Quinoxalines (including Hydrogenated) Patents (Class 544/353)
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Publication number: 20090131444Abstract: The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans.Type: ApplicationFiled: May 23, 2006Publication date: May 21, 2009Applicant: ASTRAZENECA ABInventors: Folkert Reck, Marshall Morningstar, Hajnalka Hartl
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Patent number: 7534794Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are asType: GrantFiled: October 11, 2002Date of Patent: May 19, 2009Assignee: Biovitrum ABInventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
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Publication number: 20090123423Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: May 14, 2009Inventors: Yonghua Gai, Yat Sun Or, Zhe Wang
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Publication number: 20090124625Abstract: The present invention relates to novel compounds of formula (I) wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: ApplicationFiled: June 17, 2005Publication date: May 14, 2009Applicant: Addex Pharmaceuticals SAInventors: Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
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Publication number: 20090118295Abstract: The use of a compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m, where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Z and Z? are joined by a single or a double bond and are ?C— or —N— provided that both are not N; Ra, R1, R2, R3, R3a, R4 and R8 are specified organic groups; n is 2, 3 or 4 and p is 0-4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: ApplicationFiled: December 6, 2006Publication date: May 7, 2009Applicant: SYNGENTA CROP PROTECTION, INCInventors: Jerome Cassayre, Peter Maienfisch, Fredrik Cederbaum, Louis-Pierre Molleyres
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Publication number: 20090111778Abstract: Certain 2-keto-oxazole compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: November 17, 2006Publication date: April 30, 2009Inventors: Richard Apodaca, J. Guy Breitenbucher, Matthew T. Epperson, Amy K. Fried, Daniel J. Pippel, Mark Seierstad
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Publication number: 20090105266Abstract: The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the formula (I): in which the substitutents are as defined in claim 1 and salts, solvates, hydrates and N-oxides thereof.Type: ApplicationFiled: April 18, 2008Publication date: April 23, 2009Inventors: Ralf Glatthar, David Carcache
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Publication number: 20090093469Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: ApplicationFiled: December 15, 2008Publication date: April 9, 2009Applicant: WYETHInventors: Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey Cameron McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye
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Publication number: 20090093478Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: October 26, 2007Publication date: April 9, 2009Inventors: Clive Leslie BRANCH, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
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Publication number: 20090091252Abstract: The present invention provides a novel binaphthyl compound and an organic light emitting element having a good light emitting efficiency and a high durability at a low driving voltage.Type: ApplicationFiled: October 2, 2008Publication date: April 9, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Tetsuya Kosuge, Jun Kamatani, Shigemoto Abe, Ryota Ooishi, Kengo Kishino
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Publication number: 20090088425Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: September 15, 2008Publication date: April 2, 2009Inventors: Jacques Bailly, Cornelia Hertel, Daniel Hunziker, Christian Lerner, Ulrike Obst Sander, Jens-Uwe Peters, Philippe Pflieger, Tanja Schulz-Gasch
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Patent number: 7511043Abstract: The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7?-hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR? and PPAR?.Type: GrantFiled: March 4, 2004Date of Patent: March 31, 2009Assignee: Amgen Inc.Inventors: Jonathan Houze, Sharon McKendry, Joshua Gergely, Yi Xia, Bei Shan, Frank Kayser
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Publication number: 20090072718Abstract: An object of the present invention is to provide a quinoxaline derivative represented by a general formula (1). Ar1 represents one of a substituted or unsubstituted biphenyl group, and a substituted or unsubstituted terphenyl group; Ar2 represents one of a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, and a substituted or unsubstituted terphenyl group; ?1 represents an arylene group having 6 to 25 carbon atoms; and R11 to R15 are the same or different from one another, and each of them represents any one of a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, and a substituted or unsubstituted aryl group having 6 to 25 carbon atoms.Type: ApplicationFiled: February 20, 2008Publication date: March 19, 2009Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Ryoji Nomura, Satoshi Seo
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Publication number: 20090072716Abstract: The present invention provides an aromatic amine derivative having a specific structure including a substituted diphenylamino group attached to a naphthalene structure. This aromatic amine derivative can realize an organic electroluminescent element having high emission luminance and luminous efficiency and having a prolonged lifetime. The organic electroluminescent element includes an organic thin film layer provided between a cathode and an anode. The organic thin film layer has a single layer or multilayer structure including at least a light emitting layer. At least one layer in the organic thin film layer contains the aromatic amine derivative either solely or as a component of a mixture.Type: ApplicationFiled: April 6, 2006Publication date: March 19, 2009Applicant: IDEMITSU KOSAN CO., LTD.Inventor: Masakazu Funahashi
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Publication number: 20090066231Abstract: The present invention relates to electroluminescent devices that comprise organic layers that contain triazole compounds of the formula (I), or formula (II). The compounds are suitable components of, for example, blue-emitting, durable, organo-electroluminescent layers. The electroluminescent devices may be employed for full color display panels in, for example, mobile phones, televisions and personal computer screens.Type: ApplicationFiled: April 19, 2006Publication date: March 12, 2009Inventors: Hidetaka Oka, Ramachandra V. Joshi, Junichi Tanabe, Sanjoy Lahiri, Dhaval Vashi, Preetam Ghogale
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Publication number: 20090048443Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optType: ApplicationFiled: October 16, 2008Publication date: February 19, 2009Applicant: AMR TECHNOLOGY, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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Publication number: 20090048228Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: December 9, 2005Publication date: February 19, 2009Inventors: Barbara Attenni, Federica Ferrigno, Philip Jones, Raffaele Ingenito, Olaf Kinzel, Laura Llauger Bufi, Jesus Maria Ontoria, Giovanna Pescatore, Michael Rowley, Rita Scarpelli, Carsten Schultz
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Publication number: 20090033210Abstract: To provide a novel fluoranthene derivative and an organic light emitting device having the fluoranthene derivative.Type: ApplicationFiled: April 19, 2007Publication date: February 5, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Akihito Saitoh, Keiji Okinaka, Satoshi Igawa, Jun Kamatani, Naoki Yamada, Masashi Hashimoto, Masanori Muratsubaki, Takao Takiguchi, Akihiro Senoo, Shinjiro Okada, Minako Nakasu
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Publication number: 20090036433Abstract: Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials.Type: ApplicationFiled: December 15, 2006Publication date: February 5, 2009Inventors: Nathalie Caileau, David Thomas Davies, Alan Joseph Hennessy, Graham Elgin Jones, Timothy James Miles, Neil David Pearson
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Publication number: 20090030003Abstract: The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.Type: ApplicationFiled: May 9, 2008Publication date: January 29, 2009Inventors: Patrick R. Verhoest, Caroline Proulx-Lafrance
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Publication number: 20090030176Abstract: An aminoquinoxaline compound represented by the following formula (1a), and a polyaminoquinoxaline compound obtained by polymerizing the aminoquinoxaline compound, wherein R1 and R2 independently represent a hydrogen atom, a hydroxyl group, a C1-C10 alkyl group, a C1-C10 alkoxy group, or the like, R3 and R4 independently represent a hydrogen atom, a halogen atom, a cyano group, a nitro group, an amino group, a C1-C10 alkyl group, a C1-C10 alkoxy group or the like, and X1 represents —NH—R5—NH2 or —NH—R6.Type: ApplicationFiled: January 12, 2005Publication date: January 29, 2009Inventors: Mikio Kasai, Hitoshi Furusho
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Publication number: 20090026919Abstract: The present invention relates to the improvement of organic electroluminescent devices, in particular blue-emitting devices, by using compounds of the formula (1) as host materials in the emitting layer.Type: ApplicationFiled: September 20, 2005Publication date: January 29, 2009Applicant: Merck Paten GmbH Patents & Scientific InformationInventors: Philipp Stossel, Arne Busing, Horst Vestweber, Holger Heil
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Publication number: 20090023741Abstract: The present invention relates to aryl/hetarylamide derivatives of the general formula I, process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP2 receptor.Type: ApplicationFiled: June 12, 2008Publication date: January 22, 2009Inventors: Bernd Buchmann, Nico Braeuer, Olaf Peters, Knut Eis, Marcus Koppitz, Bernhard Lindenthal, Gernot Langer, Tim Wintermantel, Antonius Ter Laak
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Publication number: 20090023733Abstract: The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.Type: ApplicationFiled: March 6, 2007Publication date: January 22, 2009Inventors: Peter Cage, Mark Furber, Christopher Luckhurst, Matthew Perry, Brian Springthorpe
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Publication number: 20090018139Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.Type: ApplicationFiled: September 17, 2008Publication date: January 15, 2009Applicant: Oxagen LimitedInventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Michael George Hunter, Mark Whittaker, Chris Palmer, Eric R. Pettipher
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Patent number: 7476673Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.Type: GrantFiled: December 17, 2004Date of Patent: January 13, 2009Assignee: Allergan, Inc.Inventors: Kwok Yin Tsang, Santosh Sinha, Xiaoxia Liu, Smita Bhat, Roshantha A. Chandraratna
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Publication number: 20090009074Abstract: There are provided oligoarylene derivatives capable of emitting blue light at high luminous efficiency which are represented by the following general formulae (1) to (4): Ar1?Ch?Ar2??(1) Ch1?L?Ch2??(2) Ar3?(L1)a?Ch3?(L2)b?Ar4??(3) Ar5?Ch4?(Ar7)n?L3?(Ar8)m?Ch5?Ar6??(4) wherein Ch, Ch1 and Ch2 are respectively a group containing at least one substituted or unsubstituted condensed aromatic ring having 14 to 20 nuclear atoms; Ch3, Ch4 and Ch5 are respectively a substituted or unsubstituted arylene group having 14 to 20 nuclear atoms; Ar1, Ar2, Ar3, Ar4, Ar5 and Ar6 are respectively a substituted or unsubstituted aryl group having 5 to 30 nuclear atoms; Ar7 and Ar8 are respectively a substituted or unsubstituted arylene group having 5 to 30 nuclear atoms; L1, L2 and L3 are respectively a connecting group; and a, b, n and m are respectively an integer of 0 to 1, as well as organic electroluminescent devices using the same.Type: ApplicationFiled: September 10, 2008Publication date: January 8, 2009Applicant: Idemitsu Kosan Co., Ltd.Inventors: Hidetsugu Ikeda, Masahide Matsuura, Hisayuki Kawamura
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Publication number: 20090005390Abstract: This invention relates to novel quinuclidine derivatives and their use as pharmaceuticals. 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: September 8, 2008Publication date: January 1, 2009Inventors: Dan PETERS, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Phillip K. Ahring, Tino Dyhring Jorgensen
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Publication number: 20080318975Abstract: A compound of formula (I) wherein R, R1, and R2, ring A and ring B are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.Type: ApplicationFiled: July 10, 2006Publication date: December 25, 2008Inventors: Jurgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
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Publication number: 20080318965Abstract: The present invention relates to alpha2-adrenergic receptor agonist nitrooxyderivatives having improved pharmacological activity and enhanced tolerability. They can be employed for the treatment of ocular diseases, in particular high intraocular pressure and glaucoma.Type: ApplicationFiled: February 2, 2007Publication date: December 25, 2008Inventors: Francesca Benedini, Francesco Impagnatiello, Stefano Biondi, Ennio Ongini, Wesley Kwan Mung Chong
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Patent number: 7468367Abstract: This invention relates to heterocyclic substituted ethylene diamine derivatives and their use as pharmaceuticals.Type: GrantFiled: December 13, 2002Date of Patent: December 23, 2008Assignee: Smithkline Beecham p.l.c.Inventors: Steven Coulton, Amanda Johns, Roderick Alan Porter
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Publication number: 20080306239Abstract: There is provided a quinoxaline-containing compound represented by the following formula (I); wherein Ar1 represents a substituted or unsubstituted monovalent aromatic group; and R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group.Type: ApplicationFiled: March 3, 2008Publication date: December 11, 2008Applicant: FUJI XEROX CO., LTD.Inventors: Koji HORIBA, Hidekazu HIROSE, Takeshi AGATA
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Publication number: 20080303423Abstract: The present invention relates to anthracene derivatives which are suitable for use in organic electroluminescent devices, and to organic electroluminescent devices containing these anthracene derivatives.Type: ApplicationFiled: December 7, 2006Publication date: December 11, 2008Applicant: Merck Patent GmbHInventors: Holger Heil, Arne Buesing, Philipp Stoessel
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Publication number: 20080300251Abstract: The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.Type: ApplicationFiled: September 1, 2006Publication date: December 4, 2008Inventors: Jitendra A. Sattigeri, Murugaiah M.S. Andappan, Kaushal Kishore, Sachin Sethi, Sachin Ramesh Kandalkar, Chanchal Kumar Pal, Dipak C. Mahajan, Shahadat Ahmed, Santhosh Sadashiv Parkale, T. Srinivasan, Lalima Sharma, Vinay S. Bansal, Anita Chugh, Joseph Alexanand Davis
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Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
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Publication number: 20080293728Abstract: A complex comprises at least an ?2-adrenergic receptor agonist and a compound that provides an opposite charge to a charge on the ?2-adrenergic receptor agonist, wherein the complex is charge neutral as a whole and has a solubility in a range from about 0.3 ?g/ml to about 2.5 mg/ml in water at pH of about 7 and temperature of about 25° C. The complex is included in a composition, device, or implant for use in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.Type: ApplicationFiled: May 15, 2008Publication date: November 27, 2008Inventors: Gregory L. McIntire, Stephen R. Davio, Arthur E. Harms, Hongna Wang
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Publication number: 20080269229Abstract: This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: July 1, 2008Publication date: October 30, 2008Inventors: Dan Peters, Birgitte L. Eriksen, Elsebet Ostergaard Nielsen, Jergen Scheel-Kruger, Gunnar M. Olsen
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Publication number: 20080261974Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.Type: ApplicationFiled: September 22, 2006Publication date: October 23, 2008Inventors: Kevin J Duffy, Duke M. Fitch, Rosanna Tedesco, Michael N. Zimmerman
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Publication number: 20080261987Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: July 21, 2006Publication date: October 23, 2008Applicant: ChemoCentryx, Inc.Inventors: Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
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Publication number: 20080261989Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I wherein A is a carbocycle or heterocycle; X is alkylene, NR4C(O), NR4C(S), NR4C(NH), NR4SO, NR4SO2, NR4C(O)NH, NR4C(S)NH, C(O)NR4, C(S)NR4, C(NH)NR4, NR4PO or NR4PO(OH) wherein R4 is H or alkyl; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl or a heterocycle each of which is optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R2 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R3 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; m is 0-3; n is 0-3; and salts and solvates thereof.Type: ApplicationFiled: April 29, 2005Publication date: October 23, 2008Inventors: Michael F.T. Koehler, Richard Goldsmith, Daniel P. Sutherlin
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Publication number: 20080255102Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: ApplicationFiled: June 23, 2008Publication date: October 16, 2008Applicant: WyethInventors: An Thien Vu, Paige Erin Mahaney, Stephen Todd Cohn
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Patent number: 7432270Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists wherein: Y represents a bond, oxygen, or a group (CH2)n, wherein n represents 1, 2 or 3; m represents 1, 2, or 3; p represents ) or 1; X is NR, wherein R is H or (C1-4)alkyl; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; any of which may be optionally substituted; A2 represents phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R1 represents hydrogen, optionally substituted (C1-4)alkoxy, halo, cyano, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclyl group containing up to 4 hetType: GrantFiled: May 2, 2002Date of Patent: October 7, 2008Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
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Patent number: 7432264Abstract: Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain.Type: GrantFiled: August 9, 2004Date of Patent: October 7, 2008Assignee: Isis Pharmaceuticals, Inc.Inventors: Elizabeth Anne Jefferson, Eric E. Swayze, Punit P. Seth, Dale E. Robinson, Jr.
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Publication number: 20080227981Abstract: The present invention relates to charge transport compositions. The invention further relates to electronic devices in which there is at least one active layer comprising such charge transport compositions.Type: ApplicationFiled: May 23, 2008Publication date: September 18, 2008Inventors: Norman Herron, Mark A. Guidry, Daniel David Lecloux, Nora Sabina Radu, Eric Maurice Smith, Ying Wang
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Publication number: 20080227789Abstract: Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 21, 2007Publication date: September 18, 2008Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland
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Publication number: 20080227787Abstract: There is provided a use of a compound of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description, and pharmaceutically-acceptable salts thereof, for the manufacture of a medicament for the treatment of a disease in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: March 2, 2005Publication date: September 18, 2008Inventors: Kristofer Olofsson, Benjamin Pelcman, Peter Nilsson, Anders Hallberg, Wesley Schaal
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Publication number: 20080210907Abstract: An ionic organic compound having a repeating unit of formula (I) can be synthesized easily from a readily available organic compound through a small number of reaction steps, can be produced without any purification technique such as chromatography, and can be used in a quite small amount for gelation of water or an ionic liquid without any other auxiliary solvent: [-(A-B-C)n-]•m(X) ??(I) wherein A represents a group having a quaternary ammonium cation which is formed from a heterocyclic compound having at least one nitrogen atom; B represents a functional group, which may have a substituent, selected from amide, urea, urethane and peptide groups; C represents a divalent hydrocarbon group, which may have a substituent, capable of linking between A and B; X represents an anion; n represents the number of repeating units; m represents the total number of anions; and n and m are the same integer.Type: ApplicationFiled: January 30, 2006Publication date: September 4, 2008Applicant: NAATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGYInventors: Masaru Yoshida, Nagatoshi Koumura, Nobuyuki Tamaoki, Hajime Kawanami, Hajime Matsumoto, Said Kazaoui, Nobutsugu Minami
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Publication number: 20080214455Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.Type: ApplicationFiled: May 3, 2006Publication date: September 4, 2008Inventors: Kevin Duffy, Deping Chai, Mirela Colon, Duke M. Fitch, Sarah Rae King, Antony N. Shaw, Rosanna Tedesco, Kenneth Wiggall, Michael N. Zimmerman, Neil W. Johnson, Jiri Kasparec
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Publication number: 20080207616Abstract: The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.Type: ApplicationFiled: October 13, 2005Publication date: August 28, 2008Applicant: AstraZeneca ABInventors: Brian Aquila, Les Dakin, Tracy Deegan, Stephanos Ioannidis, Stephen Lee, Paul Lyne, Timothy Pontz, Mei Su
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Patent number: 7417041Abstract: Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.Type: GrantFiled: February 20, 2004Date of Patent: August 26, 2008Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Laura C. Blumberg, Michael J. Munchhof, Andrei Shavnya