Patents by Inventor Masato Kashimura

Masato Kashimura has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5804565
    Abstract: An erythromycin A derivative represented by the formula (I): ##STR1## ?wherein R.sup.1 is a group represented by the formula: --OCOCH.sub.2 Y (wherein Y is a pyridyl group, a quinolyl group, a p-nitrophenyl group or a group represented by the formula: --NR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 may be the same or different, and are each a hydrogen atom, a methyl group, a pyridylmethyl, a quinolylmethyl group or a benzyloxycarbonyl group)) or a cladinosyloxy group, R.sup.2 is a hydrogen atom, or R.sup.1 and R.sup.2 together form an oxo group, R.sup.3 is a hydrogen atom, an acetyl group, an ethylsuccinyl group or a nicotinoyl group! or a pharmaceutically acceptable salt thereof has a strong antibacterial activity against not only Gram-positive bacteria but also some Gram-negative bacteria, in particular, Haemophilus influenzae which is a serious factor of infectious diseases in the respiratory organs.
    Type: Grant
    Filed: September 17, 1997
    Date of Patent: September 8, 1998
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshifumi Asaka, Tetsuya Tanikawa, Takaaki Ishii, Masato Kashimura
  • Patent number: 5631355
    Abstract: Object: To provide novel macrolide antibiotics having a strong antibacterial activity. Constitution: 5-O-desosaminylerythronolide A derivatives represented by the formula: ##STR1## [wherein -A- - is a group of --N(R.sup.3)-- (wherein R.sup.3 is a hydrogen atom or an alkyl group having 1-3 carbon atoms) or a group represented by --N.dbd., and R.sup.1 and R.sup.2 are each a hydrogen atom or an alkyl group having 1-3 carbon atoms] which is a tricyclic carbamate of 5-0-desosaminylerythronolide A derivative having a ketone at the 3-position, being substituted by a methoxy group at the 6-position, and a pharmaceutically acceptable acid addition salt thereof; and a compound represented by the formula: ##STR2## (wherein R.sup.4 is an acetyl group or a propionyl group) which is an intermediate useful for the preparation of the 3-ketone forms of 5-O-desosaminylerythronolide A derivatives.
    Type: Grant
    Filed: October 17, 1994
    Date of Patent: May 20, 1997
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshifumi Asaka, Masato Kashimura, Yoko Misawa, Shigeo Morimoto, Katsuo Hatayama
  • Patent number: 5631354
    Abstract: Object:Provision of novel macrolide antibiotics having a strong antibacterial activity.Construction:Compounds represented by the formula: ##STR1## which are obtained by introducing a certain substituted carbonyloxy group into 5-O-desosaminylerythronolide derivatives at the 3-position; and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: June 21, 1994
    Date of Patent: May 20, 1997
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshifumi Asaka, Yoko Misawa, Masato Kashimura, Shigeo Morimoto, Katsuo Hatayama
  • Patent number: 5602239
    Abstract: A novel macloride antibiotic having a potent antibacterial activity, represented by the formula: ##STR1## which is obtained by introducing a specific aryloxy or alkoxy group into the 3-position of a 5-O-desosaminylerythronolide derivative; or phamaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: July 13, 1995
    Date of Patent: February 11, 1997
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Yoko Misawa, Toshifumi Asaka, Masato Kashimura, Shigeo Morimoto, Katsuo Hatayama
  • Patent number: 5591837
    Abstract: Object: To provide a novel macrolide antibiotic having a strong antibacterial activity.Constitution: 11-Amino-3,11-dideoxy-3-oxo-5-O-desosaminyl-6-O-methylerythronolide A 11-N,12-O-cyclic carbamate which has a ketone at the 3-position and a methylated hydroxyl group at the 6-position of a 5-O-desosaminylerythronolide A derivative, and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: January 7, 1997
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshifumi Asaka, Masato Kashimura, Yoko Misawa, Shigeo Morimoto, Katsuo Hatayama
  • Patent number: 5523399
    Abstract: Provision of novel macrolide antibiotics having a strong antibacterial activity.Construction:Compounds represented by the formula: ##STR1## which are obtained by introducing a carbamoyl group into 5-O-desosaminyl-6-O-methylerythronolide derivatives at the 3-position; and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: June 20, 1994
    Date of Patent: June 4, 1996
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshifumi Asaka, Yoko Misawa, Masato Kashimura, Shigeo Morimoto, Katsuo Hatayama
  • Patent number: 5403923
    Abstract: This invention provides 6-O-methylerythromycin A derivatives represented by the following formula ##STR1## (wherein R.sup.1 and R.sup.2 each represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, and A represents a nitrogen atom or a N.fwdarw.O group) and their pharmaceutically acceptable salts. The erythromycin A derivatives have a strong antimicrobial activity against Gram-negative bacteria and have a much stronger activity against Gram-positive bacteria than previously known compounds.
    Type: Grant
    Filed: May 20, 1993
    Date of Patent: April 4, 1995
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masato Kashimura, Toshifumi Asaka, Shigeo Morimoto, Katsuo Hatayama
  • Patent number: 5350839
    Abstract: Erythromycins showing an extremely relieved bitterness at administration and an improved absorbability in vivo when orally administered are provided.A compound having a group represented by the following formula:--O--CO--O--[(CH.sub.2).sub.m --O].sub.n --R(wherein R represents an alkyl group having from 1 to 12 carbon atoms, m represents an integer of from 2 to 4, and n represents an integer of from 1 to 7) at the 2'-position of erythromycins or a salt thereof.
    Type: Grant
    Filed: April 15, 1993
    Date of Patent: September 27, 1994
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshifumi Asaka, Yoko Misawa, Masato Kashimura, Shigeo Morimoto, Yoshiaki Watanabe, Katsuo Hatayama
  • Patent number: 5302705
    Abstract: A 6-O-methylerythromycin A oxime derivative represented by the formula ##STR1## wherein X is a substituted benzyl group, a substituted phenyl group, an .alpha.-methylbenzyl group, an .alpha.-methylphenethyl group, a diphenylmethyl group, a trityl group, a dibenzosuberanyl group, or a group of the formula --(CH.sub.2).sub.n --R, and Y is a hydrogen atom, a substituted phenyl group or a 2-aminothiazol-4-ylmethylcarbonyl group, and a pharmaceutically acceptable salt thereof are disclosed. These compounds have antibacterial activity against erythromycin resistant bacteria.
    Type: Grant
    Filed: October 1, 1990
    Date of Patent: April 12, 1994
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Yoko Misawa, Toshifumi Asaka, Masato Kashimura, Shigeo Morimoto, Yoshiaki Watanabe, Katsuo Hatayama
  • Patent number: 4990602
    Abstract: Erthromycin A derivatives represented by the general formula ##STR1## wherein R.sup.1 is a group of the formula R.sup.7 CH.sub.2 -- (wherein R.sup.7 is a hydrogen group or a lower alkyl group) or a group of the formula R.sup.8 O-- (wherein R.sup.8 is a lower alkyl group), R.sup.2 is R.sup.8, a cycloalkyl group, a phenyl group or an aralkyl group.), or R.sup.2 and R.sup.7 together form an alkylene group, R.sup.3 is a hydrogen atom, a lower alkyl group, a phenyl group or an aralkyl group, or R.sup.3 and R.sup.7 together form an alkylene group, or R.sup.2 and R.sup.3 together form an alkylene group, R.sup.4 is a lower alkyl group, R.sup.5 is a substituted silyl group, and R.sup.6 is a hydrogen atom or R.sup.5, are disclosed. These compounds are useful as intermediates for the synthesis of antibacterial agents.
    Type: Grant
    Filed: December 12, 1988
    Date of Patent: February 5, 1991
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Shigeo Morimoto, Takashi Adachi, Tohru Matsunaga, Masato Kashimura, Toshifumi Asaka, Yoshiaki Watanabe, Kaoru Sota, Kazuto Sekiuchi
  • Patent number: 4670549
    Abstract: A method for the selective methylation of the hydroxy group at the 6-position of erythromycin A derivatives which comprises reacting a compound represented by the formula R-X (wherein R is a 2-alkenyl group, a benzyl group or a substituted benzyl group, and X is a halogen atom), reacting the resulting quaternary salt compound with a methylating agent, and then eliminating R groups of the resulting compound to give 6-O-methylerythromycin A 9-oxime, is disclosed.
    Type: Grant
    Filed: February 24, 1986
    Date of Patent: June 2, 1987
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Shigeo Morimoto, Takashi Adachi, Toshifumi Asaka, Masato Kashimura, Yoshiaki Watanabe, Kaoru Sota