Polyoxy Patents (Class 568/644)
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Patent number: 9517988Abstract: The present invention relates to a phenol derivative and the preparation method and use in medicine thereof, and particular to a phenol derivative represented by general formula (A) or a stereoisomer, a solvate, a metabolite, a prodrug, a pharmaceutically acceptable salt or a cocrystal thereof, a preparation method thereof, a pharmaceutical composition comprising the same, and use of the compound or composition of the present invention in the field of the central nervous system; wherein the definitions of substituents in general formula (A) are the same as those in the Description.Type: GrantFiled: November 9, 2015Date of Patent: December 13, 2016Assignee: Sichuan Haisco Pharmaceutical Co., Ltd.Inventors: Linlin Qin, Fangqiong Li, Shixu Yi, Huadong Luo, Xinfeng Luo, Songlin Wan, Lei Ren, Guoliang Liu, Yonggang Wei, Jianyu Liu, Peng Cho Tang
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Publication number: 20150141417Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: May 14, 2012Publication date: May 21, 2015Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Patent number: 9005578Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.Type: GrantFiled: May 28, 2013Date of Patent: April 14, 2015Assignees: Fluoropharma, Inc., The General Hospital CorporationInventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
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Publication number: 20150064455Abstract: This invention relates to the direct grafting of a calixarene mostly onto the surface of a material, as well as to a grafting process, and certain calixarene intermediates useful for carrying the grafting process.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Ivan Jabin, Alice Mattiuzzi, Corlnne Lagrost, Philippe Hapiot, Olivia Reinaud
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Publication number: 20150051295Abstract: The invention relates to the use of propanol and propenol derivatives as antioxidants, to compositions comprising propanol and propenol derivatives and the preparation thereof, and to certain propanol and propenol derivatives and the preparation thereof.Type: ApplicationFiled: September 27, 2012Publication date: February 19, 2015Applicant: MERCK PATENT GMBHInventors: Thomas Rudolph, Rene Peter Scheurich
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Publication number: 20140371491Abstract: The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto.Type: ApplicationFiled: March 13, 2014Publication date: December 18, 2014Applicant: Unigen, Inc.Inventors: Qi Jia, Ji-Fu Zhao
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Patent number: 8906260Abstract: To provide a liquid crystal compound showing a large absolute value of dielectric anisotropy (|??|. A compound is represented by formula (1): wherein, in formula (1), Ra and Rb are fluorine, alkyl having 1 to 10 carbons or the like, and in the alkyl, at least one of —CH2— may be replaced by —O— or the like, however, Ra and Rb are not identical; A1, A2, A3, A4 and A5 are 1,4-cyclohexylene, 1,4-phenylene or the like, and in the groups, at least one of hydrogen may be replaced by fluorine; Z1, Z2, Z4 and Z5 are a single bond or the like; Y1, Y2, Y3 and Y4 are hydrogen, fluorine or the like; and m, n, q and r are 0, 1 or 2, and a sum of m, n, q and r is 0, 1, 2, 3 or 4.Type: GrantFiled: February 28, 2013Date of Patent: December 9, 2014Assignees: JNC Corporation, JNC Petrochemical CorporationInventor: Yasuyuki Sasada
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Publication number: 20140221384Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Applicant: ERIMOS PHARMACEUTICALS LLCInventors: Jonathan Daniel Heller, Qingqi Chen, Rocio Alejandra Lopez, Amanda Jean Morris
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Patent number: 8686187Abstract: The invention discloses an ethoxydiphenylethane derivative and a synthetic method and uses thereof 4? position of phenylethane B aromatic ring is chemically modified by ethoxy and hydroxy at position 3? thereof is simultaneously modified to water soluble prodrug such as phosphate, and similarly, amino acid side chain is introduced to amino at position 3? to form amino acid amide water soluble prodrug having the structure shown as formula (I) the ethoxydiphenylethane derivative and the prodrug thereof include strong tubulin aggregation inhibiting ability and obvious target damage effect for tumor vessels, selectively cause dysfunction and structural damage of tumor vessels and induce apoptosis of vascular endothelial cells in order to play the role of killing tumor cells or inhibiting tumor metastasis in case that the tumor cells are free from the support of nutrition and oxygen.Type: GrantFiled: October 15, 2009Date of Patent: April 1, 2014Assignees: Shanghai Ecust Biomedicine Co., Ltd., Zhejiang Wild Wind Pharmaceutical Co. Ltd.Inventors: Fanhong Wu, Fanhua Xiao, Weiguo Zhou, Fangming Xu
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Publication number: 20140028964Abstract: The invention relates to a liquid-crystalline medium which comprises at least one compound of the formula I, in which R1, R1*, rings A and B, Z1, L1, L2, a and b have the meanings indicated in Claim 1, and to the use thereof for an active-matrix display, in particular based on the VA, PSA, PS-VA, PALC, FFS, PS-FFS, IPS or PS-IPS effect.Type: ApplicationFiled: March 8, 2012Publication date: January 30, 2014Applicant: MERCK PATENT GMBHInventors: Melanie Klasen-Memmer, Achim Goetz, Georg Bernatz
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Publication number: 20130315827Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.Type: ApplicationFiled: May 28, 2013Publication date: November 28, 2013Applicants: Fluoropharma, Inc., The General Hospital CorporationInventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
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Publication number: 20130303531Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: May 14, 2012Publication date: November 14, 2013Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Publication number: 20130261178Abstract: A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z1 is C1-C4 linear or branched alkyl or alkenyl; R4 is selected from unsubstituted and substituted C3-C3 cycloalkyl, C1-C8 linear or branched alkyl, C2-5 alkenyl, C6-C10 heteroaryl or aryl, or C3-C8 heterocyclyl which may be part unsaturated, and combinations thereof; Z is linear C2-3 alkylene; X1 is selected from NH and O; X2 is selected from unsaturated C and unsaturated S; and X3 is selected from NH and CH2; or one of X1 and X3 is a single bond; or X1 is O and X2 and X3 together are a single bond; and R7 is selected from oxo, F, Cl, Br, CN, NH2, NR92, NO2, CF3, OR9, COR9, OCOR9, COOR9, NR9COR9, CONR92SO2NR92, NR9SO2R9; and R8 is selected from C1-5 alkyl, C1-5 alkoxyl, C2-5 alkenyl or alkynyl, C6-10 aryl and C3-8 cycloalkyl and combinations thereof, which may be unsubstituted or further substituted by one or more F, Cl, Br, CN, NH2, NR32, NO2, CF3;Type: ApplicationFiled: July 5, 2010Publication date: October 3, 2013Inventors: Shailesh Mistry, Etienne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
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Publication number: 20130224135Abstract: The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto.Type: ApplicationFiled: December 6, 2012Publication date: August 29, 2013Applicant: UNIGEN, INC.Inventor: Unigen, Inc.
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Publication number: 20130209483Abstract: The disclosure relates to cannabinoid derivative compounds, pharmaceutical compositions made thereof, and methods for treating various diseases and disorders including cancer.Type: ApplicationFiled: November 30, 2012Publication date: August 15, 2013Applicant: SUTTER WEST BAY HOSPITALSInventor: SUTTER WEST BAY HOSPITALS
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Publication number: 20130203688Abstract: The present document describes a nutraceutical or cosmeceutical composition for the prophylaxis of an ailment comprising a therapeutically effective amount of a sugar plant syrup filtration residue in association with a pharmaceutically acceptable carrier. The present document also describes a nutraceutical or cosmeceutical composition for improving health condition of skin. The present document describes a method of producing a sugar plant syrup-derived product; wherein the improvement is characterized in the step of: collecting a sugar plant syrup residue during the production of sugar or syrup to produce a syrup-derived by-product.Type: ApplicationFiled: August 19, 2011Publication date: August 8, 2013Applicant: FÉDÉRATION DES PRODUCTEURS ACÉRI-COLES DU QUÉBECInventors: Julie Barbeau, Geneviève Béland
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Publication number: 20130187081Abstract: Presented herein are compositions including a linear tenso-active surfactant which, upon contact and mechanical stirring of a hydrocarbon body, induces emulsification, resulting in oxidation of fatty acid aliphatic bodies. The compositions solve the problem of hydrocarbon pollution. The hydrocarbon decomposer and its by-products dissolve hydrocarbons present in polluted bodies such as clays, soils, water and sand. Methods of the invention create a residue that is a fertilizer, at room temperature and with no need for high pressure.Type: ApplicationFiled: March 11, 2013Publication date: July 25, 2013Inventor: Pedro Murillo Gutierrez
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Publication number: 20130101684Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.Type: ApplicationFiled: April 15, 2011Publication date: April 25, 2013Applicant: Chromocell CorporationInventors: Jane V. Leland, Louise Slade, David Hayashi, William P. Jones, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Jessica Langer, Kambiz Shekdar
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Patent number: 8383865Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.Type: GrantFiled: September 30, 2009Date of Patent: February 26, 2013Assignee: Codman & Shurtleff, Inc.Inventor: Thomas M. DiMauro
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Publication number: 20120245393Abstract: Compounds of structure (I): including stereoisomers, tautomers and salts thereof, wherein R1, R2, R3, R4, R5, R6, X, Y and Z are as defined herein. Such compounds are useful for the preparation of diarylpropane compounds. Methods for the preparation of compounds of structure (I) are also disclosed, as are methods employing compounds of structure (I) for the preparation of diarylpropanes.Type: ApplicationFiled: March 21, 2012Publication date: September 27, 2012Applicant: Unigen, Inc.Inventors: Sandip K. Nandy, Abeysinghe Arrachchigae Padmapriya
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Publication number: 20120053180Abstract: This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.Type: ApplicationFiled: March 17, 2011Publication date: March 1, 2012Applicant: CHEMIZON, A DIVISION OF OPTOMAGIC CO., LTD.Inventors: Sang Uk Kang, Min Jeong Kim, Byung Nam Kang, Wei Tan, Albert Charles Gyorkos, Suk Young Cho
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Publication number: 20120046492Abstract: The invention discloses an ethoxydiphenylethane derivative and a synthetic method and uses thereof 4? position of phenylethane B aromatic ring is chemically modified by ethoxy and hydroxy at position 3? thereof is simultaneously modified to water soluble prodrug such as phosphate, and similarly, amino acid side chain is introduced to amino at position 3? to form amino acid amide water soluble prodrug having the structure shown as formula (I) the ethoxydiphenylethane derivative and the prodrug thereof include strong tubulin aggregation inhibiting ability and obvious target damage effect for tumor vessels, selectively cause dysfunction and structural damage of tumor vessels and induce apoptosis of vascular endothelial cells in order to play the role of killing tumor cells or inhibiting tumor metastasis in case that the tumor cells are free from the support of nutrition and oxygen.Type: ApplicationFiled: October 15, 2009Publication date: February 23, 2012Applicants: Zhejiang Wild Wind Pharmaceutical Co., Ltd., Shanghai Ecust Biomedicine Co.Ltd.Inventors: Fanhong Wu, Fanhua Xiao, Weiguo Zhou, Fangming Xu
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Publication number: 20120029216Abstract: A manufacturing process for making terameprocol (1) which includes the following reaction scheme, wherein a first general reaction is the formation of a furan intermediate (39) and a second general reaction is the ring-reduction and ring-opening of the furan intermediate (39) to form the terameprocol (1):Type: ApplicationFiled: July 31, 2009Publication date: February 2, 2012Applicant: Erimos Pharmaceuticals LLCInventors: Qingqi Chen, Jessica Andrea Blomburg
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Patent number: 8101804Abstract: A subject-matter of the present invention is a novel process for the synthesis of (E)-stilbene derivatives targeted at obtaining in particular resveratrol and piceatannol.Type: GrantFiled: July 25, 2007Date of Patent: January 24, 2012Assignee: Clariant Specialty Fine Chemicals (France)Inventors: Alain Schouteeten, Sébastien Jus, Jean-Claude Vallejos
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Patent number: 8058480Abstract: Processes for the alkoxylation of alcohols using alkylene epoxides in the presence of boron based catalysts are provided.Type: GrantFiled: April 30, 2009Date of Patent: November 15, 2011Assignee: E. I. du Pont de Nemours and CompanyInventor: Kenneth Gene Moloy
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Patent number: 8043789Abstract: A photosensitive compound whose size is smaller than conventional polymer for photoresist, and which has well-defined (uniform) structure, and a photoresist composition including the same are disclosed. The photosensitive compound represented by the following formula. Also, the present invention provides a photoresist composition comprising 1 to 85 wt % (weight %) of the photosensitive compound; 0.05 to 15 weight parts of a photo-acid generator with respect to 100 weight parts of the photosensitive compound; and 10 to 5000 weight parts of an organic solvent. In the formula, n is 0 or 1, x is 1, 2, 3, 4 or 5, y is 2, 3, 4, 5 or 6, z is 0, 1, 2, 3 or 4, R, R? and R? are independently hydrocarbon group of 1 to 30 carbon atoms, preferably 2 to 20 carbon atoms, and R?? is a hydrogen atom or hydrocarbon group of 1 to 30 carbon atoms, preferably 2 to 20 carbon atoms.Type: GrantFiled: December 17, 2008Date of Patent: October 25, 2011Assignee: Dongjin Semichem Co., Ltd.Inventors: Jae-Woo Lee, Min-Ja Yoo, Jun-Gyeong Lee, Young-Bae Lim, Jae-Hyun Kim
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Patent number: 8008531Abstract: A process for benzylating an alcohol includes mixing 2-benzyloxy-1-methylpyridinium triflate in an aromatic hydrocarbon solvent having a predetermined boiling point; adding an acid scavenger to the mixture; combining the alcohol to be benzylated with the mixture; reacting the alcohol with the 2-benzyloxy-1-methylpyridinium triflate by heating above ambient temperature to generate the benzylated alcohol; and separating the benzylated alcohol from the mixture.Type: GrantFiled: June 23, 2010Date of Patent: August 30, 2011Assignee: The Florida State University Research Foundation, Inc.Inventor: Gregory Dudley
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Publication number: 20110160433Abstract: The present invention provides a protecting reagent that can be removed in a high yield even under acidic conditions and can afford a resulting product at a high purity in an organic synthesis reaction such as peptide synthesis and the like. The inventive protecting reagent is particular benzylic compound having only one hydroxyl group substituted by an organic group having an aliphatic hydrocarbon group having a carbon number of not less than 14.Type: ApplicationFiled: December 22, 2010Publication date: June 30, 2011Applicant: AJINOMOTO CO., INC.Inventor: Daisuke TAKAHASHI
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Patent number: 7951877Abstract: A process, advantageous in producibility, for the production of a vinyl compound containing very small amounts of ionic impurities and hydrolysable halogens, which is capable of curing by means of heat and/or light and giving a cured product having excellent dielectric characteristics and heat resistance, which process can efficiently remove a generated salt and comprises reacting a non-protonic polar solvent solution of a specific bifunctional phenylene ether oligomer with a vinylbenzyl halide in the presence of an alkoxide of an alkali metal, wherein the thus-obtained reaction solution is acidified with a specific amount of an acidic substance, then a salt generated is removed, an alkali substance containing a specific amount of an alkali metal is added to the thus-obtained solution, then a salt generated is removed, and the thus-obtained solution is mixed with water or a water-alcohol mixed solution, to precipitate a solid.Type: GrantFiled: June 17, 2008Date of Patent: May 31, 2011Assignee: Mitaubishi Gas Chemical Company, Inc.Inventors: Jun Nakano, Takeru Horino, Makoto Miyamoto, Atsushi Hirashima, Yasumasa Norisue
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Patent number: 7897820Abstract: A process for preparing Erianin (Dihydro Combretastation A-4), wherein 3,4,5-trimethoxy benzaldehyde is converted to phosphonium salt or phosphonate ester or the likes thereof, then reacted with isovanillin (3-hydroxyl-4-methoxyl benzaldehyde) including a protected hydroxyl in the 3-position, followed by hydrogenation and deprotection.Type: GrantFiled: July 12, 2006Date of Patent: March 1, 2011Assignee: Zhe Jiang Cell Biomedical Research Co., Ltd.Inventors: Yiping Li, Shuangxi Liu
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Publication number: 20110015426Abstract: A liquid crystalline compound has excellent liquid crystal properties, particularly high phase transition temperature. Diamantane compounds are represented by the general formula (I): (I) wherein A and B are each a six-membered, saturated or unsaturated, carbo- or hetero-cycle, and these cycles may have substituents, which substituents may be united to form a ring; and R1 and R2 are each a hydrocarbon group having 1 to 18 carbon atoms, and part of the carbon atoms of the hydrocarbon group may be replaced by heteroatoms or heteroatom-containing groups, while part of the hydrogen atoms thereof may be replaced by halogen atoms or heteroatom-containing groups.Type: ApplicationFiled: March 11, 2008Publication date: January 20, 2011Applicants: NATIONAL UNIVERSITY CORPORATION YOKOHAMA, JX NIPPON OIL & ENERGY CORPORATIONInventors: Yasushi Yokoyama, Tsuyoshi Gushiken, Takashi Ubukata
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Patent number: 7872160Abstract: The present invention provides a single pot process for the regioselective synthesis of neolignan framework [3(R)-Ethyl-2(S)-methyl-3-(2?,4?,5?-trimethoxyphenyl)-1-(2?,4?,5?-trimethoxyphenyl)propane from toxic ?-isomer rich asarone using montmorillonite acidic clay by employing microwave organic reaction enhancement (MORE) chemistry. This may be useful as versatile synthetic protocol for the synthesis of a large number of lignan and neolignan frameworks.Type: GrantFiled: October 31, 2008Date of Patent: January 18, 2011Assignee: Council of Scientific & Industrial ResearchInventors: Venkata Mallavadhani Uppuluri, Venkata Subrahmanya Sudhakar Akella, Anita Mahapatra
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Publication number: 20110004044Abstract: Presented herein are compositions including a linear tenso-active surfactant which, upon contact and mechanical stirring of a hydrocarbon body, induces emulsification, resulting in oxidation of fatty acid aliphatic bodies. The compositions solve the problem of hydrocarbon pollution. The hydrocarbon decomposer and its by-products dissolve hydrocarbons present in polluted bodies such as clays, soils, water and sand. Methods of the invention create a residue that is a fertilizer, at room temperature and with no need for high pressure.Type: ApplicationFiled: April 27, 2010Publication date: January 6, 2011Inventor: Pedro Murillo Gutierrez
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Publication number: 20100324324Abstract: A process for benzylating an alcohol includes mixing 2-benzyloxy-1-methylpyridinium triflate in an aromatic hydrocarbon solvent having a predetermined boiling point; adding an acid scavenger to the mixture; combining the alcohol to be benzylated with the mixture; reacting the alcohol with the 2-benzyloxy-1-methylpyridinium triflate by heating above ambient temperature to generate the benzylated alcohol; and separating the benzylated alcohol from the mixture.Type: ApplicationFiled: June 23, 2010Publication date: December 23, 2010Inventor: Gregory Dudley
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Publication number: 20100310615Abstract: The invention relates to compositions comprising pholyphenol derivatives, characterised in that said polyphenols contain monomers, oligomers or polymers with units having formula (I), said units being characterised by the simultaneous presence of a resorcinol nucleus (nucleus A) and a para-phenol nucleus (nucleus B) which are interconnected by a carbon bond C, said derivatives being over-activated, in respect of the nucleophilic power thereof, by alkylation of at least one phenol function of each constituent monomer unit and stabilised by sterification by mixtures of fatty acids in proportions reflecting those of vegetable oils formed mainly by unsaturated fatty acids of all of the other phenol functions. The invention is suitable for use in cosmetics, dietetics and therapeutics.Type: ApplicationFiled: November 17, 2008Publication date: December 9, 2010Inventor: Joseph Vercauteren
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Patent number: 7838706Abstract: The invention disclosed a total synthesis process of novel ethoxy combretastatins and their prodrugs. Combretastatins are chemically modified by ethoxy substituted on the 4?-position of their B aryl ring and are converted to be their soluble prodrugs of phosphate or their inner salt of phosphorylcholine by modifying the hydroxyl on the 3?-position of their B aryl ring. Similarly, 3?-amino combretastatin is 4?-ethoxy chemically modified and further side chain of amino acid can be introduced to the amino to form soluble prodrug of amino acidamide. The structure of the said compound is showed as formula (I). Ethoxy combretastatins possess potent tubulin polymerization inhibitory activity and can be used for the treatment of inhibiting tumor or neovascular.Type: GrantFiled: May 16, 2007Date of Patent: November 23, 2010Assignee: Zhejiang Dade Pharmaceutical Group Co. LtdInventors: Weiping Shen, Jianping Wang, Jianguo Wang
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Publication number: 20100286255Abstract: The invention relates to extracting secoisolariciresinol and dihydroquercetin from wood. The inventive method consists in extracting disintegrating wood of a screen area by means of a non-splitting mixture of organic solvent and water, the solvent content ranging from 50 to 75%, in such a way that a secoisolariciresinol and dihydroquercetin-containing extract is obtained, and in processing said extract by removing the solvent in such a way that a final secoisolariciresinol and dihydroquercetin-containing mixture is obtained.Type: ApplicationFiled: March 26, 2008Publication date: November 11, 2010Inventors: Nikolay Eduardovich Nifantiev, Dmitrl Vladimirovich Yashunsky, Vladimir Mikhailovich Menshov, Yury Evgenievich Tsvetkoy, Dmitri Evgenievich Tsvetkov
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Publication number: 20100267839Abstract: The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto.Type: ApplicationFiled: June 11, 2010Publication date: October 21, 2010Applicant: UNIGEN PHARMACEUTICALS, INC.Inventors: Qi Jia, Ji-Fu Zhao
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Publication number: 20100267965Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, or a salt thereof, and a compound of formula VI or a salt thereof, wherein R3 and R4 as well as Act are as defined in the specification, and processes of manufacturing these. Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.Type: ApplicationFiled: June 25, 2010Publication date: October 21, 2010Inventors: Gottfried Sedelmeier, Dominique Grimler, Murat Acemoglu
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Publication number: 20100121062Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T ??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.Type: ApplicationFiled: September 25, 2009Publication date: May 13, 2010Applicant: The Board of Trustees of the University of IllinoisInventors: Martin D. Burke, David M. Knapp, Eric P. Gillis
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Patent number: 7700657Abstract: Novel vitamin D analogs, markedly active in the fields of cell proliferation and differentiation, are selected from among (4E,6E)-7-{3-[2-(3,4-bis-hydroxymethylphenyl)-ethyl]phenyl}-3-ethylnona-4,6-dien-3-ol, (E)-6-[3-(3,4-bis-hydroxymethylbenzyloxy)phenyl]1,1,1-trifluoro-2-trifluoromethyloct-5-en-3-yn-2-ol, (3E,5E)-6-[3-(3,4-bis-hydroxymethylbenzyloxy)-phenyl]-1,1,1-trifluoro-2-trifluoromethylocta-3,5-dien-2-ol, (E)-6-{3-[2-(3,4-bis-hydroxymethylphenyl)ethyl]phenyl}-1,1,1-trifluoro-2-trifluoromethyloct-5-en-3-yn-2-ol, and (3E,5E)-6-{3-[2-(3,4-bis-hydroxymethylphenyl)-ethyl]phenyl-1,1,1-trifluoro-2-trifluoromethylocta-3,5-dien-2-ol, and the geometric isomers thereof and these compounds in which one or more of the hydroxyl functions are protected by a protective group —(C?O)—R, in which R is a linear or branched alkyl radical having from 1 to 6 carbon atoms, an aryl radical having from 6 to 10 carbon atoms, or an aralkyl radical having from 7 to 11 carbon atoms, the aryl radical or the aralkyl radical optionalType: GrantFiled: November 24, 2003Date of Patent: April 20, 2010Assignee: Galderma Research & DevelopmentInventor: Jean-Michel Bernardon
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Publication number: 20100022528Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: October 2, 2007Publication date: January 28, 2010Applicant: ERIMOS PHARMACEUTICALS LLC.Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Publication number: 20090306070Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: October 2, 2007Publication date: December 10, 2009Applicant: Erimos Pharmaceuticals LLCInventors: Jonathan Daniel Heller, Qingqi Chen, Rocio Alejandra Lopez, Amanda Jean Morris
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Publication number: 20090198080Abstract: The invention comprises an enantioselective method of preparing a compound of formula (IV): wherein n, m, R and R1 are as defined herein. Use of the compounds of formula (IV) in a method of preparing compounds of formula (IX) and novel intermediates useful in the method are also described.Type: ApplicationFiled: April 13, 2009Publication date: August 6, 2009Inventors: Mateusz Cebula, Kevin Edward Henegar
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Patent number: 7560491Abstract: A series of Z-stilbenes derivatives are disclosed, which have the structure as shown by formula 1. In the structure of formula 1, X is hydrogen, NHR, or nitro group, and R is hydrogen. Y and Z is independently hydrogen, halogen, C1-C10 alkyl, or C1-C10 alkoxyl. Furthermore, A is hydrogen, hydroxyl, or amino group. The compounds of the present invention have both aqueous solubility and anti-tumor activity. The Z-stilbenes derivatives of the present invention can further include a pharmaceutical carrier to form pharmaceutical compositions as potent anti-mitotic agents and anti-cancer agents.Type: GrantFiled: January 19, 2007Date of Patent: July 14, 2009Assignees: Taipei Medical University, National Health Research InstitutesInventors: Jing-Ping Liou, Jang-Yang Chang
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Publication number: 20090018369Abstract: A process for preparing Erianin (Dihydro Combretastation A-4), wherein 3,4,5-trimethoxy benzaldehyde is converted to phosphonium salt or phosphonate ester or the likes thereof, then reacted with isovanillin (3-hydroxyl-4-methoxyl benzaldehyde) including a protected hydroxyl in the 3-position, followed by hydrogenation and deprotection.Type: ApplicationFiled: July 12, 2006Publication date: January 15, 2009Inventors: Yiping Li, Shuangxi Liu
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Patent number: 7312249Abstract: Novel biaromatic vitamin D analogues have the general formula (I): and are suited for a wide variety of pharmaceutical applications, whether in human or veterinary medicine, and also for cosmetic applications.Type: GrantFiled: February 28, 2005Date of Patent: December 25, 2007Assignee: Galderma Research & DevelopmentInventors: Thibaud Biadatti, Etienne Thoreau, Johannes Voegel, Andre Jomard
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Patent number: 7220784Abstract: The present invention relates to stilbene and quinone compounds related to combretastatin A-4 and their use as anticancer compounds and prodrugs. The compounds include those with an alkyl group on the double bond of cis or trans-stilbenes, compounds with one or more (and preferably 2 or 3) alkyl group substituents on the stilbene A ring, compounds with an alkoxy group other than methoxy at position 3, 4, and/or 5 of the stilbene A ring, compounds (or prodrugs) in which BOC amino acid esters are formed with the phenolic hydroxyl at the 3-position of the B ring and compounds (or prodrugs) based on a benzoquinone B ring. The present invention further relates to the photochemical reactions of stilbene compounds, either the above compounds disclosed for the first time herein or compounds based on prior art stilbenes.Type: GrantFiled: December 20, 2001Date of Patent: May 22, 2007Inventors: John Anthony Hadfield, Alan Thomson McGown, Stephen Patrick Mayalarp, Edward John Land, Ian Hamblett, Keira Gaukroger, Nicholas James Lawrence, Lucy Annette Hepworth, John Butler
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Patent number: 7193019Abstract: A process for the production of a vinyl compound of the formula (1), which process comprises reacting a bifunctional phenylene ether oligomer of the formula (2) with a vinylbenzyl halide in an aprotic polar solvent in the presence of an alkali metal alkoxide and then adding the reaction solution to water or a water/alcohol mixed solution to precipitate a solidType: GrantFiled: October 14, 2004Date of Patent: March 20, 2007Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Yasumasa Norisue, Makoto Miyamoto, Daisuke Ohno, Kenji Ishii, Michio Nawata
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Patent number: 7122708Abstract: The invention relates to high-functionality polyether polyols of the general formula where each R?1 is an unsubstituted or substituted aliphatic or aromatic radical and each R?2 is an unsubstituted or substituted aliphatic or aromatic radical, H, OH, polyalkyl ether chain or halogen, each X is a polyalkyl ether chain or H, where at least one X is a polyalkyl ether chain, and m is an integer from 0 to 20, where Xm is H when m is 0, and n is an integer from 4 to 12, to processes for preparing such high-functionality polyether polyols and also to the use thereof for preparing polyurethanes and nonionic surfactants.Type: GrantFiled: May 10, 2000Date of Patent: October 17, 2006Assignee: BASF AktiengesellschaftInventors: Peter Böhme, Michael Pcolinski, Udo Rotermund, Wolf-Dieter Habicher, Antje Ziemer