation is disclosed.Type: GrantFiled: September 8, 1992Date of Patent: December 6, 1994Assignee: Alcon Laboratories, Inc.Inventors: Abbot F. Clark, Raymond E. Conrow
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Patent number: 5362721Abstract: The disclosed invention includes corticoid-17-alkylcarbonates substituted in the 17-position, a process for their preparation and pharmaceuticals containing them. These corticoid-17-alkylcarbonates have the following formula I ##STR1## where A is CHOH in any desired steric arrangement, C.dbd.O or CH.sub.2 ; Y is H, F, or Cl; Z is H, F or CH.sub.3 ; R(1) is O-acyl, carbonylalkyl, alkylsulfonate or arylsulfonate;R(2) is branched alkyl or (CH.sub.2).sub.2-4 --OCH.sub.3 andR(3) is H or methyl. They have excellent local and topical antiinflammatory action. They are distinguished by a particularly good ratio of local to systemic antiinflammatory activity and in some cases also show stronger local antiinflammatory activities than their isomeric corticoid-17-alkylcarbonates having a linear alkyl group in the 17-alkylcarbonate moiety.Type: GrantFiled: February 8, 1993Date of Patent: November 8, 1994Assignee: Hoechst AktiengesellschaftInventors: Ulrich Stache, Walter Durckheimer, Hans G. Alpermann, Walter Petri
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Patent number: 5318961Abstract: The present invention relates to 4-amino-.DELTA..sup.4 -steroids which are inhibitors of 5.alpha.-reductase. The compounds are useful for treating DHT-mediated diseases.Type: GrantFiled: December 20, 1992Date of Patent: June 7, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Joseph P. Burkhart, Thomas R. Blohm
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Patent number: 5278156Abstract: 11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the formula ##STR1## an antiinflammatory composition thereof and a method for the production thereof.11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the present invention exhibits remarkably excellent antiinflammatory action and besides, displays reduced side effects and can be produced in high selectivity and good yield and conveniently.Type: GrantFiled: March 24, 1992Date of Patent: January 11, 1994Assignees: Kuraray Co., Ltd., Taiho Pharmaceutical Co., Ltd.Inventors: Yutaka Mizushima, Keiko Hoshi, Rie Igarashi, Hirofusa Ajioka, Noriyuki Yamamoto, Masahito Komuro, Koichi Kanehira, Masayuki Inoue, Takashi Nishida, Michio Terasawa, Kenzo Arizono
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Patent number: 5272141Abstract: The present invention relates to a drug for human use, having contraceptive and menstrual cycle controlling properties, characterized in that the drug comprises N-acetyl-5-methoxytryptamine or melatonin, in a dose of 100-200 mg per day, N-acetyl-2-bromo-5-methoxytryptamine or 2-bromomelatonin in a dose of 25-50 mg per day, N-acetyl-2-iodo-5-methoxytryptamine or 2-iodomelatonin, in a dose of 20-40 mgs per day, in association with a progestine compound. The administration is carried out for 23 days, by using an association of 2-iodomelatonin and/or melatonin and/or 2-bromomelatonin and a progestinic compound, followed by 5 days in which only 2-iodomelatonin and/or melatonin and/or 2-bromomelatonin is administered; the drug having oncostatic preventive and therapeutic properties, in mammary tumours and melanomas, characterized by the use of 2-iodomelatonin, melatonin and 2-bromomelatonin respectively with doses of 20-40 mgs., 100-200 mgs.Type: GrantFiled: September 27, 1991Date of Patent: December 21, 1993Inventors: Franco Fraschini, Bojidar Stankov, Luigi Di Bella, Ermanno Duranti, Aldo Lagguzzi
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Patent number: 5232917Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.Type: GrantFiled: August 13, 1991Date of Patent: August 3, 1993Assignee: University of Southern CaliforniaInventors: Michael Bolger, Kelvin W. Gee, Nancy C. Lan, Delia Belelli, Seid Mirsadeghi, Robert Purdy
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Patent number: 5208227Abstract: 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 ionophore (GBR) complex.Type: GrantFiled: February 13, 1991Date of Patent: May 4, 1993Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger, Roberta E. Brinton, Deborah J. Burke, Bruce S. McEwen
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Patent number: 5198225Abstract: Compositions based on hydrated lipidic lamellar phases or liposomes are disclosed containing at least in part at least one ecdysteroid or ecdysteroid derivative, in particular ecdysterone, or a plant or animal extract containing the said ecdysteroid or ecdysteroid derivative. Cosmetic or pharmaceutical compositions can be prepared as well as compositions for sericulture or a phytosanitary composition.Type: GrantFiled: March 22, 1991Date of Patent: March 30, 1993Assignee: LVMH RechercheInventors: Alain Meybeck, Frederic Bonte
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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: 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
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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
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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
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Patent number: 5064822Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenylphenyl, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms optionally containing additional unsaturations, phenoxy, furyl, cycloalkyl of 3 to 6 carbon atoms, thienyl optionally substituted with at least one member of the group consisting of halogen and alkyl and haloalkyl of 1 to 6 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, halogen, --CF.sub.3, alkyl and alkoxy of 1 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, phenoxy and alkylthio of 1 to 6 carbon atoms optionally oxidized to the sulfoxide or sulfone, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.Type: GrantFiled: November 16, 1989Date of Patent: November 12, 1991Assignee: Roussel UclafInventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
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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: 5053403Abstract: Synergistic compositions for inhibiting the action of androgens comprise the combination in a single topical preparation of a 5.alpha.-reductase enzyme inhibitor and an androgen receptor blocking agent in a pharmaceutically and dermatologically acceptable vehicle. The compositions may be topically applied to affected areas of the skin in the treatment or prevention of sebaceous gland hypertrophy, hirsutism and male-pattern baldness in mammals. The inhibitor and blocking agent are present in the composition in a weight ratio of about 1:20 to 5:1, with the inhibitor comprising up to about 0.1% w/v of the comopsition and the blocking agent comprising up to about 1% w/v of the composition.Type: GrantFiled: November 20, 1989Date of Patent: October 1, 1991Assignee: Norman OrentreichInventors: Norman Orentreich, Jonathan R. Matias
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Patent number: 5032586Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are methods for preparing these compounds.Type: GrantFiled: August 24, 1989Date of Patent: July 16, 1991Assignee: SmithKline Beecham CorporationInventors: Brian W. Metcalf, Dennis A. Holt, Mark A. Levy
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Patent number: 4948533Abstract: The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17.alpha.-hydroxy-11.alpha.-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-diene-3, 20 dione and pharmaceutically acceptable salts thereof which are useful steroid prodrugs.Type: GrantFiled: February 16, 1989Date of Patent: August 14, 1990Assignee: The Upjohn CompanyInventors: John M. Braughler, Edward D. Hall, Wendell Wierenga, John M. McCall
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Patent number: 4933332Abstract: 11-Desoxy-17.alpha.-hydroxycorticosterone derivatives of the general formula: ##STR1## wherein R is --OC(CH.sub.2).sub.n C.sub.6 H.sub.4 N(CH.sub.2 CH.sub.2 Cl).sub.2, n=1,3.Type: GrantFiled: September 30, 1988Date of Patent: June 12, 1990Inventors: Kira N. Kurdjumova, Elizaveta N. Shkodinskaya, Ljudmila P. Sushinina, Valentina P. Yaguzhinskaya, Nina D. Lagova, Zoya P. Sofiina, Irina M. Valueva, Petr V. Lopatin, Margarita A. Krasnova, Anatoly B. Syrkin, Ljudmila M. Mikhailova
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Patent number: 4920114Abstract: 19-Fluoro- and cyano- substituted 21-hydroxyprogesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pathways which will vary according to the nature of the specific 19-substituted progesterone or related compound desired.Type: GrantFiled: June 28, 1988Date of Patent: April 24, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gene W. Holbert, J. O'Neal Johnston
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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
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Patent number: 4910191Abstract: 19-Substituted progesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pathways which will vary according to the nature of the specific 19-substituted progesterone or related compound desired.Type: GrantFiled: June 28, 1988Date of Patent: March 20, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gene W. Holbert, J. O'Neal Johnston
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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
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Patent number: 4871724Abstract: The present invention is concerned with 11-aryloestrane and 11-arylpregnane derivatives, characterized in that these derivatives have the following structure: ##STR1## wherein R.sub.1 is an aryl group with an ##STR2## group as substituent,X and Y each being separately H or a (1-4 C) hydrocarbon radical or together a (2-6 C) hydrocarbon radical;R.sub.2 is an alkyl group containing 1-4 carbon atoms;R.sub.3 is H, OH, a saturated or unsaturated hydrocarbon radical containing 1-8 carbon atoms, at least provided with a hydroxyl, oxo, halogen, azido or nitrile group; an acyloxy or an alkoxy group;R.sub.4 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally provided with a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.3 and R.sub.4 together form a ring system; andR.sub.5 is a hydrocarbon group containing 1-4 carbon atoms, and further with processes for the preparation of these compounds and with pharmaceutical preparations comprising these compounds.Type: GrantFiled: April 20, 1988Date of Patent: October 3, 1989Assignee: Akzo N.v.Inventors: Marinus B. Groen, Hendrik P. de Jongh
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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
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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
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Patent number: 4861765Abstract: A 21-substituted thiosteroid represented by the general formula ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 5 or 6 carbon atoms, a phenyl group, or a benzyl group which may have a substituent on the benzene ring,R.sup.2 represents an alkanoyl group having 2 to 6 carbon atoms,R.sup.3 represents a hydrogen atom or a methyl group,X represents a hydrogen or halogen atom, andthe dotted line between 1- and 2-positions represents an optional bond. These compounds are useful an anti-inflammatory agents.Type: GrantFiled: June 23, 1986Date of Patent: August 29, 1989Assignee: JouveinalInventors: Morihiro Mitsukuchi, Tomoyuki Ikemoto, Yoshiaki Watanabe, Kaoru Sota
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Patent number: 4814327Abstract: 11 .beta.-(4-isopropenylphenyl)-estra-4,9-dienes of general Formula I ##STR1## wherein X is an oxygen atom or a hydroxyimino grouping N OH,R.sup.1 is a hydrogen atom or a methyl group,R.sup.2 is a hydrogen atom or an acyl residue of 1-10 carbon atoms,R.sup.3 is a hydrogen atom, the cyanomethyl group, --(CH.sub.2).sub.n --, CH.sub.2 Z, --CH.dbd.CH--(CH.sub.2).sub.m Z or --C.tbd.C--Y wherein n=0 to 5 and m=1 to 4, Z meaning a hydrogen atom or the OR.sup.4 group with R.sup.4 meaning a hydrogen atom, an alkyl or alkanoyl group each of 1-4 carbon atoms, and Y meaning a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group each of 1-4 carbon atoms in the alkyl or acyl residue, possess antiprogestational activity.Type: GrantFiled: July 24, 1987Date of Patent: March 21, 1989Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Rudolf Wiechert, Gunter Neef, Sybille Beier, Walter Elger, David Henderson
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Patent number: 4810701Abstract: 11-Desoxy-17.alpha.-hydroxycorticosterone derivatives of the general formula: ##STR1## wherein R is --OC(CH.sub.2).sub.n C.sub.6 H.sub.4 N(CH.sub.2 CH.sub.2 Cl).sub.2, n=1,3.Type: GrantFiled: March 21, 1986Date of Patent: March 7, 1989Assignee: Vsesojuzny Onkologichesky Nauchny Tsentr Akademii Meditsinskikh Nauk SSRInventors: Kira N. Kurdjumova, Elizaveta N. Shkodinskaya, Ljudmila P. Sushinina, Valentina P. Yaguzhinskaya, Nina D. Lagova, Zoya P. Sofiina, Irina M. Valueva, Petr V. Lopatin, Margarita A. Krasnova, Anatoly B. Syrkin, Ljudmila M. Mikhailova
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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
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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
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Patent number: RE35517Abstract: 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: November 23, 1992Date of Patent: May 20, 1997Assignee: University of Southern CaliforniaInventors: Kelvin W. Gee, Michael B. Bolger, Nancy C. Lan