Ortho Fused Patents (Class 560/119)
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Patent number: 10150723Abstract: A process to isolate a compound of Formula (2a) or a salt or solvate thereof, comprising a) reacting a mixture of diastereoisomers of Formulae (2a, 2b) with a basic heterocyclic-aldehyde compound and an optically active amine in the presence of a base; and b) separating the compound of Formula (2a) from the product of step a) by acid extraction. The compound of Formula (2a) may be produced with an enantiomeric excess of 98%. Compounds of Formula (2a) are useful intermediates in a process to prepare a bicyclic ?-amino tetrazole derivative of Formula (I) which finds utility in treating neuropathic pain and disorders of the central nervous system.Type: GrantFiled: February 2, 2016Date of Patent: December 11, 2018Assignee: Novassay S.A.Inventors: Rhonan Lee Ford, Premji Meghani
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Patent number: 10100028Abstract: Methods of synthesizing prostaglandins, prostaglandin analogs and their synthetic intermediates are described. The methods can comprise metal-catalyzed metathesis reactions. Also provided are synthetic intermediates that can be used in the synthesis of the prostaglandins and prostaglandin analogs.Type: GrantFiled: September 30, 2014Date of Patent: October 16, 2018Assignee: Patheon API Services Inc.Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Denis Viktorovich Arefyev
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Publication number: 20150141669Abstract: Provided are a fluorine-containing amino acid prodrug represented by general formula (I) that makes a fluorine-containing amino acid which is a group 2 metabotropic glutamate receptor agonist into a prodrug, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 31, 2013Publication date: May 21, 2015Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Takashi Hashihayata, Norikazu Otake, Naoki Miyakoshi, Kazunari Sakagami
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Publication number: 20150125892Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.Type: ApplicationFiled: October 10, 2014Publication date: May 7, 2015Applicant: SynAffix B.V.Inventors: Floris Louis VAN DELFT, Floris Petrus Johannes Theodorus Rutjes, Frederik Jan Dommerholt
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Publication number: 20150045574Abstract: The present invention is directed to compounds, intermediates and methods for making valerenic acid and its derivatives as well as the use of such compounds as GABAA receptor ligands.Type: ApplicationFiled: July 18, 2014Publication date: February 12, 2015Applicant: Valericon GmbHInventors: Johann Mulzer, Jurgen Ramharter, Steffen Hering, Sophia Khom
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Publication number: 20150011749Abstract: Metal-accumulating plants for preparing compositions including a metal catalyst derived from the plants. The composition is substantially devoid of organic matter. Also, carrying out chemical reactions with the compositions prepared from metal-accumulating plants.Type: ApplicationFiled: March 5, 2013Publication date: January 8, 2015Applicants: UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Claude Grison, Vincent Escande
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Publication number: 20140256782Abstract: 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: ApplicationFiled: October 19, 2012Publication date: September 11, 2014Applicant: Bikam Pharmaceuticals, Inc.Inventors: David S. Garvey, Gregory J. Larosa, Jeremy R. Greenwood, Leah L. Frye, Tan Quach, Jamie B. Cote, Judd Berman
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Publication number: 20140235665Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.Type: ApplicationFiled: April 30, 2014Publication date: August 21, 2014Applicant: SUCAMPO AGInventor: Ryuji UENO
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Patent number: 8809395Abstract: The present invention is directed to compounds, intermediates and methods for making valerenic acid and its derivatives as well as the use of such compounds as GABAA receptor ligands.Type: GrantFiled: January 22, 2010Date of Patent: August 19, 2014Assignee: Valericon GmbHInventors: Johann Mulzer, Jürgen Ramharter, Steffen Hering, Sophia Khom
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Patent number: 8742161Abstract: There is provided a process for producing a bicyclo [3.1.0] hexane derivative represented by the formula (I) and a salt thereof including; causing an enzyme to act on an optically inactive compound represented by the formula (II) causing an asymmetric acylation reaction and a highly-stereoselective conversion to an optically active compound represented by the formula (III); and converting the compound represented by the formula (III) to the compound represented by the formula (I) or a salt thereof.Type: GrantFiled: November 18, 2010Date of Patent: June 3, 2014Assignee: Taisho Pharmaceutical Co., LtdInventor: Joji Sasaki
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Publication number: 20140114086Abstract: In one aspect, methods of synthesizing clinprost, isocarbacyclin and analogs thereof are described herein which, in some embodiments, permit an abbreviated synthetic pathway in comparison to one or more prior synthetic methods. By providing a compact synthetic scheme, methods described herein can reduce cost, waste and time of clinprost and isocarbacyclin synthesis while facilitating the development and investigation of analogs of these compounds.Type: ApplicationFiled: October 21, 2013Publication date: April 24, 2014Inventor: Mitchell Croatt
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Publication number: 20140100384Abstract: Provided is a process for making non-phthalate plasticizers, by acylating an aromatic compound with a succinic anhydride to form a keto-acid, and then esterifying the keto-acid with C4-C13 OXO-alcohols to form a plasticizer compound. The aromatic rings of the aromatic compound may also be optionally hydrogenated.Type: ApplicationFiled: December 9, 2013Publication date: April 10, 2014Applicant: ExxonMobil Research and Engineering CompanyInventors: Jihad Mohammed Dakka, Edmund John Mozeleski, Lisa Saunders Baugh, Colle Karla Schall, Allen David Godwin, Diana S. Smirnova, Jorg Friedrich Wilhelm Weber, Stephen Zushma
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Publication number: 20140051577Abstract: The invention relates to substituted 5-(bicyclo[4.1.0]hept-3-en-2-yl)penta-2,4-dienes and 5-(bicyclo[4.1.0]hept-3-en-2-yl)pent-2-ene-4-ines of the formula (I) and salts thereof, where the radicals R1, R2, R3, R4, R5, [X—Y] and Q are each as defined in the description, to processes for preparation thereof and to the use thereof for enhancing stress tolerance in plants with respect to abiotic stress, and/or for increasing plant yield.Type: ApplicationFiled: March 28, 2012Publication date: February 20, 2014Inventors: Jens Frackenpohl, Thomas Müller, Ines Heinemann, Pascal Von Koskull-Döring, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Martin Jeffrey Hills
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Patent number: 8585924Abstract: A liquid crystal compound having a high stability to heat, light or the like, a high clearing point, a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large negative dielectric anisotropy, a suitable elastic constant and an excellent compatibility with other liquid crystal compounds, and a liquid crystal composition including this compound, and a liquid crystal display device containing this composition. A compound represented by formula (1-1). In the formula, for example, R1 and R2 are alkyl having 1 to 10 carbons or alkoxy having 1 to 9 carbons; ring A1 and ring A2 are 1,4-cyclohexylene, 1,4-phenylene or 2,3-difluoro-1,4-phenylene; Z1 and Z2 are a single bond or —(CH2)2—; >W1—W2— and >W4—W3— are >CH—CH2— or >C?CH—; and m and n are 0, 1 or 2, and the sum of m and n is 1 or 2.Type: GrantFiled: May 10, 2012Date of Patent: November 19, 2013Assignees: JNC Corporation, JNC Petrochemical CorporationInventor: Masahide Kobayashi
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Publication number: 20130274329Abstract: Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.Type: ApplicationFiled: August 11, 2011Publication date: October 17, 2013Applicant: NABRIVA THERAPEUTICS AGInventors: Rosemarie Riedl, Klaus Thirring, Werner Heilmayer
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Publication number: 20130261296Abstract: Catalytic complexes including a metal atom having anionic ligands, at least one nucleophilic carbene ligand, and an alkylidene, vinylidene, or allenylidene ligand. The complexes are highly stable to air, moisture and thermal degradation. The complexes are designed to efficiently carry out a variety of olefin metathesis reactions.Type: ApplicationFiled: January 25, 2013Publication date: October 3, 2013Inventors: Steven P. NOLAN, Jinkun HUANG
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Patent number: 8324425Abstract: Methods for producing compounds having activity as an ?2? ligand are provided.Type: GrantFiled: September 23, 2011Date of Patent: December 4, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Yutaka Kitagawa, Makoto Imai
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Publication number: 20120286200Abstract: A liquid crystal compound having a high stability to heat, light or the like, a high clearing point, a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large negative dielectric anisotropy, a suitable elastic constant and an excellent compatibility with other liquid crystal compounds, and a liquid crystal composition including this compound, and a liquid crystal display device containing this composition. A compound represented by formula (1-1). In the formula, for example, R1 and R2 are alkyl having 1 to 10 carbons or alkoxy having 1 to 9 carbons; ring A1 and ring A2 are 1,4-cyclohexylene, 1,4-phenylene or 2,3-difluoro-1,4-phenylene; Z1 and Z2 are a single bond or —(CH2)2—; >W1—W2— and >W4—W3— are >CH—CH2— or >C?CH—; and m and n are 0, 1 or 2, and the sum of m and n is 1 or 2.Type: ApplicationFiled: May 10, 2012Publication date: November 15, 2012Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATIONInventor: Masahide KOBAYASHI
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Publication number: 20120270934Abstract: This invention relates to novel prostacyclin derivatives and acceptable salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors.Type: ApplicationFiled: July 2, 2010Publication date: October 25, 2012Inventors: Craig E. Masse, Scott L. Harbeson, Roger D. Tung
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Publication number: 20120238763Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.Type: ApplicationFiled: November 18, 2010Publication date: September 20, 2012Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Noriaki Murase, Toshihito Kumagai, Hisaya Wada, Hisahide Tanimoto, Koumei Ohta, Yoshihiro Kimura
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Publication number: 20120232304Abstract: There is provided a process for producing a bicyclo [3.1.0] hexane derivative represented by the formula (I) and a salt thereof including; causing an enzyme to act on an optically inactive compound represented by the formula (II) causing an asymmetric acylation reaction and a highly-stereoselective conversion to an optically active compound represented by the formula (III); and converting the compound represented by the formula (III) to the compound represented by the formula (I) or a salt thereof.Type: ApplicationFiled: November 18, 2010Publication date: September 13, 2012Applicant: TAISHO PHARMACEUTICAL CO., LTDInventor: Joji Sasaki
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Publication number: 20120071685Abstract: Methods for producing compounds having activity as an ?2? ligand are provided.Type: ApplicationFiled: September 23, 2011Publication date: March 22, 2012Applicant: Daiichi Sankyo Company, LimitedInventors: Yutaka Kitagawa, Makoto Imai
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Publication number: 20120022283Abstract: The present invention is directed to compounds, intermediates and methods for making valerenic acid and its derivatives as well as the use of such compounds as GABAA receptor ligands.Type: ApplicationFiled: January 22, 2010Publication date: January 26, 2012Applicant: Valericon GMBHInventors: Johann Mulzer, Jürgen Ramharter, Steffen Hering, Sophia Khom
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Patent number: 8076502Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.Type: GrantFiled: July 30, 2010Date of Patent: December 13, 2011Assignee: Taisho Pharmaceuticals Co., Ltd.Inventors: Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Atsuro Nakazato
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Publication number: 20110269830Abstract: The present invention relates to a complex made up of at least one molecule of statin or a derivative thereof, covalently bonded to at least one hydrocarbon radical including at least 18 carbon atoms and containing at least one 2-methyl-buta-2-ene unit, to nanoparticles of such a complex, and to a method for preparing same, said complex and/or said nanoparticles optionally being in the form of a lyophilisate. The present invention also relates to a pharmaceutical composition including at least one complex and/or nanoparticles such as previously defined. The invention finally relates to said complex and/or to said nanoparticles for the treatment and/or prevention of hyperlipemia and hypercholesterolemia.Type: ApplicationFiled: October 28, 2009Publication date: November 3, 2011Inventors: Patrick Couvreur, Didier Desmaele, Fat'ma Zouhiri, Reddy Harivardhan Lakkireddy
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Patent number: 8043789Abstract: A photosensitive compound whose size is smaller than conventional polymer for photoresist, and which has well-defined (uniform) structure, and a photoresist composition including the same are disclosed. The photosensitive compound represented by the following formula. Also, the present invention provides a photoresist composition comprising 1 to 85 wt % (weight %) of the photosensitive compound; 0.05 to 15 weight parts of a photo-acid generator with respect to 100 weight parts of the photosensitive compound; and 10 to 5000 weight parts of an organic solvent. In the formula, n is 0 or 1, x is 1, 2, 3, 4 or 5, y is 2, 3, 4, 5 or 6, z is 0, 1, 2, 3 or 4, R, R? and R? are independently hydrocarbon group of 1 to 30 carbon atoms, preferably 2 to 20 carbon atoms, and R?? is a hydrogen atom or hydrocarbon group of 1 to 30 carbon atoms, preferably 2 to 20 carbon atoms.Type: GrantFiled: December 17, 2008Date of Patent: October 25, 2011Assignee: Dongjin Semichem Co., Ltd.Inventors: Jae-Woo Lee, Min-Ja Yoo, Jun-Gyeong Lee, Young-Bae Lim, Jae-Hyun Kim
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Publication number: 20110230669Abstract: This application relates to a process for the production of (2R)-dihydroartemisinic acid or (2R)-dihydroartemisinic acid esters from artemisinic acid or artemisinic acid esters, respectively, by diimine hydrogenation of the exocyclic CC-double bond, and use of said process in the production of the antimalarial drug artemisinin.Type: ApplicationFiled: September 10, 2010Publication date: September 22, 2011Inventors: VOLKER KRAFT, GERHARD KRETZSCHMAR, KAI ROSSEN
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Patent number: 7960579Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.Type: GrantFiled: June 25, 2004Date of Patent: June 14, 2011Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Atsuro Nakazato
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Publication number: 20110130454Abstract: Prodrugs of alpha-2-delta ligands, pharmaceutical compositions of prodrugs of alpha-2-delta ligands, methods of making prodrugs of alpha-2-delta ligands, and methods of using prodrugs of alpha-2-delta ligands and pharmaceutical compositions of prodrugs of alpha-2-delta ligands to treat various diseases are disclosed.Type: ApplicationFiled: November 24, 2010Publication date: June 2, 2011Applicant: XenoPort, Inc.Inventors: Mark A. Gallop, David J. Wustrow
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Publication number: 20110065934Abstract: Production of a bicyclo[3.1.0]hexane derivative, useful as a metabotropic glutamate receptor modulator, becomes possible by a production method that includes converting a compound represented by Formula (II) into a compound represented by Formula (III) by reaction with an acyl group donor in the presence of a microorganism-derived enzyme, without using an expensive optically active trans hydroxy ester as a starting material and without employing a fluorination reaction requiring an ultralow temperature reaction. Furthermore, since asymmetric synthesis can be carried out in a stage closer to the final product, the production method is useful as a production method that can mass produce a bicyclo[3.1.0]hexane derivative.Type: ApplicationFiled: November 19, 2010Publication date: March 17, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Mitsuaki HIROTSUKA, Joji SASAKI, Hiroaki KAMIYAMA, Motoko OSHIDA, Takaaki ISHII
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Publication number: 20100298367Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: March 4, 2009Publication date: November 25, 2010Inventors: Sean P. Brown, Paul J. Dransfield, Jonathan Houze, Todd J. Kohn, Jiwen Liu, Julio Medina, Vatee Pattaropong, Wang Shen, Marc Vimolratana, Yingcai Wang, Ming Yu, Liusheng Zhu
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Publication number: 20100264368Abstract: Liquid Crystal Molecules Comprising Hydroazulene Structures Compounds of formula (I); R1i-A1i-(Z2i-A2i)m-(Z3i-A3i)n-(Z4i-A4i)o-R2i (i) wherein at least one of the divalent groups Ai is derived from at least partially hydrogenated azulene, R1i and R2i being hydrogen, an optionally substituted alkyl or alkylene residue, R2i also standing for —CN, —N?C?S, —F, —Cl, —SF5, —CF3, —CHF2, CH2F—O—CF3, —O—CHF2, —O—CH2F, —O—CF2—CF2H, or —O—C2F5, A1i, A2i, A3i and A4i being partially or completely hydrogenated 2,6-azulene, trans-1,4-cyclohexylene, 1,4-cyclohexenylene, 1,4-phenylene, 2-fluoro-1,4-phenylene, 3-fluoro-14-phenylene, 2,3- and 2,6-difluoro-1,4-phenylene, and 3,5-difluoro-1,4-phenylene, pyrimidine-2,5-diyl, and 1,4-dioxane-2,5-diyl, Z1i, Z2i, Z3i and Z4i being a single bond, —CH2—CH2—, —CF2—CF2—, an ester bond —CO—O—, trans and —CF2—O—, m, n and 0 being independently 0, 1, or 2, liquid crystal media comprising these compounds and liquid crystal displays made with mixtures comprising the novel compounds.Type: ApplicationFiled: June 19, 2006Publication date: October 21, 2010Applicant: TETRAGON-CHEMIE AGInventors: Ludwig Pohl, Henning Hopf, Zakir Hussain
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Patent number: 7816476Abstract: Cyclopropyl acrylate of general formula (1), constitutional and stereoisomers thereof and their mixtures in which A is selected from:Type: GrantFiled: August 9, 2005Date of Patent: October 19, 2010Assignee: Ivoclar Vivadent AGInventors: Norbert Moszner, Frank Zeuner, Urs-Karl Fischer, Volker M. Rheinberger, Armin de Meijere, Viktor Bahutski
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Patent number: 7659358Abstract: A process for preparing polymers containing polyortho ester groups and optionally NCO groups by reacting A) and B) where A) is a polyortho ester containing at least one isocyanate-reactive group prepared by reacting at least one or more acyclic ortho esters with low molecular weight polyols having a functionality of 4-8 and a number-average molecular weight of 80-500 g/mol and B) is least one polyisocyanate. The polymers obtained from the process can be used to produce coatings, adhesive bonds and/or seals. The coating compositions can include one or more of the above-described polymers, optionally polyisocyanates, catalysts, and optionally auxiliaries and additives and can be used to coat substrates.Type: GrantFiled: January 18, 2005Date of Patent: February 9, 2010Assignee: Bayer MaterialScience AGInventors: Hanns-Peter Müller, Meike Niesten, Jörg Schmitz, Holger Mundstock
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Patent number: 7655695Abstract: Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.Type: GrantFiled: August 3, 2006Date of Patent: February 2, 2010Assignee: The Regents of The University of CaliforniaInventors: Trevor C. McMorris, Michael J. Kelner
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Publication number: 20090306408Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.Type: ApplicationFiled: July 29, 2009Publication date: December 10, 2009Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Akito YASUHARA, Kazunari Sakagami, Hiroshi Ohta, Atsuro Nakazato
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Patent number: 7534475Abstract: 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: GrantFiled: March 8, 2005Date of Patent: May 19, 2009Assignee: Fujifilm CorporationInventors: Hideyuki Nishikawa, Ryo Hamasaki, Atsuhiro Ohkawa
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Patent number: 7501222Abstract: A polymer including a monomer represented by the following Formula and a photoresist composition including the same are disclosed. The polymer and photoresist composition can improve the resolution and the process margin due to the low activation energy of the deprotection reaction of the alcohol ester group including saturated cyclic hydrocarbyl group, and also can produce fine photoresist patterns because they have a stable PEB(Post Exposure Baking) temperature sensitivity, and further, can improve the focus depth margin and the line edge roughness of the resist layer. In the above Formula, R* is a hydrogen or methyl group, R1 is saturated hydrocarbyl group of 1 to 5 carbon atoms, R is mono-cyclic or multi-cyclic homo or hetero saturated hydrocarbyl group of 3 to 50 carbon atoms, and n is an integer of at least 2.Type: GrantFiled: June 21, 2006Date of Patent: March 10, 2009Assignee: Dongjin Semichem Co., Ltd.Inventors: Jung-Youl Lee, Jae-Woo Lee, Jae-Hyun Kim
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Patent number: 7425644Abstract: The present invention provides pure pravastatin compositions and pure compactin compositions, and methods for the preparation thereof.Type: GrantFiled: November 23, 2004Date of Patent: September 16, 2008Assignee: TEVA Gyógyszergyár Zártkörűen Működő RészvénytársaságInventors: Vilmos Keri, Istvan Melczer
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Patent number: 7157594Abstract: An antidepressant comprising, as an active ingredient, a compound having an antagonistic effect on group II metabotropic glutamate receptors, as well as a 2-amino-3-alkoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative of Formula [I]: [wherein R1 and R2, which may be the same or different, each represent a hydroxyl group, a C1-10 alkoxy group, etc.; R3 represents a C1-10 acyl group, a C1-6 alkoxy-C1-6 acyl group, etc.; and R4 and R5, which may be the same or different, each represent a hydrogen atom, a C1-10 alkyl group, etc.] or a pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: December 26, 2002Date of Patent: January 2, 2007Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Shigeyuki Chaki, Kazunari Sakagami, Ryoko Dean, Hiroshi Ohta, Shiho Hirota, Akito Yasuhara
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Patent number: 7078558Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, fluvastatin and cervastatin and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to an Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor, or Penicillium genus, some are obtained by treating the fermentation products using the methods of chemical synthesis (simvastatin) or they are the products of total chemical synthesis (fluvastatin, atorvastatin and cervastatin). The present invention relates to a crystalline form of the sodium salt of pravastatin, which is known by the chemical name 1-naphthaleneheptanoic acid, 1,2,6,7,8,8a-hexahydro-?,?,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-, mono sodium salt, which is useful as a pharmaceutical substance.Type: GrantFiled: August 4, 2000Date of Patent: July 18, 2006Assignee: Lek Pharmaceutical and Chemical Company D.D.Inventor: Zlatko Pflaum
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Patent number: 7071359Abstract: A compound represented by the Formula below, and an agent for the remedy of neural damage having the said compound as the active ingredient. [Here, G represents G1 shown below R4 represents, hydrogen atoms and acyl groups, W represents single bonds and alkylenes, m represents 0 or 1, R5 and R6 represent hydrogen atoms, aliphatic hydrocarbon groups, alicyclic hydrocarbon groups, aromatic hydrocarbon groups and heterocyclic groups, and R7 represents hydrogen atoms, acyl groups and alkoxycarbonyl groups. A2 represents, single bonds, —O—, —NR3—, and —S(?O)n—, A1 and A3 represent single bonds, aliphatic hydrocarbon groups, alicyclic hydrocarbon groups, heterocyclic groups and phenylene groups, and A4 represents single bonds, carbonyl groups and aliphatic hydrocarbon groups. R1 and R2 represent hydrogen atoms, alkyl groups, cycloalkyl groups, phenyl groups and heterocyclic groups. The previously mentioned functional groups may be substituted.Type: GrantFiled: August 7, 2000Date of Patent: July 4, 2006Assignee: Teijin LimitedInventors: Satoshi Sugiura, Takaharu Tsutsumi, Yorimasa Suwa, Takami Arai, Katsutoshi Sakurai, Noboru Yoshioka, Akira Tanokura, Jun Suzuki
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Patent number: 7018818Abstract: The invention presents compounds of formula (I), where R represents H or a suitable carboxylic acid protecting group, which are intermediates in the preparation of therapeutic fused bicyclic amino acids.Type: GrantFiled: October 2, 2003Date of Patent: March 28, 2006Assignee: Pfizer Inc.Inventors: Iain Robert Gladwell, Alan John Pettman
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Patent number: 6965026Abstract: The subject invention pertains to nanoscale polyhedron-shaped molecules having molecular building blocks connected at their vertices. The subject invention also concerns methods of producing nanoscale polyhedrons utilizing a self-assembly reaction. The resultant molecules are faceted polyhedra that are porous, chemically robust, contain chemically accessible sites on their facets, and which are neutral and soluble in common laboratory solvents. The nanoscale polyhedrons can exhibit additional desirable physical properties, such as ferromagnetic properties.Type: GrantFiled: February 25, 2002Date of Patent: November 15, 2005Assignee: University of South FloridaInventors: Michael J. Zaworotko, Brian Moulton
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Patent number: 6936731Abstract: The present invention provides pravastatin sodium substantially free of pravastatin lactone and epiprava, the C-6 epimer of pravastatin. The present invention further provides a novel process for recovering pravastatin sodium from a fermentation broth in such high purity. The process includes the stages of forming an solution of the compound by extraction, obtaining an ammonium salt of pravastatin from the solution, purifying the ammonium salt of the compound and transposing the salt of the compound to pravastatin sodium.Type: GrantFiled: October 5, 2001Date of Patent: August 30, 2005Assignee: TEVA Gyógyszergyár RészvénytársaságInventors: Vilmos Keri, Lajos Deak, Ilona Forgacs, Csaba Szabo, Arvai Edit Nagyne
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Patent number: 6875867Abstract: A process is provided for preparing chiral diol sulfones of the structure where R3 is preferably where R4a is preferably aryl such as phenyl, and R1a is preferably alkyl such as t-butyl, which are intermediates used in preparing HMG CoA reductase inhibitors.Type: GrantFiled: May 30, 2002Date of Patent: April 5, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Paul R. Brodfuehrer, Thomas R. Sattelberg, Joydeep Kant, Xinhua Qian
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Patent number: 6770676Abstract: The present invention relates to 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives represented by the formula: the pharmaceutically acceptable salts thereof, or the hydrates thereof. The compounds of the present invention are useful as a medicament, and in particular, are useful as modulators acting on group 2 metabotropic glutamate receptors, having effects for treating and/or preventing psychiatric disorders such as schizophrenia, anxiety and its associated diseases, depression, bipolar disorder, and epilepsy; and/or neurological diseases such as drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, dyskinesia associated with muscular stiffness, cerebral ischemia, cerebral failure, myelopathy, and head trauma.Type: GrantFiled: December 6, 2002Date of Patent: August 3, 2004Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kosuke Kanuma, Kazunari Sakagami
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Patent number: 6756507Abstract: A process for the preparation of sodium salts of statins, namely Compactin, Lovastatin and Pravastatin.Type: GrantFiled: September 4, 2002Date of Patent: June 29, 2004Assignee: Ranbaxy Laboratories LimitedInventors: Pardeep Narula, Srinivasan Raman, M. Lakshmi Kumar, Parveen Kumar
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Patent number: 6746728Abstract: A tetrahydronaphthalene derivative represented by the general formula (I) and a liquid crystal composition containing the same. A compound represented by the general formula (I) shows superior liquid crystallinity and co-solubility with conventional liquid crystal compounds and compositions. Furthermore, addition of such a compound enables the threshold voltage to be significantly reduced with almost no deleterious effect on the responsiveness. In addition, a compound of the present invention can also be easily produced industrially, is colorless, and is chemically stable. Consequently, liquid crystal compositions containing such a compound are extremely useful as liquid crystals, and are particularly suitable for liquid crystal displays requiring a wide operating temperature range, low voltage driving and a high response speed.Type: GrantFiled: December 28, 2001Date of Patent: June 8, 2004Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Tetsuo Kusumoto, Yoshitaka Saito, Makoto Negishi, Yutaka Nagashima, Sadao Takehara, Haruyoshi Takatsu, Gerwald Grahe, Rainer Bruno Frings, Cornelia Pithart
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Patent number: 6740775Abstract: A crystalline form of the sodium salt of pravastatin, which is known by the chemical name 1-naphthaleneheptanoic acid, 1,2,6,7,8,8a-hexahydro-&bgr;, &dgr;,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-, mono sodium salt, which is useful as a pharmaceutical substance. A method for its preparation and isolation, a pharmaceutical formulation containing the sodium salt of pravastatin in the crystalline form and a pharmaceutically acceptable carrier, and the pharmaceutical method of treatment are also disclosed.Type: GrantFiled: April 4, 2003Date of Patent: May 25, 2004Assignee: LEK Pharmaceuticals d.d.Inventor: Zlatko Pflaum