Chalcogen Bonded Directly At 2-position Of The Oxazole Ring Patents (Class 548/229)
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Publication number: 20100105663Abstract: The invention relates to substituted indazoles and methods for production thereof and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, especially of cardiovascular diseases, preferably of thromboembolic diseases.Type: ApplicationFiled: July 2, 2007Publication date: April 29, 2010Applicant: BAYER HEALTHCARE AGInventors: Stephan Siegel, Dirk Schneider, Anja Buchmüller, Elke Dittrich-Wengenroth, Chrisstoph Gerdes, Mark Jean Gnoth, Stefan Heitmeier, Martin Hendrix, Ulrich Rester, Uwe Saatmann
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Publication number: 20100105919Abstract: In the preparation of zolmitriptan of formula III the reduction of the diazonium salt to (5)-4-(4-hydrazinobenzyl)-1,3-oxazolidin-2-one of formula IV is performed in a more concentrated mixture and by the effect on an alkali metal disulphite, preferably sodium disulphite. A zolmitriptan toluene solvate, characterized by a toluene content of 9 to 14% by weight according to the gas chromatography determination and by a maximum of the corresponding mass loss at temperatures of about 111° C. in the gravimetric analysis record. A zolmitriptan toluene solvate, showing strong Raman bands at the wave numbers of 1443 and 1354 cm?1, characteristic for the crystal lattice of zolmitriptan with built-in toluene, and further marked bands at 1004 and 786 cm?1, characteristic for toluene.Type: ApplicationFiled: February 25, 2008Publication date: April 29, 2010Inventors: Michal Voslar, Monika Zatopkova, Ludek Ridvan, Tomas Pekarek
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Patent number: 7705026Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: November 21, 2008Date of Patent: April 27, 2010Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20100099716Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: ApplicationFiled: November 25, 2009Publication date: April 22, 2010Inventors: Amjad ALI, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
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Patent number: 7691889Abstract: Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts act as antibacterial agents. Also mentioned is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai., including administering an antimycobacterially effective amount of the compound and/or pharmaceutically acceptable salts. There is also mentioned a process for the manufacture of the compound or its pharmaceutically acceptable salts.Type: GrantFiled: March 18, 2005Date of Patent: April 6, 2010Assignee: Lupin LimitedInventors: Sudershan Kumar Arora, Vijaykumar Jagdishwar Patil, Prathap Sreedharan Nair, Prasad Purushottam Dixit, Shankar Ajay, Rakesh Kumar Sinha
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Publication number: 20100056588Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.Type: ApplicationFiled: February 14, 2007Publication date: March 4, 2010Inventors: James Elliot Bradner, Ralph Mazitschek
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Publication number: 20100048548Abstract: The present invention relates to novel iminooxazolidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.Type: ApplicationFiled: April 8, 2006Publication date: February 25, 2010Applicant: Bayer HealthCare AGInventors: Susanne Röhrig, Jens Pohlmann, Elisabeth Perzborn, Christoph Gerdes, Karl-Heinz Schlemmer
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Publication number: 20100041724Abstract: An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The last step of the process is the coupling of an oxazolidinone derivative with a biphenyl moiety to provide a compound of formula (I). In a specific embodiment of this synthesis, a crystalline product is produced which is characterized as a non-solvated crystalline polymorph.Type: ApplicationFiled: June 29, 2006Publication date: February 18, 2010Inventors: Ross A. Miller, Aaron S. Cote
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Patent number: 7662977Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: December 21, 2007Date of Patent: February 16, 2010Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Publication number: 20100022772Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.Type: ApplicationFiled: July 28, 2004Publication date: January 28, 2010Applicant: RIB-X PHARMACEUTICALS, INC.Inventors: Yusheng Wu, Chen Shili, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
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Patent number: 7612210Abstract: A process for the enantioselective synthesis of an (S)- or (R)-1-[2-dimethylamino)-1-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described.Type: GrantFiled: December 4, 2006Date of Patent: November 3, 2009Assignee: WyethInventors: Paige Erin Mahaney, Madelene Miyoko Antane, Jerry Shunneng Sun
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Publication number: 20090264487Abstract: This invention provides analogs of hemiasterlin, methods of synthesis of the analogs and use of the analogs as a cytotoxic anti-mitotic agents.Type: ApplicationFiled: June 25, 2009Publication date: October 22, 2009Applicant: THE UNIVERSITY OF BRITISH COLUMBIAInventors: Raymond ANDERSEN, Edward Piers, James Nieman, John Coleman, Michel Roberge
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Patent number: 7582659Abstract: This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: January 22, 2007Date of Patent: September 1, 2009Assignees: Merck & Co., Inc., Kyorin Pharmaceutical Co., Ltd.Inventor: Yasumichi Fukuda
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Patent number: 7582666Abstract: The invention relates to the field of blood coagulation, more particularly, to novel compounds of general formula (I), to a method for producing the compounds and to their use as active ingredients in medicaments for the prevention and/or the treatment of diseases.Type: GrantFiled: March 31, 2006Date of Patent: September 1, 2009Assignee: Bayer Schering Pharma AGInventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Rohrig, Karl-Heinz Schlemmer
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Publication number: 20090216009Abstract: An industrially easily realizable and economical process comprising only few steps, and built on new intermediates for the production of 1-(4-3(R)-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the reaction scheme described herein.Type: ApplicationFiled: December 18, 2006Publication date: August 27, 2009Inventors: Jozsef Bodi, Janos Eles, Katalin Szoke, Krisztina Vukics, Tamas Gati, Krisztina Temesvari, Dorottya Kiss-Bartos
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Publication number: 20090209511Abstract: The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N? or —CH?; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.Type: ApplicationFiled: March 24, 2009Publication date: August 20, 2009Inventors: Takayuki Kawaguchi, Hidenori Akatsuka, Toru Iijima, Yasunori Tsuboi, Takashi Mitsui, Jun Murakami
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Publication number: 20090209590Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel inhibitors of histone deacetylases, tubulin deacetylases, and/or aggresome inhibitors, and pharmaceutically acceptable salts and derivatives thereof. The inventive compounds fall into two classes—“isotubacin” class and “isoisotubacin” class—all of which include a 1,3-dioxane core. The present invention further provides methods for treating disorders regulated by histone deacetylase activity, tubulin deacetylase activity, and/or the aggresome (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, protein degradation disorders, protein deposition disorders, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.Type: ApplicationFiled: May 2, 2007Publication date: August 20, 2009Inventors: Ralph Mazitschek, Nicholas Paul Kwiatkowski, James Elliot Bradner
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Publication number: 20090186834Abstract: Various azetidinone, pyrrolidine, imidazolidine, and oxazolidine derivatives are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.Type: ApplicationFiled: March 24, 2006Publication date: July 23, 2009Applicant: MICROBIA, INC.Inventors: John Talley, Eduardo Martinez, Daniel Zimmer, Regina Lundrigan
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Patent number: 7563904Abstract: In particular, this invention relates to the synthesis intermediates (IV), (V), (VI) and (VIII) useful for preparing zolmitriptanzohnitriptan or a pharmaceutically acceptable salt thereof, which includes a) Ppreparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with ?-keto-?-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Ttransesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Ssaponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Ddecarboxylation of the indolecarboxylic acid (VIII), to proviType: GrantFiled: November 15, 2007Date of Patent: July 21, 2009Assignee: Inke, S.A.Inventors: Pere Dalmases Barjoan, Montserrat Armengol Asparo
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Patent number: 7557214Abstract: The present invention describes intermediates (ZP) for a novel and efficient synthesis of compounds in which the pharmacophores of quinolone and oxazolidinone are linked to one another by way of a chemically stable linker.Type: GrantFiled: September 3, 2004Date of Patent: July 7, 2009Assignee: Morphochem Aktiengesellschaft für Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Jean Phillippe Surivet, Daniel Baeschlin
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Patent number: 7553860Abstract: A compound having the formula or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.Type: GrantFiled: June 6, 2007Date of Patent: June 30, 2009Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 7550448Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 11, 2007Date of Patent: June 23, 2009Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20090149520Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X is C1-4alkyl; and Y is H or F. The compounds of the present invention are useful as antibacterial agents.Type: ApplicationFiled: February 6, 2007Publication date: June 11, 2009Inventors: Gary Wayne Luehr, Sumithra Gowlugari, Mikhail Fedorovich Gordeev, Vara Prasad Venkata Nagendra Josyula
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Publication number: 20090137548Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.Type: ApplicationFiled: December 29, 2006Publication date: May 28, 2009Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
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Publication number: 20090118502Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: November 21, 2008Publication date: May 7, 2009Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Josseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20090105484Abstract: A compound of the formula (VIII) wherein each X is independently H or F; and R is selected from hydrogen, halogen, cyano, methyl, cyanomethyl, fluoromethyl, difluoromethyl, trifluoromethyl and —Si[(1-4C)alkyl]3; and processes for preparing a compound of formula (VIII) by bromination of a compound of the formula (VII),Type: ApplicationFiled: May 24, 2005Publication date: April 23, 2009Applicant: AstraZenecaInventors: Janette Cherryman, Murray Watson Cuthbert, Jerome Dubiez, Garnet Edward Howells, Keith Raymond Mulholland
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Publication number: 20090069313Abstract: The present invention provides a new medical use for the compounds of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, as MAO-A inhibitors. Also included is a method for prophylaxis and treatment of mental disorders such as depression, in a mammal, comprising administering an effective amount of a compound of formula (I). These compounds are also effective in treating a disease, condition or disorder such as weight loss, obesity, bulimia, depression, bipolar disorders, psychoses, schizophrenia, behaviors, alcoholism, tobacco abuse, memory loss, Alzheimer's disease, dementia of aging, seizure disorders, epilepsy, attention deficit disorder, and Parkinson's disease, which is modulated by a cannabinoid receptor antagonist.Type: ApplicationFiled: September 6, 2007Publication date: March 12, 2009Applicant: ORCHID RESEARCH LABORATORIES LTD.Inventors: Debendranath Dey, Gajendra Singh, Partha Neogi, Uma Ramachandran, Chithra Santhanagopalan
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Patent number: 7488829Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.Type: GrantFiled: May 7, 2007Date of Patent: February 10, 2009Assignee: Sanofi-Aventis Deutschland GmbHInventors: Heiner Glombik, Werner Krame, Stefanie Flohr, Wendelin Frick, Hubert Heuer, Gerhard Jaehne, Andreas Lindenschmidt, Hans-Ludwig Schäfer
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Patent number: 7488818Abstract: The present invention is directed to the preparation of novel compounds useful in the treatment of hyperlipidemia, arteriosclerosis, hypercholesterolemia, and other related metabolic disorders. More specifically, the present invention is a novel process for the preparation of 1,4-diphenylazetidinone derivatives from ?-substituted amino amides which are protected in the presence of silylating agents and at least one cyclization catalyst whose structural formula is represented by one of the general formula: wherein the various R-groups are defined herein.Type: GrantFiled: November 20, 2006Date of Patent: February 10, 2009Assignee: Sanofi-Aventis Deutschland GmbHInventors: Andreas Lindenschmidt, David William Will, Gerhard Jaehne, Theodor Andreas Wollmann, Wendelin Frick, Bernd Junker, David Rigal, Guenter Billen, Heiner Jendralla
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Publication number: 20090036504Abstract: The present application relates to novel 2-aminoethoxyacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.Type: ApplicationFiled: September 14, 2006Publication date: February 5, 2009Applicant: BAYER HEALTHCARE AGInventors: Christian R. Thomas, Susanne Rohrig, Elisabeth Perzborn
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Patent number: 7482467Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylococcus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.Type: GrantFiled: November 30, 2007Date of Patent: January 27, 2009Assignee: University of South FloridaInventors: Edward Turos, Rajesh Kumar Mishra
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Publication number: 20090023791Abstract: NMDA receptor blockers, including pH-sensitive NMDA receptor blockers, are provided as neurprotective drugs that are useful in stroke, traumatic brain injury, epilepsy, and other neurologic events that involve acidification of brain or spinal cord tissue. Compositions and methods of this invention are used for treating neurodegeneration resulting from NMDA receptor activation. The compounds described herein have enhanced activity in brain tissue having lower than normal pH due to pathological conditions such as hypoxia resulting from stroke, traumatic brain injury, global ischemia that may occur during cardiac surgery, hypoxia that may occur following cessation of breathing, pre-eclampsia, spinal cord trauma, epilepsy, chrounic pain, vascular dementia and glioma rumors.Type: ApplicationFiled: May 8, 2008Publication date: January 22, 2009Applicant: Emory UniversityInventors: Stephen F. Traynelis, Dennis C. Liotta, James P. Snyder, Yesim Altas, David D. Mott, James J. Doherty, JR., Raymond J. Dingledine
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Publication number: 20090023708Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.Type: ApplicationFiled: October 25, 2006Publication date: January 22, 2009Applicant: UCB PHARMA, S.A.Inventors: Sylvain Celanire, Luc Quere, Frederic Denonne, Laurent Provins
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Publication number: 20090018343Abstract: The present invention relates generally to perfluoroalkyl chiral auxiliary compounds and methods of manufacture. These compounds have the functionality to effectively support the synthesis of chiral compounds in single reactions, high-throughput parallel reactions, or combinatorial reactions The invention relates to two oxazolidinone chiral auxiliaries (1) and (2): wherein Rf is a perfluoroalkyl group having the general formula (CH2)x—CyF2y+1 where x=1-5 and y=4-10 and wherein B is an unfunctionalized aryl, alkyl or arylalkyl group in a preferred embodiment, x=2 and y=6 and B is derived from unfunctionalized amino acids The amino acids may be from either the D- or L-series, and are preferably enantiomerically pure or in very high enantiomeric excess in either configuration.Type: ApplicationFiled: March 16, 2006Publication date: January 15, 2009Applicant: The University of ManitobaInventors: Philip Gregory Hultin, Jason Ellis Hein
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Publication number: 20090012303Abstract: The present invention provides compounds and methods that can be used to convert the intermediate halomethyl ketones (HMKs), e.g., chloromethyl ketones, to the corresponding S,S- and R,S-diastereomers. More particularly, the present invention provides: (1) reduction methods; (2) inversion methods; and (3) methods involving the epoxidation of alkenes. Using the various methods of the present invention, the R,S-epoxide and the intermediary compounds can be prepared reliably, in high yields and in high purity.Type: ApplicationFiled: December 14, 2007Publication date: January 8, 2009Applicant: Aerojet Fine Chemicals LLCInventors: Aslam A. Malik, Todd E. Clement, Hasan Palandoken, James Robinson, III, Joy A. Stringer
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Publication number: 20090012089Abstract: The present invention is directed to compounds of Formula I: Wherein R1, R2, Y, m and n are further defined in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: ApplicationFiled: December 6, 2006Publication date: January 8, 2009Applicant: ASTRAZENECA ABInventors: Abdelmalik Slassi, Babu Joseph, Fupeng Ma, Ian Egle, Joshua Clayton, Methvin Isaac, Krzysztof Swierczek
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Patent number: 7473699Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein —N-HET is, for example, (Ic) or (If) wherein R1 is (1-4C)alkyl; Q is selected from, for example, Q1 wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, wherein m is 0, 1 or 2; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: GrantFiled: February 25, 2003Date of Patent: January 6, 2009Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hales, Folkert Reck, Fei Zhou, Paul Robert Fleming, Daniel Robert Carcanague, Marc Michel Girardot
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Patent number: 7462633Abstract: This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: June 29, 2004Date of Patent: December 9, 2008Assignees: Merck & Co., Inc., Kyorin Pharmaceutical Co., Ltd.Inventor: Yasumichi Fukuda
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Publication number: 20080274892Abstract: A haloalkylsulfonanilide derivative represented by the formula (I): {wherein R1 represents haloalkyl; R2 represents H, alkylcarbonyl, optionally substituted phenylcarbonyl, alkoxycarbonyl, optionally substituted phenoxycarbonyl, optionally substituted phenylsulfonyl, etc.; R3 and R4 each represents H, alkyl, cycloalkyl, halogeno, CN, etc.; R5, R6, R7, and R8 each represents H, halogeno, alkyl, cycloalkyl, optionally substituted phenyl(C1-6 alkyl), an optionally substituted heterocycle, etc.; A and W each represents O or S; and X represents one to four substituents selected among H, halogeno, alkyl, alkenyl, optionally substituted phenyl, optionally substituted phenylalkylaminocarbonyl, OH, CN, etc.} and a salt thereof; and a herbicide containing any of these compounds as an active ingredient. The herbicide is excellent in wide applicability, persistency, and selectivity for crops and effectiveness against weeds. It is excellent especially as a herbicide for rice fields.Type: ApplicationFiled: February 23, 2006Publication date: November 6, 2008Inventors: Tomokazu Hino, Toshihiko Shigenari, Takahiro Kiyokawa, Koki Mametsuka, Yasuko Yamada
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Publication number: 20080262240Abstract: Among other things, to cause directional motion of chiral objects in a mixture in a chamber, a field is rotated relative, to a chamber to cause rotation of the chiral objects. The rotation of the objects causes them to move directionally based on their chirality.Type: ApplicationFiled: April 15, 2008Publication date: October 23, 2008Inventors: Osman Kibar, Mirianas Chachisvilis, Eugene Tu, Thomas H. Marsilje
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Patent number: 7435751Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein R1 is C1-4alkyl, optionally substituted with a fluoro atom, or R1 is a cyclopropyl or cyclopropylmethyl; and R2 is methyl or ethyl. These compounds are useful as antibacterial agents.Type: GrantFiled: March 30, 2006Date of Patent: October 14, 2008Inventors: Vara Prasad Venkata Nagendra Josyula, Mikhail Gordeev, Gary Luehr
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Publication number: 20080249148Abstract: A polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form III are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. Also provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.Type: ApplicationFiled: March 10, 2008Publication date: October 9, 2008Applicant: WyethInventors: Mahmoud Mirmehrabi, Abdolsamad Tadayon, Subodh Deshmukh
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Patent number: 7432383Abstract: The present invention generally relates to at least one precursor compound and derivatives thereof, a process for preparing a taxane, and a baccatin derivative.Type: GrantFiled: March 7, 2007Date of Patent: October 7, 2008Assignee: Societe d'Etude et de Recherche En Ingenierie Pharmaceutique-SeripharmInventors: Luc Chanteloup, Bruno Chauveau, Christina Corbin, Robert Dhal, Sonia Le Guen, Arnaud Lamy, Antoine Leze, Jean-Pierre Robin
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Publication number: 20080242711Abstract: The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors.Type: ApplicationFiled: March 14, 2008Publication date: October 2, 2008Applicant: CONCERT PHARMCEUTICALS, INC.Inventor: Roger Tung
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Publication number: 20080234340Abstract: A polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form II are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. Further provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.Type: ApplicationFiled: March 10, 2008Publication date: September 25, 2008Applicant: WyethInventors: Mahmoud Mirmehrabi, Yuping Niu, Abdolsamad Tadayon, Subodh Deshmukh, Mannching Sherry Ku
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Publication number: 20080221181Abstract: The invention provides compounds of formula (I): wherein E, A, B?, R6, R7, R8, and R9 are defined in the specification which compounds exhibit anticancer activity and are useful for treating cancer.Type: ApplicationFiled: April 17, 2008Publication date: September 11, 2008Applicant: Wyeth Holdings CorporationInventors: Arie Zask, Joshua Kaplan, Ayako Yamashita, Chuan S. Niu, Gary Harold Birnberg, Emily Norton, Kinwang Cheung, Ronald Suayan, Vincent Sandanayaka, Philip Ross Hamann, Semiramis Ayral-Kaloustian
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Publication number: 20080207589Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:Type: ApplicationFiled: January 3, 2008Publication date: August 28, 2008Inventors: Rustum Boyce, Eric Martin, Weibo Wang, Hong Yang, Paul A. Barsanti
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Patent number: 7390826Abstract: Cell motility and growth inhibitors, including compounds of the general structural formula and use of the cell motility and cell growth inhibitors, and pharmaceutically acceptable salts, prodrugs, and solvates thereof, as therapeutic agents, are disclosed.Type: GrantFiled: October 26, 2005Date of Patent: June 24, 2008Assignee: The Board of Trustees of The University of IllinoisInventors: Gabriel Fenteany, Arun K. Ghosh, Kevin McHenry, Audha Ankala, Sarosh Anjum, Shoutian Zhu
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Publication number: 20080146458Abstract: Substituted oxazolidinone of the formula: wherein R2 is alkyl selected from the group consisting of methyl, ethyl, and isopropyl moieties, are described. The compounds are antibacterial.Type: ApplicationFiled: October 17, 2002Publication date: June 19, 2008Applicants: Board of Trustees of Michigan State University, Synthon Chiragenics CorporationInventors: Rawle I. Hollingsworth, Guijun Wang, Raghavakaimal Padmakumar, Jianmin Mao, Huiping Zhang, Zongmin Dai, Kanakamma Puthuparampil
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Publication number: 20080132543Abstract: A compound comprising a prodrug of a prostaglandin EP4 agonist, wherein said prodrug is an ester, ether, or amide of a carbohydrate; or said prodrug is an ester, ether, or amide of an amino acid is disclosed herein. Maintenance of the colonic mucosal barrier by method comprising administering a therapeutically effective amount of a prostaglandin EP4 agonist to a colon of a mammal is also disclosed herein. Dosage forms, medicaments, and compositions, related thereto are also disclosed.Type: ApplicationFiled: October 24, 2005Publication date: June 5, 2008Inventors: Wha Bin Im, Yariv Donde, Mark Holoboski, David W. Old, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Robert M. Burk, Todd Gac