Nippon Shinyaku Company, Ltd.

Jun Segawa

Masahiro Kise

Masakuni Ozaki

Kenji Kazuno

Yoshifumi Tomii

Masahiko Kitano

Ichiro Shirahase

Shoji Yasufuki

Yoshiaki Yoshikuni

Shoichi Chokai

Takayuki Ozaki

Hirotsugu Yoshida

Tetsuo Asaki

Haruo Tanaka

Yukiteru Sugiyama

Masahito Matsuda

The present invention is directed to an amide derivative having excellent BCR-ABL tyrosine kinase inhibitory activity, or a salt thereof. The present invention provides an amide derivative represented by the following general formula (1): [Chemical 23] (wherein Rrepresents &#x2014;CH&#x2014;R, etc.; Rrepresents alkyl, halogen, haloalkyl, etc.; Rrepresents hydrogen, etc.; Het1 represents a group of the formula [6] as above, etc.; and Het2 represents pyrimidinyl, etc.), or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.

Amide derivative and medicine

Quinolinecarboxylic acid derivatives of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is hydrogen, straight or branch chain lower alkyl or phenyl unsubstituted or substituted by one or more halo moieties; R.sup.2 is hydrogen or straight or branch chain lower alkyl; and R.sup.3 is hydrogen, halo or straight or branch chain lower alkoxy, are useful for treating bacterial infections in humans and animals.

7[4-(5 methyl-2-oxo-1,3-dioxalen-4-yl)methyl

Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, R.sup.1 is hydrogen, alkyl or aryl unsubstituted or substituted by one or two halo moieties, R.sup.3 is hydrogen or alkyl, A is N, W is O or NR.sup.3 wherein R.sup.3 is hydrogen, alkyl, acyl, haloacyl, 2alkoxycarbonyl or (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl are useful for treating bacterial infections in humans and animals.

Thiazetidine compounds

Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, R.sup.1 is hydrogen, alkyl or phenyl unsubstituted or substituted by one or two halo moieties, R.sup.2 is hydrogen or alkyl, A CX wherein X is halo, B is O or NR.sup.3 wherein R.sup.3 is hydrogen, alkyl, acyl, haloacyl, 2alkoxycarbonyl or (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl are useful for treating bacterial infections in humans and animals.

Thiazetidine derivatives

Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: ##STR1## in which R.sup.1 is hydrogen, alkyl or substituted or unsubstituted phenyl; R.sup.2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R.sup.3 is hydrogen or substituted or unsubstituted alkyl; R.sup.4 and R.sup.5 are the same or different and are alkyl or hydroxyalkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form an unsubstituted or substituted heterocyclic ring having the depicted nitrogen atom as the sole heteroatom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen.

Substituted thiazetoquinoline-3-carboxylic acids and pharmaceutically

Compounds of formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen, halogen or alkyl and R.sup.2 is hydrogen or alkyl are useful to reduce serum lipids in animals, including humans.

Growing community of inventors

Minami, Japan

Jun Segawa