A compound of formula (Ic)

##STR00001## wherein X.sup.2 represents a —CO—NR.sub.k— group, wherein R.sub.k represents a hydrogen atom or a methyl group, a —NH—CO—NH— group, a —OCH.sub.2— group, a —CH(OH)— group, a —NH—CO— group, a —O— group, a —O—(CH.sub.2).sub.s—O—, a —CO— group, a —SO.sub.2— group, a divalent 5-membered heteroaromatic ring comprising 1, 2, 3 or 4 heteroatoms, —a NH—SO.sub.2— or a —SO.sub.2—NH— group; Y.sup.2 represents a hydrogen atom, a halogen atom, a hydroxyl group, a (C.sub.1-C.sub.4)alkoxy group, a

##STR00002##

a

##STR00003##

group, a

##STR00004##

group, a morpholinyl group, optionally substituted by a (C.sub.1-C.sub.4)alkyl group, a piperazinyl group, a piperidinyl group, or a —CR.sup.1R.sup.2R.sup.3 group, or any of its pharmaceutically acceptable salt.

This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I)

##STR00001##

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.3, R.sup.3a, R.sup.4, R.sup.6, R.sup.7, R.sup.8, A, Z, X.sup.1 and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

The present disclosure provides carboxamides and sulfonamides having Formula (I); and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

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The present disclosure provides carboxamides and sulfonamides having Formula (I); and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

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The disclosure provides compounds and method useful for modulating gp130 biological activity. The disclosure also provides methods and compositions for treating disease and disorders associated with gp130 activity, particularly those associated with inflammation.

Disclosed is a compound as shown in formula (I) or a pharmaceutically acceptable salt, a stereoisomer, an isotope derivative or a prodrug thereof. The compound has an excellent activity as a cyclin-dependent kinase 9 (CDK9) inhibitor for treating hyperproliferative diseases. The experimental research on in vitro inhibition of cell proliferation and in vivo suppression of tumors shows that such compounds have a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and have a good selectivity and a low toxicity and few side effects, thereby possessing a good clinical value as novel anti-tumor drugs.

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Disclosed is a compound as shown in formula (I) or a pharmaceutically acceptable salt, a stereoisomer, an isotope derivative or a prodrug thereof. The compound has an excellent activity as a cyclin-dependent kinase 9 (CDK9) inhibitor for treating hyperproliferative diseases. The experimental research on in vitro inhibition of cell proliferation and in vivo suppression of tumors shows that such compounds have a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and have a good selectivity and a low toxicity and few side effects, thereby possessing a good clinical value as novel anti-tumor drugs.

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An object of the present invention is to provide a compound having a PDGF receptor kinase inhibitory activity.

Examples of the present invention may include, for example, a compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof.

##STR00001##

The compound of the present invention has an inhibitory activity against the PDGF receptor kinase. In addition, since the compound of the present invention has an inhibitory activity against the PDGF receptor kinase, it is useful as a therapeutic agent for respiratory diseases, cancers, smooth muscle proliferative diseases, vasoproliferative diseases, autoimmune/inflammatory diseases, metabolic diseases, vasoocclusive diseases, and the like.