Patents Assigned to Lederle (Japan), Ltd.
  • Patent number: 4977256
    Abstract: A method of deprotection which comprises reacting a compound having at least one of amino, hydroxyl, mercapto and carboxyl groups protected by a substituted or unsubstituted benzyloxycarbonyl group or by a substituted or unsubstituted benzyl group with zinc in a buffer, thereby splitting off the protective benzyloxycarbonyl or benzyl group.
    Type: Grant
    Filed: June 10, 1988
    Date of Patent: December 11, 1990
    Assignee: Lederle (Japan), Ltd.
    Inventors: Sakae Aoyagi, Takaaki Hayashi, Yasuhiro Kuramoto
  • Patent number: 4925935
    Abstract: (1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(1,2-diiminomethyl)-4-pyrazol idinyl]-thio-carbapenem-3-carboxylic acid is provided as an intermediate, which is converted into (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazolium-6-yl)]thio- 6-[R-1-hydroxyethyl]-1-methyl-carbapenem-3-carboxylate. This compound is an antibacterial agent, which also may be in the form of the corresponding acid or pharmaceutically acceptable salt, in which case there is included an anionic group balancing the traizolinium positive charge. As such an anionic group may be mentioned, for example, the chloride, acatate or carbonate. As the salt may be mentioned the alkali metal salts, for example, sodium.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: May 15, 1990
    Assignee: Lederle (Japan), Ltd.
    Inventors: Toshio Kumagai, Hiroshi Matsunaga, Yoshisuke Machida, Yunosuke Nagase, Muneo Hikida, Yoshimitsu Nagao
  • Patent number: 4925836
    Abstract: Methods and compositions are provided for controlling or preventing a bacterial infection which are based upon (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazolium-6-yl)]thio- 6-[R-1-hydroxyethyl]-1-methyl-carbapenem-3-carboxylate or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: May 15, 1990
    Assignee: Lederle (Japan), Ltd.
    Inventors: Toshio Kumagai, Hiroshi Matsunaga, Yoshisuke Machida, Yunosuke Nagase, Muneo Hikida, Yoshimitsu Nagao
  • Patent number: 4918184
    Abstract: An azetidin-2-one derivative represented by the following formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, an aryl group, an aralkyl group, a lower alkoxy group, aralkoxy group, a lower alkylthio group, an aralkylthio group, or a substituted amino group, R.sup.2 represents a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, and R.sup.3 represents a hydrogen atom or a group of the formula ##STR2## in which R.sup.4 represents a hydrogen atom or a protective group for the hydroxyl group; and a process for production thereof.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: April 17, 1990
    Assignee: Lederle (Japan), Ltd.
    Inventors: Yoshimitsu Nagao, Toshio Kumagai, Satoshi Tamai, Yasuhiro Kuramoto, Hisashi Shimidzu
  • Patent number: 4866171
    Abstract: (1R,5S,6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(1,2-diiminomethyl)-4-pyrazol idinyl]-thio-carbapenum-3-carboxylic acid is provided as an intermediate, which is converted into (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazolium-6-yl)]thio- 6-[R-1-hydroxyethyl]-1-methyl-carbapenum-3-carboxylate. This compound is an antibacterial agent, which also may be in the form of the corresponding acid or pharmaceutically acceptable salt, in which case there is included an anionic group balancing the traizolinium positive charge. As such an anionic group may be mentioned, for example, the chloride, acatate or carbonate. As the salt may be mentioned the alkali metal salts, for example, sodium.
    Type: Grant
    Filed: December 8, 1987
    Date of Patent: September 12, 1989
    Assignee: Lederle (Japan), Ltd.
    Inventors: Toshio Kumagai, Hiroshi Matsunaga, Yoshisuke Machida, Yunosuke Nagase, Muneo Hikida, Yoshimitsu Nagao
  • Patent number: 4701320
    Abstract: A pharmaceutical composition stably containing minocycline for treating periodontal diseases which comprises minocycline or a pharmaceutically acceptable salt thereof and a base composed of a polyhydric alcohol containing a magnesium compound. Optionally, the base can further contain a water soluble high molecular weight compound, ethyl methacrylate/chlrortrimethylammnoniumethyl methacrylate copolymer and its solubilizer. A method for treating periodontal diseases comprising topically applying the composition to the oral cavity is also disclosed.
    Type: Grant
    Filed: November 26, 1985
    Date of Patent: October 20, 1987
    Assignee: Lederle (Japan), Ltd.
    Inventors: Kenji Hasegawa, Koichi Nakashima, Tohru Eguchi, Masako Ota
  • Patent number: 4692519
    Abstract: Novel crystals of sodium 7.beta.-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3-[(1,2,3-th iadiazol-5-yl)thiomethyl] ceph-3-em-4-carboxylate showing characteristic peaks at interplanar spacings (d) of 9.3, 8.9, 5.3, 5.1, 4.4, 4.3 and 3.8 .ANG. in the powder X-ray diffraction pattern which are very stable and do not easily cause discoloration and decomposition.
    Type: Grant
    Filed: November 26, 1984
    Date of Patent: September 8, 1987
    Assignees: Lederle (Japan), Ltd., Takeda Chemical Industries, Ltd.
    Inventors: Kenzo Naito, Kazuo Tsukamura, Sakae Aoyagi
  • Patent number: 4647586
    Abstract: A pharmaceutical oil-in-water type micro-emulsion comprising fine particles of an oil or fat containing an effective amount of a 4-biphenylylacetic acid ester of the formula ##STR1## wherein R represents an alkyl group, an aqueous medium and a physiologically acceptable emulsifier for dispersing said fine particles in said aqueous medium.This micro-emulsion is useful for treating inflammation, pain and/or fever in a mammal.
    Type: Grant
    Filed: August 8, 1985
    Date of Patent: March 3, 1987
    Assignee: Lederle (Japan), Ltd.
    Inventors: Yutaka Mizushima, Mitsuharu Fujii, Hiroshi Takei
  • Patent number: 4540794
    Abstract: A method for preparing a 5-mercapto-1,2,3-thiadiazole salt represented by the general formula (I) is disclosed: ##STR1## the method comprises the steps of: providing a sulfonylhydrazone derivative represented by the general formula (II): ##STR2## providing a sulfide represented by the general formula (III):M--S--M' (III)(wherein R is an aryl group, X is a chlorine or bromine atom, M is an alkali metal atom and M' is a hydrogen atom or an alkali metal atom);combining the sulfonylhydrazone derivative represented by the general formula (II) and the sulfide represented by the general formula (III) and allowing a reaction to occur; andobtaining the 5-mercapto-1,2,3-thiadiazole salt represented by the general formula (I).
    Type: Grant
    Filed: September 16, 1983
    Date of Patent: September 10, 1985
    Assignee: Lederle (Japan), Ltd.
    Inventors: Kunikazu Sakai, Daiei Tunemoto, Takeo Kobori, Kiyosi Kondo
  • Patent number: 4533546
    Abstract: An antiinflammatory analgesic gelled ointment comprising a phenylacetic acid type antiinflammatory analgesic agent, a carboxyvinyl polymer in an amount sufficient for gel formation, a water-soluble organic amine, a lower alcohol and water and having a pH in the range of from 7.0 to 9.0.
    Type: Grant
    Filed: May 31, 1984
    Date of Patent: August 6, 1985
    Assignee: Lederle (Japan), Ltd.
    Inventors: Ikuo Kishi, Hideo Yoshida