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: 6677375
    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-bis-benzyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 13, 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: 6677380
    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 mercapto amines.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 13, 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: 6599861
    Abstract: Compounds of formula I wherein the substituents are defined as in claim 1, as well as the agronomically acceptable salts, isomers and enantiomers of these compounds, as well as the agronomically acceptable salts/N-oxides/isomers/enantiomers of these compounds, are eminently suitable for use as herbicides.
    Type: Grant
    Filed: June 21, 2001
    Date of Patent: July 29, 2003
    Assignee: Syngenta Participations AG
    Inventors: Jürgen Schaetzer, Alain De Mesmaeker, Shy-Fuh Lee
  • Patent number: 6586633
    Abstract: The present invention relates to amine derivatives represented by formula (1) or salts thereof. R3 represents C1-C3 alkyl, hydroxylated C1-C5 alkyl, C1-C5 acyl; C2-C5 alkenyl, or a halogen atom; and k, l, and m are each an integer of 1 to 4.) Exhibiting excellent antifungal effect, these compounds are highly useful as antifungal agents, antifungal compositions, drugs, etc.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: July 1, 2003
    Assignee: Pola Chemical Industries, Inc.
    Inventors: Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima, Takao Itoh, Takuji Nakashima, Akira Nozawa, Hiroyuki Takimoto, Kouji Yokoyama
  • Publication number: 20030060456
    Abstract: A compound of general formula (I) wherein R1 and R2 are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d=0, 1, 2 or 3; or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; Z or Y is —SR3 and the other Z or Y is halogen or —R3; wherein R3 is C1-C4 alkyl optionally substituted with fluorine; except that R3 is not CF3; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R4 and R5, which may be the same or different, are: A—X, wherein A═—CH═CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(═O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; or a 5- or 6-membered heter
    Type: Application
    Filed: August 27, 2001
    Publication date: March 27, 2003
    Inventors: Mavis Diane Adam, Mark David Andrews, Mark Leonard Elliott, Geoffrey Edward Gymer, David Hepworth, Harry Ralph Howard, Donald Stuart Middleton, Alan Stobie
  • Patent number: 6528491
    Abstract: The present invention relates to new pyranoside derivatives of general formula I, processes for preparing them as well as their use as medicaments:
    Type: Grant
    Filed: October 23, 2001
    Date of Patent: March 4, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Ralf Anderskewitz, Kurt Schromm, Franz Birke, Hans Michael Jennewein
  • Patent number: 6495496
    Abstract: Low molecular weight Mannich base condensates of hydroxy aromatic compounds, an aldehyde; and an amine, wherein the combined number of substituent carbon atoms does not exceed 80. Such compounds are useful as soot dispersants in lubricating oils when used alone, or in combination with high molecular weight dispersants.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: December 17, 2002
    Assignee: Infineum International Ltd.
    Inventors: Antonio Gutierrez, Mark G. Stevens, Ricardo A. Bloch, Robert A. Kleist
  • Patent number: 6495722
    Abstract: Provided herein are polyurethane foams which may be prepared by spray techniques. The foams of the invention are prepared using conventional isocyanates and a novel Mannich condensate polyol having a hydroxy number in the range of 250-340 and a viscosity of 3500 cps or less, and wherein the Mannich condensate polyol is derived from nonylphenol, formaldehyde, an alkanolamine, and propylene oxide as the sole alkoxylating agent. Polyurethane foams prepared according to the invention possess superior physical properties over sprayed polyurethane foams prepared using Mannich condensate polyols which are made using mixtures of propylene oxide and ethylene oxide.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: December 17, 2002
    Assignee: Huntsman Petrochemical Corporation
    Inventors: Robert L. Zimmerman, Marshall P. Devine, Patrick L. Weaver
  • Patent number: 6476057
    Abstract: The invention relates to use of 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: November 14, 2001
    Date of Patent: November 5, 2002
    Assignee: G.D. Searle & Co.
    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: 6476075
    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-bis-benzyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: November 5, 2002
    Assignee: G.D. Searle & Co.
    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: 20020156323
    Abstract: Novel N-substituted-aminomethyl cyclopropyl ketone derivatives are represented by following Formula (1): 1
    Type: Application
    Filed: April 8, 2002
    Publication date: October 24, 2002
    Inventors: Hiroki Tanaka, Li Rui Pan, Kiyoshi Ikura
  • Patent number: 6462092
    Abstract: The invention relates to use of 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: November 14, 2001
    Date of Patent: October 8, 2002
    Assignee: G.D. Searle & Co.
    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: 6462044
    Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: October 8, 2002
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
  • Patent number: 6458849
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkyamine 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 mercapto amines.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: October 1, 2002
    Assignee: G.D. Searle & Co.
    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: 20020115576
    Abstract: Low molecular weight Mannich base condensates of hydroxy aromatic compounds, an aldehyde; and an amine, wherein the combined number of substituent carbon atoms does not exceed 80. Such compounds are useful as soot dispersants in lubricating oils when used alone, or in combination with high molecular weight dispersants.
    Type: Application
    Filed: December 22, 2000
    Publication date: August 22, 2002
    Inventors: Antonio Gutierrez, Mark G. Stevens, Ricardo A. Bloch, Robert A. Kleist
  • Patent number: 6429335
    Abstract: The present invention relates to a process for preparing amines of formula (I) R1—CH2—NH2  (I), wherein R1 represents optionally branched C1-C12-alkyl, C3-C8-cycloalkyl, C6-C12-aryl or C6-C12-aryl substituted with halogen-and/or C1-C12-alkyl, C7-C10-aralkyl or C7-C10-aralkyl substituted on the aryl radical by halogen and/or C1-C12-alkyl, or an aldose residue of the formula CiH2i+1Oi in which i is 2 to 5 and wherein one hydrogen of the aldose residue is optionally replaced by a saccharide residue, by catalytically hydrogenating aldehydes of formula (II) R1—CHO  (II), wherein R1 has the meaning indicated for formula (I), in the presence of ammonia, a hydrogenation catalyst, and disodium tetraborate.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: August 6, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventor: Wolfgang Kiel
  • Patent number: 6423871
    Abstract: A method for selective mono-N-alkylation of primary amines to produce secondary amines that are substantially free of overalkylated tertiary amines and quaternary ammonium salts, under mild reaction conditions without the necessity of protecting groups. Compounds of the class of secondary amines are produced by reacting an alkyl halide with an alkyl amine in anhydrous solvent, preferably dimethyl sulfoxide or N,N-dimethylformamide, in the presence of 0.1 to 3 molar equivalents of a cesium base. Optionally, the extent and selectivity of mono-N-alkylation is enhanced by addition to the reaction mixture of a powdered molecular sieve material for removal of water produced by the reaction, and/or tetrabutylammonium iodide to promote halide exchange. The invention permits selective and efficient mono-N-alkylation of a wide variety of substrates at 23° C.
    Type: Grant
    Filed: February 25, 2000
    Date of Patent: July 23, 2002
    Assignee: University of South Florida
    Inventor: Kyung Woon Jung
  • Patent number: 6417353
    Abstract: Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst containing copper, wherein the catalytically active mass of the catalyst contains, before the reduction with hydrogen, 20 to 85% by weight of oxygen-containing compounds of zirconium, calculated as ZrO2, 1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO, 14 to 70% by weight of oxygen-containing compounds of nickel, calculated as NiO, 0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO3, and 0 to 10% by weight of oxygen-containing compounds of aluminum, calculated as Al2O3.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: July 9, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Frank Funke, Joachim Wulff-Döring, Gerhard Schulz, Wolfgang Siegel, Andreas Kramer, Johann-Peter Melder, Arthur Höhn, Philipp Buskens, Wolfgang Reif, Jan Nouwen
  • Patent number: 6342636
    Abstract: Disclosed is a process for preparing an optically active 1-aryl- or 2-aryl-alkylamines of formulas Ia, Ib and Ic with high optical purity and high yield. The process uses an optically active 1- or 2-naphthylglycolic acid of the general formula II as a resolving agent.
    Type: Grant
    Filed: October 28, 1998
    Date of Patent: January 29, 2002
    Assignee: Yamakawa Chemical Industry Co., Ltd.
    Inventors: Kazuhiko Saigo, Yukihiko Hashimoto, Kazushi Kinbara, Yoshiko Harada, Kenichi Sakai
  • Patent number: 6340773
    Abstract: A method of preparing a halogenated primary amine comprising hydrogenating a halogenated oxime in the presence of a catalyst comprising a non-palladium noble metal or a base metal under conditions sufficient to produce a halogenated primary amine.
    Type: Grant
    Filed: September 14, 1999
    Date of Patent: January 22, 2002
    Assignee: AlliedSignal Inc.
    Inventors: Mingbao Zhang, Michael A. Kocur, Mary Frances Martin
  • Patent number: 6331543
    Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: December 18, 2001
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
  • Patent number: 6331649
    Abstract: The present invention relates to a process for producing a trifluoromethylbenzylamine represented by the general formula (1). This process includes the step of reducing an oxime represented by the general formula (2), where R1 represents hydrogen atom, a halogen atom selected from the group consisting of fluorine, chlorine, bromine and iodine, or trifluoromethyl group, where R1 is defined as above, and R2 represents hydrogen atom, an alkyl group or an aralkyl group. With this process, the trifluoromethylbenzylamine can be produced with high selectivity.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: December 18, 2001
    Assignee: Central Glass Company, Limited
    Inventors: Satoru Narizuka, Yutaka Katsuhara
  • Patent number: 6288278
    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: April 7, 2000
    Date of Patent: September 11, 2001
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Helmut Buschmann
  • Patent number: 6288277
    Abstract: The present invention relates to new phenylamine derivatives, processes for preparing them and their use as pharmaceutical compositions.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: September 11, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Hans Michael Jennewein, Christopher John Montague Meade
  • Patent number: 6262278
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: July 17, 2001
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
  • Patent number: 6232467
    Abstract: Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: May 15, 2001
    Assignee: University of Southern California
    Inventors: Nicos A. Petasis, Ilia A. Zavialov
  • Patent number: 6225500
    Abstract: This invention discloses an improved method for the [2+2+2] cyclotrimerization reaction in aqueous solutions using a water soluble transition metal catalyst.
    Type: Grant
    Filed: March 13, 1997
    Date of Patent: May 1, 2001
    Assignee: Invenux, Inc.
    Inventors: Bruce Eaton, Matthew S. Sigman
  • Patent number: 6194615
    Abstract: The present invention relates to the composition, process of preparation, and use of novel derivatives prepared from 1,5-bis-(4′-carbomethoxyphenyl)-1,4-pentadien-3-one. These novel compositions can act as crosslinkers with polyfunctional monomeric, oligomeric, and/or polymeric anhydrides, esters, carboxylic acids, isocyantes, epoxies, carbonates, acetoacetates, and alkoxylated melamines.
    Type: Grant
    Filed: June 17, 1999
    Date of Patent: February 27, 2001
    Assignee: Eastman Chemical Company
    Inventors: Philip Conrad Heidt, Matthew Lynn Elliott
  • Patent number: 6127550
    Abstract: This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.
    Type: Grant
    Filed: March 11, 1999
    Date of Patent: October 3, 2000
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Luc Grondard, Jean-Paul Casimir, Patrick Leon, Michael K. O'Brien, Matthew R. Powers, Daniel Robin
  • Patent number: 6114394
    Abstract: The present invention relates to polyamine derivatives of the formula RHN-(CH.sub.2).sub.m -NH-(CH.sub.2).sub.n -NHR wherein m is an integer from 2 to 4, n is an integer from 3 to 10 and R is C.sub.2 -C.sub.6 alkyl or --(CH.sub.2).sub.p -Ar wherein Ar is phenyl or naphthyl and p is an integer from 0 to 2; and the pharmaceutically acceptable addition salts thereof which are useful as radioprotective agents. It relates also to the use of polyamines of the formula RHN-(CH.sub.2).sub.m -NH-(CH.sub.2).sub.n -NH-(CH.sub.2).sub.m -NHR wherein m is an integer from 2 to 4, n is an integer from 3 to 10 and R is C.sub.2 -C.sub.6 alkyl or --(CH.sub.2).sub.p -Ar wherein Ar is phenyl or naphthyl and p is an integer from 0 to 2; and the pharmaceutically acceptable addition salts thereof as radioprotective agents.
    Type: Grant
    Filed: October 14, 1997
    Date of Patent: September 5, 2000
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Michael L. Edwards, Ronald D. Snyder
  • Patent number: 6072085
    Abstract: The method of the present invention provides a simple general route to a wide range of secondary amines.
    Type: Grant
    Filed: September 30, 1997
    Date of Patent: June 6, 2000
    Assignee: Massachusetts Institute of Technology
    Inventors: Xavier Verdaguer, Udo E. W. Lange, Stephen L. Buchwald
  • Patent number: 6057358
    Abstract: Novel amine derivatives of the following general formula (I): ##STR1## (wherein) A may denote --(CH.sub.2)--O--, --(CH.sub.2).sub.2 --O--, or --(CH.sub.2).sub.2 --NH--;B may denote --(CH.sub.2).sub.2 --;R.sub.1 may denote a hydrogen atom, a halogen atom, a nitro group, a 1-pyrrolyl group, an acetamido group, an amino group or a dimethylamino group;R.sub.2 may denote a hydrogen atom or a nitro group;R.sub.3 and R.sub.4 may denote a hydrogen atom;R.sub.8a and R.sub.8b which are the same may denote a chlorine atom or a methoxy group;R.sub.9 may denote a hydrogen atom or an amino group;R may denote a methyl group; andX may denote a methanesulfonamido group, a 1-imidazolyl group or a nitro group or a salts thereof are useful as antiarrhythmic drugs.
    Type: Grant
    Filed: May 27, 1997
    Date of Patent: May 2, 2000
    Assignee: C&C Research Labs.
    Inventors: You Sup Chung, Hak Yeop Kim, Kyung Yun Jung, Jae Ki Min, Shigeru Tanabe
  • Patent number: 6011068
    Abstract: The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca.sup.2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: January 4, 2000
    Assignees: NPS Pharmaceuticals, Inc., The Brigham and Women's Hospital
    Inventors: Edward F. Nemeth, Bradford C. Van Wagenen, Manuel F. Balandrin, Eric G. DelMar, Scott T. Moe
  • Patent number: 5981599
    Abstract: The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders using such compounds. Preferred compounds can mimic or block the effect of extracellular calcium on a cell surface calcium receptor.
    Type: Grant
    Filed: April 30, 1997
    Date of Patent: November 9, 1999
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Scott T. Moe, Bradford C. Van Wagenen, Eric G. DelMar, Richard Trovato, Manuel F. Balandrin
  • Patent number: 5932726
    Abstract: The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1- benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
    Type: Grant
    Filed: April 11, 1997
    Date of Patent: August 3, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Michael Ernest Pierce, Anusuya Choudhury, Rodney Lawrence Parsons, Jr., Lilian Alicia Radesca
  • Patent number: 5922744
    Abstract: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.
    Type: Grant
    Filed: January 12, 1998
    Date of Patent: July 13, 1999
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Timothy Harrison, Andrew Pate Owens
  • Patent number: 5905167
    Abstract: The present invention relates to a process for cleaving optically active amides to carboxylic acids and optically active amines with retention of the center of chirality, wherein the amides are hydrolyzed in the presence of a polyol or of an amino alcohol and of an alkali metal or alkaline earth metal hydroxide.
    Type: Grant
    Filed: January 27, 1998
    Date of Patent: May 18, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Ditrich, Friedhelm Balkenhohl, Wolfgang Ladner
  • Patent number: 5872297
    Abstract: A novel ethylenically-unsaturated 1,3-diketoamide functional compound, polymers comprised thereof, and latex formulations containing polymeric ingredients having 1,3-diketoamide functional pendant moieties are disclosed. The 1,3-diketoamide functional pendant moieties have excellent hydrolytic stability.
    Type: Grant
    Filed: August 24, 1995
    Date of Patent: February 16, 1999
    Assignee: S. C. Johnson Commercial Markets, Inc.
    Inventor: David L. Trumbo
  • Patent number: 5872298
    Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.
    Type: Grant
    Filed: April 9, 1997
    Date of Patent: February 16, 1999
    Assignee: G. D. Searle & Co.
    Inventors: John S Ng, Claire A Przybyla, Richard A Mueller, Michael L Vazquez, Daniel P Getman, John J Freskos, Gary A DeCrescenzo, Deborah E Bertenshaw, Robert M Heintz, Suhong Zhang, Chin Liu, Scott A Laneman
  • Patent number: 5847215
    Abstract: A process for the racemization of optically active amines of the formula (I), where Ar is an unsubstituted or substituted aryl and R is alkyl, in whicha) (I) is reacted with the ketone (II) in which Ar and R have the same meanings as for (I), to give the condensation product (III), ##STR1## b) (III) is racemized by treatment with base, ##STR2## c) the arylalkylamine (I) is liberated as racemate from racemic (III) by reaction with optically active (I).
    Type: Grant
    Filed: February 10, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventor: Klaus Ditrich
  • Patent number: 5827333
    Abstract: Substituted biphenyl polyalkyl ethers having the formula: ##STR1## wherein R.sub.1 is hydrogen or hydroxyl; R.sub.2 is hydroxyl, cyano, nitro, amino, aminomethyl, N-alkylamino or N-alkylaminomethyl wherein the alkyl group contains 1 to about 6 carbon atoms, N,N-dialkylamino or N,N-dialkylaminomethyl wherein each alkyl group independently contains 1 to about 6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are ortho relative to each other and meta or para relative to the adjoining phenyl substitutent; and R.sub.3 is a polyalkyl group having an average molecular weight in the range of about 450 to about 5,000.The subsitituted biphenyl polyalkyl ethers of the present invention are useful as fuel additives for the prevention and control of engine deposits.
    Type: Grant
    Filed: September 30, 1997
    Date of Patent: October 27, 1998
    Assignee: Chevron Chemical Company LLC
    Inventor: Richard E. Cherpeck
  • Patent number: 5780505
    Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: July 14, 1998
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, David R. Herbst, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
  • Patent number: 5663440
    Abstract: An object of the invention is to propose diamino compounds expressed by the following general formula (1) which are suitable to obtain a raw material, a polyimide resin, for a liquid crystal aligning film without any image sticking and with a high voltage holding ratio at from a low temperature to a high temperature as well as the preparation thereof: ##STR1##
    Type: Grant
    Filed: October 2, 1995
    Date of Patent: September 2, 1997
    Assignee: Chisso Corporation
    Inventors: Toshiya Sawai, Seiji Oikawa, Masaaki Yazawa, Shizuo Murata, Masaharu Hayakawa, Etsuo Nakagawa, Shinichi Sawada
  • Patent number: 5656619
    Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5637119
    Abstract: Substituted aromatic polyalkyl ethers having the formula: ##STR1## wherein R.sub.1 is a polyalkyl group having an average molecular weight of about 450 to about 5,000;A is nitro, amino, cyano, aminomethyl, N-alkylamino or N-alkylaminomethyl wherein the alkyl group contains from about 1 to about 6 carbon atoms, or N,N-dialkylamino or N,N-dialkylaminomethyl wherein each alkyl group independently contains from about 1 to about 6 carbon atomsx is an integer from about 0 to about 1; and y is an integer from about 0 to about 10 with the proviso that one of x and y must be 0 and the other must be greater than 0.The substituted aromatic polyalkyl ethers of the present invention are useful as fuel additives for the prevention and control of engine deposits.
    Type: Grant
    Filed: December 29, 1995
    Date of Patent: June 10, 1997
    Assignee: Chevron Chemical Company
    Inventor: Richard E. Cherpeck
  • Patent number: 5597940
    Abstract: Disclosed is a process for producing .beta.-nitroenamine represented by the formula I: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and independently indicate a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group which may be optionally substituted with at least one group selected from the group consisting of a halogen atom, a lower alkoxy group, an aryloxy group, a hydroxyl group or an aryl group, or an aryl group which may be optionally substituted with a halogen atom, a lower alkyl group, a lower alkoxy group, an aryl group, an aryloxy group, a nitro group, a cyano group, an acylamino group, a di-lower alkylamino group, an arylamino group, a hydroxyl group, an arylsulfonyl group, a mercapto group, a lower alkylthio group or an arylthio group, R.sub.1 and R.sub.2 may bond together to form a cycloalkyl or bicycloalkyl and R.sub.3 is a hydrogen atom, a lower alkyl group, a cycloalkyl group or an aralkyl group; and an intermediate for producing the .beta.-nitroenamine.
    Type: Grant
    Filed: March 9, 1995
    Date of Patent: January 28, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Shinzo Seko
  • Patent number: 5596020
    Abstract: This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
    Type: Grant
    Filed: December 7, 1994
    Date of Patent: January 21, 1997
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Robert L. Morris, Kent W. Neuenschwander, Keith S. Learn, Anthony C. Scotese
  • Patent number: 5583020
    Abstract: This invention features permeability enhancer molecules, and methods, to increase membrane permeability of negatively charged polymers thereby facilitating cellular uptake of such polymers.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: December 10, 1996
    Assignee: Ribozyme Pharmaceuticals, Inc.
    Inventor: Sean Sullivan
  • Patent number: 5527945
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: June 18, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5504253
    Abstract: A method of making (R)-N- 1-(3-methoxyphenyl)ethyl!-3-(2-chlorobenzene)propanamine which involves reducing the appropriate amidyl or iminyl precursor with an appropriate reducing agent. The appropriate amidyl or iminyl precursor is made from a synthesis involving the use of (R)-3-methoxy-.alpha.-methylbenzylamine. A method of condensing a nitrile with a primary or secondary amine to form an imine involves the reaction of a nitrile with diisobutylaluminum hydride; and then reacting the resultant compound with a primary or secondary amine to form the imine. The process is especially useful for producing enantiomerically pure chiral imines, and, ultimately, amines. Typical such imines have the formula: ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, aryl and aralkyl.
    Type: Grant
    Filed: July 15, 1994
    Date of Patent: April 2, 1996
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Bradford C. VanWagenen, Thomas E. D'Ambra