This disclosure relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.

The disclosure is directed to compounds of Formula (I) and Formula (II), Formula (I) and Formula (II) and pharmaceutically acceptable salts or solvates thereof. Pharmaceutical compositions comprising compounds of Formula (I) or Formula (II), as well as methods of their use and preparation, are also described.

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There are disclosed compounds of the following formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating inflammatory and autoimmune diseases or disorders.

##STR00001##

There are disclosed compounds of the following formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating inflammatory and autoimmune diseases or disorders.

##STR00001##

The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.

The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.

HIV replication inhibitors of formula ##STR00001##
N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a.sup.1=a.sup.2-a.sup.3=a.sup.4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b.sup.1=b.sup.2-b.sup.3=b.sup.4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0, 1, 2, 3 and in certain cases also 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; optionally substituted C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; R.sup.2 is OH; halo; optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O).sub.pR.sup.6; C(═NH)R.sup.6; R.sup.2a is CN; amino; substituted amino; optionally substituted C.sub.1-6alkyl; halo; optionally substituted C.sub.1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R.sup.16; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; —C(═N—O—R.sup.8)—C.sub.1-4alkyl; R.sup.7 or —X—R.sup.7; R.sup.3 is CN; amino; C.sub.1-6alkyl; halo; optionally substituted C.sub.1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; —C(═N—O—R.sup.8)—C.sub.1-4alkyl; R.sup.7; —X—R.sup.7; R.sup.4 is halo; OH; optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; C.sub.3-7cycloalkyl; C.sub.1-6alkyloxy; CN; nitro; polyhaloC.sub.1-6alkyl; polyhaloC.sub.1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C.sub.1-4alkyl)amino or R.sup.7; -A-B— is —CR.sup.5═N—, —N═N—, —CH.sub.2—CH.sub.2—, —CS—NH—, —CO—NH—, —CH═CH—;
pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.

HIV replication inhibitors of formula ##STR00001##
N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a.sup.1=a.sup.2-a.sup.3=a.sup.4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b.sup.1=b.sup.2-b.sup.3=b.sup.4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0, 1, 2, 3 and in certain cases also 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; optionally substituted C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; R.sup.2 is OH; halo; optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O).sub.pR.sup.6; C(═NH)R.sup.6; R.sup.2a is CN; amino; substituted amino; optionally substituted C.sub.1-6alkyl; halo; optionally substituted C.sub.1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R.sup.16; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; —C(═N—O—R.sup.8)—C.sub.1-4alkyl; R.sup.7 or —X—R.sup.7; R.sup.3 is CN; amino; C.sub.1-6alkyl; halo; optionally substituted C.sub.1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl or C.sub.2-6alkynyl; —C(═N—O—R.sup.8)—C.sub.1-4alkyl; R.sup.7; —X—R.sup.7; R.sup.4 is halo; OH; optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl or C.sub.2-6alkynyl; C.sub.3-7cycloalkyl; C.sub.1-6alkyloxy; CN; nitro; polyhaloC.sub.1-6alkyl; polyhaloC.sub.1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C.sub.1-4alkyl)amino or R.sup.7; -A-B— is —CR.sup.5═N—, —N═N—, —CH.sub.2—CH.sub.2—, —CS—NH—, —CO—NH—, —CH═CH—;
pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.

Provided herein are compounds of formula (I-A), (I-B), (I-C), or (I-D), pharmaceutical compositions comprising the compounds, and methods of use thereof. The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including diseases and conditions associated with PI3 kinase activity. ##STR00001##

Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use.

##STR00001##