C07C233/87

PPAR agonists

Provided herein are compounds and compositions useful in increasing PPAR activity. The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

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##

Mitochondrial Aldehyde Dehydrogenase-2 Modulators and Methods of Use Thereof
20170320828 · 2017-11-09 ·

The present disclosure provides compounds of formula (I) that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds.

Mitochondrial Aldehyde Dehydrogenase-2 Modulators and Methods of Use Thereof
20170320828 · 2017-11-09 ·

The present disclosure provides compounds of formula (I) that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds.

Mitochondrial aldehyde dehyrogenase-2 modulators and methods of use thereof

The present disclosure provides compounds of formula (I) that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds. ##STR00001##

Mitochondrial aldehyde dehyrogenase-2 modulators and methods of use thereof

The present disclosure provides compounds of formula (I) that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity, and methods of preparing these compounds. ##STR00001##

Substituted aminobutyric derivatives as neprilysin inhibitors

The present invention provides a compound of formula I; ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Substituted aminobutyric derivatives as neprilysin inhibitors

The present invention provides a compound of formula I; ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

ALPHA 4 BETA 7 INTEGRIN MODULATORS AND USES THEREOF

The present disclosure provides small molecule compounds and pharmaceutical compositions for the modulation of alpha 4 beta 7 integrin, useful for the treatment of inflammatory conditions such as inflammatory bowel disease, including ulcerative colitis and Crohn's disease.