Abstract: The invention relates to intermediate products and a new process for the production of benzocycloheptene C. The process for the production of its new intermediate products according to the invention starts from economical starting materials, provides the intermediate stages in high yields and high purity, without chromatographic purification steps, and allows production on an industrial scale.
Type:
Grant
Filed:
October 15, 2002
Date of Patent:
January 22, 2008
Assignee:
Schering Aktiengesellschaft
Inventors:
Johannes Platzek, Wolfgang Beckmann, Jens Geisler, Holger Kirstein, Ulrich Niedballa, Eckhard Ottow, Sigmar Radau, Claudia Schulz, Thomas Wessa
Abstract: The invention relates to a process for the reduction of compounds comprising a carbon-carbon (C?C), carbon-oxygen (C?O), or carbon-nitrogen (C?N) double bond, to a corresponding hydrogenated alkane, alcohol or amine, comprising contacting a compound comprising the C?C, C?O or C?N double bond with a hydrogen donor solvent and a catalyst comprising a metal complex having a tridentate aminodiphosphine ligand under transfer hydrogenation conditions.
Abstract: The present invention relates to method(s) of treating a subject afflicted with cancer or a precancerous condition, an inflammatory disease or condition, and/or stroke or other ischemic disease or condition, the method comprising administering to the subject or patient in need a composition comprising a therapeutically effective amount of a substituted cis or trans-stilbene.
Abstract: Monocyclic and bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein Gn, Jn, R3, R8, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.
Type:
Application
Filed:
March 27, 2007
Publication date:
October 4, 2007
Inventors:
Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia
Abstract: The present invention relates to trans-derivatives of formula wherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.
Type:
Application
Filed:
March 23, 2007
Publication date:
October 4, 2007
Inventors:
Christophe Grundschober, Patrick Schnider
Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
Type:
Grant
Filed:
September 15, 2004
Date of Patent:
August 14, 2007
Assignee:
Schering Corporation
Inventors:
Dimitri A. Pissarntiski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
Abstract: The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them.
Abstract: The present invention relates generally to amino acid derivatives and to methods of making the same. In particular, the invention relates to compounds bearing a stereochemical identity, that is, the same stereochemistry, with the chiral ?-carbon of D-?-amino acids and their use in methods of therapy, including the treatment of inflammatory diseases, and to compositions and enantiomeric mixtures containing them.
Type:
Grant
Filed:
July 24, 2001
Date of Patent:
August 7, 2007
Assignee:
The University of Queensland
Inventors:
Robert C Reid, Christopher I Clark, Karl Hansford, Martin J Stoermer, Ross P McGeary, David P Fairlie, Karl Schafer
Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
Type:
Grant
Filed:
September 16, 2005
Date of Patent:
July 24, 2007
Assignee:
Massachusetts Institute of Technology
Inventors:
Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
Type:
Grant
Filed:
January 11, 2002
Date of Patent:
June 26, 2007
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
Type:
Grant
Filed:
February 5, 2003
Date of Patent:
April 24, 2007
Assignees:
Schering Corporation, Pharacopeia Drug Discovery, Inc.
Inventors:
Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
Abstract: To provide a liquid crystalline compound capable of exhibiting a biaxial liquid crystal phase, provide a trifunctional or greater functional polymerizable liquid crystalline compound having polymerizable groups, and also to provide a liquid crystalline composition and a retardation film which are using the liquid crystalline compound, a compound and a liquid crystalline compound each are represented by formula (I) defined in the specification; a liquid crystalline composition contains the compound; and a retardation film has an optically anisotropic layer formed from the compound.
Abstract: The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonist and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below.
Type:
Grant
Filed:
November 25, 2003
Date of Patent:
January 23, 2007
Assignee:
Pfizer, Inc.
Inventors:
Robert L. Dow, Kevin K. Liu, Bradley P. Morgan, Andrew G. Swick
Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
Type:
Grant
Filed:
December 6, 2005
Date of Patent:
December 12, 2006
Assignee:
H. Lundbeck A/S
Inventors:
Thomas Ruhland, Benny Bang-Andersen, Ask Puschl
Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
Type:
Grant
Filed:
December 6, 2005
Date of Patent:
November 21, 2006
Assignee:
H. Lundbeck A/S
Inventors:
Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
Abstract: The present invention relates to novel heterocyclyl-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
Type:
Grant
Filed:
February 9, 2004
Date of Patent:
October 31, 2006
Assignee:
Abbott Laboratories
Inventors:
Gary T. Wang, Sheldon Wang, Robert Gentles
Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.
Abstract: This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1–R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
Type:
Grant
Filed:
September 6, 2002
Date of Patent:
September 12, 2006
Assignee:
Euro-Celtique S.A.
Inventors:
Bin Shao, R. Richard Goehring, Samuel F Victory, Qun Sun
Abstract: The present invention relates to sulfones that are useful in the treatment of chemokine-mediated disorders. In certain embodiments, the present invention concerns the compounds that are MCP-1 receptor antagonists.
Type:
Grant
Filed:
May 21, 2003
Date of Patent:
June 27, 2006
Assignee:
Warner-Lambert Company, LLC
Inventors:
Larry D. Bratton, Alexander J. Bridges, David T. Connor, Steven R. Miller, Yuntao Song, Kuai-Lin Sun, Bharat K. Trivedi, Paul C. Unangst
Abstract: This invention encompasses novel methods of preparing sulfinamides and sulfoxides, particularly stereomerically pure sulfinamides and sulfoxides. The invention further encompasses novel compounds from which sulfinamides and sulfoxides can be prepared.
Type:
Grant
Filed:
April 12, 2002
Date of Patent:
June 20, 2006
Assignee:
Apsinterm LLC
Inventors:
Chris Hugh Senanayake, Zhengxu Han, Dhileepkumar Krishnamurthy, Derek Pflum, Harold Scott Wilkinson
Abstract: A process for preparing compounds of the formula (II), where the substituents R1 to R5 are each independently H, CH3, straight-chain or branched C1–C8-alkyl, CH(OC1–C5-alkyl)2, CH(C1–C5-alkyl)(OC1–C5-alkyl), CH2(OC1–C5-alkyl), CH(CH3)(OC1–C5-alkyl), C1–C8-alkoxy, N(C1–C5-alkyl)2, phenyl, substituted phenyl, aryl, heteroaryl, S(C1–C5-alkyl) or a radical Caryl, alkyl, and the symbols X1 to 5 are each carbon or a maximum of two neighboring X1-5 are nitrogen or X1R1 and X2R2 together are O, NH, N(C1–C5-alkyl), N(C?O—C1–C5-alkyl), N(SiR3)2 or S, or where neighboring radicals R1 to R5 form the following structural unit, where X6 to X9 and R6 to R9 have the same meaning as X1 to X5 and R1 to R5 which comprises reacting chloro- or fluoroaromatics of the formula (I) with carbon electrophiles and lithium metal.
Type:
Grant
Filed:
October 2, 2003
Date of Patent:
April 4, 2006
Assignee:
Clariant GmbH
Inventors:
Andreas Meudt, Michael Erbes, Klaus Forstinger
Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
Type:
Grant
Filed:
May 11, 2004
Date of Patent:
March 7, 2006
Assignee:
Wyeth
Inventors:
John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.
Type:
Grant
Filed:
April 11, 2003
Date of Patent:
November 8, 2005
Assignee:
Warner-Lambert Company, LLC
Inventors:
Robert Lee Bosch, Richard Joseph McCabe, Thomas Norman Nanninga, Robert Joseph Stahl
Abstract: A composition for use as an antiobestic agent and preventive or therapeutic agent for diabetes, containing a compound of the formula (I): wherein, A is substituted aryl or substituted heteroaryl with one or more group(s); (here, one of following groups is at least contained as the substituent: —RA—RB (RA is S, SO, SO2, NRC, NRCSO2 (RC is hydrogen or lower alkyl) or lower alkylene); RB is optionally substituted aryl); X is O, S, NR wherein R is hydrogen or lower alkyl, or single bond; m is an integer of 0 to 4; n is an integer of 1 to 6 p is an integer of 1 to 3, pharmaceutically acceptable salt, prodrug or hydrate thereof.
Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
Type:
Grant
Filed:
April 22, 2003
Date of Patent:
September 20, 2005
Assignee:
Massachusetts Institute of Technology
Inventors:
Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
Abstract: The invention relates to a process for the manufacture of a compound of formula or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element represents —CH2—CH2— or —CH?CH— and R represents a cyclic radical.
Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.
Type:
Grant
Filed:
February 20, 2001
Date of Patent:
May 31, 2005
Assignee:
AstraZeneca AB
Inventors:
David Cheshire, Stephen Connolly, David Cox, Antonio Mete
Abstract: The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX?) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.
Type:
Grant
Filed:
January 4, 2001
Date of Patent:
April 19, 2005
Assignee:
Ferrer Internacional, S.A.
Inventors:
Rafael Foguet, Jorge Ramentol, Diego Fernandez-Cano, Miguel P. Armengol, Inés Petschen, Juan Sallares, Francesc X. Camps, Manuel M. Raga, Josep M. Castello
Abstract: The present invention relates to the compounds of the general formula (I), a composition for and a method of treating breast cancer or other proliferative disorders in a subject using a compound of general formula [I], wherein the substituents are as defined in the specification.
Type:
Grant
Filed:
August 20, 2002
Date of Patent:
March 8, 2005
Inventors:
Gloria L. Anderson, Tawfeq Abdul-Raheem Kaimari
Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
Abstract: A process for preparing a compound of the formula: wherein n, R1, R2, R3 and X are as defined above, used as an intermediate in the synthesis of ?-adrenergic receptor agonists.
Abstract: The present invention relates to a class of compounds represented by the Formula 1.
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula 1, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or the &agr;v&bgr;5 integrin.
Type:
Grant
Filed:
September 9, 2003
Date of Patent:
December 21, 2004
Assignee:
Pharmacia Corporation
Inventors:
Thomas Rogers, Michael Clare, Hwang-Fun Lu, Mark Russell, James W. Malecha, Ish Kumar Khanna, Thomas Penning, Srinivasan Raj Nagarajan
Abstract: Compounds of formula (I), wherein the substituents R1, R2, R3, R4 and Z and the suffixes n and m are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomers of those compounds are suitable for use as herbicides.
Type:
Application
Filed:
July 14, 2004
Publication date:
December 9, 2004
Inventors:
Jurgen Schaetzer, Martin Eberle, Jean Wenger, Sabine Berteina-Raboin, Kurt Nebel, Andre Stoller, Roger Graham Hall, Steven Scott Bondy, Daniel Dennis Comer, Julie Elizabeth Penzotti, Peter Diederik Jan Grootenhuis
Abstract: Novel agents acting as co-factors for replacement of NAD(P)+/NAD(P)H co-enzyme systems in enzymatic oxido-reductive reactions. Agents mimicking the action of NAD(P)+/NAD(P)H system in enzymatic oxidation/reduction of substrates into reduced or oxidized products. A method for selection and preparation of the mimicking agents for replacement of NAD(P)+/NAD(P)H system and a device comprising co-factors for replacement of NAD(P)+/NAD(P)H system.
Type:
Application
Filed:
December 6, 2003
Publication date:
November 25, 2004
Inventors:
Richard H. Fish, John B. Kerr, H. Christine Lo
Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
Type:
Grant
Filed:
June 29, 2001
Date of Patent:
November 16, 2004
Assignees:
Paratek Pharmaceuticals, Inc., Trustees of Tufts College
Inventors:
Mark L. Nelson, Roger Frechette, Peter Viski, Beena Bhatia, David Messersmith
Abstract: The present invention provides various processes for the preparation of (R)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol.
Type:
Application
Filed:
May 4, 2004
Publication date:
October 21, 2004
Applicants:
Aventis Pharmaceuticals Inc., Aventis Pharma Deutschland GmbH
Inventors:
Thomas Heinz Eduard Hilpert, Hans-Wolfram Flemming, Sandra K. Stolz-Dunn, Jonathan C. Evans, Ian A. Tomlinson
Abstract: The invention relates to the use of chiral sulfamic acids as resolving agents, the sulfamic acid having the formula (R1, R2?) N—SO3H, ?wherein: R1 and R2, ?being the same or different, represent a hydrogen atom or a C1-C30 linear, branched or cyclic (hetero)-aliphatic or (hetero)-aromatic group, provided that R1 ?and R2 are not both hydrogen and that at least one of the R1 and R2 groups is chiral. Further, methods for resolving enantiomeric mixtures are disclosed.
Type:
Application
Filed:
May 6, 2004
Publication date:
September 23, 2004
Inventors:
Alan Arthur Smith, Franciscus Wilhelmus Petrus Damen, George Johannes Theodorus Kuster
Abstract: This invention relates to aryl substituted pyridines of Formula I:
or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1-R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, including diabetic neuropathy, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, and as antiarrhythmics.
Abstract: The present invention relates to a fungicide containing a novel benzoylpyridine derivative or its salt.
The present invention provides a fungicide containing a benzoylpyridine derivative represented by the formula (I) or its salt:
wherein X is a halogen atom, a nitro group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable hydrocarbon group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group; n is 1, 2, 3 or 4; R1 is a substitutable alkyl group; R2 is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group; and m is 1, 2, 3 or 4, provided that when m is at least 2, R2 may contain an oxygen atom to form a condensed ring.
Abstract: Compositions, methods of use, isolation and biosynthesis of diimino-piperazine derivatives useful for the modification of sphingolipid metabolism and other biological functions are described. The preferred derivative is 2,6-bis-(&ohgr;-aminobutyl)-3,5-diimino-piperazine. This is a naturally occurring biochemical compound isolated from cells. The diimino-piperazine derivatives are useful as therapeutic agents when administered to patients to treat diseases and disorders involving cell regulation.
Type:
Grant
Filed:
February 3, 2003
Date of Patent:
June 15, 2004
Assignee:
Emory University
Inventors:
Alfred H. Merrill, Jr., Lisa Warden, Dennis C. Liotta
Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.
Type:
Grant
Filed:
November 28, 2001
Date of Patent:
June 15, 2004
Assignee:
Shin-Etsu Chemical Co., Ltd.
Inventors:
Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
Abstract: Novel pyridine-based thyroid receptor ligands are provided which have the general formula I
wherein:
X is oxygen (—O—), sulfur (—S—), sulfoxide (—S(O)—), sulfonyl (—SO2—), CR8R8 or NR8;
Y is —NR8, oxygen (—O—), —CH2— or sulfur (—S—);
Z is a bond or substituted or unsubstituted C1-4 alkyl; and
wherein the substituents are as described herein.
In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
Type:
Grant
Filed:
May 7, 2003
Date of Patent:
June 8, 2004
Assignee:
Bristol-Myers Squibb Company
Inventors:
Minsheng Zhang, Jon Hangeland, Yolanda Caringal, Todd Friends
Abstract: A process for producing an organotitanium compound capable of regioselectively converting a substituted acetylene compound into polysubstituted benzene or polysubstituted pyridine. The process comprises reacting an acetylene compound represented by the formula (1)
[where R1 and R2 denote a C1-20 alkyl group or the like] in the presence of a prescribed titanium compound and a Grignard reagent with a compound represented by the formula (4)
[where R3 and R4 denote a hydrogen atom or the like] and further reacting with a compound represented by the formula (5)
[where R5 denotes a hydrogen atom or the like, Z denotes CR′ (where R′ denotes a hydrogen atom or the like), nitrogen atom, X6 denotes a halogen atom or the like, and m is 0 or 1]
thereby giving the titanium compound represented by the formula (6) and/or (7).
Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.
Type:
Grant
Filed:
October 25, 2002
Date of Patent:
April 27, 2004
Inventors:
Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanadan E. Velu
Abstract: A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough: 1
Abstract: An object of the present invention is to provide a process for producing 2-(4-pyridyl)ethanethiol easily.
According to the invention, 4-vinylpyridine is reacted with thiourea in an aqueous medium containing an acid to form a solution containing an isothiuronium salt and then the solution is made alkaline to convert the isothiuronium salt into 2-(4-pyridyl)ethanethiol.
Abstract: The present invention relates to a class of compounds represented by the Formula 1.
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula 1, and methods of selectively inhibiting or antagonizing the &agr;V&bgr;3 and/or the &agr;V&bgr;5 integrin.
Type:
Grant
Filed:
June 15, 2001
Date of Patent:
April 13, 2004
Assignee:
Pharmacia Corporation
Inventors:
Thomas Rogers, Michael Clare, Hwang-Fun Lu, Mark Russell, James W. Malecha, Ish Kumar Khanna, Thomas Penning, Srinivasan Raj Nagarajan, Heather Stenmark