The present disclosure relates to concise processes for making (−)-picrotoxinin (1, PXN) and 5-methyl-picrotoxinin (20, 5MePXN), and to 5MePXN, its pharmaceutical compositions, and its method of use for inhibiting GABA.sub.A receptor.

The present disclosure relates to concise processes for making (−)-picrotoxinin (1, PXN) and 5-methyl-picrotoxinin (20, 5MePXN), and to 5MePXN, its pharmaceutical compositions, and its method of use for inhibiting GABA.sub.A receptor.

A resist composition containing: (A) a resin containing a repeating unit having an acid-labile group and not containing a repeating unit having an aromatic substituent; (B) a photo-acid generator shown by a general formula (B-1); and (C) a solvent, where W.sub.1 represents a cyclic divalent hydrocarbon group having 4 to 12 carbon atoms and containing a heteroatom; W.sub.2 represents a cyclic monovalent hydrocarbon group having 4 to 14 carbon atoms and not containing a heteroatom; Rf represents a divalent organic group shown by the following general formula; and M.sup.+ represents an onium cation. This provides a resist composition and a patterning process that uses the resist composition that show a particularly favorable mask dimension dependency (mask error factor: MEF), LWR, and critical dimension uniformity (CDU) particularly in photolithography where a high-energy beam such as an ArF excimer laser beam is used as a light source. ##STR00001##

A resist composition containing: (A) a resin containing a repeating unit having an acid-labile group and not containing a repeating unit having an aromatic substituent; (B) a photo-acid generator shown by a general formula (B-1); and (C) a solvent, where W.sub.1 represents a cyclic divalent hydrocarbon group having 4 to 12 carbon atoms and containing a heteroatom; W.sub.2 represents a cyclic monovalent hydrocarbon group having 4 to 14 carbon atoms and not containing a heteroatom; Rf represents a divalent organic group shown by the following general formula; and M.sup.+ represents an onium cation. This provides a resist composition and a patterning process that uses the resist composition that show a particularly favorable mask dimension dependency (mask error factor: MEF), LWR, and critical dimension uniformity (CDU) particularly in photolithography where a high-energy beam such as an ArF excimer laser beam is used as a light source. ##STR00001##

The invention provides compounds, methods, pharmaceutical compositions, and kits for the treatment of proliferative disorders such as cancer. In one aspect, the methods comprise compounds that inhibit the activity of protein kinases, such as cell division cycle (Cdc) kinase. In another aspect, the methods comprise compounds that inhibit Cdc7 and/or Dbf4 activity. In another aspect, the methods comprise compounds that exhibit anti-proliferative properties useful in treating diseases such as cancer. Compounds useful for any of the methods include compounds of the Formula (A) or (B):

##STR00001##

or pharmaceutically acceptable salts thereof. Exemplary compounds of Formula (A) or (B) include granaticin A, granaticin B, dihydrogranaticin A, dihydrogranaticin B, medermycin, and actinorhodin.

The invention provides compounds, methods, pharmaceutical compositions, and kits for the treatment of proliferative disorders such as cancer. In one aspect, the methods comprise compounds that inhibit the activity of protein kinases, such as cell division cycle (Cdc) kinase. In another aspect, the methods comprise compounds that inhibit Cdc7 and/or Dbf4 activity. In another aspect, the methods comprise compounds that exhibit anti-proliferative properties useful in treating diseases such as cancer. Compounds useful for any of the methods include compounds of the Formula (A) or (B):

##STR00001##

or pharmaceutically acceptable salts thereof. Exemplary compounds of Formula (A) or (B) include granaticin A, granaticin B, dihydrogranaticin A, dihydrogranaticin B, medermycin, and actinorhodin.

The invention is directed to a process for the continuous preparation of a cycloadduct product from the reaction of a furanic with a dienophile, comprising heating a first liquid feed stream comprising the dienophile and a solvent in which the dienophile is dissolved; providing a second liquid feed stream comprising the furanic; leading the first liquid feed stream and the second liquid feed stream into a continuous reactor to produce a product solution stream comprising the cycloadduct product; and leading the product solution stream to an product isolation zone to produce an isolated cycloadduct product. A further aspect of the invention is an apparatus for carrying out this reaction.

The invention is directed to a process for the continuous preparation of a cycloadduct product from the reaction of a furanic with a dienophile, comprising heating a first liquid feed stream comprising the dienophile and a solvent in which the dienophile is dissolved; providing a second liquid feed stream comprising the furanic; leading the first liquid feed stream and the second liquid feed stream into a continuous reactor to produce a product solution stream comprising the cycloadduct product; and leading the product solution stream to an product isolation zone to produce an isolated cycloadduct product. A further aspect of the invention is an apparatus for carrying out this reaction.

Disclosed are topical compositions and methods of treatment of skin disorders selected from Molluscum contagiosum, verrucae and warts by topical administration to a subject in need thereof of a composition comprising between about 0.5%-1.0% w/w high-purity cantharidin. Also disclosed are processes for preparation of high-purity cantharidin.

Disclosed are topical compositions and methods of treatment of skin disorders selected from Molluscum contagiosum, verrucae and warts by topical administration to a subject in need thereof of a composition comprising between about 0.5%-1.0% w/w high-purity cantharidin. Also disclosed are processes for preparation of high-purity cantharidin.