Marco A Biamonte

US Patent:

7148228, Dec 12, 2006

Filed:

Sep 20, 2004

Appl. No.:

10/946637

Inventors:

Srinivas Rao Kasibhatla - San Diego CA, US
Marco A. Biamonte - San Diego CA, US
Kevin D. Hong - San Diego CA, US
David Hurst - San Diego CA, US
Marcus F. Boehm - San Diego CA, US

Assignee:

Conforma Therapeutics Corporation - San Diego CA

International Classification:

C07D 487/04
A61K 31/519
A61P 35/00
A61P 37/06
A61P 29/00

US Classification:

5142621, 544262

Abstract:

A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:.

US Patent:

7241890, Jul 10, 2007

Filed:

Oct 30, 2002

Appl. No.:

10/494414

Inventors:

Srinivas Rao Kasibhatla - San Diego CA, US
Kevin Hong - San Diego CA, US
Lin Zhang - San Diego CA, US
Marco Antonio Biamonte - San Diego CA, US
Marcus F. Boehm - San Diego CA, US
Jiandong Shi - San Diego CA, US
Junhua Fan - San Diego CA, US

Assignee:

Conforma Therapeutics Corporation - San Diego CA

International Classification:

C07D 473/40
C07D 473/24
C07D 473/34
A61K 31/52
A61P 35/00

US Classification:

544276, 544265, 544277

Abstract:

Novel purine compounds of Formula I.

US Patent:

7417058, Aug 26, 2008

Filed:

Sep 27, 2001

Appl. No.:

10/381197

Inventors:

Serge Halazy - Vetraz-Monthoux, FR
Dennis Church - Commugny, CH
Stephen J. Arkinstall - Belmont MA, US
Marco Biamonte - San Diego CA, US
Montserrat Camps - Versoix, CH
Jean-Pierre Gotteland - Beaumont, FR
Thomas Rueckle - Plan-les-Ouates, CH

Assignee:

Laboratoires Serono S.A. - Coinsins

International Classification:

A61K 31/445
A61P 25/00
A61P 37/00
C07D 211/96

US Classification:

514322, 514323, 514326, 546199, 546201, 546212

Abstract:

The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O. R1 is hydrogen or a C1-C6-alkyl group, preferably H. R2 is hydrogen, —COOR3, —CONR3R3′, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.

US Patent:

7432286, Oct 7, 2008

Filed:

Sep 28, 2000

Appl. No.:

10/088074

Inventors:

Stephen Arkinstall - Belmont MA, US
Serge Halazy - Vetraz-Monthoux, FR
Dennis Church - Commugny, CH
Montserrat Camps - Versoix, CH
Thomas Rueckle - Plan-les-Ouates, CH
Jean-Pierre Gotteland - Beaumont, FR
Marco Biamonte - San Diego CA, US

Assignee:

Laboratories Serono SA - Vaud

International Classification:

C07D 417/12
C07D 213/74
A61K 31/44

US Classification:

514336, 514614, 5462681, 564 81

Abstract:

The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonyl hydrazide derivatives as well as to methods of their preparation. In Formula (I) Arand Arare independently from each other an unsubstituted or substituted aryl or beteroaryl group, Xand Xare independently from each other O or S; R, R, Rare independently from each other hydrogen or a C-C-alkyl substituent or Rforms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar; or Rand Rform a substituted or unsubstituted 5-6-membered saturated or unsaturated ring; n is an integer from 0 to 5; G is selected from a group comprising or consisting of an unsubstituted or substituted 4-8 membered heterocycle containing at least one heteroatom, or G is a substituted or unstibstituted C-C-alkyl group.

US Patent:

7544672, Jun 9, 2009

Filed:

Mar 29, 2006

Appl. No.:

11/277918

Inventors:

Srinivas Rao Kasibhatla - San Diego CA, US
Marco Antonio Biamonte - San Diego CA, US
Jiandong Shi - San Diego CA, US
Marcus F. Boehm - San Diego CA, US

Assignee:

Conforma Therapeutics Corporation - San Diego CA

International Classification:

C07D 487/04
C07F 9/38
A61K 31/519
A61K 31/662

US Classification:

514 81, 5142651, 544243, 544280

Abstract:

Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such compounds are also described and claimed.

US Patent:

7544700, Jun 9, 2009

Filed:

Sep 27, 2001

Appl. No.:

10/381665

Inventors:

Serge Halazy - Vetraz-Monthoux, FR
Dennis Church - Commugny, CH
Stephen J. Arkinstall - Belmont MA, US
Marco Biamonte - San Diego CA, US
Montserrat Camps - Versoix, CH
Jean-Pierre Gotteland - Beaumont, FR
Thomas Rueckle - Plan-les-Ouates, CH

Assignee:

Laboratoires Serono SA - Coinsins

International Classification:

A61P 25/00
A61P 25/16
A61K 31/4535
A61K 31/55
A61K 31/4025
C07D 333/34
C07D 409/12
C07D 409/14
C07D 413/14

US Classification:

514322, 514323, 514326, 546199, 546201, 546212

Abstract:

The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl which is substituted with at least one ionizable moiety to which a lipophilic chain is attached and which is containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.

US Patent:

7638538, Dec 29, 2009

Filed:

Sep 28, 2000

Appl. No.:

10/088090

Inventors:

Stephen Arkinstall - Belmont MA, US
Serge Halazy - Vetraz-Monthoux, FR
Dennis Church - Commugny, CH
Montserrat Camps - Versoix, CH
Thomas Rueckle - Plan-les-Ouates, CH
Jean-Pierre Gotteland - Beaumont, FR
Marco Biamonte - San Diego CA, US

Assignee:

Laboratoires Serono S.A. - Coinsins

International Classification:

A61K 31/44
C07D 409/12

US Classification:

514336, 5462804

Abstract:

The present invention is related to sulfonyl amino acid derivatives of formula (I), notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl amino acid derivatives. Said sulfonyl amino acid are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 33. The present invention is furthermore related to novel sulfonyl amino acid derivatives as well as to methods of their preparation.

US Patent:

7683078, Mar 23, 2010

Filed:

Jul 15, 2002

Appl. No.:

10/484744

Inventors:

Thomas Rueckle - Plan-les-Ouates, CH
Jean-Pierre Gotteland - Beaumont, FR
Russel J. Thomas - Boars Hill Oxford, GB
Marco Biamonte - San Diego CA, US

Assignee:

Laboratoires Serono S.A. - Coinsins

International Classification:

C07D 411/12
C07D 409/12
C07D 333/32
A61K 31/445
A61K 31/44
A61K 31/40
A61K 31/38

US Classification:

514326, 514342, 514422, 514446, 546213, 5462814, 548527, 549 65

Abstract:

The present invention relates to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Formula (I) IAris a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ara substituted or unsubstituted arylene or heteroarylene group; Rand Rare independently selected from the group consisting of hydrogen and a C-C-alkyl group.