Patent classifications
C07C65/26
PROCESS FOR THE PREPARATION OF POLYMORPH FORM B OF TREPROSTINIL DIETHANOLAMINE SALT
The invention relates to a robust and reproducible process for the preparation of polymorph form B of treprostinil diethanolamine salt, comprising the following steps: a. treprostinil is dissolved in methanol, b. to the solution of step a) diethanolamine or its methanol solution is added, c. the reaction mixture of step b) is agitated till dissolution, d. when salt formation is completed in step c), first portion of an aprotic solvent is added to the solution, e. the solution of step d) is filtered to remove insoluble impurities, f. the filtrate of step e) is seeded with polymorph form B of treprostinil diethanolamine salt, g. to the crystal suspension obtained in step f) a second portion of the aprotic solvent is added, h. the suspension of step g) is agitated until crystallisation is completed, i. the crystals are separated, washed and dried.
PROCESS FOR THE PREPARATION OF POLYMORPH FORM B OF TREPROSTINIL DIETHANOLAMINE SALT
The invention relates to a robust and reproducible process for the preparation of polymorph form B of treprostinil diethanolamine salt, comprising the following steps: a. treprostinil is dissolved in methanol, b. to the solution of step a) diethanolamine or its methanol solution is added, c. the reaction mixture of step b) is agitated till dissolution, d. when salt formation is completed in step c), first portion of an aprotic solvent is added to the solution, e. the solution of step d) is filtered to remove insoluble impurities, f. the filtrate of step e) is seeded with polymorph form B of treprostinil diethanolamine salt, g. to the crystal suspension obtained in step f) a second portion of the aprotic solvent is added, h. the suspension of step g) is agitated until crystallisation is completed, i. the crystals are separated, washed and dried.
Onium Salt, Resist Composition, And Patterning Process
Provided is a novel onium salt used for a resist composition that has high sensitivity and excellent resolution, improved LWR and CDU, and that can inhibit collapse of a resist pattern for both of positive-type and negative-type resists in lithography: an onium salt represented by the following general formula (1),
##STR00001## wherein R.sup.ALU represents any one of a tertiary ether, tertiary carbonate, or acetal formed together with the adjacent oxygen atom and having a cyclic structure; R.sup.F represents any one of a fluorine atom, a fluorine-containing alkyl group having 1 to 6 carbon atoms, and a nitro group; R.sup.a represents a hydrocarbyl group having 1 to 20 carbon atoms; n1 represents an integer of 0 or 1; n2 and n3 represent an integer of 1 or 2; one of R.sup.F and one of OR.sup.ALU are bonded to carbon atoms adjacent to each other; n4 represents an integer of 0 to 3; and Z.sup.+ represents an onium cation.
Onium Salt, Resist Composition, And Patterning Process
Provided is a novel onium salt used for a resist composition that has high sensitivity and excellent resolution, improved LWR and CDU, and that can inhibit collapse of a resist pattern for both of positive-type and negative-type resists in lithography: an onium salt represented by the following general formula (1),
##STR00001## wherein R.sup.ALU represents any one of a tertiary ether, tertiary carbonate, or acetal formed together with the adjacent oxygen atom and having a cyclic structure; R.sup.F represents any one of a fluorine atom, a fluorine-containing alkyl group having 1 to 6 carbon atoms, and a nitro group; R.sup.a represents a hydrocarbyl group having 1 to 20 carbon atoms; n1 represents an integer of 0 or 1; n2 and n3 represent an integer of 1 or 2; one of R.sup.F and one of OR.sup.ALU are bonded to carbon atoms adjacent to each other; n4 represents an integer of 0 to 3; and Z.sup.+ represents an onium cation.
NOVEL AROMATIC MOLECULES
The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.
##STR00001##
NOVEL AROMATIC MOLECULES
The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.
##STR00001##
SESQUITERPENE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND USE THEREOF
Described herein is a sesquiterpene derivative or a pharmaceutically acceptable salt thereof, a composition for preventing, ameliorating or treating sarcopenia, including the derivative or salt thereof as an active ingredient, and the like. The sesquiterpene derivative or pharmaceutically acceptable salt thereof inhibits increases in the production and mRNA expression of a myostatin protein, which directly affects muscle loss and reduced muscle strength, and thus may exhibit a more fundamental effect of preventing or treating sarcopenia.
SESQUITERPENE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND USE THEREOF
Described herein is a sesquiterpene derivative or a pharmaceutically acceptable salt thereof, a composition for preventing, ameliorating or treating sarcopenia, including the derivative or salt thereof as an active ingredient, and the like. The sesquiterpene derivative or pharmaceutically acceptable salt thereof inhibits increases in the production and mRNA expression of a myostatin protein, which directly affects muscle loss and reduced muscle strength, and thus may exhibit a more fundamental effect of preventing or treating sarcopenia.
SMALL MOLECULE INHIBITOR AGAINST NASOPHARYNGEAL CARCINOMA, PREPARATION METHOD AND APPLICATION THEREOF
A small molecule inhibitor targeting EB virus antigen protein, and/or a pharmaceutical composition comprising same, capable of being used for treating diseases caused by EB virus infection, such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus or rheumatoid arthritis, especially nasopharyngeal carcinoma. The present disclosure further provides a small molecule inhibitor against nasopharyngeal carcinoma, and/or a pharmaceutical composition comprising same, capable of being used for treating nasopharyngeal carcinoma.
IRE-1α inhibitors
Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.