Spiro Ring System Patents (Class 514/409)
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Publication number: 20130065931Abstract: Methods and compositions for controlling pests of the order Coleoptera are described herein. Methods of reducing wireworm damage in potatoes by applying a compound or composition disclosed herein in a foliar treatment is also described.Type: ApplicationFiled: September 21, 2012Publication date: March 14, 2013Inventors: John Bell, Kelvan R. Luff, Philip John Sarasqueta
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Publication number: 20130065882Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxyType: ApplicationFiled: October 3, 2012Publication date: March 14, 2013Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
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Publication number: 20130065877Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: ApplicationFiled: November 6, 2012Publication date: March 14, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130059874Abstract: The present disclosure relates to a series of substituted N-phenyl spirolactam bipyrrolidines of formula (I). wherein R1, R2, R3, R4, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-phenyl spirolactam bipyrrolidines of formula (I) and intermediates therefor.Type: ApplicationFiled: November 6, 2012Publication date: March 7, 2013Applicant: SANOFIInventor: Sanofi
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Publication number: 20130053377Abstract: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.Type: ApplicationFiled: February 23, 2011Publication date: February 28, 2013Applicant: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh Singh, Yajun Zheng
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Publication number: 20130040935Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.Type: ApplicationFiled: February 8, 2011Publication date: February 14, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
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Publication number: 20130023504Abstract: 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: August 3, 2012Publication date: January 24, 2013Applicant: HUNTER-FLEMING LIMITEDInventor: ERNST WULFERT
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Publication number: 20130018067Abstract: The present invention relates to novel polycyclic pyrrolidine-2,5-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: July 3, 2012Publication date: January 17, 2013Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Vu, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8354443Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1. The compound may be used, for example, for the treatment or prophylaxis of obesity, hyperglycemia, dyslipidemia, and type 1 or type 2 diabetes.Type: GrantFiled: December 3, 2010Date of Patent: January 15, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Hongying Yun
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Publication number: 20130012563Abstract: Crystalline forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine, pharmaceutical compositions and medicaments comprising these crystalline modifications, the use of these modifications as well as a process for the enrichment of such crystalline modifications.Type: ApplicationFiled: July 6, 2012Publication date: January 10, 2013Applicant: Gruenenthal GmbHInventors: Michael Gruss, Stefan Kluge, Stefan Pruehs
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Patent number: 8334300Abstract: 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 24, 2011Date of Patent: December 18, 2012Assignee: Bayer AktiengesellshaftInventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christophe Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Patent number: 8324235Abstract: The patent application relates to new heterocyclic compounds of the general formula (I), in which R, R1, R2, Q, T, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.Type: GrantFiled: March 27, 2008Date of Patent: December 4, 2012Assignee: Novartis AGInventors: Peter Herold, Robert Mah, Stefan Stutz, Vincenzo Tschinke, Aleksandar Stojanovic, Nathalie Jotterand, Bibia Bennacer
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Publication number: 20120302540Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
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Publication number: 20120295897Abstract: 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: July 25, 2012Publication date: November 22, 2012Applicant: 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 Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Publication number: 20120289494Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: May 11, 2012Publication date: November 15, 2012Applicants: Sanofi, The Regents of the University of MichiganInventors: Shaomeng Wang, Wei Sun, Angelo Aguilar, Carlos Garcia-Echeverria
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Patent number: 8309594Abstract: Methods for purifying a compound of formula I are provided, wherein A, B, X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.Type: GrantFiled: February 12, 2009Date of Patent: November 13, 2012Assignee: Wyeth LLCInventors: Bogdan Kazimierz Wilk, Arkadiy Zinoviy Rubezhov, Anthony Francis Hadfield, Jean Louise Helom
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Patent number: 8299058Abstract: The use of a compound of formula I, wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; R?, R2, R3, R4, R8 and Ra are specified organic groups and p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2, 3, 4, 5 or 6; provided that when p is 2 then q is not 2; p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof or compositions containing them and their using in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: GrantFiled: December 9, 2004Date of Patent: October 30, 2012Assignee: Syngenta Crop Protection LLCInventors: Jérôme Cassayre, Louis-Pierre Molleyres, Peter Maienfisch, Fredrik Cederbaum
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Publication number: 20120270881Abstract: Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the ?-catenin-dependent “canonical” Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.Type: ApplicationFiled: August 3, 2010Publication date: October 25, 2012Applicant: POLYPHOR AGInventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Franck Lach, Anatol Luther, Karsten Marx, Kerstin Möhle
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Patent number: 8293758Abstract: 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: GrantFiled: March 25, 2009Date of Patent: October 23, 2012Assignee: Grunenthal GmbHInventors: Saskia Zemolka, Bert Nolte, Sven Frormann, Claudia Hinze, Klaus Linz, Wolfgang Schröder, Werner Englberger, Hans Schick, Helmut Sonnenschein
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Publication number: 20120264738Abstract: A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.Type: ApplicationFiled: March 9, 2012Publication date: October 18, 2012Inventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
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Patent number: 8288431Abstract: There is provided a compound of the formula wherein X, Y, W, R1, R2 and R3 are as described herein. The compounds have activity as anticancer agents.Type: GrantFiled: January 19, 2011Date of Patent: October 16, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Jin-Jun Liu, Jing Zhang, Zhuming Zhang
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Patent number: 8288430Abstract: 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: GrantFiled: March 25, 2009Date of Patent: October 16, 2012Assignee: Grunenthal GmbHInventors: Saskia Zemolka, Stefan Schunk, Klaus Linz, Wolfgang Schröder, Werner Englberger, Fritz Theil, Birgit Roloff
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Publication number: 20120258949Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: April 13, 2012Publication date: October 11, 2012Applicant: DAC S.r.I.Inventors: Mario Varasi, Florian Thaler, Raffaella Amici, Agnese Abate, Maria Carmela Fulco, Saverio Minucci, Ciro Mercurio
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Publication number: 20120245191Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: March 19, 2012Publication date: September 27, 2012Inventors: Daniel Hunziker, Werner Neidhart
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Publication number: 20120238594Abstract: The invention provides novel compounds having the general formula (I) wherein R1 and R2 are as described herein, compositions including the compounds, their pharmaceutically acceptable salts and esters and methods of using the compounds.Type: ApplicationFiled: March 8, 2012Publication date: September 20, 2012Inventors: Daniel Hunziker, Werner Neidhart
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Publication number: 20120238613Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and R3 are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: March 8, 2012Publication date: September 20, 2012Inventors: Daniel Hunziker, Werner Neidhart
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Publication number: 20120225873Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.Type: ApplicationFiled: April 13, 2012Publication date: September 6, 2012Applicant: Myrexis, Inc.Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
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Publication number: 20120220558Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.Type: ApplicationFiled: May 8, 2012Publication date: August 30, 2012Applicant: Wyeth LLCInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
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Patent number: 8247351Abstract: The present invention concerns boosting the activity of crop protection materials comprising active ingredients from the class of the 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: GrantFiled: December 11, 2006Date of Patent: August 21, 2012Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Stefan Lehr, Peter Marczok, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich Sanwald, Rolf Pontzen
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Patent number: 8236963Abstract: The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity.Type: GrantFiled: May 23, 2006Date of Patent: August 7, 2012Assignee: Merck Serono SAInventors: Matthias Schwarz, Eric Sebille, Christophe Cleva, Cedric Merlot, Dennis Church, Patrick Page, Jacqueline A. Macritchie, John Frederick Atherall, Stefano Crosignani, Doris Pupowicz
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Patent number: 8222288Abstract: 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: June 14, 2010Date of Patent: July 17, 2012Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Dongguang Qin, Jianyong Chen, Shanghai Yu
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Publication number: 20120178786Abstract: Compounds of the formula (I) in which A, B, G, W, X, Y and Z can have the meanings given in the description are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.Type: ApplicationFiled: September 23, 2008Publication date: July 12, 2012Inventors: Thomas E. Macom, Reiner Fischer, Gerhard Baron, Erich Sanwald, Reed Nathan Royalty, Xavier Alain Marie Van Waetermeulen, Udo Reckmann, Alexandra Gladbach, Stephen Krueger, Peter Marczok
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Patent number: 8217051Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, R1, R2 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.Type: GrantFiled: January 7, 2010Date of Patent: July 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Jing Zhang, Zhuming Zhang
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Patent number: 8216971Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance.Type: GrantFiled: December 21, 2007Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Koen van Den Eynde, Wolfgang Thielert, Heike Hungenberg
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Patent number: 8217052Abstract: The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I): wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed.Type: GrantFiled: June 2, 2011Date of Patent: July 10, 2012Assignee: SanofiInventors: Zhongli Gao, Ryan Hartung, David Stefany
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Patent number: 8211932Abstract: The present application describes organic compounds of the Formula I that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: September 10, 2010Date of Patent: July 3, 2012Assignee: Novartis AGInventors: Michael Patane, Prakash Raman, David Thomas Parker, Jiping Fu, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brandl, Francois Lenoir, Pascal Rigollier, Oliver Simic
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Patent number: 8211931Abstract: 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: GrantFiled: June 5, 2007Date of Patent: July 3, 2012Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Heike Hungenberg, Ralf Nauen, Hans-Jürgen Schnorbach, Wolfgang Thielert
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Publication number: 20120157432Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: August 17, 2010Publication date: June 21, 2012Applicant: Merck Sharp & Dohme, Corp.Inventors: Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent j. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
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Patent number: 8202875Abstract: The present invention relates to the use of selective insecticidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising (a) at least one compound of the formula (I) in which CKE, W, X, Y and Z are as defined in the description, and (b) at least one crop plant compatibility-improving compound, from the group of compounds mentioned in the description, for controlling insects and/or arachnids, and to a method for controlling insects and/or arachnids using the compositions.Type: GrantFiled: July 18, 2005Date of Patent: June 19, 2012Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Udo Reckmann, Christopher Hugh Rosinger, Erich Sanwald, Christian Arnold
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Publication number: 20120135996Abstract: Disclosed is a cytoprotective agent for use with respect to ischemic damage, including as an active ingredient a triprenyl phenol compound represented by the following general formula (I), wherein X is —CHY—C(CH3)2Z, Y and Z are each independently —H or —OH, or jointly form a single bond, and R represents a hydrogen atom or a substituent with a molecular weight of 1000 or less.Type: ApplicationFiled: February 5, 2010Publication date: May 31, 2012Inventors: Kazuo Honda, Terumasa Hashimoto, Keita Shibata, Keiko Hasegawa, Keiji Hasumi
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Publication number: 20120129833Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system.Type: ApplicationFiled: August 19, 2011Publication date: May 24, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ningshu LIU, Kai Thede, Philip Lienau, Arne Scholz, Maher Najjar, Ulf Bomer, Knut Eis, Reiner Fischer
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Publication number: 20120122696Abstract: The invention is directed to the use of oil based suspension concentrates containing a) at least one agrochemical active compound which is solid at room temperature, b) at least one penetration enhancer, c) at least one vegetable or mineral or paraffin oil, d) at least one non-ionic surfactant or dispersing agent and/or at least one anionic surfactant or dispersing agent and e) optionally one or more other additives for the reduction of the drift of a spray liquid containing the oil-based suspension concentrate during spray application.Type: ApplicationFiled: May 16, 2011Publication date: May 17, 2012Applicant: Bayer CropScience AGInventors: Ronald Vermeer, Andrew Charles Chapple, Reinhard Frießleben
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Publication number: 20120122947Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicants: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, SANOFI, ASCENTA THERAPEUTICS, INC.Inventors: Shaomeng Wang, Yujun Zhao, Wei Sun, Sanjeev Kumar, Lance Leopold, Laurent Debussche, Cedric Barriere, Jean-Christophe Carry, Kwame Amaning
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Publication number: 20120122909Abstract: 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: April 1, 2011Publication date: May 17, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Ralna, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
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Publication number: 20120115841Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: ApplicationFiled: May 17, 2010Publication date: May 10, 2012Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20120101092Abstract: 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: ApplicationFiled: December 23, 2011Publication date: April 26, 2012Applicant: 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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Patent number: 8153623Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.Type: GrantFiled: August 4, 2010Date of Patent: April 10, 2012Assignee: Convergence Pharmaceuticals LimitedInventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Patent number: 8143193Abstract: The novel active compound combinations of cyclic ketoenols of the formula (I) and the active compounds of the formula (II) listed in the description have very good insecticidal and acaricidal properties.Type: GrantFiled: June 25, 2004Date of Patent: March 27, 2012Assignee: Bayer CropScience AGInventors: Reiner Fischer, Rüdiger Fischer, Christian Funke, Wolfgang Thielert
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Patent number: 8138119Abstract: The invention relates to novel alkoxyalkyl spirocyclic tetramic and tetronic acids of the formula (I), in which A, B, D, Q1, Q2, Q3, Q4, G, W, 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/or microbicides, and also to selective herbicidal compositions comprising, firstly, the alkoxyalkyl spirocyclic tetramic and tetronic acids and, secondly, at least one crop plant compatibility-improving compound.Type: GrantFiled: October 20, 2006Date of Patent: March 20, 2012Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Dieter Feucht, Olga Malsam, Mark Wilhelm Drewes, Eva-Maria Franken, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Hugh Rosinger, Thomas Bretschneider, Guido Bojack, Jan Dittgen