C07D217/24

Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds

Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.

MICROBIOCIDAL HETEROBICYCLIC DERIVATIVES

Intermediates for compounds of the formula (I):

##STR00001##

Dual mechanism inhibitors for the treatment of disease

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.

Dual mechanism inhibitors for the treatment of disease

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.

A CATALYST BOUND ALPHA RADICAL AND SYNTHESIS OF OXO COMPOUNDS USING THE SAME
20210147364 · 2021-05-20 ·

The present invention discloses in situ generated catalyst bound alpha radical compound represented by formula (I) or (II) and a single pot process for the preparation of oxo compounds by using in situ generated catalyst bound alpha radical compound of formula (I) or (II).

A CATALYST BOUND ALPHA RADICAL AND SYNTHESIS OF OXO COMPOUNDS USING THE SAME
20210147364 · 2021-05-20 ·

The present invention discloses in situ generated catalyst bound alpha radical compound represented by formula (I) or (II) and a single pot process for the preparation of oxo compounds by using in situ generated catalyst bound alpha radical compound of formula (I) or (II).

Alpha,Beta-UNSATURATED AMIDE COMPOUND

An object of the present invention is to provide an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The α,β-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like:

##STR00001##

[wherein, “A” represents optionally substituted heterocyclic diyl, R.sup.1 represents hydrogen atom or optionally substituted lower alkyl, R.sup.2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO.sub.2—, —NR.sup.X1— (wherein, R.sup.X1 represents hydrogen atom or lower alkyl), —CHR.sup.X2— (wherein, R.sup.X2 represents hydrogen atom or hydroxy), —CH═CH—, −CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

Hydantoin containing deoxyuridine triphosphatase inhibitors

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

DERIVATIVES OF PAPAVERINE THAT ARE EFFECTIVE HYPOXIC TUMOR RADIOSENSITIZERS

Disclosed herein are compounds, compositions, and methods for inhibiting mitochondrial oxygen consumption in a cancerous tissue. The compounds, compositions, and methods can be used to treat a subject with hypoxic cancerous tissue.

DERIVATIVES OF PAPAVERINE THAT ARE EFFECTIVE HYPOXIC TUMOR RADIOSENSITIZERS

Disclosed herein are compounds, compositions, and methods for inhibiting mitochondrial oxygen consumption in a cancerous tissue. The compounds, compositions, and methods can be used to treat a subject with hypoxic cancerous tissue.