2-position Is Unsubstituted Or Hydrocarbyl Substituted Only Patents (Class 548/239)
  • Patent number: 11549130
    Abstract: An object of the present invention is to provide an enzyme showing random transesterification ability, which is suitable for food applications. Provided is a random transesterification lipase having high heat resistance in oils and fats.
    Type: Grant
    Filed: December 27, 2018
    Date of Patent: January 10, 2023
    Assignee: AMANO ENZYME INC.
    Inventors: Hiroki Fujioka, Saki Norifune, Tatsuya Hamada, Tetsuya Takahashi, Yusuke Tanaka, Toru Katase
  • Patent number: 11220495
    Abstract: Provided are a compound of 3,3,3?,3?-tetramethyl-1,1?-spirobiindane-based bisoxazoline ligand, an intermediate, a preparation method and uses thereof. The compound of bisoxazoline ligand is a compound having a structure represented by formula I, or an enantiomer, a raceme, or diastereomer thereof. The bisoxazoline ligand can be prepared via a preparation scheme in which the cheap and easily available 6,6?-dihydroxyl-3,3,3?,3?-tetramethyl-1,1?-spirobiindane is used as a starting raw material and the compound represented by formula II serves as the key intermediate through a series of reactions. The new bisoxazoline ligand developed by the present application can be used in catalytic organic reaction, in particular as a chiral bisoxazoline ligand that is widely used in many asymmetric catalytic reactions of metal catalysis, and thus it has economic practicability and industrial application prospect.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: January 11, 2022
    Assignee: ZHEJIANG UNIVERSITY
    Inventors: Xufeng Lin, Haorui Gu, Weiye Sun
  • Patent number: 9174921
    Abstract: Process for coproduction of a vinyl ester of the formula R—C(O)O—CH?CH2 by transvinylation reaction of a carboxylic acid of the formula R—C(O)OH with a transvinylating reagent of the formula R1—C(O)O—CH?CH2, characterized in that (a) the transvinylation reaction is conducted continuously at a temperature of 90 to 160° C. and at a pressure of 0.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: November 3, 2015
    Assignee: OXEA GMBH
    Inventors: Leif Johnen, Heinz Strutz
  • Patent number: 9044512
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is more efficacious than traditional cationic lipids. The present invention employs amino alcohols to enhance the efficiency of in vivo delivery of siRNA.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: June 2, 2015
    Assignee: SIRNA THERAPEUTICS, INC.
    Inventors: Brian W. Budzik, Steven L. Colletti, Darla Danile Seifried, Matthew G. Stanton, Lu Tian
  • Publication number: 20150133431
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.
    Type: Application
    Filed: July 10, 2014
    Publication date: May 14, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventor: Gary C. Look
  • Patent number: 8969585
    Abstract: Provided is a process for producing an optically active compound represented by Formula (3): (wherein R1 is an alkyl group, an alkynyl group, an alkenyl group, an aliphatic heterocyclic group, a cycloalkyl group, an aryl group, an aralkyl group, or an aromatic heterocyclic group, and any hydrogen atom of R1 may be replaced with a substituent; R2 is a hydrogen atom or a group which is not reactive in the reaction below; and * represents a chiral center) or a salt thereof by subjecting a compound represented by Formula (1): (wherein R1 and R2 have the same meanings as defined in Formula (3)) to a ring closure reaction in the presence of a chiral ligand having 1 or more coordination sites, a Lewis acid represented by Formula (2): MmZn??(2) (wherein M is a metal ion, Z is a counter anion of M, and m and n are integers of 1 to 4), and a sulfonyl halide having an optionally substituted alkyl or phenyl group.
    Type: Grant
    Filed: January 31, 2012
    Date of Patent: March 3, 2015
    Assignee: Nagasaki University
    Inventors: Osamu Onomura, Yutaro Tsuda, Masami Kuriyama, Toshiharu Yanagi, Kazuya Kodama
  • Publication number: 20150057269
    Abstract: The present invention regards compositions and methods for the modulation of amidases capable of hydrolysing N-acylethanolamines useable in the therapy of inflammatory diseases. In particular, the present invention regards a compound of general formula (I): enantiomers, diastereoisomers, racemes and mixtures, polymorphs, salts, solvates thereof, wherein: (a) R is a linear alkyl radical having 13 to 19 carbon atoms or alkenyl radical having 13 to 19 carbon atoms carrying a double bond; (b) X is 0 or S; (c) Y is a 2 or 3 carbon atom alkylene residue, optionally substituted with one or two groups equal or different from each other and selected from among the group consisting of: —CH3, —CH2OH, —COOCH3, —COOH. Y may preferably be: —CH2—CH2—, —CH2—CH2—CH2—, CH(CH3)—CH2—, —CH2—CH(CH3)—, —CH2—C(CH3)2—, —CH2—CH(CH2OH)—, —CH2—C((CH2OH)2)—, —CH?CH—, —CH2—CH(COOCH3)—, —CH2—CH(COOH)—, for use as a medicine.
    Type: Application
    Filed: February 17, 2012
    Publication date: February 26, 2015
    Applicant: Epitech Group S.r.l.
    Inventors: Francesco Della Valle, Maria Federica Della Valle, Gabriele Marcolongo, Vincenzo Di Marzo, Salvatore Cuzzocrea
  • Publication number: 20150044346
    Abstract: The present invention relates to compounds based on an oxazoline moiety which liberate Strecker aldehydes under mild and controllable conditions. In addition the invention relates to food products comprising such compounds, and uses of such compounds.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 12, 2015
    Inventors: Imre Blank, Thomas Davidek, Ondrej Novotny, Peter Schieberle, Michael Granvogl
  • Publication number: 20140323739
    Abstract: The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
    Type: Application
    Filed: May 5, 2014
    Publication date: October 30, 2014
    Applicant: Eisai R&D Management Co.. Ltd.
    Inventors: Francis G. Fang, James E. Foy, Lynn Hawkins, Charles Lemelin, Andre LesCarbeau, Xiang Niu, Kuo-Ming Wu
  • Patent number: 8802863
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is more efficacious than traditional cationic lipids. The present invention employs amino alcohols to enhance the efficiency of in vivo delivery of siRNA.
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: August 12, 2014
    Assignee: Sirna Therapeutics, Inc.
    Inventors: Brian W. Budzik, Steven L. Colletti, Darla Danile Seifried, Matthew G. Stanton, Lu Tian
  • Publication number: 20140012011
    Abstract: The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
    Type: Application
    Filed: July 22, 2013
    Publication date: January 9, 2014
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Francis G. Fang, James E. Foy, Lynn Hawkins, Charles Lemelin, Andre LesCarbeau, Xiang Niu, Kuo-Ming Wu
  • Publication number: 20140012010
    Abstract: Provided is a process for producing an optically active compound represented by Formula (3): (wherein R1 is an alkyl group, an alkynyl group, an alkenyl group, an aliphatic heterocyclic group, a cycloalkyl group, an aryl group, an aralkyl group, or an aromatic heterocyclic group, and any hydrogen atom of R1 may be replaced with a substituent; R2 is a hydrogen atom or a group which is not reactive in the reaction below; and * represents a chiral center) or a salt thereof by subjecting a compound represented by Formula (1): (wherein R1 and R2 have the same meanings as defined in Formula (3)) to a ring closure reaction in the presence of a chiral ligand having 1 or more coordination sites, a Lewis acid represented by Formula (2): MmZn??(2) (wherein M is a metal ion, Z is a counter anion of M, and m and n are integers of 1 to 4), and a sulfonyl halide having an optionally substituted alkyl or phenyl group
    Type: Application
    Filed: January 31, 2012
    Publication date: January 9, 2014
    Inventors: Osamu Onomura, Yutaro Tsuda, Masami Kuriyama, Toshiharu Yanagi, Kazuya Kodama
  • Patent number: 8552204
    Abstract: Disclosed is a novel zinc cluster compound represented by general formula (1): Zn4O (OCOR)6 (RCOOH)n, wherein R represents an alkyl group which has 1 to 4 carbon atoms and may be substituted with a halogen atom, and n represents 0.1 to 1, and also disclosed are a method for producing the compound and a reaction using the compound.
    Type: Grant
    Filed: May 31, 2010
    Date of Patent: October 8, 2013
    Assignee: Takasago International Corporation
    Inventors: Yoshimasa Matsushima, Hideki Nara, Takahiro Fujiwara
  • Publication number: 20130012719
    Abstract: Azolines are oxidized in the presence of a copper-containing catalyst to azoles in the presence of molecular oxygen. A synthetic scheme converting azolines azoles is also provided.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: University of Southern California
    Inventors: Travis J. Williams, Anna C. Dawsey, Vincent Li, Kimberly C. Hamilton, Jianmei Wang
  • Patent number: 8314252
    Abstract: Processes for preparing oxazoline compounds are disclosed. These oxazoline compounds are useful intermediates in the preparation of Florfenicol and related compounds.
    Type: Grant
    Filed: July 28, 2009
    Date of Patent: November 20, 2012
    Assignees: Intervet Inc., Intervet International B.V.
    Inventors: Leo A. Paquette, James C. Towson
  • Patent number: 8299241
    Abstract: The present invention provides processes and intermediates for the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and salts thereof which are useful as serotonin-2C (5-HT2C) receptor agonists for the treatment of, for example, obesity.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: October 30, 2012
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Tawfik Gharbaoui, Sagun K. Tandel, You-An Ma, Marlon Carlos, John Robert Fritch
  • Publication number: 20120172601
    Abstract: Disclosed is a novel zinc cluster compound represented by general formula (1): Zn4O (OCOR)6 (RCOOH)n, wherein R represents an alkyl group which has 1 to 4 carbon atoms and may be substituted with a halogen atom, and n represents 0.1 to 1, and also disclosed are a method for producing the compound and a reaction using the compound.
    Type: Application
    Filed: May 31, 2010
    Publication date: July 5, 2012
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Yoshimasa Matsushima, Hideki Nara, Takahiro Fujiwara
  • Patent number: 8071609
    Abstract: This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: December 6, 2011
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
  • Publication number: 20110166359
    Abstract: Processes for preparing oxazoline compounds are disclosed. These oxazoline compounds are useful intermediates in the preparation of Florfenicol and related compounds.
    Type: Application
    Filed: July 28, 2009
    Publication date: July 7, 2011
    Inventors: Leo A. Paquette, James C. Towson
  • Publication number: 20110098479
    Abstract: The invention relates to a method for producing an azoline compound represented by the general formula (3): wherein R1 represents an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; R3, R4, R5 and R6 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted alkoxycarbonyl group, a halogen atom, a substituted amino group, a substituted carbamoyl group or an optionally substituted heterocyclic group; two arbitrary groups selected from R3, R4, R5 and R6 may bond to each other to form a ring; and Z1 represents an oxygen atom, a sulfur atom or a selenium atom; comprising reacting a carboxylic acid or a carboxylic acid derivative represented by the general formula (1): R1CO2R2 ??(1) wherein R
    Type: Application
    Filed: December 29, 2010
    Publication date: April 28, 2011
    Inventors: KAZUSHI MASHIMA, Takashi Ohshima, Takanori Iwasaki, Hironori Maeda, Kenya Ishida
  • Patent number: 7847031
    Abstract: A continuous process for the reactive compatibilization of polymers includes I. processing monooxazoline, bisoxazoline or a mixture thereof together with a first polymer, to give a reactive polymer; and II. adding the reactive polymer to one or more second polymers. In addition, a reactive polymer contains I. a first polymer; and II. at least 5% by weight of chemically unbound monooxazoline, bisoxazoline or a mixture thereof.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: December 7, 2010
    Assignee: Evonik Degussa GmbH
    Inventors: Marianne Omeis, Jürgen Szumigala, Jochen Stegemann
  • Publication number: 20100305316
    Abstract: The present invention provides processes and intermediates for the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and salts thereof which are useful as serotonin-2C (5-HT2C) receptor agonists for the treatment of, for example, obesity.
    Type: Application
    Filed: December 4, 2007
    Publication date: December 2, 2010
    Inventors: Tawfik Gharbaoui, Sagun K. Tandel, You-An Ma, Marlon Carlos, John Robert Fritch
  • Publication number: 20100305333
    Abstract: The present disclosure provides processes for the preparation of lipid conjugated cyclic carbonate derivatives. More specifically, the present disclosure is based on the finding that reacting lipids, such as, ceramides, with N,N?-disuccinimidyl derivative, resulted in the formation of, isolatable, substituted cyclic [1,3]-dioxan-2-one and [1,3]-dioxan-2-thione compounds. These isolatable cyclic substituted compounds and derivatives thereof may be used for various applications, such as in vaccination.
    Type: Application
    Filed: May 11, 2008
    Publication date: December 2, 2010
    Applicants: BIOLAB LTD., NASVAX LTD., YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
    Inventors: Aaron Garzon, Jean Hildesheim
  • Patent number: 7671213
    Abstract: Optically active bisoxazoline compounds represented by the general formula (1), a process for producing the compounds, and a process for producing cyclopropanecarboxylic esters by using the same: wherein R1 and R2 are the same and each represents C1-6 alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted phenyl or R1 and R2 are bonded each other together with the carbon atom of oxazoline ring to which they are bonded to form a ring; R3 is substituted or unsubstituted naphthyl; R4 and R5 are the same and each represent hydrogen or C1-6 alkyl, or R4 and R5 are bonded each other together with the carbon atom to which they are bonded to form a cycloalkyl ring having 3 to 6 carbon atoms; and * represents an asymmetric center.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: March 2, 2010
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Makoto Itagaki, Katsuhisa Masumoto
  • Publication number: 20100048909
    Abstract: An objective of the present application is to provide an industrially practicable method for producing an optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof from an inexpensive easily-available starting material. The derivative or salt thereof is useful as an intermediate for a medicine. It is also intended by the present application to provide a useful intermediate of the derivative. The objective is attained by the following method. First, an easily-available 2-halo-3-oxopropionic acid derivative is asymmetrically reduced, and then epoxidated to produce an optically-active epoxycarboxylic acid derivative. Next, the derivative is converted into an optically-active epoxyamide derivative by reaction with cyclopropylamine, and then reacted with a nitrile to obtain an optically-active oxazolinamide derivative. Subsequently, selective acid solvolysis of the oxazoline skeleton gives the optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof.
    Type: Application
    Filed: May 22, 2007
    Publication date: February 25, 2010
    Inventors: Kohei Mori, Akira Nishiyama, Naoaki Taoka, Daisuke Moriyama, Nobuo Nagashima
  • Patent number: 7642303
    Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: January 5, 2010
    Inventors: Thomas L. Shakely, James John Krutak
  • Publication number: 20090291923
    Abstract: The invention provides novel trioxane dimers having formulae III, IV or V: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer and/or malaria using these compounds and compositions.
    Type: Application
    Filed: November 17, 2006
    Publication date: November 26, 2009
    Applicants: Johns Hopkins Universoty, The Government of the United States of America as Represented by the Secretary of the DHHS NIH, Offi
    Inventors: Gary H. Posner, Ikhyeon Paik, Kristina Borstnik, Wonsuk Chang, Sandra Sinishtaj, William Malo, John Gaetano D'Angelo, Lauren Elaine Woodard, Alvin Solomon Kalinda, Aimee R. Usera, Lindsey Catherine Hess, Andrew Scott Rosenthal, Seongho Oh, Astrid C. Baege
  • Publication number: 20090281309
    Abstract: The present invention is a method for producing a 2-oxazoline analogue or a 1,3-oxazine analogue represented by the following general formula (3) by reacting a 1,2-aminoalcohol compound or a 1,2-aminothiol compound with an ?,?-dihaloamine compound. (In the formula, n represents 0 or 1, and R represents an oxygen atom or a sulfur atom. R1, R2 and R3 each represents an atom or a group shown in Group 1 to Group 3, and R0 represents an atom or a group shown in Group 2 or Group 3. Two or more of R1, R2 and R3 may be bonded to each other to form a ring.
    Type: Application
    Filed: August 30, 2006
    Publication date: November 12, 2009
    Inventors: Shoji Hara, Tsuyoshi Fukuhara, Toshio Hidaka
  • Publication number: 20090274637
    Abstract: The invention relates to the cosmetic use of at least one oxazolin as a depigmenting active ingredient in a depigmenting composition, and to the associated cosmetic treatment method. The invention also relates to the use of at least one oxazolin for preparing an active medicament as a depigmenting agent, and to a depigmenting cosmetic composition comprising at least one oxazolin as a depigmenting active ingredient.
    Type: Application
    Filed: April 27, 2006
    Publication date: November 5, 2009
    Inventors: Philippe Msika, Nathalie Piccardi
  • Patent number: 7582780
    Abstract: The invention relates to a method of separating and isolating an acylated derivative of 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile by reaction of a mixture of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile and an acylated derivative thereof with a compound which form a derivative of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile containing a carboxylic acid group. The acylated derivative containing a carboxylic acid group precipitates once it is formed and may easily be separated from the reaction mixture.
    Type: Grant
    Filed: February 2, 2005
    Date of Patent: September 1, 2009
    Assignee: H. Lundbeck A/S
    Inventor: Lars Ole Lyngso
  • Patent number: 7507830
    Abstract: Methods are provided for the construction of unsymmetrical biaryl compounds and alkylated aromatic compounds from arylnitriles using a nickel or palladium catalyzed coupling in which the catalyst has at least one phosphine or phosphite ligand.
    Type: Grant
    Filed: September 23, 2004
    Date of Patent: March 24, 2009
    Assignee: Pharmacore, Inc.
    Inventor: Joseph A. Miller
  • Publication number: 20090045373
    Abstract: There are provided compounds represented by formula (I): in which R1 is F, Cl, —N(R5)2 or —CN and Q+ is selected among various organic cations that include an heterocyle. These compounds are useful as electrolytes, ionic liquids or molten salts.
    Type: Application
    Filed: March 9, 2007
    Publication date: February 19, 2009
    Inventors: Amer Hammami, Benoit Marsan
  • Publication number: 20090043096
    Abstract: A method of producing an aromatic compound of the following formula (3) comprising reacting a compound of the following formula (1) with an olefin compound of the following formula (2) in the presence of a transition metal complex: (wherein, an Ar1 ring represents an aromatic hydrocarbon ring or aromatic heterocyclic ring, an Ar2 ring represents a heterocyclic ring containing X1 and N*, and the X1 represents a nitrogen atom or carbon atom and the N represents a nitrogen atom connecting via a double bond to either one of two adjacent atoms in the Ar2 ring.) (wherein, R1, R2, R3 and R4 represent each independently a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms.) (wherein, Ar1, Ar2, X1, N*, R1, R2 and R3 represent the same meanings as described above.).
    Type: Application
    Filed: February 2, 2007
    Publication date: February 12, 2009
    Applicants: SUMITOMO CHEMICAL COMPANY, LIMITED, OSAKA UNIVERSITY
    Inventors: Fumitoshi Kakiuchi, Yusuke Matsuura, Masato Ueda
  • Publication number: 20080217580
    Abstract: The present invention relates to compounds of formula (I) a process for their production and to their use for coloring high molecular weight organic materials, as fluorescent tracers, in solid dye lasers, EL lasers, in EL devices and lighting. The compounds of formula I show unique broadband luminescence in visible region.
    Type: Application
    Filed: April 11, 2005
    Publication date: September 11, 2008
    Inventors: Junichi Tanabe, Hiroshi Yamamoto, Norihisa Dan
  • Publication number: 20080161331
    Abstract: The present invention relates to compounds comprising an oxazoline or thiazoline moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, (I), wherein A1 is CH C(CH3) or N; R1 is hydrogen or halogen; R2 is (II); A2 is O or S; R3 is hydrogen, halogen, C1-4 alkyl or C1-4 alkoxy; R4 is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or —O—(CH2)n-NR12aR each CH2 in —O—(CH2)n-NR12aR 12b being optionally substituted by one or two C1-4 alkyl; R5 is hydrogen or —O—(CH2)m—NR13aR13b, each CH2 in —O—(CH2)m—NR13aR13b being optionally substituted by one or two C1-4 alkyl, and at least one of R4 and R5 should be a —O—(CH2)n-NR12/13aR12/13b group.
    Type: Application
    Filed: March 29, 2006
    Publication date: July 3, 2008
    Applicant: UCB PHARMA, S.A.
    Inventors: Regorius Leurs, Henkdrik Timmerman, Sylvain Celanire, Patrice Talaga, Frederic Denonne, Florence Lebon
  • Patent number: 7288674
    Abstract: Optically active bisoxazoline compounds represented by the general formula (1), a process for producing the compounds, and a process for producing cyclopropanecarboxylic esters by using the same: wherein R1 and R2 are the same and each represents C1-6 alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted phenyl or R1 and R2 are bonded each other together with the carbon atom of oxazoline ring to which they are bonded to form a ring; R3 is substituted or unsubstituted naphthyl; R4 and R5 are the same and each represent hydrogen or C1-6 alkyl, or R4 and R5 are bonded each other together with the carbon atom to which they are bonded to form a cycloalkyl ring having 3 to 6 carbon atoms; and * represents an asymmetric center.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: October 30, 2007
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Makoto Itagaki, Katsuhisa Masumoto
  • Patent number: 7271268
    Abstract: The present invention provides a novel process for preparing [1-(mercaptomethyl)cyclopropyl]acetic acid with high purity and related derivatives.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: September 18, 2007
    Assignee: Formosa Laboratories Inc.
    Inventors: Rung-Tian Suen, Yu-Liang Liu, Ching-Peng Wei
  • Patent number: 7115758
    Abstract: The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.
    Type: Grant
    Filed: November 26, 2002
    Date of Patent: October 3, 2006
    Assignee: Schering AG
    Inventors: Andreas Steinmeyer, Katica Schwarz, Claudia Giesen, Martin Haberey, Marianne Fähnrich
  • Patent number: 6835831
    Abstract: Disclosed is a method of preparing a composition comprising a compound represented Structural Formula (I): The method comprises the step of reacting an aldehyde compound R10CHO with an isonitrile compound represented by Structural Formula (II):
    Type: Grant
    Filed: November 26, 2002
    Date of Patent: December 28, 2004
    Assignee: Genzyme Corporation
    Inventor: Bradford H. Hirth
  • Patent number: 6794516
    Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.
    Type: Grant
    Filed: February 7, 2003
    Date of Patent: September 21, 2004
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: François Soucy, Louis Plamondon, Mark Behnke, William Roush
  • Patent number: 6642218
    Abstract: The invention relates to vitamin D derivatives of formula (I), processes for the production thereof and uses thereof: wherein Y1, Y2, R1-R6, Q and Z are as defined herein.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: November 4, 2003
    Assignee: Schering Aktiengesellschaft
    Inventors: Andreas Steinmeyer, Gerald Kirsch, Günter Neef, Katica Schwarz, Ruth Thieroff-Ekerdt, Herbert Wiesinger, Martin Haberey, Marianne Fahnrich
  • Patent number: 6613920
    Abstract: The invention relates to vitamin D derivatives of formula (I), processes for the production thereof and uses thereof: wherein Y1, Y2, R1—R6, Q and Z are as defined herein.
    Type: Grant
    Filed: October 25, 2000
    Date of Patent: September 2, 2003
    Assignee: Schering Aktiengesellschaft
    Inventors: Andreas Steinmeyer, Gerald Kirsch, Günter Neef, Katica Schwarz, Ruth Thieroff-Ekerdt, Herbert Wiesinger, Martin Haberey, Marianne Fahnrich
  • Patent number: 6600058
    Abstract: The invention concerns new vitamin D derivatives of general formula (I) a process for their production, their use for production of medicaments, and intermediate products used in the process.
    Type: Grant
    Filed: October 25, 2000
    Date of Patent: July 29, 2003
    Assignee: Schering Aktiengellschaft
    Inventors: Andreas Steinmeyer, Gerald Kirsch, Günter Neef, Katica Schwarz, Ruth Thieroff-Ekerdt, Herbert Wiesinger, Martin Haberey, Marianne Fahnrich
  • Patent number: 6583292
    Abstract: Described herein is a method for preparing an ester by (a) admixing a compound having the formula I: with a base to form an intermediate, and (b) admixing the intermediate produced in step (a) with a compound composed of an alcohol, an alkoxide, or a combination thereof, wherein steps (a) and (b) are performed in situ.
    Type: Grant
    Filed: February 6, 2002
    Date of Patent: June 24, 2003
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Hariharan Venkatesan, Laura Captain, Michael V. Voronkov, James P. Snyder, Marcus A. Schestopol
  • Patent number: 6545030
    Abstract: 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.
    Type: Grant
    Filed: January 17, 2002
    Date of Patent: April 8, 2003
    Assignee: Warner-Lambert Company
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Haile Tecle, Lu-Yan Zhang
  • Patent number: 6498256
    Abstract: Compounds of formulae I and Ia, wherein X1 is secondary phosphino; R3 is hydrogen, a hydrocarbon radical having from 1 to 20 carbon atoms, a heterohydrocarbon radical, bonded via a carbon atom, having from 2 to 20 atoms and at least one hetero atom selected from the group O, S and NR, or ferrocenyl; R is H or C1-C4alkyl; each R4 individually or both R4 together are a hydrocarbon radical having from 1 to 20 carbon atoms; and R01 and R02 are each independently of the other a hydrogen atom or a hydrocarbon radical having from 1 to 20 carbon atoms, are chiral ligands for metal complexes with metals of sub-groups I and VII, which are catalysts for asymmetric addition reactions, for example of hydrogen, to prochiral unsaturated organic compounds.
    Type: Grant
    Filed: September 20, 2001
    Date of Patent: December 24, 2002
    Assignee: Solvias AG
    Inventors: Andreas Pfaltz, Joerg R. Blankenstein, Frederik Menges
  • Patent number: 6486196
    Abstract: The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).
    Type: Grant
    Filed: May 4, 2001
    Date of Patent: November 26, 2002
    Assignee: Dr. Reddy's Research Foundation
    Inventors: Srinivas Nanduri, Sairam Pothukuchi, Sriram Rajagopal, Venkateswarlu Akella, Sunilkumar Bhadramma Kochunarayana Pillai, Ranjan Chakrabarti
  • Patent number: 6476232
    Abstract: A 4-(2-amino-1-hydroxyethyl)oxazoline derivative of the formula [XIII] and a method for producing the same, in which R4 is an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl or an optionally substituted heteroarylalkyl, and R6 and R7 are the same or different and each is a hydrogen atom, an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl or an optionally substituted aralkyl, or R6 and R7 combinedly form, together with the adjacent nitrogen atom, a hetero ring, the hetero ring being optionally substituted by halogen atom, alkyl, alkenyl, alkoxy, amino, alkoxycarbonyl, carboxamide or alkyl-substituted carbamoyl, an enantiomer thereof or a salt thereof.
    Type: Grant
    Filed: October 26, 2001
    Date of Patent: November 5, 2002
    Assignees: Japan Tobacco Inc., Agouron Pharmaceuticals, Inc.
    Inventors: Takashi Inaba, Yasuki Yamada
  • Patent number: 6472534
    Abstract: Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: October 29, 2002
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Bennett C. Borer, Scott E. Zook, Juliette K. Busse
  • Publication number: 20020086892
    Abstract: The present invention relates to novel biphenyloxazolines of the formula (I) 1
    Type: Application
    Filed: August 23, 1999
    Publication date: July 4, 2002
    Inventors: UDO KRAATZ, WOLFGANG KRAMER, ALBRECHT MARHOLD, CHRISTOPH ERDELEN, ULRIKE WACHENDORFF-NEUMANN, ANDREAS TURBERG, NORBERT MENCKE