CAS: 75567-37-2; Ingenol Mebutate

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CAS号1356187-24-0 ingenol-20-(ter... | CAS号1356187-19-3 ingenol-5,20-(d... | CAS号565-63-9 当归酸 | CAS号77573-43-4 巨大戟醇-5,20-缩丙酮 | CAS号30220-46-3 巨大戟二萜醇 | CAS号94487-74-8 当归酸酐 | CAS号1356187-16-0 ingenol-5,20-(d...

3-O-Angeloyl-20-Deoxyingenol 在 Selenium(Iv) Oxide体系中,用 1,4-二氧六环作为反应溶剂,反应 6.0H,以19 Mg的收率获得ingenol Mebutate
参考文献:[En] Process For The Preparation Of Ingenol-3-Angelate From 20-Deoxy-Ingenol[Fr] Pr°Cédé De Préparation D'Ingénol-3-Angélate à Partir De 20-Désoxy-Ingénol
标题:[En] Process For The Preparation Of Ingenol-3-Angelate From 20-Deoxy-Ingenol[Fr] Pr°Cédé De Préparation D'Ingénol-3-Angélate à Partir De 20-Désoxy-Ingénol
摘要:本发明提供了一种制备3-安吉酯英吉醇的方法.

专利信息

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-2013331427-A1
优先权日:2006-07-28
标题:Methods of stimulating cellular growth, synaptic, remodeling and consolidation of long-term memory
发明人：ALKON DANIEL L
权利人:BRNI NEUROSCIENCES INST; BRNI NEUROSCIENCES INST
摘要:The present invention provides methods of slowing or reversing the loss of memory and learning comprising the steps of contacting an effective amount of a PKC activator with a protein kinase C (PKC) in a subject identified with memory loss slowing or reversing memory loss. The present invention provides methods of stimulating cellular growth, neuronal growth, dendritic growth, dendritic spine formation, dendritic spine density, and the translocation of ELAV to proximal dendrites, and synaptic remodeling. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to stimulate the synthesis of proteins sufficient to consolidate long-term memory. The present invention also provides methods of contacting a protein kinase C (PKC) activator with a PKC activator in a manner sufficient to downregulate PKC.

专利号:US-9416083-B2
优先权日:2011-10-04
标题 :Method of isolating ingenol
发明人：BELLIDO CABELLO DE ALBA MARIA LUZ; APPENDINO GIOVANNI; PAGANI ALBERTO; MUNOZ BLANCO EDUARDO
权利人:INDENA SPA
摘要:The present invention relates to a new method for isolating ingenol (C20H28O5) from mixtures of diterpenoid esters and ingenol esters in a single step. Ingenol isolated by means of this method can be used as a precursor for the synthesis of biologically active ingenol derivatives, such as ingenol-3-angelate and ingenol-3-tigliate.

专利号:US-9676698-B2
优先权日:2010-07-20
标 题:Method of producing ingenol-3-angelate
发明人：HOGBERG THOMAS; GRUE-SORENSEN GUNNAR; LIANG XIFU; HORNEMAN ANNE MARIE; PETERSEN ANDERS KLARSKOV
权利人:LEO LABORATORIES LTD
摘要:The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). n n n n n n n n n n Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

专利号:US-2019106684-A1
优先权日:2016-03-16
标题 :Modified cell
发明人：GRAHAM IAN; KING ANDREW
权利人:UNIV YORK
摘要:The present disclosure relates to nucleic acids that encode enzyme activities involved in the synthesis of lathyranes, intermediates in the synthesis of lathyranes and also compounds derived from lathyranes such as tiglianes, daphnanes and ingenanes; cells transformed with the nucleic acid molecules and vectors comprising the nucleic acid molecules.