ii New Patents Diels, Angelic archangelica or Levisticum off- icinale Koch are disclosed. 4843070 SUBSTITUTED THIAZETOQUINOLINE3- CARBOXYLIC ACIDS AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF Masahiro Kise, Masahiko Kitano, Masakuni Ozaki, Kenji Kazuno, Ichiro Shirahase, Yoshifumi Tomii, Jun Segawa, Kyoto, Japan assigned to Nippon Shinyaku Co Ltd Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: See Patent for Chemical Structure (I) in which Rl is hydrogen, alkyl or substituted or unsubstituted phenyl; R2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R3 is hydrogen or substituted or unsubstituted alkyl; R4 and R5 are the same or different and are alkyl or hydroxyalkyl or R4 and R5 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 hetero- atom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen. 4843080 1,12-DISUBSTITUTED OCTAHYDROINDOL0(2,3- )QUINOLIZINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS Csab Szantay, Ferenc Soti, Maria Incze, nee Kardos Zsuzsanna Balogh, Zsolt Szombathelyi, Egon Karpati, Bela Kiss, Katali Csomor, Istvan Laszlovszky, Erzsebet Lapis, Lilla Forgacs, Csaba Kuthi, Laszlo Szporny, Budapest, Hungary assigned to Richter Gedeon Vegyeszeti Gyar Rt The invention relates to new racemic and op- tically active 1, 12b-disubstituted octahydroindolo(2,3-a)quinolizine derivatives of the formula (I) See Patentfor Chemical Struc- ture (I) wherein Rl and R2 are the same or different and represent hydrogen, halogen, nitro, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or hydroxyl, R3 and R5 are the same or different and represent hydrogen, alkyl having from 1 to 6 carbon atoms or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, R4 is alkyl having from 1 to 6 carbon atoms, aryl or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, and R6 is an electron attracting substitutent, and cis and trans isomers and acid addition salts thereof. The compounds are pharmaceutically active, in par- ticular show an outstanding cardiovascular, e.g. selective peripheral vasodilating activity. Some of these compounds are valuable intermediates in the preparation of other, pharmaceutically active compounds. 4843083 2-PYRIDYLACETIC ACID DERIVATIVE, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AND METHOD OF TREATING A PEPTIC ULCER Mitsuhit Okitsu, Osaka, Japan assigned to Sun- tory Limited A 2-pyridylacetic acid derivative having the formula (I): See Patent for Chemical Structure (I) wherein RI represents an alkyl having 5 to 10 carbon atom or -(CH2)m-cycloalkyl group having C5-C8 cycloalkyl, which may be substituted with at least one alkyl group having 1 to 6 carbon atoms, where m represents zero or an integer of 1 to 4; R2 represents hydrogen, a linear alkyl, a hydroxyalkyl group, an alkenyl, an aryl, an aralkyl or a group-(CH2)-A, where n represents an integer of 0 to 3 and A represents a nitrogen-containing heterocyclic group which may be replaced by an alkyl having 1 to 10 carbon atoms or an aralkyl having 7 to 10 carbon atoms and a pharmacologically acceptable acid addition salt thereof, which has the effects of both an inhibition of gastric acid and a protec- tion of gastric mucosa, and which has a low toxi- city.

4843070 Substituted thiazetoquinoline-3-carboxylic acids and pharmaceutically acceptable salts thereof

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Page 1: 4843070 Substituted thiazetoquinoline-3-carboxylic acids and pharmaceutically acceptable salts thereof

ii New Patents

Diels, Angelic archangelica or Levisticum off- icinale Koch are disclosed.

4843070

SUBSTITUTED THIAZETOQUINOLINE3- CARBOXYLIC ACIDS AND

PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

Masahiro Kise, Masahiko Kitano, Masakuni Ozaki, Kenji Kazuno, Ichiro Shirahase, Yoshifumi Tomii, Jun Segawa, Kyoto, Japan assigned to Nippon Shinyaku Co Ltd

Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: See Patent for Chemical Structure (I) in which Rl is hydrogen, alkyl or substituted or unsubstituted phenyl; R2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R3 is hydrogen or substituted or unsubstituted alkyl; R4 and R5 are the same or different and are alkyl or hydroxyalkyl or R4 and R5 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 hetero- atom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen.

4843080

1,12-DISUBSTITUTED OCTAHYDROINDOL0(2,3-

)QUINOLIZINE DERIVATIVES, PHARMACEUTICAL

COMPOSITIONS

Csab Szantay, Ferenc Soti, Maria Incze, nee Kardos Zsuzsanna Balogh, Zsolt Szombathelyi, Egon Karpati, Bela Kiss, Katali Csomor, Istvan Laszlovszky, Erzsebet Lapis, Lilla Forgacs, Csaba Kuthi, Laszlo Szporny, Budapest, Hungary assigned to Richter Gedeon Vegyeszeti Gyar Rt

The invention relates to new racemic and op- tically active 1, 12b-disubstituted octahydroindolo(2,3-a)quinolizine derivatives of the formula (I) See Patentfor Chemical Struc- ture (I) wherein Rl and R2 are the same or different and represent hydrogen, halogen, nitro, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or hydroxyl, R3 and R5 are the same or different and represent hydrogen, alkyl having from 1 to 6 carbon atoms or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, R4 is alkyl having from 1 to 6 carbon atoms, aryl or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, and R6 is an electron attracting substitutent, and cis and trans isomers and acid addition salts thereof. The compounds are pharmaceutically active, in par- ticular show an outstanding cardiovascular, e.g. selective peripheral vasodilating activity. Some of these compounds are valuable intermediates in the preparation of other, pharmaceutically active compounds.

4843083

2-PYRIDYLACETIC ACID DERIVATIVE, AND

PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AND METHOD OF TREATING A PEPTIC ULCER

Mitsuhit Okitsu, Osaka, Japan assigned to Sun- tory Limited

A 2-pyridylacetic acid derivative having the formula (I): See Patent for Chemical Structure (I) wherein RI represents an alkyl having 5 to 10 carbon atom or -(CH2)m-cycloalkyl group having C5-C8 cycloalkyl, which may be substituted with at least one alkyl group having 1 to 6 carbon atoms, where m represents zero or an integer of 1 to 4; R2 represents hydrogen, a linear alkyl, a hydroxyalkyl group, an alkenyl, an aryl, an aralkyl or a group-(CH2)-A, where n represents an integer of 0 to 3 and A represents a nitrogen-containing heterocyclic group which may be replaced by an alkyl having 1 to 10 carbon atoms or an aralkyl having 7 to 10 carbon atoms and a pharmacologically acceptable acid addition salt thereof, which has the effects of both an inhibition of gastric acid and a protec- tion of gastric mucosa, and which has a low toxi- city.