Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
-
Publication number: 20100190763Abstract: 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: January 21, 2010Publication date: July 29, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
-
Publication number: 20100189762Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.Type: ApplicationFiled: December 21, 2009Publication date: July 29, 2010Applicant: EMORY UNIVERSITYInventor: Jack L. Arbiser
-
Patent number: 7763604Abstract: This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms by administration of the farnesylated dibenzodiazepinone compound of Formula I via continuous intravenous infusion.Type: GrantFiled: May 16, 2006Date of Patent: July 27, 2010Assignee: Thallion Pharma Ceuticals, Inc.Inventors: Henriette Gourdeau, Maxime Ranger, François Berger, Bryan Simard
-
Patent number: 7763616Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: GrantFiled: February 14, 2006Date of Patent: July 27, 2010Assignee: Schering CorporationInventors: Wensheng Yu, Seong Heon Kim, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Bandarpalle B. Shankar, Brian F. McGuinness, Douglas W. Hobbs, Yuefei Shao
-
Publication number: 20100183604Abstract: The present invention provides an agent for preventing or treating a trastuzumab-resistant cancer, which contains one or more medicaments selected from a cofilin inhibitor, a PAK1 inhibitor, a LIMK inhibitor, a RHO inhibitor, a ROCK1 inhibitor and a ROCK2 inhibitor.Type: ApplicationFiled: June 19, 2008Publication date: July 22, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yoshikazu Ohta, Akira Hayashi
-
Publication number: 20100178331Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.Type: ApplicationFiled: December 25, 2007Publication date: July 15, 2010Inventors: Ryoichi Nagata, Shunji Haruta
-
Publication number: 20100173859Abstract: Pharmaceutical formulation in the form of compacts comprising A) an agglomerated excipient content composed of a1) 60-97% by weight of sugar or sugar alcohols, a2) 1-25% by weight of a disintegrant, selected from the group consisting of crospovidone, croscarmellose, sodium carboxymethylstarch and L-hydroxypropylcellulose, a3) 1-15% by weight of water-insoluble, film-forming polymers a4) 0-15% by weight of water-soluble polymers and a5) 0-15% by weight of further pharmaceutically customary excipients, the total of the components a1) to a5) being 100% by weight, B) at least one active ingredient, C) 0 to 10% by weight, based on the total amount of A) to D), of a lubricant or mold release agent, and D), if appropriate, further pharmaceutical excipients.Type: ApplicationFiled: June 2, 2008Publication date: July 8, 2010Applicant: BASF SEInventors: Karl Kolter, Michael Schönherr, Silke Gebert, Kathrin Meyer-Böhm, Angelika Maschke
-
Publication number: 20100168086Abstract: The present invention relates to new 7,8,10,10a-tetrahydro-6H-benzo[c]chromen-9(6aH)-one modulators of cannabinoid receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 23, 2009Publication date: July 1, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manoucherhr M. Shahbaz
-
Publication number: 20100168085Abstract: Compositions and methods for modulation of the suppressive activity of CD4+CD25+regulatory T cells (Treg) on CD4+CD25? effector T cells (Teff) are provided. An agent selected from: (i) dopamine; (ii) a dopamine precursor; (iii) a D1-R agonist; (iv) a D2-R antagonist; (v) a combination of (i) and (ii); or (vi) a combination of (i), (ii) or (iii) with (iv), down-regulates the suppressive activity of Treg and is useful for treatment of cancer. An agent selected from (i) a dopamine D2-R agonist, (ii) a dopamine D1-R antagonist, and (iii) a combination of (i) and (ii), up-regulates the suppressive activity of Treg and is useful for treatment of an autoimmune disease or for controlling graft rejection in tissue/organ transplantation.Type: ApplicationFiled: May 23, 2004Publication date: July 1, 2010Applicant: YESA RESEARCH AND DEVELOPMENT CO. LTD. at the Weizmann Institute of ScienceInventors: Michal Eisenbach-Schwartz, Jonathan Kipnis
-
Publication number: 20100166887Abstract: The present invention relates to new dibenzo[b,e][1,4]diazepine modulators of dopamine receptors, serotonin receptors, adrenergic receptors, acetylcholine receptors, and/or histamine receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: October 21, 2009Publication date: July 1, 2010Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar
-
Publication number: 20100166889Abstract: The invention provides methods of treating depressive disorders, in particular major depression but other depressive orders also, with prodrug stimulants or analogs including amphetamine prodrugs, methylphenidate prodrugs, and methylphenidate analogs, Such methods of treatment may utilize the prodrug stimulant or analog as monotherapy or, more commonly, as an adjunct to antidepressant medication treatment to augment their effect. The invention includes combination methods of treatment in which an amphetamine prodrug, methylphenidate prodrug, or methylphenidate analog is administered to an individual in need with one or more other active agents, either in separate forms or as a single pharmaceutical formulation. Packaged pharmaceutical compositions containing an amphetamine or methylphenidate prodrug, instructions for using the prodrug to treat certain disorders, and optionally one or more other active agents are provided by the invention.Type: ApplicationFiled: December 23, 2009Publication date: July 1, 2010Applicant: LCS GROUP, LLCInventor: Louis Sanfilippo
-
Publication number: 20100166884Abstract: A method for treating gastric cancer, ovarian cancer, non-small cell lung cancer, or colorectal cancer in a patient is described, as well as pharmaceutical compositions comprising 7-(2,5-dihydro-4-imidazo[1,2-a]pyridine-3-yl-2,5-dioxo-IH-pyrrol-3-yl)-9-fluoro-1,2,3,4-tetrahydro-2-(1-piperidinyl-carbonyl)-pyrrolo[3,2,1-jk][1,4]benzodiazepine, useful for the method and a process for preparing said compositions.Type: ApplicationFiled: June 20, 2008Publication date: July 1, 2010Inventors: Aktham Aburub, Marcio Chedid, Thomas Albert Engler, Venkatraghavan Vasudevan
-
Patent number: 7745430Abstract: Disclosed herein is a transnasal anticonvulsive pharmaceutical composition comprising diazepam as an active ingredient, water, a fatty acid ester, diethylene glycol monoethyl ether, ethanol and sodium glycocholate, wherein the weight of the fatty acid ester is at least 2-fold higher than that of water and is at least 2-fold higher than that of ethanol. The anticonvulsive pharmaceutical composition for transmucosal delivery of diazepam according to the present invention includes a minimized content of water and ethanol, a fatty acid ester as a main ingredient and no use of a polar solvent, e.g. glycol, and, exhibits improved diazepam solubility and transmucosal permeability due to using a small amount of water and ethanol. The present invention also includes treatment of convulsions by transnasally administering to a patient in need thereof a therapeutically effective amount of the disclosed compositions.Type: GrantFiled: November 15, 2006Date of Patent: June 29, 2010Assignee: SK Holdings Co., Ltd.Inventors: Kwon Ho Kim, Paramjeet Kaur, Jae Hoon Jo, Myoung Ki Baek, Yeo Joo Yuk
-
Patent number: 7745429Abstract: The invention relates to a process for the preparation of form I of olanzapine, crystallized from a solvent mixture which comprises 2-propanol, some pseudopolymorphic forms, namely solvates of olanzapine, a new polymorphic form A of olanzapine, and processes for the preparation thereof.Type: GrantFiled: July 14, 2003Date of Patent: June 29, 2010Assignee: KRKA, D.D. Novo MestoInventors: Berta Kotar Jordan, Franc Vrecer, Marija Grcman
-
Publication number: 20100159033Abstract: The present invention relates to new benzisoxazole modulators of D2 receptors and/or 5-HT2A receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 25, 2009Publication date: June 24, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manoucherhr M. Shahbaz
-
Publication number: 20100160262Abstract: The present invention provides treatment methods involving modulating a sirtuin activity and/or a sirtuin mRNA and/or a sirtuin polypeptide level. In some embodiments, the present invention provides treatment methods involving modulating SIRT1 activity and/or SIRT mRNA and/or polypeptide level. The present invention provides methods of inhibiting SIRT1 Tat deacetylase activity. Methods of inhibiting SIRT1 Tat deacetylase activity are useful for treating immunodeficiency virus infections, particularly human immunodeficiency virus (HIV) infection. Thus, the present invention provides methods of treating an immunodeficiency virus infection, generally involving inhibiting SIRT1 Tat deacetylase activity. The present invention further provides methods of identifying agents that modulate sirtuin activity (e.g., SIRT1 activity), particularly ability of sirtuins to interact with (e.g., bind and/or deacetylate) a substrate, e.g., a viral substrate such as a Tat polypeptide.Type: ApplicationFiled: December 23, 2008Publication date: June 24, 2010Inventors: Melanie Ott, Eric M. Verdin, Manfred Jung
-
Publication number: 20100158956Abstract: Compositions and methods for combination therapy are provided. The compositions comprise a multiple unit dosage form having both a therapeutic agent and a nutritional supplement. The combination therapy is useful for restoring a nutrient depletion associated with a particular disease state. Additionally, the combination therapy can prevent or attenuate the depletion of a nutrient caused, in whole or in part, by the co-administrated therapeutic drug. Methods of manufacturing the formulations are likewise described.Type: ApplicationFiled: December 22, 2009Publication date: June 24, 2010Inventor: James R. Komorowski
-
Patent number: 7741319Abstract: The present inventors have developed a key intermediate for the production of C2 substituted PBDs, which has a leaving group at the C2 position, a carbamate protecting group at the N10 position and a protected hydroxy group at the C11 position. In a first aspect, the present invention comprises a compound with a the formula (I), wherein: R10 is a carbamate-based nitrogen protecting group; R11 is an oxygen protecting group; and R2 is a labile leaving group. In a further aspect, the present invention comprises a method of synthesising a compound of formula (III), or a solvate thereof, from a compound of formula (I) as defined in the first aspect, R16 is either O—R11, wherein R11 is as defined in the first aspect, or OH, or R10 and R16 together form a double bond between N10 and C11; and R15 is R. The other substituents are defined in the claims.Type: GrantFiled: March 1, 2005Date of Patent: June 22, 2010Assignee: Spirogen LimitedInventors: Philip Wilson Howard, Stephen John Gregson
-
Publication number: 20100152170Abstract: The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.Type: ApplicationFiled: February 10, 2010Publication date: June 17, 2010Applicant: TransTech Pharma, Inc.Inventors: Adnan M.M. Mjalli, Brian S. Grella, Govindan Subramanian, Murty N. Arimilli, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Xiaochuan Guo, Jeff Zhu
-
Publication number: 20100152161Abstract: Methods and compositions for preventing or reducing weight gain associated with drug treatment, which utilize an H1 agonist such as betahistine, betahistine metabolite or a betahistine salt are disclosed.Type: ApplicationFiled: February 28, 2010Publication date: June 17, 2010Applicant: Mor Research Applications Ltd.Inventor: Nir BARAK
-
Patent number: 7737165Abstract: A method of reducing weight gain associated with olanzapine treatment in a human subject, by orally administering to an olanzapine-treated subject betahistine or a salt thereof, is disclosed.Type: GrantFiled: November 22, 2005Date of Patent: June 15, 2010Assignee: Mor Research Applications Ltd.Inventor: Nir Barak
-
Publication number: 20100144714Abstract: The present invention relates to new derivatives of imidazo, pyrimido and diazepine-pyrimidine-dione of the general formula (I) in which R1, R2, L1, L2, Y, Z and A are various and varying groups. These products exhibit a good affinity for certain sub-types of cannabinoid receptors, in particular the CB2 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more cannabinoid receptors are involved. The invention also relates to pharmaceutical compositions containing said products, and to the use thereof for preparing a drug.Type: ApplicationFiled: December 17, 2007Publication date: June 10, 2010Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)Inventors: Lydie Poitout, Valérie Brault
-
Publication number: 20100144610Abstract: An aspect of the present invention provides for a medicament including a solution containing pleconaril or a pharmaceutically acceptable salt thereof, wherein at least one solvent including the solution is a pleconaril-dissolving hydrofluorocarbon.Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Inventors: Saeed M. Chaudhry, Julianne Berry, Joel A. Sequeira
-
Patent number: 7732435Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: GrantFiled: December 5, 2006Date of Patent: June 8, 2010Assignee: Novartis AGInventors: Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Lee Edwards, Terance William Hart, Timothy John Ritchie
-
Publication number: 20100137286Abstract: The present invention is concerned with arylcyclohexylethers of dihydro-tetraazabenzoazulenes, i.e. arylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein, their manufacture, and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: ApplicationFiled: November 19, 2009Publication date: June 3, 2010Inventor: Patrich Schnider
-
Publication number: 20100129321Abstract: The present invention relates to pharmaceutical compositions for treating virus infections and/or diseases caused thereby comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additional therapeutic agent.Type: ApplicationFiled: December 6, 2006Publication date: May 27, 2010Applicant: BAYER HEALTHCARE LLCInventors: Olaf Weber, Bernd Riedl
-
Publication number: 20100130478Abstract: This invention provides biodegradable, sustained-release pharmaceutical compositions of a psychoactive drug formulated with biocompatible, biodegradable tyrosine-derived polyarylates.Type: ApplicationFiled: July 10, 2009Publication date: May 27, 2010Applicant: TYRX PHARMA, INC.Inventors: Arikha Moses, Fatima Buevich, Satish Pulapura
-
Publication number: 20100130480Abstract: The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 18, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manoucherhr M. Shahbaz
-
Publication number: 20100130481Abstract: Methods of using orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anticonvulsant and anxiolytic activity with reduced sedative, hypnotic, muscle relaxant, or ataxic effects.Type: ApplicationFiled: January 8, 2010Publication date: May 27, 2010Inventors: James M. Cook, Qi Huang, Xiaohui He, Xioeyan Li, Jianming Yu, Dongmel Han
-
Publication number: 20100130479Abstract: The present invention provides molecules and methods for the prevention and/or treatment of memory deficit related conditions and/or enhancement of cognition. In a preferred embodiment, the invention includes compounds, salts and prodrugs thereof for the prevention and/or treatment of these conditions.Type: ApplicationFiled: August 31, 2009Publication date: May 27, 2010Inventors: James M. Cook, Terry Clayton, Yun Teng Johnson, Sundari Rallapalli, Dongmei Han
-
Publication number: 20100129473Abstract: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuropsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.Type: ApplicationFiled: November 18, 2009Publication date: May 27, 2010Applicant: ACADIA Pharmaceuticals, Inc.Inventors: Fredrik Ek, Roger Olsson, Jörgen Ohlsson
-
Publication number: 20100125063Abstract: Combinations which comprise at least one nicotinic acetylcholine alpha 7 receptor agonist and at least one compound selected from the group consisting of (a) conventional antipsychotics (b) atypical antipsychotics (c) cognition, attention and/or memory enhancers (d) and to use of these combinations in the treatment of psychiatric disorders.Type: ApplicationFiled: January 20, 2010Publication date: May 20, 2010Inventors: Hans O. KALKMAN, Joachim NOZULAK, Annick VASSOUT, Konstanze HURTH, Dominik FEUERBACH, Conrad GENTSCH, Graeme BILBE
-
Publication number: 20100124543Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.Type: ApplicationFiled: July 16, 2009Publication date: May 20, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
-
Publication number: 20100125066Abstract: The present invention is concerned with alkylcyclohexylethers of dihydro-tetraazabenzoazulenes, i.e. alkylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene s of formula I wherein R1, R2 and R3 are as described herein, their manufacture, and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists. The compounds are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: ApplicationFiled: November 12, 2009Publication date: May 20, 2010Inventor: Patrick Schnider
-
Publication number: 20100119626Abstract: This document provides methods and materials related to genetic markers of schizophrenia (SZ). For example, this document provides methods for using such genetic markers to assess risk of developing schizophrenia.Type: ApplicationFiled: November 4, 2009Publication date: May 13, 2010Applicant: SUREGENE LLCInventors: Timothy Lynn Ramsey, Mark David Brennan
-
Publication number: 20100119625Abstract: This document provides methods and materials related to genetic markers of schizophrenia (SZ), schizotypal personality disorder (SPD), and/or schizoaffective disorder (SD), (collectively referred to herein as “schizophrenia spectrum disorders” or SSDs). For example, methods for using such genetic markers to identify an SSD (e.g., SZ) endophenotype are provided.Type: ApplicationFiled: November 4, 2009Publication date: May 13, 2010Applicant: SUREGENE, LLCInventors: Mark David Brennan, Timothy Lynn Ramsey
-
Publication number: 20100120751Abstract: The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: ApplicationFiled: November 6, 2009Publication date: May 13, 2010Inventors: Caterina Bissantz, Erwin Goetschi, Roland Jakob-Roetne, Raffaello Masciadri, Emmanuel Pinard, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Publication number: 20100119622Abstract: The present invention relates to new 3H-benzooxazol-2-one modulators of D2 receptors and/or 5-HT1A receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 15, 2009Publication date: May 13, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
-
Publication number: 20100120752Abstract: The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are muscarinic, for example muscarine-1 (M1) agonists. These compounds are useful for the preparation of medicaments for treatment, amelioration or prevention of impulse control disorders. These include impulse control disorders ‘Not Elsewhere Classified,’ such as intermittent explosive disorder, pyromania, kleptomania, pathological gambling and trichotillomania, and impulse control disorders ‘Not Otherwise Specified,’ such as compulsive buying disorder, binge eating and binge drinking disorder, impulsive self-injurious behavior, sexual addictions, compulsive Internet use, and excessive mobile phone use.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Natasja M.W.J. De Bruin, Marlies L. Van Drimmelen, Arnoldus H.J. Herremans, Martinus Th.M. Tulp, Cornelis G. Kruse
-
Publication number: 20100113426Abstract: A pharmaceutical composition for intranasal administration to a mammal. The pharmaceutical composition comprises an effective amount of a benzodiazepine or pharmaceutically acceptable salt thereof; and a nasal carrier. In some embodiments, the pharmaceutical composition when administered intranasally produces a rapid physiological response. Pharmaceutical compositions may also include at least one or more sweeteners, flavoring agents, or masking agents or combinations thereof.Type: ApplicationFiled: November 4, 2009Publication date: May 6, 2010Inventor: Daniel P. Wermeling
-
Publication number: 20100113405Abstract: The present invention relates to new methylindazole modulators of 5-HT3 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 4, 2009Publication date: May 6, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
-
Publication number: 20100113427Abstract: The present invention provides novel compositions comprising a combination of a 5-HT3 receptor antagonist and a selective dopamine D2 receptor antagonist for the treatment of alcohol dependence and other dopamine pathway-associated disorders or conditions. Preferably, the pharmaceutical compositions of the present invention comprise amounts of the 5-HT3 receptor antagonist ondansetron and the selective dopamine D2 receptor antagonist olanzapine that are sufficient to control a subject's craving for alcohol or other addictive substances. Kits comprising the combination of antagonists for the treatment of addictive disorders such as alcohol dependence are also provided.Type: ApplicationFiled: January 8, 2010Publication date: May 6, 2010Inventor: NIKHILESH N. SINGH
-
Publication number: 20100113425Abstract: Compounds of the formula I: or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2?, R6?, R7?, R9?, X? and M? are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M? may together represent a divalent pharmaceutically acceptable cation.Type: ApplicationFiled: November 2, 2009Publication date: May 6, 2010Applicant: SPIROGEN LIMITEDInventors: Philip Wilson Howard, Zhizhi Chen, Stephen John Gregson
-
Publication number: 20100113359Abstract: The present invention relates to new dimethylphenoxy inhibitors of viral protease or parasitic enzymes, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 5, 2009Publication date: May 6, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
-
Patent number: 7709470Abstract: The present invention relates to novel benzodiazepine compounds exhibiting RXR-antagonist efficacy, for delaying progression of, preventing or treating a condition or disease being associated with RXR-antagonism, in particular selected from diabetes, complication of diabetes such as retinopathy, nephropathy, neuropathy, and hyperlipidemia, obesity, dyslipidemia, and osteoporosis.Type: GrantFiled: April 8, 2004Date of Patent: May 4, 2010Assignee: Novartis AGInventors: Junichi Sakaki, Kazuhide Konishi, Masashi Kishida, Masaaki Kimura, Hidefumi Uchiyama, Hironobu Mitani
-
Patent number: 7709471Abstract: There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.Type: GrantFiled: July 5, 2007Date of Patent: May 4, 2010Assignee: AstraZeneca ABInventors: Christopher Thomas Halsall, David Alan Rudge, Iain Simpson, Richard Andrew Ward
-
Publication number: 20100092563Abstract: A method for producing a composition comprising nanoparticles of a biologically active compound.Type: ApplicationFiled: June 29, 2007Publication date: April 15, 2010Applicant: ICEUTICA PTY LTD.Inventors: Cammarano Raffaele, Meiser Felix, Postma Almar, Caruso Frank
-
Publication number: 20100093704Abstract: The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.Type: ApplicationFiled: October 25, 2007Publication date: April 15, 2010Applicant: RAMOT AT TEL-AVIV UNIVERSITY LTDInventors: Moshe Portnoy, Irit Gil-Ad, Avraham Weizman
-
Publication number: 20100092549Abstract: A dosage form for administration of two or more active pharmaceutical ingredients to a subject, comprising a first pharmaceutical composition comprising a first active pharmaceutical ingredient and optionally one or more pharmaceutically acceptable excipients in a first physical form selected from the group consisting of powder, granule, pellet, bead or mini-tablet form, and at least a second pharmaceutical composition comprising a second active pharmaceutical ingredient and optionally one or more pharmaceutically acceptable excipients in a second physical form selected from the group consisting of granule, pellet, bead, mini-tablet or tablet form, wherein the composition is characterised in that said first and second physical forms are selected to be different to minimise interactions between said first and second pharmaceutical compositions and to allow separation of said first and second pharmaceutical compositions for analysis on the basis of size difference.Type: ApplicationFiled: February 11, 2008Publication date: April 15, 2010Inventors: Sandra Blundell, Panagiotis Keramidas, Brett Antony Mooney, Todd James Rutherford
-
Publication number: 20100086601Abstract: The present disclosure relates to non-aggregating nanoparticles and their associated methods of preparation. The nanoparticles may have a surface and a size range of 1 nm to 999 nm, along with a zeta potential of ?50 to 50 millivolts. A polycation and/or polyanion may be disposed on the nanoparticle surface. In addition, an active ingredient may be encapsulated within the nanoparticles or associated with the polycation or polyanion on the nanoparticle surface.Type: ApplicationFiled: October 3, 2008Publication date: April 8, 2010Applicant: SOUTHWEST RESEARCH INSTITUTEInventors: Joseph A. McDONOUGH, Hong DIXON, Maria Lucy KIMMEL, Larry Allen CABELL, Stephen T. WELLINGHOFF