Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 540/551)
  • Patent number: 9440034
    Abstract: 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: Grant
    Filed: November 13, 2013
    Date of Patent: September 13, 2016
    Assignee: 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
  • Publication number: 20150057221
    Abstract: 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: Application
    Filed: October 30, 2014
    Publication date: February 26, 2015
    Inventors: Felix Cleemann, Ulrich Hersel, Silvia Kaden, Harald Rau, Thomas Wegge
  • Patent number: 8962610
    Abstract: 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: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: 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
  • Publication number: 20140287050
    Abstract: 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: Application
    Filed: March 17, 2014
    Publication date: September 25, 2014
    Applicant: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
  • Publication number: 20140221616
    Abstract: 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: Application
    Filed: August 20, 2013
    Publication date: August 7, 2014
    Applicants: Ortho-Clinical Diagnostics, Inc., Janssen Pharmaceutica NV
    Inventors: Matthew Garrett DONAHUE, Yong Gong, Rhys Salter, Eric Hryhorenko, Thomas R. DeCory, Bart Remmerie, Banumathi Sankaran
  • Patent number: 8715699
    Abstract: 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: Grant
    Filed: December 22, 2010
    Date of Patent: May 6, 2014
    Assignee: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
  • Publication number: 20140066618
    Abstract: 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: Application
    Filed: November 11, 2013
    Publication date: March 6, 2014
    Inventors: 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
  • Patent number: 8653257
    Abstract: 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: Grant
    Filed: April 12, 2012
    Date of Patent: February 18, 2014
    Assignee: Astrazeneca AB
    Inventors: 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
  • Publication number: 20140030329
    Abstract: Methods for treating insomnia in humans not suffering from any psychiatric disorders using quetiapine.
    Type: Application
    Filed: May 10, 2011
    Publication date: January 30, 2014
    Inventor: Chui Yu Liu
  • Publication number: 20140011988
    Abstract: 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: Application
    Filed: February 14, 2013
    Publication date: January 9, 2014
    Inventors: Robert Deziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
  • Publication number: 20130158007
    Abstract: 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: Application
    Filed: February 19, 2013
    Publication date: June 20, 2013
    Applicant: KEMPHARM, INC.
    Inventor: KemPharm, Inc.
  • Patent number: 8420807
    Abstract: 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: Grant
    Filed: January 30, 2009
    Date of Patent: April 16, 2013
    Assignee: Fermion Oy
    Inventors: Arne Grumann, Dzintra Muceniece, Otto Soidinsalo
  • Patent number: 8394790
    Abstract: The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: March 12, 2013
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Moshe Portnoy, Irit Gil-Ad, Avraham Weizman
  • Patent number: 8389510
    Abstract: 11-piperazin-1-yldibenzo[b,f][1,4]thiazepine, compositions thereof, preparations thereof, formulations thereof, prodrugs thereof and pharmaceutical uses thereof.
    Type: Grant
    Filed: March 18, 2010
    Date of Patent: March 5, 2013
    Assignee: AstraZeneca AB
    Inventors: 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
  • Patent number: 8389716
    Abstract: 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: Grant
    Filed: January 30, 2009
    Date of Patent: March 5, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Siro Serafini, Filippo Tomasi, Marco Galvagni
  • Publication number: 20130053301
    Abstract: 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: Application
    Filed: January 21, 2011
    Publication date: February 28, 2013
    Applicant: Ascendis Pharma A/S
    Inventors: Harald Rau, Torben Lessmann
  • Publication number: 20120276168
    Abstract: 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: Application
    Filed: December 22, 2010
    Publication date: November 1, 2012
    Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
  • Publication number: 20120202991
    Abstract: 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: Application
    Filed: April 12, 2012
    Publication date: August 9, 2012
    Inventors: 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
  • Publication number: 20120178738
    Abstract: 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: Application
    Filed: December 12, 2011
    Publication date: July 12, 2012
    Applicant: ARYX THERAPEUTICS, INC.
    Inventors: Cyrus Becker, Courtney Rubens, Jason Adams, Monica Palme, Pascal Druzgala
  • Publication number: 20120165519
    Abstract: 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: Application
    Filed: March 6, 2012
    Publication date: June 28, 2012
    Applicant: 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
  • Publication number: 20120095217
    Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.
    Type: Application
    Filed: January 8, 2010
    Publication date: April 19, 2012
    Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
  • Patent number: 8158618
    Abstract: 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: Grant
    Filed: June 19, 2009
    Date of Patent: April 17, 2012
    Assignee: AstraZeneca AB
    Inventors: 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
  • Publication number: 20120071649
    Abstract: 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: Application
    Filed: March 4, 2010
    Publication date: March 22, 2012
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Venugopal Venkatarama Durvasula, Parendu Dhirajlal Rathod, Ram Chandra Aryan, Chandra Has Khanduri
  • Patent number: 8101596
    Abstract: The invention relates to novel compounds and methods of using them for modulating sleep.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: January 24, 2012
    Assignee: Hypnion Inc.
    Inventors: Dale M. Edgar, David G. Hangauer, Michael Solomon
  • Patent number: 8101597
    Abstract: 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: Grant
    Filed: May 7, 2008
    Date of Patent: January 24, 2012
    Assignee: Actavis Group PTC EHF
    Inventors: Girish Dixit, Anil Shahaji Khile, Jayesh Laljibhai Patel, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • Patent number: 8101782
    Abstract: 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: Grant
    Filed: February 4, 2008
    Date of Patent: January 24, 2012
    Assignee: Colucid Pharmaceuticals, Inc.
    Inventors: Nadia M. J. Rupniak, James F. White, Kazumi Shiosaki, J. David Leander, Shoucheng Du, Daniel J. Coughlin
  • Patent number: 8093237
    Abstract: 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: Grant
    Filed: March 13, 2008
    Date of Patent: January 10, 2012
    Assignee: ARYx Therapeutics, Inc.
    Inventors: Cyrus Becker, Courtney Rubens, Jason Adams, Monica Palme, Pascal Druzgala
  • Publication number: 20110280938
    Abstract: 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: Application
    Filed: January 4, 2010
    Publication date: November 17, 2011
    Applicant: TORRENT PHARMACEUTICALS LIMITED
    Inventors: Navin Ishwarlal Vaya, Narendra Dulichand Soni, Baxis Rameshchandra Joshi
  • Patent number: 8048876
    Abstract: 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: Grant
    Filed: April 21, 2006
    Date of Patent: November 1, 2011
    Assignee: Medichem S.A.
    Inventors: Jordi Bosch I Lladó, Maria Carmen Burgarolas Montero, Iolanda Chamorro Gutiérrez
  • Patent number: 8044039
    Abstract: 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: Grant
    Filed: October 26, 2006
    Date of Patent: October 25, 2011
    Assignee: Fermion Oy
    Inventors: Arne Grumann, Soini Huhta, Petteri Rummakko, Viesturs Lusis
  • Patent number: 8044038
    Abstract: 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: Grant
    Filed: September 28, 2006
    Date of Patent: October 25, 2011
    Assignee: Fermion Oy
    Inventors: Petteri Rummakko, Arne Grumann, Soini Huhta, Tuomas Koiranen
  • Patent number: 8034805
    Abstract: 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: Grant
    Filed: August 31, 2006
    Date of Patent: October 11, 2011
    Assignee: Farmak, A.S.
    Inventors: Pavel Hradil, Lubomir Kvapil, Roman Gabriel, Martin Grepl, Jan Novotny, Petr Slezar, Radek Melnicky
  • Publication number: 20110237568
    Abstract: 11-piperazin-1-yldibenzo[b,f][1,4]thiazepine, compositions thereof, preparations thereof, formulations thereof, prodrugs thereof and pharmaceutical uses thereof.
    Type: Application
    Filed: March 18, 2010
    Publication date: September 29, 2011
    Inventors: 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
  • Publication number: 20110230657
    Abstract: The present invention relates to an improved process for preparing Quetiapine fumarate of formula (I).
    Type: Application
    Filed: November 30, 2009
    Publication date: September 22, 2011
    Applicant: ALEMBIC LIMITED
    Inventors: Ravi Ponnaiah, Ashok Prasad, Dineshkumar Ramabhai Panchasara, Mitul Bipinchandra Patwa, Ketan Bharatendubhai Patel
  • Publication number: 20110183963
    Abstract: 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: Application
    Filed: December 22, 2010
    Publication date: July 28, 2011
    Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
  • Publication number: 20110118460
    Abstract: 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: Application
    Filed: January 30, 2009
    Publication date: May 19, 2011
    Inventors: Siro Serafini, Filippo Tomasi, Marco Galvagni
  • Publication number: 20110112290
    Abstract: 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: Application
    Filed: January 30, 2009
    Publication date: May 12, 2011
    Applicant: FERMION OY
    Inventors: Arne Grumann, Dzintra Muceniece, Otto Soidinsalo
  • Patent number: 7902355
    Abstract: 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: Grant
    Filed: December 21, 2005
    Date of Patent: March 8, 2011
    Assignee: Union Quimico-Farmaceutica S.A.
    Inventors: Alexander Christian Comely, Francesc Xavier Verdaguer Espaulella, Llorenç Rafecas Jané, Antonio Domingo Coto
  • Publication number: 20110053848
    Abstract: 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: Application
    Filed: January 30, 2009
    Publication date: March 3, 2011
    Applicant: ASCENDIS PHARMA AS
    Inventors: Felix Cleemann, Ulrich Hersel, Silvia Kaden, Harald Rau, Thomas Wegge
  • Patent number: 7863441
    Abstract: 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: Grant
    Filed: September 23, 2004
    Date of Patent: January 4, 2011
    Assignee: Fermion Oy
    Inventors: Petteri Rummakko, Soini Huhta, Arne Grumann
  • Patent number: 7863277
    Abstract: 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: Grant
    Filed: March 7, 2006
    Date of Patent: January 4, 2011
    Assignee: Medcara, L.L.C.
    Inventor: Craig Herman
  • Patent number: 7858777
    Abstract: 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: Grant
    Filed: September 23, 2004
    Date of Patent: December 28, 2010
    Assignee: Fermion Oy
    Inventors: Leif Hilden, Arne Grumann, Soini Huhta, Petteri Rummakko
  • Publication number: 20100311718
    Abstract: The present invention provides methods for treating depression symptoms associated with bipolar disorder.
    Type: Application
    Filed: August 17, 2010
    Publication date: December 9, 2010
    Applicant: AstraZeneca AB
    Inventors: Brian Ault, Gilbert Block, Martin Brecher, Wayne MacFadden, Robin McCoy, Margaret Minkwitz, Jamie Mullen, Ellis Wilson
  • Patent number: 7847094
    Abstract: 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: Grant
    Filed: June 8, 2007
    Date of Patent: December 7, 2010
    Assignee: IPCA Laboratories Limited
    Inventors: Ashok Kumar, Dharmendra Singh, Swapnali Hemant Patil, Ganesh Devidas Mahale, Uttamrao Arjunrao Sawant, Balasaheb Ganpat Jadhav, Ragneshkumar Rana
  • Publication number: 20100278878
    Abstract: 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: Application
    Filed: May 7, 2008
    Publication date: November 4, 2010
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Girish Dixit, Anil Shahaji Khile, Jayesh Laljibhai Patel, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • Patent number: 7807827
    Abstract: 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: Grant
    Filed: July 27, 2004
    Date of Patent: October 5, 2010
    Assignee: Inke, S.A.
    Inventors: Salvador Puig Torres, Reyes Herbera Espinal, Pere Dalmases Barjoan
  • Patent number: 7807828
    Abstract: The invention relates to novel compounds and methods of using them for modulating sleep.
    Type: Grant
    Filed: August 10, 2006
    Date of Patent: October 5, 2010
    Assignee: Hypnion, Inc.
    Inventors: Michael Solomon, Dale Edgar, David Hangauer, Kazumi Shiosaki, James White
  • Publication number: 20100168416
    Abstract: 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: Application
    Filed: March 9, 2010
    Publication date: July 1, 2010
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
  • Publication number: 20100129473
    Abstract: 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: Application
    Filed: November 18, 2009
    Publication date: May 27, 2010
    Applicant: ACADIA Pharmaceuticals, Inc.
    Inventors: Fredrik Ek, Roger Olsson, Jörgen Ohlsson
  • Patent number: 7713956
    Abstract: Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH—CH2C?CH; R is hydrogen, halogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, C5-C6 cycloalkyl; R1 is 1-peperazinyl, 1-homopiperazinyl and 1-piperidinyl; R2 is hydrogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, CH?NOH,CH2OH. The formula (I) compounds are endowed with characteristic atypical anti-psychotic activity, and are therefore useful as medicaments, in particular for the treatment and prevention of schizophrenia, paranoid states, manic-depressive states, disorders of the affective sphere, social regression, personality regression, and hallucinations. Said compounds also present advantageous pharmacokinetic properties.
    Type: Grant
    Filed: April 28, 2005
    Date of Patent: May 11, 2010
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Paolo Carminati, Maria Assunta Di Cesare, Orlando Ghirardi, Patrizia Minetti, Maria Ornella Tinti