Chalcogen And -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbons Of The Bicyclo Ring System (e.g., 4-oxo-naphthyridine -3-carboxylic Acid, Etc.) Patents (Class 546/123)
-
Patent number: 8188283Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: March 12, 2010Date of Patent: May 29, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Peter D. J. Grootenhuis, Sara S. Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Lev T. D. Fanning
-
Publication number: 20120130075Abstract: Disclosed herein are R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial. Because the R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt is more soluble and less toxic and has less side effects as an antimicrobial agent than hydrochloride and the other salts (D-aspartate and phosphate) conventionally used, the salt may be useful for oral and injectable administration.Type: ApplicationFiled: July 27, 2010Publication date: May 24, 2012Applicant: ARMED, INC.Inventors: Dong Rack Choi, Jin Yang, Sue Hye Yoon, Sung Jae Pyun, Seung Hwan Kim, Seung-Kyoo Seong, Jei Man Ryu
-
Publication number: 20120122817Abstract: Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: May 28, 2010Publication date: May 17, 2012Applicant: ASTRAZENECA ABInventors: Neil Bifulco, Allison Laura Choy, Olga Quiroga, Brian Alan Sherer
-
Patent number: 8163769Abstract: Antibacterials having formula (I) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates used in the processes, compositions containing the compounds, and methods of prophylaxis and treatment of bacterial infections using the compounds are disclosed.Type: GrantFiled: March 12, 2003Date of Patent: April 24, 2012Assignee: Abbott LaboratoriesInventors: David Anderson, Bruce Beutel, Todd D. Bosse, Richard Clark, Curt Cooper, Peter Dandliker, Caroline David, Yu-Gui Gu, Todd Matthew Hansen, Mira Hinman, Douglas Kalvin, Daniel P. Larson, Linda Lynch, Zhenkun Ma, Christopher Motter, Fabio Palazzo, Teresa Rosenberg, Tamara Rehm, William Sanders, Michael Tufano, Rolf Wagner, Moshe Weitzberg, Hong Yong, Tianyuan Zhang
-
Patent number: 8163906Abstract: Compounds of formula I are effective modulators of JNK: wherein X is CR11 or N; Y is —C(O)R3, 5-membered heteroaryl, or 5-membered heterocyclyl; Z is phenyl, cycloalkyl, heterocyclyl or heteroaryl, and is substituted with R1 and R2; R1 and R2 are each independently H, halo, CN, lower alkyl, or —Y1—Y2—Y3—R8, or R1 and R2 together form —O(CH2)nO—, where n is 1 or 2; Y1 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —S—, —SO2—, or a bond; Y2 is cycloalkylene, heterocycloalkylene, lower alkylene or a bond; Y3 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —SO2—, or a bond; R8 is H, lower alkyl, lower alkoxy, cycloalkyl, heterocycloalkyl, or —NR9R10, wherein R8 other than H is optionally substituted with lower alkyl, halo, —CF3, or —OH; R9 and R10 are each independently H or lower alkyl; R3 is OH, lower alkyl, lower alkoxy, (lower alkoxy)-lower alkoxy, or —NR9R10; R4 is lower alkyl, phenyl, heterocyclyl, cycloalkyl, heterocycloalkyl, or heteroaryl, and is optionally substituted with lower alkyl, hydroType: GrantFiled: May 14, 2008Date of Patent: April 24, 2012Assignee: Roche Palo Alto, LLCInventors: Sarah C. Abbot, Geneviève N. Boice, Bernd Buettelmann, David Michael Goldstein, Leyi Gong, Joan Heather Hogg, Pravin Iyer, Kristen Lynn McCaleb, Yun-chou Tan
-
Publication number: 20120094833Abstract: The present invention relates to novel herbicidal oxopyridine and thionopyridine derivatives of Formula (I), or an agronomically acceptable salt of said compound wherein R1, R5, R6, R7, X1, X2 and Q are as defined herein. The invention further relates to processes and intermediates for the preparation of the oxopyridine derivatives, to compositions which comprise the herbicidal compounds, and to their use for controlling weeds, in particular in crops of useful plants.Type: ApplicationFiled: March 31, 2010Publication date: April 19, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Roger Salmon, Glynn Mitchell, James Alan Morris
-
Patent number: 8158797Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.Type: GrantFiled: December 20, 2004Date of Patent: April 17, 2012Assignee: Morphochem Aktiengesellschaft fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
-
Patent number: 8148530Abstract: The present invention relates to a process for the preparation of 3,7-diazabicyclo[3.3.1]nonane compounds. According to the invention, in a first step, a dicarboxylic acid ester is reacted with a pyridine aldehyde and a primary amine. The piperidone which forms is reacted in a second stage with formaldehyde and a further primary amine. It is essential to the invention that, in the first reaction stage, a C2-C4-alcohol is used as solvent and, in the second reaction stage, a C3-C4-alcohol is used as solvent.Type: GrantFiled: June 10, 2006Date of Patent: April 3, 2012Assignee: Clariant Produkte (Deutschland) GmbHInventors: Michael Wessling, Barbara Duecker, Nicole Nitschke
-
Patent number: 8138202Abstract: Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.Type: GrantFiled: December 30, 2010Date of Patent: March 20, 2012Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Anantha Sudhakar, Jeff Jacobs, Ahmad Hashash, Sean Ritchie, Hengqin Cheng
-
Patent number: 8124773Abstract: Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions.Type: GrantFiled: June 12, 2007Date of Patent: February 28, 2012Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Daniel C. Adelman, Marc J. Evanchik, Anantha Sudhakar, Jeffrey William Jacobs, Jeffrey A. Silverman
-
Publication number: 20120040942Abstract: The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.Type: ApplicationFiled: February 24, 2010Publication date: February 16, 2012Applicant: RESPIRATORIUS ABInventors: Martin Johansson, Viveca Thornqvist Otlner, Jorgen Toftered, David Wensbo, Maria Dalence
-
Patent number: 8106072Abstract: Object To provide novel quinolinecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents. Solving Means There are provided 7-(4-substituted-3-cyclopropylaminomethylpyrrolidinyl)quinolonecarboxylic acid derivatives (such as 1-cyclopropyl-7-[(3S,4S)-3-cyclopropylaminomethyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid) that exhibit strong antibacterial activity against gram-positive bacteria, such as MRSA, PRSP and VRE, while being safe.Type: GrantFiled: February 26, 2009Date of Patent: January 31, 2012Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yoshikazu Asahina, Masaya Takei
-
Patent number: 8106068Abstract: The invention provides compounds of Formula (2), and pharmaceutical compositions thereof, wherein R1, R2, R3, R4 and L are as described herein; as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.Type: GrantFiled: December 2, 2009Date of Patent: January 31, 2012Assignee: IRM LLCInventors: Zuosheng Liu, Jon Loren, Valentina Molteni, Juliet Nabakka
-
Patent number: 8093381Abstract: The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): in which R1, R2, R3, R4, R5, R6, R7, and X are as defined in Claim 1.Type: GrantFiled: May 22, 2008Date of Patent: January 10, 2012Assignee: BiocodexInventors: Laurence Berthon-Cedille, Marie-Emmanuelle Leguern, Gilles Renaud, Francis Tombret
-
Publication number: 20110312987Abstract: 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.Type: ApplicationFiled: April 11, 2011Publication date: December 22, 2011Inventors: Ae Ri Kim, Jin Hwa Lee, Ki Sook Park, Jong Ryoo Choi, Tae Hee Lee, Jay Hyok Chang, Do Hyun Nam, Hoon Choi
-
Publication number: 20110306612Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: September 29, 2009Publication date: December 15, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Chi B. Vu, Christopher Oalmann, Robert B. Perni, Brian White
-
Publication number: 20110287937Abstract: Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C?O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.Type: ApplicationFiled: February 2, 2010Publication date: November 24, 2011Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Fumiaki Takabe, Yuuki Hirano, Akira Funyu, Masami Kobayashi, Takashi Mitsunari
-
Publication number: 20110269741Abstract: Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: March 28, 2011Publication date: November 3, 2011Applicant: Ardea Biosciences, Inc.Inventors: Huanming CHEN, Jianlin SONG, Jean-Michel VERNIER, Anthony B. PINKERTON, Johnny Y. NAGASAWA
-
Patent number: 8048892Abstract: are useful as inhibitors of HIF prolyl hydroxylases where the definitions of the variables are provided herein.Type: GrantFiled: December 17, 2007Date of Patent: November 1, 2011Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Guo-Qiang Cao, Jennifer E. Golden, Stephanie Mercede, Tanya Peterkin, Anthony Reed, Christopher M. Tegley
-
Publication number: 20110251194Abstract: The disclosure concerns heterobicyclic compounds of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as enantiomers, diastereoisomers and mixtures thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.Type: ApplicationFiled: January 7, 2011Publication date: October 13, 2011Applicant: SANOFI-AVENTISInventors: Claude BERNHART, Gary MCCORT, Samir JEGHAM, Jean Marc HERBERT, Pierre CASELLAS, Monsif BOUABOULA, Olivier DUCLOS
-
Publication number: 20110245353Abstract: The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.Type: ApplicationFiled: March 31, 2011Publication date: October 6, 2011Applicant: SENOMYS, INC.Inventors: Catherine TACHDJIAN, Xiao Qing TANG, Donald S. KARANEWSKY, Guy SERVANT, Xiaodong LI, Feng ZHANG, Qing CHEN, Hong ZHANG, Timothy DAVIS, Vincent DARMOHUSODO, Melissa WONG, Victor SELCHAU
-
Publication number: 20110245290Abstract: The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below:Type: ApplicationFiled: March 31, 2010Publication date: October 6, 2011Inventors: Sophie-Dorothee Clas, Rafik Naccache, Hongshi Yu, Jerry Murry, Narayan Variankaval
-
Publication number: 20110224248Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: May 17, 2011Publication date: September 15, 2011Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Roland Burli, Marian C. Bryan, Guo-Qiang Cao, Susana C. Neira, Anthony B. Reed
-
Publication number: 20110224247Abstract: The invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.Type: ApplicationFiled: March 11, 2011Publication date: September 15, 2011Applicant: H. LUNDBECK A/SInventors: Nikolay Khanzhin, Klaus Bæk Simonsen, Søren Møller Nielsen, Karsten Juhl
-
Publication number: 20110182850Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: ApplicationFiled: April 7, 2010Publication date: July 28, 2011Inventors: Trixi BRANDL, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
-
Publication number: 20110166123Abstract: Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: January 7, 2009Publication date: July 7, 2011Applicant: AARDEA BIOSCIENCES, INC.Inventors: Huanming Chen, Jianlin Song, Jean-Michel Vernier, Anthony B. Pinkerton, Johnny Y. Nagasawa
-
Publication number: 20110152528Abstract: The invention relates to a one-pot reaction for the production of 3,7-diaza-bicyclo[3.3.1]nonane compounds, wherein in a first step a dicarboxylic acid ester is reacted with a pyridine aldehyde and a primary amine. The piperidone created in this manner is reacted with formaldehyde and a further primary amine in a second step. It is essential to the invention that both reaction steps are carried out in a one-pot variation in a C1-C4 alcohol as the solvent, and that the reaction water created is removed by means of distillation.Type: ApplicationFiled: August 17, 2009Publication date: June 23, 2011Applicant: CLARIANT FINANCE (BVI) LIMITEDInventors: Melanie Sajitz, Steve Laborda, Peter Naumann, Michael Wessling
-
Publication number: 20110144149Abstract: The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth-yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.Type: ApplicationFiled: September 27, 2010Publication date: June 16, 2011Applicant: HETERO DRUGS LIMITEDInventors: Bandi PARTHASARADHI REDDY, Kura RATHNAKAR REDDY, Rapolu RAJI REDDY, Dasari MURALIDHARA REDDY
-
Publication number: 20110136855Abstract: The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphth-yridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.Type: ApplicationFiled: September 27, 2010Publication date: June 9, 2011Applicant: HETERO DRUGS LIMITEDInventors: Bandi PARTHASARADHI REDDY, Kura RATHNAKAR REDDY, Rapolu RAJI REDDY, Dasari MURALIDHARA REDDY
-
Publication number: 20110124643Abstract: The present invention relates to pyridopyridone derivatives of formula (I): in which the variables are as defined herein, to their preparation and to their therapeutic use as inhibitors of the kinase activity of PDGF (platelet-derived growth factor) ligand receptors and possibly of FLT3 (fms-like tyrosine kinase receptor) ligand receptors.Type: ApplicationFiled: January 6, 2011Publication date: May 26, 2011Applicant: SANOFI-AVENTISInventors: Patrice BELLEVERGUE, Gilbert LASSALLE, Gary MCCORT, Valerie MARTIN, Pierre SAVI, Cecile VOLLE-CHALLIER
-
Patent number: 7947709Abstract: Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.Type: GrantFiled: June 20, 2008Date of Patent: May 24, 2011Assignee: Roche Palo Alto LLCInventors: Todd Richard Elworthy, Joan Heather Hogg, Joshua Kennedy-Smith, Counde O'Yang, Mark Smith, Zachary Kevin Sweeney, Jeffrey Wu
-
Publication number: 20110105497Abstract: Compounds for treating, preventing or managing cancer are disclosed. Also provided are methods for using the compounds in treatment of various cancers. Also provided are methods of treatment using the compounds together with another chemotherapy, radiation therapy, hormonal therapy, biological therapy, or immunotherapy. Pharmaceutical compositions suitable for use in the methods are also disclosed.Type: ApplicationFiled: October 26, 2010Publication date: May 5, 2011Inventor: Anantha Sudhakar
-
Publication number: 20110105491Abstract: The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to their use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: July 7, 2009Publication date: May 5, 2011Inventors: Hamed Aissaoui, Christoph Boss, Julien Hazemann, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen
-
Publication number: 20110082169Abstract: Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.Type: ApplicationFiled: September 3, 2010Publication date: April 7, 2011Inventors: Anantha SUDHAKAR, Jeff Jacobs, Ahmad Hashasb, Sean Ritchie, Hengqin Cheng
-
Patent number: 7919623Abstract: A compound having HIV Integrase Inhibitory activity of the formula: (wherein: R1 is optionally substituted aralkyl; R2 and R3 are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for “optionally substituted” is a noncyclic group); R4 is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in “optionally substituted formylamino”, “optionally substituted carbamoyl” and “optionally substituted amino” may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.Type: GrantFiled: February 2, 2005Date of Patent: April 5, 2011Assignee: Shionogi & Co., Ltd.Inventors: Teruhiko Taishi, Yukio Tada
-
Publication number: 20110059946Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: September 10, 2010Publication date: March 10, 2011Applicant: Morphochem Aktiengesellschaft fuer Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin
-
Patent number: 7902226Abstract: 3-(1-Aminocycloalkyl)pyrrolidinyl-substituted-6-dehalodeno(hydrogen-substituted)quinolon carboxylic acid derivatives having specific substituents as represented by the following formula (I), its salts, and hydrates thereof exhibit a broad and potent antibacterial activity on gram-negative and gram-positive bacteria, in particular, resistant bacteria typified by gram-positive cocci, including MRSA, PRSP and VRE. Thus these compounds are usable as drugs.Type: GrantFiled: December 26, 2006Date of Patent: March 8, 2011Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hisashi Takahashi, Rie Miyauchi, Masao Itoh, Makoto Takemura, Isao Hayakawa
-
Patent number: 7897612Abstract: The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: GrantFiled: March 6, 2007Date of Patent: March 1, 2011Assignee: Glaxosmithkline, LLCInventors: Duke M. Fitch, Mariela Colón
-
Publication number: 20110021352Abstract: The present invention relates to novel herbicidal [1,8]-naphthyridines of Formula (Ia) or (Ib), or an agronomically acceptable salt of said compound wherein R2, R3, R4, R5, R6, R7, R8, n, m, X and Q are as defined herein. The invention further relates to processes and intermediates for the preparation of the [1,8]-naphthyridines, to compositions which comprise the herbicidal compounds, and to their use for controlling weeds, in particular in crops of useful plants.Type: ApplicationFiled: March 16, 2009Publication date: January 27, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Glynn Mitchell, David Phillip Bacon, Ian Henry Aspinall, Emma Briggs, Alaric James Avery, James Alan Morris, Claire Janet Russell, Roger Salmon
-
Patent number: 7875722Abstract: The present invention relates to a method for producing a quinolone compound having high antibacterial activity and high safety, at high yield and in a simple manner. A quinolonecarboxylic acid derivative (1) of interest is produced through a one-pot manner by reacting a compound (2) with a salt of a cyclic amine (3) and with a boron derivative in a solvent in the presence of a base.Type: GrantFiled: September 30, 2009Date of Patent: January 25, 2011Assignee: Daiichi Sankyo Company, LimitedInventors: Koji Sato, Kenji Sakuratani
-
Publication number: 20100305052Abstract: The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.Type: ApplicationFiled: June 1, 2007Publication date: December 2, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Santiago Figueroa Perez, Peter Kolkhof, Lars Bärfacker, Ingo Flamme, Karl-Heinz Schlemmer, Rolf Grosser, Klaus Münter, Andreas Knorr
-
Patent number: 7834027Abstract: The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1, 8-naphthyridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.Type: GrantFiled: June 15, 2005Date of Patent: November 16, 2010Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy
-
Publication number: 20100261750Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: March 12, 2010Publication date: October 14, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Hayley Binch, Peter D.J. Grootenhuis, Sara S. Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Lev T.D. Fanning
-
Publication number: 20100240694Abstract: 7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.Type: ApplicationFiled: June 2, 2010Publication date: September 23, 2010Inventors: Ae Ri KIM, Jin Hwa LEE, Ki Sook PARK, Jong Ryoo CHOI, Tae Hee LEE, Jay Hyok CHANG, Do Hyun NAM, Hoon CHOI
-
Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
-
Publication number: 20100216834Abstract: Stereoisomers of compounds of Formula I are disclosed: wherein V1, V2, R5a, R5b, R5c, R8 and R9b are defined herein and wherein the stereoisomer contains 2 chiral centers in the 8-membered ring and one of the chiral centers is due to the presence of a chiral ring carbon. The isomers are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 15, 2007Publication date: August 26, 2010Inventors: Richard C. A. Isaacs, John S. Wai, Linda S. Payne, Thorsten E. Fisher
-
Patent number: 7776857Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: GrantFiled: April 3, 2008Date of Patent: August 17, 2010Assignee: Amgen Inc.Inventors: Victor Cee, Holly Deak, Bingfan Du, Stephanie Geuns-Meyer, Brian L. Hodous, Zihao Hua, Matthew Martin, Isaac Marx, Hanh Nho Nguyen, Philip Olivieri, Kathleen Panter, Karina Romero, Laurie Schenkel, Ryan White
-
Publication number: 20100203162Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.Type: ApplicationFiled: December 30, 2009Publication date: August 12, 2010Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Sheik Mohamed Mujeebur Rahuman, Ramar Subbiah
-
Publication number: 20100197924Abstract: 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: December 16, 2009Publication date: August 5, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Alexandra E. Gould, Sean J. Harrison, Hirotake Mizutani, Ming Shen, Thomas E. Smyser, Stephen G. Stroud
-
Publication number: 20100197909Abstract: To provide a novel mutilin derivative having a substitution at the 14-position, which is a novel mutilin analogue exhibiting a potent and broad antimicrobial action against Gram-positive bacteria and Gram-negative bacteria including various drug-resistant bacteria, and which is expected to be useful as an agent for treating infectious diseases. A mutilin derivative represented by the following general formula (1): or a pharmaceutically acceptable addition salt thereof.Type: ApplicationFiled: May 23, 2008Publication date: August 5, 2010Inventors: Yasumichi Fukuda, Masanori Takadoi, Yoshikazu Asahina, Taro Sato, Haruaki Kurasaki, Hiroyuki Ebisu, Masaya Takei, Hideyuki Fukuda