The Ring Oxygens Are In The 1,2- Or 1,3-positions Of The Hetero Ring Patents (Class 549/365)
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Patent number: 10028938Abstract: The present invention relates to compounds which are found to exhibit an antiviral effect. The compounds are modulators of the activity of the viral haemagglutinin and/or neuraminidase enzymes.Type: GrantFiled: September 7, 2015Date of Patent: July 24, 2018Assignee: Griffith UniversityInventors: Mark Von Itzstein, Ibrahim El-Deeb, Larissa Dirr, Patrice Guillon, Moritz Winger
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Publication number: 20150111889Abstract: The present invention relates to compounds of the formula (I), wherein the residues A, R1 to R5, Z1 and Z2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 16, 2013Publication date: April 23, 2015Applicant: SANOFIInventors: Marc Nazare, Detlef Kozian, Martin Bossart, Werngard Czechtizky, Andreas Evers
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Patent number: 8853263Abstract: The present invention is directed to co-therapy for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, co-therapy with a therapeutically effective amount of a benzo-fused heterocycle sulfamide derivative and a therapeutically effective amount of one or more anticonvulsant and/or anti-epileptic agents.Type: GrantFiled: May 18, 2007Date of Patent: October 7, 2014Assignee: Janssen Pharmaceutica NVInventors: Virginia L. Smith-Swintosky, David F. McComsey, Michael H. Parker, Allen B. Reitz, Bruce E. Maryanoff
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Publication number: 20140219995Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: ApplicationFiled: July 13, 2012Publication date: August 7, 2014Applicant: MICROBIOTIX, INC.Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams, Matthew Torhan
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Patent number: 8791155Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: GrantFiled: September 26, 2011Date of Patent: July 29, 2014Assignee: Edison Pharmaceuticals, Inc.Inventors: Bing Wang, Gail Walkinshaw, Donald R. James
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Publication number: 20140192305Abstract: The present invention relates to photoreactive compounds that are particularly useful in materials for the alignment of liquid crystals.Type: ApplicationFiled: August 7, 2012Publication date: July 10, 2014Applicant: ROLIC AGInventors: Frederic Lincker, Izabela Bury S. Pires, Sabrina Chappellet, Patricia Scandiucci De Freitas, Mohammed Ibn-Elhaj, Qian Tang, Satish Palika, Masato Hoshino, Jean-Francois Eckert
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Patent number: 8765977Abstract: A method of diagnostic imaging is disclosed comprising administering a medical formulation to a subject, the formulation comprising a contrast enhancement agent having structure I and salts thereof wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is one or more charge balancing counterions; and one or more pharmaceutically acceptable carriers and excipients. The subject is subjected to a diagnostic imaging technique such as magnetic resonance imaging. The technique may be used in a variety of diagnostic imaging regimes, such as imaging of circulatory systems, genitourinary systems, hepatobiliary systems, central nervous systems, tumors, and abscesses among others.Type: GrantFiled: March 31, 2011Date of Patent: July 1, 2014Assignee: General Electric CompanyInventors: Brian James Grimmond, Michael James Rishel, Rong Zhang, Jeannette Christine Roberts
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Patent number: 8722020Abstract: In one aspect, the present invention provides a contrast enhancement agent comprising an iron chelate having structure I and salts thereof wherein R1 is independently at each occurrence a hydroxy group, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R2-R7 are independently at each occurrence hydrogen, a C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R1-R7 is a hydroxy group or a C1-C3 hydroxyalkyl group; and wherein Q is one or more charge balancing counterions. Also provided are a metal chelating ligand having structure IX and medical formulations comprising the contrast enhancement agent I.Type: GrantFiled: November 30, 2010Date of Patent: May 13, 2014Assignee: General Electric CompanyInventors: Brian James Grimmond, Michael James Rishel, Rong Zhang, Jeannette Christine DePuy
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Publication number: 20140121246Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: October 15, 2013Publication date: May 1, 2014Applicant: Metabolex, Inc.Inventors: Dong Fang Shi, Jiangao Song, Christopher J. Rabbat, Jingyuan Ma, Aaron Novack, Imad Nashashibi, Xin Chen
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Publication number: 20130303787Abstract: A process for preparing alditol Acetals via a dehydrocondensation reaction is disclosed. The reaction is carried out by adding an aldehyde and an aldiol using a metal salt based ionic liquid as an acid catalyst. The ionic liquid used in the process is prepared by dissolving a hydrogen donor and a compound providing counter ion in a solvent.Type: ApplicationFiled: July 8, 2013Publication date: November 14, 2013Inventors: Pavankumar ADURI, Parasu Veera UPPARA, Mangesh SAKHALKAR, Uday RATNAPARKHI
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Publication number: 20130303544Abstract: The present invention provides a kind of benzopyrone compounds having a structure of formula (I) and the pharmaceutically acceptable salts or prodrugs thereof, and the pharmaceutical compositions containing such compounds, which can be used to regulate the novel estrogen receptor ER-a36, and prevent and/or treat the related diseases mediated by the ER-a36 receptor, such as cancers, etc.Type: ApplicationFiled: December 21, 2011Publication date: November 14, 2013Applicant: BEIJING SHENOGEN PHARMA GROUP LTD.Inventors: Hongxia Ding, Kun Meng, Jin Li
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Patent number: 8569518Abstract: The invention is directed to the use of compounds of formula (I), as fragrant agents. In this formula: —R3 and R4 are independently a hydrogen atom, a C1-C6 alkyl group or a C2-C6 alkenyl group, R5 is a C1-C6 alkyl group, a C2-C6 alkenyl group or a (CH2)0-2-aryl group, R6 is a C1-C6 alkyl group, a C2-C6 alkenyl group, a (CH2)0-2-aryl group or a C5-C6 cycloalkyl or cycloalkenyl group, and R7 is a hydrogen atom, a C1-C6 alkyl group or a C2-C6 alkenyl group; or R3, R4 and R5 are as above defined, and R6 and R7 together with the carbon atom to which they are attached form a C5-C6 cycloalkyl or cycloalkenyl group.Type: GrantFiled: July 28, 2010Date of Patent: October 29, 2013Assignee: V. Mane FilsInventors: Jean-Jacques Chanot, Jean Mane, Caroline Plessis
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Publication number: 20130217879Abstract: The present invention relates to a preparation method for a medicine and an intermediate compound thereof, specifically, relates to a preparation method for entecavir, an intermediate compound thereof, and a synthesis method for the intermediate compound.Type: ApplicationFiled: July 15, 2011Publication date: August 22, 2013Applicant: AUSUN PHARMATECH. CO., LTD.Inventor: Zhiguo Zheng
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Publication number: 20130066071Abstract: Anti-virally active carbanucleosides such as entecavir are prepared by a process which utilizes, throughout the synthesis, an aromatic protectant group for the hydroxyl and the alkyl hydroxy groups of the starting material, removed as the final step of a multi-step synthesis. Such protectant groups yield intermediates which are solid and therefore easily purified at various stages of the process, for an economical and relatively fast process for synthesizing the final product.Type: ApplicationFiled: May 30, 2011Publication date: March 14, 2013Applicant: ALPHORA RESEARCH INC.Inventors: Dino Alberico, Boris Gorin, Ryan Beharrilall, Craig Dixon, Joshua Clayton, Varghese Rexon
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Publication number: 20130040389Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: September 5, 2012Publication date: February 14, 2013Applicant: Intrexon CoporationInventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Publication number: 20130035487Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: September 5, 2012Publication date: February 7, 2013Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Patent number: 8362281Abstract: In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.Type: GrantFiled: March 31, 2010Date of Patent: January 29, 2013Assignee: General Electric CompanyInventors: Brian James Grimmond, Michael James Rishel, Rong Zhang
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Patent number: 8227626Abstract: The invention relates to novel fluorinated achiral 1,3-benzodioxanes of the general formula (I-a) and (I-b) and to the preparation thereof.Type: GrantFiled: January 18, 2011Date of Patent: July 24, 2012Assignee: LANXESS Deutschland GmbHInventors: Jens Peter Joschek, Albrecht Marhold, Axel Pleschke
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Publication number: 20120165557Abstract: The invention is directed to the use of compounds of formula (I), as fragrant agents. In this formula: —R3 and R4 are independently a hydrogen atom, a C1-C6 alkyl group or a C2-C6 alkenyl group, R5 is a C1-C6 alkyl group, a C2-C6 alkenyl group or a (CH2)0-2-aryl group, R6 is a C1-C6 alkyl group, a C2-C6 alkenyl group, a (CH2)0-2-aryl group or a C5-C6 cycloalkyl or cycloalkenyl group, and R7 is a hydrogen atom, a C1-C6 alkyl group or a C2-C6 alkenyl group; or R3, R4 and R5 are as above defined, and R6 and R7 together with the carbon atom to which they are attached form a C5-C6 cycloalkyl or cycloalkenyl group.Type: ApplicationFiled: July 28, 2010Publication date: June 28, 2012Inventors: Jean-Jacques Chanot, Caroline Plessis
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Publication number: 20120123129Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R3, R9, R10, R11, R12 and G have the meanings given above as insecticides and/or acaricides and/or fungicides.Type: ApplicationFiled: April 28, 2010Publication date: May 17, 2012Applicant: Bayer CropScience AGInventor: Alfred ANGERMANN
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Publication number: 20120088783Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: September 26, 2011Publication date: April 12, 2012Applicant: Ampere Life Sciences, Inc.Inventors: Bing WANG, Gail Walkinshaw, Donald R. James
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Publication number: 20110313003Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: June 16, 2010Publication date: December 22, 2011Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
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Publication number: 20110269970Abstract: (1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol and (5R)-3-(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)-5-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)-1,3-oxazolidin-2-one are claimedType: ApplicationFiled: June 21, 2011Publication date: November 3, 2011Applicant: Glaxo Group LimitedInventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Inderjit Singh Mann, Panaylotis Alexandrou Procopiou
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Patent number: 8044097Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: GrantFiled: February 26, 2009Date of Patent: October 25, 2011Assignee: Ampere Life Sciences, Inc.Inventors: Bing Wang, Jian Chen
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Publication number: 20110207947Abstract: The present invention is aimed at a process for obtaining zaragozic acid and derivatives thereof, to the intermediate compounds of this synthesis and to the use of these intermediate compounds in the preparation of zaragozic acid.Type: ApplicationFiled: May 5, 2009Publication date: August 25, 2011Applicant: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICASInventors: Pedro Noheda Marín, Luis Miguel Lozano Gordillo
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Publication number: 20110201809Abstract: A process of making entecavir comprising converting a compound of formula (M5) to entecavir, wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.Type: ApplicationFiled: February 15, 2011Publication date: August 18, 2011Inventors: Tsung-Cheng Hu, Hung-Tsung Huang
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Publication number: 20110136796Abstract: Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.Type: ApplicationFiled: April 24, 2009Publication date: June 9, 2011Applicants: NEWLINK GENETICS, LANKEANAU INSTITUTE FOR MEDICAL RESEARCHInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Nicholas N. Vahanian, Charles J. Link, Judith Lalonde, George Prendergast, Alexander Muller, William Malachowski
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Patent number: 7955664Abstract: The chroman compounds of the formula I according to the invention R1-(A1-Z1)a—W1—(Z2-A2)b-Z3—W2—(Z4-A3)c-R2 in which R1, A1, A2, A3, W1, W2, Z1, Z2, Z3, Z4, a, b and c have the meanings indicated in claim 1, have two moieties W1 and W2 derived from chroman. The compounds are suitable as components of anisotropic switching media, as used, for example, in liquid-crystal display devices.Type: GrantFiled: December 11, 2007Date of Patent: June 7, 2011Assignee: Merck Patent GesellschaftInventors: Andreas Taugerbeck, Alexander Hahn, Achim Goetz
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Publication number: 20110112065Abstract: The present invention relates to novel 1-(4H-1,3-benzodioxin-2-yl)methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically asdopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: April 28, 2009Publication date: May 12, 2011Applicant: NSAB, FILIAL AF NEUROSEARCH SWEDEN AB, SVERIGEInventors: Clas Sonesson, Peder Svensson, Mikael Andersson
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Publication number: 20110112313Abstract: The invention relates to novel fluorinated achiral 1,3-benzodioxanes of the general formula (I-a) and (I-b) and to the preparation thereof.Type: ApplicationFiled: January 18, 2011Publication date: May 12, 2011Applicant: LANXESS DEUTSCHLAND GMBHInventors: Jens Peter Joschek, Albrecht Marhold, Axel Pleschke
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Publication number: 20110077417Abstract: In one aspect, the present invention provides a protected ligand precursor having structure XXI wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence acid sensitive protecting groups.Type: ApplicationFiled: November 9, 2009Publication date: March 31, 2011Applicant: GENERAL ELECTRIC COMPANYInventors: Brian James Grimmond, Michael James Rishel, Michael Todd Luttrell
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Publication number: 20110077396Abstract: In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.Type: ApplicationFiled: May 21, 2010Publication date: March 31, 2011Applicant: General Electric CompanyInventors: Brian James Grimmond, Michael James Rishel, Michael Todd Luttrell
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Publication number: 20100278755Abstract: An economical and simple method of producing para-menthane-3,8-diol in relatively high yield is disclosed. The product is useful as a repellent against noxious insects and other arthropods.Type: ApplicationFiled: September 12, 2008Publication date: November 4, 2010Inventor: Ian Thomas Dell
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Patent number: 7803951Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: March 24, 2006Date of Patent: September 28, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Rui Liang, Emma R. Parmee
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Publication number: 20100190831Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: December 17, 2009Publication date: July 29, 2010Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
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Publication number: 20100029588Abstract: The present invention relates to oxime ether-, hydrazone- or azomethine-substituted phenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the amidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.Type: ApplicationFiled: March 8, 2008Publication date: February 4, 2010Applicant: BAYER CROPSCIENCE AGInventors: Thomas Seitz, Klaus Kunz, Wahed Ahmed Moradi, Jörg Nico Greul, Darren James Mansfield, Urlich Heinemann, Amos Mattes, Oswald Ort, Jean-Pierre Vors, Peter Dahem, Ulrike Wachendorff-Neumann, Arnd Voerste
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Publication number: 20090192179Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: February 26, 2009Publication date: July 30, 2009Inventors: Bing Wang, Jian Chen
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Publication number: 20090182133Abstract: The invention relates to pharmaceutical compositions comprising benzopyranone derivatives for the treatment of Severe Acute Respiratory Syndrome (SARS).Type: ApplicationFiled: December 15, 2006Publication date: July 16, 2009Inventors: Chum Mok Puah, Weiliang Zhu, Jian Li, Lili Chen, Cheng Luo, Gang Chen, Zhili Zuo, Xiaomin Luo, Xu Shen, Kaixian Chen, Hualiang Jiang
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Publication number: 20090156838Abstract: There is disclosed an episesamin refining method in which a mixture of sesamin components that contains sesamin, episesamin and the like is brought into contact with an aqueous medium to form a slurried mixture, and thereafter the solids are separated from the mixture or the slurried mixture is dissolved in a suitable aqueous medium under heating and, thereafter, the solution is slowly cooled to recrystallize, thereby yielding an episesamin-enriched composition with an increased relative episesamin content. By the present invention, episesamin can be conveniently and efficiently refined from a mixture of sesamin components that mainly comprises sesamin and episesamin.Type: ApplicationFiled: November 1, 2006Publication date: June 18, 2009Applicant: SUNTORY LIMITEDInventors: Yukihiro Aoshima, Masaaki Nakai
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Patent number: 7514461Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondrial disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: GrantFiled: September 15, 2004Date of Patent: April 7, 2009Assignee: Edison Pharmaceuticals, Inc.Inventors: Bing Wang, Gail Walkinshaw, Sekhar Boddupalli, Arkadij M. Elizarov, Xianming Jin, Xianfeng Li, Donald R. James, Jiangao Song, Jian Chen, Wei Zhang
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Publication number: 20090066905Abstract: Liquid crystal compounds of Formula (I) for use in liquid crystal devices contains a dioxatetralin unit within the mesogenic liquid crystal core. The dioxatetralin unit may be located at any position within the mesogenic core of the liquid crystal compound, either at the terminus of the liquid crystal core or alternatively substantially in the middle of the liquid crystal core. The compounds of the invention exhibit fast switching and may be used in liquid crystal mixtures for particular use in imaging or display media, such as monitors or televisions.Type: ApplicationFiled: November 1, 2005Publication date: March 12, 2009Inventors: Rachel Patricia Tuffin, John William Goodby, Michael Hird, Stephane Trombotto
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Publication number: 20080318779Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: August 10, 2005Publication date: December 25, 2008Applicant: ISHIHARA SANGYO KAISHA LTDInventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Patent number: 7385067Abstract: The invention relates to a process for the preparation of compounds containing at least one —CF2—O— bridge in the molecule, in which a) an acid is added onto at least one ketene dithioketal, b) the resultant bis(alkylthio)carbenium salt is reacted with at least one compound having at least one hydroxyl group in the presence of a base, c) and subsequently, preferably in situ, the resultant dithioorthoester is subjected to oxidative fluorodesulfurisation using a fluorinating agent and an oxidant to give the compound containing at least one —CF2—O— bridge in the molecule.Type: GrantFiled: June 2, 2006Date of Patent: June 10, 2008Assignee: Merck Patent GmbHInventors: Peer Kirsch, Andreas Taugerbeck, Alexander Hahn
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Patent number: 7371874Abstract: The present invention relates to a noble 6-alkylamino-2-methyl-2?-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative, a method for preparing the same with high efficiency using a parallel synthetic method, one of combinatorial chemical synthetic techniques, and a use of the novel compound showing a high inhibitory effect to 5-lipoxygenase (5-LO) activity for preventing and treating leukotriene (LTA4, B4, C4, D4) activation-related diseases such as inflammatory diseases, rheumatoid arthritis, colitis, asthma and psoriasis.Type: GrantFiled: July 21, 2006Date of Patent: May 13, 2008Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Hyae-Gyeong Cheon, Moon-Kook Jeon, Cho Young Sik, Jong Yeon Hwang, Choi Hyung Sub, Jeon Hyun Suk, Soon-Hee Hwang, Song Jin Sook, Kim Chi Hyun, Sung-eun Yoo
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Patent number: 7368575Abstract: When a multi-step process reaction is carried out in a solution, it generally requires several treatments and purification procedures to go through with after the reaction, however, the inventive method for preparing 2,2?-disubstituted-3,4-dihydro-7,8-disubstituted-6-amino benzopyran derivative using a solid-phased synthetic method simplifies the treatment and purification procedures after the reaction, which makes possible to efficiently construct numerous drug-like libraries.Type: GrantFiled: October 20, 2004Date of Patent: May 6, 2008Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Hyae-Gyeong Cheon, Young-Sik Cho, Jin-Soo Seo, Jong-Yeon Hwang, Ji-Yeon Park, Sung-Eun Yoo
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Patent number: 7294725Abstract: A process for the preparation of a compound of formula (I) or a single enantiomer thereof, or a salt or a solvate thereof, wherein W is a chiral auxiliary or hydrogen and P1 and P2 are each independently selected from hydrogen or a protecting group, which comprises: a)treatment of a compound of formula (II), or a salt or a solvate thereof, wherein W is a chiral auxiliary and P1 and P2 are each independently chosen from a protecting group, with a compound of formula (III) to form a resulting product, b) treating the resulting product with a reducing agent to form the compound of formula (I), or a single enantiomer thereof, or a salt or a solvate thereof.Type: GrantFiled: May 13, 2005Date of Patent: November 13, 2007Assignee: SmithKline Beecham CorporationInventor: Panayiotis Alexandrou Procopiou
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Patent number: 7256218Abstract: Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.Type: GrantFiled: November 18, 2003Date of Patent: August 14, 2007Assignee: Jacobus Pharmaceutical Company, Inc.Inventors: David P. Jacobus, Guy A. Schiehser, Hong-Ming Shieh, Norman P. Jensen, Jacek Terpinski
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Patent number: 7157510Abstract: An acetal-based composition useful as a nucleating, gelling, thickening or clarifying agent is disclosed. The composition may be synthesized or provided in many different forms, including multicarbon diacetals formed from carbohydrates. Once synthesized, the compound may be employed as an additive in a plastic composition, such as (for example) a polypropylene copolymer. Co-additives may also be employed. Several aryl structures may reside upon the hydrocarbon chain backbone. One structure of such an acetal-based composition which happens to have two aryl-containing groups is shown: wherein: n is 0, 1 or 2; Ar1 and Ar2 are independently selected from substituted or unsubstituted aryl-containing groups; and R is selected from the group consisting of: alkenyls, alkyls, alkoxy, hydroxyl alkyls, and alkyl-halides.Type: GrantFiled: July 16, 2004Date of Patent: January 2, 2007Assignee: Milliken & CompanyInventors: Chunping Xie, Jiang Li, Lee Richard Rieth, Jason A. Smith, John David Orr Anderson, Shane M. Waybright, Brian M. Burkhart, Walter A. Scrivens
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Patent number: 7125853Abstract: We describe the use of bicyclic carbohydrates for the treatment of hepatitis C virus infections. Different bicyclic carbohydrates were tested in vitro against DNA-viruses, retro-viruses and Flaviviridae sp., an important family of human and animal RNA pathogens. Significant activity was observed against the bovine viral diarrhea virus (BVDV). As pestiviruses, such as BVDV, share many similarities with hepatitis C virus (HCV), the bicyclic carbohydrates in general and the preferred bicyclic carbohydrates more specifically are expected to be a treatment for hepatitis C viral infections.Type: GrantFiled: December 22, 2003Date of Patent: October 24, 2006Assignee: Kemin Pharma B.V.B.A.Inventors: Benedikt Sas, Johan Van hemel, Jan Vandenkerckhove, Eric Peys, Johan Van der Eycken, Bart Ruttens, Jan Balzarini, Eric De Clercq, Johan Neyts
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Patent number: 7125854Abstract: The use of bicyclic carbohydrates for the treatment of parasite infections is described. Different bicyclic carbohydrates have been tested in vitro against a number of protozoa. These compounds also have been screened against viruses, tumors, bacteria and fungi. Compound A1, a thiophenyl-containing bicyclic carbohydrate possessed significant activity against Trypanosoma brucei rhodiense, a parasite that causes the lethal sleeping sickness. Compound A2 and Compound A3, bicyclic carbohydrates with halogen containing aryl groups, possessed significant activity against Leishmania donovani, a parasite that causes leishmaniasis. Bicyclic carbohydrates in general, and Compound A1, Compound A2 and Compound A3 more specifically, could be possible treatments for the sleeping sickness and leishmaniasis in the future.Type: GrantFiled: January 7, 2004Date of Patent: October 24, 2006Assignee: Kemin Pharma B.V.B.A.Inventors: Benedikt Sas, Johan Van hemel, Jan Vandenkerckhove, Eric Peys, Johan Van der Eycken, Bart Ruttens