Chalcogen Bonded Directly To A Ring Carbon Of The 1,3-diazole Ring Patents (Class 546/273.7)
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Patent number: 8247566Abstract: The present invention belongs to the field of pharmaceutical industry and relates to novel crystalline omeprazole sodium ethanol solvate and to the process for its preparation, which acts as intermediary compound to the processes for its conversion into different crystalline forms, first of all to a known omeprazole sodium form A, with low amount of residual solvents, i.e. less than 0.5% by weight of residual solvent. The present invention also relates to novel crystalline omeprazole sodium form E and crystalline omeprazole sodium form F as well to the processes for their preparation as well, both with considerably low levels of residual solvents. Omeprazole sodium form A and both novel crystalline forms omeprazole sodium form E and form F are useful for the treatment of gastrointestinal disorders.Type: GrantFiled: June 7, 2006Date of Patent: August 21, 2012Assignee: Lek Pharmaceuticals d.d.Inventors: Lidija Vranicar Savanovic, Zoran Ham, Janez Rzen
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Patent number: 8247567Abstract: The present invention relates to a process for removing an organic solvent from a salt of omeprazole, in particular a magnesium salt of omeprazole, a composition comprising a salt of omeprazole, in particular a magnesium salt of omeprazole obtainable by such a process, and pharmaceutical compositions comprising said composition or a salt of omeprazole, in particular a magnesium salt of omeprazole, in particular where omeprazole is S-omeprazole.Type: GrantFiled: January 9, 2008Date of Patent: August 21, 2012Assignee: Lek Pharmaceuticals, D.D.Inventors: Dejan Mandic, Renata Toplak Casar
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Publication number: 20120208819Abstract: The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.Type: ApplicationFiled: October 5, 2010Publication date: August 16, 2012Inventors: Joseph Arndt, Timothy Chan, Kevin Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Daniel Scott, Lihong Sun, Jermaine Thomas, Kurt van Vloten, Deping Wang, Lei Zhang, Daniel Erlanson
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Publication number: 20120197021Abstract: The present invention relates to process for preparation of optical resolution of substituted 2-(2-pyridinylmethylsulphinyl)-1H-benzimidazoles either as a single enantiomer or in an enantiomerically enriched form. Thus, for example, R-1,1?-binaphtyl-2-2?-diyl hydrogen phosphate was reacted with 2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole (Lansoprazole) in a mixture of benzene and cyclohexane to obtain diasteremeric complexes. The diasteremeric complexes were subjected to fractional crystallization to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole.R-1,1?-binaphthyl-2-2?-diyl hydrogen phosphate. The separated isomer was treated with sodium bicarbonate in a mixture of ethyl acetate and water to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole (dexlansoprazole).Type: ApplicationFiled: October 9, 2009Publication date: August 2, 2012Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Bandi Vamsi Krishna, Ayyalasomayajula Satya Srinivas
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Publication number: 20120196819Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said compositon dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.Type: ApplicationFiled: January 4, 2012Publication date: August 2, 2012Applicant: NEWMARKET PHARMACEUTICALS LLCInventors: David ROCK, Mark RIDALL
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Patent number: 8222422Abstract: Provided is a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole showing an X-ray powder diffraction pattern having characteristic peaks at interplanar spacings (d) of 10.06±0.2, 8.70±0.2, 6.57±0.2, 5.59±0.2 and 4.00±0.2 Angstroms. The present invention provides a stable antiulcer drug superior in the absorbability.Type: GrantFiled: March 9, 2009Date of Patent: July 17, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Hideo Hashimoto, Tadashi Urai
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Patent number: 8198455Abstract: Process for the preparation of (R)-2-[[[3-methyl-4(2,2,2-trifluoroethoxy)-2-piridyl]methyl]sulfinyl]benzimidazole (Dexlansoprazole) and new intermediates useful in its preparation.Type: GrantFiled: November 17, 2009Date of Patent: June 12, 2012Assignee: Dipharma Francis S.r.l.Inventors: Emanuele Attolino, Vittorio Lucchini
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Publication number: 20120142738Abstract: There is proposed a pharmaceutical composition for treating dermatological autoimmune diseases, comprising a proton pump inhibitor.Type: ApplicationFiled: October 13, 2011Publication date: June 7, 2012Inventors: Günter Stephan, Charlie Farr
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Publication number: 20120122933Abstract: The present invention relates to a novel crystalline form of esomeprazole sodium salt. Further, the present invention also relates to the use of the novel crystalline form for the treatment of gastrointestinal disorders, pharmaceutical compositions containing it as well as processes for the preparation of the novel crystalline form.Type: ApplicationFiled: May 6, 2011Publication date: May 17, 2012Inventors: Ursula Hohlneicher, Silke Klick, Karin Lövqvist
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Patent number: 8173818Abstract: 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: GrantFiled: August 8, 2007Date of Patent: May 8, 2012Assignee: Jubilant Organosys LimitedInventors: Anand Singh, Khushwant Singh, Sushil Kumar Dubey
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Patent number: 8173817Abstract: The present invention relates to a process for stereoselective 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: May 8, 2012Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy
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Patent number: 8163777Abstract: The invention relates to compounds of formula (XVI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein Y2, Z, L1, R9, R10, m and u are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, immune disorders, and allergic disorders.Type: GrantFiled: March 23, 2007Date of Patent: April 24, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Lijun Sun, Yu Xie
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Publication number: 20120095054Abstract: 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: December 20, 2011Publication date: April 19, 2012Applicant: HETERO DRUGS LIMITEDInventors: Bandi PARTHASARADHI REDDY, Kura RATHNAKAR REDDY, Rapolu RAJI REDDY, Dasari MURALIDHARA REDDY, Puchakayala SRINIVASA REDDY
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Patent number: 8143409Abstract: Rabeprazole sodium in the monohydrate crystalline form, pharmaceutical compositions thereof, the use thereof in therapy, a process for its preparation, and the use thereof for the purification of rabeprazole sodium.Type: GrantFiled: December 18, 2007Date of Patent: March 27, 2012Assignee: Dipharma Francis S.R.L.Inventors: Giuseppe Barreca, Alessandro Restelli, Pietro Allegrini
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Publication number: 20120071512Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 12, 2010Publication date: March 22, 2012Applicant: NOVARTIS AGInventors: Qi-Ying Hu, Sylvie Chamoin, Christopher M. Adams, Chun Zhang
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Patent number: 8134008Abstract: A hydrate of esomeprazole magnesium in the form of an amorphous solid is provided. Methods of preparation and use of, as well as formulation containing the hydrate of esomeprazole magnesium in the form of an amorphous solid are also provided.Type: GrantFiled: September 28, 2009Date of Patent: March 13, 2012Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Manne Satyanarayana Reddy, Muppa Kishore Kumar, Koilkonda Purandhar, Keshaboina Sreenath
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Patent number: 8129536Abstract: The present invention relates to an improved process for the preparation of Lansoprazole of formula (I). More particularly, the present invention relates to a method for the purification of crude Lansoprazole in a solvent in presence of an alkali salt of an organic acid or in presence of an organic base such as piperidine or imidazole.Type: GrantFiled: September 21, 2007Date of Patent: March 6, 2012Assignee: Orchid Chemicals & Pharmaceuticals LimitedInventors: Thangavel Arulmoli, Siripragada Mahender Rao, Krishna Sumanth Peraka, Ariyamuthu Sundara Selvan
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Patent number: 8124779Abstract: The present invention relates to a new process for the preparation of new crystal modifications of esomeprazole non-salt form. Further, the present invention also relates to the use of said new crystal modifications for the treatment of gastrointestinal disorders, pharmaceutical compositions containing them as well as the crystal modifications, as such.Type: GrantFiled: December 4, 2006Date of Patent: February 28, 2012Assignee: AstraZeneca ABInventors: Martin Bohlin, Per Lindberg
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Patent number: 8124780Abstract: A novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases is provided, which has an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where R1 and R3 may be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; R2 represents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.Type: GrantFiled: August 11, 2008Date of Patent: February 28, 2012Assignee: Eisai R&D Management Co., Ltd.Inventors: Shuhei Miyazawa, Masanobu Shinoda, Tetsuya Kawahara, Nobuhisa Watanabe, Hitoshi Harada, Daisuke Iida, Hiroki Terauchi, Junichi Nagakawa, Hideaki Fujisaki, Atsuhiko Kubota, Masato Ueda
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Publication number: 20120046285Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: ApplicationFiled: August 17, 2011Publication date: February 23, 2012Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
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Publication number: 20120046319Abstract: The invention discloses a process for the preparation of compounds having structures typical for proton pump inhibitors in enantiomerically enriched form by using particular metal catalysts in an enantioselective oxidation step. Also disclosed are useful further processes and pure intermediate and subsequently final products.Type: ApplicationFiled: October 13, 2009Publication date: February 23, 2012Inventors: Barbara Mohar, Renata Toplak Casar
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Publication number: 20120045784Abstract: The present technology discloses biotinidase assay, biotinidase substrates (I) and a kit wherein the biotinidase substrate includes a label molecule separated from the biotin carbamoyl group by a linker X longer than about 4 ? but shorter than about 27 ?.Type: ApplicationFiled: March 10, 2010Publication date: February 23, 2012Applicant: Joachim Ngiamas trustee for Joachim Ngiam Trust Fund ABNInventors: Jarkko Karvinen, Pertti Hurskainen, Pekka Mattsson, Outi Mulari, Jari Peuralahti, Lassi Jaakkola
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Publication number: 20120029026Abstract: The present invention relates to a novel pyridine derivative or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the derivative or ester, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound represented by the general formula (I): [wherein R represents a pyridyl group substituted with 1 to 3 group(s) independently selected from Substituent Group A, and Substituent Group A represents a halogen atom, a C1-C6 alkyl group and a C1-C6 alkoxy group] or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the compound or ester.Type: ApplicationFiled: April 15, 2011Publication date: February 2, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi SHINOZUKA, Tomoharu TSUKADA, Kunihiko FUJII, Makoto MORI
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Patent number: 8106210Abstract: 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: GrantFiled: October 8, 2007Date of Patent: January 31, 2012Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Puchakayala Srinivasa Reddy
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Patent number: 8106076Abstract: This invention provides 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: GrantFiled: April 17, 2009Date of Patent: January 31, 2012Assignee: Hanmi Holdings 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: 8076361Abstract: 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: GrantFiled: May 21, 2010Date of Patent: December 13, 2011Assignee: AstraZeneca ABInventors: Hanna Cotton, Anders Kronström, Anders Mattson, Eva Möller
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Publication number: 20110300072Abstract: Use of benzimidazole-derived compounds of formula (I) according to the following structure, wherein x is a heteroatom selected from N, S, O, P, SO, SO2 and SO3, preferably from N, S and SO3 and most preferably from N and SO3; n may be 0 or 1, R1 is a group selected from formula (II) and formula (III) and R2 is a group selected from H and formula (IV) since the aforesaid serves for the production of a formulation used as a specific marker in the case of neurodegenerative diseases and tau pathologies.Type: ApplicationFiled: July 22, 2009Publication date: December 8, 2011Applicant: SERVICIOS CIENTIFICOS NEUROINNOVATION LTDA.Inventors: Ricardo Maccioni Baraona, Leonel Rojo, Rodrigo Kuljis Azocar
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Patent number: 8071781Abstract: The present invention provides a process for preparing the amorphous rabeprazole sodium. The process comprises the following steps: (a) Contacting rabeprazole sodium compound with a solvent system to thereby obtain a clear solution under a first temperature, wherein said solvent system is a mixture of at least two categories of organic solvents; (b) Stirring said clear solution of step (a) under a second temperature for a certain time period to obtain a solution containing resultant separated solid, wherein said second temperature is equal to or lower than said first temperature; (c) Filtering said solution containing resultant separated solid obtained from step (b) to obtain a wet solid; and (d) Drying said wet solid to obtain an amorphous rabeprazole sodium compound.Type: GrantFiled: November 11, 2008Date of Patent: December 6, 2011Assignee: Syn-Tech Chem. & Pharm. Co., Ltd.Inventors: Chin-Tsai Fan, Chen-Ming Hsiao, Rong-Bin Hsieh
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Patent number: 8063074Abstract: Polymorphic crystalline Forms J, K, L, M, and N of esomeprazole sodium.Type: GrantFiled: April 30, 2007Date of Patent: November 22, 2011Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Vijayabhaskar Bolugoddu, Amarnath Reddy Lekkala, Saurabh Shashikant Chitre, Srinivas Reddy Mamilla, Venkata Annapurna Sasikala Cheemalapati, Siva Prasad Reddy Seerapu
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Patent number: 8053580Abstract: 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: June 24, 2009Date of Patent: November 8, 2011Assignee: Eisal R&D Management Co., Ltd.Inventors: Hiroyuki Yokoi, Masanori Mizuno, Toyokazu Haga
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Publication number: 20110269798Abstract: A precursor phase of the magnesium tetrahydrate salt of an omeprazole enantiomer, and also processes for preparing it and its use for the preparation of the magnesium tetrahydrate salt are described. Crystals of the magnesium tetrahydrate salt thus obtained, and their uses, especially in the synthesis of the dihydrate form A of the magnesium salt of the enantiomer or as medicament are also disclosed.Type: ApplicationFiled: March 31, 2011Publication date: November 3, 2011Applicants: UNIVERSITE DE ROUEN, PRODUITS CHIMIQUES AUXILIAIRES ET DE SYNTHESEInventors: Snella CHOUIPPE, Jean-Marie SCHNEIDER, Guillaume TAUVEL, Gerard COQUEREL
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Publication number: 20110263526Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.Type: ApplicationFiled: April 22, 2011Publication date: October 27, 2011Applicant: PIRAMAL LIFE SCIENCES LIMITEDInventor: Apparao SATYAM
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Publication number: 20110257405Abstract: The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.n?H2O (wherein n? is about 0 to about 0.1) or a salt thereof, which characteristically includes crystallization from an organic solvent solution or suspension in which (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.nH2O (wherein n is about 0.1 to about 1.0) or a salt thereof has been dissolved or suspended, and the like, and provides a convenient method for efficiently producing an optically active sulfoxide derivative having an extremely high enantiomer excess in high yield at an industrial large scale.Type: ApplicationFiled: June 24, 2011Publication date: October 20, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Hideo HASHIMOTO, Hideaki MARUYAMA
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Patent number: 8039631Abstract: The present invention relates to a process for preparing Crystalline Form A of Lansoprazole. Specifically, the present invention relates to a process for preparing highly pure Crystalline Form A of Lansoprazole in a large scale without any additional conversion step, even by using ethanol in which Crystalline Form B is easily formed.Type: GrantFiled: January 4, 2007Date of Patent: October 18, 2011Assignees: Daewoong Pharmaceutical Co., Ltd., Daewoong Chemical Co., Ltd.Inventors: Seong Cheol Moon, In Woong Song, Doo Sung Kang, Seong Soo Oh, Sung Jae Lee
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Publication number: 20110250273Abstract: The present invention relates to compositions, kits and methods of treating diabetes. More specifically, compositions of at least one proton pump inhibitor, kits and methods of their use to treat diabetes.Type: ApplicationFiled: December 11, 2009Publication date: October 13, 2011Applicant: Melford Scientific, LLCInventor: Ivan Newton Mefford
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Patent number: 8034948Abstract: The present invention relates to the resolution by preferential crystallization of potassium salts of racemic omeprazole which is a solvate of ethanol and/or of ethylene glycol, which consists in converting the omeprazole to the potassium salt in the form of a solvate or of a mixture of these solvates in the presence of an excess of inorganic base which is a source of potassium, the said potassium salts existing in the form of conglomerates, and in then resolving the said conglomerates, independently or simultaneously, by preferential crystallization in order to separate the two (S) and (R) enantiomers of these potassium salts of omeprazole.Type: GrantFiled: August 29, 2008Date of Patent: October 11, 2011Assignee: Universite de RouenInventors: Gérard Coquerel, Guillaume Tauvel, Marie-Noelle Petit
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Publication number: 20110244035Abstract: Dosage forms comprising therapeutically active compounds are disclosed herein.Type: ApplicationFiled: November 4, 2010Publication date: October 6, 2011Inventors: Chin-Ming Chang, James N. Chang, E. Quinn Farnes
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Publication number: 20110245231Abstract: The invention relates to novel drug substance for the treatment of alcohol dependence, pharmaceutical composition, medicament and method for treatment of dependence on using ethyl alcohol containing beverages.Type: ApplicationFiled: December 15, 2009Publication date: October 6, 2011Applicant: Alla Chem, LLCInventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk
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Publication number: 20110245492Abstract: The invention provides methods, PCR primers and sequence determination oligonucleotides for determining a human's capacity to metabolise a substrate of the CYP2C19 enzyme using genetic analysis.Type: ApplicationFiled: May 16, 2011Publication date: October 6, 2011Inventors: Brahmachari Samir KUMAR, Kukreti Ritushree, Mukerji Mitali, Martis Suparna, Fernandes Ravina, Sharma Nitin
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Patent number: 8030333Abstract: A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.Type: GrantFiled: April 30, 2010Date of Patent: October 4, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Akira Fujishima, Isao Aoki, Keiji Kamiyama
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Publication number: 20110223093Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.Type: ApplicationFiled: March 11, 2011Publication date: September 15, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMAPNYInventor: MARK A. SCIALDONE
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Patent number: 8017784Abstract: Disclosed are an optically pure compound having formula I, its pharmaceutically acceptable salt and its pharmaceutically acceptable solvate, and a use thereof in manufacturing medicaments and pharmaceutical compositions. A process for preparing the compound defined therein is also provided.Type: GrantFiled: May 23, 2008Date of Patent: September 13, 2011Assignee: Livzon Pharmaceutical Group, Inc.Inventors: Jingen Deng, Qin Yang, Yongle Chen, Jin Zhu, Qiwei Wang, Qiuya Huang, Xuemei Hou
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Publication number: 20110213155Abstract: The present invention relates to process for optical purification of esomeprazole or a salt thereof. Thus, esomeprazole sodium having 20 to 1% R-omeprazole by weight of the sum of the contents of esomeprazole and R-omeprazole is precipitated from a solvent selected from an alcohol or a mixture of alcohols and the precipitated solid is collected to obtain optically pure esomeprazole sodium.Type: ApplicationFiled: November 18, 2008Publication date: September 1, 2011Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy
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Publication number: 20110207779Abstract: The present invention relates to a process for the preparation of esomeprazole magnesium containing R-isomer greater than about 0.1% by wt. In particular, the present invention relates to a process for the preparation of esomeprazole magnesium dihydrate containing R-isomer greater than about 0.1% by wt.Type: ApplicationFiled: April 28, 2010Publication date: August 25, 2011Applicant: GLENMARK GENERICS LTDInventors: Koilpillai Joseph Prabahar, Veerabhadra Swamy Hiremath, Milind Moreshwar Gharpure, Nagan Nirmalan Kandaswamy, Avekumar Digambar Dabe, Kamal Mehta, Pankajkumar Shinde
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Publication number: 20110201629Abstract: There are described cyclohexyl amide derivatives of Formula I, which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.Type: ApplicationFiled: January 31, 2011Publication date: August 18, 2011Inventors: Benjamin Atkinson, David Beattie, Andrew James Culshaw, James Dale, Nicholas James Devereux, Jeffrey McKenna
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Patent number: 7999110Abstract: The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2 -pyridinyl)-methyl]sulfinyl]-5-(1 H-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: GrantFiled: December 28, 2007Date of Patent: August 16, 2011Assignee: 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: 20110195964Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: October 19, 2009Publication date: August 11, 2011Inventors: Qun Dang, De Michael Chung, Tony S. Gibson, Daniel K. Cashion, HongJian Jiang, Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka
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Patent number: 7989632Abstract: The invention relates to crystalline forms of various solvates of 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 crystalline ilaprazole hydrate 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: GrantFiled: December 28, 2007Date of Patent: August 2, 2011Assignee: Il Yang Pharmaceutical Company, Ltd.Inventors: John M. Brackett, David T. Jonaitis, Wei Lai, Jih Hua Liu, Stephan D. Parent
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Publication number: 20110184182Abstract: Disclosed herein are novel compounds which are useful as intermediates for producing substituted sulfoxide compounds and a process for producing the same. Further disclosed is a process for producing the substituted sulfoxide compounds used as pharmacologically active agents, employing the novel intermediates of the present invention.Type: ApplicationFiled: September 29, 2009Publication date: July 28, 2011Applicant: MATRIX LABORATORIES LIMITEDInventors: Saswata Lahiri, Lakshmana Rao Vadali, Swamy Saidugari, Verra Narayana Bandlamudi, Parameshwar Makam, Seshadri Rao Manukonda, Debashish Datta
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Publication number: 20110166183Abstract: A process for preparing esomeprazole sodium comprises the steps of providing a solution of esomeprazole sodium in a solvent constituted mainly of methanol or only of methanol; and carrying out precipitation or crystallisation of esomeprazole sodium from said solution. Esomeprazole sodium is preferably obtained from pure form of neutral racemate through chiral chromatography using methanol-based mobile phase, and a subsequent reaction with sodium source. Novel crystal and semicrystal forms of esomeprazole sodium can be provided repeatedly and in physically stable and highly pure form.Type: ApplicationFiled: July 8, 2009Publication date: July 7, 2011Inventor: Dejan Mandic