Nigel H. Greig - Phoenix MD, US Harold Holloway - Middle River MD, US Arnold Brossi - Bethesda MD, US Xiaoxiang Zhu - North Brunswick NJ, US Tony Giordano - Shreveport LA, US William D. Figg - Fairfax VA, US
Assignee:
The United States of America as represented by the Department of Health and Human Services - Washington DC P2D Inc. - Cincinnati OH
International Classification:
A01N 43/40 A61K 31/445
US Classification:
514323, 546201, 546221, 514183
Abstract:
Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-α) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
Nigel H. Greig - Phoenix MD, US Harold Holloway - Middle River MD, US Arnold Brossi - Bethesda MD, US Xiaoxiang Zhu - North Brunswick NJ, US Tony Giordano - Shreveport LA, US William D. Figg - Fairfax VA, US
Assignee:
P2D, Inc. - Cincinnati OH
International Classification:
A01N 43/40 A61K 31/445
US Classification:
514323, 546201, 546221, 514183
Abstract:
Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-α) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
Tetrahydrobenzothiazole Analogues As Neuroprotective Agents
Nigel Greig - Phoenix MD, US Mark Mattson - Bel Air MD, US Xiaoxiang Zhu - North Brunswick NJ, US Harold Holloway - Middle River MD, US
International Classification:
A61K031/428
US Classification:
514/367000
Abstract:
This invention relates generally to tetrahydrobenzothiazole analogues and tetrahydrobenzooxyzole analogues, to pharmaceutical compositions which include these compounds and a pharmaceutically acceptable carrier, and to methods of treatment using these compounds. The invention also encompasses pharmaceutically acceptable esters, amides, and salts of such compounds. The invention further provides a method of reducing or delaying apoptosis in a population of cells, comprising contacting the population of cells with a tetrahydrobenzothiazole analogue or a tetrahydrobenzooxyzole analogue, thereby reducing or delaying apoptosis in the population of cells.
Hydroxy Piperidine Derivatives To Treat Gaucher Disease
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
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.
Method For The Treatment Of Pompe Disease Using 1-Deoxynojirimycin And Derivatives
Benjamin Mugrage - Cranbury NJ, US Gary Lee - Cranbury NJ, US Xiaoxiang Zhu - Cranbury NJ, US Robert Boyd - Cranbury NJ, US Kamlesh Sheth - Cranbury NJ, US
International Classification:
A61K 31/445
US Classification:
514317000, 514326000, 514327000
Abstract:
The present invention provides a method for increasing the activity of a mutant or wild-type α-glucosidase enzyme in vitro and in vivo by contacting the enzyme with a specific pharmacological chaperone which is a derivative of 1-deoxynojirimycin. The invention also provides a method for the treatment of Pompe disease by administration of chaperone small molecule compound which is a derivative of 1-deoxynojirimycin. The 1-deoxynojirimycin derivative is substituted at the N or C1 position. Combination therapy with replacement α-glucosidase gene or enzyme is also provided.
Tetrahydrobenzothiazole Analogues As Neuroprotective Agents
This invention relates generally to tetrahydrobenzothiazole analogues and tetrahydrobenzooxyzole analogues, to pharmaceutical compositions which include these compounds and a pharmaceutically acceptable carrier, and to methods of treatment using these compounds. The invention also encompasses pharmaceutically acceptable esters, amides, and salts of such compounds. The invention further provides a method of reducing or delaying apoptosis in a population of cells, comprising contacting the population of cells with a tetrahydrobenzothiazole analogue or a tetrahydrobenzooxyzole analogue, thereby reducing or delaying apoptosis in the population of cells.
Hydroxy Piperidine Derivatives To Treat Gaucher Disease
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.
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