- 4-AMINO-6-(HETEROCYCLIC)PICOLINATES AND 6-AMINO-2-(HETEROCYCLIC)PYRIMIDINE-4-CARBOXYLATES AND THEIR USE AS HERBICIDES
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Novel 4-amino-6-(heterocyclic)picolinic acids and their derivatives and 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives are useful to control undesirable vegetation.
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(2014/09/29)
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- Compounds for Use in the Detection of Neurodegenerative Diseases
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Provided are the use of the disclosed compounds as imaging agents and methods for in vivo imaging and detection of pathological characteristics unique to synuclein diseases, such as Parkinson's disease.
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- Aromatic sulfone hydroxamates and their use as protease inhibitors
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This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
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- Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors
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In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
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- Heterocyclic dihydropyrimidine compounds
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Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.
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- Cocaine receptor binding ligands
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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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- Process for making substituted 8-arylquinolinium benzenesulfonate
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A substituted 8-aryl quinoline and its benzenesulfonic acid salt is synthesized.
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- Cocaine receptor binding ligands
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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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- Trisubstituted heterocyclic compounds and their use as fungicides
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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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- Substituted amino methyl factor Xa inhibitors
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The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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- Non-peptide antagonists of GLP-1 receptor and methods of use
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Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding
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- Inhibitors of glycogen synthase kinase 3
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New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
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- Inhibitors of glycogen synthase kinase 3
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Novel pyridine and pyrimidine derivatives which selectively inhibit glycogen synthase kinase 3 are provided and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions which may be mediated by glycogen synthase kinase 3.
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- Isoxazoles and oxadiazoles as anti-inflammatory inhibitors of IL-8
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The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of IL-8 and are thus useful as anti-inflammatory agents for a variety of diseases.
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- Substituted 8-arylquinoline phosphodiesterase-4 inhibitors
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Novel sulfuric acid, methanesulfonic acid, p-toluenesulfonic acid, 2-naphthalenesulfonic acid, hydrochloride acid, or benzenesulfonic acid salts of substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-a
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- Heteroaryl-phenyl substituted factor Xa inhibitors
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The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.
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- Heteroaryl- phenyl heterobicyclic factor Xa inhibitors
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The present application describes heteroaryl-phenyl heterobicycles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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- Cocaine receptor binding ligands
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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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- Benzimidazolinones, benzoxazolinones, benzopiperazinones, indanones, and derivatives thereof as inhibitors of factor Xa
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The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3may be N or C and J, Ja, and Jbcombine to form a substituted carbocycle or heterocycle.
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- Oxadiazole benzenesulfonamides as selective beta 3 Agonist for the treatment of Diabetes and Obesity
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Oxadiazole substituted benzenesulfonamides are selective beta 3 adrenergic receptor agonists with very little beta 1 and beta 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The
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- 6-membered aromatics as factor Xa inhibitors
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The present application describes 6-membered aromatics of formula I: or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- SUBSTITUTED 1-INDOLYLPROPYL-4-BENZYLPIPERAZINE DERIVATIVES
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A class of 1-[3-(1H-indol-3-yl)propyl]-4-benzylpiperazine derivatives of formula I, substituted at the 5-position of the indole nucleus by a 1, 2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by a range of substituted alkyl groups, are selective agonists of 5-HT 1-like receptors, being potent agonists of the human 5-HT 1Dα receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT 1Dα receptor subtype relative to the 5-HT. sub.1Dβ subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT 1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT 1D receptor agonists. STR1
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- N-(AMIDINOPHENYL) CYCLOUREA ANALOGS AS FACTOR XA INHIBITORS
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The present application describes N-(amidinophenyl)cyclourea analogs of formula I: STR1 which are useful as inhibitors of factor Xa.
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- INHIBITORS OF FACTOR XA WITH A NEUTRAL P1 SPECIFICITY GROUP
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The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: STR1 or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
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- α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors
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The present application describes m-amidino phenyl analogs of formula I: wherein D can be amidino and E can be phenyl, which are useful as inhibitors of factor Xa.
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- Oxadiazoles useful in the treatment of senile dementia
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A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low lipophilicity; are potent muscarinic agonists, and have good CNS penetrability. The compounds are therefore useful in the treatment of neurological and mental illnesses.
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- Electrophotographic member
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Disclosed is an electrophotographic member containing as a charge transport material a fluorine-containing N,N,N',N'-tetraarylbenzidine derivative which is remarkably excellent in solubility in an organic solvent and/or a binder such as polycarbonate resin, etc., can show very excellent electrophotographic properties such as high sensitivity, low residual potential and high durability. Further, a fluorine-containing N,N,N',N'-tetraarylbenzidine derivative usable as a charge transport material, and a process for producing the same are disclosed. Furthermore, a fluorine-containing diarylamine usable for producing the fluorine-containing N,N,N',N'-tetraarylbenzidine derivative, and a process for producing the same are disclosed.
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- PERIPHERALLY SELECTIVE PIPERIDINE CARBOXYLATE OPIOID ANTAGONISTS
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3,4,4-trisubstitutedpiperidinyl-N-alkylcarboxylates and intermediates for their preparation are provided. These piperidine-N-alkylcarboxylates are useful as peripheral opioid antagonists.
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- Antibacterial 1-normon-2-yl-heterocyclic compounds
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Compounds of formula (I): STR1 wherein STR2 is a 5-membered heterocyclic group having a 6-?electron system, the five ring atoms being either (a) one carbon atom and four atoms selected from carbon and nitrogen, (b) two carbon atoms, two nitrogen atoms and one atom selected from oxygen and sulphur, or (c) four carbon atoms and one atom selected from oxygen and sulphur and R1 is a substituent on a carbon or nitrogen of STR3 selected from C1-20 alkyl, C2-8 alkenyl aryl, aralkyl and heterocyclyl, each of which may optionally be substituted; hydrogen and C3-7 cycloalkyl, and, where appropriate, R2 is a substituent on a carbon or nitrogen of STR4 and when present is the same or different to R1 and is selected from C1-20 alkyl, C2-8 alkenyl, aryl, aralkyl and heterocyclyl each of which may optionally be substituted; hydrogen and C3-7 cycloalkyl, have antibacterial and antimycoplasmal activity.
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- Novel oxadiazolyl-1,4-dihydropyridines useful as antihypertensive agents
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A compound of the formula STR1 wherein T1 is lower alkylene, lower alkenylene or a single bond; X is STR2 T2 is carbonyl, lower alkylene or a single bond; R2 is phenyl, phenoxy, pyridyl, pyrimidinyl, furyl, thienyl, lower cycloalkyl or adamantyl; R2 and R6, when taken together with the nitrogen to which they are attached form pyrrolidinyl, piperidinyl or azacyclooctanyl; R14 is COOR8 or --R3 R9 wherein T3 is lower alkylene and R9 is lower alkoxy, lower cycloalkyl, cyano, polyfluoro-lower alkyl or pyridyl; and R1 and R5 are each lower alkyl or lower alkenyl, useful in the treatment of cardiovascular diseases.
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- Oxadiazole and oxadiazoline derivatives
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There are described new compounds of formula STR1 in which E is selected from the group consisting of residues of formula STR2 in which R" is selected from the group consisting of amino, vinyl, allyl, ethynyl, C1 -C5 alkyl, C1 -C5 alkoxy, or C1 -C5 alkylthio or a C1 -C5 alkyl group susbstituted by at least one halogen atom; and hydrogen; in which R1 and R2 are each selected from the group consisting of hydrogen, halogen, methyl and ethyl; and R' is selected from substituted phenyl when R" is other than hydrogen, and phenyl, thienyl and substituted phenyl and thienyl when R" is hydrogen. The compounds are useful in the control of parasites. Certain of the compounds have antimicrobial properties.
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- Mono- or disubstituted 1,2,4,oxadiazoles which are substituted by at least 1-N-substituted carbamoyl group
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1,2,4-Oxadiazoles having as 3- and 5-substituents a hydrogen atom, an aliphatic, cycloaliphatic, araliphatic, aryl or heterocyclic group, or a carbamoyl group of the formula -- CONR1 R2 where R1 & R2 which can b
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