At Least Three Rings In The Polycyclo Ring System Patents (Class 514/250)
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Publication number: 20150099755Abstract: Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.Type: ApplicationFiled: December 12, 2014Publication date: April 9, 2015Inventors: Robert O. Cook, Jian Zhang, Thomas A. Armer
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Patent number: 8999967Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.Type: GrantFiled: September 28, 2011Date of Patent: April 7, 2015Assignee: Presidio Pharmaceuticals, Inc.Inventors: Leping Li, Min Zhong
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Patent number: 8999987Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: GrantFiled: March 6, 2013Date of Patent: April 7, 2015Assignee: BioMarin Pharmaceutical Inc.Inventors: Bing Wang, Daniel Chu
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Publication number: 20150093338Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: ApplicationFiled: October 8, 2014Publication date: April 2, 2015Inventor: Michael Farber
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Publication number: 20150094302Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: December 11, 2014Publication date: April 2, 2015Applicant: Genentech, Inc.Inventors: James John Crawford, Wendy B. Young
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Publication number: 20150094274Abstract: The invention relates to a combination comprising the N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2E-2-propenamide; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.Type: ApplicationFiled: December 8, 2014Publication date: April 2, 2015Inventors: Peter Wisdom Atadja, Wenlin Shao, Kapil N. Bhalla
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Publication number: 20150094313Abstract: Ecteinascidin formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided.Type: ApplicationFiled: October 9, 2014Publication date: April 2, 2015Inventors: Jacob Hendrik Beijnen, Bastiaan Nuijen, Pilar Calvo Salve, Maria Tobio Barreira
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Patent number: 8993572Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines of formula I: as described herein, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems.Type: GrantFiled: April 22, 2011Date of Patent: March 31, 2015Assignee: Intra-Cellular Therapies, Inc.Inventors: Sharon Mates, Robert Davis, Lawrence P. Wennogle, Peng Li, John Charles Tomesch, Qiang Zhang
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Publication number: 20150087633Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.Type: ApplicationFiled: December 1, 2014Publication date: March 26, 2015Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald D. Payan, Sylvia Braselmann
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Patent number: 8987271Abstract: The invention relates to a chemotherapeutic cancer treatment in which compounds (BH3Is) are administered to a mammal to treat B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. The invention also provides a method for treating types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more disclosed compounds in combination with other therapies, for example, 26S proteosome inhibitors, such as, for example, Bortezomib. The invention also relates to autoimmune treatment with pharmaceutical compositions comprising one or more disclosed compounds. The invention also relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.Type: GrantFiled: December 22, 2011Date of Patent: March 24, 2015Assignee: Eutropics Pharmaceuticals, Inc.Inventors: Michael H. Cardone, Xiang Y. Yu, Andrew F. Kolodziej
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Patent number: 8987270Abstract: The invention provides compositions and methods utilizing low concentrations of selective ?-2 adrenergic receptor agonists, preferably, brimonidine. The invention provides contact lens solutions and methods of using these solutions for pre-soaking contact lenses to achieve reduction of redness and/or increase in whitening of eyes. The invention also provides compositions including a selective ?-2 adrenergic receptor agonist in a combination with an ocular medical device, including but not limited to a bandage lens. The invention also provides combination compositions including a selective ?-2 adrenergic receptor agonist and another active agent for the treatment of an ocular condition, including but not limited to glaucoma and/or a condition associated with eye redness.Type: GrantFiled: September 7, 2012Date of Patent: March 24, 2015Assignee: Eye Therapies LLCInventor: Gerald Horn
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Publication number: 20150080405Abstract: The present invention, among other things, provides compounds, compositions and methods for treatment of cancer. In some embodiments, the present invention provides methods for treating blood cancer using agelastatin alkaloids.Type: ApplicationFiled: September 18, 2014Publication date: March 19, 2015Inventors: Mohammad Movassaghi, Paul J. Hergenrother
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Publication number: 20150079172Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems.Type: ApplicationFiled: April 14, 2013Publication date: March 19, 2015Inventors: Sharon Mates, Robert Davis, Peng Li, Lawrence Wennogle, Richard A. Lerner
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Publication number: 20150080406Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.Type: ApplicationFiled: November 19, 2014Publication date: March 19, 2015Inventors: Katerina Leftheris, Linghang Zhuang
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Publication number: 20150080404Abstract: The present invention relates to use of particular substituted heterocycle fused gamma-carbolines as described herein, in free, pharmaceutically acceptable salt or prodrug form, and pharmaceutical composition comprising the same optionally in combination with one or more agents, for the prophylaxis or treatment of one or more disorders associated with dementia, particularly behavioral or mood disturbances (e.g., agitation/aggression), psychosis, depression and sleep disturbances among others in patients suffering from dementia.Type: ApplicationFiled: April 14, 2013Publication date: March 19, 2015Inventors: Sharon Mates, Robert Davis, Kimberly Vanover, Lawrence Wennogle
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Patent number: 8980896Abstract: The present invention provides formulations which may comprise macrocyclic lactones and at least one spirodioxepinoindole derivative or a spirooxepinoindole derivative for combating parasites in birds and mammals. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.Type: GrantFiled: December 16, 2010Date of Patent: March 17, 2015Assignee: Merial, Inc.Inventors: Robert Holmes, Majid Razzak
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Publication number: 20150072964Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.Type: ApplicationFiled: April 14, 2013Publication date: March 12, 2015Inventors: Sharon Mates, Robert Davis, Kimberly Vanover, Lawrence Wennogle
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Patent number: 8975259Abstract: Disclosed are compositions and methods for treating diseases associated with G protein ?? subunit activity.Type: GrantFiled: April 28, 2008Date of Patent: March 10, 2015Assignee: University of RochesterInventors: Alan V Smrcka, Burns C. Blaxall, Jean M. Bidlack
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Publication number: 20150065515Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.Type: ApplicationFiled: March 14, 2013Publication date: March 5, 2015Inventors: Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
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Publication number: 20150065485Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Publication number: 20150057283Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: March 28, 2014Publication date: February 26, 2015Applicant: CHOONGWAE PHARMA CORPORATIONInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Publication number: 20150057287Abstract: Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (Cmax) and slightly delaying the peak such as to avoid activating the dopaminergic and adrenergic receptors, while achieving sufficient active binding to the serotonin receptors to provide relief from migraine symptoms within a timeframe that permits rapid resolution of migraine symptoms. Inhaler devices suitable for the methods are disclosed. Kits for practicing the methods of invention are disclosed.Type: ApplicationFiled: October 14, 2014Publication date: February 26, 2015Inventors: Robert O. Cook, Stephen B. Shrewsbury, Nabih N. Ramadan, Thomas A. Armer
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Patent number: 8962629Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: GrantFiled: June 9, 2009Date of Patent: February 24, 2015Assignee: AbbVie Inc.Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Bryan A. Fiamengo, Kristine E. Frank, Michael M. Friedman, Dawn M. George, Eric R. Goedken, Nathan S. Josephsohn, Biqin C. Li, Kent D. Stewart, Grier A. Wallace, Lu Wang, Kevin R. Woller
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Publication number: 20150051161Abstract: The present invention provides compositions and methods for detecting carboxymethyl-lysine (CML) and circulating receptor for advanced glycation end (RAGE) products, and methods for correlating CML and RAGE levels with age-related disease. In particular, serum CML and/or circulating receptor for advanced glycation end (RAGE) products can be used as a clinical biomarker in diagnostics to identify people who are at a higher risk of developing adverse ageing-related outcomes.Type: ApplicationFiled: April 10, 2014Publication date: February 19, 2015Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Richard David Semba, Luigi Ferruci, Edward G. Lakatta
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Publication number: 20150051191Abstract: Alcoholism, and symptoms and negative effects thereof may be treated using ibudilast or a pharmaceutically acceptable salt thereof. Abstinence from alcohol consumption may be maintained using ibudilast or a pharmaceutically acceptable salt thereof. Withdrawal from alcohol may be facilitated and negative effects thereof reduced by using ibudilast or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 14, 2014Publication date: February 19, 2015Applicant: MEDICINOVA, INC.Inventors: Yuichi IWAKI, Kirk JOHNSON
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Publication number: 20150051214Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.Type: ApplicationFiled: March 14, 2013Publication date: February 19, 2015Inventors: Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
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Patent number: 8952008Abstract: The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.Type: GrantFiled: December 12, 2013Date of Patent: February 10, 2015Assignee: Pfizer LimitedInventors: Kiyoyuki Omoto, Robert McKenzie Owen, David Cameron Pryde, Christine Ann Louise Watson, Mifune Takeuchi
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Patent number: 8946213Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: April 7, 2014Date of Patent: February 3, 2015Assignee: Genentech, Inc.Inventors: James John Crawford, Wendy B. Young
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Patent number: 8946223Abstract: This invention provides compounds of formula (I): wherein X1, X2, R1a, R1b, R1c, R1d, n, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: April 11, 2011Date of Patent: February 3, 2015Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Janice Chin, Kenneth M. Gigstad, He Xu
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Publication number: 20150031655Abstract: The disclosure provides a method of treating a mammal afflicted with an age-related disorder, comprising administering to the mammal a combination of liver X receptor (LXR) modulator and estrogen receptor (ER) modulator, in an amount effective to treat the mammal. Further disclosed are the LXR modulators and ER modulators used in the combination therapy.Type: ApplicationFiled: April 10, 2012Publication date: January 29, 2015Applicant: UNIVERSITY OF NORTH DAKOTAInventor: Othman Ghribi
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Publication number: 20150031652Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: August 1, 2014Publication date: January 29, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20150030669Abstract: The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.Type: ApplicationFiled: March 11, 2013Publication date: January 29, 2015Applicant: MERCK PATENT GMBHInventors: Michael Wilhelm Platscher, Raymond Behrendt, Viola Groehn, Simone Rachel Hoertner, Marco Silvio Passafaro, Finn Bauer
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Publication number: 20150031701Abstract: Pharmaceutical compositions comprising 5-[2-pyrazinyl]-4-methyl-1,2-3-thione or an analogue, derivative, metabolite, prodrug, solvate or a pharmaceutically acceptable salt thereof; and a pharmaceutical carrier, which promotes association with the outer wall of a subject's digestive tract are described as well as their uses in treating and preventing mucositis and cachexia.Type: ApplicationFiled: August 6, 2014Publication date: January 29, 2015Inventor: Patrick T. Prendergast
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Publication number: 20150024995Abstract: The present invention is directed to a method of treating a metabolic disorder or key elements of a metabolic disorder such method comprising the use of an agent(s) that increases central dopaminergic activity plus a first-phase insulin secretagouge.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Inventor: Anthony H. Cincotta
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Publication number: 20150023888Abstract: The invention is drawn to a novel, early interventional use of a pharmaceutical composition wherein administration of said pharmaceutical composition pre-empts the onset of migraine headaches, preferably anytime in the migraine cycle prior to pain onset. The pharmaceutical composition preferably is administered via inhalation in order to provide therapy to the subject in a timely fashion, ideally in a non-clinical setting. The pharmaceutical composition may also be administered to a subject at risk for stroke.Type: ApplicationFiled: September 30, 2014Publication date: January 22, 2015Inventors: ROBERT O. COOK, PAUL L. DURHAM
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Publication number: 20150018340Abstract: The present invention relates to compounds having a pipecolate diketoamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate diketoamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.Type: ApplicationFiled: December 24, 2012Publication date: January 15, 2015Inventors: Ranganath Gopalakrishnan, Felix Hausch
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Publication number: 20150018298Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
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Publication number: 20150018361Abstract: The present invention relates to methylene-tetrahydrofolate for use in the treatment of cancer, based on its intrinsic antitumor activity. The cancers that may be treated include breast cancer, gastric cancer, gastrointestinal cancer, gall bladder cancer, bile duct cancer, colon cancer, rectal cancer, liver cancer, pancreatic cancer, head and neck cancer, esophageal cancer, mesothelioma cancer, lung cancer including non-small-cell lung cancer, ovarian cancer, endometrial cancer, cervical cancer, peripheral cell lymphoma (PTCL), melanoma, brain tumors, adenocarcinoma, esophageal cancer, and osteosarcoma.Type: ApplicationFiled: January 18, 2013Publication date: January 15, 2015Applicant: ISOFOL MEDICAL ABInventors: Bengt Gustavsson, Björn Carlsson
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Publication number: 20150018362Abstract: The invention described herein relates to methods for treating mitochondrial diseases. In particular, the invention relates to methods for treating mitochondrial diseases by administering therapeutically effective amounts of one or more tetracyclic pyrazinoindoles, and/or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 26, 2013Publication date: January 15, 2015Inventors: Spyros Deftereos, Andreas Persidis
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Publication number: 20150018359Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein L, R5, W, X, Y1, Y2, and Z are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Manoj C. DESAI, Mingzhe JI, Haolun JIN, Teresa Alejandra TREJO MARTIN, Hyung-Jung PYUN
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Publication number: 20150018360Abstract: The present invention provides, inter alia, compositions containing enantiomerically pure (R)(+)-amisulpride or enantiomerically pure (R)(+)-sulpiride, optionally with dopamine receptor modulators. The present invention also provides compositions containing racemic (RS)-amisulpride or (RS)-sulpiride in combination with dopamine receptor modulators. Methods for preventing, treating, or ameliorating the effects of a metabolic disorder or key element thereof, for modulating blood glucose levels, and for preventing, treating, or ameliorating the effects of diabetes in a subject are also provided. Additionally, the present invention provides methods for counter-acting the dopamine antagonist activity of (S)-amisulpride in racemic (RS)-amisulpride, or the dopamine antagonist activity of (S)-sulpiride in racemic (RS)-sulpiride, administered to a subject to prevent, treat, or ameliorate the effects of a metabolic disorder.Type: ApplicationFiled: September 13, 2012Publication date: January 15, 2015Applicant: BIOMED VALLEY DISCOVERIES, INC.Inventors: Reza Halse, Jeffrey James Roix, Saurabh Saha
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Publication number: 20150018348Abstract: Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof.Type: ApplicationFiled: September 26, 2014Publication date: January 15, 2015Inventor: Francis Xavier Tavares
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Publication number: 20150011557Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.Type: ApplicationFiled: September 7, 2012Publication date: January 8, 2015Applicant: Merck Patent GmbHInventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
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Publication number: 20150010509Abstract: Disclosed herein are methods for the treatment of cancer and inflammatory-based diseases and disorders, such as hepatitis B virus infection, tuberculosis and type 2 diabetes based upon the administration of CaFolate. In one embodiment is a method of treating cancer comprising administration of CaFolate. In another embodiment is a method of treatment inflammatory-based disease and disorders comprising administration of CaFolate.Type: ApplicationFiled: January 29, 2013Publication date: January 8, 2015Applicant: SanRx Pharmaceuticals, Inc.Inventor: Phillip Moheno
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Publication number: 20150010619Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.Type: ApplicationFiled: September 26, 2014Publication date: January 8, 2015Applicant: Strategic Science & Technologies, LLCInventor: Eric T. Fossel
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Publication number: 20150005307Abstract: The invention provides a pharmaceutical composition for the transmucosal delivery of a PDE5 inhibitor, said composition comprising a PDE5 inhibitor and a carrier in which said PDE5 inhibitor is soluble or forms a suspension or emulsion. The invention also provides a pharmaceutical composition comprising a PDE5 inhibitor for use in inhibiting PDE activity in vivo, where in said use said composition is delivered by the transmucosal route.Type: ApplicationFiled: December 19, 2012Publication date: January 1, 2015Applicant: LondonPharma Ltd.Inventors: Martin James Sams, Juliet Victoria High, Paul Andrew Jamieson, Clive Booles
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Patent number: 8921369Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: GrantFiled: December 2, 2009Date of Patent: December 30, 2014Assignee: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
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Patent number: 8921353Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: March 13, 2014Date of Patent: December 30, 2014Assignee: Genentech, Inc.Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
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Publication number: 20140378415Abstract: The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C—H, C—R5, or nitrogen; G1 is oxygen or sulfur; X4 is C1-C8 haloalkyl; R4 is aryl or aryl substituted by one to five R9, or heteroaryl or heteroaryl substituted by one to five R9; and R1, R2, R4, R5, R9 and Z are as defined in the claims. The invention also provides compositions comprising the compounds of formula (I), intermediates useful in the preparation of compounds of formula (I) and methods of using the compounds of formula (I) to control insects, acarines, nematodes or molluscs.Type: ApplicationFiled: August 27, 2012Publication date: December 25, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20140378432Abstract: Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 8, 2014Publication date: December 25, 2014Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young