Quinuclidines (including Unsaturated) Patents (Class 546/133)
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Publication number: 20080171748Abstract: Substituted piperidines of formulae (I) and (II) with the substituent definitions as explained in the specification. The compounds are suitable in particular as renin inhibitors and are highly potent.Type: ApplicationFiled: March 14, 2008Publication date: July 17, 2008Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Christiane Marti, Stefan Stutz, Stjepan Jelakovic, Zenon D. Konteatis, Jennifer L. Ludington, Michael Quirmbach, Aleksandar Stojanovic, Dirk Behnke, Frank Hollinger
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Publication number: 20080161343Abstract: A series of N-substituted 9-azabicyclo[3.3.1]nonan-3?-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (?1 and ?2) receptors are described. Two new compounds, N-(9-(4-aminobutyl)-9-azabicyclo[3.3.1]nonan-3?-yl)-N?-(2-methoxy-5-methylphenyl)carbamate and N-(9-(6-aminohexyl)-9-azabicyclo[3.3.1]nonan-3?-yl)-N?-(2-methoxy-5-methylphenyl)carbamate, are shown to have a high affinity and selectivity for ?2 versus ?1 receptors. Among the disclosed compounds are biotinylated and fluorescent analogs. These compounds can serve as probes to the ?2 receptor. In addition, some disclosed compounds can induce apoptotic cell death by both caspase-dependent and caspase-independent mechanisms, and are effective for treatment of tumors. The compounds can be used as chemotherapeutics or chemosensitizers in the treatment of a wide variety of solid tumors.Type: ApplicationFiled: July 11, 2007Publication date: July 3, 2008Inventors: Robert H. Mach, Zhude Tu, Wenhua Chu, Suwanna Vangveravong, Richard Hotchkiss, William Hawkins, Rebecca Aft
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Publication number: 20080154037Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: February 15, 2008Publication date: June 26, 2008Inventors: Wenge Xie, Brian Herbert, Truc Nguyen, Carla Gauss, Ashok Tehim
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Publication number: 20080132704Abstract: This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: December 20, 2007Publication date: June 5, 2008Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Philip K. Ahring, Tino Dyhring Jorgensen
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Publication number: 20080114028Abstract: Polymorphic forms of solifenacin have been prepared and characterized. These polymorphic forms are particularly useful in pharmaceutical compositions.Type: ApplicationFiled: July 24, 2007Publication date: May 15, 2008Inventors: Tamas Koltai, Tamar Nidam, Eyal Gilboa, Nurit Perlman, Michael Pinhasov, Mili Abramov
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Publication number: 20080103170Abstract: Acetylcholine receptor ligands of formula I wherein D, E and G are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing, and methods for using the same.Type: ApplicationFiled: December 14, 2005Publication date: May 1, 2008Applicant: AstraZeneca ABInventors: Robert Jacobs, Richard J. Schmiesing
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Patent number: 7361668Abstract: The invention concerns quinuclidine derivatives of formula I or II wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention show high affinities for m3 and/or m2 muscarinic receptors and are particularly suited for treating urinary incontinence.Type: GrantFiled: September 23, 2002Date of Patent: April 22, 2008Assignee: UCB, S.A.Inventors: Michel Guyaux, Chimmanamada U. Dinesh, Charles Mioskowski, Luc Quere, Jean-Philippe Starck, Patrice Talaga, Alain Wagner, Matteo Zanda
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Patent number: 7358359Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: July 22, 2005Date of Patent: April 15, 2008Assignee: University of WashingtonInventors: Niels H. Andersen, Jason Bowman
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Patent number: 7354930Abstract: The invention relates to N-biarylamides useful for the prophylaxis and/or treatment of impairments of perception, concentration, learning and/or memory, and to processes for preparing them, and pharmaceutical compositions containing them.Type: GrantFiled: July 19, 2004Date of Patent: April 8, 2008Assignee: Bayer HealthCare AGInventors: Timo Fleβner, Frank-Gerhard Böβ, Frank-Thorsten Hafner, Joachim Luithle, Christoph Methfessel, Leila Telan
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Patent number: 7332507Abstract: This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: May 27, 2003Date of Patent: February 19, 2008Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Philip K. Ahring, Tino Dyhring Jørgensen
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Patent number: 7309699Abstract: Compounds of formula (I) wherein A is N or N+—O?; n is 0, 1, or 2; Y is O, S, —NH—, and —N-alkyl-; Ar1 is both 6-membered aromatic rings; Ar2 is 5- or 6-membered aromatic rings with a —NR8R9 group, as defined herein. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: December 17, 2004Date of Patent: December 18, 2007Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li, Ying Wang
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Patent number: 7288656Abstract: The invention relates to a compound having general formula (I): Wherein R, R1, R2, X and n are as described herein. Also disclosed and claimed in certain of the embodiments herein are the methods of preparation of compound of formula (I) and its use in therapeutics.Type: GrantFiled: April 14, 2006Date of Patent: October 30, 2007Assignee: Sanofi-AventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Pascale Magat, Benoit Marabout, Pierre Roger
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Patent number: 7282588Abstract: The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a number of diseases, including solid tumor cancers and hematological cancers.Type: GrantFiled: December 19, 2006Date of Patent: October 16, 2007Assignee: SmithKline BeechamInventors: Dashyant Dhanak, Kenneth Allen Newlander
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Patent number: 7256288Abstract: The invention relates to novel heteroaryl carboxamides, a process for their preparation, and pharmaceutical compositions containing them. These materials are useful for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.Type: GrantFiled: November 6, 2002Date of Patent: August 14, 2007Assignee: Bayer HealthCare AGInventors: Martin Hendrix, Frank-Gerhard Böss, Christina Erb, Joachim Krüger, Joachim Luithle, Christoph Methfessel, Rudy Schreiber, Welf-Burkhard Wiese
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Patent number: 7247728Abstract: This application relates to bicyclic N-aryl amides of the formula R1 is a 1-aza-bicyclo[3.2.1]octyl group, a 1-aza-bicyclo[2.2.2]oct-3-yl; R2 is an optionally sustituted 8- to 10- membered heteroaryl, naphthyl, or azulenyl group; and R3 is H or (C1C6)alkyl; or a salt, solvate, or solvate of a salt of these compounds. A process for preparing these compounds, medicaments containing them, and methods for using them in treatment are also disclosed and claimed.Type: GrantFiled: December 6, 2002Date of Patent: July 24, 2007Assignee: Bayer Healthcare AGInventors: Joachim Luithle, Frank-Gerhard Böss, Christina Erb, Timo Flessner, Martin Hendrix, Marja van Kampen, Christoph Methfessel
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Patent number: 7241773Abstract: Compounds of formula: or pharmaceutically acceptable salts, esters, amides, or prodrugs thereof, wherein: A and G are each independently N or N+—O?; m and n are each independently 0, 1, or 2; X1 and X3 are each independently O, S, and —N(R1)—; X2 is O, S, —N(R1)—, —N(Ar2)—and —N(R2)C(O)—; Ar1 is a six-membered aromatic ring; Ar2 is cyclohexyl or a mono- or bicyclic aromatic ring, and R13 is hydrogen, alkyl, or halogen, as defined herein. The compounds are useful in treating conditions or disorders prevented by or ameliorated by nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formulas (I) and (II) and methods for using such compounds and compositions.Type: GrantFiled: December 17, 2004Date of Patent: July 10, 2007Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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Patent number: 7241787Abstract: The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments. Compounds of the formula I, in which the radicals have the stated meanings, and the physiologically tolerated salts thereof, and process for their preparation are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.Type: GrantFiled: January 25, 2005Date of Patent: July 10, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Thomas Boehme, Matthias Gossel, Siegfried Stengelin
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Patent number: 7214686Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a 1-aza-2-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-2-(3-pyridyl)bicyclo[2.2.2]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.1]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.2]nonane, a 1-aza-7-(3-pyridyl) bicyclo[2.2.1]heptane, a 1-aza-3-(3-pyridyl)bicyclo[3.2.2]nonane, or a 1-aza-7-(3-pyridyl)bicyclo[3.2.2]nonane. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.Type: GrantFiled: June 4, 2003Date of Patent: May 8, 2007Assignee: Targacept, Inc.Inventors: Merouane Bencherif, Craig Harrison Miller, Gregory D. Hawkins, Balwinder S. Bhatti
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Patent number: 7214688Abstract: Compounds of formula I: wherein A, D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.Type: GrantFiled: January 5, 2006Date of Patent: May 8, 2007Assignee: AstraZeneca ABInventors: Eifion Phillips, Richard Schmiesing
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Patent number: 7176236Abstract: Etoposide analogs with improved water-solubility such as 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.Type: GrantFiled: November 13, 2003Date of Patent: February 13, 2007Assignee: University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
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Patent number: 7160876Abstract: Compounds of formula (I) wherein n is 0, 1, or 2; X is O, S, —NH—, and —N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: December 22, 2003Date of Patent: January 9, 2007Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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Patent number: 7138410Abstract: The invention relates to novel 1-aza-bicyclic N-biarylamides, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning ability and memory.Type: GrantFiled: March 3, 2003Date of Patent: November 21, 2006Assignee: Bayer HealthCare AGInventors: Joachim Luithle, Frank-Gerhard Böss, Christina Erb, Katrin Schnizler, Timo Flessner, Marja van Kampen, Christoph Methfessel, Frank-Thorsten Hafner
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Patent number: 7122558Abstract: A compound of formula (I), wherein B is a phenyl ring, a 5 to 10 membered heteroaromatic group containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl, benzo[1,3]dioxolyl, or biphenyl group; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, a phenyl group, —OR7, —SR7, —NR7R8, —NHCOR7, —CONR7R8, —CN, —NO2, —COOR7 or CF3 group, or a strait or branched, substituted or unsubstituted lower alkyl group, wherein R7 and R8 each independently represent a hydrogen atom, a straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic or alicyclic ring or a heterocyclic group.Type: GrantFiled: December 20, 2001Date of Patent: October 17, 2006Assignee: Almirall Prodesfarma AGInventors: Maria Prat Quinones, Maria Dolors Fernandez Forner, Maria Antonia Buil Albero
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Patent number: 7115768Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: September 16, 2002Date of Patent: October 3, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Francine S. Grant, Bradley S. Johnson, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 7115629Abstract: The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C1–C4)-alkylthio, (C1–C4)-alkoxyl, (C1–C4)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C1–C4)alkyl and (C1–C4)alkyl substituted by one or several F or OH radicals; R4 represents a substituted or non-substituted cycloalkyl or cycloaryl radical (a heteroalkyl radical or not). The amine of the quinuclidine ring can also be forming quaternary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M3 muscarinic receptor, and selectively, the M2 receptor. Hence, they can be used in the treatment of urinary incontinence (particularly due to bladder instability), irritable bowel syndrome, diseases of the respiratory tract (particularly chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema and rhinitis) and in ophthalmologic operations.Type: GrantFiled: June 23, 2004Date of Patent: October 3, 2006Assignee: Laboratorios S.A.L.V.A.T., S.A.Inventors: Carles Farrerons Gallemi, Juan Lorenzo Catena Ruiz, Anna Fernandez Serrat, Ignacio José Miquel Bono, Dolors Balsa Lopez, José Ignacio Bonilla Navarro, Carmen Lagunas Arnal, Carolina Salcedo Roca, Andrés Fernandez Garcia
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Patent number: 7112593Abstract: An excellent squalene synthase inhibitor is provided. Specifically, what is provided is a compound (I) represented by the following formula, a salt thereof or a hydrate of them. In formula (I), R1 represents an optionally substituted vinyl group or an aromatic ring which may be substituted. Also, n is an integer of 0 to 2. Further, X, Y and Z are the same as or different from each other and each represents an optionally substituted carbon atom, or an optionally substituted nitrogen atom, sulfur atom or oxygen atom, and Y optionally represents a single bond, and when Y represents the single bond, the ring to which X, Y and Z belong is a 5-membered ring. Also in the formula, CyA represents a 5- to 14 membered non-aromatic cyclic amino group or non-aromatic cyclic amido group which may be substituted, and the non-aromatic cyclic amino group or the non-aromatic cyclic amido group optionally having an oxygen atom or a sulfur atom.Type: GrantFiled: March 27, 2002Date of Patent: September 26, 2006Assignee: Eisai Co., Ltd.Inventors: Toshimi Okada, Nobuyuki Kurusu, Keigo Tanaka, Seiji Yoshikawa, Daisuke Shinmyo, Nobuhisa Watanabe, Hironori Ikuta, Hironobu Hiyoshi, Takao Saeki, Mamoru Yanagimachi, Masashi Ito
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Patent number: 7112592Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.Type: GrantFiled: July 24, 2001Date of Patent: September 26, 2006Assignee: Aventis Pharma S.A.Inventors: Maxime Lampilas, Jozsef Aszodi, David Alan Rowlands, Claude Fromentin
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Patent number: 7101896Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodrug derivatives of the compounds of the present invention.Type: GrantFiled: January 20, 2005Date of Patent: September 5, 2006Assignee: Targacept, Inc.Inventors: Gary Maurice Dull, Jeffrey Daniel Schmitt, Balwinder Singh Bhatti, Craig Harrison Miller
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Patent number: 7087750Abstract: The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.Type: GrantFiled: October 22, 2001Date of Patent: August 8, 2006Assignee: Biovitrum ABInventors: Patrizia Caldirola, Björn M. Nilsson, Gary Johansson
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Patent number: 7078412Abstract: The invention provides 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2] octane in salt form, pharmaceutical compositions comprising it, and methods of using it for treatment of respiratory disorders, alone or in combination with other bronchodilatory compounds.Type: GrantFiled: April 28, 2005Date of Patent: July 18, 2006Assignee: Almirall Prodesfarma AGInventors: Maria Dolors Fernandez Forner, Maria Prat Quiñones, Maria Antonia Buil Albero
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Patent number: 7067515Abstract: The invention provides compounds of Formula I: where in W is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: June 6, 2002Date of Patent: June 27, 2006Assignee: Pfizer Inc.Inventors: Donn G. Wishka, Steven Charles Reitz, David W. Piotrowski, Vincent E. Groppi, Jr.
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Patent number: 7045524Abstract: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.Type: GrantFiled: November 12, 2001Date of Patent: May 16, 2006Assignee: SmithKline Beecham p.l.c.Inventors: David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle
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Patent number: 7045530Abstract: Compounds of formula (I) wherein n1 is 0, 1, or 2; n2 is 0, 1, or 2; X is a bond, O, S, or NR1; and Ar1 is a 5-membered aromatic ring, 6-membered aromatic ring, or a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: December 15, 2004Date of Patent: May 16, 2006Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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Patent number: 7001914Abstract: Compounds of formula I: wherein A, D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.Type: GrantFiled: April 15, 2002Date of Patent: February 21, 2006Assignee: AstraZeneca ABInventors: Eifion Phillips, Richard Schmiesing
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Patent number: 6951868Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is any of: These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: November 1, 2002Date of Patent: October 4, 2005Assignee: Pfizer Inc.Inventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Vincent E. Groppi, Jr.
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Patent number: 6949539Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2001Date of Patent: September 27, 2005Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber
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Patent number: 6916828Abstract: The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C1-C4)-alkylthio, (C1-C4)-alkoxyl, (C1-C4)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C1-C4)-alkyl and (C1-C4)-alkyl substituted by one or several F or OH radicals; R4 represents a substituted or non-substituted cycloalkyl or cycloaryl radical (a heteroalkyl radical or not). The amine of the quinuclidine ring can also be forming quatemary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M3 muscarinic receptor, and selectively, the M2 receptor. Hence, they can be used in the treatment of urinary incontinence (particularly due to bladder instability), irritable bowel syndrome, diseases of the respiratory tract (particularly chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema and rhinitis) and in ophthalmologic operations.Type: GrantFiled: June 25, 2001Date of Patent: July 12, 2005Assignee: Laboratorios S.A.L.V.A.T., S.A.Inventors: Carles Farrerons Gallemi, Juan Lorenzo Catena Ruiz, Anna Fernandez Serrat, Ignacio José Miquel Bono, Dolors Balsa Lopez, José Ignacio Bonilla Navarro, Carmen Lagunas Arnal, Carolina Salcedo Roca, Andrés Fernandez Garcia
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Patent number: 6890935Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodrug derivatives of the compounds of the present invention.Type: GrantFiled: April 30, 2001Date of Patent: May 10, 2005Assignee: Targacept, Inc.Inventors: Gary Maurice Dull, Jeffrey Daniel Schmitt, Balwinder Singh Bhatti, Craig Harrison Miller
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Patent number: 6884807Abstract: This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: November 28, 2001Date of Patent: April 26, 2005Assignee: Neurosearch, A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Philip K. Ahring, Tino Dyhring Jørgensen
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Patent number: 6869946Abstract: The invention provides compounds of Formula I: wherein m1 is 0 or 1; m2 is 1 or 2; R1 is —H, alkyl, halogenated alkyl, substituted alkyl, cycloalkyl, or phenyl; R2 is —H, alkyl, halogenated alkyl, substituted alkyl, cycloalkyl, or phenyl, provided that when m1 is 1 at least one of R1 and R2 is —H; or a pharmaceutically acceptable salt, pharmaceutical composition, a pure enantiomer or racemic mixture thereof. The invention also provides a method for treating a disease or condition in a mammal, wherein the ?7 nicotinic acetylcholine receptor is implicated and for treating diseases where there is a sensory-gating deficit in a mammal comprising administering to a mammal a therapeutically effective amount of a compound of Formula I. These compounds may be in the form of pharmaceutical salts or compositions, and may be in pure enantiomeric form or may be racemic mixtures.Type: GrantFiled: April 17, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Eric Jon Jacobsen, Daniel Patrick Walker, Jason K. Myers, David W. Piotrowski, Vincent E. Groppi, Jr.
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Patent number: 6861526Abstract: A process for preparing (S,S)-cis-2-benzhydryl-3-benzylaminoquinuclidine. The process includes the steps of contacting a compound containing a mixture of R- and S-isomers and having the formula with an effective amount of a chiral organic acid in the presence of an organic solvent and an effective amount of an organic carboxylic acid for converting the R-isomer into an acid salt of the S isomer, wherein the organic solvent is capable of solubilizing the compound containing the mixture of R- and S-isomers, while precipitating the acid salt and the organic carboxylic acid is different from the chiral organic acid; neutralizing the acid salt with a base to provide an S-isomer of a chiral ketone of the formula ; and reacting the chiral ketone with an organic amine in the presence of a Lewis acid to provide the corresponding imine and reducing the imine.Type: GrantFiled: October 6, 2003Date of Patent: March 1, 2005Assignees: Pfizer Inc., DSM Pharmaceuticals, Inc.Inventors: Robert Seemayer, Thomas C. Nugent
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Patent number: 6858613Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which ?7 is known to be involved.Type: GrantFiled: February 14, 2003Date of Patent: February 22, 2005Assignee: Pfizer Inc.Inventors: Bruce N. Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Vincent E. Groppi, Jr.
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Patent number: 6849620Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: October 17, 2002Date of Patent: February 1, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, Eric Jon Jacobsen, David W. Piotrowski, Brad A. Acker, Donn G. Wishka, Jeffrey W. Corbett, Mark R. Rauckhorst, Vincent E. Groppi, Jr.
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Patent number: 6828330Abstract: The invention provides compounds of Formula I: wherein W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful to treat diseases or conditions in which &agr;7 is known to be involved.Type: GrantFiled: June 6, 2002Date of Patent: December 7, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Daniel Patrick Walker, Donn G. Wishka, David W. Piotrowski, Vincent E. Groppi, Jr.
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Patent number: 6780861Abstract: The invention provides compounds of formula (I) wherein n, A, R1, R2 and R3 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.Type: GrantFiled: October 31, 2002Date of Patent: August 24, 2004Assignee: Novartis AGInventor: Joachim Nozulak
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Patent number: 6750226Abstract: A compound according to formula (I) wherein: is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; which shows high affinity for muscarinic M3 receptors (Hm3).Type: GrantFiled: January 14, 2002Date of Patent: June 15, 2004Assignee: Almirall-Prodesfarma, S.A.Inventors: Dolors Fernandez Forner, Maria Prat Quiñones, Maria Antonia Buil Albero
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Publication number: 20040087616Abstract: The invention provides compounds of Formula I: 1Type: ApplicationFiled: July 25, 2003Publication date: May 6, 2004Inventors: David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Daniel Patrick Walker, Donn G. Wishka, Vincent E. Groppi
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Publication number: 20040034223Abstract: The present invention relates to the preparation of synthons that are used to form modules that, in turn, are used to form two-dimensional close-packed planar arrays, referred to as nanomembranes. In a presently preferred embodiment, a nanomembrane herein constitutes a filter.Type: ApplicationFiled: February 7, 2002Publication date: February 19, 2004Applicant: CoValent Partners, LLC.Inventors: Timothy B. Karpishin, Josh Kriesel, Grant Merrill, Donald B. Bivin, Thomas H. Smith, Martin Stuart Edelstein
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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