The present invention relates to imidazo[1,2-a]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Tyrosine kinase inhibitors

Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Compounds and compositions for delivering active agents

A hair dye composition containing a triazene dissociative direct dye represented by general formula (1): A-N=N-NH-B (1) wherein A and B are each a monocyclic or a bicyclic aromatic heterocyclic group that may have a substituent or a monocyclic or a bicyclic aryl group that may have a substituent and contain none of a carboxy group, a sulfo group and a quaternary ammonium group; and A and B each bind to a triazene-1,3-diyl group represented by -N=N-NH- via a carbon atom within A and B each. A and B may be the same or different.

Hair-dye composition

The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

Inhibitors of 11-beta-hydroxy steroid dehydrogenase type i

Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Compounds for the treatment of metabolic disorders

NEW MATERIAL:A phenylacetic acid derivative of formula I (R 1 and R 2 are H or lower alkyl; M is carboxyl, carbamoyl, hydroxyaminocarbonyl or lower alkoxycarbonyl; A and B are H, lower alkyl or aryl). EXAMPLE: 3-(Thiazol-2-yl)-2-hydroxyphenylacetic acid. USE: Useful as a medicine having analgesic, anti-inflammatory, antipyretic, antithrombotic and antiallergic action, etc. with high safety. PROCESS: A compound of formula II is allylated in the presence of a base in a solvent, e.g. acetone, to give a compound of formula III, which is then subjected to the Claisen rearrangement under heating at 100W300°C. The reaction product is then alkylated with an alkyl halide in the presence of a base to afford a compound of formula IV, which is then oxidized in a mixed solvent of water with acetic acid in the presence of an oxidizing agent to give the compound of formula I . COPYRIGHT: (C)1984,JPO&Japio

Novel phenylacetic acid derivative

PURPOSE: To obtain the new derivative useful as a medicine having inhibiting actions on a serine protease, especially the inhibiting actions on an elastase. CONSTITUTION: This compound is expressed by formula I [R 1 and R 2 are each p-pivaloyloxyphenyl, H, a halogen, an alkyl, a substitutive phenyl, a substitutive benzyl or CH 2 COOR 5 (R 5 is H, an alkyl or a substitutive benzyl), with the proviso that at least one is p-pivaloyloxyphenyl; R 3 and R 4 are each H, an alkyl, an (halo)alkylsulfonyl, a substitutive phenylsulfonyl, amidino, CO-R 6 {R 6 is an alkyl, a substitutive phenyl, (CH 2 ) m -COOH [(m) is 1-5], (CH 2 ) n -NHR 7 [(n) is 1-5; R 7 is H, tert-butoxycarbonyl, etc.] or (CH 2 )Q-R 8 (Q is 0-5; R 8 is an alkoxy, phenyl, etc.}], e.g. 2-(2-methoxyphenyl)amino-5-methyl-4-(4-pivaloyloxyphenyl) thiazole. The compound is obtained by reacting a compound expressed by formula II with a compound expressed by formula III. COPYRIGHT: (C)1995,JPO

New 2-aminothiazole derivative

NEW MATERIAL:A compound shown by formula I [X and Y are H, halogen or lower alkoxy; n is 0-7; R1 is H or acyl; R2 is long-chain alkyl, cycloalkyl, lower alkoxy, (substituted)phenoxy, heterocyclic group or cyclic amino] and an acid addition salt thereof useful as a drug. EXAMPLE:4,5-Diphenyl-2-(2'-morpholinoethyl)aminothiazole. USE:A drug useful as an excellent anti-inflammatory drug, analgesic, antipyretic, antirheumatic. A dose is about 1-300mg calculated as an active ingredient daily and preferably administered dividedly once-three times daily. PREPARATION:A compound shown by formula II (HI is halogen) is reacted with a compound shown by formula III in an organic solvent such as ethanol at 20-120 deg.C for 1-48hr to give a compound shown by formula I.

Novel substituted diphenylthizole derivative

PURPOSE:To provide a dermatic external preparation, esp. skin whitening cosmetic or skin aging preventive, excellent in skin whitening effect and high in safety, containing, as active ingredient, specific compound(s) having tyrosinase activity inhibitory effect. CONSTITUTION:The objective dermatic external preparation having the above- mentioned advantages, formulated with 0.001-20 (pref. 0.001-5)wt.%, as tyrosinase activity inhibitor, of at least one kind of compound selected from (A) heterocyclic compounds (pref. benzoxazole derivatives, thiourea derivatives, 2- arylimino-1,3-dithiolane derivatives, thiazolidinone derivatives, sulfur-contg. lactam derivatives, 2-mercapto-4-oxopyrimidine derivatives, or 2- mercaptoquinoline derivatives), (B) di-t-butyl-4-hydroxyphenyl derivatives (pref. chalcone derivatives or 3,5-di-t-butyl-4-hydroxystyrene derivatives), and (C) cinnamic acid derivatives.

Tyrosinase inhibitor and dermatic external preparation using the same

NEW MATERIAL:A compound expressed by formulaI[R 1 is H or lower alkyl; R 2 is cycloalkyl or group of formula IV (X is OH or lower alkoxyl; n is an integer 1W3)]. EXAMPLE: trans-4-(trans-4-n-Pentylcyclohexylcarbonylaminomethyl)cyclohexanecar- boxylic acid. USE: A remedy and preventing agent for allergic diseases, e.g. nephritis, rheumatism, collagen disease or autoimmune disease, having antiplasminic, antitumor and antithrombotic actions, and useful as a medicine. PROCESS: A compound expressed by formula II is reacted with an equimolar amount or slight excess of a reactive derivative of a compound expressed by formula III, e.g. acid chloride or anhydride, in a solvent e.g. water or methanol, and if necessary in the presence of a dehydrating agent or deacidifying agent at room temperature or under refluxing to give the compound expressed by formlaI. COPYRIGHT: (C)1982,JPO&Japio

Inoue Toshitaka

Papers

Novel phenylacetic acid derivative

New 2-aminothiazole derivative

Novel substituted diphenylthizole derivative

Tyrosinase inhibitor and dermatic external preparation using the same

4-aminomethylcyclohexanecarboxylic acid derivative