Nitrogen Attached Indirectly To The Ring Nitrogen Of The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/477)
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Publication number: 20150094314Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.Type: ApplicationFiled: March 21, 2013Publication date: April 2, 2015Inventor: Chris Dealwis
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Publication number: 20150065711Abstract: Disclosed are linear discrete PEG constructs, which can be created and produced in a precise and reproducible way. Key to being able to do these things, where x in the discrete PEGx can vary from about 2 to about 64, is that the processes used to make each linear portion is controlled to give essentially one oligomer/one compound. Having a variable length linear discrete PEG construct that is (a) primarily an linear discrete PEG construct with diagnostic or therapeutic groups attached along a chain of attachment cores, which is attached to a preferential locator; (b) is an m-discrete PEG as the terminal construct on the linear portion, and “hidden”; (c or linear discrete PEG with a terminus group that can be either negatively or positively charged, or neutral; and any of the discrete PEG portions can be designed to be cleaved after entering the cell.Type: ApplicationFiled: August 15, 2014Publication date: March 5, 2015Applicant: EquIP, LLCInventor: Paul D. Davis
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Publication number: 20130324717Abstract: This invention relates to polymerizable ultraviolet light absorbers and yellow colorants and their use in ophthalmic lenses. In particular, this invention relates to polymerizable ultraviolet light absorbing methane compounds and yellow compounds of the methine and anthraquinone classes that block ultraviolet light and/or violet-blue light transmission through ophthalmic lenses.Type: ApplicationFiled: August 5, 2013Publication date: December 5, 2013Inventors: Jason Clay Pearson, Max Allen Weaver, Jean Carroll Fleischer, Gregory Allan King
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Patent number: 8598400Abstract: The present invention generally relates to methods for performing metathesis reactions, including cross-metathesis reactions. Methods described herein exhibit enhanced activity and stereoselectivity, relative to known methods, and are useful in the synthesis of a large assortment of biologically and therapeutically significant agents.Type: GrantFiled: February 8, 2011Date of Patent: December 3, 2013Assignees: Massachusetts Institute of Technology, Trustees of Boston CollegeInventors: Amir H. Hoveyda, Simon J. Meek, Robert V. O'Brien, Josep Llaveria Cros, Richard R. Schrock
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Publication number: 20130310559Abstract: Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.Type: ApplicationFiled: February 6, 2013Publication date: November 21, 2013Applicant: SIGNUM BIOSCIENCES, INC.Inventors: Jeffry B. Stock, Maxwell Stock, Keshava Rapole, Seung-Yub Lee, Michael Voronkov, Eduardo Perez, Joel Gordon, Shuyi Chen, Jinglong Chen
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Patent number: 8552242Abstract: The present invention generally relates to methods for performing metathesis reactions, including cross-metathesis reactions. Methods described herein exhibit enhanced activity and stereoselectivity, relative to known methods, and are useful in the synthesis of a large assortment of biologically and therapeutically significant agents.Type: GrantFiled: February 8, 2011Date of Patent: October 8, 2013Assignees: Massachusetts Institute of Technology, Trustees of Boston CollegeInventors: Amir H. Hoveyda, Simon J. Meek, Robert V. O'Brien, Josep Llaveria Cros, Richard R. Schrock
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Publication number: 20130165682Abstract: The present invention relates to a method for the synthesis of an ? amino acetal, comprising (i) oxidizing a tertiary amine in the presence of a copper catalyst, at least one oxidant and a solvent, or (ii) reacting a secondary amine and an aliphatic aldehyde in the presence of a copper catalyst, at least one oxidant and a solvent.Type: ApplicationFiled: July 6, 2011Publication date: June 27, 2013Applicant: NANYANG TECHNOLOGICAL UNIVERSITYInventors: Teck Peng Loh, Jiesheng Tian
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Patent number: 8455537Abstract: A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C?O) (C1-7)alkyl; Ra is (C1-7)alkyl or (C?O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.Type: GrantFiled: June 21, 2011Date of Patent: June 4, 2013Assignee: University of Medicine and Dentistry of New JerseyInventors: William J. Welsh, Ching Y. Wang, Ni Ai
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Patent number: 8426636Abstract: A sterically bulky stabilizer that is associated non-covalently with a benzimidazolone pigment. The sterically bulky stabilizer compound includes an aromatic acid derivative, and the presence of the sterically bulky stabilizer limits an extent of particle growth and aggregation, to afford nanoscale pigment particles.Type: GrantFiled: July 25, 2011Date of Patent: April 23, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff
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Publication number: 20130052130Abstract: Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.Type: ApplicationFiled: August 30, 2012Publication date: February 28, 2013Applicants: UNIVERSITY OF WASHINGTON, QUANTA BIODESIGN, LTD.Inventors: Paul D. Davis, D. Scott Wilbur
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Publication number: 20130018159Abstract: This invention relates to polymerizable ultraviolet light absorbers and yellow colorants and their use in ophthalmic lenses. In particular, this invention relates to polymerizable ultraviolet light absorbing methane compounds and yellow compounds of the methine and anthraquinone classes that block ultraviolet light and/or violet-blue light transmission through ophthalmic lenses.Type: ApplicationFiled: September 18, 2012Publication date: January 17, 2013Applicant: Abbott Medical Optics Inc.Inventors: Jason Clay Pearson, Max Allen Weaver, Jean Carroll Fleischer, Gregory Allan King
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Patent number: 8338474Abstract: Preparation and use of phthalimide and/or sulphonamide derivatives with nitric oxide donor properties, having activities in increasing gamma-globin gene expression and anti-inflammatory and analgesic activities, effective in the treatment of hematologic diseases which require reducing the TNF-? levels and an exogenous source of nitric oxide, such as sickle-cell disease. The functionalized phthalimide derivatives are designed from the prototypes thalidomide and hydroxyurea.Type: GrantFiled: February 24, 2012Date of Patent: December 25, 2012Inventors: Jean Leandro Dos Santos, Chin Chung Man, Lídia Moreira Lima, Fernando Ferreira Costa, Carolina Lanaro
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Patent number: 8328879Abstract: Agent for lightening keratin fibers, particularly human hair. The agent for lightening keratin fibers contains at least one cationic phthalimide of formula (I) in addition to an oxidant in a cosmetic carrier.Type: GrantFiled: June 18, 2012Date of Patent: December 11, 2012Assignee: Henkel AG & Co. KGaAInventors: Wibke Gross, Ralph Nemitz, Astrid Kroos
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Patent number: 8329751Abstract: The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, R4, R5, n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.Type: GrantFiled: March 14, 2008Date of Patent: December 11, 2012Assignee: Bracco Imaging S.p.A.Inventors: Aldo Balsamo, Armando Rossello, Elisa Nuti, Elisabetta Orlandini, Tiziano Tuccinardi
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Publication number: 20120260825Abstract: Dispersants for pigments as well as dispersions containing them, and compositions such as inks and coatings containing them are described. The dispersants are the reaction product of at least one dianhydride with at least two different reactants, each of which can be an amine, alcohol, or thiol, and at least one of which is polymeric.Type: ApplicationFiled: June 20, 2012Publication date: October 18, 2012Inventors: Tatiana N. ROMANOVA, Russell J. SCHWARTZ
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Patent number: 8288566Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:Type: GrantFiled: November 16, 2009Date of Patent: October 16, 2012Assignee: Novartis AGInventors: Murat Acemoglu, Andreas Pfaltz, Claude Schaerer
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Publication number: 20120208917Abstract: The invention relates to a dental restorative material which comprises (a) at least one antimicrobially active compound of Formula (I) [AG]m-R1—Z—SP—Y—R2—[WG]p??(I), or a filler that is surface-modified with at least one compound of Formula (I), (b) at least one radically polymerizable monomer and (c) at least one initiator for the radical polymerization. The invention also relates to a use of such dental restorative material for the preparation of an adhesive, primer, cement, coating material or filling material. The invention also relates to a dental material which comprises at least one compound of Formula (I), as well as a use of a compound of Formula (I) for modifying the surface of a substrate selected from ceramic materials, noble and non-noble metals, hard tooth structure, tooth enamel, dentine, collagen, soft tissue, mucous membrane and leather.Type: ApplicationFiled: February 8, 2012Publication date: August 16, 2012Applicant: IVOCLAR VIVADENT AGInventors: Ulrich SALZ, Thorsten BOCK, Christoph Peter FIK, Jörg TILLER, Volker RHEINBERGER
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Publication number: 20120094971Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.Type: ApplicationFiled: September 3, 2009Publication date: April 19, 2012Applicant: REPLIGEN CORPORATIONInventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
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Publication number: 20110319465Abstract: A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C?O) (C1-7)alkyl; Ra is (C1-7)alkyl or (C?O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.Type: ApplicationFiled: June 21, 2011Publication date: December 29, 2011Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: William Welsh, Ching Y. Wang, Ni Ai
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Publication number: 20110263873Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:Type: ApplicationFiled: November 16, 2009Publication date: October 27, 2011Inventors: Murat Acemoglu, Andreas Pfaltz, Claude Schaerer
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Publication number: 20110212078Abstract: This invention relates to compounds of the following Formula (I); or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.Type: ApplicationFiled: June 24, 2009Publication date: September 1, 2011Inventors: Panduranga Adulla P. Reddy, Umar Faruk Mansoor, M. Arshad Siddiqui
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Publication number: 20110136824Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: February 14, 2011Publication date: June 9, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20110130436Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.Type: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
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Patent number: 7943785Abstract: The present invention provides a process for producing (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-phthalimidomethylcyclopropane, which includes reacting (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-hydroxymethylcyclopropane with an orthoester and a brønsted acid, and reacting the reaction product with a phthalimidating agent; and a process for producing (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-aminomethylcyclopropane hydrochloride through the above process.Type: GrantFiled: January 26, 2007Date of Patent: May 17, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshihide Niimoto, Hiroharu Kumazawa, Koh Kawami
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Publication number: 20110112282Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof, in which each compound is adapted to occupy the binding site of human IDO, which comprises a large hydrophobic pocket A and a second, proximal hydrophobic pocket B, the compound comprising at least one of the following elements: (i) a large hydrophobic fragment to substantially fill pocket A in the binding site of human IDO; (ii) an atom that can coordinate to the heme iron of human IDO, (iii) a positively charged group that can form a salt-bridge with the heme 7-propionate of the human IDO; (iv) a negatively charged group that can form a salt-bridge with Arg231 of the human IDO; (v) a hydrophobic group that can form van der Waals interactions with pocket B; and (vi) one or more substituents that can hydrogen bond to Ser167 and to Gly262, and as IDO inhibitors and their therapeutic use, eg in the treatment of cancer.Type: ApplicationFiled: April 15, 2009Publication date: May 12, 2011Inventors: Ute Roehrig, Loay Awad, Olivier Michelin, Benoit Van Den Eynde, Luc Pilotte, Vincent Stroobant, Pierre Larrieu
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Publication number: 20110071304Abstract: A compound represented by the following general formula (I) (R1 and R2 represent hydrogen atom, an alkyl group, a halogen atom, etc.; R3 and R4 represent hydrogen atom, an alkyl group, an alkoxy group, or an alkenyl group; R5 represents hydrogen atom, an alkyl group, or nitro group, and R6 represents hydrogen atom or an alkyl group), which acts on the transcription process of genes.Type: ApplicationFiled: February 27, 2009Publication date: March 24, 2011Applicant: RESEARCH FOUNDATION ITSUU LABORATORYInventors: Nobuko Fujimaki, Madoka Nakagomi, Koichi Shudo
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Publication number: 20110003878Abstract: The invention relates to novel compounds of general formula (I), or one of the salts thereof, particularly one of the pharmaceutically acceptable salts thereof, or one of the corresponding solvates thereof. These compounds are inhibitors of the histone deacetylase enzymes and are suitable as pharmacologically active agents in a medicament for the treatment and/or prophylaxis of disorders or diseases associated with histone deacetylases. The invention also relates to a process for obtaining the mentioned compounds and the pharmaceutical compositions containing them.Type: ApplicationFiled: June 20, 2007Publication date: January 6, 2011Applicant: UNIVERSIDAD DE GRANADAInventors: Jose Antonio Gomez Vidal, Jose Francisco Dominguez Seglar, Mavys Tabraue Chavez
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Publication number: 20100324107Abstract: The present invention refers to the use of phthalimide and/or sulphonamide derivatives with nitric oxide donor properties, which have important activities in increasing the gamma-globin gene expression and anti-inflammatory and analgesic activities, effective in the treatment of hematologic diseases which require reducing the TNF-? levels and an exogenous source of nitric oxide. More particularly, the present invention describes the use of such phthalimide and/or sulphonamide derivatives for the treatment of sickle-cell disease. The invention also has as a novel characteristic the disclosure of new functionalized phthalimide derivatives designed from the prototypes thalidomide and hydroxyurea, and designed rationally through the strategy of molecular hybridization for the treatment of said diseases.Type: ApplicationFiled: December 12, 2008Publication date: December 23, 2010Applicants: UNIVERSIDADE ESTADUAL DE CAMPINAS - UNICAMP, UNIVERSIDADE FEDERAL DO RIO DE JANEIRO - UFRJInventors: Jean Leandro Dos Santos, Chin Chung Man, Lidia Moreira Lima, Fernando Ferreira Costa, Carolina Lanaro
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Patent number: 7820831Abstract: The invention relates to compounds having the general formula (I), the method of preparation thereof and the use thereof in organic radical synthesis. The invention also relates to compounds having the formula (II), the method of preparation thereof and a method for preparing compounds having the formula (VIII).Type: GrantFiled: August 6, 2008Date of Patent: October 26, 2010Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Samir Zard, Fabien Gagosz, Lucie Tournier
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Publication number: 20100183714Abstract: The present invention relates to the pharmaceutical dosage forms which enable a controlled and/or a targeted delivery of an active substance to the selected regions of gastrointestinal tract of humans or animals. The pharmaceutical dosage forms preferably comprises the active substance N-(2(2-phthalimidoethoxy)-acetyl)-L-alanyl-D-glutamic acid (designated as LK 423). Methods of treatment of chronic inflammatory diseases of gastrointestinal tract of humans and/or animals by using the pharmaceutical dosage forms of the invention are disclosed.Type: ApplicationFiled: March 24, 2005Publication date: July 22, 2010Applicant: LEK PHARMACEUTICALS D.D.Inventors: Marija Bogataj, Ales Mrhar, Anton Lavric, Manica Cerne, Doris Tibaut, Anton Stalc, Uros Urleb, Tatjana Mateovic, Greta Cof, Janez Kerc, Rok Dreu, Fumio Yoneda, Shizuko Muraoka
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Publication number: 20100152271Abstract: A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C?O)(C1-7)alkyl; Ra is (C1-7)alkyl or (C?O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.Type: ApplicationFiled: July 6, 2007Publication date: June 17, 2010Applicant: UNIVERSIT OF MEDICINE AND DENISTRY OF NEW JERSEYInventors: William J. Welsh, Nina Ching Y. Wang, Ni Ai
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Publication number: 20090247744Abstract: The invention relates to an improved process for the preparation of an advanced synthetic intermediate of ACE inhibitors. In one aspect, the present invention is based on a novel process for the preparation of an aldehyde of formula (I), wherein (N)PrG is a protected amino group, R is an alkyl or aralkyl group and X1-4 are each independently H or a non-reacting substituent, which comprises hydroformylation of an ?-olefin of formula (II), by reaction with syngas (CO/H2) in the presence of, as catalyst, a group VII transition metal complex of a phosphorus-containing ligand. Aldehyde (I), the product of linear hydroformylation, is formed in preference to aldehyde (III). In another aspect of the invention, ?-olefin (II) is a novel composition. The process to convert (II) to (I) enables an efficient manufacturing route to MDL 28,726 and analogues.Type: ApplicationFiled: June 10, 2009Publication date: October 1, 2009Inventors: Edward D Daugs, Wei-Jun Peng, Cynthia L Rand
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Publication number: 20080306281Abstract: The invention relates to compounds having the general formula (I), the method of preparation thereof and the use thereof in organic radical synthesis. The invention also relates to compounds having the formula (II), the method of preparation thereof and a method for preparing compounds having the formula (VIII).Type: ApplicationFiled: August 6, 2008Publication date: December 11, 2008Applicant: RHODIA OPERATIONSInventors: Samir Zard, Fabien Gagosz, Lucie Tournier
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Patent number: 7456183Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C?O, C?S, S?O, SO2, S, O, (CR6R7)n, C(?O)—(CR6R7)n, and C(?S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S?O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.Type: GrantFiled: April 8, 2002Date of Patent: November 25, 2008Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Daniel Chu, Rustum Boyce, David Duhl, Bryan Chang
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Patent number: 7405237Abstract: Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed.Type: GrantFiled: July 28, 2004Date of Patent: July 29, 2008Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Patent number: 7345062Abstract: Imido and amido substituted acylhydroxamidic acids which reduce the levels of TNF? and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propandylamino)propanoate.Type: GrantFiled: February 25, 2004Date of Patent: March 18, 2008Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
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Publication number: 20080009628Abstract: One-pot condensation-reduction methods for preparing substituted allylic alcohols as well as highly selective extractive methods to separate isomeric alcohols produced in the one-pot condensation-reduction processes are provided for preparing, for example, a quinolone.Type: ApplicationFiled: June 13, 2007Publication date: January 10, 2008Inventors: Michael Reuman, Roger Faessler, Armin Roessler, Kirk Sorgi, Xun Li, Jeffrey S. Grimm
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Patent number: 7056932Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.Type: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
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Patent number: 6989401Abstract: The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.Type: GrantFiled: July 19, 2001Date of Patent: January 24, 2006Assignee: Mitsubishi Pharma CorporationInventors: Kazuhiro Maeda, Shuji Sonda, Tadahiro Takemoto, Tomokazu Goto, Fujio Kobayashi, Masahiko Kajii, Naruyasu Komorita, Fumihiro Hirayama
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Patent number: 6939986Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.Type: GrantFiled: February 22, 2002Date of Patent: September 6, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Martin Karpf, René Trussardi
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Patent number: 6911464Abstract: The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4.Type: GrantFiled: March 12, 2004Date of Patent: June 28, 2005Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller
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Patent number: 6844359Abstract: Novel imides are inhibitors of tumor necrosis factor alpha and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is (R)-2-Phthalimido-3-(3?,4?-dimethoxyphenyl)propane.Type: GrantFiled: March 25, 2002Date of Patent: January 18, 2005Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Publication number: 20040235848Abstract: Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to &agr;4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning &agr;4 integrin in which &agr;4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.Type: ApplicationFiled: June 14, 2004Publication date: November 25, 2004Applicant: Ajinomoto Co., Inc.Inventors: Tatsuya Okuzumi, Kazuyuki Sagi, Toshihiko Yoshimura, Yuji Tanaka, Eiji Nakanishi, Miho Ono, Masahiro Murata
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Patent number: 6812237Abstract: Compounds of the formula (I), wherein R1 is aryl or biaryl; R2 is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; Y is O, S, SO, SO2, CO or NR6; R3 is hydrogen or lower alkyl; or R2 and R3 combined are C2-C7-alkylene or C2-C7-alkylene interrupted by Y; R4 is hydrogen or lower alkyl; R5 is hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; R6 is hydrogen, lower alkyl or aryl-lower alkyl; and pharmaceutically acceptable salts thereof, which are useful as cysteine cathepsin inhibitorsType: GrantFiled: November 7, 2002Date of Patent: November 2, 2004Assignee: Novartis AGInventors: Scott Douglas Cowen, Paul David Greenspan, Leslie Wighton McQuire, Ruben Alberto Tommasi, John Henry Van Duzer
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Publication number: 20040167174Abstract: Imido and amido substituted acyihydroxamidic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin -2-yl)-3-(3-ethoxy-4-methoxyphenyl)propandylamino)propanoate.Type: ApplicationFiled: February 25, 2004Publication date: August 26, 2004Applicant: CelgeneInventors: Hon-Wah Man, George W. Muller, Shaei Y. Huang
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Publication number: 20040044052Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.Type: ApplicationFiled: February 24, 2003Publication date: March 4, 2004Inventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh
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Patent number: 6699899Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.Type: GrantFiled: December 21, 1999Date of Patent: March 2, 2004Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
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Patent number: 6693202Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.Type: GrantFiled: August 25, 2000Date of Patent: February 17, 2004Assignee: Theravance, Inc.Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Publication number: 20040024045Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.Type: ApplicationFiled: February 24, 2003Publication date: February 5, 2004Inventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
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Publication number: 20030229128Abstract: Novel compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, type 1 diabetes, type 2 diabetes, disorders of the lipid metabolism and obesity.Type: ApplicationFiled: December 18, 2002Publication date: December 11, 2003Inventors: Peter Madsen, Carsten Behrens