Chalcogen Bonded Directly To The Hetero Ring Patents (Class 549/475)
  • Patent number: 10301274
    Abstract: Disclosed are salts of 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 the salts of the compounds of formula 1, and intermediates used therein. The salts of the compound of formula 1 can be useful for preparation of halichondrin analogs such as eribulin.
    Type: Grant
    Filed: March 6, 2015
    Date of Patent: May 28, 2019
    Assignee: Sandoz AG
    Inventors: Fabio E. s. Souza, Ricardo Orprecio, Ming Pan
  • Patent number: 9790156
    Abstract: The present technology relates to methods of hydroformylating allyl alcohol to 4-hydroxybutanal and 2-methyl-3-hydroxypropanal, comprising (i) admixing allyl alcohol with CO and H2 to form a starting material mixture, and (ii) reacting the starting material mixture in the presence of a catalyst under conditions capable of forming a product mixture comprising 4-hydroxybutanal and 2-methyl-3-hydroxypropanal, wherein the catalyst is a transition metal complex comprising a transition metal ion and a diphosphine ligand with a bite angle from about 70° to about 100°, and wherein the ratio of 4-hydroxybutanal to 2-methyl-3-hydroxypropanal in the product mixture is less than 1.5:1.
    Type: Grant
    Filed: November 1, 2016
    Date of Patent: October 17, 2017
    Assignee: Lyondell Chemical Technology, L.P.
    Inventors: Daniel F. White, Beaven S. Mandimutsira
  • Patent number: 9440913
    Abstract: Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents —CHO, —C(?O)R5, —COOR5 (wherein R5 represents a C1-7 alkyl group), —CH2OH or —COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: September 13, 2016
    Assignee: NAI INC.
    Inventors: Hiroyuki Saimoto, Kiyoshi Kita, Yoshisada Yabu, Masaichi Yamamoto
  • Patent number: 9399629
    Abstract: This invention relates to a novel method for the preparation of 3-oxo-tetrahydrofuran comprising oxidizing 3-hydroxy-tetrahydrofuran in the presence of a catalytic amount of 2,2,6,6-tetramethyl-piperidine-N-oxyl (TEMPO) with trichloroisocyanuric acid.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: July 26, 2016
    Assignee: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Lidong Xing, Weitong Dong, Jun Lu, Ulrich Scholz, Jun Yan, Jinsong Yang
  • Patent number: 9249117
    Abstract: The present invention provides a use of compounds from Antrodia camphorata in manufacturing medicaments for treating kidney diseases, wherein the compounds is represented by formula (I): wherein R1 is a hydrogen atom or acetyl group, R2 is wherein the kidney disease is glomerulosclerosis or glomerulonephritis.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: February 2, 2016
    Inventor: Hui Ling Tseng
  • Publication number: 20150141667
    Abstract: The present invention provides catalysts, methods, and reactor systems for converting oxygenated hydrocarbons to oxygenated compounds. The invention includes methods for producing cyclic ethers, monooxygenates, dioxygenates, ketones, aldehydes, carboxylic acids, and alcohols from oxygenated hydrocarbons, such as carbohydrates, sugars, sugar alcohols, sugar degradation products, and the like, using catalysts containing palladium, molybdenum, tin, and tungsten. The oxygenated compounds produced are useful in the production of liquid fuels, chemicals, and other products.
    Type: Application
    Filed: December 30, 2014
    Publication date: May 21, 2015
    Inventors: Brian Blank, Randy Cortright, Taylor Beck, Elizabeth Woods, Mike Jehring
  • Patent number: 8999197
    Abstract: The invention provides a liquid crystal compound that has an excellent compatibility with other liquid crystal compounds and also has at least one of characteristics such as a high stability to heat, light or the like, a suitable refractive index anisotropy (?n), a low threshold voltage and a suitable dielectric anisotropy (??). A compound represented by formula (1) For example, R1 is alkyl having 1 to 10 carbons, R2 is halogen or alkenyl having 2 to 10 carbons; the ring A1, the ring A2 and the ring A3 are 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2 and Z3 are a single bond or alkylene having 1 to 4 carbons; G is —CH2— or —O—; and m is 1, and n and p is 0 or 1.
    Type: Grant
    Filed: October 24, 2013
    Date of Patent: April 7, 2015
    Assignees: JNC Corporation, JNC Petrochemical Corporation
    Inventors: Tokifumi Masukawa, Yasuyuki Goto, Tomohiro Yano
  • Publication number: 20150065733
    Abstract: Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7?, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Fabio E.S. Souza, Alena Rudolph, Ming Pan, Boris Gorin, Teng Ko Ngooi, Jason A. Bexrud, Ricardo Orprecio, Huzaifa Rangwala
  • Patent number: 8956799
    Abstract: A photoacid generator includes those of formula (I): wherein each Ra in formula 1 is independently H, F, a C1-10 nonfluorinated organic group, C1-10 fluorinated organic group, or a combination comprising at least one of the foregoing, provided at least one Ra is F or a C1-10 fluorinated organic group, the C1-10 fluorinated and nonfluorinated organic groups each optionally comprising O, S, N, or a combination comprising at least one of the foregoing heteroatoms; L1 is a linking group comprising a heteroatom comprising O, S, N, F, or a combination comprising at least one of the foregoing; G+ is an onium salt of the formula (II): wherein in formula (II), X is S or I, each R0 is independently C1-30 alkyl group; a polycyclic or monocyclic C3-30 cycloalkyl group; a polycyclic or monocyclic C4-30 aryl group; or a combination comprising at least one of the foregoing, provided at least one R0 is substituted where each R0 is a C6 monocyclic aryl group, and wherein when X is I, a is 2, and where X is S, a is 3,
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: February 17, 2015
    Assignee: Rohm and Haas Electronic Materials LLC
    Inventors: Emad Aqad, Cheng-Bai Xu, Mingqi Li, William Williams, III
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Patent number: 8933251
    Abstract: A fluorinated monomer of cyclic acetal structure has formula (1) wherein R is a C1-C20 alkyl group which may be substituted with halogen or separated by oxygen or carbonyl, and Z is a divalent organic group which forms a ring with alkylenoxy and contains a polymerizable unsaturated group. A polymer derived from the fluorinated monomer may be endowed with appropriate water repellency, water sliding property, lipophilicity, acid lability and hydrolyzability and is useful in formulating a protective coating composition and a resist composition.
    Type: Grant
    Filed: March 20, 2013
    Date of Patent: January 13, 2015
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Takeru Watanabe, Satoshi Shinachi, Takeshi Kinsho, Koji Hasegawa, Yuji Harada, Jun Hatakeyama, Kazunori Maeda, Tomohiro Kobayashi
  • Publication number: 20150011782
    Abstract: Disclosed herein is a novel route of synthesis of syn azide epoxide of formula 5, which is used as a common intermediate for asymmetric synthesis of HIV protease inhibitors such as Amprenavir, Fosamprenavir, Saquinavir and formal synthesis of Darunavir and Palinavir obtained by Cobalt-catalyzed hydrolytic kinetic resolution of racemic anti-(2SR,3SR)-3-azido-4-phenyl-1,2-epoxybutane (azido-epoxide).
    Type: Application
    Filed: January 10, 2013
    Publication date: January 8, 2015
    Inventors: Sunita Khanderao Gadakh, Reddy Santhosh Rekula, Arumugam Sudalai
  • 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
  • Publication number: 20140323502
    Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
    Type: Application
    Filed: February 13, 2014
    Publication date: October 30, 2014
    Inventors: Anton Franz Joseph Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara Eileen Segelstein
  • Publication number: 20140303377
    Abstract: An object of the present invention is to provide insecticides having high effectiveness.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 9, 2014
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba, Atsuko Kawahara
  • Publication number: 20140301981
    Abstract: The effectiveness of interferon for treating multiple sclerosis and other demyelinating diseases is synergistically potentiated by concomitant administration of a compound of Formula (I): wherein R1 is H, alkyl or OH, R2 is hydroxyalkyl or alkyl-O-L1, R3 is H or OH, X is C(?CH2), CH(OH), or spirooxirane-2, Z is CH2CH(OH) or C(=0), and R4 is an optionally substituted L2-alkyl or L2-alkenyl, wherein L2 is an optionally substituted 3-furanyl or 3-fur-3-enyl moiety.
    Type: Application
    Filed: December 19, 2012
    Publication date: October 9, 2014
    Applicant: INNOBIOSCIENCE LLC
    Inventors: Juan L Hancke Orozco, Rafael Burgos
  • Patent number: 8841467
    Abstract: The present invention relates to a novel process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol of formula I by reacting a compound of formula VII with the compound of formula R2-OH in the presence of haloginating agent to obtain a compound of formula VI and treating a compound of formula VI with dehaloginating agent to obtain a compound of formula V by reducing a compound of formula V, followed by cylization to obtain compound of formula IV and separating the enantiomer and diastereomers from compound of formula IV to yield a compound of formula I. Compound of formula I is useful as an intermediate in the preparation of protease inhibitors, in particular broad spectrum HIV protease inhibitors, the present invention also relates to process for the preparation of Darunavir from (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: September 23, 2014
    Assignee: Mylan Laboratories Limited
    Inventors: Siva Rama Prasad Vellenki, Arabinda Sahu, Nitin Ashok Shimpi, Anil Ponnuru, Satish Babu Kothari
  • Publication number: 20140275579
    Abstract: This invention relates to a novel method for the preparation of 3-oxo-tetrahydrofuran comprising oxidizing 3-hydroxy-tetrahydrofuran in the presence of a catalytic amount of 2,2,6,6-tetramethyl-piperidine-N-oxyl (TEMPO) with trichloroisocyanuric acid.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Lidong XING, Weitong DONG, Jun LU, Ulrich SCHOLZ, Jun YAN, Jinsong YANG
  • Publication number: 20140256730
    Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
    Type: Application
    Filed: January 13, 2014
    Publication date: September 11, 2014
    Applicant: Corsair Pharma, Inc.
    Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Publication number: 20140256963
    Abstract: The present invention provides a novel process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, or a salt thereof, preferably Aliskiren hemifumarate.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Inventors: Sujay Biswas, Sankareswaran Srimurugan, Anjul Kumar, Atulya Kumar Panda, Danish Jamshad, Mukesh Masand, Bidyut Biswas, Vikas Bansal, Ashish Kumar Gupta, Dharam Vir
  • Patent number: 8791254
    Abstract: A hydrofluoroether compound comprises at least one five- or six-membered, perfluorinated heterocyclic ring, each ring comprising four or five ring carbon atoms and one or two catenated heteroatoms selected from divalent ether oxygen atoms and trivalent nitrogen atoms, at least one of the catenated heteroatoms being a divalent ether oxygen atom, and each of the ring carbon atoms adjacent to the divalent ether oxygen atom bearing a fluorochemical group that comprises a tetrafluoroethylidene moiety (—(CF3)CF—) that is directly bonded to the ring carbon atom, the fluorochemical group optionally comprising at least one catenated heteroatom selected from divalent ether oxygen atoms and trivalent nitrogen atoms.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: July 29, 2014
    Assignee: 3M Innovative Properties Company
    Inventors: Daniel R. Vitcak, Richard M. Flynn, Michael G. Costello
  • Patent number: 8759379
    Abstract: The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: June 24, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Manoj C. Desai, Hon C. Hui, Hongtao Liu, Lianhong Xu
  • Publication number: 20140135511
    Abstract: The present invention relates to a method for producing a hydride having a carbon number of 4, comprising contacting, in liquid phase, an unsaturated compound having a carbon number of 4 as a raw material with a solid catalyst obtained by loading a metal element belonging to Groups 9 to 11 of the long periodic table on a support, thereby performing hydrogenation to produce a corresponding hydride having a carbon number of 4, wherein hydrogenation is performed in the presence of, as a solvent, a 1,4-butanediol having a nitrogen component concentration of 1 ppm by weight to 1 wt % in terms of nitrogen atom.
    Type: Application
    Filed: January 22, 2014
    Publication date: May 15, 2014
    Applicant: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Yusuke IZAWA, Masaru UTSUNOMIYA, Norikazu KONISHI, Kouta TANAKA
  • Patent number: 8710222
    Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: April 29, 2014
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Publication number: 20140101988
    Abstract: The present disclosure relates to a method of converting glycerol into organic reaction products. The method may include mixing glycerol with a monohydric alcohol. The mixture of glycerol and monohydric alcohol is then reacted in the presence of a heterogeneous nano-structured catalyst, wherein the monohydric alcohol is present at subcritical/supercritical temperatures and pressures. This converts the glycerol into one or more reaction products, wherein the reaction products include an oxygenated organic reaction product. Ninety percent or greater of the glycerol is converted.
    Type: Application
    Filed: October 17, 2012
    Publication date: April 17, 2014
    Applicant: SOUTHWEST RESEARCH INSTITUTE
    Inventors: Maoqi FENG, Chee-Kai TAN
  • Patent number: 8685274
    Abstract: The invention provides a liquid crystal compound that has an excellent compatibility with other liquid crystal compounds and also has at least one of characteristics such as a high stability to heat, light or the like, a suitable refractive index anisotropy (?n), a low threshold voltage and a suitable dielectric anisotropy (??). A compound represented by formula (1). For example, R1 is alkyl having 1 to 10 carbons, R2 is halogen or alkenyl having 2 to 10 carbons; the ring A1, the ring A2 and the ring A3 are 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2 and Z3 are a single bond or alkylene having 1 to 4 carbons; G is —CH2— or —O—; and m is 1, and n and p is 0 or 1.
    Type: Grant
    Filed: June 10, 2011
    Date of Patent: April 1, 2014
    Assignees: JNC Corporation, JNC Petrochemical Corporation
    Inventors: Tokifumi Masukawa, Yasuyuki Goto, Tomohiro Yano
  • Publication number: 20140054499
    Abstract: The invention provides a liquid crystal compound that has an excellent compatibility with other liquid crystal compounds and also has at least one of characteristics such as a high stability to heat, light or the like, a suitable refractive index anisotropy (?n), a low threshold voltage and a suitable dielectric anisotropy (??). A compound represented by formula (1). For example, R1 is alkyl having 1 to 10 carbons, R2 is halogen or alkenyl having 2 to 10 carbons; the ring A1, the ring A2 and the ring A3 are 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2 and Z3 are a single bond or alkylene having 1 to 4 carbons; G is —CH2— or —O—; and m is 1, and n and p is 0 or 1.
    Type: Application
    Filed: October 24, 2013
    Publication date: February 27, 2014
    Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATION
    Inventors: Tokifumi MASUKAWA, Yasuyuki GOTO, Tomohiro YANO
  • Patent number: 8658693
    Abstract: The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: February 25, 2014
    Assignee: Eli Lilly and Company
    Inventors: Jonathan Edward Green, Prabhakar Kondaji Jadhav, Venkatesh Krishnan, Donald Paul Matthews, Ashraf Saeed, Gregory Alan Stephenson
  • Publication number: 20140051867
    Abstract: The present disclosure provides processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 20, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Jared Wayne EVANS, Shinji Fujimori, Grace M. Huynh, Qi Liu, Martin Gerald Teresk
  • Publication number: 20130324514
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Application
    Filed: May 22, 2013
    Publication date: December 5, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dieter HAMPRECHT, Sara FRATTINI, Iain LINGARD, Stefan PETERS
  • Patent number: 8598364
    Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: December 3, 2013
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
  • Publication number: 20130317007
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: April 11, 2013
    Publication date: November 28, 2013
    Applicant: Reata Pharmaceuticals, Inc.
    Inventors: Eric ANDERSON, Xin JIANG, Melean VISNICK
  • Publication number: 20130309324
    Abstract: The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.
    Type: Application
    Filed: July 26, 2013
    Publication date: November 21, 2013
    Applicants: RadioRx, Inc., c/o Interwest Venture Partners, Alliant Techsystems Inc.
    Inventors: Mark D. Bednarski, Susan Knox, Louis F. Cannizzo, Kristin F. Warner, Robert B. Wardle, Stephen P. Velarde, Shoucheng Ning
  • Publication number: 20130289003
    Abstract: A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
    Type: Application
    Filed: October 25, 2011
    Publication date: October 31, 2013
    Inventors: Amjad Ali, Michael Man-Chu Lo, Robert K. Baker, Zhiqiang Guo, Brent Whitehead, Timothy J. Henderson, Edward Metzger, Lin Yan, Shrenik K. Shah, James Dellureficio, Jun Wang
  • Publication number: 20130244297
    Abstract: The present invention relates to a novel process for the preparation of (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol of formula I by reacting a compound of formula VII with the compound of formula R2-OH in the presence of haloginating agent to obtain a compound of formula VI and treating a compound of formula VI with dehaloginating agent to obtain a compound of formula V by reducing a compound of formula V, followed by cylization to obtain compound of formula IV and separating the enantiomer and diastereomers from compound of formula IV to yield a compound of formula I. Compound of formula I is useful as an intermediate in the preparation of protease inhibitors, in particular broad spectrum HIV protease inhibitors, the present invention also relates to process for the preparation of Darunavir from (3R, 3aS, 6aR)-hexahydrofuro[2, 3-b]furan-3-ol.
    Type: Application
    Filed: July 14, 2011
    Publication date: September 19, 2013
    Applicant: Mylan Laboratories Ltd.
    Inventors: Siva Rama Prasad Vellenki, Arabinda Sahu, Nitin Ashok Shimpi, Anil Ponnuru, Satish Babu Kothari
  • Publication number: 20130244945
    Abstract: An object of the present invention is to provide a medicament and method for treating lissencephaly patients. The present invention provides a lissencephaly therapeutic or preventive agent comprising a compound represented by the general formula (I): wherein R1 is lower alkyl substituted with lower alkoxy, lower alkyl substituted with a heterocyclic group, a heterocyclic group, or a group represented by the formula (IIa): wherein R4 is lower alkyl, R5 is lower alkylene, and m is an integer of 1 to 6; R2 is lower alkyl optionally substituted with phenyl; and R3 is lower alkyl optionally substituted with halogen, lower alkoxy, or phenyl; condensed polycyclic hydrocarbon; or hydrogen.
    Type: Application
    Filed: November 28, 2011
    Publication date: September 19, 2013
    Inventor: Shinji Hirotsune
  • Publication number: 20130237709
    Abstract: Intermediates useful for the synthesis of fexofenadine, processes for their preparation and processes for the synthesis of fexofenadine are described.
    Type: Application
    Filed: February 21, 2013
    Publication date: September 12, 2013
    Applicant: CHEMELECTIVA S.r.l.
    Inventors: Graziano CASTALDI, Marco BARATELLA, Mauro GABOARDI
  • Publication number: 20130233204
    Abstract: The present disclosure relates to methods of preparation of compounds resulting from the reaction of levulinic esters and epoxidized unsaturated fatty acid esters. The compounds are useful as renewable biomass-based plasticizers for a variety of polymers. Mono-, di- and tri-ketal adducts formed in a reaction between alkyl esters of levulinate and epoxidized unsaturated fatty acid esters derived from vegetable oils are also disclosed.
    Type: Application
    Filed: April 8, 2013
    Publication date: September 12, 2013
    Applicant: SEGETIS, Inc.
    Inventor: Sergey Selifonov
  • Publication number: 20130217762
    Abstract: The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.
    Type: Application
    Filed: October 5, 2012
    Publication date: August 22, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventor: Eli Lilly and Company
  • Patent number: 8513162
    Abstract: There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R1, R1a and R3 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.; R2, R2a and R4 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.
    Type: Grant
    Filed: December 24, 2009
    Date of Patent: August 20, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Hiromasa Mitsudera
  • Publication number: 20130211108
    Abstract: The present invention relates to a novel process for the preparation of Fosamprenavir or its pharmaceutically acceptable salts thereof by using novel intermediates.
    Type: Application
    Filed: June 17, 2011
    Publication date: August 15, 2013
    Inventors: Siva Rama Prasad Vellanki, Madhu Murthy Nadella, Rajendra Reddy Mulamalla, Siva Koteswara Rao Prathi, Ravathi Srinivas Rambhotla, Siva Reddy Arumalla, Debashish Datta
  • Publication number: 20130157252
    Abstract: The present invention relates to novel diagnostic markers for kidney disease and the use thereof.
    Type: Application
    Filed: October 25, 2012
    Publication date: June 20, 2013
    Applicants: HUMAN METABOLOME TECHNOLOGIES, INC., SYSMEX CORPORATION
    Inventors: SYSMEX CORPORATION, HUMAN METABOLOME TECHNOLOGIES, INC.
  • Patent number: 8445174
    Abstract: Disclosed are photo sensitizers that include a polyol moiety covalently bonded to a fused aromatic moiety. Also disclosed is a method for improving UV laser ablation performance of a coating, such as a cationic UV curable coating, by incorporating an oxalyl-containing additive into the cationic UV curable or other coating. Oxalyl-containing sensitizers having the formula Q-O—C(O)—C(O)—O—R1 wherein Q represents a fused aromatic moiety and R1 is an alkyl or aryl group, are also disclosed, as are oxalyl-containing oxetane resins, oxalyl-containing polyester polyols, and cationic UV curable coating formulations that include oxalyl-containing additives.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: May 21, 2013
    Assignee: NDSU Research Foundation
    Inventors: Dean C. Webster, Zhigang Chen
  • Patent number: 8440854
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: May 14, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Melean Visnick
  • Patent number: 8415378
    Abstract: or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally compris
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: April 9, 2013
    Assignee: AstraZeneca AB
    Inventors: Jonas Boström, Leifeng Cheng, Tomas Fex, Michael Karle, Daniel Pettersen, Peter Schell
  • Patent number: 8389202
    Abstract: A polymer includes a repeating unit shown by a general formula (1). R1 represents a hydrogen atom, a methyl group, a fluorine atom, or a trifluoromethyl group. R2 represents a substituted or unsubstituted aryl group having 6 to 22 carbon atoms. Y represents a carbon atom. X represents —X1Z1X2— which is an atomic group which forms a cyclic structure including a heteroatom together with Y. Z1 represents —O—, —S—, —CO—, —COO—, —SO—, or —SO2—. Each of X1 and X2 individually represents a single bond, a methylene group, or an alkylene group having 2 to 25 carbon atoms. Each of X1 and X2 is unsubstituted or substituted with a substituent, and optionally a carbon atom included in X1 and a carbon atom included in X2 are bonded via a divalent group.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: March 5, 2013
    Assignee: JSR Corporation
    Inventors: Ken Maruyama, Toru Kimura
  • Publication number: 20130046102
    Abstract: Glyceryl ether compounds prepared by the reaction of glycerol and olefin epoxides are disclosed. The compounds are renewable biomass-based surfactants useful as detergents and emulsifiers in formulations for cleaning, laundry, personal care, cosmetics, and industrial uses.
    Type: Application
    Filed: October 22, 2012
    Publication date: February 21, 2013
    Applicant: SEGETIS, INC.
    Inventor: SEGETIS, INC.
  • Patent number: 8338439
    Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same. In some embodiments, the present invention provides a compound of formula I-a or I-b: wherein each of Ring A, Ring B, W1, W2, Ry, Rv, Rx, m, p, and R1 is described herein.
    Type: Grant
    Filed: December 29, 2009
    Date of Patent: December 25, 2012
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Publication number: 20120309988
    Abstract: Intermediates and methods of their use in the synthesis of anslogs of halichondrin B are provided.
    Type: Application
    Filed: May 21, 2012
    Publication date: December 6, 2012
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Brian Austad, Charles E. Chase, Francis G. Fang, Marc Pesant
  • Publication number: 20120232033
    Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.
    Type: Application
    Filed: May 25, 2012
    Publication date: September 13, 2012
    Inventors: Sabine Kolczewski, Hans-Peter Marty, Robert Narquizian, Emmanuel Pinnard, Henri Stalder