Exactly One Oxygen Bonded Directly To The Cyclopentanohydrophenanthrene Ring System (e.g., 3-keto-etiocholanic Acids, Etc.) Patents (Class 552/611)
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Patent number: 11884697Abstract: Compounds are provided according to Formula (I), and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein A, R1, and R5 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.Type: GrantFiled: April 28, 2021Date of Patent: January 30, 2024Assignee: Sage Therapeutics, Inc.Inventors: Albert Jean Robichaud, Francesco G. Salituro, Gabriel Martinez Botella, Boyd L. Harrison, John Gregory Reid
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Patent number: 9855281Abstract: A composition for enhancing libido of a pharmaceutically effective amount of a libido-enhancing therapeutic of (5S,10R,13S,17S)-13-methyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17yl acetate (Formula I), (3S,5S,10R,13S,17S)-3-hydroxy-13-methylhexadecahydro-1H-cyclopenta[a]phenanthren-17yl acetate (Formula II), (5S,10S,13S,17S)-17-hydroxy-13-methyltetradecahydro-1H-cyclopenta[a]phenanthren-3(2H)-one (Formula III), isomers thereof, analogs thereof, or combinations thereof, and a pharmaceutically acceptable carrier. A method of enhancing libido, by administering the composition to an individual in need of an enhanced libido, and enhancing libido in the individual or animal which is male or female. A method of enhancing libido, by administering the composition of the present invention to an individual at an age when libido and sexual desire have naturally decreased, and enhancing libido in the individual.Type: GrantFiled: November 20, 2014Date of Patent: January 2, 2018Assignee: Scott Freeman Consultant, LLCInventor: Scott Freeman
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NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
Publication number: 20140235600Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: December 18, 2013Publication date: August 21, 2014Applicant: Washington UniversityInventors: Douglas Covey, Albert Jean Robichaud -
Patent number: 8586770Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.Type: GrantFiled: February 18, 2011Date of Patent: November 19, 2013Assignee: Harbor Therapeutics, Inc.Inventor: James M. Frincke
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Patent number: 8207150Abstract: The 17?-cyano-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity.Type: GrantFiled: June 11, 2008Date of Patent: June 26, 2012Assignee: Bayer Pharma AGInventors: Joachim Kuhnke, Jan Huebner, Rolf Bohlmann, Thomas Frenzel, Ulrich Klar, Frederik Menges, Sven Ring, Steffen Borden, Hans-Peter Muhn, Katja Prelle
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Publication number: 20110014641Abstract: The present invention relates to compounds useful for measuring aromatase activity. The invention further provides methods for measuring aromatase activity and for screening test agents which modulate aromatase activity. A kit is also provided for use in such screening methods.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: GE HEALTHCARE UK LIMITEDInventors: JOHN GERARD WHATELEY, RAHMAN AZIZ ISMAIL, PETER GORDON LAUGHTON
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Publication number: 20100292184Abstract: The 17?-cyano-19-androst-4-ene derivatives of the present invention possess gestagenic activity.Type: ApplicationFiled: June 12, 2008Publication date: November 18, 2010Applicant: BAYER SCHERING PHARMA AGInventors: Joachim Kuhnke, Jan Huebner, Rolf Bohlmann, Thomas Frenzel, Ulrich Klar, Frederik Menges, Sven Ring, Steffen Borden, Hans Peter Muhn, Katja Prelle
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Publication number: 20100160657Abstract: The present invention relates to new synthetic receptors. More particularly, the present invention relates to methods for synthesizing preferred membrane-binding elements, preferably cholesterylamine derivatives, including 3?-amino-5-cholestene (3?-cholesterylamine) and related 3?-halides through i-steroid and retro-i-steroid rearrangements. The invention further relates to use of the synthetic receptors for delivering a protein, peptide, drug, prodrug, lipid, nucleic acid, carbohydrate or small molecule into a target cell via receptor-mediated endocytosis. According to the invention, novel synthetic mimics of cell surface receptors have been designed and methods for use of the same are disclosed.Type: ApplicationFiled: December 11, 2009Publication date: June 24, 2010Applicant: THE PENN STATE RESEARCH FOUNDATIONInventors: BLAKE R. PETERSON, QI SUN
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Patent number: 7691836Abstract: The subject invention provides a compound according to Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt and/or hydrate form and/or prodrug thereof.Type: GrantFiled: March 18, 2005Date of Patent: April 6, 2010Assignee: N.V. OrganonInventors: Johannes Antonius Maria Hamersma, Johannes Bernardus Maria Rewinkel
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Publication number: 20100056488Abstract: The invention features corticosteroids conjugated to either a charged group or a bulky group in a manner that resists in vivo cleavage, the resulting conjugate is a peripherally acting steroid with reduced activity in the central nervous system. The invention provides a method for treating a patient having an inflammatory disease by administering to the patient a corticosteroid conjugate.Type: ApplicationFiled: November 4, 2009Publication date: March 4, 2010Applicant: The McLean Hospital CorporationInventors: Martin H. Teicher, Susan L. Andersen-Navalta
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Publication number: 20100041906Abstract: The present invention concerns a method for the controlled precipitation of organic compounds giving crystals with a very small average size and a very narrow size distribution.Type: ApplicationFiled: January 26, 2007Publication date: February 18, 2010Inventors: Huibert Albertus Van Boxtel, Servatius Hubertus Johannes Wilhelmus Leenen, Matheus Lambertus Spapens
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Publication number: 20090187032Abstract: The present invention relates to a new industrial process for the synthesis of solvate-free 17?-acetoxy-11?-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process.Type: ApplicationFiled: May 18, 2007Publication date: July 23, 2009Applicant: RICHTER GEDEON NYRT.Inventors: Lajosne Dancsi, Gyorgy Visky, Zoltan Tuba, Janos Csorgei, Csaba Molnar, Endrene Magyari
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Publication number: 20090131388Abstract: To inhibit production of adipocytokines, in particular, adipocytokines that elicit insulin resistance and to prevent onset of pathosis caused by the insulin resistance or ameliorate the pathosis, the present invention provides an agent or a food or drink which contains a compound having a lophenol skeleton, or an organic solvent extract or a hot water extract of a Liliaceae plant or, a fraction thereof containing the compound as an active ingredient.Type: ApplicationFiled: September 22, 2006Publication date: May 21, 2009Applicant: MORINAGA MILK INDUSTRY CO., LTD.Inventors: Miyuki Tanaka, Eriko Misawa
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Publication number: 20090042844Abstract: Compounds having the structure, their salts or N-oxide derivatives: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.Type: ApplicationFiled: April 9, 2008Publication date: February 12, 2009Inventors: Fernand LABRIE, Sylvain GAUTHIER, Julie CLOUTIER, Josee MAILHOT, Steeves POTVIN, Sylvain DION, Jean-Yves SANCEAU
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Patent number: 7402577Abstract: Compounds of structural formula as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue.Type: GrantFiled: September 27, 2002Date of Patent: July 22, 2008Assignee: Merck & Co., Inc.Inventors: Jiabing Wang, Mark E. Duggan, David B. Whitman
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Patent number: 7371741Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering compounds of the general formula: wherein the variables are defined in the specification.Type: GrantFiled: May 28, 2004Date of Patent: May 13, 2008Assignee: EntreMed, Inc.Inventors: Gregory E. Agoston, Theresa M. LaVallee, Victor S. Pribluda, Jamshed H. Shah, Anthony M. Treston
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Patent number: 7199115Abstract: New 17?-fluorosteroid compounds of formula (I) are disclosed: wherein R1 denotes H or methyl; R2 and R3 each denote H, Cl or methyl; and either a double bond or a single bond is present between C-6 and C-7 and also C-9 and C-10 of the steroid ring system respectively. These compounds have an activity profile with hybrid character so that they act as inhibitors for 5?-reductase and as high potency gestagens. Pharmaceutical compositions containing them are disclosed. They are suitable for treatment of conditions, which are caused by high levels of androgen in organs and tissues. These new compounds can be used in combination with other hormonal substances, such as estrogens, testosterone and other androgens, as contraceptives and for other applications.Type: GrantFiled: April 13, 2005Date of Patent: April 3, 2007Assignee: Schering AGInventors: Ulrich Bothe, Peter Droescher, Walter Elger, Gudrun Reddersen, Bernd Menzenbach, Hans-Udo Schweikert, Alexander Hillisch, Birgitt Schneider
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Patent number: 6953785Abstract: Provided is steroid sulfatase inhibitors comprising, as the active ingredient, an estra-1,3,5(10)-triene derivative which is represented by formula (I): {wherein R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group or, etc.; R3 represents a hydrogen atom etc.; R4 represents a hydrogen atom etc.; R5 represents a hydrogen atom etc.; R6 represents a cyano group, an amino group, COR53 (wherein R53 represents a substituted lower alkyl group etc.), a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, etc}, or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 24, 2001Date of Patent: October 11, 2005Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Tsutomu Agatsuma, Kozue Muramatsu, Takeshi Takahashi, Shiro Akinaga, Chikara Murakata
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Patent number: 6638923Abstract: Estra-1,3,5(10),16-tetraene derivatives represented by the following formula (I): (wherein R1 is as defined by the present specification.Type: GrantFiled: May 18, 2001Date of Patent: October 28, 2003Assignees: Kyowa Hakko Kogyo Co., Ltd., Duquesne University of the Holy GhostInventors: Yoji Ino, Nobuyoshi Amishiro, Taisuke Nakata, Hiroyuki Ishida, Shiro Akinaga, Chikara Murakata, Pui-Kai Li
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Patent number: 6610866Abstract: A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.Type: GrantFiled: April 12, 2001Date of Patent: August 26, 2003Assignee: Magainin Pharmaceuticals, Inc.Inventors: William A. Kinney, Steven Jones, Xuehai Zhang, Meena N. Rao, Michel Bulliard, Harold Meckler, Nancy Lee
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Patent number: 6596885Abstract: Novel compounds having a formula selected from the group consisting of wherein the substituents are defined as in the specification which are intermediates for the production of vinyl compounds having a remarkable anti-estrogenic and anti-proliferative activity.Type: GrantFiled: June 26, 2001Date of Patent: July 22, 2003Assignee: Aventis Pharma S.A.Inventors: Andre Claussner, Francois Nique, Jean-Georges Teutsch, Patrick Van de Velde
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Publication number: 20020183532Abstract: A compound for supplementing the concentration of a parent androgen in a subject in vivo, wherein the parent androgen has a skeletal structure including a 17 position and the parent androgen further has a 17&bgr;-hydroxy group comprising a 17&bgr;-hydroxy hydrogen appended to the 17 position. The compound comprises a substrate having the skeletal structure of the parent androgen including a 17 position corresponding to the 17 position of the parent androgen, and a promoiety comprising an alkoxymethyl ether appended to the 17 position of the substrate as a substitute for the 17&bgr;-hydroxy hydrogen. Related compounds and methods also are disclosed.Type: ApplicationFiled: June 1, 2001Publication date: December 5, 2002Inventor: William J. Roberts
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Patent number: 6437157Abstract: A compound selected from the group consisting of a compound of the formula wherein R1 and R2 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, R3 is an &agr;-alkyl of 1 to 8 carbon atoms, n is an integer from 2 to 15, R4 is alkyl of 1 to 12 carbon atoms, R5 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 useful for controlling fertility in male warm-blooded animals.Type: GrantFiled: March 13, 1995Date of Patent: August 20, 2002Assignee: Hoechst Marion RousselInventors: Armelle Bonfils, Daniel Philibert
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Publication number: 20020103391Abstract: The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors.Type: ApplicationFiled: March 9, 2001Publication date: August 1, 2002Inventors: David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
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Patent number: 6410760Abstract: The process of the present invention transforms a steroidal ketone of formula (III) to androst-4-en-17&bgr;-carboxylic acid (IV) by reaction with K2SO5.KHSO4.K2SO4.Type: GrantFiled: October 2, 2000Date of Patent: June 25, 2002Assignee: Pharmacia & Upjohn CompanyInventors: Kevin C. Grega, Scott W. Ashford
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Patent number: 6399595Abstract: Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.Type: GrantFiled: August 3, 2001Date of Patent: June 4, 2002Assignees: Duquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.Inventors: Pui-Kai Li, Chikara Murakata, Shiro Akinaga
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Publication number: 20020058651Abstract: Estra-1,3,5(10),16-tetraene derivatives represented by the following formula (I): 1Type: ApplicationFiled: May 18, 2001Publication date: May 16, 2002Inventors: Yoji Ino, Nobuyoshi Amishiro, Taisuke Nakata, Hiroyuki Ishida, Shiro Akinaga, Chikara Murakata, Pui-Kai Li
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Patent number: 6376687Abstract: Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.Type: GrantFiled: January 24, 2000Date of Patent: April 23, 2002Assignees: Duquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.Inventors: Pui-Kai Li, Chikara Murakata, Shiro Akinaga
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Patent number: 6288050Abstract: Sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.Type: GrantFiled: January 25, 1999Date of Patent: September 11, 2001Assignees: Duquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.Inventors: Pui-Kai Li, Chikara Murakata, Shiro Akinaga
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Patent number: 6262043Abstract: Estra-1,3,5(10),16-tetraene derivatives represented by the following formula (I): (wherein R1 represents hydroxy, alkoxy, or NR2R3 (wherein R2 and R3 are the same or different, and each represents hydrogen, straight-chain lower alkyl having 1 to 3 carbon atoms, or branched-chain lower alkyl having 3 to 8 carbon atoms)), or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 13, 2000Date of Patent: July 17, 2001Assignees: Kyowa Hakko Kogyo Co., Ltd., Duquesne University of the Holy GhostInventors: Yoji Ino, Nobuyoshi Amishiro, Taisuke Nakata, Hiroyuki Ishida, Shiro Akinaga, Chikara Murakata, Pui-Kai Li
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Patent number: 6251887Abstract: The invention relates to 17&bgr;-aryl(arylmethyl)oxy(thio)alkyl-androstane derivatives having general formula (I), wherein R1 is (H,OR), (H,OSO3H) or NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alyl; n is 0, 1, or 2; X is O, S, S(O) or S(O)2; m is 0 or 1; each of R4, R5 and R6 is independently hydrogen, hydroxy, (C1-4)alkoxy, halogen, NR7R8 or (C1-4)alkyl, optionally substituted by hydroxy, alkoxy, halogen or oxo; each of R7 and R8 is independently hydrogen or (C1-4)alkyl, and wherein the dotted lines indicate a &Dgr;7 or a &Dgr;8 double bond, or a pair of conjugated double bonds selected from &Dgr;7,14, &Dgr;8,14 and &Dgr;6,8(14); or a pharmaceutically acceptable salt thereof. The compounds of the invention have meiosis regulating activity and can be used for the control of fertility.Type: GrantFiled: June 16, 2000Date of Patent: June 26, 2001Assignee: Akzo Nobel N.V.Inventors: Christian Heijmans, Jaap van der Louw
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Patent number: 6117994Abstract: A new process for the preparation of 16.beta.-methyl-steroids of the formula ##STR1## and novel intermediates.Type: GrantFiled: April 22, 1998Date of Patent: September 12, 2000Assignee: Hoechst Marion RousselInventors: Catherine Geurts, Michel Vivat
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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: 5969168Abstract: The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors. The steroids are useful as ligands to neuroepithelial receptors in the human vomeronasal gland to stimulate autonomic and hypothalamic activity.Type: GrantFiled: September 29, 1994Date of Patent: October 19, 1999Assignee: Pherin CorporationInventors: David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
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Patent number: 5925774Abstract: The invention relates to estrene steroids, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.Type: GrantFiled: June 1, 1995Date of Patent: July 20, 1999Assignee: Pherin CorporationInventors: David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
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Patent number: 5880115Abstract: Sulfatase inhibitor compounds having the formula: ##STR1## wherein X, Y, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification. The compounds are useful in the treatment of estrogen dependent illnesses. Methods for synthesizing these compounds are also disclosed.Type: GrantFiled: July 18, 1997Date of Patent: March 9, 1999Assignee: Duquesne University of the Holy GhostInventors: Pui-Kai Li, Kyle W. Selcer
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Patent number: 5792759Abstract: Novel 17-hydroxyiminoalkyl and 17-hydroxyiminomethylalkenyl steroids of the general formula (I) ##STR1## where A, R.sup.1 and R.sup.2 are defined in the specification are disclosed. The compounds have cardiovascular activity. Pharmaceutical compositions containing compounds of formula (I) are also disclosed for the treatment of heart failure and hypertension.Type: GrantFiled: May 17, 1996Date of Patent: August 11, 1998Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Luisa Quadri, Alberto Cerri, Patrizia Ferrari, Maria Pia Zappavigna
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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: 5650526Abstract: The invention is drawn to a process for the preparation of oxoetiocholenic acid of the formula I ##STR1## by reacting a compound of the formula II ##STR2## with a halonitrile in the presence of a base followed by formation of a 3-ketone group. The intermediate formed is reacted with an acid of the formula HX in an anhydrous medium followed by dehydrohalogenation of the resulting compound in the presence of a base. The intermediate produced then undergoes alkaline hydrolysis followed by a conventional acid treatment to obtain the compound of formula I.Type: GrantFiled: August 28, 1995Date of Patent: July 22, 1997Assignee: Roussel UclafInventors: Patrick Roussel, Michel Vivat
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Patent number: 5633392Abstract: The invention relates to estrene steroids, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.Type: GrantFiled: May 31, 1995Date of Patent: May 27, 1997Assignee: Pherin CorporationInventors: David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
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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: 5561124Abstract: The invention relates to substituted 17.alpha.-acyl steroidal 5.alpha.-reductase inhibiting compounds. The invention also relates to pharmaceutical compositions containing these compounds and their use for reducing prostate size and treating prostate adenocarcinoma. Further, the invention describes a process for making these compounds by heating the corresponding substituted 17.beta.-acyl steroid in a solvent, such as ethylene glycol or dimethyl sulfoxide (DMSO), in a base, such as sodium or potassium hydroxide.Type: GrantFiled: May 17, 1995Date of Patent: October 1, 1996Inventor: Robert L. Webb
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Patent number: 5523428Abstract: A process for the production of 1-methyl-3-keto-.DELTA..sup.1,4 steroids of general formula I ##STR1## in which St symbolizes the radical of asteroid molecule, where a 3-keto-.DELTA..sup.1,4 steroid of general formula II ##STR2## in which St has the above-mentioned meaning, is reacted in an inert solvent in the presence of a nickel salt soluble therein with an organometallic compound of formula III, IV or V ##STR3## where X, Y.sub.1, Y.sub.2, Y.sub.3, Z.sub.1 and Z.sub.2 are as defined in the specification.Type: GrantFiled: April 18, 1995Date of Patent: June 4, 1996Assignee: Schering AktiengesellschaftInventors: Jurgen Westermann, Klaus Nickisch, Annette Prelle
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Patent number: 5496813Abstract: There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their preparation are disclosed.Type: GrantFiled: August 13, 1992Date of Patent: March 5, 1996Assignee: Marigen S.A.Inventors: Carl Eugster, Conrad H. Eugster, Walter Haldemann, Giorgio Rivara
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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
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Patent number: 5436401Abstract: A 22-oxacholecalciferol derivative represented by formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group; and R.sub.2 and R.sub.3, which may be the same or different, each represent a lower alkyl group having from 1 to 5 carbon atoms,and a process for preparing the same are disclosed. The compound of the present invention has potent differentiation inducing activity and cell proliferation inhibitory activity and is expected to be useful as an anti-tumor agent, an antirheumatic, a treating agent for psoriasis, and a treating agent for hyperparathyreosis. The process of the present invention makes it possible to efficiently produce a desired 22-oxacholecalciferol derivative while reducing by-production.Type: GrantFiled: June 13, 1994Date of Patent: July 25, 1995Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Masahiro Kato, Tetsuhiro Mikami, Kiyoshige Ochi, Hiroyoshi Watanabe, Noboru Kubodera
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Patent number: 5273971Abstract: 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: July 3, 1989Date of Patent: December 28, 1993Assignee: Schering AktiengesellschaftInventors: Stefan Scholz, Eckhard Ottow, Guenter Neef, Walter Elger, Sybille Beier, Krzysztof Chwalisz
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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: 5140106Abstract: A process for the production of 3-deoxy-4-ene steroids of the general formula I ##STR1## is described, in which R.sub.1, R.sub.2 and R.sub.3 mean a hydrogen atom or a methyl group,R.sub.4 represents a lower alkyl group, a phenyl group or a free, esterified or etherified hydroxy group,R.sub.5 symbolizes a hydrogen atom, a vinyl group or the grouping --C.tbd.CR.sub.6 with R.sub.6 meaning a hydrogen atom, an alkyl group with a maximum of 4 carbon atoms or a halogen atom,X represents a methylene group, a fluoromethylene group, an ethylidene group or a vinylidene group,Y and U represent a methylene group or an ethylidene group andZ symbolizes a methylene group, an ethylidene group, a vinylidene group, a chloromethylene group or a hydroxymethylene group and in which the bonds represent three single bonds or one double bond and two single bonds or a conjugated double bond.Type: GrantFiled: January 17, 1991Date of Patent: August 18, 1992Assignee: Schering AktiengesellschaftInventors: Ekkehard Winterfeldt, Ulf Tilstamm, Helmut Hofmeister, Henry Laurent
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Patent number: 5137882Abstract: Invented are 3-acetic acid-steroidal compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase including using these compounds to reduce prostate size and to treat prostatic adenocarcinoma. Also invented are intermediates used in preparing these compounds.Type: GrantFiled: June 11, 1990Date of Patent: August 11, 1992Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf