The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
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Publication number: 20150126506Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20150126503Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as phaType: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Inventors: Matthias HOFFMANN, Georg DAHMANN, Dennis FIEGEN, Sandra HANDSCHUH, Jasna KLICIC, Guenter LINZ, Gerhard SCHAENZLE, Andreas SCHNAPP, Stephen Peter EAST, Michael Philip MAZANETZ, Robert John SCOTT, Edward Walker
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Publication number: 20150119405Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.Type: ApplicationFiled: October 23, 2014Publication date: April 30, 2015Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
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Publication number: 20150119387Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.Type: ApplicationFiled: June 15, 2012Publication date: April 30, 2015Applicant: Curegenix Inc.Inventor: Songzhou An
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Publication number: 20150119385Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.Type: ApplicationFiled: October 24, 2014Publication date: April 30, 2015Applicant: Novartis AGInventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Pierre Nimsgern, Sebastien Ripoche, Jing Xiong, Bo Han, Can Wang, Xianglin Zhao
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Publication number: 20150111877Abstract: The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.Type: ApplicationFiled: May 7, 2013Publication date: April 23, 2015Inventors: Thomas D. Aicher, Kenneth J. Barr, Blair T. Lapointe, Valdimir Simov, Karin A. Stein, William D. Thomas, Peter L. Toogood, Chad A. Van Huis, Catherine M. White
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Publication number: 20150111750Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas X1 is N or CR1, X2 is N or CR2, X3 is N or CR3 and X4 is N or CR4; provided that a least one of X1, X3 and X4 is N; R, R1, R2, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.Type: ApplicationFiled: April 16, 2013Publication date: April 23, 2015Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
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Publication number: 20150112071Abstract: The present invention relates to synthetic processes for preparation of aminotetralin compounds with kinase inhibitory activity. The invention also provides synthetic intermediates useful in the processes of the invention.Type: ApplicationFiled: May 29, 2014Publication date: April 23, 2015Applicant: Millennium Pharmaceuticals, Inc.Inventors: Alexandra E. Gould, Sean J. Harrison, Hirotake Mizutani, Ming Shen, Thomas E. Smyser, Stephen G. Stroud
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Publication number: 20150111874Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: October 3, 2014Publication date: April 23, 2015Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Martin R. TREMBLAY
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Patent number: 9012443Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: GrantFiled: December 6, 2012Date of Patent: April 21, 2015Assignee: Amgen Inc.Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
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Patent number: 9012634Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the Fab1 enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: GrantFiled: August 10, 2012Date of Patent: April 21, 2015Assignee: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans
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Publication number: 20150105367Abstract: This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers.Type: ApplicationFiled: March 5, 2013Publication date: April 16, 2015Inventors: Daniel L. Flynn, Michael D, Kaufman, Lakshminarayana Vogeti, Scott Wise, Wei-Ping Lu, Bryan Smith, Timothy Malcolm Caldwell, William C. Patt, James R. Henry, Philip A. Hipskind, Sheng-Bin Peng
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Publication number: 20150105418Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 9006265Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.Type: GrantFiled: September 2, 2011Date of Patent: April 14, 2015Assignee: Bayer Intellectual Property GmbHInventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
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Publication number: 20150087840Abstract: The invention relates to a new process suitable for manufacturing the compounds of formula I (I) wherein W is H, Br, Cl or methyl, which are synthetic intermediates useful in the preparation of antibiotic compounds.Type: ApplicationFiled: April 26, 2013Publication date: March 26, 2015Inventors: Stefan Abele, Hans Meier, Gunther Schmidt, Heinz Steiner
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Patent number: 8987455Abstract: The present invention relates to a method of controlling plants or inhibiting plant growth which comprises applying to the plants or to the locus thereof a herbicidally effective amount of a compound of formula (I) wherein A1, A2, A3, A4, R3, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to intermediates used in the preparation of compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to certain novel pyridopyridines, pyridodiazines and pyridotriazines.Type: GrantFiled: September 6, 2013Date of Patent: March 24, 2015Assignee: Syngenta LimitedInventors: Matthew Robert Cordingley, Michael Drysdale Turnbull, Nigel James Willetts, Patrick Jelf Crowley
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Patent number: 8987250Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: GrantFiled: April 19, 2013Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20150080413Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Inventors: Jerome Emile Georges Guillemont, David Francis Alain Lancois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Publication number: 20150072974Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.Type: ApplicationFiled: May 9, 2013Publication date: March 12, 2015Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
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Patent number: 8975261Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: May 21, 2012Date of Patent: March 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
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Publication number: 20150065468Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.Type: ApplicationFiled: August 29, 2014Publication date: March 5, 2015Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
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Patent number: 8969568Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as welType: GrantFiled: January 26, 2011Date of Patent: March 3, 2015Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Matthias Hoffmann, Georg Dahmann, Dennis Fiegen, Sandra Handschuh, Jasna Klicic, Guenter Linz, Gerhard Schaenzle, Andreas Schnapp, Stephen Peter East, Michael Philip Mazanetz, Robert John Scott, Edward Walker
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Publication number: 20150057293Abstract: The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: October 26, 2012Publication date: February 26, 2015Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Patrick Rene Angibaud, Michel Obringer, Julien Jeremie Joseph Marin, Matthieu Jeanty
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Patent number: 8957211Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.Type: GrantFiled: October 8, 2013Date of Patent: February 17, 2015Assignee: SanofiInventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
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Patent number: 8957062Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: April 5, 2012Date of Patent: February 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
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Publication number: 20150045368Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: March 1, 2013Publication date: February 12, 2015Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Hakan Gunaydin, Angel Guzman-Perez, Zihao Hua, Hongbing Huang, Xin Huang, Matthew W. Martin, Vinod F. Patel
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Patent number: 8952163Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: May 30, 2013Date of Patent: February 10, 2015Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8952161Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: June 5, 2013Date of Patent: February 10, 2015Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
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Publication number: 20150031675Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).Type: ApplicationFiled: January 31, 2013Publication date: January 29, 2015Inventors: Jon-Paul Strachan, Daniel Yohannes
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Publication number: 20150031890Abstract: There is provided a pharmaceutical composition comprising a bicyclic pyridinol derivative as an active ingredient for preventing or treating diseases caused by angiogenesis. The bicyclic pyridinol derivative expressed by Chemical Formula 1 can be effectively used as a drug for preventing and treating diseases caused by angiogenesis since it inhibits neovascularization in a chorioallantoic membrane model.Type: ApplicationFiled: December 7, 2012Publication date: January 29, 2015Inventors: Byeong Seon Jeong, Jung Ae Kim, You Ra Kang, Tae Gyu Nam, Jin Mo Ku, Ned A. Porter
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Publication number: 20150031668Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: July 15, 2014Publication date: January 29, 2015Inventors: Kaustav Biswas, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma, Kelvin Sham, James Brown, Wenge Zhong, Thomas T. Nguyen
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Patent number: 8940742Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: GrantFiled: March 15, 2013Date of Patent: January 27, 2015Assignee: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. Castro, Katrina Chan, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Liansheng Li, Tao Liu, Yi Liu, Pingda Ren, Daniel A. Snyder, Martin R. Tremblay
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Publication number: 20150025244Abstract: The invention relates to a process and synthetic intermediates that can be used for manufacturing the compound of formula (1-6) which is a synthetic intermediate useful in the preparation of antibiotic compounds.Type: ApplicationFiled: February 8, 2013Publication date: January 22, 2015Applicant: Acteon Pharmaceuticals Ltd.Inventors: Stefan Abele, Gunther Schmidt
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Publication number: 20150018352Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: ApplicationFiled: March 7, 2013Publication date: January 15, 2015Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
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Patent number: 8927534Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.Type: GrantFiled: January 31, 2007Date of Patent: January 6, 2015Assignee: Shire Orphan Therapies GmbHInventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
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Patent number: 8927721Abstract: The present invention provides, for example, the following compound: wherein ring Z is pyridine or a carbocycle, each of which is substituted or unsubstituted, ring A is a carbocycle or a heterocycle, each of which is substituted or unsubstituted, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R4a and R4b are each independently hydrogen or substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.Type: GrantFiled: October 27, 2011Date of Patent: January 6, 2015Assignee: Shionogi & Co., Ltd.Inventors: Yasunori Mitsuoka, Yuuji Kooriyama
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Publication number: 20150005287Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.Type: ApplicationFiled: February 28, 2014Publication date: January 1, 2015Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
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Publication number: 20150005302Abstract: The present invention directs a compound represented by formula (I).Type: ApplicationFiled: December 21, 2012Publication date: January 1, 2015Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Joel R. Walker, Raymond Huntley
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Patent number: 8921389Abstract: The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).Type: GrantFiled: February 1, 2012Date of Patent: December 30, 2014Assignee: Fibrogen, Inc.Inventors: Danny Ng, Michael P. Arend, Lee A. Flippin
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Publication number: 20140371201Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: ApplicationFiled: June 11, 2014Publication date: December 18, 2014Inventors: Matthew WEISS, Alessandro BOEZIO, Christiane BOEZIO, John R. BUTLER, Margaret Yuhua CHU-MOYER, Erin F. DIMAURO, Thomas DINEEN, Russell GRACEFFA, Angel GUZMAN-PEREZ, Hongbing HUANG, Charles KREIMAN, Daniel LA, Isaac E. MARX, Benjamin Charles MILGRIM, Hanh Nho NGUYEN, Emily PETERSON, Karina ROMERO, Brian SPARLING
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Publication number: 20140371067Abstract: The present invention relates to a method of controlling weeds at a locus, said method comprising application to the locus of a weed controlling amount of a herbicidal composition comprising a compound of Formula (I), or an agronomically acceptable salt of said compounds wherein X, R1, R2, R4 and R5 are as defined herein. The invention further relates novel herbicidal compounds, to herbicidal compositions comprising said compounds and to their use for controlling weeds, in particular in crops of useful plants.Type: ApplicationFiled: December 20, 2012Publication date: December 18, 2014Applicant: SYNGENTA LIMITEDInventors: Glynn Mitchell, Alison Clare Elliott
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Patent number: 8912216Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: October 4, 2013Date of Patent: December 16, 2014Assignee: Merck Patent GmbHInventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Publication number: 20140364443Abstract: Disclosed are 1,4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1,4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, i.e., having a dual-activity, which are of potential importance as a pharmaceutical and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia.Type: ApplicationFiled: December 7, 2012Publication date: December 11, 2014Applicant: Jiangsu Simovay Pharmaceutical Co., Ltd.Inventors: Rong Chen, Lin Feng, Zhengping Zhang, Fang Fang, Qingli Dong, Fulong Li, Lei Wang, Yao Hua, Shibao Yang, Peng Wang
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Patent number: 8906923Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: GrantFiled: August 10, 2012Date of Patent: December 9, 2014Assignee: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Patent number: 8906911Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: March 29, 2013Date of Patent: December 9, 2014Assignee: AbbVie Inc.Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
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Publication number: 20140357617Abstract: The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.Type: ApplicationFiled: August 20, 2014Publication date: December 4, 2014Applicant: FAB PHARMA S.A.S.Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
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Patent number: 8901144Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.Type: GrantFiled: February 7, 2014Date of Patent: December 2, 2014Assignee: SciFluor Life Sciences, LLCInventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
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Patent number: 8901119Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: GrantFiled: March 9, 2012Date of Patent: December 2, 2014Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
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Publication number: 20140349995Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: August 8, 2014Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian HURLEY, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
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Publication number: 20140343036Abstract: The invention provides novel compounds having the general formula: wherein A, R1 and R2 are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Applicant: GENENTECH, INC.Inventors: Huifen Chen, Terry Crawford, Steven R. Magnuson, Chudi Ndubaku, Lan Wang