A61P15/16

TETRACYCLIC BROMODOMAIN INHIBITORS

The present invention provides for compounds of formula (I)

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.6, Y.sup.1, Y.sup.2, Y.sup.3, A.sup.1, A.sup.2, A.sup.3, and A.sup.4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).

TETRACYCLIC BROMODOMAIN INHIBITORS

The present invention provides for compounds of formula (I)

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.6, Y.sup.1, Y.sup.2, Y.sup.3, A.sup.1, A.sup.2, A.sup.3, and A.sup.4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).

Bicyclic bromodomain inhibitors

The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.

Bicyclic bromodomain inhibitors

The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.

NOVEL CHIRAL N-ACYL-5,6,7(8-SUBSTITUTED)-TETRAHYDRO-[1,2,4]TRIAZOLO[4,3-A]PYRAZINES AS SELECTIVE NK-3 RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN NK-3 RECEPTOR MEDIATED DISORDERS AND CHIRAL SYNTHESIS THEREOF

The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.

##STR00001##

Methods for implanting and reversing stimuli-responsive implants

Described are methods for reversible occlusion of a body lumen by way of degradation as a result of exposure to one or more stimuli such as light. The methods include administering one or more substance(s) into a body lumen of a subject and forming a stimuli-responsive polymer mass in the body lumen from the one or more substance(s). The mass is sufficient to occlude the body lumen in a manner that prevents transport of at least one material through the body lumen and is susceptible to on-command reversal in the body lumen upon exposure to one or more stimuli. The methods include administering one or more stimuli to a polymer mass in a body lumen for a time and intensity to cause the reverse the polymer mass. The methods are particular useful for applications in which it is desirable to temporarily occlude a body lumen, such as male and female contraception.

Bromodomain Inhibitors

The present invention provides for compounds of formula (I)

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.6, X.sup.1, and X.sup.2 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising compounds of formula (I).

Sustained-release lipid pre-concentrate of GNRH analogues and pharmaceutical composition comprising the same

Disclosed is a pharmaceutical composition, comprising: a) at least one sorbitan unsaturated fatty acid ester having a polar head with at least two or more OH (hydroxyl) groups; b) at least one phospholipid; c) at least one liquid crystal hardener which is free of an ionizable group and has a triacyl group with 15 to 40 carbon atoms or a carbon ring structure in a hydrophobic moiety; and d) at least one GnRH (gonadotropin-releasing hormone) analogue as a pharmacologically active substance, wherein said lipid pre-concentrate exists as a liquid phase in absence of aqueous fluid and forms into a liquid crystal in presence of aqueous fluid. The pharmaceutical composition is configured to enhance the sustained release of the pharmacologically active substance GnRH analogue.

Enzymatic process for obtaining 17 alpha-monoesters of cortexolone and/or its 9,11-dehydroderivatives
10716796 · 2020-07-21 · ·

The present invention refers to a new enzymatic process for obtaining 17-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17-propionate and 9,11-dehydro-cortexolone 17-butanoate.

BETA-AMINO HETEROCYCLIC DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES

The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV inhibitors) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.