Additional Polycyclo Heterocyclic Ring System Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 548/454)
  • Patent number: 10407397
    Abstract: A method for producing an aromatic dianhydride includes reacting an aromatic diimide with a substituted or unsubstituted phthalic anhydride in an aqueous medium in the presence of an amine exchange catalyst to provide an aqueous reaction mixture including an N-substituted phthalimide, an aromatic tetraacid salt, and at least one of an aromatic triacid salt and an aromatic imide diacid salt. The method further includes removing the phthalimide from the aqueous reaction mixture by extracting the aqueous reaction mixture with an organic solvent for a first time period, at a first extraction temperature and subsequent to the first time period, extracting the aqueous reaction mixture with an organic solvent for a second time period, at a second extraction temperature. The aromatic tetraacid salt is converted to the corresponding aromatic dianhydride. Aromatic dianhydrides prepared according to the method are also described.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: September 10, 2019
    Assignee: SABIC GLOBAL TECHNOLOGIES B.V.
    Inventors: Aaron Royer, Robert J. Werling, Jorge Jimenez, Norman Enoch Johnson
  • Patent number: 9182350
    Abstract: The present invention provides a novel category of naphthalene-based two-photon fluorescent probes having a general formula I, wherein: X is selected from the X1, X2, X3 and X4; The mentioned two-photon fluorescent probes have a low fluorescence background in the non-tumor cells and tissues, and have a strong and specific fluorescent signal in the tumor cells and tissues. These probes have a certain level of water-solubility, while having good membrane permeability. In addition, they have a bigger effective two-photon absorption cross section. The compounds of the present invention also have a lower biotoxicity, phototoxicity and photobleaching. There is sufficient difference between the spectral range thereof and that of a biological sample.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: November 10, 2015
    Assignees: DALIAN UNIVERSITY OF TECHNOLOGY, DALIAN CHROMAS BIOSCIENCE CO., LTD.
    Inventors: Xiaojun Peng, Hua Zhang, Jiangli Fan, Jingyun Wang
  • Patent number: 9035072
    Abstract: The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: May 19, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Daniel T. Belmont, Cristian Harrison, Robert Michael Hughes, Young Chun Jung, Elaine Chungmin Lee, Benjamin Joseph Littler, Peter Jamison Rose, David Andrew Siesel, Gerald J. Tanoury
  • Publication number: 20150133659
    Abstract: The present invention relates to millepachine ((E)-1-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-(4-methoxyphenyl)prop-2-en-1-one) and its analogues. The present invention provides methods for preparing these compounds, pharmaceutical compositions including these compounds, and methods of treating diseases utilizing pharmaceutical compositions including these compounds.
    Type: Application
    Filed: May 25, 2012
    Publication date: May 14, 2015
    Applicant: Sichuan University
    Inventors: Lijuan Chen, Yuquan Wei
  • Publication number: 20150119441
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: November 4, 2014
    Publication date: April 30, 2015
    Inventors: Sara S. Hadida Ruah, Peter D.J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Publication number: 20150111890
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 23, 2015
    Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
  • Publication number: 20150094330
    Abstract: The invention provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.
    Type: Application
    Filed: September 26, 2014
    Publication date: April 2, 2015
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 8987473
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Sato Pharmaceutical Co., Ltd.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Patent number: 8969592
    Abstract: Novel heterocyclic materials are disclosed. The materials contain a fused tetracyclic structure that can improve the properties of OLED devices when the novel heterocyclic materials are incorporated into such devices.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: March 3, 2015
    Assignee: Universal Display Corporation
    Inventor: Bin Ma
  • Publication number: 20150051257
    Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and
    Type: Application
    Filed: March 20, 2013
    Publication date: February 19, 2015
    Applicant: ADAMED SP. ZO.O
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
  • Publication number: 20150045404
    Abstract: The invention provides a compound of formula (I): wherein R1-R5 have any of the values defined in the specification. The compounds are useful for the treatment of cancer and other diseases.
    Type: Application
    Filed: March 25, 2013
    Publication date: February 12, 2015
    Inventors: John Kodet, Jeffrey D. Neighbors, David F. Wiemer
  • Publication number: 20150045282
    Abstract: Suppository, hot melt and ophthalmic formulations containing amino esters of the formulae (I), (II) and (III), where R1, R2 and R3 are residues of amino acids such as, but not limited to, valine, sarcosine, leucine, glutamine, tryptophan, tyrosine, alanine and 4(4-aminophenyl)butyric acid or combination thereof, and salts thereof.
    Type: Application
    Filed: August 18, 2014
    Publication date: February 12, 2015
    Inventors: Mahmoud A. ELSOHLY, Waseem GUL, Michael A. REPKA, Soumyajit MAJUMDAR, Mohammad Khalid ASHFAQ
  • Patent number: 8927971
    Abstract: Disclosed are semiconducting compounds having one or more phthalimide units and/or one or more head-to-head (H-H) substituted biheteroaryl units. Such compounds can be monomeric, oligomeric, or polymeric, and can exhibit desirable electronic properties and possess processing advantages including solution?processability and/or good stability at ambient conditions.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: January 6, 2015
    Assignee: University of Kentucky Research Foundation
    Inventor: Mark D. Watson
  • Publication number: 20140374722
    Abstract: A compound represented by Formula 1. An organic electric element includes a first electrode, a second electrode, and an organic material layer including the compound of Formula 1. The organic material layer include a light emitting layer, a hole transport layer including a compound represented by Formula 2, and an emission-auxiliary layer including the compound represented by Formula 1. When the organic electric element includes the compound in the organic material layer, luminous efficiency, color purity, and life span can be improved.
    Type: Application
    Filed: January 14, 2013
    Publication date: December 25, 2014
    Inventors: Dongha Kim, Sunhee Lee, Yeonhee Choi, Soungyun Mun, Jungcheol Park, Yongwook Park, Heesun Ji, Junghwan Park, Bumsung Lee, Sunpil Hwang
  • Patent number: 8912199
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: December 16, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Publication number: 20140361259
    Abstract: An arylamine-based compound is represented by Formula 1 below. The arylamine-based compound is included in an organic light emitting diode.
    Type: Application
    Filed: October 23, 2013
    Publication date: December 11, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
  • Publication number: 20140343065
    Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Riccardo GIOVANNINI, Yunhai CUI, Henri DOODS, Marco FERRARA, Stefan JUST, Raimund KUELZER, Iain LINGARD, Rocco MAZZAFERRO, Klaus RUDOLF
  • Patent number: 8865130
    Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: October 21, 2014
    Assignee: Vanderbilt University
    Inventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
  • Publication number: 20140275114
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides of formula 1 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: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ralf ANDERSKEWITZ, Marc GRUNDL, Gerd MORSCHHAEUSER, Thorsten OOST, Alexander PAUTSCH
  • Publication number: 20140256725
    Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: September 11, 2014
    Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Matthijs Poulie, Cornelis Marius Timmers, Saskia Vertaik
  • Publication number: 20140234238
    Abstract: The invention relates to specific benzodioxepin-3-one compounds, to a process for the preparation thereof and to the use thereof as dyes or as fluorescent emitters for organic electroluminescent devices (OLEDs) or for organic light-emitting electrochemical cells (OLECs), and to corresponding electronic devices.
    Type: Application
    Filed: September 17, 2012
    Publication date: August 21, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Thomas Rudolph, Philipp Buehle, Ralf Rosskopf
  • Patent number: 8802868
    Abstract: The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: August 12, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ali Keshavarz-Shokri, Beili Zhang, Tim Edward Alcacio, Elaine Chungmin Lee, Yuegang Zhang, Mariusz Krawiec
  • Publication number: 20140179735
    Abstract: A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of Mycobacterium protein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed in Mycobacterium tuberculosis and characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.
    Type: Application
    Filed: April 25, 2012
    Publication date: June 26, 2014
    Inventors: Zhong-Yin Zhang, Yantao He, Li-Fan Zeng
  • Publication number: 20140179750
    Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.
    Type: Application
    Filed: June 19, 2012
    Publication date: June 26, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Jianxiong Jiang, Thota Ganesh, Yuhong Du, Pahk Thepchatri, Yi Quan, Ray J. Dingledine
  • Publication number: 20140165223
    Abstract: Described are methods and compositions for inhibiting the trimerization of ligands belonging to the TNF superfamily, in particular, inhibiting RANKL trimerization. Accordingly, the methods and compositions provided herein can be used to treat disorders associated with increased RANK signaling, in particular those related to bone loss. Compounds that inhibit trimerization of ligands belonging to the TNF superfamily are also described.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Applicant: B.S.R.C. "Alexander Fleming"
    Inventors: Eleni Ntouni, Georgios Kollias
  • Publication number: 20140114068
    Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: April 24, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
  • Patent number: 8692001
    Abstract: The invention relates to sulfonamide compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.
    Type: Grant
    Filed: October 26, 2011
    Date of Patent: April 8, 2014
    Assignee: Dynamix Pharmaceuticals Ltd.
    Inventors: Oren M. Becker, Alina Shitrit, Nili Schutz, Efrat Ben-Zeev, Avihai Yacovan, Rachel Ozeri, Tzofit Kehat, Sima Mirilashvili, Alex Aizikovich, Daniel Sherman, Vered Behar, Osnat Kashtan
  • Publication number: 20140094493
    Abstract: A compound of Formula (I), and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein R1 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alkyl, C1-4alkoxy, CONH2 (optionally mono- or di-substituted by C1-4alkyl) and SO2NH2, R2 is independently selected from C1-6allkyl substituted by R3 wherein the C1-6alkyl chain optionally comprises one or two heteroatoms select from O; R3 is selected from aryl, C3-6cycloalkyl, C3-6heterocyclyl and C3-6heteroaryl, wherein the heterocyclyl and heteroaryl rings are nitrogen containing; and wherein R3 is optonally substituted by one or more groups selected from R1; n1 is zero or an integer from 1 to 2; n2 is an integer from 1 to 2; and the sum of n1 and 2 is less than or equal to 2; R5 is selected from any group defined for R1 and R2; R6a and R6b are independently selected from H or C1-4alkyl; R7 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4al
    Type: Application
    Filed: February 6, 2012
    Publication date: April 3, 2014
    Inventors: Jillian G. Baker, Peter M. Fischer, Christophe Fromont, Sheila M. Gardiner, Stephen J. Hill, Gopal Jadhav, Barrie Kellam, Shailesh Mistry, Jeanette Woolard
  • Publication number: 20140080826
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: September 25, 2013
    Publication date: March 20, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: SARA SABINA HADIDA RUAH, Peter Diederik Jan Grootenhuis, Frederick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason Mc Cartney, Mehdi Numa, Xiaoqing Yang
  • Publication number: 20140057906
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 27, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara S. Hadida Ruah, Peter D.J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Publication number: 20140024657
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Junying YUAN, Emily S. Hsu
  • Publication number: 20140005221
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Application
    Filed: January 30, 2012
    Publication date: January 2, 2014
    Applicant: SATO PHARMACEUTICAL CO., LTD.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Publication number: 20130331568
    Abstract: The invention provides compounds of formula I wherein n, A, R, R?, R?, R0, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 12, 2013
    Applicant: Novartis AG
    Inventors: Fabrizio Gasparini, Yves Auberson, Silvio Ofner, Terance W. Hart, Kaspar Zimmermann
  • Publication number: 20130324743
    Abstract: The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.
    Type: Application
    Filed: April 21, 2011
    Publication date: December 5, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Daniel T. Belmont, Cristian Harrison, Robert Michael Hughes, Young Chun Jung, Elaine Chungmin Lee, Benjamin Joseph Littler, Peter Jamison Rose, David Andrew Siesel, Gerald J. Tanoury
  • Patent number: 8598181
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: December 3, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Patent number: 8598078
    Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Publication number: 20130302378
    Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.
    Type: Application
    Filed: July 8, 2013
    Publication date: November 14, 2013
    Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
  • Publication number: 20130281450
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.
    Type: Application
    Filed: March 12, 2013
    Publication date: October 24, 2013
    Inventors: John K. Pratt, Dachun Liu, Chang H. Park, George S. Sheppard, Lisa A. Hasvold, Le Wang
  • Publication number: 20130274483
    Abstract: This invention is directed to asymmetric syntheses of certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: March 11, 2013
    Publication date: October 17, 2013
    Inventors: Shaoyi Sun, Jianmin Fu, Sultan Chowdhury, Ivan William Hemeon, Michael Edward Grimwood, Tarek Suhayl Mansour
  • Publication number: 20130267493
    Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 10, 2013
    Applicant: PFIZER INC.
    Inventors: Samit Bhattacharya, Kimberly Cameron, Matthew Dowling, Dilinie Fernando, David Ebner, Kevin Filipski, Daniel Kung, Esther Lee, Aaron Smith, Meihua Tu
  • Publication number: 20130210886
    Abstract: The invention relates to compounds of formula (I) for use in the prevention and/or treatment of viral infections: Wherein X, Y, Z, T, R1a and R1b are as defined in claim 1.
    Type: Application
    Filed: July 29, 2011
    Publication date: August 15, 2013
    Applicants: INSTITUT PASTEUR, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Pierre-Olivier Vidalain, Marianne Lucas-Hourani, Frédéric Tangy, Héléne Munier-Lehmann, Daniel Dauzonne
  • Publication number: 20130196968
    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 Q and Z are defined herein.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Publication number: 20130178453
    Abstract: The present disclosure relates to compounds useful as agonists of the cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders, either alone or in combination therapy. The compounds of the invention have Formula (I).
    Type: Application
    Filed: February 9, 2011
    Publication date: July 11, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Jason Rohde, Bo Peng, Takashi Nakai, Kevin Sprott, Ara Mermerían, Wayne C. Schairer, Galen John Carey
  • Publication number: 20130178471
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: February 28, 2013
    Publication date: July 11, 2013
    Applicant: Vextex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130175507
    Abstract: Novel heterocyclic materials are disclosed. The materials contain a fused tetracyclic structure that can improve the properties of OLED devices when the novel heterocyclic materials are incorporated into such devices.
    Type: Application
    Filed: January 10, 2012
    Publication date: July 11, 2013
    Applicant: Universal Display Corporation
    Inventor: Bin Ma
  • Publication number: 20130167932
    Abstract: Provided is an indole compound represented by the following general formula (1): wherein in formula (1), R1 and R2 each independently represent a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group; R3 to R6 each independently represent a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkoxy group or a hydroxy group; X represents an organic group having an acidic group; and Z represents a linking group including at least one selected from the group consisting of a substituted or unsubstituted aromatic ring, a substituted or unsubstituted heterocyclic ring, a vinylene group and an ethynylene group.
    Type: Application
    Filed: November 7, 2011
    Publication date: July 4, 2013
    Applicant: NEC CORPORATION
    Inventors: Katsumi Maeda, Shin Nakamura, Kentaro Nakahara, Terumasa Shimoyama
  • Publication number: 20130143918
    Abstract: The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Application
    Filed: September 21, 2012
    Publication date: June 6, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130131084
    Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.
    Type: Application
    Filed: August 17, 2012
    Publication date: May 23, 2013
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Catherine GUILLOU, Frank Kozielski, Christophe Labriere, Francoise Gueritte, Sergey Tcherniuk, Dimitrios Skoufias, Claude Thal, Henri-Philippe Husson
  • Publication number: 20130123508
    Abstract: The present invention relates to heptamethine hemicyanine chromophores of formula (I): where R1, R2, R3, R4, R?4, R5, R?5, R6, R?6, R7, X, Y1 and Y2 are as defined in claim 1, to the method for preparing same as well as to the use of such chromophores for the second-order nonlinear optical property thereof.
    Type: Application
    Filed: January 18, 2011
    Publication date: May 16, 2013
    Applicant: ECOLE NORMALE SUPERIEURE DE LYON
    Inventors: Yann Bretonniere, Chantal Andraud, Wissam Buron
  • Publication number: 20130116232
    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 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: June 8, 2011
    Publication date: May 9, 2013
    Applicant: ARAGON PHARMACEUTICALS, INC.
    Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith