Tricyclo Ring System Patents (Class 562/499)
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Patent number: 10800737Abstract: The present invention relates to a cost-effective and efficient method for preparing treprostinil with high purity, and an intermediate therefor.Type: GrantFiled: April 18, 2017Date of Patent: October 13, 2020Assignee: YONSUNG FINE CHEMICAL CO., LTD.Inventors: Hyun Ik Shin, Hyoseon Lee, Kyung Jin Lee, Kee Young Lee, Changyoung Oh
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Publication number: 20150126761Abstract: A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.Type: ApplicationFiled: May 22, 2013Publication date: May 7, 2015Inventors: Nareshkumar Jain, Michael Kirkup, Michael Marella, Sanjeevani Ghone
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Publication number: 20150105460Abstract: Provided in the present invention are various labdane diterpenoid compounds and derivatives thereof for use in preparation of a pharmaceutical composition for preventing or treating neurodegenerative diseases. Also provided in the present invention is a semen biotae extract comprising one or more labdane diterpenoid compounds and derivatives thereof for use in preparation of a pharmaceutical composition for preventing or treating neurodegenerative diseases.Type: ApplicationFiled: June 4, 2012Publication date: April 16, 2015Inventors: Weiwei Su, Yonggang Wang, Fengyin Liang, Ning Wang, Zhong Pei, Haibin Liu
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Publication number: 20150045389Abstract: The present invention is a screening assay for identifying inhibitors of Pseudomonas aeruginosa CFTR Inhibitory Factor as well as compounds identified by the screening assay for use in compositions and methods for ameliorating or treating a respiratory disease such as cystic fibrosis or secondary infection thereof.Type: ApplicationFiled: April 9, 2013Publication date: February 12, 2015Inventors: Dean R. Madden, Christopher D. Bahl, Bruce D. Hammock, Christophe Morisseau
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Publication number: 20150037734Abstract: A resist composition containing a compound represented by general formula (m0), wherein R1 and R2 each independently represents an aryl group which may have a substituent, an alkyl group which may have a substituent, or an alkenyl group which may have a substituent, provided that R1 and R2 may be mutually bonded to form a ring with the sulfur atom; R3 represents an aromatic hydrocarbon group which may have a substituent, an alkenyl group which may have a substituent, or an alkynyl group which may have a substituent; V1 represents a single bond or an alkylene group, provided that, when R3 is an aromatic hydrocarbon group which may have a substituent, V1 is an alkylene group; and X0? represents a monovalent organic anion.Type: ApplicationFiled: July 23, 2014Publication date: February 5, 2015Inventors: Takashi Nagamine, Yoshitaka Komuro, Masatoshi Arai, Yoshiyuki Utsumi
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Publication number: 20140363530Abstract: A composition contains an extract of pine leaf extract or a compound isolated therefrom. It showed potent inhibitory effect on human papillomavirus (HPV) as well as anti-cancer effect on various cancer diseases through various in vitro test and in vivo tests, and therefore, it can be used as the effective and safe therapeutics or health food for treating and preventing cancer disease.Type: ApplicationFiled: May 29, 2013Publication date: December 11, 2014Applicants: GUEULRIInventors: Chiung Moon, Jong Hwan Kwak, Young Bong Kim, Yukyoung Jeon, Hee-Jung Lee
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Publication number: 20140350100Abstract: The present disclosure provides novel glucagon-like peptide-1 (GLP-1) receptor modulators such as compounds of Formula (I) or (II), and pharmaceutically acceptable salts thereof. The present disclosure also provides pharmaceutical compositions, kits, and uses that involve the GLP-1 receptor modulators for regulating blood glucose levels and/or treating diabetes via, e.g., modulating the endogenous signaling pathways mediated by the GLP-1 receptor.Type: ApplicationFiled: May 27, 2014Publication date: November 27, 2014Applicants: Academia SinicaInventors: Klim King, Rong-Jie Chein
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Publication number: 20140322304Abstract: Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.Type: ApplicationFiled: July 10, 2014Publication date: October 30, 2014Inventors: Gavin P. Robertson, Raghavendra Gowda Chandagalu D., Subbarao V. Madhunapantula, Gajanan S. Inamdar, Omer F. Kuzu
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Patent number: 8680326Abstract: The hydrocortisone derivative of formula (I), whose IUPAC name is 3-[3,5-Dihydroxy-3-(2-hydroxy-acetyl)-3a,6-dimethyl-7-oxo-dodecahydro-cyclo-penta[alpha]naphthalen-6-yl]-propionic acid, designated as Deina®, is used in the treatment of atrophic tissues, particularly skin, cartilage, connective, and mucosal tissues and scalp skin.Type: GrantFiled: November 26, 2010Date of Patent: March 25, 2014Inventor: Giovanni Barco
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Patent number: 8653301Abstract: A novel tricyclodecane monomethanol monocarboxylic acid and derivatives thereof, which can be raw materials for highly heat-resistant alicyclic polyesters, are provided. A tricyclodecane monomethanol monocarboxylic acid represented by the following formula (I) and derivatives thereof.Type: GrantFiled: July 9, 2010Date of Patent: February 18, 2014Assignees: Hitachi Chemical Company, Ltd., National Institute of Advanced Industrial Science and TechnologyInventor: Hiroyuki Kawakami
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Publication number: 20130281729Abstract: Organic synthesis, i.e., the synthesis of carboxylic acids by direct carbonylation of alcohols in a continuous process, and more particularly, the synthesis of phenylalkylic acids, which are synthesis intermediates useful in pharmaceutical chemistry, by direct carbonylation of phenyl alkyl alcohols.Type: ApplicationFiled: December 13, 2011Publication date: October 24, 2013Inventors: Raimondo Pilia, Alexandre Trani, Sabrina Marie, Fabrice De Panthou
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Publication number: 20130197079Abstract: The present invention provides novel mGlu2/3 agonists useful in the treatment of neurological or psychiatric disorders.Type: ApplicationFiled: January 29, 2013Publication date: August 1, 2013Applicant: Eli Lily and CompanyInventor: Eli Lily and Company
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Patent number: 8324427Abstract: An objective of the present invention is to provide agricultural and horticultural disease control agents that have potent control effect against plant diseases and, at the same time, have high photostability. The agricultural and horticultural disease control agents comprise a novel substance analogous to MK8383 as an active ingredient.Type: GrantFiled: March 11, 2009Date of Patent: December 4, 2012Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kentaro Yamamoto, Nobuto Minowa, Masahisa Nakada
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Publication number: 20120157705Abstract: A novel tricyclodecane monomethanol monocarboxylic acid and derivatives thereof, which can be raw materials for highly heat-resistant alicyclic polyesters, are provided. A tricyclodecane monomethanol monocarboxylic acid represented by the following formula (I) and derivatives thereof.Type: ApplicationFiled: July 9, 2010Publication date: June 21, 2012Inventor: Hiroyuki Kawakami
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Patent number: 8022250Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.Type: GrantFiled: December 24, 2009Date of Patent: September 20, 2011Assignee: Chiesi Farmaceutici S.p.A.Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
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Publication number: 20110182864Abstract: The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent.Type: ApplicationFiled: July 29, 2010Publication date: July 28, 2011Applicants: CALIFORNIA INSTITUTE OF TECHNOLOGY, CALANDO PHARMACEUTICALS, INC.Inventors: Suzie Hwang Pun, Hector Gonzalez, Mark E. Davis, Nathalie C. Bellocq, Jianjun Cheng
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Patent number: 7910623Abstract: A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.Type: GrantFiled: January 22, 2008Date of Patent: March 22, 2011Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Stephen P. Waters
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Publication number: 20110065792Abstract: An objective of the present invention is to provide agricultural and horticultural disease control agents that have potent control effect against plant diseases and, at the same time, have high photostability. The agricultural and horticultural disease control agents comprise a novel substance analogous to MK8383 as an active ingredient.Type: ApplicationFiled: March 11, 2009Publication date: March 17, 2011Inventors: Kentaro Yamamoto, Nobuto Minowa, Masahisa Nakada
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Publication number: 20110059400Abstract: The present invention provides a photoresist composition comprising a resin which comprises a structural unit derived from a compound having an acid-labile group and which is insoluble or poorly soluble in an alkali aqueous solution but becomes soluble in an alkali aqueous solution by the action of an acid, an acid generator and a compound represented by the formula (I?): wherein R51, R52, R53 and R54 independently each represent a C1-C8 alkyl group, and A11 represents a C3-C36 divalent saturated cyclic hydrocarbon group which can contain one or more heteroatoms and which have one or more substituents or a C6-C20 divalent aromatic hydrocarbon group which can contain one or more heteroatoms and which have one or more substituents.Type: ApplicationFiled: September 3, 2010Publication date: March 10, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Akira KAMABUCHI, Yuko YAMASHITA
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Publication number: 20110009485Abstract: A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.Type: ApplicationFiled: January 22, 2008Publication date: January 13, 2011Inventors: Samuel J. Danishefsky, Stephen P. Waters
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Publication number: 20110009391Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: July 26, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Alain Jean BRAUN, Olivier CRESPIN, Claudie NAMANE, Eric NICOLAI, Francois PACQUET, Cecile PASCAL, Christophe PHILIPPO, Olivier VENIER
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Publication number: 20100324142Abstract: The present invention relates to hydrocortisone derivatives, the method of production thereof and the therapeutic or cosmetic use thereof to combat hair loss or in the treatment of cutaneous physiopathologies.Type: ApplicationFiled: September 30, 2008Publication date: December 23, 2010Inventor: John Alexander Troostwyk
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Publication number: 20100274025Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.Type: ApplicationFiled: February 25, 2010Publication date: October 28, 2010Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Truc Chi Vu, David B. Brzozowski, Rita Fox, Jollie Duaine Godfrey, JR., Ronald L. Hanson, Sergei V. Kolotuchin, John A. Mazzullo, Ramesh N. Patel, Jianji Wang, Kwok Wong, Jurong Yu, Jason J. Zhu, David R. Magnin, David J. Augeri, Lawrence G. Hamann
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Patent number: 7662995Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.Type: GrantFiled: February 19, 2004Date of Patent: February 16, 2010Assignee: Chiesi Farmaceutici S.p.A.Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
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Publication number: 20090186940Abstract: A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.Type: ApplicationFiled: January 22, 2008Publication date: July 23, 2009Inventors: Samuel J. Danishefsky, Stephen P. Waters
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Publication number: 20090099251Abstract: The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R1 is hydrogen or C1-6-alkyl; R2 is hydroxy, C3-5-acyloxy, hydroxymethyl, 1,3-dihydroxypropyl or C1-6-alkyl; R3 and R4 independently from each other are hydrogen, hydroxy, hydroxymethyl, C1-5-acyloxy or C1-6-alkoxy; R5 is C1-6-alkyl, hydroxymethyl carboxy or methoxycarbonyl; R9 is hydrogen, hydroxymethyl, methoxy, oxo or C1-5-acyloxy; R10 is hydrogen, or R5 and R9 taken together are —CH2—O— or —O—CH2—; or R5 and R10 taken together are —CO—O—, —O—CO—, —CH2—O— or —O—CH2—; R6 is hydrogen, or R5 and R6 together form a bond; R7 and R8 independently from each other are C1-6-alkyl, carboxy, x-hydroxy-Cx-alkyl (with x being an integer from 1 to 6), or C1-6-alkoxycarbonyl with the proviso that at least one of R7 and R8 is C1-6-alkyl; R11 and R12 are both hydrogen or R11 and R12 together are oxo, with the further proviso for formula (I) that if R2 is hydroxy R1 is C1-6-alkyl, for use as medicaments for the tType: ApplicationFiled: November 22, 2007Publication date: April 16, 2009Inventors: Antoine De Saizieu, Ann Fowler, Regina Goralczyk, Claus Kilpert, Goede Schueler, Christof Wehrli
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Patent number: 7517910Abstract: The present invention aims at provision of a novel compound having a GPR40 receptor function modulating action, which is useful as an insulin secretagogue, an agent for the prophylaxis or treatment of diabetes and the like. The compound represented by the formula: wherein each symbol is as defined in the description, a salt thereof, and a prodrug thereof of the present invention unexpectedly have a superior GPR40 receptor agonistic activity and superior properties as pharmaceutical products such as stability and the like, and can be safe and useful pharmaceutical agents as agents for the prophylaxis or treatment of GPR40 receptor-related pathology or diseases in mammals.Type: GrantFiled: March 28, 2005Date of Patent: April 14, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Shuji Kitamura, Nozomu Sakai
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Publication number: 20090018311Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.Type: ApplicationFiled: July 28, 2008Publication date: January 15, 2009Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Truc Chi Vu, David B. Brzozowski, Rita Fox, Jollie Duaine Godfrey, JR., Ronald L. Hanson, Sergei V. Kolotuchin, John A. Mazzullo, Ramesh N. Patel, Jianji Wang, Kwok Wong, Jurong Yu, Jason J. Zhu, David R. Magnin, David J. Augeri, Lawrence G. Hamann
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Publication number: 20080275112Abstract: The present invention describes 1-aminoadamantane derivatives and 3-aminoadamantane-1-carboxylic derivatives in which the 5- or 7-position of the basic adamantane structure can be optionally substituted, methods for the production of the compounds based on the present invention, and methods for the coupling of the monomeric 3-aminoadamantane-1-carboxylic derivatives thus obtained to oligomers. The compounds based on the present invention are suitable for the utilisation as antiviral active ingredients, artificial ion channels, as well as for the therapy, diagnostics and prophylaxis of diseases in which a dysfunction of the GABA system occurs.Type: ApplicationFiled: July 22, 2005Publication date: November 6, 2008Inventors: Peter R. Schreiner, Lukas Wanka
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Patent number: 7432400Abstract: These are described biphenylene compounds of formula (I) wherein R1 is a C1-C18alkyl, C2-C18alkenyl, C6-C10aryl or C6-C10aryl or C6-C10heteroaryl radical each unsubstituted or mono- or poly-substituted by hydroxy, halogen, C1-C18alkyl, C1-C18alkoxy, amino, C1-C5monoalkyamino or by di-C1-C5alkylamino; C5-C7cycloalkyl or C5-C7cycloalkenyl each unsubstituted or substituted by C1-C5alkyl; —OR?; or NR?R?; R2 is a C1-C18alkyl, C2-C18alkenyl, C6-C10aryl or C6-C10heteroaryl radical each unsubstituted or mono- poly-substituted by hydroxy, hadroxy, C1-C18alkoxy, amino, C1-C5monoalkylamino or by di-C1-C5alkylamino; —OR?; —NR?R?; or R1 and R2 together form a 5- to 7- membered monocyclic carbocyclic or heterocyclic ring; R3 is hydrogen; C1-C6alkyl or C1-C6alkoxy; R? and R? are each independently of the other hydrogen; unsubstituted or mono- or poly-hydroxy-, halo-, C1-C18alkyl-, C1-C18alkoxy-, amino- or quaternary ammonium groupsubstituted C1-C18alkyl, C5-C7cycloalkyl or phenyl; and n is 0 or 1; wherein, when R2 is OR? orType: GrantFiled: August 29, 2002Date of Patent: October 7, 2008Assignee: Ciba Specialty Chemicals Corp.Inventors: Barbara Wagner, Dietmar Hüglin
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Publication number: 20080183003Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.Type: ApplicationFiled: February 4, 2008Publication date: July 31, 2008Applicant: Adamas Pharmaceuticals, Inc.Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stamler, Stuart A. Lipton
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Publication number: 20080153850Abstract: The invention provides compounds of formula (I) pharmaceutically acceptable salt or solvate thereof, in which R1, A1, m and A are as defined in the specification; a process for their preparation; pharmaceutical compositions containing them; and their use in therapy.Type: ApplicationFiled: August 29, 2005Publication date: June 26, 2008Applicant: AstraZeneca ABInventors: Rhonan Ford, Barrie Martin, Toby Thompson, Nicholas Tomkinson, Paul Willis
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Patent number: 7288671Abstract: Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-? modulators, and thus are useful in the treatment of various diseases. wherein the R groups are defined as follows: if any R3-R5, R7, R8, R11-R13 is not hydrogen, R2 or R6 or R9 is not methyl, or R10 is not CH2, then R1 is selected from the group consisting of hydrogen, a halogen, COOH, C1-C12 carboxylic acids, C1-C12 acyl halides, C1-C12 acyl residues, C1-C12 esters, C1-C12 secondary amides, (C1-C12)(C1-C12) tertiary amides, (C1-C12)(C1-C12) cyclic amides, (C1-C12) amines, C1-C12 alcohols, (C1-C12)(C1-C12) ethers, C1-C12 alkyls, C1-C12 substituted alkyls, C2-C12 alkenyls, C2-C12 substituted alkenyls, and C5-C12 aryls.Type: GrantFiled: May 3, 2006Date of Patent: October 30, 2007Assignees: Nereus Pharmaceuticals, Inc., The Regents of the University of CaliforniaInventors: Michael Palladino, Emmanuel A. Theodorakis
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Patent number: 7205432Abstract: The invention relates to a process for the preparation of 3-hydroxyadamantaneglyoxylic acid of the general formula (1) or a derivative or salt thereof. In the process, an 1-acyl derivative of adamantane having the formula (2): wherein R is a C1–C5 hydrocarbyl; CH2OH; CHO; COOH, is contacted with an oxidant under oxidizing conditions leading to the 3-hydroxyadamantaneglyoxylic acid (1) or the derivative or salt thereof.Type: GrantFiled: May 31, 2005Date of Patent: April 17, 2007Assignee: Kemfine OyInventors: Mathias Berner, Reijo Partanen, Auli Salakka, Pekka Somersalo
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Patent number: 7119223Abstract: Novel compounds are disclosed that have the following chemical structures, and prodrug esters and acid-addition salts thereof, that are useful as Interleukin-1 and Tumor Necrosis Factor-? modulators, and thus are useful in the treatment of various diseases. wherein the R groups are defined as follows: if any R3–R5, R7, R8, R11–R13 is not hydrogen, R2 or R6 or R9 is not methyl, or R10 is not CH2, then R1 is selected from the group consisting of hydrogen, a halogen, COOH, C1–C12 carboxylic acids, C1–C12 acyl halides, C1–C12 acyl residues, C1–C12 esters, C1–C12 secondary amides, (C1–C12)(C1–C12) tertiary amides, (C1–C12)(C1–C12) cyclic amides, (C1–C12) amines, C1–C12 alcohols, (C1–C12)(C1–C12) ethers, C1–C12 alkyls, C1–C12 substituted alkyls, C2–C12 alkenyls, C2–C12 substituted alkenyls, and C5–C12 aryls.Type: GrantFiled: March 27, 2002Date of Patent: October 10, 2006Assignees: Nereus Pharmaceuticals, Inc., The Regents of the University of CaliforniaInventors: Michael Palladino, Emmanuel A. Theodorakis
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Patent number: 7102027Abstract: An adamantanetricarboxylic acid derivative is represented by following Formula (1): wherein X is a hydrogen atom or a hydrocarbon group; and R1, R2 and R3 may be the same as or different from one another and are each a carboxyl group which may be protected by a protecting group, or a carbonyl halide group, wherein at least one of R1, R2 and R3 is a carboxyl group which is protected by a protecting group, or a carbonyl halide group.Type: GrantFiled: March 24, 2004Date of Patent: September 5, 2006Assignee: Daicel Chemical Industries, Ltd.Inventors: Shinya Nagano, Jiichiro Hashimoto
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Patent number: 6881857Abstract: Disclosed herein are novel tricyclic diterpene compounds. These compounds, including their prodrug esters and acid-addition salts, are useful as Interleukin-1 and Tumor Necrosis Factor-? modulators, and thus are useful in the treatment of various diseases. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of the novel compounds that are useful as anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making the compounds and their analogs are also disclosed, as are methods of using these synthetic and semi-synthetic compounds in the treatment of the above-listed disease states.Type: GrantFiled: February 4, 2002Date of Patent: April 19, 2005Assignees: Nereus Pharmaceuticals, Inc., University of CaliforniaInventors: Michael Palladino, Emmanuel A. Theodorakis
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Patent number: 6875764Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.Type: GrantFiled: October 27, 2000Date of Patent: April 5, 2005Assignee: New Pharma Research Sweden ABInventors: Sabrina Muzi, Shoaá Abdul Rahman
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Patent number: 6846941Abstract: Disclosed are processes for separating valuable products, including unsaponifiable materials, from any given matrix of raw materials that is mainly composed of saponifiable components and unsaponifiable components. Preferred methods include converting sodium or potassium soaps obtained from the saponification of a starting material into metallic soaps which have a lower melting point, and when melted, have viscosity sufficiently low to enable processing such as by distillation evaporation processes. Preferred raw materials include animal or vegetable products, as well as by-products, residues, and waste products from the processing of animal or vegetable products, such as from food processing, cellulose processing and the like. Valuable products which may be obtained by the disclosed processes include sterols, vitamins, flavonoids, and tocopherols.Type: GrantFiled: February 20, 2002Date of Patent: January 25, 2005Assignee: Resitec Industria Quimica Ltda.Inventors: Rodolfo Rohr, Raul Rohr, Jose Anibal Trujillo-Quijano
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Publication number: 20040242923Abstract: An adamantanetricarboxylic acid derivative is represented by following Formula (1): 1Type: ApplicationFiled: March 24, 2004Publication date: December 2, 2004Inventors: Shinya Nagano, Jiichiro Hashimoto
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Patent number: 6750364Abstract: This invention provides compounds of the formula: wherein X is (CH2)n, O, S, SO, SO2 or CR1R2; n is 1 or 2; R1 and R2 are H, halogen, hydroxy, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or R1 and R2, taken together form cycloalkyl of 3 to 6 carbon atoms, an alkylidene of up to 6 carbon atoms or a carbonyl; R3, R4 and R5 are H or alkyl of 1 to 6 carbon atoms; Z is H, alkyl of 1 to 6 carbon atoms, alkanoyl of 1 to 6 carbon atoms or alkoxycarbonyl of 2 to 7 carbon atoms; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods for their use in treating or preventing characterized by glutamate hypofunction, including schizophrenia, schizoaffective disorder and schizophreniform disorder, and for the treatment of cognitive deficits due to aging, stroke, Alzheimer's disease or other neurodegenerative diseases.Type: GrantFiled: June 27, 2002Date of Patent: June 15, 2004Assignee: WyethInventors: Gary Paul Stack, John Dunlop, Alexander Alexei Greenfield, Jonathan Laird Gross
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Patent number: 6689905Abstract: This invention provides a process for the preparation of all four stereoisomers of formula I or a pharmaceutically acceptable salt thereof which may be represented by the following structures:Type: GrantFiled: June 27, 2002Date of Patent: February 10, 2004Assignee: WyethInventors: Reinhardt Bernhard Baudy, Jean Yi-ching Sze, Jonathan Laird Gross
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Patent number: 6689904Abstract: This invention provides processes for preparing a group of novel bridged tricyclic compounds having the formula: wherein X is (CH2)n, O, S, SO, SO2 or CR1R2; n is 1 or 2; and R1 and R2 are, independently, hydrogen, halogen, hydroxy, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, or R1 and R2, taken together with the carbon to which they are attached, form cycloalkyl of three to six carbon atoms, an alkylidene of up to six carbon atoms or a carbonyl.Type: GrantFiled: June 27, 2002Date of Patent: February 10, 2004Assignee: WyethInventors: Alexander Alexei Greenfield, John Anthony Butera
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Patent number: 6603041Abstract: Enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an optionally substituted arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; X is an O or S atom or the group NR30 group; j and k is each zero or the integer 1 or 2 provided that the sum of j and k is zero or the integer 1 or 2; Cy1 is an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof.Type: GrantFiled: September 5, 2001Date of Patent: August 5, 2003Assignee: Celltech R & D LimitedInventors: Timothy John Norman, John Robert Porter, John Clifford Head, Andrew James Ratcliffe
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Patent number: 6593363Abstract: The present invention relates to diterpene derivatives prepared from the components which are extracted from Acanthopanax Koreanum and represented by Chemical Formula (1).Type: GrantFiled: September 15, 2000Date of Patent: July 15, 2003Assignees: Sae Han Pharm. Co., Ltd.Inventors: Young Ger Suh, Young Hoon Choi, Hye Kyung Lee, Young Ho Kim, Hyoung Sup Park
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Publication number: 20030120095Abstract: Disclosed are processes for separating valuable products, including unsaponifiable materials, from any given matrix of raw materials that is mainly composed of saponifiable components and unsaponifiable components. Preferred methods include converting sodium or potassium soaps obtained from the saponification of a starting material into metallic soaps which have a lower melting point, and when melted, have viscosity sufficiently low to enable processing such as by distillation/evaporation processes. Preferred raw materials include animal or vegetable products, as well as by-products, residues, and waste products from the processing of animal or vegetable products, such as from food processing, cellulose processing and the like. Valuable products which may be obtained by the disclosed processes include sterols, vitamins, flavonoids, and tocopherols.Type: ApplicationFiled: February 20, 2002Publication date: June 26, 2003Inventors: Rodolfo Rohr, Raul Rohr
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Patent number: 6562782Abstract: The present invention related to an oligocycloalkanoid compound comprising formula (I) wherein m, n, and o are independently an integer from 0 to 2; A1 through A10 are independently a direct link, alkylene, alkylene-O—, carbonyl, oxygen, or sulfur; X and Y are independently hydrogen, hydroxy, alkyl, or in combination an electrophilic group; and R1 through R10 are independently hydrogen, hydroxy, alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, N-, S-, or O-heterocycles, fused or multi-ring aryl with or without hetero ring members, arylalkyl, arylalkenyl, arylalkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, alkoxy, alkenyloxy, alkynyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted arylalkoxy, alkylacyl, alkenylacyl, alkynylacyl, arylacyl, aroyl, alkylaroyl, aminoaroyl, aminoalkylacyl, aminoalkyl, aminoalkenyl, aminoalkynyl, amino, alkylamino, alkenylamino, alkynylamino, arylamino, dialkylamino, dialkenylamino, dialkynylamino, arylalkylamino, arylalkType: GrantFiled: May 10, 2000Date of Patent: May 13, 2003Assignee: University of RochesterInventors: Benjamin L. Miller, Robert D. Hubbard
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Publication number: 20030040640Abstract: Novel compounds are disclosed that have the chemical structure of Formula (II), and its prodrug esters and acid-addition salts, and that are useful as Interleukin-1 and Tumor Necrosis Factor-&agr; modulators, and thus are useful in the treatment of various listed diseases.Type: ApplicationFiled: February 4, 2002Publication date: February 27, 2003Inventors: Michael Palladino, Emmanuel A. Theodorakis
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Publication number: 20030018211Abstract: This invention provides a process for the preparation of all four stereoisomers of formula I or a pharmaceutically acceptable salt thereof 1Type: ApplicationFiled: June 27, 2002Publication date: January 23, 2003Applicant: WyethInventors: Reinhardt Bernhard Baudy, Jean Yi-ching Sze, Jonathan Laird Gross
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Patent number: RE39744Abstract: In the presence of an imide compound (e.g., N-hydroxyphthalimide) shown by the formula (2): wherein R1 and R2 independently represents a hydrogen atom, a halogen atom, an alkyl group, an aryl group, a cycloalkyl group; or R1 and R2 may bond together to form a double bond or an aromatic or non-aromatic ring; Y is O or OH and n=1 to 3; or the imide compound and a co-catalyst (e.g., a transition metal compound), an adamantane derivative having a functional group such as a nitro group, an amino group, a hydroxyl group, a carboxyl group, a hydroxymethyl group and an isocyanato group is oxidized with oxygen. According to the above method, an adamantane derivative having a hydroxyl group together with a functional group such as a nitro group, an amino group, a hydroxyl group, a carboxyl group, a hydroxymethyl group and an isocyanato group is efficiently obtained.Type: GrantFiled: March 5, 1998Date of Patent: July 24, 2007Assignee: Daicel Chemical Industries, Ltd.Inventors: Yasutaka Ishii, Tatsuya Nakano, Naruhisa Hirai