Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.
Type:
Grant
Filed:
January 22, 2016
Date of Patent:
May 8, 2018
Assignee:
VERSEON CORPORATION
Inventors:
Kevin Michael Short, Son Minh Pham, David Charles Williams, Somalee Datta
Abstract: A method of compounding a transdermal cream may include grinding one or more tablets of a Non-Steroidal Anti-Inflammatory Drug (NSAID) and one or more nerve depressants, anticonvulsants, or combinations thereof to produce a fine powder. The find powder may be wetted and added to an eutectic mixture of lidocaine and prilocaine in an emulsified topical cream in the form of a lidocaine 2.5%-prilocaine 2.5% cream. The compounded transdermal may include between 0.05% and 0.15% by weight meloxicam, between 1.0% and 5.0% by weight gabapentin, and at least 80% by weight of the lidocaine 2.5%-prilocaine 2.5% cream.
Abstract: A series of substituted benzotriazole derivatives, being potent modulators of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
Type:
Grant
Filed:
December 8, 2014
Date of Patent:
May 1, 2018
Assignee:
UCB BIOPHARMA SPRL
Inventors:
Daniel Christopher Brookings, Boris Kroeplien
Abstract: Methods and compounds for treating, preventing, reducing the risk of and/or delaying the onset of a microbial infection in a subject are disclosed herein, wherein the microbial infection is caused by one or more microorganisms (e.g., one or more bacteria) which can be used as a biological weapon, such as Bacillus anthracis, Franciscella tularensis, Yersinia pestis, Burkholderia mallei, and Burkholderia pseudomallei. Also disclosed are pharmaceutical compositions or kits for treating, preventing, reducing the risk of and/or delaying the onset of a microbial infection.
Abstract: A thermoformed pharmaceutical dosage form having a breaking strength of at least 300 N, said dosage form comprising a pharmacologically active ingredient (A), a free physiologically acceptable acid (B) in an amount of from 0.001 wt.-% to 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form, and a polyalkylene oxide (C) having a weight average molecular weight Mw of at least 200,000 g/mol.
Type:
Grant
Filed:
September 1, 2015
Date of Patent:
March 27, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Lutz Barnscheid, Eric Galia, Sebastian Schwier, Ulrike Bertram, Anja Geissler, Kornelia Griessmann, Johannes Bartholomäus
Abstract: The invention relates to crystalline forms of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone, processes for the preparation thereof, pharmaceutical compositions containing such crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as a medicament, especially as orexin receptor antagonists.
Type:
Grant
Filed:
December 2, 2014
Date of Patent:
March 13, 2018
Assignee:
IDORSIA PHARMACEUTICALS LTD
Inventors:
Christoph Boss, Christine Brotschi, Markus Gude, Bibia Heidmann, Thierry Sifferlen, Markus Von Raumer, Jodi T. Williams
Abstract: This invention relates to novel agents that are analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
Type:
Grant
Filed:
February 6, 2014
Date of Patent:
February 27, 2018
Assignee:
Syntarga B.V.
Inventors:
Patrick Henry Beusker, Henri Johannes Spijker, Johannes Albertus Frederikus Joosten, Tijl Huijbregts, Franciscus Marinus Hendrikus De Groot
Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.
Abstract: A tetrazolinone compound represented by formula (1): wherein Q represents a 6-membered aromatic heterocyclic group optionally having one or more atoms or groups selected from Group P1, provided that a heteroatom constituting the heterocyclic group is a nitrogen atom, and the number of nitrogen atom is 1, 2, or 3; R1, R2, R3, and R11 each represents a C1-C6 alkyl group optionally having one or more atoms or groups selected from Group P2; R4 and R5 each represents a hydrogen atom, etc.; R6 represents a C1-C6 alkyl group optionally having one or more halogen atoms, etc.; R7, R8, and R9 each represents a hydrogen atom, etc.; and X represents an oxygen atom or a sulfur atom, has excellent control activity against pests.
Abstract: This solid pharmaceutical composition is useful as a solid pharmaceutical composition of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol, which is excellently elutable and moldable and is stable in long-term storage, or a salt thereof.
Abstract: Described are personal care, preferably skin care compositions, comprising polyolefin blends comprising at least one metallocene catalyzed polyolefin with a density above 0.90 g/cm3, at least one metallocene catalyzed polyolefin with a density equal to or below 0.90 g/cm3, provided that the average melt index for the polyolefin blend is greater than 7; and a cosmetically acceptable hydrocarbon oil, provided that the composition does not contain ethylene acrylic copolymer.
Type:
Grant
Filed:
September 18, 2013
Date of Patent:
January 23, 2018
Assignees:
Dow Global Technologies LLC, Rohm and Haas Company
Inventors:
Ying O'Connor, Curtis Schwartz, Qichun Wan, Thomas H. Peterson, Thomas P. Clark, John W. Kramer
Abstract: This disclosure generally relates to methods for reducing the risk of preterm birth in a pregnant human female patient that include subcutaneous administration of HPC. The disclosure relates in part to the discovery that subcutaneous administration of HPC is actually feasible and can result in sufficient plasma levels of HPC in pregnant patients that can reduce the risk of preterm birth.
Abstract: Metformin salts of 2,4-thiazolidinediones are described for the treatment of diabetes mellitus Type2, gestational diabetes, polycystic ovary syndrome, non-alcoholic fatty liver disease, coronary artery disease, pancreatic cancer, premature puberty, and other diseases which manifest insulin resistance.
Abstract: The present specification discloses compositions comprising at least one therapeutic compound capable of modulating androgen production and methods and uses for treating a disorder associated with androgen production using such compositions and/or compounds.
Type:
Grant
Filed:
February 27, 2017
Date of Patent:
November 7, 2017
Assignee:
Tangent Reprofiling Limited
Inventors:
Suzanne Dilly, Gregory Stoloff, Paul Taylor
Abstract: The present invention is directed to antiviral compositions that provide efficacy against non-envelope viruses such as noroviruses. The antiviral compositions comprise an alkyl 2-hydroxycarboxylic acid and an effective amount of a sulfonated surfactant. The composition may be used as a topical on human skin, as a hand sanitizer or as a hard surface cleaning composition.
Type:
Grant
Filed:
March 12, 2013
Date of Patent:
November 7, 2017
Assignee:
Ecolab USA Inc.
Inventors:
Daniel E. Pedersen, Hilina Emiru, Carter Martin Silvernail
Abstract: This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.
Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
Abstract: The present invention relates to a composition comprising at least a sesterterpene for use as medicament like antibiotic or antifungal. Furthermore, the present invention relates to the use of at least a sesterterpene for increasing, assisting and/or enhancing the bacteriostatic and/or bactericidal activity of an antibiotic or the fungicidal activity of an antifungal compound.
Abstract: The present invention provides matriptase inhibitors and compositions for treating and preventing orthomyxovirus infections such as flu infections. The present invention also provides novel compounds, compositions, methods of use, uses and kits thereof for inhibiting matriptase. Such compounds are useful for treating and preventing orthomyxovirus infections, such as flu infections, and for inhibiting tumor growth, progression and/or metastasis.
Type:
Grant
Filed:
November 17, 2015
Date of Patent:
September 5, 2017
Assignee:
SOCPRA SCIENCES SANTE ET HUMAINES S.E.C.
Inventors:
Martin Richter, Richard Leduc, Eloic Colombo, Eric Marsault
Abstract: Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).
Type:
Grant
Filed:
April 25, 2014
Date of Patent:
August 29, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jongwon Lim, Xianhai Huang, Ronald D. Ferguson, Wei Zhou, Christopher W. Boyce, Phieng Siliphaivanh, David J. Witter, Milana M. Maletic, Joseph A. Kozlowski, Kevin J. Wilson