The present invention relates to novel substituted bicyclic derivatives that can inhibit Rho-kinases and/or Rho-kinase mediated phosphorylation of myosin light chain phosphates, compositions comprising the derivatives, methods for preparing the derivatives, and methods for using the derivatives and/or compositions.

Disclosed are chemical entities which are compounds of formula (I):

##STR00001##

or pharmaceutically acceptable salts thereof; wherein Y, R.sup.a, R.sup.a′, R.sup.b, R.sup.c, X.sub.1, X.sub.2, X.sub.3, R.sup.d, Z.sub.1, and Z.sub.2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.

Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I):

##STR00001##

or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1, L.sup.2, L.sup.3, L.sup.4, M, m and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomer synthesis while maintaining overall yield and purity of a synthesized oligomer.

The invention provides compounds of the formula:

##STR00001## R.sup.1 is OR.sup.11, or NR.sup.5R.sup.5′; R.sup.2 is H or F; R.sup.5 is H, C.sub.1-C.sub.6alkyl, OH, C(═O)R.sup.6, O(C═O)R.sup.6 or O(C═O)OR.sup.6; R.sup.5′ is H or C.sub.1-C.sub.6alkyl; R.sup.6 is C.sub.1-C.sub.6or C.sub.3-C.sub.7cycloalkyl; R.sup.13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R.sup.22;

and the other variables are as defined in the claims,

which are of use in the treatment of cancer, and related aspects.

The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.

The present invention covers aminoquinolone compounds of general formula (I): in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, X and n are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase alpha regulated disorders, as a sole agent or in combination with other active ingredients.

##STR00001##

Disclosed herein are therapeutic compounds capable of targeting abroad range of tumor cells. The present disclosure is further directed to compositions comprising the therapeutic compounds, methods of manufacturing the therapeutic compounds, and methods of treating cancer comprising administering the therapeutic compounds.