C07D237/28

Inhibitors of tryptophan-2,3-dioxygenase or indoleamine-2,3-dioxygenase

Provided is a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises formula (I) wherein X.sup.1, X.sup.2, and X.sup.7, may be the same or different and each is independently selected from C and N; X.sup.3, X.sup.4, X.sup.5, and X.sup.6 may be the same or different and each is independently selected from C, N, O and S wherein when X.sup.3 is N it has a double bond and wherein when X.sup.6 is N it has a double bond; the dotted line is a bond which may be present or absent; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.6 comprises a group Y; and provided that the number of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 groups present is such that the respective valencies of X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, and X.sup.7 are maintained; and wherein Y is a group having a formula selected from (II), (III), (IV), (V) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group, and R.sup.31 and R.sup.32 may be the same or different and are selected from H and a substituted or unsubstituted organic group, X.sup.8 is selected from C and N, and each R.sup.313 may be the same or different and is selected from H and a substituted or unsubstituted organic group. ##STR00001##

Pyridazine derivatives as RORc modulators

Compounds of formula I: ##STR00001##
or pharmaceutical salts thereof, wherein m, A, X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Pyridazine derivatives as RORc modulators

Compounds of formula I: ##STR00001##
or pharmaceutical salts thereof, wherein m, A, X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

NEAR-INFRARED-ABSORBING DYE, OPTICAL FILTER, AND IMAGING DEVICE

Provided is a near-infrared-absorbing dye increasing a visible light transmittance and having a near-infrared blocking characteristic. The near-infrared-absorbing dye has an absorption characteristic measured by dissolving the dye in dichloromethane satisfying the following requirements. In an absorption spectrum at a wavelength of 400 to 800 nm, there is a maximum absorption wavelength .sub.max in a wavelength region of 670 nm or more. The following relational expression is established between a maximum absorption constant .sub.A with respect to light with a wavelength of 430 to 550 nm and a maximum absorption constant .sub.B with respect to light with a wavelength of 670 nm or more, where .sub.B/.sub.A65. In a spectral transmittance curve, an average transmittance of light with a wavelength of 430 to 460 nm is 94.0% or more when a transmittance at the maximum absorption wavelength .sub.max is set to 1%.

CARBOXY SUBSTITUTED (HETERO) AROMATIC RING DERIVATIVES AND PREPARATION METHOD AND USES THEREOF

Carboxy-substituted (hetero)aryl derivatives, pharmaceutical compositions comprising these compounds, and methods of preparing such compounds and compositions are provided. The compounds or compositions are useful in inhibiting xanthine oxidase and urate anion transporter 1, and also can be used in the treatment or prevention of diseases associated with high blood uric acid level in mammals, especially humans.

KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Pyridazine derivatives as RORc modulators

Compounds of formula I: ##STR00001##
or pharmaceutical salts thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Pyridazine derivatives as RORc modulators

Compounds of the formula I: ##STR00001##
or a pharmaceutical salt thereof,
wherein X, Ar.sup.1, R1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Pyridazine derivatives as RORc modulators

Compounds of the formula I: ##STR00001##
or a pharmaceutical salt thereof,
wherein X, Ar.sup.1, R1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.