Tricyclo Ring System Patents (Class 562/499)
  • Patent number: 10800737
    Abstract: The present invention relates to a cost-effective and efficient method for preparing treprostinil with high purity, and an intermediate therefor.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: October 13, 2020
    Assignee: YONSUNG FINE CHEMICAL CO., LTD.
    Inventors: Hyun Ik Shin, Hyoseon Lee, Kyung Jin Lee, Kee Young Lee, Changyoung Oh
  • Publication number: 20150126761
    Abstract: 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: Application
    Filed: May 22, 2013
    Publication date: May 7, 2015
    Inventors: Nareshkumar Jain, Michael Kirkup, Michael Marella, Sanjeevani Ghone
  • Publication number: 20150105460
    Abstract: 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: Application
    Filed: June 4, 2012
    Publication date: April 16, 2015
    Inventors: Weiwei Su, Yonggang Wang, Fengyin Liang, Ning Wang, Zhong Pei, Haibin Liu
  • Publication number: 20150045389
    Abstract: 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: Application
    Filed: April 9, 2013
    Publication date: February 12, 2015
    Inventors: Dean R. Madden, Christopher D. Bahl, Bruce D. Hammock, Christophe Morisseau
  • Publication number: 20150037734
    Abstract: 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: Application
    Filed: July 23, 2014
    Publication date: February 5, 2015
    Inventors: Takashi Nagamine, Yoshitaka Komuro, Masatoshi Arai, Yoshiyuki Utsumi
  • Publication number: 20140363530
    Abstract: 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: Application
    Filed: May 29, 2013
    Publication date: December 11, 2014
    Applicants: GUEULRI
    Inventors: Chiung Moon, Jong Hwan Kwak, Young Bong Kim, Yukyoung Jeon, Hee-Jung Lee
  • Publication number: 20140350100
    Abstract: 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: Application
    Filed: May 27, 2014
    Publication date: November 27, 2014
    Applicants: Academia Sinica
    Inventors: Klim King, Rong-Jie Chein
  • Publication number: 20140322304
    Abstract: 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: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Gavin P. Robertson, Raghavendra Gowda Chandagalu D., Subbarao V. Madhunapantula, Gajanan S. Inamdar, Omer F. Kuzu
  • Patent number: 8680326
    Abstract: 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: Grant
    Filed: November 26, 2010
    Date of Patent: March 25, 2014
    Inventor: Giovanni Barco
  • Patent number: 8653301
    Abstract: 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: Grant
    Filed: July 9, 2010
    Date of Patent: February 18, 2014
    Assignees: Hitachi Chemical Company, Ltd., National Institute of Advanced Industrial Science and Technology
    Inventor: Hiroyuki Kawakami
  • Publication number: 20130281729
    Abstract: 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: Application
    Filed: December 13, 2011
    Publication date: October 24, 2013
    Inventors: Raimondo Pilia, Alexandre Trani, Sabrina Marie, Fabrice De Panthou
  • Publication number: 20130197079
    Abstract: The present invention provides novel mGlu2/3 agonists useful in the treatment of neurological or psychiatric disorders.
    Type: Application
    Filed: January 29, 2013
    Publication date: August 1, 2013
    Applicant: Eli Lily and Company
    Inventor: Eli Lily and Company
  • Patent number: 8324427
    Abstract: 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: Grant
    Filed: March 11, 2009
    Date of Patent: December 4, 2012
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kentaro Yamamoto, Nobuto Minowa, Masahisa Nakada
  • Publication number: 20120157705
    Abstract: 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: Application
    Filed: July 9, 2010
    Publication date: June 21, 2012
    Inventor: Hiroyuki Kawakami
  • Patent number: 8022250
    Abstract: 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: Grant
    Filed: December 24, 2009
    Date of Patent: September 20, 2011
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
  • Publication number: 20110182864
    Abstract: 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: Application
    Filed: July 29, 2010
    Publication date: July 28, 2011
    Applicants: CALIFORNIA INSTITUTE OF TECHNOLOGY, CALANDO PHARMACEUTICALS, INC.
    Inventors: Suzie Hwang Pun, Hector Gonzalez, Mark E. Davis, Nathalie C. Bellocq, Jianjun Cheng
  • Patent number: 7910623
    Abstract: 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: Grant
    Filed: January 22, 2008
    Date of Patent: March 22, 2011
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Stephen P. Waters
  • Publication number: 20110065792
    Abstract: 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: Application
    Filed: March 11, 2009
    Publication date: March 17, 2011
    Inventors: Kentaro Yamamoto, Nobuto Minowa, Masahisa Nakada
  • Publication number: 20110059400
    Abstract: 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: Application
    Filed: September 3, 2010
    Publication date: March 10, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Akira KAMABUCHI, Yuko YAMASHITA
  • Publication number: 20110009485
    Abstract: 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: Application
    Filed: January 22, 2008
    Publication date: January 13, 2011
    Inventors: Samuel J. Danishefsky, Stephen P. Waters
  • Publication number: 20110009391
    Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.
    Type: Application
    Filed: July 26, 2010
    Publication date: January 13, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Alain Jean BRAUN, Olivier CRESPIN, Claudie NAMANE, Eric NICOLAI, Francois PACQUET, Cecile PASCAL, Christophe PHILIPPO, Olivier VENIER
  • Publication number: 20100324142
    Abstract: 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: Application
    Filed: September 30, 2008
    Publication date: December 23, 2010
    Inventor: John Alexander Troostwyk
  • Publication number: 20100274025
    Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
    Type: Application
    Filed: February 25, 2010
    Publication date: October 28, 2010
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: 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
  • Patent number: 7662995
    Abstract: 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: Grant
    Filed: February 19, 2004
    Date of Patent: February 16, 2010
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
  • Publication number: 20090186940
    Abstract: 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: Application
    Filed: January 22, 2008
    Publication date: July 23, 2009
    Inventors: Samuel J. Danishefsky, Stephen P. Waters
  • Publication number: 20090099251
    Abstract: 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 t
    Type: Application
    Filed: November 22, 2007
    Publication date: April 16, 2009
    Inventors: Antoine De Saizieu, Ann Fowler, Regina Goralczyk, Claus Kilpert, Goede Schueler, Christof Wehrli
  • Patent number: 7517910
    Abstract: 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: Grant
    Filed: March 28, 2005
    Date of Patent: April 14, 2009
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Shuji Kitamura, Nozomu Sakai
  • Publication number: 20090018311
    Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
    Type: Application
    Filed: July 28, 2008
    Publication date: January 15, 2009
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: 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
  • Publication number: 20080275112
    Abstract: 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: Application
    Filed: July 22, 2005
    Publication date: November 6, 2008
    Inventors: Peter R. Schreiner, Lukas Wanka
  • Patent number: 7432400
    Abstract: 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? or
    Type: Grant
    Filed: August 29, 2002
    Date of Patent: October 7, 2008
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Barbara Wagner, Dietmar Hüglin
  • Publication number: 20080183003
    Abstract: 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: Application
    Filed: February 4, 2008
    Publication date: July 31, 2008
    Applicant: Adamas Pharmaceuticals, Inc.
    Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stamler, Stuart A. Lipton
  • Publication number: 20080153850
    Abstract: 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: Application
    Filed: August 29, 2005
    Publication date: June 26, 2008
    Applicant: AstraZeneca AB
    Inventors: Rhonan Ford, Barrie Martin, Toby Thompson, Nicholas Tomkinson, Paul Willis
  • Patent number: 7288671
    Abstract: 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: Grant
    Filed: May 3, 2006
    Date of Patent: October 30, 2007
    Assignees: Nereus Pharmaceuticals, Inc., The Regents of the University of California
    Inventors: Michael Palladino, Emmanuel A. Theodorakis
  • Patent number: 7205432
    Abstract: 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: Grant
    Filed: May 31, 2005
    Date of Patent: April 17, 2007
    Assignee: Kemfine Oy
    Inventors: Mathias Berner, Reijo Partanen, Auli Salakka, Pekka Somersalo
  • Patent number: 7119223
    Abstract: 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: Grant
    Filed: March 27, 2002
    Date of Patent: October 10, 2006
    Assignees: Nereus Pharmaceuticals, Inc., The Regents of the University of California
    Inventors: Michael Palladino, Emmanuel A. Theodorakis
  • Patent number: 7102027
    Abstract: 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: Grant
    Filed: March 24, 2004
    Date of Patent: September 5, 2006
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Shinya Nagano, Jiichiro Hashimoto
  • Patent number: 6881857
    Abstract: 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: Grant
    Filed: February 4, 2002
    Date of Patent: April 19, 2005
    Assignees: Nereus Pharmaceuticals, Inc., University of California
    Inventors: Michael Palladino, Emmanuel A. Theodorakis
  • Patent number: 6875764
    Abstract: 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: Grant
    Filed: October 27, 2000
    Date of Patent: April 5, 2005
    Assignee: New Pharma Research Sweden AB
    Inventors: Sabrina Muzi, Shoaá Abdul Rahman
  • Patent number: 6846941
    Abstract: 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: Grant
    Filed: February 20, 2002
    Date of Patent: January 25, 2005
    Assignee: Resitec Industria Quimica Ltda.
    Inventors: Rodolfo Rohr, Raul Rohr, Jose Anibal Trujillo-Quijano
  • Publication number: 20040242923
    Abstract: An adamantanetricarboxylic acid derivative is represented by following Formula (1): 1
    Type: Application
    Filed: March 24, 2004
    Publication date: December 2, 2004
    Inventors: Shinya Nagano, Jiichiro Hashimoto
  • Patent number: 6750364
    Abstract: 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: Grant
    Filed: June 27, 2002
    Date of Patent: June 15, 2004
    Assignee: Wyeth
    Inventors: Gary Paul Stack, John Dunlop, Alexander Alexei Greenfield, Jonathan Laird Gross
  • Patent number: 6689904
    Abstract: 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: Grant
    Filed: June 27, 2002
    Date of Patent: February 10, 2004
    Assignee: Wyeth
    Inventors: Alexander Alexei Greenfield, John Anthony Butera
  • Patent number: 6689905
    Abstract: 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: Grant
    Filed: June 27, 2002
    Date of Patent: February 10, 2004
    Assignee: Wyeth
    Inventors: Reinhardt Bernhard Baudy, Jean Yi-ching Sze, Jonathan Laird Gross
  • Patent number: 6603041
    Abstract: 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: Grant
    Filed: September 5, 2001
    Date of Patent: August 5, 2003
    Assignee: Celltech R & D Limited
    Inventors: Timothy John Norman, John Robert Porter, John Clifford Head, Andrew James Ratcliffe
  • Patent number: 6593363
    Abstract: The present invention relates to diterpene derivatives prepared from the components which are extracted from Acanthopanax Koreanum and represented by Chemical Formula (1).
    Type: Grant
    Filed: September 15, 2000
    Date of Patent: July 15, 2003
    Assignees: Sae Han Pharm. Co., Ltd.
    Inventors: Young Ger Suh, Young Hoon Choi, Hye Kyung Lee, Young Ho Kim, Hyoung Sup Park
  • Publication number: 20030120095
    Abstract: 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: Application
    Filed: February 20, 2002
    Publication date: June 26, 2003
    Inventors: Rodolfo Rohr, Raul Rohr
  • Patent number: 6562782
    Abstract: 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, arylalk
    Type: Grant
    Filed: May 10, 2000
    Date of Patent: May 13, 2003
    Assignee: University of Rochester
    Inventors: Benjamin L. Miller, Robert D. Hubbard
  • Publication number: 20030040640
    Abstract: 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: Application
    Filed: February 4, 2002
    Publication date: February 27, 2003
    Inventors: Michael Palladino, Emmanuel A. Theodorakis
  • Publication number: 20030018065
    Abstract: This invention provides processes for preparing a group of novel bridged tricyclic compounds having the formula: 1
    Type: Application
    Filed: June 27, 2002
    Publication date: January 23, 2003
    Applicant: Wyeth
    Inventors: Alexander Alexei Greenfield, John Anthony Butera
  • Patent number: RE39744
    Abstract: 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: Grant
    Filed: March 5, 1998
    Date of Patent: July 24, 2007
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Yasutaka Ishii, Tatsuya Nakano, Naruhisa Hirai