C=x Bonded Directly To The Nitrogen Which Is Bonded Directly To The Thiazole Ring (x Is Chalcogen) Patents (Class 514/371)
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Publication number: 20090036467Abstract: A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus.Type: ApplicationFiled: August 1, 2008Publication date: February 5, 2009Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20090029997Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: January 22, 2007Publication date: January 29, 2009Applicant: LABORATOIRES SERONO SAInventors: Anna Quattropani, Vincent Pomel, Thomas Rueckle, Tania Grippi-Vallotton
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Publication number: 20090029998Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: January 11, 2005Publication date: January 29, 2009Applicant: APPLIED RESEARCH SYSTEM ARS HOLDING N.V.Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
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Publication number: 20090005391Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: ApplicationFiled: November 3, 2006Publication date: January 1, 2009Inventors: Matthew Colin Thor Fyfe, Martin James Procter
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Publication number: 20080319033Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and X have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: December 13, 2006Publication date: December 25, 2008Inventors: Emma Budd, Julia Doris Ida Hatto, Judy Fox Hayler, Darren Mark Legrand, Barbara Valade
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Publication number: 20080319028Abstract: This invention relates to dicycloalkylcarbamoyl ureas of formula (I), which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: ApplicationFiled: July 7, 2006Publication date: December 25, 2008Applicant: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Per Vedso, Lone Jeppesen, Marit Kristiansen
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Publication number: 20080312237Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: July 18, 2008Publication date: December 18, 2008Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
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Publication number: 20080312207Abstract: Compounds of Formula (I) wherein: R1 is methyl; R2 is selected from —C (O) NR4R5, SO2NR4R5, S (O) pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C) alkyl and HET-2; R5 is hydrogen or (1-4C) alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described.Type: ApplicationFiled: February 15, 2005Publication date: December 18, 2008Inventors: Craig Johnstone, Darren McKerrecher, Kurt Gordon Pike
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Publication number: 20080312291Abstract: The present invention relates to novel thiazole and oxazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein X1 and X2 are selected from 0 and N or S and N and R1, R2 and Y are as defined in the description. For example, R1 may be alkyl, alkoxy, thioalkoxy or aryl, R2 may be alkoxy and Y may be a carbonylamino-linked substituent containing an aryl or heteroaryl group.Type: ApplicationFiled: December 21, 2006Publication date: December 18, 2008Inventors: Udo Bauer, Linda Gustafsson, Maria Saxin, Tor Svensson
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Publication number: 20080312206Abstract: The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula which possess CSF 1R kinase inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.Type: ApplicationFiled: December 19, 2006Publication date: December 18, 2008Applicant: AstraZeneca ABInventors: Brian Aquila, Donald Cook, Leslie Dakin, Stephanos Ioannidis, Paul Lyne, David Scott, Xiaolan Zheng
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Publication number: 20080306067Abstract: A compound of formula (I), wherein substituents are as given above, useful in the treatment of a disease mediated by the action of CCR3, in particular inflammatory or obstructive airway diseases.Type: ApplicationFiled: October 23, 2006Publication date: December 11, 2008Inventors: Klaus Weigand, Thomas Ullrich, Kate Hoeganauer, Philipp Lehr, Rohan Beckwith
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Publication number: 20080300136Abstract: 2-Acylaminothiazole-4-carboxamides of the formula (I) and application thereof as an insecticide. wherein R1 represents phenyl which may be optionally substituted, or a 5- or 6-membered heterocyclic group containing at least one hetero atom selected from a group consisting of N, O and S which may be optionally substituted, represents halogen, C1-6 alkyl or C1-6 haloalkyl, R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl or C1-6 haloalkylsulfonyl, R4 represents halogen, C1-6 alkyl or C1-6 haloalkyl, and X represents hydrogen, halogen, C1-6 alkyl or C1-6 haloalkyl, and the use of the new compounds as insecticides.Type: ApplicationFiled: October 26, 2006Publication date: December 4, 2008Applicant: Bayer CropScience AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
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Patent number: 7459473Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: GrantFiled: December 3, 1998Date of Patent: December 2, 2008Assignee: Glia Med, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Publication number: 20080293787Abstract: The invention relates to solid dispersions of poorly soluble compounds formed by co-precipitation and hot melt extrusion, resulting in improved stability and bioavailability. The invention also relates to hot melt extrusion processes used to prepare such solid dispersions.Type: ApplicationFiled: May 5, 2008Publication date: November 27, 2008Inventors: Ashish Chatterji, Zedong Dong, Harpreet K. Sandhu, Navnit Hargovindas Shah
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Publication number: 20080293741Abstract: Compounds of Formula (I): (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: ApplicationFiled: March 11, 2006Publication date: November 27, 2008Inventors: Matthew Colin Thor Fyfe, Martin James Procter
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Publication number: 20080287510Abstract: The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, and R4 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: May 15, 2008Publication date: November 20, 2008Applicant: Abbott LaboratoriesInventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Jennifer M. Frost, Sridhar Peddi
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Publication number: 20080280872Abstract: Compounds of Formula (I): wherein: R1 is methoxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described.Type: ApplicationFiled: February 15, 2005Publication date: November 13, 2008Inventors: Craig Johnstone, Darren McKerrecher, Kurt Gordon Pike
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Publication number: 20080280871Abstract: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: August 27, 2004Publication date: November 13, 2008Applicant: NOVARTIS AGInventors: Graham Charles Bloomfield, Ian Bruce, Judy Fox Hayler, Catherine Leblanc, Darren Mark Le Grand, Clive McCarthy
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Patent number: 7442715Abstract: A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a mammal, and the like.Type: GrantFiled: August 17, 2006Date of Patent: October 28, 2008Assignee: Astellas Pharma Inc.Inventors: Akira Nagashima, Takayuki Inoue, Mitsuru Ohkubo, Kousei Yoshihara, Takashi Tojo, Masataka Morita
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Publication number: 20080261952Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2005Publication date: October 23, 2008Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
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Publication number: 20080242709Abstract: 2-Amido-4-isoxazolyl thiazole compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.Type: ApplicationFiled: August 9, 2007Publication date: October 2, 2008Inventors: John K. Dickson, Carl Nicholas Hodge, Ke Chen
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Publication number: 20080234273Abstract: Compounds of formula (I) wherein R1, R2, R3, and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: June 3, 2006Publication date: September 25, 2008Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Patent number: 7427635Abstract: The present invention relates to compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, cognative and CNS disorders and inflammatory/autoimmune diseases.Type: GrantFiled: August 11, 2005Date of Patent: September 23, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Nader Fotouhi, Nicholas J. S. Huby, Norman Kong, Lee Apostle McDermott, John Moliterni, Zhuming Zhang
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Patent number: 7427634Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: July 16, 2004Date of Patent: September 23, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: 7425555Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: GrantFiled: April 29, 2003Date of Patent: September 16, 2008Assignee: SmithKline Beecham CorporationInventors: Richard Martyn Angell, Paul Bamborough, Ian Robert Baldwin, Anne-Marie Li-Kwai-Cheung, Timothy Longstaff, Suzanne Joy Merrick, Kathryn Jane Smith, Stephen Swanson, Ann Louise Walker
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Publication number: 20080207703Abstract: The present invention provides novel heterocyclic urea compounds having useful antibacterial activity, pharmaceutical compositions comprising one or more of these compounds, methods of making the same, and methods of using the same.Type: ApplicationFiled: July 23, 2007Publication date: August 28, 2008Applicant: Replidyne, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun
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Publication number: 20080207712Abstract: The present invention relates to compounds of the Formula I wherein R1, R3, R4, R5, R6 and R7 are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: ApplicationFiled: May 1, 2008Publication date: August 28, 2008Inventors: Yuhpyng L. Chen, Lei Zhang
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Publication number: 20080207636Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: ApplicationFiled: February 1, 2008Publication date: August 28, 2008Applicant: AstraZeneca ABInventors: Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Clifford David Jones, Darren McKerrecher, Michael Howard Block, Craig Johnstone
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Publication number: 20080200463Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: May 24, 2006Publication date: August 21, 2008Applicant: LABORATOIRES SERONO SAInventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
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Publication number: 20080200334Abstract: Method for enhancing the fungicidal effectiveness of a) ethaboxam of the formula I, which comprises applying the active compound I simultaneously, that is separately or together, with at least one active compound II from the group consisting of: b) dithiocarbamates, such as maneb, mancozeb, metam or metiram, sulfenic acid derivatives, such as captan or folpet, strobilurin derivatives, such as kresoxim-methyl or pyraclostrobin, cinnamides and analogs, such as dimethomorph or flumorph, or dithianon, famoxadone, cymoxanil, fluazinam, zoxamide, mefenoxam or chlorothalonil, N-(2-{4-[3-(4-chlorophenyl)prop-2-ynyloxy]-3-methoxyphenyl}ethyl)-2-methanesulfonylamino-3-methylbutyramide, N-(2-{4-[3-(4-chlorophenyl)prop-2-ynyloxy]-3-methoxyphenyl}ethyl)-2-ethanesulfonylamino-3-methylbutyramide or 5-chloro-7-(4-methylpiperidin-1-yl)-6-(2,4,6-trifluorophenyl)-[1,2,4]triazolo[1,5-a]pyrimidine in synergistically effective amounts, by spraying or dusting the seeds, the plants or the soils before or after sowing of theType: ApplicationFiled: November 23, 2005Publication date: August 21, 2008Applicant: BASF AktiengesellschaftInventors: Jordi Tormo I Blasco, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Matthias Niedenbruck, Horst Dieter Brix, Markus Gewehr, Christine Beck
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Patent number: 7414067Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: March 24, 2004Date of Patent: August 19, 2008Assignees: Merck & Co. Inc., Evotec OAIInventors: Edward Andrew Boyd, Michael H. Fisher, Maria L. Garcia, Gregory J. Kaczorowski, Peter T. Meinke, William H. Parsons, Stephen Price, John Stibbard
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Patent number: 7410988Abstract: 2-Amido-4-substituted-aryl-thiazole-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.Type: GrantFiled: August 11, 2005Date of Patent: August 12, 2008Assignee: Genentech, Inc.Inventors: John K. Dickson, Jr., Carl Nicholas Hodge, Jose Serafin Mendoza, Ke Chen
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Patent number: 7411071Abstract: A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I): where X is S, O or N; Z is —T—COOR1 or —T—COR1; and T, R, R1, Ra, Rb, Rc, Rd, Z, A and B are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.Type: GrantFiled: January 12, 2006Date of Patent: August 12, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei V. Yang, Lidia M. Doweyko, Arthur M. Doweyko
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Publication number: 20080188531Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: May 24, 2006Publication date: August 7, 2008Applicant: LABORATOIRES SERONO SAInventors: Anna Quattropani, Jerome Dorbais, David Covini, Gwenaelle Desforges, Thomas Rueckle
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Publication number: 20080176911Abstract: Compounds of formula (I) as defined herein: inhibit the formation of the ?-amyloid peptide (?-A4) and are, therefore, useful in the treatment of pathologies in which a ?-amyloid peptide (?-A4) formation inhibitor provides a therapeutic benefit. Particular such pathologies are senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy, cerebrovascular disorders, frontotemporal dementias and Pick's disease, post-traumatic dementias, pathologies linked to neuroinflammatory processes, Huntington's disease and Korsakov's syndrome.Type: ApplicationFiled: March 20, 2008Publication date: July 24, 2008Applicant: SANOFI-AVENTISInventors: Sylvie BALTZER, Marc PASCAL, Viviane VAN DORSSELAER
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Publication number: 20080176899Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: August 11, 2005Publication date: July 24, 2008Inventors: Sarah Hadida Ruah, Peter Grootenhuis, Mark Miller, Matthew Hamilton
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Publication number: 20080167309Abstract: The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase, the compound having the formula (I): and salts, tautomers, N-oxides or solvates thereof, wherein A is a bond, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; Q is S or CR2; J is S or CH; provided that one of Q and J is S, and the other of Q and J is not S; when Q is S, there is a double bond between the ring carbon atoms “a” and “b” and a double bond between the ring nitrogen N and J; and when J is S, there is a double bond between Q and the ring carbon atom “a” and a double bond between the ring nitrogen N and the ring carbon atom “b”; and R1 to R4 are as defined in the claims.Type: ApplicationFiled: July 22, 2005Publication date: July 10, 2008Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio Berdini, Theresa Rachael Early, Michael Alistair O'Brien, Andrew James Woodhead, Paul Graham Wyatt
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Publication number: 20080161371Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.Type: ApplicationFiled: August 11, 2006Publication date: July 3, 2008Inventors: Sarah Hadida-Ruah, Frederick Van Goor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
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Publication number: 20080153883Abstract: The present invention relates to thiazolidinylidene containing compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, and X are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: December 12, 2007Publication date: June 26, 2008Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Tongmei Li, Arturo V. Perez-Medrano, Sridhar Peddi
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Publication number: 20080153838Abstract: The invention relates to a compound of the Formula I. or salt, prodrug or solvate thereof, wherein R1, R5, R6, D, A, B, L, n, m and p are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.Type: ApplicationFiled: February 2, 2006Publication date: June 26, 2008Applicant: ASTRAZENECA ABInventors: Clifford David Jones, Richard Williams Arthur Luke, William McCoull
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Publication number: 20080146550Abstract: The invention is concerned with novel heteroarylacetamides of formula (I) R—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb) ??(I) wherein Ra to Re are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.Type: ApplicationFiled: February 4, 2008Publication date: June 19, 2008Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Narendra Panday, Fabienne Ricklin
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Patent number: 7384967Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: GrantFiled: October 6, 2003Date of Patent: June 10, 2008Assignee: Novo Nordisk A/SInventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M. M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen
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Patent number: 7384968Abstract: The present invention relates to compounds of the Formula I wherein R1, R3, R4, R5, R6 and R7 are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: March 11, 2005Date of Patent: June 10, 2008Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
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Patent number: 7381734Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: July 22, 2005Date of Patent: June 3, 2008Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
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Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal
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Publication number: 20080125432Abstract: The present invention relates to compounds that interact with ion channels. In particular, the invention relates to compounds having the structural Formula having the structural Formula I, II, III or IV, stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or a pharmaceutically acceptable salt and/or solvate thereof, wherein X, Y1, Y2, R1, n, R3, R8, R9, R10, L1, L2, Ar1 and Ar2 are defined in claim 1. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body.Type: ApplicationFiled: December 1, 2005Publication date: May 29, 2008Applicant: Devgen NVInventors: Petra Blom, Jan Octaaf De Kerpel, Eric Pierre Paul Rene Fourmaintraux, Titus Jan Kaletta, Dirk Leysen
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Publication number: 20080119462Abstract: The present invention provides a method for treating a vascular hyperpermeable disease (except macular edema), which method comprises administering to a patient in need thereof a vascular adhesion protein-1 (VAP-1) inhibitor in an amount sufficient to treat said patient for said disease.Type: ApplicationFiled: October 31, 2007Publication date: May 22, 2008Applicants: Sucampo AG, Astellas Pharma Inc.Inventors: Ryuji UENO, Akira Nagashima, Takayuki Inoue, Mitsuru Ohkubo, Kousei Yoshihara
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Patent number: 7371869Abstract: The present invention relates to compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, cognative and CNS disorders and inflammatory/autoimmune diseases.Type: GrantFiled: September 14, 2005Date of Patent: May 13, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Robert Alan Goodnow, Jr., Nicholas J. S. Huby, Norman Kong, Lee Apostle McDermott, John Anthony Moliterni, Zhuming Zhang
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Patent number: 7371770Abstract: Compounds of formula (I) as defined herein: inhibit the formation of the ?-amyloid peptide (?-A4) and are, therefore, useful in the treatment of pathologies in which a ?-amyloid peptide (?-A4) formation inhibitor provides a therapeutic benefit. Particular such pathologies are senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy, cerebrovascular disorders, frontotemporal dementias and Pick's disease, post-traumatic dementias, pathologies linked to neuroinflammatory processes, Huntington's disease and Korsakov's syndrome.Type: GrantFiled: July 14, 2006Date of Patent: May 13, 2008Assignee: SanofiaventisInventors: Sylvie Baltzer, Marc Pascal, Viviane Van Dorsselaer
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Patent number: 7361654Abstract: The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory- and immune-associated diseases, and have the structure including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR6; Z is a ring; and where R, Ra, Rb, Rc, Rd, R1, R2, R3, R4, and R5 are as defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising such compounds.Type: GrantFiled: January 12, 2006Date of Patent: April 22, 2008Assignee: Bristol-Myers Squibb Co.Inventors: James Sheppeck, T. G. Murali Dhar, Lidia Doweyko, John Gilmore, David Weinstein, Hai-Yun Xiao, Bingwei V. Yang, Arthur M. Doweyko