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| Number | Title | Issue Date |
| 5599950 | Preparation process of ginkgolide B from ginkgolide C A two-step process for converting ginkgolide C into ginkgolide B is disclosed. In the first step, ginkgolide C is reacted with a sulfonic anhydride to obtain a C-7 sulfonate of ginkgolide C. In the second step, the C-7 sulfonate of ginkgolide C is reacted... | 02/04/1997 |
| 5541223 | 4ଲ-amino podophyllotoxin analog compounds and methods Novel podophyllotoxin compounds and their use in treating tumors are disclosed. The analogs have the general formula: ##STR1## wherein NH--R is a selected aryl amine, dialkylaminoalkyleneamino, or dialkylaminoanilino group.... | 07/30/1996 |
| 5527924 | Total synthesis of taxol The present invention provides two basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as w... | 06/18/1996 |
| 5519151 | Process for preparing polyfluorooxetanes This invention concerns a process for the preparation of polyfluorooxetanes by the reaction of fluoroketones or fluoroepoxides with haloethylenes in the presence of a Lewis acid catalyst. Polyfluorooxetanes are useful as solvents and plasticizers having h... | 05/21/1996 |
| 5508447 | Short synthetic route to taxol and taxol derivatives A short route to the total synthesis of the core skeleton of the taxol ring system is described. The same sequence of transformations can be carried out to make the 7-hydroxy series, and connect the additional carbon atoms required for the A-ring. The num... | 04/16/1996 |
| 5502217 | Process for preparing lactones A lactone is prepared by catalytically hydrogenating a dicarboxylic acid having 3 to 10 carbon atoms or a functional derivative thereof in the presence of a catalyst comprising a metal selected from the elements of group VIII of the periodic table or a co... | 03/26/1996 |
| 5494930 | Caribenolide I Compound (1), isolated from a marine dinoflagellate, is a novel macrolide which has potent in vitro cytotoxicity against human colon carcinoma cell line HCT116 (IC50 =1.6 nM) and a multiple drug resistant subline. In addition, this compound has... | 02/27/1996 |
| 5489601 | Taxanes having a pyridyl substituted side-chain and pharmaceutical compositions containing them Taxane derivatives having a 3' pyridyl substituted C13 side chain.... | 02/06/1996 |
| 5488116 | Total synthesis of taxol and analogues thereof The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as... | 01/30/1996 |
| 5482701 | Microporous alkali metal bicarbonate This invention provides microporous alkali metal bicarbonate, which can contain an absorbed gaseous, liquid or solid phase as an encapsulated ingredient. A present invention microporous bicarbonate composition has utility as a lightweight deodorant ingred... | 01/09/1996 |
| 5481008 | Process for the preparation of optically active compounds A catalytic process for the manufacture of optically active compounds of the formula ##STR1## wherein R1 and R2 are alkyl, which is optionally interrupted by an O atom in a position other than the -or ଲ-position, or... | 01/02/1996 |
| 5480906 | Stereochemical Wortmannin derivatives This invention relates to derivatives of Wortmannin and particularly to 11,17 substituted derivatives of Wortmannin. The invention also relates to a method of using these compounds as PI-3-kinase inhibitors and as anti-tumor agents.... | 01/02/1996 |
| 5480992 | Anomeric fluororibosyl amines Anomeric 2,2-difluororibosyl azide and amine intermediates which are useful for the preparation of 2'-deoxynucleosides, and processes thereto, are provided. Processes for preparing 2'-deoxynucleosides also are provided.... | 01/02/1996 |
| 5478854 | Deoxy taxols Rg is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, or a radical of the formula --W--Rx in which W is a bond, C2-6 alkenediyl, or --(CH2)t --, in whic... | 12/26/1995 |
| 5472962 | Benzothiophene derivative A benzothiophene derivative represented by the formula ##STR1## or a salt thereof has an excellent antiestrogenic activity, and is useful as a therapeutic agent of breast cancer, endometrial cancer, endometriosis, mastopathy, etc. This compound is ch... | 12/05/1995 |
| 5473083 | Reduced and quaternized psoralens as photo-activated therapeutics The invention features phototherapeutic compositions comprising Type 1, Type 2, or Type 3 psoralens and methods of using such compounds for treatment of proliferative diseases of skin, blood and bone marrow.... | 12/05/1995 |
| 5470866 | Method for the conversion of cephalomannine to taxol and for the preparation of n-acyl analogs of taxol The natural product cephalomannine can be converted to the important anticancer natural product taxol by a simple process involving the steps of dihydroxylation to give cephalomannine-diols, diol cleavage, benzoylation at the 2'-position and reaction with... | 11/28/1995 |
| 5468769 | Paclitaxel derivatives A compound or prodrug thereof having the formula ##STR1## wherein --OR1 comprises the C-13 side-chain of taxol and Z is selected from the group consisting of --CHO, --CH2 OH, --CH2 OR', --CH2 NR'R", --CH.db... | 11/21/1995 |
| 5466834 | Preparation of substituted isoserine esters using metal alkoxides and .beta . A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a ଲ-lactam.... | 11/14/1995 |
| 5466810 | 2-amino-3-aroyl-benzo[ଲ]thiophenes and methods for preparing and using same to produce 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-aminoethoxy)-benzoyl]benzo[ଲ] thiophenes A group of 2-amino-3-aroyl-benzo[ଲ]thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the -hydroxy thioamide, and subsequently acylating the benzo[ଲ]thiophene to yield the 2-amino-3-a... | 11/14/1995 |
| 5466829 | Ginkgolide derivatives and a process for preparing them The present invention relates to new ginkgolide derivatives of the formula (I) as below which represents PAF-antagonistic activity and the method for the preparation thereof, by that the cyclic compounds of substituted Ginkgolide B derivatives are produce... | 11/14/1995 |
| 5463085 | Synthesis method of physiologically active delta-lactone A synthesis method of physiologically active δ-lactone, which comprises addition-reacting diethyl methylmalonate and methacrolein in the presence of a base.... | 10/31/1995 |
| 5461169 | Total synthesis of taxol and taxol analogs The total synthesis of taxol employs a convergent synthetic plan. The synthetic plan may also be employed to produce a large number of taxol analogs. Taxol analogs having skeletal extensions are inaccessible by modification of the natural product but are ... | 10/24/1995 |
| 5453519 | Process for inhibiting oxidation and polymerization of furfural and its derivatives Dialkylphenylenediamines are used to inhibit oxidation and polymerization of furfural or furfural derivatives. The preferred use of the inhibitor is in the solvent refining of lubricating oils using furfural to extract constituents from the lubricating oi... | 09/26/1995 |
| 5453520 | Baccatine III derivatives Isolation of a new taxane having pharmaceutical activity, 1a 14-beta-hydroxy-10-deacetyl-baccatine III and hemisynthesis of some derivatives useful as antitumor agents and intermediates.... | 09/26/1995 |
| 5449790 | Preparation of 10-deacetylbaccatin III and 7-protected-10-deacetylbaccatin III derivatives from 10-deacetyl taxol A, 10-deacetyl taxol B, and 10-deacetyl taxol C The present invention relates to a process for converting purified, partially purified or crude taxane mixtures into a protected precursor of 10-deacetylbaccatin III and into 10-deacetylbaccatin III. The process comprises three steps, the first of which i... | 09/12/1995 |
| 5449793 | Process for producing an optically active 1,5-disubstituted-2,4-O-isopropylidene-2,4-dihydroxypentane A novel optically active erythro-1-alkanoyloxy-2,4-O-isopropylidene-2,4-dihydroxy-5-substituted pentane expressed by the formula ##STR1## wherein R1 represents a halogen atom or cyano group and R2 represents an alkyl group ... | 09/12/1995 |
| 5447942 | N-derivatives of (phenylethyl-ଲ-ol) amine, a process for their preparation and pharamaceutical compositions containing the same The invention relates to a N-(2,4- or 2,5-disubstituted tetrahydrofuryl alkyl)-N-(phenylethyl-ଲ-ol)amine derivative, under a racemic or enantiomer form, of general formula I ##STR1## wherein R represent various radicals and n is of from 1 to 10... | 09/05/1995 |
| 5442079 | Method for preparing erythruronolactone There are described improved processes for the synthesis of a desired lactone useful as a synthon, the improved processes comprising oxidizing a protected arene diol with permanganate and periodate or subjecting a substituted epoxydiol to periodate oxidat... | 08/15/1995 |
| 5441978 | Compound and nematicide against pine wood nematodes containing the same A novel compound having nematicidal effect on pine wood nematodes which has the following structural formula: ##STR1## and a nematicide containing the compound described above against the pine wood nematodes.... | 08/15/1995 |
| 5440054 | Compound for treatment of cardiac arrhythmia, synthesis, and methods of use Described is a novel compound and method, useful for treatment of cardiac arrhythmias, especially useful in patients with congestive heart failure (CHF). A process for synthesizing the novel compound is also described.... | 08/08/1995 |
| 5432289 | Diphosphines containing silane groups, immobilized diphosphines and the use thereof as hydrogenation catalysts Compounds of formula I ##STR1## wherein R1 denotes identical or different radicals and is linear or branched C1 -C12 alkyl, unsubstituted C5 -C6 cycloalkyl or C5 -C6 cycloal... | 07/11/1995 |
| 5430160 | Preparation of substituted isoserine esters using ଲ-lactams and metal or ammonium alkoxides A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal or an ammonium alkoxide is reacted with a ଲ-lactam.... | 07/04/1995 |
| 5428180 | Oxidations using polyazamacrocycle metal complexes A method is provided for oxidizing alkenes to epoxides by treating the alkene with a transition metal ion complex which includes a salen or salophen derivative and peroxymonosulfate ion or hypochlorite ion in a two phase system with a phase transfer catal... | 06/27/1995 |
| 5422364 | Water soluble taxol derivatives Alkaline sensitive protaxol is water soluble and is hydrolyzed at physiological (alkaline) pH to render the native taxol structure and the native taxol activity. Protaxol compositions include 2'- and/or 7-O-ester derivatives of taxol and/or 2'- and/or 7-O... | 06/06/1995 |
| 5420311 | Difluoroamino oxetanes and polymers formed therefrom for use in energetic formulations This invention relates to novel oxetanes containing neopentyl difluoroamino groups. More specifically, mono- and bis-(difluoroaminomethyl)oxetanes are synthesized. These compounds are prepared by the direct fluorination of blocked neopentyl amines. These ... | 05/30/1995 |
| 5420305 | Process for the preparation of (R)-3-hexyl-5,6-dihydro-4-hydroxy-6-undecyl-2H-pyran-2-one and (R)-5,6-dihydro-6-undecyl-2H-pyran-2,4 (3H)-dione A process for the preparation of a tautomeric mixture of compounds of the formulas ##STR1## wherein W is hydrogen or C6 H13, which comprises treating a compound of the formula ##STR2## wherein R is unsubstituted or sub... | 05/30/1995 |
| 5416225 | Total synthesis of taxol The present invention provides two basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as w... | 05/16/1995 |
| 5416224 | Process for converting -acyl-substituted lactones to -alkylidene-substituted lactones A convenient stereoselective process for the preparation of -alkylidene-substituted-γ-butyrolactones and δ-valerolactones is provided. The process involves reacting an -acyl lactone, an aldehyde, and an alkali metal hydroxide in an in... | 05/16/1995 |
| 5411984 | Water soluble analogs and prodrugs of taxol Substituted 2'-benzoyl and 2', 7-dibenzoyl taxol derivatives are synthesized which have improved water solubility and stability while maintaining bioactivity. In a preferred embodiment, taxol 2',7-di(sodium 1,2-benzenedicarboxylate) is synthesized by reac... | 05/02/1995 |
