Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

Abstract: A 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2?-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

Abstract: A 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2?-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

Abstract: A crystalline form of 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer of 5(RS)-(2?-hydroxyethoxy)-20(S)-camptothecin is described that is characterized by having an X-ray powder diffraction pattern comprising one or more peak intensities expressed in degrees 2? that are selected from the group consisting of 7.2±0.1, 9.4±0.1, 11.02±0.1, 12.00±0.1, 14.54±0.1, 15.2±0.1, 18.92±0.1, 21.86±0.1, 22.74±0.1 and 26.42±0.1. Methods of making and using the compound are also described.

Abstract: A 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2?-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

Abstract: A 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2?-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

Abstract: A crystalline form of 5(S)-(2?-hydroxyethoxy)-20(S)-camptothecin diastereoisomer of 5(RS)-(2?-hydroxyethoxy)-20(S)-camptothecin is described that is characterized by having an X-ray powder diffraction pattern comprising one or more peak intensities expressed in degrees 2? that are selected from the group consisting of 7.2±0.1, 9.4±0.1, 11.02±0.1, 12.00±0.1, 14.54±0.1, 15.2±0.1, 18.92±0.1, 21.86±0.1, 22.74±0.1 and 26.42±0.1. Methods of making and using the compound are also described.