Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/447)
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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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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: 20120022116Abstract: Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject.Type: ApplicationFiled: July 13, 2011Publication date: January 26, 2012Inventors: Huayun Deng, Ye Fang, Mingqian He, Haibei Hu, Weijun Niu, Haiyan Sun
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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: 8063100Abstract: A process for the industrial synthesis of strontium ranelate of formula (I): and its hydrates.Type: GrantFiled: September 24, 2008Date of Patent: November 22, 2011Assignee: Les Laboratoires ServierInventors: Lucile Vaysse-Ludot, Jean-Pierre Lecouve, Pascal Langlois
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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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Patent number: 8048882Abstract: The invention relates to novel pharmaceutical combinations with improved sodium channel blocking effect. Further, the invention relates to the use of said pharmaceutical combinations in chronic pain, in disturbances of the motor system, in epilepsy, as well as in other therapeutic fields where the use of sodium channel blockers is acceptable.Type: GrantFiled: December 18, 2004Date of Patent: November 1, 2011Inventors: Pal Kocsis, Istvan Tarnawa, Marta Than, Karoly Tihanyi, Gyorgy Nemeth
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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: 20110251205Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: June 21, 2011Publication date: October 13, 2011Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20110251206Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: June 21, 2011Publication date: October 13, 2011Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20110245179Abstract: Provided are a composition for preventing or treating heart failure and a method for screening an agent for treating heart failure. The present disclosure demonstrates for the first time that administration of PKC? inhibitor provides inotropic effect by increasing myocardial contractility. Thus, the present disclosure will contribute greatly to the prevention or treatment of heart failure. Also, since the present disclosure is based on the change in calcium sensitivity in cardiac myocytes unlike the existing inotropic agents, it can enhance the myocardial contractility without increasing oxygen demand or the risk of arrhythmia.Type: ApplicationFiled: September 17, 2009Publication date: October 6, 2011Inventors: Woo Jin Park, Jae Gyun Oh
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Publication number: 20110245204Abstract: The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type. The compounds invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: ApplicationFiled: July 12, 2010Publication date: October 6, 2011Inventors: Kevin R. Lynch, Timothy L. MacDonald
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Patent number: 8022079Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: GrantFiled: September 18, 2009Date of Patent: September 20, 2011Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
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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: 20110190310Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: May 14, 2009Publication date: August 4, 2011Inventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
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Patent number: 7985769Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: GrantFiled: January 26, 2005Date of Patent: July 26, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constanin 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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Patent number: 7981925Abstract: 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: GrantFiled: August 26, 2009Date of Patent: July 19, 2011Assignee: 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: 20110166060Abstract: The present invention provides compositions and methods for noninvasive delivery of therapeutic agents across an intact tympanic membrane. For example, the compositions include a penetration enhancer which increases the flux of a therapeutic agent (e.g., antibiotic) across the tympanic membrane. Such compositions are particularly useful in the treatment of otitis media. Additionally, the composition may include a sustained release agents that, in some embodiments form sustained release reservoirs, in situ, once administered to a patient.Type: ApplicationFiled: May 19, 2009Publication date: July 7, 2011Applicants: Massachusettes Institute of Technology, Children's Medical Center CorporationInventors: Emmanuel John Simons, Todd R. Hoare, Daniel S. Kohane, Robert S. Langer
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Patent number: 7968560Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: GrantFiled: September 21, 2009Date of Patent: June 28, 2011Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
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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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Patent number: 7960588Abstract: Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: GrantFiled: March 29, 2010Date of Patent: June 14, 2011Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald
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Publication number: 20110112081Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: July 1, 2009Publication date: May 12, 2011Inventors: Kevin Wilson, Gabriela de Almeida, Andrew Haidle, Kaleen Konrad, Michelle Machacek, Ann Zabierek
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Publication number: 20110092564Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said composition are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).Type: ApplicationFiled: February 26, 2009Publication date: April 21, 2011Inventors: Ernest Puil, Bernard A. Macleod, Richard Wall
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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 -
Patent number: 7897596Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.Type: GrantFiled: November 12, 2007Date of Patent: March 1, 2011Assignee: King Pharmaceuticals Research & Development, Inc.Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
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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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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
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Patent number: 7872041Abstract: The invention relates to the use of rotigotine, its salts and prodrugs, as a medicament for preventing and/or treating Parkinson's plus syndrome.Type: GrantFiled: March 22, 2005Date of Patent: January 18, 2011Assignee: UCB Pharma GmbHInventor: Dieter Scheller
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Publication number: 20100317709Abstract: The invention relates to compounds, in particular 2-amino-3,4,5,-trisubstituted thiophenes, pharmaceutical compositions containing them and the uses of said compounds and compositions for diseases related to sphingosine-1-phosphate (S1P) receptors, predominantly S1P3 receptors. The diseases include cardiovascular diseases, atherosclerosis, cancer, pulmonary oedema, autoimmune disorders and Adult Respiratory Distress Syndrome.Type: ApplicationFiled: November 13, 2008Publication date: December 16, 2010Inventors: Johannes Brussee, Adriaan Pieter Ijzerman, Astrid Eline Alewijnse, Stephan Leonard Maria Peters, Margot Wilhelmia Beukers
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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: 20100280069Abstract: The present invention relates to a method of delivering local anesthetic after dental extraction surgery. The present invention relates to packing the tooth socket with a tinned release local anesthetic which is coordinated with an initial local anesthetic and which lasts up to 5 days. The socket can be surgically sealed or the implant can act as the sealing means.Type: ApplicationFiled: December 22, 2008Publication date: November 4, 2010Inventor: Khashayar Kevin Neshat
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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: 20100267690Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Applicant: Piramal Life Sciences LimitedInventors: Bansi LAL, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More, Anil Ghate, Jacqueline Trivedi, Sapna Parikh
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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: 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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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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Patent number: 7745482Abstract: Alpha crystalline form of strontium ranelate of formula (I): characterised by its powder X-ray diffraction diagram and by a water content of from 22 to 24%. Medicinal products containing the same which are useful in the treatment of osteoporosis and arthrosis.Type: GrantFiled: August 12, 2008Date of Patent: June 29, 2010Assignee: Les Laboratoires ServierInventors: Stephane Horvath, Isabelle Demuynck, Gerard Damien
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Publication number: 20100160371Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: November 17, 2009Publication date: June 24, 2010Inventors: Gerald RANGES, William Scott, Michael Bombara, Deborah Rauner, Aniko Redman, Roger Smith, Holger Paulsen, David Gunn, Jinshan Chen, Joel Renick
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Publication number: 20100152241Abstract: 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: September 22, 2009Publication date: June 17, 2010Applicant: CALCIMEDICA, INC.Inventor: Jeffrey P. Whitten
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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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Patent number: 7732484Abstract: Disclosed is the use of selective adenosine A1 allosteric enhancers to induce angiogenesis at a desired location for treating conditions in which increased angiogenesis is desired, such as stroke, heart disease and peripheral vascular disease.Type: GrantFiled: August 1, 2001Date of Patent: June 8, 2010Assignee: University of Virginia Patent FoundationInventors: Joel Linden, Amy L. Tucker, Richard Price, Rebecca Youkey
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Publication number: 20100125071Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.Type: ApplicationFiled: June 4, 2008Publication date: May 20, 2010Inventors: Neil John Press, Simon James Watson