Patent classifications
A61P29/02
COMPOUNDS, COMPOSITIONS AND METHODS
The disclosed subject matter provides certain polymorphic forms of Compound (I) as well as pharmaceutical compositions comprising Compound (I) or such polymorphic forms, and methods of using or making such compounds and pharmaceutical compositions. It has now been discovered that Compound (I) can exist in multiple crystalline forms (polymorphs). One particular crystalline form, Form II, has been found to be more thermodynamically stable and, thus, likely more suitable for bulk preparation and handling than other polymorphic forms. Efficient and economic methods have been developed to prepare Compound (I) and Form II in high purity on a large scale. In animal studies, Form II has demonstrated safety and efficacy in treating depressive disorders and, when micronized, improved absorption compared to non-micronized Form II.
##STR00001##
NOVEL COMPOUNDS
The invention is directed to compounds of formula (I):
##STR00001##
and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.
TRPA1 ANTAGONIST FOR THE TREATMENT OF PAIN ASSOCIATED TO DIABETIC NEUROPATHIC PAIN
The present patent application relates to a transient receptor potential ankyrin-1 (TRPA1) antagonist for the treatment of neuropathic pain in a subject. Particularly, the present patent application relates to a method of treating neuropathic pain in a subject in need thereof by orally administering to the subject a thienopyrimidinedione Compound as a TRPA1 antagonist. The present invention also relates to a pharmaceutical composition comprising the TRPA1 antagonist, and a process for preparing such a pharmaceutical composition.
TRPA1 ANTAGONIST FOR THE TREATMENT OF PAIN ASSOCIATED TO DIABETIC NEUROPATHIC PAIN
The present patent application relates to a transient receptor potential ankyrin-1 (TRPA1) antagonist for the treatment of neuropathic pain in a subject. Particularly, the present patent application relates to a method of treating neuropathic pain in a subject in need thereof by orally administering to the subject a thienopyrimidinedione Compound as a TRPA1 antagonist. The present invention also relates to a pharmaceutical composition comprising the TRPA1 antagonist, and a process for preparing such a pharmaceutical composition.
Transdermal Administration Of Fentanyl And Analogs Thereof
A method and a non-rate controlled, monolithic, subsaturated patch for transdermally administering fentanyl and analogs thereof, for analgetic purposes, to a subject through skin over an extended period of time are disclosed.
Pyridine derivatives
The invention relates to a compound of formula (I) ##STR00001##
wherein A and R.sup.1 to R.sup.4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
Polidocanol for use as immunomodulating agent
The present invention relates to the use of diluted, thus non-sclerosing, polidocanol solutions as immunomodulating and anti-inflammatory agents. The inventions further relates to non-sclerosing compositions 5 comprising polidocanol in concentration of from 0.03 to 0.10% w/V for the treatment of psoriatic skin rashes, for cosmetic use and for the reduction of peripheral venous stasis.
Polidocanol for use as immunomodulating agent
The present invention relates to the use of diluted, thus non-sclerosing, polidocanol solutions as immunomodulating and anti-inflammatory agents. The inventions further relates to non-sclerosing compositions 5 comprising polidocanol in concentration of from 0.03 to 0.10% w/V for the treatment of psoriatic skin rashes, for cosmetic use and for the reduction of peripheral venous stasis.
S-alkylisothiouronium derivatives for treating uterine hypercontractility disorders
The present invention relates to methods for treating uterine hypercontractility disorders. in particular, the present invention relates to methods for treating abnormal uterine bleeding and dysmenorrhea comprising administering to women suffering from such disorders a pharmaceutical composition comprising an S-alkylisothiouronium derivative.
S-alkylisothiouronium derivatives for treating uterine hypercontractility disorders
The present invention relates to methods for treating uterine hypercontractility disorders. in particular, the present invention relates to methods for treating abnormal uterine bleeding and dysmenorrhea comprising administering to women suffering from such disorders a pharmaceutical composition comprising an S-alkylisothiouronium derivative.