Patents Assigned to Jenapharm GmbH
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Patent number: 6225299Abstract: The pharmaceutical composition, especially for treating skin with seborrhea, Acne vulgaris and androgonically conditioned alopecia, contains a hormonal agent including the gestogen, dienogest, or a combination of dienogest and an estrogen, as active ingredient. Methods for treatment of this type of skin condition include topical application of the composition including the dienogest which results in an outstanding sebosuppression, a drastic reduction of androstandiol glucuronide and a moderate competitive blockage of androgen receptor sites. Galenic formulations are described which limit and/or prevent the permeation of the active ingredient through the skin.Type: GrantFiled: December 23, 1998Date of Patent: May 1, 2001Assignee: Jenapharm GmbH & Co. KGInventors: Siegfried Golbs, Michael Oettel, Michael Dittgen, Thomas Graser, Christoph Luderschmidt
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Patent number: 6214377Abstract: The use of melatonin for the production of peroral pulsatile forms of medications assures the safeguard of an effective level of the medical substance of melatonin in the blood, and which realize a relatively short invasion phase with a controlled delivery in comparison to conventional forms of medication containing melatonin, and which simultaneously exclude the known side effects. A control of the delivery of the melatonin is effected which is associated with the precise adaptation to the illness episodes or the pain attacks of certain illnesses, which can be treated prophylactically and therapeutically with the active agent melatonin.Type: GrantFiled: December 5, 1995Date of Patent: April 10, 2001Assignee: Jenapharm GmbHInventors: Michael Dittgen, Sabine Fricke, Thomas Gräser, Hermann Osterwald, Michael Oettel, Theodor Hermann Lippert
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Patent number: 6172056Abstract: The method of prophylaxis and therapy of radical-mediated cell damage includes administering an effective amount of at least one steroid and at least one pharmaceutical adjuvant to a human being. The at least one steroid is selected from the group consisting of ent-estradiol, 17&agr;-estradiol, 8-dehydro-estradiol, 8-dehydro-17&agr;-estradiol, 8(14)-dehydroestradiol, 6,8-didehydro-17&agr;-estradiol, 6-dehydroestriol, 9(11)-dehydroestriol, 20-hydroxymethyl-3-hydroxy-19-norpregna-1,3,5(10)-triene, 14&agr;, 15&agr;-methylene-8-dehydroestradiol, 14&agr;, 15&agr;-methylene-estradiol, 2-hydroxy-estradiol-3-methyl ether, 3-hydroxy-1,3,5(10)-estratriene-17S-spirooxirane, 3-hydroxy-1,3,5(10),9(11)-estratetraene-17S-spirooxirane, and 14&bgr;,15&bgr;-methylene-8-dehydroestradiol.Type: GrantFiled: May 9, 1996Date of Patent: January 9, 2001Assignee: Jenapharm GmbH & Co. KGInventors: Peter Droescher, Bernd Menzenbach, Kurt Ponsold, Bernd Undeutsch, Michael Oettel, Wolfgang Römer, G{umlaut over (u)}nter Kaufmann, Jens Schroeder
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Patent number: 6133251Abstract: The combination preparation for contraception includes a first stage of 2 to 4 first stage daily dosage portions, a second stage of two groups of second stage daily dosage portions, a third stage of 2 to 4 third stage daily dosage portions and an additional stage of 2 to 4 additional stage daily dosage portions. The first stage daily dosage portion is an effective amount of natural estrogen, the second stage daily dosage portion is an effective amount of a combination of natural estrogen and natural or synthetic gestogen, the third stage daily dosage portion is another effective amount of natural estrogen and an additional stage daily dosage portion consists of a placebo. The first group of the second stage consists of 3 to 5 daily dosage portions and the second group, 13 to 17 daily dosage portions. More of the gestogen is included in the effective amount in the second group of the second stage than in the first group.Type: GrantFiled: October 25, 1996Date of Patent: October 17, 2000Assignee: Jenapharm GmbH & Co. KGInventors: Michael Dittgen, Sabine Fricke, Herbert Hoffmann, Claudia Moore, Michael Oettel, Monika Ostertag
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Patent number: 6117450Abstract: The method of making a solid drug with controlled effective ingredient delivery for oral administration includes selecting a predetermined number of at least three of four compressed compositions containing an effective ingredient or effective ingredient combination defined by their release profile of effective ingredient and/or effective ingredient combination. The solid drug or medicinal preparation is formed according to known methods requiring only comparatively small apparatus expense and minimal time. Perorally administered solid drugs are made by this process which can provide widely varying pharmaceutically-required release profiles of effective ingredients or effective ingredient combinations, for example delayed release, uniformly maintained release or pulsatile release adjusted to fit a special rhythm.Type: GrantFiled: April 24, 1998Date of Patent: September 12, 2000Assignee: JENAPHARM GmbH & Co. KGInventors: Michael Dittgen, Sabine Fricke, Carsten Timpe, Hagen Gerecke, Annette Eichardt
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Patent number: 6080735Abstract: This invention is relating to new estra-1,3,5(10)-trien-sulfamates carrying at the 3-position an R--SO.sub.2 --O--group, with R being an R.sup.1 R.sup.2 N--group in which R.sup.1 and R.sup.2, independently of each other, represent a hydrogen atom, an alkyl residue with 1-5 C atoms or, together with the N atom, a polymethylene-imino residue with 4-6 C atoms or a morpholino residue.The compounds, according to this invention, are suitable for hormonal contraception and climacteric hormone replacement therapy (HRT) as well as for treatment of gynecological and andrological diseases. Hence, only low hepatic estrogenicity is exhibited by the compounds according to this invention.Also described are processes for preparation of the compounds according to this invention and for preparation of pharmaceutical compositions.Type: GrantFiled: February 2, 1998Date of Patent: June 27, 2000Assignee: Jenapharm GmbH & Co. KGInventors: Sigfrid Schwarz, Walter Elger, Hans-Joachim Siemann, deceased, by Margit Lucas, heir, by Frank Siemann, heir, Gudrun Reddersen, Birgitt Schneider
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Patent number: 6063404Abstract: This invention relates to a bioadhesive tablet containing at least one bioadhesive adjuvant and at least one lubricant, with at least one surface of the tablet comprising concentric or parallel, straight and/or curved depressions, and to a method for producing the bioadhesive tablets as well as to pharmaceuticals in the form of the bioadhesive tablets.Type: GrantFiled: July 29, 1998Date of Patent: May 16, 2000Assignee: Jenapharm GmbH & Co. KGInventors: Carsten Timpe, Michael Dittgen, Detlef Grawe, Jochen Schumacher, Holger Zimmermann, Herbert Hoffmann
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Patent number: 5977096Abstract: Novel substituted steroid compounds are disclosed which are more effective than known radical-trapping agents in methods of prophylaxis and therapy of radical-mediated cell damage and of treatment of diseases due to radical-mediated cell damage. The novel substituted steroid compounds can be made from steroids having an estrane, androstane, pregnane or cholestane basic skeleton and have a radical-attracting aromatic substituent of the general formula --(CH.sub.2).sub.n X, or .dbd.CH--(CH.sub.2).sub.m X at the 17 or 6 position of the steroid nucleus, wherein X=Y, OY, SY, SeY or NHY; n=0 to 5; m=n-1 and Y is a phenyl group having five substituents A, B, C, D and E, wherein A to E is independently H, alkyl, Oalkyl, Oacyl, OH, or one of the substituents B, C or D is NR.sub.2 wherein R=alkyl and each of the other substituents is hydrogen. Pharmaceutical compositions containing the novel substituted steroid compounds and methods of making them are also part of the invention.Type: GrantFiled: February 20, 1999Date of Patent: November 2, 1999Assignee: Jenapharm GmbH & Co. KGInventors: Peter Droescher, Bernd Menzenbach, Kurt Ponsold, Bernd Undeutsch, Michael Oettel, Wolfgang Romer, Gunter Kaufmann, Jens Schroder
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Patent number: 5914325Abstract: Disclosed are estrane derivatives having a radical-attracting aromatic substituent of the general formula --(CH.sub.2).sub.n X attached to the 17-position of the steroid nucleus, wherein X and n are as defined by the specification. The compounds are useful as antitumor agents and in the treatment of cardiac and circulatory disorders.Type: GrantFiled: July 8, 1996Date of Patent: June 22, 1999Assignee: Jenapharm GmbHInventors: Peter Droescher, Bernd Menzenbach, Kurt Ponsold, Bernd Undeutsch, Michael Oettel, Wolfgang Romer, Gunter Kaufmann, Jens Schroder
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Patent number: 5910493Abstract: The pharmaceutical composition, especially for treating skin with seborrhea, Acne vulgaris and androgonically conditioned alopecia, contains a hormonal agent including the gestogen, dienogest, or a combination of dienogest and an estrogen, as active ingredient. Methods for treatment of this type of skin condition include topical application of the composition including the dienogest which results in an outstanding sebosuppression, a drastic reduction of androstandiol glucuronide and a moderate competitive blockage of androgen receptor sites. Galenic formulations are described which limit and/or prevent the permeation of the active ingredient through the skin.Type: GrantFiled: September 16, 1996Date of Patent: June 8, 1999Assignee: Jenapharm GmbHInventors: Siegfried Golbs, Michael Oettel, Michael Dittgen, Thomas Graser, Christoph Luderschmidt
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Patent number: 5866559Abstract: The 17.alpha.-cyanomethylestra-4,9-diene derivative compounds are of formula I: ##STR1## wherein R.sub.1 is an alkyl group having from 1 to 2 carbon atoms; R.sub.2 is an alkyl group with 1 to 10 carbon atoms, an acyl group with 1 to 10 carbon atoms or a trialkylsilyl group; and R.sub.3 is an oxygen atom or a R--O--N group, wherein R is a hydrogen atom, an acyl group with 1 to 10 carbon atoms, an alkyl group with 1 to 10 carbon atoms, a sulfamoyl group, an alkylsilyl group or a trialkylsilyl group. These compounds, particularly in combination with at least one suitable estrogen, are suitable for treatment of endometrioses or gestagen-dependent tumors and for hormonal contraception and climacteric hormone replacement therapy (HRT). Processes for making the new steroids are described as well as methods of making the pharmaceutical compositions containing them.Type: GrantFiled: December 20, 1996Date of Patent: February 2, 1999Assignee: Jenapharm GmbHInventors: Gerhard Teichmuller, Gerd Muller, Sigfrid Schwarz, Bernd Undeutsch, Harry Henkel, Ronald Gebuhr, Gunter Kaufmann, Doris Hubler, Michael Oettel
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Patent number: 5855905Abstract: A compound preparation for the treatment of hypogonadal men and men with hypophyseal diseases. This invention relates to compound preparations containing biogenous or synthetic androgens and biogenous or synthetic estrogens that are used for the treatment of imbalances of the testosterone metabolism in old age, of hypogonadal men, and of men with hypophyseal diseases. These compound preparations are present in various galenic formulations such as ointments, gels, sprays, TTS systems, tablets, lozenges, capsules, and suppositories. These preparations are used to treat the fluctuations of the testosterone metabolism occurring in old age and with certain diseases such as hypophyseal diseases (adenoma), hypogonadism and/or metabolic syndrome, to maintain the balance between androgens and estrogens found in young and healthy men in ill and/or elderly men as well.Type: GrantFiled: April 30, 1997Date of Patent: January 5, 1999Assignee: Jenapharm GmbH & Co. KGInventors: Michael Oettel, Siegfried Golbs, Michael Dittgen, Carsten Timpe, Thomas Graser, Doris Hubler
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Patent number: 5831104Abstract: The invention is directed to novel steroid intermediate products of general formula I ##STR1## The steroid intermediate products which can be isolated according to the invention are suitable for the synthesis of 13-ethyl-11-methylene-18,19-bisnor-17.alpha.-pregn-4-en-20-in-17-ol (desogestrel).Further, processes for producing the steroid intermediate products of general formula I are described. The olefination of the 11-oxo steroids is carried out under the influence of ultrasound.Type: GrantFiled: September 9, 1994Date of Patent: November 3, 1998Assignee: Jenapharm GmbHInventors: Sven Ring, Gerhard Teichmueller, Gisela Weber, Sigfrid Schwarz, Bernd Erhart, Bernd Undeutsch, Harald Raethe, Peter Moellmann, Carmen Pfeiffer, Hans-Joachim Palme
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Patent number: 5795883Abstract: Novel androgens having one or more substituents providing radical trapping properties are disclosed as useful in methods of treating androgen deficiency in man, benign prostate hypotropy and carcinoma of the prostate, osteoporosis, vascular disease-induced or ischemically-induced cerebral edemas, subarachnoid hemorrhages, ischemic shock, cerebral insult, Parkinson's disease and Alzheimer's disease. The androgen compound used for treating androgen deficiency in man has a steroid ring with an .alpha.-tocopherol group or a trolox group substituent.Type: GrantFiled: November 6, 1995Date of Patent: August 18, 1998Assignee: Jenapharm GmbHInventors: Rolf-Dieter Hesch, Michael Oettel, Peter Droescher, Sigfrid Schwarz, Bernd Menzenbach, Wolfgang Romer, Gunter Kaufmann, Jens Schroder
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Patent number: 5705495Abstract: The invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compound and pharmaceutical preparations containing this compound are described. The compounds according to the invention have an estrogenic effect.Type: GrantFiled: October 18, 1996Date of Patent: January 6, 1998Assignee: Jenapharm GmbH & Co. KG.Inventors: Sigfrid Schwarz, Walter Elger, Gudrun Reddersen, Birgitt Schneider, Ina Thieme, Margit Richter
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Patent number: 5693628Abstract: This invention relates to new 11-benzaldoxime-estra-diene derivatives of the general formula I ##STR1## and their pharmaceutically acceptable salts, a method for their production, and pharmaceuticals containing such compounds.The compounds described show strong antigestagenic effects combined with reduced glucocorticoid activity.Type: GrantFiled: September 20, 1994Date of Patent: December 2, 1997Assignee: Jenapharm GmbHInventors: Gerd Schubert, Gunther Kaufmann, Lothar Sobeck, Michael Oettel, Walter Elger, Anatoli Kurischko
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Patent number: 5576310Abstract: This invention relates to new 11-benzaldoxime-estra-diene derivatives of the general formula I ##STR1## wherein Z is --CO--CH.sub.3, --CO--O--C.sub.2 H.sub.5, --CO--NH-phenyl, --CO--NH--C.sub.2 H.sub.5, --CO--C.sub.2 H.sub.5, --CH.sub.3, or --CO-phenyland their pharmaceutically acceptable salts, a method for their production, and pharmaceuticals containing such compounds. The compounds of the general formula I are produced by esterifying or etherizing a compound of the general formula II ##STR2## The compounds described show strong antigestagenic effects combined with reduced glucocorticoid activity.Type: GrantFiled: September 20, 1994Date of Patent: November 19, 1996Assignee: Jenapharm GmbHInventors: Gerd Schubert, G unther Kaufmann, Lothar Sobeck, Michael Oettel, Walter Elger, Anatoli Kurischko
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Patent number: 5438134Abstract: The unsaturated 17.alpha.-cyanomethyl-17.beta.-hydroxy steroids of the formula I, ##STR1## in which R.sub.1 =Me, Eth; R.sub.2 =H, Me; R.sub.3 =H, OH, an acetoxy or alkoxy group; R.sub.4 =H, R.sub.5 =OH, an acetoxy, alkoxy group of R.sub.4 and R.sub.5 together represent a keto- or ketal group and double bonds are contained in the basic structure of the steroid, particularly between the 15 and 16 position in the steroid ring, from unsaturated 17-ketosteroids of the general formula II as described herein with the aforementioned meanings of R.sub.1 to R.sub.5 by reacting the unsaturated 17-ketosteroids with LiCH.sub.2 CN and subsequently hydrolyzing.The compounds of formula I are pharmacologically interesting steroid compounds or also intermediate products for the synthesis of highly-effective steroid products which can be used in human and veterinary medicine for the treatment of endocrine disorders and for reproductive control based on their specific hormonal/anti-hormonal actions.Type: GrantFiled: June 1, 1993Date of Patent: August 1, 1995Assignee: Jenapharm GmbHInventors: Gerhard Teichmuller, Gerd Muller