Two Of The Cyclos Share At Least Three Ring Members Or A Ring Carbon Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/581)
- Having -C(=X)-, wherein X is chalcogen, bonded directly to ring nitrogen of the bicyclo ring system (Class 540/583)
- Chalcogen or nitrogen attached directly to ring nitrogen of the bicyclo ring system by nonionic bonding (Class 540/584)
- Chalcogen or nitrogen attached indirectly to ring nitrogen of the bicyclo ring system by acyclic nonionic bonding (Class 540/585)
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Publication number: 20080200451Abstract: Compounds of the formula (I), in which W, R, R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: June 2, 2006Publication date: August 21, 2008Inventors: Kai Schiemann, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Dirk Finsinger, Christiane Amendt, Frank Zenke
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Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
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Patent number: 7285546Abstract: The present invention concerns a compound of formula (I) wherein: W represents O or NH, Q represents an unbranched or branched, saturated or unsaturated or aromatic, cyclic or acyclic or heterocyclic hydrocarbon radical containing 1 to 30 carbon atoms including or not heteroatom(s), R1 is H, OH, or R1, R2 form together —O—, R3?R4?OMe or R3 and R4 form together —OCH2O—, R is H, C1-C30alkyl or O-protecting group and R6 represents an unbranched or branched, saturated or unsaturated or aromatic, cyclic or acyclic or heterocyclic hydrocarboned radical containing 1 to 30 carbon atoms including or not heteroatom(s), or R and R6 form together —CMe2-, n is 0 to 8, R5 is H, OH, OMe, O—(C1-C30)-alkyl, O-aryl-(C1-C30)-alkyl, O—(C2-C30)-alkenyl, O—(C3-C30)-cycloalkyl or O-aryl, the dotted line is null or forms a double bond depending on the meaning of R1. It also concerns their methods of preparation and their use in treatment of cancers, leukemias, parasites and as reversal agents of harringtonines.Type: GrantFiled: April 1, 2003Date of Patent: October 23, 2007Assignee: Stragen Pharma S.A.Inventors: Jean-Pierre Robin, Robert Dhal, Freddy Drouye, Jean-Pierre Marie, Nina Radosevic, Julie Robin, Karine Souchaud, Patricia Bataille
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Patent number: 7241887Abstract: The subject invention relates to 3-azabicyclo[3.2.1]octane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by opioid receptors. The subject invention also particularly relates to using such derivatives to treat certain disorders and conditions, for example irritable bowel syndrome, drug addiction, depression, anxiety, schizophrenia and eating disorders, among others.Type: GrantFiled: April 14, 2004Date of Patent: July 10, 2007Assignee: Pfizer IncInventors: Jotham W. Coe, Stanton McHardy, Crystal G. Bashore
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Patent number: 7169774Abstract: The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and functionalization are entirely preformed. The invention also concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n=2 (i.e. harringtonine) or n=3 (i.e. homoharringtonine), in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97.5%.Type: GrantFiled: June 25, 2004Date of Patent: January 30, 2007Assignee: Stragen Pharma S.A.Inventors: Jean-Pierre Robin, Julie Blanchard, Ludovic Chauviat, Robert Dhal, Jean-Pierre Marie, Nina Radosevic
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Patent number: 7166588Abstract: New compounds of general formula IType: GrantFiled: May 22, 2001Date of Patent: January 23, 2007Assignee: Sanochemia Pharmazeutika AktiengesellschaftInventors: Ulrich Jordis, Johannes Frohlich, Matthias Treu, Manfred Hirnschall, Laszlo Czollner, Beate Kälz, Stefan Welzig
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Patent number: 6992078Abstract: The present invention provides plant extracts, isolated alkaloids, synthetic alkaloids and compositions having antitussive activity. In some preferred embodiments, the plant extracts and the isolated alkaloids are from a plant of a genus in the family Stemonaceae. In other preferred embodiments, the plant extracts and the isolated alkaloids are from a plant of the genus Stemona, Croomia, or Stichoneuron. In especially preferred embodiments, the plant extracts and the isolated alkaloids are from the plant Stemona tuberosa. The present invention further provides methods for isolating such plant extracts and alkaloids. In addition, the present invention provides methods for reducing or suppressing coughing by administering plant extracts, alkaloids and compositions having antitussive activity.Type: GrantFiled: April 24, 2002Date of Patent: January 31, 2006Assignee: The Chinese University of Hong KongInventors: Ge Lin, Hoi Sing Chung, Po Ming Hon, Hui Dong, Paul P. H. But
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Patent number: 6887868Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.Type: GrantFiled: September 19, 2002Date of Patent: May 3, 2005Assignee: Pharmacia & Upjohn CompanyInventor: Jian-Min Fu
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Patent number: 6797819Abstract: The present invention provides novel alkaloid compounds and collections of these compounds, and provides methods for the synthesis of these compounds using biomimetic synthetic strategies. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as bacterial infections, proliferative diseases, and reproductive disorders, to name a few.Type: GrantFiled: May 22, 2001Date of Patent: September 28, 2004Assignees: President and Fellows of Harvard College, CBR Institute for Biomedical Research, Inc.Inventors: Matthew Shair, Nicholas Westwood, Henry Efrem Pelish
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Publication number: 20030225268Abstract: Compounds of formula I: 1Type: ApplicationFiled: April 11, 2003Publication date: December 4, 2003Inventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
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Publication number: 20030207860Abstract: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: July 24, 2002Publication date: November 6, 2003Applicant: Schering CorporationInventors: Andrew W. Stamford, Ying Huang, Guoqing Li
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Patent number: 6617452Abstract: The subject matter of the present invention concerns a process for the isolation of the alkaloid galanthamine; the galanthamine itself which has been produced according to this process; the use of the galanthamine thus produced in galenic preparations; and the galanthamine thus produced for treating narrow-angle glaucoma, Alzheimer's disease, as well as alcohol and nicotine dependence.Type: GrantFiled: September 12, 2002Date of Patent: September 9, 2003Assignee: LTS Lohmann Therapie-Systeme AGInventors: Thomas Hille, Hans-Rainer Hoffmann, Mirko Kreh, Rudolf Matusch
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Patent number: 6579869Abstract: The present invention concerns a compound of formula (I) wherein: W represents O or NH, Q represents an unbranched or branched, saturated or unsaturated or aromatic, cyclic or acyclic or heterocyclic hydrocarbon radical containing 1 to 30 carbon atoms including or not heteroatom(s), R1 is H, OH, or OMe, O-(C1-C30)-alkyl, O-aryl-(C1-C30)-alkyl, O-(C2-C30)-alkenyl, O-(C3-C30)-cycloalkyl or null, and R2 is H or OH, or R1 and R2 form together —O—, R3=R4=OMe or R3 and R4 form together —OCH2O—, R is H, C1-C30 alkyl or O-protecting group and R6 represents an unbranched or branched, saturated or unsaturated or aromatic, cyclic or acyclic or heterocyclic hydrocarbon radical containing 1 to 30 carbon atoms including or not heteroatom(s), or R and R6 form together —CMe2—, n is 0 to 8, R5 is H, OH, OMe, O-(C1-C30)-alkyl, O-aryl-(C1-C30)-alkyl, O-(C2-C30)-alkenyl, O-(C3-C30)-cycloalkyl or O-aryl, the dotted line is null or forms a double bond depType: GrantFiled: November 14, 2000Date of Patent: June 17, 2003Assignee: Oncopharm CorporationInventors: Jean-Pierre Robin, Robert Dhal, Freddy Drouye, Jean-Pierre Marie, Nina Radosevic, Julie Robin, Karine Souchaud, Patricia Bataille
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Patent number: 6573376Abstract: The subject matter of the present invention concerns a process for the isolation of the alkaloid galanthamine; the galanthamine itself which has been produced according to this process; the use of the galanthamine thus produced in galenic preparations; and the galanthamine thus produced for treating narrow-angle glaucoma, Alzheimer's disease, as well as alcohol and nicotine dependence.Type: GrantFiled: November 9, 2001Date of Patent: June 3, 2003Assignee: LTS Lohmann Therapie-Systeme AGInventors: Thomas Hille, Hans-Rainer Hoffmann, Mirko Kreh, Rudolf Matusch
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Publication number: 20030055043Abstract: The invention provides compounds of Formula I: 1Type: ApplicationFiled: April 17, 2002Publication date: March 20, 2003Inventors: Eric Jon Jacobsen, Daniel Patrick Walker, Jason K. Myers, David W. Piotrowski, Vincent E. Groppi
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Patent number: 6468998Abstract: The present invention provides a pyrrolidine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof and a pharmaceutically acceptable salt thereof. The present invention further provides a pharmaceutical composition containing a compound of the formula (I), an optically active compound thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive. The compound of the present invention has a serotonin 2 receptor antagonistic action along with a platelet aggregation suppressive action, a peripheral circulation improving action and a lacrimation promoting action. Therefore, the compound of the present invention can be a useful medicine showing effect against thrombotic embolism, dry eye and the like.Type: GrantFiled: May 1, 2001Date of Patent: October 22, 2002Assignee: Mitsubishi Pharma CorporationInventors: Takanobu Kuroita, Masakazu Fujio, Haruto Nakagawa
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Patent number: 6423842Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: GrantFiled: October 5, 2001Date of Patent: July 23, 2002Assignee: UCB, S.A.Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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Patent number: 6417365Abstract: In a process for recovering medicinal substances or active substances from preparations, their initial products or waste, a flat-shaped starting material in the form of a film with adhesive and an active substance-containing material is provided with one edge length of from 0.1 to 5 cm and a second edge length of 50 cm. A starting material having an active substance is placed in an aqueous extraction liquor. The extraction liquor then takes effect until the active substance is dissolved in the aqueous extraction liquor forming an active substance-containing solution. The active substance is isolated from the active substance-containing solution be means of precipitation.Type: GrantFiled: June 26, 2000Date of Patent: July 9, 2002Assignee: LTS Lohmann Therapie-Systeme AGInventors: Hans-Werner Wolf, Thomas Hille
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Patent number: 6407229Abstract: The invention relates to processes for the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine, or derivatives thereof. Furthermore, the invention also relates to the compounds formed during the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine.Type: GrantFiled: April 23, 1999Date of Patent: June 18, 2002Assignee: Sanochemia Pharmazeutika AGInventors: Laszlo Czollner, Johannes Fröhlich, Ulrich Jordis, Bernhard Küenburg
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Patent number: 6392038Abstract: A process for the preparation of substantially single enantiomer (−)-narwedine comprises seeding a solution of racemic narwedine dissolved in a solvent with substantially single enantiomer (−)-narwedine, provided that if an added amine base is present the ratic solvent:added amine base is greater than 15:1.Type: GrantFiled: January 10, 2000Date of Patent: May 21, 2002Assignee: Janssen Pharmaceutica, N.V.Inventors: Gerard Andrew Potter, Peter David Tiffin
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Patent number: 6387512Abstract: A photochromic grey coloring 2H-naphtho[1,2-b]pyran of formula (1) wherein R1 is selected from mono-, di- or poly-substituted aryl groups, mono-, di- or poly-substituted naphthyl groups and mono-, di- or poly-substituted heteroaryl groups, wherein at least one substituent is a nitrogen containing group, including amino, C1-C20 and C6-C20 alkylamino, C1-C20 and C6-C20 dialkylamino, C2-C20 dialkenylamino, C2-C20 or C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, tetra (C1-C10 linear or branched alkyl) guanidino and cyclic-amino groups and at least one of R7 and R9, which may be the same or different, is selected from C1-C20 N alkylamino C1-C20 N-alkylamido, C1-C20 N,N-dialkylamido, amido, nitro, amino, C1-C20 alkylamino, C1-C20 dialkylamino, C2-C20 dialkenylamino, C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, or cyclicamino groups.Type: GrantFiled: March 16, 2001Date of Patent: May 14, 2002Assignee: James Robinson LimitedInventors: David Allan Clarke, Bernard Mark Heron, Christopher David Gabbutt, John David Hepworth, Steven Michael Partington, Stephen Nigel Corns
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Publication number: 20020045617Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: ApplicationFiled: October 5, 2001Publication date: April 18, 2002Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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Patent number: 6346618Abstract: A process for the asymmetric transformation of a racemic compound of formula (I) wherein R1 is H or a alkyl group having up to 20 carbon atoms, R2 is H, or an alkyl, aryl, alkaryl or aralkyl group having up to 20 carbon atoms, and X is H, a halogen atom, tert-butyl, or any other removable substituent, comprises reaction of racemic compound (I) with an enantiomerically-enriched acid HY*, wherein Y* is a chiral group, to form a diastereomeric salt of compound (I) having Y* as a counterion. The salt obtained can then be reduced to give enantiomerically-enriched galanthamine, or a derivative thereof.Type: GrantFiled: June 28, 1999Date of Patent: February 12, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: David Andrew Chaplin, Nicholas Bernard Johnson, Gerard Andrew Potter, Jane Marie Paul
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Publication number: 20020013309Abstract: The present invention relates to diazabicyclic compounds, preferably to N-aryl diazabicyclic compounds. Of particular interest are 2-pyridyl diazabicyclic compounds, such as (1S,4S)-2-(5-(3-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. Other exemplary compounds of the present invention include: (1S,4S)-2-(5-(4-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1 ]heptane, (1S,4S)-2-(5-(3,4-dimethoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-(4-fluorophenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1 ]heptane, and (1S,4S)-2-(5-benzoyl-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. The present invention also relates to prodrug derivatives of the compounds of the present invention.Type: ApplicationFiled: May 24, 2001Publication date: January 31, 2002Inventors: Craig Harrison Miller, Gary Maurice Dull, Lan Miao, Dwo Lynm, Jeffrey Daniel Schmitt, Thomas Jeffrey Clark
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Patent number: 6323195Abstract: This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12alkylcarbonyl, (C1-C12)alkoxycarbonyl, mono(C1-C12)alkylaminocarbonyl, or di(C1-C12)alkylaminocarbonyl; R2 is hydrogen, (C3-C12)alkenylcarbonyloxy, (C3-C12)cycloalkylcarbonyloxy, (C3-C12)cycloalkyl(C1-C12)alkylcarbonyloxy, oxygen containing heterocycloxy, oxygen containing heterocyclylcarbonyloxy, sulfur containing heterocyclyloxy, sulfur containing heterocyclylcarbonyloxy, nitrogen containing hetercyclyloxy, nitrogen containing heterocyclylcarbonyloxy, haloalkylsulfonyloxy, (C1-C6)alkylsilyloxy; R3 is hydrogen, halo or (C1-C4)alkyl; R4 is hydrogen or (C1-C6)alkyl; with the proviso that R1 and R2 are not both hydrogen when R3 and R4 are hydrogen; all geometric, and optical stereoisomers thereof, or a pharmaceutically acceptable addition salt thereof; which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing tType: GrantFiled: October 15, 1993Date of Patent: November 27, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
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Patent number: 6323196Abstract: This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12)alkylcarbonyl, (C1-C12)alkoxycarbonyl, mono(C1-C12)alkylaminocarbonyl, or di(C1-C12)alkylaminocarbonyl; R2 is mono(C1-C18)alkylaminocarbonyloxy, di(C1-C8)alkylaminocarbonyloxy, or aryl(C1-C4)alkylaminocarbonyloxy; R3 is hydrogen or halo; or a pharmaceutically acceptable acid addition salt thereof, which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.Type: GrantFiled: October 15, 1993Date of Patent: November 27, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
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Patent number: 6323194Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: GrantFiled: October 17, 2000Date of Patent: November 27, 2001Assignee: UCB, S.A.Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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Patent number: 6319919Abstract: Compounds of the formula wherein the broken line represents an optionally present double bond, and R1-R3, R4, R6 and R9 are as defined herein, and compositions containing these compounds can be used to inhibit acetylcholinesterase activity and treat Alzheimer's Disease.Type: GrantFiled: June 7, 1995Date of Patent: November 20, 2001Inventors: Bonnie Davis, Madeleine M. Joullie
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Patent number: 6316439Abstract: This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12)alkylcarbonyl, (C1-C12)alkoxycarbonyl, aryl(C1-C12)alkylaminocarbonyl, mono(C1-C18)alkylaminocarbonyl or di(C1-C8)alkylaminocarbonyl; R2 is (C1-C12)alkylcarbonyloxy, aryl(C1-C4)alkylcarbonyloxy, (C1-C12)alkoxycarbonyloxy, arylcarbonyloxy, hydroxy, (C1-C6)alkoxycarbonyl(C1-C6)alkoxy or hydroxy(C1-C10)alkoxy; R3 is hydrogen or halo; and pharmaceutically acceptable addition salts; with the proviso that when R2 is hydroxy, R1 and R3 are not both hydrogen or when R2 is hydroxy and R3 is hydrogen, R1 is not methylcarbonyl; which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.Type: GrantFiled: October 15, 1993Date of Patent: November 13, 2001Assignee: Aventis Pharamaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
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Patent number: 6184004Abstract: The subject invention pertains to a process for preparing a compound having a formula (4) or (5), in either optically-enriched or racemic form, wherein R1, R2, R3 and R4 are independently selected from hydrogen, alkyl, aryl, alkaryl, aralkyl and acyl groups. In one embodiment, the process of the invention comprises mixing with a plant extract obtained from crushed daffodil bulbs or crushed snowdrop bulbs an oxidative cyclisation precursor of the compound.Type: GrantFiled: May 26, 1998Date of Patent: February 6, 2001Assignee: Janssen Pharmaceutica, N.V.Inventors: Robin Mark Bannister, Raymond McCague
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Patent number: 6150354Abstract: A method of treating Alzheimer's disease and related dementias by treatment with analogs of galanthamine, particularly those wherein the methoxy and hydroxy substituents are replaced by, for example carbamate groups, the methoxy is replaced by hydroxy and esters of galanthamine and O-desmethyl galanthamine. Many of the useful compounds are novel.Type: GrantFiled: October 19, 1993Date of Patent: November 21, 2000Assignee: Bonnie DavisInventors: Bonnie Davis, Madeleine M. Joullie
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Patent number: 6136968Abstract: Described are novel reversible photochromic compounds of the homoazaadamantane spirooxazine family. Certain substituents are present on the nitrogen atom of the homoazaadamantane portion of the compound and on the benzene ring fused to the oxazine portion of the compound. These compounds may be represented by the following formula: Also described are compositions, e.g., solvent based mediums and polymerized organic materials, used to produce ophthalmic components, that contain the homoazaadamantane compounds with or without other photochromic compounds.Type: GrantFiled: January 29, 1999Date of Patent: October 24, 2000Assignee: Transitions Optical Inc.Inventors: Karine Chamontin, Vladimir Lokshin, Andre Samat, Robert Guglielmetti
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Patent number: 6093815Abstract: A process for preparing a compound having formula (11), comprises oxidative cyclization of a tertiary amine having formula (12), wherein X.sup.1 is a removable functionality, X.sup.2 is hydrogen or a group as defined above for X.sup.1, and R.sup.1 is selected from hydrogen and alkyl, aryl, alkaryl and aralkyl groups having up to 20 carbon atoms, and R.sup.2 and R.sup.3 are independently selected from hydrogen and alkyl, aryl, alkaryl, aralkyl and acyl groups having up to 20 carbon atoms. Novel compounds are both used and produced by that process.Type: GrantFiled: August 20, 1998Date of Patent: July 25, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: David Andrew Chaplin, Neil Fraser, Peter David Tiffin
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Patent number: 6087495Abstract: The subject invention concerns a process for the preparation of enantiomerically-enriched galanthamine from racemic galanthamine, and a process for increasing the enantiomeric excess of enantiomerically-enriched galanthamine, by direct crystallization of galanthamine salts.Type: GrantFiled: July 2, 1998Date of Patent: July 11, 2000Assignee: Janssen Pharmaceutica, N.V.Inventor: Peter David Tiffin
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Patent number: 6043359Abstract: The invention relates to processes for the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine, or derivatives thereof. Furthermore, the invention also relates to the compounds formed during the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine.Type: GrantFiled: April 18, 1997Date of Patent: March 28, 2000Assignee: Sanochemia Pharmazeutica AktiengesellschaftInventors: Laszlo Czollner, Johannes Frohlich, Ulrich Jordis, Bernhard Kuenburg
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Patent number: 6017910Abstract: The invention relates to 5-(iminomethano)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene and derivatives thereof. The invention also relates to the use of such compounds for the treatment or prevention of neuronal loss in ischemia, hypoxia, brain or spinal chord trauma, as well as for the treatment of Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome.Type: GrantFiled: May 26, 1995Date of Patent: January 25, 2000Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education acting for and on behalf of the Oregon Health Sciences University and the University of OregonInventors: Eckard Weber, John F. W. Keana, Peter Barmettler
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Patent number: 5990104Abstract: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.Type: GrantFiled: March 25, 1998Date of Patent: November 23, 1999Assignee: Biochem Pharma, Inc.Inventors: John Dimaio, Dilip M. Dixit
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Patent number: 5958903Abstract: Novel galanthamine derivatives of general fonnulae (Ia) and (Ib), a method for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as cholinesterase inhibitors, are disclosed.Type: GrantFiled: January 9, 1998Date of Patent: September 28, 1999Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S.)Inventors: Dolor Renko, Pierre Potier, Yves Christen, Claude Thal, Catherine Guillou, Aude Mary
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Patent number: 5912343Abstract: A compound comprising at least one cyclic amine, having an organolithium side-chain, defined according to formula (I) ##STR1## wherein Z is a lithium atom (Li); R.sub.1 is selected from the group consisting of organic groups containing from 1 to about 12 carbon atoms and a bridging bond; each R.sub.2 is independently selected from the group consisting of hydrogen, organic groups containing from 1 to about 12 carbon atoms, and a bridging bond; each R.sub.3 is independently selected from the group consisting of hydrogen and organic groups containing from 1 to about 12 carbon atoms; a is an integer from 4 to about 16; and b is an integer from 0 to about 12; and optionally including a bridge, formed by the selection of two of said bridging bonds, the bridge having 0 to about 6 carbon atoms between the bridging ring members.Type: GrantFiled: December 31, 1996Date of Patent: June 15, 1999Assignee: Bridgestone CorporationInventors: David F. Lawson, William L. Hergenrother, Michael L. Kerns
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Patent number: 5869652Abstract: In a process for reprocessing devices for the transdermal application of active substances or their process waste, active substance-containing components are brought into solution and the active substances are recovered therefrom.Type: GrantFiled: January 2, 1998Date of Patent: February 9, 1999Assignee: LTS Lohmann Therapie-Systeme GmbHInventors: Bodo Asmussen, Hans-Rainer Hoffmann, Walter Muller
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Patent number: 5688789Abstract: The invention relates to 5-(iminomethano)-10,11-dihydro-5H-dibenzo?a,d!cycloheptene and derivatives thereof. The invention also relates to the use of such compounds for the treatment or prevention of neuronal loss in ischemia, hypoxia, brain or spinal chord trauma, as well as for the treatment of Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome.Type: GrantFiled: May 26, 1995Date of Patent: November 18, 1997Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of OregonInventors: Eckard Weber, John F. W. Keana, Peter Barmettler
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Patent number: 5599810Abstract: Alpha-adrenergic receptor antagonsists having the formula (I) as set forth below which are useful to produce alpha-adrenergic antagonism, pharmaceutical compositions thereof, and methods of treatment therewith are disclosed: ##STR1## The variables X, R, Y, Het and A are as defined in the specification.Type: GrantFiled: October 20, 1995Date of Patent: February 4, 1997Assignee: SmithKline Beecham CorporationInventors: William E. Bondinell, Robert M. Demarinis, Thomas W. Ku, Francis R. Pfeiffer, Dinubhai H. Shah, Joseph W. Venslavsky
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Patent number: 5534633Abstract: Aminoketone-substituted coumarin sensitizers having tethered tertiary amino groups are described which have extremely good photosensitivity. The sensitizers of the instant invention have the formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent an alkyl group having 1 to 6 carbon atoms, and R.sub.3 and R.sub.4 each represent hydrogen; or at least one of R.sub.1 and R.sub.3 or R.sub.2 and R.sub.4 together represent an alkylene group having 2 to 4 carbon atoms,R.sub.5 represents an alkyl group having 1 to 6 carbon atoms or H,R.sub.6 represents an alkylene group having 1 to 6 carbon atoms, andR.sub.7 and R.sub.8 each independently represent an alkyl group having 1 to 6 carbon atoms, both of R.sub.7 and R.sub.8 taken together represent an alkylene group having 4 to 6 carbon atoms, or R.sub.5 or R.sub.6 taken together with R.sub.7 or R.sub.8 represent a five, six, or seven membered heterocyclic ring group.Type: GrantFiled: February 3, 1995Date of Patent: July 9, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: M. Zaki Ali
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Patent number: 5508401Abstract: This invention involves novel neuroprotectant agents of the formula: ##STR1## in which R.sup.1 and R.sup.3 are, independently, hydrogen, cyano, nitro, halo or perhaloalkyl, with the proviso that one of R.sup.1 and R.sup.3 is other than hydrogen; R.sub.2 is alkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 20, 1991Date of Patent: April 16, 1996Assignee: American Home Products CorporationInventors: Wayne E. Childers, Jr., Magid A. Abou-Gharbia, Edward J. Podlesny
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Patent number: 5488046Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: November 3, 1993Date of Patent: January 30, 1996Assignee: G. D. Searle & Co.Inventors: Robert A. Chrusciel, Timothy J. Hagen, E. Ann Hallinan, Jinglin Li, Sofya Tsymbalov, David B. Reitz
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Patent number: 5428159Abstract: (-)-Galanthamine is obtained in substantially high yield and purity substantially without concomitant production of epigalanthamine by conversion of racemic narwedine to (-)-narwedine and subsequent reduction to (-)-galanthamine using bulky organo-aluminum or organo-boron reducing agents.Type: GrantFiled: April 8, 1994Date of Patent: June 27, 1995Assignee: Ciba-Geigy CorporationInventors: Wen-Chung Shieh, John A. Carlson
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Patent number: 5399562Abstract: This invention relates to compounds of the formula: ##STR1## which are useful as 5-HT.sub.4 agonists or antagonists and 5-HT.sub.3 antagonists.Type: GrantFiled: February 4, 1994Date of Patent: March 21, 1995Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Clara I. Villamil
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Patent number: 5374722Abstract: The compound ##STR1## is useful as an agent in the treatment of psychoses and drug dependence and for providing an analgesic effect.Type: GrantFiled: March 16, 1993Date of Patent: December 20, 1994Assignee: Schering CorporationInventors: Joel G. Berger, Wei K. Chang, John W. Clader
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Patent number: 5334591Abstract: Conformationally constrained tricyclic thienothiopyran compounds are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.Type: GrantFiled: March 4, 1993Date of Patent: August 2, 1994Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Kenneth L. Shepard, Gerald S. Ponticello, Theresa M. Williams
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Patent number: RE35218Abstract: An azatetracycle compound useful as 5HT.sub.3 antagonists of the general formula ##STR1## wherein D is a tetracycle of the structure ##STR2## wherein Ar is an aromatic moiety and B is either NH or O.Type: GrantFiled: August 18, 1994Date of Patent: April 23, 1996Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Roger Nosal, Dale P. Spangler, Daniel L. Zabrowski