Ether Oxygen Is Part Of The Chain Patents (Class 564/346)
  • Publication number: 20150018500
    Abstract: An oligomeric condensation product can be obtained from at least one (hydroxymethyl)phenol of general formula (I), in which R1 is hydrogen or —CH3, R2 is —CH2OH, and R3 is hydrogen or —CH3, at least one polyamine, and optionally at least one phenol compound having two centres reactive by means of a reaction with the methylol groups of the (hydroxymethyl)phenol.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 15, 2015
    Applicant: SIKA TECHNOLOGY AG
    Inventors: Ulrich Gerber, Jürgen Finter
  • Publication number: 20140039184
    Abstract: The present disclosure relates to a compound of formula (1): where R1 through R8, which can be identical or different from each other, each are selected from of the group comprising hydrogen and the radical —(CH2)k—X, where k is a whole number from 1 to 20 and where X is an organic radical comprising a) at least one neutral, protonizable nitrogen atom and/or b) at least one positively charged nitrogen atom, under the provision that at least 1 radical R1 through R8 is not hydrogen. The invention further relates to the production and use of said compound.
    Type: Application
    Filed: February 23, 2012
    Publication date: February 6, 2014
    Inventors: Wolfgang Bäumler, Ariane Felgenträger, Karin Lehner, Tim Maisch, Johannes Regensburger, Francesco Santarelli, Andreas Spath
  • Publication number: 20140031549
    Abstract: This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
    Type: Application
    Filed: October 1, 2013
    Publication date: January 30, 2014
    Applicant: OPKO Health, Inc.
    Inventors: George G. Wu, Gerald Werne, Xiaoyong Fu, Robert K. Orr, Frank Xing Chen, Jian Cui, Victoria M. Sprague, Fucheng Zhang, Ji Xie, Liansheng Zeng, Louis Peter Castellanos, Yuyin Chen, Marc Poirier, Ingrid Mergelsberg
  • Publication number: 20130203717
    Abstract: A process for reducing the particle size of an active pharmaceutical ingredient (API) while maintaining its polymorphic form, comprises the step of processing the active pharmaceutical ingredient by cavitation at elevated pressure. The process preferably comprises the step of isolating the processed active ingredient in the form of powder, wherein the isolation step comprises filtration or spray drying. Particles produced by the process of the invention typically have a span value of less than 2.5.
    Type: Application
    Filed: April 21, 2011
    Publication date: August 8, 2013
    Applicant: HOVIONE INTER LTD
    Inventors: Marco Gil, Constanca Cacela, Ricardo Mendonca, Filipe Gaspar
  • Patent number: 8501659
    Abstract: A process for the preparation of N-arylamine compounds, the process including: reacting a compound having an amino group with an acylating compound in the presence of a base and a transition metal catalyst under reaction conditions effective to form an N-arylamine compound; wherein the transition metal catalyst comprises a complex of a Group 8-10 metal and at least one chelating ligand comprising (R)-(?)-1-[(S)-2-dicyclohexylphosphino]-ferrocenyl]ethyldi-t-butylphosphine.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: August 6, 2013
    Assignee: Univation Technologies, LLC
    Inventor: Adam M. Johns
  • Publication number: 20130178653
    Abstract: The present invention describes intermediate(s), pre-cursor(s), for the preparation of radialabelled choline analogs to be used as radiotracers for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of diseases.
    Type: Application
    Filed: September 20, 2011
    Publication date: July 11, 2013
    Applicants: IMPERIAL COLLEGE, GE HEALTHCARE LIMITED
    Inventors: Eric Ofori Aboagye, Edward George Robins, Graham Smith, Yongjun Zhao
  • Patent number: 8450528
    Abstract: Process for the preparation of 2,2-difluoroethylamine of the formula (I) CHF2CH2NH2??(I) comprising the stages (i) and (ii): stage (i): reaction of 2,2-difluoro-1-haloethane of the general formula (II) CHF2—CH2Hal??(II), with a benzylamine compound of the formula (III) in the presence of an acid scavenger, in which, in formula (II), Hal is chlorine, bromine or iodine, and, in the formulae (III), R1 is hydrogen or C1-C12-alkyl, and R2 is hydrogen, halogen, C1-C12-alkyl or C1-C6-alkoxy; stage (ii): catalytic hydrogenation of the N-benzyl-2,2-difluoroethanamine compound obtained in the stage (i) to give 2,2-difluoroethylamine of the formula (I) or a salt thereof.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: May 28, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Norbert Lui, Jens-Dietmar Heinrich, Christian Funke, Günter Schlegel, Thomas Norbert Müller
  • Publication number: 20120220665
    Abstract: This document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake. For example, compounds, methods for synthesizing compounds, and methods for inhibiting neurotransmitter reuptake are provided.
    Type: Application
    Filed: November 2, 2010
    Publication date: August 30, 2012
    Applicant: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH
    Inventors: Elliott Richelson, Abdul H. Fauq, Dola Sinha
  • Patent number: 8242177
    Abstract: The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the BETA2 adrenergic receptor.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: August 14, 2012
    Assignee: Almirall, S.A.
    Inventors: Carlos Puig Duran, Maria Isabel Crespo Crespo, Julio Cesar Castro Palomino Laria, Silvia Gual Roig, Eloisa Navarro Romero
  • Patent number: 8158827
    Abstract: Disclosed are cationic lipid compounds and compositions of lipid aggregates for delivery of macromolecules and other compounds into cells. The compounds can be used alone or in combination with other compounds to prepare liposomes and other lipid aggregates suitable for transfection or delivery of compounds to target cells, either in vitro or in vivo. The compounds are preferably polycationic and preferably form highly stable complexes with various anionic macromolecules, particularly polyanions such as nucleic acids. These compounds have the property, when dispersed in water, of forming lipid aggregates which associate strongly, via their cationic portion, with polyanions. Also disclosed are intermediates for preparing the compound and compositions of the invention and methods of using the compounds to introduce other compounds into cells.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: April 17, 2012
    Assignee: Life Technologies Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Publication number: 20110251165
    Abstract: The present invention provides a compound of formula (I) wherein: R1 is a group selected from —CH2OH, —NHC(O)H and R2 is a hydrogen atom; or R1 together with R2 form the group —NH—C(O)—CH?CH— wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2; R3 is selected from hydrogen and halogen atoms or groups selected from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is selected from hydrogen atoms, halogen atoms and C1-4alkyl groups; R5 is a C1-4alkyl group or C3-8 cycloalkyl; R6 is independently selected from hydrogen atoms and C1-4alkyl groups; n, p and q are independently 0, 1, 2, 3 or 4; m and s are independently 0, 1, 2 or 3; r is 0, 1 or 2; with the provisos that at least one of m and r is not 0; the sum n+n+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13; the sum q+r+s is 2, 3, 4, 5 or 6 or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof.
    Type: Application
    Filed: April 26, 2011
    Publication date: October 13, 2011
    Inventors: Carlos PUIG DURAN, Maria Isabel Crespo Crespo, Julio Cesar Castro Palomino Laria, Silvia Gual Roig, Eloisa Navarro Romero
  • Publication number: 20110207599
    Abstract: A process for the preparation of N-arylamine compounds, the process including: reacting a compound having an amino group with an acylating compound in the presence of a base and a transition metal catalyst under reaction conditions effective to form an N-arylamine compound; wherein the transition metal catalyst comprises a complex of a Group 8-10 metal and at least one chelating ligand comprising (R)-(?)-1-[(S)-2-dicyclohexylphosphino]-ferrocenyl]ethyldi-t-butylphosphine.
    Type: Application
    Filed: October 21, 2009
    Publication date: August 25, 2011
    Applicant: UNIVATION TECHNOLOGIES, LLC
    Inventor: Adam M. Johns
  • Publication number: 20110118358
    Abstract: The present application describes deuterium-enriched salmeterol, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: November 11, 2010
    Publication date: May 19, 2011
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 7807854
    Abstract: To provide a medicament which efficiently expresses an immunosuppressive agent or an anti-inflammatory agent and reduces expression of side effect. A medicament includes diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure having an activity of reducing lymphocytes circulating peripherally, in combination with an immunosuppressive agent and/or an anti-inflammatory agent.
    Type: Grant
    Filed: December 31, 2009
    Date of Patent: October 5, 2010
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Shinji Kudou, Kazuhiko Kuriyama, Tokutarou Yasue
  • Publication number: 20100247439
    Abstract: Provided are dendritic nano-antioxidant compounds according to Formula I, which may further comprise active agents covalently or non-covalently attached. Further provided are compositions comprising the disclosed compounds. Also disclosed are cosmetic compositions and dietary supplements comprising the compounds according to Formula I. The invention additionally provides methods of reducing free radicals or oxidative stress in a cell, a method of treating a subject, and a method of treating a condition comprising administering the compounds according to Formula I.
    Type: Application
    Filed: March 29, 2010
    Publication date: September 30, 2010
    Inventor: Choon Young Lee
  • Patent number: 7781617
    Abstract: A medicine which effectively functions as an immunosuppressant or anti-inflammatory agent and is effective in diminishing the occurrence of side effects. The medicine comprises a combination of: a diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure and having the function of diminishing lymphocytes circulating through the periphery; and an immunosuppressant and/or an anti-inflammatory agent.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: August 24, 2010
    Assignee: Kyorin Pharmaceutical Co., Ltd
    Inventors: Shinji Kudou, Kazuhiko Kuriyama, Tokutarou Yasue
  • Patent number: 7763752
    Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects: .
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: July 27, 2010
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Kiyoaki Tanaka, Kazuhiko Kuriyama
  • Publication number: 20100174090
    Abstract: The present application relates to novel methods for the preparation of primary, secondary and tertiary carbinamine compounds, particularly the preparation of compounds of formulae I, IV and VI, from a carbonyl compound of formula II in the presence of ammonia or an ammonium equivalent of the formula NH4+X?, by way of allylation, crotylation, arylation, reductive amination and catalytic hydrogenation.
    Type: Application
    Filed: March 28, 2008
    Publication date: July 8, 2010
    Inventors: Avinash N. Thadani, Bhartesh Dhudshia
  • Publication number: 20100137592
    Abstract: A process for the preparation of famciclovir a compound of Formula (I) and its intermediates.
    Type: Application
    Filed: June 2, 2008
    Publication date: June 3, 2010
    Inventors: Asif Parvez Sayyed, Murali Krishna Ankaraju, Ravinder Reddy Vennapureddy, Shankar Rama, Ramesh Dandala, Sivakumaran Meenakshisunderam
  • Publication number: 20100009950
    Abstract: The present invention relates to new substituted ethanolamine adrenergic receptor modulators, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 29, 2009
    Publication date: January 14, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Patent number: 7601872
    Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and w
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: October 13, 2009
    Assignee: Life Technologies Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Publication number: 20090042933
    Abstract: A compound of formula (I) or a pharmaceutically-acceptable salt, solvate or stereoisomer thereof wherein R1 is a group chosen from —CH2OH and —NHC(O)H; R2 is a hydrogen atom or R1 together with R2 form the group —NH—C(O)—CH?CH—, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2; R3 is chosen from a hydrogen atom, a halogen atom and groups chosen from —SO—R5, —SO2—R5, —NH—CO—NH2, —CO—NH2, hydantoino, C1-4alkyl, C1-4alkoxy and —SO2NR5R6; R4 is chosen from a hydrogen atom, a halogen atom and a C1-4 alkyl group; R5 is chosen from a C1-4 alkyl group and a C3-8 cycloalkyl group; R6 is independently chosen from a hydrogen atom and a C1-4 alkyl group; n, p and q are independently 0, 1, 2, 3 or 4; m and s are independently 0, 1, 2 or 3; and r is 0, 1 or 2 with the provisos that at least one of m and r is not 0, the sum n+m+p+q+r+s is 7, 8, 9, 10, 11, 12 or 13, and the sum q+r+s is 2, 3, 4, 5 or 6.
    Type: Application
    Filed: May 17, 2006
    Publication date: February 12, 2009
    Inventors: Carlos Puig Duran, Maria Isabel Crespo Crespo, Julio Cesar Castro Palomino Laria, Silvia Gual Roig, Eloisa Navarro Romero
  • Patent number: 7482491
    Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects:
    Type: Grant
    Filed: September 16, 2003
    Date of Patent: January 27, 2009
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Kiyoaki Tanaka, Kazuhiko Kuriyama
  • Patent number: 7482489
    Abstract: Provided are processes for the preparation of (R)-SLB.D-DBTA salt and levalbuterol hydrochloride. Also provided are levalbuterol hydrochloride degradation products and processes for preparing them. Pharmaceutical compositions comprising at least one levalbuterol hydrochloride of the invention and at least one pharmaceutically-acceptable excipient are also provided.
    Type: Grant
    Filed: May 20, 2005
    Date of Patent: January 27, 2009
    Assignee: Teva Pharmaceutical Fine Chemicals S.r.l.
    Inventors: Valeriano Merli, Silvia Mantovani, Stefano Bianchi, Paola Daverio
  • Patent number: 7470817
    Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)I, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and w
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: December 30, 2008
    Assignee: Invitrogen Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Publication number: 20080262267
    Abstract: The present invention relates to processes for the preparation of 4-hydroxy-??-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol 1-hydroxy-2-naphthoate (salmeterol xinafoate) (12a), the preparation of 4-hydroxy-??-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol (salmeterol) (11), the preparation of protected N-[6-(4-phenylbutoxy)hexyl]amine intermediates (7), and the preparation of 6-substituted (4-phenylbutoxy)hexane intermediates (5), shown below, wherein X is a leaving group and Pg is a protecting group.
    Type: Application
    Filed: April 16, 2008
    Publication date: October 23, 2008
    Applicant: Generics [UK] Limited
    Inventors: Vinayak G. Gore, Avinash C. Gaikwad, M. Gadkar, V.K. Shukla
  • Publication number: 20080253967
    Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Application
    Filed: April 11, 2008
    Publication date: October 16, 2008
    Inventors: Hank F. Kung, Mei Ping Kung, Rajesh Manchanda
  • Patent number: 7368607
    Abstract: The invention relates to a method for isolating toremifene from a mixture of toremifene and its corresponding E isomer. The method comprises contacting the isomer mixture with a first solvent comprising methanol, allowing toremifene to crystallize in said first solvent, allowing the crystallized product of the previous step to crystallize from a second solvent comprising acetone, methyl ethyl ketone or ethyl acetate, and optionally converting toremifene crystallized from the previous step to a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: May 6, 2008
    Assignee: Orion Corporation
    Inventors: Reijo Toivola, Tuomas Huuhtanen
  • Patent number: 7323594
    Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by -X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: January 29, 2008
    Assignee: Invitrogen Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Patent number: 7247606
    Abstract: A compound of formula: wherein each R group independently is C6-C10 arylene group, a straight or branched chain C2-C°alkylene group optionally containing an arylene group, or a C4-C20 straight chain alkylene group containing one or more —NH— groups in the alkylene chain, each X is —O—, —S—, or —NR5— where R5 is hydrogen or C1-C6 alkyl, each AO group is independently ethyleneoxy, 1,2-propyleneoxy, or 1,2-butyleneoxy, n, m and p is from 1 to 50 and the sum of n, m and p is from 4 to 50, and the R4 is independently —CH2-CH(OH)—R9, wherein each R9 independently represents a C4-C18 saturated or unsaturated, substituted or unsubstituted hydrocarbon group. The compound has surfactant and defoaming properties and is useful in latex paint, an ink, an adhesive, or a metal working compositions.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: July 24, 2007
    Assignee: Cognis Corporation
    Inventors: Stephen F. Gross, Norman Milstein
  • Patent number: 7226950
    Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).
    Type: Grant
    Filed: August 7, 2006
    Date of Patent: June 5, 2007
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, David C. Green, Daniel Marquess
  • Patent number: 7179926
    Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts and solvates, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
    Type: Grant
    Filed: July 25, 2005
    Date of Patent: February 20, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yazhong Huang, Shuanghua Hu, Andrew P. Degnan
  • Patent number: 7166745
    Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)1, or {(CH2)i—Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1—L?—X2—Z or —Z; R1–R6, independently of one another, are selected from the group consisting of H, —CH2)p—D—Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: January 23, 2007
    Assignee: Invitrogen Corporation
    Inventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
  • Patent number: 6963012
    Abstract: The present invention provides diaryl ether derivatives that exhibit significant immunosuppressive effects with less side effects. The diaryl derivatives of the present invention are represented by the following general formula (1): one example is 2-amino-2-[4-(3-benzyloxyphenoxy)-2-chlorophenyl]propyl-1,3-propanediol.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: November 8, 2005
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Naoki Ando, Takahiro Tanase, Kazuhiko Kuriyama, Satoru Iwanami, Shinji Kudou
  • Patent number: 6916956
    Abstract: A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: July 12, 2005
    Assignee: Japan Tobacco, Inc.
    Inventors: Yuko Shinagawa, Takeo Katsushima, Takashi Nakagawa
  • Patent number: 6911560
    Abstract: Accordingly, the present invention provides a process for the preparation of a compound of formula (I) or a single enantiomer thereof, or a salt or a solvate thereof, wherein W is a chiral auxilary or hydrogen and P1 and P2 are each independently selected from hydrogen or a protecting group, which comprises: a) treatment of a compound of formula (II), or a salt or a solvate thereof, wherein W is a chiral auxilary and P3 and P4 are each independently selected from hydrogen or a protecting group, with a compound formula (III); b) treatment of the resulting product with a reducing agent; c) if required, deprotection to yield the compound of formula (I), or a salt or solvate thereof.
    Type: Grant
    Filed: June 13, 2001
    Date of Patent: June 28, 2005
    Assignee: SmithKline Beecham Corporation
    Inventor: Panayiotis Alexandrou Procopiou
  • Patent number: 6887871
    Abstract: There is disclosed the use of a compound of formula (I) wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy. The compounds of formulae (I) and (Ia) are inhibitors of the enzyme nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: May 3, 2005
    Assignee: AstraZeneca AB
    Inventors: David Cheshire, Stephen Connolly, David Cox, Peter Hamley, Antonio Mete, Austen Pimm
  • Patent number: 6846958
    Abstract: Benzimidates can be reacted with a large number of nucleophiles, leading to a wide variety of products. The present invention discloses a facile synthesis for ethyl 2,4-dihydroxybenzimidate, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid or 2,4-dibenzyloxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.
    Type: Grant
    Filed: May 15, 2003
    Date of Patent: January 25, 2005
    Assignee: Genzyme Corporation
    Inventors: Mukund S. Chorghade, Mukund K. Gurjar, Joseph Cherian
  • Publication number: 20040138273
    Abstract: New carbocyclic compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease, other neurodegenerative disorders, such as Parkinson's disease and Huntington's disease, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
    Type: Application
    Filed: October 20, 2003
    Publication date: July 15, 2004
    Inventors: Allan S. Wagman, Sharadha Subramanian, John M. Nuss
  • Publication number: 20040127546
    Abstract: Compounds of the general formula (I): 1
    Type: Application
    Filed: January 22, 2004
    Publication date: July 1, 2004
    Applicant: ASAHI KASEI PHARMA CORPORATION
    Inventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
  • Publication number: 20040127733
    Abstract: The present invention relates to new beta-agonists of general formula 1: 1
    Type: Application
    Filed: October 28, 2003
    Publication date: July 1, 2004
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Thomas Trieselmann, Bradford S. Hamilton, Dirk Stenkamp, Stephan Georg Mueller
  • Publication number: 20040110804
    Abstract: The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds.
    Type: Application
    Filed: July 9, 2003
    Publication date: June 10, 2004
    Inventors: Michael A. Walker, Zhuping Ma, B. Narasimhulu Naidu, Margaret E. Sorenson, Annapurna Pendri, Jacques Banville, Serge Plamondon, Roger Remillard
  • Publication number: 20040082627
    Abstract: Compound having Formula 1: 1
    Type: Application
    Filed: June 23, 2003
    Publication date: April 29, 2004
    Inventors: James W. Darrow, Robert W. DeSimone, Douglas A. Pippin, Scott A. Mitchell
  • Publication number: 20030149107
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Application
    Filed: June 12, 2002
    Publication date: August 7, 2003
    Inventors: Shalini Sharma, Reid W. von Borstel
  • Publication number: 20030144526
    Abstract: A novel calcium receptor active compound having the formula is provided:
    Type: Application
    Filed: December 19, 2002
    Publication date: July 31, 2003
    Applicant: NPS Pharmaceuticals, Inc.
    Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
  • Patent number: 6583246
    Abstract: The invention provides modifiers for the anionic polymerization of conjugated dienes or of conjugated dienes with vinylaromatic compounds, wherein the modifiers are specific aminoethers.
    Type: Grant
    Filed: November 6, 2001
    Date of Patent: June 24, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Grün, Thomas Knauf, Wilfried Braubach
  • Publication number: 20030105360
    Abstract: The present invention relates to novel polymorphic Form A of fluoxetine hydrochloride.
    Type: Application
    Filed: August 20, 2002
    Publication date: June 5, 2003
    Inventors: Grayson Walker Stowell, Robert R. Whittle
  • Publication number: 20030100754
    Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides naphthalene compounds, intermediates, formulations, and methods.
    Type: Application
    Filed: August 26, 1997
    Publication date: May 29, 2003
    Inventors: HENRY UHLMAN BRYANT, THOMAS ALAN CROWELL, CHARLES DAVID JONES
  • Publication number: 20030088113
    Abstract: The present invention relates to an improved process for preparing 4-substituted resorcinol derivatives, and intermediate compounds useful in the preparation of such resorcinol derivatives.
    Type: Application
    Filed: October 28, 2002
    Publication date: May 8, 2003
    Inventors: Stuart Edward Bradley, John Kitchin, Graham Michael Wynne
  • Publication number: 20030040545
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-l) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral fused heterocyclic amino compounds.
    Type: Application
    Filed: December 12, 2001
    Publication date: February 27, 2003
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel