The Nitrogen In R Is An Amino Nitrogen Attached Indirectly To A Ring By Acyclic Bonding Patents (Class 514/620)
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Patent number: 7741371Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The compounds are selective androgen receptor modulators (SARM) useful for, inter-alia, suppressing spermatogenesis, treating a subject having a hormone related condition, treating a subject suffering from prostate cancer, delaying the progression of prostate cancer, preventing the recurrence of prostate cancer, and treating the recurrence of prostate cancer.Type: GrantFiled: March 31, 2006Date of Patent: June 22, 2010Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Craig A. Marhefka, Wenqing Gao
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Publication number: 20100144808Abstract: Disclosed is a novel pest control agent, in particular a pesticide or a miticide. Specifically disclosed are a substituted isoxazoline compound or a substituted enone oxime compound represented by the general formula (1) below or the general formula (2) below, and a pest control agent containing any of them. (In the formulae, the symbols are as defined in the description.Type: ApplicationFiled: June 27, 2008Publication date: June 10, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takeshi Mita, Kenichi Toyama, Yuki Furukawa, Mitsuaki Komoda
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Publication number: 20100130545Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
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Publication number: 20100124550Abstract: The present invention relates to new amide inhibitors of renin, pharmaceutical compositions thereof, and methods of use thereofType: ApplicationFiled: November 20, 2009Publication date: May 20, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manouchehr M. Shahbaz
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Publication number: 20100119482Abstract: Methods are provided for treating a subject for a condition. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is modulated during at least one predetermined phase of the subject's menstrual cycle to alter the parasympathetic activity/sympathetic activity ratio in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, including various disease conditions, that increase in severity and/or occurrence during one or more phases of the menstrual cycle. Also provided are systems and kits for use in practicing the subject methods.Type: ApplicationFiled: December 24, 2009Publication date: May 13, 2010Inventors: Anthony Joonkyoo Yun, Partic Yuarn-Bor Lee
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Publication number: 20100120921Abstract: The present invention relates to methods for the prevention of, delay of progression to, or treatment of hypertension in a patient with a high sodium diet, comprising administering to such a patient a therapeutically effective amount of a renin inhibitor or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 28, 2008Publication date: May 13, 2010Applicant: NOVARTIS AGInventor: Alan N. Charney
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Publication number: 20100113591Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: November 5, 2009Publication date: May 6, 2010Applicant: BELLUS Health (International) LimitedInventors: Xianqi Kong, David Migneault, Isabelle Valade, Xinfu Wu, Francine Gervais
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Patent number: 7709523Abstract: ?-Aminoamide derivatives useful as antimigraine agents, particularly for the treatment of head pain conditions such as migraine, cluster headache or other severe headache, are disclosed. The antimigraine agents of the invention are able to reduce or even stop the pain deriving from such conditions without, virtually, any side effects.Type: GrantFiled: November 18, 2003Date of Patent: May 4, 2010Assignee: Newron Pharmaceuticals SpAInventors: Patricia Salvati, Marcello Calabresi, Luciano Dho, Orietta Veneroni, Piero Melloni
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Publication number: 20100105778Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.Type: ApplicationFiled: December 28, 2009Publication date: April 29, 2010Inventors: Jay D. Kranzler, Srinivas G. Rao
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Publication number: 20100105779Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.Type: ApplicationFiled: December 28, 2009Publication date: April 29, 2010Inventors: Jay D. Kranzler, Srinivas G. Rao
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Publication number: 20100104664Abstract: The present invention generally concerns the management of age-related diseases in domestic animals. Specifically, the present invention is directed to combination therapies for the treatment of progressive renal diseases (e.g., Chronic Renal Failure) and their accompanying secondary disease states. In a composition aspect, the present invention provides a composition comprising a phosphate binder and another pharmaceutically active ingredient. The other pharmaceutically active ingredient is selected from a group consisting of antihypertensives, calcitrol, vitamin D analogues, lipid restriction products, potassium salts, treatments for anemia and alkalization compounds.Type: ApplicationFiled: December 21, 2009Publication date: April 29, 2010Inventors: Allison Wren, Roy Graham, Randy McElreath, Michael Molnar
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Patent number: 7700655Abstract: A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represeType: GrantFiled: April 9, 2007Date of Patent: April 20, 2010Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Susumu Muto, Akiko Itai
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Publication number: 20100081719Abstract: Methods for treating fatigue associated with fibromyalgia by administering high-dose milnacipran to a patient suffering from such fatigue are provided. Also provided are methods for the long-term treatment of fatigue associated with FMS by administering milnacipran to a patient suffering from such fatigue.Type: ApplicationFiled: December 3, 2009Publication date: April 1, 2010Inventors: Srinivas G. Rao, R. Michael Gendreau, Jay D. Kranzler
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Patent number: 7683054Abstract: The present invention relates to a solid oral dosage form comprising a therapeutically effective amount of aliskiren or a pharmaceutically acceptable salt thereof, and wherein the active ingredient is present in an amount of more than 46% by weight based on the total weight of the oral dosage form.Type: GrantFiled: April 29, 2005Date of Patent: March 23, 2010Assignee: Novartis AGInventors: Petra Gisela Rigassi-Dietrich, Martin Schmid
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Publication number: 20100069318Abstract: The invention relates to a combination which comprises: (a) a HDAI; and (b) an anti-metabolite, for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of proliferative diseases, more specifically MDS or AML. The invention also relates to pharmaceutical compositions comprising such a combination and to a method of treating MDS or AML, in a mammal, particularly a human, with such a combination. The present invention further also relates to a commercial package or product comprising such a combination.Type: ApplicationFiled: November 30, 2007Publication date: March 18, 2010Applicant: NOVARTIS AGInventor: Peter Wisdom Atadja
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Patent number: 7671085Abstract: The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.Type: GrantFiled: November 14, 2003Date of Patent: March 2, 2010Assignee: The Salk Institute for Biological StudiesInventors: Michael R. Downes, Ronald M. Evans
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Publication number: 20100029654Abstract: Methods and compositions for the treatment of Alzheimer's Disease are described. More specifically, the invention demonstrates that administration of cardiovascular agents to a mammal suffering from the symptoms of Alzheimer's Disease causes an amelioration of those symptoms. The finding of the present invention can be used in treatment regimens designed to attenuate or prevent Alzheimer's Disease.Type: ApplicationFiled: March 22, 2007Publication date: February 4, 2010Inventor: Giulio Pasinetti
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Publication number: 20100016403Abstract: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias. wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.Type: ApplicationFiled: December 14, 2007Publication date: January 21, 2010Inventors: Guy Higgins, Abdelmalik Slassi, Methvin Isaac
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Publication number: 20100016437Abstract: The present invention is in the field of pharmacotherapy of cognitive deficits in learning and memory by administering an ?-aminoamide, particularly safinamide. Examples of disturbances in cognition that can be treated with compounds of the invention are the ones associated with disorders such as autism, dyslexia, attention deficit hyperactivity disorder, schizophrenia, obsessive compulsive disorders, psychosis, bipolar disorders, depression, Tourette's syndrome, Mild Cognitive Impairment (MCI) and disorders of learning in children, adolescents and adults, Age Associated Memory Impairment, Age Associated Cognitive Decline, Alzheimer's Disease, Parkinson's Disease, Down's Syndrome, traumatic brain injury Huntington's Disease, Progressive Supranuclear Palsy (PSP), HIV, stroke, vascular diseases, Pick's or Creutzfeldt-Jacob diseases, multiple sclerosis (MS), other white matter disorders and drug-induced cognitive worsening.Type: ApplicationFiled: June 13, 2007Publication date: January 21, 2010Inventors: Patricia Salvati, Stefano Rossetti, Luca Benatti
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Publication number: 20100016440Abstract: Methods of using certain a-aminoamide derivatives as anti-inflammatory agents. The anti-inflammatory agents of the invention are able to reduce or even stop inflammatory s conditions substantially without side effects.Type: ApplicationFiled: August 20, 2009Publication date: January 21, 2010Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventors: Patricia Salvati, Orietta Veneroni, Elena Barbanti, Fariello Ruggero, Luca Benatti
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Publication number: 20100004326Abstract: This invention provides metabolites of SARM compounds including inter alia glucuronidated metabolites and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, muscle wasting disease and/or disorder, a bone related disease and/or disorder, metabolic syndrome, diabetes and associated diseases, and others.Type: ApplicationFiled: June 19, 2009Publication date: January 7, 2010Inventor: Karen A. VEVERKA
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Publication number: 20090306142Abstract: Processes and compositions have been discovered that are suitable for controlling a pathogen induced disease in a plant that is at risk of being diseased from a pathogen resistant to a Qo inhibitor. Such processes and compositions comprise contacting said plant(s) with a composition comprising an effective amount of a Qi inhibitor.Type: ApplicationFiled: May 29, 2009Publication date: December 10, 2009Applicant: DOW AGROSCIENCES LLCInventors: Chris CARSON, Carla J. R. KLITTICH, W. John OWEN, Christian SCHOBERT, David H. YOUNG
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Patent number: 7629358Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: March 16, 2005Date of Patent: December 8, 2009Assignee: Pfizer IncInventors: Alan Daniel Brown, Charlotte Alice Louise Lane, Paul Alan Glossop, David Anthony Price, Russell Andrew Lewthwaite, Mark Edward Bunnage, Kim James, Graham Lunn
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Publication number: 20090291988Abstract: The instant invention relates to compounds of formula I, diagrammed below, wherein R3, E, D and Y are defined in the application, which are useful as reversible inhibitors of monoamine oxidase-B and/or monoamine oxidase-A, and therefore useful to treat or prevent neurological diseases or conditions in mammals, preferably humans.Type: ApplicationFiled: June 14, 2006Publication date: November 26, 2009Inventor: Renata Oballa
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Publication number: 20090291945Abstract: To provide a compound having an excellent cysteine protease inhibitory effect, and to provide a drug for treatment or prevention of the disease selected from the group consisting of osteoporosis, osteoarthritis, chronic rheumatoid arthritis, Paget's disease of bone, hypercalcemia, bone metastasis of cancer, and ostealgia. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, or a drug or pharmaceutical composition containing the same as an effective component.Type: ApplicationFiled: April 7, 2009Publication date: November 26, 2009Applicant: Teijin Pharma LimitedInventors: Gen Unoki, Takashi Hayamizu, Hiroshi Eguchi, Yumiko Muroga, Toshiyuki Kaneko, Naoki Yajima
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Publication number: 20090281103Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: July 20, 2006Publication date: November 12, 2009Inventors: Christopher I. Bayly, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
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Publication number: 20090281085Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: February 3, 2009Publication date: November 12, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
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Patent number: 7615664Abstract: Compounds of the general formula (I) in which the substituents R, R1, R2, R3, R4, R5 and R6 are each as defined in claim 1 have renin-inhibiting properties and can be used as medicaments.Type: GrantFiled: December 9, 2005Date of Patent: November 10, 2009Assignee: Speedel Experimenta AGInventors: Peter Herold, Stefan Stutz, Robert Mah, Vincenzo Tschinke, Christiane Marti
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Publication number: 20090264479Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition of these proteases can be useful in the treatment of these parasitic diseases, including toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis or schistosomiasis.Type: ApplicationFiled: July 24, 2006Publication date: October 22, 2009Inventors: Cameron Black, Christophe Mellon, Deborah Anne Nicoll-Griffith, Renata Oballa
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Publication number: 20090253703Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: June 12, 2009Publication date: October 8, 2009Inventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, Holger Sellner
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Publication number: 20090253701Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: June 12, 2009Publication date: October 8, 2009Inventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, holger Sellner
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Publication number: 20090247540Abstract: Methods and compositions for activating an EphA receptor can be used for identifying therapeutic agents for cancer.Type: ApplicationFiled: October 21, 2005Publication date: October 1, 2009Inventors: Bingchen Wang, Eugene Myshkin, Hui Maio
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Publication number: 20090238756Abstract: Compositions and methods for imaging and for chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns agents comprising a targeting moeity comprising a beta-adrenergic receptor targeting compound conjugated or embedded with ethylenediamine. The present invention also concerns methods of application of such agents for imaging and treatment of cardiovascular diseases, and kits for preparing a radiolabeled therapeutic or diagnostic agent.Type: ApplicationFiled: December 19, 2008Publication date: September 24, 2009Inventors: David J. Yang, Chang-Sok Oh, Saady Kohanim, Dong-Fang Yu, Richard Mendez, E. Edmund Kim
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Patent number: 7582782Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: GrantFiled: November 25, 2004Date of Patent: September 1, 2009Assignee: Novartis AGInventors: Daniel K Baeschlin, Juergen K Maibaum, Holger Sellner
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Publication number: 20090215852Abstract: The invention provides preparations, formulations, kits and other products of manufacture (e.g., blister packs) comprising combinations of beneficial ingredients that are serviceable as therapies for improving states and disease symptoms such as involving inflammation, excessive sympathoneural drive, cachexia, anorexia, and anorexia-cachexia, as well as stress or anxiety related thereto, and methods of making and using them. The invention provides compositions and therapies comprising use of a beta adrenergic antagonist (also called “beta blockers”, e.g., propranolol) in combination with an anti-inflammatory agent, e.g., a nonsteroidal anti-inflammatory drug (NSAID), an angiotensin-converting enzyme (ACE) inhibitor, an angiotensin receptor blocker (ARB), an anabolic steroid, a natural oil or fatty acid or any combination thereof.Type: ApplicationFiled: March 21, 2006Publication date: August 27, 2009Inventors: Newell Bascomb, John Maki, Fredric Young
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Publication number: 20090203669Abstract: The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to an activity) as well as to alleviate some of the symptoms experienced during menopause or associated with the menstrual cycle. Regardless of the precise formulation, the compositions of the invention can include at least one active ingredient that targets the hypothalamo-pituitary-adrenal (HPA) axis and at least one active ingredient that targets the prefrontal cortex. Either or both of these types of agents can be combined with an agent that inhibits activity in the sympathetic nervous system. Thus, the compositions or combination pharmacotherapies can also include an agent that inhibits a beta-adrenergic receptor or that otherwise acts as an anti-hypertensive or anxiolytic agent.Type: ApplicationFiled: November 13, 2006Publication date: August 13, 2009Inventor: Nicholas E. Goeders
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Publication number: 20090182019Abstract: The present invention provides novel HDAC inhibitors and methods of treating diseases using the same.Type: ApplicationFiled: April 18, 2006Publication date: July 16, 2009Applicants: The Johns Hopkins University, Wayne State UniversityInventors: Robert A. Casero, Patrick M. Woster, Sheeba Varghese
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Publication number: 20090176853Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).Type: ApplicationFiled: December 4, 2008Publication date: July 9, 2009Inventors: Lilian Alcaraz, Moya Caffrey, Mark Furber, Timothy Luker, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
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Publication number: 20090175950Abstract: Pharmaceutical safety dosage forms are provided which include a pharmaceutical and an antagonist to the pharmaceutical. The safety dosage forms are such that the antagonist has no significant bioavailability when the pharmaceutical safety dosage form is administered as intended. However, the antagonist is released and becomes bioavailable if the dosage form is disrupted. Methods of administering pharmaceuticals by providing pharmaceutical safety dosage forms are also provided.Type: ApplicationFiled: March 16, 2009Publication date: July 9, 2009Inventor: Richard H. Roberts
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Publication number: 20090163496Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: October 30, 2007Publication date: June 25, 2009Applicant: UNIVERSITY OF WASHINGTONInventors: Niels H. ANDERSEN, Jason BOWMAN
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Publication number: 20090156678Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.Type: ApplicationFiled: December 18, 2008Publication date: June 18, 2009Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventors: Elena Barbanti, Carla Caccia, Patricia Salvati, Francesco Velardi, Tiziano Ruffilli, Luigi Bogogna
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Publication number: 20090149544Abstract: This invention relates to novel alpha-aminoamide derivatives, their pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of monoamine oxidase type B (MAO-B) and/or a sodium (Na+) channel blocker, and/or a calcium (Ca2+) channel modulator.Type: ApplicationFiled: October 22, 2008Publication date: June 11, 2009Applicant: CoNCERT Pharmaceuticals, Inc.Inventor: Julie F. Liu
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Publication number: 20090137681Abstract: Provided herein are compositions and methods for treating or preventing cancer and autoimmune diseases. Compositions comprise a sirtuin inhibitory compound that decreases the activity of a sirtuin, such as SIRT1 or Sir2. Exemplary methods comprise contacting a cell or a molecule with a sirtuin inhibitory compound that decreases the activity of a sirtuin and thereby reduces the life span of a cell, kills the cell or renders it susceptible to certain cell stresses including radiation and chemotherapy. Other methods include treating pathogens expressing a sirtuin.Type: ApplicationFiled: April 6, 2006Publication date: May 28, 2009Inventors: David A Sinclair, Antonello Mai
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Publication number: 20090131473Abstract: The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables W, Y, Z, R7, R8, and R9 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.Type: ApplicationFiled: March 8, 2007Publication date: May 21, 2009Inventors: Alexandra A. Nirschl, Xiaojun Zhang
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Publication number: 20090131441Abstract: Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: January 24, 2006Publication date: May 21, 2009Applicant: DOMPE phar.r.ma S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Marco Mosca, Marcello Allegretti, Francesco Colotta
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Publication number: 20090117197Abstract: The invention provides preparations, formulations, kits and other products of manufacture (e.g., blister packs) comprising combinations of beneficial ingredients that are serviceable as therapies for improving states and disease symptoms such as involving inflammation, excessive sympathoneural drive, cachexia, anorexia, and anorexia-cachexia, as well as stress or anxiety related thereto, and methods of making and using them. The invention provides compositions and therapies comprising use of a beta adrenergic antagonist (also called “beta blockers”, e.g., propranolol) in combination with an anti-inflammatory agent, e.g., a nonsteroidal anti-inflammatory drug (NSAID), an angiotensin-converting enzyme (ACE) inhibitor, an angiotensin receptor blocker (ARB), an anabolic steroid, a natural oil or fatty acid or any combination thereof.Type: ApplicationFiled: October 23, 2008Publication date: May 7, 2009Applicant: Vicus Therapeutics LLCInventors: Newell BASCOMB, John Maki, Fredric Young
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Publication number: 20090105222Abstract: Methods for the prevention or treatment of stress-related disorders by administering a therapeutically effective amount of a dual serotonin/norepinephrine reuptake inhibitor to an individual under stress are described. A triple monoamine reuptake inhibitor for serotonin/noradrenaline/dopamine may also be administered to an individual at risk for a stress-related disorder. In a preferred embodiment the compound is milnacipran and is prophylactically administered at an effective amount to delay or prevent stress-related disorders in an individual at risk.Type: ApplicationFiled: September 19, 2008Publication date: April 23, 2009Applicant: Cypress Bioscience, Inc.Inventors: Jay D. Kranzler, Srinivas G. Rao
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Patent number: 7517896Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: GrantFiled: August 8, 2005Date of Patent: April 14, 2009Assignee: Bayer AktiengesellschaftInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Publication number: 20090088408Abstract: The present invention relates to novel pharmaceutical compositions based on anticholinergics, corticosteroids and betamimetics, processes for preparing them and their use in the treatment of respiratory diseases.Type: ApplicationFiled: August 29, 2008Publication date: April 2, 2009Inventors: Christopher J. M. Meade, Michel Pairet, Michael P. Pieper
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Publication number: 20090088480Abstract: The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.Type: ApplicationFiled: September 11, 2008Publication date: April 2, 2009Inventors: James T. DALTON, David A. Dickason, David Hong, Thomas G. Bird, Tai Ahn