C07D403/00

Substituted 2-azabicycles and their use as orexin receptor modulators

The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.

Substituted piperidine compounds and their use as orexin receptor modulators

The present invention is directed to compounds of Formula I: wherein X is CR.sub.1 or N; Y is CR.sub.2 or N; Z is NH or O; R.sub.1 is alkoxy, triazolyl, oxazolyl, isoxazolyl, oxadiazolyl, or pyrimidinyl; R.sub.2 is H, alkyl, or halo; R.sub.3 is H, alkyl, alkoxy, halo, triazolyl, oxazolyl, or pyrimidinyl; R.sub.4 is alkyl; R.sub.5 is pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl; wherein the pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl is optionally substituted with one or two substituents independently selected from the group consisting of alkyl, halo, or phenyl; and R.sub.6 is H or alkyl. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods using the compounds of the invention are also within the scope of the invention. ##STR00001##

2,4-pyrimidinediamine compounds and uses as anti-proliferative agents

The present invention provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferative diseases such as tumorigenic cancers.

4-aminoquinazolinyl-2-yl-1-pyrazole-4-carboxylic acid compounds as prolyl hydroxylase inhibitors

Aminoquinazolinyl compounds of formula (I) are described, ##STR00001##
which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.

Hole transport compositions and related devices and methods (I)

A composition comprising: at least one compound comprising a hole transporting core, wherein the core is covalently bonded to a first arylamine group and also covalently bonded to a second arylamine group different from the first, and wherein the compound is covalently bonded to at least one intractability group, wherein the intractability group is covalently bonded to the hole transporting core, the first arylamine group, the second arylamine group, or a combination thereof, and wherein the compound has a molecular weight of about 5,000 g/mole or less. Blended mixtures of arylamine compounds, including fluorene core compounds, can provide good film formation and stability when coated onto hole injection layers. Solution processing of OLEDs is a particularly important application.

Hole transport compositions and related devices and methods (I)

A composition comprising: at least one compound comprising a hole transporting core, wherein the core is covalently bonded to a first arylamine group and also covalently bonded to a second arylamine group different from the first, and wherein the compound is covalently bonded to at least one intractability group, wherein the intractability group is covalently bonded to the hole transporting core, the first arylamine group, the second arylamine group, or a combination thereof, and wherein the compound has a molecular weight of about 5,000 g/mole or less. Blended mixtures of arylamine compounds, including fluorene core compounds, can provide good film formation and stability when coated onto hole injection layers. Solution processing of OLEDs is a particularly important application.

Compound as WNT signaling inhibitor, composition, and use thereof
09556144 · 2017-01-31 · ·

The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways. ##STR00001##

Compound and labeled biological substance using the same

A compound of Formula (1) and a labeled biological substance having the compound. ##STR00001## Z.sup.1 and Z.sup.2 represent a specific 6-membered ring, and at least one of Z.sup.1 or Z.sup.2 is a benzene ring having a specific substituent at an ortho position with respect to a nitrogen atom to which L.sup.1 or L.sup.2 is bonded, or a specific nitrogen-containing 6-membered ring in which a ring-constituting atom located at the ortho position is a nitrogen atom. The compound has at least one structure represented by (CH.sub.2CH.sub.2O).sub.mR.sup.21 on a heterocyclic ring, and has at least one substituent capable of being bonded to a carboxy group or a biological substance at a specific position, and in a case where at least one of Z.sup.1 or Z.sup.2 is the specific nitrogen-containing 6-membered ring, the specific substituents may be bonded to each other to form a ring.