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)
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Patent number: 8664240Abstract: 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: GrantFiled: July 27, 2010Date of Patent: March 4, 2014Assignee: Arimed, Inc.Inventors: Dong Rack Choi, Jin Yang, Sue Hye Yoon, Sung Jae Pyun, Seung Hwan Kim, Seung-Kyoo Seong, Jei Man Ryu
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Patent number: 8658645Abstract: The present invention relates to the use of certain quinolone antibiotics for controlling bacterial disorders of the oral cavity, in particular in veterinary medicine.Type: GrantFiled: August 2, 2004Date of Patent: February 25, 2014Assignee: Bayer Intellectual Property GmbHInventors: Gert Daube, Markus Edingloh, Bernd Stephan, Franz Pirro, Agnès Limet
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Publication number: 20140046067Abstract: The invention relates to novel alicyclic N,N?-substituted diazabicyclo[3.3.1]nonane derivatives of general formula (I) which act as allosteric AMPA receptor modulators, and to drugs based thereon which can be used for treating Alzheimer's, Parkinson's and other neurodegenerative diseases.Type: ApplicationFiled: April 10, 2012Publication date: February 13, 2014Inventors: Maxim Eduardovich Zapolsky, Nokilai Serafimovich Zefirov, Vladimir Alexandrovich Palyulin, Mstislav Igorevich Lavrov
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Publication number: 20140045839Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.Type: ApplicationFiled: September 18, 2013Publication date: February 13, 2014Applicant: Bionomics LimitedInventors: Jonathan Bayldon Baell, Brad Sleebs, Bernard Luke Flynn, Ian Phillip Street, Nurul Quazi, Chinh Thien Bui
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Publication number: 20140018356Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: April 4, 2013Publication date: January 16, 2014Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Publication number: 20140018384Abstract: There is provided compounds of formula I, wherein X1 to X4, R1 to R4, Y1, Y2 and L are as defined in the description, and pharmaceutically-acceptable salts thereof, which may be useful in the treatment and/or prophylaxis of autoimmune diseases, inflammatory (e.g. chronic inflammatory) diseases and/or other diseases that may benefit from production of ROS (reactive oxygen species) by a NADPH oxidase complex.Type: ApplicationFiled: March 16, 2012Publication date: January 16, 2014Applicant: PRONOXIS ABInventors: Karl Fredrik Wallner, Jan Peter Olofsson, Malin Kristin Hultqvist, Benjamin Harry Pelcman
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Patent number: 8586570Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.Type: GrantFiled: April 27, 2011Date of Patent: November 19, 2013Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
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Patent number: 8586601Abstract: 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: September 3, 2010Date of Patent: November 19, 2013Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Anantha Sudhakar, Jeff Jacobs, Ahmad Hashash, Sean Ritchie, Hengqin Cheng
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Patent number: 8580814Abstract: Methods of treating, preventing or managing cancer, including certain leukemias are disclosed. The methods encompass the administration of enantiomerically pure (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid. Also provided are methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed.Type: GrantFiled: September 5, 2006Date of Patent: November 12, 2013Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Daniel C. Adelman, Jeffrey A. Silverman
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Publication number: 20130296275Abstract: 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: July 2, 2013Publication date: November 7, 2013Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Patent number: 8569484Abstract: 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: GrantFiled: May 28, 2010Date of Patent: October 29, 2013Assignee: Astrazeneca ABInventors: Neil Bifulco, Allison Laura Choy, Olga Quiroga, Brian Alan Sherer
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Patent number: 8552193Abstract: The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below:Type: GrantFiled: March 31, 2010Date of Patent: October 8, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Sophie-Dorothee Clas, Rafik Naccache, Hongshi Yu, Jerry Murry, Narayan Vanankaval
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Patent number: 8552026Abstract: The present invention relates to an isatin derivative having the formula (I), a medicament for treatment of tuberculoses containing that isatin derivative as well as a method for preparing isatin derivative according to formula (I).Type: GrantFiled: April 7, 2011Date of Patent: October 8, 2013Assignee: King Saud UniversityInventors: Tarek Aboul-Fadl Mohamed Hassan, Fayzah bint Ahmad S. Bin Jubair
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Publication number: 20130231363Abstract: 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: September 5, 2013Inventors: Sophie-Dorothee Clas, Rafik Naccache, Hongshi Yu, Jerry Murry, Narayan Variankaval
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Publication number: 20130217680Abstract: This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 24, 2011Publication date: August 22, 2013Inventors: Alexander Pasternak, Reynalda K. deJesus, Yuping Zhu, Lihu Yang, Shawn Walsh, Haifeng Tang, Dooseop Kim, Barbara Pio, Aurash Shahripour, Kevin Belyk
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Patent number: 8501774Abstract: 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: February 8, 2012Date of Patent: August 6, 2013Assignee: Morphochem Aktiengesellschaft für Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Muller, Michael W. Cappi
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Patent number: 8497282Abstract: 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: GrantFiled: December 30, 2009Date of Patent: July 30, 2013Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Sheik Mohamed Mujeebur Rahuman, Ramar Subbiah
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Publication number: 20130190499Abstract: 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: July 25, 2013Applicant: H. Lundbeck A/SInventors: Nikolay Khanzhin, Klaus Bæk Simonsen, Søren Møller Nielsen, Karsten Juhl
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Publication number: 20130190498Abstract: The present invention relates to an isatin derivative having the formula (I), a medicament for treatment of tuberculoses containing that isatin derivative as well as a method for preparing isatin derivative according to formula (I).Type: ApplicationFiled: April 7, 2011Publication date: July 25, 2013Applicant: King Saud UniversityInventors: Tarek Hassan, Fayzah Jubair
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Publication number: 20130178496Abstract: 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: February 27, 2013Publication date: July 11, 2013Inventors: Hayley Binch, Peter D.J. Grootenhuis, Sara S. Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Lev T.D. Fanning
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Publication number: 20130178472Abstract: The invention relates to pyridine-pyridinone derivatives general formula (I): in which R1, R2, R3, R4, n, n?, V, W, Y, Z, Ar are as defined in the description, and to their methods of preparation and their therapeutic applications.Type: ApplicationFiled: July 2, 2012Publication date: July 11, 2013Applicant: SANOFIInventors: Patrice BELLEVERGUE, Patrick GRAILHE, Gary MCCORT, Stephen O'CONNOR, Olivier DUCLOS
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Publication number: 20130172344Abstract: An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.Type: ApplicationFiled: June 20, 2012Publication date: July 4, 2013Inventors: Motohide SATOH, Hiroshi Kawakami, Yoshiharu Itoh, Hisashi Shinkai, Takahisa Motomura, Hisateru Aramaki, Yuji Matsuzaki, Wataru Watanabe, Shuichi Wamaki
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Patent number: 8476429Abstract: An intermediate for production of a quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria.Type: GrantFiled: April 25, 2012Date of Patent: July 2, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Hisashi Takahashi, Hiroaki Inagaki, Satoshi Komoriya, Makoto Takemura, Rie Miyauchi
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Patent number: 8471027Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: GrantFiled: April 3, 2012Date of Patent: June 25, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Adrian Wai-Hing Cheung, Kevin Richard Guertin, Nancy-Ellen Haynes, Eric Mertz, Lida Qi, Yimin Qian, Nathan Robert Scott
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Patent number: 8470817Abstract: 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: GrantFiled: October 26, 2010Date of Patent: June 25, 2013Assignee: Sunesis Pharmaceuticals, Inc.Inventor: Anantha Sudhakar
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Patent number: 8470847Abstract: The disclosure relates to 7-alkynyl-1,8-naphthyridones of formula (I): wherein R1, R2, R3, and R4 are as defined in the disclosure, to compositions containing them, to processes for preparing them, and to their use in therapeutics.Type: GrantFiled: December 4, 2009Date of Patent: June 25, 2013Assignee: SanofiInventors: Antoine Alam, Sandrine Biscarrat, Isabelle Blanc, Françoise Bono, Olivier Duclos, Gary Mccort
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Publication number: 20130150400Abstract: In part, the present invention is directed to antibacterial compounds and salts thereof.Type: ApplicationFiled: August 9, 2012Publication date: June 13, 2013Applicant: Affinium Pharmaceuticals, Inc.Inventors: Henry Pauls, Jailall Ramnauth
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Patent number: 8461083Abstract: 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: GrantFiled: March 16, 2009Date of Patent: June 11, 2013Assignee: Syngenta LimitedInventors: Glynn Mitchell, David Phillip Bacon, Ian Henry Aspinall, Emma Briggs, Alaric James Avery, James Alan Morris, Claire Janet Russell, Roger Salmon
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Patent number: 8450243Abstract: 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: GrantFiled: March 31, 2010Date of Patent: May 28, 2013Assignee: Syngenta LimitedInventors: Roger Salmon, Glynn Mitchell, James Alan Morris
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Publication number: 20130116229Abstract: The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: November 8, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co.KG, AbbVie Inc.
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Patent number: 8415333Abstract: 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: GrantFiled: February 24, 2010Date of Patent: April 9, 2013Assignee: Respiratorious ABInventors: Martin Johansson, Viveca Thornqvist Otlner, Jorgen Toftered, David Wensbo, Maria Dalence
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Patent number: 8410132Abstract: 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: April 23, 2012Date of Patent: April 2, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Peter D. J. Grootenhuis, Sara S Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Lev T. D. Fanning
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Patent number: 8404709Abstract: 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: GrantFiled: June 1, 2007Date of Patent: March 26, 2013Assignee: Bayer Intellectual Property GmbHInventors: Santiago Figueroa Perez, Peter Kolkhof, Lars Bärfacker, Ingo Flamme, Karl-Heinz Schlemmer, Rolf Grosser, Klaus Münter, Andreas Knorr, Adam Nitsche
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Publication number: 20130065917Abstract: 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 26, 2012Publication date: March 14, 2013Inventors: Ae Ri KIM, Jin Hwa Lee, Ki Sook Park, Jong Ryoo Choi, Tae Hee Lee, Jay Hyok Chang, Do Hyun Nam, Hoon Choi
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Patent number: 8367831Abstract: Disclosed is a compound represented by the general formula: wherein R1 represents an aryl or heterocyclic group which may be substituted or the like; X1 represents a C2-C4 alkylene group or the like; X2, X3 and X5 independently represent NH, a bond or the like; X4 represents a lower alkylene group, a bond or the like; Y1 represents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z1, Z2, Z3, Z4, Z5 and Z6 independently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z3, Z4, Z5 and Z6 represents a nitrogen atom, or a salt thereof, which is useful as an antibacterial agent.Type: GrantFiled: May 10, 2012Date of Patent: February 5, 2013Assignees: Toyama Chemical Co., Ltd., Taisho Pharmaceutical Co., Ltd.Inventors: Taro Kiyoto, Junichi Ando, Tadashi Tanaka, Yasuhiro Tsutsui, Mai Yokotani, Toshiya Noguchi, Fumihito Ushiyama, Hiroki Urabe, Hiromasa Horikiri
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Patent number: 8334236Abstract: 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: GrantFiled: February 2, 2010Date of Patent: December 18, 2012Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Fumiaki Takabe, Yuuki Hirano, Akira Funyu, Masami Kobayashi, Takashi Mitsunari
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Patent number: 8329908Abstract: 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: September 10, 2010Date of Patent: December 11, 2012Assignee: Morphochem Aktiengesellschaft fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin
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Patent number: 8324238Abstract: Disclosed are aspartic acid salts of 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid, methods for preparing the same, and antimicrobial pharmaceutical compositions comprising the same.Type: GrantFiled: April 14, 2008Date of Patent: December 4, 2012Assignee: Dong Wha Pharmaceutical Co. Ltd.Inventors: Jei Man Ryu, Dong Rack Choi, Jin Yang, Sue Hye Yoon, Seung Hwan Kim, Sae Kwang Ku
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Patent number: 8314120Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: March 28, 2011Date of Patent: November 20, 2012Assignee: Abbott GmbH & Co. KGInventors: Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker
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Publication number: 20120277207Abstract: 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: November 17, 2010Publication date: November 1, 2012Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
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Publication number: 20120259119Abstract: The present invention relates to an isatin derivative having the formula (I), a medicament for treatment of tuberculoses containing that isatin derivative as well as a method for preparing isatin derivative according to formula (I).Type: ApplicationFiled: April 7, 2011Publication date: October 11, 2012Inventors: Tarek Aboul-Fadl Mohamed Hassan, Fayzah bint Ahmad S. Bin Jubair
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Publication number: 20120258982Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: ApplicationFiled: April 3, 2012Publication date: October 11, 2012Inventors: Adrian Wai-Hing Cheung, Kevin Richard Guertin, Nancy-Ellen Haynes, Eric Mertz, Lida Qi, Yimin Qian, Nathan Robert Scott
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Patent number: 8263613Abstract: In part, the present invention is directed to antibacterial compounds and salts thereof.Type: GrantFiled: February 15, 2008Date of Patent: September 11, 2012Assignee: Affinium Pharmaceuticals, Inc.Inventors: Henry Pauls, Jailall Ramnauth
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Patent number: 8263614Abstract: The disclosure relates to compounds of formula (I): wherein R1, R2, R3, and R4 are as defined in the disclosure, to compositions containing them, to processes for preparing them, and to their use in therapeutics.Type: GrantFiled: December 4, 2009Date of Patent: September 11, 2012Assignee: Sanofi-AventisInventors: Antoine Alam, Francoise Bono, Olivier Duclos, Gary McCort
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Publication number: 20120220571Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein X is O or N(R3); and R1, R2, R3 and Y are defined herein. The compounds 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 as hydrates or solvates thereof) 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: August 16, 2010Publication date: August 30, 2012Inventors: John S. Wai, Dai-shi Su, Catherine M. Wiscount
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Publication number: 20120184562Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.Type: ApplicationFiled: January 12, 2012Publication date: July 19, 2012Inventor: Kin-Chun Luk
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Patent number: 8222407Abstract: 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: GrantFiled: May 23, 2008Date of Patent: July 17, 2012Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasumichi Fukuda, Masanori Takadoi, Yoshikazu Asahina, Taro Sato, Haruaki Kurasaki, Hiroyuki Ebisu, Masaya Takei, Hideyuki Fukuda
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Publication number: 20120165322Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: June 29, 2011Publication date: June 28, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
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Publication number: 20120142635Abstract: 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: February 8, 2012Publication date: June 7, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Publication number: 20120135961Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.Type: ApplicationFiled: January 10, 2011Publication date: May 31, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Hans Locher, Christine Schmitt