A61P15/16

Salt of fused heterocyclic derivative and crystal thereof

The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.

METHODS FOR IMPLANTING AND REVERSING STIMULI-RESPONSIVE IMPLANTS
20180185096 · 2018-07-05 ·

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.

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.

MICROFLUIDIZED MYCOBACTERIUM AVIUM FRAGMENTS AS AN ADJUVANT AND CARRIER FOR MUCOSAL VACCINE DELIVERY
20180177869 · 2018-06-28 ·

A vaccine adjuvant and immunogenic composition may be described herein. The vaccine adjuvant may comprise cell wall fragments of the genus Mycobacterium, and more particularly, of M avium. The immunogenic composition may include the vaccine adjuvant conjugated to an antigen. For example, cell wall fragments of M. avium (herein also referred to as MAF) may be conjugated to an antigen targeting Gonadotropin releasing hormone (GnRH). The MAF-antigen conjugate may be delivered for the purposes of treatment through one of several methods, including intramuscular injection, naso-pharyngeal, or oral.

MICROFLUIDIZED MYCOBACTERIUM AVIUM FRAGMENTS AS AN ADJUVANT AND CARRIER FOR MUCOSAL VACCINE DELIVERY
20180177869 · 2018-06-28 ·

A vaccine adjuvant and immunogenic composition may be described herein. The vaccine adjuvant may comprise cell wall fragments of the genus Mycobacterium, and more particularly, of M avium. The immunogenic composition may include the vaccine adjuvant conjugated to an antigen. For example, cell wall fragments of M. avium (herein also referred to as MAF) may be conjugated to an antigen targeting Gonadotropin releasing hormone (GnRH). The MAF-antigen conjugate may be delivered for the purposes of treatment through one of several methods, including intramuscular injection, naso-pharyngeal, or oral.

NOVEL 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.

Mucoadhesive nanoparticle delivery system

The present disclosure relates generally to a mucoadhesive nanoparticle delivery system. The nanoparticles are formed from amphiphilic macromolecules conjugated to a mucosal targeting moiety in such a manner that the surface of the nanoparticle is coated with the targeting moiety. The surface density of the targeting moiety can be tuned for adjustable targeting of the nanoparticles to a mucosal site without substantially compromising the stability of the particles. The particles were found to have high loading efficiency and sustained release properties at the mucosal site. The present disclosure also relates to polymers and macromolecules useful in the preparation of the mucoadhesive nanoparticles, as well as compositions, methods, commercial packages, kits and uses related thereto.

Bromodomain inhibitors

The present invention provides for compounds of formula (I) wherein R.sup.x, X, Y, Y.sup.1, L.sup.1, A.sup.1, A.sup.2, A.sup.3, A.sup.4, A.sup.5, A.sup.6, A.sup.7, and A.sup.8, 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 comprised of one or more compounds of formula (I). ##STR00001##

N-acyl-(3-substituted)-(8-methyl)-5,6-dihydro-[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
09969745 · 2018-05-15 · ·

Novel compounds of Formula I ##STR00001##
methods of manufacturing the compounds and their use in therapeutic treatments are presented.