Abstract: The present invention belongs to the pharmaceutical field, and in particular, it relates to a pharmaceutical formulation of palbociclib and a preparation method thereof. The pharmaceutical formulation comprises palbociclib, an acidic auxiliary material, and optionally a hydrophilic high-molecular material, which has better solubility and in vitro dissolution property as compared with the conventional formulation and can be used for enhancing in vivo absorption and bioavailability of palbociclib.
Abstract: The invention provides compounds that inhibit human MLKL, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.
Type:
Application
Filed:
August 26, 2019
Publication date:
December 19, 2019
Applicant:
National Institute of Biological Sciences, Beijing
Inventors:
Zhiyuan Zhang, Xiaodong Wang, Shaoqiang Huang, Bo Yan, Lei Liu, Huayi Wang, Jianguang Han, Zhi Huang, Weiye Cao
Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.
Type:
Application
Filed:
July 1, 2019
Publication date:
December 19, 2019
Inventors:
Rebecca TAUB, Charles H. REYNOLDS, Lianhe SHU, Ping WANG, Duk Soon CHOI
Abstract: The disclosure generally relates to compounds of formulas (I) and (II)7 including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV-1 integrase, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
Type:
Application
Filed:
January 26, 2018
Publication date:
December 19, 2019
Inventors:
Mark D. ANDRAKE, Anna Marie SKALKA, George W. Merkel
Abstract: A use of an inhibitor of the cytochrome bc1 complex for preparing a pharmaceutical composition which treats diseases related to smooth muscle spasms, inflammatory diseases, and relieves pain.
Abstract: Described herein are methods for the administration of reboxetine, or a pharmaceutically acceptable salt thereof, to a human being in need thereof, resulting in a first maximum plasma concentration and a second maximum plasma concentration, wherein the two maxima are separated by a time period of about 2 hours to about 6 hours.
Abstract: Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.
Type:
Application
Filed:
January 17, 2019
Publication date:
December 19, 2019
Inventors:
Mark W. SURBER, Keith A. BOSTIAN, Michael N. DUDLEY, Olga RODNY, David C. GRIFFITH
Abstract: Neuroblastoma is a tumor primarily affecting children. The current standard of care is not curative except in the rare case of a surgically-resectable lesion, although very high survival rates have been documented for low-risk neuroblastoma and moderate-risk neuroblastoma. Taurolidine was developed as an anti-infective, but it has been found to have surprising oncolytic activity in cell cultures and now in a rodent cancer model. This invention relates to the use of taurolidine for the treatment of neuroblastoma in juvenile mammals.
Abstract: Neuroblastoma is a tumor primarily affecting children. The current standard of care is not curative except in the rare case of a surgically-resectable lesion, although very high survival rates have been documented for low-risk neuroblastoma and moderate-risk neuroblastoma. Taurolidine was developed as an anti-infective, but it has been found to have surprising oncolytic activity in cell cultures and now in a rodent cancer model. The efficacy in rodent model is superior to the efficacy in cell culture. This invention relates to the use of taurolidine hydrolysis products (tarultam and/or taurinamide and/or methylene glycol and/or selected combinations thereof) for the treatment of neuroblastoma in juvenile mammals.
Abstract: A method for treating a cancer which overexpresses any of N-myc genes, C-myc genes and/or L-myc genes in a mammalian body, the method comprising: administering a composition to the mammalian body, wherein the composition comprises at least one from the group consisting of taurolidine; taurultam; taurinamide; methylene glycol; taurultam and taurinamide in a ratio of 1 taurultam:7 taurinamide; and taurultam, taurinamide and methylene glycol in a ratio of 1 taurultam:7 taurinamide:1 methylene glycol.
Abstract: Each unit form of an analgesic composition for prolonging the duration of action of a local anesthetic comprises: 0.5 to 20 mg of composite vitamin B, 10 to 20 mg of methylene blue, 10 to 100 mg of dexamethasone, 2 to 100 ml of 5% sodium bicarbonate, and 0.9% normal saline.
Abstract: The present invention is directed to nanoparticulate compositions comprising meloxicam particles having an effective average particle size of less than about 2000 nm.
Type:
Application
Filed:
August 25, 2019
Publication date:
December 19, 2019
Inventors:
Eugene R. Cooper, Tuula Ryde, John Pruitt, Laura Kline
Abstract: Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.
Type:
Application
Filed:
January 18, 2019
Publication date:
December 19, 2019
Applicant:
Supernus Pharmaceuticals, Inc.
Inventors:
Padmanabh P. BHATT, Argaw KIDANE, Kevin EDWARDS
Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
Type:
Application
Filed:
August 22, 2019
Publication date:
December 19, 2019
Applicant:
AMGEN INC.
Inventors:
Paul E. HARRINGTON, Kate ASHTON, Sean P. BROWN, Matthew R. KALLER, Todd J. KOHN, Brian Alan LANMAN, Kexue LI, Yunxiao LI, Jonathan D. LOW, Ana Elena MINATTI, Alexander J. PICKRELL, Markian M. STEC, Joshua TAYGERLY
Abstract: Tricyclic dibenzothiazepine compounds for use in the treatment of CDKL5 disorder. Specifically, a compound of Formula I, or a pharmaceutically or veterinarily acceptable salt thereof, or a pharmaceutically or veterinarily acceptable solvate of either entity for use in the treatment of CDKL5 disorder in a mammal, wherein a compound of Formula I comprises: or a pharmaceutically or veterinarily acceptable salt thereof, or a pharmaceutically or veterinarily acceptable solvate of either entity, wherein: R1 and R3 each independently represent, at each occurrence when used herein, H or C1 to C5 alkyl; R2 represents halo; R4 and R5 each independently represent H; R6 represents —C(O)OR9; X represents CH2, O or S; R9 represents H or C1 to C5 alkyl; and, m is an integer from 1 to 6 inclusive.
Abstract: Beneficial topical compositions for treating scar or aging skin are provided. In one embodiment, the compositions include Bulbine frutescens, Centella asiatica and a phenol derived from olives, such as oleuropein. The composition may be used in the treatment of scars formed during surgery. The composition may also be used cosmeceutically in the treatment of aged skin, and may include phosphatidylserine, vitamins, and other beneficial anti-aging ingredients.
Abstract: The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.
Abstract: This disclosure provides progesterone formulations, methods of using these formulations, and their related pharmacokinetic parameters. In particular embodiments, the formulations disclosed herein allow for a reduction in the amount of progesterone administered to a patient in need thereof, while still providing the benefits of a larger dosage amount.
Type:
Application
Filed:
February 12, 2019
Publication date:
December 19, 2019
Applicant:
TherapeuticsMD, Inc.
Inventors:
Julia AMADIO, Brian Bernick, Peter H.R. Persicaner
Abstract: The present invention provides the steroid compound 3beta-hydroxy-5alpha-pregnan-20-one for use in treatment of essential tremor, as well as methods for treating essential tremor and pharmaceutical compositions for use in treatment of essential tremor.
Abstract: The present specification is directed to systems, apparatus and methods for prophylactically preventing, or for treating the onset and/or progression of Cerebral Amyloid Angiopathy (CAA), acute stroke conditions, or Alzheimer's disease. The progression of, stabilizing, or improving symptoms related to these conditions are treated by monitoring a pathophysiological change indicative of the conditions in a patient, based on the monitoring, determining if amyloid plaque is present in a perivascular space of the patient, optionally determining an extent of amyloid plaque in the perivascular space, and based on the presence of amyloid plaque in the perivascular space of the patient, determining a treatment protocol for the patient. The treatment protocol includes administering to the patient a high density lipoprotein composition derived from mixing a blood fraction with a lipid removing agent.
Type:
Application
Filed:
May 10, 2019
Publication date:
December 19, 2019
Inventors:
Hollis Bryan Brewer, JR., Michael M. Matin
Abstract: This invention relates to methods of treating and/or preventing the progression and/or onset of age-related neurodegeneration. The invention also relates to methods of reversibly slowing the growth and/or aging of a subject, and/or extending the potential lifespan of the subject, comprising administration of the naturally occurring aminosterol MSI-1436, or derivatives or salts thereof. Also described are methods of treating, preventing or delaying the onset of age-related diseases or conditions comprising administration of Aminosterol 1436, or derivatives or salts thereof.
Abstract: A preparation for preventing and treating atypical osteoporosis with normal or increased bone tissue mineralization with the presence of cavities in trabecular bone sections, and conditions close to same, comprises between 10 mg and 1000 mg of drone brood and between 50 IU and 100,000 IU of vitamin D or vitamins of this group and/or the active metabolites in a daily dose. The preparation can be provided in powder, tablet or capsule form. It facilitates the redistribution of calcium in the body, reducing mineralization in soft tissues, vessels and other organs, as well as filling cavities in trabecular bone.
Type:
Application
Filed:
October 27, 2017
Publication date:
December 19, 2019
Inventors:
Villorij I. Strukov, Olga Jones, Evgenij N. Krutiakov, Konstantin G. Elistratov
Abstract: The present invention relates to a topical spray composition comprising a biologically active vitamin D derivative or analogue and a corticosteroid, and its use in the treatment of dermal diseases and conditions.
Abstract: The present invention relates to a topical spray composition comprising a biologically active vitamin D derivative or analogue and a corticosteroid, and its use in the treatment of dermal diseases and conditions.
Abstract: What is described is a method for treating cancer in a patient assaying levels of (a) CXCR1 and/or CXCR2 ligands or (b) myeloid derived suppressor cells (MDSCs) and/or neutrophils in the patient, and if the patient has increased levels of (a) or (b), then administering a therapeutically effective amount of a compound having a structure selected from the group consisting of formulas SX-517, SX-576, and SX-682
Type:
Application
Filed:
August 26, 2019
Publication date:
December 19, 2019
Inventors:
John A. Zebala, Dean Y. Maeda, Aaron D. Schuler
Abstract: Disclosed are methods of modulating and/or decreasing serum corticosterone levels in an individual affected by stress. Further disclosed are methods of modulating the hypothalamic pituitary adrenal response in an individual. The methods include administration of 2-fucosyl-lactose to an individual.
Abstract: The present invention relates to a foodstuff comprising feather hydrolysate for use in improving performance during exercise and/or improving recovery after exercise in a dog. It also relates to a method of improving the performance in a dog during exercise and/or improving recovery after exercise, the method comprising administering to a dog a foodstuff which comprises feather hydrolysate.
Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.
Type:
Application
Filed:
June 21, 2019
Publication date:
December 19, 2019
Applicant:
Janssen BioPharma, Inc.
Inventors:
Guangyi WANG, David Bernard SMITH, Leonid BEIGELMAN, Jerome DEVAL, Marija PRHAVC
Abstract: Disclosed is an application of verbascoside in the preparation of drugs for preventing and treating type II diabetic nephropathy. The protective effect of verbascoside on type II diabetic nephropathy and the action mechanism thereof are also included in the invention. The results show that verbascoside may improve liver injuries caused by high glucose, and reduce levels of serum creatinine, urea nitrogen, microalbuminuria and blood lipid (total cholesterol and triglyceride), fasting blood sugar and serum insulin in spontaneous diabetic db/db mice, and significantly reduce expressions of TGF-?1 and its signal transduction protein Smad3 and Smad4 and ?-SMA in kidney tissues. Meanwhile, verbascoside may improve liver injuries caused by high glucose, and inhibit HK-2 proliferation and EMT formation.
Type:
Application
Filed:
December 29, 2018
Publication date:
December 19, 2019
Inventors:
Shulan SU, Jinao DUAN, Dawei QIAN, Yue ZHU, Hui YAN, Xinxin DAI
Abstract: The invention relates to a nutritional adjuvant, comprising baicalin and/or baicalein diluted on a medium, and to a feed comprising such an adjuvant, for improving production performance in farm animals in stressful situations.
Abstract: This invention relates to a combination of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-phosphate (chemical name: 2?-Deoxy-2?,2?-difluoro-D-cytidine-5?-O-[phenyl (benzoxy-L-alaninyl)] phosphate) (NUC-1031) and a platinum-based anticancer agent selected from cisplatin, picoplatin, lipoplatin and triplatin. The combinations are useful in the treatment of cancer, particularly biliary tract and bladder cancer.
Abstract: A solid composition comprising sofosbuvir and at least one pharmaceutically acceptable matrix compound wherein at least 99 weight-% of the sofosbuvir comprised in the composition are present in amorphous form, at least 99 weight-% of the solid composition consist of the sofosbuvir and the at least one matrix compound, and wherein the solid composition contains the sofosbuvir in an amount of at least 55 weight-% based on the combined weight of the sofosbuvir and the at least one matrix compound.
Abstract: Disclosed herein are methods and compositions for inhibiting neddylation using Glycyl-tRNA synthase (GlyRS) inhibitors. Also disclosed are related compositions and methods for treating diseases such as cancer.
Type:
Application
Filed:
October 13, 2016
Publication date:
December 19, 2019
Inventors:
Xiang-Lei Yang, Zhongying Mo, Paul Schimmel
Abstract: The present invention relates to methods for treating and preventing ophthalmological disease and disorders, comprising administering Antagonist A or another pharmaceutically acceptable salt thereof, optionally in combination with another treatment, to a subject in need thereof. The present invention also relates to methods for treating and preventing ophthalmological disease and disorders, comprising administering an anti-C5 agent (e.g., ARC1905), optionally in combination with another treatment, to a subject in need thereof.
Type:
Application
Filed:
June 6, 2019
Publication date:
December 19, 2019
Applicant:
IVERIC bio, Inc.
Inventors:
Samir Patel, Richard Everett, Douglas Brooks, Shane Xinxin Tian
Abstract: The present invention provides an anti-IL-17 aptamer comprising a compound represented by the following formula (I): (each symbol is as defined in the DESCRIPTION) or a pharmaceutically acceptable salt, solvate or hydrate thereof, and showing improved in vivo stability.
Abstract: The invention relates to the fields of medicine and immunology. In particular, it relates to novel antisense oligonucleotides that may be used in the treatment, prevention and/or delay of Usher Syndrome type II and/or USH2A-associated non syndromic retina degeneration, especially by skipping a pseudo exon (PE40) between exon 40 and 41 in the human USH2A gene.
Type:
Application
Filed:
April 25, 2017
Publication date:
December 19, 2019
Inventors:
Hester Catharina VAN DIEPEN, Hee Lam CHAN, Janne Juha TURUNEN
Abstract: The present embodiments relate to the use of dextran sulfate having an average molecular weight below 10 000 Da for inducing angiogenesis in a subject and for increasing blood flow in a subject suffering from ischemia.
Abstract: The invention relates to substituted cyclodextrins and pharmaceutically acceptable salts thereof, pharmaceutical compositions, kits of parts and their use as procoagulants. The invention further relates to methods of reversing an anticoagulant effect of an anticoagulant in a subject, methods for reducing or preventing bleeding in a subject and methods for the treatment or prevention of a blood coagulation disorder.
Type:
Application
Filed:
May 1, 2017
Publication date:
December 19, 2019
Inventors:
Josephus Cornelis Maria MEIJERS, Kamran BAKHTIARI, Stephan Leonard Maria PETERS, Daniel Philipp ZOLLINGER
Abstract: The present invention provides pharmaceutical formulations including a non-anticoagulant, non-saccharide polymer that with at least one sulfate or sulfonate moiety. The pharmaceutical formulations of the invention are of use to improve blood clotting in a subject. Also provided are useful analytical methods utilizing these polymers to query the dynamics of blood clotting in vitro.
Type:
Application
Filed:
June 28, 2019
Publication date:
December 19, 2019
Inventors:
Michael Dockal, Fritz Scheiflinger, Sabine Knappe, Susanne Till, Ton Hai, Paul Sanders
Abstract: This invention relates generally to an emollient topical composition of matter that contains molecular iodine with a reduced effective vapor pressure. In specific embodiments, the composition reduces the loss of molecular iodine to the atmosphere under storage conditions after application to mammalian tissue.
Type:
Application
Filed:
July 19, 2017
Publication date:
December 19, 2019
Inventors:
Jack KESSLER, David C. LITZINGER, Christopher RHODES, Andrew M. CERRO
Abstract: The method of enhancing diamagnetic anisotropy in cell membranes that occur under the influence of disassociated polymorphic bCl? comprising changes in chloride ion channel expression and cell physiology. Direct current from a device generates an electromagnetic field in a 3 hypotonic saline solution leading to a dielectrophoretic disassociation of the chloride ion from its chloro-metabolites transforming it into a polymorphic diamagnetically disassociated bio-chloride (bCl?). This field treated aqueous solution induces a magnetic moment change in solution for some hours when no longer under the influence of the direct current; for when this field influenced solution is used to reconstitute growth media of human breast carcinoma (MDA-MB-231) and human breast epithelial (MCF-10A) cells in vitro, significant changes in chloride ion channel expression, membrane potential, cell volume, and a massive transcriptional reprogramming of 2,468 genes expressions by Human Genome U133 Plus 2.
Abstract: The present invention relates to compositions of extracellular vesicles (EVs) which are characterized by a strong proangiogenic activity and are effective in the therapeutic treatment of ischemic diseases and ischemic injuries or in wound healing. The extracellular vesicles (EVs) suitable for use in the compositions of the invention are either derived from a blood component or are selected by means of a potency test for pro-angiogenesis. Also disclosed is a method of manufacturing a pharmaceutical preparation of extracellular vesicles (EVs) characterized by a strong proangiogenic activity.
Type:
Application
Filed:
October 11, 2017
Publication date:
December 19, 2019
Applicant:
UNICYTE EV AG
Inventors:
Maria Felice BRIZZI, Giovanni CAMUSSI, Andrea RANGHINO
Abstract: The present invention is directed to a method of generating multilineage potential cells by de-differentiation of somatic leukocytes in a mixed leukocyte suspension from a blood sample. The present invention is also directed to the use of the generated multilineage potential cells to treat conditions in humans and mammals.
Abstract: Systems and methods for acquiring, preserving, and administering delipidated plasma. Extracted delipidated plasma, comprising pre-beta HDL, is obtained and are spot tested to establish baseline amounts or concentrations of pre-beta HDL. The batches are subjected to preservation, stored, and then prepared again for use at some later date. A portion of the batch may be tested again to determine if the pre-beta HDL in the delipidated plasma has degraded or is no longer effective.
Type:
Application
Filed:
December 19, 2018
Publication date:
December 19, 2019
Inventors:
Hollis Bryan Brewer, JR., Michael M. Matin
Abstract: Disclosed herein are methods of treating multiple myeloma in a human patient in need thereof, comprising administering to the human patient a population of allogeneic cells comprising WT1-specific allogeneic T cells. Also disclosed herein are methods of treating plasma cell leukemia in a human patient in need thereof, comprising administering to the human patient a population of allogeneic cells comprising WT1-specific allogeneic T cells.
Abstract: The present invention pertains to the field of T Cell receptors (TCR) identification and clonotyping, and especially concerns particular TCRs identified by clonotyping of a HIV-specific TCR repertoire, or fragments thereof. The invention relates especially to TCRs recognizing Gag peptide located between positions 293-312 in the GAG protein of HIV-1. The present invention further relates to nucleic acid constructs suitable as means for cloning or expressing nucleic acid molecules or TCRs of the invention, such as plasmids, vectors, especially lentiviraltransfer vectors. The invention is of particular interest in the context of therapeutic treatment of human beings seropositive for HIV.
Type:
Application
Filed:
February 23, 2017
Publication date:
December 19, 2019
Inventors:
Lisa Amita CHAKRABARTI, Daniela BENATI, Moran GALPERIN
Abstract: The present invention provides compositions and methods for combination therapy comprising administering to a patient in need thereof, drug-resistant immunotherapy, immune checkpoint inhibitors, and chemotherapy for the treatment of cancer.
Type:
Application
Filed:
February 18, 2019
Publication date:
December 19, 2019
Inventors:
Steven A. Lisi, William Ho, Lawrence S. Lamb, JR.