Sulfur Containing Patents (Class 564/154)
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Patent number: 8013183Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: February 23, 2010Date of Patent: September 6, 2011Assignee: ViroBay, Inc.Inventors: Michael Graupe, John O. Link, Michael G. Roepel
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Publication number: 20110196014Abstract: Provided are methionine analogs which may be useful for inhibiting protein synthesis, inhibiting microbial growth and/or treating infectious diseases. In some instances, the analogs exhibit bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and/or antiviral properties. Also provided are methods of treatment and methods of preparation, as well as kits and unit dosages.Type: ApplicationFiled: July 31, 2009Publication date: August 11, 2011Inventors: Mansour Bassiri, Afsaneh Rahimi-Larijani
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Patent number: 7977509Abstract: A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.Type: GrantFiled: April 6, 2009Date of Patent: July 12, 2011Assignee: Hoffmann-La Roche Inc.Inventor: Ursula Hoffmann
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Patent number: 7964752Abstract: A bifunctional compound containing an amino group and diaminedithiol ligand and a manufacturing method thereof are revealed, the bifunctional compound includes at least one amino group and a diaminedithiol (N2S2) ligand. The amino groups is for reacting with compounds containing carboxylic acids or halogens while the N2S2 ligand binds with technetium or rhenium so as to form an anion complex. The thiol group in the N2S2 ligand is protected by a protecting group for prevention of oxidation and easy storage. This protecting group is released easily during complex reactions. Due to the bifunctional property, the compound is applied to preparation of radiopharmaceuticals such as imaging agents and targeted agents.Type: GrantFiled: August 13, 2009Date of Patent: June 21, 2011Assignee: Atomic Energy Council—Institute of Nuclear Energy ResearchInventors: Show-Wen Liu, Cheng-Hsien Lin, Tsyh-Lang Lin, Cheng-Fang Hsu
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Publication number: 20110136878Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.Type: ApplicationFiled: June 29, 2009Publication date: June 9, 2011Applicant: Mitsui Chemicals Agro., Inc.Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
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Publication number: 20110124664Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: ApplicationFiled: December 17, 2010Publication date: May 26, 2011Applicant: POLYMEDIX, INC.Inventors: Shaker Mousa, Dahui Liu
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Publication number: 20110082120Abstract: The invention relates to substituted thioacetic acid salicylate derivatives; compositions comprising an effective amount of a substituted thioacetic acid salicylate derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a substituted thioacetic acid salicylate derivative.Type: ApplicationFiled: October 5, 2010Publication date: April 7, 2011Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20110040123Abstract: A bifunctional compound containing an amino group and diaminedithiol ligand and a manufacturing method thereof are revealed, the bifunctional compound includes at least one amino group and a diaminedithiol (N2S2) ligand. The amino groups is for reacting with compounds containing carboxylic acids or halogens while the N2S2 ligand binds with technetium or rhenium so as to form an anion complex. The thiol group in the N2S2 ligand is protected by a protecting group for prevention of oxidation and easy storage. This protecting group is released easily during complex reactions. Due to the bifunctional property, the compound is applied to preparation of radiopharmaceuticals such as imaging agents and targeted agents.Type: ApplicationFiled: August 13, 2009Publication date: February 17, 2011Inventors: Show-Wen Liu, Cheng-Hsien Lin, Tsyh-Lang Lin, Cheng-Fang Hsu
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Publication number: 20110016642Abstract: The present invention relates to the dyeing of keratin materials using two colorless dye precursors, at least one of which contains a disulfide/thiol unit, said precursors reacting together chemically to form the color in situ. The process according to the invention makes it possible in the context of certain variants to solve the problems caused by the color generated during the process, while at the same time not degrading the efficacy of the coloration, and especially of the lightening effect. The colorations obtained are moreover powerful, chromatic, sparingly selective, and fast with respect to external agents such as sunlight, perspiration and especially shampoo.Type: ApplicationFiled: September 23, 2008Publication date: January 27, 2011Inventors: Andrew Greaves, Nicolas Daubresse
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Patent number: 7875268Abstract: The present disclosure relates to specific dimercaptoamides, reducing compositions for permanently reshaping keratin fibers comprising the dimercaptoamides, for instance, human keratin fibers such as the hair; and processes for reshaping keratin fibers comprising the application of said reducing compositions. The present disclosure also relates to processes for preparing the dimercaptoamides.Type: GrantFiled: April 6, 2005Date of Patent: January 25, 2011Assignee: L'Oreal S.A.Inventors: Michel Philippe, Gérard Malle, Christian Blaise
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Patent number: 7875746Abstract: A photosensitive composition comprising: (A) a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation, a pattern forming method using the photosensitive composition, and a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation.Type: GrantFiled: May 23, 2006Date of Patent: January 25, 2011Assignee: FUJIFILM CorporationInventor: Kenji Wada
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Publication number: 20100305331Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: February 23, 2010Publication date: December 2, 2010Applicant: ViroBay, Inc.Inventors: Michael Graupe, John O. Link, Michael G. Roepel
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Publication number: 20100298344Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: ApplicationFiled: March 10, 2010Publication date: November 25, 2010Inventors: Shaker Mousa, Dahui Liu
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Publication number: 20100286109Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: ApplicationFiled: July 22, 2010Publication date: November 11, 2010Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
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Publication number: 20100261788Abstract: Various phenylamine derivatives are described as well as the use of compounds to inhibit BID protein for controlling apoptotic cascade.Type: ApplicationFiled: June 22, 2010Publication date: October 14, 2010Inventors: John C. Reed, Maurizio Pellecchia
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Publication number: 20100249424Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.Type: ApplicationFiled: August 4, 2008Publication date: September 30, 2010Applicant: E.I.DuPont De Nemours and CompanyInventors: Gary David Annis, Brenton Todd Smith
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Patent number: 7786046Abstract: The present invention relates to benzoyl-substituted serinamides of the formula I in which the variables R1 to R11 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.Type: GrantFiled: March 29, 2006Date of Patent: August 31, 2010Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Cyrill Zagar, Eike Hupe, Toralf Kühn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Robert Reinhard, Bernd Sievernich, Klaus Groβmann, Thomas Ehrhardt
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Publication number: 20100196502Abstract: One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.Type: ApplicationFiled: August 2, 2007Publication date: August 5, 2010Applicant: Georgetown UniversityInventors: Alan P. Kozikowski, Mira Jung, Anatoly Dritschilo, Arsen Gaysin, Pavel A. Petukhov, Werner Tueckmantel, Hongbin Yuan
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Publication number: 20100197736Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.Type: ApplicationFiled: July 13, 2009Publication date: August 5, 2010Applicant: Japan Tobacco Inc.Inventors: Hisashi SHINKAI, Kimiya Maeda, Hiroshi Okamoto
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Patent number: 7741521Abstract: Various phenylamine derivatives are described as well as the use of compounds to inhibit BID protein for controlling apoptotic cascade.Type: GrantFiled: December 22, 2006Date of Patent: June 22, 2010Assignee: The Burnham InstituteInventors: John C. Reed, Maurizio Pellecchia
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Patent number: 7728171Abstract: A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.Type: GrantFiled: August 25, 2008Date of Patent: June 1, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Ursula Hoffmann, Goesta Rimmler
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Patent number: 7718684Abstract: A modest (2-5 fold) increase in androgen receptor (AR) mRNA is the only expression change consistently associated with developing resistance to antiandrogen therapy. Increased levels of AR confer resistance to anti-androgens by amplifying signal output from low levels of residual ligand and altering the normal response to antagonists. This invention provides cell based assays for use in the examination of new therapeutic modalities and provides for the design of novel antiandrogen compounds.Type: GrantFiled: February 23, 2005Date of Patent: May 18, 2010Assignee: The Regents of the University of CaliforniaInventors: Michael E. Jung, Samedy Ouk, Charles L. Sawyers, Charlie D. Chen, Derek Welsbie
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Patent number: 7696382Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X—Y is other than meta-C?—C—(CH2)2CO2H, meta-C?—C—(CH2)2OH, meta-C?C—(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X—Y is other than meta-C?Type: GrantFiled: February 21, 2005Date of Patent: April 13, 2010Assignee: University College LondonInventors: Masahiro Okuyama, David Selwood, Cristina Visintin, David Baker, Gareth Pryce
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Publication number: 20100081665Abstract: The present invention provides tricyclic compounds, arylamide compounds, and other compounds, and compositions comprising the same, for treating malaria, and methods of treating malaria comprising administering such compounds to an animal.Type: ApplicationFiled: July 28, 2009Publication date: April 1, 2010Inventors: Richard W. Scott, Doron Greenbaum, Dahui Liu, Xiaodong Fan, Yongjiang Xu, Haizhong Tang, Ehab Khalil
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Publication number: 20100062937Abstract: Benzanilides of the formula: in which X represents hydrogen, halogen, nitro, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl or C1-6 alkylsulfonyloxy; Y represents halogen or C1-6 alkyl; R1 represents C1-6 alkyl, C1-6 alkylthio C1-6 alkyl, C1-6 alkylsulfinyl-C1-6 alkyl or C1-6 alkylsulfonyl-C1-6 alkyl; R2 represents hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 represents hydrogen or hydroxy; W represents CH or N; and Q represents optionally substituted phenyl or optionally substituted pyridyl wherein the substituent is at least one group selected from the group consisting of halogen, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl and C1-6 haloalkylsulfoxy; provided that when R3 is hydroxy, R2 is not C1-6 alkyl, or when R2 is C1-6 haloalkyl, R3 is hydroxy, W is CH, and the substituents of Q are two or more C1-6 haloalkyl. Insecticides comprising the benzanilides are herein provided.Type: ApplicationFiled: June 2, 2006Publication date: March 11, 2010Applicant: BAYER CROPSCIENCE AGInventors: Katsuaki Wada, Tetsuya Murata, Katsuhiko Shibuya, Eiichi Shimojo
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Publication number: 20090312569Abstract: The present invention relates to a process for the preparation of 1-(2-ethyl-butyl)-cyclohexanecarboxylic acid which is useful as an intermediate in the preparation of pharmaceutically active compounds.Type: ApplicationFiled: June 12, 2009Publication date: December 17, 2009Inventor: Bruno Lohri
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Patent number: 7615187Abstract: This present invention provides materials for use as solid or concentrated chemical precursors for the production of organic peroxy acids (peracids). Organic peroxy acids are formed using a precursor according to the invention when they are combined with hydrogen peroxide or a hydrogen peroxide precursor such as a percarbonate or a perborate in aqueous medium. Organic peroxy acids, such as peroxyacetic acid, are used currently to disinfect medical equipment such as endoscopes and related items.Type: GrantFiled: August 24, 2007Date of Patent: November 10, 2009Assignee: D H Technologies, LLPInventors: Danny O. Helton, David W. Hobson
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Publication number: 20090253672Abstract: This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3, R4, R5, R6, R7, X and Y are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsms K L, S and B These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis, osteoarthritis and rheumatoid arthritisType: ApplicationFiled: October 10, 2006Publication date: October 8, 2009Inventors: Serge Leger, Christopher Bayly, Jean-Francois Truchon
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Patent number: 7579379Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.Type: GrantFiled: August 3, 2007Date of Patent: August 25, 2009Assignee: Japan Tobacco Inc.Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
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Patent number: 7553646Abstract: The present invention provides novel methods for the synthesis of racemic and enantiomers of modafinil via microbial oxidation-amidation transformation. The methods include the successive oxidation-amidation of benzhydrylsulfanyl carboxylic acid to produce racemic and enantiomers of modafinil using at least one microorganism of yeast, bacteria, or fungus. Also disclosed are pharmaceutical compositions of racemic and enantiomers of modafinil along with their use in the treatment of diseases, including attention deficit hyperactivity disorder and drug addiction.Type: GrantFiled: July 27, 2006Date of Patent: June 30, 2009Assignee: University of Iowa Research FoundationInventors: Horacio F. Olivo, Antonio Victor Osorio-Lozada
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Publication number: 20090163543Abstract: One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.Type: ApplicationFiled: December 19, 2008Publication date: June 25, 2009Applicant: Georgetown UniversityInventors: Alan P. Kozikowski, Bin Chen
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Publication number: 20090118375Abstract: Novel optically active phthalamides of the formula (I) in which A, q, R1, R2, E1, E2, X, m, Y, n and Z are as defined in the description, processes for preparing these compounds and their use for controlling pests.Type: ApplicationFiled: August 20, 2005Publication date: May 7, 2009Inventors: Rudiger Fischer, Christian Funke, Olga Malsam, Peter Losel, Ulrich Gorgens, Christian Arnold, Masanori Tohnischi, Minoru Yamaguchi, Hiroto Harayama, Shinsuke Fujioka
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Publication number: 20090099204Abstract: The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. The compound represented by the general formula (1) and an insecticide comprising the compound as an active ingredient, wherein, in the formula, A1, A2, A3 and A4 each represent a carbon atom or the like; R1 and R2 are each a hydrogen atom, an alkyl group or the like; G1 and G2 are each an oxygen atom or the like; X represents a hydrogen atom, a halogen atom or the like; n is an integer of 0 to 4; Q1 represents a substituted phenyl group, a substituted heterocyclic group or the like; Q2 represents a phenyl group having a haloalkyl sulfur group or the like, a heterocyclic group or the like.Type: ApplicationFiled: June 20, 2006Publication date: April 16, 2009Applicant: Mitsui Chemicals, Inc.Inventors: Kei Yoshida, Yumi Kobayashi, Michikazu Nomura, Nobuyuki Kawahara, Hidenori Daido, Shinichi Inomata
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Publication number: 20090091234Abstract: A salt molten at room temperature that does not contain any organic solvent, excelling in stability; and a display device that is improved in the durability in high-temperature environment by virtue of the use thereof. There is provided a salt molten at room temperature characterized by being composed of a silver salt and any of compounds of the following general formula (I) or general formula (II).Type: ApplicationFiled: April 6, 2006Publication date: April 9, 2009Applicant: KONICA MINOLTA HOLDINGS, INC.Inventor: Noriyuki Kokeguchi
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Publication number: 20090053817Abstract: The present invention relates to fixed charge reagents and kits for use in tandem mass spectrometry methods involving multiplex analysis. The compounds of the invention are phenacylamide compounds. The invention also relates to methods for the quantification of for example peptides and proteins by tandem mass spectrometry techniques using said reagents and kits. The reagents and kits of the invention enable multiplexed analysis of several samples in one experiment.Type: ApplicationFiled: August 16, 2005Publication date: February 26, 2009Applicants: LUDWIG INSTITUTE FOR CANCER RESEARCH, GE HEALTHCARE BIO-SCIENCES ABInventors: Gavin E. Reid, Kade D. Roberts, Henrik Neu, Maria Liminga
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Patent number: 7488848Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: March 17, 2006Date of Patent: February 10, 2009Assignee: Virobay, Inc.Inventors: Michael Graupe, John O. Link, Michael G. Roepel
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Publication number: 20090036311Abstract: The present invention relates to benzoyl-substituted alanines of the formula I in which the variables R1 to R12 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.Type: ApplicationFiled: February 7, 2007Publication date: February 5, 2009Applicant: BASF SEInventors: Matthias Witschel, Cyrill Zagar, Eike Hupe, Toralf Kuhn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt
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Patent number: 7476763Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I: methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical formulations and related methods of treating or inhibiting certain diseases or conditions.Type: GrantFiled: November 9, 2006Date of Patent: January 13, 2009Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann
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Publication number: 20080299637Abstract: A method of reacting a first chemical entity and a second chemical entity to form a conjugate in which the first and second chemical entities are covalently bound with respect to each other, comprises bringing into simultaneous contact the first chemical entity, the second chemical entity and a thiol generator, wherein the thiol generator reacts with the first chemical entity in a thiolation reaction resulting in formation of a free sulfhydryl group on the first chemical entity, and the free sulfhydryl group reacts with the second chemical entity to form the conjugate, and wherein the second chemical entity is polyvalent with respect to its reactivity with sulfhydryl groups. The present invention primarily differs from the prior art in that no separation step is involved between reaction of the thiol generator and first chemical entity and reaction with the second chemical entity. The invention also provides a conjugation kit.Type: ApplicationFiled: December 12, 2006Publication date: December 4, 2008Inventors: Nicholas Gee, Michael Knowles
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Patent number: 7459585Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: March 24, 2005Date of Patent: December 2, 2008Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Publication number: 20080287499Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antiinflammatory, antiarthritic and antiviral activity.Type: ApplicationFiled: June 19, 2008Publication date: November 20, 2008Applicant: INDENA S.P.A.Inventors: Ezio Bombardelli, Gabriele Fontana
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Patent number: 7449493Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.Type: GrantFiled: July 14, 2005Date of Patent: November 11, 2008Assignees: Bristol-Myers Squibb Pharmaceutical Company, Bristol-Myers Squibb Pharma CompanyInventors: Percy Carter, Robert Cherney
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Publication number: 20080261235Abstract: The present invention provides novel fluorescent compounds and covalent attachment chemistries which facilitate the use of these compounds as labels for ultrasensitive and quantitative fluorescent detection of low levels of biomolecules. In a preferred embodiment, the fluorescent labels of this invention are novel derivatives of the hydroxy-pyrene trisulpbonic and disulphonic acids which may be used in any assay in which radioisotopes, colored dyes or other fluorescent molecules are currently used. Thus, for example, any assay using labeled antibodies, proteins, oligonucleotides or lipids, including fluorescent cell sorting, fluorescence microscopy (including dark-field microscopy), fluorescence polarization assays, ligand, receptor binding assays, receptor activation assays and diagnostic assays can benefit from use of the compounds disclosed herein.Type: ApplicationFiled: December 29, 2007Publication date: October 23, 2008Inventors: Ram Bhatt, Michael J. Conrad, Azzouz Bencheikh, Yifeng Xiong
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Patent number: 7439394Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.Type: GrantFiled: November 9, 2006Date of Patent: October 21, 2008Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann
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Patent number: 7435849Abstract: A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.Type: GrantFiled: October 17, 2006Date of Patent: October 14, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Ursula Hoffmann, Goesta Rimmler
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Publication number: 20080200542Abstract: The present invention relates to benzoyl-substituted serineamides of the formula I in which the variables R1 to R11 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.Type: ApplicationFiled: March 29, 2006Publication date: August 21, 2008Applicant: BASF AktiengesellschaftInventors: Matthias Witschel, Cyrill Zagar, Eike Hupe, Toralf Kuhn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt
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Publication number: 20080176807Abstract: The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.Type: ApplicationFiled: October 31, 2007Publication date: July 24, 2008Inventors: William F. DeGrado, Gregory N. Tew, Michael L. Klein, Dahui Liu, Jing Yuan, Sungwook Choi
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Patent number: 7399788Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula (I) in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —COHN—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula (I) have antiproliferative, antinflammatory, antiarthritic and antiviral activity.Type: GrantFiled: February 1, 2005Date of Patent: July 15, 2008Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Gabriele Fontana
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Publication number: 20080138309Abstract: The present invention relates to the use of aminodithiols as reducing agents for hair perming. It further relates to a hair perming method using these aminodithiols.Type: ApplicationFiled: January 19, 2006Publication date: June 12, 2008Inventors: Gerald Malle, Christian Blaise
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Publication number: 20080095704Abstract: The invention relates to compounds suitable for use in an imaging agent said imaging agent showing an improved pharmacokinetic profile.Type: ApplicationFiled: July 1, 2005Publication date: April 24, 2008Inventors: Alan Cuthbertson, Magne Solbakken