C07D295/10

Polymerization initiator and radically polymerizable composition containing same

Provided is an -aminoalkylphenone compound that has good stability and low sublimability, efficiently generates radicals when irradiated with a bright line at 365 nm (I line) or the like, and is useful as a polymerization initiator to be used in a radically polymerizable composition. The -aminoalkylphenone compound is represented by Formula (I) mentioned below. ##STR00001##
In Formula (I) mentioned above, it is preferable that R.sup.11 is a nitro group, an alkoxy group having 1 to 12 carbon atoms, or an alkoxycarbonyl group having 1 to 12 carbon atoms. The -aminoalkylphenone compound can be preferably used in a polymerization initiator.

INHIBITORS OF KRAS G12C MUTANT PROTEINS
20180141927 · 2018-05-24 ·

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):

##STR00001##

or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, G.sup.1, G.sup.2, L, m.sup.1, m.sup.2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

INHIBITORS OF KRAS G12C MUTANT PROTEINS
20180141927 · 2018-05-24 ·

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):

##STR00001##

or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, G.sup.1, G.sup.2, L, m.sup.1, m.sup.2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula I:

##STR00001##

where R.sup.1-R.sup.6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Benzamide derivatives useful in the treatment of muscular disorders and pain and for controlling spasticity and tremors
09908843 · 2018-03-06 · ·

The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein: n is 0 or 1; R1 is selected from H, alkyl and aralkyl, wherein said alkyl and aralkyl groups may be optionally substituted by one or more OH groups; X is a group selected from CC(CH.sub.2).sub.p; C(R.sup.5)C(R.sup.6)(CH.sub.2).sub.q; and C(R.sup.5)(R.sup.6)C(R.sup.7)(R.sup.8)(CH.sup.2)r-; where each of R.sup.5, R.sup.6, R.sup.7 and R.sup.8 is independently H or alkyl, and each of p, q and r is independently 1, 2, 3, 4 or 5; Y is a group selected from: CN; COOR.sup.2; CONR.sup.3R.sup.4; SO.sub.2NR.sup.9R.sup.10; NR.sup.12COR.sup.13; NR.sup.14SO.sub.2R.sup.15; and a heterocyclic group selected from oxadiazolyl, thiazolyl, iso-thiazolyl, oxazolyl, iso-oxazolyl, pyrazolyl and imidazolyl; where each of R.sup.2, R.sup.3 and R.sup.4 is independently H or alkyl; or R.sup.3 and R.sup.4 are linked, together with the nitrogen to which they are attached, to form a 5 or 6-membered heterocycloalkyl or heterocycloalkenyl group, said heterocycloalkyl or heterocycloalkenyl group optionally containing one or more further groups selected from O, N, CO and S, and where each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 is independently H or alkyl. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, pain, or for controlling spasticity or tremors, for example, spasticity in MS. ##STR00001##

Benzamide derivatives useful in the treatment of muscular disorders and pain and for controlling spasticity and tremors
09908843 · 2018-03-06 · ·

The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein: n is 0 or 1; R1 is selected from H, alkyl and aralkyl, wherein said alkyl and aralkyl groups may be optionally substituted by one or more OH groups; X is a group selected from CC(CH.sub.2).sub.p; C(R.sup.5)C(R.sup.6)(CH.sub.2).sub.q; and C(R.sup.5)(R.sup.6)C(R.sup.7)(R.sup.8)(CH.sup.2)r-; where each of R.sup.5, R.sup.6, R.sup.7 and R.sup.8 is independently H or alkyl, and each of p, q and r is independently 1, 2, 3, 4 or 5; Y is a group selected from: CN; COOR.sup.2; CONR.sup.3R.sup.4; SO.sub.2NR.sup.9R.sup.10; NR.sup.12COR.sup.13; NR.sup.14SO.sub.2R.sup.15; and a heterocyclic group selected from oxadiazolyl, thiazolyl, iso-thiazolyl, oxazolyl, iso-oxazolyl, pyrazolyl and imidazolyl; where each of R.sup.2, R.sup.3 and R.sup.4 is independently H or alkyl; or R.sup.3 and R.sup.4 are linked, together with the nitrogen to which they are attached, to form a 5 or 6-membered heterocycloalkyl or heterocycloalkenyl group, said heterocycloalkyl or heterocycloalkenyl group optionally containing one or more further groups selected from O, N, CO and S, and where each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14 and R.sup.15 is independently H or alkyl. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, pain, or for controlling spasticity or tremors, for example, spasticity in MS. ##STR00001##

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula:

##STR00001##

where R.sup.1-R.sup.6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula:

##STR00001##

where R.sup.1-R.sup.6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Inhibitors of KRAS G12C mutant proteins
09862701 · 2018-01-09 · ·

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): ##STR00001##
or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, G.sup.1, G.sup.2, L, m.sup.1, m.sup.2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Inhibitors of KRAS G12C mutant proteins
09862701 · 2018-01-09 · ·

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): ##STR00001##
or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, G.sup.1, G.sup.2, L, m.sup.1, m.sup.2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.