The Aryl Ring Or Ring System And Amino Nitrogen Are Bonded Directly To The Same Acyclic Carbon, Which Carbon Additionally Has Only Hydrogen Or Acyclic Hydrocarbyl Substituents Bonded Directly Thereto Patents (Class 564/384)
  • Patent number: 7714170
    Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, use in the reduction of A? peptide in vivo, use in modulating APP processing, and use in modulating the activity of APP secretase.
    Type: Grant
    Filed: December 8, 2008
    Date of Patent: May 11, 2010
    Assignee: Proteotech, Inc.
    Inventors: Alan D. Snow, Qubai Hu, Judy A. Cam
  • Patent number: 7700658
    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-I) 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.
    Type: Grant
    Filed: January 29, 2008
    Date of Patent: April 20, 2010
    Assignee: Pfizer Inc.
    Inventors: James A. Sikorsky, 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
  • Publication number: 20100016621
    Abstract: The present invention relates to a process for converting a substrate to a product comprising exposing the substrate to a hydrosilane in the presence of a carbene catalyst.
    Type: Application
    Filed: September 28, 2006
    Publication date: January 21, 2010
    Inventors: Yugen Zhang, Jackie Y. Ying
  • Publication number: 20100009970
    Abstract: The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.
    Type: Application
    Filed: March 18, 2009
    Publication date: January 14, 2010
    Applicant: Combinatorx (Singapore) Pte. Ltd.
    Inventors: Lisa M. Johansen, Christopher M. Owens, Christina Mawhinney, Todd W. Chappell, Alexander T. Brown, Michael G. Frank, Michael A. Foley, Ralf Altmeyer, Yu Chen
  • Publication number: 20090326272
    Abstract: There is provided a method for producing an optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative, which includes the steps of conducting reductive alkylation of an optically active secondary amine and a formaldehyde (including an equivalent thereof) or lower aldehyde in the presence of a transition metal catalyst under a hydrogen gas atmosphere, thereby converting the secondary amine to an optically active tertiary amine of the formula, and subjecting the tertiary amine to hydrogenolysis. The target optically active compound can be produced efficiently by this production method.
    Type: Application
    Filed: June 25, 2007
    Publication date: December 31, 2009
    Applicant: Central Glass Company, Limited
    Inventors: Akihiro Ishii, Kaori Mogi, Hideyuki Tsuruta, Kenjin Inomiya
  • Publication number: 20090298879
    Abstract: The present invention relates to impurities of donepezil, or a pharmaceutically acceptable salt thereof, which may be produced during synthesis and storage of donepezil, or a pharmaceutically-acceptable salt thereof, and to methods of identifying such impurities. The invention also relates to the use of these impurities in analytical techniques and to product that contain certain low levels of these impurities in particular the following impurities are disclosed: formula (I) and formula (II).
    Type: Application
    Filed: May 18, 2007
    Publication date: December 3, 2009
    Applicant: PLIVA Hrvatska d.o.o.
    Inventors: Irena Krizmanic, Lidija Lerman, Zrinka Samardzic, Katarzyna Kaczorowska, Andrzej Manikowski, Barbara Zioro, Ivica Grebenar, Jasna Dogan Koruznjak
  • Patent number: 7601876
    Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, AA/SAA amyloidosis, such as observed in systemic AA amyloidosis and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Grant
    Filed: March 5, 2007
    Date of Patent: October 13, 2009
    Assignee: Proteotech, Inc.
    Inventors: Alan D. Snow, Beth P. Nguyen, Gerardo M. Castillo, Virginia J. Sanders, Thomas P. Lake, Lesley Larsen, Rex T. Weavers, Stephen D. Lorimer, David S. Larsen, David L. Coffen, Charlotte Coffen, legal representative
  • Publication number: 20090252694
    Abstract: Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of: reacting aminoacetophenone with sulfonylchloride under the presence of an appropriate salt; and reacting the compound prepared in the above step with hydroxybenzaldehide under the presence of an appropriate catalyst. The chalcone derivative of formula 1 in accordance with the present invention having strong enzyme inhibitory activities for glycosidase can be effectively used in preventing and treating various diseases induced by glycosidase, and the chalcone derivative of the invention having tyrosinase and melanin synthesis inhibitory activities can be effectively used as a skin-whitening compound.
    Type: Application
    Filed: April 3, 2006
    Publication date: October 8, 2009
    Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION GYEONGSANG NATIONAL UNIVERSTIY
    Inventors: Ki Hun Park, Jin Hyo Kim, Woo Duck Seo, Young Bae Ryu, Hyung Won Ryu, Woo Song Lee, Sang Wan Gal
  • Publication number: 20090198084
    Abstract: The present invention relates to a process for the deprotection of protected amine compounds, wherein the protected amine compound is contacted with an electrophilic oxidating agent that is optionally formed in situ, said electrophilic oxidating agent being selected from the group of I2, Br2, Cl2 and compounds comprising a halogen atom having a formal oxidation state of 1+, 3+, 5+ or 7+, provided that the electrophilic oxidating agent is not iodobenzene diacetate. The process can be conveniently employed in the synthesis of 1,3-amino alcohols, ?-amino acids and heterocyclic compounds, in particular ?-amino acids.
    Type: Application
    Filed: May 1, 2007
    Publication date: August 6, 2009
    Inventors: Paulus Lambertus Alsters, Jorge Merijn Mathieu Verkade, Peter Jan Leonard Mario Quaedflieg, Floris Petrus Johannes Theodorus Rutjes
  • Publication number: 20090163719
    Abstract: There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group V heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or diastereomer in the product composition being greater than the ratio of second to first enantiomer or diastereomer in the enantiomerically enriched composition.
    Type: Application
    Filed: October 27, 2005
    Publication date: June 25, 2009
    Inventors: Andrew John Blacker, Matthew John Stirling
  • Publication number: 20090137653
    Abstract: This invention is directed to substituted benzylamines which are useful as inhibitors of the CYP2A6 enzyme. Pharmaceutical compositions comprising the compounds and methods of using the compounds to treat nicotine dependence are also disclosed.
    Type: Application
    Filed: April 6, 2006
    Publication date: May 28, 2009
    Applicant: INFLAYZME PHARMACEUTICALS LTD.
    Inventors: Omar Ghosheh, Jeffery R. Raymond
  • Publication number: 20090082469
    Abstract: The present application describes deuterium-enriched terbinafine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 19, 2008
    Publication date: March 26, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20080293751
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Application
    Filed: November 15, 2007
    Publication date: November 27, 2008
    Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Patent number: 7439400
    Abstract: The invention disclosed a new process of asymmetric alkynylation of ketone or ketimine, involving the chiral ligand-mediated asymmetric addition of zinc or copper acetylide to a trifluoromethyl ketone or ketimine intermediate to give a chiral tertiary proparglic alcohols or amines. The adduct compounds include the key precursors to the potent HIV reverse transcriptase inhibitor Efavirenz (DMP 266), DPC 961 and DPC 083. The invention also disclosed a novel chiral amino alcohol ligand.
    Type: Grant
    Filed: June 16, 2003
    Date of Patent: October 21, 2008
    Assignee: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
    Inventors: Biao Jiang, Yugui Si
  • Patent number: 7432399
    Abstract: A polyol monomer comprising the formula: R1 and R3 are —H, aliphatic, aromatic, or ether; R2 is aliphatic, aromatic, ester, ether, or acrylic, and R1 contains a hydroxyl group, R3 contains a hydroxyl group, R2 contains —O—CH2—CH(OH)—, or any combination thereof. The polyol monomer may be made by reacting an epoxy and an amine. Either the epoxy contains more than one epoxide groups, the amine contains a hydroxyl group, or both. A thermoset made by reacting the polyol monomer with a polyisocyanate.
    Type: Grant
    Filed: November 2, 2004
    Date of Patent: October 7, 2008
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Jozef Verborgt, Arthur Anthony Webb
  • Publication number: 20080146620
    Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.
    Type: Application
    Filed: November 13, 2007
    Publication date: June 19, 2008
    Applicant: Japan Tobacco Inc.
    Inventors: Kimiya Maeda, Hironobu Nagamori, Hiroshi Nakamura, Hisashi Shinkai, Yasunori Suzuki, Daisuke Takahashi, Toshio Taniguchi
  • Publication number: 20080139847
    Abstract: The present invention relates to a method for the preparation of tertiary carbinamine compounds from diastereoselective allylation and crotylation of N-unsubstituted imines derived from ketones.
    Type: Application
    Filed: October 4, 2007
    Publication date: June 12, 2008
    Inventors: Avinash N. Thadani, Bhartesh Dhudshia
  • Patent number: 7368609
    Abstract: An optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative represented by the formula 4 is produced by a process including (a) reacting an optically active secondary amine, represented by the formula 1, with an alkylation agent R2—X, in the presence of a base, thereby converting the secondary amine into an optically active tertiary amine represented by the formula 3; and (b) subjecting the tertiary amine to a hydrogenolysis, thereby producing the N-monoalkyl derivative, wherein R represents a fluorine atom, trifluoromethyl group or trifluoromethoxy group, n represents an integer of from 1 to 5, each of R1 and R2 independently represents an alkyl group having a carbon atom number of from 1 to 6, Me represents a methyl group, Ar represents a phenyl group or 1- or 2-naphthyl group, * represents a chiral carbon, and X represents a leaving group.
    Type: Grant
    Filed: February 12, 2007
    Date of Patent: May 6, 2008
    Assignee: Central Glass Company, Limited
    Inventors: Akihiro Ishii, Masatomi Kanai, Yokusu Kuriyama, Manabu Yasumoto, Kenjin Inomiya, Takashi Ootsuka, Koji Ueda
  • Patent number: 7312343
    Abstract: Compounds of formula I and a process for the preparation of such compounds are disclosed.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: December 25, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rudolf Schmid, Ulrich Zutter
  • Patent number: 7297821
    Abstract: A fluorine compound represented by Formula (1) is provided. The above fluorine compound is effective for introducing a fluorine atom into a compound having an active group such as an oxygen-containing functional group, and it can be used for uses of surface treatment, cleaning and coating. Further, after the fluorination reaction, the above compound is recovered and can be reused as a starting material for producing the above fluorine compound, and it is useful for various fluorination processes. (wherein X represents a nitrogen or phosphorus atom; R0, R1, and R2 represent hydrogen, an alkyl group or aryl group which may have a substituent, and they each may be the same or different; and R0, R1, and R2 may be combined with each other to form a ring).
    Type: Grant
    Filed: December 9, 2005
    Date of Patent: November 20, 2007
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Toshio Hidaka, Norio Fushimi, Takafumi Yoshimura, Takeshi Kawai
  • Patent number: 7276630
    Abstract: A process is provided for preparing optionally substituted arylated benzylamines from the corresponding optionally substituted aryl halides and optionally substituted benzylamines using a specific solvent mixture, a base and a catalyst comprising a palladium compound and a bisaryldialkylphosphine.
    Type: Grant
    Filed: September 22, 2006
    Date of Patent: October 2, 2007
    Assignee: Saltigo GmbH
    Inventors: Michael Dockner, Ulrich Scholz, Torsten Neugebauer
  • Patent number: 7226951
    Abstract: Compounds of formulas 1 through 17 provided in the specification specifically or selectively inhibit either the cytochrome P450RAI-1 enzyme or the cytochrome P450RAI-2 enzyme.
    Type: Grant
    Filed: December 16, 2004
    Date of Patent: June 5, 2007
    Assignee: Allergan, Inc.
    Inventors: Jayasree Vasudevan, Liming Wang, Xiaoxia Liu, Kwok Yin Tsang, Ling Li, Janet A. Takeuchi, Thong Vu, Richard Beard, Smita Bhat, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 7186865
    Abstract: An optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative represented by the formula 4 is produced by a process including (a) reacting an optically active secondary amine, represented by the formula 1, with an alkylation agent R2—X, in the presence of a base, thereby converting the secondary amine into an optically active tertiary amine represented by the formula 3; and (b) subjecting the tertiary amine to a hydrogenolysis, thereby producing the N-monoalkyl derivative, wherein R represents a fluorine atom, trifluoromethyl group or trifluoromethoxy group, n represents an integer of from 1 to 5, each of R1 and R2 independently represents an alkyl group having a carbon atom number of from 1 to 6, Me represents a methyl group, Ar represents a phenyl group or 1- or 2-naphthyl group, * represents a chiral carbon, and X represents a leaving group.
    Type: Grant
    Filed: September 5, 2003
    Date of Patent: March 6, 2007
    Assignee: Central Glass Company, Limited
    Inventors: Akihiro Ishii, Masatomi Kanai, Yokusu Kuriyama, Manabu Yasumoto, Kenjin Inomiya, Takashi Ootsuka, Koji Ueda
  • Patent number: 7179945
    Abstract: A di(aminomethyl)-substituted aromatic compound is produced by a two-stage hydrogenation. In the first stage, an aromatic dinitrile is hydrogenated into a cyano(aminomethyl)-substituted aromatic compound in the presence of a Pd-containing catalyst. The resultant cyano(aminomethyl)-substituted aromatic compound is then hydrogenated in the second stage into the target di(aminomethyl)-substituted aromatic compound in the presence of a Ni- and/or Co-containing catalyst. By the above method, the di(aminomethyl)-substituted aromatic compound is produced in a high selectivity and a sufficiently high yield without reducing the catalyst life.
    Type: Grant
    Filed: February 20, 2004
    Date of Patent: February 20, 2007
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Yoshinori Kanamori, Shuji Ebata, Kengo Tsukahara, Yoshiaki Yamamoto
  • Patent number: 7119122
    Abstract: There are provided novel compounds of formula (I) wherein A, R1, R3, R4, R5, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.
    Type: Grant
    Filed: October 2, 2002
    Date of Patent: October 10, 2006
    Assignee: Astrazeneca AB
    Inventors: Stephen Connolly, Glen Ernst
  • Patent number: 7078567
    Abstract: The present invention provides methodology for carbon-nitrogen bond formation via vinyl or aryl amination. In the process of the invention, an sp2 hybridized radical is reacted with an azomethine moiety to form pyrrolidine and indole compounds. The methodology provides a facile process for the synthesis of compounds having the pyrrolidine or indole subunit and is especially advantageous for compounds having acid or base labile functional groups and/or is comprised of chiral centers susceptible to acid/base epimerization.
    Type: Grant
    Filed: October 16, 2003
    Date of Patent: July 18, 2006
    Inventors: Jeffrey N. Johnston, Rajesh Viswanathan
  • Patent number: 7078226
    Abstract: A process for preparing optically active amines, a process for preparing racemic amines which can be resolved using optically active carboxylic acids or enzymes, and racemic and optically active amines and optically active amides are described.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: July 18, 2006
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Ditrich, Wolfgang Siegel
  • Patent number: 7019173
    Abstract: A fluorine compound represented by Formula (1) is provided. The above fluorine compound is effective for introducing a fluorine atom into a compound having an active group such as an oxygen-containing functional group, and it can be used for uses of surface treatment, cleaning and coating. Further, after the fluorination reaction, the above compound is recovered and can be reused as a starting material for producing the above fluorine compound, and it is useful for various fluorination processes. (wherein X represents a nitrogen or phosphorus atom; R0, R1, and R2 represent hydrogen, an alkyl group or aryl group which may have a substituent, and they each may be the same or different; and R0, R1, and R2 may be combined with each other to form a ring).
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: March 28, 2006
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Toshio Hidaka, Norio Fushimi, Takafumi Yoshimura, Takeshi Kawai
  • Patent number: 6984664
    Abstract: Disclosed are compounds of the formula (I) wherein R1, R2 R3 R4 R5, R6 and N are as disclosed herein. The compounds are useful for the treatment of chronic and acute pain.
    Type: Grant
    Filed: December 6, 2000
    Date of Patent: January 10, 2006
    Assignee: Euro-Celtique, S.A.
    Inventors: Donald Kyle, R Richard Goehring, Sam Victory
  • Patent number: 6982350
    Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.
    Type: Grant
    Filed: February 17, 2005
    Date of Patent: January 3, 2006
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Michel Lerestif, Isaac Gonzalez Blanco, Jean-Pierre Lecouve, Daniel Brigot
  • Patent number: 6951958
    Abstract: Described is method for preparing tertiary amines comprising sequential, exhaustive alkylation of a hydroxylamine derivative and cleavage of the O—N bond using the following steps: a) reacting the hydroxylamine derivative with an alkylating agent or with a carbonyl compound to form an oxime intermediate. b) reacting the oxime intermediate with a reducing agent to produce an alkylated derivative c) reacting the alkylated derivative with an alkylating agent or a carbonyl compound in the presence of a reducing agent to produce a dialkylated derivative d) reacting the dialkylated derivative with an alkylating agent to produce a quaternized derivative e) reacting the quaternized derivative with a reagent causing cleavage of the O—N bond to produce a tertiary amine.
    Type: Grant
    Filed: August 3, 2000
    Date of Patent: October 4, 2005
    Assignee: Acadia Pharmaceuticals Inc.
    Inventors: Carl-Magnus A. Andersson, Magnus Gustafsson, Kent R. I. Olsson
  • Patent number: 6908982
    Abstract: An object of the present invention is to provide an amino composition which provides, when used as a curing agent for epoxy resin, a long pot life and an excellent appearance of a coating film to an epoxy resin composition without deteriorating the reactivity of the composition. The amino composition is obtained by addition reaction of diamine such as metaxylylenediamine and 1,3-bis(aminomethyl) cyclohexane and styrene, wherein the content of the diamine is less than 15% by weight based upon the total weight of the amino composition and the content of 1-addition product of having one phenethyl group is 50 to 100% by weight based upon the total weight of amino compound(s) obtained by the addition reaction.
    Type: Grant
    Filed: June 18, 2003
    Date of Patent: June 21, 2005
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Tetsushi Ichikawa, Hisayuki Kuwahara, Masatoshi Echigo
  • Patent number: 6894195
    Abstract: A process for the preparation of 4-methyl-2,3,5,6-tetrafluorobenzyl alcohol comprising hydrogenating 4-methyl-2,3,5,6-tetrafluorobenzonitrile to 4-methyl-2,3,5,6-tetrafluorobenzylamine and converting 4-methyl-2,3,5,6-tetrafluorobenzylamine to 4-methyl-2,3,5,6-tetrafluorobenzyl alcohol. The process optionally also comprises the further step of reacting 4-Methyl-2,3,5,6-tetrafluobenzyl alcohol with cis-Z-3-(2-chloro-1,1,1-trifluoro-2-propenyl)-2,2-dimethylcyclopropanecarbonyl chloride to the form tefluthrin. 4-Methyl-2,3,5,6-tetrafluorobenzylamine and salts thereof are also claimed.
    Type: Grant
    Filed: October 18, 2001
    Date of Patent: May 17, 2005
    Assignee: Syngenta Limited
    Inventors: Raymond Vincent Heavon Jones, Stephen Martin Brown
  • Patent number: 6861561
    Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.
    Type: Grant
    Filed: September 26, 2002
    Date of Patent: March 1, 2005
    Assignee: G. D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
  • Patent number: 6803462
    Abstract: This invention discloses a rubbery polymer which is comprised of repeat units that are derived from (1) at least one conjugated diolefin monomer, and (2) at least one functionalized monomer having of the structural formula: wherein R represents an alkyl group containing from 1 to about 10 carbon atoms or a hydrogen atom, and wherein R1 and R2 can be the same or different and represent hydrogen atoms or a moiety selected from the group consisting of wherein R3 groups can be the same or different and represent alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, allyl groups, and alkyloxy groups of the structural formula —(CH2)y—O—(CH2)z—CH3, wherein Z represents a nitrogen containing heterocyclic compound, wherein R4 represents a member selected from the group consisting of alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, and allyl groups, and wherein n, x, y and z represents integers from 1 to about 10, with the
    Type: Grant
    Filed: June 30, 2003
    Date of Patent: October 12, 2004
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Stephan Rodewald, Steven Kristofer Henning, Brian Earl Burkhart
  • Patent number: 6797842
    Abstract: An optically active 1-(fluoro- or trifluoromethyl-substituted phenyl)ethylamine is produced with high optical purity and in an industrially simple and efficient manner by asymmetrically reducing an optically active imine, obtained by dehydration and condensation of a fluoro- or trifluoromethyl-substituted phenylmethyl ketone and an optically active primary amine under acidic conditions, using a hydride reducing agent to convert to an optically active secondary amine, and subjecting the secondary amine or its salt of an inorganic acid or organic acid to hydrogenolysis.
    Type: Grant
    Filed: May 11, 2001
    Date of Patent: September 28, 2004
    Assignee: Central Glass Company, Limited
    Inventors: Akihiro Ishii, Manabu Yasumoto, Yokusu Kuriyama, Masatomi Kanai, Takashi Hayami
  • Patent number: 6787570
    Abstract: The invention relates to substituted N-Alkyl/Alkenyl/Cycloalkyl/Heterocycyl N-Aryl/Heteroaryl tertiary-Heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease. Preferred tertiary-heteroalkylamine compounds are substituted N-cycloalkyl N-benzyl aminoalcohols.
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: September 7, 2004
    Assignee: Pfizer, Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Deborah A. Mischke, Emily J. Reinhard, Barry L. Parnas, Melvin L. Rueppel
  • Publication number: 20040171615
    Abstract: The invention relates to substituted 1-aryl-but-3-enylamine and 1-aryl-but-2-enylamine compounds, to a method for the production thereof, to medicaments containing said compounds and to their use in the production of medicaments.
    Type: Application
    Filed: January 5, 2004
    Publication date: September 2, 2004
    Inventors: Bernd Sundermann, Corinna Sundermann, Helmut Buschmann, Babette-Yvonne Koegel
  • Publication number: 20040162432
    Abstract: The invention relates to substituted octahydrophenanthrene compounds of general formula (I), to a method for their production, to medicaments containing these compounds and to the use of said compounds for producing medicaments.
    Type: Application
    Filed: February 13, 2004
    Publication date: August 19, 2004
    Inventors: Helmut Buschmann, Werner Englberger, Michael Przewosny, Hans Schick, Birgitta Henkel, Michael Sattlegger
  • Patent number: 6770785
    Abstract: The present invention relates to a novel antiozonant as well as antioxidant based on functionalized hindered phenol and the process for the preparation thereof of formula 1 wherein R1 is tert-butyl and R2 and R3 are C1 to C8 linear or branched alkyl. The present invention also relates to a process for the preparation thereof comprising dissolving a compound of formula 3 wherein R1 is tert-butyl, with liquid bromine in a non polar organic solvent at temperature range 80 to 95° C. for a period of 4 to 7 hours, evaporating the solvent under reduced pressure to obtain a compound of formula 2 wherein R1 is a tertiary butyl group and X is Br, reacting the compound of formula 2 with a compound of formula 4 wherein R2 and R3 are C1 to C8 linear or branched alkyl, dissolved in an organic solvent in presence of a suitable mild base at a temperature ranging from 80 to 95° C.
    Type: Grant
    Filed: March 25, 2003
    Date of Patent: August 3, 2004
    Assignee: Council of Scientific and Industrial Research
    Inventors: Shrojal Mohitkumar Desai, Shailendra Singh Solanky, Raj Pal Singh
  • Patent number: 6765023
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: July 20, 2004
    Assignee: Pfizer, Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Publication number: 20040132828
    Abstract: A crystalline form of sertraline hydrochloride was found, referred to hereinafter as polymorphic form CSC2 having a dissolution rate which surprisingly will increase rate of absorption of a drug.
    Type: Application
    Filed: December 15, 2003
    Publication date: July 8, 2004
    Inventors: Paul Adriaan Van Der Schaaf, Franz Schwarzenbach, Hans-Jorg Kirner, Martin Szelagiewicz, Claudia Marcolli, Andreas Burkhard, Regine Peter
  • Patent number: 6723752
    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-I) 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 N-benzyl-N-phenyl aminoalcohols.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: April 20, 2004
    Assignee: Pharmacia Corporation
    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
  • Patent number: 6723753
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.
    Type: Grant
    Filed: February 7, 2002
    Date of Patent: April 20, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Publication number: 20040073065
    Abstract: A fluorine compound represented by Formula (1) is provided. The above fluorine compound is effective for introducing a fluorine atom into a compound having an active group such as an oxygen-containing functional group, and it can be used for uses of surface treatment, cleaning and coating. Further, after the fluorination reaction, the above compound is recovered and can be reused as a starting material for producing the above fluorine compound, and it is useful for various fluorination processes.
    Type: Application
    Filed: June 4, 2003
    Publication date: April 15, 2004
    Inventors: Toshio Hidaka, Norio Fushimi, Takafumi Yoshimura, Takeshi Kawai
  • Patent number: 6713652
    Abstract: The present invention relates to a process for hydrolyzing optically active amides to carboxylic acids and optically active amines with retention of the center of chirality, where the hydrolysis of the amides is carried out with an alkali metal or alkaline earth metal hydroxide in the presence of 5-30% by weight, based on the amide employed, of a polyol or an amino alcohol.
    Type: Grant
    Filed: September 11, 2001
    Date of Patent: March 30, 2004
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Ditrich, Wolfgang Ladner, Johann-Peter Melder
  • Patent number: 6710210
    Abstract: Novel N-substituted-aminomethyl cyclopropyl ketone derivatives are represented by following Formula (1): wherein R1, R2 and R3 are each a hydrogen atom or an aliphatic hydrocarbon group; and R4 and R5 are each a hydrogen atom or an arylmethyl group which may have a substituent, where at least one hydrogen atom or aryl group as a substituent is combined with a carbon atom in the methyl moiety of the arylmethyl group, and at least one of R4 and R5 is an arylmethyl group which may have a substituent. These compounds are useful for the preparation of aminomethyl cyclopropyl ketone derivatives and 2-amino-1-cyclopropylethanol derivatives or salts thereof.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: March 23, 2004
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Hiroki Tanaka, Li Rui Pan, Kiyoshi Ikura
  • Patent number: 6683099
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted cycloalkyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 27, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6683113
    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-I) 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 N,N-bis-benzyl aminoalcohols.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: January 27, 2004
    Assignee: Pharmacia Corporation
    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
  • Patent number: RE39530
    Abstract: 3-amino-3-arylpropan-1-ol compounds corresponding to the formula I in which R1 to R5, A and X have the meanings according to claim 1, and their preparation and use as medicaments.
    Type: Grant
    Filed: September 11, 2003
    Date of Patent: March 27, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Helmut Buschmann