Patents Assigned to Lederle (Japan), Ltd.
-
Patent number: 6479478Abstract: 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: GrantFiled: March 8, 2001Date of Patent: November 12, 2002Assignee: Wyeth Lederle Japan, Ltd.Inventors: Takao Abe, soh-ichi Kaneda, Kazuhiko Hayashi
-
Patent number: 6080755Abstract: 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: GrantFiled: February 3, 1998Date of Patent: June 27, 2000Assignee: Wyeth Lederle Japan, Ltd.Inventors: Hiroshi Matsunaga, Souiti Kaneda, Hisashi Shimidzu, Yoshiyuki Shikata, Toshio Kumagai
-
Patent number: 6063777Abstract: 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: GrantFiled: June 15, 1999Date of Patent: May 16, 2000Assignees: Wyeth Lederle Japan, Ltd., Photochemical Co., Ltd.Inventors: Muneo Hikida, Masahiko Mori, Isao Sakata, Susumu Nakajima, Hiroyuki Takata
-
Patent number: 5976175Abstract: 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: GrantFiled: June 18, 1996Date of Patent: November 2, 1999Assignees: Lederle (Japan), Ltd., Hamamatsu Photonics K.K., Moritex Corp.Inventors: Toru Hirano, Akio Tanaka, Masami Ohsawa, Takuya Kohno
-
Patent number: 5886172Abstract: 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: GrantFiled: July 17, 1997Date of Patent: March 23, 1999Assignee: Lederle (Japan) Ltd.Inventors: Takao Abe, Toshio Kumagai
-
Patent number: 5783703Abstract: 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: GrantFiled: February 5, 1997Date of Patent: July 21, 1998Assignee: Lederle (Japan), Ltd.Inventors: Kazuhiko Hayashi, Chisato Sato, Satoshi Tamai, Takao Abe, Takeshi Isoda, Ado Mihira, Toshio Kumagai
-
Patent number: 5679790Abstract: 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: GrantFiled: April 12, 1996Date of Patent: October 21, 1997Assignee: Lederle (Japan), Ltd.Inventors: Takao Abe, Takeshi Isoda, Chisato Sato, Ado Mihira, Satoshi Tamai, Toshio Kumagai
-
Patent number: 5659043Abstract: 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: GrantFiled: December 12, 1995Date of Patent: August 19, 1997Assignee: Lederle (Japan) Ltd.Inventors: Kazuhiko Hayashi, Chisato Sato, Satoshi Tamai
-
Patent number: 5579423Abstract: 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: GrantFiled: July 28, 1995Date of Patent: November 26, 1996Assignees: Lederle (Japan), Ltd., Hamamatsu Photonics K.K., Moritex Corp.Inventors: Akio Tanaka, Toru Hirano, Takuya Kohno, Masami Ohsawa
-
Patent number: 5534510Abstract: 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: GrantFiled: June 29, 1994Date of Patent: July 9, 1996Assignee: Lederle (Japan), Ltd.Inventors: Takao Abe, Takeshi Isoda, Chisato Sato, Ado Mihira, Satoshi Tamai, Toshio Kumagai
-
Patent number: 5530780Abstract: A polyolefin resin light diffusion tip is attached to an optical fiber end for conducting a pulse laser beam.Type: GrantFiled: June 7, 1995Date of Patent: June 25, 1996Assignees: Lederle (Japan), Ltd., Hamamatsu Photonics K.K., Moritex Corp.Inventor: Masami Ohsawa
-
Patent number: 5412103Abstract: 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: GrantFiled: May 11, 1993Date of Patent: May 2, 1995Assignee: Lederle (Japan), Ltd.Inventors: Satoshi Tamai, Takao Abe, Yunosuke Nagase
-
Patent number: 5361316Abstract: 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: GrantFiled: November 23, 1993Date of Patent: November 1, 1994Assignees: Lederle (Japan) Ltd., Hamamatsu Photonics K.K., Moritex CorporationInventors: Akio Tanaka, Toru Hirano, Masami Ohsawa
-
Patent number: 5182267Abstract: 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: GrantFiled: December 12, 1990Date of Patent: January 26, 1993Assignees: Lederle (Japan), Ltd., Nisshin Flour Milling Co., Ltd.Inventors: Osamu Ogawa, Ikuo Kishi, Yoshiyuki Tahara, Masanori Sugita
-
Patent number: 5116621Abstract: 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: GrantFiled: December 24, 1990Date of Patent: May 26, 1992Assignees: Lederle (Japan), Ltd., Teikoku Seiyaku Co., Ltd.Inventors: Akihito Oji, Yukihiro Tada, Noriyuki Sasaki, Mitsuo Mizumura
-
Patent number: 5052384Abstract: 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: GrantFiled: October 10, 1990Date of Patent: October 1, 1991Assignee: Lederle (Japan), Ltd.Inventor: Tsuneyo Kaneko
-
Patent number: 5039699Abstract: 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: GrantFiled: March 27, 1989Date of Patent: August 13, 1991Assignee: Lederle (Japan), Ltd.Inventors: Masaaki Kurihara, Keiichiro Ohta
-
Patent number: 5004756Abstract: 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: GrantFiled: August 8, 1989Date of Patent: April 2, 1991Assignees: Lederle (Japan) Ltd., Nisshin Flour Milling Co., Ltd.Inventors: Osamu Ogawa, Ikuo Kishi, Yoshiyuki Tahara, Masanori Sugita
-
Patent number: 4990613Abstract: (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: GrantFiled: February 26, 1990Date of Patent: February 5, 1991Assignee: Lederle (Japan), Ltd.Inventors: Toshi Kumagai, Hiroshi Matsunaga, Yoshisuke Machida, Yunosuke Nagase, Muneo Hikida, Yoshimitsu Nagao
-
Patent number: 4983385Abstract: 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: GrantFiled: September 29, 1988Date of Patent: January 8, 1991Assignees: Sunstar Kabushiki Kaisha, Lederle (Japan), Ltd.Inventors: Kenji Hasegawa, Nakashima Nakashima, Toru Eguchi, Ota Masako