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7576124 |
Anti-first-pass effect compounds
Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for their preparation and for...
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7576123 |
Anti-first-pass effect compounds
Compositions, methods, etc. for addressing the first-pass effect.
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7316884 |
5-methylene-1,3-dioxolan-4-one derivatives, process for their production, polymers of the derivatives, resist compositions, and pattern formation process
A 5-methylene-1,3-dioxolan-4-one derivative and a monomer and copolymer thereof and a resist composition containing the polymer or copolymer where the 5-methylene-1,3 -dioxolan-4-one derivative is...
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7314942 |
Methylenelactones syntheses in supercritical fluids
Alpha-methylenelactone is produced from butyrolactone and valerolactone by the addition of formaldehyde in a supercritical fluid.
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7232915 |
Process for the synthesis of 1,3-diols
An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a...
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6808724 |
Artemisolide compound isolated from the aerial parts of Artemisia sylvatica, isolation method, and use thereof
The present invention relates to a novel compound isolated from Artemisia Sylvatica , expressed by the formula 1, a method of isolation, and its use thereof, and more particularly to a novel...
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6486195 |
Thermodynamically stable crystal form of 4″-deoxy-4″-epi-methylamino avermectin B1a/B1b benzoic acid salt and processes for its preparation
The most thermodynamically stable crystalline form of the benzoic acid salt of 4″-deoxy-4″-epi-methylamino avermectin B1a/B1b as the hemihydrate is obtained by crystallization from organic...
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6410590 |
Compounds having antitumor activity: process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel derivatives of Andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable...
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6388099 |
Production of 8,8a-dihydroxy-6-deoxyerythronolide B
The heterologous expression of the OlePKS in Streptomyces lividans , produces 8,8a-deoxyoleandolide, an aglycone precursor of oleandomycin. The co-expression with DEBS in S. lividans of the P450...
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6387948 |
8-Acetylarteminolide and process for preparing same
8-Acetylarteminolide of the formula (I) having inhibitory activities against farnesyl-protein transferase(FPTase), a progression of the cell cycle and angiogenesis may be useful for the prevention...
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6372781 |
Compounds for treating gastroduodenal diseases
Spirolaxine, the compound of formula (I) wherein R is H, and the novel compounds of formula (I) wherein R is (C 1 -C 5 ) alkyl or CH 3 (CH 2 ) n CO and n is 1, 2, 3 or 4 are useful in treating...
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6362168 |
Antiparasitic agents
Compounds of the formula: wherein X represents a single or a double bond; R 1 is H or OH; provided that when X is a single bond, R 1 is H or OH, and when X is a double bond, R 1 is absent; R...
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6355810 |
Multibinding inhibitors of HMG-CoA reductase
Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-COA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding...
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6255337 |
Anti-first-pass effect compounds and citrus extract
First-pass effective substances derived from citrus.
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6239073 |
Brassinosteroid analogs useful as plant growth regulators
Disclosed are compositions and methods for promoting plant growth. The compounds are cyclopropyl-, cyclobutyl-, and cyclopentyl-substituted brassinosteroids having high growth promoting ability....
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6174710 |
Spirolaxine derivatives for treating gastrobuodenal diseases
Spirolaxine, the compound of formula (I) ##STR1## wherein R is H, and the novel compounds of formula (I) wherein R is (C 1 -C 6 )alkyl or CH 3 (CH 2 ) n CO and n is 1, 2, 3 or 4 are useful in...
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5962659 |
Anthelmintic milbemycins and avermectins
Novel compounds of formula (I): ##STR1## wherein R 1 is hydrogen or optionally protected hydroxy; R 2 is alkoxy, optionally protected hydroxy, oxo or optionally O-substituted oximino; R 3 is...
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5883080 |
Antiparastic auermectin derivatives
Antiparasitic avermectin derivatives of formula (I), where the broken line represents an optional bond, R 1 and R 4 are independently H, OH, halo, oximino, or an organic radical, R 2 , R 6 and R...
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5871938 |
Dioxetane compounds for the chemiluminescent detection of proteases, methods of use and kits therefore
1,2-dioxetane compounds bearing a proteolytic enzyme specific amino acid or peptide are provided, which amino acid or peptide can be removed by action of the corresponding protease. When the amino...
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5861518 |
Phthalide compounds and their production process
This invention provides processes for producing phthalide compounds which comprise cultivating Phanerochaete avelutina FERM BP-4787 and then isolating phthalide compounds from the fermentation broth.
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5861429 |
13-substituted milbemycin 5-oxime derivatives, their preparation and their use against insects and other pests
Compounds of formula (I): ##STR1## wherein: R 1 is methyl, ethyl, isopropyl or sec-butyl; X is carbonyl or methylene; Z is C(R 2 ) 2 or C(CH 2 ) m , in which R 2 is alkyl, and m is...
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5840728 |
Conformationally locked nucleoside analogs as antiherpetic agents
A method for treatment of herpes virus infection by administering an effective virus-inhibiting amount of a cyclopropanated carbocyclic 2'-deoxynucleoside to an individual in need thereof. The...
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5840704 |
Antiparasitic agents and process for their preparation
The invention provides novel compounds having the formula: ##STR1## wherein R when taken individually is H; R 1 when taken individually is H or OH; R and R 1 when taken together represent a...
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5830875 |
24-and 25-substituted avermectin and milbemycin derivatives
Novel avermectin and milbemycin derivatives are disclosed, where the C-24 and C-25 carbon atoms are substituted by hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl groups. These...
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5811034 |
7-methylidene-5-oxo-furo fused naphthopyrans
Described are novel 7-methylidene-5-oxo-furo fused naphthopyran compounds having certain substituents at the 2 position of the pyran ring. Also described are polymeric organic host materials that...
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5728719 |
Systemic control of parasites
The present invention is a method for controlling ectoparasites. More particularly, the invention relates to a method of treatment in which the warm blooded animal is dosed with an ovicidally...
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5721271 |
Parasiticidal milbemycin derivatives
Compounds of formula (I): ##STR1## wherein R 1 is hydrogen or methyl, R 2 is hydrogen or (E)-2-methyl 2-butenoyloxy, and R 3 is hydrogen or hydroxy, with the proviso that when R 3 is hydrogen,...
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5686484 |
Milbemycin derivatives, their preparation and their use
Compounds of formula (I): ##STR1## and of formula (I) w : ##STR2## in which: A represents group having one of the following formulae: ##STR3## wherein R 2 , R 3 and R 4 are independently...
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5677332 |
Antiparasitic agents
This invention is directed to novel antiparasitic compounds of formula (I), wherein the broken line represents an optional bond, R 1 and R 4 being absent when this bond is present, R 1 , R 3 , R...
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5656748 |
Process for the preparation of ivermectin
The invention relates to a process for the selective hydrogenation of avermectins with the aid of a rhodium-phosphine complex based on a hydrazine.
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5625078 |
Processes for the production of 13-ether derivatives of milbemycins and novel intermediates therefor
An intermediate useful in the synthesis of milbemycin derivatives having an ether bond at the 13-position and which is represented by the general formula (IIId): ##STR1## wherein R represents a...
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5616729 |
Enhanced chemiluminescence from 1,2-dioxetanes through energy transfer to tethered fluorescers
Triggerable dioxetanes with a fluorescent substituent bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are of the formula: ##STR1##...
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5614470 |
13-substituted milbemycin derivatives, their preparation and their use
13-Substituted milbemycin derivatives having the formula (I): ##STR1## wherein: R 1 is methyl, ethyl, isopropyl or sec-butyl; R 2 is hydrogen or alkyl; X is (α-hydroxyimino- or...
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5604182 |
Milbemycin ether derivatives, their preparation and their therapeutic and agrochemical uses
Compounds of formula (I): ##STR1## and salts and esters thereof have valuable anthelmintic, acaricidal and insecticidal activities. Methods of preparing the compounds are also provided.
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5559249 |
7'-amino-naphthazarin antibiotic derivatives
Compound of general formula V ##STR1## wherein Hal is a chlorine or bromine atom. The compounds are useful as starting materials in preparing gamma-rubromicin amino derivatives.
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5556868 |
Antiparasitic avermectin and milbemycin derivatives
Avermectin and milbemycin derivatives of formula (I) ##STR1## having a double bond at the 3-4 position and a cyano substituent at the 3-position have outstanding anthelmintic properties. They may...
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5539089 |
A83543 aglycones and pseudoglycones
A83543 Aglycones A83543AgA, A83543AgD, A83543AgE, and A83543AgF, and A83543 pseudoaglycones A83543PsaA2, A83543PsaB2, A83543PsaD2, and A83543PsaN2 are intermediates useful in preparation of known...
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5519050 |
Isolation and structural elucidation of halistatin 3
The Micronesian marine sponge Phakellia sp. has been found to contain cern key members of the antineoplastic halichondrin/halistatin family. These compounds include halichondrin B, homohalichondrin...
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5510372 |
Antiparasitic macrolide antiobiotics
The present invention relates to certain antibiotic compounds, designated N787-182 compounds herein and derivatives thereof, which are antiparasitic agents, active against insect pest, acari,...
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5478951 |
Method for the purification of 23-E isomers of 23-imino derivatives of LL-F28249 compounds
The present invention provides a method for the purification of a 23-E isomer of a 23-imino derivative of a LL-F28249 compound having the structural formula I ##STR1##
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5436355 |
Process for making avermectin/zein compositions
Their is disclosed a novel solvent-depletion process for making an avermectin/zein composition and the composition itself, which has excellent photostability and unexpected bioavailability to...
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5420260 |
Process for 4"-epi-acetylamino-4"-deoxy-5-oximinoavermectin B.sub.1
An improved process for formation of a 5-oxime on avermectin derivatives comprises the treatment of the oxo-compound with hydroxylamine in aqueous isopropanol at pH 1.8-2.1.
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5411946 |
Avermectin derivatives
Avermectin derivatives, wherein the C-17-21-25-dioxaspirane substructure has been modified to include substitutions of heteratomic nucleophilic thiols at the 23,24-α-epoxide. These compounds can...
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5405867 |
Macrolide compounds, their preparation and their use
Compounds having a 16-membered macrolide ring, and related to the milbemycins and avermectins, with substituents at positions 5.13, 25 and optionally also 23, have acaricidal, insecticidal and...
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5399717 |
Glycosidation route to 4"-epi-methylamino-4"-deoxyavermectin B.sub.1
A stereocontrolled glycosidation with thiophenyl 4-(N-allyloxycarbonyl)-epi-methylamino-4-deoxyoleandrose and 5-O-allyloxycarbonyl avermectin B 1 monosaccharide using N-iodosuccinimide produces...
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5384078 |
Soluble highly reactive form of calcium and reagents thereof
A soluble highly reactive form of calcium, prepared from Ca(II) salts and a reducing agent in ethereal, polyethereal, or hydrocarbon solvents, is presented. This form of calcium can be used in the...
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5380838 |
Stable solvates of avermectin compounds
There is disclosed a novel form of avermectin compounds wherein the avermectin compounds are crystallized as alcohol solvates to greatly enhance stability of the avermectin drug during long-term...
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5376678 |
Active principle based on avermectins, related strain and process for the preparation thereof, as well as veterinary compositions containing it
By carrying out the fermentation of Streptomyces avermitilis ATCC 55278, a dried mycelium is obtained which, orally administered to animals, particularly to ovines, has an antiparasitic activity.
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5360917 |
Process for producing macrolide compounds
A process for recovering at least one Antibiotics S541 compound or chemical derivative thereof from solution in an organic solvent, which comprises the steps of contacting the said solution with...
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5352804 |
Isolation and structure of Halistatin 2
An intensive long-term investigation of marine organisms as sources of new anticancer drugs has led to the isolation and structural elucidation (primarily by high field NMR and mass spectrometry)...
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