Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 514/327)
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Publication number: 20100298382Abstract: This application describes compositions of receptor inhibitors, including antipsychotic agents, for example haloperidol, and methods of use for alleviating clinical depression, improving cognition and/or treating other syndromes, conditions or diseases for which anti-depressant agents are prescribed. Furthermore, this application describes compositions and methods to induce supersensitivity in dopamine D2 and other receptors involved in depression and/or cognition as a means of alleviating clinical depression or improving cognition.Type: ApplicationFiled: February 5, 2009Publication date: November 25, 2010Applicant: CLERA INC.Inventors: Philip Seeman, Philip M. Tokeikis
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Publication number: 20100292206Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 17, 2008Publication date: November 18, 2010Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20100291069Abstract: Maternal diabetes can lead to a developmental malformation of an embryo. A developmental malformation caused by maternal diabetes is commonly referred to as a diabetic embryopathy. There is currently no effective treatment for reducing or inhibiting a diabetic embryopathy. To this end, the present invention is drawn to novel methods of treating a diabetic embryopathy.Type: ApplicationFiled: May 13, 2010Publication date: November 18, 2010Applicant: UNIVERSITY OF MARYLAND, BALTIMOREInventors: E. Albert REECE, Zhiyong ZHAO, Peixin YANG
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Publication number: 20100284944Abstract: Disclosed are Compounds that block off-notes in consumables and methods of blocking off-notes in consumables including off-notes provided by artificial sweeteners including aspartame, Saccharin, acesulfame K (Acesulfame potassium), sucralose and cyclamate; and including stevioside, swingle extract, glyccerhizin, perillartine, naringin dihydrochalcone, neohesperidine dihydrochalcone, mogroside V, rubusoside, rubus extract, and rebaudioside A.Type: ApplicationFiled: March 27, 2008Publication date: November 11, 2010Inventors: Ioana Maria Ungureanu, Nicole Erna Irene Brune, Jay Patrick Slack, Kimberley Gray, Christopher Todd Simons, Jenny Ellen Evans Pennimpede
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Patent number: 7829583Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: July 13, 2007Date of Patent: November 9, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yan Chen
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Method for the treatment of neurological disorders by enhancing the activity of ?-glucocerebrosidase
Patent number: 7829579Abstract: Provided is a method of increasing the stability of wild-type ?-glucocerebrosidase. Also provided are methods of treating and/or preventing an individual having a neurological disease in which increased expression or activity of ?-glucocerebrosidase in the central nervous system would be beneficial. This method includes administering an effective amount of a pharmacologic chaperone for ?-glucocerebrosidase, with the proviso that the individual does not have a mutation in the gene encoding ?-glucocerebrosidase. Further provided are ?-glucocerebrosidase inhibitors which have been identified as specific pharmacologic chaperones and which have been shown to increase activity of ?-glucocerebrosidase in vivo in the central nervous system.Type: GrantFiled: June 25, 2007Date of Patent: November 9, 2010Assignee: Amicus Therapeutics, Inc.Inventor: Brandon Alan Wustman -
Publication number: 20100279986Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Yue-Mei ZHANG, Bangping Xiang, Shyh-Ming Yang, Kenneth Rhodes, Robert Scannevin, Paul Jackson, Davraj Chakravarty, Xiaodong Fan, Lawrence J. Wilson, Prabha Karnachi
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Publication number: 20100280047Abstract: Polymeric water-soluble salts of medicaments that are sparingly soluble in water, consisting of a polymer with anion character that is soluble in water at pH values of 2-13 and a sparingly soluble medicament with cation character.Type: ApplicationFiled: December 10, 2008Publication date: November 4, 2010Applicant: BASF SEInventors: Karl Kolter, Maximilian Angel, Kathrin Meyer-Böhm
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Patent number: 7825133Abstract: The present invention provides N-substituted-2(1H) pyridones or the pharmaceutical acceptable salts thereof, and the pharmaceutical preparations containing the compounds. The compounds of the present invention can be used to treat various fibrotic diseases effectively, e.g., hepatic fibrosis.Type: GrantFiled: November 14, 2003Date of Patent: November 2, 2010Assignee: Shanghai Genomics, Inc.Inventor: Xianghui Yi
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Publication number: 20100264055Abstract: A vehicle to carry a powered medication that addresses the limitations of the prior art. It includes a system and method. A powder delivery system includes a first panel and a second panel coupled together around a periphery of the panels to form a sealed void therebetween, each the panel having a width and length about equal to a standard credit card width and length, respectively; and a powder, disposed in the void, having a quantity at least about equal to an active dose of the powder; wherein a thickness of the panels with the powder disposed therebetween is not greater than about 0.1 inches and more preferably not greater than about 0.03 inches.Type: ApplicationFiled: April 20, 2009Publication date: October 21, 2010Inventor: Jordan Eisenberg
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Patent number: 7812035Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.Type: GrantFiled: December 11, 2002Date of Patent: October 12, 2010Assignee: Sepracor Inc.Inventors: Heike Radeke, Liming Shao
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Patent number: 7812159Abstract: The present invention relates to processes for preparing aromatic ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.Type: GrantFiled: January 9, 2006Date of Patent: October 12, 2010Assignee: Arena Pharamaceuticals, Inc.Inventors: Tawfik Gharbaoui, John R. Fritch, Ashwin M. Krishnan, Beverly Wolgast Throop, Naomi S. Kato
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Publication number: 20100249045Abstract: The present invention is in the field of oral, abuse resistant pharmaceutical compositions of opioid agonists, extended release pharmaceutical compositions of opioid agonists and extended release abuse resistant pharmaceutical compositions of opioid agonists and the use thereof. The present invention is also directed to extended release pharmaceutical compositions and the use thereof for preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering. The present invention is further directed at a method of preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering.Type: ApplicationFiled: April 26, 2008Publication date: September 30, 2010Applicant: THERAQUEST BIOSCIENCES, INC.Inventor: Najib Babul
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Publication number: 20100249163Abstract: The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: November 26, 2008Publication date: September 30, 2010Inventors: Daniel Dube, Erich L. Grimm, Dwight MacDonald, Bruce MacKay
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Publication number: 20100240703Abstract: The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ?O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: May 30, 2008Publication date: September 23, 2010Inventors: Moriyasu Masui, Hidenori Mikamiyama, Naoki Tsuno
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Publication number: 20100234349Abstract: This invention relates to novel pharmaceutical compositions comprising therapeutically effective combination of a positive allosteric modulator of nicotine receptors; and a cognitive enhancer selected from the group consisting of a nicotine acetylcholine receptor agonist, an acetylcholine esterase inhibitor, a positive AMPA receptor modulator, an antipsychotic drug, an antidepressant drug and an anti Parkinson drug. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating cognitive disorders.Type: ApplicationFiled: September 4, 2007Publication date: September 16, 2010Inventors: Gunnar M. Olsen, Dan Peters, Bjarne H. Dahl, Jeppe Kejser Christensen, Steven Charles Loechel, Daniel B. Timmermann
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Patent number: 7790898Abstract: Substituted 3-phenylpiperidine compounds corresponding to Formula I in which R1 and R2 have the meanings defined in the specification, methods for preparing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds for treating or inhibiting various conditions, especially pain.Type: GrantFiled: January 26, 2007Date of Patent: September 7, 2010Assignee: Gruenenthal GmbHInventors: Joerg Holenz, Helmut Buschmann, Michael Finkam
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Publication number: 20100222366Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.Type: ApplicationFiled: July 23, 2008Publication date: September 2, 2010Inventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
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Publication number: 20100215774Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin and/or other active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: February 8, 2008Publication date: August 26, 2010Inventor: Todd Maibach
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Publication number: 20100216784Abstract: Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods for screening for such compounds, by measuring capacitative calcium entry in cells which optionally overexpress APP or a fragment thereof. Also provided are methods of treating or reducing the risk of developing ?-amyloid production, ?-amyloid deposition, ?-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of compounds which decrease ?-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of compounds which inhibit capacitative calcium entry in cells.Type: ApplicationFiled: April 29, 2010Publication date: August 26, 2010Inventors: Michael J. Mullan, Daniel Paris, Pancham Bakshi
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Publication number: 20100216776Abstract: Provided are methods of determining whether a compound is an inhibitor of an S100 protein. The methods utilize a biosensor that comprises the S100 protein that has a covalently bound fluorescent dye at an amino acid residue of the S100 protein that becomes less exposed to the aqueous solution upon activation of the S100 protein, where the fluorescent dye has decreased fluorescence when exposed to the aqueous solution than when protected from exposure to the aqueous solution. Also provided are methods of treating a subject having metastatic cancer.Type: ApplicationFiled: August 10, 2006Publication date: August 26, 2010Inventors: Anne Reba Bresnick, Sarah Claire Garrett
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Publication number: 20100209514Abstract: Patients are treated with 24-hour oral sustained release opioid formulations which, upon administration, provide an initially rapid opioid absorption such that the minimum effective analgesic concentration of the opioid is more quickly achieved. These sustained release opioid formulations include an effective amount of at least one retardant material to cause said opioid analgesic to be released at a such a rate as to provide an analgesic effect after oral administration to a human patient for at least about 24 hours, and are characterized by providing an absorption half-life from 1 to about 8 hours. A method of titrating a human patient utilizing these sustained release opioid formulations is also disclosed.Type: ApplicationFiled: December 8, 2009Publication date: August 19, 2010Inventors: Richard S. Sackler, Robert F. Kaiko, Paul Goldenheim
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Publication number: 20100210592Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Inventors: Sabine Kolczewski, Hans-Peter Marty, Robert Narquizian, Emmanuel Pinard, Henri Stalder
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Publication number: 20100210631Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly used for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital, and gastrointestinal diseases.Type: ApplicationFiled: May 14, 2008Publication date: August 19, 2010Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventors: Piero Melloni, Alessandra Restivo, Emanuela Izzo, Simona Francisconi, Elena Colombo, Cibele Sabido-David
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Publication number: 20100197661Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.Type: ApplicationFiled: March 23, 2010Publication date: August 5, 2010Inventors: Gideon Dreyfuss, Jin Wang
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Publication number: 20100197680Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: March 15, 2008Publication date: August 5, 2010Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
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Publication number: 20100197715Abstract: The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.Type: ApplicationFiled: January 20, 2010Publication date: August 5, 2010Inventors: Sabine Kolczewski, Emmanuel Pinard, Henri Stalder
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Publication number: 20100197667Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: April 14, 2010Publication date: August 5, 2010Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Patent number: 7763657Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salt thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.Type: GrantFiled: March 15, 2006Date of Patent: July 27, 2010Assignee: Amorepacific CorporationInventors: Hee-Doo Kim, Young-Ger Suh, Hyeung-Geun Park, Uh Taek Oh, Seol Rin Park, Joo Hyun Kim, Mi Jung Jang, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-Il Kim, Byoung Young Woo
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Publication number: 20100172974Abstract: Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques are disclosed.Type: ApplicationFiled: March 12, 2010Publication date: July 8, 2010Inventors: Benjamin Oshlack, Mark Chasin, Hua-Pin Huang
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Publication number: 20100173880Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: ApplicationFiled: December 22, 2009Publication date: July 8, 2010Applicant: Chiesi Farmaceutici S.p.A.Inventors: Antonio Caligiuri, Mauro Riccaboni, Gabriele Amari
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Publication number: 20100168080Abstract: The present invention relates to novel morpholine, oxazapane and piperidine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: December 16, 2009Publication date: July 1, 2010Inventors: Uttam KHAMRAI, Sumit Kumar Karak, Matthew Ronsheim, Ashis Kumar Saha
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Publication number: 20100168167Abstract: There is provided compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, m and n have meanings given in the description, and pharmaceutically acceptable derivatives thereof, which compounds are useful in the treatment of diseases and conditions associated with inflammation.Type: ApplicationFiled: March 12, 2008Publication date: July 1, 2010Inventors: Benjamin Pelcman, Christian Krog-Jensen, Yaping Shen, James Gee Kan Yee, Lloyd F. MacKenzie, Yuanlin Zhou, Kang Han, Jeffery R. Raymond
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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
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Publication number: 20100168171Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of interfering with the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.Type: ApplicationFiled: March 20, 2008Publication date: July 1, 2010Inventors: Paul John Beswick, Robert James Gleave, Jon Graham Anthony Steadman, Daryl Simon Walter
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Publication number: 20100168170Abstract: There is provided compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, m, n, q and r have meanings given in the description, and pharmaceutically acceptable derivatives thereof, which compounds are useful in the treatment of diseases and conditions associated with inflammation.Type: ApplicationFiled: March 12, 2008Publication date: July 1, 2010Inventors: Benjamin Pelcman, Christian Krog-Jensen, Yaping Shen, James Gee Kan Yee, Lloyd F. Mackenzie, Yuanlin Zhou, Kang Han, Jeffery R. Raymond
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Publication number: 20100160305Abstract: 3,4,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4,5-substituted piperidine compound, a method for the manufacture of a 3,4,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The compounds are of the formula I, wherein the substitutents are as defined in the specification.Type: ApplicationFiled: March 7, 2006Publication date: June 24, 2010Applicant: NOVARTIS AGInventors: Keiichi Masuya, Fumiaki Yokokawa, Osamu Irie, Atsuko Nihonyanagi, Takeru Ehara, Kazuhide Konishi, Takanori Kanazawa, Masaki Suzuki
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Publication number: 20100159034Abstract: The present invention relates to new pyrrolidinone inhibitors of PDE-4 activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 15, 2009Publication date: June 24, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100150986Abstract: The present invention relates to a film preparation having both rapid solubility and flexibility at the same time. The film preparation is characterized by comprising: an active-ingredient-containing layer comprising an active ingredient, a water-soluble polymer selected from the group consisting of methyl cellulose, hydroxypropyl cellulose, and hydroxypropyl methyl cellulose, and a disintegrating agent; and an active-ingredient-free layer comprising methyl cellulose and/or hydroxypropyl methyl cellulose. It is further characterized in that the amount of the active ingredient is 0.1-75.0 mass % of a total mass of the film preparation and a total content of the active ingredient and the water-soluble polymer in the active-ingredient-containing layer is 15.0-95.0 mass % of a total mass of the active-ingredient-containing layer.Type: ApplicationFiled: June 7, 2007Publication date: June 17, 2010Applicant: SATO PHARMACEUTICAL CO., LTD.Inventors: Toshiro Nagaso, Mitsutoshi Tatara, Toshihito Shimizu
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Publication number: 20100144718Abstract: The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.Type: ApplicationFiled: June 17, 2009Publication date: June 10, 2010Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
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Publication number: 20100144657Abstract: The present invention relates to new phenylpiperidine modulators of opioid ?-receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 8, 2009Publication date: June 10, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100125079Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: January 25, 2010Publication date: May 20, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Publication number: 20100119623Abstract: The present invention relates to new imidazolyl modulators of 5-HT3 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 16, 2009Publication date: May 13, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100113469Abstract: This invention concerns compositions for the treatment of Lower Urinary Tract Symptoms (LUTS), and especially LUTS which results from benign prostatic hypertrophy. The compositions of the invention comprise a Beta-3 agonist described below, optionally in combination with a 5-alpha reductase inhibitor, or an NK-1 antagonist or an alpha-1 adrenergic antagonist or an anti-muscarinic agent. The invention also includes compositions comprising a beta-3 agonist and two additional active agents selected from a 5-alpha reductase inhibitor, an NK-1 antagonist, an alpha-1 adrenergic antagonist or an anti-muscarinic agent.Type: ApplicationFiled: March 25, 2008Publication date: May 6, 2010Applicant: MERCK & CO., INC.Inventors: Tara Frenkl, Stuart A. Green, Enan Macintyre, Sander G. Mills
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Patent number: 7709503Abstract: Compounds of Formula (1) and their pharmaceutically acceptable salts are described: Formula (1) Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: GrantFiled: September 10, 2004Date of Patent: May 4, 2010Assignee: AstraZeneca ABInventors: Oluyinka Morenike Green, Kenneth Gregory Hull, Haihong Ni, Sheila Irene Hauck, George Byron Mullen, Alexander Louis Breeze, Neil James Hales, David Timms
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Publication number: 20100104618Abstract: Surgically implantable drug delivery systems for long-term delivery of haloperidol containing a biodegradable polymer and haloperidol fabricated into the surgically implantable drug delivery systems via solvent casting and compression molding are provided. Also provided are methods for producing the surgically implantable drug delivery systems and methods for using these systems in the treatment of psychotic disorders such as schizophrenia.Type: ApplicationFiled: October 20, 2009Publication date: April 29, 2010Inventors: Steven J. SIEGEL, Karen I. Winey, Raquel E. Gur, Robert H. Lenox
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Publication number: 20100105736Abstract: A compound having the general formula wherein A is selected from the group consisting of to the formation of a compound of the general formula (1) and a compound of the general formula (2) respectively, and pharmaceutically acceptable salts thereof, wherein R1 is a member selected from the group consisting of CF3, OSO2CF3, OSO2CH3, SOR4, SO2R4, COR4, CN, OR4, NO2, CONHR4, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br and I, wherein R4 is as defined below; R2 is a member selected from the group consisting of H, F, Cl, Br, I, CN, CF3, CH3, OCH3, OH, NH2, SOmCF3, O(CH2)mCF3, SO2N(R4)2, CH?NOR4, COCOOR4, COCOON(R4)2, (C1-C8)alkyl, (C3-C8)cykloalkyl, CH2OR4, CH2(R4)2, NR4SO2CF3, NO2, at phenyl at positions 2, 4, 5 or 6, wherein x and R4 are as defined below; R3 is a member selected from the group consisting of hydrogen, CF3, CH2CF3, (C1-C8)alkyl, (C3-C8)cykloalkyl, (C4-C9)cycloalkylmethyl, (C2-C8)alkenyl, (C2-C8)alkynyl, 3,3,3-tri-fluoropropyl, 4,4,4-trifluorobutyl, CH2SCH3, CH2CH2OCH3,Type: ApplicationFiled: April 14, 2008Publication date: April 29, 2010Applicant: NSAB, Filial af NeuroSearch Sweden Ab, SverigeInventor: Håkan V. Wikström
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Publication number: 20100098690Abstract: The present invention provides a pharmaceutical composition comprising a combination of an Hsp 90 family protein inhibitor and at least one compound, the said pharmaceutical composition wherein the Hsp 90 family protein inhibitor is a benozoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl, or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom, hydroxy or halogen; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like], or a prodrug thereof; or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: March 5, 2008Publication date: April 22, 2010Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Shiro Soga, Toshihiko Ishii, Takayuki Nakashima, Yukimasa Shiotsu, Shiro Akinaga
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Patent number: 7700627Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, prodrug, or bioisostere thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: July 17, 2007Date of Patent: April 20, 2010Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 7700587Abstract: Haloperidol analogs that conforms to the structural formulae: wherein: R is H, or —(CH2)n—OH, n is an integer from 0 to 2, and A is a heterocyclic bridging group, consisting essentially of carbon and at least one nitrogen atom, which effectively maintains the distance between the moieties connected thereby such that the compound (1) is incapable of metabolizing to BCPP+ like species, (2) has an affinity for the D2 receptor subtype of 15<D2<250 and (3) functions as a dopamine receptor antagonist, or the structural formulae: wherein: R1 is H, or —(CH2)n—OH, n is an integer from 0 to 2, B is an aza- or diaza-bicyclo group, which effectively maintains the distance between the moieties connected thereby such that the compound is incapable of metabolizing to BCPP+ like species; and Z is —CH— or N; and pharmaceutically acceptable salts, esters, derivatives, metal complexes, conjugates and prodrugs thereof.Type: GrantFiled: September 7, 2004Date of Patent: April 20, 2010Assignee: Florida A&M UniversityInventors: Seth Y. Ablordeppey, Donald M. N. Sikazwe