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1060 results about "Aceglatone" patented technology

Aceglatone (Glucaron) is an antineoplastic drug available in Japan. It is an inhibitor of the enzyme β-glucuronidase.

Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents

The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat meningiomas; to treat uterine leiomyomas; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce cervical ripening; to induce labor; and for contraception.
Owner:HEALTH & HUMAN SERVICES THE GOVERNMENT OF THE US SEC THE DEPT OF

Industrial process for the synthesis of 17a-acetoxy-11ss-[4-(n,n-dimethyl-amino)- phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process

The present invention relates to a new industrial process for the synthesis of solvate- free 17a-acetoxy-11ss-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB -2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process. The process according to the invention is the following: i) 3-(ethylene-dioxy)-estra-5(10),9(11)-diene-17-one of formula (X) is reacted with potassium acetilyde formed in situ in dry tetrahydrofuran by known method, ii) the obtained 3-(ethylene-dioxy)-17a-ethynyl-17ss-hydroxy-estra-5(10),9(11)-diene of formula (IX) is reacted with phenylsulfenyl chloride in dichloromethane in the presence of triethylamine and acetic acid, iii) the obtained isomeric mixture of 3-(ethylene-dioxy)-21-(phenyl-sulfinyl)-19-norpregna-5(10),9(11),17(20),20-tetraene of formula (VIII) is reacted first with sodium methoxide in methanol, then with trimethyl phosphite, iv) the obtained 3-(ethylene-dioxy)-17a-hydroxy-20-methoxy-19-norpregna-5(10),9(11),20-triene of formula (VII) is reacted with hydrogen chloride in methanol, then v) the obtained 3-(ethylene-dioxy)-17a-hydroxy-19-norpregna-5(10),9(11l); -diene-20- one of formula (VI) is reacted with ethylene glycol hi dichloromethane in the presence of trimethyl orthoformate and p-toluenesulfonic acid by known method, vi) the obtained 3,3,20,20-bis(ethylene-dioxy)-17a-hydroxy-19-norpregna- 5(10),9(11)-diene of formula (V) is reacted with hydrogen peroxide in a mixture of pyridine and dichloromethane in the presence of hexachloroacetone by known method, vii) the obtained 3,3,20,20-bis(ethylene-dioxy)-17a-hydroxy-5,10-epoxy-19-norpregn-9(11)-ene of formula (IV), containing approximately a 1:1 mixture of 5a,10a- and 5ss,10ss-epoxides, is isolated from the solution and reacted with a Grignard reagent obtained from 4-bromo-N,N-dimethyl-aniline in tetrahydrofuran.
Owner:RICHTER GEDEON NYRT

Application of chitosanoligosaccharide and derivatives thereof in plant cold resisting

The invention discloses a wide-spectrum plant cold-resisting agent for plants such as food crops, economic crops, vegetables, fruit trees, economic trees, flowers, and lawns. The active component of the agent is chitosanoligosaccharide or a derivative thereof. The chitosanoligosaccharide is oligosaccharide of glucosamine linked through beta-1,4-glucosidic bond, and has a molecular weight of 300-10000Da, and a deacetylation degree of 50-100%. The chitosanoligosaccharide derivatives are chitosanoligosaccharide sulfuric acid derivative, chitosanoligosaccharide hydrochloric acid derivative, chitosanoligosaccharide phosphoric acid derivative, chitosanoligosaccharide sulfonamide derivative, chitosanoligosaccharide acyl isothiocyanate derivative, chitosanoligosaccharide phosphoric derivative, chitosanoligosaccharide guanidine derivative, chitosanoligosaccharide nicotinicacyl isothiocyanate derivative, chitosanoligosaccharide-cerium (IV) complex, and the like.
Owner:DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI

Antibody composition-containing medicament

A medicament for treating a patient who cannot be cured with a medicament comprising as an active ingredient an antibody composition produced by a cell unresistant to a lectin which recognizes a sugar chain in which 1-position of fucose is bound to 6-position of N-acetylglucosamine in the reducing end through α-bond in a complex N-glycoside-linked sugar chain, which comprises as an active ingredient an antibody composition produced by a cell resistant to a lectin which recognizes a sugar chain in which 1-position of fucose is bound to 6-position of N-acetylglucosamine in the reducing end through α-bond in a complex N-glycoside-linked sugar chain, and a method for screening the patient by using the medicament.
Owner:KYOWA HAKKO KIRIN CO LTD

Nutrient compositions and methods for enhanced effectiveness of the immune system

The invention provides a nutrient composition for augmenting immune strength or physiological detoxification. The nutrient composition consists of an optimal combination of an effective amount of at least one vitamin antioxidant, at least one mineral antioxidant and a highly saturable amount of at least three high potency antioxidants. The at least one vitamin antioxidant can be vitamin C, bioflavonoid complex, vitamin E, vitamin B6 or beta-carotene and the at least one mineral antioxidant can be zinc or selenium. The at least three high potency antioxidants can be alpha lipoic acid, acetyl L-carnitine, N-acetyl-cysteine, co-enzyme Q10 or glutathione. Also provided is a nutrient composition for augmenting immune strength or physiological detoxification that consists of an optimal combination of an effective amount of at least three vitamin antioxidants, at least two mineral antioxidants and a highly saturable amount of at least three high potency antioxidants. Further provided is a method of stimulating immune system function or a method of augmenting a therapeutic treatment of a disease. The method consists of administering to an individual a nutrient composition of the invention one or more times a day over a period of about 5-7 weeks, the immune system function being stimulated to result in an increase of CD4+ cells of at least about 15% compared to pre-administration levels. A method of stimulating a physiological detoxification function of an individual or a method of augmenting a therapeutic treatment of a disease is also provided. The method consists of administering to an individual a nutrient composition of the invention one or more times a day over a period of about 5-7 weeks, the physiological detoxification function being stimulated to result in a decrease of one or more free radical markers by about 20% compared to pre-administration levels.
Owner:INTEGRATIVE HEALTH CONSULTING INC

Betaine compositions

The invention refers to the pharmaceutical combination including at least: a first compound selected among the group consisting of acetylsalicylic acid, salicylic acid, pharmaceutical derivatives thereof, and a second compound selected from the group consisting of lipidic betaines, betaines lipids, betaines of Formula (CH3)3N+(CH2)nCOO− with n an integer from 1 to 5, pharmaceutically acceptable salts thereof, esters thereof, precursors thereof, and mixtures thereof, with the proviso that the second compound is different from the first compound and in an amount by weight at least three times the amount of first compound.
Owner:BIO ETHIC

Recombinant corynebacterium crenatum for over expression of N-acetylglutamate kinase and application thereof

The invention relates to a recombinant corynebacterium crenatum to enhance the expression of N-acetyl glutamic acid kinase and the application thereof, which belongs to the technical field of gene engineering. The classification and nomenclature of the recombinant corynebacterium crenatum to enhance the expression of N-acetyl glutamic acid kinase is corynebacterium crenatum SYPA / pJC1-tac-argB with an access number of CCTCC NO: M 208133; The application is as follows: using a key enzyme N-acetyl glutamic acid kinase from corynebacterium crenatum pathway arginine to construct a corynebacterium crenatum expression vector pJC1-tac-argB; introducing the corynebacterium crenatum expression vector pJC1-tac-argB into corynebacterium crenatum SYPA by electrotransformation to obtain the recombinant corynebacterium crenatum SYPA / pJC1-tac-argB; and excessively expressing N-acetyl glutamic acid kinase, which greatly enhances the utilization rate of a precursor glutamic acid and allows the metabolic flow to flow to the arginine synthesis pathway, weakens the synthesis of proline, achieves the purpose of improving the output of arginine and the output of arginine is increased by 23.4 percent than C. crenatum SYPA.
Owner:JIANGNAN UNIV

Fucosylated glycosaminoglycan derivative and preparation method thereof

InactiveCN102329397APotent anticoagulant activityOrganic active ingredientsBlood disorderOrganosulfateCarboxylic ester
The invention discloses a carboxylic ester of fucosylated glycosaminoglycan (CEFG) with anticoagulation activity, a pharmaceutically acceptable salt thereof, a preparation method of the CEFG and the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the CEFG or the salt thereof, and application of the pharmaceutical composition in preparation of anticoagulants. The monosaccharides for preparing the CEFG comprise D-glucuronic acid or D-glucuronate (D-GlcU), D-2-deoxy-2-acetyl galactosamine sulfate (D-GalNAcS) and L-fucose sulfate (L-FucS), wherein the molar ratio of D-GlcU to D-GalNAc to L-Fuc to -OSO3<-> is 1:(1+ / -0.3):(1+ / -0.3):(3.5+ / -0.5); the esterification degree of the D-GlcU is not lower than 20%; and the weight average molecular weight of the CEFG is 3000-20000 Da. The glycosylated chondroitin sulfate esterification derivative has strong anticoagulation activity, and can be applied in preparation of drugs for preventing and / or treating thrombotic diseases.
Owner:KUNMING INST OF BOTANY - CHINESE ACAD OF SCI

Method and test strips for the measurement of fat loss during weight loss programs

Disposable test strips and a wet chemistry method for measuring each of beta-hydroxybutyrate alone, combined beta-hydroxybutyrate and acetoacetate or total ketone bodies (i.e., beta-hydroxybutyrate, acetoacetate and acetone) in human bodily fluid samples, including but not limited to urine, saliva or sweat are described. The test strips need only be dipped in the sample and can be used by anyone in almost any milieu. Measurement can be made electrochemically, spectrophotometrically, fluorometrically or by comparision to a color standard. Combined acetoacetate and beta-hydroxybutyrate which account for 97-98% of total ketone bodies and may be measured in a cyclic reaction that occurs at pH about 7.0 to about 8.3 with beta-hydroxybutyrate dehydrogenase, (beta-HBD), nicotinamide adenine dinucleotide, a tetrazolium dye precursor and an electron mediator. Using this reaction, false positive results obtained from urine samples taken from patients on sulfhydryl drugs are avoided. beta-HBD from some sources was found to cause false negative results in samples (e.g. urine) containing high chloride content due to chloride inhibition of beta-HBD. Using a simple test for chloride inhibition, it was found that beta-HBD from Alcaligenes is not so inhibited. Using either beta-HBD that is not inhibited by chloride or using 10-20 times the normal concentration of this enzyme eliminates false negatives in samples having substantial chloride content, such as urine, both in the reaction described above and in other reactions disclosed for measuring each of beta-hydroxybutyrate alone, combined beta-hydroxybutyrate and acetoacetate and total ketone bodies, all of which reactions occur in the pH range of about 8.6 to about 9.5.
Owner:GUPTA SURENDRA

Methods and compositions for treating cancer

Methods and compositions for treating cancer are described herein. More particularly, the methods for treating cancer comprise administering a 17a-hydroxylase / C17, 20-lyase inhibitor, such as abiraterone acetate (i.e., 3beta-acetoxy-17-(3-pyridyl) androsta-5, 16-diene), in combination with at least one additional therapeutic agent such as an anti-cancer agent or a steroid. Furthermore, disclosed are compositions comprising a 17a- hydroxylase / C17, 20-lyase inhibitor, and at least one additional therapeutic agent, such as an anti-cancer agent or a steroid.
Owner:库伽尔生物科技公司
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