Justin Du Bois

20120238526, Sep 20, 2012

Mar 15, 2012

13/421809

Justin Du Bois - Menlo Park CA, US
Brian M. Andresen - Sharon MA, US
Frederic Menard - Notre-Dame-Du-Mont-Carmel, CA

A61K 31/439
C07D 405/12
C07F 7/18
A61K 31/695
A61P 25/00
A61P 21/02
A61P 29/00
A61P 1/00
A61P 19/02
A61P 25/06
A61P 35/00
A61P 9/06
A61P 25/08
A61P 21/00
A61P 13/10
A61P 17/00
C07D 221/22

514 63, 546 39, 546 14, 514279

Compound derivatives of aconitine are provided, in particular derivatives that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. The subject compounds are useful in treatments, including treatments to modulate neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the aconitine derivatives.

20100284913, Nov 11, 2010

May 7, 2010

12/800053

Justin Du Bois - Palo Alto CA, US
John Mulcahy - Stanford CA, US
Brian Andresen - Menlo Park CA, US
David C. Yeomans - Sunnyvale CA, US
Sandip Biswal - Stanford CA, US

The Board of Trustees of the Leland Stanford Junio - Palo Alto CA

A61K 51/04
C07D 487/14
C07K 16/00
C07K 14/00
C07H 21/04
A61K 31/519
A61K 47/48
A61K 38/02
A61P 1/00
A61P 13/00
A61P 25/00
A61P 25/08
A61P 29/00
A61K 49/16
A61K 49/14
A61K 49/12
A61K 49/10
A61K 38/43
A61P 17/00
A61K 31/58
C12N 9/96

424 165, 544251, 5303917, 530350, 536 231, 514267, 4241781, 514 183, 514 11, 514 177, 424 934, 424 935, 424 93, 424 943, 514176, 435188, 977774

Saxitoxin analogue compounds, compositions, pharmaceutical compositions, methods of synthesis of saxitoxin analogues, methods of imaging, methods of treatment, including methods of treating pain, are provided. Saxitoxin (STX), gonyautoxin (GTX), and zetekitoxin, and variant STX compounds bind to sodium channels and are effective to reduce or block flow of sodium ions through such channels. Such channel block affects nerve and muscle action, and may be effective to reduce or block pain sensations, relax muscles, reduce muscle spasm, and reduce wrinkles. STX analogue binding to sodium channels may also be useful to locate, image, or mark sodium channels, and so be useful in studying sodium channels and sodium channel disorders, and in the diagnosis and treatment of patients suffering from sodium channel disorders. In embodiments, the variant STX compounds include conjugates having increased serum half-life as compared to STX when administered to a subject.In embodiments, the present disclosure provides a method for alleviating pain in a subject in need of treatment, the method comprising administering to the subject an effective amount of a saxitoxin analogue compound, or a pharmaceutically acceptable salt, isomer, tautomer or prodrug thereof, whereby pain in said subject is alleviated.

20220259218, Aug 18, 2022

Jan 26, 2022

17/585530

- South San Francisco CA, US
- Stanford CA, US
George Miljanich - Redwood City CA, US
Anton Delwig - Albany CA, US
Jacob Beckley - Bozeman MT, US
Grant Masaaki Shibuya - South San Francisco CA, US
Justin Du Bois - Menlo Park CA, US

C07D 487/14

Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): where R, R, R, R, and Xare as described herein.

20200102317, Apr 2, 2020

Mar 29, 2018

16/499201

- Bozeman MT, US
- Stanford CA, US
George MILJANICH - Bozeman MT, US
Anton DELWIG - Bozeman MT, US
Jacob BECKLEY - Bozeman MT, US
Grant Masaaki SHIBUYA - Bozeman MT, US
Justin DU BOIS - Stanford CA, US

C07D 487/14

Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): where R, X, and Xare as described herein.

20200102318, Apr 2, 2020

Mar 29, 2018

16/499205

- Bozeman MT, US
- Stanford CA, US
George MILJANICH - Redwood City CA, US
Anton DELWIG - Albany CA, US
Jacob BECKLEY - Bozeman MT, US
Grant Masaaki SHIBUYA - South San Francisco CA, US
Justin DU BOIS - Menlo Park CA, US

C07D 487/14

Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): where R, R, R, R, and Xare as described herein.

20200016103, Jan 16, 2020

Jun 21, 2019

16/449021

- Stanford CA, US
Justin Du Bois - Palo Alto CA, US
Merritt C. Maduke - Palo Alto CA, US

A61K 31/196

Provided herein are small-molecules for use in modulating chloride ion channel (CLC) activity, particularly the activity of CLC-2, to elucidate the role of CLC-2 in disorders associated with CLC-2 malfunction, and to identify therapeutic leads for their treatment. Compositions and methods for modulating CLC activity are also provided. In certain aspects, the subject compounds and compositions are useful for imaging or channel pull-down studies.

20170233398, Aug 17, 2017

Sep 30, 2016

15/283187

- Bozeman MT, US
- Stanford CA, US
Grant Masaaki SHIBUYA - South San Francisco CA, US
Anton DELWIG - Albany CA, US
George MILJANICH - Redwood City CA, US
Justin DU BOIS - Menlo Park CA, US

C07D 487/14

Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I):where R, Xand Xare as described herein.

20170029431, Feb 2, 2017

Apr 9, 2015

15/302964

- Redwood City CA, US
- Stanford CA, US
John MULCAHY - Redwood City CA, US
Justin DU BOIS - Menlo Park CA, US
Matthew AXTMAN - Cary NC, US
James WALKER - Menlo Park CA, US
Jeffrey E. MERIT - San Diego CA, US

C07D 487/14

Provided herein are compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function, for example conditions associated with pain. The compounds are 10′,11′-modified saxitoxins. The compounds are optionally additionally modified at carbon 13. In certain embodiments, the 10′,11′-modified saxitoxins are of Formula I: where R, Rand Rare as described herein. Also provided herein are methods of treating pain in a mammal comprising administering an effective treatment amount of a 10′,11′ modified saxitoxin or composition to a mammal. In an embodiment, the mammal is a human.