Chalcogen Bonded Directly To Ring Carbon Of The Quinuclidine Ring System Patents (Class 546/137)
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Publication number: 20100113510Abstract: The invention provides compounds of formula (I) wherein R5 is a group of formula (II) or (III) and R1, R2, R3, R4, R6, a, b, Z, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation.Type: ApplicationFiled: December 17, 2007Publication date: May 6, 2010Inventors: Rhonan Ford, Antonio Mete, Ian Millichip, Barry Teobald
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Publication number: 20100105658Abstract: [Problems] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like. [Means for Solving Problems] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.Type: ApplicationFiled: February 7, 2008Publication date: April 29, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Shinya Nagashima, Toru Kontani, Hiroshi Nagata, Yuji Matsushima, Hisao Hamaguchi, Tadatsura Koshika
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Patent number: 7705152Abstract: An alcohol oxidation catalyst which is an organic oxidation catalyst to oxidize an alcohol, which contains azabicyclo[3.3.1]nonane N-oxyl represented by the following formula (1) having an N-oxyl group incorporated in a bicycle[3.3.1]nonane skeleton: wherein X is H2, O or NOH.Type: GrantFiled: November 21, 2007Date of Patent: April 27, 2010Assignee: Nissan Chemical Industries, Ltd.Inventors: Yoshiharu Iwabuchi, Masatoshi Shibuya, Masaki Tomizawa
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Patent number: 7687630Abstract: The invention provides a method for producing optically active 3-quinuclidinols having one or more substituted groups at the 2-position; wherein 3-quinuclidinones having one or more substituted groups at the 2-position are reacted with compounds providing hydrogen in the presence of a certain metal complex.Type: GrantFiled: September 28, 2007Date of Patent: March 30, 2010Assignee: Kanto Kagaku Kabushiki KaishaInventors: Takeaki Katayama, Kunihiko Murata
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Patent number: 7683075Abstract: The present invention relates to novel isoquinoline-3-carboxylic acid amides having ?7 nicotinic acetylcholine receptor agonistic activity, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.Type: GrantFiled: May 11, 2004Date of Patent: March 23, 2010Assignee: Novartis AGInventor: Max Peter Seiler
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Patent number: 7674794Abstract: 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: November 15, 2006Date of Patent: March 9, 2010Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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Publication number: 20100056565Abstract: This invention relates to M3 antagonists of formula (I) wherein R2, R4, R5, R6, W, V, A, D, X, t, u and v are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment of diseases where enhanced M3 receptor activation is implicated.Type: ApplicationFiled: February 14, 2008Publication date: March 4, 2010Applicant: ARGENTA DISCOVERY LIMITEDInventors: Barbara Giuseppina Avitabile, Harry Finch, Jamie David Knight, Alan John Nadin, Nicholas Charles Ray
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Publication number: 20100041887Abstract: Compounds of formula I in salt or zwitterionic form wherein, wherein R1, R2, R3, and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: October 20, 2009Publication date: February 18, 2010Inventors: Stephen Paul Collingwood, Brian Cox, Urs Baettig, Gurdip Bhalay, Nicholas James Devereux
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Publication number: 20100035922Abstract: Quinuclidine carbonate derivatives act as muscarinic receptor antagonists and are effective for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: ApplicationFiled: July 30, 2009Publication date: February 11, 2010Applicant: Chiesi Farmaceutici S.p.A.Inventors: Gabriele Amari, Maurizio Delcanale
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Publication number: 20100029944Abstract: This invention provides improved methods for making solifenacin and pharmaceutically acceptable salts thereof. The instant methods are unexpectedly advantageous in their simplicity and efficiency.Type: ApplicationFiled: November 20, 2007Publication date: February 4, 2010Applicant: Corporacion Medichem, S.L.Inventors: Jordi Puig, Laura Sanchez, Ester Masllorens, Ignasi Auger, Jordi Bosch
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Patent number: 7652010Abstract: Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, 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 may be used for the treatment of various diseases or disorders, including 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: October 14, 2005Date of Patent: January 26, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen
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Publication number: 20100010225Abstract: The present invention provides an isoquinuclidine derivative which can be used to easily synthesize oseltamivir or an analog thereof. In particular, the present invention provides an isoquinuclidine derivative represented by the following formula (1) or an enantiomer thereof: wherein in the formula (1), A represents a protective group for the nitrogen atom; R1 to R1 each independently represent an alkyl group which may have a substituent, an aryl group which may have a substituent, or a hydrogen atom; and X represents a halogen atom.Type: ApplicationFiled: July 27, 2007Publication date: January 14, 2010Applicant: The University of TokyoInventors: Tohru Fukuyama, Satoshi Yokoshima, Nobuhiro Satoh
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Publication number: 20090326230Abstract: The present invention relates to solifenacin in solid form and a process for its preparation and to a process for the preparation of (1S)-1-Phenyl-1,2,3,4-tetrahydro-isoquinoline, a key intermediate in the synthesis of solifenacin and its salts.Type: ApplicationFiled: July 18, 2007Publication date: December 31, 2009Applicants: Dr. Reddy's Laboratories Ltd., Dr. Reddy's Laboratories, Inc.Inventors: Vijayavitthal Thippannachar Mathad, Jaydeepkumar Dahyabhai Lilakar, Goverdhan Gilla, Sriramireddy Kikkuru, Raveendra Reddy Chinta, Swaroopa Dudipala
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Patent number: 7629466Abstract: The subject invention provides methods and/or processes for making 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: April 25, 2008Date of Patent: December 8, 2009Assignee: ARYx Therapeutics, Inc.Inventors: Kolbot By, Jinun-Ban Yeh, Ponny Pang
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Publication number: 20090270369Abstract: Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.Type: ApplicationFiled: February 9, 2009Publication date: October 29, 2009Applicant: Eisai R&D Management Co., Ltd.Inventors: Fumihiro Ozaki, Motohiro Soejima, Tasuku Ishida, Yoshihiko Norimine, Nobuyuki Kurusu, Eriko Doi, Toshihiko Kaneko, Daiju Hasegawa, Kiyoaki Kobayashi, Noburu Yamamoto
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Patent number: 7608710Abstract: A surfactant comprising a polyether segment including at least one pendant alkoxyfluoroalkyl group, and a cationic substituent defined by one of the formulae: or the substituted derivatives thereof.Type: GrantFiled: June 7, 2006Date of Patent: October 27, 2009Assignee: OMNOVA Solutions Inc.Inventors: Charles M. Kausch, Yongsin Kim, Richard R. Thomas, David L. Hardman, Jr.
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Publication number: 20090216019Abstract: A novel ruthenium complex which is a highly efficient catalyst useful for the production of optically active 3-quinuclidinols, and a process for production of optically active 3-quinuclidinols using the ruthenium complex as a catalyst, where the optically active 3-quinuclidinols are useful as an optically active, physiologically active compound utilized in medicines and agrichemicals or as a synthetic intermediate such as a liquid crystal material.Type: ApplicationFiled: March 30, 2005Publication date: August 27, 2009Inventors: Ryoji Noyori, Takeshi Okuma, Kunihiko Tsutsumi, Nariyuki Utsumi, Kunihiko Murata, Takeaki Katayama
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Patent number: 7579362Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: June 26, 2007Date of Patent: August 25, 2009Assignee: Novartis AGInventors: Dominik Feuerbach, Konstanze Hurth, Timothy J Ritchie
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Patent number: 7566727Abstract: This invention encompasses nicotinic acetylcholine receptor reactive compounds in accord with formula (I) Wherein: D represents O; E represents CH2, NH, O or S; n is 1 or 2 and stereoisomers, enantiomers, in vivo-hydrolysable precursors and pharmaceutically-acceptable salts of such compounds, pharmaceutical compositions and formulations containing them, methods of using them to treat diseases and conditions either alone or in combination with other therapeutically-active compounds or substances, processes and intermediates used to prepare them, uses of them as medicaments, uses of them in the manufacture of medicaments and uses of them for diagnostic and analytic purposes.Type: GrantFiled: April 6, 2005Date of Patent: July 28, 2009Assignee: AstraZeneca ABInventors: Marc Chapdelaine, Keith J. Herzog
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Publication number: 20090124807Abstract: The present invention relates to intermediates useful in the synthesis of Dolasetron and synthetic precursors thereof, as well as to processes for obtaining them. In addition, it refers to the hydrochloric salt of Dolasetron and polymorphic forms of Dolasetron and precursors thereof.Type: ApplicationFiled: January 22, 2008Publication date: May 14, 2009Inventors: Juan Antonio Perez Andres, Pere Dalmases Barjoan, Joan Huguet Clotet
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Patent number: 7521559Abstract: The invention relates to the quinuclidine compounds of formula I having quaternary ammonium group, its preparation, and the pharmaceutical composition comprising an effective amount of the compound of formula I. The compound and the composition are used to prevent and treat the diseases by blocking acetylcholine receptor. Wherein: R1 is selected from C1-12 saturated straight-chain alkyl and cycloalkyl; R2 is selected from C1-12 saturated straight-chain alkyl or straight-chain alkyl; X is selected from halogen ion, organic and inorganic acid radical.Type: GrantFiled: September 15, 2004Date of Patent: April 21, 2009Inventor: Shuqiang Zhao
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Patent number: 7514450Abstract: This invention relates to novel azabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors. 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 10, 2005Date of Patent: April 7, 2009Assignee: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Daniel B. Timmermann
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Publication number: 20090054480Abstract: Carbamates of formula (I) or pharmaceutically acceptable salts thereof, including quaternary ammonium salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.Type: ApplicationFiled: September 5, 2008Publication date: February 26, 2009Inventors: Maria PRAT QUINONES, Maria Antonia Buil Albero, Maria Dolors Fernandez Forner
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Publication number: 20090054446Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: October 31, 2008Publication date: February 26, 2009Inventors: Dominik FEUERBACH, Konstanze Hurth, Timothy John Ritchie
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Publication number: 20090048281Abstract: Compounds of Formula (I); in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: October 31, 2005Publication date: February 19, 2009Inventors: Neil John Press, Stephen Paul Collingwood, Urs Baettig, Brian Cox, Sudhakar Devidasrao Garad, Hyungchul Kim, Dimitris Papoutsakis, Simon James Watson
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Patent number: 7488735Abstract: New quinuclidine amide derivatives having the chemical structure of general formula (I) and pharmaceutically acceptable salts thereof including quaternary salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions 10 comprising them and their use in therapy as antagonists of M3 muscarinic receptors.Type: GrantFiled: June 25, 2003Date of Patent: February 10, 2009Assignee: Laboratorios Almirall S.A.Inventor: Maria Prat Quinones
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Publication number: 20090023702Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR 119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.Type: ApplicationFiled: July 16, 2008Publication date: January 22, 2009Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
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Patent number: 7462722Abstract: An object of the present invention is to provide a process for producing optically active 3-quinuclidinol having high optical purity or the salt thereof at high yield. The invention relates to a process for producing optically active 3-quinuclidinol or the salt thereof by reacting 3-quinuclidinone or the salt thereof with hydrogen in the presence of a basic compound, a complex of a transition metal in Groups 8 to 10, an optically active bidentate ligand and an optically active diamine.Type: GrantFiled: August 4, 2005Date of Patent: December 9, 2008Assignee: Takasago International CorporationInventor: Motonobu Takenaka
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Publication number: 20080293678Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.Type: ApplicationFiled: March 17, 2006Publication date: November 27, 2008Applicant: NitroMed, Inc.Inventor: David S. Garvey
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Patent number: 7452904Abstract: Carbamate of general formula (I), wherein R1, R2, and R3 are H, OH, NO2, SH, CN, F, Cl, Br, I, COOH, CONH2, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylsulfanyl, (C1-C4)-alkylsulfinyl, (C1-C4)-alkylsulfonyl, (C1-C4)-alkoxyl optionally substituted with one or several F, and (C1-C4)-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C5-C10)-alkyl, a substituted (C1-C10)-alkyl; and X? is a physiologically acceptable anion. Carbamate (I) is selective M3 receptor antagonists versus M2 receptor and may be used for the treatment of urinary incontinence (particularly, the one caused by overactive bladder), irritable bowel syndrome, and respiratory disorders (particularly, chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema, and rhinitis), as well as in ophthalmic interventions.Type: GrantFiled: December 18, 2002Date of Patent: November 18, 2008Assignee: Chiesi Farmaceutici S.p.A.Inventors: Juan Lorenzo Catena Ruiz, Carles Farrerons Gallemi, Anna Fernandez Serrat, Ignacio José Miquel Bono, Dolors Balsa Lopez, Carmen Lagunas Arnal, Carolina Salcedo Roca, Natividad Toledo Mesa, Andrés Fernandez Garcia
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Patent number: 7435742Abstract: Carbamates of formula (I) or pharmaceutically acceptable salts thereof, including quaternary ammonium salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.Type: GrantFiled: June 18, 2003Date of Patent: October 14, 2008Assignee: Laboratorios Almirall S.A.Inventors: Maria Prat Quinones, Maria Antonia Buil Albero, Maria Dolors Fernandez Forner
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Publication number: 20080249312Abstract: An industrially acceptable process for the preparation of 2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine. The cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine is known generally as Cevimeline.Type: ApplicationFiled: April 4, 2007Publication date: October 9, 2008Inventors: Svetoslav S. Bratovanov, Elena Bejan, Zhi-Xian Wang, Stephen E. Horne
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Publication number: 20080247963Abstract: The invention relates to the quinuclidine compounds of formula I having quaternary ammonium group, its preparation, and the pharmaceutical composition comprising an effective amount of the compound of formula I. The compound and the composition are used to prevent and treat the diseases by blocking acetylcholine receptor. Wherein: R1 is selected from C1-12 saturated straight-chain alkyl and cycloalkyl; R2 is selected from C1-12 saturated straight-chain alkyl or straight-chain alkyl; X is selected from halogen ion, organic and inorganic acid radical.Type: ApplicationFiled: September 15, 2004Publication date: October 9, 2008Inventor: Shuqiang Zhao
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Patent number: 7432280Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).Type: GrantFiled: May 25, 2004Date of Patent: October 7, 2008Assignee: Eli Lilly and CompanyInventors: Christopher David Beadle, Manuel Javier Cases-Thomas, Barry Peter Clark, Peter Thaddeus Gallagher, John Joseph Masters, Graham Henry Timms, Magnus Wilhelm Walter, Maria Ann Whatton, Virginia Ann Wood, Jeremy Gilmore
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Publication number: 20080242697Abstract: The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: March 28, 2008Publication date: October 2, 2008Applicant: Medichem, S.A.Inventors: Jordi Puig Serrano, Pelayo Camps
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Publication number: 20080221331Abstract: An alcohol oxidation catalyst which is an organic oxidation catalyst to oxidize an alcohol, which contains azabicyclo [3.3.1]nonane N-oxyl represented by the following formula (1) having an N-oxyl group incorporated in a bicycle[3.3.1]nonane skeleton: wherein X is H2, O or NOH.Type: ApplicationFiled: November 21, 2007Publication date: September 11, 2008Applicant: Nissan Chemical Industries Ltd.Inventors: Yoshiharu IWABUCHI, Masatoshi Shibuya, Masaki Tomizawa
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Publication number: 20080214600Abstract: Compounds of formula (I) wherein the different substituents and/or radicals have the values defined in the claims. The invention also relates to a process for the preparation of said compounds, to pharmaceutical compositions comprising them, as well as to combinations of said compounds with other compounds which are active in the treatment of respiratory, urological or gastrointestinal disorders or diseases. Finally the invention also relates to the use of the compounds of formula (I) for the treatment of respiratory, urological or gastrointestinal disorders or diseases.Type: ApplicationFiled: March 10, 2005Publication date: September 4, 2008Applicant: ALMIRALL PRODESFARMA, SAInventors: Maria Dolors Fernandez Forner, Maria Prat Quinones, Maria Antonia Buil Albero
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Publication number: 20080194562Abstract: The invention provides compounds of the formula (I) or a salt, tautomer, solvate or N-oxides thereof; wherein: R1 is selected from (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents are fluorine, chlorine, methyl or methoxy; and (d) a group R0 wherein R0 is a 3-12 membered carbocyclic or heterocyclic group; or optionally substituted C1-8 hydrocarbyl; R2a and R2b are each hydrogen or methyl; and R3 is as defined in the claims. The compounds have activity as inhibitors of Cyclin Dependent Kinases (CDK) and Glycogen Synthase Kinases (GSK) kinases and are useful in the treatment or prophylaxis of disease states or conditions mediated by the kinases.Type: ApplicationFiled: January 20, 2006Publication date: August 14, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Paul Graham Wyatt, Valerio Berdini, Adrian Liam Gill, Gary Trewartha, Andrew James Woodhead, Eva Figueroa Navarro, Michael Alistair O'Brien, Theresa Rachael Phillips
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Publication number: 20080194824Abstract: The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.Type: ApplicationFiled: June 26, 2006Publication date: August 14, 2008Applicant: INKE, S.A.Inventor: Juan Antonio Perez Andres
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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: 20080114171Abstract: Polymorphic forms of solifenacin base have been prepared and characterized. These polymorphic forms are particularly useful for preparing solifenacin salts.Type: ApplicationFiled: August 3, 2007Publication date: May 15, 2008Inventors: Tamas Koltai, Nurit Perlman, Tamar Nidam, Mili Abramov
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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: 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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Patent number: 7326787Abstract: The subject invention provides methods and/or processes for making 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: August 31, 2006Date of Patent: February 5, 2008Assignee: ARYx Therapeutics, Inc.Inventors: Kolbot By, Jinun-Ban Yeh, Ponny Pang
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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: 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: 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: 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