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41 results about "Cyclopamine" patented technology

Cyclopamine (11-deoxojervine) is a naturally occurring chemical that belongs in the family of steroidal alkaloids. It is a teratogen isolated from the corn lily (Veratrum californicum) that causes fatal birth defects. It prevents the fetal brain from separating into two lobes (an extreme form of holoprosencephaly), which in turn causes the development of a single eye (cyclopia). The chemical was named after this effect, as it was originally noted by Idaho lamb farmers who contacted the US Department of Agriculture after their flocks gave birth to cycloptic lambs in 1957. It then took more than a decade to identify the corn lily as the culprit. Later work suggested that different rain patterns caused the sheep to graze differently, impacting the amount of corn lily ingested by pregnant sheep. The poison interrupts the sonic hedgehog signaling pathway during development, thus causing birth defects.

Cyclopamine analogues and methods of use thereof

ActiveUS7230004B2Antagonize Smo-dependent pathway activationStop and slow cell proliferationBiocideNervous disorderGain of function mutationBiological activation
The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.
Owner:ROYALTY SECURITY LLC

Micelles for the solubilization of gossypol

The invention provides biocompatible micelles loaded with one or more active agents. The micelles can encapsulate anticancer drugs such as gossypol, and combinations of drugs, such as gossypol and paclitaxel, gossypol and 17-AAG, gossypol and cyclopamine, gossypol, paclitaxel, and 17-AAG, and gossypol, paclitaxel, and cyclopamine. The micelle compositions provide effective solubilization of difficult to solubilize drug combinations without the need for additional surfactants that can be toxic to patients. Thus, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity.
Owner:WISCONSIN ALUMNI RES FOUND

Hedgehog signaling and cancer stem cells in hematopoietic cell malignancies

The present disclosure relates generally to methods of treating hematopoietic cell malignancy in a subject by administering to the subject a Hedgehog (Hh) pathway antagonist, such as a Smoothen (Smo) antagonist alone or in combination with an ABL-kinase antagonist. Specifically, the disclosure relates to a method of treating hematopoietic cell malignancy in a subject by administering the Hh pathway antagonist, such as the Smo antagonist cyclopamine, in combination with the ABL-kinase antagonist imatinib.
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV +1

Preparation method of cyclopamine

ActiveCN101798307AHigh Fritillaria ContentAbundant resourcesOrganic chemistryStrong acidsCyclopamine
The invention discloses a preparation method of cyclopamine, which comprises the steps of: taking peimisine as raw material; leading the peimisine and benzene sulfonyl hydrazide to have condensation reaction in alcohol under the catalysis of strong acid, and preparing intermediate 1 toluene sulfonamide; and leading the intermediate 1 toluene sulfonamide and strong base to have backflow reaction in organic solvent, and obtaining the cyclopamine. The peimisine is extracted from traditional Chinese medicine fritillary, and the invention also provides a method for extracting the peimisine. As the fritillary has rich source and low price, by adopting the peimisine as raw material to prepare the cyclopamine, the method optimizes the reaction condition, reduces the cost, is simple and convenient for operation, prepares the cyclopamine with high efficiency, and is suitable for large-scale industrial production.
Owner:BASILEA PHARM CHINA LTD

Micelles for the solubilization of gossypol

The invention provides biocompatible micelles loaded with one or more active agents. The micelles can encapsulate anticancer drugs such as gossypol, and combinations of drugs, such as gossypol and paclitaxel, gossypol and 17-AAG, gossypol and cyclopamine, gossypol, paclitaxel, and 17-AAG, and gossypol, paclitaxel, and cyclopamine. The micelle compositions provide effective solubilization of difficult to solubilize drug combinations without the need for additional surfactants that can be toxic to patients. Thus, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity.
Owner:WISCONSIN ALUMNI RES FOUND

Method of preparing cyclopamine from jervine

The invention discloses a making method of cyclopamine and application in the medical domain, which comprises the following steps: adopting jervine from Veratrum plant as raw material; reacting jervine and hydrazine hydrate to produce hydrazone in the high-boiling point solvent; denitrifying acted by potassium hydroxide and tert-butanol potassium to form jervine; using carbowax 400 and TEBA as phase transmitting catalyst; connecting tumour cell Hh and Smo protein; dying cancer cell due to non-gene toxicity without influencing normal cell.
Owner:SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY +1

Method for separating cyclopamine analogs from Veratrum plants by high-speed counter-current chromatography

The invention relates to a separation method of a natural drug, and discloses a method for separating cyclopamine analogs from Veratrum plants by high-speed counter-current chromatography. The method is characterized in that Veratrum total alkaloid powder is separated and purified by high-speed counter-current chromatography twice, wherein the solvent system of the first high-speed counter-current chromatography is a mixed solvent composed of dichloromethane, methanol and water; and in the second high-speed counter-current chromatography, the jervine fraction obtained by the first high-speed counter-current chromatography is separated and purified as a reflux sample, and the solvent system is a mixed solvent composed of normal hexane, ethyl acetate, methanol and water. The method is simple and quick, and has the advantages of high recovery rate and high purity of the target compound.
Owner:CHINA PHARM UNIV

Cyclopamine analogues and methods of use thereof

The present invention provides compositions and methods for modulating smootheneddependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-offunction mutations. The compounds of the present invention are particularly useful in treating cancers.
Owner:INFINITY PHARMA

Steroid-derived cyclopamine analogs and methods for using the same in the prevention or treatment of cancer

The present invention relates to steroid-derived cyclopamine analogs and methods for using the same for inhibiting sonic hedgehog signaling and preventing or treating cancer. A method for synthesizing the analogs of the present invention from a steroid is also provided.
Owner:WISTAR INSTITUTE +1

Drug treatment of tumors wherein hedgehog/smoothened signaling is utilized for inhibition of apoptosis of tumor cells

This invention concerns use of cyclopamine or another selective inhibitor of hedgehog / smoothened signaling in vivo on basal cell carcinomas and other tumors wherein hedgehog / smoothened signalling is utilized for inhibition of differentiation and for inhibition of apoptosis of tumor cells to achieve differentiation and apoptotic death and removal of the tumor cells while preserving normal tissue cells and functions. Causation of apoptosis is by a non-genotoxic mechanism and thus unlike in the radiation therapy and most of the currently used cancer treatments which act by causing DNA-damage.
Owner:TAS SINAN

Shh pathway regulation and control biological rhythm and related application thereof

The invention relates to the technical field of biology, in particular to Shh pathway regulation and control biological rhythm and related application thereof. Specifically, the invention provides application of a Hedgehog pathway inhibitor and an SMO inhibitor in regulating the biological rhythm and treating diseases related to the biological rhythm. Preferably, the Hedgehog pathway inhibitor comprises the following components: PF-5274857, Mebendazole, HPI-4, SANT-1, Taladegib, Grasdegib, Cyclopamine, Itracazole, GANT61, JK184, Robotnikinin, Vismodegib, Purmorphamine, and Sonidegib Phoshate, and the Hedgehog pathway inhibitor comprises the following components: PF-5274857, the Mebendazole, the HPI-4, the SANT-1, the Taladegib, the Grasdegib, the Cyclopamine, the Itracazole, the GANT61, the JK184, the Robotnikinin, the Vismodegib, the
Owner:ACADEMY OF MILITARY MEDICAL SCI

Respiratory syncytial virus infection treating compound and preparation method and application thereof

The invention discloses a respiratory syncytial virus infection treating compound and a preparation method and application thereof. The compound refers to chemical analogues of cyclopamine and is characterized by suppressing replication of respiratory syncytial virus without suppressing Hedgehog signal pathway. The preparation method includes synthesizing the chemical analogues of cyclopamine in a medicinal chemistry way and then screening the analogues by means of in-vitro tests performed in parallel. The compound is applied to treatment of respiratory virus infection, paramyxovirus infection, respiratory syncytial virus infection, and capillary bronchitis, pneumonia and tympanitis which are all caused by respiratory syncytial virus, is free of toxic and side effect to cause fetal anomaly, overcomes teratogenicity of cyclopamine, and fills the blank of drugs especially pediatric drugs for treating respiratory syncytial virus infection.
Owner:SHANGHAI MEDUSA BIOTECHNOLOGY CO LTD

Anti-tumor drug and use thereof

The invention discloses an anti-tumor drug and a use thereof. The invention concretely discloses a pharmaceutical composition for reducing a cyclopamine teratogenic risk. The pharmaceutical composition contains one or more of gentiopicroside, loganic acid and sophocarpidine. The pharmaceutical composition substantially inhibits tumor cell growth activity and greatly reduces a cyclopamine use amount.
Owner:RUIAN PULUO BIOTECH

Mass spectrum guided separation method of cyclopamine analogues in fritillaria plants

ActiveCN106053623AComponent separationLc qqq msSteroidal alkaloid
The invention relates to a mass spectrum guided separation method of cyclopamine analogues in fritillaria plants. According to the method, common product ions of a jerveratrum isosteroidal alkaloid reference substance are taken as the guide, an LC-QTOF-MS / MS technology is introduced to establish a rapid characterization method of jerveratrum isosteroidal alkaloid; then a series of cyclopamine analogues is screened out from fritillaria herbals by using the strong screening functions of LC-QQQ-MS / MS, and finally an automatic purification system is adopted to prepare fractions according to the mass spectrum response signals of fractions.
Owner:NANJING FORESTRY UNIV +1

Heterocyclic cyclopamine analogs and methods of use thereof

The present invention relates to steroidal alkaloid-like compounds that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.
Owner:INFINITY DISCOVERY INC

Traditional Chinese and Western medicine composition for treating hypertension and preparation method of traditional Chinese and Western medicine composition

The invention discloses a traditional Chinese and Western medicine composition for treating hypertension. The traditional Chinese and Western medicine composition for treating the hypertension is prepared from the following main raw materials in parts by weight: 5 to 12 parts of rhizoma chuanxiong, 8 to 9 parts of spica prunellae, 20 to 35 parts of folium apocyni veneti, 4 to 7 parts of cyclopamine, 15 to 20 parts of aurapten, 2 to 4 parts of isosakuranetin, 7 to 9 parts of menthol, 4 to 8 parts of luteolin-7-O-glucuronide and 4 to 6 parts of 3-butylidenephthalide. According to the traditional Chinese and Western medicine composition provided by the invention, raw material components are strictly selected according to a know mechanism on the hypertension and the traditional Chinese and Western medicine composition is used for carrying out physiological and pathological all-directional conditioning and treatment on middle-aged and aged people with the hypertension.
Owner:ZHENGZHOU ZHENGXIAN PHARMA CO LTD

Cyclopamine tartrate salt and uses thereof

InactiveUS20110092530A1Reduce morbidityAntagonize Smo-dependent pathway activationBiocideOrganic chemistryWater solubleBiological activation
The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides highly water-soluble analogs of cyclopamine that are potent, hedgehog signaling inhibitors less toxic than cyclopamine. The compounds of the present invention are particularly useful in treating cancers associated with hedgehog signalling.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

Cyclopamine tartrate salt and uses thereof

InactiveUS8658664B2Antagonize Smo-dependent pathway activationStop and slow cell proliferationBiocideOrganic chemistryWater solubleBiological activation
The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides highly water-soluble analogs of cyclopamine that are potent, hedgehog signaling inhibitors less toxic than cyclopamine. The compounds of the present invention are particularly useful in treating cancers associated with hedgehog signalling.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

Compound for treating respiratory syncytial virus infection and its preparation method and application

The invention discloses a compound for treating respiratory syncytial virus infection, a preparation method and application thereof. The compound is a chemical analogue of cyclopamine, which has the property of inhibiting the replication of respiratory syncytial virus, but does not have the property of inhibiting Hedgehog signaling pathway. The preparation method synthesizes the chemical analogs of the cyclopamine through pharmaceutical chemistry, and screens the analogs through two parallel in vitro tests. The compound can be used to treat respiratory virus infection, paramyxovirus infection, respiratory syncytial virus infection, bronchiolitis caused by respiratory syncytial virus, pneumonia caused by respiratory syncytial virus, otitis media caused by respiratory syncytial virus, It does not have the toxic and side effects of causing fetal malformation, overcomes the teratogenic properties of cyclopamine, and fills in the blank of drugs for treating respiratory syncytial virus infection, especially pediatric drugs.
Owner:SHANGHAI MEDUSA BIOTECHNOLOGY CO LTD

Methods for obtaining cyclopamine

The present invention relates to a process for extracting, purifying and isolating cyclopamine from cyclopamine-containing biomass comprising the steps of contacting cyclopamine-containing organic matter with an extractant (e.g., aqueous extractant) capable of extracting cyclopamine, separating the extracted organic matter from the cyclopamine / extract solution, concentrating the cyclopamine / extract solution leaving a concentrated aqueous solution, contacting the concentrated aqueous solution with an organic extractant capable of selectively extracting cyclopamine from the aqueous phase, concentrating the cyclopamine-containing organic phase, providing an enriched extract containing cyclopamine, separating cyclopamine from the enriched extract using column chromatography, providing at least one fraction containing cyclopamine, and crystallizing select chromatography fractions to provide purified cyclopamine.
Owner:RADIENT TECH
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