Polycyclo-carbocyclic Ring System Patents (Class 546/128)
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Patent number: 8334303
    Abstract: 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: Grant
    Filed: February 28, 2006
    Date of Patent: December 18, 2012
    Assignee: Glazo Group Limited
    Inventors: Alan Collier, Michael Anthony Forth, Darren Hewitt, Paul Oxley
  • Patent number: 8110586
    Abstract: 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: Grant
    Filed: November 9, 2006
    Date of Patent: February 7, 2012
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Birgitte L. Eriksen, Elsebet Ostergaard Nielsen, John Paul Redrobe, Gunnar M. Olsen
  • Publication number: 20110112139
    Abstract: 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: Application
    Filed: January 14, 2011
    Publication date: May 12, 2011
    Inventors: Dan PETERS, Birgitte L. ERIKSEN, Elsebet Østergaard NIELSEN, Jergen SCHEEL-KRÜGER, Gunnar M. OLSEN
  • Publication number: 20100267764
    Abstract: 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: Application
    Filed: November 9, 2006
    Publication date: October 21, 2010
    Inventors: Dan Peters, Birgitte L. Eriksen, Elsebet Ostergaard Nielsen, John Paul Redrobe, Gunnar M. Olsen
  • Publication number: 20100184987
    Abstract: Provided are processes for preparation of Retapamulin via its pleuromutilin-thiol precursor.
    Type: Application
    Filed: November 12, 2009
    Publication date: July 22, 2010
    Inventors: Nimer Jaber, Lilach Hedvati, Eyal Gilboa, Sharon Avhar-Maydan
  • Publication number: 20090234125
    Abstract: 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: Application
    Filed: November 26, 2008
    Publication date: September 17, 2009
    Inventors: Eli Lancry, Lilach Hedvati, Greta Sterimbaum, Ariel Mittelman, Tali Katav
  • Publication number: 20090149655
    Abstract: 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: Application
    Filed: December 5, 2008
    Publication date: June 11, 2009
    Inventors: Lilach Hedvati, Eyal Gilboa, Sharon Avhar-Maydan, Sharona Shachan-Tov
  • Patent number: 7507745
    Abstract: 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: Grant
    Filed: January 18, 2005
    Date of Patent: March 24, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christopher John Montague Meade, Michel Pairet, Michael P. Pieper
  • Publication number: 20090076071
    Abstract: The present application describes deuterium-enriched retapamulin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 5, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 7429600
    Abstract: 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: Grant
    Filed: November 10, 2006
    Date of Patent: September 30, 2008
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhauser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Publication number: 20080161342
    Abstract: 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: Application
    Filed: February 28, 2006
    Publication date: July 3, 2008
    Inventors: Alan Collier, Michael Anthony Forth, Darren Hewitt, Paul Oxley
  • Patent number: 7214797
    Abstract: 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: Grant
    Filed: October 20, 2005
    Date of Patent: May 8, 2007
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhauser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Patent number: 6998406
    Abstract: 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: Grant
    Filed: August 9, 2004
    Date of Patent: February 14, 2006
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Patent number: 6815452
    Abstract: 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: Grant
    Filed: February 5, 2004
    Date of Patent: November 9, 2004
    Assignee: Boehringer Ingelheim Pharma KG & Co GmbH
    Inventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Patent number: 6790856
    Abstract: 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: Grant
    Filed: January 2, 2003
    Date of Patent: September 14, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Publication number: 20030236409
    Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.
    Type: Application
    Filed: May 29, 2003
    Publication date: December 25, 2003
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Rolf Banholzer, Gisela Bodenbach, Andreas Mathes, Helmut Meissner, Peter Specht
  • Publication number: 20030199539
    Abstract: Flourenecarboxylic acid esters of general formula 1 1
    Type: Application
    Filed: January 2, 2003
    Publication date: October 23, 2003
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Publication number: 20030105125
    Abstract: 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: Application
    Filed: December 27, 2001
    Publication date: June 5, 2003
    Inventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell
  • Publication number: 20030032645
    Abstract: The present invention includes compounds of formula I 1
    Type: Application
    Filed: May 20, 2002
    Publication date: February 13, 2003
    Applicant: Wyeth
    Inventor: Adam M. Gilbert
  • Patent number: 6482831
    Abstract: 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: Grant
    Filed: April 26, 2000
    Date of Patent: November 19, 2002
    Assignee: Entropin, Inc.
    Inventors: James E. Wynn, Lowell M. Somers
  • Patent number: 6228867
    Abstract: 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: Grant
    Filed: March 25, 1999
    Date of Patent: May 8, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla
  • Patent number: 6200957
    Abstract: 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: Grant
    Filed: July 14, 1998
    Date of Patent: March 13, 2001
    Assignee: 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
  • Patent number: 6077848
    Abstract: 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: Grant
    Filed: April 21, 1998
    Date of Patent: June 20, 2000
    Assignee: Entropin, Inc.
    Inventors: James E. Wynn, Lowell M. Somers
  • Patent number: 5780437
    Abstract: 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: Grant
    Filed: December 5, 1996
    Date of Patent: July 14, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Wallace T. Ashton, Lin Chu, Michael H. Fisher, Narindar N. Girotra, Peter Lin, Matthew J. Wyvratt
  • Patent number: 5763456
    Abstract: 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: Grant
    Filed: February 28, 1997
    Date of Patent: June 9, 1998
    Assignee: Entropin, Inc.
    Inventors: James E. Wynn, Lowell M. Somers
  • Patent number: 5643855
    Abstract: 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: Grant
    Filed: June 15, 1995
    Date of Patent: July 1, 1997
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: John Jolly Kilama
  • Patent number: 5583142
    Abstract: 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: Grant
    Filed: January 6, 1995
    Date of Patent: December 10, 1996
    Assignee: Fidia S.p.A.
    Inventors: Alessandro Bartolini, Carla Ghelardini, Alberto Giotti, Fulvio Gualtieri, Serena Scapecchi, Gino Toffano
  • Patent number: 5525613
    Abstract: 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: Grant
    Filed: June 16, 1994
    Date of Patent: June 11, 1996
    Assignee: Entropin, Inc.
    Inventors: James E. Wynn, Lowell M. Somers
  • Patent number: 5506359
    Abstract: 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: Grant
    Filed: August 24, 1993
    Date of Patent: April 9, 1996
    Assignee: President and Fellows of Harvard College
    Inventors: Bertha K. Madras, Peter Meltzer
  • Patent number: 5356905
    Abstract: 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: Grant
    Filed: July 23, 1992
    Date of Patent: October 18, 1994
    Assignee: Pfizer Inc.
    Inventor: Todd W. Butler
  • Patent number: 5011853
    Abstract: 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: Grant
    Filed: January 26, 1990
    Date of Patent: April 30, 1991
    Assignee: Washington University
    Inventor: John W. Olney
  • Patent number: 4803199
    Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: February 7, 1989
    Inventors: 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
  • Patent number: 4789673
    Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: December 6, 1988
    Inventors: Peter Donatsch, Gunter Engel, Bruno Hugi, Brian P. Richardson, Hildegard R. Stadler, Brigitte M. Stadler, Sigrid A. Stadler, Gerald Breuleux
  • Patent number: 4778793
    Abstract: 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: Grant
    Filed: July 18, 1986
    Date of Patent: October 18, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Ulrich Lerch, Joachim Kaiser
  • Patent number: 4322532
    Abstract: A method of catalytically converting acrylonitrile and water with a metallic conversion catalyst into pure acrylamide crystals.
    Type: Grant
    Filed: November 17, 1980
    Date of Patent: March 30, 1982
    Assignee: Nalco Chemical Company
    Inventor: David G. Braithwaite
  • Patent number: RE39128
    Abstract: 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: Grant
    Filed: October 27, 1998
    Date of Patent: June 13, 2006
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt
  • Patent number: RE43390
    Abstract: 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: Grant
    Filed: October 27, 1998
    Date of Patent: May 15, 2012
    Assignees: GlaxoSmithKline LLC, SmithKline Beecham Limited
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt