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- Inventor(s):
- Olaf G. Wiest, Paul Helquist, Frederick R. Maxfield
- Patent Number:
- US 9333222 B2
- Description:
Embodiments herein relate to the field of lysosomal storage disorders, and, more specifically, to methods of treating lysosomal storage disorders such as Niemann-Pick type C disease, for instance with inhibitors of histone deacetylases, particularly inhibitors of class 1 histone deacetylases. In various embodiments, methods of treating Niemann-Pick type C disease with inhibitors of class 1 histone deacetylases are described.
- Date Issued:
- May 10, 2016
- Record Visibility:
- Public
- Title
- Histone deacetylase inhibitors as therapeutic agents for Niemann-Pick type C disease
- Description
- Embodiments herein relate to the field of lysosomal storage disorders, and, more specifically, to methods of treating lysosomal storage disorders such as Niemann-Pick type C disease, for instance with inhibitors of histone deacetylases, particularly inhibitors of class 1 histone deacetylases. In various embodiments, methods of treating Niemann-Pick type C disease with inhibitors of class 1 histone deacetylases are described.
- Creator
- Olaf G. Wiest, Paul Helquist, Frederick R. Maxfield
- Publisher
- United States Patent and Trademark Office
- Language
- English
- Rights
- All rights reserved
- Resource Type
- Patent
-
- Inventor(s):
- Paul Helquist
- Patent Number:
- US 6730788 B2
- Description:
Process for preparing 1,10-phenanthroline ligands represented by the formula ##STR1## which comprises coupling a 1,10-phenanthroline of the formula ##STR2## with a ketone e.g. a dialkyl, cycloalkyl or bicycloalkyl ketone with a metal coupling reagent, preferably a lanthanide II e.g. samarium II, wherein R is hydrogen, alkyl, cycloalkyl, bicycloalkyl or aryl e.g. phenyl. The hydroxy group of the product may be converted to derivatives e.g. esters and ethers to form additional ligands. The hydr…
- Date Issued:
- 2004-05-04
- Record Visibility:
- Public
- Title
- Process for 1,10-phenanthroline ligands
- Description
- Process for preparing 1,10-phenanthroline ligands represented by the formula ##STR1## which comprises coupling a 1,10-phenanthroline of the formula ##STR2## with a ketone e.g. a dialkyl, cycloalkyl or bicycloalkyl ketone with a metal coupling reagent, preferably a lanthanide II e.g. samarium II, wherein R is hydrogen, alkyl, cycloalkyl, bicycloalkyl or aryl e.g. phenyl. The hydroxy group of the product may be converted to derivatives e.g. esters and ethers to form additional ligands. The hydroxy group of the product also may be converted to a reducible group e.g. the methoxy ether and the ether replaced by hydrogen in the reduction. The reduction product wherein R of the starting material is hydrogen can be coupled with a ketone in the process to provide 2,9-disubstituted 1,10-phenanthroline ligands. The ligands provided are preferably in chiral form and complex with metals, e.g. transition metals, which serve as catalysts in many processes such as addition and substitution reactions.
- Creator
- Paul Helquist
- Publisher
- United States Patent and Trademark Office
- Language
- English
- Rights
- http://creativecommons.org/publicdomain/zero/1.0/
- Resource Type
- Patent
-
- Inventor(s):
- Paul Helquist, Carlo Cocito
- Patent Number:
- US 5587475 B2
- Description:
Derivatized type A virginiamycins having a reactive functionalized side chain, and a process for making the virginiamycin derivatives. The side chain contains a thioether linkage and a reactive group, such as a carboxylate ester or free carboxylic acid group.
- Date Issued:
- 1996-12-24
- Record Visibility:
- Public
- Title
- Derivatized virginiamycin M.sub.1
- Description
- Derivatized type A virginiamycins having a reactive functionalized side chain, and a process for making the virginiamycin derivatives. The side chain contains a thioether linkage and a reactive group, such as a carboxylate ester or free carboxylic acid group.
- Creator
- Paul Helquist, Carlo Cocito
- Publisher
- United States Patent and Trademark Office
- Language
- English
- Rights
- http://creativecommons.org/publicdomain/zero/1.0/
- Resource Type
- Patent
-
- Inventor(s):
- Paul Helquist, Joakim Loefstedt
- Patent Number:
- US 7235688 B2
- Description:
A process for preparing unsaturated esters useful as intermediates for HDAC inhibitors, by reacting an aldehyde or ketone having the following formula I: ##STR00001## wherein R.sub.1 is an aromatic group or a combined aliphatic and aromatic group; X is –O–, –S–, –COO–, –OOC–, –CONR.sub.7–, or –R.sub.7NCO–; L.sub.1 an aliphatic linking group, an aromatic linking group, or a combined aliphatic and aromatic linking group; R.sub.2 and R.sub.3 are each independently hydrogen, a hydroxy…
- Date Issued:
- 2007-06-26
- Record Visibility:
- Public
- Title
- Process for preparing histone deacetylase inhibitors and intermediates thereof
- Description
- A process for preparing unsaturated esters useful as intermediates for HDAC inhibitors, by reacting an aldehyde or ketone having the following formula I: ##STR00001## wherein R.sub.1 is an aromatic group or a combined aliphatic and aromatic group; X is --O--, --S--, --COO--, --OOC--, --CONR.sub.7--, or --R.sub.7NCO--; L.sub.1 an aliphatic linking group, an aromatic linking group, or a combined aliphatic and aromatic linking group; R.sub.2 and R.sub.3 are each independently hydrogen, a hydroxy group, an alkoxy group, an amino group, a carboxyl group, an amide group, an ester group, a carbamate group, an aliphatic group, an aromatic group, a combined aliphatic and aromatic group, R.sub.2 and R.sub.3 together are .dbd.O, or one of R.sub.2 and R.sub.3 form a double bond with one of R.sub.4 and R.sub.5; R.sub.4 and R.sub.5 are each independently hydrogen, a hydroxy group, an alkoxy group, an amino group, a carboxy group, an amide group, an ester group, a carbamate group, an aliphatic group, an aromatic group, a combined aliphatic and aromatic group, or one of R.sub.4 and R.sub.5 form a double bond with one of R.sub.2 and R.sub.3; R.sub.6 is hydrogen, an aliphatic group, an aromatic group, or a combined aliphatic and aromatic group; R.sub.7 is hydrogen, an aliphatic group, an aromatic group, or a combined aliphatic and aromatic group; m is 0 or 1; n is 0 or 1; and p is 0 or 1; with an ester having the following formula II: ##STR00002## wherein R.sub.8 is an aliphatic group, an aromatic group, or a combined aliphatic and aromatic group; R.sub.9 and R.sub.10 each independently hydrogen, an aliphatic group, an aromatic group, a combined aliphatic and aromatic group, or one of R.sub.9 and R.sub.10 form a double bond with L.sub.2; R.sub.11 and R.sub.12 are each an aliphatic group, an aromatic group, or a combined aliphatic and aromatic group; L.sub.2 is an aliphatic linking group, an aromatic linking group, or a combined aliphatic and aromatic linking group; A is P or As; and p is 0 or 1.
- Creator
- Paul Helquist, Joakim Loefstedt
- Publisher
- United States Patent and Trademark Office
- Language
- English
- Rights
- http://creativecommons.org/publicdomain/zero/1.0/
- Resource Type
- Patent