Abstract: A method for preparation of liquid, semi-liquid or solid particles through formation of an initial emulsion and consecutive deformation and/or breakage of the particles by means of temperature change. The formed particles may further be polymerized, physically or chemically modified and/or functionalized. The shape and size of the particles depend on the oil used, the size of the emulsion droplets in the initial emulsion, the surfactant used and the cooling/heating rate or temperature, and finally the nature of the additives. The method allows the preparation of a diverse range of particle shapes: rod-like, with different aspect ratios (1a, 1b); triangular (1c); triangular with inscribed geometrical shapes (d); deformed and/or elongated triangular shapes (e, f); quadrilateral shapes (g, h); quadrilateral shapes with inscribed geometrical shapes (i); hexagonal (j); hexagonal with inscribed geometrical shapes (k, l); and/or polygonal shape (m).
Type:
Application
Filed:
November 18, 2016
Publication date:
December 27, 2018
Applicant:
SOFIA UNIVERSITY "ST. KLIMENT OHRIDSK"
Inventors:
Stoyan Smoukov, Nikolai Denkov Denkov, Slavka Stoyanova Tcholakova, Ivan Igorov Lesov, Diana Peychova Cholakova, Zhulieta Nedyalkova Valkova
Abstract: The invention relates to a formulation for the delayed and controlled delivery of an adsorbent into the lower intestine of mammals. The formulation includes a carrageenan and an adsorbent, such as activated charcoal. The invention further relates to uses of this formulation, in particular to pharmaceutical uses. In one embodiment, the formulation is used to eliminate or reduce the side effects in the intestine, in particular in the colon, of pharmaceutical agents that are administered as a treatment for a disorder, but that have side effects when they reach the late ileum, the caecum or the colon.
Abstract: An oral controlled-release multiparticulate dosage form comprises a plurality of individually enteric coated particulates containing an L-carnitine that independently disperse in a patient's stomach after oral ingestion and travel through the stomach and past the pyloric sphincter without substantially releasing the L-carnitine in the stomach. The individual particulates contain (a) a solid core containing the L-carnitine, (b) a subcoating containing a cellulosic water soluble polymer over the core, and (c) an enteric coating over the subcoating. The dosage form may be used to treat conditions associated with a reduction of the amount of L-carnitine in the body.
Abstract: The present disclosure provides multifunctional nanoparticles. More particularly, the present disclosure relates to multifunctional nanoparticles having one or more of nucleic acid ligands; and methods of using such nanoparticles for treatment and/or diagnosis of diseases and conditions.
Abstract: The invention relates to protein nanocapsules that exhibit material properties that change in different in vivo environments. A zwitterion moiety on the surface of the nanocapsule can protect the protein from opsonization in a first environment, yet uncouples from the protein nanocapsule in a second environment (e.g. at a pH of less than 6.5). In embodiments of the invention, the uncoupled protein nanocarrier is then internalized by mammalian cells (e.g. tumor cells).
Type:
Application
Filed:
December 14, 2016
Publication date:
December 27, 2018
Inventors:
Yunfeng LU, Jie LI, Yang LIU, Jie REN, Jing WEN
Abstract: Devices for local delivery of tacrolimus or a derivative thereof are provided, wherein the devices comprise a polymeric matrix containing tacrolimus or a derivative thereof that provides for delayed and extended release of tacrolimus or a derivative thereof. The devices can locally deliver tacrolimus or a derivative thereof to injured nervous system tissue upon implantation in a subject. Thus, techniques for local delivery of tacrolimus or a derivative thereof and methods of treatment using such devices are also provided.
Type:
Application
Filed:
June 18, 2018
Publication date:
December 27, 2018
Applicants:
UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION, DEPARTMENT OF VETERANS AFFAIRS
Inventors:
Kia M. Washington, William R. Wagner, Michael Brandt Steketee, Yolandi Van der Merwe, Xinzhu Gu
Abstract: The present invention relates to a nalfurafine-containing percutaneous absorption patch having a support, a drug layer and a control layer which are laminated successively, wherein the drug layer contains at least one kind of a drug selected from the group consisting of nalfurafine and a salt thereof, and capable of maintaining a given level of drug skin permeation amount without permeation of an excess amount of the drug through the skin in a short time even when applied to the skin in which the horny cell layer and the like are damaged and the skin barrier is insufficient.
Type:
Application
Filed:
June 24, 2016
Publication date:
December 27, 2018
Applicant:
UNIVERSITY OF TSUKUBA
Inventors:
Hiroshi NAGASE, Makiko TADA, Megumi YASHIMA, Takeshi SAIKI
Abstract: The present invention relates to a pharmaceutical composition comprising pinocarveol for preventing or treating metabolic diseases, and functional food composition using the pharmaceutical composition for improving or alleviating metabolic diseases. Pinocarveol according to the present invention reduces weight, visceral fat, and cholesterol concentration, improves blood liver function index, reduces blood sugar, and additionally inhibits a metabolic inflammation reaction, and thus can be effectively used ultimately as a medical or functional food composition exhibiting prevention or treatment activities for metabolic diseases selected from the group consisting of obesity, diabetes, dyslipidemia, and syndromes of fatty liver and insulin-resistance.
Type:
Application
Filed:
May 30, 2016
Publication date:
December 27, 2018
Applicant:
INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
Abstract: Synthetically-derived S,S-heterodisubstituted disulfides that exhibit potent in vitro antibacterial activity against a variety of bacteria, including Staphylococcus aureus, methicillin-resistant Staphylococcus aureus and Francisella tularensis. The present invention provides compounds, methods and compositions effective to treat microbial/bacterial infections, and, especially, infections arising from bacteria which have developed resistance to conventional antibiotics.
Abstract: The present invention is directed, in part, to methods of treating Epidermolysis Bullosa (EB) in a subject in need thereof, comprising topical administration of a pharmaceutical composition comprising a therapeutically effective amount of a of Coenzyme Q10 (CoQ10) to the subject.
Type:
Application
Filed:
May 16, 2018
Publication date:
December 27, 2018
Applicant:
Berg LLC
Inventors:
Niven Rajin Narain, Rangaprasad Sarangarajan, Michael Andrew Kiebish
Abstract: A deacetylnemorone abietane diterpenoid is utilized in the prevention of growth and development of pathogenic cells, e.g., cancer cells. The deacetylnemorone can have the following structure: or a tautomer there of in which R1, R2, and R3 are independently selected from —H, C1-10 alkyl, C1-10 alkoxy, C1-10 alkenyl, C1-10 alkenoxy, —OH, —OAc, —CHO, -Ph, —OC6H5, —OC6H4OH, —COC6H5, —OCONH2, —OCONHCH3, —OCOC6H4NH2, —NH2, or ?O. The deacetylnemorone shows efficacy in treatment and prevention of a wide range of cancer types as well as other neoplastic diseases as a chemo-preventative, a primary or secondary cytotoxic agent, a sensitizer for other therapies, or one component of a combinatorial treatment.
Type:
Application
Filed:
June 11, 2018
Publication date:
December 27, 2018
Inventors:
Ehsan Jabbarzadeh, Wesley F. Taylor, Sara Eslambolchimoghada
Abstract: Disclosed is the use of garcinol for the therapeutic management of ER stress. More specifically, the invention discloses the ability of garcinol in decreasing ER stress and mitigating toxicity by reducing protein aggregation and decreasing expression of ER stress markers SXBP, GRP78 and ATF4, which indicates translational attenuation and recovery in hyperglycemia, paracetamol, alcohol, thapsigargin and high fat diet induced toxicity models.
Type:
Application
Filed:
June 22, 2018
Publication date:
December 27, 2018
Inventors:
Muhammed Majeed, Kalyanam Nagabhushanam, Lakshmi Mundkur
Abstract: The present invention relates to methods of treating patients with advanced forms of cancer, such as clear cell renal cell carcinoma, in which X4P-001 is administered in order to reduce angiogenic escape that typically occurs with TKI therapy. The methods demonstrate surprising results, including regression of tumor size and cell number, with comparatively little toxicity.
Type:
Application
Filed:
December 14, 2016
Publication date:
December 27, 2018
Inventors:
Robert D. Arbeit, Paula Marie Ragan, Michael B. Atkins, James W. Mier, David McDermott
Abstract: The present invention relates to dexmecamylamine and the use of dexmecamylamine, substantially free of exo-R-mecamylamine, in the treatment of hyperhidrosis.
Abstract: The invention provides methods and compositions for treating cancers and myeloproliferative disorders using sphingosine kinase-1 inhibitors, such as SK1-I, and selective sphingosine-1-phosphate receptor agonists, such as ozanimod.
Type:
Application
Filed:
June 25, 2018
Publication date:
December 27, 2018
Applicant:
Enzo Biochem, Inc.
Inventors:
Elazar Rabbani, James J. Donegan, Paul Diamond
Abstract: Disclosed herein are compounds, pharmaceutical compositions, and methods for the treatment of diseases such as inflammation and/or pain, comprising the administration of a therapeutically effective amount of a non-steroidal, non-opioid compound having GI-/renal-/platelet-sparing activities, and wide safety margins with no appreciable inhibition of either form of cyclooxygenase.
Abstract: Described herein are PPAR? agonists, including, but not limited to, endocannabinoids that can be used for treatment of a neuropsychiatric disorder and/or symptom thereof. Also described herein are pharmactiutical formulations containing an effective amount of a PPAR? agonists, including but not limited to endocannabinoids, where the effective amount is effective for treating a neuropsychiatric disorder and/or symptom thereof. Also described herein are methods of treating a neuropsychiatric disorder and/or a symptom thereof in a subject in ned thereof.
Abstract: Disclosed is a method of promoting wound healing with reduced scarring after glaucoma filtration surgery in a mammalian subject in need thereof, which involve the use of a HDAC inhibitor (HDACi), such as, but not limited to, suberoylanilide hydroxamic acid (SAHA).
Abstract: The present invention discloses and claims compositions, methods of treatment, and kits which cause an increase in the time of survival in cancer patients, wherein the cancer: (i) overexpresses thioredoxin or glutaredoxin and/or (ii) exhibits evidence of thioredoxin- or glutaredoxin-mediated resistance to one or more chemotherapeutic interventions. The present invention also discloses and claims methods and kits for the administration of said compositions to properly treat cancer patients. Additionally, the present invention discloses and claims methods and kits for quantitatively determining the level of expression of thioredoxin or glutaredoxin in the cancer cells of a cancer patient, methods of using those determined levels in the initial diagnosis and/or planning of subsequent treatment methodologies for said cancer patient, as well as ascertaining the potential growth “aggressiveness” of the particular cancer and treatment responsiveness of the particular type of cancer.
Abstract: The present disclosure provides methods and compositions which treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms associated with peripheral neuropathies (e.g., neuropathic pain) or sunburn in a subject. Specifically, the present invention relates to topically administering a therapeutically effective amount of a pharmaceutically safe therapeutic agent directly to the region exhibiting pain in a subject.
Type:
Application
Filed:
December 16, 2016
Publication date:
December 27, 2018
Inventors:
Crist J. FRANGAKIS, William WILKISON, Servet BUYUKTIMKIN, Nadir BUYUKTIMKIN, James L. YEAGER
Abstract: A formulation and method for treating or preventing a deficiency of certain nutrients in patients undergoing a therapy in which one or more proton pump inhibitors is administered. The formulation includes: a) 1000 mcg of B12, as methylcobalamin; b) 150 mg of Vitamin C; c) 500 mg of calcium citrate; d) 15 mg of elemental iron in a ferrous form. The formulation may also include 10-50 mg of a proton pump inhibitor.
Abstract: An aqueous composition with a higher-than-neutral pH includes a significant amount of one or more surfactants and large amounts of osmotically active solutes. This composition, as well as an acidic counterpart and solid materials, can be used in a variety of applications such as wound care, oral care, medical equipment reprocessing, healthcare acquired infection and implant treatment.
Abstract: The invention provides methods of treatment that induce satiety in a subject for a period of at least around twenty-four hours by once-daily administration to the subject of a controlled release dosage form, wherein the dosage form is administered while the subject is in the fasted state and at a time of around six to around nine hours prior to the subject's next intended meal, and wherein the dosage form comprises a controlled release composition, which comprises an enterically-coated, ileum hormone-stimulating amount of a nutritional substance and releases the majority of the nutritional substance in vivo upon reaching the subject's ileum. The invention also provides a diagnostic tool for probing the health and disease state of the ileal hormones, excess or deficiencies. The invention provides a safe vehicle for targeted deliveries of chemical, pharmaceuticals, natural substances and nutrition to the ileum.
Abstract: The invention includes a method of preventing or treating a fibrotic lung disease in a subject, comprising administering to the subject a thyroid hormone by inhalation and/or aerosolization. The invention further comprises compositions and kits comprising compositions useful within the invention.
Abstract: The present invention relates to a topical pharmaceutical composition comprising acitretin and a process for its preparation. It also relates to a method of treating skin disorders by administering said topical pharmaceutical composition.
Abstract: The present invention relates to pharmaceutical compositions comprising dimethyl fumarate and a pharmaceutically acceptable agent which inhibits the enzyme catalyzed degradation of dimethyl fumarate.
Abstract: A method for delivering a benefit agent to the surface of the eye, the method comprising applying an ocular benefit composition to a lid margin of the eye wherein the ocular benefit composition comprises at least 5 wt % of one or more lipid and/or lipid derived compounds.
Type:
Application
Filed:
December 14, 2016
Publication date:
December 27, 2018
Applicant:
The University of Manchester
Inventors:
Philip Morgan, Carole Maldonado-Codina, Michael Read, Curtis Dobson
Abstract: This invention provides a self-emulsifying composition comprising 50 to 95% by weight in total of at least one compound selected from the group consisting of ?3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters; and 5 to 50% by weight of an emulsifier having a hydrophilic lipophilic balance of at least 10. The composition has no or reduced ethanol content, and exhibits excellent self-emulsifying property, dispersibility in the composition, emulsion stability, and absorption property. The composition is adapted for use as a drug.
Abstract: The present disclosure relates to method of modulating autophagy by modulators of autophagy, wherein the autophagy includes but is not limited to macroautophagy, chaperone mediated autophagy and microautophagy. The present disclosure further relates to modulators of autophagy for increasing or decreasing the autophagic flux. The disclosure also relates to modulator per se in modulating autophagy including but not limiting to macroautophagy, chaperon mediated autophagy and microautophagy.
Abstract: The present invention relates to a method of treating allergic rhinitis in a subject (e.g., a human) in need thereof comprising nasally administering to the subject an effective amount of a fixed-dose pharmaceutical composition comprising mometasone or its salt and olopatadine or its salt.
Type:
Application
Filed:
December 14, 2017
Publication date:
December 27, 2018
Inventors:
Neelima Khairatkar-Joshi, Abhay Kulkarni, Dinesh Pradeep Wale, Vikram M. Bhosale, Piyush Agarwal, Patrick Keohane, Sudeesh K. Tantry, Chad Oh
Abstract: The present invention discloses uses of a novel phosphodiesterase 4 (PDE4) inhibitor ZL-n-91 in preparing drugs against lung cancer proliferation and metastasis. The mouse survival curves and in vitro cell experiments show that the PDE4 inhibitor ZL-n-91 can significantly inhibit the proliferation and metastasis of lung cancer cells, indicating that this PDE4 inhibitor ZL-n-91 can become an important target for the studies on anti-lung cancer proliferation and metastasis, to provide a basis for preparing drugs against lung cancer proliferation and metastasis, with promising prospect of development and application.
Type:
Application
Filed:
March 30, 2017
Publication date:
December 27, 2018
Inventors:
Allan Zijian ZHAO, Sijia GONG, Yan LIN, Fanghong LI, Xiaoxi LI
Abstract: A phosphatidylserine targeted peptoid has been identified with the ability to bind to cancer cells globally and specifically. A dimer of the peptoid decreases cancer cell viability. Use of the dimerized peptoid enhances the efficacy of docetaxel. The peptoid can be used for including but not limited to diagnosing and treating cancer, diagnosing and treating a viral condition, and diagnosing and treating diabetes.
Abstract: Two isoforms of thyroid receptor alpha (THR?1 and THR?2) have been found to be associated with the growth of cancer. Use of inhibitors of THR?1 (Formula I) and/or agonists of THR?2 (Formula II) in the treatment of such cancers is disclosed. Treatment of other disorders associated with such receptors is also contemplated, as is the use of diagnostic methods for predicting therapeutic outcomes based on the levels of expression of THR?1 and THRa?2 in a tissue sample.
Type:
Application
Filed:
December 22, 2016
Publication date:
December 27, 2018
Applicant:
MCMASTER UNIVERSITY
Inventors:
Sukhbinder Dhesy-Thind, Katarzyna J. Jerzak, Anita Bane, Jessica G. Cockburn, John A. Hassell
Abstract: Blended, processed marijuana and/or hemp cannabis compounds and methods of making the same are provided. In particular, the compound includes one or more species of cannabis mixed in various ways with other ingredients in order to produce a new matter, food product, oil, or drink, in the form of gummies, creams, salves, tablets, capsules, pastes, gelatin suppositories, crystals, ointments, jellies, e-juices, powders, pills, syrups, drops, patches, chewing gums, dried whole or partial plant parts, and dusts, such that it is safe for mammals and provides assistance in dealing with various ailments and diseases.
Abstract: The present disclosure generally relates to terpene-based compositions for applications in the pharmaceutical and recreational fields. In some embodiments, the compositions are enriched compositions or non-naturally occurring compositions which contain defined concentrations of one or more cannabis-derived chemical compounds, such as terpenes and cannabinoids that have a distinctive characteristic that mimics that of a cannabis plant matter or a product thereof. Also provided in some embodiments of the disclosure are methods for the preparation of the compositions, as well as methods for use thereof.
Abstract: The invention relates to an avocado extract rich in polyphenols, containing at least 10% by weight of polyphenols, expressed in gallic acid equivalent relative to the dry extract obtained, wherein said polyphenols contain procyanidins, cafeic acid and cafeic acid derivatives, typically in a proportion of at least 70% by weight, expressed in gallic acid equivalent relative to the total polyphenol content by weight. The invention also relates to a composition comprising an extract according to the invention as active agent and a suitable excipient. The invention also relates to such a composition or such an extract for use thereof in preventing or treating disorders or pathological conditions of the skin, the mucous membranes or the superficial body growths.
Type:
Application
Filed:
August 30, 2018
Publication date:
December 27, 2018
Applicant:
Laboratoires Expanscience
Inventors:
Alex SAUNOIS, Caroline BAUDOUIN, Sophie LECLERE-BIENFAIT, Sebastien GARNIER, Philippe MSIKA
Abstract: A tablet which comprises (1) 1-(3-(2-(1-benzothiophen-5- yl)ethoxy)propyl)azetidin-3-ol or a salt thereof and (2) ethyl cellulose, said tablet having excellent elution properties and good moldability, remaining stable during prolonged storage, and exhibiting high impact resistance.
Abstract: The present disclosure provides a pharmaceutical composition that inhibits the proliferation of a cancer cell, comprising a first compound selected from indole-3-carbinol (I3C), 1-benzyl I3C, or a pharmaceutically acceptable salt or ester thereof, and a second compound that binds to and inhibits: i) an oncogenic RAF polypeptide at a site that is distinct from the site at which the first compound binds; ii) a polypeptide of the RAF signaling pathway; iii) a polypeptide of the Wnt-?-catenin signaling pathway; iv) or a polypeptide of the PI3K/AKT/mTOR signaling pathway. The present disclosure also provides a method of treating cancer in a subject.
Abstract: The invention provides methods of treatment of a progressive bone disease, such as osteoporosis, Paget's Disease, multiple myeloma, or hyperparathyroidism, comprising administration of an effective amount of a non-agonist PPARG modulator to a patient afflicted with the disease.
Type:
Application
Filed:
July 6, 2018
Publication date:
December 27, 2018
Inventors:
Patrick R. Griffin, Theodore Kamenecka, Beata Lecka-Czernik
Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.
Type:
Application
Filed:
September 10, 2018
Publication date:
December 27, 2018
Inventors:
Lin Zhi, Keith Marschke, Virginia H. Grant, Steven L. Roach, Yixing Shen, Jason C. Pickens, Bijan Pedram, Cornelius Arjan van Oeveren, Lino J. Valdez, Andrew R. Hudson
Abstract: The present invention relates to methods and pharmaceutical compositions for the treatment of obesity. In particular, the present invention relates to a method of treating obesity in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an indoleamine 2-3 dioxygenase (IDO) inhibitor.
Abstract: The invention relates to Cebranopadol for use in the treatment of pain, wherein Cebranopadol is administered according to an administration regimen comprising (i) a first administration interval, which lasts for at least 2 consecutive days, wherein a first daily dose of Cebranopadol is administered on every day of the first administration interval; and (ii) a second administration interval, which lasts for at least 2 consecutive days and directly follows the first administration interval without interruption, wherein a second daily dose of Cebranopadol is administered on every day of the second administration interval; wherein the first daily dose of Cebranopadol is lower than the second daily dose of Cebranopadol.
Type:
Application
Filed:
August 29, 2018
Publication date:
December 27, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Shaonan WANG, Chiara PIANA, Roberta BURSI
Abstract: The present invention relates to the pyrrolidine substituted with flavone derivatives, represented by the compounds of Formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a diastereoisomer thereof for use in the treatment of cancers associated with human papillomavirus. The present invention also relates to the pharmaceutical compositions containing the compounds of Formula (I) for the treatment of cancers associated with human papillomavirus.
Abstract: The present invention relates to the use of DBH inhibitors (e.g., disulfiram and Nepicastat), and pharmaceutical compositions thereof, for treating subjects with certain types of memory loss, for instance memory loss associated with a neurodegenerative disease, disorder, or condition, such as Alzheimer's Disease.
Abstract: The present invention provides 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine˜2˜carbonitrile and pharmaceutically acceptable salts and solvates thereof that is capable of inhibiting CHK1 and is useful in the treatment of neuroblastomas and/or soft tissue sarcomas.
Abstract: Presently disclosed are methods of treating cancer comprising administering a MEK inhibitor in combination with a proteasome inhibitor. In some embodiment, the cancer is a solid tumor. In some instances, the cancer has at least one mutation chosen from a NF1, RAS (including N-, K-, and H-RAS), RAF (including A-, B-, and C-RAF), and MEK (including MEK1 and MEK2) mutation. In some embodiments, the cancer is resistant to treatment with at least one of a proteasome inhibitor or a MEK inhibitor. In some embodiments, the combination therapy produces a synergistic effect.
Abstract: The present invention is directed to a combination comprising a proteasome inhibitor and a compound of formula I or a pharmaceutically acceptable salt thereof: to a pharmaceutical composition and to a kit both comprising said combination, to the combination, composition or kit for use in the treatment of cancer, and to a method of treatment of cancer in a patient in need thereof comprising administering to said patient an effective amount of said combination, composition or kit.
Type:
Application
Filed:
May 21, 2018
Publication date:
December 27, 2018
Inventors:
Thomas Jorg Mehrling, Enrique Maria Ocio