The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
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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: 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: 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: 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: 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: 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: 20080312435Abstract: An imine compound represented by the formula: wherein A represents a heterocyclic group; R1, R2, an R3 each represent a hydrogen atom, a halogen atom, a C1-10 alkyl group optionally substituted with an aryl group(s) substituted with a halogen atom(s), a C3-10 cycloalkyl group, a C1-6 haloalkyl group, a C1-10 alkoxy group, etc.; R4 represents an optionally substituted C1-10 alkyl, C2-6 alkenyl, or aryl group; R5 represents a hydrogen atom, a C1-10 alkoxy group, a C1-6 haloalkyl group, an optionally substituted C1-10 alkyl or C2-6 alkenyl group, an optionally substituted aryl or heterocyclic group, etc.; W represents —CO—, —CO—CO—, —CO—NH—, —CS—NH—, or —SO2—, or a cannabinoid-receptor agonist comprising said imine compound as an active ingredient. The imine compound of the present invention has a cannabinoid-receptor agonist effect, and is useful as a therapeutic or prophylactic drug for pains and autoimmune diseases.Type: ApplicationFiled: October 31, 2005Publication date: December 18, 2008Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Shiuji Saito, Hiroshi Ohta, Tomoko Ishizaki, Mitsukane Yoshinaga, Makoto Tatsuzuki, Yuji Yokobori, Yasumitsu Tomishima, Aki Morita, Yoshihisa Toda, Kimiko Tokugawa, Ayaka Kaku, Tomomi Murakami, Hiromitsu Yoshimura, Shingo Sekine, Takao Yoshimizu
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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: 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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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: 20080293730Abstract: Compounds of Formula (I): (formula) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: ApplicationFiled: November 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: 20080269295Abstract: The present invention relates to substituted thiazoles, to methods for their production, to drugs containing these compounds and to the use of said compounds for producing drugs.Type: ApplicationFiled: June 26, 2008Publication date: October 30, 2008Applicant: Grunenthal GmbHInventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH
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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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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: 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: 20080210907Abstract: An ionic organic compound having a repeating unit of formula (I) can be synthesized easily from a readily available organic compound through a small number of reaction steps, can be produced without any purification technique such as chromatography, and can be used in a quite small amount for gelation of water or an ionic liquid without any other auxiliary solvent: [-(A-B-C)n-]•m(X) ??(I) wherein A represents a group having a quaternary ammonium cation which is formed from a heterocyclic compound having at least one nitrogen atom; B represents a functional group, which may have a substituent, selected from amide, urea, urethane and peptide groups; C represents a divalent hydrocarbon group, which may have a substituent, capable of linking between A and B; X represents an anion; n represents the number of repeating units; m represents the total number of anions; and n and m are the same integer.Type: ApplicationFiled: January 30, 2006Publication date: September 4, 2008Applicant: NAATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGYInventors: Masaru Yoshida, Nagatoshi Koumura, Nobuyuki Tamaoki, Hajime Kawanami, Hajime Matsumoto, Said Kazaoui, Nobutsugu Minami
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Publication number: 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: 20080207912Abstract: A process for preparation of ceftiofur of formula (I) of high purity and substantially free from impurities is disclosed.Type: ApplicationFiled: April 30, 2008Publication date: August 28, 2008Inventors: Om Dutt Tyagi, Santosh Kumar Richhariya, Rajesh Kumar Ramchandra Pawar, Yuvaraj Atmaram Chavan
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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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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: 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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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: 7408069Abstract: A method for preparing a compound of the structure I,Type: GrantFiled: August 3, 2006Date of Patent: August 5, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Bernd Schaefer, Frank Haunert, Norbert Goetz
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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: 20080176865Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.Type: ApplicationFiled: December 13, 2007Publication date: July 24, 2008Applicant: PFIZER LIMITEDInventors: Denis Billen, Jessica Boyle, Douglas James Critcher, David Morris Gethin, Kim Thomas Hall, Graham Michael Kyne
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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: 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: 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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Patent number: 7390908Abstract: 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: GrantFiled: August 15, 2002Date of Patent: June 24, 2008Assignee: AstraZeneca ABInventors: Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Craig Johnstone, Clifford David Jones, Darren McKerrecher, Michael Howard Block
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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: 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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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: 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: 7335673Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient.Type: GrantFiled: August 10, 2001Date of Patent: February 26, 2008Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Yoichiro Hoshina, Satoru Ikegami, Akihiko Okuyama, Tatsuhiro Harada, Atsushi Matsuo
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Publication number: 20080045560Abstract: Compounds of the following structure are described: wherein R1-R6, R11, R12, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.Type: ApplicationFiled: August 13, 2007Publication date: February 21, 2008Applicant: WyethInventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski
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Patent number: 7329680Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: GrantFiled: April 30, 2004Date of Patent: February 12, 2008Assignee: The Institute for Pharmaceutical Discovery, LLCInventors: Darren Whitehouse, Shaojing Hu, Haiquan Fang, Kerry Combs, Michael C. Van Zandt
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Patent number: 7326728Abstract: 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) its stereoisomers thereof, or a solvate thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Z is CONR1R2 or CH2NR1R2 and where R, R?, 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 13, 2005Date of Patent: February 5, 2008Assignee: Bristol-Myers Squibb CompanyInventor: Bingwei Vera Yang
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Patent number: 7323482Abstract: The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R2, R3, Z1 m and n are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: December 4, 2006Date of Patent: January 29, 2008Assignee: Bristol-Myers Squibb CompanyInventors: John Hynes, Hong Wu, Katerina Leftheris, Chunjian Liu, Jagabandhu Das, Robert V. Moquin
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Patent number: 7291636Abstract: This invention discloses and claims a compound conforming to the general formula (I): Wherein R1, R2, R?2, R3, R4 and R5 are as described herein. The compounds of the present invention exhibit an inhibitory effect on the production of ?-amyloid peptide (?-A4) by inhibition of gamma protease. Therefore, the compounds of the present invention are useful in the treatment of pathologies such as senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy and/or cerebrovascular disorders.Type: GrantFiled: January 14, 2005Date of Patent: November 6, 2007Assignee: Sanofi-AventisInventors: Sylvie Baltzer, Bruno Schoentjes, Viviane Van Dorsselaer
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Patent number: 7288659Abstract: The invention concerns a compound of general formula (I), wherein: X represents an oxygen or sulphur atom; R1 represents, independently of each other when n=2 or 3, a halogen atom, a hydroxy, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, a trifluoromethyloxy or a methylenedioxy; R2 represents a C1-C6 alkyl group optionally substituted, a C3-C7 cycloalkyl, piperidinyl or phenyl group, the C3-C7 cycloalkyl, piperidinyl or phenyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-C6 alkyl group optionally substituted; R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 and R5? represent, independently of each other, a hydrogen atom, a hydroxy, a halogen atom, a C1-C3 alkyl group, or R5 and R5? form together an oxo group; R6 represents a hydrogen atom, a halogen atom, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, or a trifluoromethoxy; in the form of a base, addition to an acid, hydrate or solvate.Type: GrantFiled: August 5, 2002Date of Patent: October 30, 2007Assignee: Sanofi-AventisInventors: Paul De Cointet, Pierre Despeyroux, Daniel Frehel, Chantal Guenet, Corinne Heckel, Jean-Pierre Maffrand, Rebecca Pruss
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Patent number: 7285567Abstract: A halogenated benzamide derivative characterized by greater specificity for viral pathogens and less disruptive to beneficial gut microflora, according to formula (III): in which R1 is a halogen atom, and R2-R6 are independently hydrogen, hydroxyl, C1-C4 alkyl, —C1-C4 alkoxy, acyloxy, nitro, halogen, —C(O)R7 where R7 is —C1-C4 alkyl, or, aromatic including salts and hydrates of these compounds.Type: GrantFiled: September 6, 2005Date of Patent: October 23, 2007Assignee: Romark Laboratories, L.C.Inventor: Jean Francois Rossignol
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Patent number: 7273881Abstract: 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) its stereoisomers thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, where Z is S, O or NH; and R, R1, R2 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 13, 2005Date of Patent: September 25, 2007Assignee: Bristol-Myers Squibb CompanyInventor: Bingwei Vera Yang
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Patent number: 7259166Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: April 10, 2006Date of Patent: August 21, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Jagdish Kumar Racha, Ramakanth Sarabu, Ka Wang
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Patent number: 7220765Abstract: The present invention is drawn to compounds of the formula in racemic and enantiomeric form or all combinations of these forms wherein the various substituents are as defined in the application which compounds have a good affinity for certain subtypes of somatostatin receptors and have useful pharmacological properties.Type: GrantFiled: July 8, 2003Date of Patent: May 22, 2007Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (SCRAS)Inventors: Christophe Moinet, Carole Sackur, Christophe Thurieau
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Patent number: 7169931Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: X1—Y1-Z1 ??(I) wherein X1 is optionally substituted aryl, optionally substituted heteroaryl or the like; Y1 is —NRACO—(CH2)0-2— or the like (wherein RA is hydrogen atom or the like); and Z1 is a cyclic group fused the same or different two ring selected from optionally substituted carbocyclic group and optionally substituted heterocyclic group.Type: GrantFiled: January 25, 2002Date of Patent: January 30, 2007Assignee: Shionogi & Co., Ltd.Inventors: Hiroshi Takemoto, Masami Takayama, Yutaka Yoshida
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Patent number: 7160902Abstract: Amide derivatives of the general formulae Ia and Ib: are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing gastrointestinal disorders, pain, and pruritus are also disclosed.Type: GrantFiled: November 14, 2003Date of Patent: January 9, 2007Assignee: Adolor CorporationInventors: Roland E. Dolle, Guo-Hua Chu, Minghua Gu
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Patent number: 7125901Abstract: 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: January 27, 2004Date of Patent: October 24, 2006Assignee: Astellas Pharma Inc.Inventors: Takayuki Inoue, Takashi Tojo, Masataka Morita, Mitsuru Ohkubo, Kousei Yoshihara, Akira Nagashima