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39results about "Androstane derivatives" patented technology
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Lif/lifr antagonist in oncology and nonmalignant diseases
InactiveUS20200087340A1Reduce the amount requiredOrganic active ingredientsAndrostane derivativesDiseaseImmunotherapeutic agent
Described herein are methods of using compounds that inhibit leukemia inhibitory factor (LIF) and / or block of the leukemia inhibitory factor receptor for treatment of liver fibrosis, proliferation of spinal tumors, and in combination therapy with an immunotherapeutic agent.
Owner:EVESTRA
(S)-6-methyloxaalkyl exemestane compounds and related methods of use
6-Methyloxaalkyl exemestane compounds and related compositions, as can be used, chemotherapeutically, to inhibit growth and proliferation of cancer cells.
Owner:ENDECE LLC
Estrene steroids as neurochemical initiators of change in human hypothalamic function and related pharmaceutical compositions
InactiveUS6140316AAltered functionAffect brain functionOrganic active ingredientsBiocideSemiochemicalMedicine
The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human semiochemical, e.g. an Estrene steroid, or a pharmaceutical composition containing an Estrene steroid, such that the ligand semiochemical binds to a specific neuroepithelial receptor. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.
Owner:PHERIN PHARMA INC
Exemestane compounds, compositions and related methods of use
Owner:ENDECE LLC
Use of 5.alpha.-androstane (alkyl)-3.beta.,5,6.beta.-triol in preparation of neuroprotective drugs
ActiveUS8809309B2Improve survival rateReduce releaseOrganic active ingredientsNervous disorderSpinal cordAndrostane
Disclosed is the use of 5α-androstane(alkyl)-3β,5,6β-triol in preparing neuroprotective drugs. The compound has significant protective effect against neuron injuries caused by cerebral ischemia, spinal cord ischemia or hypoxia and has no obvious toxic reaction within effective dose thereof.
Owner:GUANGZHOU CELLPROTEK PHARMA
Ship inhibitors and uses thereof
ActiveUS20130102577A1Additional componentEngraftment can be facilitatedOrganic active ingredientsBiocideLymphatic SpreadGackstroemia
The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.
Owner:THE RES FOUND OF STATE UNIV OF NEW YORK +1
Preparation method of canrenone intermediate
The invention provides a preparation method of a canrenone intermediate. The preparation method comprises the following steps: taking 4-androstenedione as a substrate, adding tetrahydrofuran, p-toluenesulfonic acid and trimethyl orthoformate into the substrate, stirring the mixture until complete reaction, cooling, adding a small amount of water for a hydrolysis reaction, stirring the mixture, adding weak base solution to terminate the hydrolysis reaction, performing crystallization and filtering separation in the water, and drying, so as to obtain a compound I. In the preparation method, by optimizing reaction conditions and adding a small amount of water for a differentiation reaction after an anhydrous reaction is ended, a dual etherification phenomenon when a protection reaction is simultaneously performed on a 3-ketone group and a 17-ketone group in the prior art can be overcome, so that the purity of a product is effectively improved, the production cost is lowered, and the operation difficulty in production is lowered.
Owner:GUANGXI WANDE PHARMA
Processes for preparing C-7 substituted 5-androstenes
This invention relates to processes for the preparation of novel , substituted steroid compounds of Formula 1, wherein R1 is H or -COR2; R2 is C1-C6 alkyl or Ct-C6 alkoxy; Z1 is CH2, or wherein OR3 is in the alpha configuration; R3 is H or -COR2; Z2 is -CH-; or Z1 and Z2 may be taken together to form a carbon-carbon double bond; Q is or Y is -CN, -CH2-CH=CH2, C1-6- Alkyl C1-6 alkyl CHR4C (O)Ar, or CHR4 C (O)XC1-6 alkyl; CHR4(O)XAr, or CHR4 HC(O)XC1-6 alkyl; where R4 = O C1-6 alkyl or aryl X=O or S.
Owner:PHARMACIA & UPJOHN CO
Use of 5alpha-androstane (ALKYL)-3beta,5,6beta-triol in preparation of neuroprotective drugs
ActiveUS20130157993A1Avoid damageImprove survival rateOrganic active ingredientsNervous disorderSpinal cordNeuroprotective Drugs
Disclosed is the use of 5α-androstane(alkyl)-3β,5,6β-triol in preparing neuroprotective drugs. The compound has significant protective effect against neuron injuries caused by cerebral ischemia, spinal cord isehemia or hypoxia and has no obvious toxic reaction within effective dose thereof.
Owner:GUANGZHOU CELLPROTEK PHARMA
Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof
Owner:EPIRIUM BIO INC
Cracked-ring lupane derivatives and pharmaceutical application thereof
The invention relates to cracked-ring lupane derivatives, a P2Y12 receptor antagonist function of pharmaceutical composition containing the cracked-ring lupane derivatives and an application of the cracked-ring lupane derivatives to preparation of drugs for preventing, treating and relieving thrombotic diseases. Conventional structural constraints of natural products are changed with a semisynthetic method, a series of cracked-ring lupane derivatives are designed and synthesized, the P2Y12 receptor antagonist function of the cracked-ring lupane derivatives is verified in vitro, and the compounds can be applied to research of the drugs for preventing, treating and relieving the thrombotic diseases through further experiments.
Owner:JILIN AGRICULTURAL UNIV
Ship inhibitors and uses thereof
ActiveUS9447139B2Engraftment can be facilitatedPrevent obesityOrganic active ingredientsAndrostane derivativesLymphatic SpreadApoptosis
Owner:THE RES FOUND OF STATE UNIV OF NEW YORK +1
CRYSTALLINE FORMS OF 5alpha-ANDROSTANE-3beta,5,6beta-TRIOL AND PREPARATION METHODS THEREFOR
The present invention relates to four crystalline forms (crystalline forms A, B, C and D) of 5α-androstane-3β,5,6β-triol (YC-6) and preparation methods therefor. The four crystalline forms have significant difference in their lattice parameters, 2θ values and intensity in X-ray power diffraction, and melting points, etc. The study on its polymorphism is very important for further studying its effect, bioavailability and stability.
Owner:GUANGZHOU CELLPROTEK PHARMA
Reducing dehalogenating method of organic halogenated compound
ActiveCN109265499AEasy to separate and purifyMild conditionsEsterified saccharide compoundsAndrostane derivativesArylBromine
The invention discloses a reducing dehalogenating method of an organic halogenated compound. The reducing dehalogenating method comprises: mixing an organic halogenated compound R-X, a non-noble metalpromoter, a sulfide and an alkali, and carrying out a reducing dehalogenating reaction to obtain a reducing product R-H, wherein R is at least one selected from alkyl and aryl, and X is at least oneselected from iodine, bromine and chlorine. According to the present invention, the types and the ratio (especially the specific type of the promoter) of various raw materials used in the reducing dehalogenating reaction, the corresponding reaction conditions and the like are researched and improved, such that the problems of use of highly-toxic or expensive reagent, poor tolerance of the group, narrow application range of the substrate and the like in the prior art can be effectively solved.
Owner:HUAZHONG UNIV OF SCI & TECH
6,7-Oxygenated steroids and uses related thereto
Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6α and 7β oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6α and 7β oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and δ-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.
Owner:INFLAZYME PHARMA +2
Amphiphilic compounds with neuroprotective properties
Amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use in methods of treatment of neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing compound.
Owner:USTAV ORGANICKE CHEM A BIOCHEM AV CR +1
Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof
Owner:EPIRIUM BIO INC
17-Iodoandrosta-5,16-dien-3beta-ol preparation method
The invention discloses a 17-Iodoandrosta-5,16-dien-3beta-ol preparation method. The 17-Iodoandrosta-5,16-dien-3beta-ol preparation method takes dehydroeopiandrosterone-17-hydrazone, trichloroisocyanuric acid (TCCA), tetramethyl guanidine (TMG) and elemental iodine as raw materials to react at 0-90 DEG C with existence of solvent and then performing treatment to obtain the 17-Iodoandrosta-5,16-dien-3beta-ol. According to the 17-Iodoandrosta-5,16-dien-3beta-ol preparation method, the TCCA serves as oxidizing agent, the elemental iodine serves as iodinating agent, an oxidizing iodination methodis applied to iodinating dehydroeopiandrosterone-17-hydrazone, so that, compared with traditional methods, the 17-Iodoandrosta-5,16-dien-3beta-ol preparation method can reduce consumption of the elemental iodine by a half and is simple in operation of reaction processes and easy to control, thereby having a good industrialized application prospect.
Owner:ZHEJIANG UNIV OF TECH +1
6,7-Oxygenated steroids and uses related thereto
Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6α and 7β oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6α and 7β oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and δ-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.
Owner:INFLAZYME PHARMA +2
Synthetic method for carbonyl steroid-containing compound derivatization reagent
InactiveCN112125827ALow costEfficient productionAndrostane derivativesComponent separationChemical synthesisDibromopropane
The invention relates to a synthetic method for a carbonyl steroid-containing compound derivatization reagent, and belongs to the technical field of chemical synthesis. The synthesis method comprisesthe following steps of: firstly, reacting 1, 3-dibromopropane with N-hydroxyphthalimide to synthesize 2- (3-bromopropoxy) isoindoline -1, 3-diketone; preparing 3-((1,3-dioxo-2-isoindolyl)-oxy)-N, N, N-trimethylpropylammonium bromide by utilizing 2-(3-bromopropoxy) isoindoline -1, 3-diketone; and finally, carrying out hydrazinolysis on the 3-((1, 3-dioxo-2-isoindoline)-oxy)-N, N, N-trimethylpropylammonium bromide. The synthesis method is low in cost, simple in step and high in yield; the carbonyl-containing steroid compound can be derivatized; a permanently charged group N+Me3 is introduced into the carbonyl-containing steroid compound, and the detection sensitivity of the carbonyl-containing steroid compound in ESIMS / MS is improved.
Owner:HUAZHONG UNIV OF SCI & TECH
Ship inhibitors and uses thereof
ActiveUS20170051006A1Engraftment can be facilitatedPrevent obesityOrganic active ingredientsAndrostane derivativesGackstroemiaApoptosis
The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.
Owner:THE RES FOUND OF STATE UNIV OF NEW YORK +1
Synthetic method of abiraterone acetate and intermediate thereof
The invention relates to a synthetic method of abiraterone acetate and an abiraterone acetate intermediate. According to the synthetic method of the abiraterone acetate intermediate, chlorination reaction is carried out on a compound as shown in a formula (I), a chlorination reagent and alkali to obtain the abiraterone acetate intermediate as shown in a formula (II); the mass ratio of the compoundshown in the formula (I) to the alkali is controlled to be 1: (1.5-3); the structures of the compound shown as the formula (I) and the abiraterone acetate intermediate are described in the descriptions of the invention. The synthetic method can reduce the occurrence probability of side reaction in the chlorination process while maintaining high reaction activity, so that the yield and purity of the abiraterone acetate intermediate are improved, and the process is simple.
Owner:HUNAN NORCHEM PHARMACEUTICAL CO LTD
12beta-hydroxy-androstane4,14-diene-16-ketone compounds and application thereof
ActiveCN108558975AGood immunosuppressive activityPromote development and utilizationAndrostane derivativesImmunological disordersDouble bondKetone
The invention discloses 12beta-hydroxy-androstane4,14-diene-16-ketone compounds or pharmaceutically acceptable salt thereof, and the application of the compounds to preparation of immunosuppressive medicines and anti-tumor medicines. The compounds are extracted and separated from epigynum plants, and the structural formula is as shown in the specification, wherein R is selected from hydrogen, methoxyl, ethyoxyl, halogen, aliphatic group and fat amino; and in the formula, the formula as shown in the description represents single bond or double bonds. The experiment proves that the compounds reported in the invention have high immunosuppressive activity and anti-tumor activity; and the compounds provided by the invention provide leading compounds for developing immunosuppressive preparationsand anti-tumor preparations, and are favorable for developing and utilizing plant medicinal resources.
Owner:KUNMING UNIV OF SCI & TECH
A kind of preparation method of 17-iodo-androst-5,16-dien-3β-ol
InactiveCN109134571BReduce dosageSave iodine resourcesAndrostane derivativesHydrazoneTrichloroisocyanuric acid
Owner:ZHEJIANG UNIV OF TECH +1
A kind of reductive dehalogenation method of organic halogenated compound
ActiveCN109265499BEasy to separate and purifyMild conditionsEsterified saccharide compoundsAndrostane derivativesArylBromine
The invention discloses a reducing dehalogenating method of an organic halogenated compound. The reducing dehalogenating method comprises: mixing an organic halogenated compound R-X, a non-noble metalpromoter, a sulfide and an alkali, and carrying out a reducing dehalogenating reaction to obtain a reducing product R-H, wherein R is at least one selected from alkyl and aryl, and X is at least oneselected from iodine, bromine and chlorine. According to the present invention, the types and the ratio (especially the specific type of the promoter) of various raw materials used in the reducing dehalogenating reaction, the corresponding reaction conditions and the like are researched and improved, such that the problems of use of highly-toxic or expensive reagent, poor tolerance of the group, narrow application range of the substrate and the like in the prior art can be effectively solved.
Owner:HUAZHONG UNIV OF SCI & TECH
Steroid compound as well as preparation method and application thereof
PendingCN113321695ANovel chemical structureSignificant in vitro antitumor activityAndrostane derivativesAntineoplastic agentsProtein-Tyrosine KinasesChemical compound
The invention relates to the field of natural medicines, and discloses a steroidal compound which is derived from artocarpus heterophyllus pulp and has a novel chemical structure, a preparation method of the steroidal compound and application of the steroidal compound in antitumor medicines. Various in-vitro antitumor activity evaluation results of the compound artoheterophoid show that the compound has remarkable antitumor activity, presents protein tyrosine kinase inhibition activity equivalent to the tyrosine kinase inhibition activity of a positive control drug, can be further developed into an anti-tumor drug taking protein tyrosine kinase as a target, can be applied to the anti-tumor drug, is simple in separation and purification process and mild in reaction conditions, and has practical significance.
Owner:HAINAN NORMAL UNIV
2β,3α,5α-trihydroxy-androst-6-one and preparation methods and use thereof
ActiveUS9428539B2Simple structureImprove bioavailability in vivoOrganic active ingredientsSenses disorderCombinatorial chemistryOrganic chemistry
Owner:GUANGZHOU CELLPROTEK PHARMA
Methods for Preparing Bile Acids
PendingUS20220009957A1Antibacterial agentsOrganic active ingredientsChenodeoxycholic acidDHEA - Dehydroepiandrosterone
The present disclosure provides methods of preparing cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, and novel and useful synthetic intermediates, for example, as described for methods 1, 1A, 1B, 2, 3, 3A, and 4. The method can start with a plant derived steroid as a starting material, such as dehydroepiandrosterone (DHEA) or Acetyl-dehydroepiandrosterone (Ac-DHEA). Also provided are pharmaceutical or cosmetic compositions and uses thereof, which comprise one or more of cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, which is of high purity, for example, free of animal derived impurities.
Owner:MEDY TOX INC
Polyenoid androsterone compound and application thereof
ActiveCN108191937AEliminate the effects of growthAndrostane derivativesImmunological disordersHalogenHydrogen
The invention discloses a polyenoid androsterone compound and application thereof. The compound is extracted and separated from an epigynum auritum plant, and the structural formula is as shown in thedescription, wherein R1, R2 and R3 are selected from hydrogen, hydroxyl, methyl, halogen, an aliphatic group and fat amino. The experiment proves that the compound reported in the invention has highImmunosuppressive activity. The compound provided by the invention provides a lead compound for development of an immunosuppressive agent and an anti-tumor preparation, and is favorable for developingand utilizing plant medicinal resources.
Owner:KUNMING UNIV OF SCI & TECH
3,16-androstenedione compounds and application thereof
ActiveCN108822175AGood immunosuppressive activityEnhanced inhibitory effectOrganic active ingredientsAndrostane derivativesHydrogenHalogen
The invention discloses 3,16-androstenedione compounds or pharmaceutically acceptable salts thereof and application of the 3,16-androstenedione compounds or pharmaceutically acceptable salts in preparation of immunosuppressive and anti-tumor drugs. The 3,16-androstenedione compounds are represented in a following formula, are obtained by performing extraction and separation from Epigynum, and havefollowing structural formula, wherein R1 is selected from hydrogen, hydroxyl groups, methyl groups, halogen, carbonyl groups, aliphatic hydrocarbon groups and fatty amino groups, and R2 is selected from hydrogen, hydroxyl groups, methyl groups, halogen, aliphatic hydrocarbon groups and fatty amino groups. It is proven through experiments that the compounds have strong immunosuppressive and anti-tumor activities, and lead compounds are provided for development of immunosuppressants and anti-tumor preparations by the compounds, so that development and utilization of plant medicinal resources are facilitated.
Owner:KUNMING UNIV OF SCI & TECH
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