Spiro Patents (Class 552/508)
-
Publication number: 20140303385Abstract: The present invention provides processes for the production of chiral compounds in a stereoisomeric excess. The present processes involve reacting a hydrometallated alkene compound with a compound comprising a conjugated-bond system under conditions such that the compounds undergo an asymmetric 1,4- or 1,6-conjugate addition reaction, generating a chiral compound in a stereoisomeric excess. The reaction is performed in the presence of a metal catalyst, which catalyst preferably comprises a non-racemic chiral ligand.Type: ApplicationFiled: October 12, 2012Publication date: October 9, 2014Applicant: Isis Innovation LimitedInventors: Stephen P. Fletcher, Rebecca M. Maksymowicz, Philippe M.C. Roth
-
Publication number: 20120283450Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: ApplicationFiled: July 18, 2012Publication date: November 8, 2012Inventors: Eric Anderson, Gary L. Bolton, Deborah A. Ferguson, Xin Jiang, Robert M. Kral, JR., Patrick M. O'Brien, Melean Visnick
-
Publication number: 20110144363Abstract: The invention relates to processes for obtaining steroids with a spirolactone group in position 17, particularly to industrially obtaining 6?,7?; 15?,16?-dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, commonly known as Drospirenone, as well as to intermediates useful in said process.Type: ApplicationFiled: June 16, 2010Publication date: June 16, 2011Applicant: CRYSTAL PHARMA, S.A.Inventors: Jesús Miguel Iglesias Retuerto, Luis Gerardo Gutiérrez Fuentes, Antonio Lorente Bonde-Larsen
-
Publication number: 20110053902Abstract: Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. Said compounds are used for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.Type: ApplicationFiled: April 11, 2007Publication date: March 3, 2011Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Alberto Cerri, Marco Torri, Silvia Armaroli, Leonardo Banfi, Giuseppe Bianchi, Giulio Carzana, Patrizia Ferrari, Rosamaria Michaeletti, Simona Sputore, Maria Pia Zappavigna
-
Publication number: 20110046402Abstract: The subject of the invention is a method for preparing compounds of general formula (I): in which A, Z, R3 are as defined in the description, and the intermediate compounds for carrying out this method.Type: ApplicationFiled: October 29, 2010Publication date: February 24, 2011Applicant: Aventis Pharma S.A.Inventors: Denis Prat, Christian Moratille, Francoise Benedetti, Lahlou Nait-Bouda
-
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
-
Publication number: 20100130455Abstract: Described herein are bismethylene-17? carbolactone derivatives having progestational and/or antimineralocorticoid and/or aldosterone antagonistic activity. Also described herein are methods of preparing and using these novel compounds.Type: ApplicationFiled: March 4, 2009Publication date: May 27, 2010Inventors: Klaus Nickisch, Pemmaranu N. Rao, James W. Cessac, Anne Marie Simmons
-
Patent number: 7112670Abstract: The present invention involves a novel crystal form of 17?-hydroxy-7?-(5?-methyl-2?-furyl)-pregna-4,9(11)-dien-3-one-21-carboxylic acid, ?-lactone, having the formula which is an intermediate useful in preparation of an important pharmaceutical, eplerenone.Type: GrantFiled: September 19, 2003Date of Patent: September 26, 2006Assignee: Pharmacia CorporationInventors: Bruce Allen Pearlman, Frederick J. Antosz
-
Publication number: 20040236125Abstract: The present invention provides, in one aspect, novel derivatives comprising sterols and/or stanols and an NSAID selected from salicylic acids and arylalkanoic acids, including salts of these derivatives, and having one or more of the following formulae: 1Type: ApplicationFiled: September 25, 2002Publication date: November 25, 2004Applicant: FORBES MEDI-TECH INC.Inventors: James P. Kutney, P. Haydn Pritchard, Yanbing Ding, Kishor M. Wasan
-
Patent number: 6534490Abstract: Described are new, unsaturated 14,15-cyclopropano-androstanes of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are characterized by hormonal (gestagenic and/or androgenic) activity and may be used for hormone replacement therapy.Type: GrantFiled: December 21, 2000Date of Patent: March 18, 2003Assignee: Jenapharm GmbH & Co. KG.Inventors: Sven Ring, Sigfrid Schwarz, Walter Elger, Birgitt Schneider, Günter Kaufmann, Lothar Sobek
-
Patent number: 6388109Abstract: Described are new 14,15-cyclopropano steroids of the 19-norandrostane series of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are distinguished by hormonal (gestagenic and/or androgenic) activity.Type: GrantFiled: December 20, 2000Date of Patent: May 14, 2002Assignee: Jenapharm GmbH & Co. KGInventors: Sigfrid Schwarz, Gerd Schubert, Sven Ring, Walter Elger, Birgitt Schneider, Günter Kaufmann, Lothar Sobek
-
Publication number: 20020016455Abstract: Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I 1Type: ApplicationFiled: April 3, 2001Publication date: February 7, 2002Inventors: John S. Ng, Ping T. Wang, Julio A. Baez, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Gennaro Mucciariello, Fortunato Vanzanella, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
-
Publication number: 20020007079Abstract: Certain novel sterol derivatives having no hydroxy group in the 3-position can be used to regulate the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.Type: ApplicationFiled: July 9, 1999Publication date: January 17, 2002Inventors: ANTHONY MURRAY, PETER FAARUP
-
Publication number: 20010005757Abstract: Certain compounds, structurally related to natural compounds which can be extracted i.a. from bull testes and from human follicular fluid, can be used for regulating the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.Type: ApplicationFiled: January 17, 2001Publication date: June 28, 2001Inventors: Christian Grondahl, Frederik Christian Gronvald, Peter Faarup, Anthony Murray, Jan Lund Ottesen
-
Patent number: 6177418Abstract: The invention is directed to compounds, compositions and method of preparation of compounds of formulae I and II: wherein X, Q1, Q2, R1 and R2 are as defined by the specification. The compounds are disclosed as useful cholesterol-lowering and anti-atherosclerosis agents.Type: GrantFiled: March 16, 1998Date of Patent: January 23, 2001Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Welf von Daehne, Wagn Ole Godtfredsen
-
Patent number: 6043236Abstract: Compounds of the formula I ##STR1## a process for their preparation, their use in the treatment of autoimmune disorders as well as new intermediates for their preparation.Type: GrantFiled: April 23, 1997Date of Patent: March 28, 2000Assignee: Astra AktiebolagInventors: Ralph Brattsand, Rikard Holmdahl, Liselotte Jansson, Marjana Loncar, Lars Pettersson
-
Patent number: 5981744Abstract: Multiple reaction schemes, process steps and intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other 9,11-epoxy-steroids.Type: GrantFiled: December 11, 1996Date of Patent: November 9, 1999Assignee: G. D. Searle and Co.Inventors: John S. Ng, Ping T. Wang, Julio A. Baez, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
-
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
-
Patent number: 5523298Abstract: In this invention, the new etheno- and ethano-19,11-bridged 4-estrenes of general formula I ##STR1## are described, in which W, R.sup.1, R.sup.2, R.sup.6a, R.sup.6b, R.sup.7, R.sup.14, R.sup.15, R.sup.16, R.sup.11, R.sup.11' and R.sup.19 have the meaning indicated in the description, as well as a process for their production.The new compounds have strong progestational activity and are suitable for the production of pharmaceutical agents.Type: GrantFiled: October 13, 1993Date of Patent: June 4, 1996Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Wolfgang Schwede, Wolfgang Halfbrodt, Karl-Heinrich Fritzemeier, Rolf Krattenmacher
-
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: 5426179Abstract: Steroid compounds active on the cardiovascular system of formula ##STR1## wherein X, n, R, R.sub.1 and R.sub.2 have the meanings mentioned in the description are described.Type: GrantFiled: February 12, 1992Date of Patent: June 20, 1995Assignee: Zambon Group S.p.A.Inventors: Giorgio Bertolini, Cesare Casagrande, Stefania Montanari, Gabriele Norcini, Francesco Santangelo
-
Patent number: 5319115Abstract: This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3.alpha.-hydroxy,3.beta.-substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereoselectively into a 3(R)-pregnan-3-spiro-2'oxirane-20-one intermediate. This intermediate can then be converted regioselectively by a second set of reactions to the 3.alpha.-hydroxy,3.beta.-substituted-20-one form, which can be further modified at the 20-keto position.Through this method, each ketone group is independently treated. By modifying the ketones one at a time, one can obtain the desired stereo-specificity at each site.Type: GrantFiled: March 4, 1992Date of Patent: June 7, 1994Assignee: Cocensys Inc.Inventors: Hasan Tahir, Michael Bolger, Richard Buswell, Richard Gabriel, Jay Stearns
-
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: 5182381Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity.Type: GrantFiled: September 10, 1991Date of Patent: January 26, 1993Assignee: Roussel UlcafInventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
-
Patent number: 5128464Abstract: 6,6-Ethylenedioxy-22R-hydroxy-2R,3S-isopropylidenedioxy-5.alpha.-cholest-23 -yne, useful as an intermediate for the synthesis of brassinolide.Type: GrantFiled: May 21, 1990Date of Patent: July 7, 1992Assignee: Fuji Yakuhin Kogyo Kabushiki KaishaInventors: Masakazu Aburatani, Tadashi Takeuchi, Kenji Mori
-
Patent number: 5084450Abstract: Compounds of the formula ##STR1## wherein .dbd.X is .dbd.O or ##STR2## R is hydrogen or acyl of an organic carboxylic acid of 1 to 12 carbon atoms, the wavy lines indicate the .alpha.- or .beta.-position, the dotted line in the 17-position indicates the bond is in the .alpha.-position and the dotted lines in the 9'(10') and 11'(12') positions indicate an optional double bond in the 9'(10') position or two optional double bonds in the 9'(10') and 11'(12') positions having progestomimetic and antiestrogenic activity.Type: GrantFiled: February 20, 1991Date of Patent: January 28, 1992Assignee: Roussel UclafInventors: Martine Gaillard-Kelly, Lucien Nedelec, Francois Nique, Daniel Philibert
-
Patent number: 5043332Abstract: 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 least 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: October 13, 1989Date of Patent: August 27, 1991Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
-
Patent number: 5001119Abstract: Compounds of the formula: ##STR1## are useful as anti-cancer, anti-obesity, anti-diabetic, anti-coronary agents, anti-aging agents, anti-hypolipidemic agents and anti-autoimmune agents.Type: GrantFiled: November 25, 1987Date of Patent: March 19, 1991Inventors: Arthur G. Schwartz, Marvin L. Lewbart
-
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: RE34136Abstract: 9 alpha, 11 beta and 11 beta-substituted estranes are disclosed which exhibit elevated estrogenic and postcoital contraceptive activities. A process for their manufacture and their use in pharmaceuticals is also disclosed.Type: GrantFiled: November 9, 1989Date of Patent: December 1, 1992Assignee: SRI InternationalInventors: David F. Crowe, Masato Tanabe, Richard Peters