Patents Issued in May 4, 2017
  • Publication number: 20170119702
    Abstract: A compound of formula I: wherein X is O, S, SO or SO2; R1 is halogen, trihalomethyl, —OH, C1-7alkyl, C1-4alkoxy, trifluoromethoxy, phenoxy, cyclohexylmethyloxy, pyridylmethoxy, cinnamyloxy, naphthylmethoxy, phenoxymethyl, —CH2—OH, —CH2—CH2—OH, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, benzylthio, acetyl, nitro or cyano, or phenyl, phenylC1-4alkyl or phenyl-C1-4alkoxy each phenyl group thereof being optionally substituted by halogen, CF3, C1-4alkyl or C1-4alkoxy; R2 is H, halogen, trihalomethyl, C1-4alkoxy, C1-7alkyl, phenethyl or benzyloxy; R3 H, halogen, CF3, OH, C1-7alkyl, C1-4alkoxy, benzyloxy, phenyl or C1-4alkoxymethyl; each of R4 and R5, independently is H or a residue of formula (a) wherein each of R8 and R9, independently, is H or C1-4alkyl optionally substituted by halogen; and n is an integer from 1 to 4; or a pharmaceutically acceptable salt, hydrate, solvate, isomer or prodrug thereof; or a compound of formula II wherein R1a is halogen, trihalomethyl, C1-4alkyl, C1-4alko
    Type: Application
    Filed: October 19, 2016
    Publication date: May 4, 2017
    Applicant: Novartis AG
    Inventors: Peter Gergely, Erik Wallstroem, Eric Legangneux
  • Publication number: 20170119703
    Abstract: Dapsone compositions can be useful for treating acne. The methods and formulations disclosed herein show efficacy for treating acne vulgaris and/or post inflammatory hyperpigmentation.
    Type: Application
    Filed: November 4, 2016
    Publication date: May 4, 2017
    Inventors: Kevin S. Warner, Ajay P. Parashar, Vijaya Swaminathan, Varsha Bhatt, Alexandre Kaoukhov
  • Publication number: 20170119704
    Abstract: Provided are methods of treating cognitive impairment and/or psychosis and/or movement disorders by administering a pharmaceutical composition of eplivanserin or a pharmaceutically acceptable salt thereof to a subject in need thereof.
    Type: Application
    Filed: October 13, 2016
    Publication date: May 4, 2017
    Inventor: Matthew DURING
  • Publication number: 20170119705
    Abstract: The present invention relates to a composition comprising an antibacterial agent in an amount insufficient to provide antibacterial effect, a physiologically acceptable divalent metal ion in a very low concentration and a physiologically acceptable polymer for preventing and/or treating halitosis, bad breath, dry mouth or sore throat.
    Type: Application
    Filed: June 17, 2015
    Publication date: May 4, 2017
    Inventor: Thomas BERGLUND
  • Publication number: 20170119706
    Abstract: Described herein are pharmaceutical compositions containing Adelmidrol. In particular, the Adelmidrol is used in the treatment of diseases characterized by insufficient specific agonism of the PPAR-gamma receptor in humans or animals, more particularly in the treatment of articular chondropathies of mechanical, toxic, iatrogenic, degenerative origin, or associated with inflammatory phenomena mainly related to organs and tissues not belonging to the osteoarticular system; fibrogenesis of the articular cartilages; chronic inflammatory bowel diseases (IBDs) such as Crohn's disease and ulcerative colitis; Irritable Bowel Syndrome (IBS); diseases characterized by an abnormal fibrosis of the connective tissue, such as systemic sclerosis, particularly of the skin and lung; eye disorders characterized by angiogenesis, fibrosis, inflammation and oxidative stress.
    Type: Application
    Filed: October 24, 2016
    Publication date: May 4, 2017
    Applicant: Epitech Group S.P.A.
    Inventors: Francesco DELLA VALLE, Maria Federica DELLA VALLE, Salvatore CUZZOCREA
  • Publication number: 20170119707
    Abstract: A homeopathic topical gel for transdermal delivery of colchicine formulations is disclosed. The colchicine formulations are effective in the treatment of constantly recurring acute gout flares. The homeopathic topical gels deliver an attenuated colchicine which has been produced using a degree of succussion and a level of water purity in excess of the guidelines for manufacturing homeopathic medicines set forth in the Homeopathic Pharmacopoeia of the United States.
    Type: Application
    Filed: January 17, 2017
    Publication date: May 4, 2017
    Inventors: Carlos A. Alfaras, Urbano Zamora
  • Publication number: 20170119708
    Abstract: The present disclosure comprises methods and compositions comprising an extracted mineral element composition to modulate muscle and/or bone loss, or deleterious muscle tone change.
    Type: Application
    Filed: October 31, 2016
    Publication date: May 4, 2017
    Inventors: Luke Blotsky, Krys Bojanowski
  • Publication number: 20170119709
    Abstract: A method of treatment for third spacing is provided. The method includes identifying an adverse factor, which includes conditions causing an increase in vascular permeability resulting in third spacing. The method also includes diagnosing the patient with third spacing, which can include third spacing of fluids, materials, or both. The patient is treated with a therapeutically effective amount of a non-increased vascular permeability modifier loop diuretic, such as a non-sulfonamide loop diuretic like ethacrynic acid or ethacrynate sodium.
    Type: Application
    Filed: March 10, 2016
    Publication date: May 4, 2017
    Inventor: Robin L. Webb
  • Publication number: 20170119710
    Abstract: Techniques are disclosed for prevention or treatment of physiological shock by administering a specific therapeutic agent, which is able to use smaller volumes of reagent to achieve complete inhibition, than other previously described techniques.
    Type: Application
    Filed: January 11, 2017
    Publication date: May 4, 2017
    Inventors: Geert W. Schmid-Schoenbein, Frank A. DeLano
  • Publication number: 20170119711
    Abstract: Described herein are soft capsules and enteric soft capsules comprising cationic Type A gelatin and acid insoluble enteric polymers. In particular, the compositions and methods for manufacturing all-natural enteric soft capsules comprising Type A gelatin and matrix fills are described. In one embodiment, the enteric soft capsules comprise active ingredients such as non-steroidal anti-inflammatory drugs (NSAIDs). In another embodiment, the enteric soft capsule comprises matrix fills of omega-3 fatty acids.
    Type: Application
    Filed: January 12, 2017
    Publication date: May 4, 2017
    Inventors: Yunhua Hu, Martin Piest, Qi Fang, Henricus van Duijnhoven
  • Publication number: 20170119712
    Abstract: Methods of suppressing cyclooxygenase activity or reducing platelet aggregation of a mammal in need thereof by administering to a mammal in need thereof an effective amount of trans-resveratrol and arginine for a period of at least two weeks.
    Type: Application
    Filed: October 28, 2015
    Publication date: May 4, 2017
    Inventors: SHIL KOTHARI, GARY TROXEL
  • Publication number: 20170119713
    Abstract: Disclosed herein are methods of treating disease with a combination of a RXR agonist and a thyroid hormone.
    Type: Application
    Filed: October 31, 2016
    Publication date: May 4, 2017
    Inventors: Roshantha A. Chandraratna, Martin E. Sanders
  • Publication number: 20170119714
    Abstract: Disclosed herein are methods of treating disease with a combination of a RXR agonist and a thyroid hormone.
    Type: Application
    Filed: October 31, 2016
    Publication date: May 4, 2017
    Inventors: Roshantha A. Chandraratna, Martin E. Sanders
  • Publication number: 20170119715
    Abstract: Isolated polynucleotide molecules and peptides encoded by these molecules are used in the analysis of human carbamyl phosphate synthetase I phenotypes, as well as in diagnostic and therapeutic applications, relating to a human carbamyl phosphate synthetase I polymorphism. By analyzing genomic DNA or amplified genomic DNA, or amplified cDNA derived from mRNA, it is possible to type a human carbamyl phosphate synthetase I with regard to the human carbamyl phosphate synthetase I polymorphism, for example, in the context of diagnosing and treating hepatic veno-occlusive disease (HVOD) associated with bone marrow transplants.
    Type: Application
    Filed: November 4, 2016
    Publication date: May 4, 2017
    Inventors: Marshall L. SUMMAR, Brian W. Christman, Frederick E. Barr
  • Publication number: 20170119716
    Abstract: Herein described are deuterated catecholamine derivatives of the general Formula I wherein, R1 is deuterium, R2, and R3 are independently selected from hydrogen and deuterium and wherein at least one of R2 and R3 has a deuterium enrichment in the range from 0.02 mol % to 100 mol % deuterium, and wherein the deuterium enrichment of R2 and R3 is different from each other and that the difference between the deuterium enrichment of R2 and R3 is at least 5 percentage points, R4 is hydrogen, deuterium, C1 to C6-alkyl or C5 to C6-cycloalkyl, deuterated C1 to C6-alkyl or C5 to C6-cycloalkyl, or a group that is easily hydrolytically or enzymatically cleavable under physiological conditions, as well as their physiologically acceptable salts and their stereoisomers, enantiomers or diastereomers in optically pure form. The compounds can easily be prepared by mixing deuterated and non-deuterated compounds in a predefined ratio. The compounds show anti-Parkinson effect at lower doses and show lower side effects.
    Type: Application
    Filed: January 10, 2017
    Publication date: May 4, 2017
    Inventors: Rudolf-Giesbert Alken, Frank Schneider
  • Publication number: 20170119717
    Abstract: Described herein are nitrated lipids and methods of making and using the nitrated lipids.
    Type: Application
    Filed: November 21, 2016
    Publication date: May 4, 2017
    Inventors: Bruce A. Freeman, Francisco Schopfer, Valerie O'Donnell, Paul Baker, Yuqing E. Chen, Bruce Branchaud
  • Publication number: 20170119718
    Abstract: Methods of increasing the plasma concentration of resveratrol in a mammal in need thereof by administering to a mammal in need thereof an effective amount of trans-resveratrol and arginine for a period of at least two weeks.
    Type: Application
    Filed: October 28, 2015
    Publication date: May 4, 2017
    Inventors: SHIL KOTHARI, GARY TROXEL
  • Publication number: 20170119719
    Abstract: The present invention relates to novel crystalline forms of ingenol ingenol-3-angelate and methods of preparation and use thereof. More specifically, the invention relates to a novel crystalline form and purified forms of the compound of Formula 1 (ingenol-3-mebutate; ingenol-3-angelate; isoform ‘b’; PEP005), which is characterized by, for example, attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy, single crystal X-Ray crystallography (XRC), X-ray powder diffraction, and, Differential Scanning calorimetry (DSC), and methods of preparation and use thereof.
    Type: Application
    Filed: November 14, 2016
    Publication date: May 4, 2017
    Inventor: Steven Martin Ogbourne
  • Publication number: 20170119720
    Abstract: The present invention relates to homogeneous formulations comprising omega-3 polyunsaturated fatty acids (n-3 PUFA) and resveratrol for oral administration, in which the resveratrol is solubilized in a solvent system consisting of omega-3 polyunsaturated fatty acids (n-3 PUFA), or their alkyl esters, and a ionic emulsifier. The composition according to the present invention can be formulated as food or nutritional supplement or medicament in the prevention or treatment of cardiovascular diseases due to lipid metabolism disorders and increased platelets aggregation, as well as damages due to free radicals and/or viral diseases.
    Type: Application
    Filed: March 26, 2015
    Publication date: May 4, 2017
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
    Inventors: Giuseppe GIANNINI, Mosè SANTANIELLO
  • Publication number: 20170119721
    Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases.
    Type: Application
    Filed: November 14, 2016
    Publication date: May 4, 2017
    Inventor: Joseph S. Zakrzewski
  • Publication number: 20170119722
    Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.
    Type: Application
    Filed: January 17, 2017
    Publication date: May 4, 2017
    Inventors: Mehar Manku, Ian Osterloh, Pierre Wicker, Rene Braeckman, Paresh Soni
  • Publication number: 20170119723
    Abstract: In various embodiments, the present invention provides methods of reducing the risk of a cardiovascular event in a subject on statin therapy and, in particular, a method of reducing the risk of a cardiovascular event in a subject on statin therapy having a fasting baseline triglyceride level of about 135 mg/dL to about 500 mg/dL, and administering to the subject a pharmaceutical composition comprising about 1 g to about 4 g of eicosapentaenoic acid ethyl ester or a derivative thereof.
    Type: Application
    Filed: January 18, 2017
    Publication date: May 4, 2017
    Inventor: Paresh Soni
  • Publication number: 20170119724
    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.
    Type: Application
    Filed: January 18, 2017
    Publication date: May 4, 2017
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Hirosato FUJII, Motoo YAMAGATA
  • Publication number: 20170119725
    Abstract: The present invention relates to purified 3-methanesulfonylpropionitrile or a pharmaceutically acceptable salt thereof, and a method for preparing such compound. The compound has at least 90% (w/w) purity. The present invention is also directed to a pharmaceutical composition comprises the purified compound and a pharmaceutically acceptable carrier. The present invention is further directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering 3-methanesulfonylpropionitrile or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.
    Type: Application
    Filed: November 11, 2016
    Publication date: May 4, 2017
    Inventor: Joseph ST. LAURENT
  • Publication number: 20170119726
    Abstract: Disclosed herein are improved formulations for the cabazitaxel. The formulations exhibit increased storage stability relative to other formulations, and are simpler for health care providers to prepare and administer to patients.
    Type: Application
    Filed: November 3, 2016
    Publication date: May 4, 2017
    Inventors: Geena Malhotra, Sarabjit Singh, Ravichandra Bhadravathi Vedamurthy, Anirban Mallik Thakur, Dhiraj Abhyankar
  • Publication number: 20170119727
    Abstract: The present invention is directed to a pharmaceutical combination for treating proliferative disease comprising a compound of formula (I), or a salt, solvate or prodrug thereof, carboplatin or cisplatin, and gemcitabine. The present invention is further directed to a therapeutic protocol to manage ovarian cancer treatment in a female subject involving the administration of the combination to an ovarian cancer subject with recurrent or persistent ovarian cancer following treatment with platinum-based therapy. Kits comprising the combination as well as the use of the combination in the treatment of a proliferative disease are further contemplated.
    Type: Application
    Filed: May 30, 2014
    Publication date: May 4, 2017
    Applicant: Bionomics Limited
    Inventors: Gabriel Kremmidiotis, David C. BIBBY, Danny RISCHIN
  • Publication number: 20170119728
    Abstract: A composition of an edible base product, the composition comprising a cannabis concentrate containing at least one cannabinoid, a starch concentrate containing tapioca maltodextrin, a rice concentrate, and a lipid concentrate containing lecithin. The method of producing the composition comprises sheering the ingredients at a proper temperature in a dry environment. Preferably, the rice concentrate acts as a natural desiccate and silicate and also an anti-caking agent. The lecithin is added to the powdered cannabis concentrate to enhance the absorption of THC into the blood stream of the individuals.
    Type: Application
    Filed: October 27, 2016
    Publication date: May 4, 2017
    Applicant: NBDD, Inc.
    Inventor: Doug DeGeeter
  • Publication number: 20170119729
    Abstract: The invention provides compounds and plant extract compositions that inhibit pancreatic enzymes, such as lipases and amylases, and most particularly pancreatic lipase and phospholipase A2 (PLA2), and COX-2 enzyme, and improve the inflammatory state or response conditions in animals. The compounds and plant extracts can be used in methods and administration regimens to treat animals for obesity-related conditions, diabetes and related conditions, metabolic syndrome, metabolic endotoxemia, and inflammatory conditions. The compounds and plant extracts can also be used to produce comestible compositions to be incorporated into a normal diet to improve health or prevent or reduce the uptake of free fatty acids during digestion or the production of inflammatory eicosanoids or cytokines. The inhibitor compounds and compositions include cocoa-derived polymers of epicatechin, such as epicatechin-rich polymers of 2 units through polymers of 14 units, or 5 to 14 units, and combinations of them.
    Type: Application
    Filed: November 10, 2016
    Publication date: May 4, 2017
    Applicant: THE HERSHEY COMPANY
    Inventors: W. Jeffrey HURST, David A. STUART, Joshua D. LAMBERT, Yeyi GU
  • Publication number: 20170119730
    Abstract: The present invention features a novel therapy for effecting weight loss which involves treating a subject with a sympathomimetic agent (e.g., phentermine or a phentermine-like drug) in combination with an anticonvulsant sulfamate derivative (e.g., topiramate) such that the subject experiences weight loss. The combination methods of the present invention also are effective against symptoms associated with Syndrome X. The invention also features pharmaceutical compositions and kits for use in the practice of these novel therapies.
    Type: Application
    Filed: June 3, 2016
    Publication date: May 4, 2017
    Inventor: Thomas Najarian
  • Publication number: 20170119731
    Abstract: The invention provides compounds, methods, pharmaceutical compositions, and kits for the treatment of proliferative disorders such as cancer. In one aspect, the methods comprise compounds that inhibit the activity of protein kinases, such as cell division cycle (Cdc) kinase. In another aspect, the methods comprise compounds that inhibit Cdc7 and/or Dbf4 activity. In another aspect, the methods comprise compounds that exhibit anti-proliferative properties useful in treating diseases such as cancer. Compounds useful for any of the methods include compounds of the Formula (A) or (B): or pharmaceutically acceptable salts thereof. Exemplary compounds of Formula (A) or (B) include granaticin A, granaticin B, dihydrogranaticin A, dihydrogranaticin B, medermycin, and actinorhodin.
    Type: Application
    Filed: November 11, 2016
    Publication date: May 4, 2017
    Applicant: Sloan-Kettering Institute for Cancer Research
    Inventors: Mark G. Frattini, Hakim Djaballah, Thomas J. Kelly
  • Publication number: 20170119732
    Abstract: Provided herein are compositions and methods for preventing or reducing scar formation (e.g., hypertrophic scars). Certain embodiments provide a method of preventing hypertrophic scar formation in a subject comprising administering a HMG-CoA reductase-inhibiting agent to a wound site. In some embodiments, the wound site comprises scar tissue.
    Type: Application
    Filed: January 17, 2017
    Publication date: May 4, 2017
    Inventors: Thomas A. Mustoe, Peter Kim, Jason Ko, Xianzhong Ding, Yanan Zhao
  • Publication number: 20170119733
    Abstract: The present invention describes peptides comprising phycocyanobilin (PCB), as well as the medical use of said peptides and that of PCB, due to the neuroprotector and/or neuroregenerative effects identified for them. Furthermore, pharmaceutical combinations of said peptides and of PCB with proteins or other peptides with synergic effect justify their use for ischemic or neurodegenerative CNS disease treatment.
    Type: Application
    Filed: November 10, 2016
    Publication date: May 4, 2017
    Inventors: Giselle Penton Rol, Alexey Llopiz Arzuaga, Javier Marin Prida, Eduardo Penton Arias, Efrain Rodriguez Jimenez, Alexis Musacchio Lasa, Vladimir Armando Besada Perez, Gilberto Lazaro Pardo Andreu, Luis Javier Gonzalez Lopez, Nancy Pavon Fuentes, Gerardo Enrique Guillen Nieto, Pedro Antonio Lopez Saura
  • Publication number: 20170119734
    Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof, wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.
    Type: Application
    Filed: April 22, 2016
    Publication date: May 4, 2017
    Inventors: Adilah Bahadoor, Alfredo C. Castro, Lawrence K. Chan, Gregg F. Keaney, Marta Nevalainen, Vesa Nevalainen, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20170119735
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: June 10, 2016
    Publication date: May 4, 2017
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kevin Wayne Kuntz
  • Publication number: 20170119736
    Abstract: Disclosed are a compound of Formula I, having higher inhibition of protein kinase G (PKG) activity and pharmaceutically acceptable salts thereof. In Formula I, R1 and R2 are the same or different, each being independently chosen from the halogens, the C1-C6 alkoxyl group, the C1-C6 alkyl group, the C2-C6 alkenyl group, and the C2-C6 alkynyl group; R3 is chosen from H, the halogens, the substituted or unsubstituted C1-C6 alkyl group, C3-C6 cycloalkyl group, C2-C6 alkenyl group, and C2-C6 alkynyl group, aryl group, and heteroaryl group; and n is an integer between 0 and 15. Also disclosed is a pharmaceutical composition comprising said compound, the use of the compound in treating pains, in particular chronic pain, a preparation method for the compound, and a new intermediate.
    Type: Application
    Filed: January 18, 2017
    Publication date: May 4, 2017
    Inventors: Zewang Feng, Xuan Zhao, Zhenguo Wang, Yan Liu
  • Publication number: 20170119737
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: January 18, 2017
    Publication date: May 4, 2017
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20170119738
    Abstract: The present application relates to a method of treating a migraine headache in a patient by administering a pharmaceutical composition including rizatriptan or pharmaceutically acceptable salts thereof contained in a unit dose.
    Type: Application
    Filed: October 28, 2016
    Publication date: May 4, 2017
    Inventors: Rajeev Singh RAGHUVANSHI, Piyush GUPTA, Rajesh Ramesh PATIL, Mohan RATHI
  • Publication number: 20170119739
    Abstract: The object of the present invention is to inhibit oxidative metabolism of a compound of formula I by co-administration with ritonavir, a cytochrome P450 inhibitor.
    Type: Application
    Filed: January 12, 2017
    Publication date: May 4, 2017
    Applicant: Roche Palo Alto LLC
    Inventor: Jonathan Q. Tran
  • Publication number: 20170119740
    Abstract: Methods for treating cancer by activation of the Bmp pathway are disclosed. In particular, the invention relates to methods of treating cancer using agents that activate BMP signaling, e.g., FK506 (tacrolimus), to treat a subject for cancer.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 4, 2017
    Inventors: Philip A. BEACHY, Kunyoo SHIN
  • Publication number: 20170119741
    Abstract: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites, N-oxides and prodrugs thereof.
    Type: Application
    Filed: June 13, 2016
    Publication date: May 4, 2017
    Inventors: John Yan, Xiaoxia Zheng, Vinayak D. Bhat
  • Publication number: 20170119742
    Abstract: The present invention relates to a medicament for preventing and/or treating stress diseases, said medicament being characterized in that (1S)-2-acetyl-1-(4-chloro-2-methoxyphenyl)-5-fluoro-1,2,3,9-tetrahydrospiro[?-carboline-4,1?-cyclopropane] is administered at such a specific dose that a brain TSPO occupancy requiring for expressing the pharmacological effects of the medicament can be obtained.
    Type: Application
    Filed: June 11, 2015
    Publication date: May 4, 2017
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Seishi KATSUMATA, Katsukuni MITSUI
  • Publication number: 20170119743
    Abstract: A method for treating rheumatoid arthritis, multiple sclerosis, or a disease involving JAK3, including administering a compound of the formula (I) or a salt thereof to a subject
    Type: Application
    Filed: January 12, 2017
    Publication date: May 4, 2017
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masayuki NAKAMURA, Hiroyoshi YAMANAKA, Kazuaki SHIBATA, Morihiro MITSUYA, Takafumi HARADA
  • Publication number: 20170119744
    Abstract: The present invention relates to pharmaceutical compositions for inhalation which comprise one or more bronchodilators.
    Type: Application
    Filed: June 18, 2015
    Publication date: May 4, 2017
    Applicant: Cipla Limited
    Inventors: Geena MALHOTRA, Preeti RAUT
  • Publication number: 20170119745
    Abstract: Methods of treating, preventing or managing hematologic disorders, such as leukemia are disclosed. The methods encompass the administration of SNS-595. Also provided are methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. In certain embodiments, the method of treatment comprise administering SNS-595 in combination with Ara-C. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed.
    Type: Application
    Filed: June 3, 2016
    Publication date: May 4, 2017
    Inventors: Daniel C. Adelman, Jeffrey A. Silverman, Glenn Michelson, Caroline Dame Scatena
  • Publication number: 20170119746
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: September 28, 2015
    Publication date: May 4, 2017
    Inventors: Merouane Bencherif, Nikolai Federov, Terry Hauser, Kristen G. Jordan, Sharon Rae Letchworth, Anatoly Mazurov, Julio A. Munoz, Jason Speake, Daniel Yohannes
  • Publication number: 20170119747
    Abstract: A method of treating a patient in need of treatment for a disease selected from the group consisting of cancer, hamartoma syndrome and hereditary myopathy, the method comprising administering to the patient an effective dose of at least one PRCP and PREP dual antagonist pyridine compound of Formula (I) or an acid salt thereof, which can be administered either alone or in combination with at least one mTOR inhibitor.
    Type: Application
    Filed: November 22, 2016
    Publication date: May 4, 2017
    Inventors: Lei Duan, Victor Levenson, GuoGuang Ying
  • Publication number: 20170119748
    Abstract: This invention provides methods, compounds and compositions for the treatment of musculoskeletal disease, muscle dysfunction, muscle-wasting disease or disorder, including hereditary myopathy, neuromuscular disease, muscular dystrophy, muscular atrophy, drug-induced myopathy, and related disease, disorder or condition that causes a decrease in muscle strength, comprising the use of heterocyclic non-peptidic compounds that act as Mas agonists and/or mimics of angiotensin 1-7.
    Type: Application
    Filed: July 17, 2015
    Publication date: May 4, 2017
    Inventors: Kevin J. GAFFNEY, Kathleen E. RODGERS, Stan G. LOUIE, Gere S. DIZEREGA, Nicos A. PETASIS
  • Publication number: 20170119749
    Abstract: Methods and compositions for enhancing female sexual arousal and treating female sexual dysfunction utilize L-arginine or equivalents and/or derivatives thereof, and an agent that enhances the activity of the L-arginine or equivalent thereof These enhancing agents include niacin and/or nicotinamide. Niacin and/or nicotinamide, in combination with L-arginine or its equivalent allow a desired amount of nitric oxide to be delivered or generated at the female genitals in order to increase vasodilation and blood flow to the area to enhance sexual arousal and/or pleasure and to treat sexual dysfunction.
    Type: Application
    Filed: October 30, 2015
    Publication date: May 4, 2017
    Inventors: Guy M. Stofman, Michael J. Pelekanos
  • Publication number: 20170119750
    Abstract: Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
    Type: Application
    Filed: November 15, 2016
    Publication date: May 4, 2017
    Inventors: Stephen John Atkinson, Michael David Barker, Matthew Campbell, Hawa Diallo, Clement Douault, Neil Stuart Garton, John Liddle, Robert John Sheppard, Ann Louise Walker, Christopher Wellaway, David Matthew Wilson
  • Publication number: 20170119751
    Abstract: The present invention provides an aminopyridine compound, or a pharmaceutically acceptable salt thereof, that inhibits Aurora A and, therefore may be useful in treating cancer.
    Type: Application
    Filed: January 17, 2017
    Publication date: May 4, 2017
    Inventor: James Robert Henry