Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 548/953)
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Patent number: 8299053Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.Type: GrantFiled: March 4, 2009Date of Patent: October 30, 2012Assignees: RadioRx, Inc., Alliant Techsystems Inc.Inventors: Mark D. Bednarski, Lynn M. Oehler, legal representative, Susan Knox, Louis Cannizzo, Kirstin Warner, Robert Wardle, Stephen Velarde, Shoucheng Ning
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Publication number: 20120252776Abstract: Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula: wherein the variables are 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 the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.Type: ApplicationFiled: March 12, 2012Publication date: October 4, 2012Inventors: Eric Anderson, Christopher F. Bender, Xiaofeng Liu, Xin Jiang, Melean Visnick
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Publication number: 20120245137Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity, are disclosed. Specifically, a series of compounds containing aryl sulphone derivatives, as exemplified by Formula (I).Type: ApplicationFiled: September 17, 2010Publication date: September 27, 2012Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan A. Pajouhesh, Robert Galemmo, JR., Richard Holland, Yuanxi Zhou, Yongbao Zhu, Eric Simonson, Navjot Chahal, Mike Grimwood
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Patent number: 8273902Abstract: A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula: wherein X1 represents a halogen atom, is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.Type: GrantFiled: January 6, 2011Date of Patent: September 25, 2012Assignee: Toyama Chemical Co., Ltd.Inventors: Akihito Saitoh, Yoshiaki Suzuki, Kenji Yonezawa, Mitsuhide Kawamura, Takahiko Kusanagi, Takashi Nakai
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Publication number: 20120228151Abstract: An extraction component enabling the concurrent recovery of gold and/or palladium selectively from a hydrochloric acid media containing the base metals and other contaminants. The disclosed extractant disclosed eliminates the conventional multi-step process for such extraction by providing for an extraction method which uses a single solvent extraction reagent. Further enhancing the conventional multi step process, the conventional scrubbing stage is eliminated by a single stripping stage. The resulting solutions can be obtained from leaching many types of material such as copper anode slimes, the treatment of scrap such as electronic circuit boards and plating effluents, PGM, or refractory gold ores.Type: ApplicationFiled: March 7, 2011Publication date: September 13, 2012Inventors: Loghman Moradi, Hiwa Salimi, Mohammad Piltan, Issa Yavari
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Publication number: 20120232053Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: May 17, 2012Publication date: September 13, 2012Applicant: THERAVANCE, INC.Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
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Publication number: 20120220564Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).Type: ApplicationFiled: September 17, 2010Publication date: August 30, 2012Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
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Patent number: 8236792Abstract: Certain substituted pyrrolidine amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: GrantFiled: May 19, 2009Date of Patent: August 7, 2012Assignee: Janssen Pharmaceutica NVInventors: Nicholas I Carruthers, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, Daniel J. Pippel, Chandravadan R. Shah, Akinola Soyode-Johnson, Emily M. Stocking, Lana Young
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Patent number: 8232269Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally substituType: GrantFiled: September 17, 2009Date of Patent: July 31, 2012Assignee: Pfizer Inc.Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
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Publication number: 20120190649Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: August 5, 2010Publication date: July 26, 2012Applicant: BIOGEN IDEC MA INC.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Publication number: 20120178732Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 6, 2011Publication date: July 12, 2012Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20120171116Abstract: The present invention includes arginase enzyme inhibitors, compositions comprising these arginase inhibitors, and methods of treating or diagnosing conditions characterized either by abnormally high arginase activity or abnormally low nitric oxide levels in a mammal, comprising administering compositions of the invention to the mammal.Type: ApplicationFiled: July 26, 2011Publication date: July 5, 2012Inventors: Bruce Edward Tomczuk, Gary Lee Olson, Richard Scott Pottorf, Jane Wang, Bhaskara Rao Nallaganchu
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Patent number: 8207355Abstract: This invention discloses and claims an industrial method for the production of azetidine derivatives, such as, N-(1-benzhydrylazetidin-3-yl)-N-phenylmethylsulphonamide.Type: GrantFiled: June 14, 2010Date of Patent: June 26, 2012Assignee: Sanofi-AventisInventors: Antony Bigot, Philippe Boffelli, Maxime Lampilas, Pascale Marolleau, Alain Medard, Gilles Oddon, Daniel Varraillon
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Patent number: 8207155Abstract: In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: March 31, 2010Date of Patent: June 26, 2012Assignee: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Publication number: 20120149860Abstract: A compound represented by the following formula (a): CH2?CR1—CONJ-CKR2—(CH2)n—COO-Q1-Rf1??(a) is provided. This compound is capable of forming a polymer having an oil repellency equivalent to polymers containing a polyfluoroalkyl group containing at least 8 carbon atoms, although the polyfluoroalkyl group contains up to 6 carbon atoms. In the formula, R1 is hydrogen atom or methyl group, R2 is hydrogen atom or a group represented by —(CH2)m—COO-Q2-Rf2 (r), n and m are independently an integer of 0 to 4, Rf1 and Rf2 are independently a polyfluoroalkyl group or a polyfluoroether group containing 1 to 6 carbon atoms, Q1 and Q2 are independently single bond or a divalent linkage group, J is hydrogen atom or an alkyl group containing 1 to 3 carbon atoms, K is hydrogen atom or an alkyl group containing 1 to 3 carbon atoms, and j and k are independently single bond or an alkylene group containing 1 to 3 carbon atoms with the proviso that j and k are not simultaneously single bond.Type: ApplicationFiled: August 17, 2010Publication date: June 14, 2012Applicant: AGC SEIMI CHEMICAL CO.,LTD.Inventors: Fusae Ishiwata, Ryo Hirabayashi, Hirotaka Shimizu
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Publication number: 20120142661Abstract: The present invention relates to novel oxime azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: November 21, 2011Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin IM
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Publication number: 20120142666Abstract: Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: June 8, 2010Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
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Publication number: 20120142662Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: November 28, 2011Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Santosh C. SINHA, Smita S. BHAT, Evelyn G. CORPUZ, Ken CHOW, Wenkui K. FANG, Wha-Bin IM
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Patent number: 8188090Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q and R1-R3 are defined in the detailed description and claims. The invention is also concerned with the compounds of formula Z: and pharmaceutically acceptable salts and esters thereof, wherein R1-R3 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I and Z as well as pharmaceutical compositions containing such compounds. The compounds of formula I and Z are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: GrantFiled: November 9, 2009Date of Patent: May 29, 2012Assignee: Hoffman-La Roche Inc.Inventors: Fariborz Firooznia, Tai-An Lin, Sung-Sau So, Baoxia Wang, HongYing Yun
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Publication number: 20120129828Abstract: The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.Type: ApplicationFiled: June 18, 2009Publication date: May 24, 2012Inventors: Victor J. Cee, Jian Lin, Xiang Y. Yu, Zhaoda Zhang
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Patent number: 8178698Abstract: The present invention provides cyclic nitro compounds, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.Type: GrantFiled: May 26, 2010Date of Patent: May 15, 2012Assignee: Alliant Techsystems Inc.Inventors: Louis F. Cannizzo, Kirstin F. Warner, Robert B. Wardle, Stephen P. Velarde
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Publication number: 20120115840Abstract: This invention relates to a hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.Type: ApplicationFiled: December 16, 2009Publication date: May 10, 2012Inventors: Lech Ciszewski, Marilyn De La Cruz, Piotr H. Karpinski, Michael Mutz, Christian Riegert, Caspar Vogel, Ricardo Schneeberger
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Publication number: 20120115819Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.Type: ApplicationFiled: May 13, 2010Publication date: May 10, 2012Inventors: Roger B. Clark, Diana Katharine Hunt, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus P. Rönn
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Publication number: 20120115841Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: ApplicationFiled: May 17, 2010Publication date: May 10, 2012Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Patent number: 8173634Abstract: This invention relates to a novel crystalline form (Form A) of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this crystalline form, to processes for forming it and to its use in medical treatment.Type: GrantFiled: December 17, 2009Date of Patent: May 8, 2012Assignee: Novartis AGInventors: Yugang Liu, Dimitris Papoutsakis, Elizabeth Roddy
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Publication number: 20120101080Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.Type: ApplicationFiled: June 25, 2010Publication date: April 26, 2012Applicant: BioVersys AGInventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
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Publication number: 20120094973Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.Type: ApplicationFiled: December 21, 2011Publication date: April 19, 2012Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Yueh-Hsiung Kuo, Ming-Jai Su
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Publication number: 20120088749Abstract: The present invention relates to amides that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: ApplicationFiled: December 16, 2011Publication date: April 12, 2012Applicants: EPIX PHARMACEUTICALS, INC., AMGEN, INC.Inventors: Susana C. Neira, Xiang Yu, Roland Burli, Victor Cee, Brian Lanman
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Publication number: 20120064060Abstract: Provided are: a compound represented by formula (I): (wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocylic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, and when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt, an N-oxide form, a solvate, or a prodrug thereof; and a medicament which includes those. The compound of formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Shinji NAKADE
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Publication number: 20120058986Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.Type: ApplicationFiled: September 2, 2011Publication date: March 8, 2012Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
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Publication number: 20120040960Abstract: The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: October 25, 2011Publication date: February 16, 2012Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui
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Publication number: 20120035149Abstract: Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes.Type: ApplicationFiled: December 16, 2009Publication date: February 9, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Qun-Yong Zhou, Jia-Da Li, Qi Huang
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Publication number: 20120028937Abstract: Provided is a compound useful as a therapeutic drug for pain and inflammation caused by various pathological conditions such as neuropathic pain and rheumatoid arthritis. The compound of the formula (I) or a salt thereof [wherein R1 is a methyl group or a hydrogen atom, R2 represents a hydrogen atom, an alkyl group, an alkylcarbonyl group or an aryl carbonyl group, A represents a cycloalkyl group, a cycloalkenyl group, an aryl group or a heteroaryl group (each group may be substituted with a substituent selected from the group consisting of alkyl, alkenyl, cycloalkyl and halogen), n and m each represent an integer of 1, 2 or 3, and p represents an integer of 0, 1, 2 or 3].Type: ApplicationFiled: May 7, 2009Publication date: February 2, 2012Inventors: Yasunori Tsuzuki, Toshiya Morie, Takanori Nakamura, Isao Shimizu, Masanori Miyauchi
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Publication number: 20120028249Abstract: Disclosed are near IR emitting fluorescent compounds; methods of making and kits containing the described compounds; and their use in fluorescence-based detection of biological materials.Type: ApplicationFiled: October 20, 2009Publication date: February 2, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Stephen Yue, Shih-Jung Huang, Jolene Bradford
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Patent number: 8106191Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.Type: GrantFiled: June 13, 2003Date of Patent: January 31, 2012Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Publication number: 20120022263Abstract: The present invention herein provides a 3-aminooxalylaminobenzamide derivative which is used as an insecticide or miticide. The 3-aminooxalylaminobenzamide derivative is one represented by the following general formula [1]: (R1 and R2 each represent, for instance, a C1 to C3 alkoxy group or a C1 to C3 haloalkoxy group; R3 and R4 each represent, for instance, a C1 to C8 alkyl group or a C1 to C8 haloalkyl group; R5 represents, for instance, a C1 to C5 haloalkyl group; R6 and R7 each represent, for instance, a hydrogen atom or a C1 to C5 alkyl group; Y represents, for instance, a hydrogen atom or a halogen atom; Z represents, for instance, a hydrogen atom; n is an integer ranging from 0 to 4 and m is an integer ranging from 0 to 2).Type: ApplicationFiled: February 5, 2010Publication date: January 26, 2012Applicant: AGRO-KANESHO Co., Ltd.Inventors: Shuichi Usui, Toshiki Fukuchi, Sachiko Kinoshita
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Patent number: 8093252Abstract: A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, processes for making it and its use as an activator of glucokinase are described.Type: GrantFiled: February 15, 2010Date of Patent: January 10, 2012Assignee: AstraZeneca ABInventors: Sharon Ann Bowden, David Peter Hoile, Karin Lövqvist
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Publication number: 20110311466Abstract: 4-(azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.Type: ApplicationFiled: December 2, 2009Publication date: December 22, 2011Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Jean-Guy Boiteau, Karine Bouquet, Sandrine Talano, Corinne Millois Barbuis
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Publication number: 20110311593Abstract: The invention relates to N-hydroxylated amidines, guanidines and aminohydrazones for application on the skin. In particular, the invention relates to transdermal therapeutic systems containing N-hydroxylated amidines, guanidines and aminohydrazones as a prodrug, and to methods for producing and using such systems.Type: ApplicationFiled: February 5, 2010Publication date: December 22, 2011Inventors: Rudolf Matusch, Hans-Rainer Hoffmann, Bodo Asmussen, Andreas Koch
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Patent number: 8080542Abstract: The present invention relates to amides that have activity as SIP receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: GrantFiled: September 19, 2008Date of Patent: December 20, 2011Assignees: Amgen, Inc., Epix Pharmaceuticals, Inc.Inventors: Susana C. Neira, Xiang Yu, Roland Burli, Victor Cee, Brian Lanman
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Patent number: 8080541Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.Type: GrantFiled: August 19, 2010Date of Patent: December 20, 2011Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard
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Patent number: 8076481Abstract: A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R1, n, m, R3, R6, X1, X2, X3 and X4 are as defined in the specification, is described. Novel intermediates are also described and claimed.Type: GrantFiled: February 15, 2010Date of Patent: December 13, 2011Assignee: AstraZeneca ABInventors: Michael Butters, Jeffrey Crabb, Philip Hopes, Bharti Patel
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Publication number: 20110269736Abstract: The present invention relates to compounds defined by formula (I) wherein the group R is 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.Type: ApplicationFiled: July 24, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
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Publication number: 20110263558Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.Type: ApplicationFiled: March 15, 2011Publication date: October 27, 2011Applicant: EXELIXIS, INC.Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
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Publication number: 20110257150Abstract: This invention relates to a hydrochloride, malate, oxalate and tartrate salt forms of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of each of these salts, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.Type: ApplicationFiled: December 17, 2009Publication date: October 20, 2011Inventors: Marilyn De La Cruz, Piotr H. Karpinski, Yugang Liu
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Publication number: 20110251170Abstract: This invention relates to a novel crystalline form (Form A) of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this crystalline form, to processes for forming it and to its use in medical treatment.Type: ApplicationFiled: December 17, 2009Publication date: October 13, 2011Inventors: Yugang Liu, Dimitris Papoutsakis, Elizabeth Roddy
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Publication number: 20110251379Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.Type: ApplicationFiled: March 3, 2011Publication date: October 13, 2011Applicant: Satori Pharmaceuticals, Inc.Inventors: Brian Scott Bronk, Wesley Francis Austin, Steffen Phillip Creaser, Mark A. Findeis, Nathan Oliver Fuller, Jed Lee Hubbs, Jeffrey Lee Ives, Ruichao Shen
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Publication number: 20110230463Abstract: [Object] Provided is a compound which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient for an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells. [Means for Solution] According to the present invention, a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient of an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells can be provided. The 2H-chromene compound and a derivative thereof which are the compounds of the present invention have an S1P1 agonist action, and can be used particularly for prevention and/or treatment of a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.Type: ApplicationFiled: December 4, 2009Publication date: September 22, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Sunao Imada, Tatsuaki Morokata
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Patent number: 8012955Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: December 21, 2007Date of Patent: September 6, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
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Patent number: RE43676Abstract: An alkyl ether represented by the general formula: or its salt. This compound has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.Type: GrantFiled: October 18, 2002Date of Patent: September 18, 2012Assignee: Toyama Chemical Co., Ltd.Inventors: Akihito Saitoh, Noboru Iwakami, Tamotsu Takamatsu