Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/75)
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Patent number: 8362279Abstract: A process for the preparation of pure Duloxetine hydrochloride comprises the steps of: a) reacting 1-(thiophen-2-yl)ethanone with dimethylamine hydrochloride, b) purifying the component in a solvent, c) reducing the component with an alkali metal borohydride, d) resolving the compound with a chiral acid, and treating the obtained compound with weak inorganic base, e) reacting the compound to give Duloxetine oxalate salt and f) converting the Duloxetine salt into its hydrochloride salt. Further the purifications of the obtained compound and of two intermediate products are described.Type: GrantFiled: January 4, 2007Date of Patent: January 29, 2013Assignee: MSN Laboratories LimitedInventors: Manne Satyanarayana Reddy, Muppa Kishore Kumar, Srinivasan Thirumalai Rajan, Durgadas Shyla Prasad
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Publication number: 20130023463Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: April 19, 2012Publication date: January 24, 2013Applicant: ABBOTT LABORATORIESInventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Publication number: 20130005992Abstract: The present invention provides a method for producing an N-monoalkyl-3-hydroxy-3-arylpropylamine compound represented by Formula (2): wherein Ar represents an optionally substituted aryl or an optionally substituted heteroaryl, R represents an optionally substituted C1-5 alkyl, and * represents an asymmetric carbon atom; the method comprising:reacting, in the presence of an asymmetric reduction catalyst, hydrogen gas with an N-benzyl-N-monoalkyl-3-oxo-3-arylpropenylamine compound represented by Formula (1): wherein Ar and R are as defined above. The present invention allows an optically active N-monoalkyl-3-hydroxy-3-arylpropylamine compound to be produced easily and inexpensively under industrially advantageous conditions.Type: ApplicationFiled: March 23, 2011Publication date: January 3, 2013Applicant: SUMITOMO SEIKA CHEMICALS CO., LTD.Inventors: Kenji Kogami, Shuzo Satake
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Patent number: 8344165Abstract: An isolated and pure crystalline rotigotine base of polymorph Form I, and processes for producing the crystalline rotigotine base are disclosed. Also disclosed is a transdermal patch for the delivery of rotigotine base using the disclosed isolated and pure form of rotigotine base, which can be used in treatment of Parkinson's Disease and other disorders ameliorated or treated by rotigotine, including restless leg syndrome.Type: GrantFiled: May 28, 2008Date of Patent: January 1, 2013Assignee: CHEMAGIS Ltd.Inventors: Sonia Krivonos, Alex Weisman
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Publication number: 20120269724Abstract: The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.Type: ApplicationFiled: December 13, 2011Publication date: October 25, 2012Applicant: President and Fellows of Harvard CollegeInventors: Ashfaq Mahmood, Alun G. Jones, Naengnoi Limpa-Amara, Yijie Peng, Zeynep Akgun
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Patent number: 8283376Abstract: The invention relates to the use of substituted 2-aminotetralins of general formula (I) as a medicament for the preventive treatment of Parkinson's disease.Type: GrantFiled: December 23, 2004Date of Patent: October 9, 2012Assignee: UCB Pharma GmbHInventors: Dieter Scheller, Frank Dressen
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Patent number: 8278463Abstract: The present invention relates to a process for the preparation of pure Duloxetine hydrochloride. The present invention further relates to duloxetine hydrochloride substantially free of residual hydrochloric acid.Type: GrantFiled: April 6, 2009Date of Patent: October 2, 2012Assignee: Ranbaxy Laboratories LimitedInventors: Sujoy Biswas, Keya Karanjai
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Patent number: 8258338Abstract: A process for the preparation of N-monosubstituted ?-aminoalcohol sulfonates of formula (Ia), (Ib): wherein R1 is C6-20-aryl or C4-12-heteroaryl, each optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, R2 is C1-4-alkyl or C6-20-aryl, each aryl optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups and wherein R3 is selected from the group consisting of C1-18-alkyl, C6-20-cycloalkyl, C6-20-aryl and C7-20-aralkyl residues. The process has the steps of (a) reacting a methyl ketone, a primary amine, formaldehyde and a sulfonic acid, at a pressure above 1.5 bar, optionally in a organic solvent, the organic solvent optionally containing water, to afford N-monosubstituted ?-aminoketone sulfonates of formula (II): wherein R1, R2 and R3 are as defined above, and (b) asymmetrically hydrogenating.Type: GrantFiled: February 14, 2006Date of Patent: September 4, 2012Assignee: Lonza AGInventors: Walter Brieden, Martin Clausen, John McGarrity, Hanspeter Mettler, Colette Mettler, legal representative, Dominique Michel
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Publication number: 20120220590Abstract: Compounds of formula (I) and pharmaceutical compositions containing them are described. The use of the compounds and compositions are also described.Type: ApplicationFiled: July 30, 2010Publication date: August 30, 2012Inventors: Pravin S. Thombare, Amitgiri Goswami, Edouard Zamaratski, Tomas Hansson, Thomas Norin
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Publication number: 20120205638Abstract: In OLEDs, improved efficiency is obtained by compounds which can form inter alia electron injection layers of the formula (I) wherein R1 is a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with one or more C1-C4 alkyl, alkoxy or cyano; R2 and R3 together form a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with C1-C4 alkyl, alkoxy or cyano; R4 is hydrogen, C1-C4 alkyl or aryl; and Ar is monocyclic, bicyclic or tricyclic aryl or heteroaryl which is optionally substituted with one or more C1-C4-alkyl or alkoxy groups, or an oligomer thereof.Type: ApplicationFiled: April 27, 2012Publication date: August 16, 2012Applicant: Merck Patent GmbHInventors: Poopathy Kathirgamanathan, Yun Fu Chan
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Publication number: 20120202869Abstract: The invention provides a pharmaceutical composition of duloxetine or its pharmaceutically equivalent derivatives like salts, isomers, complexes, polymorphs, hydrates or esters thereof and at least one buffering agent. The duloxetine or its pharmaceutically equivalent derivative is present from about 2 mg to approximately 200 mg; and the buffering agent is present in an amount of approximately 0.1 mEq to approximately 2.5 mEq per mg of duloxetine. Also provided is a method for treating of major depressive disorder and or diabetic peripheral neuropathic pain comprising administering to a mammal in need of such treatment a therapeutically effective amount of a composition.Type: ApplicationFiled: January 10, 2012Publication date: August 9, 2012Applicant: WOCKHARDT LTD.Inventor: Ramesh Sesha
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Publication number: 20120202867Abstract: Compounds of formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: ApplicationFiled: October 14, 2010Publication date: August 9, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Harald Walter, Daniel Stierli
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Publication number: 20120196917Abstract: The invention provides for the first time an oral liquid composition of duloxetine or its pharmaceutically equivalent derivatives like salts, isomers, complexes, polymorphs, hydrates or esters thereof. The duloxetine or its pharmaceutically equivalent derivative is present from about 2 mg to approximately 200 mg; and a buffering agent was used to stabilize the acid sensitive duloxetine. The composition has duloxetine from about 0.1 mEq to about 2.5 mEq per mg of duloxetine. The invention further discloses an oral liquid composition of duloxetine or its pharmaceutically equivalent derivative wherein the degradation product 1-Naphthol is less than 0.01%. Also provided is a method for treating of major depressive disorder and or diabetic peripheral neuropathic pain comprising administering to a mammal in need of such treatment a therapeutically effective amount of a composition.Type: ApplicationFiled: April 10, 2012Publication date: August 2, 2012Applicant: WOCKHARDT LTD.Inventor: Ramesh Sesha
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Patent number: 8232414Abstract: The present invention relates to a novel polymorphic form of rotigotine characterized by at least one of the following powder X-ray diffraction peaks: 12.04, 13.68, 17.72 and 19.01±0.2 (° 2?), measured with a Cu—K? irradiation (1.54060 ?), and a process for production thereof, which is useful for the manufacture of a stable medicament for treating or alleviating symptoms of Parkinson's disease and other dopamine-related disorders.Type: GrantFiled: November 26, 2008Date of Patent: July 31, 2012Assignee: UCB Pharma GmbHInventors: Hans-Michael Wolff, Luc Quere, Jens Riedner
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Publication number: 20120190869Abstract: The present invention provides an (S)-methylhydroxylaminopropanol compound and the (S)-methylhydroxylaminopropanol compound of the present invention is used as an intermediate for preparation of (S)-(?)-3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing (S)-(+3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol compound is used as an intermediate.Type: ApplicationFiled: March 30, 2012Publication date: July 26, 2012Applicant: SCI PHARMTECH, INC.Inventors: Bo-Fong CHEN, Jinun-Ban YEH, Weichyun WONG
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Publication number: 20120190725Abstract: The present disclosure concerns a compound, or a pharmaceutically acceptable salt thereof, having a formula: where at least one of R1-R4 is a heterocycle, at least one of R1-R4 is an aryl group coupled to the ring by a linker atom, functional group, or other moiety, or where none of R1-R4 is an amide, and any and all combinations thereof. Remaining R1-R4 substituents independently are aliphatic, substituted aliphatic, amine, substituted amine, aryl, substituted aryl, cyclic, substituted cyclic, halide, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, hydrogen or hydroxyl. A method for treating a subject also is provided comprising administering a disclosed compound or compounds, or a prodrug that is converted into the disclosed compound or compounds, or a composition comprising the compound, compounds, or prodrugs thereof, to a subject. A method for making disclosed compounds also is provided.Type: ApplicationFiled: January 20, 2012Publication date: July 26, 2012Inventors: James David White, David T. Wong, David B. Chan, Jongtae Yang, Rajan Juniku
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Patent number: 8207356Abstract: A method for the preparation of a duloxetine hydrochloride salt from a duloxetine base, comprising the steps of: reacting duloxetine base with concentrated hydrochloric acid in ethylmethylketone; and crystallizing duloxetine hydrochloride salt from said concentrated hydrochloric acid in ethylmethylketone.Type: GrantFiled: October 5, 2011Date of Patent: June 26, 2012Assignee: Zentiva k.s.Inventors: Ludek Ridvan, Kamal Jarrah, Josef Cinibulk, Monika Zatopkova, Lukas Placek
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Patent number: 8183281Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.Type: GrantFiled: June 4, 2008Date of Patent: May 22, 2012Assignee: Novartis AGInventors: Neil John Press, Simon James Watson
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Patent number: 8168805Abstract: The present invention provides an (S)-methylhydroxylaminopropanol derivative and the (S)-methylhydroxylaminopropanol derivative of the present invention is used as an intermediate for preparation of (S)-(?)-3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing (S)-(?)-3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol derivative is used as an intermediate.Type: GrantFiled: May 15, 2008Date of Patent: May 1, 2012Assignee: SCI Pharmtech, IncInventors: Bo-Fong Chen, Jinun-Ban Yeh, Weichyun Wong
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Publication number: 20120101327Abstract: The present invention concerns an apparatus and a method for stimulating brain tissue with pulsed electromagnetic fields weaker than the limit for elicitation of the action potentials of the cells of the tissue to be stimulated, the apparatus comprising: at least one electrically conducting coil positioned at a bitemporal position such that hippocampus is stimulated by at least one magnetic field upon supplying a pulse to said coil as well as a coil positioned at a occipital and parietal position; and a pulse generation means operationally connected to said at least one coil for supplying a series of current pulses for conduction, allowing generation of pulsed electromagnetic fields sufficiently strong to cause protein activation, and weaker than the limit for elicitation of the action potentials of the cells of the tissue to be stimulated.Type: ApplicationFiled: June 22, 2010Publication date: April 26, 2012Inventors: Steen Dissing, Mogens Unden
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Publication number: 20120095024Abstract: The present invention provides novel compounds that inhibit cell proliferation and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition comprising a compound of the invention and a second therapeutic agent or radiation useful for the treatment or prevention of the mentioned diseases or disorders. In a first aspect the present invention relates to a compound having a structure according to formula (I).Type: ApplicationFiled: December 30, 2009Publication date: April 19, 2012Applicants: Elara Pharmaceuticals GmbH, European Molecular Biology Laboratory (EMBL)Inventors: Jorge Alonson, Arantxa Encionas Lopez, Marcel Muelbaler, Lochen Ammenn, Bernd Vendt, Joe Lewis, Christoph Schultes, Bernd Janssen
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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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Publication number: 20120095239Abstract: The present invention relates to a process for the preparation of Duloxetine hydrochloride of formula (I).Type: ApplicationFiled: March 5, 2010Publication date: April 19, 2012Applicant: ALEMBIC PHARMACEUTICALS LIMITEDInventors: Ravi Ponnaiah, Ashok Prasad, Killol Patel, Hitarth Harshendu Acharya
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Patent number: 8148549Abstract: The present invention provides a (S)-methylhydroxylaminopropanol derivative as an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine. The present invention also provides a process for preparing (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol derivative is used as an intermediate.Type: GrantFiled: March 12, 2009Date of Patent: April 3, 2012Assignee: SCI Pharmtech, Inc.Inventors: Bo-Fong Chen, Jinun-Ban Yeh, Wei-Chyun Wong
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Publication number: 20120041038Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.Type: ApplicationFiled: October 21, 2011Publication date: February 16, 2012Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
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Publication number: 20120041039Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.Type: ApplicationFiled: October 21, 2011Publication date: February 16, 2012Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
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Publication number: 20120029212Abstract: A method for the preparation of a duloxetine hydrochloride salt from a duloxetine base, comprising the steps of: reacting duloxetine base with concentrated hydrochloric acid in ethylmethylketone; and crystallizing duloxetine hydrochloride salt from said concentrated hydrochloric acid in ethylmethylketone.Type: ApplicationFiled: October 5, 2011Publication date: February 2, 2012Inventors: Ludek RIDVAN, Kamal Jarrah, Josef Cinibulk, Monika Zatopkova, Lukas Placek
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Publication number: 20120029048Abstract: The method of treating patients by administering N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea for treatment of leukotriene related pathologies and compositions for this use.Type: ApplicationFiled: February 10, 2011Publication date: February 2, 2012Applicant: VIA Pharmaceuticals, Inc.Inventors: Rebecca Taub, Tilmann Brotz, John Franc, Larry Cohen, Hemantkumar H. Patel, Sanjay R. Chemburkar, David P. Sawick
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Publication number: 20120015911Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: September 20, 2011Publication date: January 19, 2012Applicant: Bellus Health Inc.Inventors: 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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Patent number: 8093407Abstract: Crystalline duloxetine hydrochloride, compositions containing the same and methods for the production thereof.Type: GrantFiled: September 10, 2010Date of Patent: January 10, 2012Assignees: Arrow International Limited, Chongqing Shenghuaxi Pharmaceutical Co. LtdInventors: Wei Ping Jiang, Chun Rong Jia
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Publication number: 20110313176Abstract: Provided herein are convenient, industrially advantageous and environmentally friendly processes for the preparation of (?)-(S)-5-hydroxy-2-[N-n-propyl-N-2-(2-thienyl)ethylamino]tetralin (rotigotine) or a pharmaceutically acceptable salt thereof. Provided further herein is a highly pure rotigotine or a pharmaceutically acceptable salt thereof substantially free of impurities, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure rotigotine or a pharmaceutically acceptable salt thereof substantially free of impurities.Type: ApplicationFiled: December 22, 2009Publication date: December 22, 2011Applicant: ACTAVIS GROUP PTC EHFInventors: Mayur Devjibhai Khunt, Shrikant Varma, Nilesh Sudhir Patil, Haushabhau Shivaji Pagire, Nitin Sharadchandra Pradhan
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Publication number: 20110306776Abstract: The present invention describes a novel process for the preparation of (6S)-(?)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine) comprising: (a) acetylating (S)-(?)-5-hydroxy-N-n-propyl-2-aminotetraline to afford the acetate; (b) reacting this acetate, (?)-5-acetoxy-N-n-propyl-2-aminotetraline, with 2-(2-thienyl)ethanol 2-nitrobenzenesul-fonate; (d) hydrolyzing (6S)-(?)-1-acetoxy-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthalene to afford (6S)-(?)-5,6,7,8-tetrahydro-6-[propyl-(2-thienypethyl]amino-1-naphthol (Rotigotine) and (d) purifying rotigotine either by the acetylation reaction and subsequent hydrolysis of the formed acetate or by salification of rotigotine through hydrochloride or hydrobromide formation and subsequent base release. Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson's disease.Type: ApplicationFiled: December 9, 2009Publication date: December 15, 2011Applicant: INTERQUIM, S.A.Inventors: Marta Pomares, Francisco Marquillas
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Patent number: 8071791Abstract: A method of preparation of (S)-N-methyl-3-(1-naphthyloxy)-3-(2-mienyl)propylamine of Formula (I) and its pharmaceutically acceptable salts, comprising a) reaction of (RS)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with optically active D-tartaric acid or an acid salt derived from D-tartaric acid forming a mixture of diastereoisomeric salts of N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine and D-tartaric acid (2:1), b) isolation of the salt (S)-N,N-dimethyl-3-(naphthyloxy) -3-(2-thienyl)propylamine/D-tartrate (2:1) from the mixture of diastereoisomeric salts in an organic solvent, water or a mixture thereof and release of (S)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine by action of an inorganic or organic base, c) demethylation of (S)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine by action of an alkylchloroformate of formula ClCOOR (R=C1-C5 alkyl, or C6-C12 aryl or alkylraryl), especially phenyl, ethyl or methyl chloroformate, and d) hydrolytic release of the duloxetType: GrantFiled: December 22, 2006Date of Patent: December 6, 2011Assignee: Zentiva k.s.Inventors: Ludek Ridvan, Kamal Jarrah, Josef Cinibulk, Monika Zatopkova, Lukas Placek
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Publication number: 20110281924Abstract: Compounds of formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: ApplicationFiled: January 14, 2010Publication date: November 17, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Harald Walter, Daniel Stierli
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Publication number: 20110275836Abstract: The present invention relates to improved process for the preparation of Duloxetine of formula (I) and salts thereof wherein said improvement takes place in step of condensation.Type: ApplicationFiled: December 28, 2009Publication date: November 10, 2011Applicant: ALEMBIC PHARMACEUTICALS LIMITEDInventors: Ravi Ponnaiah, Ashok Prasad, Killol Patel, Hitarth Harshendu Acharya, Vilas Katore, Bhavik Shah
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Publication number: 20110257226Abstract: There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R1, R1a and R3 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.; R2, R2a and R4 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.Type: ApplicationFiled: December 24, 2009Publication date: October 20, 2011Inventor: Hiromasa Mitsudera
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Patent number: 8039493Abstract: The invention is concerned with novel biaryl sulfonamide derivatives of formula (I) wherein R1 to R3 and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: September 17, 2008Date of Patent: October 18, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Ulrike Obst Sander, Tanja Schulz-Gasch, Matthew Wright
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Publication number: 20110250655Abstract: The present invention relates to novel phenylethanol dehydrogenase mutants, to a method for the manufacture thereof; to coded nucleic acid sequences therefor, to expression cassettes, to vectors and recombinant microorganisms that contain said sequences; to a method for the biocatalytic synthesis of substituted, optically active alcohols and to the use of said mutants; and particularly to a method for manufacturing duloxetine alcohol or duloxetine, comprising a synthesis step catalyzed biocatalytic by said mutants.Type: ApplicationFiled: December 16, 2009Publication date: October 13, 2011Applicant: BASF SEInventors: Nina Schneider, Hans Wolfgang Höffken
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Publication number: 20110230541Abstract: A process for the preparation of Rotigotine (I) and of pharmaceutically acceptable salts thereof, which comprises the reductive amination of an amine of formula 6 with the 2-thienylacetic acid-sodium boron hydride complex and which makes use of hydrobromide 5 as an intermediate (II) The process is advantageous from the industrial point of view in that it allows to obtain Rotigotine with high enantiomeric purity starting from optically active 5,6,7,8-tetrahydro-6-(S)-N-propylamino-1-methoxy-naphthalene (2), avoiding the use of dangerous reactives, the need for difficult chromatographic separation or the formation of by-products. Furthermore, two novel crystalline forms are disclosed.Type: ApplicationFiled: September 24, 2009Publication date: September 22, 2011Applicant: FIDIA FARMACEUTICI S.P.A.Inventors: Aldo Banfi, Gianluca Belogi, Claudio Fuganti, Roberta Pizzocaro
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Publication number: 20110230666Abstract: The present patent application relates to an improved process for the separation of enantiomerically pure compounds. Specifically it relates to separation of enantiomerically enriched Rivastigmine, Duloxetine, Escitalopram and their intermediates in high yields.Type: ApplicationFiled: February 5, 2009Publication date: September 22, 2011Applicant: SHODHANA LABORATORIES LIMITEDInventors: Thota Giridhar, Gudipati Srinivasulu, Kotaru Srinivasa Rao
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Publication number: 20110207946Abstract: Provided is a process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols, particularly of (S)-(?)- and (R)-(+)-3-N-methylamino-1-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of formula (II), wherein R1 is selected from the group consisting of 2-thienyl, 2-furanyl and phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkoxy groups, and wherein R2 is C1-4-alkyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein the corresponding aminoalcohols are obtained by subsequent hydrolysis of their salts. Furthermore provided are salts of a carboxylic acid with said aminoketones and the aminoalcohols obtained by asymmetriacally hydrogenating said aminoketones, respectively.Type: ApplicationFiled: March 8, 2011Publication date: August 25, 2011Inventors: Dominique Michel, Hanspeter Mettler, John McGarrity
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Patent number: 7985767Abstract: Compounds of the formula are disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: September 6, 2007Date of Patent: July 26, 2011Assignee: Allergan, Inc.Inventors: David W. Old, Robert M. Burk, Todd S. Gac
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Publication number: 20110152543Abstract: The present invention describes a novel process for the preparation of optically active (S)-(?)-2-(N-propylamino)-5-methoxytetraline and (S)-(?)-2-(N-propylamino)-5-hydroxytetraline compounds based on the optical resolution of mixtures of the enantiomers of 2-(N-propylamino)-5-methoxytetraline and 2-(N-propylamino)-5-hydroxytetraline respectively. This process comprises (a) reacting a mixture of the enantiomers of said compounds with an optically active organic acid to form diastereoisomeric salts and separating the salts by crystallization. Said compounds are useful in the preparation of (6S)-(?)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine). Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson's disease.Type: ApplicationFiled: October 9, 2009Publication date: June 23, 2011Inventors: Francisco Marquillas Olondriz, Marta Pomares Marco
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Publication number: 20110150942Abstract: The present invention relates to a pharmaceutical composition comprising an active core comprising duloxetine or its pharmaceutically acceptable derivatives, a separating layer comprising a pH modifier and a gastro-resistant coating comprising a gastro-resistant polymer selected from methacrylic acid copolymers and optionally an over-coating layer. The present invention also relates to a process for the preparation of duloxetine hydrochloride. It also relates to a packaged medicament.Type: ApplicationFiled: June 12, 2009Publication date: June 23, 2011Inventors: Natalija Zajc, Franc Vrecer, Primoz Benkic, Polona Bukovec, Jaroslav Tihi, Andrej Gartner
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Publication number: 20110137049Abstract: The invention provides a chiral iridium aqua complex which has good preservation stability, can be easily produced, and enables asymmetric transfer hydrogenation in a higher yield and with higher stereoselectivity.Type: ApplicationFiled: July 6, 2009Publication date: June 9, 2011Applicants: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Erick M. Carreira
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Publication number: 20110130426Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: October 26, 2005Publication date: June 2, 2011Applicant: ASTRAZENECA ABInventors: Håkan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepistö
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Patent number: 7951837Abstract: The present invention is concerned with duloxetine free base in crystalline form, and also novel polymorphic forms thereof.Type: GrantFiled: May 11, 2005Date of Patent: May 31, 2011Assignee: Cipla LimitedInventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Srinivas Laxminarayan Pathi, Revikumar Puppala
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Publication number: 20110112166Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein B, Y, and A are as described in claims 1-10. Methods, compositions, and medicaments related thereto are also disclosed, for treating baldness, glaucoma or inflammatory bowel diseases.Type: ApplicationFiled: May 4, 2009Publication date: May 12, 2011Applicant: ALLERGAN, INCInventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20110070299Abstract: A pharmaceutical composition comprising duloxetine or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipient(s) characterised in that the duloxetine has a D90 particle size of 2 to 40 ?m.Type: ApplicationFiled: January 9, 2009Publication date: March 24, 2011Applicant: ALPHAPHARM PTY LTD.Inventors: Brett Antony Mooney, Panagiotis Keramidas, Phillip John Ferguson
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Publication number: 20110071207Abstract: The invention relates to (among other things) oligomer-aryloxy-substituted propanamine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated aryloxy-substituted propanamine compounds.Type: ApplicationFiled: April 13, 2009Publication date: March 24, 2011Applicant: NEKTAR THERAPEUTICSInventors: Jennifer Riggs-Sauthier, Franco J. Duarte