Quinoline Or Isoquinoline (including Hydrogenated) Patents (Class 544/363)
  • Patent number: 10166296
    Abstract: The invention relates to compounds of Formula I, wherein R1, R2, and R3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from aripiprazole. The invention also relates to conjugates of an aripiprazole hapten and a protein.
    Type: Grant
    Filed: October 20, 2017
    Date of Patent: January 1, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Ronghui Lin, Rhys Salter, Thomas R. DeCory, Eric Hryhorenko, Bart M. Remmerie, Banumathi Sankaran
  • Patent number: 9776970
    Abstract: The present subject matter relates to solvates and the amorphous form of bosutinib; the solvates namely being a propylene glycol solvate and an acetonitrile solvate. Also provided are processes for preparing the propylene glycol solvate, the amorphous form and the crystalline acetonitrile solvate of bosutinib; as well as compositions comprising said forms. Bosutinib is a 3-quinolinecarbonitrile kinase inhibitor and is indicated for the treatment of adult patients with chronic, accelerated, or blast phase Ph+ chronic myelogenous leukemia (CMS) with resistance or intolerance to prior therapy.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: October 3, 2017
    Assignee: Apotex Inc.
    Inventors: Padiyath Mohammed Akbarali, Venkata Ramana Kintali, Heggadde Nanjunda Bhatta Shreenivasa Murthy, Girisha Meenkere, Somanath Bhupal Venkata, Raja Ramesh Manda, Vishal Amrutlal Sodha, Abbulu Kante
  • Patent number: 9504682
    Abstract: The invention relates to compounds of Formula I, wherein R1, R2, and R3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from aripiprazole. The invention also relates to conjugates of an aripiprazole hapten and a protein.
    Type: Grant
    Filed: August 20, 2013
    Date of Patent: November 29, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Ronghui Lin, Rhys Salter, Thomas R. DeCory, Eric Hryhorenko, Bart Remmerie, Banumathi Sankaran
  • Patent number: 9278934
    Abstract: The present invention provides a novel method for producing fine particles of aripiprazole anhydride crystals B. The method for producing fine particles of aripiprazole anhydride crystals B comprises the steps of: (1) heating and dissolving crude aripiprazole in a lower alcohol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcohol solvate; (2) subjecting the crystals of aripiprazole lower alcohol solvate to wet-milling in the form of a slurry containing the lower alcohol; and (3) subjecting the dispersion of the wet-milled crystals to solid-liquid separation to obtain the crystals, and heating the crystals.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: March 8, 2016
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Takuji Bando, Katsuhiko Yano, Makoto Fukana, Satoshi Aoki
  • Patent number: 9206133
    Abstract: The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts.
    Type: Grant
    Filed: June 5, 2012
    Date of Patent: December 8, 2015
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Walter Cabri, Roberto Castagnani, Silvia Armaroli, Gianandrea Quattrociocchi, Vincenzo Colangeli
  • Patent number: 9206169
    Abstract: The present invention provides a method for producing a compound of Formula (4): wherein R1 is a hydrogen atom etc. by reacting a compound of Formula (2): wherein X1 is a leaving group, with a compound of Formula (3): wherein R1 is as defined above, in the presence of (a) a palladium compound and a tertiary phosphine or (b) a palladium carbene complex, in an inert solvent or without a solvent. The present invention can produce the compound of Formula (4), with high purity and high yield, and by a simple operation.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: December 8, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Koichi Shinhama, Naoto Utsumi, Masahiro Sota, Shigeo Fujieda, Shin Ogasawara
  • Patent number: 9073857
    Abstract: A method for preparing an aripiprazole type I microcrystal, including the following steps: dissolving aripiprazole in an acidifier, acquiring a medicament-having acid solution; adding an alkalizer while stirring, then adding water or aqueous ethanol 10 to 60 wt % while stirring, and separating by precipitation the aripiprazole type I microcrystal. Furthermore, a method for preparing a solid preparation having the aripiprazole type I microcrystal, an aripiprazole microcrystal having an average particle size of less than 20 ?m, and a solid preparation having the microcrystal. The method for preparing the aripiprazole type I microcrystal allows reduced pollution and loss, great safety, easy and convenient, reduced use of organic solvents, obviated need for demanding process conditions (such as cooling condition) and apparatus, low cost, and facilitated applicability in industrialized manufacturing.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: July 7, 2015
    Assignees: SHANGHAI ZHONGXI PHARMACEUTICAL CORPORATION, SHANGHAI ZHONGXI SUNVE PHARMACEUTICAL CO., LTD.
    Inventors: Siji Zheng, Bo Tan, Linyong Fu, Xiaoyi Liu, Shaoqing Yuan, Zhihui Cao
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Publication number: 20150148330
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Patent number: 9040021
    Abstract: Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.
    Type: Grant
    Filed: November 7, 2011
    Date of Patent: May 26, 2015
    Assignee: GE Healthcare Limited
    Inventors: Clare Jones, Amanda Ewan, Duncan Wynn, Alessandra Gaeta, James Nairne
  • Publication number: 20150141424
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 21, 2015
    Inventors: Qingping ZENG, Andras TORO, John Bruce PATTERSON, Warren Stanfield WADE, Zoltan ZUBOVICS, Yun YANG, Zhipeng WU
  • Publication number: 20150141409
    Abstract: Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.
    Type: Application
    Filed: June 26, 2013
    Publication date: May 21, 2015
    Inventors: Eui Hwan Cho, Sung Ju Choi, Sung Woo Lee, Hee Jong Shin, Ho Seok Kwon, Jae Woong Lee, Jeong Ho Joo, Hyun Tae Kim, Woo Heon Song, Jong Bae Yoon, Ki Seok Park, Ho Joon Park, Ho Tae Nam
  • Publication number: 20150139916
    Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Fabio RANCATI, Ian Linney, Chris Knight, Wolfgang Schmidt
  • Patent number: 9034877
    Abstract: A precursor for the deposition of a thin film by atomic layer deposition is provided. The compound has the formula MxLy where M is a metal and L is an amidrazone-derived ligand or an amidate-derived ligand. A process of forming a thin film using the precursors is also provided.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: May 19, 2015
    Assignee: Wayne State University
    Inventor: Aloke K. Dutta
  • Publication number: 20150133449
    Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
  • Publication number: 20150133427
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: October 15, 2014
    Publication date: May 14, 2015
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Publication number: 20150111870
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 23, 2015
    Applicant: JOHNSON & JOHNSON
    Inventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE, MAXWELL D. CUMMINGS, KELLY MCCLURE, VIRGINIA TANIS
  • Publication number: 20150105337
    Abstract: The present invention provides novel enterobactin-cargo conjugates, such as compounds of Formula (I), and salts thereof, where X is the cargo and may be an antibiotic, a fluorophore, or biotin. The present invention also provides complexes, compositions, kits, and methods that involve the compounds of Formula (I) and are useful in delivering a cargo to a bacterium, treating a bacterial infection, cystic fibrosis, and/or inflammatory bowel disease in a subject, preventing a bacterial infection, cystic fibrosis, and/or inflammatory bowel disease in a subject, inhibiting the growth of or killing a bacterium, or determining the concentration of a bacterium in a biological sample. In certain embodiments, the bacterium is a Gram-negative bacterium.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 16, 2015
    Applicant: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Elizabeth Marie Nolan, Tengfei Zheng, Phoom Chairatana
  • Publication number: 20150105376
    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 endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Patent number: 9006248
    Abstract: The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: April 14, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Shaun Jordan, Tetsuro Kikuchi, Katsura Tottori, Tsuyoshi Hirose, Yasufumi Uwahodo
  • Publication number: 20150099732
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
    Type: Application
    Filed: March 7, 2013
    Publication date: April 9, 2015
    Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliot, Dan Niculescu-Duvaz, Roderick Porter, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Ashley Nicholas Jarvis, Trevor Robert Perrior, Rebekah Elisabeth Key
  • Patent number: 8999982
    Abstract: The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: April 7, 2015
    Assignees: Lead Discovery Center GmbH, Max-Planck-Gesellschaft zur Förderung der Wissenschaften E.V.
    Inventors: Carsten Schultz-Fademrecht, Bert Klebl, Axel Choidas, Uwe Koch, Jan Eickhoff, Alexander Wolf, Axel Ullrich
  • Patent number: 8999991
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Harry R. Chobanian
  • Patent number: 9000165
    Abstract: The present invention relates to a process for preparation of aripiprazole crystal form II by recrystallizing aripiprazole in a mixture of acetone and 1-methoxy-2-propanol or a single solvent of 1-methoxy-2-propanol. The simple process according to the present invention can produce aripiprazole crystal form II with high purity and high yield in a mass scale.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: April 7, 2015
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Soo Jin Choi, Seong Soo Oh, Yong Suk Jin, Yong Tae Kim, Seung Jae Lee, Jeong Hyun Son
  • Patent number: 8999990
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
  • Patent number: 8993554
    Abstract: Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: March 31, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Jonathan Thomas Seal
  • Patent number: 8993761
    Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: March 31, 2015
    Assignee: Otsuka Pharamceutical Co. Ltd.
    Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
  • Publication number: 20150087886
    Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-1) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers.
    Type: Application
    Filed: October 9, 2014
    Publication date: March 26, 2015
    Inventors: Robert Hromas, Andrei Leitao, Tudor I. Oprea, Larry A. Sklar, Elizabeth A. Williamson, Justin Wray, Wei Wang
  • Publication number: 20150087655
    Abstract: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases. The present invention provides a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof, and a process for producing the same.
    Type: Application
    Filed: April 23, 2013
    Publication date: March 26, 2015
    Inventors: Hiroshi Yamashita, Tetsuya Sato, Takuya Minowa, Yusuke Hoshika, Hidekazu Toyofuku, Tatsuya Yamaguchi, Masahiro Sota, Shuuji Kawano, Takayuki Nakamura, Ryohei Eto, Takuma Ikebuchi, Kei Moriyama, Nobuaki Ito
  • Patent number: 8987448
    Abstract: The present technology provides methods of making anhydrous crystalline Form II and monohydrate crystalline Form B of the lactic acid salt of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one.
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: March 24, 2015
    Assignee: Novartis AG
    Inventors: Arnaud Grandeury, Christian Riegert, Andreas Schreiner
  • Publication number: 20150080365
    Abstract: This invention relates to certain heteroaryl compounds for use as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of helminth infections and the treatment of parasitosis caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 19, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Publication number: 20150080364
    Abstract: Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 19, 2015
    Applicants: Abide Therapeutics, Inc., The Scripps Research Insititute
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Dong-Hui Wang, Olivia Weber, Benjamin F. Cravatt, Micah J. Niphakis, Armand Cognetta, Jae Won Chang
  • Publication number: 20150072974
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 12, 2015
    Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
  • Publication number: 20150065480
    Abstract: The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.
    Type: Application
    Filed: April 13, 2012
    Publication date: March 5, 2015
    Applicant: INNOVIMMUNE BIOTHERAPEUTICS, INC.
    Inventors: Anderson Gaweco, John Walker, Joseph B. Monahan, Jerry W. Cubbage, Jeffery Carroll
  • Publication number: 20150065711
    Abstract: Disclosed are linear discrete PEG constructs, which can be created and produced in a precise and reproducible way. Key to being able to do these things, where x in the discrete PEGx can vary from about 2 to about 64, is that the processes used to make each linear portion is controlled to give essentially one oligomer/one compound. Having a variable length linear discrete PEG construct that is (a) primarily an linear discrete PEG construct with diagnostic or therapeutic groups attached along a chain of attachment cores, which is attached to a preferential locator; (b) is an m-discrete PEG as the terminal construct on the linear portion, and “hidden”; (c or linear discrete PEG with a terminus group that can be either negatively or positively charged, or neutral; and any of the discrete PEG portions can be designed to be cleaved after entering the cell.
    Type: Application
    Filed: August 15, 2014
    Publication date: March 5, 2015
    Applicant: EquIP, LLC
    Inventor: Paul D. Davis
  • Patent number: 8962607
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: February 24, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J Connolly, Christopher Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark M McDonnell, Philip M Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Publication number: 20150051189
    Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Application
    Filed: January 23, 2013
    Publication date: February 19, 2015
    Inventors: Thierry Le Diguarher, Patrick Casara, Jérôme-Benoît Starck, Jean-Michel Henlin, James Edward Paul Davidson, James Brooke Murray, Christopher John Graham, I-Jen Chen, Olivier Geneste, John Hickman, Stéphane Depil, Arnaud Le Tiran, Miklos Nyerges, Guillaume De Nanteuil
  • Patent number: 8957075
    Abstract: The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: February 17, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Suzanne Walker Kahne, Michael Block Lazarus, Benjamin J. Gross
  • Publication number: 20150045356
    Abstract: Provided is a superior, novel heterocyclic compound with improved solubility in oil such as sesame oil and benzyl benzoate, which has a broader treatment spectrum, causes less side effects, and is superior in tolerability and safety, and use thereof. A heterocyclic compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: September 7, 2012
    Publication date: February 12, 2015
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Yamashita, Yohji Sakurai, Motoyuki Miyamoto, Yuichi Nakamura, Hideaki Kuroda, Takuya Minowa
  • Publication number: 20150038493
    Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 5, 2015
    Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
  • Publication number: 20150031673
    Abstract: Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Application
    Filed: July 21, 2014
    Publication date: January 29, 2015
    Inventors: Arnaud LE TIRAN, Thierry LE DIGUARHER, Jérôme-Benoît STARCK, Jean-Michel HENLIN, Anne-Françoise GUILLOUZIC, Guillaume DE NANTEUIL, Olivier GENESTE, Imre FEJES, Janos TATAI, Miklos NYERGES, James Edward Paul DAVIDSON, James Brooke MURRAY, I-Jen CHEN, Didier DURAND
  • Publication number: 20150025085
    Abstract: 8-Hydroxy-quinoline derivatives and 8-ethers, 8-esters, 8-carbonates, 8-acyloxymethyl, 8-phosphates, 8(phosphoryloxy)methyl, and 8-carbamates derivatives thereof substituted at the 5-position are described as useful for iron chelation and neuroprotective therapies.
    Type: Application
    Filed: January 30, 2013
    Publication date: January 22, 2015
    Inventors: Vincent R. Zurawski, JR., Theodore J. Nitz
  • Publication number: 20150018366
    Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.
    Type: Application
    Filed: September 26, 2014
    Publication date: January 15, 2015
    Inventor: Laykea TAFESSE
  • Publication number: 20150018335
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 7, 2013
    Publication date: January 15, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150018352
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 15, 2015
    Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
  • Publication number: 20150018333
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha ABEYWARDANE, John BROADWATER, Hidenori TAKAHASHI
  • Patent number: 8933016
    Abstract: It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide (“AMP”) and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: January 13, 2015
    Assignee: MetalloPharm, LLC
    Inventors: James A. Cowan, Ada S. Cowan
  • Publication number: 20150011551
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Applicant: Sanford- Burnham Medical Reseach Institute
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
  • Publication number: 20150011562
    Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R10 and X have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 8, 2015
    Inventors: Henry Yu, Thomas E. Richardson, Pandi Bharathi, Brian H. Heasley, Matthew G. Jenks, Robert J. Foglesong