Quinuclidines (including Unsaturation) Patents (Class 514/305)
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Publication number: 20080146548Abstract: This disclosure relates to amides, aryl sulphonamides, aryl ureas, and ?,?-diketones derivatives useful as carboxylesterase esterase inhibitors. The disclosure is also directed to the use of these compounds as selective human intestinal carboxylesterase inhibitors and insect carboxylesterase inhibitors. The disclosure is also directed to pharmaceutical compositions and pesticide formulations containing these compounds, and to methods for treating or ameliorating the toxic effects following administration of drugs such as cancer therapy drugs, treating or ameliorating the effects of a drug overdose, and to the use of the compounds for increasing the effectiveness of insecticides and pesticides.Type: ApplicationFiled: February 15, 2008Publication date: June 19, 2008Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITALInventors: Philip M. Potter, Janice L. Hyatt, Christopher L. Morton, Paul P. Beroza, Komath V. Damoradan
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Publication number: 20080145318Abstract: Methods and formulations for delivering atomoxetine compounds that minimize drug metabolism and thus increase the effectiveness of the drug are disclosed. The in vivo potency of the atomoxetine compound may be maximized by minimizing the in vivo conversion of the atomoxetine compound to an atomoxetine compound metabolite.Type: ApplicationFiled: December 13, 2006Publication date: June 19, 2008Inventor: Kamal K. Midha
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Publication number: 20080132538Abstract: A method of treating overactive bladder disorders characterized by involuntary neurogenic detrusor contractions associated with the pathology of multiple sclerosis by administering fluoroalkoxybenzylamino derivatives of nitrogen containing heterocyclic compounds, and specifically, by administering compounds of the formula wherein Q, X1, X2 and X3 are as defined below, and their pharmaceutically acceptable salts.Type: ApplicationFiled: August 5, 2004Publication date: June 5, 2008Inventors: Phillip Branch Chappell, Brian Thomas O'Neill, Mario David Saltarelli
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Publication number: 20080118553Abstract: The subject invention provides a composition comprising a mixture of polypeptides in the form of a tannate salt wherein each polypeptide is a copolymer of the amino acids L-glutamic acid, L-alanine, L-tyrosine and L-Lysine, methods of preparation and uses thereof.Type: ApplicationFiled: June 12, 2007Publication date: May 22, 2008Inventors: Anton Frenkel, Arthur A. Komlosh
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Patent number: 7375219Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: GrantFiled: April 13, 2006Date of Patent: May 20, 2008Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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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: 20080113902Abstract: The invention features a method of treating or preventing a disease associated with the use of antibiotics in a patient in need thereof by administering to the patient ramoplanin in an amount and for a duration effective to treat said disease. The disease may be caused, for example, by the presence of a bacterium such as enterotoxin producing strains of C. difficile, C. perfringens, or S. aureus.Type: ApplicationFiled: October 3, 2007Publication date: May 15, 2008Applicant: Oscient Pharmaceuticals CorporationInventors: Daniela Jabes, Timothy S. Leach, Richard F. Labaudiniere, Steven M. Rauscher, Giorgio Mosconi
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Publication number: 20080103171Abstract: The present invention relates to the provision of a stable particulate pharmaceutical composition of solifenacin or a salt thereof, which is in a spherical shape suitable for coating and in which degradation with time can be inhibited when a pharmaceutical preparation of solifenacin or a salt thereof is supplied to clinical fields. More particularly, it relates to a particulate pharmaceutical composition that can be obtained by using a binder having a Tg or mp lower than 174C upon formulating a particulate composition of solifenacin into a pharmaceutical preparation. Further, by performing a crystallization-promoting treatment after the particulate pharmaceutical composition is produced, a more stable particulate composition of solifenacin or a salt thereof can be provided.Type: ApplicationFiled: December 26, 2005Publication date: May 1, 2008Applicant: ASTELLAS PHARMA INC.Inventors: Hiroyuki Umejima, Hiroshi Ohi, Katsumi Saito, Yuko Taketani
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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: 7358260Abstract: The invention provides 1-phenethyl-3 (R)-(9[H]-xanthene-9-carbonyloxy)-1 -azoniabicyclo[2.2.2]octane in salt form, pharmaceutical compositions comprising it, and methods of using it for treatment of respiratory disorders.Type: GrantFiled: December 8, 2006Date of Patent: April 15, 2008Assignee: Laboratories Almirall, S.A.Inventors: María Dolors Fernandez Forner, María Prat Quiñones, María Antonia Buil Albero
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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: 7348330Abstract: The present invention provides novel compounds, corresponding to formulae I and II, respectively, which are able to reactivate the apoptosis-inducing function of mutant p53 proteins. This reactivation is provided by restoration of sequence-specific DNA-binding activity and transcriptional transactivation function to mutant p53 proteins, and modulation of the conformation-dependent epitopes of the p53 protein. Accordingly, the substances according to the invention will be used in pharmaceutical compositions and methods for treatment of patients suffering from various types of tumors.Type: GrantFiled: December 14, 2004Date of Patent: March 25, 2008Assignee: Aprea ABInventors: Vladimir Bykov, Galina Selivanova, Klas Wiman
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Patent number: 7335668Abstract: A depressant of capsaicin-sensitive sensory nerve, containing quinuclidin-3?-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a salt thereof as an active ingredient, specifically a therapeutic drug of interstitial cystitis, hypersensitive disorder of the lower urinary tract, and/or abacterial prostatitis.Type: GrantFiled: July 8, 2002Date of Patent: February 26, 2008Assignee: Astellas Pharma Inc.Inventors: Ken Ikeda, Makoto Takeuchi
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Publication number: 20080045564Abstract: Disclosed herein is a method of using quinine. The method comprises informing a user that quinine does not induce the activity of a cytochrome p450 isozyme.Type: ApplicationFiled: January 5, 2007Publication date: February 21, 2008Applicant: MUTUAL PHARMACEUTICAL COMPANY, INC.Inventors: Richard Howard Roberts, Jie Du, Matthew William Davis, Kurt R. Nielsen
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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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Publication number: 20080039492Abstract: Disclosed herein is a method of using quinine. In one embodiment, the method comprises obtaining quinine from a container associated with published material providing information that quinine affects the activity of a cytochrome p450 isozyme. In another embodiment, the method comprises informing a user that quinine affects the activity of a cytochrome p450 isozyme. Also included are articles of manufacture comprising a container containing a dosage form of quinine, wherein the container is associated with published material informing that quinine affects activity of a cytochrome p450 isozyme. Also disclosed are a method of treatment and a method of manufacturing a quinine product.Type: ApplicationFiled: July 25, 2006Publication date: February 14, 2008Inventors: Richard Howard Roberts, Jie Du, Matthew William Davis, Kurt R. Nielsen
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Patent number: 7312231Abstract: A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 31, 2003Date of Patent: December 25, 2007Assignee: Almirall Prodesfarma AGInventors: Maria Antonia Buil Albero, Dolors Fernandez Forner, Maria Prat Quiñones
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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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Publication number: 20070259053Abstract: Increased positive charge of compounds or agents leads to increased glomerular filtration, increased binding by positively charged agents by the cells of the proximal tubules and decreased digestion of the reabsorbed materials. The present invention concerns the use of non-toxic positively charged materials to saturate binding sites on the proximal tubular brush border. If the binding sites on the brush border are saturated, then there should be decreased binding and absorption of the toxic agents by the proximal tubular renal cells. Specifically the invention is the use of combination of therapeutic positively charged agents comprising one or more of the following compounds; pyridoxal, niacin, thiamine and their relatively non-toxic analogs, amprolium, and isoniazid. These compounds are administered prior to the dosing of such positively charged therapeutics such as Trasylol® (aprotinin), cisplatin. or antimicrobiological peptides such as reported in patent application publication 2005/0065072.Type: ApplicationFiled: April 27, 2007Publication date: November 8, 2007Inventor: William M. Selenke
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Patent number: 7265133Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 are as defined specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: September 4, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
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Publication number: 20070190190Abstract: Compositions and methods of treating skin irritation are disclosed where a conditioning composition is applied to the skin of a user. The compositions and methods are useful to prevent, reduce and/or eliminate irritation of the skin subjected to topical treatment.Type: ApplicationFiled: December 30, 2006Publication date: August 16, 2007Inventors: Jose E. Ramirez, Joseph Faryniarz
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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: 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: 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: 7214687Abstract: 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, in association with phosphodiesterase 4 inhibitors.Type: GrantFiled: January 3, 2006Date of Patent: May 8, 2007Assignee: Almirall AGInventors: Maria Dolors Fernandez Forner, Maria Prat Quiñones, Maria Antonia Buil Albero
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Patent number: 7208501Abstract: A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 10, 2002Date of Patent: April 24, 2007Assignee: Almirall Prodesfarma AGInventors: Maria Antonia Buil Albero, Dolors Fernandez Forner, Maria Prat Quiñones
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Patent number: 7196098Abstract: 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, in association with steroids.Type: GrantFiled: January 3, 2006Date of Patent: March 27, 2007Assignee: Almirall Prodesfarma AGInventors: Maria Dolors Fernandez Forner, Maria Prat Quiñones, Maria Antonia Buil Albero
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Patent number: 7179818Abstract: This invention is directed towards substituted aminoquinuclidine compounds useful as delta-opioid receptor modulators, delta-opioid receptor agonists useful as analgesics and delta-opioid receptor antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.Type: GrantFiled: October 14, 2003Date of Patent: February 20, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert E. Boyd, Allen B. Reitz
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Patent number: 7176218Abstract: The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.Type: GrantFiled: January 7, 2005Date of Patent: February 13, 2007Assignee: ARYx TherapeuticsInventors: Ian Irwin, Monica Palme, Cyrus Becker
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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: 7176219Abstract: There is provided an acid addition salt of (?)-(3R)-quinuclidin-3-yl(1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate with an acid selected from the group consisting of (?)-(2S,3S)-tartaric acid, (+)-(2S,3S)-di-O-benzoyltartaric acid, (+)-(2S,3S)-di-O-(4-methylbenzoyl)tartaric acid, (?)-L-phenylalanine, benzenesulfonic acid, cyclohexanesulfamic acid, hydrobromic acid, naphthalene-2-sulfonic acid, sebacic acid, (+)-camphor-10-sulfonic acid, p-toluenesulfonic acid, ethanesulfonic acid, methanesulfonic acid and methyl phosphate, which has little hygroscopicity that affects the use as a drug or its drug substance, and is very useful as a drug or its drug substance.Type: GrantFiled: May 13, 2005Date of Patent: February 13, 2007Assignee: Astellas Pharma Inc.Inventors: Masahiko Hayakawa, Kiyohiro Samizu, Hiroshi Uebayashi, Ken Ikeda, Makoto Takeuchi
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Patent number: 7164024Abstract: This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] [in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease, drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.Type: GrantFiled: April 19, 2002Date of Patent: January 16, 2007Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takeru Yamakawa, Yoshio Ogino, Yufu Sagara, Kenji Matsuda, Akira Naya, Toshifumi Kimura, Norikazu Otake
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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: 7115745Abstract: The present invention is directed to a new class of 6-benzyl urea/thiourea-quinolin-2-one derivatives and 2-oxo-6-benzylurea/thiourea-chromene derivatives. These compound are androgen antagonists and are useful in the treatment of alopecia, acne and other conditions associated with inappropriate activation of the androgen receptor.Type: GrantFiled: February 10, 2004Date of Patent: October 3, 2006Assignee: Warner Lambert Company LLCInventors: Daniel Y. Du, Martin James Procter, Matthew Colin Thor Fyfe, Vilasben Kanji Shah, Geoffrey Martyn Williams, Karen Lesley Schofield
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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: 7109210Abstract: Compounds of the formula wherein: {circle around (C)} is phenyl, C4 to C9 heteroaromatic, naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl; R1, R2 and R3 are hydrogen or a substituent; n is 0 to 4; A represents —CH2—, —CH?CR6, —CR6?CH—, —CR6R7—, —CO—, —O—, —S—, —S(O)—, SO2 or —NR6—, wherein R6 and R7 are hydrogen or lower alkyl, or R6 and R7 together form an alicyclic ring; m is 0 to 8; (when m=0, A is not —CH2—); p is 1 or 2; B represents a group of the formula ii): wherein R10 is hydrogen, hydroxy or methyl; and Q represents a single bond, —CH2—, —CH2—CH2—, —O—, —O—CH2—, —S—, —S—CH2— or —CH?CH—, and x represents an anion and wherein the compounds show high affinity for muscarinic M3 receptors (Hm3).Type: GrantFiled: December 17, 2003Date of Patent: September 19, 2006Assignee: Almirall Prodesfarma AGInventors: Maria Dolors Fernandez Forner, Maria Prat Quiñones, Maria Antonia Buil Albero
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Patent number: 7101894Abstract: Methods for treating CMV or a CMV-related disease are provided that use compounds having the formula: wherein Ar is a substituted or unsubstituted 5–14 membered heteroaryl group having from 1 to 5 heteroatoms as ring members; R1 is selected from the group consisting of substituted or unsubstituted aryl(C1–C4)alkyl, heteroaryl(C1–C4)alkyl, —C(O)R11, and —C(O)NR11R12, wherein each R11 and R12 independently is substituted or unsubstituted aryl, substituted or unsubstituted aryl(C1–C4)alkyl, substituted or unsubstituted (C4–C8)cycloalkyl(C1–C4)alkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaryl(C1–C4)alkyl and substituted or unsubstituted hetero(C4–C8)cycloalkyl(C1–C4)alkyl; R2 is H or (C1–C8)alkyl; and ZN is a substituted or unsubstituted hetero(C6–C10)bicycloalkyl group.Type: GrantFiled: August 29, 2002Date of Patent: September 5, 2006Assignee: ChemoCentryx, Inc.Inventors: Brian E. McMaster, Thomas J. Schall, Mark Penfold, J. J. Wright, Daniel J. Dairaghi
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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: RE39128Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.Type: GrantFiled: October 27, 1998Date of Patent: June 13, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt
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Patent number: RE39300Abstract: Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA-receptor activation, e.g., a ganglioside such as GM1 or GT1b, a phenothiazine such as trifluoperazine or a naphthalenesulfonamide such as N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide, inhibit the development of tolerance to and/or dependence on addictive drugs, e.g., narcotic analgesics such as morphine, codeine, etc.Type: GrantFiled: June 15, 2001Date of Patent: September 19, 2006Assignee: Virginia Commonwealth University Medical College of VirginiaInventors: David J. Mayer, Jianren Mao