4- Or 5-position Substituent Contains Chalcogen Patents (Class 548/232)
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Patent number: 11142608Abstract: Described herein are processes for producing moldings comprising oxazolidinone groups, where polyisocyanate (a) is mixed with at least one organic compound (b) having two or more epoxide groups, at least one catalyst (c) for the isocyanate/epoxide reaction, and optionally auxiliary and additive materials (d) to form a reaction mixture, which is introduced into or applied to a mold and reacted to give moldings including oxazolidinone groups, where the catalyst (c) for the isocyanate/epoxide reaction includes a compound of the general formula [M(R1)(R2)(R3)(R4)]+ [X In]?, where M is a nitrogen atom or a phosphorus atom, R1, R2, R3 and R4 are an organic radical, X is fluorine, chlorine, bromine or iodine, I is iodine, and n stands for rational numbers from 0.1 to 10.Type: GrantFiled: March 15, 2018Date of Patent: October 12, 2021Inventors: Berend Eling, Hans-Josef Thomas, Peter Deglmann, Janina Hengelsberg, Tristan Pelzer, Gerrit A. Luinstra
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Publication number: 20150011776Abstract: Disclosed is a compound of formula 1, as shown below, where R1, R2, R3, R4, R5, R6 and R7 are as described herein. Also, disclosed is a process for the preparation of compounds of formula 1, and intermediates used therein. The compound of formula 1 can be useful for preparation of halichondrin analogs such as Eribulin.Type: ApplicationFiled: December 24, 2012Publication date: January 8, 2015Inventors: Fabio E.S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Dino Alberico
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Patent number: 8912291Abstract: Embodiments include oxazolidone ring containing adducts obtainable by combining an aliphatic epoxy compound, an aromatic epoxy compound, and a diisocyanate. Embodiments further include a curable powder coating composition including a resin component and a hardener component, where the resin component includes the oxazolidone ring containing adduct.Type: GrantFiled: December 20, 2010Date of Patent: December 16, 2014Assignee: DOW Global Technologies LLCInventors: Joseph Gan, Emile C. Trottier
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Publication number: 20140364398Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: PFIZER INC.Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
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Patent number: 8895741Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.Type: GrantFiled: September 14, 2012Date of Patent: November 25, 2014Assignee: Melinta Therapeutics, Inc.Inventors: Yusheng Wu, Shili Chen, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
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Patent number: 8871793Abstract: The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalone adipic acid cocrystal, a 1:0.5 metaxalone fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them.Type: GrantFiled: December 22, 2010Date of Patent: October 28, 2014Assignee: Nuformix LimitedInventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
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Patent number: 8822516Abstract: This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.Type: GrantFiled: June 9, 2011Date of Patent: September 2, 2014Assignee: Technion Research & Development Foundation LimitedInventors: Gennady Nisnevich, Mark Gandelman, Kseniya Kulbitski
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Publication number: 20140221373Abstract: The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein A1, A2, A3, L1, L2 and D are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the Compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: July 17, 2012Publication date: August 7, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alexander Heim-Riether, Anil Kumar Padyana, Shuang Liang, Steven John Taylor, Qiang Zhang
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Patent number: 8722715Abstract: The present application relates to N-chlorinated oxazolidinone, hydantoin and imidazolidinone compounds of Formula I or pharmaceutically acceptable salts thereof, and associated compositions and methods of use as antimicrobial agents.Type: GrantFiled: November 4, 2009Date of Patent: May 13, 2014Assignee: NovaBay PharmaceuticalsInventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Bum Kim, Satheesh K. Nair
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Publication number: 20140121299Abstract: A liquid adduct consisting essentially of a reaction product of (a) an aliphatic epoxy resin, and (b) an isocyanate compound, wherein the viscosity of the adduct comprises less than about 60 Pa-s at about 25° C. is disclosed. The adduct can be used in an epoxy resin composition.Type: ApplicationFiled: July 4, 2011Publication date: May 1, 2014Applicant: DOW GLOBAL TECHNOLOGIES LLCInventors: Yan L. Feng, Joseph Gan, Wayne Y. Zhang, Patrick P. Yan
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Publication number: 20140100195Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: October 5, 2012Publication date: April 10, 2014Inventors: Richard D. Caldwell, Kevin M. GUCKIAN, Gnanasambandam KUMARA VEL, Wen-Cherng LEE, Edward Yin-Shiang LIN, Xiaogao LlU, Bin MA, Daniel M. SCOTT, Zhan SHl, Jermaine THOMAS, Arthur G. TAVERAS, Guo Zhu ZHENG
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Publication number: 20140039198Abstract: An object of the present invention is to provide a pyrrole derivative useful as an immunosuppressive agent and a method for producing the same. For achieving the object, the present invention provides a method for producing a compound represented by the general formula (I) by heating a compound represented by the general formula (III) and a compound represented by the general formula (IV) in a nonpolar solvent under reduced pressure.Type: ApplicationFiled: May 31, 2013Publication date: February 6, 2014Inventors: Makoto YAMAOKA, Yoshitaka NAKAMURA
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Publication number: 20130296281Abstract: The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: June 16, 2011Publication date: November 7, 2013Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Chiyou Ni, Laykea Tafesse, Jiangchao Yao
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Publication number: 20130261160Abstract: The present invention relates to a method of preparation of metaxalone comprising reaction of triglycidyl isocyanurate (TGIC) with m-xylenol, characterized in that said reaction is carried out in a solvent mixture comprising an aprotic polar solvent with dielectric constant greater than or equal to 30 and at least one other solvent selected from the group comprising apolar solvents and aprotic polar solvents with dielectric constant below 30 said solvent mixture comprising from 5 to 40 wt. % of said first solvent and from 95 to 60 wt. % of said second solvent, adding the TGIC at a temperature between 30° C. and 50° C., and after adding the TGIC, raising the temperature of the reaction solution to a value between 80° C. and 180° C. in a time between 120 and 180 minutes at a rate of increase not greater that 1.25° C. per minute. The invention also relates to a metaxalone with a reduced content of impurities derived from incomplete reactions and/or side reactions of the method of production.Type: ApplicationFiled: January 17, 2012Publication date: October 3, 2013Applicant: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.Inventors: Tommaso Iacoangeli, Mario Chiavarini, Antonello Fazio, Marcello Marchetti, Giovanni Battista Ciottoli
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Publication number: 20130217732Abstract: This invention provides compounds of formula I, pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds and intermediates useful in the preparation of same.Type: ApplicationFiled: September 27, 2011Publication date: August 22, 2013Inventor: Chris P. Miller
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Publication number: 20130210769Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
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Publication number: 20130158083Abstract: The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalone adipic acid cocrystal, a 1:0.5 metaxalone fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them.Type: ApplicationFiled: December 22, 2010Publication date: June 20, 2013Inventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
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Publication number: 20130066076Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.Type: ApplicationFiled: September 14, 2012Publication date: March 14, 2013Inventors: Yusheng Wu, Shili Chen, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
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Publication number: 20120283264Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.Type: ApplicationFiled: November 2, 2011Publication date: November 8, 2012Inventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
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Publication number: 20120202773Abstract: A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).Type: ApplicationFiled: April 23, 2012Publication date: August 9, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Toru Maruyama, Kaoru Kobayashi, Tohru Kambe, Takayuki Maruyama, Hideyuki Yoshida, Akio Nishiura, Nobutaka Abe
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Publication number: 20120010200Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20110306773Abstract: An improved process for the preparation of Metaxalone of formula I wherein, reacting 3,5-dimethyl phenol with 3-chloro-1,2-propane diol in presence of a base, to produce 3-(3,5-dimethylphenoxy)propane-1,2-diol which is further reacted with urea in presence of polyalkylene glycol to obtain Metaxalone, which is optionally crystallized in ethyl acetate in presence of mineral acid.Type: ApplicationFiled: April 12, 2011Publication date: December 15, 2011Inventor: Battula Srinivasa Reddy
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Publication number: 20110294813Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: ApplicationFiled: June 30, 2011Publication date: December 1, 2011Applicants: SHIONOGI & CO., LTD., INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20110190302Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”).Type: ApplicationFiled: September 18, 2009Publication date: August 4, 2011Applicant: PIMCO 2664 LIMITEDInventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
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Publication number: 20110172223Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 21, 2009Publication date: July 14, 2011Inventors: Prasun K. Chakravarty, Pengcheng Patrick Shao
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Publication number: 20110152332Abstract: The present invention relates to novel pesticidal azolidine derivatives as well as to oxazolidinone derivatives and their use as pesticides for combating animal parasites which occur in the agrochemical field and in the field of veterinary medicine, respectively. wherein X, m, R?, Q, G, U, l, A1 to A4 and R are as defined herein.Type: ApplicationFiled: November 1, 2010Publication date: June 23, 2011Applicant: Bayer CropScience AGInventors: Tetsuya Murata, Mamoru Hatazawa, Peter Brüchner, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
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Publication number: 20110152333Abstract: The invention provides new oxazolidinone compounds of formula (I) wherein R1, R2 and R3 have different meanings. Preparative processes, pharmaceutical compositions, and uses thereof in the treatment of bacterial infections are also provided.Type: ApplicationFiled: June 29, 2009Publication date: June 23, 2011Applicant: FERRER INTERNACIONAL, S.A.Inventors: Montserrat Cano, Albert Palomer, Antonio Guglietta
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Publication number: 20110136829Abstract: The invention provides new oxazolidinone compounds of formula (I) wherein R, R1, R2 and R3 have different meanings. Preparative processes, pharmaceutical compositions, and uses thereof in the treatment of bacterial infections are also provided.Type: ApplicationFiled: June 29, 2009Publication date: June 9, 2011Applicant: FERRER INTERNACIONAL, S.A.Inventors: Montserrat Cano, Albert Palomer, Antonio Guglietta
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Publication number: 20110092700Abstract: The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N? etc., Y3 and Y4 are selected from —CH? etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.Type: ApplicationFiled: December 3, 2010Publication date: April 21, 2011Inventors: Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
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Publication number: 20110009631Abstract: Compounds of the formula (II) and (IV) are provided, which may be employed as intermediates for making compounds useful in treating respiratory diseases.Type: ApplicationFiled: July 14, 2010Publication date: January 13, 2011Applicant: Glaxo Group LimitedInventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Inderjit Singh Mann, Panayiotis Alexandrou Procopiou
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Publication number: 20100292241Abstract: The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: January 14, 2009Publication date: November 18, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
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Publication number: 20100286211Abstract: The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: ApplicationFiled: October 6, 2005Publication date: November 11, 2010Inventors: Biswajit Das, Shahadal Ahmed, Ajay Singh Yadav, Soma Ghosh, Arti Gujrati, Pankaj Sharma, Ashok Rattan
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Patent number: 7781431Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: GrantFiled: September 7, 2004Date of Patent: August 24, 2010Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpAInventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
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Publication number: 20100160357Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: October 30, 2009Publication date: June 24, 2010Inventors: Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Xiaogao Liu, Bin Ma, Daniel M. Scott, Zhan Shi, Jermaine Thomas, Arthur G. Taveras, Guo Zhu Zheng
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Publication number: 20100137349Abstract: The present application relates to N-chlorinated oxazolidinone, hydantoin and imidazolidinone compounds of Formula I or pharmaceutically acceptable salts thereof, and associated compositions and methods of use as antimicrobial agents.Type: ApplicationFiled: November 4, 2009Publication date: June 3, 2010Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Bum Kim, Satheesh K. Nair
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Publication number: 20100113448Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: ApplicationFiled: March 27, 2008Publication date: May 6, 2010Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Patent number: 7705026Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: November 21, 2008Date of Patent: April 27, 2010Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20090270469Abstract: The present invention relates to new oxazolidinone modulators of skeletal muscle function and tone, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 22, 2009Publication date: October 29, 2009Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20090247527Abstract: A compound having the formula or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. Y, A, U, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.Type: ApplicationFiled: March 20, 2009Publication date: October 1, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
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Publication number: 20090233974Abstract: A compound having the formula or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.Type: ApplicationFiled: May 22, 2009Publication date: September 17, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
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Patent number: 7582666Abstract: The invention relates to the field of blood coagulation, more particularly, to novel compounds of general formula (I), to a method for producing the compounds and to their use as active ingredients in medicaments for the prevention and/or the treatment of diseases.Type: GrantFiled: March 31, 2006Date of Patent: September 1, 2009Assignee: Bayer Schering Pharma AGInventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Rohrig, Karl-Heinz Schlemmer
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Publication number: 20090163561Abstract: The present invention provides various amorphous forms of the compound metaxalone (I), such as solid amorphous metaxalone and amorphous dispersions comprising metaxalone. The present invention further provides pharmaceutical compositions comprising these amorphous forms, and methods of their preparation. The present invention additionally provides methods of treating painful conditions (e.g., such as painful musculoskeletal conditions) comprising administering a therapeutically effective amount of any one of these amorphous forms to a subject in need thereof.Type: ApplicationFiled: December 11, 2008Publication date: June 25, 2009Applicant: URL Pharma, Inc.Inventors: Keith Lorimer, Kevin Wayne Meyer, Tong Sun, Shawn Watson, Kurt R. Nielsen
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Publication number: 20090156653Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects:Type: ApplicationFiled: November 21, 2008Publication date: June 18, 2009Inventors: Yasushi Kohno, Kiyoaki Tanaka, Kazuhiko Kuriyama
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Publication number: 20080306279Abstract: In particular, this invention relates to the synthesis intermediates (IV), (V), (VI) and (VIII) useful for preparing zolmitriptanzohnitriptan or a pharmaceutically acceptable salt thereof, which includes a) Preparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with ?-keto-?-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Transesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Saponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Decarboxylation of the indolecarboxylic acid (VIII), to provide zType: ApplicationFiled: November 15, 2007Publication date: December 11, 2008Applicant: INKE, S.A.Inventors: Montserrat Armengol Asparo, Pere Dalmases Barjoan
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Patent number: 7456206Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: July 14, 2006Date of Patent: November 25, 2008Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20080221182Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.Type: ApplicationFiled: May 21, 2008Publication date: September 11, 2008Applicant: NEREUS PHARMACEUTICALS, INC.Inventors: Venkata Rami Reddy Macherla, Benjamin Nicholson, Kin Sing Lam
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Patent number: 7417156Abstract: In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (I), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60° C. for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer activities.Type: GrantFiled: September 26, 2003Date of Patent: August 26, 2008Assignee: Johns Hopkins UniversityInventors: Gary H. Posner, Theresa A. Shapiro, Surojit Sur, Tanzina Labonte, Kristina Borstnik, Ik-Hyeon Paik, Andrew J. McRiner
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Patent number: 7358254Abstract: A method is provided for treating atherosclerosis and related diseases, employing an aP2 inhibitor or a combination of an aP2 inhibitor and another antiatherosclerotic agent, for example, an HMG CoA reductase inhibitor such as pravastatin.Type: GrantFiled: June 21, 2004Date of Patent: April 15, 2008Assignees: Bristol-Myers Squibb Company, President & Fellows of Harvard CollegeInventors: Jeffrey A. Robl, Rex A. Parker, Scott A. Biller, Haris Jamil, Bruce L. Jacobson, Krishna Kodukula, Gokhan Hotamisligil
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Patent number: 7348342Abstract: We describe substituted benzenesulfoximine compounds having anti-inflammatory activity, processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of inflammatory diseases.Type: GrantFiled: April 1, 2003Date of Patent: March 25, 2008Assignee: Cadila Healthcare LimitedInventors: Braj B. Lohray, Vidya B. Lohray, Mukul R. Jain, Gautam D. Patel, Harikishore Pingali
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Patent number: 7259263Abstract: The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I): The invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method.Type: GrantFiled: June 29, 2005Date of Patent: August 21, 2007Assignee: Jansen Pharmaceutica N.V.Inventors: Dennis J. Hlasta, Craig A. Zificsak