Conforma Therapeutics Corporation

Laboratoires Serono S.a.

Merck Serono S. A.

Laboratories Serono Sa

Marco Antonio Biamonte

Thomas Rueckle

Jean-Pierre Gotteland

Dennis Church

Serge Halazy

Stephen Arkinstall

Montserrat Camps

Marcus F Boehm

Srinivas Rao Kasibhatla

Kevin Hong

Jiandong Shi

Lin Zhang

Junhua Fan

Jean-Yves Le Brazidec

Russel J Thomas

David Hurst

Jean Pierre Gotteland

Alkynyl pyrrolo [2,3-d] pyrimidines of Formula I 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. 

Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors

Sulfonyl hydrazide compounds according to formula I geometrical isomers thereof, optically active enantiomers thereof, diastereomers thereof, racemates thereof, and/or pharmaceutically acceptable salts thereof are useful in method for treating a neuronal disorder, an autoimmune disease, a cardiovascular disease, or cancer in a patient in need of such treatment.

Pharmaceutically active sulfonyl hydrazide derivatives

The present invention is related to sulfonamide derivatives of formula (I0 notably for use as pharmaceutically active compounds, as well as 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 Arand Arare independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; Ris hydrogen or a C-C-alkyl group, or Rforms a substituted or unsubstituted 5-6 membered saturated or unsaturated ring with Ar; 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 containing at least one nitrogen atom, whereby 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.

Pharmaceutically active sulfonamide derivatives

The present invention relates to benzsulfonamide derivatives of formula I and methods of use thereof. The benzsulfonamide derivatives of the present invention are efficient modulators of the JNK pathway. In particular the benzsulfonamide derivatives of the present invention are selective inhibitors of JNK 2 and 3. 

Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases

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. 

Arylsulfonamide derivatives as C-Jun-N-Terminal Kinases (JNK's) inhibitors

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. 

Pharmaceutically active sulfonyl amino acid derivatives

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. 

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.

Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein JunKinases

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. 

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, &#x2014;COOR3, &#x2014;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.

Novel purine compounds of Formula I. and tautomers, pharmaceutically acceptable salts, and prodrugs thereof, wherein X is S, S(O), or S(O); and O is selected from alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl, and heterocyclic, all optionally substituted, are described, as are pharmaceutical compositions comprising the same, complexes comprising the same, e.g., HSP90 complexes, and methods of using the same.

Purine analogs having HSP90-inhibiting activity

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

Pyrazolopyrimidines and related analogs as HSP90-inhibitors

2-Aminopurine analogs are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various HSP90 mediated disorders, e.g., proliferative disorders. Method of synthesis and use of such compounds are also described and claimed.

2-aminopurine analogs having HSP90-inhibiting activity

The present invention provides compounds represented by Formula I. Ris selected from hydrogen, halogen, lower alkyl, &#x2014;SR, &#x2014;OR, &#x2014;CN, and &#x2014;NHR, Ris halogen, or lower alkyl; Ris &#x2014;NHR; Ris selected from the group consisting of hydrogen, halogen, &#x2014;SR, &#x2014;OR, &#x2014;CN, &#x2014;C(O)R, &#x2014;C(O)OH, &#x2014;NO, &#x2014;NRR, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, and Ris aryl, heteroaryl, alicyclic, or heterocyclic: 

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San Diego, CA, United States of America

Marco Antonio Biamonte