Patents Issued in March 16, 2017
  • Publication number: 20170073321
    Abstract: Provided is an enzyme-specific fluorescent compound capable of being retained in cells, which can emit fluorescence specifically in a target cell, particularly a cell capable of expressing a reporter enzyme such as ?-galactosidase, and can covalently bind to a protein in the cell to exhibit an excellent property of being retained in the cell. The fluorescent compound comprises a compound represented by formula (I?) or a salt thereof. In formula (I?), A, X, Y and R1 to R9 are as described in claim 1.
    Type: Application
    Filed: May 13, 2015
    Publication date: March 16, 2017
    Applicant: The University of Tokyo
    Inventors: Yasuteru URANO, Mako KAMIYA, Tomohiro DOURA
  • Publication number: 20170073322
    Abstract: In one embodiment, the present application discloses mixtures comprising (a) water in an amount of at least 1% wt/wt of the mixture; (b) a transition metal catalyst; and (c) one or more solubilizing agents; and methods for using such mixtures for performing transition metal mediated bond formation reactions.
    Type: Application
    Filed: June 16, 2014
    Publication date: March 16, 2017
    Applicant: MyCell Technologies, LLC
    Inventor: Volker Berl
  • Publication number: 20170073323
    Abstract: Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: wherein R2, R3 and R4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.
    Type: Application
    Filed: November 23, 2016
    Publication date: March 16, 2017
    Applicant: CHIROGATE INTERNATIONAL INC.
    Inventors: Shih-Yi Wei, Yu-Chih Yeh, Min-Kuan Hsu, Li-Ta Kao
  • Publication number: 20170073324
    Abstract: A new compound, bifidenone, is provided. Compositions and methods useful for reducing or inhibiting tumor growth including the bifidenone is also provided.
    Type: Application
    Filed: September 11, 2015
    Publication date: March 16, 2017
    Inventor: Russell B. Williams
  • Publication number: 20170073325
    Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
    Type: Application
    Filed: November 2, 2016
    Publication date: March 16, 2017
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Publication number: 20170073326
    Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: November 9, 2016
    Publication date: March 16, 2017
    Inventors: Indu T. BHARATHAN, Chris BLACKBURN, Jeffrey P. CIAVARRI, Jouhara CHOUITAR, Courtney A. CULLIS, Natalie D'AMORE, Paul E. FLEMING, Kenneth M. GIGSTAD, Krista E. GIPSON, Mario GIRARD, Yongbo HU, Janice LEE, Gang LI, Mansoureh REZAEI, Michael D. SINTCHAK, Francois SOUCY, Stephen G. STROUD, Tricia J. VOS, Tzu-Tshin WONG, He XU, Tianlin XU, Yingchun YE
  • Publication number: 20170073327
    Abstract: The present invention relates to novel crystal forms M and N of dabigatran etexilate mesylate and preparation method and uses thereof, wherein the X-Ray powder diffractogram of the crystal form M has characteristic peaks at the following 2? diffraction angles: 5.7±0.2°, 6.2±0.2°, 11.2±0.2°, 12.4±0.2°, 18.2±0.2°, 21.4±0.2°, 21.8±0.2° and 23.6±0.2°; and the X-Ray powder diffractogram of the crystal form N has characteristic peaks at the following 20 diffraction angles: 6.0±0.2°, 11.8±0.2°, 18.2±0.2°, 21.6±0.2°, 24.4±0.2°, 27.7±0.2° and 29.7±0.2°. The crystal forms of the present invention have excellent properties in the aspects of leaching time, biological release, chemical stability and processing adaptability.
    Type: Application
    Filed: March 4, 2015
    Publication date: March 16, 2017
    Applicant: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Liang Zhang, Chuan Liu, Jinyi Xu, Zhaozhao Zhang, Zhi Chen, Jian Chai, Zhiqing Yang, Hairong Luo, Xiangyang Zhang
  • Publication number: 20170073328
    Abstract: Compounds that target vascular endothelial growth factor receptors for therapy and imaging are disclosed. Methods for making the compounds and detecting or imaging cells expressing VEGFR using the compounds are also provided. In accordance with the purposes of the disclosed subject matter, as embodied and broadly described herein, disclosed are compounds, and methods of making and using the compounds. The disclosed compounds, in one aspect, are quinazoline compounds.
    Type: Application
    Filed: May 14, 2015
    Publication date: March 16, 2017
    Inventors: Zheng Li, Feng Li
  • Publication number: 20170073329
    Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
    Type: Application
    Filed: November 23, 2016
    Publication date: March 16, 2017
    Inventors: Geoff G.Z. ZHANG, Michael F. BRADLEY, David M. BARNES, Rodger HENRY
  • Publication number: 20170073330
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: November 28, 2016
    Publication date: March 16, 2017
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Publication number: 20170073331
    Abstract: The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.
    Type: Application
    Filed: April 17, 2015
    Publication date: March 16, 2017
    Applicant: IMMUNOMET THERAPEUTICS INC.
    Inventors: Sung Wuk Kim, Hong Woo Kim, Sang Hee Yoo, Ji Sun Lee, Hye Jin Heo, Hong Bum Lee, Ji Ae Kook, Young Woo Lee, Mi Jeong Kim, Woong Cho
  • Publication number: 20170073332
    Abstract: Compounds for the treatment of bacterial and parasitic infections which are hybrid compounds of compounds having antibacterial or antiparasitic activity and compounds that decrease the absorption of the hybrid compound from the gastrointestinal tract. The compounds are preferably for use against C. difficile infections and comprise a hybrid molecule of an anti-C. difficile compound such as a nitroimidazole and a tetramic acid derivative.
    Type: Application
    Filed: March 12, 2015
    Publication date: March 16, 2017
    Inventors: Richard E. Lee, Philip T. Cherian, Julian G. Hurdle, Xiaoqian WU
  • Publication number: 20170073333
    Abstract: The invention relates to new substituted heteroaryls of formula 1 or of formula 1? wherein A is either N or CH, wherein R2 is selected from the group consisting of —C1-3-alkyl, —C1-3-haloalkyl, F, Br, Cl, wherein Y is selected from —O— or —CH2—, and wherein R3 is defined as in claim 1, and the pharmaceutically acceptable salts thereof, and the use of these aforementioned compounds for the treatment of diseases such as asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
    Type: Application
    Filed: September 2, 2016
    Publication date: March 16, 2017
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias HOFFMANN, Georg DAHMANN, Christian GNAMM, Daniel FANDRICK, John SCOTT, Clive McCARTHY
  • Publication number: 20170073334
    Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
    Type: Application
    Filed: September 7, 2016
    Publication date: March 16, 2017
    Applicants: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLC
    Inventors: Ning Xi, Minxiong Li, Xiaobo Li, Wuhong Chen, Tao Zhang, Haiyang Hu, Weilong Dai, Yanjun Wu
  • Publication number: 20170073335
    Abstract: The present invention provides a compound having a particular chemical structure or a pharmacologically acceptable salt thereof which has an excellent inhibitory effect on EZH1 and/or EZH2 activity. The present invention provides a compound having a 1,3-benzodioxole structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, or a pharmaceutical composition comprising the compound (wherein R1, R2, R3, R4, R5, R6, and V in the formula (I) are each as defined in the present specification).
    Type: Application
    Filed: March 16, 2015
    Publication date: March 16, 2017
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Osamu KANNO, Jun WATANABE, Takao HORIUCHI, Akira NAKAO, Keisuke SUZUKI, Tomonori YAMASAKI, Nobuaki ADACHI, Daisuke HONMA, Yoshito HAMADA
  • Publication number: 20170073336
    Abstract: The present invention provides a novel process for the preparation of Canagliflozin (I) and its hydrates thereof by employing novel intermediates. The present invention is also provides commercially and industrial applicable process.
    Type: Application
    Filed: August 23, 2016
    Publication date: March 16, 2017
    Inventors: Srinivas Reddy DESI REDDY, Dnyandev Ragho RANE, Venkata Srinivasa Rao VELIVELA
  • Publication number: 20170073337
    Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ? production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent, for diseases induced by production, secretion and/or deposition of amyloid ? proteins. A compound of the formula (I) wherein X is —S— or —O—, R3a is alkyl, haloalkyl or the like, R2a is H, halogen, alkyloxy, haloalkyloxy or the like, R2b is H or the like, R3b is H or alkyl, ring A and ring B is each independently a substituted or unsubstituted aromatic carbocycle, a substituted or unsubstituted aromatic heterocycle or the like, and R1 is substituted or unsubstituted alkyl or the like, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 10, 2015
    Publication date: March 16, 2017
    Inventors: Ken-ichi KUSAKABE, Genta TADANO, Kazuo KOMANO, Kouki FUCHINO, Kenji NAKAHARA
  • Publication number: 20170073338
    Abstract: This invention relates to a novel crystalline form of 6-[(4R)-4-methyl-1,1-dioxido-1,2,6-thiadiazinan-2-yl]isoquinoline-1-carbonitrile which is useful as a selective androgen receptor modulator (SARM), and to compositions thereof and suitable processes for the preparation thereof.
    Type: Application
    Filed: May 1, 2015
    Publication date: March 16, 2017
    Applicant: Pfizer Inc.
    Inventors: Eugene Lvovich Piatnitski CHEKLER, Roberta Louise DOROW, Jeffrey Braden SPERRY
  • Publication number: 20170073339
    Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CYP17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.
    Type: Application
    Filed: November 23, 2016
    Publication date: March 16, 2017
    Inventors: Roger A. Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
  • Publication number: 20170073340
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, Formula (I) wherein L, X, Ra, Rb, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: February 19, 2015
    Publication date: March 16, 2017
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Charlotte Fieldhouse, Angela Glen, Tatsuhiko Fujimoto, John Stephen Robinson
  • Publication number: 20170073341
    Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Application
    Filed: October 26, 2016
    Publication date: March 16, 2017
    Inventor: Tara Renae Rheault
  • Publication number: 20170073342
    Abstract: The invention relates to novel compounds of the formula (I) in which the R1, R2a, R2b, R3, A1, A2, A3, A4, A5 and n radicals are each as defined above, to the use thereof as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for preparation thereof.
    Type: Application
    Filed: February 5, 2015
    Publication date: March 16, 2017
    Inventors: Rüdiger FISCHER, Bernd ALIG, Kerstin ILG, Olga MALSAM, Ulrich GÖRGENS, Andreas TURBERG, Jun LI, Sergey ZHERSH, Alexander ARLT
  • Publication number: 20170073343
    Abstract: The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof wherein R1, R1a, R1b, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
    Type: Application
    Filed: September 12, 2016
    Publication date: March 16, 2017
    Applicant: Pfizer Inc.
    Inventors: Paul Galatsis, Jaclyn Louise Henderson, Bethany Lyn Kormos, Ravi G. Kurumbail, Matthew Richard Reese, Antonia Friederike Stepan, Patrick Robert Verhoest, Travis T. Wager, Martin Youngjin Pettersson, Michelle Renee Garnsey
  • Publication number: 20170073344
    Abstract: The present invention related to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.
    Type: Application
    Filed: November 23, 2016
    Publication date: March 16, 2017
    Inventor: Songzhu An
  • Publication number: 20170073345
    Abstract: The invention relates to the compounds and compositions of Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprises a salt of dipeptidyl peptidase-4 inhibitor and the methods for treating or preventing metabolic syndrome, prediabetes and diabetes may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compounds and compositions may be used to treatment of diabetes mellitus, obesity, lipid disorders, hypertriglyceridemia, hyperglycemia, hyperinsulinemia and insulin resistance.
    Type: Application
    Filed: November 11, 2015
    Publication date: March 16, 2017
    Inventor: Mohan Murali Alapati
  • Publication number: 20170073346
    Abstract: Compounds of the formula (I), wherein Y—X, R1, R2, R3, R4, R5, R6, R7, R8, A1, A2, A3, Ra and n areas defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
    Type: Application
    Filed: February 26, 2015
    Publication date: March 16, 2017
    Applicant: Syngenta Participations AG
    Inventors: Laura QUARANTA, Stephan TRAH, Farhan BOU HAMDAN, Clemens LAMBERTH
  • Publication number: 20170073347
    Abstract: Compounds of the formula I in which W, X and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Application
    Filed: April 16, 2015
    Publication date: March 16, 2017
    Applicant: Merck Patent GmbH
    Inventors: Hans-Peter BUCHSTALLER, Dieter DORSCH
  • Publication number: 20170073348
    Abstract: The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with heterocyclic derivatives of Formula (I) wherein R1, R2, R3, R4 and Het have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: November 3, 2016
    Publication date: March 16, 2017
    Inventors: Lieven Meerpoel, Louis Jules Roger Marie MAES, Kelly de Wit, Koen Jan Ludovicus AUGUSTYNS
  • Publication number: 20170073349
    Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
    Type: Application
    Filed: November 23, 2016
    Publication date: March 16, 2017
    Applicant: BeiGene, Ltd.
    Inventors: Zhiwei WANG, Yunhang GUO
  • Publication number: 20170073350
    Abstract: Disclosed is a method for preparing Volasertib (I), comprising the following steps: an intermediate 2-amino-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) is nucleophilically substituted with an intermediate N-[trans-4-[4-(cylopropylmethyl)-1-piperazinyl]cyclohexyl]-4-halo-3-methoxylbenzamide (III), so as to prepare Volasertib (I). The preparation method has a simple process, mild conditions and few side effects, which meets the requirements for industrial enlargement. In addition, also disclosed are an intermediate 2-amino-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) and an intermediate N-[trans-4-[4-(cylopropylmethyl)-1-piperazinyl]cyclohexyl]-4-halo-3-methoxylbenza-mide (III) of Volasertib and the preparation methods thereof.
    Type: Application
    Filed: November 25, 2016
    Publication date: March 16, 2017
    Applicant: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
    Inventor: Xuenong XU
  • Publication number: 20170073351
    Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.
    Type: Application
    Filed: September 28, 2016
    Publication date: March 16, 2017
    Inventors: Mikhail Chafeev, Jianmin Fu, Jean-Jacques Alexandre Cadieux
  • Publication number: 20170073352
    Abstract: This invention relates to a compound of formula I wherein A and Cy have one of the meanings as indicated in the specification and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: November 29, 2016
    Publication date: March 16, 2017
    Inventors: Viktor VINTONYAK, Matthias GRAUERT, Marc GRUNDL, Alexander PAUTSCH
  • Publication number: 20170073353
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the ?-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
    Type: Application
    Filed: September 15, 2016
    Publication date: March 16, 2017
    Inventors: Jürgen DINGES, Achim MOELLER, Michael OCHSE, Martin SCHMIDT, Michael SCHULZ, Sean TURNER, Elizabeth Louise VAN DER KAM, Anil VASUDEVAN
  • Publication number: 20170073354
    Abstract: The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
    Type: Application
    Filed: March 6, 2015
    Publication date: March 16, 2017
    Applicants: Merck Sharp & Dohme Corp., MSD R&D (China) Co., Ltd.
    Inventors: Peter D. Williams, John A. McCauley, Christopher J. Bungard, David Jonathan Bennett, Sherman T. Waddell, Gregori J. Morriello, Lehua Chang, Michael P. Dwyer, M. Katharine Holloway, Alejandro Crespo, Xin-Jie Chu, Catherine Wiscount, H. Marie Loughran, Jesse J. Manikowski, Jurgen Schulz, Kartik M. Keertikar, Bin Hu, Bin Zhong, Tao Ji
  • Publication number: 20170073355
    Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 19, 2015
    Publication date: March 16, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Raphaelle Berger, Guizhen Dong, Subharekha Raghavan, Zhiqiang Yang
  • Publication number: 20170073356
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in intro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: September 30, 2016
    Publication date: March 16, 2017
    Applicants: GILEAD CONNECTICUT, INC., GENENTCH INC.
    Inventors: Antonio J.M. BARBOSA, Peter A. BLOMGREN, Kevin S. CURRIE, Ravi KRISHNAMOORTHY, Jeffrey E. KROPF, Seung H. LEE, Scott A. MITCHELL, Daniel ORTWINE, Aaron C. SCHMITT, Xiaojing WANG, Jianjun XU, Wendy YOUNG, Honglu ZHANG, Zhongdong ZHAO, Pavel E. ZHICHKIN
  • Publication number: 20170073357
    Abstract: Benzodiazepine dimers having a structure represented by wherein R1 is wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).
    Type: Application
    Filed: November 15, 2016
    Publication date: March 16, 2017
    Inventors: Yong ZHANG, Ivar M. MCDONALD, Naidu S. CHOWDARI, Tram N. HUYNH, Robert M. BORZILLERI, Sanjeev GANGWAR
  • Publication number: 20170073358
    Abstract: There is described a phthalocyanine derivative of formula (I) consisting of 4 isomers wherein the relative isomer B content is less than or equal to 1% by weight.
    Type: Application
    Filed: January 28, 2016
    Publication date: March 16, 2017
    Inventors: Gabrio RONCUCCI, Donata DEI, Giacomo CHITI, Daniele NISTRI
  • Publication number: 20170073359
    Abstract: The present invention relates to compounds that are substrates for an enzyme, and upon reaction with the enzyme provide a detectable response, such as an optically detectable response. In particular, the compounds have utility in detecting the presence of a ?-lactamase in a sample. In addition to the compounds, methods are disclosed for analyzing a sample for the presence of a ?-lactmase, for example, as an indicator of expression of a nucleic acid sequence including a sequence coding for a ?-lactmase. Kits are disclosed that include the disclosed compounds and additional components, for example, cells, antibodies, a ?-lactmase or instructions for using the components in an assay.
    Type: Application
    Filed: September 26, 2016
    Publication date: March 16, 2017
    Inventors: Schuyler CORRY, William DOWNEY, Brian FILANOSKI, Kyle GEE, Lawrence GREENFIELD, James HIRSCH, Iain JOHNSON, Aleksey RUKAVISHNIKOV
  • Publication number: 20170073360
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Application
    Filed: September 9, 2016
    Publication date: March 16, 2017
    Inventors: Christopher J. BURNS, Bin LIU, Jiangchao YAO, Denis DAIGLE, Steven A. BOYD
  • Publication number: 20170073361
    Abstract: The present application provides precursor compounds useful for deposition of a group 11 metal on a substrate, for example, a microelectronic device substrate, as well as methods of synthesizing such precursor compounds. The precursor compounds provided are mono-metallic compounds comprising a diaminocarbene (DAC) having the general formula: “DAC-M-X”, where the diaminocarbene is an optionally substituted, saturated N-heterocyclic diaminocarbene (sNHC) or an optionally substituted acyclic diaminocarbene, M is a group 11 metal, such as copper, silver or gold; and X is an anionic ligand. Also provided are methods of synthesizing the precursor compounds, metal deposition methods utilizing such precursor compounds, and to composite materials, such as, e.g., microelectronic device structures, and products formed by use of such precursors and deposition methods.
    Type: Application
    Filed: September 23, 2016
    Publication date: March 16, 2017
    Inventors: Sean BARRY, Jason COYLE, Timothy James CLARK, Jeffrey J.M. HASTIE
  • Publication number: 20170073362
    Abstract: Large scale (bulk) compositions comprising high-purity stannsoporfin are disclosed, as well as methods of synthesizing such compositions.
    Type: Application
    Filed: November 4, 2016
    Publication date: March 16, 2017
    Inventors: George S. DRUMMOND, Robert CAROSELLI, Keith A. COOKE, Daniel LEVIN, David G. ROE, Christopher P. BOUCHER
  • Publication number: 20170073363
    Abstract: Platinum(II) complexes having thione-based heterocyclic ligands as anticancer agents. The central platinum atom is coordinated by four of the ligands, each having a five-, six- or seven-membered heterocyclic ring with two nitrogen atoms at positions 1 and 3 of the ring and a thiocarbonyl group at position 2. Pharmaceutical compositions incorporated the platinum(II) complexes, methods of synthesizing the complexes and methods of treating cancers with the complexes or pharmaceutical compositions thereof are also described.
    Type: Application
    Filed: September 30, 2016
    Publication date: March 16, 2017
    Applicant: KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS
    Inventors: Muhammad ALTAF, Anvarhusein Abdulkadir ISAB
  • Publication number: 20170073364
    Abstract: Compositions and methods comprising metal organic frameworks (MOFs) and related uses are generally provided. In some embodiments, a MOF comprises a plurality of metal ions, each coordinated with at least one ligand comprising at least two sets of ortho-diimine groups arranged about an organic core.
    Type: Application
    Filed: May 6, 2015
    Publication date: March 16, 2017
    Applicant: Massachusetts Institute of Technology
    Inventors: Mircea Dinca, Dennis Sheberla, Lei Sun, Casey R. Wade, Michael Glenn Campbell
  • Publication number: 20170073365
    Abstract: A method for the preparation of lignin from lignocellulosic material by pulping with alcohol, in particular with a C1-4 alcohol, water and a base, in particular NaOH, at a temperature below 100° C., in particular from 40° C. to 90° C., in particular from 50° C. to 70° C., characterized in that 3 to 12 parts of base, in particular 4 to 10 parts of base, in particular preferable 5 to 8 parts of base, are used per 100 parts of the dry lignocellulosic material to be pulped.
    Type: Application
    Filed: November 4, 2016
    Publication date: March 16, 2017
    Inventors: Karin Fackler, Thomas Ters, Ortwin Ertl, Kurt Messner
  • Publication number: 20170073366
    Abstract: The present invention includes crystalline forms of N-acetylneuraminic acid (NeuAc) and crystalline forms of salts and/or solvates of N-acetylneuraminic acid (NeuAc). Furthermore, the present invention provides compositions comprising these crystalline forms and therapeutic use of the crystalline forms.
    Type: Application
    Filed: September 14, 2016
    Publication date: March 16, 2017
    Inventors: John Klopp, Hayley Reece, Jean-Baptiste Arlin, Corinna Marie Reisinger-Becker, Fabrice Dufour
  • Publication number: 20170073367
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Application
    Filed: December 23, 2014
    Publication date: March 16, 2017
    Inventors: Stephen Critchley, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
  • Publication number: 20170073368
    Abstract: The present disclosure provides methods for synthesizing modified nucleosides, nucleotides, and oligonucleotides comprising at least one 2?-C-Bridged Bicyclic Nucleotide, and to intermediates used in the process.
    Type: Application
    Filed: March 16, 2015
    Publication date: March 16, 2017
    Applicant: MiRagen Therapeutics, Inc.
    Inventor: Kurt VAGLE
  • Publication number: 20170073369
    Abstract: The disclosure provides methods of treating X-linked hypophosphatemia, related bone demineralization and renal phosphate wasting disorders in a mammalian subject.
    Type: Application
    Filed: November 8, 2016
    Publication date: March 16, 2017
    Inventors: Marc K. DREZNER, Baozhi YUAN
  • Publication number: 20170073370
    Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. The compounds provided herein can in other embodiments overcome the resistance conferred by single amino acid mutations at defined positions of bacterial Signal Peptidases (SPases) and in other embodiments provide for a broader spectrum of antibiotic bioactivity compared to the natural product. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
    Type: Application
    Filed: November 21, 2016
    Publication date: March 16, 2017
    Inventors: Tucker Curran ROBERTS, Peter Andrew SMITH, David CAMPBELL, Sergio G. DURON, Robert I. HIGUCHI