Abstract: Described herein are methods for treating transthyretin (TTR) amyloidosis in a subject. The methods include specific dosing regimens that have great efficacy in treating the subjects and that are well tolerated in subjects.
Abstract: The present disclosure relates to a novel use of a sesquiterpene derivative, more particularly to a composition for preventing, improving or treating macular degeneration or macular edema caused by vascular leakage in the eye, the composition containing a sesquiterpene derivative compound represented by Chemical Formula 1 of the present disclosure or a pharmaceutically acceptable salt thereof as an active ingredient. Whereas the intraocular disease-related treating agents available in the market should be injected directly into the vitreous cavity, thus causing pain and side effects, the sesquiterpene derivative compound of the present disclosure is delivered to the target tissue (eye) via different administration routes (oral, intraperitoneal, etc.) other than the intravitreal route. Accordingly, the sesquiterpene derivative compound provides excellent therapeutic effect without being restricted by the administration routes.
Type:
Application
Filed:
October 14, 2016
Publication date:
September 26, 2019
Applicant:
KOOKMIN UNIVERSITY INDUSTRY ACADEMY COOPERATION FOUNDATION
Abstract: The present invention relates generally to methods of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight loss-promoting anti-convulsant either alone or in combination with bupropion or metabolites thereof or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.
Abstract: Disclosed are methods of treating cancer using a combination of an immunotherapeutic agent, such as, for example, a PD-1, PD-L1 or CTLA-4 checkpoint inhibitor, and a glutamate modulating agent such as riluzole or trigriluzole. Pharmaceutical compositions including the immunotherapeutic agents and glutamate modulating agents are also disclosed.
Abstract: The present invention relates to applications of a novel thiazole derivative in treating ulcerative colitis and in the preparation of drugs for treating ulcerative colitis.
Abstract: Pharmaceutical compositions comprising a combination of a Class I isoform-selective histone deacetylase inhibitor and a protein kinase C modulator are described as well as methods of using these compositions for treating HIV-1 latency.
Type:
Application
Filed:
November 9, 2017
Publication date:
September 26, 2019
Inventors:
Alexander B. Barnes, George Kyei, Brice Albert
Abstract: The disclosure relates to compositions and methods of preventing or treating a subject suffering from opioid toxicity or overdose. The method comprises administering to a patient in need of treatment an effective amount of methocinnamox.
Abstract: A method for the prevention of the onset of pulmonary oxygen toxicity and/or reduction of decrements of pulmonary function due to pulmonary oxygen toxicity comprising administration of a prophylactically effective amount of an anticholinergic, optionally together with a pharmaceutically acceptable excipient.
Type:
Application
Filed:
March 26, 2019
Publication date:
September 26, 2019
Inventors:
Aaron A. Hall, William A. Cronin, Richard T. Mahon, William R. Johnson
Abstract: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
Type:
Application
Filed:
November 1, 2018
Publication date:
September 26, 2019
Inventors:
James Densmore Copp, Ann W. Newman, Anne Luong
Abstract: This application relates to a method of treatment with tradipitant, and more particularly, to a method of treatment of pruritus with tradipitant.
Type:
Application
Filed:
June 4, 2019
Publication date:
September 26, 2019
Inventors:
Mihael H. Polymeropoulos, Louis William Licamele
Abstract: This application relates to a method of treatment with tradipitant, and more particularly, to a method of treatment of pruritus with tradipitant.
Type:
Application
Filed:
June 4, 2019
Publication date:
September 26, 2019
Inventors:
Mihael H. Polymeropoulos, Louis William Licamele
Abstract: The present invention relates to a Pim kinase inhibitor compound that can be used alone or in a pharmaceutical combination. One such combination comprises (a) a JAK inhibitor compound, (b) a Pim kinase inhibitor compound, and optionally, at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the treatment of a myeloid neoplasm or leukemia; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of myeloid neoplasm or leukemia; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a mammal, especially a human.
Type:
Application
Filed:
June 14, 2019
Publication date:
September 26, 2019
Inventors:
Zhu Alexander Cao, Abdel Saci, K. Gary J. Vanasse, Joseph Daniel Growney
Abstract: Provided are a niraparib sustained and controlled release pharmaceutical composition and use thereof. The sustained and controlled release pharmaceutical composition contains dissolution-improved niraparib and a matrix polymer used for regulating release rate; the steady-state plasma concentration trough value Cmin,ss of the pharmaceutical composition is 0.5-4 ?M; the steady-state plasma concentration peak value Cmax,ss is 0.8-6 ?M.
Abstract: The present invention provides combination therapy that includes an MDM2 inhibitor and one or more additional pharmaceutically active agents, particularly for the treatment of cancers. The invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers.
Type:
Application
Filed:
December 21, 2018
Publication date:
September 26, 2019
Inventors:
Sean Caenepeel, Jude Canon, Paul Hughes, Jonathan D. Oliner, Richard J. Rickles, Anne Y. Saiki
Abstract: It is an object of the present invention to provide a solid pharmaceutical composition, which can suppress a reduction in the content of an active ingredient caused by decomposition of rapamycin or a derivative thereof due to light irradiation, can ensure long-term stability, and has high storage convenience. In the present invention, the inventors have found that a preparation comprising rapamycin or a derivative thereof wherein a iron oxide is dispersed in the preparation can ensure light stability of the active ingredient, thereby completing the present invention. The present invention relates to a solid pharmaceutical preparation comprising rapamycin or a derivative thereof and iron oxide, wherein the iron oxide is dispersed in the solid pharmaceutical preparation.
Abstract: The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.
Type:
Application
Filed:
February 14, 2019
Publication date:
September 26, 2019
Inventors:
Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying Wang, Jason Brewer, Anil Vasudevan, Yanbin Lao, Charles Hutchins, Hongyu Zhao, Huan-Qiu Li
Abstract: The present invention relates to a sterile pharmaceutical composition comprising tiotropium or a pharmaceutically acceptable salt thereof, for inhalation via nebulization to a subject (e.g. a human). The invention also relates to a process for preparing the pharmaceutical composition and its use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease (COPD) in a subject.
Abstract: The invention provides therapeutic compositions that contain an inhibitor of dihydroorotate dehydrogenase (DHODH) and promote sustained elevation of dihydroorotate (DHO) levels in a patient. The compositions are useful for treating disorders associated with unregulated DHODH activity, such as acute myeloid leukemia. The invention also provides methods of determining therapeutically effective doses of compositions that contain a DHODH inhibitor. The invention further provides methods of synthesis of 2-(2?-halo-1-1?-biphenyl-4-yl)-quinoline carboxylic acids, which are useful as DHODH inhibitors.
Abstract: The invention provides methods of treating brain cancer by providing an agent that inhibits an enzyme in a metabolic pathway in a cancer cell. In some methods of the invention, the agent is an inhibitor of dihydroorotate dehydrogenase. The invention also provides methods of determining a dosage of the therapeutic agent based on measured levels of a metabolite in the pathway.
Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
Type:
Application
Filed:
October 26, 2018
Publication date:
September 26, 2019
Inventors:
Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
Abstract: The present invention encompasses compounds of formula (I) wherein the groups R2 to R5, A, X and q have the meanings given in the claims and specification, their use as inhibitors of CDK8/19, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
Type:
Application
Filed:
May 19, 2017
Publication date:
September 26, 2019
Inventors:
Harald ENGELHARDT, Heribert ARNHOF, Sebastian CAROTTA, Marco Hans HOFMANN, Marc KERENYI, Dirk SCHARN
Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a hydrolyzable moiety.
Abstract: Compositions and methods for treatment of conditions affecting skin and/or mucosal surfaces of a subject that make use of an imidazoquinoline compound and a retinoid agent are described.
Abstract: The present invention relates to the field of skin and/or hair repair, for therapeutic and cosmetic purposes. It more specifically relates to an agent stimulating the 5-hydroxytryptamine 1B receptor, for use for boosting skin and/or hair repair.
Type:
Application
Filed:
July 13, 2017
Publication date:
September 26, 2019
Inventors:
Raphael GAILLARD, Fabrice Bruno CHRETIEN, Pierre ROCHETEAU, Nicolas TORNO
Abstract: Methods of treating mitochondrial fatty acid b-oxidation and/or transport disorders arising from mutant proteins in the mitochondrial fatty acid ?-oxidation and transport metabolic pathways in patients are provided. The methods modulate the mitochondrial fatty acid ?-oxidation pathway at the last step so that the product of the mutant protein accumulates and stabilizes the mutant protein and/or the substrate(s)/product(s) of the down stream reactions accumulate and possibly bind to allosteric sites on the mutant protein to stabilize it. Trimetazidine pharmacodynamics function as such in the ?-oxidation pathway. Further, a synergistic effect is observed where trimetazidine and PPAR? agonist combination enhanced enzyme activity and presence significantly more than either alone.
Abstract: Compositions and methods of using nintedanib for improving the success rate of glaucoma filtration surgery are disclosed herein. Nintedanib can be used alone or in combination with an anti-metabolite drug in a topical or implant eye formulation.
Abstract: Therapeutic methods of treating chronic lymphocytic leukemia (CLL) and small lymphocytic leukemia (SLL) are described. In certain embodiments, the invention includes therapeutic methods of treating CLL and SLL using a BTK inhibitor. In certain embodiments, the invention includes therapeutic methods of treating subtypes of CLL and SLL using a BTK inhibitor, including subtypes of CLL in patients sensitive to thrombosis and subtypes of CLL that increase monocytes and NK cells in peripheral blood after treatment with a BTK inhibitor. In certain embodiments, the invention includes therapeutic methods of treating CLL and SLL using a combination of a BTK inhibitor and an anti-CD20 antibody.
Type:
Application
Filed:
March 11, 2019
Publication date:
September 26, 2019
Inventors:
Ahmed Hamdy, Wayne Rothbaum, Raquel Izumi, Brian Lannutti, Todd Covey, Roger Ulrich, Dave Johnson, Tjeerd Barf, Allard Kaptein
Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
Type:
Application
Filed:
February 14, 2019
Publication date:
September 26, 2019
Inventors:
Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying Wang, Jason Brewer, Anil Vasudevan, Yanbin Lao, Charles Hutchins, Hongyu Zhao, Huan-Qiu Li
Abstract: Provided are methods and compositions for the treatment of cancer. The methods comprise administering to a subject an HDAC inhibitor and an immunotherapeutic agent. In certain instances the immunotherapeutic is an NK cell or a chimeric antigen receptor NK cell.
Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: (I), (II) where the definitions of the variables are provided herein.
Type:
Application
Filed:
November 3, 2017
Publication date:
September 26, 2019
Applicant:
AMGEN INC.
Inventors:
Yinhong CHEN, Mikkel V. DEBENEDETTO, Paul John DRANSFIELD, James S. HARVEY, Jonathan HOUZE, Aarif Yusuf KHAKOO, Su-Jen LAI, Zhihua MA, Nobuko NISHIMURA, Vatee PATTAROPONG, Gayathri SWAMINATH, Wen-Chen YEH, Philip Dean RAMSDEN, Ankit SHARMA
Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: (I) (II) where the definitions of the variables are provided herein.
Type:
Application
Filed:
November 3, 2017
Publication date:
September 26, 2019
Applicant:
AMGEN INC.
Inventors:
Yinhong CHEN, Paul John DRANSFIELD, James S. HARVEY, Julie Anne HEATH, Jonathan HOUZE, Aarif Yusuf KHAKOO, David J. KOPECKY, Su-Jen LAI, Zhihua MA, Nobuko NISHIMURA, Vatee PATTAROPONG, Gayathri SWAMINATH, Wen-Chen YEH, Philip Dean RAMSDEN
Abstract: Compounds of Formula 1 as inhibitors of protein tyrosine phosphatase SHP2 are disclosed. The pharmaceutical compositions comprising compounds of Formula 1, methods of synthesis of these compounds, methods of treatment for diseases associated with the aberrant activity of SHP2 such as cancer using these compounds or compositions containing these compounds are also disclosed.
Abstract: Disclosed are formulations/compositions comprising a BTK inhibitor, particularly ibrutinib: as well as processes for preparing such formulations/compositions and methods of treatment of a disease or condition that comprises the use of such formulations/compositions.
Abstract: The present invention provides compositions and methods for the treatment of neoplasms, in particular, by targeting of quiescent cancer cells with therapeutic agents in combination with other treatments effective against certain neoplastic conditions, in particular, anti-cancer treatment with therapeutic agents that are inhibitors of mitosis (a mitotic inhibitor).
Type:
Application
Filed:
June 10, 2019
Publication date:
September 26, 2019
Inventors:
Maria Vilenchik, Michael Frid, Alexandra Kuznetsova, Yuriy Gankin, Marc Duey
Abstract: The present invention relates to the use of Volasertib or a salt thereof or the hydrate thereof for treating patients suffering from solid malignancies including advanced or metastatic solid malignancies comprising a high frequency administration of Volasertib according to a specific dosage schedule.
Type:
Application
Filed:
June 13, 2019
Publication date:
September 26, 2019
Inventors:
Tillmann TAUBE, Gerd Michael MUNZERT, Dorothea RUDOLPH
Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH; W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N; R1 and R2 are independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrenc
Type:
Application
Filed:
May 17, 2017
Publication date:
September 26, 2019
Inventors:
Doriano FABBRO, Paul HEBEISEN, Petra HILLMANN-WUELLNER, Anton STUETZ, John T. SEYKORA, Florent BEAUFILS
Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Type:
Application
Filed:
April 1, 2019
Publication date:
September 26, 2019
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux, Jinwang Xu, Kevin Michael Cottrell, Mark A. Morris, Nathan D. Waal, John J. Court, Wenxin Gu, Hongbo Deng
Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
Type:
Application
Filed:
April 23, 2019
Publication date:
September 26, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Kimberly VANOVER, Peng LI, Sharon MATES, Robert DAVIS, Lawrence P. WENNOGLE
Abstract: Disclosed is a method for treating a condition associated with hyperproliferating cells, the method including the steps of administering to a subject having the condition a composition including at least one cannabinoid receptor agonist, optionally administering to the subject a photodynamic compound, and administering radiation to the subject in whom the at least one cannabinoid receptor agonist is present so as to treat the condition.
Abstract: Disclosed herein are compounds, compositions and methods for the treatment of neurological, psychiatric disorders which are characterised by a fundamental disruption of social behaviour, and substance use disorders. In particular, disclosed herein are compounds of Formula (I), or salts or prodrugs thereof. Methods of treating or preventing neurological, psychiatric disorders and substance use disorders, using compounds of Formula (I), or salts and prodrugs are also disclosed.
Type:
Application
Filed:
July 6, 2016
Publication date:
September 26, 2019
Inventors:
Iain Stewart MCGREGOR, Michael KASSIOU, Michael Thomas BOWEN, Callum HICKS, William JORGENSEN
Abstract: The present disclosure provides for methods of treating or preventing a cardiovascular disorder and/or a related pulmonary disorder in a subject. In certain embodiments, the method comprises administering a therapeutically effective amount of an inhibitor of Glucose-6-phosphate dehydrogenase (G6PD), or a pharmaceutically acceptable salt, non-salt amorphous form, solvate, poly-morph, tautomer or prodrug thereof.
Abstract: An injectable, flowable composition, kits that include the same, and methods of medical treatment of a mammal (e.g., human) that include the administration of the same are provided.
Abstract: Disclosed are compositions, methods of treatment using the compositions and methods of preparing the compositions for the treatment of acne vulgaris. The compositions include succinic acid and an API selected from the group consisting of salicylic acid, azelaic acid, picolinic acid, benzoyl peroxide, antibiotic, retinoid and combinations thereof in a pharmaceutically acceptable preparation. The compositions that include the combination of succinic acid and another API produce improved efficacy in treating acne vulgaris.
Abstract: The present disclosure provides a one-stop surgical method of coronary intervention therapy combined with endovascular aortic repair. The present disclosure specifically provides for the sequential implementation of endovascular aortic repair and coronary intervention therapy in a patient. The present disclosure belongs to the field of medical treatment, and the implementation of the present disclosure has the following advantages: (1) one-stop treatment of two kinds of diseases not only avoids the contradiction in anti-platelet treatment during separate surgeries, but also minimise the potential risk of the separate surgeries; (2) the patient only undergoes one anesthesia and one surgical process for the treatment of two diseases, which is easier to be accepted psychologically; and (3) hospitalization expenses and total hospitalization duration are reduced, and medical resource consumption is reduced.
Abstract: Oral dosage forms of osteoclast inhibitors, such as neridronic acid, in an acid or a salt form, can be used to treat or alleviate pain or related conditions, such as complex regional pain syndrome.
Abstract: Oral dosage forms of osteoclast inhibitors, such as neridronic acid, in an acid or a salt form, can be used to treat or alleviate pain or related conditions, such as complex regional pain syndrome.