Unsaturation Between The 4- And 5-positions (e.g., 19-nortestosterones, 13 Beta-alkyl-4-gonene-3,17-diones Etc.) Patents (Class 552/646)
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Publication number: 20150094291Abstract: The invention provides a method for improving the emotional development of an infant by performing controlled exposure of the infant aged less than six months old to human fear pheromone, preferably with visual fear stimuli, so that the natural synaptic connections in the brain associated with normal fear mechanisms are stimulated and exercised. This can reduce the occurrence of mental illness later in life, in particular reduce the occurrence of schizophrenia. Advantageously the exposure to fear pheromone and visual fear stimuli is terminated and followed by comforting stimuli such as feeding, physical contact, or comforting or happy visual or audible stimuli such as laughter.Type: ApplicationFiled: October 2, 2013Publication date: April 2, 2015Applicant: Opendot Research Co LimitedInventor: Derek John GOLDSMITH
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Publication number: 20150018322Abstract: Various prodrug compounds having the general structure: Active agent-(acid)-(linker)-SO2NR1R2 are described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.Type: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Klaus Nickisch, Bindu Santhamma, Gulzar Ahmed, Frederick Meece, Walter Elger, Ralf Wyrwa, Hareesh Nair
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Publication number: 20140011785Abstract: The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient.Type: ApplicationFiled: September 6, 2013Publication date: January 9, 2014Applicant: Yale UniversityInventor: Richard Hochberg
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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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Publication number: 20130018022Abstract: The present invention relates to a pharmaceutical composition including a testis extract serving as an active ingredient for treating and preventing anemia, in which since the testis extract induces proliferation of hematopoietic stem cell, an increase in the number of red blood cell, and an increase in the amount of hemoglobin, it is effectively used as a therapeutic agent for treating anemia related to red blood cell and hemoglobin in women of childbearing age, post-childbearing age, and during pregnancy, as well as in men.Type: ApplicationFiled: April 22, 2010Publication date: January 17, 2013Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YEUNGNAM UNIVERSITYInventors: In-Ho Choi, Dong-Mok Lee, Eun-Ju Lee, Ki-Ho Lee, Yong-Pil Cheon, Tae-Hoon Chun
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Publication number: 20120258941Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-aryl derivatives of the formula I with progesterone-antagonising action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.Type: ApplicationFiled: July 8, 2010Publication date: October 11, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Klar, Wolfgang Schwede, Carsten Möller, Andrea Rotgeri, Wilhelm Bone
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Patent number: 8148558Abstract: Method of producing ?4-Tibolone by contacting tibolone with Fusarium lini (ATCC 9593) is reported.Type: GrantFiled: January 27, 2011Date of Patent: April 3, 2012Inventors: Attaur Rahman, Muhammed Iqbal Choudhary, Syed Adnan Ali Shah, Shamsun Nahar Khan
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Publication number: 20110152544Abstract: The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol comprising i) the preparation of a compound of general formula (II) by reacting a compound of general formula (I) in one or more steps to a compound of general formula II wherein R1 is a C1-C10 alkyl, alkenyl or aryl group; —Cl, —Br, —I, —F; —CN; —OH; or a —OR2, —O(CO)R2 or —R2-OH group, wherein R2 is an alkyl or alkylene group having 1-6 C atoms; and the bonding between atoms 9 and 10 is a single or a double bond. ii) aromatization of the compound of general formula II to a compound of general formula III wherein R1 and R2 have the above defined meanings; and iii) optionally, reduction of the compound of general formula III to a compound of general formula IV wherein R1 and R2 have the above defined meanings. Furthermore the invention provides several novel compounds, which can be intermediates in the above process, and processes to prepare these novel compounds.Type: ApplicationFiled: February 22, 2011Publication date: June 23, 2011Applicant: N. V. OrganonInventors: Johannes STOELWINDER, Nicolaas Elisabeth Cornelis MOERS
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Patent number: 7820642Abstract: Disclosed are compounds of the formula (I) wherein R is C1-C30 alkyl, which may be optionally further substituted with one or more of C5-C8 cycloalkyl groups, or a C5-C12 cycloalkyl, which may be optionally substituted with one or more C1-C30 alkyl groups, R? is hydrogen or lower alkyl, R? is a C1-C30 alkyl or halo, and the bond between C14 and C15 can be a single bond or double bond. Also disclosed are pharmaceutical compositions comprising such compounds and methods of use thereof. These compounds can find use in treating a number of diseases or conditions such as hypogonadism, osteoporosis, and anemia, in providing hormonal therapy and contraception, as an anabolic agent, and in suppressing the release of hormones such as the luteinizing hormone.Type: GrantFiled: January 24, 2006Date of Patent: October 26, 2010Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Richard P. Blye, Hyun K. Kim
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Publication number: 20100184735Abstract: The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient.Type: ApplicationFiled: May 2, 2008Publication date: July 22, 2010Inventor: Richard Hochberg
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Publication number: 20090023695Abstract: Methods of using 7?,11?-dimethyl-17?-hydroxy-4-estren-3-one bucyclate (I) and 7?,11?-dimethyl-17?-hydroxyestr-4-en-3-one 17-undecanoate (II) for various hormonal therapies, dosage forms comprising 7?,11?-dimethyl-17?-hydroxy-4-estren-3-one bucyclate and 7?,11?-dimethyl-17?-hydroxyestr-4-en-3-one 17-undecanoate, and processes for their preparation.Type: ApplicationFiled: August 1, 2008Publication date: January 22, 2009Applicants: and Human ServicesInventors: Richard P. Blye, Hyun K. Kim
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Patent number: 6797834Abstract: The invention is a process for the preparation of a &Dgr;4,9-steroid of formula (II) which comprises contacting a &Dgr;5(10),9(11)-steroid of formula (I) with a phosphorous containing acid.Type: GrantFiled: December 10, 2002Date of Patent: September 28, 2004Assignee: Pharmacia & Upjohn CompanyInventor: Rajappa Vaidyanathan
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Patent number: 6790971Abstract: A 19-nor-steroid having a formula selected from the group consisting of wherein the A and B rings have a structure selected from the group consisting of having hormonal properties and their preparation and novel intermediates.Type: GrantFiled: May 17, 1995Date of Patent: September 14, 2004Assignee: Aventis Pharma S.A.Inventors: Andrè Claussner, Lucien Nedelec, Daniel Philibert, Patrick Van De Velde, François Nique, Jean-Georges Teutsch
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Patent number: 6498153Abstract: An extended release composition comprising a first composition comprising growth promoters and a second composition comprising growth promoters and a biodegradable polymer is described. A method of increasing weight gain in food animals utilizing the composition, a pharmaceutical dosage form containing the composition and a method of preparing the pharmaceutical dosage form are also described, as are pellets of the composition for implantation in food animals.Type: GrantFiled: March 22, 1999Date of Patent: December 24, 2002Assignees: Akzo Nobel N.V., Southern BioSystemsInventors: Susan Mancini Cady, Claude Macar, John W. Gibson
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Patent number: 6492536Abstract: The subject of the invention is the products of formula (I): in which either R1 represents halogen, hydroxyl, (C1-C8) alkyloxy or (C1-C12) acyloxy, and R2 represents halogen or hydrogen, or R1 and R2 form together a double bond, Z is chosen from optionally substituted (C1-C8) alkylthio, optionally substituted arylthio, (C1-C8) alkyloxy, halogen, cyano, mercapto, thiocyanato and (CH2)0-1—CO2H, optionally esterified, Y represents hydrogen or methyl, the dotted line in position 1-2 or 5-6 optionally representing a second bond, as well as their addition salts, their preparation process, the intermediates of this process and the pharmaceutical compositions containing them.Type: GrantFiled: June 25, 2001Date of Patent: December 10, 2002Assignee: Aventis Pharma S.A.Inventors: Neerja Bhatnagar, Andre Claussner, Christian Marchandeau, Michele Resche Rigon, Jean-Georges Teutsch
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Patent number: 6369047Abstract: An androgenic steroid compound of the formula: wherein: X Y, Z, R1, R2, R3, R5 and R6 are as defined herein.Type: GrantFiled: June 9, 1999Date of Patent: April 9, 2002Assignee: Research Triangle InstituteInventors: C. Edgar Cook, John A. Kepler, Yue-Wei Lee, Mansukh C. Wani
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Publication number: 20020002156Abstract: An androgenic steroid compound of the formula: 1Type: ApplicationFiled: June 9, 1999Publication date: January 3, 2002Inventors: C. EDGAR COOK, JOHN A. KEPLER, YUE-WEI LEE, MANSUKH C. WANI
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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
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Patent number: 5986115Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.Type: GrantFiled: January 28, 1999Date of Patent: November 16, 1999Assignee: Schering AGInventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Kunzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
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Patent number: 5939570Abstract: 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 4, 1997Date of Patent: August 17, 1999Assignee: Pherin CorporationInventors: David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
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11.beta.-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents
Patent number: 5843933Abstract: Compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings indicated in the description, are described, as well as processes for their production, pharmaceutical preparations containing these compounds as well as their use for treatment of diseases. The compounds have antigestagenic, antiglucocorticoid, antimineralocorticoid and antiandrogenic properties.Type: GrantFiled: May 3, 1995Date of Patent: December 1, 1998Assignee: Schering AktiengesellschaftInventors: Arwed Cleve, Cornelius Scheidges, Gunter Neef, Eckhard Ottow, Walter Elger, Sybille Beier -
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: 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: 5679788Abstract: Intermediate compounds of a formula selected from the group consisting of ##STR1## which are useful intermediates for the preparation of final products of the formula ##STR2## wherein the substituents are defined in the specification.Type: GrantFiled: October 16, 1996Date of Patent: October 21, 1997Assignee: Roussel UclafInventors: Francois Nique, Jean-Georges Teutsch, Patrick Van de Velde
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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
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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: 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: 5149696Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2## having hormonal properties and their preparation and intermediates.Type: GrantFiled: February 23, 1990Date of Patent: September 22, 1992Assignee: Roussel UclafInventors: Andre Claussner, Lucien Nedelec, Daniel Philibert, Patrick Van De Velde
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Patent number: 5132299Abstract: New 11.beta. phenyl-4,9,15-estratrienes of formula I ##STR1## are described, where X implies an oxygen atom or a hydroxyimino grouping N.about.OH,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 implies a hydrogen atom, an alkyl radical or an acyl radical with in each case 1 to 10 carbon atoms,R.sup.3 stands for a hydrogen atom, a cyanomethyl group, --(CH.sub.2).sub.n CH.sub.2 Z where n implies the numbers 0, 1, 2, 3, 4 or 5, Z=--H or --OR.sup.5 with R.sup.5 having the significance of a hydrogen atom or an alkyl or acyl group with in each case 1 to 10 carbon atoms, or for --(CH.sub.2).sub.m --C.tbd.C--Y where m=0-2 and Y implies a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group with in each case 1 to 10 carbon atoms,R.sup.4 represents a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 8 carbon atoms which contains the grouping ##STR2## with X having the above significance.Type: GrantFiled: January 16, 1990Date of Patent: July 21, 1992Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Helmut Hofmeister, Stefan Scholz, Guenter Neef, Walter Elger, Sybille Beier, Krzysztof Chwalisz
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Patent number: 4954446Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.Type: GrantFiled: July 14, 1989Date of Patent: September 4, 1990Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
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Patent number: 4943566Abstract: A compound selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 is an organo of 1 to 18 carbon atoms optionally containing at least one heteroatom connected to the C ring by a carbon atom, R.sub.2 is methyl or ethyl, the A and B rings being selected from the group consisting of ##STR2## Re is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl and the D ring is selected from the group consisting of ##STR3## one of R.sub.3 and R.sub.4 is selected from the group consisting of hydroxy, protected hydroxy, acyl and alkoxy and the other is an optionally substituted aryl, R.sub.5 is an optionally substituted aryl and their non-toxic, pharmaceutically acceptable salts with acids and bases with the proviso that when the A and B rings are ##STR4## R.sub.1 is ##STR5## R.sub.2 is methyl, R.sub.3 is --OH, R.sub.4 is phenyl having anti proliferative properties.Type: GrantFiled: July 28, 1988Date of Patent: July 24, 1990Assignee: Roussel UclafiInventors: Lucien Nedelec, Francois Nique, Daniel Philibert, Martine Moguilewsky, Marie-Madeleine Bouton
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Patent number: RE39592Abstract: An extended release composition comprising a first composition comprising growth promoters and a second composition comprising growth promoters and a biodegradable polymer is described. A method of increasing weight gain in food animals utilizing the composition, a pharmaceutical dosage form containing the composition and a method of preparing the pharmaceutical dosage form are also described, as are pellets of the composition for implantation in food animals.Type: GrantFiled: December 22, 2004Date of Patent: April 24, 2007Assignee: Intervet Inc.Inventors: Susan Mancini Cady, Claude Macar, John W. Gibson