-c(=o)-o-is Part Of A Hetero Ring (e.g., Lactone, Etc.) Patents (Class 514/175)
-
Publication number: 20020103392Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compoundsType: ApplicationFiled: July 22, 1997Publication date: August 1, 2002Inventors: ULRICH STACHE, HANS-GEORG ALPERMANN, WALTER DURCKHEIMER, MANFRED BOHN
-
Publication number: 20020086838Abstract: Plasminogen activator inhibitor-1 (PAI-1) antagonists can be used in the treatment of asthma and chronic obstructive pulmonary disease.Type: ApplicationFiled: January 12, 2001Publication date: July 4, 2002Applicant: TANOX, INC.Inventors: Chad K. Oh, Seong H. Cho, Sossiena Demissie-Sanders, David W. Thomas, Sun W. Tam
-
Patent number: 6410524Abstract: Combinations of an ACE inhibitor, an aldosterone antagonist, and a loop diuretic are described for use in treatment of circulatory disorders. Of particular interest are therapies using captopril, enalapril or lisinopril co-administered with spironolactone. This co-therapy would be particularly useful to reduce the death rate or the number of non-fatal hospitalizations or prevent the progression of congestive heart failure in patients with cardiovascular disease.Type: GrantFiled: November 5, 1999Date of Patent: June 25, 2002Assignee: G. D. Searle & Co.Inventors: Alfonzo T. Perez, Debra J. Asner, Richard J. LaChapelle, John C. Alexander, Barbara Roniker
-
Patent number: 6410054Abstract: The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.Type: GrantFiled: December 8, 1999Date of Patent: June 25, 2002Assignee: G. D. Searle & Co.Inventors: Shilpa S. Thosar, Rajeev D. Gokhale, Dwain S. Tolbert
-
Publication number: 20020072624Abstract: Novel compounds having a formula selected from the group consisting of 1Type: ApplicationFiled: June 26, 2001Publication date: June 13, 2002Applicant: Roussel UclafInventors: Andre Claussner, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
-
Patent number: 6391867Abstract: Use of an aldosterone receptor antagonist, spironolactone, is described for treatment of heart failure. This therapy would be particularly useful to treat or retard the development of symptomatic heart failure, while avoiding or reducing aldosterone-antagonist-induced side effects, such as hyperkalemia.Type: GrantFiled: January 9, 2001Date of Patent: May 21, 2002Assignee: G.D. Searle & Co.Inventors: Todd E. MacLaughlan, Alfonso T. Perez
-
Publication number: 20020042405Abstract: A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a calcium channel blocker is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred calcium channel blockers are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9&agr;,11&agr;-substituted epoxy moiety. A preferred combination therapy includes the calcium channel blocker verapamil HCl (Benzenacetonitrile, (±)-&agr;[3[[2-(3,4-dimethoxyphenyl) ethyl]methylamino]propyl]-3,4-dimethoxy-&agr;-(1-methylethyl)hydrochloride) and the aldosterone receptor antagonist epoxymexrenone.Type: ApplicationFiled: July 27, 2001Publication date: April 11, 2002Inventor: Joseph R. Schuh
-
Publication number: 20020013303Abstract: This invention discloses a method of using an aldosterone antagonist such as spironolactone, at a dosage which does not disrupt a patient's normal electrolyte and water-retention balance, to inhibit myocardial fibrosis, including left ventricular hypertrophy (LVH).Type: ApplicationFiled: April 24, 2000Publication date: January 31, 2002Inventor: Karl T. Weber
-
Publication number: 20020006919Abstract: There is provided a pharmaceutical composition comprising eplerenone in solid particulate form, wherein at least 90% of the eplerenone particles are smaller than about 15 &mgr;m, for example about 0.01 &mgr;m to about 1 &mgr;m, in diameter. The composition can be adapted for oral administration, for example as a tablet or capsule comprising eplerenone in a unit dosage amount of about 10 mg to about 1000 mg and one or more excipients.Type: ApplicationFiled: December 7, 2000Publication date: January 17, 2002Inventors: Shilpa S. Thosar, Rajeev D. Gokhale, Subhash Desai, Dwain S. Tolbert
-
Patent number: 6306845Abstract: The present invention provides a method for treating a demyelinating disease in a subject which includes administering to the subject a therapeutically effective amount of a high affinity neuromodulatory Na,K-ATPase so as to treat the demyelinating disease.Type: GrantFiled: January 29, 1999Date of Patent: October 23, 2001Assignee: The Trustees of Columbia University in the City of New YorkInventor: Vincent P. Butler, Jr.
-
Patent number: 6245755Abstract: This invention discloses a method of inhibiting aldosterone-mediated myocardial, perivascular and interstitial fibrosis using epoxymexrenone and other aldosterone antagonists.Type: GrantFiled: February 16, 1999Date of Patent: June 12, 2001Assignee: Curators of the Unversity of MissouriInventor: Karl T. Weber
-
Patent number: 6239121Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.Type: GrantFiled: November 29, 1999Date of Patent: May 29, 2001Assignee: Hoechst Marion RousselInventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
-
Patent number: 6177416Abstract: 3-Oxyiminopregnane-21-carbolactones of formula I, wherein R is as defined by the specification, their production and use as pharmaceutical agents are described.Type: GrantFiled: October 5, 1999Date of Patent: January 23, 2001Assignee: Schering AktiengesellschaftInventors: Henry Laurent, Ralph Lipp, Peter Esperling, Johannes-Wilhelm Tack
-
Patent number: 6150347Abstract: This invention discloses a method of using an aldosterone antagonist such as spironolactone, at a dosage which does not disrupt a patient's normal electrolyte and water-retention balance, to inhibit myocardial fibrosis, including left ventricular hypertrophy (LVH).Type: GrantFiled: March 29, 1999Date of Patent: November 21, 2000Assignee: The Curators of the University of MissouriInventor: Karl T. Weber
-
Patent number: 6093708Abstract: This invention discloses a method of using an aldosterone antagonist such as spironolactone, at a dosage which does not disrupt a patient's normal electrolyte and water-retention balance, to inhibit myocardial fibrosis, including left ventricular hypertrophy (LVH).Type: GrantFiled: March 22, 1999Date of Patent: July 25, 2000Assignee: The Curators of the University of MissouriInventor: Karl T. Weber
-
Patent number: 6011026Abstract: A method of treating menopause or perimenopause without estrogenic activity at the uterine level in women comprising administering to women an amount of a steroid of the formula ##STR1## wherein the substituents are defined as in the specification sufficient to treat menopause or perimenopause symptoms without estrogenic activity at the uterine level.Type: GrantFiled: February 12, 1999Date of Patent: January 4, 2000Assignee: Hoeschst Marion RousselInventors: Yamina Bouali, Daniel Philibert, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
-
Patent number: 5981516Abstract: A method of treating cholesterol without estrogenic activity at the uterine level in women comprising administering to women an amount of a steroid of the formula ##STR1## wherein the substituents are defined as in the specification without estrogenic activity at the uterine level.Type: GrantFiled: December 18, 1997Date of Patent: November 9, 1999Assignee: Hoechst Marion RousselInventors: Yamina Bouali, Daniel Philibert, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
-
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
-
Patent number: 5837269Abstract: The invention relates to a vaccine which comprises an antigen and an immune response augmenting agent. The immune response augmenting agent is capable of enhancing T cell lymphokine production. Suitable immune response augmenting agents include, but are not limited to, DHEA, DHEA-derivatives and DHEA congeners.The invention also relates to a method for enhancing a vaccine-induced humoral immune response which comprises administering a vaccine which comprises an antigen and an immunomodulator. The immunomodulator may be an immune response augmenting agent, a lymphoid organ modifying agent or a mixture of the immune response augmenting agent and lymphoid organ modifying agent. Suitable lymphoid organ modifying agents include, but are not limited to, 1,25-dihydroxy Vitamin D.sub.3, 25-hydroxy Vitamin D.sub.3, biologically active 1,25-dihydroxy Vitamin D.sub.3, derivatives which are capable of activating the intra-cellular Vitamin D.sub.Type: GrantFiled: June 7, 1995Date of Patent: November 17, 1998Assignee: University of Utah Research FoundationInventors: Raymond A. Daynes, Barbara A. Araneo
-
Patent number: 5777134Abstract: The novel compounds of the present invention are those of structural formula I: ##STR1## wherein X is selected from O and S, or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, and are inhibitors of 5.alpha.-reductase. The compounds of formula I are useful in the oral, systemic, parenteral or topical treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia which includes female and male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as in the treatment of prostatitis. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis are provided, as well as pharmaceutical compositions for the compounds of formula I.Type: GrantFiled: October 24, 1996Date of Patent: July 7, 1998Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Gool F. Patel, Gary H. Rasmusson, Richard L. Tolman
-
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
-
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
-
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
-
Patent number: 5760069Abstract: A method of treatment using a compound of Formula I: ##STR1## wherein: R.sub.1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl;R.sub.2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl;R.sub.3 is hydrogen or lower alkyl of up to 6 carbon atoms;R.sub.4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2, oxygen or sulfur;Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH.sub.2 -- group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; orR.sub.5 and R.sub.Type: GrantFiled: June 7, 1995Date of Patent: June 2, 1998Assignee: Boehringer Mannheim Pharmaceuticals Corporation-SmithKline Beecham Corporation Limited Partnership #1Inventors: Mary Ann Lukas-Laskey, Robert Ruffolo, Jr., Neil Howard Shusterman, Gisbert Sponer, Klaus Strein
-
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
-
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
-
Patent number: 5668125Abstract: This invention discloses a method of using an aldosterone antagonist such as spironolactone, at a dosage which does not disrupt a patient's normal electrolyte and water-retention balance, to inhibit myocardial fibrosis, including left ventricular hypertrophy (LVH).Type: GrantFiled: December 28, 1995Date of Patent: September 16, 1997Inventor: Karl T. Weber
-
Patent number: 5668124Abstract: This invention discloses a method of using an aldosterone antagonist such as spironolactone, at a dosage which does not disrupt a patient's normal electrolyte and water-retention balance, to inhibit myocardial fibrosis, including left ventricular hypertrophy (LVH).Type: GrantFiled: March 28, 1996Date of Patent: September 16, 1997Inventor: Karl T. Weber
-
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
-
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
-
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
-
Patent number: 5529992Abstract: This invention discloses a method of using an aldosterone antagonist such as spironolactone, at a dosage which does not disrupt a patient's normal electrolyte and water-retention balance, to inhibit myocardial fibrosis, including left ventricular hypertrophy (LVH).Type: GrantFiled: December 2, 1993Date of Patent: June 25, 1996Assignee: Curators of the University of MissouriInventor: Karl T. Weber
-
Patent number: 5489582Abstract: 14-Deoxy-14.alpha.-cardenolides 3.beta.-thioderivatives and pharmaceutical compositions comprising same for treating cardiovascular disorders, such as heart failure and hypertension, are disclosed.Type: GrantFiled: June 24, 1993Date of Patent: February 6, 1996Assignee: Sigma-Tau Industrie Farmaceutiche Riuntie S.p.AInventors: Mauro Gobbini, Luigi Bernardi, Mara Ferrandi, Piero Melloni, Luisa Quadri, Roberto Villa
-
Patent number: 5478817Abstract: Digitoxigenin and dihydrodigitoxigenin 3.beta.-derivatives, a process for their preparation and pharmaceutical compositions containing same for the treatment of cardiovascular disorders such as heart failure and hypertension are disclosed.Type: GrantFiled: June 23, 1993Date of Patent: December 26, 1995Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Piero Melloni, Luigi Bernardi, Patrizia Ferrari, Mauro Gobbini, Marco Torri, Loredana Valentino
-
8-En-19 11 .beta.-bridged steroids, their production and pharmaceutical preparations containing them
Patent number: 5478956Abstract: 8-En-19,11.beta.-bridged steroids of general formula I ##STR1## that have the 8,9-double bond as a new structural feature, and a process for their production are described. The substituents R.sup.1 R.sup.4 -Y, R.sup.4' -Y.sup.', X and Z have the meaning indicated in the description. The new compounds especially have at their disposal pronounced antigestagen effectivenss and are suitable for the production of pharmaceutical preparations.Type: GrantFiled: September 28, 1993Date of Patent: December 26, 1995Assignee: Schering AktiengesellschaftInventors: Eckhardt Ottow, Gunter Neef, Walter Elger, Martin Schneider, Karl Fritzemeier -
Patent number: 5446036Abstract: There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.Type: GrantFiled: November 2, 1993Date of Patent: August 29, 1995Assignee: Schering AktiengesellschaftInventors: Stefan Scholz, Eckhard Ottow, Guenter Neef, Walter Elger, Sybille Beier, Krzysztof Chwalisz
-
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
-
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
-
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
-
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
-
Patent number: 5244886Abstract: New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.Type: GrantFiled: March 20, 1991Date of Patent: September 14, 1993Assignee: Schering AktiengesellschaftInventors: Stefan Scholz, Gunter Neef, Eckhard Ottow, Walter Elger, Sybille Beier, Krzysztof Chwalisz
-
Patent number: 5198427Abstract: The present invention relates to novel sweet compounds derived from the leaves of the subtropical weed Abrus precatorius, and their use as sweeteners. In particular, the present invention contemplates four novel sweet compounds isolated from A. precatorius or A. fruticulosus, and particularly, Abrusosides A, B, C and D and related compounds. The present invention also contemplates the use of these abrusosides and related compounds as sugar substitutes. The present invention contemplates the use of Abrusosides A-D as individual components or in mixtures, in a method for sweetening comestibles, foodstuffs, beverages and medicinal agents.Type: GrantFiled: July 9, 1990Date of Patent: March 30, 1993Assignee: Research Corporation Technologies, Inc.Inventors: A. Douglas Kinghorn, Young-Hee Choi
-
Patent number: 5173483Abstract: A method of stimulating ovulation in warm-blooded animals comprising administering to warm-blooded animals an ovulation stimulating effective amount of at least one anti-progestomimetic compound.Type: GrantFiled: September 5, 1990Date of Patent: December 22, 1992Assignee: Roussel UclafInventor: J. A. Grandadam
-
Patent number: 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
-
Patent number: 4987128Abstract: Novel 10.beta.-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R.sub.6 and R.sub.7 taken together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms and acetylthio, R.sub.Type: GrantFiled: February 24, 1987Date of Patent: January 22, 1991Assignee: Roussel UclafInventors: Lucien Nedelec, Francois Nique, Anne-Marie Moura
-
Patent number: 4978657Abstract: 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 leat 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, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.Type: GrantFiled: December 17, 1985Date of Patent: December 18, 1990Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
-
Patent number: 4921845Abstract: The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: ##STR1## in which R.sub.1 is an aryl group with a ##STR2## group as substituent, X and Y each being separately H or a (1-4 C) hydrocarbyl group or together a (2-C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom;R.sub.2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group;R.sub.3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.2 and R.sub.Type: GrantFiled: December 8, 1988Date of Patent: May 1, 1990Assignee: Akzo N.V.Inventors: Hendrick Paul de Jongh, Nicolaas P. van Vliet
-
Patent number: 4904462Abstract: Novel, multiple-tritiated steroid-20,17-spirolactones of general Formula I ##STR1## wherein --A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or ##STR2## and --C--D-- is ##STR3## R is hydrogen or tritium and n is 0 or 1,are usable as tracer materials for the detection of mineralocorticoid receptors.Type: GrantFiled: April 12, 1985Date of Patent: February 27, 1990Assignee: Schering AktiengesellschaftInventors: Paul-Eberhard Schulze, Klaus Nickisch, Henry Laurent, Kunhard Pollow
-
Patent number: 4891365Abstract: 17-Substituted estradienes and estratrienes of Formula I ##STR1## wherein ##STR2## R is alkyl, alkenyl or cycloalkyl of up to 5 carbon atoms if ##STR3## R is hydrogen, alkyl, alkenyl or cycloalkyl of up to 5 carbon atoms if ##STR4## is a CC-single or CC-double bond, exhibit, an aldosterone-antagonistic activity and a strong gestagen potency.Type: GrantFiled: July 2, 1987Date of Patent: January 2, 1990Assignee: Schering AktiengesellschaftInventors: Rudolf Wiechert, Sybille Beier, Walter Elger, Klaus Annen, Klaus Nickisch, Henry Laurent
-
Patent number: 4885289Abstract: The rate and character of androgen-stimulated beard hair growth in intact, sexually mature males is altered by the topical application out of a dermatologically acceptable carrier of an antiandrogen material. In a preferred practice of the invention, compositions containing both a steroid 5-alpha-reductase inhibitor and a cytoplasmic androgen receptor binding agent are employed.Type: GrantFiled: December 11, 1985Date of Patent: December 5, 1989Inventors: Miklos M. Breuer, Edwin G. Kaszynski, Douglas Shander, Vera R. Usdin, Hermes van der Lee