One Double Bond Between The Ring Members Of The Oxazole Ring Patents (Class 548/237)
  • Publication number: 20150057269
    Abstract: The present invention regards compositions and methods for the modulation of amidases capable of hydrolysing N-acylethanolamines useable in the therapy of inflammatory diseases. In particular, the present invention regards a compound of general formula (I): enantiomers, diastereoisomers, racemes and mixtures, polymorphs, salts, solvates thereof, wherein: (a) R is a linear alkyl radical having 13 to 19 carbon atoms or alkenyl radical having 13 to 19 carbon atoms carrying a double bond; (b) X is 0 or S; (c) Y is a 2 or 3 carbon atom alkylene residue, optionally substituted with one or two groups equal or different from each other and selected from among the group consisting of: —CH3, —CH2OH, —COOCH3, —COOH. Y may preferably be: —CH2—CH2—, —CH2—CH2—CH2—, CH(CH3)—CH2—, —CH2—CH(CH3)—, —CH2—C(CH3)2—, —CH2—CH(CH2OH)—, —CH2—C((CH2OH)2)—, —CH?CH—, —CH2—CH(COOCH3)—, —CH2—CH(COOH)—, for use as a medicine.
    Type: Application
    Filed: February 17, 2012
    Publication date: February 26, 2015
    Applicant: Epitech Group S.r.l.
    Inventors: Francesco Della Valle, Maria Federica Della Valle, Gabriele Marcolongo, Vincenzo Di Marzo, Salvatore Cuzzocrea
  • Publication number: 20140364618
    Abstract: The present invention relates to a method of making indeno-fused naphthol materials, that involves, with some embodiments, forming an indanone acid intermediate, represented by the following general Formula V, With Formula V, m is from 0 to 4, and R1 for each m, Rg and Rh can each be independently selected from, for example, hydrogen and hydrocarbyl.
    Type: Application
    Filed: May 13, 2014
    Publication date: December 11, 2014
    Applicant: Transitions Opticals, Inc.
    Inventors: Anu Chopra, Barry Van Gemert, Wenjing Xiao, Huayun Yu
  • Patent number: 8883797
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: November 11, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger
  • Publication number: 20140287011
    Abstract: Disclosed is an arthropod pest control composition comprising 2-(2,6-difluorophenyl)-4-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydrooxazole and an inert carrier, wherein the volume median diameter of 2-(2,6-difluorophenyl)-4-[4-(1,1-dimethylethyl)-2-ethoxyphenyl]-4,5-dihydrooxazole is from 1.5 to 5.
    Type: Application
    Filed: November 2, 2012
    Publication date: September 25, 2014
    Inventors: Katsuya Natsuhara, Yusuke Kimura, Mamoru Takiuchi
  • Patent number: 8809402
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: August 19, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
  • Patent number: 8754236
    Abstract: The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: June 17, 2014
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Francis G. Fang, James E. Foy, Lynn Hawkins, Charles Lemelin, Andre LesCarbeau, Xiang Niu, Kuo-Ming Wu
  • Patent number: 8658735
    Abstract: The graft copolymer comprises a polymerizable monomer (A1) represented by general formula (III) and a polymerizable monomer (B1) containing a pyridyl group, and a ligand can be bonded via the functional group at the terminus of R3a. In the formula, R1a represents a polymerizable group, R2a represents an alkylene group having a carbon number of 2-5, R3a represents an organic group having at a terminus a functional group selected from among an azide group, a phenyl azide group, a carboxyl group, a primary to quaternary amino group, an acetal group, an aldehyde group, a thiol group, a disulfide group, an active ester group, a trialkoxysilyl group, and a polymerizable group, and n represents any integer from 5 to 20,000.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: February 25, 2014
    Assignee: Tokyo University of Science Educational Foundation Administrative Organization
    Inventors: Hidenori Otsuka, Masayuki Fukaishi, Takashi Ishiduka
  • Publication number: 20140012010
    Abstract: Provided is a process for producing an optically active compound represented by Formula (3): (wherein R1 is an alkyl group, an alkynyl group, an alkenyl group, an aliphatic heterocyclic group, a cycloalkyl group, an aryl group, an aralkyl group, or an aromatic heterocyclic group, and any hydrogen atom of R1 may be replaced with a substituent; R2 is a hydrogen atom or a group which is not reactive in the reaction below; and * represents a chiral center) or a salt thereof by subjecting a compound represented by Formula (1): (wherein R1 and R2 have the same meanings as defined in Formula (3)) to a ring closure reaction in the presence of a chiral ligand having 1 or more coordination sites, a Lewis acid represented by Formula (2): MmZn??(2) (wherein M is a metal ion, Z is a counter anion of M, and m and n are integers of 1 to 4), and a sulfonyl halide having an optionally substituted alkyl or phenyl group
    Type: Application
    Filed: January 31, 2012
    Publication date: January 9, 2014
    Inventors: Osamu Onomura, Yutaro Tsuda, Masami Kuriyama, Toshiharu Yanagi, Kazuya Kodama
  • Patent number: 8487114
    Abstract: Disclosed are compounds having one of the following formulae (11), (12), wherein X is an aromatic nucleophilic substitution leaving group; R1 is hydrogen, an alkyl group, or an aryl group; and Q1 is a carboxyl protecting group or an aldehyde protecting group. Also disclosed are fused thiophenes that can be prepared using these compounds, as well as stannylthio-containing thiophene, thienothiophene, and dithienothiophene compounds that can be used to prepare fused thiophenes. Methods for making and using the aforementioned compounds, fused thiophenes, and stannylthio-containing thiophene, thienothiophene, and dithienothiophene compounds are also disclosed.
    Type: Grant
    Filed: March 30, 2009
    Date of Patent: July 16, 2013
    Assignee: Corning Incorporated
    Inventors: Mingqian He, Thomas Mark Leslie, Feixia Zhang
  • Patent number: 8460447
    Abstract: Substituted oxazoline compounds and/or substituted oxazoline derivatives having amorphous, semi-crystalline, or crystalline properties and methods for producing such compounds and derivatives are presented. The substituted oxazoline compounds and/or substituted oxazoline derivatives are useful for various applications. For example, the substituted oxazoline compounds and/or substituted oxazoline derivatives may function as phase-change agents, a binder resins, rheology modifiers or plasticizers for ink compositions.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: June 11, 2013
    Assignee: Xerox Corporation
    Inventors: Rina Carlini, Guerino G. Sacripante, Stephan V. Drappel, Bo Wu
  • Patent number: 8399675
    Abstract: This invention relates to novel compounds and a process for preparation of montelukast sodium.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: March 19, 2013
    Assignee: Formosa Laboratories, Inc.
    Inventors: Jui-Te Hung, Ching-Peng Wei
  • Publication number: 20130053387
    Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.
    Type: Application
    Filed: May 4, 2011
    Publication date: February 28, 2013
    Applicant: FerroKin BioScience, Inc.
    Inventor: James W. Malecha
  • Publication number: 20130012719
    Abstract: Azolines are oxidized in the presence of a copper-containing catalyst to azoles in the presence of molecular oxygen. A synthetic scheme converting azolines azoles is also provided.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: University of Southern California
    Inventors: Travis J. Williams, Anna C. Dawsey, Vincent Li, Kimberly C. Hamilton, Jianmei Wang
  • Publication number: 20120272859
    Abstract: Substituted oxazoline compounds and/or substituted oxazoline derivatives having amorphous, semi-crystalline, or crystalline properties and methods for producing such compounds and derivatives are presented. The substituted oxazoline compounds and/or substituted oxazoline derivatives are useful for various applications. For example, the substituted oxazoline compounds and/or substituted oxazoline derivatives may function as phase-change agents, a binder resins, rheology modifiers or plasticizers for ink compositions.
    Type: Application
    Filed: April 27, 2011
    Publication date: November 1, 2012
    Applicant: XEROX CORPORATION
    Inventors: Rina CARLINI, Guerino G. SACRIPANTE, Stephan V. DRAPPEL, Bo WU
  • Patent number: 8143418
    Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
    Type: Grant
    Filed: February 7, 2011
    Date of Patent: March 27, 2012
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
  • Patent number: 8093275
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: January 10, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
  • Publication number: 20110275636
    Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.
    Type: Application
    Filed: May 4, 2011
    Publication date: November 10, 2011
    Applicant: FerroKin BioSciences, Inc.
    Inventor: James Malecha
  • Publication number: 20110098478
    Abstract: Disclosed are compounds having one of the following formulae (11), (12), wherein X is an aromatic nucleophilic substitution leaving group; R1 is hydrogen, an alkyl group, or an aryl group; and Q1 is a carboxyl protecting group or an aldehyde protecting group. Also disclosed are fused thiophenes that can be prepared using these compounds, as well as stannylthio-containing thiophene, thienothiophene, and dithienothiophene compounds that can be used to prepare fused thiophenes. Methods for making and using the aforementioned compounds, fused thiophenes, and stannylthio-containing thiophene, thienothiophene, and dithienothiophene compounds are also disclosed.
    Type: Application
    Filed: March 30, 2009
    Publication date: April 28, 2011
    Inventors: Mingqian He, Thomas Mark Leslie, Feixia Zhang
  • Publication number: 20110098479
    Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2 ??(1) wherein R
    Type: Application
    Filed: December 29, 2010
    Publication date: April 28, 2011
    Inventors: KAZUSHI MASHIMA, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
  • Publication number: 20110091508
    Abstract: The invention features oligofluorinated cross-linked polymers and their use in the manufacture of articles and coating surfaces.
    Type: Application
    Filed: October 2, 2008
    Publication date: April 21, 2011
    Applicant: Interface Biologics ,Inc.
    Inventors: Roseita Esfand, J. Paul Santerre, Mark J. Ernsting, H. Hung Pham, Vivian Z. Wang, Meilin Yang
  • Patent number: 7888513
    Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2??(1) wherein R1
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: February 15, 2011
    Assignee: Takasago International Corporation
    Inventors: Kazushi Mashima, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
  • Publication number: 20110034700
    Abstract: The present invention describes a heterogeneous chiral catalyst comprising a heterogeneous chiral catalyst precursor complexed with a metal species. The precursor comprises a chiral bisoxazoline group coupled to an inorganic substrate. The heterogeneous chiral catalyst may be capable of catalysing a chemical reaction, for example cyclopropanation, and the chemical reaction may be capable of generating a chiral product.
    Type: Application
    Filed: March 8, 2005
    Publication date: February 10, 2011
    Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
    Inventors: Jackie Y. Ying, Su Seong Lee, Sukandar Hadinoto
  • Patent number: 7884211
    Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: February 8, 2011
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
  • Publication number: 20110003787
    Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hyd
    Type: Application
    Filed: July 26, 2010
    Publication date: January 6, 2011
    Inventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
  • Publication number: 20100324025
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: September 21, 2009
    Publication date: December 23, 2010
    Applicant: University of Washington
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Patent number: 7842839
    Abstract: It is provided to an optically active cycloalkylidenebisamidoalcohol compound represented by the formula (3): wherein R1 represents a C1-6 alkyl group, an optionally substituted phenyl group, an optionally substituted aralkyl group or a hydrogen atom, or two R1s, which are bonded to the same carbon atom, are bonded to form a ring together with the carbon atom to which they are bonded, R2 represents a C1-6 alkyl group, an optionally substituted aralkyl group or an optionally substituted phenyl group and * represents an asymmetric center, a method for producing it and a method for producing an optically active cycloalkylidenebisoxazoline compound represented by the formula (4): wherein R1, R2 and * are as defined above, using thereof.
    Type: Grant
    Filed: December 21, 2004
    Date of Patent: November 30, 2010
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Makoto Itagaki
  • Patent number: 7834190
    Abstract: An objective of the present application is to provide an industrially practicable method for producing an optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof from an inexpensive easily-available starting material. The derivative or salt thereof is useful as an intermediate for a medicine. It is also intended by the present application to provide a useful intermediate of the derivative. The objective is attained by the following method. First, an easily-available 2-halo-3-oxopropionic acid derivative is asymmetrically reduced, and then epoxidated to produce an optically-active epoxycarboxylic acid derivative. Next, the derivative is converted into an optically-active epoxyamide derivative by reaction with cyclopropylamine, and then reacted with a nitrile to obtain an optically-active oxazolinamide derivative. Subsequently, selective acid solvolysis of the oxazoline skeleton gives the optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof.
    Type: Grant
    Filed: May 22, 2007
    Date of Patent: November 16, 2010
    Assignee: Kaneka Corporation
    Inventors: Kohei Mori, Akira Nishiyama, Naoaki Taoka, Daisuke Moriyama, Nobuo Nagashima
  • Patent number: 7816538
    Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: October 19, 2010
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
  • Publication number: 20100217008
    Abstract: The present invention relates to a new method for the production of valsartan, a valine derivative having the chemical N name is (S)—N-(1-carboxy-2-methylprop-1-yl)-N-pentanoyl-N-[2?-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]amine, and pharmacologically acceptable salts thereof. Furthermore the invention relates to new intermediate compounds which are suitable for the production of valsartan and new methods for the production of intermediate compounds which are suitable for the production of valsartan.
    Type: Application
    Filed: December 11, 2007
    Publication date: August 26, 2010
    Applicant: ratiopharm GmbH
    Inventors: Jiri Stohandl, Pavel Bobal, Jaroslav Frantisek
  • Patent number: 7767825
    Abstract: The present invention relates to a method for preparing 2,2?,6,6?-tetraoxazolinyl biphenyl ligand in chemical industry field. In the present invention, compound (III) is reacted with an activator that can activate the hydroxyl group selected from the group consisting of alkyl halosulfonium compound, aryl halosulfonium compound, phosphoryl chloride, phosphorus pentachloride, thionyl chloride and triphenyl phosphine, in the presence of alkali(s), to give the target product (IV), 2,2?,6,6?-tetraoxazolinyl biphenyl ligand. The ligand of the present invention can be used in various asymmetric reactions catalyzed by metals, with high reactivity and stereoselectivity, and thus represents a good application outlook.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: August 3, 2010
    Assignee: Shanghai Jiaotong University
    Inventors: Wanbin Zhang, Yongjian Zhang, Feijun Wang
  • Patent number: 7767667
    Abstract: It has now been found that certain novel heterocyclic derivitives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)?C(R7)N(R8)—, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)?C(R12)C(R13)?C(R14) 1 12, -, where R,R,R6, R7, R8, RI1, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound with at least one insecticidally compatable carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: August 22, 2008
    Date of Patent: August 3, 2010
    Assignee: FMC Corporation
    Inventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
  • Patent number: 7754891
    Abstract: The present invention relates to a 5,5?-position linked 1,1?-biphenyl axis chiral ligand in chemical industry field. The present invention incorporates both the central chirality of oxazoline and the axial chirality of diphenyls. Such ligand can be used in various asymmetric reactions catalyzed by metal with high reactivity and stereoselectivity, and thus represents a good application outlook. The ligand of the present invention has the formula of: wherein: n=5, 6, 7, 8, 9, 10, 11 or 12; R1=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R2=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R3=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R4=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: July 13, 2010
    Assignee: Shanghai Jiaotong University
    Inventors: Wanbin Zhang, Yongjian Zhang, Feijun Wang
  • Publication number: 20100152453
    Abstract: This invention relates to novel compounds and a process for preparation of montelukast sodium.
    Type: Application
    Filed: February 22, 2010
    Publication date: June 17, 2010
    Applicant: FORMOSA LABORATORIES, INC.
    Inventors: Jui-Te Hung, Ching-Peng Wei
  • Publication number: 20100069367
    Abstract: Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: December 7, 2007
    Publication date: March 18, 2010
    Applicant: EXELIXIS, INC.
    Inventors: Brant Clayton Boren, Brett B. Busch, Xiao-Hui Gu, Vasu Jammalamadaka, Shao Po Lu, Richard Martin, Raju Mohan, Edwin Schweiger, William C. Stevens, Tie-Lin Wang, Yinong Xie, Wei Xu
  • Patent number: 7659296
    Abstract: The present invention relates to novel, non-secosteroidal, phenyl-benzoxazole compounds of Formula (I) wherein the variables R, R?, RP, RP3, LP1, LP2, ZP, RB, RB?, LXB and ZXB are as hereinafter defined, their preparation, pharmaceutical compositions, and methods of use.
    Type: Grant
    Filed: December 19, 2005
    Date of Patent: February 9, 2010
    Assignee: Eli Lilly and Company
    Inventors: Quanrong Shen, Alan M. Warshawsky, Ying Kwong Yee
  • Patent number: 7626035
    Abstract: The present invention relates to new optically active heteroaromatic ?-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.
    Type: Grant
    Filed: January 3, 2005
    Date of Patent: December 1, 2009
    Assignee: Bayer Schering Pharma AG
    Inventors: Johannes Platzek, Ludwig Zorn, Bernd Buchmann, Werner Skuballa, Orlin Petrov
  • Publication number: 20090281155
    Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
    Type: Application
    Filed: July 24, 2009
    Publication date: November 12, 2009
    Inventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
  • Patent number: 7579478
    Abstract: The present invention provides processes for the purification of substituted benzoxazole compounds, and in particular 2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol. The processes include recrystallizing the compound from a solution comprising acetone and acetonitrile; treating the crude purified product with a clarifying agent in a solution comprising ethyl acetate, and precipitating or triturating the compound from a mixed solvent system.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: August 25, 2009
    Assignee: Wyeth
    Inventor: Silvio Iera
  • Publication number: 20090198070
    Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2??(1) wherein
    Type: Application
    Filed: December 4, 2006
    Publication date: August 6, 2009
    Applicants: OSAKA UNIVERSITY, TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Kazushi Mashima, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
  • Patent number: 7560570
    Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having Ki's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an ?-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other ?-unsaturation corresponding to the arachidonyl ?8,9/?11,12 and/or oleyl ?9,10 positions. A preferred ?-keto heterocylic head group is ?-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).
    Type: Grant
    Filed: March 28, 2005
    Date of Patent: July 14, 2009
    Assignee: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Publication number: 20090156829
    Abstract: The present invention relates to a 5,5?-position linked 1,1?-biphenyl axis chiral ligand in chemical industry field. The present invention incorporates both the central chirality of oxazoline and the axial chirality of diphenyls. Such ligand can be used in various asymmetric reactions catalyzed by metal with high reactivity and stereoselectivity, and thus represents a good application outlook. The ligand of the present invention has the formula of: wherein: n=5, 6, 7, 8, 9, 10, 11 or 12; R1=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R2=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R3=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl; R4=hydrogen, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted benzyl.
    Type: Application
    Filed: December 29, 2006
    Publication date: June 18, 2009
    Applicant: SHANGHAI JIAOTONG UNIVERSITY
    Inventors: Wanbin Zhang, Yongjian Zhang, Feijun Wang
  • Patent number: 7538228
    Abstract: A chiral ligand represented by the formula and its enantiomer: wherein A, X, Y and Z are as defined in the specification is provided. Also provided is a process of making the chiral ligands and catalysts prepared from these ligands and a transition metal, a salt thereof or a complex thereof. In addition, a method of preparing an asymmetric compound by a transition metal catalyzed asymmetric reaction, such as, hydrogenation, hydride transfer reaction, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, allylic alkylation, epoxidation, cyclopropanation, Diels-Alder reaction, Aldol reaction, ene reaction, Heck reaction and Michael addition is provided.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: May 26, 2009
    Assignee: The Penn State Research Foundation
    Inventors: Xumu Zhang, Duan Liu
  • Publication number: 20090043104
    Abstract: The present invention relates to a method for preparing 2,2?,6,6?-tetraoxazolinyl biphenyl ligand in chemical industry field. In the present invention, compound (III) is reacted with an activator that can activate the hydroxyl group selected from the group consisting of alkyl halosulfonium compound, aryl halosulfonium compound, phosphoryl chloride, phosphorus pentachloride, thionyl chloride and triphenyl phosphine, in the presence of alkali(s), to give the target product (IV), 2,2?,6,6?-tetraoxazolinyl biphenyl ligand. The ligand of the present invention can be used in various asymmetric reactions catalyzed by metals, with high reactivity and stereoselectivity, and thus represents a good application outlook.
    Type: Application
    Filed: December 29, 2006
    Publication date: February 12, 2009
    Applicant: SHANGHAI JIAOTONG UNIVERSITY
    Inventors: Wanbin Zhang, Yongjian Zhang, Feijun Wang
  • Publication number: 20090012070
    Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)=C(R7)N(R8)-, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)=C(R12)C(R13)=C(R14) 112, -, where R, R, R6, R7, R8, R11, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Application
    Filed: August 22, 2008
    Publication date: January 8, 2009
    Applicant: Bayer Cropscience AG
    Inventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
  • Publication number: 20080319200
    Abstract: A method of preparing oxazoline-protected aminodiol compounds is disclosed. These compounds are useful intermediates in processes for preparing Florfenicol and related compounds.
    Type: Application
    Filed: May 28, 2008
    Publication date: December 25, 2008
    Inventor: JAMES C. TOWSON
  • Publication number: 20080207913
    Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.
    Type: Application
    Filed: April 27, 2007
    Publication date: August 28, 2008
    Applicant: Intezyne Technologies
    Inventors: Kurt Breitenkamp, Kevin N. Sill, Habib Skaff
  • Publication number: 20080194782
    Abstract: A solid, hydrocarbon-insoluble, catalyst component useful in polymerizing olefins containing magnesium, titanium, and halogen further contains an internal electron donor comprising a compound containing electron donating substituents with a structure: wherein D1 and D2 are selected individually from and R, R2, R3, R4, R5, R6, and R7 individually are hydrocarbon or substituted hydrocarbon groups containing 1 to 20 carbon atoms and R2, R3, R4, R6, and R7 may be hydrogen; R4 may be —NR2; and wherein groups R1 and R2, R2 and R3, R3 and R4, R3 and R5, and groups R6 and R7 may be joined to form a cyclic structure.
    Type: Application
    Filed: April 1, 2008
    Publication date: August 14, 2008
    Inventors: Roger Uhrhammer, John P. Lalka
  • Patent number: 7358368
    Abstract: Compounds represented by formula (II): wherein M is a hydrogen atom, sodium, potassium, or lithium; P is a hydrogen atom, an alkyl group, and the like; and the wavy line indicates a cis form, a trans form, or a mixture thereof for the double bond to which it is attached, may be prepared by hydrolyzing a compound represented by formula (I), or a salt thereof: wherein R1 and R2 are the same or different and each is an alkyl group, or R1 and R2 together with the adjacent nitrogen atom may form an aliphatic heterocycle, and P and the wavy line are as defined above, in the presence of alkali metal hydroxide.
    Type: Grant
    Filed: November 4, 2004
    Date of Patent: April 15, 2008
    Assignee: Ajinomoto Co., Inc.
    Inventors: Daisuke Takahashi, Kunisuke Izawa
  • Patent number: 7348436
    Abstract: Compounds and methods useful for the synthesis of (+)-discodermolide, a naturally occurring microtubule stabilizing agent useful as an anti-cancer agent.
    Type: Grant
    Filed: March 1, 2005
    Date of Patent: March 25, 2008
    Assignee: Kosan Biosciences Incorporated
    Inventors: David C. Myles, Simon James Shaw, Kurt F. Sundermann
  • Patent number: RE46129
    Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
    Type: Grant
    Filed: January 10, 2014
    Date of Patent: August 30, 2016
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrick G Harran, Xiaodong Wang, Jef K. DeBrabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki