C07D417/02

Heteroaromatic compounds as BTK inhibitors

The present invention encompasses compounds of the formula (I) ##STR00001##
wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

Heteroaromatic compounds as BTK inhibitors

The present invention encompasses compounds of the formula (I) ##STR00001##
wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

HIV replication inhibiting pyrimidines

This invention concerns HIV replication inhibitors of formula ##STR00001##
the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(?O).sub.pR.sup.6, NHS(?O).sub.pR.sup.6, C(?O)R.sup.6, NHC(?O)H, C(?O)NHNH.sub.2, NHC(?O)R.sup.6, C(?NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, N?N, O, C(?O), C.sub.1-4alkanediyl, CHOH, S, S(?O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(?O)NHR.sup.13; C(?O)NR.sup.13R.sup.14; C(?O)R.sup.15; CH?NNHC(?O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(?NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

3-HYDROXY-5-(ISOXAZOL-5-YL) PYRIDINE FORMYLGLYCINE COMPOUNDS, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE

A series of 3-hydroxy-5-(isoxazol-5-yl) pyridine formylglycine compounds, a preparation method, a pharmaceutical composition, and the use. A structure of the compounds is shown as formula (I), and the compound derivatives comprise pharmaceutically acceptable salt thereof. The compounds and the pharmaceutical composition thereof have a high inhibition effect on HIF inhibition factors, and the activity can optimally reach the nano-molar concentration level, so that the compounds can be used for preparing a drug for treating fat metabolic diseases.

##STR00001##

HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS

The present invention encompasses compounds of the formula (I)

##STR00001##

wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS

The present invention encompasses compounds of the formula (I)

##STR00001##

wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

Orexin receptor antagonists

The disclosures herein relate to novel compounds of formula ##STR00001##
wherein W, X and Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.

Orexin receptor antagonists

The disclosures herein relate to novel compounds of formula ##STR00001##
wherein W, X and Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.

Estrogen receptor modulators and uses thereof

Described herein are compounds that are estrogen receptor modulators of Formula (I): ##STR00001## and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Described herein are compounds that are estrogen receptor modulators of Formula (I):

##STR00001## and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.