The Additional Hetero Ring Also Contains Nitrogen Patents (Class 548/518)
  • Patent number: 10456375
    Abstract: Biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases, fluorescence diagnosis and PDT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, opthamological or urological disorders are provided as well as providing methods to obtain them in pharmaceutical quality. One embodiment consists of a method to synthesize a porphyrin with a defined arrangement of meso-substituents and then converting this porphyrin system to a chlorin system by dihydroxylation or reduction, and if more than one isomer is formed separate them by chromatography either on normal or reversed phase silica. In another embodiment the substituents on the porphyrin are selected to direct the reduction or dihydroxylation to the chlorin so that a certain isomer is selectively formed.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: October 29, 2019
    Assignee: Biolitec Unternehmensbeteiligungs II AG
    Inventors: Hartwig Richard Arthur Golf, Arno Wiehe, Susanna Graefe, Volker Albrecht, Hans-Ulrich Reißig
  • Patent number: 9586900
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: March 7, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Guohua Zhao, William N. Washburn
  • Patent number: 9545106
    Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH-0- or —CH?C—CH2-0-; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C=0, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and R9 a
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: January 17, 2017
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Patent number: 9447231
    Abstract: An outer casing for an electric device which is a molded article of a environmental resin wherein poly(lactic acid) and/or a lactic acid copolymer is used, is constituted by molding a flame-retarded resin composition including a resin component containing poly(lactic acid) and/or the lactic acid copolymer as a main ingredient, and silica-magnesia catalyst particles as a flame retardance-imparting component which imparts flame retardance, wherein an organometallic compound is attached to a part of surfaces or the entire surfaces of the silica-magnesia catalyst particles. The organometallic compound is preferably a titanium-based coupling agent or a zirconium-based coupling agent.
    Type: Grant
    Filed: October 16, 2012
    Date of Patent: September 20, 2016
    Assignee: PANASONIC INTELLECTUAL PROPERTY MANAGEMENT CO., LTD.
    Inventor: Takehiko Yamashita
  • Patent number: 9040534
    Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
  • Publication number: 20150126485
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Patent number: 9023882
    Abstract: 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.
    Type: Grant
    Filed: June 12, 2012
    Date of Patent: May 5, 2015
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Publication number: 20150119549
    Abstract: Sulfur-containing polymer adducts such as polythioethers, polysulfides, and sulfur-containing polyformals having terminal maleimide groups, and in particular, sulfur-containing polymers and sulfur containing adducts having terminal 1,1?-(methylenedi-4,1-phenylene)bismaleimide groups are disclosed. The adducts provide cured sealants having improved tensile strength and elongation and are useful as aerospace sealants.
    Type: Application
    Filed: October 29, 2013
    Publication date: April 30, 2015
    Applicant: PRC-DeSoto International, Inc.
    Inventors: Chandra Rao, Renhe Lin
  • Publication number: 20150119377
    Abstract: This invention recites substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in animals. The substituents A, B, R1a, R1b, R1c, R2, R3, R4, R6, and n are as described herein.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Inventors: Susan M. K. Sheehan, Valerie A. Vaillancourt
  • Publication number: 20150094267
    Abstract: The present invention relates to succinimide-activated nitroxyl compounds and methods for the synthesis of such compounds. The present invention also relates to the use of succinimide-activated nitroxyl compounds to prepare nitroxylated proteins, for example nitroxylated heme proteins (e.g., nitroxylated hemoglobin and nitroxylated myoglobin). The nitroxylated proteins are optionally also conjugated to a polyalkylene oxide (PAO), for example to a polyethylene glycol (PEG). Polynitroxylated heme proteins are useful as oxygen therapeutic agents (OTAs). The invention further relates to pharmaceutical compositions of the nitroxylated proteins and methods for the use of nitroxylated proteins in the treatment of various conditions.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 2, 2015
    Inventors: Kim D. Vandegriff, Ashok Malavalli, Gnel Mkrtchyan
  • Publication number: 20150084016
    Abstract: An organic electroluminescent element including a luminescent compound represented by the following formula (in which R1 to R14 each independently represent a hydrogen atom, a deuterium atom, an alkyl group, an aryl group, a heteroaryl group, a fluorine atom, a cyano group, an amino group, an alkoxy group, an aryloxy group, a thio group, or a silyl group, and 8 to 13 groups out of R1 to R14 each represent a hydrogen atom or a deuterium atom.) in a light emitting layer has high durability and excellent chromaticity.
    Type: Application
    Filed: October 5, 2012
    Publication date: March 26, 2015
    Applicant: UDC IRELAND LIMITED
    Inventors: Toru Watanabe, Yuki Hirai, Tianhua Ouyang, Koji Takaku, Wataru Sotoyama, Tetsu Kitamura, Yasunori Yonekuta
  • Publication number: 20150080632
    Abstract: Marinopyrrole derivatives and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing cancer.
    Type: Application
    Filed: February 1, 2013
    Publication date: March 19, 2015
    Inventors: Rongshi Li, Said M. Sebti, Yan Liu
  • Publication number: 20150073139
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: July 21, 2014
    Publication date: March 12, 2015
    Inventors: Ulrich GÖRGENS, Jun MIHARA, Tetsuya MURATA, Daiei YAMAZAKI, Yasushi YONETA, Koichi ARAKI, Norio SASAKI, Kei DOMON, Mamoru HATAZAWA, Eiichi SHIMOJO, Teruyuki ICHIHARA, Masashi ATAKA, Katsuhiko SHIBUYA
  • Publication number: 20150051262
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Application
    Filed: October 24, 2012
    Publication date: February 19, 2015
    Applicant: NORTHWESTERN UNIVERSITY
    Inventors: M. Amin Khan, Joseph Moskal
  • Patent number: 8957058
    Abstract: The invention relates to compounds of formula (I): where A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: October 3, 2011
    Date of Patent: February 17, 2015
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Berthon
  • Publication number: 20150030618
    Abstract: The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: May 5, 2014
    Publication date: January 29, 2015
    Applicant: SEATTLE GENETICS, INC.
    Inventors: Hans-Georg LERCHEN, Lars Linden, Sherif El Sheikh, Jörg Willuda, Charlotte C. Kopitz, Joachim Schuhmacher, Simone Greven, Christoph Mahlert, Beatrix Stelte-Ludwig, Sven Golfier, Rudolf Beier, Iring Heisler, Axel Harrenga, Karl-Heinz Thierauch, Sandra Bruder, Heike Petrul, Hannah Jörissen, Sandra Borkowski
  • Patent number: 8940776
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: January 27, 2015
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Publication number: 20150025222
    Abstract: The invention discloses new substituted anthraquinone dyes that may be useful as cellular stains. In some aspect of the invention, the nuclear stains are useful for staining the nuclei of dead or fixed cells. Another aspect of the invention relates to substituted anthraquinone dyes comprising an enzyme substrate moiety that is transformable or cleavable by an enzyme such that the transformation or cleavage of the substrate moiety causes a detectable change in the functionality or spectral properties of the dye.
    Type: Application
    Filed: April 9, 2014
    Publication date: January 22, 2015
    Applicant: Biotium, Inc.
    Inventors: Fei MAO, Wai-Yee LEUNG, Ching-Ying CHEUNG, Lori Michelle ROBERTS
  • Publication number: 20150005283
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 1, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
  • Publication number: 20140371138
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, John A. McCauley, Steven W. Ludmerer, Kun Liu, Joseph P. Vacca, Hao Wu, Bin Hu, Richard Soll, Fei Sun, Xinghai Wang, Man Yan, Chengren Zhang, Mingwei Zheng, Bin Zhong, Jian Zhu
  • Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • Patent number: 8889683
    Abstract: The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: November 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Clifford Cheng, Gerald W. Shipps, Jr., Xiaohua Huang, Ying Huang, Ning Shao, Ashwin Rao, Anandan Palani, Peter Orth, Johannes H. Voigt, Robert J. Herr, Lana Michele Rossiter, Qi Zeng, Xianfeng Sun
  • Publication number: 20140336285
    Abstract: The present invention relates to demulsifying and dehydrating formulations of heavy crude oil based block copolymers amine bifunctionalized with low polydispersities. These formulations can contain solvents whose boiling point is in the range from 35 to 200° C.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Gabriel Cendejas Santana, Eugenio Alejandro Flores Oropeza, Laura Veronica Castro Sotelo, Aristeo Estrada Buendia, Marcelo Lozada y Cassou, Flavio Salvador Vazquez Moreno
  • Publication number: 20140336158
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • Patent number: 8883821
    Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: November 11, 2014
    Assignee: Pierre Fabre Medicament
    Inventors: El Bachir Kaloun, Karim Bedjeguelal, Rémi Rabot, Anna Kruczynski, Philippe Schmitt, Michel Perez, Nicolas Rahier
  • Patent number: 8877772
    Abstract: Provided are compounds having an inhibitory effect on Mixed Lineage Kinases, having a structural Formula, Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders which comprise the inhibition of Mixed Lineage Kinases.
    Type: Grant
    Filed: November 25, 2009
    Date of Patent: November 4, 2014
    Assignee: University of Rochester
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Colin Loweth, Torsten Wiemann
  • Patent number: 8877942
    Abstract: The present invention relates to 2,2?-di-substituted dipyrrins. The invention also relates to methods for the preparation of 2,2?-disubstituted dipyrrins, and to the use of 2,2?-disubstituted dipyrrins in, for example, sensing, imaging and laser applications.
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: November 4, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Mikhail Filatov, Andrei Cheprakov, Sergei A. Vinogradov, Artem Y. Lebedev
  • Patent number: 8877759
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: September 4, 2012
    Date of Patent: November 4, 2014
    Assignee: Vertex Pharnaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8865715
    Abstract: The invention relates to compounds the formula (I): and pharmaceutically usable salts, tautomers and stereoisomers thereof, wherein R1, R2 and R3 are defined herein. The compounds of formula (I) and their pharmaceutically usable salts, tautomers and stereoisomers are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: October 21, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Margarita Wucherer-Plietker, Thomas J. J. Mueller, Eugen Merkul
  • Patent number: 8859785
    Abstract: A compound comprising one or more polyfunctionalized pyrrolyl anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-pyrrolyl anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: October 14, 2014
    Assignee: Air Products and Chemicals, Inc.
    Inventor: John Anthony Thomas Norman
  • Patent number: 8853679
    Abstract: A semiconducting compound comprising the structure: where R1 to R4 independently comprise, but are not limited to, optionally substituted straight, branched or cyclic alkyl chains having 2 to 20 (e.g. 2 to 12) carbon atoms, alkoxy, amino, amido, silyl, alkyl, alkenyl, aryl or hetero aryl; where X1 and X2 independently comprise S, O, NR5 or SiR6R7 where R8 to R7 independently comprise C1 to C5 branched, straight or cyclic alkyl chains; and where Ar1 comprises a heterocyclic ring, and where n is an integer between 1 and 4.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: October 7, 2014
    Assignee: Cambridge Display Technology Limited
    Inventors: Sheena Zuberi, Tania Zuberi
  • Patent number: 8846953
    Abstract: The present invention provides for synthetic processes for the making of substituted 3-((pyrrol-2-yl)methylene)-2-pyrrolones, including sunitinib. The present invention also provides for a process of crystallizing substantially pure sunitinib L-malate.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: September 30, 2014
    Assignee: Scinopharm Taiwan, Ltd.
    Inventors: Julian P. Henschke, Yung-Fa Chen
  • Publication number: 20140288144
    Abstract: A compound of formula (I): R?—O-A-O—R??, in which R? and R? are a hydrogen atom or a monovalent radical of formula (IIa), or a monovalent radical of formula (IIb), it being understood that at least one of the radicals R? or R? is not a hydrogen atom and that, when none of the radicals R? and R? is a hydrogen atom, R? and R? are identical, and in which A is a divalent radical of formula (III): —CH(X1)-[C(X2)(X3)]p-CH(X4) in which X1, X2, X3 and X4 are identical or different and are either a hydrogen atom or a methyl radical or an ethyl radical, and p is an integer greater than or equal to 1 and less than or equal to 6. Also the method for preparing the compound of formula (I) and to the use thereof in cosmetics and as a drug.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 25, 2014
    Applicant: Societe D'Exploitation de Produits Pour Les Industries Chimiques Seppic
    Inventors: Sandy Dumont, Jerome Guilbot, Stephanie Garcel, Laetitia Cattuzzato
  • Publication number: 20140288065
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Publication number: 20140249319
    Abstract: Chemical crosslinkers and methods of their synthesis are disclosed.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 4, 2014
    Inventor: Mark Quang Nguyen
  • Patent number: 8822469
    Abstract: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: September 2, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Somhairle MacCormick, Pierre-Henri Storck, Michael Paul Mortimore, Jean-Damien Charrier, Ronald Knegtel, Stephen Clinton Young, Joanne Pinder, Steven John Durrant
  • Patent number: 8816099
    Abstract: A polyfunctional polyoxyalkylene compound represented by the following formula (1): wherein Z represents a hydroxyl group-removed residue of pentaerythritol or dipentaerythritol, R represents a hydrocarbon group having 1 to 24 carbon atoms, OA1 and OA2 represent an oxyalkylene group having 2 to 4 carbon atoms, L1 and L2 represent an alkylene group which may have an ester bond or the like in the alkylene chain or at the terminal end, and X represents a functional group capable of reacting chemically; R, OA1, OA2, L1, and L2 are the same or different from one another in one molecule, m and n are an average number of moles of the oxyalkylene group added, m represents 5 to 1,000, and n represents 0 to 1,000; p and q represent 0 or 1; r1+r2=4 or 6; and r1 and r2 are an integer of 2 or more.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: August 26, 2014
    Assignee: NOF Corporation
    Inventors: Ken-ichiro Nakamoto, Masaki Kamiya, Tsuyoshi Takehana
  • Patent number: 8815869
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: August 26, 2014
    Assignee: AbbVie Inc.
    Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
  • Publication number: 20140221644
    Abstract: Bacteriochlorin of Formula I: wherein R is H or silyl are described, along with compositions containing the same and methods of making and using the same.
    Type: Application
    Filed: August 24, 2012
    Publication date: August 7, 2014
    Inventors: Jonathan S. Lindsey, Olga Mass
  • Patent number: 8790892
    Abstract: The invention discloses new substituted anthraquinone dyes that may be useful as cellular stains. In some aspect of the invention, the nuclear stains are useful for staining the nuclei of dead or fixed cells. Another aspect of the invention relates to substituted anthraquinone dyes comprising an enzyme substrate moiety that is transformable or cleavable by an enzyme such that the transformation or cleavage of the substrate moiety causes a detectable change in the functionality or spectral properties of the dye.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: July 29, 2014
    Assignee: Biotium, Inc.
    Inventors: Fei Mao, Wai-Yee Leung, Ching-Ying Cheung, Lori Michelle Roberts
  • Patent number: 8791118
    Abstract: The invention provides new pyridopyrazine compounds according to formula (I) which are highly selective as Ras-Raf-Mek-Erk signal transduction pathway inhibitors and in particular are highly selective Erk inhibitors.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: July 29, 2014
    Assignee: Aeterna Zentaris GmbH
    Inventors: Matthias Gerlach, Irene Seipelt, Lars Blumenstein, Gilbert Mueller, Eckhard Guenther, Tilmann Schuster, Michael Teifel
  • Patent number: 8791119
    Abstract: Compounds corresponding to the general formula (I) wherein R2 represents a group C1-10-alkyl, C3-10-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl-C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6-alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy-C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; X6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Sanofi
    Inventors: Sylvain Cote Des Combes, Jacques Froissant, Jean-Francois Gibert, Frank Marguet, Christophe Pacaud, Frédéric Puech, Antoine Ravet
  • Patent number: 8785639
    Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: July 22, 2014
    Assignee: AbbVie Inc.
    Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
  • Patent number: 8778942
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: July 15, 2014
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
  • Publication number: 20140187795
    Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as CRTH2 antagonists. Compounds prepared by the processes of the invention are of Formula (AI), (All) and Compound (I).
    Type: Application
    Filed: June 17, 2011
    Publication date: July 3, 2014
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: James Jia, Regina Graul, Wayne C Schairer, Vishnu Karnati, Ray Forslund
  • Publication number: 20140174736
    Abstract: A method of servicing a wellbore in a subterranean formation comprising placing a composition comprising a carrier fluid and a degradable polymer into the subterranean formation wherein the degradable polymer comprises polyimide, allowing the degradable polymer to form a diverter plug at a first location in the wellbore or subterranean formation, diverting the flow of a wellbore servicing fluid to a second location in the wellbore or subterranean formation that is different than the first location; and removing all or a portion of the diverter plug by contacting the diverter plug with a degradation accelerator wherein the degradation accelerator comprises an amino alcohol, an amino alcohol precursor, an organic amine, an organic amine precursor or combinations thereof. A wellbore servicing fluid comprising polysuccinimide wherein the wellbores servicing fluid has a pH of less than about 7.
    Type: Application
    Filed: December 21, 2012
    Publication date: June 26, 2014
    Applicant: HALLIBURTON ENERGY SERVICES, INC.
    Inventors: B. Raghava REDDY, Wirdansyah LUBIS, Hsin-Chen CHUNG, Natalie Lynn PASCARELLA
  • Publication number: 20140178416
    Abstract: Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.
    Type: Application
    Filed: November 14, 2013
    Publication date: June 26, 2014
    Applicant: IMMUNOGEN, INC.
    Inventors: Ravi V.J. Chari, Robert Yongxin Zhao, Yelena Kovtun, Rajeeva Singh, Wayne C. Widdison
  • Patent number: 8759541
    Abstract: The current application relates to a metal catalyst of formula (I): M[ADC][X]n, wherein M is a metal, ADC is a chiral acyclic diaminocarbene ligand, and X is a neutral or anionic ligand. The ADC ligand is prepared from the corresponding chiral formamidium salt precursor. The metal catalyst is used for asymmetric organic synthesis reactions such as hydrosilations, hydrogenations, conjugate additions, and cross-couplings.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: June 24, 2014
    Inventors: Avinash N. Thadani, Rukundo Ntaganda, Mira M. Beshai