Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
Abstract: A pharmaceutical composition, comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound represented by the following structural formula at least one acidifying agent; and a vehicle base comprising at least one pharmaceutically acceptable non-aqueous solvent. Values and preferred values of the variables in structural formula (I) are defined herein.
Abstract: The instant invention relates to pharmaceutical compositions containing cathespin K inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
Type:
Application
Filed:
September 5, 2017
Publication date:
December 21, 2017
Inventors:
Wayne Parent, Mahtab Afaghi, David Breslin, Mireille Granger, Lei Wang, Jeff Zimmerman
Abstract: Provided in the present invention is a compound having these structure of formula I or a pharmaceutically acceptable salt thereof. Also provided in the present invention is a pharmaceutical composition containing the compound, and a use of the compound for treating cancers.
Type:
Application
Filed:
May 4, 2016
Publication date:
December 21, 2017
Inventors:
Xinhua LIN, Hong YAO, Shaoguang LI, Youjia WU, Yuxia SUI
Abstract: A pharmaceutical composition for the prevention and treatment of cancer with specific flavanoid-based compounds selected from among the groups of Flavone, Flavanone and Flavanol, a method for the prevention and treatment of cancer and inflammation using the specific flavonoid-based pharmaceutical compositions, a method for isolating the flavonoid-based pharmaceutical compositions from raw plant material, and a method for synthesizing said specific flavonoid-based pharmaceutical compositions.
Type:
Application
Filed:
June 27, 2017
Publication date:
December 21, 2017
Inventors:
Henry Lowe, Ngeh J. Toyang, Joseph Bryant
Abstract: The invention relates to the extraction of pharmaceutically active components from plant materials, and more particularly to the preparation of a botanical drug substance (BDS) for incorporation in to a medicament. It also relates to a BDS, for use in pharmaceutical formulations.
Abstract: The present invention provides a crystalline Form A of Compound 1, also referred to as Granaticin B, and pharmaceutically compositions thereof. The present invention also provides methods of treating a microbial infection, or a disease, disorder, or condition associated with abnormal cellular proliferation, using crystalline Form A of Compound 1 or pharmaceutical compositions thereof.
Type:
Application
Filed:
December 22, 2015
Publication date:
December 21, 2017
Applicant:
Sloan-Kettering Institute for Cancer Research
Abstract: The present invention provides methods of treating nasal polyps in cystic fibrosis patients using zileuton. The present invention also provides methods of treating nasal polyps in cystic fibrosis patients using zileuton in combination with surgical debridement and/or steroid treatment.
Abstract: The present invention relates to selective Histone deacetylase 6 (HDAC6) inhibitors and compositions containing the same. Methods of treating diseases and conditions wherein inhibition of HDAC6 provides a benefit, like a cell proliferative disease, an autoimmune or inflammatory disorder, a neurodegenerative disease, or a combination thereof, also are disclosed.
Abstract: A pharmaceutical composition for aerosol administration and method of preventing or treating a pulmonary disease or condition in a subject with a SphK1 inhibitor are provided.
Type:
Application
Filed:
November 24, 2015
Publication date:
December 21, 2017
Inventors:
Ananatha Harijith, Viswanathan Natarajan, Roberto F. Machado, Jeffrey Jacobson
Abstract: Methods for increasing the encapsulation or incorporation of Sunitinib into polymeric matrices have been developed. The resulting formulations provide for more sustained controlled release of sunitinib or other inhibitors of JNK signaling, which bind to DLK. Increased loading is achieved using an alkaline solvent system. The pharmaceutical compositions can be administered to treat or reduce neuronal death due to elevated intraocular pressure. Upon administration, the sunitinib or other inhibitor is released over an extended period of time at concentrations which are high enough to produce therapeutic benefit, but low enough to avoid unacceptable levels of cytotoxicity, and which provide much longer release than inhibitor without conjugate.
Type:
Application
Filed:
December 15, 2015
Publication date:
December 21, 2017
Inventors:
Jie Fu, Justin Hanes, Donald Jeffrey Zack, Zhiyong Yang, Derek Stuart Welsbie, Cynthia Ann Berlinicke
Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.
Type:
Application
Filed:
December 7, 2015
Publication date:
December 21, 2017
Applicant:
Intra-Cellular Therapies, Inc.
Inventors:
Peng LI, Hailin ZHENG, Gretchen SNYDER, Lawrence P. WENNOGLE, Joseph HENDRICK
Abstract: The present invention concerns pharmaceutical formulations of ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastatic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise a solid dispersion of ARN-509 and HPMCAS. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by melt-extruding a mixture comprising ARN-509 and HPMCAS and optionally subsequently milling said melt-extruded mixture.
Type:
Application
Filed:
December 3, 2015
Publication date:
December 21, 2017
Inventors:
Dennis Martin Hester, Jason Michael Vaughn
Abstract: A method of treating disorders associated with NO/SNO deficiency or benefiting from increased SNO in a subject in need thereof includes administering to the subject an ADH inhibitor, AKR inhibitor, SNO-CoAR inhibitor, and/or SNO-CoA at an amount(s) effective to promote S-nitrosylation of proteins in the subject.
Abstract: The present application relates to substituted heterocycles compound of Formula I and pharmaceutical compositions thereof useful for the inhibition of BET protein function by binding to bromodomains (Formula I).
Type:
Application
Filed:
December 11, 2015
Publication date:
December 21, 2017
Inventors:
Samuel David BROWN, Craig Alan COBURN, Oiesya KHARENKO
Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).
Type:
Application
Filed:
June 2, 2017
Publication date:
December 21, 2017
Inventors:
DiZhong CHEN, Hong Yan SONG, Eric T. Sun, Niefang YU, Yong ZOU
Abstract: The present disclosure relates to a composition for exterminating scuticociliates in fish, comprising Mebendazole as an active ingredient, and to a method for exterminating scuticociliates by performing oral administration or immersion administration of Mebendazole in fish. According to the present disclosure, the composition and the extermination method have excellent effects in exterminating scuticociliates in fish, and can be efficiently used in the aquaculture industry by performing oral administration or immersion administration.
Type:
Application
Filed:
June 12, 2017
Publication date:
December 21, 2017
Inventors:
Jung Soo Seo, Na Young Kim, Sung-hee Jung, Myoung Sug Kim
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:
June 20, 2017
Publication date:
December 21, 2017
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 present disclosure relates to compounds capable of acting as covalent inhibitors of bromodomains and the therapeutic use of these inhibitors.
Type:
Application
Filed:
December 16, 2015
Publication date:
December 21, 2017
Inventors:
Olesya KHARENKO, Peter Ronald YOUNG, Samuel David BROWN, Bryan Cordell DUFFY, Shuang LIU, Peter GUZZO
Abstract: The present invention relates to methods of selectively modulating (for example inhibiting) the activity of histone deacetylase 6 and/or 8 (HDAC6 and/or HDAC8), and treating HDAC6 and/or HDAC8 associated diseases, including, for example, cancers, inflammatory disorders, and neurodegenerative disorders.
Abstract: The present disclosure relates generally to methods for treating neurodegenerative diseases, including their progressive forms. In particular, the present disclosure pertains to methods of treating or preventing neurodegenerative diseases, including their progressive forms and their associated symptoms by administering a combination of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) and riluzole, or pharmaceutically acceptable salts of one or both thereof.
Abstract: This invention relates to a compound with EP4 antagonistic activity, or a pharmaceutically acceptable salt with EP4 receptor antagonistic activities, which is useful in the treatment of cartilage disease. This invention also relates to a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof with EP4 receptor antagonistic activities, which is useful in the treatment of cartilage disease. This invention also relates to a pharmaceutical composition for the treatment of cartilage disease which comprises a therapeutically effective amount of a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof.
Abstract: The disclosure relates to substituted pyridines, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
Type:
Application
Filed:
December 1, 2015
Publication date:
December 21, 2017
Inventors:
May Xiaowu Jiang, Bruce Francis Molino, Shuang Liu, Ruifang Wang, Bryan Cordell Duffy, John Frederick Quinn, Gregory Steven Wagner
Abstract: Described are a group of isoxazol-3(2H)-one analogues and their use in topical formulations for the treatment and prophylaxis of dermatological disorders.
Abstract: The invention provides a multi-layered pharmaceutical composition comprising two or more formulations with varying properties. In some embodiments, the pharmaceutical compositions provide combinations of different organoleptic properties within the same product. In certain embodiment, these combinations allow for a modified release profile of active ingredients as the user enjoys the pharmaceutical composition. The invention further provides methods for making and using the pharmaceutical composition.
Type:
Application
Filed:
August 31, 2017
Publication date:
December 21, 2017
Inventors:
Donna Walker Duggins, John-Paul Mua, Darrell Eugene Holton, Jr., Daniel Verdin Cantrell
Abstract: Methods of prevention of symptomatic malaria in a malaria-naïve, G6PD-normal human subject comprising administering to the human subject a compound of Formula (I), a pharmaceutically acceptable salt thereof, or pharmaceutical composition comprising a compound of Formula (I). A compound of Formula (I) can be administered prior to potential exposure of a species of Plasmodium, during potential exposure of a species of Plasmodium, and after potential exposure of a species of Plasmodium. The methods of the invention also pertains to kits comprising specific doses of Formula (I), a pharmaceutically acceptable salt thereof, or pharmaceutical composition comprising a compound of Formula (I), and instructions for administration of dosing quantity and frequency. The methods of the invention also pertain to determining doses of Formula (I) that meet the general regulatory requirement for a drug to be efficacious in the prevention of malaria in malaria-naïve subjects.
Type:
Application
Filed:
December 2, 2015
Publication date:
December 21, 2017
Applicant:
60 Degrees Pharmaceuticals LLC
Inventors:
Bryan L Smith, John Paul Jones, Moshe Shmuklarsky, Budda Balasubrahmanyam
Abstract: Disclosed herein is an injectable anticancer composition for local administration, which contains a suspension of quinine hydrochloride. The anticancer composition for local administration according to the present invention shows an IC50 value against MKN-45 cells, which is about 10 times lower than Paclitaxel, as determined by an MTT assay in vitro, suggesting that the anticancer composition has an excellent cytotoxic effect. The anticancer composition can be administered as a safe anticancer agent in clinical applications, and also shows an anticancer effect by inducing the necrosis and detachment of solid cancer cells. Particularly, the anticancer composition has an anticancer mechanism by which the composition acts locally in a tumor tissue administered with the composition and shows a rapid antitumor effect (1-2 weeks after administration).
Abstract: The present invention relates to therapeutic immunoconjugates comprising SN-38 attached to an anti-HLA-DR antibody or antigen-binding antibody fragment. The immunoconjugate may be administered at a dosage of between 3 mg/kg and 18 mg/kg, preferably 4, 6, 8, 9, 10, 12, 16 or 18 mg/kg, more preferably 8, 10 or 12 mg/kg. When administered at specified dosages and schedules, the immunoconjugate can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy. The methods and compositions are particularly useful for treating AML, ALL or multiple myeloma.
Type:
Application
Filed:
August 4, 2017
Publication date:
December 21, 2017
Inventors:
Serengulam V. Govindan, Thomas M. Cardillo, David M. Goldenberg
Abstract: Methods, compositions, systems, and packaging are disclosed for reducing postoperative nausea and/or vomiting (PONV) in a human patient in need of general anesthesia for surgery. Such methods may include scheduling a surgery for the human patient, and administering to the patient one or more series of prescribed medicines for at least three successive days during a regimen immediately preceding general anesthesia. Compositions may include cholinergic receptor agonists, muscarinic receptor agonists, dopamine receptor agonists, MAO inhibitors, serotonin receptor agonists, selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, selective serotonin releasing agents, serotonin-norepinephrine-dopamine reuptake inhibitors, opioids, or analgesics.
Abstract: Methods and compositions are provided which comprise effective amounts of an analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.
Type:
Application
Filed:
August 14, 2017
Publication date:
December 21, 2017
Inventors:
Paul BOSSE, John AMELING, Bernard SCHACHTEL, Ray TAKIGIKU
Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
Abstract: Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.
Type:
Application
Filed:
September 5, 2017
Publication date:
December 21, 2017
Applicant:
YALE UNIVERSITY
Inventors:
Vladimir Coric, John H. Krystal, Gerard Sanacora
Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
Abstract: 1-[2-(2,4-dimethylphenylsulphanyl)phenyl)]piperazine exhibits potent activity on SERT, 5-HT3 and 5-HT1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients.
Type:
Application
Filed:
August 10, 2017
Publication date:
December 21, 2017
Inventors:
André Faldt, Heidi Lopez de Diego, Rene Holm
Abstract: The present disclosure provides a method for inhibiting cytomegalovirus (CMV) replication in a cell infected with CMV, the method comprising contacting the cell with a bisbenzimidazole compound. The present disclosure provides a method of treating a CMV infection in an individual, the method comprising administering to the individual an effective amount of a bisbenzimidazole compound.
Abstract: [Problem] Provided is a pharmaceutical composition for treating lung cancer in which mitochondrial Complex I is involved, particularly non-small cell lung cancer. [Means for Solution] The inventors of the present invention conducted examinations on a compound having an effect of inhibiting mitochondrial Complex I, and confirmed that a bicyclic nitrogen-containing aromatic heterocyclic amide compound of the present invention has the effect of inhibiting mitochondrial Complex I and that this compound exhibits an anti-tumor effect on mice bearing tumors of non-small cell lung cancer-derived cells, and therefore completed the present invention.
Abstract: [Problem] Provided is a pharmaceutical composition for treating multiple myeloma. [Means for Solution] The inventors of the present invention conducted examinations on a compound having an effect of inhibiting mitochondrial Complex I, and confirmed that a bicyclic nitrogen-containing aromatic heterocyclic amide compound of the present invention has the effect of inhibiting mitochondrial Complex I and that this compound exhibits the effect of inhibiting growth of multiple myeloma, and therefore completed the present invention.
Abstract: [Problem] Provided is a pharmaceutical composition for treating various types of cancer in which mitochondrial Complex I is involved, particularly colorectal cancer, leukemia and/or malignant lymphoma. [Means for Solution] As a result of intensive examination for creating a pharmaceutical composition for treating various types of cancer, the inventors of the present invention confirmed that a specific bicyclic nitrogen-containing aromatic heterocyclic amide compound has the effect of inhibiting mitochondrial Complex I and activating AMPK, and that a pharmaceutical composition comprising the compound as an active ingredient has a treatment effect on various types of cancer in which mitochondrial Complex I is involved, particularly colorectal cancer, leukemia and/or malignant lymphoma, and therefore completed the present invention.
Abstract: A pharmacotherapy is provided for preventing glaucoma or preventing or treating ocular hypertension, the pharmacotherapy providing potent intraocular pressure-lowering action with fast-acting properties and prolonged duration. A combination of (S)-(?)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or a salt thereof, or a solvate of (S)-(?)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine or the salt thereof and an ?2 agonist for preventing or treating glaucoma.
Abstract: The present invention features interferon-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 16 weeks, alternatively no more than 12 weeks, or alternatively no more than 8 weeks. In one aspect, the treatment comprises administering at least two direct acting antiviral agents to a subject with HCV infection, wherein the treatment lasts for 16, 12, or 8 weeks and does not include administration of either interferon or ribavirin, 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:
Application
Filed:
September 1, 2017
Publication date:
December 21, 2017
Applicant:
AbbVie Inc.
Inventors:
Christine Collins, Emily O. Dumas, Bo Fu, Abhishek Gulati, Yiran Bonnie Hu, Jens Kort, Matthew Kosloski, Preethi Krishnan, Yang Lei, Chih-Wei Lin, Ran Liu, Federico Mensa, Iok Chan Ng, Tami Pilot-Matias, David Pugatch, Susan Rhee, Nancy S. Shulman, Roger Trinh, Rolado M. Viani, Stanley Wang, Zhenzhen Zhang
Abstract: In one aspect, the invention relates to triazol-1-ol compounds, analogs thereof, compositions comprising same, and methods of using same, alone or in combination with other agents, to reactivate latent retroviruses, and more particularly to reactivate latent HIV-1. Such compounds, compositions, and methods can be used, for example, in connection with diagnosing and/or treating a retrovirus, and more specifically HIV-1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Application
Filed:
June 30, 2017
Publication date:
December 21, 2017
Inventors:
Vincente Planelles, Alberto Bosque-Pardos, Chris M. Ireland, Ryan Van Wagoner, Mary Kay Harper-Ireland, John Alan Maschek
Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Application
Filed:
December 30, 2016
Publication date:
December 21, 2017
Inventors:
Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan
Abstract: The present invention relates to methods and compositions for modulating levels of amyloid-? peptide (A?) exhibited by non-neuronal (i.e., peripheral) cells, fluids, or tissues. The invention also relates to modulation of AP levels via selective modulation (e.g., inhibition) of ?-secretase activity. The invention also relates to methods of preventing, treating or ameliorating the symptoms of a disorder, including but not limited to an A?-related disorder, by administering a compound that results in the modulation of ?-secretase in a non-neuronal tissue, either directly or indirectly to prevent, treat or ameliorate the symptoms of a brain AP disorder, such as Alzheimer's disease.
Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinazoline structure or a quinoline structure which function as dual inhibitors of EGFR proteins and PI3K proteins, and their use as therapeutics for the treatment of cancer and other diseases.
Type:
Application
Filed:
December 15, 2015
Publication date:
December 21, 2017
Inventors:
Christopher Emil Whitehead, Judith S. Leopold
Abstract: The present invention relates to compounds, compositions and methods comprising nanoparticles (NP) that are based on hyaluronic acid (HLA) that have been modified with hydrophobic moieties that can entrap FASN inhibitor compounds. In one embodiment, the FASN inhibitor compounds include Orlistat. In one embodiment, the hydrophobic moieties comprise 5-?CA, Pba, or ODA, or combinations thereof. In a variation, the present invention relates to a composition comprising NPs based upon HLA, Orlistat, one or more of the hydrophobic moieties comprising 5-?CA, Pba, or ODA, and one or more of members selected from the group consisting of PEG and a dilute solution containing SDS.
Type:
Application
Filed:
July 24, 2015
Publication date:
December 21, 2017
Inventors:
Aaron M. Mohs, Steve J. Kreidel, Tanner K. Hill