Abstract: The present invention provides compounds of formula (I) which are potent inhibitors of Chk1 and have the structural formula below: wherein R1, R2, R3, R4, and R5 are as defined herein. Pharmaceutical compositions comprising the compounds, uses thereof and their preparation process are also provided.

Abstract: The present invention provides compounds of formula (I) which are potent inhibitors of Chk1 and have the structural formula below: wherein R1, R2, R3, R4, and R5 are as defined herein. Pharmaceutical compositions comprising the compounds, uses thereof and their preparation process are also provided.

Abstract: Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X is —O—, —N(R3)—, —S—, —S(O)— or —S(O)2—; R2 is a C1-4 alkyl group or —CF3; and R1, R3, R4 and p are as defined herein; wherein the compounds are useful as kinase inhibitors. Also disclosed are pharmaceutical compositions containing, and intermediate compounds and methods for making the compounds of formula (I) and their pharmaceutically acceptable salts; and methods of using the foregoing to treat inflammatory and autoimmune diseases such as asthma, colitis, multiple sclerosis, psoriasis, arthritis, rheumatoid arthritis, inflammatory bowel disease, and joint inflammation.

Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.

Abstract: The present invention is directed to a process for preparing compounds of formula (I): wherein A, R1-R3, X, s, t, u, m and Z are defined herein, comprising the step of reacting a reagent of formula (II): in the presence of Pd(O) metal with a compound of formula (III): or salts thereof. Another aspect of this invention is a method of preparing compounds of formula (VI).

Abstract: The present invention relates to Benzo[c][2,7]naphthyridine Derivatives, compositions comprising an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for modulating PDK-1 activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c][2,7]naphthyridine Derivative.

Abstract: There is herein provided a process for Zr-mediated hydroboration of alkynes which offers (E)-vinylboronic esters in high yield with stereoselectivity and regioselectivity.

Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.

Abstract: There is provided a process for the preparation of 7-substituted-3-quinolinecarbonitriles and intermediates useful in a process to prepare 7-substituted-3-quinolinecarbonitriles and pharmaceutically acceptable salts is described. Where 7-fluoro-4-oxo-1,4-dihydro-3-quinolinecarbonitrile is converted in three steps to 7-substituted-3-quinolinecarbonitriles which inhibit the action of certain protein kinases and are useful in the treatment of cancer.

Abstract: There is provided a process for the preparation of 7-substituted-3-quinolinecarbonitriles and intermediates useful in a process to prepare 7-substituted-3-quinolinecarbonitriles and pharmaceutically acceptable salts is described. Where 7-fluoro-4-oxo-1,4-dihydro-3-quinolinecarbonitrile is converted in three steps to 7-substituted-3-quinolinecarbonitriles which inhibit the action of certain protein kinases and are useful in the treatment of cancer.

Abstract: This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.