And Oxygen Bonded Directly At The 20-position Of The Compound Patents (Class 552/556)
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Patent number: 11912737Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.Type: GrantFiled: October 9, 2020Date of Patent: February 27, 2024Assignee: Sage Therpeutics, Inc.Inventors: Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro, Richard Thomas Beresis
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Patent number: 8513228Abstract: The present invention relates to novel crystalline Form A of 17?-acetoxy-21-methoxy-11?-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124) and methods for the preparation of it in excellent purity.Type: GrantFiled: March 22, 2010Date of Patent: August 20, 2013Assignee: Richter Gedeon Nyrt.Inventors: Csaba Santa, Adam Demeter, Balazs Havasi, Sandor Maho
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Publication number: 20130203718Abstract: The present invention relates to a compound of formula (I): for its use as progesterone receptor antagonist, in particular for its use for the prevention and/or the treatment of cancer or uterine pathologies.Type: ApplicationFiled: May 9, 2011Publication date: August 8, 2013Inventors: Marie-Edith Rafestin-Oblin, Mouad Alami, Hugues Loosfelt, Abdallah Hamze, Ali Junaid Khan, Abdellatif Tikad, Marc Lombes, Jean-Daniel Brion
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Patent number: 8211881Abstract: The invention concerns compounds called pyrene-cholesterols, of general formula (I), wherein: X represents a CH2 group or an oxygen atom and n is an integer from 2 to 10, as well as their use for implementing a method for detecting and measuring the effects of specific products on biological membranes, and a method for preparing the compounds.Type: GrantFiled: March 23, 2006Date of Patent: July 3, 2012Assignee: Centre National de la Recherche ScientifiqueInventors: Christophe Le Roux, André Lopez
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OXYSTEROLS FOR ACTIVATION OF HEDGEHOG SIGNALING, OSTEOINDUCTION, ANTIADIPOGENESIS, AND WNT SIGNALING
Publication number: 20110008297Abstract: Synthetic oxysterols can be made and can be used for the treatment of bone disorders, obesity, cardiovascular disorders, and neurological disorders.Type: ApplicationFiled: December 3, 2008Publication date: January 13, 2011Applicant: The Regents of the University of CaliforniaInventors: Farhad Parhami, Michael E. Jung, Khanhlinh Nguyen, Dongwon Yoo, Woo-Kyun Kim -
Patent number: 6900193Abstract: The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ?O and ?N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.Type: GrantFiled: March 17, 2000Date of Patent: May 31, 2005Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Hyun K. Kim, Richard P. Blye, Pemmaraju N. Rao, James W. Cessac, Carmie K. Acosta, Anne Marie Simmons
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Patent number: 6861415Abstract: A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ?O and ?N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.Type: GrantFiled: April 30, 1997Date of Patent: March 1, 2005Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Hyun K. Kim, Richard P. Blye, Pemmaraju N. Rao, James W. Cessac, Carmie K. Acosta
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Patent number: 6528501Abstract: The invention relates to 22S hydroxycholesta-8, 14-diene derivatives having general formula (I) wherein R1 is OR, 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)alkyl; R4 is hydrogen, (C1-6)alkyl or (C1-6)acyl; R5 is hydrogen; or R5 designates, together with R6, an additional bond between the carbon atoms at which R5 and R6 are placed; R6 is hydrogen, hydroxy or halogen, or R6 designates, together with R5, an additional bond between the carbon atoms at which R6 and R5 are placed; each or R7 and R8 is independently hydrogen or (C1-4)alkyl, optionally substituted with OH, (C1-4)alkoxy, or halogen; or a pharmaceutically acceptable salt thereof. The compounds of the invention have meiosis activating activity and can be used for the control of fertility.Type: GrantFiled: July 16, 2001Date of Patent: March 4, 2003Assignee: Akzo Nobel N.V.Inventors: Dirk D. Leysen, Jaap J. van der Louw, Robert Gerard Jules Marie Hanssen, A. Anja Wiersma
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Publication number: 20020025951Abstract: A compound having the general formula: 1Type: ApplicationFiled: May 24, 1999Publication date: February 28, 2002Inventors: HYUN K. KIM, RICHARD P. BLYE, PEMMARAJU N. RAO, JAMES W. CESSAC, CARMIE K. ACOSTA
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Patent number: 6046186Abstract: Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.Type: GrantFiled: December 24, 1997Date of Patent: April 4, 2000Assignee: SRI InternationalInventors: Masato Tanabe, Richard H. Peters, Wan-Ru Chao, Kazuhiko Shigeno
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Patent number: 6043603Abstract: The invention relates to a low-pressure discharge lamp with at least one porting element (12) placed inside a discharge vessel (10). Said supporting element is provided with a mercurial coating (13) and is coated with a getter material (14). The coated surfaces of the supporting element (12) are inclined at an angle of at least 30 degrees in relation to the longitudinal axis (A--A) of the discharge vessel (10).Type: GrantFiled: May 21, 1998Date of Patent: March 28, 2000Assignee: Patent-Treuhand-Gesellschaft fuer elektrische Gluehlampen mbHInventor: Erolf Weinhardt
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Patent number: 6037339Abstract: A C-11 substituted steroid and a method of use of a C-11 substituted steroid to treat osteoporosis.Type: GrantFiled: January 16, 1998Date of Patent: March 14, 2000Assignee: Akzo Nobel N.V.Inventors: Hubert Jan Jozef Loozen, Lodewijk Pieter Cornelis Schot, Jane Margretha Lena van der Werf-Pieters
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Patent number: 5710144Abstract: A C-11 substituted steroid and a method of use of a C-11 substituted steroid to treat osteoporosis.Type: GrantFiled: January 29, 1997Date of Patent: January 20, 1998Assignee: Akzo Nobel N.V.Inventors: Hubert Jan Jozef Loozen, Lodewijk Pieter Cornelis Schot, Jane Margretha Lena van der Werf-Pieters
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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: 5473087Abstract: Mixtures of compounds of ##STR1## or a mixture of the latter and a compound of the formula ##STR2## which are useful intermediates for the preparation 20-keto-21(S)-hydroxy steroids.Type: GrantFiled: September 16, 1994Date of Patent: December 5, 1995Assignee: Roussel-UclafInventors: Jean Buendia, Jean-Yves Godard, Philippe Mackiewicz, Christian Richard
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Patent number: 5399685Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 12 carbon atoms, R.sub.3 is alkyl of 1 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.4 is a remainder of an easily cleavable ether, K is a protected ketone function in the form of ketal, thioketal or mixed ketal and R.sub.1 has the above definition with a magnesium organic compound reagent of the formulaHalMg--CH.sub.2 --R.sub.2 Awherein Hal is a halogen and R.sub.2 is defined as above to obtain a compound of the formula ##STR3## wherein R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an acylation agent to obtain a compound of the formula ##STR4## wherein R.sub.5 is alkyl of 1 to 6 carbon atoms or aryl of 6 to 10 carbon atoms and R.sub.1, R.sub.2 and K are defined as above, reacting the latter with an appropriate alkylation agent to obtain a compound of the formula ##STR5## wherein R.sub.1, R.sub.2, R.sub.Type: GrantFiled: June 11, 1993Date of Patent: March 21, 1995Assignee: Roussel-UclafInventors: Jean Buendia, Veronique Crocq, Christian Masson, Denis Prat, Michel Vivat
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Patent number: 5384419Abstract: An improved process for the preparation of 20-keto-21(S)-hydroxy steroids of the Formula ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 12 carbon atoms, and R.sub.3 is alkyl of 1 to 4 carbon atoms and novel intermediates therefrom.Type: GrantFiled: June 2, 1993Date of Patent: January 24, 1995Assignee: Roussel-UclafInventors: Jean Buendia, Jean-Yves Godard, Philippe Mackiewicz, Christian Richard
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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: 5068368Abstract: A process for the preparation of ethynyl carbinols of the formula: ##STR1## wherein R" is hydrogen, a substituted or unsubstituted aliphatic or aromatic hydrocarbon, R'" is a substituted or unsubstituted aliphatic or aromatic hydrocarbon or R" and R'" together to the carbon atom to which they are joined represent a steroid, which comprises the steps ofA. reacting in a solvent system comprising an aromatic hydrocarbon, at least one lithium alkylamide selected from the group consisting of: ##STR2## wherein R is a hydrogen or lower alkyl, R' is hydrogen, lower alkyl, a substituted or unsubstituted aliphatic, alicyclic or aromatic hydrocarbon, x is an integer of 2 to 8, y and z are each 0 to 1, with acetylene to form a monolithium acetylideB. reacting in a solvent system comprising an aromatic hydrocarbon, the monolithium acetylene from Part A with a ketone of the formula R"R'"C.dbd.O, wherein R" and R'" are as hereinbefore defined, and thenC.Type: GrantFiled: May 10, 1990Date of Patent: November 26, 1991Assignee: Cyprus Foote Mineral CompanyInventors: W. Novis Smith, Christopher Louer
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Patent number: 4954491Abstract: The present invention is directed to a method for the treatment of hyperaldosteronism and related disorders which comprises administering to an appropriate patient an appropriate 18-cyanopregnane.Type: GrantFiled: January 27, 1989Date of Patent: September 4, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: J. O'Neal Johnston, Gene W. Holbert
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Patent number: D506923Type: GrantFiled: September 19, 2003Date of Patent: July 5, 2005Assignee: Stokely-Van Camp, Inc.Inventors: Gerald Zboch, Tracy M. Momany, Robert J. Groll