Xiaoxiang Zhu from Hammond, IN, age 64

Hydroxy Piperidine Derivatives To Treat Gaucher Disease
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US Patent:

20050130972, Jun 16, 2005
Filed:

Nov 12, 2004
Appl. No.:

10/988428
Inventors:

Jian-Qiang Fan - Demarest NJ, US
Xiaoxiang Zhu - North Brunswick NJ, US
Kamlesh Sheth - North Brunswick NJ, US
International Classification:

A61K031/501
A61K031/454
C07D043/02
A61K031/50
A61K031/445
US Classification:

514247000, 514326000, 514328000, 514252010, 544238000, 544239000, 546207000
Abstract:

The present invention provides novel hydroxy piperidine (HP) derivatives having (i) a positive charge at the position corresponding to the anomeric position of a pyranose ring; (ii) a short, flexible linker emanating from the corresponding position of the ring oxygen in a pyranose; and (iii) a lipophilic moiety connected to the linker and pharmaceutically acceptable salts thereof. The linker can be absent if the lipophilic moiety corresponds to a hydrocarbon chain with a linear length of 6 or more carbons. The present invention further provides a method for treating individuals having Gaucher disease by administering the novel HP derivative as “active-site specific chaperones” for the mutant glucocerebrosidase associated with the disease.

Glucoimidazole And Polyhydroxycyclohexenyl Amine Derivatives To Treat Gaucher Disease
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US Patent:

20050137223, Jun 23, 2005
Filed:

Nov 12, 2004
Appl. No.:

10/988427
Inventors:

Jian-Qiang Fan - Demarest NJ, US
Xiaoxiang Zhu - North Brunswick NJ, US
Kamlesh Sheth - North Brunswick NJ, US
International Classification:

C07D471/02
A61K048/00
A61K031/4745
US Classification:

514303000, 546118000, 564123000, 514044000
Abstract:

The present invention provides glucoimidazole (GIZ) and polyhydroxycyclohexenyl amine (PHCA) derivatives, methods of making them, and methods of use where the GIZ and PHCA derivatives have a short, flexible linker emanating from the corresponding position of the ring oxygen in a pyranose; and a lipophilic moiety connected to the linker and pharmaceutically acceptable salts thereof. More particularly, the present invention further provides a method for treating individuals having Gaucher disease by administering the novel GIZ or PHCA derivatives as “active-site specific chaperones” for the mutant glucocerebrosidase associated with the disease.

Hydroxy Piperidine Derivatives To Treat Gaucher Disease
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US Patent:

20100189708, Jul 29, 2010
Filed:

Apr 8, 2010
Appl. No.:

12/756382
Inventors:

Jian-Qiang Fan - Demarest NJ, US
Xiaoxiang Zhu - North Brunswick NJ, US
Kamlesh Sheth - North Brunswick NJ, US
Assignee:

AMICUS THERAPEUTICS, INC. - Cranbury NJ
International Classification:

A61K 31/45
A61K 38/47
A61K 31/7088
A61P 43/00
US Classification:

424 9461, 514315, 514 44 R
Abstract:

The present invention provides novel hydroxy piperidine (HP) derivatives having (i) a positive charge at the position corresponding to the anomeric position of a pyranose ring; (ii) a short, flexible linker emanating from the corresponding position of the ring oxygen in a pyranose; and (iii) a lipophilic moiety connected to the linker and pharmaceutically acceptable salts thereof. The linker can be absent if the lipophilic moiety corresponds to a hydrocarbon chain with a linear length of 6 or more carbons. The present invention further provides a method for treating individuals having Gaucher disease by administering the novel HP derivative as “active-site specific chaperones” for the mutant glucocerebrosidase associated with the disease.