4- Or 5-position Substituent Contains Chalcogen Patents (Class 548/232)
  • Publication number: 20150011776
    Abstract: 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: Application
    Filed: December 24, 2012
    Publication date: January 8, 2015
    Inventors: Fabio E.S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Dino Alberico
  • Patent number: 8912291
    Abstract: 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: Grant
    Filed: December 20, 2010
    Date of Patent: December 16, 2014
    Assignee: DOW Global Technologies LLC
    Inventors: Joseph Gan, Emile C. Trottier
  • Publication number: 20140364398
    Abstract: 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: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER INC.
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
  • Patent number: 8895741
    Abstract: 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: Grant
    Filed: September 14, 2012
    Date of Patent: November 25, 2014
    Assignee: Melinta Therapeutics, Inc.
    Inventors: Yusheng Wu, Shili Chen, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
  • Patent number: 8871793
    Abstract: 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: Grant
    Filed: December 22, 2010
    Date of Patent: October 28, 2014
    Assignee: Nuformix Limited
    Inventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
  • Patent number: 8822516
    Abstract: 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: Grant
    Filed: June 9, 2011
    Date of Patent: September 2, 2014
    Assignee: Technion Research & Development Foundation Limited
    Inventors: Gennady Nisnevich, Mark Gandelman, Kseniya Kulbitski
  • Publication number: 20140221373
    Abstract: 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: Application
    Filed: July 17, 2012
    Publication date: August 7, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alexander Heim-Riether, Anil Kumar Padyana, Shuang Liang, Steven John Taylor, Qiang Zhang
  • Patent number: 8722715
    Abstract: 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: Grant
    Filed: November 4, 2009
    Date of Patent: May 13, 2014
    Assignee: NovaBay Pharmaceuticals
    Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Bum Kim, Satheesh K. Nair
  • Publication number: 20140121299
    Abstract: 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: Application
    Filed: July 4, 2011
    Publication date: May 1, 2014
    Applicant: DOW GLOBAL TECHNOLOGIES LLC
    Inventors: Yan L. Feng, Joseph Gan, Wayne Y. Zhang, Patrick P. Yan
  • Publication number: 20140100195
    Abstract: 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: Application
    Filed: October 5, 2012
    Publication date: April 10, 2014
    Inventors: 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
  • Publication number: 20140039198
    Abstract: 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: Application
    Filed: May 31, 2013
    Publication date: February 6, 2014
    Inventors: Makoto YAMAOKA, Yoshitaka NAKAMURA
  • Publication number: 20130296281
    Abstract: 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: Application
    Filed: June 16, 2011
    Publication date: November 7, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: Donald J. Kyle, Chiyou Ni, Laykea Tafesse, Jiangchao Yao
  • Publication number: 20130261160
    Abstract: 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: Application
    Filed: January 17, 2012
    Publication date: October 3, 2013
    Applicant: 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
  • Publication number: 20130217732
    Abstract: 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: Application
    Filed: September 27, 2011
    Publication date: August 22, 2013
    Inventor: Chris P. Miller
  • Publication number: 20130210769
    Abstract: 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: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Applicant: IRM LLC
    Inventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
  • Publication number: 20130158083
    Abstract: 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: Application
    Filed: December 22, 2010
    Publication date: June 20, 2013
    Inventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
  • Publication number: 20130066076
    Abstract: 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: Application
    Filed: September 14, 2012
    Publication date: March 14, 2013
    Inventors: Yusheng Wu, Shili Chen, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
  • Publication number: 20120283264
    Abstract: 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: Application
    Filed: November 2, 2011
    Publication date: November 8, 2012
    Inventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
  • Publication number: 20120202773
    Abstract: 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: Application
    Filed: April 23, 2012
    Publication date: August 9, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Toru Maruyama, Kaoru Kobayashi, Tohru Kambe, Takayuki Maruyama, Hideyuki Yoshida, Akio Nishiura, Nobutaka Abe
  • Publication number: 20120010200
    Abstract: 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: Application
    Filed: September 22, 2011
    Publication date: January 12, 2012
    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
  • Publication number: 20110306773
    Abstract: 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: Application
    Filed: April 12, 2011
    Publication date: December 15, 2011
    Inventor: Battula Srinivasa Reddy
  • Publication number: 20110294813
    Abstract: 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: Application
    Filed: June 30, 2011
    Publication date: December 1, 2011
    Applicants: SHIONOGI & CO., LTD., INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.
    Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
  • Publication number: 20110190302
    Abstract: 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: Application
    Filed: September 18, 2009
    Publication date: August 4, 2011
    Applicant: PIMCO 2664 LIMITED
    Inventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
  • Publication number: 20110172223
    Abstract: 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: Application
    Filed: September 21, 2009
    Publication date: July 14, 2011
    Inventors: Prasun K. Chakravarty, Pengcheng Patrick Shao
  • Publication number: 20110152332
    Abstract: 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: Application
    Filed: November 1, 2010
    Publication date: June 23, 2011
    Applicant: Bayer CropScience AG
    Inventors: Tetsuya Murata, Mamoru Hatazawa, Peter Brüchner, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
  • Publication number: 20110152333
    Abstract: 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: Application
    Filed: June 29, 2009
    Publication date: June 23, 2011
    Applicant: FERRER INTERNACIONAL, S.A.
    Inventors: Montserrat Cano, Albert Palomer, Antonio Guglietta
  • Publication number: 20110136829
    Abstract: 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: Application
    Filed: June 29, 2009
    Publication date: June 9, 2011
    Applicant: FERRER INTERNACIONAL, S.A.
    Inventors: Montserrat Cano, Albert Palomer, Antonio Guglietta
  • Publication number: 20110092700
    Abstract: 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: Application
    Filed: December 3, 2010
    Publication date: April 21, 2011
    Inventors: 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
  • Publication number: 20110009631
    Abstract: Compounds of the formula (II) and (IV) are provided, which may be employed as intermediates for making compounds useful in treating respiratory diseases.
    Type: Application
    Filed: July 14, 2010
    Publication date: January 13, 2011
    Applicant: Glaxo Group Limited
    Inventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Inderjit Singh Mann, Panayiotis Alexandrou Procopiou
  • Publication number: 20100292241
    Abstract: 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: Application
    Filed: January 14, 2009
    Publication date: November 18, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
  • Publication number: 20100286211
    Abstract: 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: Application
    Filed: October 6, 2005
    Publication date: November 11, 2010
    Inventors: Biswajit Das, Shahadal Ahmed, Ajay Singh Yadav, Soma Ghosh, Arti Gujrati, Pankaj Sharma, Ashok Rattan
  • Patent number: 7781431
    Abstract: 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: Grant
    Filed: September 7, 2004
    Date of Patent: August 24, 2010
    Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
    Inventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
  • Publication number: 20100160357
    Abstract: 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: Application
    Filed: October 30, 2009
    Publication date: June 24, 2010
    Inventors: 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
  • Publication number: 20100137349
    Abstract: 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: Application
    Filed: November 4, 2009
    Publication date: June 3, 2010
    Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Bum Kim, Satheesh K. Nair
  • Publication number: 20100113448
    Abstract: 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: Application
    Filed: March 27, 2008
    Publication date: May 6, 2010
    Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.
    Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
  • Patent number: 7705026
    Abstract: 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: Grant
    Filed: November 21, 2008
    Date of Patent: April 27, 2010
    Assignee: 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
  • Publication number: 20090270469
    Abstract: The present invention relates to new oxazolidinone modulators of skeletal muscle function and tone, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: April 22, 2009
    Publication date: October 29, 2009
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20090247527
    Abstract: 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: Application
    Filed: March 20, 2009
    Publication date: October 1, 2009
    Applicant: ALLERGAN, INC.
    Inventor: David W. Old
  • Publication number: 20090233974
    Abstract: 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: Application
    Filed: May 22, 2009
    Publication date: September 17, 2009
    Applicant: ALLERGAN, INC.
    Inventor: David W. Old
  • Patent number: 7582666
    Abstract: 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: Grant
    Filed: March 31, 2006
    Date of Patent: September 1, 2009
    Assignee: Bayer Schering Pharma AG
    Inventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Rohrig, Karl-Heinz Schlemmer
  • Publication number: 20090163561
    Abstract: 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: Application
    Filed: December 11, 2008
    Publication date: June 25, 2009
    Applicant: URL Pharma, Inc.
    Inventors: Keith Lorimer, Kevin Wayne Meyer, Tong Sun, Shawn Watson, Kurt R. Nielsen
  • Publication number: 20090156653
    Abstract: 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: Application
    Filed: November 21, 2008
    Publication date: June 18, 2009
    Inventors: Yasushi Kohno, Kiyoaki Tanaka, Kazuhiko Kuriyama
  • Publication number: 20080306279
    Abstract: 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 z
    Type: Application
    Filed: November 15, 2007
    Publication date: December 11, 2008
    Applicant: INKE, S.A.
    Inventors: Montserrat Armengol Asparo, Pere Dalmases Barjoan
  • Patent number: 7456206
    Abstract: 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: Grant
    Filed: July 14, 2006
    Date of Patent: November 25, 2008
    Assignee: 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
  • Publication number: 20080221182
    Abstract: 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: Application
    Filed: May 21, 2008
    Publication date: September 11, 2008
    Applicant: NEREUS PHARMACEUTICALS, INC.
    Inventors: Venkata Rami Reddy Macherla, Benjamin Nicholson, Kin Sing Lam
  • Patent number: 7417156
    Abstract: 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: Grant
    Filed: September 26, 2003
    Date of Patent: August 26, 2008
    Assignee: Johns Hopkins University
    Inventors: Gary H. Posner, Theresa A. Shapiro, Surojit Sur, Tanzina Labonte, Kristina Borstnik, Ik-Hyeon Paik, Andrew J. McRiner
  • Patent number: 7358254
    Abstract: 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: Grant
    Filed: June 21, 2004
    Date of Patent: April 15, 2008
    Assignees: Bristol-Myers Squibb Company, President & Fellows of Harvard College
    Inventors: Jeffrey A. Robl, Rex A. Parker, Scott A. Biller, Haris Jamil, Bruce L. Jacobson, Krishna Kodukula, Gokhan Hotamisligil
  • Patent number: 7348342
    Abstract: 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: Grant
    Filed: April 1, 2003
    Date of Patent: March 25, 2008
    Assignee: Cadila Healthcare Limited
    Inventors: Braj B. Lohray, Vidya B. Lohray, Mukul R. Jain, Gautam D. Patel, Harikishore Pingali
  • Patent number: 7259263
    Abstract: 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: Grant
    Filed: June 29, 2005
    Date of Patent: August 21, 2007
    Assignee: Jansen Pharmaceutica N.V.
    Inventors: Dennis J. Hlasta, Craig A. Zificsak
  • Patent number: 7217726
    Abstract: The present invention provides novel compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them.
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: May 15, 2007
    Assignee: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Shiv Kumar Agarwal, Mrinal Kanti Guha, Surendrakumar Satyanarayan Pandey, Matte Marianna Samuel