Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 540/551)
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Patent number: 11649218Abstract: Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as “c-Abl”). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.Type: GrantFiled: March 8, 2019Date of Patent: May 16, 2023Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Pontificia Universidad Catolica de ChileInventors: Juan J. Marugan, Marc Ferrer, Noel T. Southall, Andres E. Dulcey, Xin Hu, Christopher R. Dextras, Daniel C. Talley, Alejandra Alvarez, Silvana Zanlungo, Rommy M. Von Bernhardi
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Patent number: 9440034Abstract: The present invention provides novel condensation aerosols for the treatment of disease and/or intermittent or acute conditions. These condensation aerosols have little or no pyrolysis degradation products and are characterized by having an MMAD of between 1-3 microns. These aerosols are made by rapidly heating a substrate coated with a thin film of drug having a thickness of between 0.05 and 20 ?m, while passing a gas over the film, to form particles of a desirable particle size for inhalation. Kits comprising a drug and a device for producing a condensation aerosol are also provided. The device contained in the kit typically, has an element for heating the drug which is coated as a film on the substrate and contains a therapeutically effective dose of a drug when the drug is administered in aerosol form, and an element allowing the vapor to cool to form an aerosol. Also disclosed, are methods for using these aerosols and kits.Type: GrantFiled: November 13, 2013Date of Patent: September 13, 2016Assignee: ALEXZA PHARMACEUTICALS, INC.Inventors: Ron L. Hale, Craig C. Hodges, Peter M. Lloyd, Amy T. Lu, Daniel J. Myers, Joshua D. Rabinowitz, Martin J. Wensley, Jeffrey A. McKinney, Alejandro C. Zaffaroni
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Publication number: 20150057221Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I): wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R1, R1a, R2, R2a, R3, R3a, X, X1, X2, X3 have the meaning as indicated in the description and the claims and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer; and Z is a carrier group. The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.Type: ApplicationFiled: October 30, 2014Publication date: February 26, 2015Inventors: Felix Cleemann, Ulrich Hersel, Silvia Kaden, Harald Rau, Thomas Wegge
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Patent number: 8962610Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: June 29, 2012Date of Patent: February 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20140287050Abstract: The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.Type: ApplicationFiled: March 17, 2014Publication date: September 25, 2014Applicant: KemPharm, Inc.Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
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Publication number: 20140221616Abstract: The invention relates to compounds of Formula I, wherein R1, R2, and R3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from quetiapine. The invention also relates to conjugates of a quetiapine hapten and a protein.Type: ApplicationFiled: August 20, 2013Publication date: August 7, 2014Applicants: Ortho-Clinical Diagnostics, Inc., Janssen Pharmaceutica NVInventors: Matthew Garrett DONAHUE, Yong Gong, Rhys Salter, Eric Hryhorenko, Thomas R. DeCory, Bart Remmerie, Banumathi Sankaran
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Patent number: 8715699Abstract: The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.Type: GrantFiled: December 22, 2010Date of Patent: May 6, 2014Assignee: KemPharm, Inc.Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
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Publication number: 20140066618Abstract: The present invention relates to the inhalation delivery of aerosols containing small particles. Specifically, it relates to a method of forming an aerosol for use in inhalation therapy. The method involves: (a) heating a substrate coated with a composition comprising a drug to form a vapor, wherein the coated composition is in the form of a film less than 10 ?thick; and, (b) allowing the vapor to cool, thereby forming an aerosol, which is used in inhalation therapy. In another aspect, a method of forming an aerosol for use in inhalation therapy is provided, wherein the method comprises: (a) heating a substrate coated with a composition comprising a drug to form a vapor in less than 100 milliseconds, wherein the vapor has a mass greater than 0.Type: ApplicationFiled: November 11, 2013Publication date: March 6, 2014Inventors: Ron L. Hale, Craig C. Hodges, Peter M. Lloyd, Daniel Mufson, Daniel D. Rogers, Soonho Song, Martin J. Wensley, Daniel J. Myers, Jeffrey A. McKinney, Reynaldo J. Quintana, Joshua D. Rabinowitz
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Patent number: 8653257Abstract: Compounds the following formula: wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds.Type: GrantFiled: April 12, 2012Date of Patent: February 18, 2014Assignee: Astrazeneca ABInventors: Dean Brown, James R. Damewood, Phil Edwards, James Hulsizer, James Campbell Muir, M. Edward Pierson, Jr., Ashokkumar Bhikkappa Shenvi, Steven Wesolowski, Dan Widzowski, Michael Wood
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Publication number: 20140030329Abstract: Methods for treating insomnia in humans not suffering from any psychiatric disorders using quetiapine.Type: ApplicationFiled: May 10, 2011Publication date: January 30, 2014Inventor: Chui Yu Liu
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Publication number: 20140011988Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.Type: ApplicationFiled: February 14, 2013Publication date: January 9, 2014Inventors: Robert Deziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
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Publication number: 20130158007Abstract: The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided.Type: ApplicationFiled: February 19, 2013Publication date: June 20, 2013Applicant: KEMPHARM, INC.Inventor: KemPharm, Inc.
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Patent number: 8420807Abstract: The invention relates to a method for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo [b,f]-1,4-thiazepine and pharmaceutically acceptable salts thereof comprising the reaction of 1-[2-(hydroxyethoxy)-ethyl]piperazine with dibenzo[b,f][1,4]thiazepin-11-ylamine.Type: GrantFiled: January 30, 2009Date of Patent: April 16, 2013Assignee: Fermion OyInventors: Arne Grumann, Dzintra Muceniece, Otto Soidinsalo
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Patent number: 8394790Abstract: The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.Type: GrantFiled: October 25, 2007Date of Patent: March 12, 2013Assignee: Ramot at Tel-Aviv University Ltd.Inventors: Moshe Portnoy, Irit Gil-Ad, Avraham Weizman
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Patent number: 8389716Abstract: The present invention relates to a process for the synthesis of quetiapine. In particular, a process is provided for the synthesis of quetiapine of formula (A) comprising reacting dibenzo[b,f][1,4]thiazepin-11(10H)-one, intermediate (I) with phosphorous oxychloride to give 11-chlorodibenzo[b,f][1,4]thiazepine, intermediate (II) wherein the said reaction of intermediate (I) to intermediate (II) is performed in an organic solvent in the presence of a mixture of an organic base together with an inorganic base.Type: GrantFiled: January 30, 2009Date of Patent: March 5, 2013Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Siro Serafini, Filippo Tomasi, Marco Galvagni
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Patent number: 8389510Abstract: 11-piperazin-1-yldibenzo[b,f][1,4]thiazepine, compositions thereof, preparations thereof, formulations thereof, prodrugs thereof and pharmaceutical uses thereof.Type: GrantFiled: March 18, 2010Date of Patent: March 5, 2013Assignee: AstraZeneca ABInventors: Simon N. Black, Simon D. Broady, Alan S. Kirschner, James A. Osborn, Stewart D. Jolly, Dan B. Brown, Daniel Korey, Karen B. Main, Richard J. R. Creekmore, Jean M. Surian, Vivian Y. Bi, Peter Bernstein, James B. Campbell, Greg Christoph, Scott W. Grimm, Dan Widzowski, James Hulsizer, Phil Edwards
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Publication number: 20130053301Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aliphatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.Type: ApplicationFiled: January 21, 2011Publication date: February 28, 2013Applicant: Ascendis Pharma A/SInventors: Harald Rau, Torben Lessmann
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Publication number: 20120276168Abstract: The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized bu chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.Type: ApplicationFiled: December 22, 2010Publication date: November 1, 2012Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
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Publication number: 20120202991Abstract: Compounds the following formula: wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds.Type: ApplicationFiled: April 12, 2012Publication date: August 9, 2012Inventors: Dean Brown, James R. Damewood, Phil Edwards, James Hulsizer, James Campbell Muir, M. Edward Pierson, JR., Ashokkumar Bhikkappa Shenvi, Steven Wesolowski, Dan Widzowski, Michael Wood
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Publication number: 20120178738Abstract: The present invention relates to 11-(piperazin-1-yl)dibenzo[b,f][1,4]oxazapine compounds of the formula: where the variables are as defined herein, their salts and pharmaceutically acceptable compositions thereof. Methods of preparing these compounds are also described. These compounds may be used in the treatment of disorders such as schizophrenia, treatment resistant schizophrenia, bipolar disorder, psychotic depression, treatment resistant depression, schizophrenia-associated depression, treatment resistant OCD, autism, senile psychosis, psychotic dementia, L-DOPA induced psychosis, psychogenic polydipsia, psychotic symptoms of neurological disorders, sleep disorders.Type: ApplicationFiled: December 12, 2011Publication date: July 12, 2012Applicant: ARYX THERAPEUTICS, INC.Inventors: Cyrus Becker, Courtney Rubens, Jason Adams, Monica Palme, Pascal Druzgala
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Publication number: 20120165519Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: March 6, 2012Publication date: June 28, 2012Applicant: Cephalon, Inc.Inventors: Gulzar Ahmed, Henry Joseph Breslin, Jason Burke, Matthew A. Curry, James L. Diebold, Bruce Dorsey, Benjamin J. Dugan, Daming Feng, Diane E. Gingrich, Tao Guo, Keith S. Learn, Joseph G. Lisko, Rong-qiang Liu, Eugen Mesaros, Karen Milkiewicz, Gregory R. Ott, Jay P. Theroff, Tho V. Thieu, Rabindranath Tripathy, Theodore L. Underiner, Gregory J. Wells, Craig A. Zificsak
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Publication number: 20120095217Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.Type: ApplicationFiled: January 8, 2010Publication date: April 19, 2012Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
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Patent number: 8158618Abstract: Compounds the following formula: wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds.Type: GrantFiled: June 19, 2009Date of Patent: April 17, 2012Assignee: AstraZeneca ABInventors: Dean Brown, James R. Damewood, Phil Edwards, James Hulsizer, James Campbell Muir, M. Edward Pierson, Jr., Ashokkumar Bhikkappa Shenvi, Steven Wesolowski, Dan Widzowski, Michael Wood
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Publication number: 20120071649Abstract: The present invention relates to an improved process for the preparation of quetiapine and pharmaceutically acceptable salts. It also relates to improved process for the preparation of intermediates of quetiapine.Type: ApplicationFiled: March 4, 2010Publication date: March 22, 2012Applicant: RANBAXY LABORATORIES LIMITEDInventors: Venugopal Venkatarama Durvasula, Parendu Dhirajlal Rathod, Ram Chandra Aryan, Chandra Has Khanduri
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Patent number: 8101782Abstract: Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The compounds of the invention are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.Type: GrantFiled: February 4, 2008Date of Patent: January 24, 2012Assignee: Colucid Pharmaceuticals, Inc.Inventors: Nadia M. J. Rupniak, James F. White, Kazumi Shiosaki, J. David Leander, Shoucheng Du, Daniel J. Coughlin
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Patent number: 8101597Abstract: The present invention relates to novel and stable salt forms of quetiapine, processes for preparation, pharmaceutical compositions, and method of treating thereof. More particularly, the present invention provides novel acid addition salts of quetiapine wherein the acid counter ion is provided by an acid selected from the group consisting of benzene sulfonic acid, dibenzoyl-L-(+)-tartaric acid and di-p-toluoyl-L-(+)-tartaric acid. The present invention also provides novel polymorphic forms of quetiapine salts selected from the group consisting of quetiapine hydrobromide, quetiapine sulfate, quetiapine nitrate and quetiapine citrate.Type: GrantFiled: May 7, 2008Date of Patent: January 24, 2012Assignee: Actavis Group PTC EHFInventors: Girish Dixit, Anil Shahaji Khile, Jayesh Laljibhai Patel, Nitin Sharadchandra Pradhan, Jon Valgeirsson
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Patent number: 8101596Abstract: The invention relates to novel compounds and methods of using them for modulating sleep.Type: GrantFiled: March 25, 2009Date of Patent: January 24, 2012Assignee: Hypnion Inc.Inventors: Dale M. Edgar, David G. Hangauer, Michael Solomon
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Patent number: 8093237Abstract: The present invention relates to 11-(piperazin-1-yl)dibenzo[b,f][1,4 ]oxazapine compounds of the formula: where the variables are as defined herein, their salts and pharmaceutically acceptable compositions thereof. Methods of preparing these compounds are also described. These compounds may be used in the treatment of disorders such as schizophrenia, treatment resistant schizophrenia, bipolar disorder, psychotic depression, treatment resistant depression, schizophrenia-associated depression, treatment resistant OCD, autism, senile psychosis, psychotic dementia, L-DOPA induced psychosis, psychogenic polydipsia, psychotic symptoms of neurological disorders, sleep disorders.Type: GrantFiled: March 13, 2008Date of Patent: January 10, 2012Assignee: ARYx Therapeutics, Inc.Inventors: Cyrus Becker, Courtney Rubens, Jason Adams, Monica Palme, Pascal Druzgala
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Publication number: 20110280938Abstract: The present invention relates to sustained release pharmaceutical composition of quetiapine, and process for preparing such composition. More particularly, it relates to sustained release pharmaceutical composition of quetiapine comprising a non gelling agents such as carrageenan and pharmaceutically acceptable excipients.Type: ApplicationFiled: January 4, 2010Publication date: November 17, 2011Applicant: TORRENT PHARMACEUTICALS LIMITEDInventors: Navin Ishwarlal Vaya, Narendra Dulichand Soni, Baxis Rameshchandra Joshi
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Patent number: 8048876Abstract: The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][1,4]thiazepin-11(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo[bf][1,4]thiazepine. Thereafter, the 11-chloro-dibenzo[bf][1,4]thiazepine is reacted with 2-(2-piperazin-1-ylethoxy)-ethanol to yield, following several processing steps, quetiapine. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations.Type: GrantFiled: April 21, 2006Date of Patent: November 1, 2011Assignee: Medichem S.A.Inventors: Jordi Bosch I Lladó, Maria Carmen Burgarolas Montero, Iolanda Chamorro Gutiérrez
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Patent number: 8044038Abstract: The present invention relates to a process for preparing crystalline quetiapine hemifumarate, which comprises crystallizing or re-crystallizing quetiapine hemifumarate from a mixture of water and a water soluble alcohol.Type: GrantFiled: September 28, 2006Date of Patent: October 25, 2011Assignee: Fermion OyInventors: Petteri Rummakko, Arne Grumann, Soini Huhta, Tuomas Koiranen
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Patent number: 8044039Abstract: The present invention relates to a process for preparing and purifying crystalline quetiapine hemifumarate, which comprises preparing crystalline quetiapine hemifumarate via a crystalline salt, which is not a salt of fumaric acid.Type: GrantFiled: October 26, 2006Date of Patent: October 25, 2011Assignee: Fermion OyInventors: Arne Grumann, Soini Huhta, Petteri Rummakko, Viesturs Lusis
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Patent number: 8034805Abstract: A method for the preparation of salts of 2-[2-(4-dibenzo[b,fj[1,4]thiazepin-11-yl-1 -piperazinyl)ethoxy]ethanol (quetiapine) from the quetiapine base and the respective acid, wherein the salt is precipitated from a mixture of solvents, the mixture being either a mixture of an aromatic hydrocarbon and a ketone or ester, or that of an aromatic hydrocarbon, water and a ketone or ester. The salts of quetiapine are purified by partial crystallization, wherein only a part of the salt of quetiapine is dissolved in a C1 to C6 alcohol used.Type: GrantFiled: August 31, 2006Date of Patent: October 11, 2011Assignee: Farmak, A.S.Inventors: Pavel Hradil, Lubomir Kvapil, Roman Gabriel, Martin Grepl, Jan Novotny, Petr Slezar, Radek Melnicky
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Publication number: 20110237568Abstract: 11-piperazin-1-yldibenzo[b,f][1,4]thiazepine, compositions thereof, preparations thereof, formulations thereof, prodrugs thereof and pharmaceutical uses thereof.Type: ApplicationFiled: March 18, 2010Publication date: September 29, 2011Inventors: SIMON N. BLACK, SIMON D. BROADY, ALAN S. KIRSCHNER, JAMES A. OSBORN, STEWART D. JOLLY, DAN B. BROWN, DANIEL KOREY, KAREN B. MAIN, RICHARD J.R. CREEKMORE, JEAN M. SURIAN, VIVIAN Y. BI, PETER BERNSTEIN, JAMES B. CAMPBELL, GREG CHRISTOPH, SCOTT W. GRIMM, DAN WIDZOWSKI, JAMES HULSIZER, PHIL EDWARDS
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Publication number: 20110230657Abstract: The present invention relates to an improved process for preparing Quetiapine fumarate of formula (I).Type: ApplicationFiled: November 30, 2009Publication date: September 22, 2011Applicant: ALEMBIC LIMITEDInventors: Ravi Ponnaiah, Ashok Prasad, Dineshkumar Ramabhai Panchasara, Mitul Bipinchandra Patwa, Ketan Bharatendubhai Patel
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Publication number: 20110183963Abstract: The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating amino acids to quetiapine. The present technology also provides methods of treating patients, pharmaceutical compositions and methods of synthesizing conjugates of the present technology.Type: ApplicationFiled: December 22, 2010Publication date: July 28, 2011Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
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Publication number: 20110118460Abstract: The present invention relates to a process for the synthesis of quetiapine. In particular, a process is provided for the synthesis of quetiapine of formula (A) comprising reacting dibenzo[b,f][1,4]thiazepin-11(10H)-one, intermediate (I) with phosphorous oxychloride to give 11-chlorodibenzo[b,f][1,4]thiazepine, intermediate (II) wherein the said reaction of intermediate (I) to intermediate (II) is performed in an organic solvent in the presence of a mixture of an organic base together with an inorganic base.Type: ApplicationFiled: January 30, 2009Publication date: May 19, 2011Inventors: Siro Serafini, Filippo Tomasi, Marco Galvagni
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Publication number: 20110112290Abstract: The invention relates to a method for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f]-1,4-thiazepine and pharmaceutically acceptable salts thereof comprising the reaction of 1-[2-(hydroxyethoxy)-ethyl]piperazine with dibenzo[b,f][1,4]thiazepin-11-ylamine.Type: ApplicationFiled: January 30, 2009Publication date: May 12, 2011Applicant: FERMION OYInventors: Arne Grumann, Dzintra Muceniece, Otto Soidinsalo
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Patent number: 7902355Abstract: A process for the preparation of an 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine derivative, of general Formula (I), where A is hydrogen or a —(CH2)2—OH group or a —(CH2)2-0-(CH2)2—OH group, or of a salt thereof, comprises a step in which 10H-dibenzo[b,f][1,4]thiazepin-11-one is reacted with a piperazine derivative in the presence of a titanium alkoxide of general formula Ti(OR)4, where R is a straight or branched alkyl group, having from one to eight carbon atoms to obtain said Formula I derivative or a salt thereof. Where A is —CH2)2-0-(CH2)2—OH, then the piperazine derivative is 1-(2-(2-hydroxyethoxy)ethyl)piperazine and the 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine is quetiapine, (11-(4-(2-(2-hydroxyethoxy)ethyl)-1-piperazinyl)dibenzo[b,f][1,4]thiazepine). The process may comprise an additional step of reacting the quetiapine with fumaric acid to obtain quetiapine hemifumarate.Type: GrantFiled: December 21, 2005Date of Patent: March 8, 2011Assignee: Union Quimico-Farmaceutica S.A.Inventors: Alexander Christian Comely, Francesc Xavier Verdaguer Espaulella, Llorenç Rafecas Jané, Antonio Domingo Coto
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Publication number: 20110053848Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I), wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R1, R1a, R2, R2a, R3, R3a, X, X1, X2, X3 have the meaning as indicated in the description and the claims and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer; and Z is a carrier group. The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.Type: ApplicationFiled: January 30, 2009Publication date: March 3, 2011Applicant: ASCENDIS PHARMA ASInventors: Felix Cleemann, Ulrich Hersel, Silvia Kaden, Harald Rau, Thomas Wegge
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Patent number: 7863441Abstract: The present invention discloses a process for the preparation of quetiapine, which comprises the ring closure of a compound of the formula shown below, as well as novel intermediates in the process.Type: GrantFiled: September 23, 2004Date of Patent: January 4, 2011Assignee: Fermion OyInventors: Petteri Rummakko, Soini Huhta, Arne Grumann
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Patent number: 7863277Abstract: A transdermal composition that contains an antipsychotic is provided for the treatment of neuropsychiatric disorders. Also, provided are methods for preparing a topical antipsychotic composition. Methods for treating neuropsychiatric disorders, including schizophrenia, are further disclosed. The transdermal composition includes a therapeutically effective amount of an antipsychotic in an amount sufficient to treat neuropsychiatric disorders in a pharmaceutically acceptable carrier.Type: GrantFiled: March 7, 2006Date of Patent: January 4, 2011Assignee: Medcara, L.L.C.Inventor: Craig Herman
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Patent number: 7858777Abstract: The present invention discloses a process for the preparation of quetiapine, which comprises the ring closure and deprotection of a compound of the formula (I), as well as novel intermediates in the process.Type: GrantFiled: September 23, 2004Date of Patent: December 28, 2010Assignee: Fermion OyInventors: Leif Hilden, Arne Grumann, Soini Huhta, Petteri Rummakko
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Publication number: 20100311718Abstract: The present invention provides methods for treating depression symptoms associated with bipolar disorder.Type: ApplicationFiled: August 17, 2010Publication date: December 9, 2010Applicant: AstraZeneca ABInventors: Brian Ault, Gilbert Block, Martin Brecher, Wayne MacFadden, Robin McCoy, Margaret Minkwitz, Jamie Mullen, Ellis Wilson
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Patent number: 7847094Abstract: Disclosed herein is an industrial preparation of Quetiapine by the reaction of 11-piperazinyldibenzo[b,f][1,4]-thiazepine or its salt with 2-(2-chloroethoxy)ethanol in presence of an organic or inorganic base under neat or aqueous condition to form 11-[4-{2-(2-hydroxyethoxy)ethyl}-1-piperazinyl]dibenzo[b,f]-[1,4]thiazepine. The quetiapine free base obtained is further converted to its hemi-fumarate salt.Type: GrantFiled: June 8, 2007Date of Patent: December 7, 2010Assignee: IPCA Laboratories LimitedInventors: Ashok Kumar, Dharmendra Singh, Swapnali Hemant Patil, Ganesh Devidas Mahale, Uttamrao Arjunrao Sawant, Balasaheb Ganpat Jadhav, Ragneshkumar Rana
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Publication number: 20100278878Abstract: The present invention relates to novel and stable salt forms of quetiapine, processes for preparation, pharmaceutical compositions, and method of treating thereof. More particularly, the present invention provides novel acid addition salts of quetiapine wherein the acid counter ion is provided by an acid selected from the group consisting of benzene sulfonic acid, dibenzoyl-L-(+)-tartaric acid and di-p-toluoyl-L-(+)-tartaric acid. The present invention also provides novel polymorphic forms of quetiapine salts selected from the group consisting of quetiapine hydrobromide, quetiapine sulfate, quetiapine nitrate and quetiapine citrate.Type: ApplicationFiled: May 7, 2008Publication date: November 4, 2010Applicant: ACTAVIS GROUP PTC EHFInventors: Girish Dixit, Anil Shahaji Khile, Jayesh Laljibhai Patel, Nitin Sharadchandra Pradhan, Jon Valgeirsson
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Patent number: 7807827Abstract: The invention relates to a procedure for preparing quetiapine by reaction between a compound of formula (II) and a compound of formula (III), in which X means a leaving group and P a protective group of alcohols resistant to alkaline conditions, in the presence of a base, followed by a step of deprotection and, optionally, obtaining a pharmaceutically acceptable salt thereof. Said procedure permits the obtaining of quetiapine with a high degree of purity under soft temperature conditions, with short reaction times and avoiding the use of toxic solvents.Type: GrantFiled: July 27, 2004Date of Patent: October 5, 2010Assignee: Inke, S.A.Inventors: Salvador Puig Torres, Reyes Herbera Espinal, Pere Dalmases Barjoan
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Patent number: 7807828Abstract: The invention relates to novel compounds and methods of using them for modulating sleep.Type: GrantFiled: August 10, 2006Date of Patent: October 5, 2010Assignee: Hypnion, Inc.Inventors: Michael Solomon, Dale Edgar, David Hangauer, Kazumi Shiosaki, James White
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Publication number: 20100168416Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: March 9, 2010Publication date: July 1, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Publication number: 20100129473Abstract: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuropsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.Type: ApplicationFiled: November 18, 2009Publication date: May 27, 2010Applicant: ACADIA Pharmaceuticals, Inc.Inventors: Fredrik Ek, Roger Olsson, Jörgen Ohlsson