Patent•
Short synthetic route to taxol and taxol derivatives
24 May 1994-
TL;DR: A short route to the total synthesis of the core skeleton of the taxol ring system is described in this paper, where 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.
Abstract: 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 number of steps to the taxane skeleton is 13, making it the shortest route from readily available inexpensive starting materials
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TL;DR: In this paper, the authors have presented methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0, where X is N or CH, and Y is n or CR5.
Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
113 citations
Patent•
26 Sep 2013TL;DR: In this article, the ERK inhibitors of formula (1) and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocycyclic heterocycloalkyl ring, or a monocyteclic HHO ring; or a bridged moncyclic HHHO ring or a fused HHO-cyclopropyl ring.
Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring)cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
70 citations
Patent•
01 Mar 2002
TL;DR: An optical deflecting unit includes a torsion mirror which is pivotable about an axis and has a deflecting reflection surface which receives a light beam at an incident angle inclined with respect to a plane which is perpendicular to the axis and the reflecting reflection surface.
Abstract: An optical deflecting unit includes a torsion mirror which is pivotable about an axis and has a deflecting reflection surface which receives a light beam at an incident angle inclined with respect to a plane which is perpendicular to the axis and the deflecting reflection surface, and at least one fixed mirror surface confronting the torsion mirror and arranged so that the light beam is reflected between the torsion mirror and the at least one fixed mirror surface a plurality of times. A moving direction of a reflection position of the light beam on the torsion mirror in a sub scan direction reverses.
47 citations
Patent•
25 May 2000
TL;DR: In this article, a process for the extraction and purification of Paclitaxel from a natural source of taxanes is described, which comprises the following steps: a) extracting with an organic solvent, a raw material comprising PACLITYEL from said natural source, b) treating said raw material with a base or an acid to obtain a biomass by precipitation, isolating said biomass and drying it; c) percolorizing the so-isolated biomass by removing resin and natural pigments contained therein, dissolving said biomass in acetone and then adding thereto at least
Abstract: A process for the extraction and purification of Paclitaxel from a natural source of taxanes. This process comprises the following steps: a) extracting with an organic solvent, a raw material comprising Paclitaxel from said natural source of taxanes; b) treating said raw material with a base or an acid to obtain a biomass by precipitation, isolating said biomass and drying it; c) percolorizing the so-isolated biomass by removing resin and natural pigments contained therein, dissolving said biomass in acetone and then adding thereto at least one non-polar solvent until a Paclitaxel-enriched oily phase is obtained; d) treating with a base or an acid the biomass contained in the Paclitysel-enriched oily phase recovered in the preceding step to obtain another biomass by precipitation, isolating said other biomass and drying it; e) chromatographically purifying at least once a solution of the isolated other biomass obtained in the preceding step in a volatile solvent, and crystallizing at least once the purified solution obtained by chromatography. This process comprises a limited number of steps and allows, after filtration and drying, to obtain a mixture of Paclitaxel crystals consisting of: about 53% of crystals having a purity higher than 99%, about 22% of crystals having a purity higher than 98%, and about 23% of crystals having a purity hither than 92%.
38 citations
Patent•
01 Nov 2001TL;DR: In this article, the authors proposed a combination therapy for treating cell proliferative disorders, which consists of administering a therapeutic effective amount of a cytotoxic agent followed by the administration of a heat shock protein 90 inhibitor.
Abstract: The administration of cytotoxic agents followed by the administration of heat shock protein 90 inhibitors, such as ansamycins, has a synergistic effect on the growth inhibition of cells. This synergy occurs at doses of each cytotoxic agent that normally only causes minimal growth inhibition of cells. Such combination therapy thus allows one to use lower doses of cytotoxic agents to avoid or reduce their respective toxicity to patients without compromising their growth inhibitory effects. Thus, these combinations can be used for the treatment of an animal, preferably a mammal, that has a cell proliferative disorder, whether the cells have wild-type Rb or are Rb deficient or Rb negative. One such method, directed to treating cell proliferative disorders includes the step of administering a therapeutic effective amount of a cytotoxic agent followed by administering a therapeutic effective amount of a heat shock protein 90 inhibitor. The cytotoxic agent may be a microtubule-affecting agent, topoisomerase II inhibitor, a platinum complex, paclitaxel, or a paclitaxel derivative. The HSP90 inhibitor may be an ansamycin, radicicol or a synthetic compound that binds to the ATP-binding site of HSP90.
28 citations
References
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TL;DR: The total synthesis of taxol is reported by a convergent strategy, which opens a chemical pathway for the production of both the natural product itself and a variety of designed taxoids.
Abstract: Taxol, a substance originally isolated from the Pacific yew tree (Taxus brevifolia) more than two decades ago, has recently been approved for the clinical treatment of cancer patients. Hailed as having provided one of the most significant advances in cancer therapy, this molecule exerts its anticancer activity by inhibiting mitosis through enhancement of the polymerization of tubulin and consequent stabilization of microtubules. The scarcity of taxol and the ecological impact of harvesting it have prompted extension searches for alternative sources including semisynthesis, cellular culture production and chemical synthesis. The latter has been attempted for almost two decades, but these attempts have been thwarted by the magnitude of the synthetic challenge. Here we report the total synthesis of taxol by a convergent strategy, which opens a chemical pathway for the production of both the natural product itself and a variety of designed taxoids.
976 citations
573 citations
Patent•
16 Jul 1987TL;DR: Taxol derivatives of formula STR1 are useful antitumor agents as mentioned in this paper, in which R represents hydrogen or acetyl, one of R 1 or R 2 represents hydroxy and the other represents tert-butoxy carbonylamino.
Abstract: Taxol derivatives of formula ##STR1## in which R represents hydrogen or acetyl, one of R 1 or R 2 represents hydroxy and the other represents tert-butoxycarbonylamino and their isomers are useful antitumor agents.
380 citations
TL;DR: In this paper, a chiral ester enolate-imine condensation giving 3-hydroxy-4-aryl-β-lactams with excellent enantiomeric purity is successfully applied to the asymmetric synthesis of the enantiomersically pure taxol C-13 side chain, N-benzoyl-(2R,3S)-3-phenyl-isoserine and its analogs.
370 citations
Patent•
10 Mar 1993TL;DR: Taxol, 10-deacetyltaxol and other taxane derivatives are prepared from naturally occurring taxane-7-xylosides by the oxidative cleavage of the 7-Xyloside moieties as mentioned in this paper.
Abstract: Taxol, 10-deacetyltaxol and other taxane derivatives are prepared from naturally occurring taxane-7-xylosides by the oxidative cleavage of the 7-xyloside moieties.
251 citations