Benzene Ring Containing Patents (Class 514/520)
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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: 7713519Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from a UV-absorbing molecule has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds of formulas (I) and (V) having an alkoxy radical preferably in the four (para) position (hereinafter methoxy crylenes) on one or both of the phenyl rings: wherein at least one of R1 and R2 is a straight or branched chain C1-C12 alkoxy radical, preferably C1-C8, more preferably C1-C4, and most preferably methoxy, and any non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C24 alkyl radical, preferably C12-C24, more preferably C20; wherein A and B are the same or different and are selected from the group consisting of oxygen, amino and sulfur; R1 and R3 are the same or different and are selected from the group consisting of C1-C30 alkyl, C2-C30 alkylene, C2-C30 alkyne, C3-C8 cycloalkyl, C1-C30 substituted alkylene, C2-C30 substituted alkyne, aryl, substituted aryl, heType: GrantFiled: October 29, 2008Date of Patent: May 11, 2010Assignee: Hallstar Innovations Corp.Inventors: Craig A. Bonda, Anna Pavlovic
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Publication number: 20100081714Abstract: Mixtures containing gamma-cyhalothrin [(S)-?-cyano-3-phenoxybenzyl (Z)-(1R,3R)-3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethylcyclopropanecarboxylate] and another compound having insecticidal, nematicidal, acaricidal, molluscicidal, fungicidal, plant growth regulating or herbicidal activity are provided. Compositions containing the mixture and insecticidal methods using such mixtures or compositions are also provided.Type: ApplicationFiled: December 8, 2009Publication date: April 1, 2010Inventor: Martin Stephen Clough
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Publication number: 20100048700Abstract: New agrochemical formulations have been found, comprising at least one active agrochemical compound from the group of the pyrethroids at least one surfactant at least one solvent a polar co-solvent, which exhibit improved rain resistance and improved biological activity over known pyrethroid formulations.Type: ApplicationFiled: June 27, 2007Publication date: February 25, 2010Applicant: Bayer CropScience AGInventors: Lorna Elizabeth Davies, Peter Baur, Wolfgang Thielert, Richard Dickmann, Jurgen Kuhnhold, Heike Hungenberg
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Patent number: 7662849Abstract: 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: June 4, 2004Date of Patent: February 16, 2010Assignee: ViroBay, Inc.Inventors: John W. Patterson, Soon H. Woo
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Publication number: 20100035985Abstract: An ester compound represented by the formula (1): wherein R represents a C1-C4 alkyl group or a C3-C4 alkenyl group, and A represents a single bond or an oxygen atom, has an excellent pest controlling efficacy, and it is useful as an active ingredient of a pest controlling agent.Type: ApplicationFiled: February 27, 2009Publication date: February 11, 2010Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Tatsuya Mori
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Publication number: 20100028348Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as heart failure.Type: ApplicationFiled: September 17, 2009Publication date: February 4, 2010Applicant: MITOTEK, LLCInventor: Paul Q. Anziano
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Publication number: 20100022640Abstract: Esters of 2-phenylalkanenitriles, such as 3-acetoxy-2-(2-chloro-5-(difluoromethoxy)phenyl)propanenitrile and 3-acetoxy-2-(4-chlorophenyl)propanenitrile, and compositions containing such esters, are useful as fungicides at very low concentrations.Type: ApplicationFiled: December 10, 2007Publication date: January 28, 2010Inventor: Donald Wesley Stoutamire
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Patent number: 7649018Abstract: Compounds of formula II wherein each R1 and R2 is independently selected from H and —P(O)(R3)(R4), provided that at least one of R1 and R2 is —P(O)(R3)(R4); each R3 and R4 is independently selected from the group consisting of H, —OH, C1-C6 alkyl, and C1-C6 alkoxy; or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising a compound of formula II, and methods of administering such compounds and compositions.Type: GrantFiled: February 20, 2008Date of Patent: January 19, 2010Assignee: Wyeth LLCInventors: Mahdi B. Fawzi, Parimal R. Desai, Tianmin Zhu
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Publication number: 20090298887Abstract: The present invention is directed to a method for improving the quality of seeds harvested from seed-producing plants. The method comprises treating the pre-planted seeds of the seed-producing plants with a seed treatment insecticide and treating the resulting plant with foliar applications of a foliar insecticide; or treating the pre-planted seeds of the seed-producing plants with a seed treatment insecticide; or treating seed-producing plants with foliar applications of a foliar insecticide.Type: ApplicationFiled: December 8, 2005Publication date: December 3, 2009Applicant: Syngenta Corp Protection, Inc.Inventor: Clifford Watrin
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Publication number: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Patent number: 7597825Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from a UV-absorbing molecule has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds of formulas (I) and (V) having an alkoxy radical preferably in the four (para) position (hereinafter methoxy crylenes) on one or both of the phenyl rings: wherein at least one of R1 and R2 is a straight or branched chain C1-C12 alkoxy radical, preferably C1-C8, more preferably C1-C4, and most preferably methoxy, and any non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C24 alkyl radical, preferably C12-C24, more preferably C20; wherein A and B are the same or different and are selected from the group consisting of oxygen, amino and sulfur; R1 and R3 are the same or different and are selected from the group consisting of C1-C30 alkyl, C2-C30 alkylene, C2-C30 alkyne, C3-C8 cycloalkyl, C1-C30 substituted alkylene, C2-C30 substituted alkyne, aryl, substituted aryl, heType: GrantFiled: August 9, 2007Date of Patent: October 6, 2009Assignee: Hallstar Innovations Corp.Inventors: Craig A. Bonda, Anna Pavlovic
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Patent number: 7588702Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from a UV-absorbing molecule has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds of formulas (I) and (V) having an alkoxy radical preferably in the four (para) position (hereinafter methoxycrylenes) on one or both of the phenyl rings: wherein at least one of R1 and R2 is a straight or branched chain C1-C12 alkoxy radical, preferably C1-C8, more preferably C1-C4, and most preferably methoxy, and any non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C24 alkyl radical, preferably C12-C24, more preferably C20; ?wherein A and B are the same or different and are selected from the group consisting of oxygen, amino and sulfur; R1 and R3 are the same or different and are selected from the group consisting of C1-C30 alkyl, C2-C30 alkylene, C2-C30 alkyne, C3-C8 cycloalkyl, C1-C30 substituted alkylene, C2-C30 substituted alkyne, aryl, substituted aryl,Type: GrantFiled: January 30, 2008Date of Patent: September 15, 2009Assignee: Hallstar Innovations Corp.Inventors: Craig A. Bonda, Anna Pavlovic
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Publication number: 20090170883Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.Type: ApplicationFiled: November 12, 2008Publication date: July 2, 2009Applicants: KUMIAI CHEMICAL INDUSTRY CO., LTD., IHARA CHEMICAL INDUSTRY CO., LTD.Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
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Publication number: 20090163582Abstract: Pesticide concentrates are provided containing an emulsifier that is an EPA list 4 inert and is a polyglycerol fatty acid ester, a sorbitan fatty acid ester or a combination thereof, a pesticide and a solvent that is either a EPA list 3 inert of acetyl ester, EPA list 4 inert of a methyl fatty ester, an acetyltributyl citrate, white mineral oil or a combination thereof. The pesticide can be a water-insoluble synthetic pyrethroid, natural pyrethrum, channel blocking insecticide, acetylcholinesterase inhibitor, oxadiazine, organophosphate, neonicotinoid insecticide, thiamethoxam, imidacloprid, acetamiprid, thiacloprid, clothianidin, nitenpyran, insect growth regulator, juvenile hormone mimic, fermentation insecticide, plant oil insecticide acaracide, miticide, fungicide, herbicide and combinations thereof. The pesticide concentrate is diluted with a hydrocarbon solvent, a white mineral oil or a combination thereof and mixed with water.Type: ApplicationFiled: April 4, 2006Publication date: June 25, 2009Inventors: Yueh Wang, Ian R. Gecker, John Lucas, Ashish Shah
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Publication number: 20090130156Abstract: The present invention relates to a new formulation characterised by the presence of two components, one of which (A) possesses insecticidal, acaricidal, fungicidal, snailcidal or vermicidal activity and the other (B) exhibits synergistic activity with the first by enhancing its effectiveness, and in which the average release time of component (A) is 1 to 12 hours later than the average release time of component (B). The formulation is obtained by: a) separate microencapsulation of both components (A) and (B) within a multilayer system of specific polymers in which component (A) is in a more interior portion of the capsule than component (B), being separated from component (B) by a polymer layer of suitable thickness (FIG. 1); b) microencapsulation of both components within a single layer system (FIG. 2), combined with an immediate-release emulsion/microemulsion containing an additional amount of component (B).Type: ApplicationFiled: April 20, 2006Publication date: May 21, 2009Applicant: ENDURA S.P.A.Inventors: Valerio Borzatta, Oreste Picolo, Elisa Capparella
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Patent number: 7531573Abstract: The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. the compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.Type: GrantFiled: June 3, 2003Date of Patent: May 12, 2009Assignee: Children's Medical Center CorporationInventors: Carlo Brugnara, Jose Halperin, Emile M. Bellot, Jr., Mark Froimowitz, Richard John Lombardy, John J. Clifford, Ying-Duo Gao, Reem M. Haidar, Eugene W. Kelleher, Falguni M. Kher, Adel M. Moussa, Yesh P. Sachdeva, Minghua Sun, Heather N. Taft
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Publication number: 20090110707Abstract: Disclosed are compositions and methods related to powder and granular emulsifiable concentrate pesticide formulations. As disclosed, emulsions from non-aqueous based liquid or solvent soluble pesticide actives may be prepared using a high purity, high molecular weight sulfonated lignin as the emulsion stabilizer. The resulting emulsions may then be dried to obtain a powder or granular emulsion concentrate where the high molecular weight sulfonated lignin acts as a solid matrix for the pesticide active. The powder or granular emulsifiable concentrate formulations thus formed have high loading rates, good storage properties and are easily reconstituted when added to water.Type: ApplicationFiled: October 29, 2007Publication date: April 30, 2009Inventors: Thomas S. Winowiski, Stuart E. Lebo, JR., Scott E. Davis, Stig Are Gundersen
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Publication number: 20090099135Abstract: Embodiments of the present invention provide compositions for controlling a target pest including a pest control product and at least one active agent, wherein: the active agent can be capable of interacting with a receptor in the target pest; the pest control product can have a first activity against the target pest when applied without the active agent and the compositions can have a second activity against the target pest; and the second activity can be greater than the first activity.Type: ApplicationFiled: January 16, 2008Publication date: April 16, 2009Applicant: TyraTech, Inc.Inventor: Essam Enan
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Patent number: 7518013Abstract: The present invention relates to androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity, which are nonsteroidal ligands for the androgen receptor.Type: GrantFiled: February 14, 2006Date of Patent: April 14, 2009Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
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Publication number: 20090075902Abstract: The present invention relates to methods and compositions for reducing and/or delaying one or more signs of aging which comprise inhibiting NF-kappa B activation. It is based, at least in part, on the discovery that a peptide which inhibits IKK-? interaction with NEMO, linked to a transducing peptide, inhibits the development of various indicia of senescence in a murine model of aging, Ercc1?/? mice.Type: ApplicationFiled: May 23, 2008Publication date: March 19, 2009Inventors: Paul D. Robbins, Laura J. Niedernhofer
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Publication number: 20090018143Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: ApplicationFiled: November 8, 2007Publication date: January 15, 2009Applicants: Cephalon, Inc., Cephalon FranceInventors: Brigitte Lesur, Philippe Louvet, Rabindranath Tripathy
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Patent number: 7476650Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.Type: GrantFiled: June 17, 2004Date of Patent: January 13, 2009Assignee: Yale UniversityInventors: Craig M. Crews, Mikael Elofsson, Ute Splittgerber, Kyung Bo Kim
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Patent number: 7470723Abstract: The present invention relates to Diphenylethylene Compounds and compositions comprising a Diphenylethylene Compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more Diphenylethylene Compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more Diphenylethylene Compounds. The present invention further relates to articles of manufacture and kits comprising one or more Diphenylethylene Compounds.Type: GrantFiled: September 3, 2004Date of Patent: December 30, 2008Assignee: Celgene CorporationInventors: George W. Muller, Faribourz Payvandi, Ling H. Zhang, Michael J. Robarge, Roger Chen, Hon-Wah Man, Alexander L. Ruchelman
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Patent number: 7468446Abstract: The present invention relates to substituted heterocyclic compounds and compositions comprising a substituted heterocyclic compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more substituted heterocyclic compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more substituted heterocyclic compounds. The present invention further relates to articles of manufacture and kits comprising one or more substituted heterocyclic compounds.Type: GrantFiled: September 1, 2005Date of Patent: December 23, 2008Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Publication number: 20080312290Abstract: Agrochemical formulation comprising at least one room-temperature-solid active substance from the class of the neonicotinoids, at least one room-temperature-solid active substance from the class of the pyrethroids, at least one penetrant, at least one vegetable oil, cyclohexanone, at least one nonionic surfactant and/or at least one anionic surfactant, and one or more additives, process for producing it, and its use for controlling harmful organisms.Type: ApplicationFiled: September 28, 2006Publication date: December 18, 2008Applicant: Bayer CropScience AGInventors: Ronald Vermeer, Manuela Eberhard
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Publication number: 20080300178Abstract: The present invention relates to a method for treating patients having Huntington's disease by a drug increasing the phosphorylation of huntingtin at position S421, thereby decreasing the polyQ-huntingtin-induced toxicity.Type: ApplicationFiled: January 18, 2007Publication date: December 4, 2008Applicants: Insitut Curie, Centre National De La Recherche ScientifiqueInventors: Raul Pardo, Sandrine Humbert, Frederic Saudou
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Publication number: 20080293809Abstract: The present invention relates to a pest control composition that includes a pest control active ingredient and a polyoxypropylene-polyoxyethylene ether of a long chain fatty alcohol as an agent to reduce or eliminate paraesthesia of the active ingredient to a warm blooded mammal. The system releases the active ingredient efficiently and uniformly. The pest control formulation is less irritating to the animal's skin as compared to prior art systems. The formulation is useful for making animal collars, ear tags, pest strips, liquid spot-on treatments, and the like.Type: ApplicationFiled: May 21, 2008Publication date: November 27, 2008Inventor: Donald W. Kelley
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Publication number: 20080269283Abstract: Aryl sulfone compounds of formula I and II are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: ApplicationFiled: June 27, 2008Publication date: October 30, 2008Inventors: Pingchen Fan, Hiroyuki Goto, Xiao He, Makoto Kukutani, Marc Labelle, Dustin L. McMinn, Jay P. Powers, Yosup Rew, Daqing Sun, Xuelei Yan
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Publication number: 20080176280Abstract: This invention relates to the field of biotechnology or genetic engineering. Specifically, this invention relates to the field of gene expression. More specifically, this invention relates to a novel ecdysone receptor/chimeric retinoid X receptor-based inducible gene expression system and methods of modulating gene expression in a host cell for applications such as gene therapy, large-scale production of proteins and antibodies, cell-based high throughput screening assays, functional genomics and regulation of traits in transgenic organisms.Type: ApplicationFiled: August 20, 2007Publication date: July 24, 2008Inventors: Marianna Zinovjevna Kapitskaya, Subba Reddy Palli
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Patent number: 7402704Abstract: Aryl sulfone compounds of formula I and II are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: GrantFiled: April 14, 2005Date of Patent: July 22, 2008Assignee: Amgen Inc.Inventors: Pingchen Fan, Hiroyuki Goto, Xiao He, Makoto Kakutani, Marc Labelle, Dustin L. McMinn, Jay P. Powers, Yosup Rew, Daqing Sun, Xuelei Yan
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Publication number: 20080167380Abstract: Novel acyl hydrazides of the formula (I), in which R1-R9 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.Type: ApplicationFiled: March 10, 2006Publication date: July 10, 2008Inventors: Rolf Gericke, Dieter Dorsch, Werner Mederski, Markus Klein, Norbert Beier, Florian Lang
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Patent number: 7390833Abstract: The present invention relates to methods of treating ADAMTS-5-associated diseases and particularly osteoarthritis comprising administering an agent capable of modulating ADMATS-5 activity to a subject afflicted with the disease. The agent is preferably a biaryl sulfonamide compound. The invention is based, in part, on the discovery that transgenic animals that do not express functional ADAMTS-5 show a reduction in the degree of osteoarthritis after the induction of osteoarthritis as compared to WT animals. Furthermore, the ADAMTS-5 transgenic animals have reduced aggrecanase activity in articular tissue as compared to WT animals. These animals are good models for ADAMTS-5-associated diseases, and for screening of drugs useful in the treatment and/or prevention of these diseases. There are no other animal models in which the deletion of the activity of a single gene is capable of abrogating the course of osteoarthritis.Type: GrantFiled: November 8, 2004Date of Patent: June 24, 2008Assignee: WyethInventors: Elisabeth A. Morris, Sonya Glasson, Jason Shaoyun Xiang
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Publication number: 20080132568Abstract: Compounds having anti-androgenic activities are disclosed. Further disclosed are methods of using the compounds to prevent or treat androgen-dependent diseases or to provide nutraceutical benefits. Pharmaceutical and nutraceutical compositions containing the anti-androgenic compounds are also disclosed.Type: ApplicationFiled: November 8, 2007Publication date: June 5, 2008Inventors: Todd A. Thompson, Debra A. MacKenzie
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Publication number: 20080119499Abstract: There are provided conjugated systems of formula (I) based on stilbene derivatives serving as improved Donor-Acceptor-Donor compounds and their use in non linear optics including chromophoric optical medium of a 3-dimensional optical memory.Type: ApplicationFiled: January 12, 2006Publication date: May 22, 2008Applicant: MEMPILE INC.Inventors: Andrew N. Shipway, Nimer Jaber, Moshe Greenwald, Michael Grishko, Ariel Litwak
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Publication number: 20080119440Abstract: Disclosed herein are methods of treating a proliferative disease, such as cancer, with bis(thio-hydrazide amides) or a tautomer, pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, in combination with hyperthermia treatment. Also disclosed are methods of treating a proliferative disease, such as cancer, with bis(thio-hydrazide amides) or a tautomer, pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, in combination with radiotherapy.Type: ApplicationFiled: August 30, 2007Publication date: May 22, 2008Inventor: Keizo Koya
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Patent number: 7371747Abstract: The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.Type: GrantFiled: November 13, 2002Date of Patent: May 13, 2008Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Sheldon N. Crane, Dana Davis, Eduardo L. Setti
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Patent number: 7368479Abstract: The invention relates to ?-sulfonylamino-acetonitrile derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein Ar1, and Ar2 independently of each other stand for an optionally substituted aryl or heteroaryl group, R1, and R2 stand independently of each other for hydrogen, optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R3 designates hydrogen, C3-C5alkenyl, C3-C5alkynyl or optionally substituted C1,-C5alkyl; R4 is optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R5 and R6 are independently of each other hydrogen or optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; R7, and R8 are independently of each other hydrogen or optionally substituted C1,-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally suType: GrantFiled: June 18, 2003Date of Patent: May 6, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Eberle, Daniel Stierli, Urs Müller
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Publication number: 20080103144Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2 I in which A, R1 and R2 are as defined in the description, and b) dimethomorph or flumetover, and/or c) a valinamide of the formula III in which R13 is C3-C4-alkyl and R14 is naphthyl or phenyl, where the phenyl radical is substituted in the 4-position by a halogen atom, a C1-C4-alkyl or C1-C4-alkoxy group, and/or d) benalaxyl, ofurace, metalaxyl, furalaxyl or oxydixyl, and/or e) 1-(2-cyano-2-methoxyiminoacetyl)-3-ethylurea in a synergistically effective amount.Type: ApplicationFiled: December 30, 2005Publication date: May 1, 2008Inventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 7317066Abstract: Liquid crystal polyester derived from phenylene-naphthalene monomers and one or more comonomers display an improved balance of properties, including low melt viscosity, fast cycle time in molding, very low mold shrinkage, high tensile and/or flexural strength, solvent resistance, excellent barrier properties, low water absorption, low thermal expansion coefficient, excellent thermostability, and/or low flammability. The phenylene-naphthalene monomers are The one or more comonomers include 4-hydroxybenzoic acid, 2-hydroxy-6-naphthoic acid, terephthalic acid, isophthalic acid, and derivatives and combinations thereof.Type: GrantFiled: August 29, 2006Date of Patent: January 8, 2008Assignee: Rensselaer Polytechnic InstituteInventors: Brian Benicewicz, Jiping Shao
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Patent number: 7253318Abstract: The invention relates to compounds of the formula and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, n, m, and o are as defined in the specification. The compounds are selective monoamine oxidase ? inhibitors and are useful for the treatment and prevention of Alzheimer's disease and senile dementia, as well as other CNS disorders. The invention also relates to processes for preparing such compounds and pharmaceutical compositions containing them.Type: GrantFiled: June 20, 2005Date of Patent: August 7, 2007Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
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Patent number: 7235587Abstract: Diesters that include one or more of a crylene and/or a fluorene moiety, and sunscreen compositions including a mixture of a photoactive compound and one or more of a diester that includes one or more of a crylene and/or a fluorene moiety are described herein. Also disclosed are methods for stabilizing a sunscreen composition, methods of stabilizing a dibenzoylmethane derivative, and methods for protecting human skin from ultraviolet radiation with one or more of a diester that includes one or more of a crylene and/or a fluorene moiety are described herein.Type: GrantFiled: July 1, 2004Date of Patent: June 26, 2007Assignee: CPH Innovations CorporationInventors: Craig A. Bonda, Anna B. Pavlovic
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Patent number: 7196081Abstract: The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1–C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.Type: GrantFiled: October 29, 2002Date of Patent: March 27, 2007Assignee: Chugai Seiyaku Kabushiki KaishaInventors: JaeChon Jo, HeeAn Kwon, HyunSuk Lim, JaeYoung Choi, Kazumi Morikawa, Yoshitake Kanbe, Masahiro Nishimoto, MyungHwa Kim, Yoshikazu Nishimura
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Patent number: 7148255Abstract: The invention relates to compounds of formula I wherein R1, R2, R3, R4, R5, R6, R8, R8?, R9, W, X, A1, A2, a, b and c have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.Type: GrantFiled: May 21, 2003Date of Patent: December 12, 2006Assignee: Novartis Animal Health US, Inc.Inventors: Pierre Ducray, Thomas Goebel, Jacques Bouvier, Corinne Durano
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Patent number: 7109238Abstract: Novel calcilytic compounds and methods of using them are provided.Type: GrantFiled: January 21, 2004Date of Patent: September 19, 2006Assignees: Smith Kline Beecham Corporation, NPS Pharmaceuticals, Inc.Inventors: Maria Amparo Lago, James Francis Callahan, Pradip Kumar Bhatnagar, Eric G. Del Mar, William M. Bryan, Joelle L. Burgess
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Patent number: 7109214Abstract: The present invention relates to substituted cyclopentene compounds of the general formula I, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use thereof for the production of pharmaceutical preparations.Type: GrantFiled: November 19, 2004Date of Patent: September 19, 2006Assignee: Grunenthal GmbHInventors: Oswald Zimmer, Michael Haurand, Klaus Schiene, Clemens Gillen, Johannes Schneider, Gregor Bahrenberg
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Patent number: 7102026Abstract: The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2-hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4-fluorophenylthio) propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof. The present invention further discloses a new process for the isolation and purification of racemic and optically active bicalutamide.Type: GrantFiled: June 25, 2003Date of Patent: September 5, 2006Assignee: TEVA Gyógyszergyár Zártkörüen Müködö RészvénytársaságInventors: Ben-Zion Dolitzky, Ofer Reany, Jenny Shammai
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Patent number: 7053245Abstract: This invention relates to N-acylamino aryl derivatives of the formula where R1, R21, R22, R23, R24, R3, R4, R5, R6, R7, R8, R, and n are as defined herein and where X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH?CH— or —C?C—. The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.Type: GrantFiled: May 5, 2004Date of Patent: May 30, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 7019031Abstract: Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.Type: GrantFiled: October 23, 2001Date of Patent: March 28, 2006Assignee: The Arizona Disease Control Research CommissionInventors: Seth D. Rose, Scott R. Lefler, Steven R. Ottersberg, Ann Y. Kim, Karl J. Okolotowicz, Rosemarie F. Hartman
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Patent number: 7019030Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor ?, nuclear factor ?B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: GrantFiled: July 17, 2003Date of Patent: March 28, 2006Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire