The -c(=x)- Is Bonded Directly To Ring Nitrogen Of The Diazole Ring Patents (Class 548/334.1)
  • Patent number: 8969395
    Abstract: Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: March 3, 2015
    Assignee: Universidade de Coimbra
    Inventors: Jorge Antonio Ribeiro Salvador, Rita Catarina Mendes Dos Santos, Marta Cascante Serratosa
  • Publication number: 20140371232
    Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Publication number: 20140364602
    Abstract: Methods and intermediates useful for preparing a compound of formula I: and salts thereof.
    Type: Application
    Filed: February 1, 2013
    Publication date: December 11, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Aaron J. Cullen, Richard Hung Chiu Yu
  • Publication number: 20140242606
    Abstract: The present invention relates to a probe for iFRET and use thereof. Specifically, the present invention relates to a novel probe for iFRET, a method for preparing the probe for iFRET, a method for searching a target protein-specific binding site or a molecule having the binding site using the probe for iFRET, and a method for imaging the target protein using the probe for iFRET. The probe for iFRET according to the present invention utilizes an amino acid in a protein as a fluorescent donor, unlike the conventional FRET method. Therefore, only one fluorescent material is used, and its emission wavelength is distinct from the intrinsic fluorescence of the protein. Thus, high specificity and sensitivity are ensured, and the quantity, activity and mechanism of various proteins can be analyzed in an easy and accurate manner.
    Type: Application
    Filed: June 25, 2012
    Publication date: August 28, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Sang Jeon Chung, Ju Hwan Kim, Elena Ruchkina, Hyo Jin Kang
  • Publication number: 20140231729
    Abstract: A negative-type photosensitive resin composition capable of forming a pattern having favorable adhesiveness at a low light exposure; a pattern forming method using the resin composition; a cured film, an insulating film, a color filter formed using resin composition; and a display device provided with the cured film, insulating film, or color filter. The resin composition contains a compound represented by the following formula (1). In the formula, R1 and R2 each independently indicate a hydrogen atom or an organic group, but at least one indicates an organic group. R1 and R2 may be bonded to form a ring structure and may contain a hetero atom bond. R3 indicates a single bond or an organic group. R4 to R9 each independently indicate a hydrogen atom, an organic group, etc., but R6 and R7 are never hydroxyl groups. R10 indicates a hydrogen atom or an organic group.
    Type: Application
    Filed: June 15, 2012
    Publication date: August 21, 2014
    Applicant: TOKYO OHKA KOGYO CO., LTD.
    Inventors: Dai Shiota, Mayumi Kuroko, Kunihiro Noda, Yoshinori Tadokoro
  • Publication number: 20140221649
    Abstract: A novel compound suitable for obtaining a negative-type photosensitive resin composition capable of forming a pattern having favorable adhesiveness at a low light exposure. The compound is represented by the following formula (1). In the formula, R1 and R2 each independently indicate a hydrogen atom or an organic group, but at least one indicates an organic group. R1 and R2 may be bonded to form a ring structure and may contain a hetero atom bond. R3 indicates a single bond or an organic group. R4 to R9 each independently indicate a hydrogen atom, an organic group, etc., but R6 and R7 are never hydroxyl groups. R10 indicates a hydrogen atom or an organic group.
    Type: Application
    Filed: June 15, 2012
    Publication date: August 7, 2014
    Applicants: DAICEL CORPORATION, TOKYO OHKA KOGYO CO., LTD.
    Inventors: Dai Shiota, Mayumi Kuroko, Kunihiro Noda, Yoshinori Tadokoro, Yasuyuki Akai, Hideyuki Takai
  • Patent number: 8796459
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: August 5, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
  • Publication number: 20140148601
    Abstract: An dabigatran etexilate intermediate of Formula-6a, and the use in the preparation of dabigatran etexilate thereof.
    Type: Application
    Filed: December 7, 2011
    Publication date: May 29, 2014
    Applicant: MSN Laboratories Limited
    Inventors: Manne Satyanarayana Reddy, Chakilam Nagaraju, Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Achampeta Kodanda Ramprasad, Suraparaju Raghuram
  • Publication number: 20140107124
    Abstract: Disclosed herein are compositions comprising an amide related to a prostaglandin and a biogenic amine. Other aspects relate to certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 17, 2014
    Applicant: Allergan, Inc.
    Inventors: David F. Woodward, Robert M. Burk
  • Patent number: 8697335
    Abstract: A radiation-sensitive resin composition includes a compound, a resin and a radiation-sensitive acid generator. The compound has a structure in which a group represented by a following formula (1) is bound to a nitrogen atom. The resin has an acid-dissociative dissolution-controlling group and has a property such that alkali solubility of the resin increases by an action of an acid. In the formula (1), Y is a monovalent group having 5 to 20 carbon atoms, and “*” represents a bonding hand with the nitrogen atom. In the formula (i), R1, R2 and R3 each independently represent a linear or branched alkyl group having 1 to 4 carbon atoms or a monovalent alicyclic hydrocarbon group having 4 to 12 carbon atoms, or R1 and R2 are linked with each other to form a bivalent alicyclic hydrocarbon group, and “*” represents a bonding hand with the oxygen atom.
    Type: Grant
    Filed: January 17, 2012
    Date of Patent: April 15, 2014
    Assignee: JSR Corporation
    Inventors: Kazuo Nakahara, Mitsuo Sato
  • Publication number: 20140100227
    Abstract: Disclosed herein are novel C17-alkanediyl and alkenediyl derivatives of oleanolic acid, including those of 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, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: September 10, 2013
    Publication date: April 10, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Christopher F. BENDER, Xin JIANG, Eric ANDERSON, Melean VISNICK
  • Publication number: 20140024657
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Junying YUAN, Emily S. Hsu
  • Publication number: 20130313669
    Abstract: A coating film forming composition includes an amino acid generator including a protecting group that is eliminated to generate an amino acid. A coating film forming composition includes a component (A): the amino acid generator; a component (B): a hydrolyzable silane, a hydrolysis product thereof, a hydrolysis-condensation product thereof, or a mixture thereof; and a component (C): a solvent.
    Type: Application
    Filed: July 15, 2013
    Publication date: November 28, 2013
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Taku KATO, Junpei KOBAYASHI, Satoko TAKANO, Naoki SAKUMOTO
  • Publication number: 20130172569
    Abstract: The present invention provides a base generator having the structure of formula (1): wherein R1, R2, R3, R4, R5, and Y{circle around (?)} are defined as in the specification. The base generator of the present invention can be used for imidization of a polyimide precursor, promoting crosslinking of epoxy monomers, or crosslinking of polyurethane or polyurea.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 4, 2013
    Applicant: Eternal Chemical Co., Ltd.
    Inventor: Eternal Chemical Co., Ltd.
  • Patent number: 8455663
    Abstract: The present invention relates to novel imidazoline derivatives and their use as insecticidal, acaricidal, molluscicidal and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests.
    Type: Grant
    Filed: September 9, 2008
    Date of Patent: June 4, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Anthony Cornelius O'Sullivan, Thomas Pitterna, Jürgen Harry Schaetzer, Christoph Luethy
  • Publication number: 20130123493
    Abstract: A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof, Formula (II): Formula (I): the process comprising the reaction of a carbamate of Formula (II?): or formula (I?): with a primary or secondary amine of the formula: R1R2NH, wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.
    Type: Application
    Filed: July 28, 2011
    Publication date: May 16, 2013
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Brian Broadbelt, Jorge Bruno Reis Wahnon
  • Publication number: 20130116437
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Application
    Filed: September 14, 2012
    Publication date: May 9, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
  • Publication number: 20130053556
    Abstract: Morpholinos are widely used to block the activity of selected single-stranded genetic sequences. This invention comprises Morpholinos containing one or more integral photolinkers (Photo-Morpholinos) wherein the photolinkers are directly incorporated into the sequence of a Morpholino, where the photolinker has a size and structure which emulates the size and structure of a Morpholino subunit. This integrated photolinker design substantially simplifies and reduces cost of production relative to earlier photocleavable compositions. The invention also comprises use of these Photo-Morpholinos for modulating the expression of any selected gene transcript at any selected time and at any selected site simply by exposure to light. These Photo-Morpholinos afford a new use wherein a gene transcript is rendered inactive by contacting with a Photo-Morpholino—and then later exposure to light cleaves the Photo-Morpholino to inactive fragments—thereby reactivating that previously inactivated gene transcript.
    Type: Application
    Filed: August 26, 2011
    Publication date: February 28, 2013
    Applicant: GENE TOOLS, LLC
    Inventors: Yong-Fu Li, James E. Summerton, Paul A. Morcos
  • Publication number: 20130005739
    Abstract: The present invention relates to pharmaceutical compositions comprising a COS releasing compound according to formula (I) and to methods of preparing such compositions. Said pharmaceutical compositions may preferably be used for the treatment and/or the prevention of cardiovascular diseases.
    Type: Application
    Filed: December 28, 2010
    Publication date: January 3, 2013
    Applicants: LUDWIG BOLTZMANN CLUSTER FUER KARDIOVASKULAERE FORSCHUNG, UNIVERSITAET WIEN
    Inventors: Thomas Erker, Gerda Brunhofer, Christian Studenik, Bruno Podesser, Gabriela Pomper
  • Patent number: 8324244
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: December 4, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
  • Patent number: 8318750
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: November 27, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Patent number: 8293948
    Abstract: A reagent for organic synthesis with which a chemical reaction can be conducted in a liquid phase and unnecessary compound(s) can be easily separated at low cost from the liquid phase after completion of the reaction. The reagent for organic synthesis reversibly changes from a liquid-phase state to a solid-phase state with changes in solution composition and/or solution temperature, and is for use in organic synthesis reactions. This reagent for organic syntheses facilitates process development. With the reagent, research on and development of, e.g., medicines through, e.g., compound library synthesis, etc. can be accelerated. It can hence contribute to technical innovations in the biochemical industry and chemical industry.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: October 23, 2012
    Assignee: Jitsubo Co., Ltd.
    Inventors: Kazuhiro Chiba, Shokaku Kim, Yusuke Kono
  • Publication number: 20120252776
    Abstract: Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of 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, for example as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: March 12, 2012
    Publication date: October 4, 2012
    Inventors: Eric Anderson, Christopher F. Bender, Xiaofeng Liu, Xin Jiang, Melean Visnick
  • Patent number: 8258141
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Grant
    Filed: April 19, 2007
    Date of Patent: September 4, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120129901
    Abstract: Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.
    Type: Application
    Filed: May 20, 2010
    Publication date: May 24, 2012
    Inventors: Jorge Antonio Ribeiro Salvador, Rita Catarina Mendes Dos Santos, Marta Cascante Serratosa
  • Publication number: 20120116095
    Abstract: The present invention aims to provide novel compounds represented by formula [I] or pharmaceutically acceptable salts thereof: which are useful for prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, convulsion, tremor, pain, or sleep disorders, based on their inhibitory effect against glycine uptake.
    Type: Application
    Filed: July 15, 2010
    Publication date: May 10, 2012
    Applicant: TAISHO PHARMACEUTICAL C0., LTD.
    Inventors: Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Masato Hayashi, Yoshihisa Shirasaki, Shuji Yamamoto, Youichi Shimazaki, Yuko Araki, Kumi Abe, Xiang-Min Sun
  • Patent number: 8153801
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: April 10, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Eric Dowdy, Steven Pfeiffer
  • Publication number: 20120065191
    Abstract: The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.
    Type: Application
    Filed: December 23, 2009
    Publication date: March 15, 2012
    Applicant: BIAL - PORTELA & Cª, S.A.
    Inventors: Laszlo Erno Kiss, David Alexander Learmonth, Carla Patrícia da Costa Pereira Rosa, Rita Gusmão de Noronha, Pedro Nuno Leal Palma, Patrício Manuel Vieira Araújo Soares da Silva, Alexander Beliaev
  • Publication number: 20120052441
    Abstract: An aralkylcarbamate of imidazole base is effective as the quencher. In a chemically amplified positive resist composition comprising the carbamate, deprotection reaction of carbamate takes place by reacting with the acid generated upon exposure to high-energy radiation, whereby the composition changes its basicity before and after exposure, resulting in a pattern profile with advantages including high resolution, rectangular shape, and minimized dark-bright difference.
    Type: Application
    Filed: August 25, 2011
    Publication date: March 1, 2012
    Inventors: Masayoshi SAGEHASHI, Takeru Watanabe, Tomohiro Kobayashi
  • Publication number: 20120022257
    Abstract: Disclosed is a method for preparing HIV reverse transcriptase inhibitors which inhibit replication of HIV in HIV infected cells, and novel intermediate compounds used therein.
    Type: Application
    Filed: January 26, 2010
    Publication date: January 26, 2012
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Stacey Heumann, Christopher M. Levins, Steven Pfeiffer, Donald Tang
  • Publication number: 20110318688
    Abstract: The present invention is a salt represented by the formula (I) wherein R1 and R2 independently represent a fluorine atom or a C1 to C6 perfluoroalkyl group; L1 represents a C1 to C17 divalent saturated hydrocarbon group, a —CH2— contained in the saturated hydrocarbon group may be replaced by —O— or —CO—; ring W1 represents a C2 to C36 heterocycle; R3 represents a hydrogen atom or a C1 to C12 hydrocarbon group, a —CH2— contained in the hydrocarbon group may be replaced by —O— or —CO—; R4 in each occurrence independently represent a C1 to C6 hydrocarbon group, a —CH2— contained in the hydrocarbon group may be replaced by —O— or —CO—; m represents an integer of 0 to 6; and Z+ represents an organic cation.
    Type: Application
    Filed: June 28, 2011
    Publication date: December 29, 2011
    Inventors: Takashi HIRAOKA, Hiromu Sakamoto, Koji Ichikawa
  • Publication number: 20110315659
    Abstract: According to one embodiment, a pattern formation method is disclosed. The method can include forming a foundation film on a patterning film. The foundation film includes a reaction initiator to produce at least one of an acid and a base. The method can include forming an imprint film having an uneven configuration by coating an imprint material onto the foundation film and by causing a template to contact the imprint material. The method can include increasing an etching rate of a first portion of the imprint film higher than a second portion by introducing the at least one of acid and base into the first portion. The first portion is on the foundation film side. The second portion is a portion excluding the first portion. The method can include patterning the patterning film using a protruding portion of the uneven configuration as a mask.
    Type: Application
    Filed: June 24, 2011
    Publication date: December 29, 2011
    Inventors: Yusuke SEKIGUCHI, Yoshihisa Kawamura
  • Publication number: 20110312996
    Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: May 16, 2011
    Publication date: December 22, 2011
    Applicant: InterMune, Inc.
    Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
  • Patent number: 8039501
    Abstract: This invention provides compounds having the structural formula: wherein: R1 is an acyl or sulfonyl group, R2 is an acyl group selected from the group consisting of acyl groups derived from cycloaliphatic, aromatic or heterocyclic monocarboxylic acids, imidazolylcarbonyl and triazolylcarbonyl, and R3 is hydrogen or an amino-protecting group, a stereoisomer thereof, a solvate thereof, or a salt thereof, being useful as anti-inflammatory agents and anti-cancer agents.
    Type: Grant
    Filed: June 23, 2008
    Date of Patent: October 18, 2011
    Assignee: Universiteit Gent
    Inventors: Wim Vanden Berghe, Karolien De Bosscher, Serge Van Calenbergh, Guy Haegeman, Carl Jeffrey Lacey
  • Publication number: 20110245311
    Abstract: Disclosed herein are the compositions and methods for a compound of Formula Ia or Ib.
    Type: Application
    Filed: April 2, 2010
    Publication date: October 6, 2011
    Inventor: Dennis Wright
  • Publication number: 20110201823
    Abstract: A salt represented by the formula (I0): wherein Q1 and Q2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents a divalent C1-C17 hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, m represents 1 or 2, and Zm+ represents m-valent organic or inorganic cation.
    Type: Application
    Filed: February 11, 2011
    Publication date: August 18, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Isao YOSHIDA, Koji ICHIKAWA
  • Publication number: 20110172195
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: March 15, 2011
    Publication date: July 14, 2011
    Applicant: ARIZONA BOARD OF REG. ON BEHALF OF THE UNIV. OF AZ
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Publication number: 20110166138
    Abstract: Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.
    Type: Application
    Filed: March 17, 2009
    Publication date: July 7, 2011
    Inventors: Alexandros Makriyannis, Lakshmipathi Pandarinathan, Nikolai Zvonok, Teija Parkkari, Lauren Chapman
  • Patent number: 7964724
    Abstract: and the pharmaceutically acceptable salts and esters thereof, wherein X1, X2, X3, Y1, Y2 and R are described herein inhibit the interaction of MDM2 protein with a p53-like peptide and hence have anti proliferative activity.
    Type: Grant
    Filed: May 13, 2005
    Date of Patent: June 21, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Nader Fotouhi, Gregory Jay Haley, Klaus B. Simonsen, Binh Thanh Vu, Stephen Evan Webber
  • Publication number: 20110086311
    Abstract: A photosensitive resin composition which is excellent in resolution, low in cost, and usable in a wide range of structures of polymer precursors each of which is reacted into a final product by a basic substance or by heating in the presence of a basic substance. The photosensitive resin composition includes a base generator which has a specific structure and generates a base by exposure to electromagnetic radiation and heating, and a polymer precursor which is reacted into a final product by the base generator and by a basic substance or by heating in the presence of a basic substance.
    Type: Application
    Filed: March 30, 2009
    Publication date: April 14, 2011
    Inventors: Mami Katayama, Shunji Fukuda, Katsuya Sakayori
  • Patent number: 7893278
    Abstract: The present invention relates to compounds of the formula and the pharmaceutically acceptable salts and esters thereof, a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show antiproliferative activity and may be especially useful for the treatment of cancer.
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: February 22, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Gregory Jay Haley, Norman Kong, Emily Aijun Liu, Binh Thanh Vu
  • Publication number: 20110039109
    Abstract: Activators for heat-curing epoxy resin compositions, as well as use thereof in heat-curing epoxy resin compositions. These activators are distinguished by a good activation effect as well as good storage stability.
    Type: Application
    Filed: April 30, 2009
    Publication date: February 17, 2011
    Applicant: SIKA TECHNOLOGY AG
    Inventors: Karsten Frick, Ulrich Gerber, Juergen Finter, Andreas Kramer
  • Publication number: 20100292480
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Application
    Filed: September 11, 2008
    Publication date: November 18, 2010
    Applicant: Gilead Sciences, Inc
    Inventors: Eric Dowdy, Steven Pfeiffer
  • Publication number: 20100249393
    Abstract: The present invention provides for reagents for the introduction of colorimetric-oxycarbonyl protecting groups, compounds bearing colorimetric-oxycarbonyl protecting groups, and the use thereof in solid-supported organic syntheses of oligonucleotides, polypeptides, polysaccharides, and combinatorial libraries.
    Type: Application
    Filed: March 30, 2009
    Publication date: September 30, 2010
    Applicant: Berry and Associates, Inc.
    Inventors: John C. Hodges, Yam Foo Poon, William H. Pearson
  • Patent number: 7745458
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: June 29, 2010
    Assignee: Glaxo Group Limited
    Inventors: Luca Arista, Anna Checchia, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli
  • Publication number: 20100120881
    Abstract: The present invention relates to imidazoline derivatives and their use as insecticidal, acaricidal, molluscicidal and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests. In particular the present invention relates to imidazolines with alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heteroaryl or heterocyclyl substituents.
    Type: Application
    Filed: January 18, 2008
    Publication date: May 13, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Anthony Cornelius O'Sullivan, Christoph Luethy, Jurgen Harry Schaetzer
  • Patent number: 7704543
    Abstract: This invention provides a new method of obtaining a high density, reproducible and uniform coverage of a solid surface, compounds suitable for such a method and methods of preparing such compounds. This invention further relates to methods of the chemical modification (carboxylation) of solid surfaces and their subsequent use for the attachment of amine-containing molecules including DNA, proteins and other polymers.
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: April 27, 2010
    Assignee: Illumina Cambridge Limited
    Inventors: Milan Fedurco, Anthony Romieu, Gerardo Turcatti
  • Publication number: 20100041898
    Abstract: Disclosed is a new class of chiral bidentate ligands capable of performing asymmetric hydrogenation. Also disclosed are processes of performing asymmetric hydrogenation the chiral bidentate ligands.
    Type: Application
    Filed: November 20, 2007
    Publication date: February 18, 2010
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Carl Alan Busacca, Jon Charles Lorenz
  • Publication number: 20090253913
    Abstract: Methods for the synthesis of the N-carbamoyl imidazole (I) and its 1:1 adduct with imidazole are provided. Methods for the preparation of these crystalline intermediates in a high state of purity are also provided. These intermediates react cleanly under mild conditions to produce sorafenib in high yield and purity, without generating difficult-to-remove impurities.
    Type: Application
    Filed: March 5, 2009
    Publication date: October 8, 2009
    Inventors: Pierluigi Rossetto, Peter Lindsay MacDonald, Augusto Canavesi
  • Publication number: 20090176837
    Abstract: Disclosed herein are novel compounds with activity at RAR? 2 receptors. Further disclosed are the use of such compounds for treatment of or to alleviate symptoms of cancer, neurological disorders such as memory deficits and schizophrenia, neurodegenerative disorders such as Parkinson's and Alzheimer's diseases, inflammatory disorders such as psoriasis and rheumatoid arthritis, eye disorders and depression.
    Type: Application
    Filed: July 12, 2006
    Publication date: July 9, 2009
    Applicant: SONY CORPORATION
    Inventors: Roger Olsson, Fabrice Piu, Birgitte Lund