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Inventor:
Nicolaou; K. C.
Address:
La Jolla, CA
No. of patents:
16
Patents:












Patent Number Title Of Patent Date Issued
6271384 Self-assembled taxo-diterpenoid nanostructures August 7, 2001
Onium salts of taxo-diterpenoid-C.sup.n,2-O-aza-arenes form water soluble self-assembling nanostructures above a critical aggregation concentration. The onium salt of aza-arene includes a delocalized charge which renders derivatized taxo-diterpenoids amphoteric, enhances their solubility
6252094 Chemical switching of taxo-diterpenoids between low solubility active forms and high solubility June 26, 2001
Cyclic chemical switching method is employed for solubilizing and desolubilizing taxo-diterpenoids with respect to aqueous solvents. 2-Halogenated onium salts of aza-arenes are employed to derivatize taxo-diterpenoids so as to alter their solubility in aqueous solvents. The onium sal
6043382 Transformations of taxol March 28, 2000
A method for esterifying C13 deoxy taxoid intermediates employs three steps, i.e., oxygenation of the C13 deoxy taxoid intermediate to produce a C13 enone taxoid intermediate; reduction of the C13 enone to produce an alcohol; followed by esterification of the C13 alcohol. Key intermediat
5817840 Water soluble taxol derivatives October 6, 1998
Alkaline sensitive protaxol is water soluble and is hydrolyzed at physiological (alkaline) pH to render the native taxol structure and the native taxol activity. Protaxol compositions include 2'- and/or 7-O-ester derivatives of taxol and/or 2'- and/or 7-O-carbonate derivatives taxol.
5760240 Taxoid synthesis June 2, 1998
Bioactive ABC taxoids accessible by convergent synthesis have an intact AB ring framework of taxol, including the C.sup.13 side chain, and an aromatic C ring which substitutes for the CD ring system found on native taxol. The aromatic C ring may be substituted or unsubstituted. MPT d
5750691 Access to taxol analogs May 12, 1998
Transformations of taxol, baccatin III and of 10-deacetyl baccatin III provide access to novel taxol analogs and key intermediates thereto.
5608087 Water soluble taxol derivatives March 4, 1997
Alkaline sensitive protaxol is water soluble and is hydrolyzed at physiological (alkaline) pH to render the native taxol structure and the native taxol activity. Protaxol compositions include 2'- and/or 7-O-ester derivatives of taxol and/or 2'- and/or 7-O-carbonate derivatives taxol.
5550246 Calicheamicin mimics August 27, 1996
Synthetic calicheamicin mimics employ alternative activation triggers and trigger cites and include tithers for conjugation to DNA targeting systems.
5504222 Transformations of taxol April 2, 1996
A method for esterifying C13 deoxy taxoid intermediates employs three steps, i.e., oxygenation of the C13 deoxy taxoid intermediate to produce a C13 enone taxoid intermediate; reduction of the C13 enone to produce an alcohol; followed by esterification of the C13 alcohol. Key intermediat
5500432 Induction and inhibition of apoptosis March 19, 1996
A method for inducing apoptosis in target cells employs designed enediynes which are triggered to become chemically reactive when bound to target cells. Conversely, a method for inhibiting the induction of apoptosis employs compounds which compete with the above compounds which induce
5481007 Taxoid synthesis January 2, 1996
Bioactive ABC taxoids accessible by convergent synthesis have an intact AB ring framework of taxol, including the C.sup.13 side chain, and an aromatic C ring which substitutes for the CD ring system found on native taxol. The aromatic C ring may be substituted or unsubstituted. MPT d
5461169 Total synthesis of taxol and taxol analogs October 24, 1995
The total synthesis of taxol employs a convergent synthetic plan. The synthetic plan may also be employed to produce a large number of taxol analogs. Taxol analogs having skeletal extensions are inaccessible by modification of the natural product but are readily produced by employing
5440057 Access to taxol analogs August 8, 1995
Transformations of taxol, baccatin III and of 10-deacetyl baccatin III provide access to novel taxol analogs and key intermediates thereto.
5422364 Water soluble taxol derivatives June 6, 1995
Alkaline sensitive protaxol is water soluble and is hydrolyzed at physiological (alkaline) pH to render the native taxol structure and the native taxol activity. Protaxol compositions include 2'- and/or 7-O-ester derivatives of taxol and/or 2'- and/or 7-O-carbonate derivatives taxol.
5274137 Intermediates for preparation of taxols December 28, 1993
A taxol intermediate selected from the group consisting of: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each selected from hydrogen, hydroxyl, or a protected hydroxyl; or R.sup.1 and R.sup.2 together form an oxo or a protected oxo; R.sup.3 is formyl, a protecte
5237101 Propargylic and allenic sulfones August 17, 1993
Propargylic and allenic sulfones are disclosed having the ability to selectively cleave nucleic acids, especially deoxyribonucleic acid. Such compositions are capable of being synthetically modified to effect cleavage at selected, sequenced sites on nucleic acids.










 
 
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