Chalcogen Bonded Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 514/428)
  • Patent number: 11192865
    Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
    Type: Grant
    Filed: August 20, 2018
    Date of Patent: December 7, 2021
    Assignee: VIVACE THERAPEUTICS, INC.
    Inventors: Andrei W. Konradi, Tracy Tzu-Ling Tang Lin
  • Patent number: 10946007
    Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 17, 2020
    Date of Patent: March 16, 2021
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Lori Jean Patterson, Eric L. Stangeland
  • Patent number: 10894768
    Abstract: The present invention relates to a novel salt of (R)-(1-methylpyrrolidine-3-yl)methyl(3?-chloro-4?-fluoro-[1,1?-biphenyl]-2-yl)carbamate and a crystal form thereof. Also, the novel salt of (R)-(1-methylpyrrolidine-3-yl)methyl(3?-chloro-4?-fluoro-[1,1?-biphenyl]-2-yl)carbamate and the crystal form thereof according to examples of the present invention have remarkably excellent stability, hygroscopicity and solubility.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: January 19, 2021
    Assignee: Dong-A St Co., Ltd.
    Inventors: Woo Young Kwak, Chang-Yong Shin, Punna Reddy Ullapu, Sun-Ho Choi, Min-Jung Lee, Ji-Su Kim
  • Patent number: 10744092
    Abstract: The present invention relates to a temperature-sensitive composite and a method for preparing the same. The temperature-sensitive composite according to the present invention is maintained in a liquid state at room temperature and solidified at the time of delivery in the body, and shows remarkably excellent improvement in mechanical properties compared with an existing temperature-sensitive polymer composite, and as a result, the temperature-sensitive composite can promote the stability of a drug delivery system in the body and the sustainment of drug release.
    Type: Grant
    Filed: March 14, 2017
    Date of Patent: August 18, 2020
    Assignee: Korea University Research and Business Foundation, Sejong Campus
    Inventor: Soon Hong Yuk
  • Patent number: 10722504
    Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: July 28, 2020
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Lori Jean Patterson, Eric L. Stangeland
  • Patent number: 10034870
    Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: May 10, 2017
    Date of Patent: July 31, 2018
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Lori Jean Patterson, Eric L. Stangeland
  • Patent number: 9944596
    Abstract: Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4. A compound represented by the formula (I): wherein each symbol is as defined in the Description, or a salt thereof has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: April 17, 2018
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yoshihiro Banno, Masahiro Kamaura, Takahiko Taniguchi, Kazuaki Takami, Koichiro Fukuda, Shigekazu Sasaki
  • Patent number: 9783519
    Abstract: This invention relates to the quick and efficient synthesis of anti-tumor or anti-cancer compounds. More particularly, it relates to the quick and efficient synthesis of anti-tumor or anti-cancer compounds comprising phenylacetophenone derivatives using oxabenzonorbornadienes with terminal alkynes.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: October 10, 2017
    Assignees: HONG KONG BAPTIST UNIVERSITY, YUNNAN MINZU UNIVERSITY
    Inventors: Zhaoxiang Bian, Chengyuan Lin, Huaixue Mu, Baomin Fan, Yongyun Zhou, Jingchao Chen, Aiping Lu, Albert Sun-Chi Chan
  • Patent number: 9120746
    Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: September 1, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Daisuke Roland Saito
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Patent number: 9040508
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: May 26, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20150141483
    Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Pierre-Jean Colson, Timothy Fass, Venkat R. Thalladi
  • Publication number: 20150141482
    Abstract: The present invention relates to 1-(p-tolyl)cyclopropyl substituted bridged spiro[2.4]heptane derivatives of formula (I), wherein R1 is as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: May 15, 2013
    Publication date: May 21, 2015
    Inventors: Olivier Corminboeuf, Sylvaine Cren
  • Publication number: 20150126577
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Eric Stangeland, Daisuke Roland Saito, Priscilla Van Dyke, Lori Jean Patterson
  • Patent number: 9006282
    Abstract: This invention relates to the discovery of novel rosuvastatin and atorvastatin analogues.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: April 14, 2015
    Assignee: Redx Pharma Limited
    Inventors: Derek Lindsay, Peter Jackson, Stephen Hindley, Inder Bhamra
  • Publication number: 20150099720
    Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.
    Type: Application
    Filed: October 20, 2014
    Publication date: April 9, 2015
    Inventors: Lin Zhi, Robert I. Higuchi, E. Adam Kallel, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Daniel A. Ruppar, Bijan Pedram, Thomas Lot Stevens Lau, Todd A. Miller
  • Patent number: 9000191
    Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: April 7, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
  • Publication number: 20150093338
    Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 2, 2015
    Inventor: Michael Farber
  • Publication number: 20150093365
    Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 2, 2015
    Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
  • Publication number: 20150080450
    Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Application
    Filed: June 24, 2014
    Publication date: March 19, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventor: Daisuke Roland Saito
  • Publication number: 20150080369
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 19, 2015
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Patent number: 8969403
    Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: March 3, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Pierre-Jean Colson, Timothy Fass, Venkat R. Thalladi
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Publication number: 20150031656
    Abstract: The present invention relates to a combination therapy for elevating testosterone levels in male mammals in which an antiestrogen or pharmaceutically acceptable salt thereof is co-administered to the mammal with an additional therapeutic agent selected from an androgen and an aromatase inhibitor. The invention is also directed to a combination therapy for treating males with hypogonadism and disorders related thereto, including reduction of muscle mass. limitation of body performance capacity, reduction of bone density, reduction of libido, reduction of potency, reduction of benign prostatic hyperplasia and infertility.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 29, 2015
    Inventors: Joseph S. Podolski, Ronald D. Wiehle
  • Patent number: 8940776
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: January 27, 2015
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Publication number: 20150018360
    Abstract: The present invention provides, inter alia, compositions containing enantiomerically pure (R)(+)-amisulpride or enantiomerically pure (R)(+)-sulpiride, optionally with dopamine receptor modulators. The present invention also provides compositions containing racemic (RS)-amisulpride or (RS)-sulpiride in combination with dopamine receptor modulators. Methods for preventing, treating, or ameliorating the effects of a metabolic disorder or key element thereof, for modulating blood glucose levels, and for preventing, treating, or ameliorating the effects of diabetes in a subject are also provided. Additionally, the present invention provides methods for counter-acting the dopamine antagonist activity of (S)-amisulpride in racemic (RS)-amisulpride, or the dopamine antagonist activity of (S)-sulpiride in racemic (RS)-sulpiride, administered to a subject to prevent, treat, or ameliorate the effects of a metabolic disorder.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 15, 2015
    Applicant: BIOMED VALLEY DISCOVERIES, INC.
    Inventors: Reza Halse, Jeffrey James Roix, Saurabh Saha
  • Patent number: 8933249
    Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: January 13, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
  • Publication number: 20150010638
    Abstract: It is an object of the present invention to provide a method for improving the solubility of a poorly-soluble substance, which is capable of increasing the solubility of substantially all poorly-soluble substances. This is a method comprising coating the surface of a poorly-soluble substance particle with microparticles of a calcium compound such as calcium phosphate or calcium carbonate, and at least one selected from a pH adjuster and a surfactant, by applying mechanical energy thereto.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Inventors: Shuji Sakuma, Keiichiro Kikukawa, Ryosuke Miyasaka
  • Publication number: 20140343064
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-substituted oleanolic acid 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.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 20, 2014
    Applicant: Hanghzhou Bensheng Pharmaceutical Co., Ltd
    Inventors: Rongzhen Xu, Frank Rong, Hongxi Lai, Fuwen Xie
  • Publication number: 20140336174
    Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.
    Type: Application
    Filed: April 17, 2014
    Publication date: November 13, 2014
    Applicant: Genzyme Corporation
    Inventors: Oxana Ibraghimov-Beskrovnaya, Thomas A. Natoli
  • Patent number: 8883845
    Abstract: Administration of a loop diuretic in nebulized dry powder form directly to a patient's lungs for treating bronchial disease.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: November 11, 2014
    Assignee: Microdose Therapeutx, Inc.
    Inventor: Andrew Abrams
  • Patent number: 8877754
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
  • Publication number: 20140309275
    Abstract: The disclosure relates to compounds, pharmaceutical compositions, and methods of treating or preventing disease. In certain embodiments, the disclosure relates to methods of treating an infection or cancer comprising administering a pharmaceutical composition disclosed herein to a subject in need thereof. In a typical embodiment, one administers a pharmaceutical composition comprising sphingosine or a sphingosine analog to a subject at risk for, exhibiting symptoms of or diagnosed with a malaria infection.
    Type: Application
    Filed: September 27, 2012
    Publication date: October 16, 2014
    Inventors: Dennis C. Liotta, Jason Holt, JR., Michael G. Natchus, Mark T. Baillie, Eric J. Miller, Mary R. Galinski
  • Patent number: 8853255
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: April 25, 2013
    Date of Patent: October 7, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam D. Hughes, Lori Jean Patterson
  • Patent number: 8853423
    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: Grant
    Filed: June 15, 2011
    Date of Patent: October 7, 2014
    Assignee: Seragon Pharmaceuticals, Inc.
    Inventors: Steven P. Govek, Nicholas D. Smith
  • Patent number: 8840923
    Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: September 23, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Vincenzo Russo, Elisa Liberati, Nicola Cazzolla, Leonardo Marchitto, Lorella Ragni
  • Publication number: 20140275086
    Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
  • Publication number: 20140275048
    Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Publication number: 20140256698
    Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Inventors: Robert Booth, Jeff Dener, Michael Green
  • Publication number: 20140256730
    Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
    Type: Application
    Filed: January 13, 2014
    Publication date: September 11, 2014
    Applicant: Corsair Pharma, Inc.
    Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Publication number: 20140243374
    Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.
    Type: Application
    Filed: October 4, 2012
    Publication date: August 28, 2014
    Inventors: Corinne E. Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe, Cuiman Cai
  • Publication number: 20140234402
    Abstract: Compositions and methods for treating systemic diseases by intravenous administration of formulations of synthesized curcumin (diferuloylmethane) and concomitantly a calcium channel blocker to human subjects with neoplastic and neurodegenerative diseases are disclosed herein. The diseases are treated by prolonged administration of sub-optimal doses of liposomal curcumin or polymeric nanocurcumin or the sustained release curcumin from PLGA nanocurcumin at dosages below systemic hemolytic thresholds concomitantly with or without calcium channel blockers.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: SignPath Pharma Inc.
    Inventor: Lawrence Helson
  • Publication number: 20140221284
    Abstract: The invention provides compositions and methods for determining GLP-1 analog and/or DPPIV inhibitor response in a subject. In one embodiment, the composition comprises a solid support comprising probes for measuring a biomarker panel comprising, for example, adiponectin, C-peptide, hsCRP, insulin, proinsulin. The simultaneous use of multiple biomarkers with independent classification power will increase the performance of the biomarker panel in characterizing GLP-1 analog and DPPIV inhibitor response. The invention also provides methods of treating a subject (e.g. one experiencing cardiodiabetes) and determining the efficacy of a therapy through assaying the various biomarkers of a biomarker panel disclosed herein.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 7, 2014
    Applicant: IR2DX, Inc.
    Inventor: Andreas Pfuetzner
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Patent number: 8791151
    Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: July 29, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Daisuke Roland Saito
  • Patent number: 8785647
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: July 22, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ulrich Görgens, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • Patent number: 8772290
    Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: July 8, 2014
    Assignee: Oscotech Inc.
    Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
  • Patent number: 8754117
    Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Grant
    Filed: January 28, 2013
    Date of Patent: June 17, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Jianguo Ma
  • Publication number: 20140161830
    Abstract: Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.
    Type: Application
    Filed: November 25, 2013
    Publication date: June 12, 2014
    Applicant: Massachusetts Institute of Technology
    Inventors: Daniel Griffith Anderson, Kathryn Ann Whitehead, Joseph R. Dorkin, Arturo Jose Vegas, Yunlong Zhang
  • Publication number: 20140148438
    Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.
    Type: Application
    Filed: September 22, 2011
    Publication date: May 29, 2014
    Inventor: Michael Farber