Abstract: N-heterocyclic (“NHC”) carbenes and NHC carbene-metal complexes. The NHC carbene having a formula: wherein R1 is an aromatic or aliphatic group, and R2 is an aromatic or aliphatic group, R3 is a fluorinated alkyl chain, R4 is a fluorinated alkyl chain or a proton.
Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.
Abstract: The present invention relates to novel imidazoline derivatives and their use as insecticidal, acaricidal, molluscicidal and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests. A compound of formula (I): and the salts and N-oxides thereof.
Type:
Grant
Filed:
October 24, 2008
Date of Patent:
July 30, 2013
Assignee:
Syngenta Crop Protection LLC
Inventors:
Christoph Luethy, Anthony Cornelius O'Sullivan, Thomas Pitterna, Jurgen Harry Schaetzer
Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.
Abstract: The disclosure provides new methods for preparing nitrogen-containing amphiphiles and their use in the preparation of liposomes and other lipid-containing carriers of pharmaceutical substances, including nucleic acids used in gene therapy.
Abstract: The present invention relates to novel imidazoline derivatives and their use as insecticidal, acaricidal, mollus and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests. A compound of formula (I): and the salts and N-oxides thereof.
Type:
Application
Filed:
October 24, 2008
Publication date:
April 28, 2011
Applicant:
SYNGENTA CROP PROTECTION, INC.
Inventors:
Christoph Luethy, Anthony Cornelius O'Sullivan, Thomas Pitterna, Jurgen Harry Schaetzer
Abstract: The invention relates to novel imidazolinium salts, to processes for preparation thereof and to the use of the imidazolinium salts or of a mixture of imidazolinium salts with further (lubricating) substances as lubricants.
Type:
Application
Filed:
December 18, 2008
Publication date:
July 2, 2009
Inventors:
Peter SCHWAB, Hans-Juergen Koehle, Thomas Salomon, Kerstin Hell
Abstract: The present invention relates to compounds of formula I wherein X—Y, R1, and n are as defined herein and to their pharmaceutically active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
Type:
Application
Filed:
June 25, 2008
Publication date:
January 15, 2009
Inventors:
Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
Abstract: The present invention provides novel compounds possessing antibacterial, and/or antifungal activities. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
Type:
Grant
Filed:
September 18, 2003
Date of Patent:
November 28, 2006
Assignee:
Genelabs Technologies, Inc.
Inventors:
Janos Botyanszki, Dong-Fang Shi, Christopher Don Roberts, Mikail Hakan Gezginci, Stephen Corey Valdez, Sherwin Sattarzadeh
Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-?B as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 ?m/mL.
Type:
Grant
Filed:
January 17, 2003
Date of Patent:
April 12, 2005
Assignee:
Board of Trustees of Michigan State University
Inventors:
Jetze J. Tepe, Satyamaheshwar Peddibhotla
Abstract: The present invention discloses novel substituted aryl alkylamine compounds of Formula (I) or pharmaceutically acceptable salts thereof which have selective histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat obesity and other histamine H3 receptor-related diseases.
Type:
Application
Filed:
September 18, 2003
Publication date:
June 10, 2004
Inventors:
Lisa Selsam Beavers, Robert Alan Gadski, Philip Arthur Hipskind, Craig William Lindsley, Karen Lynn Lobb, James Arthur Nixon, Richard Todd Pickard, John Mehnert Schaus, Takako Takakuwa, Brian Morgan Watson
Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I, Formula (I) wherein R1 is (C1-3)alkyloxy, (C1-3)alkyloxy(C1-3)alkyl, (C1-3)alkylthio, (C1-3)alkylthio(C1-3)alkyl, (C1-3)alkylsulfinyl, (C1-3)alkylsulfinyl(C1-3)alkyl, (C1-3)alkylsulfonyl, (C1-3)alkylsulfonyl(C1-3)alkyl, (C1-3)alkyloxycarbonyl, (CH2)n—CO—NR8R9? or (CH2)n—NR8R9?; n is 0, 1 or 2; R2 is hydrogen or (C1-3?)alkyl; R3 is (C1-3)alkyl or (C1-3)alkyloxy(C1-3?)alkyl; R4 is (C1-3)alkyloxy(C1-3)alkyl; or R3 and R4 form together with the nitrogen atom to which they are bound a 5-, 6-, or 7-membered ring, optionally containing a further heteroatom selected from O and S, and which ring may optionally contain a double bond and be optionally substituted with (C1-3)alkyl or (C1-3)alkyloxy; R5 and R6 are independently (C1-3)alkyl; R7 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R8 and R9 are independently (C1-3)alkyl; or R8 and R9 form together with
Type:
Application
Filed:
July 18, 2003
Publication date:
March 25, 2004
Inventors:
Niall Morton Hamilton, David Jonathan Bennett
Abstract: The invention relates to compounds of formula (2) in which R1, R2, R3 and R4 have the meanings indicated in the description, their preparation and their further reaction to give compounds of formula (1), in which A1, A2 and R4 have the meanings indicated in the description. The compounds of the formula (1) are valuable intermediates for the preparation of medicaments.
Abstract: The present invention provides dihydro-2H-napthalene-1-ones of formula (V), and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis. Specifically, the present invention relates to compounds that inhibit the farnesyl transferase enzyme.
Type:
Application
Filed:
October 8, 2002
Publication date:
December 18, 2003
Inventors:
Daniele Marie Leonard, Joseph Thomas Repine, Gordon William Rewcastle
Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
Type:
Grant
Filed:
July 28, 2000
Date of Patent:
November 25, 2003
Assignee:
Telik, Inc.
Inventors:
Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
Abstract: Compounds of formula (1) containing sterically hindered groups, polymers thereof and the use of these polymers in papermaking processes and dewatering processes.
Abstract: Derivatives of aryl(or heteroaryl)azolylcarbinoles of general formula (I), in which Ar represents a phenyl radical or a thienyl radical, optionally substituted, R1 represents a hydrogen atom or a lower alkyl group, R2 represents a dialkylaminoalkyl or azaheterocylclylalkyl and Het represents an azole unsubstituted or optionally substituted by one or two substituents, and their physiologically acceptable salts; are useful as drugs in human and/or veterinary therapeutics to treat urinary incontinence in mammals, including man.
Type:
Application
Filed:
July 3, 2002
Publication date:
January 30, 2003
Applicant:
Laboratorios del Dr. Esteve, S.A.
Inventors:
Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
Abstract: The invention relates to novel diphenylimidazolines of the formula (I)
in which
Ar1, Ar2 and R are each as defined in the description,
and a plurality of processes for their preparation and to their use for controlling animal pests.
Type:
Grant
Filed:
February 5, 2001
Date of Patent:
April 30, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Alan Graff, Andrew Plant, Christoph Erdelen, Norbert Mencke, Andreas Turberg
Abstract: The invention relates to compounds of the formula 1
R1—O—(A—O)x—(CH2)y—R2 (1)
in which
R1 is branched or straight-chain C4-C30-alkyl, C4-C30-alkenyl or C4-C30-alkylaryl,
A is C2-C4-alkylene,
x is an integer from 1 to 100,
y is 1, 2, 3 or 4 and
R2 is a radical selected from structures of the formulae 2 and 3
—CO—NR3R4 (2)
in which one of the radicals R3 and R4 is a hydrocarbon chain which has at least one free NH or NH2 group and the other radical is hydrogen or a hydrocarbon chain which has at least one free NH or NH2 group and R5 is hydrogen or a hydrocarbon chain which has at least one free NH or NH2 group.
Abstract: This invention provides a series of substituted 2-imidazolines which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these compounds.
Type:
Grant
Filed:
June 10, 1994
Date of Patent:
January 16, 2001
Assignee:
Eli Lilly and Company
Inventors:
Philip A. Hipskind, J. Jeffry Howbert, Brian S. Muehl