Divalent Chalcogen Or Acyclic Nitrogen Double Bonded Directly At Both 2- And 4- Positions, Or Tautomeric Equivalent (e.g., Hydantoin, Etc.) Patents (Class 514/389)
-
Publication number: 20090306162Abstract: A composition for treating fungus infection of turfgrass, such as snow mould infection, comprises a mixture of fungicidally effective amounts of formulae 1 and 2: And in particular mixtures of oprodione and trifloxystrobin. A method for treating snow moulds comprises applying the mixture before the onset of continuous snow cover, in at least one application.Type: ApplicationFiled: October 19, 2005Publication date: December 10, 2009Applicant: Bayer CropScience Inc.Inventor: Edwin Vandenberg
-
Publication number: 20090306047Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: June 8, 2009Publication date: December 10, 2009Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
-
Publication number: 20090298900Abstract: Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.Type: ApplicationFiled: May 11, 2009Publication date: December 3, 2009Inventors: David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Charles Erec Stabbins, Vincent A. Fischetti
-
Patent number: 7612212Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.Type: GrantFiled: January 25, 2007Date of Patent: November 3, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, Steven Gregory Mischke, John Anthony Moliterni, Hong Wang, Zhuming Zhang
-
Publication number: 20090257968Abstract: The present invention provides an enhanced gelling agent composition comprising a mixture of an anionic surfactant and a coupling agent. The invention also describes compositions in gel form comprising: (a) a solvent selected from the group consisting of polar solvents, non-polar solvents and combinations thereof; and (b) a gelling agent in an amount sufficient to impart gelation to the composition, the gelling agent being a mixture comprising an anionic surfactant and a coupling agent. The gels of the invention may be substantially anhydrous or may optionally contain water as part of the formulation.Type: ApplicationFiled: May 6, 2009Publication date: October 15, 2009Inventors: Richard Walton, Edward T. Borish
-
Publication number: 20090258868Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 10, 2008Publication date: October 15, 2009Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
-
Publication number: 20090253763Abstract: An ester compound represented by the formula (I): (wherein, R1 represents a C1-C3 alkyl group, a 2-propenyl group or a 2-propynyl group.) has excellent pest controlling activity and is useful as an active ingredient for a pest controlling agent.Type: ApplicationFiled: August 24, 2007Publication date: October 8, 2009Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Jun Ohshita, Toru Uekawa
-
Publication number: 20090239888Abstract: Compositions and uses of mGluR5 antagonists for the treatment and inhibition of amyloid precursor protein (APP), A? protein, and APP proteolytic products in Alzheimer's disease, Fragile X Syndrome, autism, and Down's Syndrome are provided. The invention provides methods for diagnosing Fragile X Syndrome via the assessment of A?1-42 levels in blood plasma.Type: ApplicationFiled: February 12, 2009Publication date: September 24, 2009Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: James Malter, Cara Westmark
-
Patent number: 7589057Abstract: Biocompatible microparticles include an ophthalmically active alpha-2 adrenergic receptor agonist and a biodegradable polymer. The microparticles include oil-in-water emulsified microparticles which can be used to treat an ocular condition, such as glaucoma.Type: GrantFiled: March 31, 2006Date of Patent: September 15, 2009Assignee: Allergan, Inc.Inventors: James Chang, Patrick Hughes
-
Publication number: 20090220559Abstract: Solid formulations for use in water conditioning of circulating reservoirs, processes of preparing same and methods for water conditioning utilizing same are disclosed. The solid formulations combine a sanitizer with a bath salt and/or an odoriferous substance.Type: ApplicationFiled: April 25, 2007Publication date: September 3, 2009Applicant: Bromine Compounds Ltd.Inventors: David Feldman, Theodore M. Fishler, Amiram Groweiss, Aharon Weissman, Gideon Shikolsky, Moshe Link
-
Publication number: 20090215846Abstract: The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).Type: ApplicationFiled: December 13, 2006Publication date: August 27, 2009Applicant: Medivir ABInventors: Hans Wallberg, Ming-Hua Xu, Guo-Qiang Lin, Xin-Sheng Lei, Piaoyang Sun, Kevin Parkes, Tony Johnson, Bertil Samuelsson
-
Patent number: 7579018Abstract: Microbiological control is achieved by continuously and inexpensively dosing water in contact with biofilm, or that comes into contact with biofilm, using a highly effective biocide that provides very effective microbiocidal control of planktonic microorganisms and of biofilm species, even where the biofilm infestations have been in existence for long periods of time and thus have encased themselves in a substantial quantity of slimy defensive polysaccharide layers or films. In addition, the biocide used makes possible significant reduction in copper and/or iron surfaces in contact with the water as compared to N,N?-bromochloro- 5,5-dimethyl hydantoin. Still other advantages are made possible by the described technology.Type: GrantFiled: October 17, 2003Date of Patent: August 25, 2009Assignee: Albemarle CorporationInventors: Jonathan N. Howarth, Christopher J. Nalepa, Michael J. Sanders, David L. Shelton
-
Publication number: 20090186882Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: ApplicationFiled: January 21, 2009Publication date: July 23, 2009Inventors: Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo
-
Publication number: 20090156586Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: ApplicationFiled: February 3, 2009Publication date: June 18, 2009Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Lei Chen, De-Yi Yang, Robert Feltz, Seong Heon Kim
-
Publication number: 20090155385Abstract: A method for reducing or eliminating Salmonella in reptiles and/or reptile eggs through the use of at least one N,N-dihalo-5,5-dialkylhydantoin in which each of the alkyl groups is independently selected from those containing in the range of from 1 to about 6 carbon atoms.Type: ApplicationFiled: June 15, 2007Publication date: June 18, 2009Inventors: Joe D. Sauer, George W. Cook, Jr., Christopher J. Nalepa
-
Publication number: 20090149417Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.Type: ApplicationFiled: October 17, 2008Publication date: June 11, 2009Inventors: Valeria Ossovskaya, Barry M. Sherman
-
Publication number: 20090149522Abstract: The invention concerns a process for producing a preserved customised consumer composition, preferably from a Vending machine, wherein a plurality of ingredient streams are mixed together in predefined relative amounts, characterised in that At least two streams consist of water and preservative only, at least two of which having different concentrations of preservative. The Invention permits the final preservative mix to be independently variable to the formation.Type: ApplicationFiled: July 28, 2006Publication date: June 11, 2009Inventors: Geetha Basappa, Maria Teresa Belmar, Ana Martin-Herranz, Iain Sunil Young
-
Publication number: 20090117202Abstract: Novel formulations containing a non-oxidative biocide, such as DBNPA, and a source of an in situ produced active biocide, such as a concentrated aqueous solution of an inorganic halide salt, are disclosed. These novel formulations are particularly effective in the treatment of water, and are characterized by high stability, desirable rheological properties and an excellent biocidal activity.Type: ApplicationFiled: February 25, 2007Publication date: May 7, 2009Applicant: BROMINE COMPOUNDS LTD.Inventors: David Feldman, Michel Adda, Raymond J. Roccon
-
Publication number: 20090111803Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF—or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: April 30, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankat
-
Publication number: 20090105323Abstract: In the growing of crops for consumption, a method for the removal of pathogens includes the addition to irrigation water for the crops of an anti-pathogen composition and supplying the anti-pathogen composition to the crops prior to harvest while normal irrigation is effected. The anti-pathogen composition is based on halogens, such as chlorine, bromine and iodine, or mixtures of halogens or halogens combined with other organic radicals including cyanurate, hydantoin, peroxide and chlorine dioxide. BCDMH and TICA are preferred anti-pathogen components of the anti-pathogen composition and may be added to a carrier concentrate and measured and dosed into the irrigation water.Type: ApplicationFiled: May 18, 2006Publication date: April 23, 2009Inventor: William Bliss
-
Patent number: 7521465Abstract: Novel diphenyl ether derivatives are provided that exhibit activity useful for reducing glucose, cholesterol, and/or triglyceride levels in plasma, and for treatment of obesity, inflammation, immunological diseases, autoimmune diseases, diabetes and disorders associated with insulin resistance.Type: GrantFiled: March 31, 2005Date of Patent: April 21, 2009Assignee: Bexel Pharmaceuticals, Inc.Inventors: Bishwajit Nag, Abhijeet Nag, Debendranath Dey, Shiv Kumar Agarwal, Partha Neogi, Gaddam Om Reddy, Sangamesh Badiger, Gajendra Singh, Surendra Kumar Pandey, Santhanagopalan Chithra
-
Patent number: 7514462Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives. The PGE derivatives used in accordance with the invention are represented by the following formula I: wherein the hatched segment represents an ? bonds, the solid triangle represents a ? bond, the wavy segments represent ? or ? bond, dashed lines represent a double bond or a single bond, X is selected from the group consisting of hydrogen and halogen radicals, R3 is heteroaryl or a substituted heteroaryl radical, R1 and R2 are independently selected from the group consisting of hydrogen or a lower alkyl radical having up to six carbon atoms, or a lower acyl radical having up to six carbon atoms, R is selected from the group consisting of CO2R4, CONR42, CH2OR4, CONR4SO2R4, P(O)(OR4) and wherein R4 is selected from the group consisting of H, phenyl and lower alkyl having from one to six carbon atoms and n is 0 or an integer of from 1 to 4.Type: GrantFiled: June 6, 2007Date of Patent: April 7, 2009Assignee: Allergan, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
-
Publication number: 20090076045Abstract: Compounds of formula I, wherein R1, X1, X2 and A, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.Type: ApplicationFiled: May 30, 2008Publication date: March 19, 2009Inventors: Joshua Kennedy-Smith, Zachary Kevin Sweeney, Jeffrey Wu
-
Publication number: 20090075986Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: June 9, 2006Publication date: March 19, 2009Inventors: Daniel L. Flynn, Peter A. Petillo
-
Publication number: 20090012066Abstract: The present invention provides methods of treating and/or preventing pathologic cardiac hypertrophy and heart failure comprising administering hydroxamate compounds which are deacetylase inhibitors.Type: ApplicationFiled: August 9, 2006Publication date: January 8, 2009Inventors: Seigo Izumo, Suraj Shivappa Shetty
-
Publication number: 20080318987Abstract: Methods and compositions for modulating bone formation and mineralization are described.Type: ApplicationFiled: February 15, 2008Publication date: December 25, 2008Inventor: Laurie H. GLIMCHER
-
Publication number: 20080306065Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: ApplicationFiled: May 6, 2008Publication date: December 11, 2008Inventors: Anders Eriksson, Matti Lepisto, Michael Lundkvist, Magnus Munck Af Rosenschold, Pavol Zlatoidsky
-
Publication number: 20080262045Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: ApplicationFiled: May 5, 2008Publication date: October 23, 2008Inventors: Anders Eriksson, Matti Lepisto, Michael Lundkvist, Magnus Munck Af Rosenschold, Pavol Zlatoidsky
-
Publication number: 20080234204Abstract: Provide is a method for evaluating test agents as candidates for treating prostatic diseases, including benign prostatic hyperplasia (BPH) and androgen dependent and androgen independent prostate cancer. The method comprises providing a mouse comprising a human prostate primary xenograft, where the xenograft contains blood vessels that include human endothelial cells, initiating androgen deprivation in the mouse, administering to the mouse a test agent within a period of 1-7 days after initiating the androgen deprivation, and determining a reduction in human epithelial cells in the xenografts and/or a reduction in number of the endothelial cells or blood vessels in the xenograft. Also provided is a method for treating an individual for human prostate cancer or benign prostatic hyperplasia.Type: ApplicationFiled: January 30, 2008Publication date: September 25, 2008Inventors: Gary J. Smith, Howard M. Reisner, Danny R. Gray, Wendy Huss
-
Publication number: 20080226618Abstract: This invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.Type: ApplicationFiled: August 29, 2007Publication date: September 18, 2008Inventors: Umar Faruk Mansoor, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
-
Publication number: 20080221181Abstract: The invention provides compounds of formula (I): wherein E, A, B?, R6, R7, R8, and R9 are defined in the specification which compounds exhibit anticancer activity and are useful for treating cancer.Type: ApplicationFiled: April 17, 2008Publication date: September 11, 2008Applicant: Wyeth Holdings CorporationInventors: Arie Zask, Joshua Kaplan, Ayako Yamashita, Chuan S. Niu, Gary Harold Birnberg, Emily Norton, Kinwang Cheung, Ronald Suayan, Vincent Sandanayaka, Philip Ross Hamann, Semiramis Ayral-Kaloustian
-
Patent number: 7381737Abstract: A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G? is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.Type: GrantFiled: September 29, 2005Date of Patent: June 3, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Albert J. DelMonte, T. G. Murali Dhar, Yu Fan, Jack Z. Gougoutas, Mary F. Malley, Douglas D. McLeod, Robert E. Waltermire, Chenkou Wei
-
Publication number: 20080118553Abstract: The subject invention provides a composition comprising a mixture of polypeptides in the form of a tannate salt wherein each polypeptide is a copolymer of the amino acids L-glutamic acid, L-alanine, L-tyrosine and L-Lysine, methods of preparation and uses thereof.Type: ApplicationFiled: June 12, 2007Publication date: May 22, 2008Inventors: Anton Frenkel, Arthur A. Komlosh
-
Patent number: 7371397Abstract: Microbiological control in aqueous media and/or eradication or reduction of biofilm on a surface in contact with such media is achieved by introducing into the aqueous medium a microbiocidally effective quantity of one or more 1,3-dibromo-5,5-dialkylhydantoins where one of the alkyls is methyl and the other is a C1-4 alkyl, wherein (i) the molar quantity of 1,3-dibromo-5,5-dialkylhydantoin introduced is less than the molar quantity of N,N?-bromochloro-5,5-dimethylhydantoin that would be required to effect the same degree of microbiological control in that medium, (ii) the molar quantity of the 1,3-dibromo-5,5-dialkylhydantoin introduced releases an amount of “free chlorine” that is greater than the amount of “free chlorine” that would be released in that medium by an equimolar quantity of N,N?-bromochloro-5,5-dimethylhydantoin, and (iii) the amount of “free chlorine” released by the quantity of the 1,3-dibromo-5,5-dialkylhydantoin introduced is greater than the amount of “free chlorine” that could be predicteType: GrantFiled: October 17, 2003Date of Patent: May 13, 2008Assignee: Albemarle CorporationInventors: Jonathan N. Howarth, Christopher J. Nalepa, Michael J. Sanders
-
Patent number: 7368465Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: GrantFiled: March 13, 2002Date of Patent: May 6, 2008Assignee: AstraZeneca ABInventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
-
Publication number: 20080096923Abstract: The present invention relates to a method for treating one or more diabetic microvascular complications in a patient in need of said treatment comprising: (a) diagnosing the severity of at least three different microvascular complications in said patient by calculating a diabetes microvascular complications score with a diabetes microvascular complications scoring tool; and (b) administering to said patient in need thereof a therapeutic amount of a compound selected from the group consisting of ruboxistaurin, enzastaurin, PKC 412, candesartan cilexetil, fidarestat, lidorestat, pyridoxamine and pegaptanib, or a pharmaceutically acceptable salt thereof, and ranibizumab; in an amount that is effective in treating one or more diabetic microvascular complications in said diabetic patient.Type: ApplicationFiled: July 13, 2005Publication date: April 24, 2008Inventor: Aniz Girach
-
Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
-
Patent number: 7354940Abstract: The invention provides compounds of formula (I) in which L, X, Y, Z1, Z2, R1, R2, R3 and G2 have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds of the invention are inhibitors of metalloproteinase MMP12 and are among other things useful for the treatment of obstructive airways diseases, such as asthma and chronic obstructive pulmonary disease (COPD).Type: GrantFiled: August 26, 2003Date of Patent: April 8, 2008Assignee: AstraZeneca ABInventors: Krister Henriksson, Magnus Munck Af Rosenschöld
-
Patent number: 7354933Abstract: The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.Type: GrantFiled: February 2, 2004Date of Patent: April 8, 2008Assignee: Aventis Pharma SAInventors: Marcel Patek, Anil Nair, Augustin Hittinger, Conception Nemecek, Daniel Bond, Greg Harlow, Herve Bouchard, Jacques Mauger, Jean-Luc Malleron, Mark Palermo, Fahad Al-Obeidi, Thomas Faitg, Hartmut Strobel, Sven Ruf, Kurt Ritter, Youssef El-Ahmad, Dominique Lesuisse, Didier Bénard
-
Publication number: 20080081052Abstract: A method for enhancing solubility of allantoin in an aqueous vehicle using a solubilization enhancer is described. Aqueous compositions containing the solubilized allantoin at a level of 0.5% by weight or higher are able to be obtained by using urea or urea derivatives as the solubilization enhancer. The aqueous topical compositions are suitable for cosmetic, dermatological, and pharmaceutical use.Type: ApplicationFiled: October 2, 2006Publication date: April 3, 2008Inventor: Jerry Zhang
-
Publication number: 20080069791Abstract: The present invention relates to the use of IL-15 polynucleotides, polypeptides or compounds which bind to an antibody which specifically recognizes the IL-15 polypeptide or which specifically bind to an IL-15 receptor alpha chain for the preparation of a composition for stimulating hair growth or for treating, preventing and/or ameliorating hair loss. Moreover the present invention encompasses a transgenic non-human animal comprising an IL-15 polynucleotide. The present invention also relates to a method for stimulating hair growth in a non-human animal and to methods for manufacturing animal hair. Finally, the present invention relates to a method of treating, preventing and/or ameliorating a subject which suffers from hair loss.Type: ApplicationFiled: December 7, 2004Publication date: March 20, 2008Applicant: Universitaetsklinikum MuensterInventor: Stefan Beissert
-
Publication number: 20070197617Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.Type: ApplicationFiled: January 25, 2007Publication date: August 23, 2007Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, Steven Gregory Mischke, John Anthony Moliterni, Hong Wang, Zhuming Zhang
-
Patent number: 7226940Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel DiseaseType: GrantFiled: August 24, 2005Date of Patent: June 5, 2007Assignees: Incyte San Diego, Inc., Ortho McNeil Pharmaceutical Inc.Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul, David P. M. Pleynet, Lyle W. Spruce
-
Patent number: 7202251Abstract: The present invention is directed to compounds of the formula: that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: April 10, 2007Assignee: Merck & Co., Inc.Inventors: Ian M. Bell, Steven N. Gallicchio, Cory R. Theberge, Xu-Fang Zhang, Craig Stump, C. Blair Zartman
-
Patent number: 7202366Abstract: Novel diphenylethylene compounds and derivatives thereof containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.Type: GrantFiled: March 25, 2004Date of Patent: April 10, 2007Assignee: Theracos, Inc.Inventors: Bishwajit Nag, Debendranath Dey, Satyanarayana Medicherla, Partha Neogi
-
Patent number: 7189722Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: March 13, 2007Assignee: Merck & Co., Inc.Inventors: Ian M. Bell, Cory R. Theberge, Xu-Fang Zhang, C. Blair Zartman
-
Patent number: 7179831Abstract: 5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2,4-dione and analogues useful as inhibitors of macrophage elastase are disclosed.Type: GrantFiled: August 17, 2005Date of Patent: February 20, 2007Assignee: Quest Pharmaceutical ServicesInventor: Fude Yang
-
Patent number: 7176223Abstract: Process for the synthesis of 5-(3-pyridylmethyl)imidazolidine-2,4-dione, according to which 5-(3-pyridylmethylene)imidazolidine-2,4-dione is subjected to a hydrogenation reaction.Type: GrantFiled: October 24, 2005Date of Patent: February 13, 2007Assignee: Solvay S.A.Inventor: Roland Callens
-
Patent number: 7173057Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: February 6, 2007Assignee: Schering CorporationInventors: Kevin X. Chen, F. George Njoroge, Mousumi Sannigrahi, Latha G. Nair, Weiying Yang, Bancha Vibulbhan, Srikanth Venkatraman, Ashok Arasappan, Stephane L. Bogen, Frank Bennett, Viyyoor M. Girijavallabhan
-
Patent number: 7144583Abstract: A pesticidal composition comprising an oxadiazine compound given by formula (A): and an ester compound given by formula (B): as active ingredients, wherein the weight ratio of the oxadiazine compound given by formula (A) to the ester compound given by formula (B) is within the range of 50:1 to 1:10, has an excellent efficacy for controlling pests.Type: GrantFiled: February 3, 2004Date of Patent: December 5, 2006Assignee: Sumitomo Chemical Company, LimitedInventor: Satoshi Sembo