Polycyclo-carbocyclic Ring System Patents (Class 546/128)
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Patent number: 8828908Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.Type: GrantFiled: May 27, 2008Date of Patent: September 9, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
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Patent number: 8334303Abstract: Disclosed is a novel polymorphic form of the compound of formula (I) also known as mutilin 14-(exo-8-methyl-8-azabicyclo[3.2.1]oct-3-ylsulfanyl)-acetate, a process for the preparation of the polymorphic form, pharmaceutical compositions comprising the polymorphic form, and the use of the polymorphic form in medicine, particularly in antibacterial therapy.Type: GrantFiled: February 28, 2006Date of Patent: December 18, 2012Assignee: Glazo Group LimitedInventors: Alan Collier, Michael Anthony Forth, Darren Hewitt, Paul Oxley
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Patent number: 8110586Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: November 9, 2006Date of Patent: February 7, 2012Assignee: Neurosearch A/SInventors: Dan Peters, Birgitte L. Eriksen, Elsebet Ostergaard Nielsen, John Paul Redrobe, Gunnar M. Olsen
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Publication number: 20110112139Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: January 14, 2011Publication date: May 12, 2011Inventors: Dan PETERS, Birgitte L. ERIKSEN, Elsebet Østergaard NIELSEN, Jergen SCHEEL-KRÜGER, Gunnar M. OLSEN
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Publication number: 20100267764Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: November 9, 2006Publication date: October 21, 2010Inventors: Dan Peters, Birgitte L. Eriksen, Elsebet Ostergaard Nielsen, John Paul Redrobe, Gunnar M. Olsen
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Publication number: 20100184987Abstract: Provided are processes for preparation of Retapamulin via its pleuromutilin-thiol precursor.Type: ApplicationFiled: November 12, 2009Publication date: July 22, 2010Inventors: Nimer Jaber, Lilach Hedvati, Eyal Gilboa, Sharon Avhar-Maydan
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Publication number: 20090234125Abstract: An amorphous form of Retapamulin, preferably in powder form, and processes for preparation thereof, are provided. Amorphous Retapamulin of the present invention can contain less than about 10 percent crystallinity, preferably less than about 5 percent crystallinity. Pharmaceutical compositions comprising amorphous Retapamulin are also provided.Type: ApplicationFiled: November 26, 2008Publication date: September 17, 2009Inventors: Eli Lancry, Lilach Hedvati, Greta Sterimbaum, Ariel Mittelman, Tali Katav
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Publication number: 20090149655Abstract: Processes for preparing tropine derivatives of the following Formula B are provided where LG represents a leaving group. The tropine derivatives may be used to prepare Retapamulin, preferably in substantially pure form.Type: ApplicationFiled: December 5, 2008Publication date: June 11, 2009Inventors: Lilach Hedvati, Eyal Gilboa, Sharon Avhar-Maydan, Sharona Shachan-Tov
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Patent number: 7507745Abstract: The present invention relates to novel pharmaceutical compositions based on fluorene carboxylic acid ester derived anticholinergics of formula 1 and soluble TNF receptor fusion proteins, processes for preparing them and their use in the treatment of respiratory diseases.Type: GrantFiled: January 18, 2005Date of Patent: March 24, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Christopher John Montague Meade, Michel Pairet, Michael P. Pieper
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Publication number: 20090076071Abstract: The present application describes deuterium-enriched retapamulin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 5, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7429600Abstract: Fluorenecarboxylic acid esters of general formula 1 wherein X? and the groups A, R, R1, R2, R3, R3?, R4, and R4? have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.Type: GrantFiled: November 10, 2006Date of Patent: September 30, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhauser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
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Publication number: 20080161342Abstract: Disclosed is a novel polymorphic form of the compound of formula (I) also known as mutilin 14-(exo-8-methyl-8-azabicyclo [3.2.1]oct-3-ylsulfanyl)-acetate, a process for the preparation of the polymorphic form, pharmaceutical compositions comprising the polymorphic form, and the use of the polymorphic form in medicine, particularly in antibacterial therapy.Type: ApplicationFiled: February 28, 2006Publication date: July 3, 2008Inventors: Alan Collier, Michael Anthony Forth, Darren Hewitt, Paul Oxley
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Patent number: 7214797Abstract: Fluorenecarboxylic acid esters of general formula 1 wherein X? and the groups A, R, R1, R2, R3, R3?, R4, and R4? have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.Type: GrantFiled: October 20, 2005Date of Patent: May 8, 2007Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhauser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
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Patent number: 6998406Abstract: Fluorenecarboxylic acid esters of general formula 1 wherein X? and the groups A, R, R1, R2, R3, R3?, R4, and R4? have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.Type: GrantFiled: August 9, 2004Date of Patent: February 14, 2006Assignee: Boehringer Ingelheim Pharma KGInventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
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Patent number: 6815452Abstract: Fluorenecarboxylic acid esters of general formula 1 wherein X− and the groups A, R, R1, R2, R3, R3′, R4, and R4′ have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.Type: GrantFiled: February 5, 2004Date of Patent: November 9, 2004Assignee: Boehringer Ingelheim Pharma KG & Co GmbHInventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
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Patent number: 6790856Abstract: Flourenecarboxylic acid esters of general formula 1 wherein X− and the groups A, R, R1, R2, R3, R3′, R4, and R4′ have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.Type: GrantFiled: January 2, 2003Date of Patent: September 14, 2004Assignee: Boehringer Ingelheim Pharma KGInventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
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Publication number: 20030236409Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.Type: ApplicationFiled: May 29, 2003Publication date: December 25, 2003Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Rolf Banholzer, Gisela Bodenbach, Andreas Mathes, Helmut Meissner, Peter Specht
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Publication number: 20030199539Abstract: Flourenecarboxylic acid esters of general formula 1 1Type: ApplicationFiled: January 2, 2003Publication date: October 23, 2003Applicant: Boehringer Ingelheim Pharma KGInventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
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Publication number: 20030105125Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.Type: ApplicationFiled: December 27, 2001Publication date: June 5, 2003Inventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell
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Publication number: 20030032645Abstract: The present invention includes compounds of formula I 1Type: ApplicationFiled: May 20, 2002Publication date: February 13, 2003Applicant: WyethInventor: Adam M. Gilbert
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Patent number: 6482831Abstract: The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. Accordingly, this invention also relates to pharmaceutical compositions and methods for their use.Type: GrantFiled: April 26, 2000Date of Patent: November 19, 2002Assignee: Entropin, Inc.Inventors: James E. Wynn, Lowell M. Somers
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Patent number: 6228867Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: March 25, 1999Date of Patent: May 8, 2001Assignee: Merck & Co., Inc.Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla
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Patent number: 6200957Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: July 14, 1998Date of Patent: March 13, 2001Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Wallace T. Ashton, Lin Chu, Michael H. Fisher, Peter Lin, Mitree M. Ponpipom, Matthew J. Wyvratt, Narindar N. Girotra, Jonathan Young
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Patent number: 6077848Abstract: The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. Accordingly, this invention also relates to pharmaceutical compositions and methods for their use.Type: GrantFiled: April 21, 1998Date of Patent: June 20, 2000Assignee: Entropin, Inc.Inventors: James E. Wynn, Lowell M. Somers
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Patent number: 5780437Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: December 5, 1996Date of Patent: July 14, 1998Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Wallace T. Ashton, Lin Chu, Michael H. Fisher, Narindar N. Girotra, Peter Lin, Matthew J. Wyvratt
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Patent number: 5763456Abstract: The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. Accordingly, this invention also relates to pharmaceutical compositions and methods for their use.Type: GrantFiled: February 28, 1997Date of Patent: June 9, 1998Assignee: Entropin, Inc.Inventors: James E. Wynn, Lowell M. Somers
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Patent number: 5643855Abstract: Compounds such as Formula I having herbicidal utility are disclosed: ##STR1## wherein Q is ##STR2## R.sub.1 is H; alkyl, haloalkyl or halogen R.sup.2 is C.sub.1 -C.sub.2 alkyl optionally substituted with one or more halogens, OR.sup.8, CN, COR.sup.9, CO.sub.2 R.sup.31 or CONR.sup.32 R.sup.33 ; CN; CO.sub.2 R.sup.34 ; CONR.sup.35 R.sup.36 ; S(O).sub.n R.sup.8 ; S(O).sub.n NR.sup.19 R.sup.8 or COR.sup.37 ; orR.sup.1 and R.sup.2 can be taken together along with the carbon to which they are attached to form C.dbd.CHCO.sub.2 R.sup.31 ; C.dbd.(CH.sub.3)CO.sub.2 R.sup.31 ; C.dbd.(C.sub.2 H.sub.5)CO.sub.2 R.sup.31 ; C.dbd.CHCONR.sup.32 R.sup.33 ; C.dbd.C(CH.sub.3)CONR.sup.32 R.sup.33 or C.dbd.C(C.sub.2 H.sub.5)CONR.sup.32 R.sup.33.Type: GrantFiled: June 15, 1995Date of Patent: July 1, 1997Assignee: E. I. Du Pont de Nemours and CompanyInventor: John Jolly Kilama
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Patent number: 5583142Abstract: Compounds of general formula: ##STR1## where: Ar=phenyl or beta-naphtyl, or aromatic heterocyclic 6-membered ring containing one or two nitrogen atoms;R.sub.1 =one or more substituents of the Ar nucleus, preferably in para position, and selected out of the group consisting of H, CH.sub.3, CH.sub.2 --CH--(CH.sub.3).sub.2, O--CH.sub.3, Cl, F, Br, CF.sub.3, NH.sub.2, S--CH.sub.3, CN, NO.sub.2 R.sub.2 =H, CH.sub.3, C.sub.2 H.sub.5, CH(CH.sub.3).sub.2 ;R.sub.3 = ##STR2## Where R.sub.4 =H, CH.sub.3, C.sub.2 H.sub.5 R.sub.5 =H, CH.sub.3X=none O, S, NH, NCH.sub.3, --CH=CH--, --C.ident.C--Y=O, NH,both in the racemic Form and in the isomeric enantiomeric forms,which produce a nootropic effect, i.e. memory enhancement and learning facilitation, as well as an analgesic effect.Type: GrantFiled: January 6, 1995Date of Patent: December 10, 1996Assignee: Fidia S.p.A.Inventors: Alessandro Bartolini, Carla Ghelardini, Alberto Giotti, Fulvio Gualtieri, Serena Scapecchi, Gino Toffano
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Patent number: 5525613Abstract: The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. Accordingly, this invention also relates to pharmaceutical compositions and methods for their use.Type: GrantFiled: June 16, 1994Date of Patent: June 11, 1996Assignee: Entropin, Inc.Inventors: James E. Wynn, Lowell M. Somers
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Patent number: 5506359Abstract: Disclosed are benztropine and CFT analogs useful for imaging of cocaine receptors and treatment of cocaine abuse. Also disclosed are analogs useful for imaging and treatment of Parkinson's disease.Type: GrantFiled: August 24, 1993Date of Patent: April 9, 1996Assignee: President and Fellows of Harvard CollegeInventors: Bertha K. Madras, Peter Meltzer
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Patent number: 5356905Abstract: 3-Piperidino-1-chromanol derivatives and analogs having the formula ##STR1## wherein A and B are taken together and are --CH.sub.2 CH.sub.2 -- or A and B are taken separately and are each H;X is CH.sub.2 or O;X.sup.1 is H or OH;Z is H, F, Cl, Br or OH;Z.sup.1 is H, F, Cl, Br or (C.sub.1 -C.sub.3)alkyl;n is 0 or 1; andm is 0 or an integer from 1 to 6;pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.Type: GrantFiled: July 23, 1992Date of Patent: October 18, 1994Assignee: Pfizer Inc.Inventor: Todd W. Butler
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Patent number: 5011853Abstract: This invention discloses the use of muscarinic anti-cholinergic agents for reducing or preventing the toxic or lethal effects (such as seizures and brain damage) caused by cholinergic neurotoxins. The parent application disclosed that certain muscarinic anti-cholinergics classified as aryl-cycloalkyl-alkanolamines are effective in reducing or preventing the neurotoxicity of soman, a powerful nerve gas. This invention extends that discovery and identifies other muscarinic anti-cholinergic agents, including scopolamine, benactyzine, and benztropine, as highly effective and useful agents to protect against two major classes of cholinergic neurotoxins (acetylcholine receptor agonists, and cholinesterase inhibitors). Analogs of those compounds may also be effective in protecting against cholinergic neurotoxicity, as can be determined through routine screening tests using rats.Type: GrantFiled: January 26, 1990Date of Patent: April 30, 1991Assignee: Washington UniversityInventor: John W. Olney
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Patent number: 4803199Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.Type: GrantFiled: November 25, 1987Date of Patent: February 7, 1989Inventors: Peter Donatsch, Gunter Engel, Bruno Hugi, Brian P. Richardson, Paul A. Stadler, deceased, by Hildegard R. Stadler, heir, by Brigitte M. Stadler, heir, by Sigrid A. Stadler, heir, by Gerald Breuleux, legal representative
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Patent number: 4789673Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.Type: GrantFiled: November 10, 1987Date of Patent: December 6, 1988Inventors: Peter Donatsch, Gunter Engel, Bruno Hugi, Brian P. Richardson, Hildegard R. Stadler, Brigitte M. Stadler, Sigrid A. Stadler, Gerald Breuleux
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Patent number: 4778793Abstract: Compounds of the formula I ##STR1## where R(1), R(2), R(3), R(4) and R(5) are, inter alia, hydrogen and alkyl, m is 1-4, n is 0 or 1, p is 0-4 and R(6) is identical or different dialkylamine derivatives, and salts thereof, have a calcium-antagonistic action. They are obtained by reacting corresponding amines with a compound II which carries, on the side chain, a leaving group which can be displaced nucleophilically, or from a hydroxyphenyl-dihydroquinolin-2-one compound by reaction with a corresponding side chain compound which has a leaving group which can be displaced nucleophilically.Type: GrantFiled: July 18, 1986Date of Patent: October 18, 1988Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Ulrich Lerch, Joachim Kaiser
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Patent number: 4322532Abstract: A method of catalytically converting acrylonitrile and water with a metallic conversion catalyst into pure acrylamide crystals.Type: GrantFiled: November 17, 1980Date of Patent: March 30, 1982Assignee: Nalco Chemical CompanyInventor: David G. Braithwaite
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Patent number: RE39128Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.Type: GrantFiled: October 27, 1998Date of Patent: June 13, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt
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Patent number: RE43390Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.Type: GrantFiled: October 27, 1998Date of Patent: May 15, 2012Assignees: GlaxoSmithKline LLC, SmithKline Beecham LimitedInventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt