Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 514/418)
  • Patent number: 10646471
    Abstract: The disclosure provides bisindole suitable for inhibiting lipoxygenases or A?-formation, and treating associated diseases, such as Alzheimer's disease. The bisindoles are indolo[2,3-b]carbazole derivatives, and may be administered to a patient as part of a pharmaceutical formulation.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: May 12, 2020
    Assignee: SRI International
    Inventor: Ling Jong
  • Patent number: 10646470
    Abstract: Methods and compositions for treating acute myeloid leukemia and diffuse large B cell lymphoma using combinations of venetoclax and indolinone derivatives are provided.
    Type: Grant
    Filed: August 27, 2018
    Date of Patent: May 12, 2020
    Assignee: Oncternal Therapeutics, Inc.
    Inventors: Brian Lannutti, Katayoun Jessen, James Bradley Breitmeyer
  • Patent number: 10537552
    Abstract: The present invention provides compounds and compositions which are useful in methods for modulating pain and fevers in a subject. These compounds are of the structure of formula (I), wherein Rx-R4, X, Y, and Z are defined herein, or a pharmaceutically acceptable salt, solvate, or prodrug thereof to the subject. In one embodiment, the compound is 5-hydroxy-7-methyloxindole.
    Type: Grant
    Filed: May 3, 2016
    Date of Patent: January 21, 2020
    Assignee: Carafe Drug Innovation, LLC
    Inventors: John R. Carson, Robert B. Raffa, Kenneth G. Carson
  • Patent number: 10537611
    Abstract: Methods of treating cancers comprising FGFR1 gene amplification are provided. In some embodiments, the methods comprise administering a fibroblast growth factor receptor 1 (FGFR1) extracellular domain (ECD) and/or an FGFR1 ECD fusion molecule. In some embodiments, the methods comprise administering a fibroblast growth factor receptor 1 (FGFR1) extracellular domain (ECD) and/or an FGFR1 ECD fusion molecule in combination with at least one additional therapeutic agent.
    Type: Grant
    Filed: June 8, 2018
    Date of Patent: January 21, 2020
    Assignee: Five Prime Therapeutics, Inc.
    Inventors: Thomas Harding, Servando Palencia, Li Long, Kevin Hestir
  • Patent number: 10342480
    Abstract: Methods for screening for therapies against autism spectrum disorders and methods for determining whether a subject would be responsive to a therapy against an autism spectrum disorder are disclosed.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: July 9, 2019
    Assignee: The Children's Hospital of Philadelphia
    Inventors: Timothy P. L. Roberts, James Christopher Edgar
  • Patent number: 10159659
    Abstract: The present invention relates to cancer markers that are predictive for cancer patent response to treatment with an m TOR inhibitor and a vascular disrupting agent. The present invention further relates to methods of treating a cancer patient subpopulation with a combination of an m TOR inhibitor and a vascular disrupting agent.
    Type: Grant
    Filed: March 18, 2015
    Date of Patent: December 25, 2018
    Assignee: BIONOMICS LIMITED
    Inventor: Jose Iglesias
  • Patent number: 10022336
    Abstract: A patch containing free ropinirole (ropinirole in free form) in an adhesive base is provided, in which the patch exhibits favorable and continuous transdermal absorbability, high drug stability, and excellent adhesiveness. A transdermal absorption patch includes free ropinirole added to an adhesive base that contains a styrene-isoprene-styrene block copolymer (SIS), one or two or more tackifier resins containing a rosin-based resin, and a softener. The transdermal absorption patch is characterized in that the compounding ratio of the rosin-based resin to the free ropinirole represented as the ratio of the weight of the combined rosin-based resin to the free ropinirole is 3.5 to 8.0. In particular, a ropinirole-containing patch wherein the rosin-based resin is a hydrogenated rosin glycerol ester and the softener is liquid paraffin is provided.
    Type: Grant
    Filed: November 28, 2013
    Date of Patent: July 17, 2018
    Assignee: Teikoku Seiyaku Co., Ltd.
    Inventors: Katsuyuki Inoo, Akiko Katayama, Daiki Takano
  • Patent number: 9989847
    Abstract: Sulfonium and iodonium salts of nitrogen-containing carboxylic acids are novel. The onium salt functions as an acid diffusion controlling agent in a resist composition, enabling to form a pattern of good profile with high resolution, improved MEF, LWR and DOF.
    Type: Grant
    Filed: August 19, 2015
    Date of Patent: June 5, 2018
    Assignee: SHIN-ETSU CHEMICAL CO., LTD.
    Inventors: Masaki Ohashi, Jun Hatakeyama, Masahiro Fukushima
  • Patent number: 9962370
    Abstract: Some embodiments include methods for treating, preventing, reversing, halting, or slowing the progression of cancer, comprising administering to a subject in need thereof an effective amount of one or more chemotherapeutic agents, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition, wherein at least one of the chemotherapeutic agents is a cytotoxic granulocyte colony-stimulating factor receptor (GCFR) modulator. Methods are also disclosed for treating, preventing, reversing, halting, or slowing the progression of a hematopoietic disorder, comprising administered a therapeutically effective cytotoxic amount of a GCFR modulator to a subject in need thereof.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: May 8, 2018
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Keith B. Marschke, Lin Zhi
  • Patent number: 9895352
    Abstract: Indolinone derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.
    Type: Grant
    Filed: November 21, 2016
    Date of Patent: February 20, 2018
    Assignee: Oncternal Therapeutics, Inc.
    Inventor: Jean-Michel Vernier
  • Patent number: 9751896
    Abstract: A compound with antitumor activities is represented by formula: R1, R2, R3, and R4 are independently hydrogen, nitro, alkoxy, halogen, unsubstituted or substituted phenyl, or unsubstituted or substituted alkyl or cycloalkyl.
    Type: Grant
    Filed: April 17, 2017
    Date of Patent: September 5, 2017
    Assignee: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Chengyuan Liang, Minyi Jia, Danni Tian, Xuechuan Wang, Xuefeng Chen, Juan Li, Guang Tong
  • Patent number: 9693963
    Abstract: Disclosed is a 2,2?,6,6?-tetraisopropyl-4,4?-biphenol soft capsule composed of a capsule shell and the contents in the capsule, wherein the contents in the capsule include 2,2?,6,6?-tetraisopropyl-4,4?-biphenol, a solvent, and an antioxidant, among others.
    Type: Grant
    Filed: August 2, 2012
    Date of Patent: July 4, 2017
    Assignee: Xi'an Libang Pharmaceutical Co., Ltd.
    Inventors: Rutao Wang, Long An, Huijing Hu, Shupan Guo, Tao Chen, Weijiao Wang
  • Patent number: 9656957
    Abstract: Hydrazone compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: May 23, 2017
    Assignee: The Cleveland Clinic Foundation
    Inventors: Mohamed Naguib Attala, Philippe Diaz
  • Patent number: 9586964
    Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: October 28, 2012
    Date of Patent: March 7, 2017
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
  • Patent number: 9394267
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: July 19, 2016
    Assignee: The Cleveland Clinic Foundation
    Inventors: Mohamed Naguib Attala, Philippe Diaz
  • Patent number: 9382205
    Abstract: Disclosed herein are processes for the preparation of a pharmaceutically active agent and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 25, 2014
    Date of Patent: July 5, 2016
    Assignee: H. Lundbeck A/S
    Inventors: Frans Therkelsen, Michael Harold Rock, Svend Treppendahl
  • Publication number: 20150148389
    Abstract: The invention is directed to methods of treating organ specific infections in a host organism by administering compounds that target host receptors and/or host cellular signaling molecules to prevent a pathogen from infecting the organ. For example, the administration of a compound to prevent a pathogen from crossing the blood-brain barrier to prevent a brain infection.
    Type: Application
    Filed: February 3, 2015
    Publication date: May 28, 2015
    Inventor: Kwang S. Kim
  • Patent number: 9040574
    Abstract: The present invention is directed to a method treating prostate cancer. The method comprises administering to a patient in need thereof at least one compound selected from N-methyl-?3,3?-dihydroindole-2,2? diketone; N-1-(?-D-O-triacetyl-xylopranosyl)-?3,3?-dihydroindole-2,2? diketone; and N-1-(?-D-O-triacetyl-xylopranosyl)-N?-methyl-?3,3?-dihydroindole-2,2? diketone. Preferably the compound is in an amount sufficient to inhibit growth, invasion, and/or metastasis of prostate cancer cells.
    Type: Grant
    Filed: September 20, 2012
    Date of Patent: May 26, 2015
    Assignee: Natrogen Therapeutics International, Inc.
    Inventors: Longgui Wang, Simon K. Mencher, James P. McCarron, Jr.
  • Patent number: 9018231
    Abstract: The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment/prevention of various disorders that are related to 5-HT6 receptor functions.
    Type: Grant
    Filed: March 24, 2010
    Date of Patent: April 28, 2015
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Rajesh Kumar Badange, Veena Reballi, Anil Kashinath Chindhe, Rambabu Namala, Mohamad Sadik Abdulhamid Mulla, Ishtiyaque Ahmad, Renny Abraham, Venkateswarlu Jasti
  • Publication number: 20150080422
    Abstract: Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.
    Type: Application
    Filed: September 25, 2014
    Publication date: March 19, 2015
    Applicant: PharmoRx Therapeutics, Inc.
    Inventors: David M. Bear, Robert M. Kessler
  • Patent number: 8980926
    Abstract: The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: March 17, 2015
    Assignees: Genzyme Corporation, President and Fellows of Harvard College, Massachusetts Institute of Technology
    Inventors: Ralph Mazitschek, Jon C. Clardy, Dyann Wirth, Roger Wiegand, Sameer Urgaonkar, Mary Lynn Baniecki, Joseph Cortese, Cassandra Celatka, Yibin Xiang, Renato Skerlj, Elyse M. J. Bourque
  • Publication number: 20150065552
    Abstract: Novel use of small molecules, particularly indolyl and indolinyl hydroxamates is disclosed herein. The indolyl and indolinyl hydroxamates are useful as lead compounds for manufacturing a medicament or a pharmaceutical composition for treating a patient suffering from heart failure or neuronal injury.
    Type: Application
    Filed: September 15, 2012
    Publication date: March 5, 2015
    Applicant: Taipei Medical University
    Inventors: Yi-Jen Chen, Kuo-Sheng Hung, Yu-Hsun Kao, Jing-Ping Liou, Pei-Wen Shan
  • Patent number: 8962697
    Abstract: The invention features biodegradable polymers for the delivery of biologically active agents. The polymers include at least one biologically active agent covalently attached via a polyamide linker susceptible to selective hydrolysis by peptidase enzymes. Hydrolysis of the polyamide linker releases the biologically active agent in vivo.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: February 24, 2015
    Assignee: Interface Biologics Inc.
    Inventors: Frank Laronde, Hanje Chen
  • Publication number: 20150051260
    Abstract: Compounds, compositions and methods relating to EWS-FLI1 protein inhibitors are provided. The compounds have utility in the treatment of cancers including the Ewing's sarcoma family of tumors.
    Type: Application
    Filed: April 11, 2013
    Publication date: February 19, 2015
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Jeffrey A. Toretsky, Milton Lang Brown, Perrer N. Tosso, Aykut Uren, Yali Kong
  • Publication number: 20150045395
    Abstract: This invention relates to methods of reversing and inhibiting liver fibrosis and hepatitis using a small indolinone molecule Hesperadin and related compounds. Methods of identifying such agents and using them to inhibit the expression of collagens and ECM proteins including MMPs and TIMPs in purified hepatic stellate cells are provided. In vivo data of Hesperadin in inhibiting induced collagen production are presented. This method of specifically targeting drugs to hepatic stellate cells in vivo, provides a novel therapy for liver diseases.
    Type: Application
    Filed: August 9, 2013
    Publication date: February 12, 2015
    Applicant: Acclaim BioMed USA LLC
    Inventors: Kenneth Ka-Ho Lee, Stanton Hon-Lung Kok, Tsz-Wai Kok, Sing-Wan Wong, John Yeuk-Hon Chan
  • Publication number: 20150038465
    Abstract: The invention relates to the use of a derivative compound of 1,3-benzodioxole of formula (I) wherein R is a linear or branched (C4-C10) alkyl substituent as a synergistic compound of insecticidal active ingredients insecticidal compositions comprising at least one compound of Formula (I) and at least one insecticidal active ingredient are also described.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 5, 2015
    Applicant: ENDURA S.P.A.
    Inventors: Carlotta Gobbi, Valerio Borzatta, Elisa Capparella
  • Publication number: 20150038543
    Abstract: This invention provides a series of new oxindole derivatives 1-21, evaluated for their antiglycation potential by using in vitro BSA-MG glycation model. These derivatives showed a varying degree of antiglycation activity with IC50 values ranging between 150-856 ?M. Compound 14 (IC50=150.4±2.5 ?M) was found to be the most potent among all derivatives, even better than the standard inhibitor i.e. rutin (IC50=294.5±1.50 followed by compounds 13 and 8 with IC50 value of 194.40±2.5 and 211.41±4.1 ?M, respectively.
    Type: Application
    Filed: July 30, 2013
    Publication date: February 5, 2015
    Inventors: Muhammad Iqbal Choudhary, Saima Rasheed, Nessar Ahmed, Khalid M. Khan, Momin Khan, Atta-ur Rahman, Atia-tul- Wahab
  • Publication number: 20150031655
    Abstract: The disclosure provides a method of treating a mammal afflicted with an age-related disorder, comprising administering to the mammal a combination of liver X receptor (LXR) modulator and estrogen receptor (ER) modulator, in an amount effective to treat the mammal. Further disclosed are the LXR modulators and ER modulators used in the combination therapy.
    Type: Application
    Filed: April 10, 2012
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NORTH DAKOTA
    Inventor: Othman Ghribi
  • Patent number: 8940732
    Abstract: The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: January 27, 2015
    Assignee: Massachusetts Institute of Technology
    Inventors: Damon Theron Page, Mriganka Sur
  • Patent number: 8937095
    Abstract: The invention describes dual Aurora kinase/MEK inhibitors and their use in therapy.
    Type: Grant
    Filed: July 9, 2013
    Date of Patent: January 20, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephan Karl Zahn, Patrizia Sini, Bojan Bister
  • Publication number: 20150018301
    Abstract: Leucine-rich repeat kinase-2 (LRRK2) mutations are a common cause of Parkinson's disease. Inhibitors of LRRK2 kinase that are protective in in vitro and in vivo models of LRRK2-induced neurodegeneration were identified. The presently disclosed subject matter establishes that LRRK2-induced degeneration of neurons in vivo is kinase dependent and that LRRK2 kinase inhibition provides a potential new neuroprotective paradigm for treating Parkinson's disease.
    Type: Application
    Filed: November 8, 2010
    Publication date: January 15, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Byoung Dae Lee, Ted M. Dawson, Valina L. Dawson, Andrew B. West, Howard Federoff
  • Publication number: 20150004215
    Abstract: A method for producing a patch comprising a support layer and an adhesive agent layer arranged on at least one surface of the support layer, the method comprising: step A) obtaining an adhesive agent layer composition comprising free ropinirole in an amount which results in a content of 5 to 13.2% by mass in an obtained adhesive agent layer; step B) heating the adhesive agent layer composition at a temperature in a range from 50 to 76° C. for 5 minutes to 24 hours; and step C) cooling the heated adhesive agent layer composition to normal temperature at an average rate of temperature drop of 1 to 20° C./hour, thereby obtaining the adhesive agent layer comprising the free ropinirole at a supersaturated concentration in a dissolved form.
    Type: Application
    Filed: June 27, 2014
    Publication date: January 1, 2015
    Applicant: HISAMITSU PHARMACEUTICAL CO., INC.
    Inventors: Takahito YOSHIZAKI, Kouji Tanaka, Kazunosuke Aida, Terumitsu Kaiho, Nobuo Tsutsumi
  • Publication number: 20150005337
    Abstract: The invention relates to a transdermal or transmucosal non-occlusive, semi-solid pharmaceutical formulation that includes at least one systemically active agent that acts on the Central Nervous System (CNS) of a mammal; and a permeation enhancing solvent system present in an amount sufficient to solubilize the at least one active ingredient.
    Type: Application
    Filed: September 17, 2014
    Publication date: January 1, 2015
    Inventors: Dario Norberto R. Carrara, Arbaud Grenier, Igno Alberti, Laetitia Henry, Celine Decaudin
  • Patent number: 8920837
    Abstract: The novel sustained release dosage form comprising an active agent and a combination of a non-swelling pH dependent release retardant and a non swelling pH independent release retardant polymer which provides pH-independent drug release for a considerable period of time after administration.
    Type: Grant
    Filed: July 3, 2006
    Date of Patent: December 30, 2014
    Assignee: Rubicon Research Private Limited
    Inventors: Pratibha S. Pilgaonkar, Maharukh T. Rustomjee, Anilkumar S. Gandhi, Paras R. Jain, Atul A. Kelkar
  • Publication number: 20140377329
    Abstract: The invention features sublingual film formulations of dopamine agonists and methods of treating Parkinson's disease, tremors, restless leg syndrome, sexual dysfunction, and depressive disorders therewith.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Inventors: Nathan John BRYSON, Anthony John GIOVINAZZO, Scott David BARNHART, Michael Clinton KOONS
  • Publication number: 20140364477
    Abstract: Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Applicants: Ohio State University, National Taiwan University
    Inventors: Ching-Shih Chen, Jing-Ping Liou, Hsing-Jin Liu, Kuo-Sheng Hung, Pei-Wen Shan, Wen-Ta Chiu, Che-Ming Teng
  • Publication number: 20140356373
    Abstract: The invention relates to compositions and methods for treating lupus. The methods typically comprise the step of administrating one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA in an amount sufficient to treat the lupus; preferably by modulating cytokine expression. Preferably the compound is in an amount less than sufficient to substantially inhibit cyclin dependent kinases.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 4, 2014
    Applicant: NATROGEN THERAPEUTICS INTERNATIONAL, INC.
    Inventors: Longgui Wang, Simon K. Mencher
  • Publication number: 20140343115
    Abstract: Provided is an adhesive patch containing ropinirole serving as a therapeutic drug for Parkinson's disease, with the ropinirole used being free ropinirole (ropinirole in free form) added to an adhesive base, wherein the patch exhibits favorable drug permeability and excellent drug stability. Also provided is a transdermal absorption patch using, as an adhesive base, an acrylic-based adhesive having no specific carboxyl group and having a hydroxyl group or a pyrrolidone group, with the patch including free ropinirole added to the adhesive base. Further provided is a ropinirole-containing transdermal absorption patch including a transdermal absorption promoting agent.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 20, 2014
    Inventors: Katsuyuki Inoo, Akiko Katayama, Daiki Takano
  • Publication number: 20140343114
    Abstract: This invention provides compounds of formulas (I), (II), (III), and (IV) as defined in the specification, and pharmaceutical compositions comprising the same, and methods of inhibiting, treating, or abrogating a poxvirus infection in a subject using the compounds or compositions.
    Type: Application
    Filed: March 10, 2014
    Publication date: November 20, 2014
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: Robert P. RICCIARDI, Manunya Nuth
  • Patent number: 8889729
    Abstract: Indole derivatives, compositions including same, and methods utilizing same for the treatment of amyloid associated diseases, such as type II diabetes mellitus, Alzheimer's dementia or diseases, systemic and localized amyloidosis, and prion-related encephalopathies are provided.
    Type: Grant
    Filed: June 6, 2010
    Date of Patent: November 18, 2014
    Assignee: Tel Aviv University Future Technology Development L.P.
    Inventors: Ehud Gazit, Tomer Cohen
  • Patent number: 8883843
    Abstract: This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogs of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: November 11, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Julie F. Liu
  • Patent number: 8877944
    Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: November 4, 2014
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Alexander Khvat, Mikhail Yurievitch Krasavin, Barbara Forte, Fabio Zuccotto
  • Publication number: 20140302141
    Abstract: This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.
    Type: Application
    Filed: February 24, 2014
    Publication date: October 9, 2014
    Applicant: OSMOTICA KERESKEDELMI ES SZOLGALTATO KFT
    Inventors: FERNANDO G. TONEGUZZO, GLENN A. MEYER, Marcelo A. RICCI, Marcelo A. COPPARI, ANA C. PASTINI, GUSTAVO A. FISCHBEIN
  • Publication number: 20140296292
    Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 2, 2014
    Inventors: Lin Zhi, Keith Marschke, Virginia H. Grant, Steven L. Roach, Yixing Shen, Jason C. Pickens, Bijan Pedram, C. Arjan van Oeveren, Lino J. Valdez, Andrew R. Hudson
  • Publication number: 20140296217
    Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
    Type: Application
    Filed: February 20, 2014
    Publication date: October 2, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: John Edward PARK, Gerald Juergen ROTH, Armin HECKEL, Nveed CHAUDHARY, Trixi BRANDL, Georg DAHMANN, Matthias GRAUERT
  • Patent number: 8846748
    Abstract: Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: September 30, 2014
    Assignees: Taipei Medical University, Ohio State University, National Taiwan University
    Inventors: Ching-Shih Chen, Jing-Ping Liou, Hsing-Jin Liu, Kuo-Sheng Hung, Pei-Wen Shan, Wen-Ta Chiu, Che-Ming Teng
  • Publication number: 20140288127
    Abstract: The present invention provides compounds of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Inventors: Li Chen, Lichun Feng, Mengwei Huang, Jia Li, Fajun Nan, Tao Pang, Lifang Yu, Mei Zhang
  • Publication number: 20140271480
    Abstract: The present invention provides a method of using indole-ketone or indolidone to treat or prevent a neurodegenerative disease or disorder. In one embodiment, the neurodegenerative disease is Parkinson's disease. In another embodiment, the neurodegenerative disease or disorder is associated with excessive neuronal Nitric Oxide Synthase (nNOS) activity. Examples of indole-ketone include, but are not limited to, SU4312, SU5416, SU11248 (Sunitinib), and indirubin-3-oxime.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Inventors: Ming Yuen Lee, Yifan Han, Chung Lit Choi, Zaijun Zhang, Wei Cui
  • Publication number: 20140275202
    Abstract: Compositions and methods are provided that utilize an injectable ropinirole having a therapeutically effective amount of ropinirole in an aqueous solvent, the composition having a pH of from about 3.0 to about 6.5. The compositions and methods provided contain less than 3% by weight of impurities and are suitable for administration by infusion pumps. In some embodiments, the compositions are made in an oxygen free environment and/or are made with an antioxidant to reduce impurities and improve stability. In some embodiments, the compositions provided are utilized to treat Parkinson's disease.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 18, 2014
    Applicant: Medtronic, Inc.
    Inventors: Michael C. Schmitz, Roger E. Harrington, Carmen E. Snaza, Keith R. Hildebrand, Ngoc N. Lu
  • Publication number: 20140275075
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 18, 2014
    Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER