Richard P Silva

US Patent:

6489512, Dec 3, 2002

Filed:

Jun 21, 2002

Appl. No.:

10/177381

Inventors:

Frederick Hicks - Somerville MA
Da-Ming Gou - Lexington MA
Salvatore Anthony Marchese - Malden MA
Lawrence J. Martel - Manchester NH
Atena Necula - Everett MA
Richard E. Benetti - Somerville MA
Richard A. Silva - Foxboro MA

Assignee:

Rhodia Chirex Inc. - Boston MA

International Classification:

C07C25100

US Classification:

564310, 564313, 564314, 546249, 5462774, 546329

Abstract:

A method for making an indole compound includes transition metal-catalyzed arylation of a hydrazone to form an aryl hydrazone, hydrolysis of the aryl hydrazone to form an aryl hydrazine, and acid catalyzed cyclization of the aryl hydrazine to form the indole compound.

US Patent:

6858734, Feb 22, 2005

Filed:

Apr 23, 2003

Appl. No.:

10/421564

Inventors:

Richard A. Silva - Foxborough MA, US

Assignee:

Rhodia Pharma Solutions Inc. - Cranbury NJ

International Classification:

C07D515/02
C07D401/02
C07D409/02

US Classification:

546114, 514301

Abstract:

A process for producing enantiomerically enriched (S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5 (4H)-acetic acid hydrocarbyl ester, represented by the formula: Is provided, wherein Rand Rare hydrogens and Ris methyl (i. e. , (S)-Clopidogrel). The process includes the steps of: (a) contacting N-2-chlorobenz-aldehyde-ylidene-1-ethylamine-2(2-thiophenyl)imine and an HCN source, in the presence of a non-metallic asymmetric Strecker catalyst to form enantiomerically enriched (S)-α,α-(2-thiophenylethylamino)(2-chlorophenyl)acetonitrile; (b) contacting the enantiomerically enriched (S)-α,α-(2-thiophenylethylamino)(2-chlorophenyl)acetonitrile and a formaldehyde equivalent, in the presence of an acid catalyst to form enantiomerically enriched α-5(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorobenzyl)-nitrile; and (c) contacting the enantiomerically enriched α-5(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorobenzyl)-nitrile and a reagent capable of converting a cyano group into an ester group to form enantiomerically enriched hydrocarbyl ester of (S)-α-(2-chlorophenyl)-6,7-dihydrothieno-[3,2-c]pyridine-5(4H)-acetic acid.

US Patent:

8304447, Nov 6, 2012

Filed:

May 30, 2008

Appl. No.:

12/601871

Inventors:

Craig Siegel - Woburn MA, US
Cecilia M. Bastos - South Grafton MA, US
David J. Harris - Lexington MA, US
Angeles Dios - Waltham MA, US
Edward Lee - Sudbury MA, US
Richard Silva - Needham MA, US
Lisa M. Cuff - Leominster MA, US
Mikaela Levine - Swampscott MA, US
Cassandra A. Celatka - Hull MA, US
Frederic Vinick - Lexington MA, US
Thomas H. Jozefiak - Belmont MA, US
Yibin Xiang - Acton MA, US
John Kane - Maynard MA, US
Junkai Liao - Tewksbury MA, US

Assignee:

Genzyme Corporation - Cambridge MA

International Classification:

A61K 31/40
A61K 31/4025
C07D 207/04
C07D 405/02

US Classification:

514408, 514422, 548400, 548526

Abstract:

A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-α, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

US Patent:

8309593, Nov 13, 2012

Filed:

Oct 2, 2009

Appl. No.:

13/122135

Inventors:

Craig Siegel - Woburn MA, US
Cecilia M. Bastos - South Grafton MA, US
David J. Harris - Lexington MA, US
Angeles Dios - Waltham MA, US
Edward Lee - Sudbury MA, US
Richard Silva - Needham MA, US
Lisa M. Cuff - Leominster MA, US
Mikaela Levine - Swampscott MA, US
Cassandra A. Celatka - Hull MA, US
Frederic Vinick - Mechanicville NY, US
Yibin Xiang - Acton MA, US
John Kane - Maynard MA, US
Junkai Liao - Tewksbury MA, US

Assignee:

Genzyme Corporation - Cambridge MA

International Classification:

A61K 31/4025
A61K 31/40

US Classification:

514408, 514422

Abstract:

A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

US Patent:

20020119909, Aug 29, 2002

Filed:

Jan 17, 2002

Appl. No.:

10/051771

Inventors:

Roger Pettman - Weston MA, US
Richard Silva - Foxborough MA, US
Jay Larrow - Wakefield MA, US
Isabelle Storet - Les Eparres, FR

Assignee:

Rhodia ChiRex, Inc.

International Classification:

A61K007/46
C07C029/10

US Classification:

512/025000, 568/867000

Abstract:

The present invention includes a process for enantioselective preparation of a non-racemic compound, which is either usable as a fragrance or flavor component or is convertible to a fragrance or flavor component by one or more additional reaction steps. The process includes the step of contacting either a substrate capable of forming a non-racemic compound by an enantioselective reaction and a co-reactant in the presence of a non-racemic catalyst, or a non-racemic or enantiopure substrate and a co-reactant, optionally in the presence of a racemic or non-racemic catalyst. The contacting is carried out at a temperature and length of time that is sufficient to produce the non-racemic compound with high optical purity. The process is used in stereoselective preparation of enantiomerically enriched intermediates useful in the preparation of non-racemic, chiral flavor and fragrance components.

US Patent:

20020177738, Nov 28, 2002

Filed:

May 23, 2002

Appl. No.:

10/155204

Inventors:

Jay Larrow - Wakefield MA, US
Roger Pettman - Weston MA, US
Richard Silva - Foxborough MA, US
Isabelle Storet - Les Eparres, FR

International Classification:

C07C043/235
C07C029/44

US Classification:

568/662000, 568/814000

Abstract:

The present invention relates to novel optically active benzylalkylcarbinols, to their preparation and to their use, in particular in perfumery.

US Patent:

20050049226, Mar 3, 2005

Filed:

Oct 13, 2004

Appl. No.:

10/963707

Inventors:

Richard Silva - Foxborough MA, US

Assignee:

Rhodia Pharma Solutions Inc. - Cranbury NJ

International Classification:

A01N057/00
A61K031/66
A01N043/62
A01N047/40

US Classification:

514114000, 514514000, 514301000

Abstract:

A process for producing enantiomerically enriched (S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5 (4H)-acetic acid hydrocarbyl ester, represented by the formula: Is provided, wherein Rand Rare hydrogens and Ris methyl (i.e., (S)-Clopidogrel). The process includes the steps of: (a) contacting N-2-chlorobenz-aldehyde-ylidene-1-ethylamine-2 (2-thiophenyl)imine and an HCN source, in the presence of a non-metallic asymmetric Strecker catalyst to form enantiomerically enriched (S)-α,α-(2-thiophenylethylamino) (2-chlorophenyl) acetonitrile; (b) contacting the enantiomerically enriched (s)-α,α-(2-thiophenylethylamino) (2-chlorophenyl) acetonitrile and a formaldehyde equivalent, in the presence of an acid catalyst to form enantiomerically enriched α-5 (4,5,6,7-tetrahydro[3,2-c] thienopyridyl) (2-chlorobenzyl)-nitrile; and (c) contacting the enantiomerically enriched α-5(4,5,6,7-tetrahydro[3,2-c] thienopyridyl) (2-chlorobenzyl)-nitrile and a reagent capable of converting a cyano group into an ester group to form enantiomerically enriched hydrocarbyl ester of (S)-α-(2-chlorophenyl)-6,7-dihydrothieno-[3,2-c]pyridine-5(4H)-acetic acid.

US Patent:

20060166963, Jul 27, 2006

Filed:

Dec 15, 2005

Appl. No.:

11/304238

Inventors:

Richard Silva - Needham MA, US
Andrew Jones - Needham MA, US
Todd Blythe - Georgetown MA, US

International Classification:

A61K 31/55
A61K 31/541
A61K 31/5377
A61K 31/517
C07D 417/02
C07D 413/02
C07D 403/02

US Classification:

514210210, 514217060, 514234200, 514252170, 514249000, 514227800, 514266210, 514266200, 544060000, 544121000, 544284000, 540600000

Abstract:

The present invention relates to methods for preparing compounds of formula I: or suitable salts thereof useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also relates to methods for preparing intermediates related thereto.