Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis

Inhibitors of akt activity

Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease.

Compounds and methods for kinase modulation, and indications therefor

4-Tetrazolyl-4-phenylpiperidine Compounds, compositions comprising an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound, methods for treating or preventing pain or diarrhea in an animal comprising administering to an animal in need thereof an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound are disclosed.

Therapeutic agents useful for treating pain

The invention relates to compounds of formula (I), wherein Z, R1-8, n, A1, X1 and X2 have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.

Dpp-IV Inhibitors

The present invention relates to compounds of formula (I) wherein Q, Z, R1 , R2 , and R3 are as described in claim 1 useful as inhibitors of protein kinases, particularly of JAK family and ROCK family 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.

Pyrrolopyridines useful as inhibitors of protein kinase

The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Akt protein kinase inhibitors

CD71-mediated Liposomal Arsenic-nickel Complex Combined with All-trans Retinoic Acid for the efficacy of Acute Promyelocytic Leukemia

A small molecule chaperone for alpha-1 antitrypsin deficiency-associated liver disease reduces liver polymer burden in the PiZ mouse model

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Akt protein kinase inhibitors

CD71-mediated Liposomal Arsenic-nickel Complex Combined with All-trans Retinoic Acid for the efficacy of Acute Promyelocytic Leukemia

A small molecule chaperone for alpha-1 antitrypsin deficiency-associated liver disease reduces liver polymer burden in the PiZ mouse model