At Least Three Rings In The Polycyclo Ring System Patents (Class 514/250)
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Publication number: 20140371208Abstract: Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Inventors: Theresa A. ZESIEWICZ, Kelly L. SULLIVAN
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Publication number: 20140371228Abstract: The present invention includes a method of treating or preventing a disease or disorder such as a mycobacterial infection, a Gram-positive bacterium infection, a yeast infection, an inflammatory condition, an auto-immune disorder and/or a proliferative disorder in a subject in need thereof. The method comprises administering to the subject a therapeutically effective amount of at least one compound of the invention, which includes clofazimine derivatives.Type: ApplicationFiled: December 21, 2012Publication date: December 18, 2014Inventors: Harvey Rubin, Takahiro Yano, Sacha Kassovska-Bratinova, Norman Schechter, Jiah Shin Teh, Jeffrey Winkler
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Publication number: 20140371227Abstract: The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.Type: ApplicationFiled: September 14, 2012Publication date: December 18, 2014Applicants: The Scripps Research Institute, University of KansasInventors: Jeffrey Aube, Laura Bohn, Thomas Edward Prisinzano, Frank John Schoenen, Kevin John Frankowski
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Publication number: 20140371229Abstract: The present invention relates to compositions and methods for the treatment of Parkinson's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Parkinson's disease and related disorders targeting the alpha-synuclein aggregation network. In particular, the invention relates to compounds which, alone or in combination(s), can effectively protect neuronal cells from alpha-synuclein aggregates. The invention also relates to methods of producing a drug or a drug combination for treating Parkinson's disease and to methods of treating Parkinson's disease or a related disorder.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Inventors: DANIEL COHEN, SERGUEI NABIROCHKIN, ILYA CHUMAKOV, RODOLPHE HAJJ
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Patent number: 8906923Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: GrantFiled: August 10, 2012Date of Patent: December 9, 2014Assignee: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Publication number: 20140357642Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: January 11, 2013Publication date: December 4, 2014Applicant: NOVARTIS AGInventors: Steven Carl Chatlton, Catherine Leblanc, Stephen Carl McKeown
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Publication number: 20140357643Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: , or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.Type: ApplicationFiled: August 18, 2014Publication date: December 4, 2014Inventor: Brian Alvin Johns
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Patent number: 8901126Abstract: Substituted imidazo[1,5-a]quinoxalin-4-one compounds of formula (I) described herein exhibit PDE9-inhibitory action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.Type: GrantFiled: March 7, 2013Date of Patent: December 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Mari Sugita, Hirofumi Yamamoto, Kazunori Kamijo, Kazuyuki Tsuchiya, Ryushi Seo, Satoshi Yamamoto
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Publication number: 20140350021Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart.Type: ApplicationFiled: August 6, 2014Publication date: November 27, 2014Inventors: Nestor F. Gonzalez-Cadavid, Jacob Rajfer
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Publication number: 20140349992Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Applicant: Sunovion Pharmaceuticals Inc.Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
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Publication number: 20140349970Abstract: The invention provides a compound of Formula (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), or (Il) as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Applicant: ABBVIE INC.Inventors: Neil Wishart, Maria A. Argiriadi, Eric C. Breinlinger, David J. Calderwood, Anna M. Ericsson, Bryan A. Fiamengo, Kristine E. Frank, Michael Friedman, Dawn M. George, Eric R. Goedken, Michael Z. Hoemann, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Kelly D. Mullen, Gagandeep Somal, Kent D. Stewart, Jeffrey W. Voss, Grier A. Wallace, Lu Wang, Kevin R. Woller
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Patent number: 8894989Abstract: The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly(ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.Type: GrantFiled: June 19, 2012Date of Patent: November 25, 2014Assignee: Eisai Inc.Inventors: Weizheng Xu, Greg Delahanty, Ling Wei, Jie Zhang
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Patent number: 8895557Abstract: Ecteinascidin formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided.Type: GrantFiled: October 28, 2005Date of Patent: November 25, 2014Assignee: Pharma Mar, S.A., Sociedad UnipersonalInventors: Jacob Hendrik Beijnen, Bastiaan Nuijen, Pilar Calvo Salve, Maria Tobio Barreira
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Publication number: 20140342002Abstract: Embodiments of the invention relate to particles of active substances, methods for preparing the particles, formulations containing the particles, and metered dose inhalers containing such particles or formulations. In one embodiment, a composition of an aerosol formulation is provided and contains a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 10 ?m suspended in a hydrofluorocarbon fluid vehicle at a concentration within a range from about 0.2% w/v to about 5% w/v. The aerosol formulation exhibits a flocculation volume of about 85% or greater about 1 minute after mixing the particulate active substance and the hydrofluorocarbon fluid vehicle. The particulate active substance contains an alkaloid ergotamine, pharmaceutically acceptable salts thereof, analogues thereof, or derivatives thereof.Type: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Inventors: Andreas KORDIKOWSKI, Stephen Ernest WALKER, Peter YORK
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Patent number: 8889687Abstract: This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.Type: GrantFiled: March 2, 2012Date of Patent: November 18, 2014Assignee: Concert Pharmaceuticals, Inc.Inventors: Julie F. Liu, Roger Tung, Scott L. Harbeson
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Publication number: 20140335153Abstract: A method of preparing a thin film, the method comprising: (a) mixing a lipid, emulsifier, and solvent to provide a uniform first mixture; (b) contacting an active ingredient with the uniform first mixture to provide a thickened second mixture; (c) contacting a binder with the thickened second mixture to provide a slurry; and (d) hot extruding, casting, and condensing the slurry to provide the thin film; or cooling, shearing, mixing, casting, and condensing the slurry to provide the thin film.Type: ApplicationFiled: October 31, 2013Publication date: November 13, 2014Applicant: CURE Pharmaceutical CorporationInventors: Eric Allen, Robert Steven Davidson, Jose Bernardo
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Publication number: 20140336184Abstract: The present invention concerns methods and compositions regarding suppression of double stranded RNA-activated protein kinase (PKR) to enhance cognition in an individual. In specific cases, an inhibitor of PKR is provided to the individual such that cognition is enhanced thereby, including by enhancing memory, for example. Kits are encompassed in certain embodiments.Type: ApplicationFiled: November 29, 2012Publication date: November 13, 2014Inventors: Mauro Costa-Mattioli, Ping Jun Zhu, Jeremy A. May
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Publication number: 20140336197Abstract: The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.Type: ApplicationFiled: July 31, 2014Publication date: November 13, 2014Inventors: Makoto OKADA, Shuichiro SATO, Kenji KAWADE, Kotaro GOTANDA, Atsushi SHINBO, Youichi NAKANO, Hideo KOBAYASHI
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Patent number: 8883830Abstract: The invention is directed to topical formulations and methods of treating a migraines and/or cluster headaches, muscle sprains, muscle spasms, spasticity, tension headaches, tension related migraines and related conditions associated with muscle tension and pain with a therapeutically effective amount of an ergot alkaloid, skeletal muscle relaxant, serotonin agonist, combinations thereof, pharmaceutically acceptable salt thereof, prodrugs thereof or derivative thereof.Type: GrantFiled: January 13, 2012Date of Patent: November 11, 2014Assignee: Afgin Pharma LLC.Inventor: Ronald Aung-Din
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Patent number: 8883787Abstract: The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.Type: GrantFiled: June 10, 2013Date of Patent: November 11, 2014Assignee: Eisai Inc.Inventors: Weizheng Xu, Greg Delahanty, Jie Zhang
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Publication number: 20140329823Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes.Type: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventors: Stephen M. Condon, Matthew G. Laporte, Yijun DENG, Susan R. Rippin
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Publication number: 20140323491Abstract: The present invention relates to toluenesulfonic acid addition salt crystals of specific substituted heterocycle fused gamma-carbolines, the method of making and using such crystals.Type: ApplicationFiled: February 11, 2014Publication date: October 30, 2014Applicant: INTRA-CELLULAR THERAPIES, INC.Inventors: John Tomesch, Lawrence P. Wennogle
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Publication number: 20140322229Abstract: The present document describes compounds of Formula I, pharmaceutical compositions comprising the same as well as methods of treating diseases such as a cancer, neurological disease, neurodegenerative disorder, stroke, traumatic brain injury, parasitic infection, inflammation or an autoimmune disease with said compounds.Type: ApplicationFiled: November 29, 2012Publication date: October 30, 2014Inventors: Zhaoyin Wang, Lianhai Li
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Publication number: 20140316333Abstract: A dissolving solid solution perforator (SSP) patch for oral cavity administration may include at least one perforator. The at least one perforator may contain a first drug and be configured to pierce an outside layer of an oral cavity for promptly delivering the first drug. The at least one perforator may penetrate an epithelium layer of the oral cavity and to deliver the antimigraine drug into blood vessels in a submucosa layer.Type: ApplicationFiled: October 29, 2012Publication date: October 23, 2014Inventor: Sung-Yun KWON
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Publication number: 20140315883Abstract: The invention provides a compound of Formula (I as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: April 18, 2014Publication date: October 23, 2014Applicant: ABBVIE INC.Inventors: Eric Breinlinger, Heather Davis, Michael Hoemann, Bin Li, Biqin Li, Gagandeep Somal, Stacy Van Epps, Lu Wang, Lu Wang
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Publication number: 20140315888Abstract: The present invention relates to novel heterocyclic compounds useful in preparing drugs for treatment of diseases associated with various functions of the histamine 4 receptor. Especially, the said drugs are useful for treatment of inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer.Type: ApplicationFiled: September 28, 2012Publication date: October 23, 2014Applicant: C&C RESEARCH LABORATORIESInventors: Pil Su Ho, Dong Oh Yoon, Sun Young Han, Won Il Lee, Jung Sook Kim, Woul Seong Park, Sung Oh Ahn, Hye Jung Kim
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Publication number: 20140315911Abstract: Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.Type: ApplicationFiled: November 12, 2012Publication date: October 23, 2014Inventors: Meizhong Jin, Mridula Kadalbajoo, An-Hu Li, Mark J. Mulvihill, Kam W. Siu, Arno G. Steinig, Jing Wang
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Patent number: 8865713Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: GrantFiled: September 3, 2013Date of Patent: October 21, 2014Assignee: Janssen Pharmaceutica NVInventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Patent number: 8865716Abstract: The present invention relates to spiroheterocycl-dihydropyrimidines, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.Type: GrantFiled: February 14, 2013Date of Patent: October 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Christian Eickmeier, Kai Gerlach, Niklas Heine, Alexander Weber, Ulrike Gross
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Publication number: 20140309185Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
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Publication number: 20140309181Abstract: Small compounds that modulate the expression of and/or function of sodium channel, voltage-gated, alpha subunit (SCNxA) are presented. Pharmaceutical compositions containing such small molecules and their use in treating diseases and disorders associated with the expression of SCNxA are also presented.Type: ApplicationFiled: August 28, 2012Publication date: October 16, 2014Applicant: CuRNA, Inc.Inventors: Joseph Collard, Olga Khorkova Sherman, Jane H. Hsiao
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Publication number: 20140309213Abstract: This invention relates to compounds of Formula I-VI having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with —(CH2)n1— and —(CH2)n2—, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: October 16, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
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Publication number: 20140309232Abstract: The present invention relates to a bioengineering strain for production of novel microorganism-originated fungicides and uses thereof. The bioengineering strain for production of microorganism-originated fungicides of the present invention is obtained by transforming a phzH gene recombination expression plasmid into a strain producing phenazine-1-carboxylic acid, wherein the bioengineering strain produces phenazine-1-carboxamide. The present invention utilizes an existing strain producing phenazine-1-carboxylic acid to carry the phzH gene recombination expression plasmid, thereby achieving efficient expression of the phzH gene and transforming phenazine-1-carboxylic acid into phenazine-1-carboxamide. The present invention further discloses uses of the bioengineering strain, including a microorganism-originated fungicide produced by the bioengineering strain through fermentation, and preparation and application of the microorganism-originated fungicide.Type: ApplicationFiled: November 21, 2011Publication date: October 16, 2014Applicant: SHANGHAI JIAOTONG UNIVERSITYInventors: Yuquan Xu, Huifeng Shen, Ya-Wen He, Wanping Zhou
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Patent number: 8853125Abstract: The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, etc.Type: GrantFiled: September 23, 2009Date of Patent: October 7, 2014Assignee: BASF SEInventors: Steffen Groβ, Karsten Körber, Wolfgang von Deyn, Florian Kaiser, Ronan Le Vezouet, Sebastian Sörgel, Matthias Pohlman, Prashant Deshmukh, Joachim Dickhaut, Douglas D. Anspaugh, Deborah L. Culbertson, Faraneh Oloumi
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Publication number: 20140296209Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B—The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: October 2, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventors: Andrew Asher Protter, Sarvajit Chakravarty
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Publication number: 20140296244Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.Type: ApplicationFiled: February 17, 2014Publication date: October 2, 2014Inventors: Michael J. Gerber, Christopher Dufton
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Publication number: 20140288085Abstract: Provided herein are methods and systems for the treatment of cardiovascular conditions, including pulmonary hypertension (PH), in subjects that are being treated with a treatment regimen that includes a phosphodiesterase-5 (PDE-5) inhibitor.Type: ApplicationFiled: March 17, 2014Publication date: September 25, 2014Applicant: CardioMEMS, Inc.Inventor: Jay Yadav
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Publication number: 20140286931Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventor: Chengzhi Zhang
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Publication number: 20140288062Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
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Publication number: 20140288078Abstract: The present invention relates to methods of treating multidrug resistance in cancerous cells with phosphodiesterase (PDE) inhibitors, e.g., PDE5 inhibitors. More specifically, the invention relates to methods of treating multidrug resistance that arises, e.g., during administration of chemotherapeutic/antineoplastic (anticancer) agents for treatment of cancer, with a PDE5 inhibitor (e.g., sildenafil, vardenafil, and tadalafil). The invention also relates to methods of treating cancer, e.g., multidrug resistant cancer, using a PDE5 inhibitor in combination with an antineoplastic therapeutic agent. Further, the invention relates to pharmaceutical compositions for treating multidrug resistant cancers comprising a PDE5 inhibitor, or a combination of a PDE5 inhibitor and an antineoplastic agent.Type: ApplicationFiled: March 17, 2014Publication date: September 25, 2014Applicant: St. John's UniversityInventors: Zhe-Sheng CHEN, Zhi SHI, Charles R. ASHBY
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Patent number: 8841300Abstract: A new treatment methodology and pharmacological composition for the treatment and remission of Parkinson's Disease and other neurological diseases are provided. The medication and treatment are based on the use of a combination of a phosphodiesterase inhibitor medication, commonly used to treat male erectile dysfunction, and a high-dose of serotonergic synaptic reuptake inhibitor medication, commonly used to treat depression, anxiety disorders, obsessive compulsive disorder and various panic phobias. The treatment regime is based upon the discovery that the primary cause of PD and various other related neurological conditions is dysfunction in the serotonergic pathways involving the brainstem, nucleus of Raphe, and various projecting serotonergic fibers.Type: GrantFiled: October 2, 2006Date of Patent: September 23, 2014Inventor: Jerry M. Held
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Publication number: 20140271701Abstract: The present invention concerns antibodies recognizing Mycobacterium avium paratuberculosis epitopes able to cross-reacting with the beta-cell antigen ZnT8 to be used as early biomarkers of type 1 diabetes, epitopes for in vitro prognostic and diagnostic methods suitable to reveal a risk to develop type 1 diabetes, therapies for the prevention of T1D by avoiding, controlling or monitoring Mycobacterium paratuberculosis infection.Type: ApplicationFiled: October 25, 2012Publication date: September 18, 2014Inventors: Leonardo Antonio Sechi, Roberto Mallone
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Publication number: 20140275099Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the treatment comprises administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection, wherein the treatment lasts for 12 weeks, and said at least two direct acting antiviral agents comprise (a) Compound 1 or a pharmaceutically acceptable salt thereof and (b) Compound 2 or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: Barry M. Bernstein, Sandeep Dutta, Wei Liu, Thomas J. Podsadecki, Andrew L. Campbell, Rajeev M. Menon, Chih-Wei Lin, Tianli Wang, Walid M. Awni
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Publication number: 20140275098Abstract: Provided are formulations comprising therapeutically effective amounts of ambrisentan or a pharmaceutically acceptable salt thereof and tadalafil or a pharmaceutically acceptable salt thereof and methods of treating and/or preventing pulmonary hypertension by administration of the formulations.Type: ApplicationFiled: November 13, 2013Publication date: September 18, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Luiz Belardinelli, Hunter Campbell Gillies, Faquan Liang, John Shryock, Suya Yang
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Publication number: 20140274896Abstract: This invention is in the area of improved compounds and methods for transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC), from the damage associated with ionizing radiation (IR) exposure using selective radioprotectants.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: G1 THERAPEUTICS, INC.Inventors: Norman E. Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
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Publication number: 20140275056Abstract: The present invention is directed to a compound of Formula (I): The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael A. Letavic, Dale A. Rudolph
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Publication number: 20140271466Abstract: This invention is in the area of improved compounds for and methods of treating selected RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, improved treatment of select RB-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as highly selective and, in certain embodiments, short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: G1 THERAPEUTICS, INC.Inventors: Norman E. Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
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Publication number: 20140271847Abstract: There is disclosed a formulation for creating a rapid penile erection within 30 minutes. In an embodiment, a lozenge has a preparation configured to create a rapid penile erection. The preparation is effective to create the rapid penile erection with sildenafil citrate in a range of 50-100 mg. The preparation is effective to create the rapid penile erection with tadalafil in a range of 5-40 mg. The preparation is effective to create the rapid penile erection with vardenafil hydrochloride in a range of 5-40 mg. In various embodiments, the formulation includes a solvent configured to permeate skin. Other embodiments are also disclosed.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Ray L. Hauser, BoLin Zheng
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Publication number: 20140275067Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: G1 Therapeutics, Inc.Inventors: Norman E. Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
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Publication number: 20140275066Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: G1 THERAPEUTICS, INC.Inventors: Norman E. Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares