- Gold(I)-catalyzed protodecarboxylation of (Hetero)aromatic carboxylic acids
-
Readily available, inexpensive and easy to handle, carboxylic acids have been shown to be very effective, greener coupling partners compared to costly organometallic reagents for the formation of C-C bonds. The use of well-defined gold complexes furnished 3 in slightly better yield with butyric acid, and in quantitative yield with adamantane-1-carboxylic acid. All reactions reached completion within 16 h. As with silver systems, this reactivity trend highlights, as previously observed, the benefits of potential coordinating groups in the ortho position to the gold binding site, which possibly facilitate the decarboxylation step. Additional reaction time and increased temperatures were necessary to afford the gold aryl products in satisfactory yields. Yet, some substrates such as 2-nitrobenzoic acids reacted poorly and could only be transformed in 50% yield.
- Dupuy, Stéphanie,Nolan, Steven P.
-
supporting information
p. 14034 - 14038
(2013/11/19)
-
- 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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-
-
- 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)
-
- PROCESS FOR THE RECOVERY OF OXAZOLE
-
A process for the recovery of oxazole comprising contacting a mixture comprising oxazole and acetonitrile with an acid to form an acid salt of oxazole; separating acid salt of the oxazole from the mixture; and neutralizing the acid salt of oxazole separated from the mixture to release oxazole.
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-
-
- Gastrin and cholecystokinin receptor ligands(II)
-
Substituted imidazoles (1) are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure. Pharmaceutical compositions containing the novel imidazoles and pharmaceutical methods using them, alone and in conjunction with other drugs, especially diuretics and non-steroidal antiinflammatory drugs (NSAID's) are also described.
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-
-
- 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.
- -
-
-
- Viral polymerase inhibitors
-
An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; ---- represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.
- -
-
-
- Piperazine carboxamide intermediates of HIV protease inhibitors and processes for their preparation
-
Piperazine carboxamide intermediates of HIV protease inhibitors and a process for their preparation are disclosed. The piperazine carboxamide compounds are of Formula (III): wherein R1, R2, R3, R4, R5, and R6 are defined herein. The process for preparing the intermediates comprises coupling an iminium salt of Formula I: with a metallated derivative of a compound of Formula (II): R1—H??(II), wherein L? is a counterion. A process for preparing the iminium salt of Formula (I) is also disclosed, as is a process for preparing HIV protease inhibitors from Compound III.
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-
-
- Antidiabetic agents
-
The present invention provides compounds of Formula (I): wherein A, X, Q, Y, B, D, Z, and E have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antidiabetic agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.
- -
-
-
- Macrocyclic peptides active against the hepatitis C virus
-
The present invention covers macrocyclic compounds of formula I active in-vitro and in cellular assays against the NS3 protease of the hepatitis C virus. wherein W, R21, R22, R3, R4, D and A are as defined herein, or a pharmaceutically acceptable salts or ester thereof.
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-
-
- 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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-
-
- 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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-
-
- Fatty acid synthase inhibitors
-
This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
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-
-
- Oxazole PPAR antagonist
-
A method is disclosed for rational design of a PPAR, FXR, LXR-alpha, or LXR-beta antagonist comprising chemical modification of a PPAR, FXR, LXR-alpha, or LXR-beta agonist to: a) prevent formation of a hydrogen bond between the agonist and tyrosine or histidine, or tryptophan involved in receptor activation; and/or b) displace the tyrosine or histidine, or tryptophan involved in receptor activation from its agonist bound position. Preferably, little or no additional changes are made in the structure of the agonist so that the resulting antagonist is a close structural analogue of the agonist. Specific examples of PPAR gamma antagonists designed and prepared using the method of this invention are compounds of Formula (I) or (II), or pharmaceutically acceptable salts or solvates thereof, where in Formula (I) X is O, S, or NH; and R is methyl, ethyl, n-propyl, i-propyl, cyclopropyl, n-butyl, phenyl, or —CH2OCH3and wherein in Formula (II) X is C or N; and R is methyl, ethyl, n-propyl, i-propyl, —CH2OCH3, or —CO2CH3.
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-
-
- Naphthol derivatives
-
Novel naphthol derivatives, and various azo compounds and metal complexes prepared by using the derivatives are provided. The instant invention provides naphthol derivatives represented by general formula (1); wherein at least one of Y1and Y2is a group represented by formula (2); wherein X1is —O—, —S— or —NH—; and Z is an optionally substituted aromatic group or heterocyclic group having conjugated double bonds, and salts thereof; mono-, bis-, and trisazo compounds prepared from the derivatives; and metal complexes containing the derivatives as the ligand.
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-
-
- Novel chain-breaking antioxidants
-
Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.
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-
-
- 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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-
-
- 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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- Piperazine compounds, their preparation, and methods of using them
-
Novel piperazine and piperidine derivative compounds having interesting and advantageous pharmacological properties. The disdosed compounds have the general formula (a) and salts thereof. These compounds have high affinity for both the dopamine D2receptors and serotonine 5-HT1Areceptors, rendering them useful for the treatment of CNS-disorders, in particular schizophrenia.
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-
-
- A practical synthesis of 1,3-oxazole
-
A short synthesis of oxazole (1,3-oxazole, 1) is described.
- Shafer, Cynthia M.,Molinski, Tadeusz F.
-
p. 1167 - 1170
(2007/10/03)
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- Total synthesis of (-)-colchicine by an oxyallyl [4 + 3] cycloaddition
-
An enantioselective synthesis of (-)-colchicine, free from isocolchicine, is delineated and features tandem application of the intramolecular Diels-Alder reaction of acetylene-tethered oxazoles and the [4+3] cycloaddition of oxyallyls. This work underscores the synthetic utility of little explored α-alkoxy substituted oxyallyls. (C) 2000 Elsevier Science Ltd.
- Lee, Jae Chol,Cha, Jin Kun
-
p. 10175 - 10184
(2007/10/03)
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- 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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-
- Substituted oxazolyl compounds for the treatment of inflammation
-
A class of substituted oxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: STR1 wherein R is selected from alkyl, hydroxyalkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl optionally substituted at a substitutable position by carboxy, alkyl, alkoxy and halo, aralkyl optionally substituted at a substitutable position on the aryl radical by carboxy, alkyl, alkoxy and halo, aryloxyalkyl optionally substituted at a substitutable position on the aryl radical with halo, carboxy, alkyl and alkoxy, aralkoxyalkyl optionally substituted at a substitutable position by alkyl, carboxy, alkoxy and halo, heteroaryloxyalkyl optionally substituted at a substitutable position with halo, carboxy, alkyl and alkoxy, alkoxycarbonylalkyl, carboxyalkyl and aminocarbonylalkyl; wherein R1 is selected from cycloalkyl, cycloalkenyl, heteroaryl and aryl optionally substituted at a substitutable position by alkyl, alkoxy and halo, and wherein R2 is alkyl; or a pharmaceutically-acceptable salt thereof; provided R1 is not phenyl when R2 is methyl and R is isopropyl or tert-butyl.
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-
-
- Prostaglandin analogs
-
Thromboxane receptor antagonist activity is exhibited by compounds of the formula STR1 wherein: V is --(CH 2) m --, --O--, or STR2 but if V is --O--or STR3 R 3 and R 4 must complete an aromatic ring; W is --(CH 2) 2 --, --CH CH-- or phenylene;X is a single bond, --CH CH--, --(CH 2) n --, or --O--(CH 2) n --; or X is branched alkylene or --O--branched alkylene wherein W is linked to Y through a chain n carbon atoms long;Y is --CO 2 H, --CO 2 alkyl, --CO 2 alkali metal, --CH 2 OH, --CONHSO 2 R 5, --CONHR 6, or --CH 2 -5-tetrazolyl;Z is O or NH;R 3 and R 4 are each independently hydrogen or alkyl or R 3 and R 4 together complete a ring optionally substituted through a ring carbon with a halo, lower alkyl, phenyl, halo (lower alkyl), halophenyl, oxo or hydroxyl group; and the remaining symbols are as defined in the specification.
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-
- Preparation of substituted alkenoic acids
-
This invention relates to a highly selective process for preparation of E-ω-phenyl-ω-(3-pyridyl)-ω-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as to intermediates therefor.
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-
- Carbamoyl substituted oxazoles as thromboxane receptor antagonists
-
This invention relates to carbamoyl substituted heterocycles which are ω-phenyl-ω-(3-pyridyl)-ω-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring and which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as pharmaceutical formulations containing them, methods for their use, and processes and intermediates for their preparation.
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-
- Adenosine re-uptake inhibiting derivatives of diphenyl oxazoles, thiazoles and imidazoles
-
A series of 1-piperazinyl-N-phenylacetamide derivatives of 4,5-diphenyl-oxazoles, thiazoles, and imidazoles which are novel adenosine transport inhibitors have been found to provide effective antiischemic protection for CNS and cardiac tissue, particularly neurons. A method of treatment to protect against CNS ischemia, such as that resulting from trauma, stroke, or other ischemic conditions, comprises administration of these novel compounds to an individual in need of such treatment.
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-
- BIS-HETEROCYCLIC PROSTAGLANDIN ANALOGS
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Thromboxane receptor antagonist activity is exhibited by compounds of the formula STR1 wherein: W is--(CH 2) m--or STR2 but if R. sup.3 and R 4 complete an aromatic ring, then W cannot be STR3 X is--(CH 2) 2--,--CH=CH--or phenylene; Y is--O--, a single bond or vinylene, except that Y cannot be--O--when n is 0, and if Y is vinylene, then n must be 0;Z is O or NH;R 3 and R 4 are each independently hydrogen, alkyl, alkenyl, or alkynyl, or R. sup.3 and R 4 together complete a ring as defined in the specification, optionally substituted through a ring carbon with an oxo or hydroxyl group; and the remaining symbols are as defined in the specification.
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-
- 7-oxabicycloheptyl substituted heterocyclic thioamide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
-
7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasospastic disease have the structural formula STR1 wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH2)2 --, --CH=CH-- or STR2 wherein Y is O, a single bond or vinyl, with the proviso that when n is O, if Z is STR3 then Y cannot be O, and when Z is --CH=CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO2 H, CO2 lower alkyl, CH2 OH, CO2 alkali metal, CONHSOR3, CONHR3a or --CH2 -5-tetrazolyl, X is O, S or NH; and where R1, R2, R3 and R3a are as defined herein.
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-
- OXAZOLES AND THIAZOLES FOR THE TREATMENT OF SENILE DEMENTIA
-
1,3-Oxazole and 1,3-thiazole compounds of formula I, and their pharmaceutically acceptable salts and prodrugs: STR1 wherein X represents oxygen or sulphur;R 1 represents a non-aromatic azacyclic or azabicyclic ring system.
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-
- 2-substituted-4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidines useful as antiinflammatory agents
-
The present invention is novel compounds which are 2-substituted-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever and the like. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.
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-
-
- A Retro-Diels-Alder Approach to Oxazoles and Imidazoles
-
Heating N-acyl derivatives 4 of 3-endo-aminobicyclohept-5-en-2-endo-ol (3) at 185-195 deg C for 4-5 h provides oxazoles 1a-e in 49-88percent yields.The reaction proceeds via an initial dehydration to an oxazoline which undergoes retro-Diels-Alder reaction to provide the oxazole.Similarly, imidazoles 7a-f may be obtained in 40-79percent yields by heating imidazolines 6a-f to effect the cycloreversion.
- Eissenstat, Michael A.,Weaver, John D.
-
p. 3387 - 3390
(2007/10/02)
-
- 2-SUBSTITUTED-4,6-DI-TERITARYBUTYL-5-HYDROXY-1,3-PYRIMIDINES USEFUL AS ANTIIINFLAMMATORY AGENTS
-
The present invention is novel compounds which are 2-substituted-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrmidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenease and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever and the like. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions
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-
- 7-oxabicycloheptyl substituted heterocyclic amide or ester prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
-
7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasopastic disease have the structural formula STR1 wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH2)2 --, --CH=CH-- or STR2 wherein Y is O, a single bond or vinyl, with the proviso that when n is 0, if Z is STR3 then Y cannot be O, and Z is --CH=CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO2 H, CO2 lower alkyl, CH2 OH, CO2 alkali metal, CONHSOR3, CONHR3a or --CH2 --5-tetrazolyl, X is O, S or NH; and where R1, R2, R3 and R3a are as defined herein.
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-
-
- Reactivity of Heterocyclic Nitrogen Donors in Systems containing the Tetrachloroaurate(III) Anion
-
A series of gold(III) complexes of the type has been prepared and characterized (L = oxazole, benzoxazole, thiazole, their benzo and methyl-substituted derivatives, or 2-methylbenzoselenazole).The five-membered N.O-, N,S- and N,Se-heterocyclic bases are all bound to Au(III) through nitrogen.The kinetics of the displacement of L by chloride to give (1-) has been studied in methanol-water (95:5. v/v) at 25.0 deg C and I = 0.20 mol dm-3 (LiClO4).The equilibrium constants for the reversible processes have also been determined.The reactions of the corresponding pyridine, 4-chloro-, 4-cyano- and 2,6-bis(chloromethyl)-pyridine complexes have also been reexamined under the same conditions.The equlibrium constants, K2, depend upon the basicity of the nitrogen in the ligands and points for all ligands, irrespective of ring size and composition, lie roughly on the same log K2 versus pKa curve.There is no significant systematic steric effect on the equilibrium constants of the sort found for the more basic methyl pyridines.The complexes of the five-membered heterocyclic ligands are approximately ten times less reactive than those of the six-membered N-heterocycles of comparable basicity and exhibit steric retardation from ortho-methyl substituents.The nucleophilicities of these ligands have been calculated and five-membered N,O- and N,S-heterocycles are considerably less reactive than six-membered N-heterocycles of similar basicity.
- Canovese, Luciano,Cattalini, Lucio,Tomaselli, Michele,Tobe, Martin L.
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p. 307 - 314
(2007/10/02)
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- New redox indicators
-
The invention provides new redox indicators and uses for these redox compounds (I): STR1 Wherein X is oxygen or sulphur, R1 is julolidine or tetrahydroquinoline, which can carry an alkyl radical on the nitrogen atom which, in turn, can be substituted by a sulphuric, phosphonic or carboxylic acid residues, or is (II); wherein R4 is hydroxyl or a mono- or dialkylated amino group, R5 and R6, which can be the same or different, are hydrogen, alkyl or alkoxy, R2 is hydrogen or alkyl, julolidine or tetrahydroquinoline, which can carry an alkyl on the nitrogen atom which alkyl can be substituted by sulphuric, phosphonic or carboxylic acids, or is III; wherein R5 and R6 are the same as in R1 and R'4 is hydroxyl, an amino or a mono-or dialkylated amino group, whereby the alkyl radicals can be substituted one or more times by hydroxyl, alkoxy, halogen, morpholine or a sulphuric, carboxylic or phosphonic acid residue, which acids can also be esterified, and R3 is the same as R2 or is an alkyl substituted by hydroxyl, alkoxy, dialkylamino or phenyl, or is cycloalkyl, phenyl or pyridyl; as well as the salts thereof.
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-
- Rigidized oxazole dyes
-
The quaternary salts of rigidized 1,3-oxazole compounds of the formula: STR1 where R is either H or CH3 O. The compounds are produced in a modif Robinson-Gabriel synthesis of oxazoles. These dyes are used in solution with non-interfering polar solvents, such as ethanol and H2 O, to form lasing media useful in dye lasers.
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- Benzo-fused cyclic compounds
-
Herbicidal benzo-fused cyclic compounds of the formula STR1 wherein Q is STR2 Y is O or S, W is STR3 T is O, S, --NH-- or STR4 and R4 may represent, together with T, chlorine, Z is O or S, X is hydrogen or halogen, n is 0 or 1 and R is C3-6 cycloalkyl, an optionally substituted 5-membered heterocyclic group or an optionally substituted 6-membered heteroaromatic group which contains one to three nitrogen atoms, and salts thereof.
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-
- Monic acid derivatives
-
Compounds of formula (I): wherein, is a divalent or a trivalent, 5-membered heterocyclic group having a 6-? electron system, and containing from 1 to 4 heteroatoms, each selected from oxygen, nitrogen and sulphur;, R1 is a substituted C3 7 cycloalkyl group attached to a carbon or nitrogen of and where appropriate, R2 is a group attached to a carbon or nitrogen of and, when present, is selected from optionally substituted C1 20 alkyl, optionally substituted C3 7 cycloalkyl, optionally substituted C2 8 alkenyl, aryl, aralkyl, heterocyclyl and hydrogen;, and where the trisubstituted carbon-carbon double bond preferably has the E- configuration;, have anti-bacterial activity.
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- Antibacterial monic acid derivatives
-
A compound of the formula (I) STR1 wherein R is a group STR2 R1 is hydrogen, phenyl, C1-20 alkyl, C2-8 alkenyl or C2-8 alkynyl each of which may optionally be substituted; or C3-7 cycloalkyl, X is a divalent group --Y--C=C--, and Y is oxygen or sulphur, have antibacterial and/or antimycoplasmal activity.
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-
- Di-heterocyclic compounds and their use as antiviral agents
-
Compounds of the formulas: STR1 wherein Het is an oxazole or oxazine moiety; X is O, S or SO, n is an integer from 3 to 9, Y is an aliphatic bridge; and the various R groups represent hydrogen or various substituents as described herein, are useful as antiviral agents, especially against picornaviruses. N-(Chloroalkyl)amide intermediates for the compounds of Formula I are also active as antiviral agents. Related compounds outside the scope of the above formulas are also disclosed.
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-
- Phosphorus esters of 5-pyrimidinols
-
Compounds of the formula: STR1 wherein R is hydrogen; alkyl of 1 to 8 carbons; alkylthiomethyl, alkylsulfinylmethyl or alkylsulfonylmethyl wherein alkyl contains 1 to 4 carbons; phenyl; phenylthio; alkylthio, alkylsulfinyl or alkylsulfonyl wherein alkyl contains 1 to 4 carbons; or alkylthio-ethylthio wherein alkyl contains 1 to 2 carbons; R' is hydrogen, methyl or alkylthio of 1 to 2 carbons; R" is hydrogen or methyl; X is oxygen or sulfur; R'" is alkyl of 1 to 2 carbons; and R"" is --OR'" or --S-alkyl of 1 to 4 carbons, are highly useful insecticides which are paricularly valuable when applied to the soil, but are also useful applied to foliage of crops or trees. Especially good control is obtained of corn rootworm, codling moth, thrips, leafhoppers, and nematodes. The compounds are conveniently applied in the form of a composition containing a pesticidal carrier such as an inert solvent or a finely divided inert solid in which case the composition is preferably granulated. An effective application rate is in the range of about 0.1 to about 5 pounds per acre when soil incorporated, and about 0.5 to about 2,000 ppm for foliar applications.
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-
- Mercaptoalkylpyridine disulfides
-
Mercaptoalkylpyridines carrying an ethenyl or ethynyl substituent are prepared from known pyridine compounds, principally pyridoxine, by known chemical procedures, and are useful in the treatment of rheumatoid arthritis and related inflammatory diseases.
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-
- PYRIDYL-ALKYLAMINOETHYLENE COMPOUNDS
-
The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-2-((4-methyl-5-imidazolyl) methylthio)ethylamino!-2-2-((3-chloro-2-pyridyl)methylthio) ethylamino!ethylene.
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-
- IMIDAZOLE ALKYLAMINOETHYLENE COMPOUNDS
-
The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-methylamino-2-2-((4-methyl-5-imidazolyl)methylthio)-ethylamino!ethylene.
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-
- PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
-
The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
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-
- PHARMACEUTICAL COMPOSITIONS AND METHODS OF INHIBITING H-1 AND H-2 HISTAMINE RECEPTORS
-
Pharmaceutical compositions and methods of inhibiting H-1 and H-2 histamine receptors by administering an antihistamine and an H-2 histamine receptor inhibitor. Exemplary of the antihistamine in the compositions and methods of this invention is mepyramine and exemplary of the H-2 histamine receptor inhibitor is N-cyano-N'-methyl-N"-2-((4-methyl-5-imidazolyl)-methylthio)ethyl!guanidine. "
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