cas 288-47-1, Thiazole | Articles data

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Iversen
p. 484
(1972)
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An Efficient Synthesis of 1,3-Thiazole
The cyclocondensation of methyl dithiocarbamate with chloroacetaldehyde in aqueous ethanol affords 2-methylthio-1,3-thiazole (82-88percent) which is demethylsulfenylated to 1,3-thiazole (78-81percent) by reaction with lithium in liquid ammonia followed by hydrolysis with aqueous ammonia chloride.
Brandsma, L.,Jong, R. L. P. de,VerKruijsse, H. D.
p. 948 - 949
(1985)
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PYRAZINE DERIVATIVE AND APPLICATION THEREOF IN INHIBITING SHP2
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(2022/01/23)

Characteristic flavor formation of thermally processed N-(1-deoxy-α-D-ribulos-1-yl)-glycine: Decisive role of additional amino acids and promotional effect of glyoxal
The role of amino acids and α-dicarbonyls in the flavor formation of Amadori rearrangement product (ARP) during thermal processing was investigated. Comparisons of the volatile compounds and their concentrations when N-(1-deoxy-α-D-ribulos-1-yl)-glycine r
Zhan, Huan,Cui, Heping,Yu, Junhe,Hayat, Khizar,Wu, Xian,Zhang, Xiaoming,Ho, Chi-Tang
(2021/09/28)

Protodeboronation of (Hetero)Arylboronic Esters: Direct versus Prehydrolytic Pathways and Self-/Auto-Catalysis
The kinetics and mechanism of the base-catalyzed hydrolysis (ArB(OR)2→ ArB(OH)2) and protodeboronation (ArB(OR)2→ ArH) of a series of boronic esters, encompassing eight different polyols and 10 polyfluoroaryl and heteroaryl moieties, have been investigated by in situ and stopped-flow NMR spectroscopy (19F,1H, and11B), pH-rate dependence, isotope entrainment,2H KIEs, and KS-DFT computations. The study reveals the phenomenological stability of boronic esters under basic aqueous-organic conditions to be highly nuanced. In contrast to common assumption, esterification does not necessarily impart greater stability compared to the corresponding boronic acid. Moreover, hydrolysis of the ester to the boronic acid can be a dominant component of the overall protodeboronation process, augmented by self-, auto-, and oxidative (phenolic) catalysis when the pH is close to the pKaof the boronic acid/ester.
Hayes, Hannah L. D.,Wei, Ran,Assante, Michele,Geogheghan, Katherine J.,Jin, Na,Tomasi, Simone,Noonan, Gary,Leach, Andrew G.,Lloyd-Jones, Guy C.
supporting information
p. 14814 - 14826
(2021/09/13)

Photocatalytic Generation of 2-Azolyl Radicals: Intermediates for the Azolylation of Arenes and Heteroarenes via C-H Functionalization
The 2-azolyl radical, generated from 2-bromoazoles via photocatalysis, is a powerful intermediate for the intermolecular arylation of unmodified (hetero)arenes. The reaction is characterized by mild conditions, operational simplicity, tolerance toward functional and sterically demanding groups, broad scope, and anti-Minisci selectivity. A working mechanism is provided, and a low-solubility amine is essential for successful coupling. The utility of the reaction is demonstrated via late-stage functionalization of methyl estrone and application toward other bromoarenes.
Arora, Amandeep,Weaver, Jimmie D.
supporting information
p. 3996 - 3999
(2016/08/30)

Reduction of Aryl Halides into Arenes with 2-Propanol Promoted by a Substoichiometric Amount of a tert-Butoxy Radical Source
Aryl halides are reduced into the corresponding arenes in high yields, using 2-propanol, cesium carbonate, and di-tert-butyl peroxide (or di-tert-butyl hyponitrite) as a reductant/solvent, a base, and a radical initiator, respectively. This simple system reduces a wide variety of aryl bromides, chlorides, and iodides through single-electron-transfer mechanism with high functional-group tolerance.
Ueno, Ryota,Shimizu, Takashi,Shirakawa, Eiji
supporting information
p. 741 - 744
(2016/03/12)

Reductive Alkylation of 2-Bromoazoles via Photoinduced Electron Transfer: A Versatile Strategy to Csp2-Csp3 Coupled Products
Access to Csp2-Csp3-coupled products is a challenging goal at the forefront of catalysis. The photocatalytic reductive coupling of aryl bromides with unactivated alkenes is introduced as a convenient method that circumvents any need for synthesis of sp3-hybridized coupling partners. The reaction takes place via photoinduced electron transfer from a tertiary amine to an aryl bromide that fragments to provide an aryl radical and subsequently reacts with an alkene to form a C-C bond. Conveniently, the amine also serves as the final reductant. The method is operationally simple, functional group tolerant, and takes place with selectivities that will allow it to be used in the context of complex molecule synthesis.
Arora, Amandeep,Teegardin, Kip A.,Weaver, Jimmie D.
p. 3722 - 3725
(2015/08/18)

Rhodium-catalyzed 2-methylthiolation reaction of thiazoles/oxazoles using 2-(methylthio)thiazole
RhH(PPh3)4 and 1,3-bis(dicyclohexyl)phosphinopropane (dcypp) catalyze the 2-methylthiolation of oxazoles and thiazoles using 2-(methylthio)thiazole as a thiolating reagent. The methylthio transfer reaction is under equilibrium, and various 2-methylthiolated thiazoles and oxazoles were obtained in moderate to good yields by removing thiazole under refluxing o-dichlorobenzene.
Arisawa, Mieko,Nihei, Yuri,Yamaguchi, Masahiko
p. 939 - 949
(2015/03/04)

Photooxygenation of N-(2-thiazolyl)sulfanilamide, 2-(4-thiazolyl) benzimidazole, and thiacetazone
In the present work, photolysis of N-(2-thiozolyl)sulfanilamide, 2-(4-thiazolyl)benzimidazole and thiacetazone in presence of benzophenone as a sensitizer under 125 W UV Lamp has been reported. Structures of the products have been established by spectral and elemental analysis.
Jain, Shubha,Chourey, Meena,Jetti, Srinivasa Rao
p. 155 - 157,3
(2020/09/09)

Lipopeptide Compounds and Their Use
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain lipopeptide compounds comprising a cyclic peptide bearing a lipid side chain (for convenience, collectively referred to herein as “LP compounds”), which, inter alia, are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.
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(2011/10/04)

OLIGONUCLEOTIDE PROBE AND USE THEREOF
The present teaching provides a fluorescent oligonucleotide probe having a high degree of design flexibility and wide applicability, as well as the use thereof. This is an oligonucleotide probe capable of forming a stem and loop, comprising at least one fluorophore located between adjacent nucleotides in the stem and is linked to a unit represented by Formula (1) and at least one quencher located at a site capable of pairing up with the at least one fluorophore located between the adjacent nucleotides in the stem and is linked to a unit represented by Formula (2). (In the formulae, X represents the fluorophore, Y represents the quencher, R1 represents an optionally substituted C2 or C3 alkylene chain, R2 represents an optionally substituted C0-2 alkylene chain, and Z represents a direct bond or linker.)
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(2011/10/10)

Method for Producing Intermediates for the Production of Novel Macrocycles that are Inhibitors of the Proteasomic Degradation of p27, such as Argyrin and Derivatives Thereof, and Uses of Said Macrocycles
The present invention relates to the use of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular argyrin and derivatives thereof, for a treatment in a variety of conditions, such as the induction of immunotolerance, autoimmune diseases, bacterial infections, and proliferative diseases, such as cancers.
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(2012/01/12)

Investigation of the aroma-active compounds formed in the maillard reaction between glutathione and reducing sugars
Aroma-active compounds formed during the thermal reaction between glutathione (GSH) and reducing sugars were analyzed by gas chromatography-mass spectrometry (GC-MS) and GC-olfactometry (GC-O) with aroma extract dilution analysis (AEDA). Application of AEDA to glutathione Maillard reaction products (GSH MRPs) led to the identification of 19 aroma-active compounds in the thermal reaction of glutathione with glucose or fructose. In addition, the carbohydrate module labeling (CAMOLA) approach was also employed to elucidate the formation pathways for selected target sulfur aroma compounds, such as 5-methylthiophene-2-carbaldehyde and 3-methylthiophene-2-carbaldehyde, which have not been reported previously. The intact carbon skeleton of glucose via 3-deoxyhexosone is incorporated into 5-methylthiophene-2-carbaldehyde with the hydrogen sulfide of GSH. On the other hand, the formation of 3-methylthiophene2-carbaldehyde may occur via the recombination of a C-4 sugar fragment and mercaptoacetaldehyde.
Lee, Sang Mi,Jo, Ye-Jin,Kim, Young-Suk
experimental part
p. 3116 - 3124
(2011/08/05)

Method for producing intermediates for the production of novel macrocycles that are inhibitors of the proteasomic degradation of p27, such as argyrin and derivatives thereof, and uses of said macrocycles
The present invention relates to the use of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular argyrin and derivatives thereof, for a treatment in a variety of conditions, such as the induction of immunotolerance, autoimmune diseases, bacterial infections, and proliferative diseases, such as cancers.
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(2010/01/07)

Primer, primer set, and nucleic acid amplification method and mutation detection method using the same
The present invention provides a primer that effectively can detect, for example, the double helix structure of a nucleic acid. The primer is a labeled nucleic acid containing at least one structure represented by the following formula (16), where B is an atomic group having a nucleobase skeleton, E is an atomic group having a deoxyribose skeleton, a ribose skeleton, or a structure derived from either one of them, or an atomic group having a peptide structure or a peptoid structure, and Z11 and Z12 are each an atomic group that exhibits fluorescence and are identical to or different from each other.
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(2008/12/07)

Reactivity of neutral nitrogen donors in square-planar d8 metal complexes: The system chloro(2,2′:6′,2″-terpyridine)platinum(II) cation with five-membered N-donor heterocycles in methanol
The kinetics of the forward and reverse steps of the reaction [Pt(terpy)Cl]+ + nu ? [Pt(terpy)(nu)]2+ + Cl- (terpy = 2,2′:6′,2″-terpyridine, nu = one of a number of thiazoles, oxazole, isoxazole, imidazole, pyrazole and 3,5-dimethylpyrazole, covering a wide range of basicities) have been studied in methanol at 25 °C. Both forward and reverse reactions obey the usual two-term rate law observed in square-planar substitution. The second-order rate constants for the forward reactions, k2f, show a slight dependence upon the basicity of the entering nu, while the steric hindrance due to the presence of one methyl group in the α position to the nitrogen markedly decreases the reactivity. The second-order rate constants for the reverse reactions, k2r, are very sensitive to the nature of the leaving group and a plot of log k2r against the pKa of the conjugate acids of the unhindered five-membered N-donors is linear with a slope of -0.51. The results are compared with data from the literature regarding a series of pyridines reacting with the [Pt(terpy)Cl]+ cation under the same experimental conditions. Both in the forward and in the reverse reaction, the reactivity depends not only upon the ligand basicity but also upon the nature of the nucleophile in the order: (thiazoles, oxazole, isoxazole, imidazole, pyrazoles) > pyridines for the entry of N-donors and on the contrary for the displacement by Cl-. Steric retardation, due to the presence of a methyl group in the α position to the nitrogen, is remarkably lower for five-membered N-donors if compared to pyridines both in the forward and in the reverse reaction.
Pitteri, Bruno,Bortoluzzi, Marco
p. 2698 - 2704
(2008/10/09)

Synthesis of epothilones, intermediates thereto and analogues thereof
The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
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(2008/06/13)

Method for synthesizing epothilones and epothilone analogs
A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. Exemplary novel compounds include those according to the formula: With respect the formula, G is selected from the group consisting of R2 substituents independently are selected from the group consisting of H and lower alkyl groups; Z is selected from the group consisting of the halogens and —CN; M is selected from the group consisting of O and NR3; R3 is selected from the group consisting of H, lower alkyl, R4CO, R4OCO, and R4SO2; R4 is selected from the group consisting of H, lower alkyl, and aryl; T is selected from the group consisting of CH2, CO, HCOH and protected derivatives thereof; W is H or OR; and X and Y independently are selected from the group consisting of O, NH, S, CO, and C. Embodiments of the method provide convenient access to analogs of the epothilones, such as those having alternate stereochemistry and those containing an ester, amide, thioester, or alkyne moieties in the macrocycle.
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(2008/06/13)

Method for synthesizing epothilones and epothilone analogs
A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. Exemplary novel compounds include those according to the formula: With respect the formula, G is selected from the group consisting of R2 substituents independently are selected from the group consisting of H and lower alkyl groups; Z is selected from the group consisting of the halogens and —CN; M is selected from the group consisting of O and NR3; R3 is selected from the group consisting of H, lower alkyl, R4CO, R4OCO, and R4SO2; R4 is selected from the group consisting of H, lower alkyl, and aryl; T is selected from the group consisting of CH2, CO, HCOH and protected derivatives thereof; W is H or OR; and X and Y independently are selected from the group consisting of O, NH, S, CO, and C. Embodiments of the method provide convenient access to analogs of the epothilones, such as those having alternate stereochemistry and those containing an ester, amide, thioester, or alkyne moieties in the macrocycle.
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(2008/06/13)

ACE-2 modulating compounds and methods of use thereof
ACE-2 modulating compounds for the treatment of body weight disorders are disclosed. Methods of using the compounds and pharmaceutical compositions containing the compounds are also claimed.
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(2008/06/13)

Thiazines and thiazoles as agents for protecting materials
The novel and known thiazines and thiazoles of the formula (I) in which R1, R2 and n are as defined in the description, are highly suitable for use as biocides for protecting industrial materials.
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(2012/09/11)

Cocaine receptor binding ligands
The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases.
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(2008/06/13)

Potent, simplified derivatives of immunosuppressive agents
The present invention provides a compound of Formula I, all of its related stereoisomers, and their pharmaceutically acceptable salts, wherein A-B, K, Q, X, Y, Z, R and R1 are as defined in claim 1. The present invention also provides processes for the preparation thereof, the use thereof in treating immune mediated disease and conditions, and pharmaceutical compositions for use in such therapy.
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(2008/06/13)

Heterocycle substituted purine derivatives as potent antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: with Y, V, A, R1, R2, R3, R4, R7, and n1 defined herein.
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(2008/06/13)

Method for synthesizing epothilones and epothilone analogs
A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B.
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(2008/06/13)

Cocaine receptor binding ligands
The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases.
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(2008/06/13)

Trisubstituted heterocyclic compounds and their use as fungicides
Compounds of general formula (I): in which:Het represents a five or six membered saturated, partially unsaturated or aromatic ring containing between one and six heteroatoms of the group N, O, S, in which the heterocycle is substituted in an adjacent manner with -P-Q1-T-Q2, -GZ and Y, such that the substituant -GZ is adjacent to both. the other substituants being as defined in the description,process for preparing these compounds,fungicidal compositions comprising these compounds,processes for treating plants by applying these compounds or compositions.
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(2008/06/13)

Synthesis of epothilones, intermediates thereto and analogues thereof
The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
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(2008/06/13)

MATERIALS AND METHODS TO POTENTIATE CANCER TREATMENT
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(2008/06/13)

Method for synthesizing epothilones and epothilone analogs
A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B.
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(2008/06/13)

Thiazole, imidazole and oxazole compounds and treatments of disorders associated with protein aging
Provided are, among other things, compounds of formula I or IA, . Also provided are methods of treatment with such compounds.
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(2008/06/13)

Method for treating glaucoma IIB
Provided is a method of decreasing intraocular pressure or improving ocular accommodation in an animal, including a human, comprising administering an intraocular pressure decreasing amount or ocular accommodation improving amount of a compound of the formula I or IA, wherein J is oxygen, sulfur, or N—Rd.
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(2008/06/13)

Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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(2008/06/13)

Epothilone analogs
Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancer agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the anlogs are demonstrated to have a superior cytotoxic activities as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.
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(2008/06/13)

Epothilone analogs
Novel analogs of epothilone A, epothilone B, and epothilone C are synthesized by Stille coupling thazole-stannanes to macrolactone intermediates. The synthetic epothilone analogs selectively prevent mitosis in cancer cells through the induction and stabilization of microtubulin assembly. Selected synthetic epothilone analogs are demonstrated to have greater bioactivity than their corresponding native compound.
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(2008/06/13)

Heterocyclic compounds and medical use thereof
The present invention provides an AP-1 activation inhibitor, a NF-kappaB activation inhibitor, an inflammatory cytokine production inhibitor, a production inhibitor for matrix metalloprotease or an inflammatory cell adhesion factor expression inhibitor, which contains a heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient.
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(2008/06/13)

Synthesis of epothilones, intermediates thereto and analogues thereof
The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
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(2008/06/13)

Thienycyclohexanone derivatives as ligands of the GABAA α5 receptor subtype
A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.
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(2008/06/13)

Artemisinin analogs having antimalarial antiproliferative and antitumor activities and chemoselective methods of making the same
Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and artemisinin dimers have the following structure or diastereomers thereof, having antimalarial, and antiproliferative and antitumor activities wherein, the monomers of the present invention are formed when n is 1 and R is alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl. The dimers of the present invention are formed when n is 2 and R is a linker including, but not limited to, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl.
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(2008/06/13)

Cocaine receptor binding ligands
The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases or in determining the doses of therapeutic agents that occupy significant numbers of receptors.
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(2008/06/13)

Substituted thiadiazolesulfonamides
Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1β participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).
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(2008/06/13)

Pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R14and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
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(2008/06/13)

Substituted thienobenzisoxazole derivatives for enhancing cognition
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: STR1 wherein A is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, arylC1-6 alkyl, aryl, S(O)p R1, OR1 or NR1 R12 ; B is optionally substituted 5- or 6-membered heteroaromatic ring or C(O)NR10 R11 ; R1 is hydrogen, optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl or C3-6 cycloalkenyl, optionally substituted aryl, arylC1-6 alkyl, arylC2-6 alkenyl or arylC2-6 alkynyl or an optionally substituted 5- or 6-membered heteroaromatic ring; R2 and R3 are hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl or CH2 (CO)m NR8 R9 ; R5 is NR6 R7, C1-6 alkyl or C1-6 alkoxy; R6 is independently as defined for R4 ; R7 is aryl optionally substituted by halogen, nitro or cyano; R8 is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C3-6 cycloalkenyl, C2-6 alkenyl, C2-6 alkynyl; arylC1-6 alkyl, arylC2-6 alkenyl or arylC2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro or cyano; thiophene or pyridine; R9 is C1-6 alkyl; C2- alkenyl; C2-6 alkynyl; or phenyl optionally substituted by one, two or three substituents independently chosen from halogen, CF3, OCH3, nitro and cyano; R10 and R11 are individually hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C3-8 cycloalkyl or R10 and R11, together with the nitrogen atom to which they are attached, form a saturated 4 to 8 membered ring optionally containing an oxygen atom or a further nitrogen atom as a ring member, the further nitrogen atom being unsubstituted or substituted by C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl; R12 is hydrogen or C1-6 alkyl; m is zero or 1; p is zero, 1 or 2; q is 0, 1 or 2; and r is 0, 1 or 2; the preparation of these compounds, their use in enhancing cognition in disease states, particularly Alzheimer's disease, and methods of treatment using them.
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(2008/06/13)

Heterocycle-fused thiazole derivatives
PCT No. PCT/KR96/00082 Sec. 371 Date Jul. 3, 1997 Sec. 102(e) Date Jul. 3, 1997 PCT Filed Jun. 1, 1996 PCT Pub. No. WO97/03076 PCT Pub. Date Jan. 30, 1997A thiazole compound represented by general formula (I), wherein R is hydrogen atom, a hydroxy group, a straight or branched C1-C6 lower alkyl group, a C1-C4 lower alkoxy group, phenyl group, a phenyl group having one to three substituents selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, fluorine, chlorine, bromine and an amino group, a C1-C5 alkylphenyl group, a phenyl group having one to three substituents selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, fluorine, chlorine, bromine and an amino group, a substituted or unsubstituted guanidino group, or an amino group having a general formula: NR3R4 in which R3 and R4, identical to or different from each other, represent independently a hydrogen atom, a C1-C6 lower alkyl group, a C3-C6 cycloalkyl group, a substituted or unsubstituted pyridyl group, a phenyl group having one to three substituents selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, a halogen atom, an amino group, a cyano group and a nitro group, a piperidine group or C1-C4 alkylpiperidine group; R1 and R2, identical to or different from each other, are independently a hydrogen atom, a hydroxy group, a C1-C6 lower alkyl group, phenyl group, a phenyl group having one substituent selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, a halogen atom, a nitro and a cyano group, a C1-C5 alkylphenyl group, or a pyridine group; R5, R6, R7 and R8, identical to or different from each other, are independently a hydrogen atom, a hydroxy group, a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, phenyl group, or a phenyl group substituted with a C1-C4 alkyl group, a C1-C4 alkoxy group or a halogen atom, or a C1-C3 alkylphenyl group; Het is a 3-, 4- or 5-membered unsaturated monocyclic group, or 6- to 12-membered unsaturated fused cyclic group, said monocyclic and fused cyclic group being comprised of one or more hetero atoms selected from oxygen, oxidative nitrogen and oxidative sulfur atom are disclosed. These compounds show excellent anti-ulcer activity.
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(2008/06/13)

Reductive coupling of halogenothiophenes and halogenothiazoles catalysed by PdII in a basic alcohol medium
A catalytic reductive coupling method has been developed whereby 2- and 3-bromo- and 2-iodothiophenes, 2-bromothiazole and 2-bromofuran are converted into their corresponding bithiophene, bithiazole and bifuran derivatives. The use of a basic alcohol medium favours the reductive coupling pathway over the hydrodehalogenation pathway, which is generally more facile when other reducing agents are used. The catalytic mechanisms are discussed. The syntheses and characterization of the proposed intermediate complexes, trans-[PdBr(C4H3S-C)(PPh3)2] 1, trans-[PdI(C4H3S-C)(PPh3)2] 2 and trans-(N,P)-[{PdBr(μ-C3H2NS-C2,N)(PPh 3)}2]·1/2CHCl3 3 support the proposed mechanism and the catalytic results. Single-crystal X-ray crystallographic structure determinations of 2 and 3 were carried out.
Xie, Yang,Tan, Geok Kheng,Yan, Yaw Kai,Vittal, Jagadese J.,Ng, Siu Choon,Hor, T. S. Andy
p. 773 - 779
(2007/10/03)

METHODS FOR CONTROLLING INVERTEBRATE PESTS USING COCAINE RECEPTOR BINDING LIGANDS
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(2008/06/13)

Fluorescent group-containing carbodiimide compound
Using the fluorescent group-containing carbodiimide compound represented-by the following formula (I) as the label and the like in the nucleic acid detection method, immunoassay, or chemiluminescence assay, labeling can be made efficiently for a short time, a nucleic acid derived from nature can be labelled, and highly sensitive assay is enabled. wherein F represents a fluorescent group; A represents a moiety selected from the group consisting of --CH2 --, --NHCO--, --CONH--, --O--, --S--, --NR-- wherein R is an alkyl group, --COO--, --OCO--, --NHSO2 --, and --SO2 NH--; n is 0 or 1; W represents a direct bond or a quaternary ammonium group; Y1, Y2 and Y3 each represents an alkylene group which may have a functional group in its main chain; and B represents H or a monovalent organic group which may be the same as or different from that represented by --W--Y1 --?A!n --F.
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(2008/06/13)

Aqueous ink composition for use in an ink jet printer
An aqueous ink composition for ink jet printers, which gives reliable printing performance and yields printed images which have excellent print quality and which dry rapidly is disclosed. The ink compositions are suitable for printing on plain paper. The ink comprises water as the principal solvent, an anionic colorant, pectic acid, a base, and at least one of a penetrable solvent and/or a penetrability-imparting surfactant. The pectic acid is composed primarily of α-1,4 linked polygalacturonic acid having a degree of esterification not more than 5% where the degree of esterification is defined as the percentage of the total number of galacturonic acid units in the pectic acid which are esterified.
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(2008/06/13)

1,2,3-Benzothiadiazole derivatives
Novel 1,2,3-benzothiadiazole derivatives of the formula STR1 in which Het has the meanings set forth in the specification, and addition products thereof with an acid or metal salt are very effective for the control of undesired microorganisms. Novel intermediates of the formulae STR2 in which Het1 and R5 have the meanings given in the specification.
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(2008/06/13)

Technetium-99m labeled chelator incorporated cyclic peptides that bind to the GPIIb/IIIa receptor as imaging agents
The present invention describes novel radiopharmaceuticals of formula (I): STR1 wherein J, K, L, and M, are amino acids or derivatives thereof and R', R1, R2 and n are as defined herein, that are radiolabeled cyclic compounds containing chelators which act as antagonists of the platelet glycoprotein IIb/IIIa complex, methods of using the same as imaging agents for the diagnosis of arterial and venous thrombi, and novel reagents for the preparation of the same and kits comprising the reagents.
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(2008/06/13)

SUBSTITUTED 6- AND 7- AMINOTETRAHYDROISOQUINOLINECARBOXYLIC ACIDS
Compounds of the formula I STR1 are suitable for the preparation of pharmaceuticals for the prophylaxis and therapy of disorders involving increased activity of matrix-degrading metalloproteinases.
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(2008/06/13)