Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
Type:
Application
Filed:
January 2, 2020
Publication date:
May 7, 2020
Inventors:
Peter Tai Wah Cheng, Robert F. Kaltenbach, III, Jun Li, Jun Shi, Yan Shi, Shiwei Tao, Hao Zhang, Suresh Dhanusu, Kumaravel Selvakumar, Ramesh Babu Reddigunta, Steven J Walker, Lawrence J. Kennedy, James R. Corte, Tianan Fang, Sutjano Jusuf
Abstract: The invention disclosed herein is directed to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a therapeutically effective amount of a selective PPAR? antagonist.
Type:
Application
Filed:
December 20, 2019
Publication date:
May 7, 2020
Inventors:
Nicholas Simon STOCK, Austin Chih-Yu CHEN, Yalda Mostofi BRAVO, Jason Duarte JACINTHO, Jill Melissa BACCEI, Brian Andrew STEARNS, Ryan Christopher CLARK
Abstract: The present invention is directed to methods of inhibiting LTA4-h in a human patient and method of treating a condition ameliorated by the inhibition of leukotriene A4 hydrolase activity in a human patient comprising administering to said human patient the compound, 4-{5-[4-(4-Oxazol-2-yl-phenoxy)-benzyl]-2,5-diaza-bicyclo[2.2.1]hept-2-ylmethyl}-benzoic acid.
Type:
Application
Filed:
June 17, 2019
Publication date:
May 7, 2020
Inventors:
Eric B. Springman, Margaret McCrann Pugh, Lopa Bhatt, Ralph Grosswald
Abstract: The present invention relates to a combination of zonisamide with pramipexole or a pharmaceutically acceptable salt or solvate of pramipexole for treating a synucleinopathy.
Type:
Application
Filed:
May 23, 2018
Publication date:
May 7, 2020
Applicant:
CHASE THERAPEUTICS CORPORATION
Inventors:
Thomas N. CHASE, Kathleen E. CLARENCE-SMITH
Abstract: The present invention provides methods and compositions for treating bladder cancer, including metastatic bladder cancer and non-muscle-invasive bladder cancer, by administering a composition comprising nanoparticles that comprise mTOR inhibitor and optionally an albumin.
Abstract: In alternative embodiments, provided are pharmaceutical compositions and methods for treating, ameliorating, reversing and/or preventing (acting as a prophylaxis) autism, e.g., regressive autism. In alternative embodiments, these pharmaceutical compositions and methods are dosaged and administered to children in need thereof. In alternative embodiments, pharmaceutical compositions and methods are dosaged, formulated and dosaged as solid, liquid or aerosol preparations or formulations. In alternative embodiments, pharmaceutical compositions comprise rifaximin as the sole antibiotic, or rixafimin and other antimicrobial or antibiotic agent, for example, vancomycin, metronidazole, tinidazole or a combination thereof.
Abstract: The present invention provides methods for predicting or determining a subject's response to an antiplatelet agent, and methods for determining a subject's suitability to a treatment regime or intervention for a disease associated with platelet aggregation, using analysis of genetic polymorphisms. The present invention also relates to the use of genetic polymorphisms in assessing a subject's response to an antiplatelet agent.
Type:
Application
Filed:
May 9, 2019
Publication date:
May 7, 2020
Inventors:
Patrick A. Gladding, Marja-Liisa Dahl, Mark W. Webster
Abstract: Compositions and methods for inhibiting and/or sensitizing or re-sensitizing a parasite to an antiparasitic drug are provided. The compositions can comprise a an arylphenoxypropionate derivative, an aryloxyphenoxyacetate derivative, an aryloxyphenylacetate derivative, one or more substituted quinols, or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, or a combination thereof in an amount and formulation sufficient to sensitize the parasite to the drug, treating infection of a patient by a parasite with a drug, or to prevent symptomatic infection of a patient by a parasite with a drug.
Type:
Application
Filed:
December 19, 2019
Publication date:
May 7, 2020
Inventors:
Manchi CM Reddy, James C. Sacchettini, Nian E. Zhou, Billy F. McCutchen
Abstract: A series of substituted spirocyclic 2-oxoindoline derivatives, and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.
Type:
Application
Filed:
June 12, 2018
Publication date:
May 7, 2020
Inventors:
Gareth Neil Brace, Rose Elizabeth Chappell, Hervé Jean Claude Deboves, Anne Marie Foley, Gregory Foulkes, Elizabeth Pearl Jones, Fabien Claude Lecomte, Joanna Rachel Quincey, Monika-Sarah Elisabeth Dorothea Schulze, Matthew Duncan Selby, Adam Peter Smalley, Richard David Taylor, Robert James Townsend, Zhaoning Zhu
Abstract: Compound I of the formula (I) and/or pharmaceutically acceptable salt(s) of Compound I comprised in a pharmaceutical composition and methods of using the same to treat cystic fibrosis.
Type:
Application
Filed:
July 17, 2018
Publication date:
May 7, 2020
Inventors:
Weichao George Chen, Eric L. Haseltine, Samuel Moskowitz, Sarah Robertson, David Waltz
Abstract: Inhibition of the expression and/or function of nicotinamide phosphoribosyltransferase (NAMPT) can reduce, prevent or reverse the pathophysiological vascular changes associated with the onset and progression of Pulmonary Fibrosis. Compositions and methods to inhibit the expression and function of NAMPT for treating and preventing Pulmonary Fibrosis in a subject in need are provided. The compositions and methods are useful for the modulation of pathophysiological processes that contribute to the development and progression of Pulmonary Fibrosis by reducing lung inflammation, aberrant myofibroblast accumulation and deposition of collagen in fibrotic foci.
Abstract: The present invention relates to a method of treatment of movement disorders, comprising administering to a patient in need thereof an effective amount of befiradol, wherein the administering step provides an average patient's maximum plasma concentration of befiradol below 15 ng/mL which occurs more than 4 hours post administration, said method minimizing side effects of dizziness and nausea. Sustained release pharmaceutical compositions that can be used according to this method are also described.
Type:
Application
Filed:
December 17, 2019
Publication date:
May 7, 2020
Applicant:
PIERRE FABRE MEDICAMENT
Inventors:
Bruno PAILLARD, Laurence DEL FRARI, Valérie BRUNNER, Adrian NEWMAN TANCREDI, Mark VARNEY
Abstract: Methods of preventing or delaying onset of myopia in pre-myopic patients and also methods of reducing or preventing progression of myopia in patients having low myopia through the use of compositions comprising less than 0.025% of atropine are disclosed.
Type:
Application
Filed:
February 20, 2018
Publication date:
May 7, 2020
Inventors:
Donald Tiang Hwee TAN, Audrey CHIA, Roger BEUERMAN, Amutha Barathi VELUCHAMY
Abstract: The present invention provides a pharmaceutical composition containing a quinoline derivative or a salt thereof. Specifically, the invention provides a pharmaceutical composition containing (R,E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)-propeneamide or a pharmaceutically acceptable salt thereof, a cross-linked polyvinylpyrrolidone, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition has a property of rapid dissolution.
Abstract: The present invention relates to methods of treating cancer, in which a CXCR4 inhibitor such as X4P-001 or a pharmaceutically acceptable salt thereof or pharmaceutical composition thereof is administered in combination with an additional therapeutic agent, such as an immune checkpoint inhibitor. The methods demonstrate surprising results, including regression of disease, with comparatively little toxicity.
Abstract: Disclosed in certain embodiments is a pharmaceutical formulation (e.g., parenteral formulation) comprising a therapeutically effective amount of nalmefene or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable adjuvant (e.g., parenterally acceptable adjuvant) that promotes the rate at which the nalmefene or salt thereof is more rapidly absorbed into the systemic circulation of a subject identified as in need thereof.
Abstract: Methods for inducing the regeneration of non-cancerous tissues in a cancer patient undergoing radiotherapy and/or chemotherapy using continuous administration of tyrosine kinase inhibitors for at least 90 days following a cancer treatment in the patient.
Abstract: The present invention relates to novel heteroaryl amide derivatives of formula (1) as selective inhibitors of histone deacetylase 1 and 2 (hdac1-2) to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said compounds for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by inhibition the activity of histone deacetylase class I, particularly HDAC1 and HDAC2, such as cancer, neurodegenerative diseases, Infectious diseases, inflammatory diseases, heart failure and cardiac hypertrophy, diabetes, polycystic kidney disease, sickle cell disease and ?-thalassemia disease and to methods for the treatment of the disesases mentioned above.
Type:
Application
Filed:
July 9, 2018
Publication date:
May 7, 2020
Inventors:
Julio CASTRO PALOMINO LARIA, Juan CAMACHO GÓMEZ, Rodolfo RODRÍGUEZ IGLESIAS
Abstract: Disclosed herein are methods of treating cholangiocarcinoma in a patient comprising: evaluating a biological sample from the patient for the presence of one or more FGFR mutants including at least the FGFR2 SNP C383R; and treating the patient with an FGFR inhibitor if one or more FGFR mutants including at least the FGFR2 SNP C383R are present in the sample.
Abstract: The present invention provides methods for detecting and/or treating a subject having an aneurysm or at risk for developing an aneurysm. It has been discovered that a key metabolite of the kynurenine (Kyn) pathway, a major route for the metabolism of essential amino acid tryptophan (Trp) into nicotinamide adenine dinucleotide (NAD+), plays a critical role in the formation of aneurysms, for example abdominal aortic aneurysms. In particular, it has been discovered that 3-Hydroxyanthranilic acid (3-HAA), a product of kynureninase (KYNU), plays a causative role in the formation of aneurysms by, for example exerting pro-inflammatory effects on vascular smooth muscle cells. It has further been discovered that elevated levels of 3-HAA are indicative of the presence and/or progression of an aneurysm, and 3-HAA levels correlate with the size (aortic diameter) of the aneurysm.
Type:
Application
Filed:
December 20, 2019
Publication date:
May 7, 2020
Applicant:
Georgia State University Research Foundation, Inc.
Abstract: The present invention describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the invention have activity as Janus Kinase inhibitors and are useful in the treatment or control of pruritus, associated with allergic dermatitis, atopic dermatitis in animals, and other disorders and indications where immunosuppression/immunomodulation would be desirable. Also described herein are methods of treating pruritus and atopic dermatitis by administering the compounds of the invention, which are JAK 1 inhibitors.
Type:
Application
Filed:
November 4, 2019
Publication date:
May 7, 2020
Inventors:
Jason D. SPEAKE, Bharathi PANDI, Joe B. PERALES, Weiming FAN
Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
Type:
Application
Filed:
May 21, 2019
Publication date:
May 7, 2020
Inventors:
Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
Abstract: The present invention relates to combinations comprising a positive allosteric modulator (“PAM”) of metabotropic glutamatergic receptor subtype 2 (“mGluR2”) or a pharmaceutically acceptable salt or a solvate thereof, or an orthosteric agonist of metabotropic glutamatergic receptor subtype 2 compound or a pharmaceutically acceptable salt or a solvate thereof, and a synaptic vesicle protein 2A (“SV2A”) ligand.
Type:
Application
Filed:
December 19, 2019
Publication date:
May 7, 2020
Inventors:
Brian D. KLEIN, Hilde LAVREYSEN, Stefan Maria, Christiaan PYPE, Roy E. TWYMAN, Nancy Eulalie, Sylvain VAN OSSELAER, H. Steven WHITE, Marc André CEUSTERS, José Maria CID-NÚÑEZ, Andrés Avelino TRABANCO-SUÁREZ, Roger Francis BONE
Abstract: The present invention relates to combinations comprising a positive allosteric modulator (“PAM”) of metabotropic glutamatergic receptor subtype 2 (“mGluR2”) or a pharmaceutically acceptable salt or a solvate thereof, or an orthosteric agonist of metabotropic glutamatergic receptor subtype 2 compound or a pharmaceutically acceptable salt or a solvate thereof, and a synaptic vesicle protein 2A (“SV2A”) ligand.
Type:
Application
Filed:
December 19, 2019
Publication date:
May 7, 2020
Inventors:
Brian D. KLEIN, Hilde LAVREYSEN, Stefan Maria, Christiaan PYPE, Roy E. TWYMAN, Nancy Eulalie, Sylvain VAN OSSELAER, H. Steven WHITE, Marc André CEUSTERS, José Maria CID-NÚÑEZ, Andrés Avelino TRABANCO-SUÁREZ, Roger Francis BONE
Abstract: The invention described herein provides a method for the treatment of an oestrogen receptor positive breast cancer in a subject in need thereof comprising administering to said subject a therapeutically effective amount of a compound capable of inhibiting MPS1, wherein: (i) said subject has previously been treated with a CDK4/6 inhibitor; and/or (ii) said breast cancer is resistant to treatment with a CDK4/6 inhibitor.
Abstract: The present disclosure provides a method of treating a subject that is resistant to one or more drugs by identifying a subject having one or more drug resistant cells; administering to the subject a pharmaceutically effective amount of an inhibitor compound, and contacting one or more drug resistant cells with the inhibitor compound to reduce the export of the inhibitor compound from the one or more drug resistant tumor cells and to block the transport of drug(s) from the one or more drug resistant cells.
Type:
Application
Filed:
December 16, 2019
Publication date:
May 7, 2020
Inventors:
John G. Wise, Pia D. Vogel, Frances K. Brewer, Courtney A. Follit
Abstract: The present invention relates to a tablet comprising Afatinib or a pharmaceutically acceptable salt thereof, wherein the tablet is obtained by direct compression. The present invention further relates to a process for manufacturing a tablet of the invention as well as the use of the tablet of the invention.
Abstract: A method of treating pain is disclosed, which involves administering an effective amount of lapatinib or a pharmaceutically-acceptable salt thereof to a subject in need of treatment for pain.
Abstract: The invention provides methods of treating endometriosis in a patient by administration of a gonadotropin-releasing hormone (GnRH) antagonist, for instance, according to dosing regimens predicated on the patient's level of anti-Müllerian hormone (AMH) or ?17-estradiol (E2).
Abstract: The present invention relates to PDEI inhibitory compounds of Formula I as described herein, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
Abstract: Aryl hydrocarbon receptor (AHR) agonists and their use for treating, preventing, or reducing the risk of necrotizing enterocolitis in premature infants are disclosed.
Type:
Application
Filed:
May 25, 2018
Publication date:
May 7, 2020
Inventors:
David Hackam, Peng Lu, Chhinder P. Sodhi, Jun O. Liu
Abstract: Described herein are pharmaceutical compositions including in combination at least one antiparasitic drug and one antiprotozoal drug. In some embodiments, the compositions can be formulated as a non-solid for oral administration. The compositions can be used to treat neurological conditions. Methods of treatment using the compositions are also described.
Type:
Application
Filed:
November 1, 2019
Publication date:
May 7, 2020
Inventors:
David Clayton Sutherland, James Kyle Zorn, Dennis J. Carlo
Abstract: Selective cancer treatment regimes based on assaying for the presence or absence of a mutation in PI3K in a blood or serum sample obtained from a patient having cancer. The cancer is treated with 5-(2,6-di-mor-pholin-4-yl-pyrimidin-4-yl)-4-trifluoromethyl-pyridin-2-ylamine or its hydrochloride salt, or (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide) on the basis that the patient is determined to have in their ctDNA a PIK3CA mutation.
Abstract: The disclosure provides a method of treating a malignant rhabdoid tumor in a subject in need thereof including administering to the subject a therapeutically-effective amount of an enhancer of a zeste homolog 2 (EZH2) inhibitor. In certain embodiments of this method the malignant rhabdoid tumor is small cell cancer of the ovary of the hypercalcemic type (SCCOHT) and the EZH2 inhibitor is tazemetostat (also known as Tazemetostat).
Abstract: This invention generally relates to substituted imidazopyridine compounds, particularly substituted 4-(imidazo[1,2-a]pyridin-2-yl)benzamide compounds and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.
Abstract: The present invention relates to compounds of formula (I). The compounds may be used to modulate the Stimulator of Interferon Genes (STING) protein and thereby treat diseases such as cancer and microbial infections.
Abstract: The present disclosure relates to a method of treating a subject with cancer with a ferroptosis inducer, including use of the ferroptosis inducer in combination with a second therapeutic agent.
Abstract: Embodiments methods of reducing an inflammatory immune response (e.g., inhibiting a Th1 response) and/or promoting a regulatory immune response (e.g., enhancing Treg(s)) in a mammal are provided where the method methods involve administering to the mammal a GABAA receptor positive allosteric modulator (PAM) in an amount sufficient to reduce an inflammatory immune response and/or to promote a regulatory immune response said mammal. In certain embodiments the PAM is administered in conjunction with a GABA receptor activating ligand (e.g., GABA).
Type:
Application
Filed:
June 20, 2018
Publication date:
May 7, 2020
Applicant:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Abstract: Methods and compositions are provided for the prevention and/or treatment of symptoms associated with lipid accumulation disorders caused by attenuated leptin activity and by lipid storage disorders. The methods involve administering at least one oxygenated cholesterol sulfate (OCS) to a subject with the disorder. The disorder may be acquired or congenital (hereditary).
Abstract: The invention provides inhibitors of ?-crystallin aggregation, including prodrugs of a steroid and/or sterol, and methods of using said ?-crystallin aggregation inhibitors to, e.g., treat or prevent cataracts in a subject having or at risk of developing cataracts.
Type:
Application
Filed:
September 30, 2019
Publication date:
May 7, 2020
Inventors:
Jason E. Gestwicki, Kathryn McMenimen, Brian DeVree, Leah Makley
Abstract: In the present invention, a new combination is disclosed comprising (i) 5-aminosalicylic acid (5-ASA) or a derivative thereof, or a pharmacologically acceptable salt thereof, and (ii) a group D vitamin, a derivative thereof, a metabolite or analogue, for use in the prevention and/or treatment of colorectal cancer (CRC). A further aspect of the invention is directed to pharmaceutical compositions comprising said combination together with at least one physiologically acceptable excipient and the use thereof in the prevention and/or in the treatment of the colorectal cancer.
Abstract: The present invention relates to a composition for treating osteoarthritis and a method for preparing the same, and more specifically, relates to a composition comprising hydrophilized sulfasalazine as an active ingredient and hyaluronic acid so as to enable effective treatment of osteoarthritis such as degenerative osteoarthritis by preventing joint wear in addition to symptom relief through intraarticular or local administration, and a method for preparing the same.
Type:
Application
Filed:
December 19, 2019
Publication date:
May 7, 2020
Inventors:
Suhwan Kim, Kyeong Woo Min, Yeong Jun Baik, Sung Hee Lee, Koo Woo, Min-Kyoung Kim
Abstract: Disclosed are formulations comprising brincidofovir. The formulations can be intravenous formulations. The formulations can be used in cases where a subject experiences gastrointestinal issues in response to oral administration of brincidofovir. The formulations can also be used in cases where oral administration of drug is not possible due to underlying conditions or concern around inadequate oral absorption.
Type:
Application
Filed:
December 20, 2019
Publication date:
May 7, 2020
Inventors:
Mohammed Anowrul KABIR, Odin Johann NADERER, Irma Marisa GROSSI
Abstract: The present invention relates to a nutritional composition comprising at least two human milk oligosaccharides, for use to decrease the concentration of detrimental proteolytic metabolites (e.g. branched short chain fatty acids) in the digestive tract in an infant or a young child.
Abstract: Provided are a composition for inhibiting immune cell proliferation, including sialyllactose or a derivative thereof as an active ingredient, and a method of inhibiting immune cell proliferation, wherein the composition and the method may decrease expression of chemokines, decrease expression of pro-inflammatory cytokines, decrease production of inflammatory mediators, decrease expression of COX2, and decrease production of PEG2, and therefore, may be useful for the prevention or treatment of atopic dermatitis or arthritis.
Type:
Application
Filed:
November 18, 2019
Publication date:
May 7, 2020
Applicant:
SYNOVIZEN CO., LTD.
Inventors:
Siyoung YANG, Jimin JEON, Li-Jung KANG, Chanmi CHO
Abstract: A method, in one embodiment, includes administering to a non-infant human an effective amount of a combination of the human milk oligosaccharides (“HMO”s) 2?-FL and DFL, where the amount of the combination of HMOs is effective for modulating the microbiota of the non-infant human and reducing one or more post-treatment condition such as pain and/or a perception of visceral pain in the non-infant human.
Type:
Application
Filed:
December 6, 2019
Publication date:
May 7, 2020
Inventors:
Bruce McConnell, Louise Kristine Vigsnæs, Gabriela Bergonzelli, Laurent Favre, Laurent Ferrier, Clara Lucia Garcia-Rodenas