Halogen Or Nitro Attached Directly Or Indirectly To The Quinoline Ring System By Nonionic Bonding Patents (Class 546/180)
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Patent number: 9487487Abstract: Disclosed is a process for the preparation of montelukast sodium. The process comprises a) reacting 2-(2-(3(S)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-hydroxypropyl)phenyl)-2-propanol with methane sulfonyl chloride and coupling the resultant mesylate compound with 1-(mercaptomethyl)cyclopropane acetic acid in presence of a base and free alkali source followed by saltification with an amine in a single step reaction and b) converting the montelukast amine salt to montelukast sodium salt.Type: GrantFiled: May 17, 2013Date of Patent: November 8, 2016Assignee: LAURUS LABS PRIVATE LIMITEDInventors: Srinivas Simhadri, Yaseen Mohammad, Venkata S. Indukuri, Seeta R. Gorantla, Satyanarayana Chava
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Patent number: 8940499Abstract: The present disclosure provides a reagent for blood analysis which may include: (1) a compound having the general formula I as a fluorescent dye, wherein n, X, R1, R2, R3, R4, R5 and Y? are as defined in the specification; (2) a surfactant selected from cationic surfactants, zwitterionic surfactants and anionic surfactants. The present disclosure also provides a method to perform blood analysis including the following steps of: (a) mixing the blood sample with the reagent for blood analysis disclosed to form a cell suspension; (b) detecting the scattered light signals and fluorescence signals from the cells; and (c) differentiating and counting the cells in the blood in terms of the scattered light signals and fluorescence signals.Type: GrantFiled: October 16, 2009Date of Patent: January 27, 2015Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventors: Yuji Kuang, Baohua Zhang, Bing Xu, Jianhui Shao, Ting Lei, Li Zhang
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Publication number: 20140296529Abstract: The present disclosure relates to a bis-quinaldine compound of formula I and a process for the same. wherein R2 is a substituent selected from the group consisting of H, C1-C20 straight or branched chain alkyl substituents, aromatic substituents, aliphatic substituents, combinations thereof and the like.Type: ApplicationFiled: October 22, 2012Publication date: October 2, 2014Inventor: Keki Hormusji GHARDA
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Publication number: 20140235548Abstract: Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed. The compounds and compositions inhibit the enzymatic activity of a JAMM domain, including the JAMM domain of the CSN5 subunit of the COP9-signalsome (CSN), the JAMM domain of the Rpn11/Poh1/Psmd14 subunit of the 26S proteasome, the JAMM domain of AMSH, the JAMM domain of AMSH-LP, the JAMM domain of BRCC36, among other JAMM domains.Type: ApplicationFiled: May 10, 2012Publication date: August 21, 2014Applicant: Cleave Biosciences, Inc.Inventors: Han-Jie Zhou, Francesco Parlati, Matthieu Roufflet, Ethan D. Emberley, Raymond J. Deshaies, Seth Cohen
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Publication number: 20140228572Abstract: Provided are a novel chiral iridium(III) complex; and a method for producing optically active 2-substituted-1,2,3,4-tetrahydroquinolines from 2-substituted-quinolines with the use of the chiral iridium(III) complex through a more economical and easy production process.Type: ApplicationFiled: July 13, 2012Publication date: August 14, 2014Applicant: HAMARI CHEMICALS, LTD.Inventors: Sadayuki Maeda, Tatsunori Sato, Yasuhiko Kawano, Toshio Miyawaki
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Publication number: 20140221655Abstract: The invention provides methods for substituting polyaromatic hydrocarbons or polyheterocyclic compounds with perfluoroalkyl groups. The methods can include heating a polyaromatic hydrocarbon substrate or a polyheterocyclic compound substrate in the presence of a perfluoroalkyl iodide, typically in a closed system, wherein the heating is sufficient to bring both the polyaromatic hydrocarbons or polyheterocyclic compound, and the perfluoroalkyl iodide, into the gas phase, thereby allowing the substrate to react with the perfluoroalkyl iodide in the gas phase to form polyaromatic hydrocarbons or polyheterocyclic compounds having one or more perfluoroalkyl substituents. The methods allow for the creation of versatile libraries of novel perfluoroalkyl-containing derivatives that can serve as important building blocks and active components in biomedical, electronic, and materials applications.Type: ApplicationFiled: February 6, 2014Publication date: August 7, 2014Applicant: Colorado State University Research FoundationInventors: Steven S. Strauss, Olga V. Boltalina, Igor V. Kuvychko
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Publication number: 20140088079Abstract: The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.Type: ApplicationFiled: June 1, 2012Publication date: March 27, 2014Applicant: GREEN CROSS CORPORATIONInventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon KIM, Dong Ho Hong, Misuk Kang
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Patent number: 8653260Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: June 20, 2012Date of Patent: February 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
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Patent number: 8592175Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; U is N or N+R and V is CZ6N or N+R or V is N or N+R and U is CZ6, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; and Z1, Z2, Z3, Z4, Z5 and Z6 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.Type: GrantFiled: July 29, 2010Date of Patent: November 26, 2013Assignee: bioMérieux, S.A.Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
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Patent number: 8592174Abstract: The present invention relates to the use of a compound of the following formula (I), as an enzyme substrate for the detection of a peptidase activity or as a pH indicator: according to which: Y1 is a peptide, H or an alkyl; W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination thereof; n=0, 1 or 2; U is N or N+R and V is CZ6N or N+R or else V is N or N+R and U is CZ6; R is H, alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl; Z1, Z2, Z3, Z4 and Z5 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulfonyl, including the carboxyl or sulfonyl esters or amides, and salts thereof.Type: GrantFiled: July 28, 2010Date of Patent: November 26, 2013Assignee: bioMérieux, S.A.Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
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Patent number: 8586739Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.Type: GrantFiled: May 10, 2012Date of Patent: November 19, 2013Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20130296561Abstract: The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.Type: ApplicationFiled: January 13, 2012Publication date: November 7, 2013Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.Inventors: Karin Henderika Maria Bessembinder, Dennis Heemskerk, Ben De Lange
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Patent number: 8569508Abstract: A synthesis method for preparing Montelukast sodium intermediate 2-(2-(3-(2-(7-chloro-2-quinolyl)vinyl)phenyl-3-oxopropyl)phenyl) propanol is provided. In this method, the target compound is prepared by condensing the starting materials 7-chloroquinaldine and 3-cyanobenzaldehyde, and then reacting the resultant product with 2-(2-ortho-(2-haloethyl)-phenylpropyl)tetrahydropyrane ether. The present invention can easily obtain start materials and is applicable for mass production.Type: GrantFiled: August 24, 2010Date of Patent: October 29, 2013Assignee: Shandong New Time Pharmaceutical Co., Ltd.Inventors: Zhiquan Zhao, Haixin Wang, Zengxue Wang
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Patent number: 8524739Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).Type: GrantFiled: April 25, 2011Date of Patent: September 3, 2013Assignee: State of Oregon acting by and through the State Board of Higher Education on behalf of Portland State UniversityInventors: David H. Peyton, Steven Burgess
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Publication number: 20130225815Abstract: A method of forming a fluorinated molecular entity includes reacting in a reaction mixture an aromatic halide, copper, a fluoroalkyl group, and a ligand. The aromatic halide includes an aromatic group and a halogen substituent bonded to the aromatic group. The ligand includes at least one group-V donor selected from phosphorus and an amine. The overall molar ratio of copper to aromatic halide in the reaction mixture is from 0.2 to 3. The method further includes forming a fluoroalkylarene including the aromatic group and the fluoroalkyl group bonded to the aromatic group. A composition, which may be used in the method, consists essentially of copper, the fluoroalkyl group, and the ligand, where the molar ratio of copper to the fluoroalkyl group is approximately 1.Type: ApplicationFiled: February 19, 2013Publication date: August 29, 2013Applicant: The Board of Trustees of the University of IllinoisInventors: John F. Hartwig, Hiroyuki Morimoto, Patrick Fier
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Patent number: 8481742Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.Type: GrantFiled: March 13, 2012Date of Patent: July 9, 2013Assignee: Kaneq Pharma Inc.Inventors: John Colucci, Marie-Claire Wilson, Yongxin Han, Claude Dufresne, Michel Belley, Cheuk K. Lau, Christopher Bayly
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Patent number: 8476432Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.Type: GrantFiled: June 30, 2011Date of Patent: July 2, 2013Assignee: Yuhan CorporationInventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
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Publication number: 20130131036Abstract: Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.Type: ApplicationFiled: October 23, 2012Publication date: May 23, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Patent number: 8399675Abstract: This invention relates to novel compounds and a process for preparation of montelukast sodium.Type: GrantFiled: February 22, 2010Date of Patent: March 19, 2013Assignee: Formosa Laboratories, Inc.Inventors: Jui-Te Hung, Ching-Peng Wei
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Patent number: 8367834Abstract: A method for the preparation of montelukast and salts thereof has been described. The method comprises of following steps: (a) (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyljpropyl methane sulphonate (styrene mesylate salt) (b) coupling with 1-(mercaptomethyl)cyclopropane acetic acid followed by salification with an amine gives styrene amine salt (c) Converting styrene amine salt to Montelukast amine salt (d) Converting Montelukast amine salt to Montelukast free acid and or its required alkali/alkaline salt.Type: GrantFiled: May 17, 2012Date of Patent: February 5, 2013Assignee: Laurus Labs Private LimitedInventors: Venkata Sunil Kumar Indukuri, Srinivas Simhadri, Satyanarayana Chava
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Publication number: 20130012503Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 20, 2012Publication date: January 10, 2013Applicant: VIAMET PHARMACEUTICALS, INC.Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson
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Publication number: 20120316341Abstract: Methods for fluorinating organic compounds are described herein.Type: ApplicationFiled: April 11, 2012Publication date: December 13, 2012Inventors: Tobias Ritter, Pingping Tang
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Publication number: 20120289702Abstract: Provided is an agricultural fungicide that contains at least one selected from the group consisting of a novel nitrogen-containing heterocyclic compound represented by Formula (I), a salt thereof, or an N-oxide compound thereof. In Formula (I), R represents a group represented by CR1R2R3 or a cyano group. R1 to R3 each independently represents a hydrogen atom, an unsubstituted or substituted C1-8 alkyl group, an unsubstituted or substituted hydroxyl group, or the like. R4 or R5 represents a halogeno group or the like. Y or Z represents a carbon atom or the like, and A or D represents a benzene ring or the like. X represents an oxygen atom or a nitrogen atom or the like.Type: ApplicationFiled: December 28, 2010Publication date: November 15, 2012Applicant: Nippon Soda Co., Ltd.Inventors: Kotaro Shibayama, Jun Inagaki, Yuto Saiki, Akira Mitani, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Mami Kuboki
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Publication number: 20120215002Abstract: The present invention relates to the synthesis of optically active alcohols by means of enantioselective hydrogenation of ketones in biphasic systems. In particular the present invention relates to the synthesis of an optically active alcohol of general formula (1).Type: ApplicationFiled: October 5, 2010Publication date: August 23, 2012Inventor: Laurent Lefort
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Patent number: 8207343Abstract: A method for the preparation of montelukast and salts thereof has been described. The method comprises of following steps: (a) (S)-1-(3-((E)-2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-isopropenylphenyl)propyl methane sulphonate (styrene mesylate salt) (b) coupling with 1-(mercapto methyl)cyclopropane acetic acid followed by salification with an amine gives styrene amine salt (c) Converting styrene amine salt to Montelukast amine salt (d) Converting Montelukast amine salt to Montelukast free acid and or its required alkali/alkaline salt.Type: GrantFiled: May 25, 2009Date of Patent: June 26, 2012Assignee: Laurus Labs Private LimitedInventors: Venkata Sunil Kumar Indukuri, Srinivas Simhadri, Satyanarayana Chava
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Patent number: 8193199Abstract: Substituted bicyclic heteroaryls having the structures: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid LeukemiType: GrantFiled: March 24, 2008Date of Patent: June 5, 2012Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20120129204Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; U is N or N+R and V is CZ6 N or N+R or V is N or N+R and U is CZ6, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; and Z1, Z2, Z3, Z4, Z5 and Z6 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.Type: ApplicationFiled: July 29, 2010Publication date: May 24, 2012Applicant: bioMerieux, SAInventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
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Publication number: 20120035371Abstract: The current invention describes novel chiral synthetic routes and intermediates for the manufacture of chiral anti-inflammatory agents of general formula VIII in which at least one of the groups X1, X2, X3 is selected from fluoro, chloro, bromo, hydroxy, methoxy, ethoxy, trifluoromethyl, amino whereas the other groups X1, X2, X3 have the meaning of a hydrogen atom, in which at least one of the groups Z1, Z2, Z3 is selected from —O—, —S—, —NH—, —N(—CH3)—, whereas the other groups Z1, Z2, Z3 have the meaning of a —CH2— group, and in which Ar is an aromatic group.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Inventor: Steffen SCHWEIZER
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Patent number: 8106206Abstract: Provided is a solid luminescent quinoline compound capable of emitting light in a crystalline state, capable of changing the luminescent color not requiring modification of molecular configuration and capable of emitting light in response to external pressure such as heat, physical pressure, etc. The quinoline compound is represented by the following general formula (1): wherein R1 may be the same or different, each representing any of CF3 or CF3CF2; R2 represents any of an amino group, an N,N-dimethylamino group, an N-phenylamino group, a carbazole group, an N-methylamino group or an N-methyl-N-phenylamino group.Type: GrantFiled: November 19, 2010Date of Patent: January 31, 2012Assignee: Kyushu University, National University CorporationInventors: Noboru Koga, Satoru Karasawa, Yuichiro Abe
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Patent number: 8067602Abstract: Asymmetric cyanine fluorescent dyes are represented by general formula I. These kinds of dyes may be used as a staining agent for nucleic acids, with the spectra at 600-900 nm in the near-infrared region and without interference from background fluorescence. These kinds of dyes may be useful with small-type red semiconductor lasers as the light source (such as 633 nm). Compositions comprising these dyes and methods for staining biological samples using these dyes or compositions are also provided.Type: GrantFiled: December 12, 2008Date of Patent: November 29, 2011Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventor: Jianhui Shao
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Patent number: 8017775Abstract: An object of the present invention is to study synthesis of a novel 1,2-dihydroquinoline derivative and to find a pharmacological action of the derivative. A compound represented by the general formula (1) or a salt thereof is effective in the treatment of a glucocorticoid receptor-related disease. In the formula, the ring X represents a benzene ring or a pyridine ring; R1 represents a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, an amino group or the like; p represents an integer of 0 to 5; R2 represents a halogen atom, an alkyl group, a hydroxy group or the like; q represents an integer of 0 to 2; R3 represents a hydrogen atom, an alkyl group, an alkenyl group or the like; R4 and R5 represent a hydrogen atom or the like; R6 represents a hydrogen atom or the like; A represents an alkylene group or the like; and R7 represents OR8, NR8R9, SR8, S(O)R8 or S(O)2R8, wherein R8 represents an aryl group, a heterocyclic group or the like and R9 represents a hydrogen atom or the like.Type: GrantFiled: September 14, 2006Date of Patent: September 13, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Toshiyuki Mori, Kenji Kawashima, Masato Nagatsuka, Sachiko Kobayashi, Minoru Yamamoto, Masatomo Kato, Miwa Takai, Tomoko Oda
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Patent number: 8008498Abstract: The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represents a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a nitro group or a cyano group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; and P represents 0, 1, 2 or 3.Type: GrantFiled: November 14, 2007Date of Patent: August 30, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Patent number: 8008496Abstract: The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represent a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or a nitro group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; Z represents a chalcogen atom; and P represents 0, 1, 2 or 3.Type: GrantFiled: November 14, 2007Date of Patent: August 30, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Patent number: 8008497Abstract: The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represent a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a nitro group or a cyano group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; Z represents a benzene ring or a heterocyclic ring; and P represents 0, 1, 2 or 3.Type: GrantFiled: November 14, 2007Date of Patent: August 30, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Publication number: 20110144344Abstract: The present invention provides an improved method for fluoridation of an iodonium salt wherein a solution of the iodonium salt comprising a free radical trap is stored before the reaction is carried out. The method of the invention may be automated, which is particularly convenient when the method of the invention is radiofluoridation. As such the present invention also provides a cassette comprising the iodonium salt solution suitable for carrying out the method of the invention on an automated synthesizer.Type: ApplicationFiled: August 13, 2009Publication date: June 16, 2011Inventor: John Woodcraft
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Publication number: 20110137039Abstract: The present invention relates to an improved process for the preparation of 1-[[[(IR)-I-[3[(IE)-2-(7chloro-2-quino-linyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid and its salts using Methyl 2-[(3S)-[3-[(2E)-(7-chloro quinolin-2-yl)ethenyl]phenyl]-3-halopropyl]benzoate.Type: ApplicationFiled: November 24, 2010Publication date: June 9, 2011Inventors: CHAVA SATYANARAYANA, GORANTLA SEETA RAMANJANEYULU, INDUKURI VENKATA SUNIL KUMAR, SIMHADRI SRINIVAS, JAMMULA VEERA VENKATA KRISHNA KISHORE
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Patent number: 7928239Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions in such therapy.Type: GrantFiled: February 7, 2001Date of Patent: April 19, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, Bernd Riedl, Uday Khire, Jill E. Wood, Robert N. Sibley, Mary-Katherine Monahan, Joel Renick, David E. Gunn, Timothy B. Lowinger, William J. Scott, Roger A. Smith
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Patent number: 7786138Abstract: A compound of the following formula wherein R? is a straight or branched C1-C4 alkyl group is useful in processes associated with the synthesis of montelukast and its salts.Type: GrantFiled: November 20, 2006Date of Patent: August 31, 2010Assignee: Synthon BVInventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
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Publication number: 20100217004Abstract: Tertiary alcohols are prepared by reacting carboxylic esters with Grignard reagents in ethereal solvents in the presence of lanthanum trichloride and lithium chloride. The method is particularly suitable for the production of (?S)-?-[3-[(1E)-2-(7-chloro-2-quino-linyl)ethenyl]phenyl]-2-(1-hydroxy-1-methylethyl)benzenepropanol of formula (A) which is an intermediate in the production of montelukast.Type: ApplicationFiled: July 10, 2008Publication date: August 26, 2010Inventors: John McGarrity, Francis Djojo
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Publication number: 20100190987Abstract: The tertiary alcohol ?-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-2-(1-hydroxy-1-methylethyl)benzene-propanol, the (?S)-enantioner of which is an intermediate in the production of montelukast, is produced by reacting the novel lactone of formula (II) with a methylmagnesium halide in an ethereal solvent in the presence of lanthanum trichloride and lithium chloride. The lactone II can be prepared by reacting a corresponding hydroxyester with a Grignard reagent in the absence of a lanthanoid compound or with a strong base.Type: ApplicationFiled: July 10, 2008Publication date: July 29, 2010Inventors: John McGarrity, Francis Djojo
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Publication number: 20100152453Abstract: This invention relates to novel compounds and a process for preparation of montelukast sodium.Type: ApplicationFiled: February 22, 2010Publication date: June 17, 2010Applicant: FORMOSA LABORATORIES, INC.Inventors: Jui-Te Hung, Ching-Peng Wei
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Patent number: 7728007Abstract: The invention provides compounds of the formula: wherein X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions comprising a compound of the above formula or a salt thereof, intermediates useful for preparing a compound of the above formula, and therapeutic methods comprising administering a compound of the above formula or a salt thereof to a mammal in need thereof.Type: GrantFiled: October 29, 2008Date of Patent: June 1, 2010Assignee: Wayne State UniversityInventors: Jerome P. Horwitz, Thomas H. Corbett, Eduardo Palomino, Lisa Polin, Stuart T. Hazeldine
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Publication number: 20100099879Abstract: The reaction of methylmagnesium halide is improved by the presence of a cerium (III) salt such as cerium trichloride. The reactions are typically associated with the production of montelukast, a pharmaceutically useful compound of the following formula and salts thereof. Further enhancements can be derived from certain intermediates, salts thereof and/or purification thereof before and/or after the reaction involving methylmagnesium halide.Type: ApplicationFiled: October 9, 2009Publication date: April 22, 2010Inventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
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Patent number: 7700776Abstract: This invention relates to novel compounds and a process for preparation of montelukast sodium.Type: GrantFiled: October 24, 2006Date of Patent: April 20, 2010Assignee: Formosa Laboratories, Inc.Inventors: Jui-Te Hung, Ching-Peng Wei
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Publication number: 20100081688Abstract: The invention relates to processes for making montelukast and to intermediates for use in the process, in particular compounds of formulas 2-7: L=OAc, OTs, OTf5OMs; where X=Cl, Br, I.Type: ApplicationFiled: September 14, 2007Publication date: April 1, 2010Applicant: CIPLA LIMITEDInventor: Srinivas Laxminarayan Pathi
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Publication number: 20100022777Abstract: An improved, scalable, and environmentally friendly manufacturing procedure for the preparation of E-3-[2-(7-chloro-2-quinolinyl)ethenyl]benzaldehyde, which is a key early intermediate used in the preparation of montelukast sodium, and the compound prepared by such a process.Type: ApplicationFiled: October 29, 2008Publication date: January 28, 2010Applicant: Sterling Biotech LimitedInventors: Sugata Chatterjee, Ajay Singh Rawat, Neeraj Kumar, Mukesh Chavda, Rushikesh Kadu
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Publication number: 20100004271Abstract: The invention provides Compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, wherein R3, R4, G, Y, W and R5 are as defined in the specification. The invention also provides the use of such Compounds in the treatment or Prophylaxis of a condition associated with a disease or disorder associated with thyroid receptor activity.Type: ApplicationFiled: July 4, 2006Publication date: January 7, 2010Applicant: KARO BIO ABInventors: Ana Maria Garcia Collazo, Eva Kristina Koch, Anton Joakim Lofstedt, Aiping Cheng, Thomas Fredrik Hansson, Edouard Zamaratski
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Patent number: 7601741Abstract: The reaction of methylmagnesium halide is improved by the presence of a cerium (III) salt such as cerium trichloride. The reactions are typically associated with the production of montelukast, a pharmaceutically useful compound of the following formula and salts thereof. Further enhancements can be derived from certain intermediates, salts thereof and/or purification thereof before and/or after the reaction involving methylmagnesium halide.Type: GrantFiled: November 20, 2006Date of Patent: October 13, 2009Assignee: Synthon BVInventors: Petr Benovsky, Lambertus Thijs, Arjanne Overeem, Jakub Castulik, Jie Zhu, Petr Bartos, Radomir Skoumal
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Publication number: 20090143590Abstract: The present invention relates to an improved process for the preparation of 1-[[[(1R)-1-[3[(1E)-2-(7chloro-2-quinolinyl) ethenyl] phenyl]-3-[2-(1-hydroxy-1-methylethyl) phenyl] propyl] thio] methyl] cyclopropaneacetic acid (Formula-1) and its salts using Methyl 2-[(3S)-[3-[(2E)-(7-chloro quinolin-2-yl) ethenyl] phenyl]-3-halopropyl] benzoate (Formula-2)Type: ApplicationFiled: July 19, 2004Publication date: June 4, 2009Applicant: MATRIX LABORATORIES LTD.Inventors: Satyanarayana Chava, Seeta Ramanjaneyulu Gorantla, Venkata Sunil Kumar Indukuri, Srinivas Simhadri, Vera Venkata Krishna Kishore Jammula
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Patent number: 7528254Abstract: The present invention provides a process for preparing highly pure montelukast and salts thereof by reacting the side-chain precursor 1-(mercaptomethyl)-cyclopropaneacetic acid with 2-(2-(3S)-(3-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(methanesulfonyloxypropyl)phenyl-2-propanol in a solvent mixture containing a base.Type: GrantFiled: February 27, 2007Date of Patent: May 5, 2009Assignee: Chemagis Ltd.Inventors: Michael Brand, Moty Shookrun, Oded Arad, Joseph Kaspi