Hetero Ring In The Polycyclo Ring System Patents (Class 546/196)
  • Patent number: 9034219
    Abstract: Described herein are compounds generally comprising an indeno[2?,3?:3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: May 19, 2015
    Assignee: Transitions Optical, Inc.
    Inventors: Meng He, Darrin R. Dabideen, Xiao-Man Dai, Wenjing Xiao, Ruisong Xu, Sujit Mondal, Anil Kumar, Anu Chopra
  • Patent number: 9028728
    Abstract: The present invention relates to photochromic materials that include one or more indeno-fused naphthopyrans that have particular groups at the 7, 11, and 13 positions thereof, and at the position alpha to the oxygen of the pyran ring thereof. With some embodiments, hydrogen or an alkoxy group is bonded to the 7 position, an optionally substituted phenyl is bonded to the 11 position, two alkyl groups are bonded to the 13 position, and two optionally substituted phenyl groups are bonded to the position alpha to the oxygen of the pyran ring of the indeno-fused naphthopyran compound. The 13 position of the indeno-fused naphthopyrans is free of ether groups in which an ether oxygen is bonded to the 13 position, and hydroxyl. The present invention also relates to photochromic articles and compositions that include such indeno-fused naphthopyrans.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: May 12, 2015
    Assignee: Transitions Optical, Inc.
    Inventors: Kevin E. Bancroft, Anu Chopra, Xiao-Man Dai, Beon-Kyu Kim, David B. Knowles, Jason R. Lewis, Victor A. Montes, Stephen D. Straight, Massimiliano Tomasulo, Barry Van Gemert, Robert W. Walters, Wenjing Xiao, Huayun Yu, Elizabeth A. Zezinka
  • Publication number: 20150126552
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-aminated methylene or 2-esterified methylene tanshinone I derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments. When X is nitrogen, formula I indicates 2-aminated methylene tanshinone I; when X is oxygen, formula I indicates 2-esterified methylene tanshinone I.
    Type: Application
    Filed: November 30, 2012
    Publication date: May 7, 2015
    Applicant: Hangzhou Bensheng Pharmaceutical Co., Ltd.
    Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
  • Patent number: 9018213
    Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: April 28, 2015
    Assignees: Huazhong University of Science & Technology, NHWA Pharma. Corporation
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Minquan Yu, Yinli Qiu
  • Publication number: 20150111888
    Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
  • Patent number: 8981131
    Abstract: The present invention provides compounds represented by formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: March 17, 2015
    Assignee: Piramal Enterprises Limited
    Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
  • Patent number: 8969345
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: March 3, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Patent number: 8946265
    Abstract: The present invention relates to improved processes for preparing 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (I) (lenalidomide) and its intermediate 3-(1-oxo-4-nitro-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to improved processes for preparing lenalidomide crystalline form A, use of said crystalline form A as an active pharmaceutical ingredient or as an intermediate in the preparation of further crystalline or amorphous forms of lenalidomide, compositions comprising lenalidomide crystalline form A and their use in the treatment of disease.
    Type: Grant
    Filed: March 1, 2010
    Date of Patent: February 3, 2015
    Assignee: Generics [UK] Limited
    Inventors: Vinayak Govind Gore, Vinay Kumar Shukla, Shreyas Shrikant Bhandari, Suresh Hasbe
  • Patent number: 8940726
    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: Grant
    Filed: December 20, 2013
    Date of Patent: January 27, 2015
    Assignee: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Publication number: 20150024935
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols RA1, RA2, X, Y, L1, L2, RB1, RB2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Thomas Seitz, Stefan Hillebrand, Jürgen Benting, Jan Peter Schmidt, Pierre Cristau
  • Publication number: 20150018542
    Abstract: Provided in the present invention are a 2-arylbenzofuran-7-formamide compound as shown in general formula I or a pharmacologically or physiologically acceptable salt thereof, a preparation method thereof and use thereof in preparing anti-tumour drugs, wherein R1 and R2 are each independently hydrogen, straight or branched chained C1-C4 alkyl, C3-C4 cycloalkyl or saturated 5- or 6-membered heterocyclyl containing oxygen or nitrogen; or R1 and R2 together with N form an unsubstituted or substituted saturated 5- or 6-membered heterocyclyl containing at least one heteroatom, wherein the heteroatom is O, N and S, the substituent is a methyl on N; R3 is a hydrogen atom or a chlorine atom; R4 is a hydrogen atom or a fluorine atom; X is CH, CF or N; and Y is CH, CF or N.
    Type: Application
    Filed: January 14, 2013
    Publication date: January 15, 2015
    Inventors: Chunhao Yang, Zehong Miao, Jian Ding, Meng Wang, Jinxue He, Cun Tan, Yi Chen
  • Patent number: 8933100
    Abstract: A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: wherein R1 is a hydrogen atom or C1-6 alkyl group.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: January 13, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Keigo Tanaka, Tomoki Nishioka
  • Publication number: 20150011557
    Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 8, 2015
    Applicant: Merck Patent GmbH
    Inventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
  • Publication number: 20150011541
    Abstract: The present invention relates to compounds having a pipecolate sulfonamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate sulfonamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
    Type: Application
    Filed: December 28, 2012
    Publication date: January 8, 2015
    Inventors: Ranganath Gopalakrishnan, Felix Hausch
  • Patent number: 8927544
    Abstract: The present invention relates to benzofuran-2-sulfonamide derivatives with the following formula: or pharmaceutically acceptable salts thereof. The derivatives are useful as modulators of chemokine receptors.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: January 6, 2015
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20150005282
    Abstract: Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutic agents, especially the GPR40 agonist and in preparation of drugs for treating diseases such as diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.
    Type: Application
    Filed: December 27, 2012
    Publication date: January 1, 2015
    Inventors: Fanglong Yang, Qing Dong, Jihui Han, Chunfei Wang, Ling Zhang, Yang Wang
  • Publication number: 20150005286
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: December 14, 2012
    Publication date: January 1, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Johnny Y. Nagasawa, Andiliy G. Lai, Celine Bonnefous
  • Patent number: 8921568
    Abstract: Iminosugar compounds are described that have inbuilt delivery features by virtue of covalent incorporation of a tocopherol moiety, or alternative moieties that are analogs of tocopherol or select analogs of cholesterol, or its antagonist “Ezitimibe”; and are likely to have broad spectrum antiviral activity. The compounds differ from previous iminosugar compounds, even lipophillic ones, being more hydrophobic and resembling fats and oils in their partition behavior in vivo into lipid phases of lipoproteins, cellular lipid droplet organelles and biological membranes. These features confer a number of unique delivery attributes in vivo, favorable to the therapy of virus infections involving cells of the lymphoid system and the liver, in particular, but these features are also favorable in general for the treatment of virus infections of man and animals.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: December 30, 2014
    Assignees: Unither Virology, LLC, The Chancellor, Masters and Scholars of The University of Oxford
    Inventors: J. L. Kiappes, Peter Laing, Raymond Dwek, Nicole Zitzmann, Stephanie Pollock
  • Patent number: 8921397
    Abstract: The present invention is concerned with novel selective dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein R1, R2, R3, n, and Y are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: December 30, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Publication number: 20140371207
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Application
    Filed: December 13, 2013
    Publication date: December 18, 2014
    Applicants: Kyowa Hakko Kirin Co., Ltd., Millennium Pharmaceuticals, Inc.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C.B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Publication number: 20140364433
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
  • Publication number: 20140364432
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
  • Patent number: 8906900
    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: Grant
    Filed: December 20, 2013
    Date of Patent: December 9, 2014
    Assignee: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Publication number: 20140356417
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: June 12, 2014
    Publication date: December 4, 2014
    Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20140349991
    Abstract: Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 27, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Katsuhiro Kawakami, Toshihiro Kiho, Atsushi Tengeiji, Kentoku Gotanda, Kazumasa Aoki, Kazuki Yano
  • Publication number: 20140349987
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 8889716
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 18, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
  • Publication number: 20140335157
    Abstract: The present invention relates to a compound represented by the formula (1) wherein Xa and Xb are each independently X1 or X2; s is 1 or 2, R4 is an alkyl group having 1-6 carbon atoms, na and nb are each independently 0 or 1, R1a and R1b are each independently an alkylene group having 1-6 carbon atoms, R2a and R2b are each independently an alkylene group having 1-6 carbon atoms, Ya and Yb are each independently an ester bond, an amide bond, a carbamate bond, an ether bond or a urea bond, and R3a and R3b are each independently a sterol residue, a liposoluble vitamin residue or an aliphatic hydrocarbon group having 12-22 carbon atoms, and use thereof.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 13, 2014
    Inventors: Kota TANGE, Masaya ARAI, Kazuhiro KUBO, Hidetaka AKITA, Hideyoshi HARASHIMA, Hiroto HATAKEYAMA, Ryohei ISHIBA, Masami UKAWA, Hiroki TANAKA
  • Publication number: 20140329857
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: July 18, 2014
    Publication date: November 6, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Patent number: 8877778
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: November 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Patent number: 8853239
    Abstract: The present invention relates to compounds of formula I, wherein R1, LP, LQ, X, A, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: October 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf
  • Publication number: 20140296232
    Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicants: Massachusetts General Hospital, The Broad Institute, Inc.
    Inventors: Deborah Hung, Sarah Stanley, Tomohiko Kawate, Noriakie Iwase, Motohisa Shimizu
  • Publication number: 20140288106
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Applicant: Sanofi
    Inventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
  • Publication number: 20140275020
    Abstract: This invention relates to compounds of Formula I having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato
  • Patent number: 8815907
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: August 26, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Publication number: 20140225049
    Abstract: The present invention provides ophthalmic devices comprising at least one photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic materials. Other non-limiting embodiments relate to methods of making the ophthalmic devices comprising photochromic materials.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 14, 2014
    Applicant: Johnson & Johnson Vision Care, Inc.
    Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, JR., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
  • Publication number: 20140221349
    Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: February 3, 2014
    Publication date: August 7, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Matthias ECKHARDT
  • Patent number: 8790691
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: July 29, 2014
    Assignee: The University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20140206722
    Abstract: Disclosed herein are compositions and methods for treating depression using compositions comprising a compound of formula I. Disclosed herein are compositions and methods for treating depression using compositions comprising phenoxypropylamine compounds and derivatives having selective affinity for and antagonistic activity against the 5-HT1A receptor, as well as 5-HT reuptake inhibitory activity. In addition, compositions and methods for treating depression using compositions comprising a compound of formula II are disclosed. Methods of treating or diminishing at least one symptom of depression in a human subject with a composition comprising a compound of the formula (I) or formula (II), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, are also disclosed.
    Type: Application
    Filed: January 24, 2014
    Publication date: July 24, 2014
    Applicant: MINERVA NEUROSCIENCES, INC.
    Inventors: Lorenzo Pellegrini, Argeris Karabelas, Remy Luthringer
  • Publication number: 20140205688
    Abstract: The present invention relates to a stimulating agent comprising a pungent component having astringency, a stimulating composition including the agent, as well as a flavor or fragrance composition, a food, a drink, an oral care product and an external skin preparation containing the agent or the composition, and also relates to the use of a pungent component having astringency as a stimulating agent. Examples of the pungent component having astringency include a plant extract of Asteraceae Spilanthes, Rutaceae Zanthoxyium, Rutaceae Fagara, or Piperaceae Piper, or an amide derivative represented by general formula (1) (where R1 represents an alkenyl group having 2 to 12 carbon atoms which may be substituted by a methylenedioxyphenyl at the end, R2 and R3 may be the same or different from each other and each are a hydrogen atom or a lower alkyl group in which a hydroxyl group may be substituted, and R2 and R3, together with the nitrogen atom adjacent thereto, may form a heterocyclic ring).
    Type: Application
    Filed: May 29, 2012
    Publication date: July 24, 2014
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Kaori Takahashi, Miyuki Takayanagi
  • Publication number: 20140197361
    Abstract: A naphthopyran compound represented by the formula B1 and B2 are selected independently from the group consisting of a phenyl, naphthyl, or heterocyclic aromatic group, or may combine to form one or more aromatic rings. B1 and B2 may further include one or more substituents. R3, R4, R5, R6, and R16 are selected independently from the group consisting of hydrogen, halogen, —Ra, —OH, —ORa, —O—CO—Ra, —CN, —NO2, —SO2Ra, —SORa, —SH, —SRa, —NH2, —NHRa, —NRaRa, or —NRbRc; or wherein R5 and R6 combine to form a cyclic group. Ra may include an alkyl, polycycloalkyl, alkenyl, polyalkenyl, haloalkyl, perhaloalkyl, alkynyl, polyalkynyl, hydroxyalkynyl, polyhydroxyalkynyl; or (C3-20)cycloalkyl group. Rb and Rc may include hydrogen or alkyl groups, or may combine to form a saturated heterocyclic group, or together with an adjacent phenyl group may form a julolidinyl group. R7 is a mesogenic group.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Applicant: AlphaMicron Incorporated
    Inventors: Ludmila Sukhomlinova, Linli Su, Tamas Kosa, Bahman Taheri
  • Patent number: 8778970
    Abstract: Provided is a new serotonin-reuptake inhibitor that exhibits affinity for serotonin-1A receptors. Said serotonin-reuptake inhibitor is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. In the formula, R1 represents a hydrogen atom, a 2-hydroxyethyl group, or a 2-methoxyethyl group. R2 represents one of the following bonded to a methylene group which is bonded to a piperidine ring: a chlorine atom bonded in a p-position; a bromine atom bonded in a p-position; a methyl group bonded in a p-position; a chlorine atom bonded in an m-position; or a bromine atom bonded in an m-position. Either Y1 represents a hydrogen atom and Y2 represents a hydrogen atom or a hydroxyl group, or Y1 and Y2 together represent an oxo group. Z represents a group represented by one of the following formulas: formula (3-1-1), formula (3-1-2), formula (3-2-1), formula (3-2-2), formula (3-3-1), formula (3-3-2), formula (3-4-1), or formula (3-4-2).
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: July 15, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd
    Inventors: Tomohiro Toyoda, Tomoaki Nishida, Hidefumi Yoshinaga
  • Patent number: 8778926
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, X1, X2, X3, A, n and m are as defined in the application. The compounds of formula I have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: July 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf, Bernd Nosse
  • Publication number: 20140166948
    Abstract: The present invention relates to compounds represented by the following Formula (II), Ring-A of Formula II can be, for example, an aryl group, and Q? and Q?? can each be independently selected from groups, such as, halogen, —OH, —CN, amine groups, amide groups, carboxylic acid ester groups, carboxylic acid groups, alkenyl groups, alkynyl groups, carbonate groups, sulfide groups, and sulfonic acid ester groups. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds such as represented by Formula II.
    Type: Application
    Filed: February 19, 2014
    Publication date: June 19, 2014
    Inventors: Meng He, Anil Kumar, Darrin R. Dabideen
  • Publication number: 20140171442
    Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.
    Type: Application
    Filed: July 31, 2012
    Publication date: June 19, 2014
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Miquan Yu, Yinli Qiu
  • Publication number: 20140161729
    Abstract: The present invention is directed to method of using a collection of monomers capable of forming multimers as a fluorescence reporter in different applications such as ligand detection/screening, disease diagnosis, drug discovery or screening, fluorescent labeling and imaging, or other fluorescent methodologies. Each monomer in the collection includes one or more ligand elements useful for binding to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the ligand elements directly or indirectly through a connector. Association of linker elements of different combinations of monomers, with their ligand elements bound to the target molecule to form a multimer, will generate a unique fluorescent signature different from that produced by those monomers either alone or in association with each other in the absence of the target molecule, when subjected to electromagnetic excitement.
    Type: Application
    Filed: April 9, 2012
    Publication date: June 12, 2014
    Applicant: CORNELL UNIVERSITY
    Inventors: Francis Barany, Maneesh Pingle, Donald E. Bergstrom, Sarah F. Giardina, Lee Daniel Arnold
  • Patent number: 8741188
    Abstract: The present invention provides ophthalmic devices comprising at least one photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic materials. Other non-limiting embodiments relate to methods of making the ophthalmic devices comprising photochromic materials.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: June 3, 2014
    Assignee: Johnson & Johnson Vision Care, Inc.
    Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, Jr., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
  • Publication number: 20140135298
    Abstract: This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for treating cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EGFR, including EGFR-related cancers, particularly for expanding the efficacy of drugs previously developed for this purpose, and for methods of treatments using the compounds for this purpose.
    Type: Application
    Filed: March 16, 2012
    Publication date: May 15, 2014
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Alan Berezov, Mark I. Greene, Natalie Minkovsky, Zheng Cai, Hongtao Zhang
  • Publication number: 20140114048
    Abstract: Dark quencher constructs, termed “multi-chromophoric quenchers” are described herein that comprise at least two dark quenching moieties, which can be the same or different, linked together by at least one multivalent linking moiety. The structure of the multi-chromophoric quenchers can be varied to selectively enhance quenching within a specific range of reporter emission wavelengths, to quench a broader range of reporter emission wavelengths than previously possible, or can combine both concepts. Multiple types of quenching moieties can be employed to increase the absorption range and a multiple number of each type of quenching moiety can be used to increase the total absorptivity within the absorption range. The multi-chromophoric quenchers can be tethered to probes for biomolecules, insoluble supports and/or fluorescent dyes for use in a wide variety of biomolecular assays.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 24, 2014
    Applicant: Applied Biosystems, LLC
    Inventors: Scott BENSON, Steven MENCHEN, Krishna UPADHYA