Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/221)
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Publication number: 20110274740Abstract: The present invention is directed to methods of reducing symptoms associated with an abrupt reduction in an endogenous or exogenous chemical in subjects, the methods comprising: (a) administering to the subject a single dosage form comprising an active agent, wherein the release rate of the active agent from the single dosage form tapers throughout the administration; and (b) removing the single dosage form from the subjects after the release rate of the active agent is at or below a terminal symptom threshold level.Type: ApplicationFiled: May 5, 2011Publication date: November 10, 2011Inventors: Charles E. DiLiberti, Anu Mahashabde
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Publication number: 20110269748Abstract: This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(?O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(?O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(?O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkylType: ApplicationFiled: February 13, 2008Publication date: November 3, 2011Inventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Christopher James Grantham, Theodorus Dinklo, Anne Simone Josephine Lesage
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Publication number: 20110263577Abstract: This invention relates to novel oxadiazolyl-diazabicyclononane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 8, 2009Publication date: October 27, 2011Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Philip K. Ahring, Tino Dyhring, Jeppe Kejser Christensen
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Publication number: 20110263576Abstract: The invention relates to a pharmaceutical composition characterized in that it comprises a benzodiazapine and/or benzodiazapine derivative, and a non-ionic solubilizer, and induces in said combination an analogous effect to an opiate, described as a Straub phenomenon.Type: ApplicationFiled: January 15, 2009Publication date: October 27, 2011Inventor: Rainer Hoernecke
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Publication number: 20110263575Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: August 15, 2008Publication date: October 27, 2011Inventors: Francoise Pierard, Jean-Damien Charrier
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Publication number: 20110263545Abstract: The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.Type: ApplicationFiled: May 20, 2009Publication date: October 27, 2011Inventors: Naweed Muhammad, Keith R. Bley, Jeffrey Tobias
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Patent number: 8044043Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).Type: GrantFiled: March 31, 2009Date of Patent: October 25, 2011Assignee: Bristol-Myers Squibb CompanyInventor: Guanglin Luo
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Publication number: 20110257162Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein m, n, X, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: June 29, 2011Publication date: October 20, 2011Inventors: Vincenzo Summa, Paola Pace, Philip Jones, Alessia Petrocchi, Maria del Rosario Rico Ferreira, Giuseppe Cecere
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Publication number: 20110253135Abstract: The present disclosure provides a drug delivery device comprising a housing defining an airway, wherein the airway comprises at least one air inlet and a mouthpiece having at least one air outlet, at least one heated metal substrate disposed within the airway, at least one drug disposed on the at least one heated metal substrate. Drugs that can be complexed with metals or metal salts and could be deposited as thin films on heated metal substrate for generating thermal condensation aerosols are particularly suited. The metal substrate could be electrically or chemically heated. Further, the chemically heated metal source could be activated by an igniter that generates heat or spark.Type: ApplicationFiled: April 1, 2011Publication date: October 20, 2011Applicant: ALEXZA PHARMACEUTICALS, INC.Inventors: Ron L. HALE, C.V Krishnamohan Sharma, Mingzu Lei
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Publication number: 20110257161Abstract: This invention relates to novel diazabicyclononyl-phenyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: December 3, 2009Publication date: October 20, 2011Applicant: NEUROSEARCH A/SInventors: Dan Peters, Daniel B. Timmermann, Elsebet ?stergaard Nielsen, Jeppe Kejser Christensen, Tino Dyhring
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Patent number: 8039616Abstract: Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R?, —CONR?R?, —NH—CO—R?, —S(O)R?, —S(O)2R?, —NH—S(O)2R?, —S(O)NR?R? or —S(O)2NR?R?, wherein each R? and R? is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; —R4 represents hydrogen or C1-6 alkyl; —R5 represents C1-6alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, aryl-C(O)—Type: GrantFiled: September 19, 2005Date of Patent: October 18, 2011Assignee: AstraZeneca ABInventors: Helena Dennison, Justin Warne, Keith Spencer, George Cockerill, James Lumley
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Patent number: 8039460Abstract: Compounds of Formula (I): and Formula (II): (where variables R2, R4, A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: October 12, 2005Date of Patent: October 18, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W. Shaw, Diem N. Nguyen, Zhengwu J. Deng, Theresa M. Williams, Joseph P. Vacca, Craig M. Potteiger, Harold G. Selnick
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Publication number: 20110250142Abstract: Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing hypertension and complications in patients with diabetes and/or metabolic syndrome. More particularly, aspects of the present invention are related to using a combination of cicletanine and a second antihypertensive agent (preferably a calcium antagonist, an ACE inhibitor, or an angiotensin II receptor antagonist) for treating and/or preventing hypertension and complications in patients with diabetes and/or metabolic syndrome.Type: ApplicationFiled: March 1, 2011Publication date: October 13, 2011Inventors: Benson M. Fong, Glen V. Cornett
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Publication number: 20110251177Abstract: The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I) and (II): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.Type: ApplicationFiled: April 13, 2011Publication date: October 13, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Jiaxin Yu, Jeffrey Clough, Rajinder Singh
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Publication number: 20110251184Abstract: 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: ApplicationFiled: April 11, 2011Publication date: October 13, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Janice Chin, Kenneth M. Gigstad, He Xu
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Publication number: 20110245235Abstract: The present inventions provide combination therapies, kits, and methods for providing relief and/or for improving one or more symptoms associated with an auditory system disorder in a subject diagnosed with the auditory system disorder, comprising an effective amount of at least one pharmaceutical agent and at least one auditory system disorder device, as well as methods for using at least one pharmaceutical agent and/or at least one auditory system disorder device in the manufacture of said kits.Type: ApplicationFiled: October 9, 2009Publication date: October 6, 2011Inventors: Peter J. Hanley, Robert H. Frater, Arjun Goyal, Paul B. Davis
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Publication number: 20110243985Abstract: Disclosed is a self-adhesive matrix system comprising a styrene-ethylene/butylene-styrene (SEBS) copolymer in an oil/ethyl acetate mixture, a hydrogenated resin and a pharmaceutical or cosmetic active ingredient.Type: ApplicationFiled: December 10, 2009Publication date: October 6, 2011Inventors: Stefania Pagani, Maurizio Di Grigoli, Sergio Comuzio
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Publication number: 20110244028Abstract: The invention describes a method of preparing lipid compositions by associating pH sensitive compounds which maybe weak acids, bases or amphoteric compounds with at least one ionisable or pH sensitive group and low water solubility into preformed and standardised lipid particles by pH manipulation. Drug association is carried out in situ by changing the pH of the aqueous medium to pH 6-8 wherein the compound spontaneously partitions into the lipid particles. Drug association may also be carried out by exploiting pH changes in the GI tract. The lipophilic compound is solubilised by the lipid particles and may be used as such for in-vitro and pharmacokinetic assessments or processed for oral, parenteral or topical therapy.Type: ApplicationFiled: September 28, 2009Publication date: October 6, 2011Inventors: Steve Leigh, Mathew Leuis Steven Leigh, Peter Van Hoogevest
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Publication number: 20110245208Abstract: A method of combating a somatosensory disorder in a subject, comprising administering to the subject an effective amount of a composition comprising bupranolol and/or pharmaceutically acceptable derivative(s) thereof. Compositions useful for such administration are described, including salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine, in which such salt, ester, solvate, etc. compound is in enantiomeric excess or homoenantiomeric in the R isomer thereof, or is formulated with racemic mixtures of the R and S stereoisomers of the salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine. Combination therapy compositions of opioid receptor agonists and such compounds are also described. A method is disclosed of referential genotypic screening of candidate subjects in connection with therapeutic intervention using the compositions of the disclosure to combat the somatosensory disorder.Type: ApplicationFiled: March 30, 2011Publication date: October 6, 2011Applicant: ALGYNOMICS INC.Inventors: Luda Diatchenko, William Maixner
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Publication number: 20110245238Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.Type: ApplicationFiled: June 17, 2011Publication date: October 6, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Manzer Durrani, William B. Geiss, David J. Fairfax, Dmytro O. Tymoshenko, Van-Duc Le, Lisa H. Peterson
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Publication number: 20110237563Abstract: The present invention related to the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with critical buccal condition, leading to difficulties in swallowing oral medicine forms and thus difficulties in treating said illnesses. Particularly, the present invention discloses the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with dysphagia and/or odynophagia and/or aspiration risk. Another aspect of the present invention is the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for the treatment of dysphagia and/or odynophagia and/or aspiration risk.Type: ApplicationFiled: March 23, 2010Publication date: September 29, 2011Inventor: Dominique Costantini
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Patent number: 8026234Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: September 24, 2008Date of Patent: September 27, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Takashi Ichikawa, Stephen W. Kaldor
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Publication number: 20110230473Abstract: Disclosed herein are methods, kits and compositions for treating, preventing, inhibiting, or reducing a seizure, status epilepticus, neuropathogenesis or a neuropathology caused by overstimulation of the NMDA receptor pathway and/or exposure to an OP compound.Type: ApplicationFiled: October 9, 2009Publication date: September 22, 2011Inventors: Richard K. Gordon, Madhusoodana P. Nambiar, James C. Demar, Ruthie H. Ratcliffe, Bhupendra P. Doctor, Roberta R. Owens
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Publication number: 20110230472Abstract: It is an object of the present invention to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused azole compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 25, 2009Publication date: September 22, 2011Applicant: Shionogi & Co., Ltd.Inventors: Yasunori Mitsuoka, Manami Masuda, Daisuke Taniyama
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Patent number: 8022061Abstract: Compounds having formula I: where A1, A2, L, V, W, R1, R2, R3, R4 and R5 are as described herein, compositions thereof, and their use for the treatment or prevention of type 2 diabetes and type 2 diabetes-related conditions are provided herein.Type: GrantFiled: October 9, 2007Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Yasuyuki Ogawa, Ryo Okuyama, Satoshi Shibuya, Narihiro Toda, Zhaodan Cao, Zice Fu, Xiaolin Hao, Yong-Jae Kim, Leping Li, Sarah E. Lively, Mike Lizarzaburu, Hui Tian, Ming Yu
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Publication number: 20110217387Abstract: A pharmaceutical composition for the treatment of fibromyalgia, which includes pilocarpine or a pharmacologically acceptable salt thereof. The pharmaceutical composition can be used as a novel therapeutic agent for fibromyalgia.Type: ApplicationFiled: May 15, 2009Publication date: September 8, 2011Applicant: AXIS, INC.Inventors: Kusuki Nishioka, Hiroshi Oka, Rieko Nohara
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Patent number: 8012960Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: June 7, 2010Date of Patent: September 6, 2011Assignee: Schering CorporationInventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
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Publication number: 20110206783Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: October 21, 2009Publication date: August 25, 2011Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw
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Publication number: 20110207722Abstract: This invention relates to the treatment of anxiety disorders. The invention furthermore relates to novel pharmaceutical compositions comprising a therapeutically effective amount of the compound exo-7-(8-H-8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one, or a therapeutically effective amount of the compound exo- 7-(8-H-8- aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one and a benzodiazepine drug.Type: ApplicationFiled: August 19, 2009Publication date: August 25, 2011Applicant: NEUROSEARCH A/SInventors: Dan Peters, John Paul Redrobe, Alexander Norup Nielsen
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Publication number: 20110201601Abstract: The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.Type: ApplicationFiled: June 17, 2009Publication date: August 18, 2011Applicants: COMMISSAR. A L'ENERG. ATOM. ET AUX ENERG. ALTERN., INSTITUT CURIE, CENTRE NAT DE LA RECHERCHE SCIENTIFIQUEInventors: Daniel Gillet, Julien Barbier, Ludger Johannes, Bahne Stechmann, Siau-Kun Bai
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Publication number: 20110201675Abstract: The invention includes compositions and methods of treatment of cancers susceptible to treatment with nucleotide analog chemotherapeutic agent, including cancers in which nucleotide analog resistant tumors have developed, including identifying a subject having cancer susceptible to treatment with a nucleotide analog chemotherapeutic agent and a mitotic disruptor/polo-like kinase (Plk) pathway inhibitor to a subject; and monitoring the subject for a reduction or stabilization of at least one sign or symptom of cancer.Type: ApplicationFiled: April 17, 2008Publication date: August 18, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Antonio Jimeno, Manuel Medina Hidalgo
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Patent number: 7998953Abstract: It has been found that inhibitors of the rennin-angiotensin system are useful for the treatment or prevention of conditions associated with hypoxia or impaired metabolic function or efficiency. In particular, they may be used in connection with therapy of stroke or its recurrence, the acute treatment of myocardial infarction, and the treatment or prevention of wasting or cachexia, and are thus useful in treatment of the symptoms and signs of aging. These inhibitors may also be used to enhance function in healthy subjects.Type: GrantFiled: April 29, 2005Date of Patent: August 16, 2011Assignee: Ark Therapeutics Group, p.l.c.Inventors: Hugh Edward Montgomery, John Francis Martin, Jorge Daniel Erusalimsky
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Publication number: 20110195959Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like.Type: ApplicationFiled: December 7, 2010Publication date: August 11, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventor: Gary D. Glick
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Publication number: 20110195954Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as mentioned in the description, the tautomers thereof, the isomers thereof, the diastereomers thereof, the enantiomers thereof, the hydrates thereof, the mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.Type: ApplicationFiled: November 21, 2008Publication date: August 11, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Publication number: 20110195933Abstract: The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: July 27, 2009Publication date: August 11, 2011Inventors: Jason D. Katz, Sandra L. Knowles, James P. Jewell, David L. Sloman, Matthew G. Stanton, Njamkou Noucti
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Patent number: 7994161Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.Type: GrantFiled: November 10, 2008Date of Patent: August 9, 2011Assignee: Sanofi-AventisInventors: Jidong Zhang, Yannick Benedetti, Alain Commerçon
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Patent number: 7994160Abstract: Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula I indicates a single bond or a double bond; X is O, S or N—R5; R1, R2 are independently selected from the group consisting of H, NH2, NH—C1-C6-alkyl, OH, ?O, (i.e.Type: GrantFiled: July 12, 2006Date of Patent: August 9, 2011Assignee: Abbott GmbH & Co. KGInventors: Sean C. Turner, Margaretha Bakker, Roland Grandel, Michael Vierling
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Publication number: 20110190276Abstract: A method of treatment of anxiety disorders which comprises administering to a host in need thereof an effective amount of a compound of formula (I):Type: ApplicationFiled: February 23, 2011Publication date: August 4, 2011Inventors: Giuseppe Alvaro, Sandro Belvedere
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Publication number: 20110190262Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.Type: ApplicationFiled: November 14, 2008Publication date: August 4, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
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Patent number: 7985747Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: GrantFiled: February 17, 2010Date of Patent: July 26, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Alexander Dreyer, Kirsten Arndt, Gerhard Schaenzle, Henri Doods, Marco Santagostino, Fabio Paleari
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Publication number: 20110178069Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.Type: ApplicationFiled: May 24, 2010Publication date: July 21, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M.C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L.C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Publication number: 20110178070Abstract: The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: June 23, 2009Publication date: July 21, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xianchang Gong, Bohan Jin, Massaki Hirose, Feng Zhou, Qing Dong
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Publication number: 20110172171Abstract: The present invention relates to taurine or taurine-like substances for the prevention of brain oedema, particularly brain intramyelinic oedema and more particularly brain intramyelinic oedema induced by an anti-convulsive drug such as vigabatrin. The invention relates to a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis for the prevention of brain oedema.Type: ApplicationFiled: September 4, 2009Publication date: July 14, 2011Inventors: Serge Picaud, José-Alain Sahel, Firas Jammoul
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Publication number: 20110172211Abstract: There is provided a transnasal anticonvulsive pharmaceutical composition including a poorly soluble anti-convulsant. The anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether and fatty acid ester, wherein the fatty acid ester is selected from the group consisting of caprylocaproyl polyoxylglyceride, isopropyl palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20, methyl laurate, ethyl laurate, and polysorbate 20. Also, the anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether, fatty acid ester, methylpyrrolidone, water and alcohol. Therefore, the transnasal anticonvulsive pharmaceutical composition may be useful to highly enhance the bioavailability of the poorly soluble anticonvulsant.Type: ApplicationFiled: November 5, 2010Publication date: July 14, 2011Inventors: Myoung-Ki Baek, Jae-Hoon Jo, Hye-Jin Chang
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Publication number: 20110172188Abstract: The invention first relates to a product containing at least one connexin-blocking agent and a psychotropic drug as combination products for use simultaneously, separately, or spread over time in patients suffering from psychiatric and/or neurodegenerative disorders. The connexin-blocking agent is advantageously selected from the group comprising meclofenamic acid, 18-?-glycyrrhetinic acid, carbenoxolone, mefloquine, and 2-APB, and preferably consists of meclofenamic acid. The invention first relates to a product containing at least one connexin-blocking agent and a psychotropic drug as combination products for use simultaneously, separately, or spread over time in patients suffering from psychiatric and/or neurodegenerative disorders. The connexin-blocking agent is advantageously selected from the group comprising meclofenamic acid, 18-?-glycyrrhetinic acid, carbenoxolone, mefloquine, and 2-APB, and preferably consists of meclofenamic acid.Type: ApplicationFiled: September 10, 2009Publication date: July 14, 2011Applicant: BIO MODELING SYSTEMS OU BMSYSTEMSInventors: Franck Mouthon, Mathieu Charveriat, Jean-Philippe Deslys, Francois Iris
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Publication number: 20110172212Abstract: Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; typically, A1 and A2 represent a hydrogen atom or a substitutable monocyclic or polycyclic heteroaromatic ring and W represents a substitutable benzene ring or any group represented by the following formula (10) or (11): where X represents O, CH2, C(?O), NR11, or CHR35 and D represents a group represented by the following formula (6): [Formula 4] -Q-Y—B??(6) where Q represents a single bond, NR12, or a group represented by the formula (13): and Y represents a group represented by the following formula (7): [Formula 6] —(CR18R19)m3- or —(CR20R21)m4-z-(CR22R23)m5-??(7) where z represents a substitutable monocyclic or polycyclic aromatic ring; and B represents —NR25R26; and R1 to R26 in the above formulae represent a hydrogen atom, an alkyl group, an alkenyl group, or an alkynyl group.Type: ApplicationFiled: March 18, 2011Publication date: July 14, 2011Applicant: KUREHA CORPORATIONInventors: Atsushi SAITOU, Shigeyuki Kikumoto, Masahiro Ono, Ryo Matsui, Masashi Yamamoto, Tomohiro Sawa, Shigeru Suzuki, Mikiro Yanaka
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Patent number: 7977330Abstract: The invention relates to salts of 1-(2-Fluoro-phenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-urea and crystalline forms thereof, their production and usage, and pharmaceutical preparations containing such salts and crystalline forms.Type: GrantFiled: May 21, 2007Date of Patent: July 12, 2011Assignee: Novartis AGInventors: Lilli Feng, Xinglong Jiang, Piotr H. Karpinski
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Publication number: 20110165259Abstract: [Problem to be Solved] The purpose of present invention is to provide a medicine which has low contamination with a fine-pulverizing medium, is safe and has improved bioavailability. [Solution] A method for producing a composite organic compound powder for medical use is used which comprises: mixing a poorly water-soluble and crystalline organic compound powder, a physiologically acceptable salt, a physiologically acceptable polyol, and a carboxyvinyl polymer and fine-pulverizing the organic compound powder; and removing at least the salt and the polyol during or after fine-pulverizing.Type: ApplicationFiled: September 15, 2009Publication date: July 7, 2011Applicant: ACTIVUS PHARMA CO., LTD.Inventors: Takashi Hirokawa, Takahiro Tada, Jun Nihira
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Publication number: 20110160154Abstract: Disclosed herein are substituted piperazine late Na+ channel modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: January 6, 2011Publication date: June 30, 2011Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar
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Patent number: 7968536Abstract: The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: June 30, 2008Date of Patent: June 28, 2011Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin