Bicyclo Ring System Having The Lactone Ring As One Of The Cyclos Patents (Class 549/302)
  • Patent number: 10995080
    Abstract: Synthetic methods of preparing perhydro-3,6-dimethyl-2-benzo[b]furanones, in particular dihydromintlactone, and analogs through reaction of dehydrogenation of menthanediols and analogs with a base in the presence of (carbonylchlorohydrido[bis-(2-diphenylphosphinoethyl)amine]ruthenium(II) as catalyst in good stereoselectivity and yields under stereochemistry controlled conditions are disclosed.
    Type: Grant
    Filed: May 28, 2020
    Date of Patent: May 4, 2021
    Assignee: INTERNATIONAL FLAVOR & FRAGRANCES INC.
    Inventors: Yigal Becker, Michael Cheskis
  • Publication number: 20150057207
    Abstract: The present invention relates to novel compounds and their use as fragrance materials.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Inventors: Benjamin Amorelli, Edward Mark Arruda, Robert P. Belko, Tingwei Cai, Adam P. Closson, Nicole L. Giffin, Gary J. Mertz, Michael G. Monteleone
  • Publication number: 20140256782
    Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic is visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Applicant: Bikam Pharmaceuticals, Inc.
    Inventors: David S. Garvey, Gregory J. Larosa, Jeremy R. Greenwood, Leah L. Frye, Tan Quach, Jamie B. Cote, Judd Berman
  • Patent number: 8673578
    Abstract: The present invention relates to antagonists and agonists of the human bitter-taste receptors hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and hTAS2R47. The invention also relates to methods for identifying further molecules that suppress or enhance bitter taste transduction or bitter taste response mediated by hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and/or hTAS2R47 and uses thereof.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: March 18, 2014
    Assignee: Deutsches Institut für Ernahrungsforschung Potsdam-Rehbrücke
    Inventors: Giovanni Appendino, Maik Behrens, Anne Brockhoff, Wolfgang Meyerhof
  • Patent number: 8623946
    Abstract: Described is the use of specific lactone compounds for protecting body-care and household products from photolytic and oxidative degradation. These compounds perform outstanding antioxidant properties.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: January 7, 2014
    Assignee: BASF SE
    Inventors: Oliver Reich, Michael Schork
  • Publication number: 20130316966
    Abstract: Disclosed is a use of albiflorin or a metabolite thereof in preparation of antianxiety and sleep disorder improving drugs or health-care food. Tests prove that albiflorin has significant antianxiety effects and sleep disorder improving effects achieved by prolonging SWS and low the toxic side effects, thus being a safety monomer compound capable of effectively treating anxiety and sleep disorder.
    Type: Application
    Filed: November 9, 2011
    Publication date: November 28, 2013
    Inventor: Zuoguang Zhang
  • Patent number: 8586743
    Abstract: The present disclosure is directed to a reactive ester agent capable of conjugating a reporter molecule to a carrier molecule or solid support. The reactive ester agent has the general formula: wherein the variables are described throughout the application.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: November 19, 2013
    Assignee: Life Technologies Corporation
    Inventors: Kyle Gee, Aleksey Rukavishnikov, Diane M. Witczak
  • Publication number: 20130303466
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: November 14, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley, Alain D. Baron
  • Publication number: 20130252815
    Abstract: Embodiments of the invention relate to compounds and methods for controlling algal growth, for example, in bodies of water or surfaces exposed to algae. Provided are compounds having algicidal activities and methods of use of these compounds as well as formulations and compositions comprising the compound having algicidal activities.
    Type: Application
    Filed: August 22, 2011
    Publication date: September 26, 2013
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Roberto Kolter, Rebecca Case, Jon Clardy, Mohammad Seyedsayamdost
  • Publication number: 20130245286
    Abstract: The present invention relates to a method comprising (A) reacting a ?-keto ester with a 2-halo ester under basic conditions to obtain a 2-aceto-3-methyl-succinic acid ester; (B) reacting the resulting 2-aceto-3-methyl-succinic acid ester with methyl vinyl ketone under basic conditions, optionally followed by a decarboxylation reaction and hydrolysis, etc., to obtain an ?-methyl-?-keto acid; and (C) reducing the resulting ?-methyl-?-keto acid to obtain wine lactone or a stereoisomer thereof or a mixture thereof.
    Type: Application
    Filed: May 6, 2013
    Publication date: September 19, 2013
    Applicant: Takasago International Corporation
    Inventors: Kenji Yagi, Yasuhiro Komatsuki, Hideo Ujihara, Kenya Ishida
  • Publication number: 20130197077
    Abstract: A class of bicyclic brominated furanone structures that have reduced toxicity and high activity for inhibiting biofilm formation and quorum sensing by microbes. The molecules have two fused cyclic alkyl groups that provide a structural framework that retain one or more bromine groups on the structure. The bicyclic furanones have reduced toxicity to mammalian cells as compared to other brominated furanones but retain the ability to inhibit biofilm formation in bacterial populations.
    Type: Application
    Filed: January 25, 2013
    Publication date: August 1, 2013
    Applicant: SYRACUSE UNIVERSITY
    Inventor: Syracuse University
  • Patent number: 8481758
    Abstract: The present invention relates to an improved process for the production of prostaglandins and prostaglandin analogs. In particular, this invention relates to the production of prostaglandins of the PGF2?-series, including latanoprost, travoprost, and bimatoprost, which are active pharmaceutical ingredients used for the reduction of elevated intra-ocular pressure in patients with glaucoma and ocular hypertension.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: July 9, 2013
    Assignee: Sandoz AG
    Inventors: Martin Albert, Andreas Berger, Dominic De Souza, Kerstin Knepper, Hubert Sturm
  • Publication number: 20120283324
    Abstract: The present invention relates to antagonists and agonists of the human bitter-taste receptors hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and hTAS2R47. The invention also relates to methods for identifying further molecules that suppress or enhance bitter taste transduction or bitter taste response mediated by hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and/or hTAS2R47 and uses thereof.
    Type: Application
    Filed: October 27, 2010
    Publication date: November 8, 2012
    Applicant: DEUTSCHES INSTITUT FUR EMAHRUNGSFORSCHUNG POTSDAM-REHBRUCKE
    Inventors: Giovanni Appendino, Maik Behrens, Anne Brockhoff, Wolfgang Meyerhof
  • Publication number: 20120270820
    Abstract: A pharmaceutical composition containing albiflorin and use thereof in manufacturing medicaments for preventing and treating depression are provided by the present invention.
    Type: Application
    Filed: August 24, 2010
    Publication date: October 25, 2012
    Inventor: Zuoguang Zhang
  • Publication number: 20120231141
    Abstract: [Object] To improve bitterness or astringency, for example, to reduce stimulative bitterness or astringency of bitter or astringent food and drink, without imparting unnecessary taste or aroma to the food and drink. [Solution] A bitterness- or astringency-improving agent for bitter or astringent food and drink includes phthalides as an active ingredient. Addition of a very small amount of phthalides that are not sensed as aroma to food and drink improves undesirable bitterness or astringency of various bitter or astringent food and drink products and enhances or provides pleasant bitterness or astringency.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 13, 2012
    Inventors: Yoshiko Kurobayashi, Setsuko Nakai, Kikue Kubota
  • Publication number: 20120164120
    Abstract: The present invention relates to a novel monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.
    Type: Application
    Filed: December 23, 2011
    Publication date: June 28, 2012
    Applicant: FOOD INDUSTRY RESEARCH AND DEVELOPMENT INSTITUTE
    Inventors: Ming-Jen Cheng, Ping-Hsun Yang, Ming-Der Wu, Shie-Jea Lin, Gwo-Fang Yuan, Yen-Lin Chen, Hsuen-Chun Liao, Kai-Ping Chen
  • Patent number: 8173699
    Abstract: Compounds of formula 1 and hetero derivatives thereof and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: May 8, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Horst Dollinger, Rolf Goeggel, Birgit Jung, Joerg Kley, Jurgen Mack, Peter Nickolaus, Rainer Walter
  • Publication number: 20110313032
    Abstract: The present invention is directed to a compound of formula (I), its diastereoisomers, its enantiomers or its pharmaceutically acceptable salts or solvates, formula (I), to procedures of obtaining the same, to intermediates thereof, and use as competitive inhibitors of the third enzyme of the shikimic acid pathway, the type II dehydroquinase.
    Type: Application
    Filed: December 23, 2009
    Publication date: December 22, 2011
    Applicant: UNIVERSIDADE DE SANTIAGO DE COMPOSTELA
    Inventors: Cóncepcion González Bello, Verónica Filipa Vieira Prazeres, Sonia Paz Gómez, Cristina Sánchez Sixto, Lorena Tizón Valverde
  • Patent number: 7897793
    Abstract: The invention relates to a process for the preparation of 13,14-dihydro-PGF2? derivatives of R or S configuration at carbon 15, represented by the general formula (I), wherein the identity of the substituents is defined in the description. Compounds of the formula (I) are valuable biologically-active substances or intermediates in the preparation thereof. The invention especially relates to the process for preparation of 13,14-dihydro-15(R)-17-substituted-18,19,20-trinor-PGF2?, i.e., latanoprost.
    Type: Grant
    Filed: October 18, 2007
    Date of Patent: March 1, 2011
    Assignee: Instytut Farmaceutyczny
    Inventors: Jacek Martynow, Julita Szyc, Wieslaw Szelejewski, Osman Achmatowicz, Andrzej Kutner, Krzysztof Wiśniewski, Jerzy Winiarski, Oliwia Zegrocka-Stendel, Piotr Golebiewski
  • Publication number: 20100298427
    Abstract: The present invention relates to the use of compounds of the formula (I) wherein the clotted line is an optional bond; R1 is butyl or butyryl if R2 is hydroxyl but is butyl if R2 is hydrogen; or R1 and R2 taken together are 1-butylidene optionally substituted by hydroxyl, methyl, or 3-(?,?-dimethylacrylyloxy)-pentylidenyl; X is a residue selected from the group consisting of X1, X2, X3, X4, and X5; wherein X is X2, X3 or X5 if the dotted line in formula (I) is absent; and X is X1, X4 or X5 if the dotted line signifies a bond in formula (I) above; R3 is hydroxyl or butyryl; and n is 1 or 2, as agents for the prevention, control and treatment of conditions requiring modulation of inflammation in mammals. In another aspect, the present invention relates to the use of compounds of the formula (I) as active ingredients in the manufacture of medicaments/compositions for the prevention, control and treatment of conditions requiring modulation of inflammation.
    Type: Application
    Filed: June 18, 2010
    Publication date: November 25, 2010
    Applicant: DSM IP ASSETS B.V.
    Inventors: Ann Fowler, Daniel Raederstorff, Goede Schuler, Joseph Schwager
  • Patent number: 7807607
    Abstract: There are described novel rhodamine color-forming compounds. The rhodamine color-forming compounds exhibit a first color when in a crystalline form and a second color, different from the first color, when in an amorphous form. Thermal imaging members containing these color-formers are also described.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: October 5, 2010
    Assignee: Zink Imaging, Inc.
    Inventors: Kap-Soo Cheon, Michael P. Filosa, Fariza Hasan, Xavier Herault, John L. Marshall
  • Publication number: 20100130498
    Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.
    Type: Application
    Filed: March 31, 2008
    Publication date: May 27, 2010
    Applicant: Deutshes Institut Fur Ernahrungsforschung Potsdam- Rehbrucke
    Inventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
  • Patent number: 7723381
    Abstract: Compounds of formula 1 and hetero derivatives thereof and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
    Type: Grant
    Filed: April 21, 2006
    Date of Patent: May 25, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Horst Dollinger, Rolf Goeggel, Birgit Jung, Joerg Kley, Juergen Mack, Peter Nickolaus, Rainer Walter
  • Patent number: 7687645
    Abstract: Methods for manufacture of 5-alkoxycarbonylphthtalides are disclosed. The 5-alkoxycarbonylphthtalides are useful in syntheses of the well-known antidepresssants citalopram and escitalopram.
    Type: Grant
    Filed: March 17, 2004
    Date of Patent: March 30, 2010
    Assignee: H. Lundbeck A/S
    Inventors: Thomas Pittelkow, Andrea Castellin, Federico Sbrogiò, Poul D. Nielsen, Jacobo Zanon, Steen Sogaard, Rikke E. Humble
  • Patent number: 7683188
    Abstract: Provided are processes for preparation of mycophenolic acid.
    Type: Grant
    Filed: April 26, 2005
    Date of Patent: March 23, 2010
    Assignee: TEVA Gyógyszergyár Zártkōrūen Mūkōdō Részvénytársaság
    Inventors: Vilmos Keri, Zoltan Czovek
  • Publication number: 20100056621
    Abstract: The present invention relates to agonists of the hTAS2R14 bitter taste receptor and its role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block hTAS2R14 bitter taste transduction or bitter taste response.
    Type: Application
    Filed: April 20, 2005
    Publication date: March 4, 2010
    Applicant: Deutsches Institut fur Ernahrungsforschung
    Inventors: Maik Behrens, Anne Brockhoff, Bernd Bufe, Christina Kuhn, Wolfgang Meyerhof, Marcel Winnig
  • Publication number: 20100010239
    Abstract: The present invention relates to an improved process for the production of prostaglandins and prostaglandin analogs. In particular, this invention relates to the production of prostaglandins of the PGF2?-series, including latanoprost, travoprost, and bimatoprost, which are active pharmaceutical ingredients used for the reduction of elevated intra-ocular pressure in patients with glaucoma and ocular hypertension.
    Type: Application
    Filed: July 10, 2009
    Publication date: January 14, 2010
    Applicant: Sandoz AG
    Inventors: Martin ALBERT, Andreas BERGER, Dominic DE SOUZA, Kerstin KNEPPER, Hubert STURM
  • Publication number: 20090274984
    Abstract: Carboxyl-containing lactone compounds having formula (1) are novel wherein R1 is H, F, methyl or trifluoromethyl, R2 and R3 are H or monovalent hydrocarbon groups, or R2 and R3 may together form an aliphatic ring, W is CH2, O or S, k1 is an integer of 0 to 4, and k2 is 0 or 1. They are useful as monomers to produce polymers which are transparent to radiation ?500 nm. Radiation-sensitive resist compositions comprising the polymers as base resin exhibit excellent properties including resolution, LER, pattern density dependency and exposure margin.
    Type: Application
    Filed: May 1, 2009
    Publication date: November 5, 2009
    Inventors: Satoshi SHINACHI, Tsunehiro Nishi, Koji Hasegawa, Takeshi Kinsho, Seiichiro Tachibana, Takeru Watanabe
  • Publication number: 20090275761
    Abstract: Preparation of cyclic esters by hydrogenation of a carbonyl group in at least one anhydride radical —C(O)—O—C(O)— of a cyclic dicarboxylic or polycarboxylic anhydride by means of hydrogen in the presence of a homogeneous noble metal catalyst, characterized in that the hydrogenation is carried out in a homogeneous reaction mixture using an iridium catalyst. The cyclic esters are obtained in good chemical and optical yields when prochiral anhydrides are used together with chiral iridium catalysts.
    Type: Application
    Filed: April 7, 2006
    Publication date: November 5, 2009
    Inventor: Felix Spindler
  • Patent number: 7595408
    Abstract: The present invention relates to methods for the preparation of diastereomerically pure (3R,3aS,6aR) hexahydro-furo[2,3-b]furan-3-ol as well as a novel intermediate, (3aR,4S,6aS) 4-methoxy-tetrahydro-furo[3,4-b]furan-2-one for use in said methods. More in particular the invention relates to a stereoselective method for the preparation of diastereomerically pure (3R,3aS,6aR) hexahydro-furo[2,3-b]furan-3-ol, as well as methods for the crystallization of (3aR,4S,6aS) 4-methoxy-tetrahydro-furo[3,4-b]furan-2-one and for the epimerization of (3aR,4R,6aS) 4-methoxy-tetrahydro-furo[3,4-b]-furan-2-one to (3aR,4S,6aS) 4-methoxy-tetrahydro-furo[3,4-b]furan-2-one.
    Type: Grant
    Filed: March 31, 2005
    Date of Patent: September 29, 2009
    Assignee: Tibotec Pharmaceuticals, Ltd.
    Inventors: Peter Jan Leonard Mario Quaedflieg, Bart Rudolf Romanie Kesteleyn, Robert Jan Vijn, Constantinus Simon Maria Liebregts, Jacob Hermanus Matheus Hero Kooistra, Franciscus Alphons Marie Lommen
  • Patent number: 7572606
    Abstract: Disclosed are methods of modulating biosynthesis of Salinosporamide A and its analogs, which are useful in treating cancer, inflammatory conditions, and/or infectious disease. The methods involve, for example, genetic manipulation, selection of reagents in the fermentation feedstock, and selection of fermentation conditions.
    Type: Grant
    Filed: September 8, 2006
    Date of Patent: August 11, 2009
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventors: Kin Sing Lam, Michael Palladino, Ginger Tsueng
  • Publication number: 20090118157
    Abstract: The present invention provides a method for producing wine lactone, a method for producing intermediates that are usable in production of wine lactone, and techniques for the application of wine lactone. The method for producing the wine lactone (Compound (6)) of the present invention comprises the following steps (A) to (E): wherein R1 is a C1-4 lower alkyl group.
    Type: Application
    Filed: September 10, 2004
    Publication date: May 7, 2009
    Applicant: San-Ei Gen F.F.I. Inc.
    Inventors: Mineko Omoto, Chiyoki Yukawa, Yoshiteru Nishijo
  • Patent number: 7511168
    Abstract: The present invention provides novel processes for the preparation of a cyclopentanone of Formula II and a lactone of Formula I, which are useful in the production of prostaglandins: wherein Z, R2, R3, X1, X2, and are as defined in the specification. The invention also provides novel enantiomerically enriched compounds.
    Type: Grant
    Filed: January 18, 2006
    Date of Patent: March 31, 2009
    Inventors: Shih-Yi Wei, Yu-Chih Yeh
  • Patent number: 7488836
    Abstract: A compound of the following formula: wherein X, Y, and Z are as defined herein. Also disclosed are methods for inhibiting TNF? expression, IL-1? expression, iNOS expression, and NF-?B activity and methods for treating autoimmune disease, cancer, or atherosclerosis with such a compound.
    Type: Grant
    Filed: August 14, 2007
    Date of Patent: February 10, 2009
    Assignee: Hutchison Medipharma Enterprises Limited
    Inventors: Weiguo Su, Hong Jia, Weihan Zhang, Xiaoqiang Yan, Jifeng Duan, Tao Wang, Yu Cai
  • Patent number: 7488752
    Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein z,1 represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein A, B, G, M, X, J, n, Het, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
    Type: Grant
    Filed: October 5, 2005
    Date of Patent: February 10, 2009
    Assignee: Schering Corporation
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia, Keith A. Eagen
  • Patent number: 7427684
    Abstract: A homogeneous process for the hydrogenation of dicarboxylic acid and/or derivative thereof with an amine in the presence of a catalyst comprising: (a) ruthenium or osmium; and (b) an organic phosphine; and wherein the hydrogenation is carried out in the presence of water.
    Type: Grant
    Filed: October 15, 2004
    Date of Patent: September 23, 2008
    Assignee: Davy Process Technology Limited
    Inventors: Simon Peter Crabtree, Derek Vincent Tyers, Mohammed Sharif
  • Publication number: 20080207926
    Abstract: The invention relates to a process for the preparation of 13,14-dihydro-PGF2? derivatives of R or S configuration at carbon 15, represented by the general formula (I), wherein the identity of the substituents is defined in the description. Compounds of the formula (I) are valuable biologically-active substances or intermediates in the preparation thereof. The invention especially relates to the process for preparation of 13,14-dihydro-15(R)-17-substituted-18,19,20-trinor-PGF2?, i.e., latanoprost.
    Type: Application
    Filed: October 18, 2007
    Publication date: August 28, 2008
    Applicant: INSTYTUT FARMACEUTYCZNY
    Inventors: Jacek MARTYNOW, Julita SZYC, Wieslaw SZELEJEWSKI, Osman ACHMATOWICZ, Andrzej KUTNER, Krzysztof WISNIEWSKI, Jerzy WINIARSKI, Oliwia ZEGROCKA-STENDEL, Piotr GOLEBIEWSKI
  • Patent number: 7345051
    Abstract: The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds of Formula II in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases. wherein X is S, N, O or CR; Y is CRR?, O, NR6, CRR?—CRR? or CR?CR; Z is NR6, O, S, CRR? or CRR?—CRR?; R1-R3 are independently selected from the group consisting of H, C1-C8 alkyl, C1-C8 alkoxy, amino, hydroxy, halosubstituted alky and halo; R4 is Q is CR, NR6 or R5 is H or benzyl; R6 is H, C1-C8 alkyl, C1-C8 alkoxy, OH or halo; and R and R? are independently H, C1-C8 alkyl, C1-C8 alkoxy, OH or halo, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 8, 2002
    Date of Patent: March 18, 2008
    Assignee: Genaera Corporation
    Inventors: Yuhong Zhou, Roy C. Levitt, Nicholas C. Nicolaides, Steve Jones, Mike McLane
  • Publication number: 20080058536
    Abstract: Methods for manufacture of 5-alkoxycarbonylphthtalides are disclosed. The 5-alkoxycarbonylphthtalides are useful in syntheses of the well-known antidepresssants citalopram and escitalopram.
    Type: Application
    Filed: March 17, 2004
    Publication date: March 6, 2008
    Applicant: H. Lundbeck A/S
    Inventor: Thomas Pittelkow
  • Patent number: 7307175
    Abstract: Process for the preparation of compounds of formula (I) wherein R is halogen, R1O1R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkly, aryl-C1-C8alkyl, C1-C8haloalkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, in which process, in a solvent, (1) an aniline derivative of formula (IV) wherein R is as defined above, and R3 is C1-C5alkyl or C1-C5haloalkyl, is diazotised in the presence of a mineral acid to form the corresponding diazonium salt of formul (II) wherein R and R3 are as defined above, Am? is an anion, and m is 1 or 2, (2) the resulting diazonium salt of formula (II) is carbonylated in the presence of a catalyst, CO and optionally a buffer, to form a benzoic acid derivative of formula (III) wherein R and R3 are as defined above, and (3) the benzoic acid derivative of formula (III) is then subjected to benzylic lactonisation in the ortho-position alkyl chain R3 in the presence of a free-radical initiator and a halogenating agent.
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: December 11, 2007
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Anita Schnyder, Marco Passafaro, Thomas Rapold
  • Patent number: 7276533
    Abstract: This invention features the use of the spirolaxine of formula (I) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the Type 2 insulin-resistant diabetes. This invention also features a pharmaceutical composition in which the spirolaxine of formula (I) acts as active principle in association with the all-trans retinoic acid of formula (II) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the acute malignant haemopathies.
    Type: Grant
    Filed: July 13, 2004
    Date of Patent: October 2, 2007
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Claudio Pisano, Teresa Riccioni
  • Patent number: 7049459
    Abstract: This invention relates to 1-[(4-methyl thio)phenyl]-2-(phenyl acetoxy)-1-ethanone. This compound is convertible into 4-(4-methyl thio phenyl)-3-phenyl-2 (5H)-furanone by an economically viable process. This substituted furanone is an intermediate or starting compound for synthesising COX II inhibitor Rofecoxib. This invention also includes a process for preparing the ethanone derivative by halogenating methyl thio aceto phenone and coupling the resulting 2 halosubstituted ethanone with sodium salt of phenyl acetic acid to obtain 1-[(4-methyl thio) phenyl]-2-(phenyl acetoxy)-1-ethanone.
    Type: Grant
    Filed: October 10, 2001
    Date of Patent: May 23, 2006
    Assignee: Shasun Chemicals and Drugs Limited
    Inventors: Tangiraja Venkata Subramanya Krishna Vittal, Mudduluru Hari Krishna
  • Patent number: 6872839
    Abstract: Benzofuran-2-ones, compositions comprising benzofuranones, processes for preparing them, and their use as colorants for high or low molecular mass organic material.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: March 29, 2005
    Assignee: Cibaspecialty Chemicals Corp.
    Inventors: Leonhard Feiler, Thomas Ruch, Olof Wallquist, Peter Nesvadba
  • Publication number: 20040259856
    Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
    Type: Application
    Filed: April 30, 2004
    Publication date: December 23, 2004
    Applicant: The Regents of the University of California
    Inventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H.R. Feling
  • Publication number: 20040249172
    Abstract: Disclosed are processes for the synthesis and purification of prostaglandins and analogues thereof, especially analogues of PGF2&agr;.
    Type: Application
    Filed: June 8, 2004
    Publication date: December 9, 2004
    Inventors: Alan Kenneth Greenwood, Derek McHattie, David George Thompson, Derek Clissold
  • Patent number: 6784302
    Abstract: An optically active lactone compound is produced by using a Zr(salen) complex of the following formula (I) or its enantiomer as a catalyst and subjecting a cyclic ketone compound to a Baeyer-Villiger reaction with at least one oxidizer selected from hydrogen peroxide, aqueous hydrogen peroxide and urea-hydrogen peroxide adduct in a solvent: wherein Ar1 is an aryl group having a carbon number of 10 to 16 and Y is a phenoxy group or an alkoxy group having a carbon number of 1 to 10.
    Type: Grant
    Filed: April 3, 2003
    Date of Patent: August 31, 2004
    Assignee: Kyushu University
    Inventors: Tsutomu Katsuki, Akira Watanabe, Tatsuya Uchida
  • Publication number: 20040158080
    Abstract: Process for the preparation of compounds of formula (I) wherein R is halogen, R1O1R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkly, aryl-C1-C8alkyl, C1-C8haloalkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, in which process, in a solvent, (1) an aniline derivative of formula (IV) wherein R is as defined above, and R3 is C1-C5alkyl or C1-C5haloalkyl, is diazotised in the presence of a mineral acid to form the corresponding diazonium salt of formul (II) wherein R and R3 are as defined above, Am− is an anion, and m is 1 or 2, (2) the resulting diazonium salt of formula (II) is carbonylated in the presence of a catalyst, CO and optionally a buffer, to form a benzoic acid derivative of formula (III) wherein R and R3 are as defined above, and (3) the benzoic acid derivative of formula (III) is then subjected to benzylic lactonisation in the ortho-position alkyl chain R3 in the presence of a free-radical initiator and a halogenating agent.
    Type: Application
    Filed: April 7, 2004
    Publication date: August 12, 2004
    Inventors: Anita Schnyder, Marco Passafaro, Thomas Rapold
  • Patent number: 6762327
    Abstract: A safe and effective process for the oxidation of a primary or secondary alcohol to the corresponding aldehyde or ketone via the reaction of said alcohol with an anhydride solution of a 1,1,1-tri(C2-C4 alkanoyloxy-1,1-dihydro-1,2-benziodoxol-3(1H)-one, and a composition useful in this process.
    Type: Grant
    Filed: April 3, 2003
    Date of Patent: July 13, 2004
    Assignee: Wyeth
    Inventors: Ugo Chiacchio, Antonio Rescifina, Giuseppe Miraglia, Mariangela Magnano, Paola Di Raimondo
  • Publication number: 20040106805
    Abstract: Compounds of general formula (I): wherein R1, Y, (X)0, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therpeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.
    Type: Application
    Filed: January 8, 2004
    Publication date: June 3, 2004
    Inventors: Martin Quibell, Manoj Kumar Ramjee
  • Patent number: RE39754
    Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.
    Type: Grant
    Filed: August 14, 2003
    Date of Patent: July 31, 2007
    Assignee: Schering AG
    Inventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka