Polycyclo Ring System Having The Additional 1,3-diazine Ring As One Of The Cyclos Patents (Class 514/252.16)
  • Publication number: 20130225597
    Abstract: The present invention is a method for treating post-radical prostatectomy erection dysfunction in a patient using a PDE-4, PDE-5, PDE-6 and/or PDE-7 inhibitor, wherein said PDE inhibitor is delivered at the incision site via an adhesion barrier.
    Type: Application
    Filed: April 29, 2013
    Publication date: August 29, 2013
    Applicant: University of Medicine and Dentistry of New Jersey
    Inventor: University of Medicine and Dentistry of New Jersey
  • Publication number: 20130225575
    Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from certain neurological conditions.
    Type: Application
    Filed: June 16, 2011
    Publication date: August 29, 2013
    Applicant: AFRAXIS, INC.
    Inventors: Jay Lichter, David Campbell, Sergio G. Duron, Benedikt Vollrath
  • Publication number: 20130225564
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Application
    Filed: March 18, 2013
    Publication date: August 29, 2013
    Applicant: Signal Pharmaceuticals, LLC
    Inventor: Signal Pharmaceuticals, LLC
  • Publication number: 20130217697
    Abstract: The invention relates to a pharmaceutical film formulation comprising one or more bitter-tasting drug(s) or pharmaceutically acceptable salts thereof, one or more film formers, a bitterness masker containing one or more inorganic and/or organic salt(s) and at least two monocyclic monoterpenes, and one or more sweetening agent(s).
    Type: Application
    Filed: October 27, 2011
    Publication date: August 22, 2013
    Applicant: HEXAL AG
    Inventors: Thomas Kohr, Petra Obermeier
  • Publication number: 20130217696
    Abstract: A method of treatment of erectile dysfunction (ED) comprises the step of administering fispemifene to a subject in need thereof in an amount effective to raise the subject's testosterone level. Fispemifene may be used in combination with a PDE-5 inhibitor in individuals who have failed to respond sufficiently to conventional ED treatment. Methods are also disclosed of treating ED by administering clomifene, enclomifene, ospemifene, toremifene and mixtures thereof in combination with a PDE-5 inhibitor.
    Type: Application
    Filed: March 21, 2013
    Publication date: August 22, 2013
    Applicant: QuatRX Pharmaceuticals Company
    Inventors: Robert L. Zerbe, Alexander Bridges, Risto Lammintausta, Rochelle Hanley, Stuart Dombey
  • Publication number: 20130217698
    Abstract: This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
    Type: Application
    Filed: November 9, 2011
    Publication date: August 22, 2013
    Applicants: Astex Therapeutics LTD, Novartis AG
    Inventors: John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena
  • Publication number: 20130209543
    Abstract: The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.
    Type: Application
    Filed: November 21, 2012
    Publication date: August 15, 2013
    Applicant: Intellikine LLC
    Inventor: Intellikine LLC
  • Publication number: 20130210830
    Abstract: The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved.
    Type: Application
    Filed: September 5, 2012
    Publication date: August 15, 2013
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventor: Martine CLOZEL
  • Patent number: 8507672
    Abstract: Substituted pyrrolo[2,3-d]pyrimidine-based compounds useful as inhibitors of LIM kinase 2 are disclosed. Also disclosed are pharmaceutical compositions comprising the compounds and methods of their use to treat, manage and prevent inflammatory diseases and disorders, cancer, and diseases and disorders of the eye.
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: August 13, 2013
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Bryce Alden Harrison, Spencer David Kimball, Ross Mabon, David Brent Rawlins, Dennis S. Rice, Michael Victor Voronkov, Yulian Zhang
  • Publication number: 20130203731
    Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: March 28, 2013
    Publication date: August 8, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventor: TAKEDA PHARMACEUTICAL COMPANY LIMITE LIMITED
  • Publication number: 20130203767
    Abstract: This invention relates to the use of certain cyclic guanosine 3?,5?-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 8, 2013
    Applicant: Pfizer Inc.
    Inventor: Pfizer Inc.
  • Publication number: 20130203765
    Abstract: The invention is directed to novel deuterated pyrrolopyrimidine compounds of formula (I) wherein R1 and R2 are defined below and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: February 17, 2011
    Publication date: August 8, 2013
    Applicant: Novartis AG
    Inventors: Christopher Thomas Brain, Lawrence Blas Perez
  • Publication number: 20130203766
    Abstract: The invention relates to new pharmaceutical compositions for the treatment of sexual disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment of sexual disorders and methods for the preparation thereof.
    Type: Application
    Filed: October 18, 2012
    Publication date: August 8, 2013
    Applicant: SPROUT PHARMACEUTICALS, INC.
    Inventor: Sprout Pharmaceuticals, Inc.
  • Publication number: 20130202549
    Abstract: The disubstituted piperazine analogs (DPAs) derivative compound and DPAs amine complex compound disclosed in the present aspects have characterized by presented pharmaceutics having functions to improve lipolysis, such as inhibiting obesity hyperlipidemia, and atherosclerosis.
    Type: Application
    Filed: September 6, 2012
    Publication date: August 8, 2013
    Inventor: Ing-Jun Chen
  • Publication number: 20130203768
    Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: September 28, 2011
    Publication date: August 8, 2013
    Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
  • Publication number: 20130196985
    Abstract: The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.
    Type: Application
    Filed: June 3, 2011
    Publication date: August 1, 2013
    Applicant: Guangzzhou Institute of Biomedicine and Health, Chineses Academy of Sciences
    Inventors: Ke Ding, Deping Wang, Duanqing Pei, Zhang Zhang, Mengjie Shen, Kun Luo, Yubing Feng
  • Patent number: 8497370
    Abstract: A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R1, Ra and RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: July 30, 2013
    Assignee: Kaohsiung Medical University
    Inventor: Ing-Jun Chen
  • Publication number: 20130190297
    Abstract: The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.
    Type: Application
    Filed: May 20, 2011
    Publication date: July 25, 2013
    Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D
    Inventors: Steven De Jonghe, Ling-Jie Gao, Piet Herdewijn, Jean Herman, Miyeon Jang, Pieter Leyssen, Thierry Louat, Johan Neyts, Christophe Pannecouque, Bart Vanderhoydonck
  • Publication number: 20130190320
    Abstract: The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.
    Type: Application
    Filed: January 12, 2013
    Publication date: July 25, 2013
    Applicant: ACEA BIOSCIENCES, INC.
    Inventor: ACEA Biosciences, Inc.
  • Publication number: 20130190305
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R6, A, B, C, n, p, q and r are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Application
    Filed: January 22, 2013
    Publication date: July 25, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventor: Matthias TREU
  • Publication number: 20130190292
    Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
    Type: Application
    Filed: August 12, 2011
    Publication date: July 25, 2013
    Applicant: CELLZOME LIMITED
    Inventors: Kathryn Bell, Nelly Piton, Claudio Dagostin, Cyrille Boussard, Andrew Ratcliffe, Nigel Ramsden
  • Patent number: 8492377
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y represents —C3-9alkyl-, —C1-5alkyl-NR6—C1-5alkyl- or —C1-5alkyl-NR7—CO—C1-5alkyl-; X1 represents —O —; X2 represents NR5—C1-2alkyl-; R1 represents hydrogen, halo or Het3-O—; R2 represents hydrogen; R3 represents hydroxy, C1-4alkyloxy- or C1-4alkyloxy substituted with one or two substituents each independently selected from Het4, hydroxy, C1-4alkyloxy-, C1-4alkyloxy-C1-4alkyloxy and NR9R10; R5 represents hydrogen or C1-4alkyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen; R9 and R10 each independently represent hydrogen; C1-4alkyl-S(?O)2—C1-4alkyl-C(?O)—; C1-4alkyl or C1-4alkyl substituted with hydroxy; Het3 represents pyridinyl optionally substituted with C1-4alkyl; Het4 represents morpholinyl, piperidinyl or piperazinyl wherein said Het4 is optionally substituted with hydroxy-C1-4alkyl or C1-4alkyl-S(?O)2—C1-4a
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: July 23, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Alexandra Papanikos, Eddy Jean Edgard Freyne, Peter Ten Holte, Marc Willems, Werner Constant Johan Embrechts, Laurence Anne Mevellec, Pierre-Henri Storck
  • Patent number: 8492373
    Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: July 23, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Jiaxin Yu, Joane Litvak
  • Publication number: 20130184270
    Abstract: The present invention relates to: combinations of: component A: one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: one or more N-(2-arylamino)aryl sulfonamide compounds of general formula (B), or Lapatinib, or Paclitaxel, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C: one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and a kit comprising such a combination.
    Type: Application
    Filed: April 14, 2011
    Publication date: July 18, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventor: Ningshu Liu
  • Publication number: 20130184253
    Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: July 19, 2012
    Publication date: July 18, 2013
    Applicant: NOVARTIS AG
    Inventors: Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian Hurley, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
  • Publication number: 20130184285
    Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.
    Type: Application
    Filed: March 6, 2013
    Publication date: July 18, 2013
    Applicants: ASTEX THERAPEUTICS, NOVARTIS AG
    Inventors: NOVARTIS AG, ASTEX THERAPEUTICS
  • Patent number: 8486948
    Abstract: The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2, preferably however SO, and wherein R3, R4, R4?, R5, R6 and R7 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: July 16, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pascale Pouzet, Christoph Hoenke, Peter Nickolaus, Rolf Goeggel, Thomas Fox, Dennis Fiegen, Klaus Klinder
  • Patent number: 8486952
    Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: July 16, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
  • Publication number: 20130178462
    Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 11, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130178469
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof.
    Type: Application
    Filed: July 15, 2011
    Publication date: July 11, 2013
    Applicants: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY (SIOC), AVEXA LIMITED
    Inventors: David Ian Rhodes, John Joseph Deadman, Giang Thanh Le, Nicholas Andrew Van de Graff, Lu Long, Li Xinming, Feng Xiao, Yu Changjiang
  • Publication number: 20130172338
    Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.
    Type: Application
    Filed: February 20, 2013
    Publication date: July 4, 2013
    Applicant: Cell Therapeutics, Inc.
    Inventor: Cell Therapeutics, Inc.
  • Patent number: 8476285
    Abstract: The invention relates to compounds of Formulae I-III: and therapeutic uses thereof, wherein A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group; B is chosen from a substituted or unsubstituted piperidine, homopiperidine, piperazine, pyrrolidine or azetidine group; R1 is chosen from hydro, alkyl, aryl, heteroaryl, amino, or halo; and L1, L2, are as defined herein.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: July 2, 2013
    Assignee: Myrexis, Inc.
    Inventors: Ashok C. Bajji, Se-Ho Kim, Benjamin Markovitz, Richard Trovato, Rajendra Tangallapally, Mark B. Anderson, Daniel Wettstein, Mark Shenderovich, John A. Vanecko
  • Publication number: 20130164259
    Abstract: The present invention relates to 1,4-Substituted Piperazine Derivatives, compositions comprising one or more 1,4-Substituted Piperazine Derivatives, and methods of using the 1,4-Substituted Piperazine Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 27, 2013
    Inventors: Cliff C. Cheng, Xiaohua Huang, Gerald W. Shipps, JR.
  • Publication number: 20130164280
    Abstract: The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventor: Gilead Sciences, Inc.
  • Publication number: 20130165448
    Abstract: The invention provides a 1-[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d] pyridine-5-group)-4-ethoxy-benzenesulfonyl]-cis-3,5-dimethylpiperazine citrate or an Aildenafil citrate crystal form O and a preparation method thereof. And the invention also provides pharmaceutical compositions containing the Aildenafil citrate crystal form O and the use thereof in preparing drugs for treating Male Erectile Dysfunction (ED). The above crystal form O can be prepared through the steps of: dissolving a raw material, namely, the Aildenafil citrate in a mixture of distilled water and tetrahydrofuran, stirring, heating, filtering, stirring a filtrate, cooling, insulating heat, crystallizing, filtering and the like. The crystal form O can be adopted to prepare drugs with pharmaceutically acceptable excipients, so as to treat the male sexual dysfunction diseases.
    Type: Application
    Filed: March 11, 2011
    Publication date: June 27, 2013
    Inventor: Guikun Liu
  • Publication number: 20130165427
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: August 24, 2012
    Publication date: June 27, 2013
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventor: Jayhong A. Chong
  • Patent number: 8470805
    Abstract: A series of monoquarternary piperazium salts including a structure of a formula I or II are provided. In formula I or II, R1, Ra, and RX are as defined in the specification. The monoquarternary piperazium salt of KMUP or piperazine disclosed in the present invention is characterized by being presented in a pro-drug form and having various pharmaceutical functions.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: June 25, 2013
    Assignee: Kaohsiung Medical University
    Inventor: Ing-Jun Chen
  • Patent number: 8470370
    Abstract: The present invention provides stable, self-assembling, biocompatible and biodegradable hydrogel formulations, into which one or more compounds may be incorporated allowing for delayed release or controlled release of the incorporated compounds as the hydrogel is degraded in the body.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: June 25, 2013
    Assignees: Aegis Therapeutics, LLC, The UAB Research Foundation
    Inventors: Edward T. Maggio, Elis Meezan, Dennis J. Pillion, Sarah L. Morgan, Joe Baggott
  • Publication number: 20130158042
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.
    Type: Application
    Filed: December 10, 2012
    Publication date: June 20, 2013
    Inventors: Annekatrin HEIMANN, Georg DAHMANN, Marc GRUNDL, Stephan Georg MUELLER, Bernd WELLENZOHN
  • Publication number: 20130158043
    Abstract: Provided herein are methods of utilizing PAK inhibitors for the treatment of cancer. Further provided herein are compounds and formulations utilized for the treatment of cancer.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 20, 2013
    Applicant: AFRAXIS, INC.
    Inventor: Afraxis, Inc.
  • Publication number: 20130150355
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3, R3a have meanings given in the description.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER
  • Publication number: 20130150370
    Abstract: Pharmaceutical composition for oral administration comprises at least one phosphodiesterase inhibitor and at least one sugar alcohol selected from mannitol, sorbitol, xylitol, maltitol, lactitol, erythritol, threitol and Isomalt, and sodium hydrogen carbonate as pharmaceutical excipients in the following weight proportions: phosphodiesterase inhibitor: about 10 to about 150 parts by weight in total; sugar alcohol: about 50 to about 600 parts by weight in total; and sodium hydrogen carbonate: about 2 to about 100 parts by weight. The above composition for use in a method of treating male erectile dysfunction with an accelerated onset of action is also disclosed.
    Type: Application
    Filed: June 24, 2011
    Publication date: June 13, 2013
    Inventor: Hartwig Steckel
  • Patent number: 8461165
    Abstract: The invention relates to the compounds of formula I, their preparation and the pharmaceutical compositions containing the compounds. The invention also relates to the use of the compounds of formula I in preparing medicines, which can treat sexual dysfunction of animals including human (male and female), especially erectile dysfunction of male and the diseases in which the function of phospholipase 5 (cGMP PDE5) is involved.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: June 11, 2013
    Assignees: Yangtze River Pharmaceutical (Group) Co., Ltd, Tianjin North Pharma Sci-Tech Co., Ltd
    Inventors: Yongfeng Wang, Kejun Zhao
  • Publication number: 20130143865
    Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: January 29, 2013
    Publication date: June 6, 2013
    Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.
    Inventors: Array BioPharma Inc., GENENTECH, INC.
  • Publication number: 20130143895
    Abstract: The present invention relates to substituted aromatic bicyclic compounds containing pyrimidine and pyridine rings of formula (I) having the structure as well as pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as tyrosine kinase inhibitors, preferably SRC family kinases (SFKs) inhibitors, in particular as multi SFK/JAK. kinases inhibitors and even preferably as dual c-SRC/JAK kinases inhibitors, thereby inhibiting the STAT3 activation and therefore abnormal growth of particular cell types. Notably, the compounds of the present invention are useful for the treatment or inhibition of certain diseases that are the result of deregulation of STAT3.
    Type: Application
    Filed: January 14, 2013
    Publication date: June 6, 2013
    Inventors: Andrès Mc Allister, Maximilien Murone, Saumitra Sengupta, Shankar Jayaram Shetty
  • Publication number: 20130143866
    Abstract: Compositions of matter including ?-tocotrienol and SU11274 are disclosed herein. A variety of Met kinase inhibitors may be used in conjunction with tocotrienols in the treatment or prevention of cancer. Combinations of ?-tocotrienol and SU11274 inhibit the cell growth of +SA mammary tumor cells.
    Type: Application
    Filed: December 2, 2012
    Publication date: June 6, 2013
    Inventor: Paul W. Sylvester
  • Publication number: 20130143894
    Abstract: The present disclosure is directed to chemically-stable and pharmaceutically-acceptable sildenafil oral spray formulations for the treatment of male erectile dysfunction, wherein the oral spray formulation has a pH of about 1.5 to less than 3.0. The present disclosure is also directed to methods for treating male erectile dysfunction.
    Type: Application
    Filed: June 7, 2011
    Publication date: June 6, 2013
    Applicant: vadel Pharma Inc.
    Inventors: David Bergstrom, Foyeke Opawale
  • Publication number: 20130143896
    Abstract: The present invention relates to substituted isoxazolo-quinazolines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular human MPS1 and PERK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: July 20, 2011
    Publication date: June 6, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Italo Beria, Nicoletta Colombo, Claudia Piutti, Matteo Salsa, Gabriella Traquandi
  • Publication number: 20130137688
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Application
    Filed: November 26, 2012
    Publication date: May 30, 2013
    Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF
  • Publication number: 20130131058
    Abstract: Compounds according to Formula (I), as well salts thereof: wherein R1 and R2 are as defined herein, are useful as antiproliferative agents and kinase inhibitors. Synthetic methods for preparing the compounds of Formula (I) are also provided.
    Type: Application
    Filed: July 21, 2011
    Publication date: May 23, 2013
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy