Patents Assigned to Lederle (Japan), Ltd.
  • Patent number: 6479478
    Abstract: It is provided carbapenem compounds represented by the following formula (I): wherein R is hydrogen atom, or substituted or unsubstituted lower alkyl group; and, n is an integer of 1 or 2, or a pharmaceutically acceptable salt thereof, and an antibacterial compositions containing these compounds as an active ingredient. These carbapenem compounds exhibit potent antibacterial activities and are excellent in the resistance against renal dehydropeptidase.
    Type: Grant
    Filed: March 8, 2001
    Date of Patent: November 12, 2002
    Assignee: Wyeth Lederle Japan, Ltd.
    Inventors: Takao Abe, soh-ichi Kaneda, Kazuhiko Hayashi
  • Patent number: 6080755
    Abstract: Disclosed are diazabicyclo compounds of formula (I) ##STR1## in which R.sup.1 is a substituted or unsubstituted lower alkyl, lower alkenyl or lower alkynyl; R.sup.2 is a hydroxy; R.sup.3 is a lower alkoxycarbonyl; R.sup.4 and R.sup.7 are hydrogens or substituted or unsubstituted phenyl groups; R.sup.5 and R.sup.6 are hydrogens or lower alkyl groups; or pharmaceutically acceptable salts thereof, having cardioprotective activity. Also disclosed are methods of treating cardiovascular disease using a compound of formula (I) or pharmaceutically acceptable compositions comprising the compound of formula (I).
    Type: Grant
    Filed: February 3, 1998
    Date of Patent: June 27, 2000
    Assignee: Wyeth Lederle Japan, Ltd.
    Inventors: Hiroshi Matsunaga, Souiti Kaneda, Hisashi Shimidzu, Yoshiyuki Shikata, Toshio Kumagai
  • Patent number: 6063777
    Abstract: The present invention provides an iminochlorin aspartic acid derivative represented by the following formula (I): ##STR1## Wherein Asp represents an aspartic acid residue, or a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a photosensitizer for photophysico-chemical diagnosis and therapy of cancer, because it has a high accumulability to cancerous cells, reactivity to external energy and a cancerous cell destroying effect which is effective even against cancers developing in deep site, while it is rapidly excreted from normal cells and therefore causes no damage thereto.
    Type: Grant
    Filed: June 15, 1999
    Date of Patent: May 16, 2000
    Assignees: Wyeth Lederle Japan, Ltd., Photochemical Co., Ltd.
    Inventors: Muneo Hikida, Masahiko Mori, Isao Sakata, Susumu Nakajima, Hiroyuki Takata
  • Patent number: 5976175
    Abstract: A fiber optic laser conducting probe is used for photodynamic therapy. In this fiber optic laser conducting probe, an optical fiber has an end used for conducting a pulse laser beam. The laser beam is conducted through the optical fiber and irradiated from the end. A end tip is made of polyamide resin. The end tip has a hollow portion, and is attached to the end of the optical fiber such that the pulse laser beam can be irradiated through the end of the optical fiber, through the hollow portion and through the end tip.
    Type: Grant
    Filed: June 18, 1996
    Date of Patent: November 2, 1999
    Assignees: Lederle (Japan), Ltd., Hamamatsu Photonics K.K., Moritex Corp.
    Inventors: Toru Hirano, Akio Tanaka, Masami Ohsawa, Takuya Kohno
  • Patent number: 5886172
    Abstract: Disclosed are carbapenem-3-carboxylic acid ester derivatives of formula (I), wherein R.sup.1 is a hydrogen atom or a lower alkyl group, R.sup.2 is an alkyl group which may be substituted by a cycloalkyl group having about 4 to 7 carbon atoms and which may be substituted by a lower alkyl group, or is a cycloalkyl group having 4 to 7 carbon atoms which may be substituted by a lower alkyl group and n is 0 or 1. The compounds are highly absorbable through the digestive tract and are rapidly converted in the body to the active compound, which shows strong antibacterial activity.
    Type: Grant
    Filed: July 17, 1997
    Date of Patent: March 23, 1999
    Assignee: Lederle (Japan) Ltd.
    Inventors: Takao Abe, Toshio Kumagai
  • Patent number: 5783703
    Abstract: A first embodiment of the invention relates to novel carbapenem compounds, (1R, 5S, 6S)-2-?1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-6-?(R)-1-hydroxy-ethyl!-1- methylcarbapen-2-em-3-carboxyic acid derivatives. These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a ?1-(1,3-thia-zolin-2-yl)azetidin-3-yl!thio group introduced at the 2-position. ##STR1## In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group; group --COOR.sup.1 (R.sup.1 is hydrogen or lower alkyl group); or group --CONR.sup.2 R.sup.3 (R.sup.2 and R.sup.3 are, independently each other, hydrogen or lower alkyl), and Y is carboxy, --COO.sup..crclbar. or protected carboxy. These compounds are useful antibiotics for prevention and treatment of bacterial infections.
    Type: Grant
    Filed: February 5, 1997
    Date of Patent: July 21, 1998
    Assignee: Lederle (Japan), Ltd.
    Inventors: Kazuhiko Hayashi, Chisato Sato, Satoshi Tamai, Takao Abe, Takeshi Isoda, Ado Mihira, Toshio Kumagai
  • Patent number: 5679790
    Abstract: Novel carbapenem compounds, (1R,5S,6S)-2-?1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-6-?(R)-1-hydroxyeth yl!-1-methyl-carbapen-2-em-3-carboxyic acid derivatives.These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a ?1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio group introduced at the 2-position. ##STR1## In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group; group --COOR.sup.1 (R.sup.1 is hydrogen or lower alkyl group); or group --CONR.sup.2 R.sup.3 (R.sup.2 and R.sup.3 are, independently each other, hydrogen or lower alkyl), andY is carboxy, --COO.sup..crclbar. or protected carboxy.These compounds are useful antibiotics for prevention and treatment of bacterial infections.
    Type: Grant
    Filed: April 12, 1996
    Date of Patent: October 21, 1997
    Assignee: Lederle (Japan), Ltd.
    Inventors: Takao Abe, Takeshi Isoda, Chisato Sato, Ado Mihira, Satoshi Tamai, Toshio Kumagai
  • Patent number: 5659043
    Abstract: This invention relates to 3-mercapto-1-(1,3-thiazolin-2-yl)azetidine represented by the following formula and its acid addition salts ##STR1## and to the production process therefor. The above compounds are useful as intermediates for preparing carbapenem compounds, which have strong antibacterial activity, with convenience and high yield.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: August 19, 1997
    Assignee: Lederle (Japan) Ltd.
    Inventors: Kazuhiko Hayashi, Chisato Sato, Satoshi Tamai
  • Patent number: 5579423
    Abstract: A plane side of a semispherical lens is opposed to an end of optical fibers for guiding a pulse laser beam, and a semispherical lens is disposed in a predetermined spaced relation.
    Type: Grant
    Filed: July 28, 1995
    Date of Patent: November 26, 1996
    Assignees: Lederle (Japan), Ltd., Hamamatsu Photonics K.K., Moritex Corp.
    Inventors: Akio Tanaka, Toru Hirano, Takuya Kohno, Masami Ohsawa
  • Patent number: 5534510
    Abstract: Novel carbapenem compounds, (1R,5S,6S)-2-[1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio-6-[(R)-1-hydroxyeth yl]-1-methyl-carbapen-2-em-3 -carboxyic acid derivatives.These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a [1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio group introduced at the 2-position. ##STR1## In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group; group --COOR.sup.1 (R.sup.1 is hydrogen or lower alkyl group); or group --CONR.sup.2 R.sup.3 (R.sup.2 and R.sup.3 are, independently each other, hydrogen or lower alkyl), andY is carboxy, --COO.sup..crclbar. or protected carboxy.These compounds are useful antibiotics for prevention and treatment of bacterial infections.
    Type: Grant
    Filed: June 29, 1994
    Date of Patent: July 9, 1996
    Assignee: Lederle (Japan), Ltd.
    Inventors: Takao Abe, Takeshi Isoda, Chisato Sato, Ado Mihira, Satoshi Tamai, Toshio Kumagai
  • Patent number: 5530780
    Abstract: A polyolefin resin light diffusion tip is attached to an optical fiber end for conducting a pulse laser beam.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 25, 1996
    Assignees: Lederle (Japan), Ltd., Hamamatsu Photonics K.K., Moritex Corp.
    Inventor: Masami Ohsawa
  • Patent number: 5412103
    Abstract: Novel and improved simple process for preparing carbapenem compound, (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-carbap enem-3-carboxylate represented by the following formula: ##STR1## This compound may be prepared by using a mercapto reagent, 6,7-dihydro-6-mercapto-5H-pyrazolo[1,2-a][1,2,4]triazolium derivative of the following formula: ##STR2## wherein X.sup..crclbar. is an anion charge.
    Type: Grant
    Filed: May 11, 1993
    Date of Patent: May 2, 1995
    Assignee: Lederle (Japan), Ltd.
    Inventors: Satoshi Tamai, Takao Abe, Yunosuke Nagase
  • Patent number: 5361316
    Abstract: An optical fiber laser device, used as a pulse laser device, has a spherical lens made of optical glass having a refractive index of 2 or less. The spherical lens is provided on an extreme end of an optical fiber which guides a pulse laser beam. An object side of the spherical lens is projected externally of a base housing the spherical lens therein.
    Type: Grant
    Filed: November 23, 1993
    Date of Patent: November 1, 1994
    Assignees: Lederle (Japan) Ltd., Hamamatsu Photonics K.K., Moritex Corporation
    Inventors: Akio Tanaka, Toru Hirano, Masami Ohsawa
  • Patent number: 5182267
    Abstract: A pharmaceutical oil-in-water type microemulsion having an action of potentiating the activities of anti-cancer agents, said micro-emulsion comprisesfine particles of a vegetable oil or a triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing 0.1 to 10% (w/v) of N-solanesyl-N,N'-bis(3,4-dimethoxybenzyl)ethylenediamine malate of formula (I) below, ##STR1## an aqueous medium, and 0.05 to 25% (w/v) of a physiologically acceptable phospholipid for dispersing said fine particles in said aqueous medium.
    Type: Grant
    Filed: December 12, 1990
    Date of Patent: January 26, 1993
    Assignees: Lederle (Japan), Ltd., Nisshin Flour Milling Co., Ltd.
    Inventors: Osamu Ogawa, Ikuo Kishi, Yoshiyuki Tahara, Masanori Sugita
  • Patent number: 5116621
    Abstract: An anti-inflammatory analgesic patch having a drug reservoir layer comprising 4-biphenylylacetic acid as the effective ingredient, a homo- and/or co-polymer of acrylic acid and ordinary adjuvants such as a shape-retaining agent, humectant, thickener, etc., which is characterized in that said drug reservoir further contains crotamiton and pH of the drug reservoir is adjusted within a range of 6 to 8 with a water-soluble organic amine and an organic acid.
    Type: Grant
    Filed: December 24, 1990
    Date of Patent: May 26, 1992
    Assignees: Lederle (Japan), Ltd., Teikoku Seiyaku Co., Ltd.
    Inventors: Akihito Oji, Yukihiro Tada, Noriyuki Sasaki, Mitsuo Mizumura
  • Patent number: 5052384
    Abstract: A breathing apparatus has first bellows and second bellows, the first bellows being so designed as to expand by a part of air exhaled by the diver or wearer of the breathing apparatus being supplied thereto through a mouth piece and the second bellows being so designed as to contract as the pressure of a surrounding atmosphere around the breathing apparatus, i.e., the atmospheric pressure under water. When the sum of an expanded amount of the first bellows and a contracted amount of the second means reaches a value which is equal to or larger than a predetermined value, an exhalation discharge valve disposed on a mouth piece is so opened as to discharge the exhaled air into a surrounding atmosphere around the breathing apparatus. This arrangement for the breathing apparatus enables the number of times of re-utilizing the exhaled air as air for inhalation to increase as the pressure of the surrounding atmosphere increases.
    Type: Grant
    Filed: October 10, 1990
    Date of Patent: October 1, 1991
    Assignee: Lederle (Japan), Ltd.
    Inventor: Tsuneyo Kaneko
  • Patent number: 5039699
    Abstract: An anti-peptic ulcer agent comprising (a) a powdery material which includes tocopheryl retinoate, light silicic anhydride, and an antioxidant; (b) a low substituted hydroxypropylcellulose; and (c) polyvinylpyrrolidone which is orally administrable.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: August 13, 1991
    Assignee: Lederle (Japan), Ltd.
    Inventors: Masaaki Kurihara, Keiichiro Ohta
  • Patent number: 5004756
    Abstract: A pharmaceutical oil-in-water type microemulsion having an action of potentiating the activities of anti-cancer agents, said micro-emulsion comprises fine particles of a vegetable oil or a triglyceride of a medium-chain fatty acid having 8 to 12 carbon atoms containing 0.1 to 10% (w/v) of N-solanesyl-N,N'-bis(3,4-dimethoxybenzyl)ethylenediamine malate of formula (I) below, ##STR1## an aqueous medium, and, 0.05 to 25% (w/v) of a physiologically acceptable phospholipid for dispersing said fine particles in said aqueous medium.
    Type: Grant
    Filed: August 8, 1989
    Date of Patent: April 2, 1991
    Assignees: Lederle (Japan) Ltd., Nisshin Flour Milling Co., Ltd.
    Inventors: Osamu Ogawa, Ikuo Kishi, Yoshiyuki Tahara, Masanori Sugita
  • Patent number: 4990613
    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 as 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: February 26, 1990
    Date of Patent: February 5, 1991
    Assignee: Lederle (Japan), Ltd.
    Inventors: Toshi Kumagai, Hiroshi Matsunaga, Yoshisuke Machida, Yunosuke Nagase, Muneo Hikida, Yoshimitsu Nagao
  • Patent number: 4983385
    Abstract: An ointment base which comprises:(a) a hydrogel formed by a water-soluble polymer and a material selected from the group consisting of water, a polyhydric alcohol and a mixture thereof;(b) a methacrylate copolymer selected from a group consisting of dimethylaminoethyl methacrylate/methyl methacrylate copolymer, ethyl methacrylate/chlorotrimethylammonium ethyl methacrylate copolymer or a mixture thereof; and(c) a solubilizer which dissolves the methacrylate copolymer but is incompatible with water and the polyhydric alcohol,a weight ratio of the methacrylate copolymer to the solubilizer being 1:2-1:25.
    Type: Grant
    Filed: September 29, 1988
    Date of Patent: January 8, 1991
    Assignees: Sunstar Kabushiki Kaisha, Lederle (Japan), Ltd.
    Inventors: Kenji Hasegawa, Nakashima Nakashima, Toru Eguchi, Ota Masako