And Chalcogen Bonded Directly To A Ring Carbon Of The Five Membered Hetero Ring Which Is Not Adjacent To The Ring Nitrogen (e.g., 2,4 Pyrrolidinediones, Etc.) Patents (Class 548/544)
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Patent number: 8188145Abstract: Natural and synthetic compounds having a lactone structure methods for alleviation of pain, especially pain associated with disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. Initial studies have shown that patients can be taken off of morphine when the preferred alpha-methylene-gamma-butyrolactone is administered in a dosage of between 60 and 120 mg/day intramuscularly.Type: GrantFiled: April 18, 2005Date of Patent: May 29, 2012Assignee: Magnachem International Laboratories, Inc.Inventors: Federico M. Gomez, C. Federico Gomez Garcia-Godoy
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Patent number: 8173697Abstract: The invention relates to new alkoxyalkyl-substituted cyclic ketoenols of the formula (I) in which A, B, D, G, W, X, Y and Z have the definitions indicated above, to a number of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or microbicides. The invention further provides selectively herbicidal, compositions which comprise alkoxyalkyl-substituted cyclic ketoenols on the one hand and a crop plant tolerance promoter compound on the other. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetration promoters.Type: GrantFiled: May 23, 2007Date of Patent: May 8, 2012Assignee: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Olga Malsam, Christian Arnold, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger, Rolf Pontzen, Ulrich Görgens, Jan Dittgen
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Publication number: 20120101257Abstract: The present application describes general process for the preparation of amino-substituted gamma-lactams involving the reaction of synthons of the general Formulae (I) and (VI): with amines. The processes are amenable to solid phase synthetic techniques and therefore allow the efficient incorporation of amino-substituted gamma-lactams into a wide variety of structural scaffolds, including, in particular peptides.Type: ApplicationFiled: March 18, 2010Publication date: April 26, 2012Applicant: UNIVERSITE DE MONTREALInventors: William Lubell, Andrew Jamieson, Nicolas Boutard, Luisa Ronga, Daniel St-Cyr, Stephane Turcotte, Wang Chen
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Publication number: 20120046337Abstract: Novel 5-membered iminocyclitol derivatives were found to be a potent and selective inhibitors of the glycoprotein processing ?- and ?-glucosidase which were further found to be active antiviral agents against Japanese encephalitis virus, dengue virus serotype 2 (DEN-2), human SARS coronavirus and human ?-hexosaminidase, a new target for development of osteoarthritis therapeutics.Type: ApplicationFiled: February 24, 2011Publication date: February 23, 2012Inventors: Pi-Hui Liang, Yi-Ling Lin, Chi-Huey Wong
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3-biphenyl-substituted-3-substituted-4-ketolactam and ketolactone and their utilization as pesticide
Patent number: 8119570Abstract: The present invention relates to novel 3-biphenyl-substituted, 3-substituted 4-keto-lactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y and Z are as defined in the disclosure, to processes for their preparation, and to their use as pesticides and/or microbicides and/or herbicides.Type: GrantFiled: October 23, 2007Date of Patent: February 21, 2012Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Mark Wilhelm Drewes, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Dieter Feucht, Udo Reckmann, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann -
3-BIPHENYL-SUBSTITUTED-3-SUBSTITUTED-4-KETOLACTAM AND KETOLACTONE AND THEIR UTILIZATION AS PESTICIDE
Publication number: 20120028804Abstract: The present invention relates to novel 3-biphenyl-substituted, 3-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y and Z are as defined in the disclosure, to processes for their preparation, and to their use as pesticides and/or microbicides and/or herbicides.Type: ApplicationFiled: October 23, 2007Publication date: February 2, 2012Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Mark Wilhelm Drewes, Christoph Erdelen, Angelika Lubos-Erdelen, Dieter Feucht, Udo Reckmann, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann -
Patent number: 8093405Abstract: An iodonium compound of formula (I): where RAR1 is a C5-6 aryl group, bearing at least one substituent selected from formyl, thionoacyl, acylamidocarboxy, thionoester, azo, C2-20 alkenyl, C2-20 alkynyl, and (CH2)nRC, where RC is selected from ether, amino, azo and thioether; RAR2 is a C5-10 aryl group, optionally substituted by one or more groups selected from C1-12 alkyl, C5-12 aryl, C3-12 heterocyclyl, ether, thioether, nitro, cyano and halo, and may be linked to a solid support or fluorous tag; and X is a counteranion.Type: GrantFiled: May 15, 2009Date of Patent: January 10, 2012Assignee: University of Newcastle Upon TyneInventors: Michael Andrew Carroll, Ran Yan
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Patent number: 8080673Abstract: This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R3, R4 and R5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.Type: GrantFiled: February 19, 2010Date of Patent: December 20, 2011Assignee: Cardiome Pharma Corp.Inventors: Grace Jung, James Gee Ken Yee, Doug Ta Hung Chou, Bertrand M. C. Plouvier
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Patent number: 8071388Abstract: The invention provides compositions and methods for the detection of biological targets, (e.g. nucleic acids and proteins) by nucleic acid-templated chemistry, for example, by generating fluorescent polymethine dyes.Type: GrantFiled: February 24, 2009Date of Patent: December 6, 2011Assignee: Ensemble Therapeutics CorporationInventors: Yumei Huang, James M. Coull
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Publication number: 20110294783Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: August 10, 2011Publication date: December 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
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Publication number: 20110281879Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: January 12, 2011Publication date: November 17, 2011Applicant: ViroBay, Inc.Inventor: Craig Mossman
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Patent number: 8058455Abstract: A compound having a structure expressed by the following Structural Formula (1) and a compound having a structure expressed by the following Structural Formula (2):Type: GrantFiled: February 23, 2011Date of Patent: November 15, 2011Assignee: Kinki UniversityInventors: Masayuki Igarashi, Ryutaro Utsumi
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Publication number: 20110269973Abstract: The present invention relates to a new process for preparing dithiine-tetracarboximides.Type: ApplicationFiled: April 14, 2011Publication date: November 3, 2011Applicant: Bayer CropScience AGInventors: Thomas HIMMLER, Winfried ETZEL, Frank VOLZ
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Patent number: 8034949Abstract: The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of R1 and R2 is (A) optionally substituted aryl (or heteroaryl) group, or (B) both of the groups combine to form a group of the formula: one of R3 and R4 is hydrogen and another is hydrogen, hydroxyl, hydroxyalkyl, etc., or both of R3 and R4 combine to form oxo group, R5 is hydrogen or alkyl, Y is single bond, oxygen atom or a group of the formula: —N(R7)—, R6 is optionally substituted hydrocarbon group or optionally substituted cyclic group, R7 is alkyl or alkyloxycarbonylalkyl, provided that R6 is not 4-amino-5-chloro-2-methoxyphenyl group when Y is single bond and one of the R3 and R4 is hydrogen and another is hydroxymethyl, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 27, 2005Date of Patent: October 11, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yasunori Moritani, Shigeru Furukubu, Yasunori Tsuboi, Chieko Okagaki, Akira Oku, Naomitsu Hirano
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Publication number: 20110245218Abstract: The present invention relates to the use of new and known maleimide salts for controlling phytopathogenic fungi, and also to methods for controlling phytopathogenic fungi in crop protection, in the household and hygiene sectors and in materials protection, and also to crop protection compositions comprising these maleimide salts.Type: ApplicationFiled: March 4, 2011Publication date: October 6, 2011Applicant: Bayer CropScience AGInventors: Thomas SEITZ, Thomas Himmler, Jürgen Benting, Ulrike Wachendorff-Neumann
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Patent number: 8030459Abstract: The present invention relates to biodegradable biocompatible polyketals, methods for their preparation, and methods for creating animals by administration of biodegradable biocompatible polyketals. In one aspect, a method for forming the biodegradable biocompatible polyketals comprises combining a glycol-specific oxidizing agent with a polysaccharide to form an aldehyde intermediate, which is combined with a reducing agent to form the biodegradable biocompatible polyketal. The resultant biodegradable biocompatible polyketals can be chemically modified to incorporate additional hydrophilic moieties. A method for treating animals includes the administration of the biodegradable biocompatible polyketal in which biologically active compounds or diagnostic labels can be disposed. The present invention also relates to chiral polyketals, methods for their preparation, and methods for use in chromatographic applications, specifically in chiral separations.Type: GrantFiled: July 18, 2003Date of Patent: October 4, 2011Assignee: The General Hospital CorporationInventors: Mikhail I. Papisov, Alexander Yurkovetskiy
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Patent number: 8013172Abstract: The disclosure relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the disclosure relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The disclosure furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.Type: GrantFiled: February 8, 2007Date of Patent: September 6, 2011Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Dieter Feucht, Eva-Maria Franken, Olga Malsam, Alfred Angermann, Guido Bojack, Christian Arnold, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger
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Publication number: 20110213160Abstract: The invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I), in which CKE, W, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2,4,6-phenyl-substituted cyclic ketoenols and secondly at least one compound which improves crop plant tolerance.Type: ApplicationFiled: April 15, 2011Publication date: September 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Thomas BRETSCHNEIDER, Reiner Fischer, Oliver Gaertzen, Klaus Kunz, Stefan Lehr, Dieter Feucht, Peter Lösel, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Jeffrey Martin Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20110207944Abstract: Compound represented by formula (1) or a pharmaceutically acceptable solvate thereof, useful for treating or preventing Paget's disease of bone, hypercalcaemia, osteoporosis or asthma. (1) R1 represents a C1-C6 alkyl group or C7-C15 aralkyl group (the aromatic ring of which can be substituted by a C1-C6 alkyl group, C1-C6 alkoxy group, a hydroxyl group, a halogenatom or a trifluoromethyl group), R2 represents a C1-C6 alkyl group, and R3 represents a C1-C6 alkyl or alkoxy group, which can be substituted with a hydroxyl group.Type: ApplicationFiled: November 2, 2009Publication date: August 25, 2011Applicant: TEIJIN PHARMA LIMITEDInventors: Yuko Nakamura, Hiroshi Saito, Kazuo Nagasawa, Atsushi Kittaka
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Publication number: 20110201807Abstract: The present invention provides 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylates of the formula (I): wherein R1 is a C1-6 alkyl group, etc., R2 is a hydrogen atom or a COOR3 group, wherein R3 is a tert-C4-6 alkyl group, a 2,2,2-trichloroethyl group or a benzyl group in which the benzene ring moiety may be optionally substituted by one or two atoms or groups independently selected from the group consisting of a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a cyano group and a nitro group, and a salt thereof, which are useful as a novel intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3?-pyrrolidine derivatives such as Ranirestat being promising therapeutic agents for diabetic complications in a short process and in an economically advantageous and safe manner, and the process for preparing the same.Type: ApplicationFiled: April 25, 2011Publication date: August 18, 2011Inventor: Daisuke TANAKA
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Publication number: 20110183849Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: ApplicationFiled: March 24, 2011Publication date: July 28, 2011Applicant: Bayer AktiengesellschaftInventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
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Publication number: 20110172240Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.Type: ApplicationFiled: January 7, 2011Publication date: July 14, 2011Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20110144355Abstract: A compound having a structure expressed by the following Structural Formula (1) and a compound having a structure expressed by the following Structural Formula (2):Type: ApplicationFiled: February 23, 2011Publication date: June 16, 2011Applicant: KINKI UNIVERSITYInventors: Masayuki Igarashi, Ryutaro Utsumi
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Publication number: 20110143943Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: ApplicationFiled: February 17, 2011Publication date: June 16, 2011Applicant: Bayer AktiengesellschaftInventors: Michael RUTHER, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Patent number: 7947704Abstract: The invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I), in which CKE, W, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2,4,6-phenyl-substituted cyclic ketoenols and secondly at least one compound which improves crop plant tolerance.Type: GrantFiled: March 11, 2005Date of Patent: May 24, 2011Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Oliver Gaertzen, Klaus Kunz, Stefan Lehr, Dieter Feucht, Peter Lösel, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20110108765Abstract: A polymerizable optically-active imide compound represented by the following general formula (I). Preferable among the polymerizable optically-active imide compound are compounds wherein X3 and X4 in general formula (I) are both —CO—, compounds wherein the rings A2 and A3 in general formula (I) are both naphthalene rings, compounds wherein the rings A1, A2, A3, and A4 are all benzene rings, compounds wherein M1 and M2 in general formula (I) are both hydrogen atoms, or compounds wherein rings A1 and A4, as well as rings A2 and A3, in general formula (I) are the same ring, the groups M1 and M2, X1 and X6, X2 and X5, as well as X3 and X6 are the same group in each pair, and n and m are the same number.Type: ApplicationFiled: August 25, 2009Publication date: May 12, 2011Applicant: ADEKA CORPORATIONInventors: Satoshi Yanagisawa, Masatomi Irisawa
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Publication number: 20110105565Abstract: Provided herein are highly water soluble, thiazolidinone derivative compounds and glycine hydrazide derivative compounds that inhibit the ion transport activity of the cystic fibrosis transmembrane conductance regulator (CFTR). The compounds, and compositions comprising the compounds, described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea. The compounds may also be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.Type: ApplicationFiled: March 25, 2009Publication date: May 5, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan S. Verkman, Nitin D. Sonawane
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Publication number: 20110098336Abstract: A compound represented by the formula (I) according to claim 1 or a salt thereof has a superior androgen receptor modulating action.Type: ApplicationFiled: August 6, 2008Publication date: April 28, 2011Applicant: Takeda Pharmaceutical Company LimitedInventor: Atsushi Hasuoka
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Publication number: 20110092368Abstract: The present invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y and CKE have the meanings given in the disclosure, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention further relates to selectively herbicidal compositions containing 2,4,6-phenyl-substituted cyclic ketoenols and a compound which improves crop plant tolerance.Type: ApplicationFiled: December 17, 2010Publication date: April 21, 2011Inventors: Reiner Fischer, Klaus Kunz, Stefan Lehr, Michael Ruther, Udo Schneider, Markus Dollinger, Mark Wilhelm Drewes, Dieter Feucht, Jörg Konze, Ulrike Wachendorff-Neumann, Guido Bojack, Thomas Auler, Martin Jeffrey Hills, Thomas Bretschneider, Olga Malsam, Christoph Erdelen, Angelika Lubos-Erdelen, Alfred Angermann, Hein Kehne, Christopher Hugh Rosinger
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3-biphenyl-substituted-3-substituted-4-ketolactam and ketolactone and their utilization as pesticide
Patent number: 7928037Abstract: The present invention relates to novel 3-biphenyl-substituted, 3-substituted 4-keto-lactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y and Z are as defined in the disclosure, to processes for their preparation, and to their use as pesticides and/or microbicides and/or herbicides.Type: GrantFiled: October 23, 2007Date of Patent: April 19, 2011Assignee: Bayer CropScience AGInventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Mark Wilhelm Drewes, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Dieter Feucht, Udo Reckmann, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann -
Patent number: 7915282Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: March 21, 2001Date of Patent: March 29, 2011Assignee: Bayer AktiengesellschaftInventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Patent number: 7868188Abstract: The invention provides thiazole derivatives of formula (I), or pharmaceutically acceptable salts thereof in which Ring A, R1, R2 and R3 are as defined in the specification; a processes for their preparation; pharmaceutical compositions containing them; and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.Type: GrantFiled: November 7, 2005Date of Patent: January 11, 2011Assignee: AstraZeneca ABInventors: Malena Bengtsson, Joakim Larsson, Grigorios Nikitidis, Peter Storm, John Peter Bailey, Edward Jolyon Griffen, Jean-Claude Arnould, Thomas Geoffrey Colerick Bird
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Publication number: 20100311593Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.Type: ApplicationFiled: March 11, 2010Publication date: December 9, 2010Applicant: Bayer Cropscience AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Görgens, Jan Dittgen, Dieter Feucht, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Alfred Angermann
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Patent number: 7834051Abstract: The present invention relates to pharmaceutical agents which are agents for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia or osteoporosis; the pharmaceutical agents frailty suppressants, muscle strength enhancers, muscle increasing agents, cachexia suppressants, body weight decrease suppressants, agents for the prophylaxis or treatment of prostate hypertrophy, amyotrophy or muscle loss caused by a disease or an agent for reducing the prostate weight.Type: GrantFiled: August 6, 2008Date of Patent: November 16, 2010Assignee: Takeda Pharmaceutical Company LimitedInventor: Atsushi Hasuoka
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Patent number: 7825268Abstract: Compounds of the Formula I, wherein A1 is O or NH; A2 is O or S; each of R1 and R2 is independently hydrogen, a methyl or C2-C8-saturated or mono- or doubly unsaturated, branched or linear hydrocarbon group; and R3 is a C1-C18-saturated or mono- or doubly unsaturated, branched or linear hydrocarbon group wherein, each of R1, R2 and R3 comprises a heteroatom selected from the group consisting of O and S in the chain and/or is mono- or multiply-substituted by a substituent selected from the group consisting of halogen, hydroxy, C1-C6-alkyl, trifluoromethyl, C1-C6-alkoxy, C6-C10-aryl, and C1-C6-alkyl-C6-C10-aryl are useful for controlling the interaction process between microorganisms such as in the development and/or maturation of biofilms; multicellular swarm behavior; the concerted development of antibiotic resistances; the concerted synthesis of antibiotics; the concerted synthesis of pigments; the concerted production of extracellular enzymes; or the concerted production of virulence factors.Type: GrantFiled: June 22, 2006Date of Patent: November 2, 2010Assignee: Henkel AG & Co. KGaAInventors: Stefan Stumpe, Roland Breves, Ursula Huchel, Frank Janssen, André Hätzelt
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Patent number: 7812178Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.Type: GrantFiled: November 3, 2008Date of Patent: October 12, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masakazu Fujio, Hiroyuki Satoh, Shinya Inoue, Toshifumi Matsumoto, Yasuhiro Egi
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Patent number: 7799823Abstract: The present invention is directed to a new class of benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.Type: GrantFiled: November 7, 2006Date of Patent: September 21, 2010Assignee: Warner-Lambert Company LLCInventors: Stephen Douglas Barrett, Victor Fedij, Lain-Yen Hu, Donna M Iula, Bruce A Lefker, Raj Kumar Raheja, Karen Sexton, Jennifer Ann Van Camp
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Patent number: 7786119Abstract: This invention is directed to drug conjugates of certain ion channel modulating compounds having the following formula: wherein A, X, R1, R2, R3, R4, R5, LB, L and DM are defined herein, including isolated enantiomeric and diastereomeric isomers thereof, and mixtures thereof. Pharmaceutical compositions and methods of use are also disclosed.Type: GrantFiled: March 31, 2005Date of Patent: August 31, 2010Assignee: Cardiome Pharma Corp.Inventors: Elizabeth L. S. Cheu, Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Alan M. Ezrin, Grace Jung, Bertrand M. C. Plouvier, Aregahegn S. Yifru
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Publication number: 20100215574Abstract: The invention relates to a method for producing injectable medicament preparations containing a therapeutically and/or diagnostically effective substance which is comprised of an active agent, of a spacer molecule and of at least one protein-binding molecule. After being brought into contact with the body, said therapeutically and/or diagnostically effective substance covalently bonds to the body fluid constituents or tissue constituents via the protein-binding molecule, thus providing a form of transport of the active agent that an be hydrolytically or enzymatically cleaved, according to pH, in the body while releasing the active agent.Type: ApplicationFiled: October 22, 2009Publication date: August 26, 2010Inventor: FELIX KRATZ
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Publication number: 20100217014Abstract: This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R3, R4 and R5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.Type: ApplicationFiled: February 19, 2010Publication date: August 26, 2010Applicant: CARDIOME PHARMA CORP.Inventors: Grace Jung, James Gee Ken Yee, Doug Ta Hung Chou, Bertrand M. C. Plouvier
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Patent number: 7776791Abstract: The invention relates to novel N-heterocyclylphenyl-substituted cyclic ketoenols of the formula (I) in which CKE, W, X, Y and Z are as defined in the disclosure, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides. The invention further relates to selective herbicidal compositions comprising firstly the N-heterocyclylphenyl-substituted cyclic ketoenols and secondly a compound which improves crop plant tolerance.Type: GrantFiled: June 7, 2004Date of Patent: August 17, 2010Assignee: Bayer CropScience AGInventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Stefan Lehr, Klaus Kunz, Jörg Konze, Olga Malsam, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann, Wahed Ahmed Moradi, Guido Bojack, Thomas Auler, Martin Hills, Heinz Kehne
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Publication number: 20100184730Abstract: The invention relates to fatty acid acylated salicylate derivatives; compositions comprising an effective amount of a fatty acid acylated salicylate derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a fatty acid acylated salicylate derivative.Type: ApplicationFiled: February 26, 2010Publication date: July 22, 2010Inventors: Chi B. Vu, Jean E. Bemis, Michael R. Jirousek, Jill C. Milne, Jesse J. Smith
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Publication number: 20100184764Abstract: The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Formula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.Type: ApplicationFiled: March 19, 2010Publication date: July 22, 2010Applicant: ELI LILLY AND COMPANYInventors: Thomas Daniel AICHER, Mark Joseph CHICARELLI, Ronald Jay HINKLIN, Hongqi TIAN, Owen Brendan WALLACE, John Gordon ALLEN, Zhaogen CHEN, Thomas Edward MABRY, Jefferson Ray MCCOWAN, Nancy June SNYDER, Leonard Larry WINNEROSKI, JR.
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Publication number: 20100174084Abstract: The invention relates to novel 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) in which A, B, D, G, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant tolerance promoter compound.Type: ApplicationFiled: March 16, 2010Publication date: July 8, 2010Applicant: Bayer CropScience AGInventors: Reiner FISCHER, Stefan Lehr, Mark Wilhelm Drewes, Dieter Feucht, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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3-Biphenyl-substituted-3-substituted-4-ketolactam and ketolactone and their utilization as pesticide
Publication number: 20100173778Abstract: The present invention relates to novel 3-biphenyl-substituted, 3-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y and Z are as defined in the disclosure, to processes for their preparation, and to their use as pesticides and/or microbicides and/or herbicides.Type: ApplicationFiled: October 23, 2007Publication date: July 8, 2010Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Mark Wilhelm Drewes, Christoph Erdelen, Angelika Lubos-Erdelen, Dieter Feucht, Udo Reckmann, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann -
Publication number: 20100152464Abstract: Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed.Type: ApplicationFiled: November 18, 2005Publication date: June 17, 2010Applicant: CARDIOME PHARMA CORP.Inventors: Bertrand M. C. Plouvier, Doug Ta Hung Chou, Grace Jung, Lewis Siu Leung Choi, Tao Sheng, Anthony G. M. Barrett, Marco S. Passafaro, Martin Kurz, Daniel Moeckli, Pirmin Ulmann, Alfred Hedinger
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Publication number: 20100143500Abstract: A method of treating a glial cell related disorder in a mammalian subject includes administering a drug which enhances or prolongs GSK-3 ? or ? inactivation.Type: ApplicationFiled: October 31, 2007Publication date: June 10, 2010Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Sean E. Lawler, Michal Oskar Nowicki, E. Antonio Chiocca
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Patent number: 7727933Abstract: The invention relates to novel 2-ethyl-4,6-dimethylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) in which A, B and G are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2-ethyl-4,6-dimethylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) (where G may also be hydrogen) and secondly at least one crop plant compatibility-improving compound.Type: GrantFiled: November 9, 2004Date of Patent: June 1, 2010Assignee: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Mark Wilhelm Drewes, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Dieter Feucht, Jörg Konze, Peter Lösel, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger
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Patent number: RE43038Abstract: A compound represented by the general formula (I): (I) wherein R represents linear, branched, or cyclic alkyl or aryl; a process for producing the compound; and an antitumor agent containing the compound as an active ingredient.Type: GrantFiled: June 6, 2003Date of Patent: December 20, 2011Assignee: RikenInventors: Hiroyuki Osada, Hideaki Kakeya, Yujiro Hayashi