Chalcogen Bonded Directly To A Ring Carbon Of The 1,3-diazole Ring Patents (Class 546/273.7)
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Publication number: 20110130570Abstract: The present invention relates to a novel form of the (?)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2 -pyridinyl)-methyl]sulfinyl]-1H-benzimidazole, i.e. S-omeprazole. More specifically, it relates to a novel form of the magnesium salt of the S-enantiomer of omeprazole trihydrate. The present invention also relates to processes for preparing such a form of the magnesium salt of S-omeprazole and pharmaceutical compositions containing it. Furthermore, the present invention also relates to new intermediates used in the process.Type: ApplicationFiled: May 21, 2010Publication date: June 2, 2011Inventors: Hanna Cotton, Anders Kronström, Anders Mattson, Eva Mõller
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Publication number: 20110124657Abstract: The present invention relates to compounds having pharmacological activity towards the 5-HT7 receptor; to a method for identifying them as 5-HT7 ligands, especially as agonists, by using a pharmacophore and a descriptor's profile filter; to pharmaceutical compositions comprising them; and to their use in therapy, in particular for the treatment and or prophylaxis of a disease in which 5-HT7 is involved, such as CNS disorders.Type: ApplicationFiled: July 30, 2009Publication date: May 26, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Rosalia Pascual-Ramon, H. Helmut Buschmann
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Patent number: 7947840Abstract: The present invention provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. Thus, for example, a compound containing a mixture of 1-(S)-camphorsulfonyl-5-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole and 1-(S)-camphorsulfonyl-6-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole is hydrolyzed with barium hydroxide, isolated the resulting esomeprazole barium salt followed by neutralization with an acid to yield substantially enantiomerically pure esomeprazole in neutral form and then converted into its pharmaceutically acceptable salts.Type: GrantFiled: September 25, 2007Date of Patent: May 24, 2011Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy
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Publication number: 20110118248Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: January 13, 2009Publication date: May 19, 2011Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
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Publication number: 20110112067Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20110111510Abstract: The present invention relates, generally to a method of determining and assessing cytochrome P450 2C19-related (CYP2C19) metabolic capacity in an individual mammalian subject via a breath assay, by determining the relative amount of 13CO2 exhaled by the subject upon intravenous or oral administration of a 13C-labeled CYP2C19 substrate compound. The present invention is useful as anon-invasive, in vivo assay for evaluating CYP2C19 enzyme activity in a subject using the metabolite 13CO2 in expired breath, to phenotype individual subjects and to determine the selection, optimal dosage and timing of drug administration.Type: ApplicationFiled: November 9, 2010Publication date: May 12, 2011Inventors: David A. Flockhart, Zeruesenay Desta, Anil S. Modak, Yasuhisa Kurogi
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Patent number: 7928240Abstract: The present invention relates to a process for preparing substituted sulfoxides either as a single enantiomer or in an enantiomerically enriched form. Thus, racemic omeprazole is reacted with (S)-camphorsulfonyl chloride to form a diastereomeric mixture and the diastereomers are separated by fractional crystallization, followed by deprotection to give esomeprazole.Type: GrantFiled: January 8, 2007Date of Patent: April 19, 2011Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Raji Reddy, Dasari Muralidhara Reddy
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Patent number: 7928241Abstract: The present invention relates to a process for stereo selective synthesis of substituted sulfoxides either as a single enantiomer or in an enantiomerically enriched form. Thus, 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl) methyl]thio]-1H-benzimidazole is reacted with (R)-camphorsulfonyl chloride to form a mixture of 1-(R)-camphorsulfonyl-5- (and 6-)methoxy-2-[(3,5-dimethyl-4-methoxy -2-pyridyl)methylthio]-1H-benzimidazole, oxidized to obtain a diastereomeric excess of 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl -4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole over 1-(R)-camphorsulfonyl -(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl) methyl-(R)-sulfinyl]-1H-benzimidazole, the diastereomers are separated by fractional crystallization and the separated 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy -2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole is deprotected to give esomeprazole.Type: GrantFiled: October 1, 2007Date of Patent: April 19, 2011Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy
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Publication number: 20110086884Abstract: The invention relates to crystalline barium salt of (S)-omeprazole, which is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole. The invention also relates to processes for preparing crystalline barium salt of (S)-omeprazole and pharmaceutical compositions that include the crystalline barium salt of (S)-omeprazole so prepared.Type: ApplicationFiled: December 20, 2010Publication date: April 14, 2011Inventors: Yatendra KUMAR, Mahavir Singh Khanna, Mohan Prasad
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Publication number: 20110082174Abstract: The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.Type: ApplicationFiled: November 4, 2010Publication date: April 7, 2011Applicant: IL YANG PHARMACEUTICAL COMPANY, LTD.Inventors: John M. BRACKETT, David T. JONAITIS, Wei LAI, Jih Hua LIU, Stephan D. PARENT, Jinyu SHEN
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Patent number: 7915422Abstract: The present invention relates to a process for enantioselective synthesis of substituted pyridinylmethyl sulfinyl-benzimidazole of compound of Formula (I). The process includes enantioselective catalytic oxidation of a substituted pyridinylmethyl prochiral sulfide derivative of compound of Formula (II) with an oxidizing agent in the presence of a chiral transition metal complex and a base in the absence of an organic solvent.Type: GrantFiled: October 4, 2005Date of Patent: March 29, 2011Assignee: Ranbaxy Laboratories LimitedInventors: Neela Praveen Kumar, Mahavir Singh Khanna, Mohan Prasad, Yatendra Kumar
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Patent number: 7915423Abstract: Crystalline pantoprazole sodium Forms II, IV, V, VI, VIII, IX, X, XI, XII, XIII, XIV, XV, XVI, XVII, XVIII, XIX and XX; pantoprazole sodium solvates containing water, acetone, butanol, methylethylketone, dimethylcarbonate, propanol and 2-methylpropanol; and amorphous pantoprazole sodium are disclosed.Type: GrantFiled: July 27, 2007Date of Patent: March 29, 2011Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Nina Finkelstein, Barnaba Krochmal, Shlomit Wizel, Viviana Braude
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Publication number: 20110065755Abstract: A stable R-(+)-lansoprazole alkylamine salt and a process for preparing the salt.Type: ApplicationFiled: May 12, 2009Publication date: March 17, 2011Applicant: Watson Pharma Private LimitedInventors: Manjunath Narayan Bhanu, Samir Naik, Arjun Bodkhe
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Patent number: 7902370Abstract: New solid forms of the active ingredient magnesium salt of S-omeprazole, obtainable by a preparation process including: a) crystallizing a magnesium salt of S-omeprazole from a solution of a magnesium salt of S-omeprazole in a solvent system that includes a mixture of methanol/water with an amount of water equal to or greater than about 0.01 ml/g of the magnesium salt of S-omeprazole starting material; b) isolating the magnesium salt of S-omeprazole that appears in the prior operation; c) separating the free organic solvent from the magnesium salt of S-omeprazole obtained or, alternatively, separating both the free solvent and the solvation solvent. The new solid forms are obtained by a reproducible and robust process, with high yield and elevated optical purity, which is useful for the preparation of pharmaceutical products that contain said active ingredient.Type: GrantFiled: June 29, 2005Date of Patent: March 8, 2011Assignee: Esteve Quimica, S.A.Inventors: Ramón Berenguer Maimó, Laura Coppi, Yolanda Gasanz Guillén, Jorge Medrano Rupérez
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Publication number: 20110046184Abstract: The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.Type: ApplicationFiled: November 4, 2010Publication date: February 24, 2011Applicant: IL YANG PHARMACEUTICAL COMPANY, LTD.Inventors: John M. BRACKETT, David T. JONAITIS, Wei LAI, Jih Hua LIU, Stephan D. PARENT, Jinyu SHEN
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Publication number: 20110046383Abstract: Disclosed are a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.Type: ApplicationFiled: October 28, 2010Publication date: February 24, 2011Applicant: Hanmi Pham. Co., Ltd.Inventors: Tae Hee HA, Hee Sook Oh, Won Jeoung Kim, Chang Hee Park, Eun Young Kim, Young Hoon Kim, Kwee Hyun Suh, Gwan Sun Lee
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Patent number: 7888511Abstract: Optically pure esomeprazole and its salt can be simply prepared by dissolving (S)-(?)-binol, a weak base and the racemic form of omeprazole in a mixture of a water-compatible organic solvent and water at a high temperature, cooling the mixed solution to crystallize the inclusion complex of esomeprazole and (S)-(?)-binol, and removing the (S)-(?)-binol moiety from the crystallized inclusion complex.Type: GrantFiled: July 11, 2006Date of Patent: February 15, 2011Assignee: Hanmi Holdings Co., Ltd.Inventors: Tae Hee Ha, Won Jeong Kim, Hee Sook Oh, Chang Hee Park, Jae Chul Lee, Han Kyong Kim, Kwee-Hyun Suh
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Publication number: 20110028728Abstract: Process for the preparation of crystalline anhydrous (R)-2-[[[3-methyl-4-(2,2,2-trifluoroetoxy)-2-piridyl]methyl]sulphinyl]benzimidazole (dexlansoprazole).Type: ApplicationFiled: July 6, 2010Publication date: February 3, 2011Applicant: DIPHARMA FRANCIS S.r.l.Inventors: Chiara VLADISKOVIC, Alessandro Restelli, Gabriele Razzetti
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Publication number: 20110028518Abstract: Processes for the preparation of dexlansoprazole, an amorphous form of dexlansoprazole, a solid dispersion of amorphous dexlansoprazole and a pharmaceutically acceptable carrier, and processes for their preparation. Also provided are crystalline compounds 2-[(R)-[(4-chloro-3-methyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole and 2-[(R)-[(4-nitro-3-methyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, and methods for their preparation.Type: ApplicationFiled: March 18, 2009Publication date: February 3, 2011Applicants: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.Inventors: Naveen Kumar Kolla, Nagaraju Manne, Srinivas Gangula, Udaykumar Neelam, Anitha Naredla, Sudhakar Reddy Baddam, Sumeet Vishwasrao Patil, Arjunkumar Tummala, Subbareddy Peddireddy, Sachin Gulabrao Shinde, Ashok Sigala, Satish Varma Mudunuru, Madhu Kiran Tummidi
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Patent number: 7875723Abstract: The present invention discloses a process for preparing a magnesium salt of S-omeprazole. The S-omeprazole salt preferably has a water content below about 4.8% by weight, a magnesium content of about 3.4-4.0% by weight, calculated on the weight of anhydrous, solvent free S-omeprazole magnesium, and has an optical purity of at least about 85% entantiomeric excess (“e.e.”). In addition, the present invention provides a magnesium salt of S-omeprazole which is substantially free of neutral omeprazole, meaning that the product contains less than about 3% by weight of a sum of neutral S-omeprazole and neutral omeprazole. Moreover, the S-omeprazole magnesium according to the invention preferably has assay of related substances and degradation products of less than about 0.1% by weight as determined by high performance liquid chromatography (HPLC).Type: GrantFiled: April 1, 2009Date of Patent: January 25, 2011Assignee: Lek Pharmaceuticals d.d.Inventors: Lidija Vranicar Savanovic, Dejan Mandic, Renata Toplak Casar
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Patent number: 7872140Abstract: The invention relates to crystalline barium salt of (S)-omeprazole, which is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole. The invention also relates to processes for preparing crystalline barium salt of (S)-omeprazole and pharmaceutical compositions that include the crystalline barium salt of (S)-omeprazole so prepared.Type: GrantFiled: May 15, 2009Date of Patent: January 18, 2011Assignee: Ranbaxy Laboratories LimitedInventors: Yatendra Kumar, Mahavir Singh Khanna, Mohan Prasad
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Publication number: 20110009624Abstract: The present invention provides a compound that has superior gastric acid secretion inhibitory action, ample long-lasting gastric acid secretion inhibitory action, and is able to maintain intragastric pH at a high level for an extended period of time, making it useful as a therapeutic or prophylactic agent for diseases or symptoms caused by gastric acid, as well as an active form of this compound (form to which the compound is converted in the body following administration thereof) in the form of a compound represented by general formula (1a) (wherein R2 represents a group represented by formula (I) or the like, and R1, R3, W1 and X? are as defined in the description).Type: ApplicationFiled: October 11, 2007Publication date: January 13, 2011Inventors: Masato Ueda, Daisuke Iida, Sachiko Kikuchi, Masaharu Gotoda
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Patent number: 7855082Abstract: The present invention relates to a novel method to determine the ratio of 5-methoxy and 6-methoxy isomers of omeprazole present in a mixture thereof. The method uses different Raman scattering efficiency values for the 5-methoxy and 6-methoxy isomers. This is of importance since the two isomers have different stability in the solid state in bulk form and in admixture with pharmaceutical excipients.Type: GrantFiled: January 8, 2009Date of Patent: December 21, 2010Assignee: AstraZeneca ABInventor: Frans Langkilde
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Publication number: 20100286400Abstract: The novel hydrate, methanol solvate, ethanol solvate, ethanol•hydrate and isopropanol•hydrate crystals of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole of the present invention are useful as excellent antiulcer agents.Type: ApplicationFiled: December 30, 2008Publication date: November 11, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Koji Urakami, Keith Lorimer, Kevin Meyer, Mark Christopher Andres
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Publication number: 20100286208Abstract: Disclosed is a novel potassium salt of esomeprazole in polymorph form X, which can be used in pharmaceutical compositions. Processes for preparing polymorph form X of esomeprazole potassium are also provided.Type: ApplicationFiled: June 21, 2007Publication date: November 11, 2010Inventors: Bobba Venkata Siva Kumar, Pravin BalachandrA Kulkarni, Anil Ganpat Suryawanshi, Sachin Bapurao Sawant
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Patent number: 7829718Abstract: It is an object of the present invention to provide (1) a process for manufacturing alkali metal salts of 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1H-benzimidazole which are useful as gastric acid secretion inhibitors, anti-ulcer agents and other drugs and (2) salts of 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1H-benzimidazole with amines which are intermediates for the production of the alkali metal salts, and a process for manufacturing the same. According to the present invention, disclosed are salts represented by the following formula (I): (wherein A+ represents an isopropylammonium ion, sec-butylammonium ion or cyclopentylammonium ion).Type: GrantFiled: August 5, 2005Date of Patent: November 9, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Hiroyuki Yokoi, Masanori Mizuno, Toyokazu Haga
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Publication number: 20100280077Abstract: A process for preparing stable amorphous R-(+)-lansoprazole comprising optically resolving racemic lansoprazole by the formation of host-guest inclusion complexes by selectively and reversibly including chiral guest molecules in the lansoprazole.Type: ApplicationFiled: December 18, 2008Publication date: November 4, 2010Applicant: WATSON PHARMA PRIVATE LIMITEDInventors: Samir Naik, Arjun Bodke, Kishor Mahajan, Manjunath Narayan Bhanu
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Publication number: 20100267959Abstract: The present invention relates to a process for the preparation of esomeprazole magnesium dihydrate, specifically, esomeprazole magnesium crystalline dihydrate form A; and pharmaceutical compositions thereof.Type: ApplicationFiled: July 8, 2009Publication date: October 21, 2010Applicant: Glenmark Generics LimitedInventors: Joseph Prabahar KOILPILLAI, Pravin Bhalchandra Kulkami, Avikumar Digambar Dabe, Mubeen Ahmed Khan
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Publication number: 20100249124Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Patent number: 7799925Abstract: A process for the preparation of (S)-omeprazole from racemic omeprazole via the formation of an inclusion complex with (S)-1,1,2-triphenyl-1,2-ethanediol. (S)-Omeprazole is recovered in a substantially optically pure form either in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The (S)-omeprazole 2[(S)-1,1,2-triphenyl-1,2-ethanediol] inclusion complex is new. This resolution process proceeds with high yields and high optical purity.Type: GrantFiled: December 18, 2006Date of Patent: September 21, 2010Assignee: Unión Químico Farmacéutica, S.A.Inventors: Antonio Domingo Coto, Alexander Comely, Xavier Verdaguer Espaulella, Llorenç Rafecas Jané
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Publication number: 20100227891Abstract: Dosage forms of sodium {4-[5-Methoxy-2-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethanesulfinyl)-benzoimidazole-1-sulfonyl]-phenoxy}-acetate, and methods of use of the dosage forms are disclosed herein.Type: ApplicationFiled: October 13, 2009Publication date: September 9, 2010Inventors: Edward Lee, Dale K. Yu, John Sefton, Dari D. Parizadeh, Diane Tang-Liu
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Publication number: 20100227890Abstract: The present invention relates to a high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention further provides an improved and commercially viable process for preparation of high assayed esomeprazole magnesium dihydrate substantially free of its trihydrate form. The present invention also provides an improved process for preparation of pure amorphous esomeprazole magnesium. The present invention further provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The present invention also provides solid form of esomeprazole calcium salt, its polymorphs (form 1, form 2 and amorphous form) and processes for their preparation thereof.Type: ApplicationFiled: October 8, 2007Publication date: September 9, 2010Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Puchakayala Srinivasa Reddy
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Patent number: 7790891Abstract: A process for the preparation of a compound of formula (I), or a salt thereof, wherein Q is ?CR8— or ?N—; and R1-R8 are as herein defined; comprising the reaction of a compound of formula (II), or a salt thereof, wherein Q, R1-R7 are as herein defined; with a reducing agent selected from a trivalent phosphorous compound, an oxidizable solvent and a sulfonic acid chloride; and, if desired, the conversion of a compound of formula (I) to another compound of formula (I) or a salt thereof.Type: GrantFiled: October 29, 2007Date of Patent: September 7, 2010Assignee: Dipharma Francis S.R.L.Inventors: Pietro Allegrini, Marcello Rasparini, Gabriele Razzetti, Simone Mantegazza, Vittorio Lucchini, Alberto Bologna
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Patent number: 7790755Abstract: A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient.Type: GrantFiled: October 15, 2003Date of Patent: September 7, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Yohko Akiyama, Takashi Kurasawa, Hiroto Bando, Naoki Nagahara
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Publication number: 20100222591Abstract: The novel optically pure compounds Na+, Mg2+, Li+, K+, Ca2+ and N+(R)4 salts of (+)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole or (?)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, in particular sodium and magnesium salt form thereof, where R is an alkyl with 1-4 carbon atoms, processes for the preparation thereof and pharmaceutical preparations containing the compounds as active ingredients, as well as the use of the compounds in pharmaceutical preparations and intermediates obtained by preparing the compounds.Type: ApplicationFiled: September 1, 2009Publication date: September 2, 2010Inventors: Per Lennart Lindberg, Sverker Von Unge
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Publication number: 20100222390Abstract: Disclosed herein are liquid compositions comprising a therapeutically effective concentration of a prodrug of a sulfonyl-containing proton pump inhibitor, wherein said compositions have a pH of from 3 to 7.3. Solid compositions related thereto are also disclosed. Methods of delivering a proton pump related thereto are also disclosed. Compositions comprising a second therapeutically active agent are also disclosed herein.Type: ApplicationFiled: October 2, 2009Publication date: September 2, 2010Applicant: Alevium Pharmaceuticals, Inc.Inventor: Patrick M. Hughes
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Patent number: 7786309Abstract: A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.Type: GrantFiled: May 9, 2007Date of Patent: August 31, 2010Assignee: Apotex Pharmachem Inc.Inventors: Fan Wang, Laura Kaye Montemayor, Daqing Che, Stephen E. Horne
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Publication number: 20100210847Abstract: The present invention relates to a process for the preparation of pantoprazol sodium sesquihydrate of formula (I) and pantoprazole sodium.Type: ApplicationFiled: July 17, 2008Publication date: August 19, 2010Applicant: RANBAXY LABORATORIES LIMITEDInventors: Ashish M. Trivedi, Shailendra Kumar Singh, Neera Tewari, Mohan Prasad
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Publication number: 20100210848Abstract: The present invention discloses novel processes for preparing optically active sulphoxide compounds of formula I by asymmetric oxidation of prochiral sulphide compounds of Formula II. More particularly, the invention discloses processes for preparation of optically active proton pump Inhibitors (PPIs) or their optically active precursor (=intermediate) compounds (Formula I) that can be converted into pharmaceutically useful PPIs.Type: ApplicationFiled: October 3, 2008Publication date: August 19, 2010Applicant: IPCA Laboratories Ltd.Inventors: Ashok Kumar, Dharmendra Singh, Nellithanath Thankachen Byju, Prasad Shankar Kadam, Harishankar Prahladkumar Vishwakarma, Vijay Ojha, Umeshkumar Suresh Ninawe
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Publication number: 20100210846Abstract: The present invention relates to a process for preparing 2-(2-pyridylmethyl)sulphinyl-1H-benzimidazoles that are proton pump inhibitors, using as intermediates 2-benzimidazolyl-sulphinic acid derivatives. The present invention also relates to the intermediate compounds, their use and a process for the preparation thereof. These novel intermediate compounds are 2-benzimidazolylsulphinicacid esters that are obtained from their corresponding alkaline salts, which are in turn obtained by oxidation of substituted 2-mercaptobenzimidazoles. The intermediate compounds of the invention are converted into 2-(2-pyridylmethyl)sulphinyl-1H-benzimidazoles by reaction with substituted 2-methylpyridines.Type: ApplicationFiled: May 15, 2008Publication date: August 19, 2010Inventors: Francisco Eugenio Palomo Nicolau, Alfredo Pastor Del Castillo, Andres Molina Ponce
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Patent number: 7777044Abstract: Process for the preparation of optically active derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole, or salts thereof, by resolution of the corresponding racemic derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole. The resolution is performed through the formation of inclusion complexes with (S)-(?) or (R)-(+)-[1,1?-Binaphthalene]-2,2?-diol in the presence of an amine, followed by the break of the inclusion complex by treatment with an hydroxide of an alkaline metal. The enantiomer of the derivative of 2-(2-piridylmethylsulfinyl)-benzimidazole may be obtained by extractions at a particular pH with a suitable organic solvent. The process allows to perform the resolution with high yields and high optical purity, without using neither toxic solvents nor chromatography.Type: GrantFiled: February 22, 2006Date of Patent: August 17, 2010Assignee: Esteve Quimica, S.A.Inventors: Laura Coppi, Ramón Berenguer Maimó, Yolanda Gasanz Guillén, Jorge Medrano Rupérez
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Publication number: 20100204479Abstract: The present invention relates to novel crystalline forms of Dexlansoprazole and a process for the preparation of amorphous Dexlansoprazole.Type: ApplicationFiled: January 26, 2010Publication date: August 12, 2010Applicant: DIPHARMA FRANCIS S.R.IInventors: CHIARA VLADISKOVIC, GABRIELE RAZZETTI
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Publication number: 20100204279Abstract: Therapeutic salt compositions and methods are disclosed herein.Type: ApplicationFiled: September 21, 2009Publication date: August 12, 2010Inventors: Mark P. Rubino, Gyorgy F. Ambrus
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Publication number: 20100204478Abstract: The present invention provides an improved and efficient process for the preparation of highly pure amorphous rabeprazole sodium. Thus, for example, rabeprazole is dissolved in an alcoholic sodium hydroxide solution followed by carbon treatment, the resulting filtrate is distilled under vacuum at 50-52° C. followed by co-distillation with cyclohexane and the resulting residue is dissolved in anisole; the solution is added to cyclohexane under agitation and then the precipitated solid collected by filtration or centrifugation.Type: ApplicationFiled: May 25, 2007Publication date: August 12, 2010Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy
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Publication number: 20100190989Abstract: The present invention relates to a process for the preparation of pure Rabeprazole sulfoxide using the solvent mixture for the extraction steps and this invention further relates to the process for the preparation of amorphous Rabeprazole sodium using pure rabeprazole base in presence of aqueous NaOH and water miscible solvent and adding an anti-solvent.Type: ApplicationFiled: June 19, 2008Publication date: July 29, 2010Applicant: MATRIX LABORATORIES LTDInventors: Om Dutt Tyagi, Purna Chandra Ray, Madhuresh Kumar Sethi, Bhausaheb Chavhan
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Publication number: 20100183710Abstract: A process for preparing pure omeprazole Form B, and compositions containing omeprazole Form B.Type: ApplicationFiled: July 7, 2006Publication date: July 22, 2010Inventors: Vijayabhaskar Bolugoddu, Jaydeepkumar Dahyabhai Lilakar, Ramchandra Reddy Pingili, Swarupa Reddy Dudipala, Adolf Ceasor Goldwyn, Bala Murali Krishna Pittala, Mailatur Sivaraman Mohan, Indu Bhushan, Ravinder Kodipyaka, Rahul Sudhakar Gawande, Srikanth Basety
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Publication number: 20100179328Abstract: Disclosed herein, a process for producing sulphoxide compound of the Formula (I) by asymmetrically oxidizing a prochiral sulphide of the Formula (II) with an effective amount of oxidizing agent in the presence of a chiral transition metal complex without using an organic solvent and base.Type: ApplicationFiled: August 8, 2007Publication date: July 15, 2010Applicant: Jubilant Organosys LimitedInventors: Anand Singh, Khushwant Singh, Sushil Kumar Dubey
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Patent number: 7754887Abstract: Process for producing sulfoxide derivatives or salts thereof in the amorphous state, characterized by heat-drying solvated crystals of a sulfoxide derivative or a salt thereof represented by the general formula (I): wherein R1 represents a hydrogen atom, a methoxy group, or a difluoromethoxy group; R2 represents a methyl group or a methoxy group; R3 represents a 3-methoxypropoxy group, a methoxy group, or a 2,2,2-trifluoroethoxy group; R4 represents a hydrogen atom or a methoxy group; and B represents a hydrogen atom, an alkali metal or ½ alkaline earth metal.Type: GrantFiled: November 13, 2007Date of Patent: July 13, 2010Assignee: EISAI R&D Management Co., Ltd.Inventors: Masahiko Tsujii, Yukio Morita
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Publication number: 20100173944Abstract: Disclosed are: a compound which is stable in an acid, has an antibacterial effect against a bacterium Helicobacter pylori, can exert a satisfactory level of an antibacterial effect when used singly, does not affect an enteric bacterium, has an antibacterial effect against a bacterium resistant to an antibacterial agent, and has an inhibitory effect on gastric acid secretion; and a pharmaceutical composition comprising the compound. Specifically disclosed are: a compound represented by the general formula (I) or a salt thereof; and a pharmaceutical composition comprising the compound or the salt thereof: wherein R represents a linear alkyl group having 4 to 8 carbon atoms, preferably 5 to 7 carbon atoms.Type: ApplicationFiled: December 18, 2007Publication date: July 8, 2010Applicant: ARIGEN PHARMACEUTICALS, INC.Inventors: Masaharu Ito, Masaichi Yamamoto
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Publication number: 20100174087Abstract: The present invention provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. Thus, for example, a compound containing a mixture of 1-(S)-camphorsulfonyl-5-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole and 1-(S)-camphorsulfonyl-6-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole is hydrolyzed with barium hydroxide, isolated the resulting esomeprazole barium salt followed by neutralization with an acid to yield substantially enantiomerically pure esomeprazole in neutral form and then converted into its pharmaceutically acceptable salts.Type: ApplicationFiled: September 25, 2007Publication date: July 8, 2010Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy