Spiro Ring System Patents (Class 514/409)
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Publication number: 20100204224Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels.Type: ApplicationFiled: July 7, 2006Publication date: August 12, 2010Applicant: VERNALIS R & D LIMITEDInventors: Richard Hamlyn, Glyn Addison, Christopher Geoffrey Earnshaw, Harry Finch, Mike Huckstep, Rosemary Lynch, Sarah Mellor
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Publication number: 20100197645Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.Type: ApplicationFiled: February 2, 2010Publication date: August 5, 2010Applicant: Wyeth LLCInventor: Bogdan Kazimierz Wilk
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Publication number: 20100190764Abstract: This invention relates to novel Spiro cyclopentane derivatives of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.Type: ApplicationFiled: July 24, 2008Publication date: July 29, 2010Inventors: Emiliano Castiglioni, Romano Di Fabio, Massimo Gianotti, Milan Mesic, Francesca Pavone, Slavko Rast, Luigi Piero Stasi
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Publication number: 20100190688Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.Type: ApplicationFiled: July 12, 2005Publication date: July 29, 2010Inventors: Bin Chao, Thomas L. Deckwerth, Paul S. Furth, Steven D. Linton, Alfred P. Spada, Brett R. Ullman, Michael I. Weinhouse
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Patent number: 7763635Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.Type: GrantFiled: August 17, 2007Date of Patent: July 27, 2010Assignee: Supermus Pharmaceuticals, Inc.Inventors: Argaw Kidane, Henry H. Flanner, Padmanabh Bhatt, Arash Raoufinia
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Patent number: 7759359Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.Type: GrantFiled: August 17, 2007Date of Patent: July 20, 2010Assignee: Supernus Pharmaceuticals, Inc.Inventors: Argaw Kidane, Henry H. Flanner, Padmanabh Bhatt, Arash Raoufinia
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Patent number: 7759383Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: GrantFiled: February 22, 2006Date of Patent: July 20, 2010Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
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Publication number: 20100173967Abstract: This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of hypercholesterolemia, benign prostatic hyperplasia, pruritis and cancer.Type: ApplicationFiled: October 12, 2007Publication date: July 8, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Rajender Kamboj, Duanjie Hou, Shifeng Liu, Mehran Seid Bagherzadeh, Serguei Sviridov, Shaoyi Sun, Jianyu Sun, Nagasree Chakka, Tom Hsieh, Vandna Raina
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Publication number: 20100168090Abstract: The novel active compound combinations comprising compounds of the formula (I-1) or (I-2) and the agonists or antagonists of nicotinergic acetylcholine receptors listed in the description have very good insecticidal and/or acaricidal properties.Type: ApplicationFiled: July 6, 2007Publication date: July 1, 2010Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Wolfram Andersch, Thomas König, Anton Kraus, Emmanuel Salmon, Heike Hungenberg
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Publication number: 20100150866Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: December 10, 2009Publication date: June 17, 2010Inventors: Alan Xiangdong Wang, Paul Michael Scola
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Publication number: 20100137299Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 13, 2009Publication date: June 3, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Publication number: 20100137270Abstract: A variety of diseases and disorders associated with the metabolic pathways involved in the activities of cyclooxygenase and the synthesis of prostaglandins, for example type 2 diabetes mellitus and its sequelae, ischemic vascular diseases, pain associated with inflammation, inflammatory skin conditions, spinal cord injury, peripheral neuropathy, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis, as well as various types of cancer may be treated or prevented by the use of an agent which selectively enhances production of 15-deoxy-prostaglandin J2.Type: ApplicationFiled: November 29, 2007Publication date: June 3, 2010Applicant: Hunter-Fleming LimitedInventor: Ernst Wülfert
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Publication number: 20100137284Abstract: The combination of nitric oxide generating compounds which are not dependent upon aldehyde dehydrogenase for bioactivation, or are specifically targeted to nNOS or the sarcoplasmic reticulum of cardiac muscle cells, and xanthine oxidase inhibitors are effective in the treatment of heart disease, specifically congestive heart failure and ischemic coronary disease. This treatment is particularly effective in patients who have particularly heavy oxidative burdens, e.g. diabetics, patients with lung disorders, patients with sickle cell anemia and patients of Asian descent.Type: ApplicationFiled: June 25, 2009Publication date: June 3, 2010Inventors: Jonathan S. Stamler, Gregory T. Went
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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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Publication number: 20100130487Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: ApplicationFiled: December 30, 2009Publication date: May 27, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Raina, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20100130578Abstract: The new active compound combinations comprising compounds of the formula (I) and the active compounds (1) to (3) recited in the description possess very good insecticidal and/or acaricidal properties.Type: ApplicationFiled: July 11, 2007Publication date: May 27, 2010Inventors: Reiner Fischer, Wolfram Andersch, Thomas Bretschneider, Anton Kraus, Heike Hungenberg, Olga Malsam
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Patent number: 7723372Abstract: There are provided compounds of the general formulas wherein W, X, Y, R1, R2, R3, and R4 are as described herein. The compounds exhibit anticancer activity.Type: GrantFiled: February 18, 2009Date of Patent: May 25, 2010Assignee: Hoffman-La Roche Inc.Inventor: Jin-Jun Liu
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Publication number: 20100125072Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: ApplicationFiled: December 30, 2009Publication date: May 20, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Raina, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20100113437Abstract: The novel active compound combinations comprising compounds of the formula (I) or (II) and active compounds (1) to (30) listed in the description have very good insecticidal and acaricidal properties.Type: ApplicationFiled: July 6, 2007Publication date: May 6, 2010Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Wolfram Andersch, Thomas König, Anton Kraus, Emmanuel Salmon, Heike Hungenberg
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Publication number: 20100113436Abstract: A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=—C(O)NR1R2, —NR1R2 or —S(O)2R4, where R1, R2 and R4 are each individually selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring, or any combination thereof, or R1 and R2 are linked so as to form part of a substituted or unsubstituted heterocyclic ring, or X=N and Y=—S(O)2R3 or —C(O)R3, where R3 is selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring or any combination thereof.Type: ApplicationFiled: October 1, 2007Publication date: May 6, 2010Inventors: Richard Amewu, Paul Micheal O'Neill, Andrew Stachulski, Gemma Ellis, Stephen Andrew Ward
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Publication number: 20100099728Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 13, 2009Publication date: April 22, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Zenova
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Publication number: 20100099717Abstract: It is possible to increase the uptake of active compounds from crop protection compositions using suitable adjuvants, and thus to improve the action of crop protection agents. The present invention describes suitable adjuvants, methods and compositions.Type: ApplicationFiled: September 18, 2007Publication date: April 22, 2010Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Ronald Vermeer, Peter Baur, Heike Hungenberg, Wolfgang Thielert, Udo Reckmann, Peter Marczok, Isidro Bailo-Schleiermacher
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Patent number: 7700641Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: GrantFiled: April 11, 2006Date of Patent: April 20, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Raina, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20100087320Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: ApplicationFiled: November 12, 2009Publication date: April 8, 2010Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark-Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
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Publication number: 20100063087Abstract: Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R ; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.Type: ApplicationFiled: September 14, 2006Publication date: March 11, 2010Applicant: SPEEDEL EXPERIMENTA AGInventor: Peter HEROLD
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Publication number: 20100056598Abstract: The invention relates to a plurality of processes for the preparation of novel cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives of the formula (I) in which A, G, X and Y are as defined in the disclosure.Type: ApplicationFiled: November 10, 2009Publication date: March 4, 2010Inventors: Thomas Himmler, Reiner Fisher, Bernd Gallenkamp, Hans-Joachim Knops, Lubbertus Mulder, Reinhard Lantzsch, Christoph Erdelen, Angelika Lubos-Erdelen, Jorg Konze, Ralf Nauen, Olga Malsam, Christian Arnold
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Publication number: 20100048661Abstract: The novel active compound combinations consisting, firstly, of cyclic ketoenols and, secondly, of beneficial species (natural enemies) have very good insecticidal and/or acaricidal properties.Type: ApplicationFiled: June 5, 2007Publication date: February 25, 2010Applicant: Bayer CropScience AGInventors: Reiner Fischer, Heike Hungenberg, Ralf Nauen, Hans-Jürgen Schnorbach, Wolfgang Thielert
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Publication number: 20100041710Abstract: Methods for enhancing penetration of agrochemical active substances through the cuticle of a plant are disclosed. Also disclosed are compositions comprising at least one penetration enhancer.Type: ApplicationFiled: December 7, 2007Publication date: February 18, 2010Applicant: BAYER CROPSCIENCE AGInventors: Peter Baur, Ronald Vermeer, Rainer Suessmann
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Patent number: 7659300Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and 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: September 6, 2005Date of Patent: February 9, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump
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Patent number: 7655686Abstract: The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4.4]non-7-yl)-propionamides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.Type: GrantFiled: June 26, 2007Date of Patent: February 2, 2010Assignee: Novartis AGInventors: Yves Auberson, Ralf Glatthar, Rhys Salter, Oliver Simic, Marina Tintelnot-Blomley
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Publication number: 20100016399Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R1, R2, R3, R4, R5, R6, R7, R8, R21 and m are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further discloses pharmaceutical compositions and combinations comprising the compounds.Type: ApplicationFiled: January 30, 2008Publication date: January 21, 2010Inventors: Nadia Mamoona Ahmad, Albert Andrzej Jaxa-Chamiec, Justine Yeun Quai Lai, Roderich Alan Porter
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Publication number: 20100010051Abstract: The present invention relates to novel suspension concentrates of certain agrochemically active compounds, to a process for preparing these formulations and to their use for applying the active comprised therein.Type: ApplicationFiled: September 18, 2007Publication date: January 14, 2010Applicant: BAYER CROPSCIENCE AGInventors: Ronald Vermeer, Peter Baur
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Publication number: 20100009850Abstract: The invention relates to novel iodophenyl-substituted cyclic ketenols of the formula (I) in which CKE, J, 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 iodophenyl-substituted cyclic ketonols of the formula (I) and secondly at least one crop plant compatibility-improving compound.Type: ApplicationFiled: September 13, 2005Publication date: January 14, 2010Inventors: Reiner Fischer, Thomas Bretschneider, Kerstin Ilg, Stefan Lehr, Dieter Feucht, Olga Malsam, Udo Rechkmann, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Waltraud Hempel, Erich Sanwald
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Publication number: 20100004215Abstract: Provided herein are pharmaceutical compositions comprising one or more phosphodiesterase inhibitors of type IV (“PDE-IV”), and at least one other active ingredient such as muscarinic receptor antagonists (MRA), ?2-agonists, p38 MAP Kinase inhibitors, or corticosteroids and optionally one or more pharmaceutically acceptable excipients. In addition, methods of treating autoimmune, inflammatory or allergic diseases or disorders are provided.Type: ApplicationFiled: April 25, 2008Publication date: January 7, 2010Inventors: Abhijit Ray, Sunanda G. Dastidar, Rajkumar Shirumalla, Suman Gupta
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Publication number: 20100004127Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D, Q1, Q2 and G are as defined above, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides and/or fungicides and also to selective herbicidal compositions comprising, firstly, the 3?-alkoxyspirocyclopentyl-substituted tetramic and tetronic acids of the formula (I) and, secondly, at least one crop plant compatibility-improving compound, and also to boosting the activity of crop protection compositions comprising active compounds from the class of the 3?-alkoxyspirocyclopentyl-substituted tetramic and tetronic acids of the formula (I) by adding ammonium salts and/or phosphonium salts or by adding ammonium salts and/or phosphonium salts and penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection.Type: ApplicationFiled: December 11, 2006Publication date: January 7, 2010Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Eva-Maria Franken, Olga Malsam, Guido Bojack, Christian Arnold, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger, Jan Dittgen
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Publication number: 20090326032Abstract: The present invention relates to pharmaceutical compositions comprising an NK1 receptor antagonist and a sodium channel blocker compound of formula (I) wherein R1 and R2 are independently hydrogen, C1-6alkyl or C3-6cycloalkylC1-6alkyl; or R1 and R2, together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; R3 is C1-6alkyl, C1-6haloalkyl, C1-3alkoxyC1-3alkyl or C1-3haloalkoxyC1-3alkyl; or R1 and R3, together with the interconnecting atoms, form a saturated or unsaturated 4- to 6-membered ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R4 is independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; q is 1 or 2; either R5 or R6 is —O—R7 or —OCH2R7, wherein the other R5 or R6 is hydrogen or R4; and wherein R7 is either a phenyl ring or a 5- or 6-membered aromatic heterocyclic ring (independently containing one or more nitrogen, sulphur or oxygenType: ApplicationFiled: January 21, 2008Publication date: December 31, 2009Applicant: GLAXO GROUP LIMITEDInventors: Giuseppe Alvaro, Charles Large
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Publication number: 20090326015Abstract: The present invention relates to a compound having benzopyran core, a preparation method of the derivatives by liquid phase synthesis and solid phase synthesis through diversity-oriented synthesis, and an anticancer agent comprising the compound that exhibit excellent cytotoxicity against cancer cells.Type: ApplicationFiled: June 9, 2009Publication date: December 31, 2009Applicant: SNU R&DB FoundationInventors: Seung Bum Park, Hwan Jong Jang, Sung Kon Ko, EunHa Kim, Sangmi Oh, Jongmin Park
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Patent number: 7638547Abstract: The invention relates to novel cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives of the formula (I) in which A, G, X and Y are as defined in the disclosure, to a plurality of processes for their preparation and to their use as pesticides.Type: GrantFiled: July 1, 2003Date of Patent: December 29, 2009Assignee: Bayer CropScience AGInventors: Thomas Himmler, Reiner Fischer, Bernd Gallenkamp, Hans-Joachim Knops, Lubbertus Mulder, Reinhard Lantzsch, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Jörg Konze, Ralf Nauen, Olga Malsam, Christian Arnold
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Patent number: 7638548Abstract: There are provided compounds of the general formulas wherein X, Y, R1, R2, R3 and R4 are as described herein. The compounds exhibit anticancer activity.Type: GrantFiled: October 4, 2007Date of Patent: December 29, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Jin-Jun Liu, Zhuming Zhang
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Patent number: 7632953Abstract: The present invention provides an improved process for the preparation of gabalactam of formula 1 that includes preparing an aqueous solution of an alkali or alkaline earth metal hydroxide, adding bromine to the resulting solution to give an appropriate alkali or alkaline earth metal hypobromite; adding an amide of the formula 4 aging the resultant mixture; heating the mixture to a temperature in a range of 80 to 100 degrees C.; extracting with nonpolar solvent and distilling under reduced pressure to obtain gabalactam.Type: GrantFiled: November 20, 2002Date of Patent: December 15, 2009Assignee: Hikal LimitedInventors: Nagarajan Kuppuswamy, Sivaramakrishnan Hariharan, Arulselvan Mariadas
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Publication number: 20090306147Abstract: In soil applications, the action of crop protection compositions comprising active compounds from the classes of the neonicotinoids, the pyrethroids, the butenolides, the ketoenols, the phenylpyrazoles or the fungicides can be improved by adjuvants. The present invention describes corresponding methods and suitable compositions.Type: ApplicationFiled: September 18, 2007Publication date: December 10, 2009Applicant: Bayer CropScience AGInventors: Peter Marczok, Peter Baur, Ronald Vermeer, Wolfgang Thielert, Heike Hungenberg, Kai-Uwe Brueggen, Dirk Ebbinghaus, Peter Losel, Udo Reckmann
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Publication number: 20090298903Abstract: An improved miniature portable child's training toilet comprises a first chamber with a toilet seat opening, a second chamber connected thereto, and a flap member at a connection point. A miniaturized tank portion with valve means and means of selectively causing the valve to open, allows fluid from the tank to move under gravity to the first chamber and continue into the second chamber, flushing material into the second chamber of the toilet. A means of separating the first and second chambers of the toilet for emptying the second chamber after flushing comprises a gasket for sealing the junction of the chambers. An electronic sound and light producing means plays congratulatory sounds and causes the toilet to illuminate when flushed. An alternate embodiment further comprises an “S” bend connecting the chambers, forming a water trap, and causing siphon action when the toilet is flushed.Type: ApplicationFiled: May 9, 2007Publication date: December 3, 2009Inventors: Reiner Fischer, Ernst Brueck, Xavier Alain Marie Van Waetermeulen
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Publication number: 20090298808Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: January 6, 2009Publication date: December 3, 2009Inventors: Wenqing Yao, Chunhong He, Jingcong Zhuo
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Publication number: 20090286788Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (29) listed in the disclosure.Type: ApplicationFiled: July 22, 2009Publication date: November 19, 2009Inventors: Reiner Fischer, Christoph Erdelen
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Publication number: 20090281157Abstract: The novel active compound combinations comprising compounds of the formula (I) or (II) and active compounds (1) to (23) listed in the description have very good insecticidal and acaricidal properties.Type: ApplicationFiled: July 6, 2007Publication date: November 12, 2009Applicant: Bayer Cropscience AGInventors: Reiner Fischer, Wolfram Andersch, Thomas König, Anton Kraus, Emmanuel Salmon, Heike Hungenberg
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Publication number: 20090275560Abstract: The invention relates to organic compounds which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi and parasites of the Leishmania genus such as, for example, Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.Type: ApplicationFiled: April 27, 2009Publication date: November 5, 2009Applicant: NOVARTIS AGInventors: Shi Hua ANG, Philipp KRASTEL, Seh Yong LEONG, Liying Jocelyn TAN, Wei Lin Josephine WONG, Bryan K.S YEUNG, Bin ZOU
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Publication number: 20090247505Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.Type: ApplicationFiled: March 25, 2009Publication date: October 1, 2009Applicant: Grunenthal GMBHInventors: Saskia ZEMOLKA, Stefan SCHUNK, Klaus LINZ, Wolfgang SCHRODER, Werner ENGLBERGER, Fritz THEIL, Birgit ROLOFF
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Publication number: 20090247561Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.Type: ApplicationFiled: March 25, 2009Publication date: October 1, 2009Applicant: Grunenthal GmbHInventors: Saskia Zemolka, Bert Nolte, Sven Frorman, Claudia Hinze, Klaus Linz, Wolfgang Schroder, Werner Englberger, Hans Schick, Helmut Sonnenschein
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Publication number: 20090239889Abstract: There are provided compounds of the general formulas wherein W, X, Y, R1, R2, R3, and R4 are as described herein. The compounds exhibit anticancer activity.Type: ApplicationFiled: February 18, 2009Publication date: September 24, 2009Inventor: Jin-Jun Liu
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Publication number: 20090233952Abstract: [Object] To provide a substituted cycloalkene derivative having an action to suppress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-?, pharmacologically acceptable salts therefor, a medicament containing them as an active ingredient, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.Type: ApplicationFiled: September 13, 2006Publication date: September 17, 2009Inventors: Tomio Kimura, Nobuyuki Ohkawa, Takayoshi Nagasaki, Atsuhiro Sugidachi, Osamu Ando