Isis Pharmaceuticals, Inc.

Sgx Pharmaceuticals, Inc.

Elizabeth Anne Jefferson

Eric E Swayze

Punit P Seth

Richard Holmes Griffey

Christopher Ronald Smith

Pierre-Yves Bounaud

Eduardo Torres

Yun He

Patrick S Lee

Dale E Robinson, Jr

The present disclosure provides bicyclic triazole protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.

Bicyclic triazoles as protein kinase modulators

Benzimidazoles and analogs thereof as antivirals

The present disclosure relates to triazolopyridazine protein kinase modulators of Formula (I), methods of using these compounds to treat diseases mediated by kinase activity. 

Triazolopyridazine protein kinase modulators

Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistantstrain.

Antimicrobial biaryl compounds

The present invention is directed to novel benzimidazoles according to representative structures I and II, and their derivatives that possess antibacterial activity. This invention is also directed to compositions including the benzimidazole derivatives, and methods for using the same.

Benzimidazole compounds

Provided are antibacterial compounds having Formula I:In such compositions, X is O or S; Y is CH; n isor. One of Rand Ris &#x2014;C(O)NRR, &#x2014;C(O)&#x2014;Q&#x2014;NRR, &#x2014;CHNRRor &#x2014;S(O)NRRand the other is H or R. One of Rand Ris &#x2014;NHC(O)Ror &#x2014;NHS(O)Rand the other is H or R. Q is an amino acid or peptide. Ris H, halogen, &#x2014;NRRor &#x2014;NHC(O)R; and Ris selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. Ris selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; Ris H or Rand Rtogether form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide. Ris selected from the group consisting of H; amino; alkyl, alkenyl or alkynyl, each optionally substituted with halogen, amino, amidinyl, guanidinyl, urea, carboxyl or carboxamide; a 5-16 member carbocycle or heterocycle; and a 5-16 member heterocycle-substituted alkyl or carbocycle-substituted alkyl, wherein said carbocycle and heterocycle are optionally substituted with halogen, OH, amino, alkyl, carboxyl, oxo or carboxamide.

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La Jolla, CA, United States of America

Elizabeth Anne Jefferson