Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Nitrogen Patents (Class 549/69)
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Publication number: 20120035251Abstract: The invention provides a compound which is (a) a thiophene carboxamide derivative of formula (IA) or (IB), or a tautomer thereof; or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof, wherein L1, A1 and W are as defined herein. The compounds are useful as IKK? inhibitors. The compounds can thus be used in medicine, for example in the treatment of autoimmune and inflammatory diseases.Type: ApplicationFiled: April 20, 2010Publication date: February 9, 2012Applicant: CHROMA THERAPEUTICS LD.Inventors: Alan Hastings Drummond, Richard James Testar
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Publication number: 20120028977Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.Type: ApplicationFiled: January 28, 2010Publication date: February 2, 2012Applicant: EMORY UNIVERSITYInventors: Stephen F. Traynelis, Dennis C. Liotta, Rose M. Santangelo, Ethel C. Garnier
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Patent number: 8106091Abstract: Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- whereiType: GrantFiled: October 29, 2007Date of Patent: January 31, 2012Assignee: Chroma Therapeutics Ltd.Inventors: David Charles Festus Moffat, Stephen John Davies, Michael Hugh Charlton, Simon Christopher Hirst, Stuart Thomas Onions, Jonathon Gareth Williams
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Publication number: 20120010187Abstract: The invention provides FIG. 1 novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: March 16, 2010Publication date: January 12, 2012Applicant: University of Virginia Patent FoundationInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, JR.
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Patent number: 8071790Abstract: Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.Type: GrantFiled: September 1, 2009Date of Patent: December 6, 2011Assignee: Los Alamos National Security, LLCInventors: Rashi Iyer, Kumkum Ganguly, Louis A. Silks
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Patent number: 8053435Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.Type: GrantFiled: November 1, 2007Date of Patent: November 8, 2011Assignees: Korea Research Institute of Chemical Technology, Crystalgenomics, Inc.Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee, Dongkyu Shin
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Publication number: 20110251216Abstract: The present invention relates to therapeutic targets for cancer. In particular, the present invention relates to small molecules and nucleic acids that target EZH2 expression in cancer (e.g., prostate cancer, breast cancer, other solid tumors, multiple myeloma).Type: ApplicationFiled: February 10, 2011Publication date: October 13, 2011Applicant: The Regents of The University of MichiganInventors: Arul M. Chinnaiyan, Sooryanaryana Lnu, Qi Cao
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Publication number: 20110213157Abstract: A compound represented by the following general formula (I): [wherein R1 represents hydrogen atom or a C1-6 alkyl group, A and B represent —(CH2)2—, —(CH2)3— or —(CH2)4—, X represents —N(R2)—CO— (R2 represents hydrogen atom or a C1-6 alkyl group), —CO—N(R3)— (R3 represents hydrogen atom or a C1-6 alkyl group), —C(R4)?C(R5)— (R4 and R5 represent hydrogen atom or a C1-6 alkyl group), or —N(R6)—SO2— (R6 represents hydrogen atom or a C1-6 alkyl group), and Ar represents an aryldiyl group or a heteroaryldiyl group], which has a retinoid action and is useful as an active ingredient of a medicament.Type: ApplicationFiled: August 14, 2008Publication date: September 1, 2011Applicant: RESEARCH FOUNDATION ITSUU LABORATORYInventors: Yohei Amano, Masayuki Noguchi, Koichi Shudo
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Publication number: 20110212970Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: March 17, 2011Publication date: September 1, 2011Applicant: CALCIMEDICA, INC.Inventors: GONUL VELICELEBI, KENNETH A. STAUDERMAN, JEFFREY P. WHITTEN, YAZHONG PEI, JIANGUO CAO, ZHIJUN WANG, EVAN ROGERS, BRIAN DYCK, JONATHAN GREY
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Patent number: 8003685Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: GrantFiled: November 15, 2007Date of Patent: August 23, 2011Assignee: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson, Constantin G. Yannopoulos, Guy Falardeau, Louis Vaillancourt, Réal Denis
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Publication number: 20110200553Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: April 7, 2011Publication date: August 18, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammed Arshad Siddiqui, Wuyi Wang, Constanin G. Yannopoulos
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Publication number: 20110178129Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: January 14, 2011Publication date: July 21, 2011Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Michael O' Neil Hanrahan Clarke, Scott E. Lazerwith, Willard Lew, Philip Anthony Morganelli, William J. Watkins
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Publication number: 20110152234Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 23, 2010Publication date: June 23, 2011Inventors: Alan Faull, Craig Johnstone, Andrew Morley, Jeffrey Philip Poyser
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Publication number: 20110105564Abstract: Novel thienylpyridylcarboxamides of the formula (I) The present application is also directed to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: December 5, 2006Publication date: May 5, 2011Applicant: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Benoit Hartmann, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
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Publication number: 20110086818Abstract: The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.Type: ApplicationFiled: March 11, 2009Publication date: April 14, 2011Applicants: Presidents and Fellows of Harvard College, The General Hospital CorporationInventors: Bruce P. Bean, Clifford J. Woolf
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Publication number: 20110077244Abstract: The present invention relates to synthetic studies of a novel thiophenediamine derivative having a urea structure and to finding pharmaceutical actions thereof. The present invention provides a compound represented by the following general formula (1) or a salt thereof. In the formula (1), R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, etc. R3 represents a hydroxy group, a lower alkoxy group which may have a substituent, a lower cycloalkyloxy group which may have a substituent, etc. R4 and R5 are the same or different and represent a halogen atom, a lower alkyl group, a hydroxy group, etc. X represents a lower alkylene group which may have a substituent, etc. Y represents a single bond or a lower alkylene group which may have a substituent, etc. W1-W2 represents N—CH, CH—N, etc. and l and m are the same or different and represent 0, 1, etc.Type: ApplicationFiled: May 25, 2009Publication date: March 31, 2011Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyaki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe
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Publication number: 20110065724Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: September 15, 2010Publication date: March 17, 2011Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers
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Publication number: 20110065782Abstract: The present invention relates to methods of identifying compounds that inhibit the activation between a biomolecule, pharmaceutical compositions comprising such compounds, and methods of treating and/or to reducing the risk of Bacillus anthracis and Bordetella pertussis infection by administering such pharmaceutical compositions.Type: ApplicationFiled: September 15, 2009Publication date: March 17, 2011Inventors: Thérèse Malliavin, Elodie Laine, Arnaud Blondel, Daniel Ladant, Johanna Karst, Sylvain Rault, Aurélien Lesnard
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MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20110053958Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: March 17, 2009Publication date: March 3, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou -
Publication number: 20110046210Abstract: Compounds of formula (IA) or (IB) are IKK inhibitors useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; A is an optionally substituted aryl or heteroaryl of 5-13 ring atoms; Z is a radical of formula R1C(R2)(R3)NH—Y-L1-X1-(CH2)z— wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 independently represent the side chain of a natural or non-natural alpha amino acid but neither of R2 and R3 is hydrogen, or R2 and R3 taken together with the carbon atom to which they are attached form a C3-C7 cycloalkyl ring, and z, Y, L1 and X1 are as defined in the claims.Type: ApplicationFiled: April 23, 2009Publication date: February 24, 2011Applicant: CHROMA THERAPEUTICS LTD.Inventors: David Festus Charles Moffat, Stephen John Davies
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Publication number: 20110039920Abstract: Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5(carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl(25,4E)-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and tert-Butyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKK? activity.Type: ApplicationFiled: April 23, 2008Publication date: February 17, 2011Applicant: CHROMA THERAPEUTICS LTD.Inventors: David Festus Charles Moffat, Stephen John Davies, Michael Hugh Charlton, Simon Christopher Hirst, Jonathon Gareth Williams, Stuart Thomas Onions
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Patent number: 7880020Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psorias.Type: GrantFiled: June 3, 2009Date of Patent: February 1, 2011Assignee: Topotarget UK LimitedInventors: Clare J Watkins, Maria Rosario Romero-Martin, Kathryn G Moore, James Ritchie, Paul W Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma M Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Semenikhina, Andris Amolins, C. John Harris, James E S Duffy
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Publication number: 20100305200Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: December 10, 2008Publication date: December 2, 2010Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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Publication number: 20100292229Abstract: The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. In general aspects, compounds of the present invention are tyrphostin-like in structure. Compounds of the present invention, in certain embodiments, display significant potency by causing, for example, inhibition of Stat3 activation, reduction in c-myc protein levels and/or induction of apoptosis in tumor cells. In general aspects, compounds of the present invention induce one or more of these activities at nanomolar concentrations and typically function through a unique mechanism involving the induction of stress granules that bind specific signaling molecules and prevent them from participating in signal transduction and oncogenesis.Type: ApplicationFiled: July 2, 2007Publication date: November 18, 2010Applicant: The Board of Regents of the University of Texas SystemInventors: Nicholas J Donato, David Maxwell, Moshe Talpaz, William Bornmann, Zhenghong PENG, Ashutosh Pal, Dongmei Han, Shimei Wang, Geoffrey Bartholomeusz, Vaibhav Kapuria
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100261725Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 26, 2009Publication date: October 14, 2010Applicant: CALCIMEDICA, INC.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20100240677Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: ApplicationFiled: January 26, 2010Publication date: September 23, 2010Applicant: AVENTIS PHARMA LIMITEDInventors: Garry FENTON, Tahir Nadeem MAJID, Malcolm Norman PALFREYMAN
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Publication number: 20100240720Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, for the targeted delivery of chemotherapeutic agents.Type: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Patent number: 7795456Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: GrantFiled: November 11, 2009Date of Patent: September 14, 2010Assignee: Dow AgroSciences LLCInventors: Yuanming Zhu, Richard B. Rogers, Jim X. Huang
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Patent number: 7741479Abstract: The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.Type: GrantFiled: December 7, 2005Date of Patent: June 22, 2010Assignee: Locus Pharmaceuticals, Inc.Inventors: Enrique Luis Michelotti, Eric Bruce Springman, Duyan Nguyen, Rupa S. Shetty, Younghee Lee, Kristofer Kent Moffett, Jennifer Lee Ludington, Ted Tsutomis Fujimoto, Zenon D. Konteatis, Bin Liu, Frank Hollinger, Bruce D. Dorsey
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Patent number: 7732452Abstract: The invention is concerned with novel substituted thiophene derivatives of formula (I) wherein R1 to R8, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used as medicaments.Type: GrantFiled: December 13, 2006Date of Patent: June 8, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Uwe Grether, Nicole A. Kratochwil, Robert Narquizian, Constantinos G. Panousis
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Publication number: 20100137347Abstract: Disclosed herein is a compound of the formula (I). Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.Type: ApplicationFiled: January 21, 2008Publication date: June 3, 2010Applicant: ALLERGAN, INC.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20100087515Abstract: Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— wherein: z is 0 or 1; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O)—, —S(?P)2-, —C(?O)O—, —C(?O)NR3-, —C(?S)—NR3, —C(?NH)—NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent linker radical of formula -(Alk1)m(Q)(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.Type: ApplicationFiled: October 29, 2007Publication date: April 8, 2010Applicant: Chroma Terapeutics LtdInventors: David Festus Charles Moffat, Stephen John Davies, Michael Hugh Charlton, Simon Christopher Hirst, Stuart Thomas Onions, Jonathan Gareth Williams
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Publication number: 20100069473Abstract: Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- whereinType: ApplicationFiled: October 29, 2007Publication date: March 18, 2010Applicant: CHROMA THERAPEUTICS LTD.Inventors: David Festus Charles Moffat, Stephen John Davies, Michael Hugh Charlton, Simon Christopher Hirst, Stuart Thomas Onions, Jonathon Gareth Williams
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Publication number: 20100063065Abstract: The invention discloses compounds of formula (I); wherein: R is a carboxylic acid or a derivative thereof; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylthio, halo or trihalomethyl; R2 is aryl, heteroaryl, arylalkyl or heteroarylalkyl; R3 is H or F; and L is a linking group comprising a chain of from 2 to 8 atoms linking R and the carbonyl group (A); and pharmaceutically acceptable derivatives thereof, useful for treating disorders mediated by peroxisome-proliferator-activated receptor (PPAR) subtype ? (PPAR?). The compounds of the invention are therefore useful in the treatment of metabolic syndrome, obesity, type-II diabetes, dyslipidemia, wound healing, inflammation, neurodegenerative disorders and multiple sclerosis.Type: ApplicationFiled: September 28, 2006Publication date: March 11, 2010Applicant: Inpharmatica LimitedInventors: Andrew Ayscough, David Rodyney Owen, Paul Meo, David James Pearson, Yvonne Walker, Richard Justin Boyce, Fabio Zuccotto
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Publication number: 20100063136Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: ApplicationFiled: November 11, 2009Publication date: March 11, 2010Applicant: DOW AGROSCIENCES LLCInventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang
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Publication number: 20100063088Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: November 17, 2009Publication date: March 11, 2010Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Publication number: 20100029754Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 7, 2009Publication date: February 4, 2010Applicant: ASTRAZENECA ABInventors: Alan Wellington Faull, Craig Johnstone, Andrew David Morley, Jeffrey Philip Poyser
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Publication number: 20100022525Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: October 4, 2007Publication date: January 28, 2010Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
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Publication number: 20090215829Abstract: The invention relates to thiophene carboxamides of formula (I), wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: May 4, 2009Publication date: August 27, 2009Inventors: Andrew David Morley, Jeffrey Philip POYSER
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Patent number: 7579346Abstract: Novel compounds of the formula (I), in which D, W, X, Y, T, m and R1 have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: GrantFiled: October 30, 2003Date of Patent: August 25, 2009Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Hanns Wurziger, Johannes Gleitz, Christoph van Amsterdam
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Patent number: 7572826Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: January 13, 2004Date of Patent: August 11, 2009Assignee: AstraZeneca ABInventors: Alan Wellington Faull, Craig Johnstone, Andrew David Morley, Jeffrey Philip Poyser
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Publication number: 20090192175Abstract: Novel heteroaromatic compounds of formula (I): wherein A1, A2, A3, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: April 25, 2007Publication date: July 30, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Pierre Jung, Patricia Durieux, William Lutz, Peter Maienfisch, Thomas Pitterna, Peter Renold, Werner Zambach
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Publication number: 20090181962Abstract: The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2, and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 3, 2007Publication date: July 16, 2009Inventors: Andrew Baxter, Stephen Brough, Alan Faull, Craig Johnstone, Thomas Mcinally
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Publication number: 20090170891Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: April 6, 2007Publication date: July 2, 2009Inventors: Steven L. Colletti, James R. Tata, Weichun Chen, Richard T. Beresis, Fa-Xiang Ding, Darby Rye Schmidt, Hong Shen, Subharekha Raghavan
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Patent number: 7553868Abstract: The invention relates to thiophene carboxamides of formula (I) wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: January 13, 2004Date of Patent: June 30, 2009Assignee: AstraZeneca ABInventors: Andrew David Morley, Jeffrey Philip Poyser
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Publication number: 20090137659Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 15, 2008Publication date: May 28, 2009Applicant: CALCIMEDICA, INC.Inventors: Gonul VELICELEBI, Kenneth A. STAUDERMAN, David P.M. PLEYNET, Song CHENG, Jeffrey P. WHITTEN
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Publication number: 20090054396Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.Type: ApplicationFiled: September 8, 2008Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Susan Ashwell, Thomas Gero, Stephanos Ioannidis, James Janetka, Paul Lyne, Vibha Oza, Mei Su, Dingwei Yu, Stephanie Springer
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Publication number: 20090041747Abstract: The invention relates to novel compounds with formula (I) and their use in stabilization of Factor VIIa or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof.Type: ApplicationFiled: February 24, 2006Publication date: February 12, 2009Applicant: NOVO NORDISK HEALTH CARE AGInventors: Anders Klarskov Petersen, Andrew Neil Bowler
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Publication number: 20080299080Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: November 15, 2007Publication date: December 4, 2008Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson, Constantin G. Yannopoulos, Guy Falardeau, Louis Vaillancourt, Real Denis