- Method for Small-Scale Production of Deuterochloroform
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Deuterochloroform (CDCl3) is a common deuterated solvent for nuclear magnetic resonance (NMR) analyses. The synthesis of significant amounts of CDCl3 for both research use and large undergraduate organic laboratories in a safe and in
- Tansukawat, Natha D.,See, Alyaa E.,Jiranuntarat, Sadudee,Corbin, Joshua R.,Schomaker, Jennifer M.
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- H/D Exchange Reaction between CHCl3 and D2O in Two-Liquid-Phase System
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The kinetics of hydrogen isotope exchange between CHCl3 and D2O has been studied by using a system which is composed of two liquid phases, a chloroform phase and an aqueous phase.The area of the interface between these two phases was kept constant (5.7 x 10-3 m2) during the reaction, where the reaction may be controlled by the interfacial transfer of chloroform.The isotopic content of chloroform in the chloroform phase was determined by an infrared absorption measurement.After the reaction, disappearance of deuteroxide ion was observed, which is caused by the chloroform hydrolysis reaction.The experimental results are reasonably explained on the basis of the model in which the reaction process is assumed to be composed of two steps: interfacial transfer of chloroform from the chloroform phase to the aqueous phase or vice versa, and the hydrogen isotope exchange reaction between CHCl3 and D2O in the aqueous phase.The rate constants for the interfacial transfer of chloroform and for the exchange reaction in the aqueous phase at 26.0 deg C were 0.107 +/- 0.003 m-2s-1 and 0.231 +/- 0.013 Lmol-1s-1, respectively.
- Iwasaki, Matae,Sakka, Tetsuo,Ohashi, Shigeyuki,Matsushita, Hiroshi,Yokoyama, Atsushi,Suzuki, Kazuya
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- A straightforward catalytic approach to obtain deuterated chloroform at room temperature
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We report the catalytic activity for the complexes—cis-[RuCl2(dppb)(bipy)] (A), and [η6-(p-cymene)Ru (dppb)Cl]PF6 (B), wherein dppb = 1,4-bis(diphenylphosphine)butane, and bipy = 2,2′-bipyridine—for the synthesis of CDCl3 from CHCl3 using D2O as deuterium source. H/D exchange reactions were performed using a chloroform/D2O, 1:2 molar ratio, vigorously stirred, at room temperature. One mole of KOH was dissolved in D2O fraction and catalytic complexes from 0.002 to 0.05 mmol were dissolved in chloroform. The H/D exchange reactions were monitored using 13C nuclear magnetic resonance sequences without proton decoupling. The reaction using 0.01 mmol of compound A reached approximately 55percent of H/D conversion in 1 h. In the same time, the reactions with 0.002 mmol of compound A and without catalyst show approximately 28percent and 3percent H/D exchange, respectively. Without the catalysts, the H/D exchange was only 12.0percent in 5 h. For compound B, 55percent H/D conversion was observed in 1 h, only when 0.05 mmol was used, which is much higher catalyst concentration. After the isolation of the chloroform fraction and two more addition of D2O, it was possible to obtain 95.0percent H/D exchange in approximately 3 h, using 0.01 mmol of the compound A. Therefore, compound A is an efficient catalyst for a rapid and straightforward synthesis of CDCl3 from CHCl3 at room temperature and using D2O as deuterium source.
- Higuera-Padilla, Angel Ruben,Kock, Flávio Vinícius Crizóstomo,Batista, Alzir Azevedo,Colnago, Luiz Alberto
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- Novel chiral derivatizing reagent for the determination of enantiomeric excesses
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A method for the determination of the enantiomeric composition of a chiral compound comprising (a) derivatising said chiral compound with a enantiomerically and diastereomerically pure compound of general formula I and (b) analysing the resulting mixture by an analytic technique. wherein Ar is an optionally substituted aromatic or heteroaromatic group.
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- Mechanisms and Products of Surface-Mediated Reductive Dehalogenation of Carbon Tetrachloride by Fe(II) on Goethite
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Aliphatic chlorinated hydrocarbons, including CCl4, are widespread groundwater contaminants. Mechanisms and product formation of CCl4 reduction by Fe(II) sorbed to goethite, which may lead to completely dehalogenated products or to form chloroform, a toxic product that is fairly persistent under anoxic conditions, were studied. A simultaneous transfer of two electrons and cleavage of two C-Cl bonds of CCl4 would completely circumvent chloroform production. Product formation pathways did not primarily depend on the competition between an initial one- and two-electron transfer, but on the presence of different radical scavengers and the properties of the mineral surface with respect to stabilization of reaction intermediates. Specific adsorption of major anions or pH effects could modify the capability of the goethite surface to stabilize short-lived radical intermediates.
- Elsner, Martin,Haderlein, Stefan B.,Kellerhals, Thomas,Luzi, Samuel,Zwank, Luc,Angst, Werner,Schwarzenbach, Rene P.
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p. 2058 - 2066
(2008/12/21)
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- Organophotoreceptor with a compound having a toluidine group
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An improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate wherein the photoconductive element comprisesa) a charge transport material with the following formula where R1 and R2 are, independently, a carbazolyl group, an (N,N-disubstituted) aminoaryl group, such as a triphenyl amine group, or a julolidine group, and R3 and R4 are, independently, hydrogen, branched or linear alkyl group (e.g., a C1-C20 alkyl group), branched or linear unsaturated hydrocarbon group, cycloalkyl group (e.g. cyclohexyl group), or aryl group (e.g., phenyl group, naphthyl group, stilbenyl group, (9H-fluoren-9-ylidene)benzyl group, or tolanyl group);(b) an optional charge transport compound; and(c) a charge generating compound.
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- BENZOXAZOLE COMPOUND, PROCESS FOR PRODUCING THE SAME, AND HERBICIDE
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The present invention relates to benzoxazole compounds represented by the following formula (I): wherein R1 to R4 may be the same or different from each other, and each represent a hydrogen atom, alkyl group having 1 to 6 carbon atoms, alkoxy group having 1 to 4 carbon atoms, haloalkyl group having 1 to 4 carbon atoms, haloalkoxy group having 1 to 4 carbon atoms, halogen atom, nitro group, cyano group, R12S(O)n, alkoxycarbonyl group having 1 to 4 carbon atoms, amino group, -NHCOR11 or carbonyl group, where R11 and R12 each represent an alkyl group having 1 to 6 carbon atoms, and n is an integer of 0 to 2, A represents a single bond, CHR5-Y, CR5=CR6, CR5R7-CHR6 or CHR5, where R5 represents a hydrogen atom, hydroxyl group, halogen atom or alkyl group, R6 and R7 each represent a hydrogen atom, hydroxyl group, alkyl group, halogen atom or substituted sulfonyloxy group, Y represents O, S or NH, and W represents a substituted or unsubstituted benzene ring or hetero ring, and processes for preparing the same.
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- Hydroalkylation of aromatic hydrocarbons
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There is described a process the hydroalkylation of an aromatic hydrocarbon, particularly benzene, to produce a cycloalkyl-substituted aromatic compound, particularly cyclohexylbenzene, comprising the step of contacting the aromatic hydrocarbon with hydrogen in the presence of a catalyst comprising MCM-68 and at least one metal having hydrogenation activity.
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- Substituted tetrahydronaphthaline and analogous compounds
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Substituted tetrahydro-naphthalenes and analogous compounds are prepared by reducing or condensing appropriate functional substituents in substituted tetrahydro-naphthalenes and analogous compounds by customary methods and converting functional groups in this manner into the desired groups. The compounds according to the invention are suitable for use as active compounds in pharmaceuticals, in particular in pharmaceuticals for treating arteriosclerosis and also dyslipidaemias.
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- Chemokine receptor antagonists and methods of use therefor
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Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: and physiologically acceptable salts thereof.
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- Solvent-free mechanochemical preparation of phosphonium salts, phosphorus ylides, and olefins
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The present invention provides a method of preparing a phosphonium salt of the formula [R1R2R3P—CR4R5R6]X, comprising ball-milling a phosphine of the formula R1R2R3P with a compound of the formula XCR4R5R6; a method of preparing a phosphorus ylide of the formula R1R2R3P═CR4R5, comprising ball-milling a phosphonium salt of the formula [R1R2R3P—HCR4R5]X in the presence of a base; and a method of preparing an olefin of the formula R4R5C═CR7H or R4R5C═CR7R8, comprising ball-milling a phosphorus ylide of the formula R1R2R3P═CR4R5 with a compound of the formula R7C(O)H or R7C(O)R8. The inventive method produces phosphonium salts and phosphorus ylides by mechanical processing solid reagents under solvent-free conditions. The advantages of the present invention over conventional solution methods, include: (1) extremely high selectivity; (2) high yields; (3) low processing temperatures; (4) simple and scalable reactions using commercially available equipment; and (5) the complete elimination of solvents from the reaction.
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- Pyrazole derivatives
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The invention provides compounds of formula 1 wherein R1, R2, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating and preventing diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission. Also described are pharmaceutical compositions and methods comprising compounds of formula 1 for treating male fertility and sperm motility; diabetes mellitus; impaired glucose tolerance; metabolic syndrome or syndrome X; polycystic ovary syndrome; adipogenesis and obesity; myogenesis and frailty, for example age-related decline in physical performance; acute sarcopenia, for example muscle atrophy and/or cachexia associated with burns, bed rest, limb immobilization, or major thoracic, abdominal, and/or orthopedic surgery; sepsis; hair loss, hair thinning, and balding; and immunodeficiency.
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- Bicyclic amino derivatives and PGD2 antagonist containing the same
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A compound of the formula (I): wherein for example, a compound below: whereinR1 is CH3, H or Na; and X1-X2-X3 is or its salt or a hydrate thereof is useful as PGD2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.
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- Acaricidal and insecticidal substituted pyrimidines and a process for the preparation thereof
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The present invention provides compounds of Formula I methods for their preparation and their use as acaricidal and insecticidal agents.
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- Carbamate-based cationic lipids
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The present invention provides novel carbamate-based cationic lipids of the general structure: or a salt, or solvate, or enantiomers thereof, wherein (a) R1 is a lipophilic moiety; (b) R2 is a positively charged moiety; (c) n is an integer from 1 to 8; (d) X is an anion or polyanion; and (e) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid. The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions, and a kit for preparing the same.
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- Phosphosugars and phosphosugar-containing compounds having anti-inflammatory activity
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D-mannoside-6-phosphate compounds having anti-inflammatory activity are disclosed, and use thereof in treating inflammatory diseases, particularly cell-mediated inflammatory diseases.
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- Synthesis and use of thiophene- and pyrrole-based heteroaromatic compounds
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Methods for preparing thiophene and pyrrole-based heterocyclic compounds are disclosed. Also disclosed are libraries of thiophene and pyrrole-based heterocyclic compounds, methods for preparing the libraries of thiophene and pyrrole-based heterocyclic compounds, and methods for using the thiophene and pyrrole-based heterocyclic compounds and compound libraries of the invention. The compounds of the invention have biological activity including anti-cancer activity.
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- Phosphonic acid-based cationic lipids
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The present invention provides novel phosphonic acid-based cationic lipids of the general structure: STR1 or a salt, or solvate, or enantiomers thereof wherein; (a) R1 is a lipophilic moiety; (b) R2 is a positively charged moiety; (c) R3 is a lipophilic moiety of 1 to about 24 carbon atoms, a positively charged moiety, or a negatively charged moiety; (d) n is an integer from 0 to 8; (e) X- is an anion or polyanion; (f) Y is N or O, and (g) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid. The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.
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- Lewis-associated compound, process for producing the same, and anti-inflammatory
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A Lewis-associated compound, represented by general formula (I), a process for producing the same, and an anti-inflammatory, wherein R1 and R3 represent each hydrogen, m SO3 H or CH2 COOH; R2 represents hydrogen, SO3 H, CH2 COOH or N-acetyl-neutraminic acid residue; R4 represents hydrogen; R5 represents O-lower alkyl, O-lower alkenyl, O-ceramide residue, O-mannose residue, O-galactose residue or O-lactose residue; R6 represents acetylamine; and R7 and R8 represent each hydrogen. STR1
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- Method of preventing abnormal stimulation of AT1 and AT2 receptors
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Products of formula (1), wherein R1 is particularly STR1 alkyl, alkylthio or alkoxy; R2 is particularly halogen, --S--R, --O--R or --C(OH)(R)--COOH, where R is alkyl or alkenyl; R3 is particularly carboxy, acyl, halogen, alkyl, alkenyl or alkylthio; and R4 is particularly --(CH2)m1 --COOR4, --(CH2)m1 --CONHR14, --(CH2)m1 --CN, --SO2 --NH--SO2 --R14, 13 NH--SO2 --R14, --PO3 R14, or --NH--SO2 --CF3, where m1 is 0-4 and R14 is hydrogen, alkyl or alkenyl; are useful for preparing pharmaceutical compositions for treating disorders resulting from abnormal stimulation of angiotensin II receptors AT1 and AT2.
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- Erythromycin derivatives
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A compound selected from the group consisting of a compound of the formula STR1 wherein R1 and R2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 24 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen and optionally having at least one functional group or taken together form STR2 and R'1 and R'2 are individually selected from the group consisting of hydrogen and an optionally unsaturated hydrocarbon of up to 23 carbon atoms optionally interrupted by at least one heteroatom selected from the group consisting of nitrogen, oxygen and sulfur and optionally having at least one functional group, Z is hydrogen or acyl of an organic carboxylic acid of 1 to 18 carbon atoms and the wavy line indicates the 10-methyl may have R or S configuration or a mixture of R+S and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic properties.
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- Condensed heterocyclic compounds, their production and use
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A condensed heterocyclic compound of the general formula: STR1 wherein Q is a condensed heterocyclic group having a nitrogen atom in the bridgehead which is unsubstituted or substituted, X is a hydrogen atom or a group attached through C, O, S or N, and Y is an electron attractive group, or its salt which is useful as agricultural chemical.
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- Multi-substituted tetrahydrofurans
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Novel odorant compositions which are characterized by a content of one or more compounds selected from the group consisting of tetrahydrofurans of structures 1 or 2, or tetrahydropyrans of structure 3. STR1 wherein R can be an acyclic, where acyclic refers to a chain of at least four carbon atoms substituted with at least three methyl groups in the chain, carbocyclic, where carbocyclic refers to a ring of 5-8 carbon atoms, and with at least two methyl groups on the ring, or bicyclic where bicyclic refers to two carbon rings, each ring having between 5-8 carbon atoms fused together, substituted with at least two methyl groups, and where R1 =CH3, or higher alkyl group, R2 =H, CH3, or higher alkyl group, R3 =H, or CH3, R4 and R5 =H, CH3, or higher alkyl group.
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- Cephalosporins
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A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula STR1 in the form of an internal salt or a non-toxic, pharmaceutically acceptable acid addition salt wherein R1, R2, R3 and R5 are individually defined in the specification, R4 is --OH or alkoxy of 1 to 8 carbon atoms, A and A' are individually selected from the group consisting of hydrogen, an equivalent of an alkali metal or alkaline earth metal, magnesium, ammonium and an organic amine, or one or two of --COOA or --COOA' ARE --CO2 --, the wavy line means --CH2 R6 can be in the E or Z position, R6 in the quaternary ammonium form is selected from the group consisting of STR2 X is defined as in the specification with the proviso that when R3 is --OH or alkoxy of 1 to 8 carbon atoms, at least one R1, R2 and R5 is other than hydrogen having antibacterial properties.
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- Aryl esters of phosphonous halides and a process for the preparation thereof
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Aryl esters of phosphonous halides of the formula I STR1 in which R' is a phenyl or benzyl radical which bears 1 to 3 substituents, α-methylbenzyl, α, α-dimethylbenzyl, naphthyl or a naphthyl radical bearing 1 to 5 substituents, where the substituents are identical or different and are a non-aromatic hydrocarbon radical, an alkoxy radical or alkylthio radical each having 1 to 8 carbon atoms, aryl or aryloxy each having 6 to 10 carbon atoms or halogen having an atomic number from 9 to 35, R2 is a non-aromatic hydrocarbon radical having 1 to 18 carbon atoms, aryl, arylmethyl, arylethyl or arylisopropyl, where each aryl contains 6 to 10 carbon atoms, R3 is hydrogen or one of the groups mentioned under R2, and X is chlorine or bromine. The invention further relates to a process for the preparation of aryl esters of phosphonous halides of the formula I.
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- Novel heterocyclic dicarboxylic acids
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A compound selected from the group consisting of a compound of the formula STR1 wherein the dotted lines represent a possible endo or exo double bond, R1 and R2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms and STR2 R'2 is alkyl of 1 to 8 carbon atoms or aryl of 6 to 14 carbon atoms, X is --O-- or --NR--, R is selected from the group consisting of hydrogen STR3 and --COOR', R' is hydrogen or alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, all optionally substituted with at least one halogen or --OH, with the proviso that if Y is --OH, X is not --NH-- and their non-toxic, pharmaceutically acceptable addition salts of acids or bases having antibacterial and immunological properties.
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- Platinum(II) complexes, their preparation and use as anti-tumor agents
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Compounds of formula I STR1 wherein R1 and R2, that can be the same or different, are hydrogen, alkyl, aryl, aralkyl groups or, if taken together, cycloalkyl groups; A is a carbon atom, a residue of 2,3-dioxybutandioic-2,4-dioxyphtalic acid or disubstituted malonic acid derivatives; n1 and n2 are selected in such a manner that the result of their addition is from 2 to 40; T1 and T2 that can be the same or different, are hydrogen, alkyl, benzyl, phenyl, acyl or cycloalkyl or a residue of formulae STR2 Compounds I are useful as anti-tumor agents in human therapy.
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- Compounds of the anthraquinone series
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Anthralin analogues containing a thio-substituent, especially in one or more of the positions 2-, 7- and 10- of the anthralin ring. They may be made by reacting an anthralin derivative (e.g. 10-bromoanthralin) with a thiol or a compound containing a group convertible to a thio-group. Alternatively, a 1,8-dihydroxy anthraquinone containing a thio-substituent may be reduced. Reactive intermediates may be made by introducing one or more nuclear allylic groups into a 1,8-dihydroxy anthraquinone and then converting them into a reactive form, e.g. by epoxydation or halide addition. The intermediate can then be reduced to the oxidation state corresponding to anthralin. Additional compounds, having the 10-carbon atom of the anthralin ring as part of a heterocyclic ring, may be made by oxidising anthralins containing various substituted thioalkyl groups as the 10-substituent. The compounds are useful for treatment of psoriasis, and may be formulated in the conventional vehicles for topical application, especially petrolatum.
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- Kinetic Isotope Effects for Proton Abstraction from Methanol by Polyhalogenomethyl Carbanions. Cleavage of Me3SiCHX2 and Me3SiCX3 by Base in Methanol.
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The carbanions XxH(3-x)C- (X=Cl or Br; x=2 or 3) generated by base cleavage of Me3SiCH(3-x)Xx (or some related compounds) in MeOH, show a kinetic isotope kH/kD of ca. 1.1 in proton abstraction from methanol, as given by the product ratio XxH(3-x)CH/XxH(3-x)CD observed for reaction in MeOH-MeOD (1:1) at ca. 21 deg C.The low value of the isotope effect is attributed to the fact that the free electron pair in the carbanion is localized on the carbon centre; carbanions derived from acids of acidities comparable with those of X3CH and X2CH2 but in which the electron pair is conjugatively delocalized, show much larger isotope effects.
- Eaborn, Colin,Stanczyk, Wlodzimierz A.
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p. 471 - 473
(2007/10/02)
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- 5-(aryl and heteroaryl)-6-(aryl and heteroaryl)-1,2-dihydro-2-oxo 3-pyridinecarboxylic acids and derivatives thereof
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This invention relates to a method of treating bacterial infections with 5-(aryl and heteroaryl)-6-(aryl and heteroaryl)-1,2-dihydro-2-oxo--3-pyridinecarboxylic acids and derivatives thereof. This invention further relates to pharmaceutical compositions that are useful in the treatment of bacterial infections.
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- Pyrrolizidine derivative and pharmaceutical composition thereof
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A novel pyrrolizidine derivative of the formula, STR1 which has potent antiarrhythmic activity and low toxicity is produced. The derivative can be synthesized: by acylating 2,6-xylidine to protect the amino group, nitrating the protected xylidine to introduce a nitro group at 3-position, reducing the nitro group to an amino group, followed by diazotizing and hydrolyzing, and then the resulted 3-hydroxy-2,6-dimethylaniline being condensed with 8-halocarbonylmethylpyrrolizidine; or by nitrating N-(2',6'-dimethyl)phenyl-8-pyrrolizidineacetamide to introduce a nitro group at 3'-position, reducing the nitro group to amino group, diazotizing the amino group and hydrolyzing the diazonium compound.
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- MECHANISMS OF FREE-RADICAL REACTIONS. XXVI. SELECTIVITY OF THE TRICHLOROMETHYL RADICAL IN HYDROGEN ABSTRACTION REACTIONS
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A method is developed for the determination of the relative rate constants for the abstraction of a hydrogen atom by the dichloromethyl radical on the basis of the decomposition of tert-butyl trichloroperacetate in the presence of two substrates, one of which is fully deuterated at the reactive positions.The value of the reaction parameter ρ in the chlorination of substituted toluenes indicates that the trichloromethyl radical has moderately low electrophilicity.The significant value of the kinetic isotope effect makes it possible to suppose that tunneling makes an appreciable contribution at the hydrogen transfer stage.
- Dneprovskii, A. S.,Iz"yurov, A. L.,Boyarskii, V. P.,Beloshapko, A. N.
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p. 2250 - 2253
(2007/10/02)
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- 2-(2-quinazolinylaminoalkoxymethyl)-1,4-dihydropyridine derivatives as cardiovascular agents
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Dihydropyridines of the formulae STR1 wherein R is chlorothienyl or mono- or disubstituted phenyl where said substituent is fluoro, chloro, bromo or trifluoromethyl; R1 and R2 are each alykl; R3 and R4 when taken separately are each hydrogen or alkyl; R3 and R4 when taken together with the nitrogen to which they are attached are piperidine or pyrrolidine; R5 is alkyl or 2-hydroxyethyl; R6 is hydrogen or methoxy; X and Z are each hydrogen or methoxy; Y is alkylene; R7 is chlorophenyl or trifluoromethyl-chlorophenyl; p is 0 or 1; and Q is CH or N are useful in the treatment of hypertension, heart failure and angina.
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- Prostaglandins
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Novel compounds have a formula (I) STR1 wherein STR2 represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R1 and at the 6-position by the group ANR2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R1 and at the 3-position by the group ANR2 R or at the 2-position by the group ANR2 R and at the 3-position by the group R1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R1 and at the 5-position by the group ANR2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R1 and at the 2-position by the group ANR2 R, R1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein; A is an unbranched or branched aliphatic hydrocarbon group with a chain length between the points of attachment to the divalent cyclic group and to the group NR2 R of 1 to 5 carbon atoms or such a group substituted by an aromatic group; R2 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups; and R is a group --CO.NR3 R4, --CS.NR3 R4, --CNH.NR3 R4, --CO.R4 or --CS.R4 in which R3 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R4 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly by an aromatic group or groups and/or through an oxygen or sulphur atom either by an aromatic group or by an aliphatic hydrocarbon group substituted directly by an aromatic group or groups. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.
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- Derivatives of cephalosporins, their process of separation and antibiotic drugs containing the said derivatives
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The present invention relates to cephalosporins having the formula: STR1 in which COOA is an acidic radical, salt or ester, and R1 represents a group: STR2 in which RA and RB are H or alkyl or together form a cycloalkyl with the carbon to which they are bonded, R2 and R3 are H, alkyl or alkenyl, R4 and R5 are H, alkyl or alkenyl or together form a ring to the nitrogen atom with which they are bonded. This invention also relates to a process for the preparation of these compounds and to drugs containing them.
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- Water-soluble alkanoyloxy and alkoxycarbonyloxy rifampicin derivatives, process for its preparation, intermediates, and its pharmaceutical composition as antibacterials
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The present invention is directed to new water soluble rifampicin derivatives which are suitable for preparing aqueous solutions for oral or parenteral administration. The new derivatives of the invention are 4 and/or 8 alkanoyl or alkanoyloxyalkyl esters of rifampicin and possess essentially the same antibacterial activity of this widely known antibiotic substance.
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- Dihydroapovincaminic acid amines
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16,17-Dihydroapovincaminic acid amides of the general formula: STR1 wherein B is an --NR1 R2 group wherein R1 is a hydrogen atom or a saturated or unsaturated, linear or branched C1-4 aliphatic hydrocarbon group, and R2 is a saturated or unsaturated, linear or branched C1-4 aliphatic hydrocarbon group, a phenyl C1-4 alkyl or a cycloalkyl C1-4 alkyl group; or B is a STR2 group wherein A is a saturated C4-6 alkylene group which may be interrupted by a hetero-atom; or a pharmaceutically acceptable acid addition salt thereof which are useful for the treatment of cardiovascular disorders, and a method for their preparation.
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