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5350742 |
Avermectin difluoro derivatives
Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are...
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5338865 |
Synthesis of halichondrin B and norhalichondrin B
Novel chemical compounds that can be used to synthesize halichondrin B and norhalichondrin B, and related derivatives, are described. The synthesis of halichondrin B and norhalichondrin B from...
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5336789 |
Macrolide compounds
Compounds of formula (I) ##STR1## and salts thereof wherein R 1 is a methyl, ethyl or isopropyl group; R 2 is a hydrogen atom or a group OR 4 (where OR 4 is a hydroxyl group or a substituted...
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5306809 |
Acid-labile linker molecules
This invention relates to the field of immune therapy of cancer, more specifically to immunoconjugates of a cytotoxic moiety with a targeting moiety, more specifically to immunoconjugates of...
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5290804 |
Anthelmintic milbemycin analogs of novel microorganisms
There is disclosed a series of macrolides isolated from the fermentation broth of microorganisms identified as MA-6825, MA-6864 and MA-6865. The structure of the novel compounds isolated from the...
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5262400 |
4α-substituted avermectin derivatives
Avermectin compounds are substituted at the 4a-position: the 4a-methyl group is first derivatized with a hydroxy group which is then substituted with a variety of alkyl, alkoxy alkyl, or polyalkoxy...
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5244879 |
23-nor-23-oxa avermectin analogs are active anthelmintic agents
Avermectin analogs are prepared where the 23-position ring carbon atom is deleted and replaced by an oxygen atom. The compounds are prepared by opening the outer spiroketal ring to gain access to...
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5240915 |
Avermectin derivatives
There are disclosed avermectin derivatives which are avermectin modified at the 3- and 4-positions. The 3-hydroxy and 4-keto, epoxide and hydroxy (hydroxymethyl) derivatives and the 4-oxo compound...
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5241083 |
Process for converting the 13-α-hydroxy group of avermectin aglycones
The natural stereochemistry at the 13-position of avermectin aglycones, normally α-oriented or below the plane of the molecule, is inverted or epimerized into the β-position. The procedure starts...
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5239064 |
A59770 antibiotics
A novel antibiotic complex, A59770, individual factors and derivatives thereof, are provided. The A59770 compounds are useful as pesticides, particularly as rodenticides. Further provided are...
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5229415 |
Alkylthio alkyl avermectins are active antiparasitic agents
Avermectin compounds are substituted at the 4", 4' or 13-postion hydroxy group with an alkylthioalkyl group and are optionally substituted at the other reactive positions of the avermectin...
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5208349 |
Process for preparing milbemycin derivatives and certain novel compounds employed therein
13-Hydroxy-5-ketomilbemycin derivatives are prepared by oxidizing a 5-ketomilbemycin with selenium dioxide in the presence of a lower aliphatic carboxylic acid. A range of new...
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5192777 |
Macrolide compounds
Compounds of formula (I) ##STR1## and salts thereof, wherein R 1 represents a methyl, ethyl or ispropyl group; R 2 represents a C 2 -7 alkyl group interrupted by an oxygen or sulphur atom or an...
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5177063 |
Avermectin compounds with a 6,5-spiroketal ring system
Avermectin analogs are disclosed wherein the 6,6-spiroketal ring system has been reduced in size to a 6,5-spiroketal ring system by the deletion of the 25-position carbon atom and the 25-alkyl...
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5169956 |
Macrolide antibiotic compounds
This invention relates to new agents designated LL-F28249α, LL-F28249β, LL-F28249γ, LL-F28249δ, LL-F28249ε, LL-F28249ζ, LL-F28249η, LL-F28249θ, LL-F28249.iota., LL-F28249κ, LL-F28249λ,...
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5162550 |
Bisphthalide lactones, their preparation and the use thereof in recording materials
Bisphthalide lactones of formula ##STR1## wherein R 1 , R 2 , R 3 and R 4 are each independently of one another hydrogen, alkyl of at most 12 carbon atoms which is unsubstituted or substituted by...
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5149832 |
Mono and diacyl derivatives of LL-F28249 Compounds
The present invention relates to novel 5-acyl, 23-acyl and 5,23-diacyl derivtaives of the LL-F28249 compounds. These LL-F28249 compounds (collectively) are isolates from the fermentation broth of...
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5140042 |
28-hydroxy ivermectin aglycone
Fermentation of S. erythraea produces the novel avermectin, 28-hydroxy ivermectin aglycone.
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5122618 |
Insecticides and parasiticides
The present invention relates to novel derivatives of formula I that can be derived from milbemycins, to their preparation and their use for controlling pests, and also to pesticides that contain...
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5118705 |
Water soluble salts of purpuromycin and pharmaceutical formulations thereof
Water soluble salts of purpuromycin, their use for the topical treatment of infectious vaginitis and topical dosage forms containing said products. Oral and parenteral formulations for...
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5116968 |
Macrolide compounds
Compounds of formula (1) ##STR1## wherein R represents a sugar residue or an acylated derivative thereof; R 1 represents a methyl, ethyl or isopropyl group; Y 1 is --CH 2 , Y 2 is --CH--...
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5104871 |
Macrolide compounds
Compounds of formula (I) ##STR1## and salts thereof, wherein R is a C 1 -4 alkyl group, R 1 is a methyl, ethyl or isopropyl group; and OR 2 is a hydroxyl or substituted hydroxyl group having up...
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5077308 |
Avermectin ketal derivatives useful as antiparasitic
There are disclosed avermectin aglycone derivatives which incorporate a ketal at position 13. The synthetic ketal analogs are derived from the corresponding ketones which in turn are prepared by...
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5073567 |
Antiparasitic agent
An antibiotic compound of the formula: ##STR1## is an antiparasitic agent active against insect pests, acari, free living nematodes and endo- and ectoparasites. It is prepared by fermentation using...
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5071871 |
Pharmaceutically useful benzo(β)pyranes and pyranopyridines
New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R 3 to R 5 , R 9 , R 10 , m, X, Y and Z are given in claim 1 and their N-oxides and...
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5066670 |
Macrolide derivatives with parasiticidal activity
Compounds of formula (I): ##STR1## wherein R 1 is methoxy or optionally protected hydroxy have anthelmintic activity and are useful in the treatment of helminthiasis in humans and animals.
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5057499 |
Avermectin derivatives
There are disclosed novel avermectin derivatives wherein the outer oleandrose ring of avermectin or avermectin monosaccharide is homologated by addition of diazomethane to 4"- or 4'-oxo-avermectin...
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5057536 |
Macrolide compounds
Compounds of formula (1) ##STR1## and salts thereof, wherein R 1 represents a methyl, ethyl or isopropyl group; Y 1 is --CH 2 --, Y 2 is --CH-- and X represents ##STR2## where R 2 ...
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5055596 |
Derivatives of avermectin and milbemycin
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 hydrogen,...
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5055486 |
13-alkyl-23-imino derivative of LL-F28249 compounds and their use as endo- and ectoparasiticidal, insecticidal, acaricidal and nematocidal agents
There are provided certain 13-alkyl-23-imino-LL-F28249 compounds which are useful for controlling endo- and ectoparasites, insects, acarids and nematodes.
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5055454 |
13-epi-avermectin derivatives useful as antiparasitic agents
There are disclosed avermectin derivatives in which position 13 of the avermectins has been inverted from the normal (alpha) stereoschemistry to the epimeric 13-beta stereochemistry. The synthetic...
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5034542 |
Preparation of macrolide compounds
A process for the preparation of a compound of formula (I) ##STR1## (in which R 1 is methyl, ethyl or isopropyl) by hydrogenation of a corresponding compound having a double bond at the...
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5030650 |
13-halo-23-imino derivatives of LL-F28249 compounds and their use as endo- and ectoparasiticidal, insecticidal, acaricidal and nematocidal agents
There are provided certain 13-halo-23-imino-LL-F28249 compounds which are useful for controlling endo- and ectoparasites, insects, acarids and nematodes.
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5023348 |
Process for the preparation of macrolide compounds
A process for preparing a compound of formula (I) ##STR1## (where (i) R 1 is an ethoxy group and R 2 is a hydrogen atom, (ii) R 1 is a hydrogen atom and R 2 is a bromine atom or (iii) (R 1 and...
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5019589 |
Δ.sup.23 -LL-F28249 compounds
The present invention relates to novel derivatives of LL-F28249 compounds wherein the 23-hydroxy group is eliminated to introduce a double bond at the 23,24 position. These resulting derivatives...
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5015630 |
5-oxime avermectin derivatives
Novel avermectin derivatives are disclosed, wherein the 5-hydroxy group is replaced by an oxime group. The avermectin-5-oximes can further be derivatized at the 4"- or 4'-positions as amino,...
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5008405 |
Selective etherification
There is disclosed an improved process for substitution of the hydroxy group at 2-position of an ascorbic acid derivative according to the following reaction scheme: ##STR1## wherein R 0 is...
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5008250 |
Avermectins with a cleaved furan ring and an 8a hydroxy group
There are disclosed novel avermectin compounds having a cleaved furan ring and a hydroxy group in the 8a position. Processes for preparing these novel compounds are also disclosed. These compounds...
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5001255 |
Idene analogs of mevalonolactone and derivatives thereof
Compounds of the formula ##STR1## the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and...
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5001128 |
HMG-COA reductase inhibitors
Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy...
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4996228 |
Macrolide antibiotics
Compounds are described of formula (I) ##STR1## and salts therof, wherein R 1 represents a methyl, ethyl or isopropyl group; R 2 is alkyl; alkyl substituted by a carboxy or alkoxycarbonyl;...
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4988824 |
Process for the preparation of 23-(C1-C6 alkyloxime)-LL-F28249 compounds
There is provided a process for the preparation of 23-(C 1 -C 6 alkyloxime)-LL-F28249 compounds via the oxidation of crystalline 5-O-p-nitrobenzoyl-LL-F28249 compounds.
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4978677 |
C(29)-carbonyloxymilbemycin derivatives for controlling parasitic pets of animals and plants
the invention relates to novel C(29)-carbonyloxymilbemycin derivatives of formula I, to the preparation thereof and to the use thereof ffor controlling pests, as well as to pesticidal compositions...
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4978675 |
Macrolide antibiotics and their preparation
Compounds are described of formula (II) ##STR1## and salts thereof, wherein R 1 reprsents a methyl, ethyl or isopropyl group; R 2 represents a hydrogen atom or a group OR 5 (where OR 5 is a...
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4973711 |
Composition for controlling parasites in productive livestock
Novel 13-spiro-2'-[tetrahydrofuran]-milbemycins of the formula I ##STR1## in which X represents one of the groups --CH(OR 1 )--, --C(O)-- or --C(N--OH)--; R 1 represents hydrogen or a...
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4959386 |
Pesticides
The present invention relates to novel compounds of the formula ##STR1## wherein R 1 is hydrogen, a silyl group or an acyl group, R 2 is methyl, ethyl, is propyl or sec-butyl, and R is...
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4956479 |
23-deoxy-27-chloro derivatives of LL-F28249 compounds
The present invention relates to novel derivatives of LL-F28249 compounds. These LL-F28249 compounds preferably are derived via a controlled microbiological fermentation of Streptomyces...
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4954484 |
Parasiticides and insecticides
Novel compounds of formula ##STR1## in which A is a ##STR2## group wherein R 1 is hydrogen or an OH-protecting group, and R 11 is hydrogen, an OH-protecting group, or an alkyl, cycloalkyl or acyl...
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4950683 |
Macrolide antibiotics
Compounds are described of formula (I) ##STR1## and salts thereof, wherein OR is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms, R 1 represents a methyl, ethyl or...
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4945105 |
13-Halomilbemycin derivatives, their preparation and compositions containing them
Derivatives of milbemycins D, A 3 and A 4 and of the corresponding sec-butyl compound have a halogen atom at the 13-position; at the 5-position, they have an oxygen (keto) atom, an oxime group or...
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