- Synthesis and characterization of novel analogues of cefpodoxime proxetil
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The present work describes the origin, identification, synthesis, characterization and control of four novel analogues of cefpodoxime proxetil, which are ethyl, methyl, propyl and N-propyl analogues of cefpodoxime proxetil.
- Reddy, Peketi Rajesh,Musunuri, Sivanadh,Reddy, D. Ramasekhara,Chittala, V. Subrahmanyam,Murthy,Krishnamohan
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- Regioselective synthesis of 2-O-acyl-3-O-(1-acyloxyalkyl) prodrugs of 5,6-isopropylidene-L-ascorbic acid
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An efficient regioselective synthesis of 2-O-acyl-3-O-(1-acyloxyalkyl) prodrugs of vitamin C 5,6-acetonide has been developed which does not involve tedious column chromatographic separation of the desired products from contaminants exhibiting very similar Rf values. Vitamin C 5,6-acetonide is first acylated with one equivalent of acyl halide in the presence of two equivalents of pyridine. The crude 2-O-acylated product is then alkylated with one equivalent of 1-acyloxyalkyl-1-iodide in the presence of one equivalent of triethylamine. The 2-O-acyl-3-O-(1-acyloxyalkyl) vitamin C 5,6-acetonides are obtained in moderate yields.
- Prybylski, John,Thiele, Nikki A.,Sloan, Kenneth B.
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- Benzodiazepine compound as well as preparation method and medical action thereof (by machine translation)
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The invention provides a benzodiazepine compound as well as a preparation method and a medicine effect thereof, and belongs to the field of chemical medicine. The benzodiazepine compound is a compound shown in formula I. Or a salt thereof, or a stereoisomer thereof, or a solvate thereof, or a eutectic thereof, or a composition thereof. The anesthetic effect of the compound of the invention is good, and the anesthetic effect of the compound is equivalent to that of Ramozolam, and even better than that of repirzolam, and particularly shows that the effective dosage is obviously reduced, and the duration and the recovery time are remarkably reduced. At the same time, in the rat tail vein anesthesia model, the compound of the present invention is remarkably improved in comparison with the quality of the Ramozolam wake-up. The compound has the advantages of high effectiveness, short duration, fast resuscitation and good tolerance, can be used for anesthesia induction, anesthesia maintenance and inter-day operation anesthesia, and has a good application prospect. (by machine translation)
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Paragraph 0234-0236
(2021/01/11)
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- PYRAZOLE DERIVATIVE
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A pyrazole derivative having the following formula stru-1: The pyrazole derivative is used for prevention and control of pests.
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Paragraph 0100; 0114; 0116-0117
(2020/11/30)
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- Halogenated imidazole compound as well as preparation method and application thereof
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The invention discloses alogenated imidazole compounds as well as a preparation method and application thereof. The structure of the halogenated imidazole compounds is disclosed in the invention, wherein, C * in the formula is R-type chiral carbon, and R1 and R2 can be independently selected from H and C1-6 alkyl; R3 is a substituted or unsubstituted C1-18 saturated or unsaturated aliphatic hydrocarbon, the aliphatic hydrocarbon comprises linear, branched or cyclic aliphatic hydrocarbon groups; X is H or a halogen atom; Y is H or a halogen atom; and X and Y cannot be H at the same time. The compounds or pharmaceutically acceptable salts or solvates thereof almost have no corticoid inhibition effect, can generate a rapid reversible anesthetic effect, can be rapidly metabolized into inactivecarboxylic acid metabolites, and have good revival quality after drug withdrawal; the corticoid function of the body can be rapidly recovered after single administration or continuous administration,the occurrence rate of muscular tremor after administration is low, and the body is rapidly awakened after drug withdrawal. The compounds or the salt compounds thereof can be used for preparing central inhibitory drugs which have sedative-hypnotic and/or anesthetic effects on humans or animals.
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Paragraph 0025-0031
(2020/01/25)
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- N-substituted imidazole carboxylate compound, preparation method and use thereof
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A N-substituted imidazole carboxylate compound shown as a formula (I), a preparation method and use thereof are disclosed. In the formula (I), C * is a R type chiral carbon atom, R 1 and R 2 are independently selected from the group consisting of H, methyl, ethyl, cyclopropyl, cyclobutyl or isopropyl or a C2-5 ene-group formed by R1 and R2; and R3 is substituted or unsubstituted C1-18 saturated orunsaturated aliphatic hydrocarbon or aromatic hydrocarbon, wherein the aliphatic hydrocarbon includes a linear, branched or cyclic aliphatic hydrocarbon group. The N-substituted imidazole carboxylatecompound or pharmaceutically acceptable salts thereof can be used to prepare central inhibitory drugs that exert sedative, hypnotic and/or anesthetic effects on humans or animals, can produce rapid and reversible anesthetic effects, and rapidly metabolises into inactive etomidate acid, and after drug withdrawal, recovery quality is good; body's corticosteroid function can be quickly recovered after single administration or continuous administration, the incidence of muscle tremor is low after the administration, and after the drug withdrawal, the recovery is quick.
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Paragraph 0098
(2018/03/26)
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- A class of pyrazole derivatives, preparation method and application thereof (by machine translation)
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The invention discloses a following formula stru - 1 indicated by the pyrazole derivatives, The definition of each substituent in the specification. This invention relates to pyrazole derivatives suitable for use in the pest. (by machine translation)
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Paragraph 0228; 0229; 0230
(2018/10/11)
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- NEW HYDROXYACID DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, A and n are as defined in the description. Medicaments.
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Page/Page column 70
(2017/01/09)
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- Substituted aza indole compounds and salts thereof, composition and use thereof
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The invention provides a substituted azaindole compound having a structure as represented by a formula (I) and a pharmaceutically acceptable salt and a medicinal preparation thereof. The compound is used for adjusting activity of protein kinase and adjusting intercellular or intracellular signal response. The invention further relates to a pharmaceutical composition including the compound and a method of applying the pharmaceutical composition to treatment of highly proliferative diseases of mammals, especially of mankind.
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Paragraph 0586; 0587; 0602; 0604; 0605
(2018/11/03)
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- New orally active dual enkephalinase inhibitors (DENKIs) for central and peripheral pain treatment
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Protecting enkephalins, endogenous opioid peptides released in response to nociceptive stimuli, is an innovative approach for acute and neuropathic pain alleviation. This is achieved by inhibition of their enzymatic degradation by two membrane-bound Zn-metallopeptidases, neprilysin (NEP, EC 3.4.24.11) and aminopeptidase N (APN, EC 3.4.11.2). Selective and efficient inhibitors of both enzymes, designated enkephalinases, have been designed that markedly increase extracellular concentrations and half-lives of enkephalins, inducing potent antinociceptive effects. Several chemical families of Dual ENKephalinase Inhibitors (DENKIs) have previously been developed but devoid of oral activity. We report here the design and synthesis of new pro-drugs, derived from co-drugs combining a NEP and an APN inhibitor through a disulfide bond with side chains improving oral bioavailability. Their pharmacological properties were assessed in various animal models of pain targeting central and/or peripheral opioid systems. Considering its efficacy in acute and neuropathic pain, one of these new DENKIs, 19-IIIa, was selected for clinical development.
- Poras, Hervé,Bonnard, Elisabeth,Dangé, Emilie,Fournié-Zaluski, Marie-Claude,Roques, Bernard P.
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supporting information
p. 5748 - 5763
(2014/08/05)
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- SUBSTITUTED AZAINDOLE COMPOUNDS, SALTS, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHODS OF USE
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The present invention provides substituted azaindole prodrugs, methods of making said prodrugs, pharmaceutical compositions of said prodrugs and methods of using said prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as cancer.
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Paragraph 0435-0436; 0447-0448
(2014/03/24)
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- PYRIDAZIN-3(2H)-ONE DERIVATIVES AND THEIR USE AS PDE4 INHIBITORS
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The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives, to processes for their preparation and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention and suppression of related pathological conditions, diseases and disorders, in particular asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, topic dermatitis, psoriasis or irritable bowel disease.
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Page/Page column 66-67
(2008/06/13)
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- BENZIMIDAZOLE COMPOUND, PROCESS FOR PRODUCING THE SAME, AND USE THEREOF
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The present invention relates to a compound represented by the following formula wherein each symbol is as defined in the specification, or a salt thereof, which has superior stability to acid and which is a prodrug of 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-1H-benzimidazole. This compound (1) shows a superior anti-ulcer activity, a gastric acid secretion-suppressive action, a mucosa-protecting action, an anti-Helicobacter pylori action and the like in living organisms, (2) shows low toxicity, (3) shows superior stability to acid (which obviates the need to formulate an enteric-coated preparation, thereby lowering the cost, and reduces the size of preparation to facilitate swallowing for patients having difficulty in swallowing), (4) shows faster absorption than enteric-coated preparations (rapid expression of gastric acid secretion-suppressive action), and (5) is sustainable.
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- Contrast agents comprising gas-containing or gas-generating polymer microparticles or microballoons
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Contrast agents comprising gas-containing or gas-generating polymer microparticles and/or microballoons, in which the polymer is a biodegradable polymer containing units of formula (wherein R1 and R2 each represent hydrogen or a carbon-attached monovalent organic group or together form a carbon-attached divalent organic group, and m and n are each independently zero or one) may be used in diagnostic applications such as ultrasound and MR imaging.
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- Cleavage of carbon-sulfur bonds in the synthesis of α-haloalkyl carbonates
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α-Chloroalkyl and α-bromoalkyl carbonates have been prepared by cleavage of α-arylthioalkyl carbonates with sulfuryl chloride or bromine, respectively. The α-arylthioalkyl carbonates are prepared by reaction of the hemithioacetal 1 with chloroformates or by a destannylative tin-Pummerer rearrangement of α-stannyl sulfoxides. Acta Chemica Scandinavica 1996.
- Hatlelid, Jostein,Benneche, Tore,Undheim, Kjell
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p. 1041 - 1044
(2007/10/03)
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- Synthesis of iodoalkylacylates and their use in the preparation of S-alkyl phosphorothiolates
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Synthesis of iodoalkylacylates 3a-f and use of 3c in the preparation of an oligonucleoside phosphorothiate prodrug analog 5 is described.
- Iyer,Yu,Ho,Agrawal
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p. 2739 - 2749
(2007/10/02)
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- Alkyl 1-Chloroalkyl Carbonates: Reagents for the Synthesis of Carbamates and Protection of Amino Groups
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The synthesis of 1-chloroalkyl carbonates and their reaction with various type of amines are described.This reaction is useful for the synthesis of carbamate pesticides and for the protection of various amino groups, including amino acids.
- Barcelo, Gerard,Senet, Jean-Pierre,Sennyey, Gerard,Bensoam, Jean,Loffet, Albert
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p. 627 - 632
(2007/10/02)
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- [(Alkoxycarbonyl)oxy]alkyl esters of methyldopa
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Novel prodrugs of methyldopa which are [(alkoxycarbonyl)oxy]alkyl esters of methyldopa are disclosed. Also, pharmaceutical compositions containing these compounds are disclosed. Upon administration to warm-blooded animals, these prodrugs liberate methyldopa along with innocuous side products.
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- Carbapenams and carbapen-2-ems and process therefor
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Carbapenam-3-carboxylic acids and carbapen-2-em-3-carboxylic acids substituted at the 1-position with an oxo, a hydroxy or an acetoxy group, variously substituted at the 2-position with such groups as methyl, acetoxymethyl, methanesulfonyloxy, alkoxy, alkylthio, aminoalkylthio or amidinoalkylthio and optionally substituted at the 6-position with a hydroxyalkyl group, an acetoxyalkyl group or a conventional penicillin side-chain, pharmaceutically-acceptable salts thereof and various esters thereof wherein the esterifying group is selectively removed in the laboratory, or hydrolyzed under physiological conditions. These compounds are useful either systemically or topically in the treatment of diseases caused by susceptible microorganisms, as animal feed additives for promotion of growth, or in the preservation of biodegradable materials, or as intermediates to compounds having such antibacterial activity. Key to the synthesis of these compounds is the light catalyzed rearrangement of 2-diazo-1-oxoceph-3-em-4-carboxylates to 1-oxocarbapen-2-em-3-carboxylates, a newly discovered reaction determined to be of general applicability.
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