Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/370.1)
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Patent number: 11578012Abstract: The present invention relates to the use of novel nitrification inhibitors of formula (I), which are N-functionalized alkoxy pyrazole compounds. Moreover, the invention relates to the use of compounds of formula (I) as nitrification inhibitors, i.e. for reducing nitrification, as well as agrochemical mixtures and compositions comprising the nitrification inhibitors of formula (I).Type: GrantFiled: February 28, 2019Date of Patent: February 14, 2023Assignee: BASF SEInventors: Peter Nesvadba, Allan F. Cunningham, Shrirang Hindalekar, Barbara Nave, Tejas Pothi, Olof Wallquist, Alexander Wissemeier
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Publication number: 20150073153Abstract: Provided are improved processes for the preparation of 1-aryl pyrazole compounds of formula (I) and (IB): which are substituted at the 5-position of the pyrazole ring with a carbon-linked functional group. The process described are efficient and scalable and do not utilize hazardous sulfenyl halide reagents.Type: ApplicationFiled: November 17, 2014Publication date: March 12, 2015Applicant: Merial LimitedInventors: Charles Q. Meng, Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Xinxi Zhan, Jean Robert Labrosse, Michel Mulhauser
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Publication number: 20150024032Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.Type: ApplicationFiled: July 18, 2014Publication date: January 22, 2015Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
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Publication number: 20150018388Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.Type: ApplicationFiled: December 11, 2013Publication date: January 15, 2015Inventors: Richard B. Silverman, Yinan Zhang
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Publication number: 20140323305Abstract: The present invention relates to the use of strobilurine type compounds of formula I and the N-oxides and the salts thereof for combating phytopathogenic fungi containing a mutation in the mitochondrial cytochrome b gene conferring resistance to Qo inhibitors, and to methods for combating such fungi. The invention also relates to novel compounds, processes for preparing these compounds, to compositions comprising at least one such compound, to plant health applications, and to seeds coated with at least one such compound.Type: ApplicationFiled: December 6, 2012Publication date: October 30, 2014Applicant: BASF SEInventors: Joachim Rheinheimer, Violeta Terteryan, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Sebastian Georgios Rohrer, Wassilios Grammenos, Christian Pilger, Franz Roehl, Markus Gewehr, Gerd Stammler, Jurith Montag, Hubert Sauter
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Publication number: 20140315971Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.Type: ApplicationFiled: July 7, 2014Publication date: October 23, 2014Inventors: Izumi SASAKI, Tomohiro TOYODA, Hidefumi YOSHINAGA, Itaru NATSUTANI, Yoko TAKAHASHI
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Publication number: 20140256701Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins, Sean Turner
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Publication number: 20140243366Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: May 1, 2014Publication date: August 28, 2014Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 8809383Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.Type: GrantFiled: September 30, 2013Date of Patent: August 19, 2014Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Izumi Sasaki, Tomohiro Toyoda, Hidefumi Yoshinaga, Itaru Natsutani, Yoko Takahashi
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Patent number: 8802666Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: GrantFiled: December 21, 2010Date of Patent: August 12, 2014Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Patent number: 8802713Abstract: To provide pesticides such as insecticides, miticides and nematicides, which are excellent in the safety, pesticidal effects, residual effectiveness, etc., which further have infiltration, and which can be applied by soil treatment. A pesticide comprising a 3-alkoxy-1-phenyl-pyrazole derivative represented by the formula [I] or an agriculturally acceptable salt thereof as an active ingredient: wherein, for example, R1 is a C1-C10 alkyl group or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or the like, and each of R4, R5, R6 and R8 which are independent of one another, is a hydrogen atom or the like, and R7 is a C2-C4 haloalkylthio group or the like.Type: GrantFiled: October 17, 2008Date of Patent: August 12, 2014Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Satoru Ohata, Katsuya Kato, Keiji Toriyabe, Yoshihiro Ito, Ryuji Hamaguchi, Yuki Nakano
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Publication number: 20140221337Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.Type: ApplicationFiled: February 6, 2014Publication date: August 7, 2014Applicant: Xention LimitedInventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
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Patent number: 8785372Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.Type: GrantFiled: May 15, 2013Date of Patent: July 22, 2014Assignee: Aventis AgricultureInventors: Hyoung Ik Lee, Loic Patrick Le Hir de Fallois, Philip Reid Timmons, William Glenn Cawthorne, Adalberto Perez de Leon
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Publication number: 20140179637Abstract: A compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.Type: ApplicationFiled: December 21, 2013Publication date: June 26, 2014Applicants: The Research Foundation for The State University of New York, Northwestern UniversityInventors: Jonathan Leis, Carol Carter
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Publication number: 20140051857Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: October 28, 2013Publication date: February 20, 2014Applicant: Nissan Chemical Industries LimitedInventors: Shingo OWADA, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Publication number: 20140031406Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.Type: ApplicationFiled: September 30, 2013Publication date: January 30, 2014Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Izumi SASAKI, Tomohiro TOYODA, Hidefumi YOSHINAGA, Itaru NATSUTANI, Yoko TAKAHASHI
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Publication number: 20140031331Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: September 19, 2013Publication date: January 30, 2014Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
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Patent number: 8633237Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: GrantFiled: April 8, 2010Date of Patent: January 21, 2014Assignee: Merck Sharp & Dohme B.V.Inventors: Kevin J. Gillen, Jonathan Gillespie, Craig Jamieson, John K. F. MacLean, Elizabeth M. Moir, Zoran Rankovic
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Publication number: 20130324457Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.Type: ApplicationFiled: May 15, 2013Publication date: December 5, 2013Applicants: AVENTIS AGRICULTURE, MERIAL LIMITEDInventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Philip Reid Timmons, William Glenn Cawthorne, Jr., Alberto Perez de Leon
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Patent number: 8598078Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: August 21, 2008Date of Patent: December 3, 2013Assignee: Syngenta Crop Protection, LLCInventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
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Patent number: 8569353Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.Type: GrantFiled: July 14, 2011Date of Patent: October 29, 2013Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Izumi Sasaki, Tomohiro Toyoda, Hidefumi Yoshinaga, Itaru Natsutani, Yoko Takahashi
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Publication number: 20130281710Abstract: Provided are improved processes for the preparation of 1-aryl pyrazole compounds of formula (I) and (IB): which are substituted at the 5-position of the pyrazole ring with a carbon-linked functional group. The process described are efficient and scalable and do not utilize hazardous sulfenyl halide reagents.Type: ApplicationFiled: April 22, 2013Publication date: October 24, 2013Applicant: MERIAL LIMITEDInventors: Charles Q. Meng, Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Xinxi Zhan, Jean Robert Labrosse, Michel Mulhauser
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Patent number: 8492425Abstract: The invention relates to compounds having the formula (I): wherein the dashed line (represented by - - - ) represents an optional double bond; R1 is hydrogen and R2 is hydroxyethyl; or R1 and R2 together with the nitrogen atom to which they are attached form a morpholinyl ring optionally substituted with one or two hydroxy groups; each R3 is independently hydroxy or C1-6alkoxy; n is selected from 0, 1, and 2; or a N-oxide, salt, prodrug, solvate or stereoisomer thereof; with the proviso that the compound where the dashed line represents a double bond, R1 and R2 together with the nitrogen atom to which they are attached form a morpholinyl ring, and n is 0, is excluded. Also provided are methods for the preparation of compounds of formula (I); their uses as a medicaments, particularly for the treatment or prophylaxis of a sigma receptor mediated diseases or conditions.Type: GrantFiled: April 27, 2009Date of Patent: July 23, 2013Assignee: Laboratories Del Dr. Esteve, S.A.Inventors: Antoni Torrens Jover, Maria Rosa Cuberes-Altisent, Maria Jose Pretel Sanchez, Maria Magdalena Bordas Gelabert
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Patent number: 8470867Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: GrantFiled: February 9, 2010Date of Patent: June 25, 2013Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Christian Laggner, María Rosa Cuberes-Altisent, Joerg Holenz, Juana María Berrocal-Romero, Maria Montserrat Contijoch-Llobet
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Publication number: 20130143879Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: January 31, 2013Publication date: June 6, 2013Applicant: GENKYOTEX SAInventor: Genkyotex Sa
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Publication number: 20130116296Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.Type: ApplicationFiled: July 14, 2011Publication date: May 9, 2013Inventors: Izumi Sasaki, Tomohiro Toyoda, Hidefumi Yoshinaga, Itaru Natsutani, Yoko Takahashi
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Patent number: 8404734Abstract: The present invention relates to novel crystalline modifications of pyraclostrobin, to processes for their preparation and to the use of the novel modifications for preparing crop protection compositions.Type: GrantFiled: September 16, 2010Date of Patent: March 26, 2013Assignee: BASF SEInventors: Hans Ziegler, Winfried Mayer, Thomas Kroehl, Karl-Heinrich Schneider, Gerhard Cox, Peter Erk, Uwe Josef Vogelbacher, Rainer Noack, Roland Goetz, Joerg Wuckelt, Matthias Rauls
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Patent number: 8362064Abstract: Compounds of formula (I) are agonists of PPAR?, useful for the treatment of respiratory disease; formula (I): wherein R1, R2 or R3 each independently represents halo, cyano, nitro, amino, alkyl, haloalkyl, alkoxy, haloalkoxy, carboxylic acid or an ester or amide thereof; R4 represents hydrogen or alkyl; m, n or p independently represents 0, 1, 2 or 3.Type: GrantFiled: December 23, 2009Date of Patent: January 29, 2013Assignee: Pulmagen Theraputics (Inflammation) LimitedInventors: Vidya Ramdas, Harry Finch, Craig Fox
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Publication number: 20130018044Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: December 21, 2010Publication date: January 17, 2013Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20130012708Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: Nissan Chemical Industries LimitedInventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Patent number: 8329880Abstract: The invention relates to a process for preparing naphthalen-2-yl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.Type: GrantFiled: April 24, 2009Date of Patent: December 11, 2012Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Antoni Torrens Jover, Jordi Corbera Arjona, Maria Rosa Cuberes-Altisent
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Publication number: 20120289506Abstract: 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.Type: ApplicationFiled: June 12, 2012Publication date: November 15, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Publication number: 20120209005Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: October 22, 2010Publication date: August 16, 2012Applicant: Nissan Chemical Industries, Ltd.Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
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Publication number: 20120202781Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: ApplicationFiled: April 8, 2010Publication date: August 9, 2012Inventors: Kevin James Gillen, Jonathan Gillespie, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
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Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
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Patent number: 8217038Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: GrantFiled: October 7, 2010Date of Patent: July 10, 2012Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20120149710Abstract: Bacterial infections, including Methicillin resistant Staphylococcus aureus (MRSA) infections are a major health problem that has created a pressing need for new antibiotics. Pyridazinone, rhodanine, and pyrazolethione compounds effective inhibit the enzymatic activity of sortase A (srtA) found in gram positive bacteria are disclosed. A structure activity relationship (SAR) analysis led to the identification of several pyridazinone and pyrazolethione analogs that inhibit SrtA with IC50 values in the sub-micromolar range. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Many of these molecules also inhibit the sortase enzyme from B. anthracis suggesting that they may be generalized sortase inhibitors. The novel compounds, compositions, uses, formulations, medicaments, articles of manufacture provide improved materials, uses, and treatments useful in combating infectious disorders.Type: ApplicationFiled: August 23, 2010Publication date: June 14, 2012Inventors: Michael E. Jung, Robert T. Clubb, Sung Wook Yi, Nutee Suree, Jeremy Justin Clemens
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Publication number: 20120077796Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 10, 2011Publication date: March 29, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Frauke POHLKI, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins, Wilfried Hornberger, Mario Mezler, Sean Turner
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Publication number: 20120041043Abstract: Compounds of formula (I) are agonists of PPAR?, useful for the treatment of respiratory disease; formula (I): wherein R1, R2 or R3 each independently represents halo, cyano, nitro, amino, alkyl, haloalkyl, alkoxy, haloalkoxy, carboxylic acid or an ester or amide thereof; R4 represents hydrogen or alkyl; m, n or p independently represents 0, 1, 2 or 3.Type: ApplicationFiled: December 23, 2009Publication date: February 16, 2012Applicants: Pulmagen Therapeutics (Inflammation) Limited, Dr. Reddy's Laboratories LTDInventors: Vidya Ramdas, Harry Finch, Craig Fox
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Publication number: 20120040947Abstract: The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
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Publication number: 20120040948Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Frauke POHLKI, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
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Publication number: 20120029192Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).Type: ApplicationFiled: October 7, 2011Publication date: February 2, 2012Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
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Patent number: 8088812Abstract: The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: GrantFiled: March 2, 2007Date of Patent: January 3, 2012Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20110257178Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: ApplicationFiled: October 7, 2010Publication date: October 20, 2011Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Patent number: 7994204Abstract: The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].Type: GrantFiled: February 6, 2007Date of Patent: August 9, 2011Assignee: Taisho Pharmaceutical Co., LtdInventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Takeshi Koami, Rie Nishikawa
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Publication number: 20110178081Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: September 22, 2009Publication date: July 21, 2011Applicant: Genkyotex SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Publication number: 20110118253Abstract: The invention relates to compounds having the formula (I): wherein the dashed line (represented by - - - - -) represents an optional double bond; R1 is hydrogen and R2 is hydroxyethyl; or R1 and R2 together with the nitrogen atom to which they are attached form a morpholinyl ring optionally substituted with one or two hydroxy groups; each R3 is independently hydroxy or C1-6alkoxy; n is selected from 0, 1, and 2; or a N-oxide, salt, prodrug, solvate or stereoisomer thereof; with the proviso that the compound where the dashed line represents a double bond, R1 and R2 together with the nitrogen atom to which they are attached form a morpholinyl ring, and n is 0, is excluded. Also provided are methods for the preparation of compounds of formula (I); their uses as a medicaments, particularly for the treatment or prophylaxis of a sigma receptor mediated diseases or conditions.Type: ApplicationFiled: April 27, 2009Publication date: May 19, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Antoni Torrens Jover, Maria Rosa Cuberes-Altisent, Maria Jose Pretel Sanchez, Maria Magdelena Bordas Gelabert
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Publication number: 20110054000Abstract: The present invention relates to novel crystalline modifications of pyraclostrobin, to processes for their preparation and to the use of the novel modifications for preparing crop protection compositions.Type: ApplicationFiled: September 16, 2010Publication date: March 3, 2011Applicant: BASF SEInventors: Hans ZIEGLER, Winfried MAYER, Thomas KRÖHL, Karl-Heinrich SCHNEIDER, Gerhard COX, Peter ERK, Uwe Josef VOGELBACHER, Rainer NOACK, Roland GÖTZ, Jörg WUCKELT, Matthias RAULS
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara