Abstract: An object of the present invention is to provide a probe for imaging a ?-sheet structure protein which can be used for the diagnosis of conformational diseases, particularly disease (tauopathy) having a cardinal symptom such as intracerebral accumulation of tau protein, for example, Alzheimer's disease. Another object of the present invention is to provide a compound which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or non-recognized toxicity. According to the present invention, the above problems are solved by providing a compound of a formula I (wherein A, R1, R2, R3, R4, R5, R6, Ra and Rb are as defined in the present description) or a pharmaceutically acceptable salt or solvate thereof.
Abstract: The present invention relates to the preparation of Cynara scolymus leaf extracts, which are useful for the prevention and treatment of dyslipidaemia, in particular to increase HDL cholesterol in patients at cardiovascular risk. Said extracts are useful to normalize the lipid and carbohydrate balances and significantly increase the value of HDL cholesterol by favorably changing the LDL/HDL ratio, especially in post-infarction patients with drug-induced dyslipidaemia.
Abstract: A disinfecting shower cleaner composition including a medium-chain fatty acid coupled with a nonionic surfactant providing temperature stable antimicrobial compositions. The invention specifically relates to antimicrobial compositions including fatty acid antimicrobial agents coupled with an ethoxylated amine and methods of using the antimicrobial compositions.
Type:
Grant
Filed:
March 9, 2015
Date of Patent:
June 27, 2017
Assignee:
Ecolab USA Inc.
Inventors:
Elizabeth Kiesel, Michael E. Besse, Lisa A. Hellickson, Mark Levitt, Daniel E. Pedersen
Abstract: The present inventions concerns derivatives of aminocyclobutane, particularly as NMDA receptor antagonists, their application in human therapy and their method of preparation. These compounds correspond to the general formula (1): wherein: X1 represents a hydrogen atom or fluorine atom; X2 is a hydrogen atom or fluorine atom or chlorine atom; R1 represents a hydrogen atom or fluorine atom or chlorine atom or methyl group or methoxy group or cyano group; R2 represents independently or together a methyl group or ethyl group.
Type:
Grant
Filed:
September 12, 2016
Date of Patent:
June 27, 2017
Assignee:
PIERRE FABRE MEDICAMENT
Inventors:
Bernard Vacher, Elodie Blanc, Ronan Depoortere
Abstract: It is an object of the present invention to provide a novel form of (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, which is useful for preventing and/or treating diseases such as dyslipidemia. (S)-trans-{4-[({2-[({1-[3,5-bis(Trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid hydrochloride.
Abstract: A method for rapid delivery of an active compound to innervate a cranial nerve of a subject. Also provided is a method for treating a disease or condition by topically applying a pharmaceutical composition to the face excluding the palpebral part of the eye, in an amount effective for treating the disease or condition.
Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
Type:
Grant
Filed:
June 18, 2015
Date of Patent:
June 6, 2017
Assignees:
Abbvie B.V., AbbiVie Inc.
Inventors:
Pieter Smid, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Leonardus A. J. M. Sliedregt, Maria J. P. van Dongen, Jacobus A. J. den Hartog, Adrian Hobson
Abstract: An object of the present invention is to provide a therapeutic preparation and method for diseases associated with cartilage loss, cartilage degeneration and/or cartilage thinning. The present invention provides a therapeutic preparation comprising a pterosin derivative or a pharmaceutically acceptable salt thereof for diseases associated with cartilage loss, cartilage degeneration and/or cartilage thinning; and a therapeutic method for the diseases.
Abstract: The present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of increasing the ratio of dopaminergic neuronal to noradrenergic neuronal activity within the central nervous system and particularly the hypothalamus of the central nervous system of the patient.
Abstract: The present disclosure refers to a synergistic blend of heptyl glucoside and olive oil derivatives, which is included as a natural solubilizer agent in transdermal compositions to improve API solubilization. Improved solubilization of APIs increases the absorption of APIs into the patient's bloodstream resulting in desired levels of hormones. Reduction of the amount of APIs within the transdermal compositions to achieve the desired levels of hormones will reduce symptoms of hormone deficiency. The synergistic blend within transdermal compositions functions as a solubilizer agent, which allows complete dissolution of hormones, improves water solubility and increases skin permeation. Hormones that can be used in transdermal compositions comprising the synergistic blend include systemically active hormones, which are delivered through the skin with the assistance of natural solubilizer agents and skin penetration enhancers to achieve a desired effect.
Type:
Grant
Filed:
April 9, 2015
Date of Patent:
May 16, 2017
Assignee:
Professional Compounding Centers of America
Abstract: Methods of treating at least one condition chosen from pain, inflammation, and fever in a critically ill patient in need thereof, comprising administering to the critically ill patient an intravenous pharmaceutical composition comprising ibuprofen using a first dosage regimen, wherein the first dosage regimen produces a first pharmacokinetic profile in critically ill patients that is about equivalent to a second pharmacokinetic profile produced by administration of the intravenous pharmaceutical composition using a second dosage regimen of ibuprofen to non-critically ill patients, wherein the at least one condition of the critically ill patient is thereby treated.
Abstract: Compounds of the general formula I wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.
Abstract: The present disclosure relates to pharmaceutical compositions of pyrimidinedione derivative compounds and methods of preparing and uses thereof. The disclosure also relates to methods of enhancing bioavailability of pyrimidinedione derivative compounds in pharmaceutical compositions administered to a subject and methods of reducing the amount of a pyrimidinedione derivative compound in a pharmaceutical composition while achieving the same bioavailability in a subject.
Type:
Grant
Filed:
October 18, 2013
Date of Patent:
April 25, 2017
Assignee:
AbbVie Inc.
Inventors:
Yanxia Li, Ping Gao, Yi Shi, Geoff G. Zhang, Yi Goa, Jianwei Wu
Abstract: The present invention relates to a synergistic pharmaceutical composition comprising Compound C2 (Neo-isopulegol), C3 (Iso-pulegol) and C4 (Citronellol) derived from herbal seed extract of Litsea cubeba useful for the treatment of lung cancer. The present invention also relates to the activity of compounds C2 or C3 or C4 either alone or in combination in killing of A549 lung cancer cells.
Type:
Grant
Filed:
September 5, 2012
Date of Patent:
April 18, 2017
Assignee:
Council of Scientific & Industrial Research
Abstract: Embodiments of the invention relate to compositions for topical administration to dogs and cats comprising the active components dinotefuran and flumethrin, and methods for the treatment and prevention of flea and tick infestation comprising topical administration of such compositions.
Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
Type:
Grant
Filed:
April 7, 2016
Date of Patent:
April 11, 2017
Assignee:
Roche Palo Alto LLC
Inventors:
Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
Abstract: Contemplated compounds, compositions, and methods are presented for use in the treatment, or prevention, of a cognitive, neurodegenerative or neuronal disorder or disease, such as Alzheimer's disease.
Abstract: A pharmaceutical composition comprising an active contraceptive drug and one or more pharmaceutically-acceptable excipients. The pharmaceutical composition, when subjected to an in vitro dissolution test according to the USP XXIII Paddle Method, results in no more than 50% of said active drug initially present being dissolved within 30 minutes, and at least 50% of the active drug being dissolved in a time range from about 3 hours to about 4 hours. The pharmaceutical composition is administered daily to a patient having a BMI of about 25 kg/m2 or more for at least a portion of a treatment cycle. The pharmaceutical composition does not cause a number of days of bleeding events in the patient exceeding an average of 15% per treatment cycle in consecutive treatment cycles of administration after an initial treatment cycle of administration.
Type:
Grant
Filed:
June 23, 2015
Date of Patent:
March 28, 2017
Assignee:
LABORATORIOS LEON FARMA SA
Inventors:
Philippe Perrin, Dominique Drouin, Cécile Boyer-Joubert
Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
Type:
Grant
Filed:
August 5, 2014
Date of Patent:
February 14, 2017
Assignee:
ChemoCentryx, Inc.
Inventors:
Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang