The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/238)
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Patent number: 11440882Abstract: Disclosed herein a process for the preparation of highly pure dexmethylphenidate hydrochloride (Formula-I) which comprises the steps of neutralization of dl-threomethylphenidate hydrochloride to dl-threo methylphenidate; subsequent resolution of dl-threo methylphenidate using amino acid or its derivatives as chiral resolution agent to yield dexmethylphenidate salt; hydrolysis of the salt and further conversion of dexmethylphenidate into its hydrochloride salt.Type: GrantFiled: July 17, 2017Date of Patent: September 13, 2022Assignee: HARMAN FINOCHEM LIMITEDInventors: Vijay Trimbak Kadam, Nareesh Saranapu, Santosh Uttamrao Chavan, Harpreet Singh Minhas, Gurpreet Singh Minhas
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Patent number: 9573896Abstract: Novel methods and systems for producing a substantially pure d-threo stereoisomer of methylphenidate or a salt thereof are provided. In particular, methods and systems for producing d-threo-methylphenidate hydrochloride in pure stereoisomeric form from d-threo-ritalinic acid hydrochloride using diazomethane are described. The described methods can be performed on a large scale, and thus provide d-threo methylphenidate or a salt thereof, and particularly the hydrochloride salt of d-threo-methylphenidate, in stereoisomerically pure form and in large quantities from a single batch reaction. Also described are novel compositions of d-threo methylphenidate hydrochloride.Type: GrantFiled: December 4, 2015Date of Patent: February 21, 2017Assignee: AMPAC Fine Chemicals LLCInventors: Aslam Malik, Francis Hempenstall, Nicholas Duda, Ali Suleman
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Patent number: 9512077Abstract: The present invention relates to an industrially feasible and economically viable process for the preparation of methylphenidate hydrochloride of formula I and its intermediates thereof.Type: GrantFiled: July 24, 2014Date of Patent: December 6, 2016Assignee: ZCL CHEMICALS LTD.Inventors: Agarwal Nand Lal, Chandrashekhar Singh, Mubashshir Ahmed, Bhavsar Rahul Arunbhai
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Patent number: 9475770Abstract: The present invention describes a process for the preparation of methylphenidate hydrochloride. The process involves the esterification of ritalinic acid and methanol in the presence of an acid catalyst at a low temperature. The process may optionally involve the addition of an orthoester.Type: GrantFiled: December 16, 2011Date of Patent: October 25, 2016Assignee: Rhodes TechnologiesInventors: C. Frederick M. Huntley, Erik Wayne Kataisto, Knicholaus Dudley La Lumiere, Helge Alfred Reisch
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Patent number: 9233924Abstract: Novel methods and systems for producing a substantially pure d-threo stereoisomer of methylphenidate or a salt thereof are provided. In particular, methods and systems for producing d-threo-methylphenidate hydrochloride in pure stereoisomeric form from d-threo-ritalinic acid hydrochloride using diazomethane are described. The described methods can be performed on a large scale, and thus provide d-threo methylphenidate or a salt thereof, and particularly the hydrochloride salt of d-threo-methylphenidate, in stereoisomerically pure form and in large quantities from a single batch reaction. Also described are novel compositions of d-threo methylphenidate hydrochloride.Type: GrantFiled: March 11, 2014Date of Patent: January 12, 2016Assignee: AMPAC Fine Chemicals LLCInventors: Aslam Malik, Francis Hempenstall, Nicholas Duda, Ali Suleman
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Publication number: 20150133667Abstract: The present invention is directed to an improved process for the preparation of methylphenidate, stereoisomer, mixture of stereoisomers and pharmaceutically acceptable salts thereof, more particularly, the sulfate and hydrochloride salts of methylphenidate, di-threo-methylphenidate and dex-methylphenidate. Methods of removing or reducing the amount of impurities from the above described process are also disclosed.Type: ApplicationFiled: October 29, 2014Publication date: May 14, 2015Inventors: Charla Barr, Mark C. Dobish, Brian J. Smith, Stephen M. Stefanick
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Publication number: 20150079520Abstract: An acid diffusion control agent includes a compound represented by a formula (1), a compound represented by a formula (2) or both thereof. R1 represents a hydrocarbon group comprising a monovalent alicyclic structure, or the like. R2 and R3 each independently represent a monovalent hydrocarbon group, or the like. R4 and R5 each independently represent a monovalent hydrocarbon group, or the like. R6 and R7 each independently represent a monovalent hydrocarbon group, or the like. R8 represents a monocyclic heterocyclic group together with the ester group and with the carbon atom. n is an integer of 1 to 6. R9 represents a monovalent hydrocarbon group, or the like. R10 represents a monovalent hydrocarbon group having 1 to 10 carbon atoms. R11 and R12 each independently represent a monovalent hydrocarbon group, or the like. R13 and R14 each independently represent a monovalent hydrocarbon group, or the like.Type: ApplicationFiled: November 14, 2014Publication date: March 19, 2015Applicant: JSR CORPORATIONInventors: Hayato NAMAI, Norihiko IKEDA
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Patent number: 8980880Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.Type: GrantFiled: April 10, 2012Date of Patent: March 17, 2015Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Publication number: 20150051400Abstract: The present invention relates to an industrially feasible and economically viable process for the preparation of methylphenidate hydrochloride of formula I and its intermediates thereof.Type: ApplicationFiled: July 24, 2014Publication date: February 19, 2015Inventors: AGARWAL NAND LAL, CHANDRASHEKHAR SINGH, MUBASHSHIR AHMED, BHAVSAR RAHUL ARUNBHAI
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Patent number: 8957067Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.Type: GrantFiled: April 12, 2012Date of Patent: February 17, 2015Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Publication number: 20150038720Abstract: The present invention describes a process for the preparation of methylphenidate hydrochloride. The process involves the esterification of ritalinic acid and methanol in the presence of an acid catalyst at a low temperature. The process may optionally involve the addition of an orthoester.Type: ApplicationFiled: December 16, 2011Publication date: February 5, 2015Applicant: Rhodes TechnologiesInventors: C. Frederick M. Huntley, Erik Wayne Kataisto, Knicholaus Dudley La Lumiere, Helge Alfred Reisch
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Publication number: 20150038533Abstract: The invention relates to the treatment of an attention deficit hyperactivity disorder (ADHD) with alpha-phenyl(piperidin-2-yl)methanol, or the pharmaceutically acceptable salts and esters thereof, in particular the acetate derivative, more particularly dextrophacetoperane. The invention additionally provides a method of synthesis of the (S,S) enantiomer of alpha-phenyl(piperidin-2-yl)methanol as well as a method of synthesis of dextrophacetoperane.Type: ApplicationFiled: November 29, 2012Publication date: February 5, 2015Inventors: Eric Konofal, Bruno Figadere
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Patent number: 8940729Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.Type: GrantFiled: April 11, 2012Date of Patent: January 27, 2015Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Patent number: 8912217Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.Type: GrantFiled: April 12, 2012Date of Patent: December 16, 2014Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Publication number: 20140329746Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Publication number: 20140287038Abstract: An oral methylphenidate powder which is reconstitutable into a final oral aqueous sustained release formulation containing at least about 50%, or at least about 80% by weight water based on the total weight of the suspension, is provided. The powder is a blend containing a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and a water soluble buffering agent such that upon formed into an aqueous liquid formulation, the formulation has a pH in the range of about 3.5 to about 5, or about 4 to about 4.5. Following administration of a single dose of the oral aqueous methylphenidate suspension, a therapeutically effective amount of methylphenidate is reached in less than one hour and the composition provides a twelve-hour extended release profile.Type: ApplicationFiled: June 9, 2014Publication date: September 25, 2014Inventors: Ketan Mehta, Yu-Hsing Tu, Ashok Perumal
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Patent number: 8716278Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.Type: GrantFiled: April 11, 2012Date of Patent: May 6, 2014Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Patent number: 8679773Abstract: This invention pertains to methods, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.Type: GrantFiled: January 16, 2007Date of Patent: March 25, 2014Assignee: DH Technologies Development Pte. Ltd.Inventors: Darryl J. C. Pappin, Michael Bartlett-Jones
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Patent number: 8680276Abstract: The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.Type: GrantFiled: March 4, 2010Date of Patent: March 25, 2014Inventors: Riccardo Motterle, Giancarlo Arvotti, Elisabetta Bergantino, Andrea Castellin, Stefano Fogal, Marco Galvagni
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Patent number: 8653065Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.Type: GrantFiled: April 11, 2012Date of Patent: February 18, 2014Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Patent number: 8586575Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.Type: GrantFiled: April 10, 2012Date of Patent: November 19, 2013Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Publication number: 20130274280Abstract: This invention provides an oral pharmaceutical composition comprising a physiologically tolerable gelled oil-in-water emulsion containing a drug of abuse.Type: ApplicationFiled: April 11, 2011Publication date: October 17, 2013Applicant: AYANDA GROUP ASInventors: Kurt Ingar Draget, Ingvild Johanne Haug, Steinar Johan Engelsen, Tore Seternes, Magnus N. Hattrem
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Patent number: 8552195Abstract: The method in accordance with the present invention has: mixing E2M, an organic solvent, a weak base, sodium dithionite, and a phase transfer catalyst to obtain an E2M mixture solution; heating the E2M mixture solution and adding water to obtain a heated E2M aqueous solution having an organic layer; and extracting the organic layer from the heated E2M aqueous solution, and condensing and drying the organic layer to obtain donepezil. Employing sodium dithionite as a reducing agent improves safety over hydrogen gas used in conventional methods and lowers the cost in contrast to the conventional noble metal catalysts that are extremely expensive. Furthermore, the method of the present invention requires only 60 minutes of reaction time to synthesize donepezil with a promising yield more than 85%, which greatly raises the efficiency and economic value of the manufacture of donepezil.Type: GrantFiled: August 5, 2011Date of Patent: October 8, 2013Assignee: Taiwan Biotech Co., Ltd.Inventors: Kuen-Wang Sheu, Shu-Fen Huang
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Publication number: 20130190502Abstract: Disclosed is a selective ester production process of an alcoholic hydroxyl group, which proceeds under chemically mild conditions, while having adequate environmental suitability, operability and economical efficiency. Specifically disclosed is a process for producing an ester compound, which is characterized in that an alcohol and a carboxylic acid ester compound are reacted in the presence of a compound containing zinc element, thereby selectively acylating a hydroxyl group of the alcohol.Type: ApplicationFiled: March 5, 2013Publication date: July 25, 2013Applicant: Takasago International CorporationInventor: Takasago International Corporation
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Patent number: 8431709Abstract: Disclosed is a selective ester production process of an alcoholic hydroxyl group, which proceeds under chemically mild conditions, while having adequate environmental suitability, operability and economical efficiency. Specifically disclosed is a process for producing an ester compound, which is characterized in that an alcohol and a carboxylic acid ester compound are reacted in the presence of a compound containing zinc element, thereby selectively acylating a hydroxyl group of the alcohol.Type: GrantFiled: October 10, 2008Date of Patent: April 30, 2013Assignee: Takasago International CorporationInventors: Kazushi Mashima, Takashi Ohshima, Takanori Iwasaki, Noboru Sayo
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Patent number: 8318942Abstract: A process for producing a Donepezil derivative represented by the formula (I), wherein R1, R2, R3, and R4 each independently represents H, F, an alkyl having from 1 to 4 carbon atoms, or an alkoxy having from 1 to 4 carbon atoms; R5 represents a phenyl or a substituted phenyl; and n is an integer from 0 to 2, characterized in that the process comprises: (a) a reaction of 4-pyridinecarboxaldehyde with a compound of formula (II) in the presence of a strong acid HX to form a compound of formula (III); (b) a catalytic hydrogenation of a compound of formula (III) or a compound of formula (V) to yield a compound of formula (IV); and (c) an alkylation reaction of a compound of formula (IV) to yield a compound of formula (I).Type: GrantFiled: October 28, 2004Date of Patent: November 27, 2012Assignee: Tianjin Hemay Bio-Tech Co., Ltd.Inventor: Heshang Zhang
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Patent number: 8309341Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a group of formula COR4, or R1 represents a group of formula (A): R2 represents a group of formula NR5R6, or R2 represents a nitrogen-containing heterocyclic group, an aryl group or a heteroaryl group, R3 represents a hydrogen atom or an alkyl group, m represents an integer between 1 and 6 inclusive, n represents 0, 1 or 2, their optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating and/or preventing thrombotic events.Type: GrantFiled: June 25, 2010Date of Patent: November 13, 2012Assignees: Les Laboratories Server, L'Institut National des Sciences Appliquées de Rouen, Le Centre National de la Recherche Scientifique, L'Universite de RouenInventors: Philippe Gloanec, Guillaume De Nanteuil, Jean-Gilles Parmentier, Anne-Françoise Guillouzic, Tony Verbeuren, Alain Rupin, Philippe Mennecier, Marie-Odile Vallez, Jean-Charles Quirion, Philippe Jubault, Nicolas Boyer
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Patent number: 8283472Abstract: A synthetic process for the preparation of amino acid esters such as methylphenidate and analogs thereof is disclosed. The process involves reacting an amino acid such as ?-phenyl-?-(2-piperidinyl)acetic acid or an analog thereof with an alcohol such as methanol in the presence of an acid and a water sequestrant such as trimethyl orthoacetate. In some embodiments, the water sequestrant is added to the reaction mixture after an initial period of esterification and then the reaction is allowed to continue. The ?-phenyl-?-(2-piperidinyl)acetic acid methyl ester or analog thereof is then isolated from the reaction mixture. In one variation of the process, the supernatant liquid may be recycled in subsequent runs to increase yield and product purity.Type: GrantFiled: January 6, 2010Date of Patent: October 9, 2012Assignee: Mallinckrodt LLCInventors: Joseph P. Haar, Jr., Carl J. Schaefer, Charles S. Kuivila
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Patent number: 8153657Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.Type: GrantFiled: October 22, 2004Date of Patent: April 10, 2012Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Jia Zhou
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Patent number: 8124783Abstract: Disclosed herein the process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]piperidine or its salt thereof employing novel intermediates.Type: GrantFiled: December 30, 2004Date of Patent: February 28, 2012Assignee: Jubilant Organosys LimitedInventors: Shailendra Kumar Dubey, Amit Kumar Sharma, Beena S. Rani, Soumendu Paul, Rajesh Kumar Thaper, Dubey Sushil Kumar, Jag Mohan Khanna
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Publication number: 20110224256Abstract: The invention features methods, kits, and compositions for the treatment of psychiatric disorders using therapeutic imprinting in pre-pubescent subjects.Type: ApplicationFiled: June 12, 2009Publication date: September 15, 2011Inventor: Susan L. Andersen
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Publication number: 20110130569Abstract: The invention disclosed in this application relates to an improved process for the manufacture of d-threo-ritalinic acid hydrochloride and l-threo-ritalinic acid hydrochloride in an optically pure form by the resolution of dl-threo-ritalinic acid using a chiral carboxylic acid The d-threo-ritalinic acid hydrochloride prepared by the process of the present invention on esterification gives d-threo-methylphenidate, a very well known CNS stimulant.Type: ApplicationFiled: July 3, 2009Publication date: June 2, 2011Inventors: Tangirala Prakasam, Borkatte Narasimha Hitesh Kumar, Sangu Perumal, Kothandapani Loganathan
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Publication number: 20110002985Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.Type: ApplicationFiled: August 12, 2008Publication date: January 6, 2011Applicant: ABUSE DETERRENT PHARMACEUTICAL, LLCInventors: Manish J. Shah, Ray J. Difalco
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Publication number: 20100330064Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a group of formula COR4, or R1 represents a group of formula (A): R2 represents a group of formula NR5R6, or R2 represents a nitrogen-containing heterocyclic group, an aryl group or a heteroaryl group, R3 represents a hydrogen atom or an alkyl group, m represents an integer between 1 and 6 inclusive, n represents 0, 1 or 2, their optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating and/or preventing thrombotic events.Type: ApplicationFiled: June 25, 2010Publication date: December 30, 2010Applicants: LES LABORATOIRES SERVIER, L'INSTITUT NATIONAL DES SCIENCES APPLIQUEES DE ROUEN, LE CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, L'UNIVERSITE DE ROUENInventors: Philippe Gloanec, Guillaume De Nanteuil, Jean-Gilles Parmentier, Anne-Françoise Guillouzic, Tony Verbeuren, Alain Rupin, Philippe Mennecier, Marie-Odile Vallez, Jean-Charles Quirion, Philippe Jubault, Nicolas Boyer
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Publication number: 20100249422Abstract: Disclosed is a selective ester production process of an alcoholic hydroxyl group, which proceeds under chemically mild conditions, while having adequate environmental suitability, operability and economical efficiency. Specifically disclosed is a process for producing an ester compound, which is characterized in that an alcohol and a carboxylic acid ester compound are reacted in the presence of a compound containing zinc element, thereby selectively acylating a hydroxyl group of the alcohol.Type: ApplicationFiled: October 10, 2008Publication date: September 30, 2010Applicant: Takasago International CorporationInventors: Kazushi Mashima, Takashi Ohshima, Takanori Iwasaki, Noboru Sayo
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Patent number: 7759364Abstract: The invention relates to non-hydrated fexofenadine hydrochloride which can be obtained from a fexofenadine base and hydrogen chloride, according to the reaction conditions, either in the form of a novel polymorph (“form A”), in an amorphous form, or in the form of a mixture of different polymorphs. Said novel polymorph (“form A”) can be used as a therapeutic active ingredient and can be processed to form a pharmaceutical containing the same and a pharmaceutically acceptable carrier. Said pharmaceutical is suitable for use as an antihistaminic agent, an antiallergic agent and/or a bronchodilating agent.Type: GrantFiled: January 17, 2002Date of Patent: July 20, 2010Assignee: Cilag AGInventor: Volker Kirsch
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Publication number: 20100179327Abstract: A synthetic process for the preparation of amino acid esters such as methylphenidate and analogs thereof is disclosed. The process involves reacting an amino acid such as ?-phenyl-?-(2-piperidinyl)acetic acid or an analog thereof with an alcohol such as methanol in the presence of an acid and a water sequestrant such as trimethyl orthoacetate. In some embodiments, the water sequestrant is added to the reaction mixture after an initial period of esterification and then the reaction is allowed to continue. The ?-phenyl-?-(2-piperidinyl)acetic acid methyl ester or analog thereof is then isolated from the reaction mixture. In one variation of the process, the supernatant liquid may be recycled in subsequent runs to increase yield and product purity.Type: ApplicationFiled: January 6, 2010Publication date: July 15, 2010Applicant: Mallinckrodt Inc.Inventors: Joseph P. Haar, JR., Carl J. Schaefer, Charles S. Kuivila
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Publication number: 20100160482Abstract: The invention relates to an ophthalmologic composition including a dye of the general formula I in which R1=substituted or unsubstituted hydrocarbon radical, R2=substituted or unsubstituted hydrocarbon radical with at least one polymerizable double bond, R3?H or substituted or unsubstituted hydrocarbon radical, R4?H, electron-withdrawing substituent or substituted or unsubstituted hydrocarbon radical and X?O, S, NH or NR5, wherein R5 is a substituted and/or unsubstituted hydrocarbon radical. Moreover, the invention relates to another ophthalmologic composition and an ophthalmologic lens.Type: ApplicationFiled: December 17, 2009Publication date: June 24, 2010Inventor: Juergen Nachbaur
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Patent number: 7678538Abstract: Asymmetric cyanine dyes of Formula I bind nucleic acid but not red blood cell membrane, and function as photosensitizers when rigidly bound but not when free in solution. Unbound dye thus causes minimal oxidative damage. The dyes do not substantially accumulate in red blood cells, thereby minimizing hemolysis due to oxidative damage. Biological fluids can be disinfected by mixing the fluid with these asymmetric cyanine dye that binds to nucleic acid, irradiating the mixture, and recovering clinically significant components from the biological fluid and/or assaying the fluid for pathogens.Type: GrantFiled: May 10, 2006Date of Patent: March 16, 2010Assignee: American National Red CrossInventor: Stephen J. Wagner
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Publication number: 20100048623Abstract: Compounds of formula (I) are modulators of gamma-secretase, and hence are useful in treatment of Alzheimer's disease.Type: ApplicationFiled: April 25, 2007Publication date: February 25, 2010Inventors: Yudith Garcia, Joanne Clare Hannam, Timothy Harrison, Christopher L. Hamblett, Jed L. Hubbs, Janusz Josef Kulagowski, Andrew Madin, Mark Peter Ridgill, Eileen Seward
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Publication number: 20090275614Abstract: The present invention provides methods of using compounds of formula I: and salts and prodrugs thereof, wherein n, R1 and R2 are defined herein. The invention also provides certain novel compounds of formula I and pharmaceutical compositions comprising them.Type: ApplicationFiled: October 29, 2008Publication date: November 5, 2009Inventors: David Bar-Or, Nagaraja R. K. Rao
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Patent number: 7592359Abstract: This invention generally relates to derivatives of substituted azabicyclo hexanes. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.Type: GrantFiled: April 10, 2003Date of Patent: September 22, 2009Assignee: Ranbaxy Laboratories LimitedInventors: Anita Mehta, Arundutt Viswanatham Silamkoti, Jang Bahadur Gupta
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Publication number: 20090111993Abstract: A process for preparing a compound of formula (I) comprising reacting a compound of formula (II) with a fluorinated boron species of formula (III) in the presence of: an alcohol; a rhodium (I) pre-catalyst species; a suitable ligand that binds to the rhodium (I) pre-catalyst species to form a catalyst complex; a base; and, a suitable solvent; the process being carried out at a temperature in the range 40 to 110° C. The compounds of formula (I) are useful in the preparation of pharmaceutically active compounds.Type: ApplicationFiled: November 13, 2006Publication date: April 30, 2009Applicant: ASTRAZENECA ABInventors: John Oldfield, Ian Patel, Andrew Williams
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Patent number: 7517892Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.Type: GrantFiled: September 12, 2001Date of Patent: April 14, 2009Assignee: Sepracor Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
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Publication number: 20090076079Abstract: The present application describes deuterium-enriched methylphenidate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7459467Abstract: The present invention discloses selective and complete reduction of pyridine ring in a biaryl system comprising ?-substituted or non-substituted benzene ring and relates more specifically, not exclusively, for the manufacture of methylphenidate, which is used for treatment of Attention Deficit Hyperactive Disorder (ADHD) and also acts as central nervous system stimulant, by using palladium/C in a solvent such as C1-C4 alcohols in presence of molar quantities of organic and/or inorganic acids.Type: GrantFiled: June 10, 2005Date of Patent: December 2, 2008Assignee: IPCA Laboratories, Ltd.Inventors: Ashok Kumar, Dharmendra Singh, Swapnali Hemant Patil, Ganesh Devidas Mahale, Uttamrao Arjunrao Sawant
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Publication number: 20080167470Abstract: A process for preparing the d-threo isomer of methylphenidate hydrochloride which includes (i) resolving a racemic mixture of racemic threo-methylphenidate hydrochloride with a less than stoichiometric amount of tertiary amine base to obtain a methylphenidate-chiral acid salt, (ii) basifying the methylphenidate-chiral acid salt to obtain methylphenidate free base, and (iii) converting the methylphenidate free base into d-threo-methylphenidate hydrochloride.Type: ApplicationFiled: January 5, 2007Publication date: July 10, 2008Inventors: Alexei Kalinin, Guofang Qiu, Thomas J. Marren, James E. Aldred, Yu Ji
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Publication number: 20080153843Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: September 28, 2007Publication date: June 26, 2008Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie REICH, Stefan SCHUNK, Sabine HEES, Ruth JOSTOCK, Michael Franz-Martin ENGELS, Achim KLESS, Thomas CHRISTOPH, Klaus SCHIENE, Tieno GERMANN, Edward BIJSTERVELD
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Patent number: 7294637Abstract: One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.Type: GrantFiled: February 4, 2004Date of Patent: November 13, 2007Assignee: Sepracor, Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike S. Radeke, Fengjiang Wang, Liming Shao
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Patent number: 7195751Abstract: This invention pertains to methods, mixtures, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.Type: GrantFiled: January 27, 2004Date of Patent: March 27, 2007Assignee: Applera CorporationInventors: Darryl J. C. Pappin, Michael Bartlet-Jones