Chalcogen Attached Directly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/51)
  • Patent number: 9975870
    Abstract: Amino acid protecting groups are provided for use in peptide synthesis. Particular compounds disclosed include 5,6-dimethoxy-1,1-dioxobenzo[b]thiophi methyloxycarbonyl (DM-Bsmoc) and related amino-protecting groups.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: May 22, 2018
    Assignee: MASSACHUSETTS, UNIVERSITY OF
    Inventors: Louis A. Carpino, Adel A. Abdel-Maksoud, Hesham A. Ahmed, Calin Dan Sferdean
  • Publication number: 20150115199
    Abstract: The present description relates to a polymerizable liquid crystal compound, a polymerizable liquid crystal composition including the same, and an optically anisotropic body.
    Type: Application
    Filed: April 19, 2013
    Publication date: April 30, 2015
    Inventors: Dai Seung Choi, Sung Ho Chun, Dong Woo Yoo, Mi Ra Hong, Kyung Chang Seo, Hyeong Bin Jang, Jung Hyun Kim, Min Hyung Lee, Eun Seok Park
  • Patent number: 8980938
    Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: March 17, 2015
    Assignee: Sanofi
    Inventors: Stephanie Hachtel, Juergen Dedio, Josef Pernerstorfer, Stephen Shimshock, Carolina Lanter
  • Publication number: 20150018547
    Abstract: The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: February 22, 2013
    Publication date: January 15, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Takakura, Yoshihiro Banno, Yoshito Terao, Atsuko Ochida, Sachie Morimoto, Shuji Kitamura, Yoshihide Tomata, Tsuneo Yasuma, Minoru Ikoma, Kei Masuda
  • Publication number: 20150005500
    Abstract: Disclosed are novel ruthenium compounds of formula (Ia) and (Ib): wherein R1 and the moiety are defined herein. Also disclosed is a process for using these novel ruthenium compounds as catalysts for asymmetric hydrogenation and transfer hydrogenation of ketones with high reactivities and excellent selectivities.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 1, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Nizar HADDAD, Heewon LEE, Bo QU, Sonia RODRIGUEZ, Chris Hugh SENANAYAKE
  • Publication number: 20140235660
    Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 21, 2014
    Applicant: NOVARTIS AG
    Inventors: Heather Elizabeth BURKS, Michael A. DECHANTSREITER, Guo HE, Jill NUNEZ, Stefan PEUKERT, Clayton SPRINGER, Yingchuan SUN, Noel Marie-France THOMSEN, George Scott TRIA, Bing YU
  • Publication number: 20140186771
    Abstract: A radiation-sensitive resin composition includes a polymer that includes a structural unit represented by a formula (1), and an acid generator. R1 is a hydrogen atom, a fluorine atom, or the like. R2 is a hydrogen atom or a monovalent hydrocarbon group. R3 is a hydrogen atom, a monovalent chain hydrocarbon group, or the like. R4 is a hydrogen atom, a monovalent chain hydrocarbon group, or the like. R5 is a hydrogen atom, a monovalent chain hydrocarbon group, or the like. R6 is a monovalent chain hydrocarbon group. R6 is bonded to R3 to form a first alicyclic structure, or R6 is bonded to R5 to form a second alicyclic structure. At least one hydrogen atom of R2, R3, or R4 is optionally substituted with a fluorine atom.
    Type: Application
    Filed: March 7, 2014
    Publication date: July 3, 2014
    Applicant: JSR CORPORATION
    Inventor: Hayato NAMAI
  • Patent number: 8680135
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: March 25, 2014
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
  • Patent number: 8530388
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: January 18, 2010
    Date of Patent: September 10, 2013
    Assignee: Syngenta Limited
    Inventors: William Guy Whittingham, Christopher John Mathews, Jeffrey Steven Wailes, Stephane André Marie Jeansmart, Louisa Robinson
  • Patent number: 8440843
    Abstract: A dye sensitized solar cell, comprising a heteroleptic polypyridil complex of Ru, Os or Fe. The donating ligand has an extended conjugated ?-system increasing the light absorbance and keeing the LUMO energy level higher than that of the anchoring ligand. A compacting compound whose molecular structure comprises a terminal group, a hydrophobic part and an anchoring group may be co-adsorbed together with the dye on the semi-conductive metal oxide layer of the photoanode, forming a dense mixed self-assembled monolayer.
    Type: Grant
    Filed: April 7, 2011
    Date of Patent: May 14, 2013
    Assignee: Ecole Polytechnique Fédérale de Lausanne
    Inventors: Shaik Mohammad Zakeeruddin, Cêdric Klein, Peng Wang, Michael Graetzel
  • Publication number: 20130005767
    Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 3, 2013
    Applicant: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20120214994
    Abstract: The present invention relates to (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or to the pharmaceutically acceptable salt thereof, to a method for preparing same, and to a pharmaceutical composition containing same as active ingredients for the diagnosis or treatment of neurodegenerative brain diseases. The aryl derivatives of the present invention are (3-fluoro-2-hydroxy)propyl-functionalized to increase the polarity thereof, and therefore the drugs containing the aryl derivatives can easily permeate into the cerebrovascular membrane, thus increasing the effectiveness of the drugs. As the aryl derivatives of the present invention strongly bind to ?-amyloid, the aryl derivatives, when labeled with radioisotope, can be used as a diagnostic agent for non-invasively diagnosing early Alzheimer's disease.
    Type: Application
    Filed: September 14, 2010
    Publication date: August 23, 2012
    Inventors: Dae-Yoon Chi, Byoung-Se Lee, Sirion Uthaiwan, So-Young Chu, Yu-Jin Bae, Chansoo Park, Dae-Hyuk Moon, Jin-Sook Ryu, Jae-Seung Kim, Seung-Jun Oh
  • Publication number: 20120214770
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.
    Type: Application
    Filed: May 1, 2012
    Publication date: August 23, 2012
    Applicant: BIONOMICS LIMITED
    Inventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
  • Publication number: 20120100566
    Abstract: Chemiluminescent compositions, methods, assays and kits for oxidative enzymes are described. Further disclosed are dioxetane compounds of the form: 0-0 ?R R R T (i) where R can independently be any branched alkyl or cycloalkyl group which provides stabilization for the dioxetane or where both R groups together form a cycloalkyl or polycycloalkyl moiety spiro bound to the dioxetane ring, wherein each R group or the spiro bound moiety can be unsubstituted or substituted with one or more electron-withdrawing groups or electron donating groups, or groups providing preferential oxidative isozyme substrate recognition, and wherein Ri is an aryl group, or an alkyl group of 1-20 carbon atoms, which can be optionally substituted with 1 or more halogen atoms, and wherein T is an aryl or heteroaryl ring capable of emitting light upon enzyme activated decomposition of the dioxetane I. Kits, methods and assays are also disclosed that comprise the dioxetane compounds.
    Type: Application
    Filed: March 1, 2010
    Publication date: April 26, 2012
  • Publication number: 20120091437
    Abstract: An object of the present invention is to provide a polymer having a low LUMO, a high charge transport property, and further high solubility in a solvent. The present invention provides a polymer having a repeating unit represented by the formula (I): wherein Ar0 means an aromatic ring that may have a substituent or substituents, or a heterocycle that may have a substituent or substituents, and X1 and X2 are the same or different and each mean an oxygen atom or a sulfur atom.
    Type: Application
    Filed: March 8, 2010
    Publication date: April 19, 2012
    Applicants: OSAKA UNIVERSITY, SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yutaka Ie, Atsuki Yoshimura, Yoshio Aso, Masato Ueda
  • Patent number: 8133998
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6).
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: March 13, 2012
    Assignee: Zalicus Pharmaceuticals, Ltd.
    Inventors: Hassan Pajouhesh, Hossein Pajouhesh, Yanbing Ding, Jason Tan, Mike Grimwood, Francesco Belardetti, Ramesh Kaul, Richard Holland, Navjot Chahal
  • Publication number: 20120053352
    Abstract: A branched compound having a construction with a core portion, at least 3 side chain portions bonded to the core portion, and end portions bonded to each of the side chain portions, wherein the side chain portions arc groups in which a plurality of conjugated units are linked, at least one of the conjugated units being a divalent heterocyclic group, at least one of the end portions is a group represented by formula (1), and the side chain portions and the end portions are conjugated with the core portion. [In the formula, Ar represents a trivalent aromatic hydrocarbon or a trivalent heterocyclic group, and X represents oxygen, sulfur, or a group represented by formula (a).] [In the formula, A represents hydrogen, a halogen or a monovalent group, and at least one A group is an electron-withdrawing group.
    Type: Application
    Filed: March 10, 2010
    Publication date: March 1, 2012
    Applicants: OSAKA UNIVERSITY, SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yutaka Ie, Makoto Okabe, Yoshio Aso, Masato Ueda
  • 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
  • Publication number: 20110213162
    Abstract: A condensation compound of a fluorinated cyclopentane ring and an aromatic ring, which is useful, for example, for electronic materials, and a process for producing the same are provided. For instance, according to Scheme 1 below, a compound (68) containing a condensed structure formed of a hexafluorocyclopentane ring and an aromatic ring is synthesized. The aromatic ring is not limited to a thiophene ring but can be any ring and any substituent can be used. Thus a compound containing a condensed ring structure formed of a hexafluorocyclopentane ring and an aromatic ring, particularly, for instance, a thiophene ring, which was impossible to produce conventionally, can be produced easily with high yield. The compound of the present invention is particularly suitable to be applied to, for example, electronic materials or semiconductors.
    Type: Application
    Filed: May 12, 2011
    Publication date: September 1, 2011
    Applicant: SUMITOMO CHEMICAL CO., LTD.
    Inventors: Yutaka IE, Yoshio ASO
  • Patent number: 7932404
    Abstract: A dye sensitized solar cell, comprising a-heteroleptic polypyridil complex of Ru, Os or Fe. The donating ligand has an extended conjugated n-system increasing the light absorbance and keeing the LUMO energy level higher than that of the anchoring ligand. A compacting compound whose molecular structure comprises a terminal group, a hydrophobic part and an anchoring? group may be co-adsorbed together with the dye on the semi-conductive metal oxide layer of the photoanode, forming a dense mixed self-assembled monolayer.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: April 26, 2011
    Assignee: Ecole Polytechnique Federale de Lausanne (EPFL)
    Inventors: Shaik Mohammad Zakeeruddin, Cédric Klein, Peng Wang, Michaël Graetzel
  • Publication number: 20110044938
    Abstract: Compounds of a certain formula I, in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.
    Type: Application
    Filed: August 15, 2007
    Publication date: February 24, 2011
    Applicant: NYCOMED GMBH
    Inventors: Bjorn Bartels, Mathias Schmidt, Klaus Pekari, Thomas Beckers, Astrid Zimmermann, Volker Gekeler
  • Patent number: 7872024
    Abstract: The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: January 18, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joey Methot, Thomas A. Miller, David J. Witter
  • Publication number: 20100298356
    Abstract: Compounds of the general formula (I), wherein the substituents are as defined in claim 1, are useful as fungicides.
    Type: Application
    Filed: September 3, 2008
    Publication date: November 25, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Fiona Kessabi Murphy, Hans-Georg Brunner, Renaud Beaudegnies, Laura Quaranta, Frederik Cederbaum, Jayant Umarye
  • Patent number: 7834034
    Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dawn M. Mampreian, Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
  • Publication number: 20100261727
    Abstract: 2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for ?-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes: wherein R1-R4, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight ?-amyloid peptide binding compound, generation of malignant high-molecular weight ?-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.
    Type: Application
    Filed: October 15, 2009
    Publication date: October 14, 2010
    Inventors: Dae Yoon Chi, Byoung Se Lee, Youjung Jung, Uthaiwan Sirion, Yoo Jin Lim, Yu Jin Bae, Heejun Kim, So Young Chu, Dae Hyuk Moon, Jin-Sook Ryu, Jae Seung Kim, Seung Jun Oh
  • Publication number: 20100105725
    Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
    Type: Application
    Filed: October 26, 2007
    Publication date: April 29, 2010
    Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
  • Patent number: 7655680
    Abstract: Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): wherein A is any one of the following groups (i) and (ii): (i) —CO—B— wherein B is a C1-6 alkylene group and (ii) —CO—Ba— wherein Ba is a C2-6 alkenylene group, and include optical isomers and salts of the compounds.
    Type: Grant
    Filed: May 16, 2005
    Date of Patent: February 2, 2010
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Isao Takemura, Kenji Watanabe, Kunio Oshima, Nobuaki Ito, Junpei Haruta, Hidetaka Hiyama, Masatoshi Chihiro, Hideki Kawasome, Yoko Sakamoto, Hironobu Ishiyama, Takumi Sumida, Kazuhiko Fujita, Hideki Kitagaki
  • Patent number: 7655641
    Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
    Type: Grant
    Filed: February 10, 2004
    Date of Patent: February 2, 2010
    Assignee: Eli Lilly and Company
    Inventors: Scott Eugene Conner, Lynn Stacy Gossett, Jonathan Edward Green, Winton Dennis Jones, Jr., Nathan Bryan Mantlo, Donald Paul Matthews, Daniel Ray Mayhugh, Daryl Lynn Smith, Jennifer Ann Vance, Xiaodong Wang, Alan M Warshawsky, Leonard Larry Winneroski, Jr., Yanping Xu, Guoxin Zhu
  • Publication number: 20090286863
    Abstract: The invention relates to novel compound of the general formula (I), in which R has the meanings indicated in Claim 1, to the preparation thereof and to the use thereof as medicaments. The compounds (I) are inhibitors of steroid sulfatase and are used for the treatment of cancer.
    Type: Application
    Filed: June 5, 2007
    Publication date: November 19, 2009
    Inventors: David Bruge, Wolfgang Staehle, Gerald Scholz, Benoit Rondot, Jean Lafay
  • Publication number: 20090258936
    Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Application
    Filed: December 18, 2008
    Publication date: October 15, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Stephanie HACHTEL, Juergen DEDIO, Josef PERNERSTORFER, Stephen SHIMSHOCK, Carolina LANTER
  • Patent number: 7592375
    Abstract: Disclosed herein is an ion conductive polymer comprising a unit represented by Formula (1) below: —SO2[N?SO2(M+)]X1-??(1) wherein X1 is an integer greater than 1, and M+ is H+ or Li+. Further disclosed is an imide monomer represented by Formula (A) below: Z1-SO2[N?SO2M+]Y-Z2 ??(A) wherein Y is an integer of 2 or greater, Z1 is OH, F, Cl, Br, I or NZ3Z4 (in which Z3 and Z4 are each independently H, M or SiMe3, and M is a metal element), Z2 is OH, F, Cl, Br, I or NZ3Z4 (in which Z3 and Z4 are each independently H, M or SiMe3, and M is a metal element), and M+ is H+ or Li+.
    Type: Grant
    Filed: May 2, 2006
    Date of Patent: September 22, 2009
    Assignee: Kabushiki Kaisha Toyota Chuo Kenkyusho
    Inventors: Greg Shafer, Masaya Kawasumi, Yoichi Hosokawa, Naoki Hasegawa, Satoru Yamamoto, Kenji Imai, Yuko Murayama, Shiaki Hyodo
  • Publication number: 20090221564
    Abstract: Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.
    Type: Application
    Filed: February 20, 2007
    Publication date: September 3, 2009
    Applicant: TRIGEN LIMITED
    Inventors: Shouming Wang, Toby Jonathan Blench, Frederic Marlin, Richard Beck, Roger Peter Dickinson
  • Publication number: 20090216014
    Abstract: The present invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative and antiangiogenic activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, or associated with unregulated angiogenesis including growth and metastasis of solid tumors, ocular diseases and especially retinopathies, or arthritis, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers (such as leukemia), ocular diseases and arthritis.
    Type: Application
    Filed: February 19, 2009
    Publication date: August 27, 2009
    Applicant: EXONHIT THERAPEUTICS SA
    Inventors: Bertrand LEBLOND, Silvere Petit, Virginie Picard, Thierry Taverne, Fabien Schweighoffer
  • Patent number: 7534475
    Abstract: A new liquid crystal compound comprises two condensed and substituted rings. The ring preferably is a five-membered heterocyclic ring. The heterocyclic ring is preferably condensed with benzene ring or an aromatic six-membered heterocyclic ring. The benzene ring or the aromatic six-membered heterocyclic ring is preferably substituted with a group comprising a cyclic structure and a chain structure. The liquid crystal compound is advantageously used in preparation of a thin phase retarder, such as a wide-ranged ?/4 plate, which gives inverse wavelength distribution. The phase retarder can be easily produced according to a simple process by using the new liquid crystal compound.
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: May 19, 2009
    Assignee: Fujifilm Corporation
    Inventors: Hideyuki Nishikawa, Ryo Hamasaki, Atsuhiro Ohkawa
  • Patent number: 7531672
    Abstract: The present invention relates to a process for preparing heterocyclic ketones of the formulae (I) and (la), by reacting a heterocyclic compound of the formula (II), with an ?, ?-unsaturated carboxylic acid of the formula (III), or with its anhydride of the formula (IV), where R1 is hydrogen or a C1-C40 carbon-containing group, R2 is hydrogen or a C1-C40 carbon-containing group, or R1 and R2 together form a cyclic ring system, R3 is a C1-C40 carbon-containing group and X is an element of the 16th group of the Periodic Table or is a divalent nitrogen group —(N—R4)—, where R4 is an electron-withdrawing radical which is selected from the group consisting of perhalogenated C1-C40 carbon-containing radicals and C1-C40 organosulfonyl groups.
    Type: Grant
    Filed: December 17, 2003
    Date of Patent: May 12, 2009
    Assignee: Basell Polyolefine GmbH
    Inventors: Michael J. Elder, Robert L. Jones
  • Publication number: 20090118323
    Abstract: The present invention provides antitumor compounds of the formula (I); and antitumor methods.
    Type: Application
    Filed: September 11, 2007
    Publication date: May 7, 2009
    Inventors: Mary Margaret Mader, Luisa Maria Martin-Cabrejas, Michael Enrico Richett
  • Publication number: 20080319047
    Abstract: The invention provides a glucitol derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): wherein m is an integer selected among 1-3; R1 to R4 each independently is optionally substituted alkyl, etc.; Ar1 is optionally substituted naphthyl; and A is optionally substituted heteroaryl, a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, and the like each containing the compound.
    Type: Application
    Filed: July 27, 2005
    Publication date: December 25, 2008
    Inventors: Hiroharu Matsuoka, Tsutomu Sato, Masahiro Nishimoto, Yasuharu Kato, Masahiro Sakaitani, Sang-Hak Lee
  • Patent number: 7425631
    Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: April 12, 2004
    Date of Patent: September 16, 2008
    Assignees: Amgen Inc., Array BioPharma Inc.
    Inventors: Robert D. Groneberg, Benny C. Askew, Jr., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak
  • Patent number: 7417064
    Abstract: There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: August 26, 2008
    Assignee: Eli Lilly and Company
    Inventors: Serge Louis Boulet, Sandra Ann Filla, Peter Thaddeus Gallagher, Kevin John Hudziak, Anette Margareta Johansson, Rushad E. Karanjawala, John Joseph Masters, Victor Giulio Matassa, Brian Michael Mathes, Richard Edmund Rathmell, Maria Ann Whatton, Chad Nolan Wolfe
  • Patent number: 7410996
    Abstract: There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0,
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: August 12, 2008
    Assignee: Eli Lilly and Company
    Inventors: Serge Louis Boulet, Sandra Ann Filla, Peter Thaddeus Gallagher, Kevin John Hudziak, Anette Margareta Johansson, Rushad E. Karanjawala, John Joseph Masters, Victor Giulio Matassa, Brian Michael Mathes, Richard Edmund Rathmell, Maria Ann Whatton, Chad Nolan Wolfe
  • Patent number: 7399781
    Abstract: The present invention relates to an N-substituted benzothiophenesulfonamide derivative or a pharmaceutically acceptable salt thereof and applications thereof. Furthermore, it provides an agent for preventing or treating cardiac or circulatory disease and so on caused by abnormal increase of production of angiotensin II or endothelin I based on chymase activity, or by activation of mast cell, and an agent for preventing adhesion after surgery, wherein the agent has a selective inhibitory action on chymase.
    Type: Grant
    Filed: January 10, 2006
    Date of Patent: July 15, 2008
    Assignee: TOA EIYO Ltd.
    Inventors: Shoji Satoh, Akira Tatsui, Takeshi Hasegawa, Hideki Yamada, Shin-ichi Kazayama, Takahiro Morita, Hidekazu Masaki, Atsuo Takahashi, Fumiya Yoneyama, Tetsuo Kuze, Yusuke Mizuno, Mizuo Miyazaki, Shinji Takai
  • Patent number: 7375130
    Abstract: The invention relates to compounds of the general formula (I) below: in which R1, R2, R3, R4, R5, R6 and X are as defined in claim 1. These compounds can be used in the treatment of pathologies associated with insulin resistance syndrome.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: May 20, 2008
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Gérard Moinet, Caroline Leriche, Micheline Kergoat
  • Patent number: 7371774
    Abstract: The invention relates to compounds of the general formula (I) below: in which R1, R2, R3, R4, R5, R6 and X are as defined in claim 1. These compounds can be used in the treatment of pathologies associated with insulin resistance syndrome.
    Type: Grant
    Filed: November 8, 2004
    Date of Patent: May 13, 2008
    Assignee: Merck Patent GmbH
    Inventors: Gérard Moinet, Caroline Leriche, Micheline Kergoat
  • Patent number: 7271264
    Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: September 18, 2007
    Assignee: Eli Lilly and Company
    Inventors: Ronald Jay Hinklin, Owen Brendan Wallace
  • Patent number: 7270871
    Abstract: A dispersion, and a film and optoelectronic devices formed from the dispersion are provided. The dispersion comprising conducting polymer containing particles having a particle size of less than 450 nm, wherein the conducting polymer comprises substituted or unsubstituted, uncharged or charged polymerized units of thieno[3,4-b]thiophene, and wherein a film drop cast from the dispersion has a conductivity from 10?1 to 10?6 S/cm measured using the four point probe method.
    Type: Grant
    Filed: January 12, 2004
    Date of Patent: September 18, 2007
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Xuezhong Jiang, Roy Daniel Bastian
  • Patent number: 7244763
    Abstract: This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.
    Type: Grant
    Filed: February 6, 2004
    Date of Patent: July 17, 2007
    Assignee: Warner Lambert Company LLC
    Inventors: Larry D. Bratton, Xue-Min Cheng, Noe Erasga, Gary F. Filzen, Andrew G. Geyer, Chitase Lee, Bharat K. Trivedi, Paul C. Unangst
  • Patent number: 7157491
    Abstract: This invention provides estrogen receptor modulators having the structure where R1–R5 are as defined in the specification; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 13, 2004
    Date of Patent: January 2, 2007
    Assignee: Wyeth
    Inventors: Richard Eric Mewshaw, Stephen Todd Cohn
  • Patent number: 7094365
    Abstract: Thienothiophene monomers having an SF5 group and conducting oligomers and polymers formed by the polymerization of such monomers and their use as hole injection materials, charge transport materials, or as semiconductors. The compound may be of the formula: where X and X? are independently H, halogen atoms (e.g., F, Cl, Br, and I), MgCl, MgBr, MgI, Sn(R?)3, where R? is C1-6 alkyl or —OC1-6 alkyl, boronic acid, boronic ester, —CH?CHR? (where R? is H or C1-6 alkyl), —OC1-6 alkyl, —COOC1-6 alkyl, —S—COR?? and —COR?? (where R?? is H or C1-6 alkyl), —C?CH, or polymerizable aromatic rings (such as phenyl, naphthalene, pyrrole, dithiophene, thienothiophene, thiophene and so forth.
    Type: Grant
    Filed: October 4, 2004
    Date of Patent: August 22, 2006
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Steffen Zahn, Andrew Francis Nordquist, Kristen Elaine Minnich, Gauri Sankar Lal, William Franklin Burgoyne, Jr., Axel Klauck-Jacobs
  • Patent number: 7084136
    Abstract: A compound of the formula (I): wherein A is alkylene optionally having an unsaturated bond; R is —C(?O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.
    Type: Grant
    Filed: May 28, 2001
    Date of Patent: August 1, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Norihiko Tanimoto, Akinori Arimura
  • Patent number: 7037932
    Abstract: There is provided a heretoaryloxy 3-substituted propanamine compound of formula (I): wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents selected from halo, C1–C4 alkyl and C1–C4 alkoxy, and thienyl optionally substituted with up to 3 substituents selected from halo and C1–C4 alkyl; Y is selected from benzothienyl, indolyl and benzofuranyl, optionally substituted with up to 5 substituents selected from halo, C1–C4 alkyl, C1–C4 alkoxy, nitro, acetyl and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1–C4 alkyl; R1 and R2 are each independently H or C1–C4 alkyl; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 6, 2002
    Date of Patent: May 2, 2006
    Assignee: Eli Lilly and Company
    Inventors: Peter Gallagher, Richard Edmund Rathmell, Maria Ann Fagan