Patents by Inventor Kyosuke Kitoh

Kyosuke Kitoh 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: 5854274
    Abstract: Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have excellent antitumor activity and are represented by the following general formula (I) and processes for producing the same are provided. The present sulfonamide derivatives or a sulfonic ester derivatives are represented by the following general formula (I): ##STR1## wherein G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- and --R.sup.1 represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from among the following; ##STR2## rings A and B each represent an unsaturated 5- or 5 -membered ring; X represents N(R.sup.2) wherein R.sup.2 represents hydrogen or lower alkyl, or NHCO; Y represents 0, S(O).sub.n, C(R.sup.3) (R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10) C(O), N.dbd.CR.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15); Z represents nitrogen or C(R.sup.
    Type: Grant
    Filed: December 5, 1996
    Date of Patent: December 29, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
  • Patent number: 5846969
    Abstract: A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).
    Type: Grant
    Filed: June 11, 1997
    Date of Patent: December 8, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
  • Patent number: 5834462
    Abstract: Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have each an antitumor action and are represented by the following general formula (I) and processes for producing the same are provided. These compounds have each an excellent antitumor activity.A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alky); and M represents a tricyclic structure selected from among the following ones; ##STR2## ?rings A and B represent each an unsaturated 5- or 6-membered ring; X represents N(R.sup.2), (wherein R.sup.2 represents hydrogen or lower alkyl), or NHCO;Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15);Z represents nitrogen or C(R.sup.
    Type: Grant
    Filed: March 23, 1995
    Date of Patent: November 10, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
  • Patent number: 5688800
    Abstract: A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a hydroxyl or amino group;R.sup.2 represents a phenylene, pyridinediyl, thiendiyl furandiyl or thlazoldiyl group --CO.sub.2 R.sup.5 and --CO.sub.2 R.sup.6 may be the same or different from each other and each represents a carboxyl group or a carboxylic acid ester, the part ##STR2## A represents an oxygen atom, a group represented by the formula: ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different from each other and each represents a hydrogen or halogen atom or a hydrocarbon group which may be substituted, or alternatively R.sup.3 and R.sup.4 may be united to form an alkylidene group which may be substituted) or a group represented by the formula: ##STR4## (wherein R.sup.
    Type: Grant
    Filed: March 29, 1995
    Date of Patent: November 18, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroaki Nomura, Toru Haneda, Yoshihiko Kotake, Norihiro Ueda, Kyosuke Kitoh
  • Patent number: 5610320
    Abstract: Sulfonamide compounds of the formula or pharmacologically acceptable salts thereof: ##STR1## wherein: R.sup.1 is a hydrogen atom, halogen atom, lower alkyl group, lower alkoxy group, hydroxyl group, nitro group, phenoxy group, cyano group, acetyl group, amino group or a protected amino group; R.sup.2 and R.sup.3 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkyl group or lower alkoxy group; R.sup.4 and R.sup.7 may be the same or different from each other and each is a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 may be the same or different from each other and each is a hydrogen atom, halogen atom, lower alkoxy group, amino group or amino group substituted with a lower alkyl or a phenyl group; A is .dbd.CH--; B is .dbd.CH--; and E is selected from the group consisting of ##STR2## in which Q is an oxygen atom or a sulfur atom; and R.sup.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: March 11, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Hirovuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Nozomu Koyanagi, Tatsuo Watanabe, Makoto Asada, Kentaro Yoshimatsu, Atsumi Iijima, Takeshi Nagasu, Kappei Tsukahara, Kyosuke Kitoh
  • Patent number: 5610304
    Abstract: Sulfonamide compounds of formula (I) or a pharmacologically acceptable salt thereof: ##STR1## exhibit excellent antitumor activity and low toxicity.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: March 11, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Hiroyuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Nozomu Koyanagi, Tatsuo Watanabe, Makoto Asada, Kentaro Yoshimatsu, Atsumi Iijima, Takeshi Nagasu, Kappei Tsukahara, Kyosuke Kitoh
  • Patent number: 5554615
    Abstract: A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a hydroxyl or amino group; R.sup.2 represents a phenylene, pyridinediyl, thiendiyl, furandiyl or thiazoldiyl group, --CO.sub.2 R.sup.5 and --CO.sub.2 R.sup.6 may be the same or different from each other and each represents a carboxyl group or a carboxylic acid ester, the part ##STR2## A represents an oxygen atom, a group represented by the formula: ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different from each other and each represents a hydrogen or halogen atom or a hydrocarbon group which may be substituted, or alternatively R.sup.3 and R.sup.4 may be united to form an alkylidene group which may be substituted) or a group represented by the formula: ##STR4## (wherein R.sup.
    Type: Grant
    Filed: September 6, 1994
    Date of Patent: September 10, 1996
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroaki Nomura, Toru Haneda, Yoshihiko Kotake, Norihiro Ueda, Kyosuke Kitoh
  • Patent number: 5434172
    Abstract: Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.
    Type: Grant
    Filed: April 22, 1994
    Date of Patent: July 18, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Hiroyuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Nozomu Koyanagi, Tatsuo Watanabe, Makoto Asada, Kentaro Yoshimatsu, Atsumi Iijima, Takeshi Nagasu, Kappei Tsukahara, Kyosuke Kitoh
  • Patent number: 5332751
    Abstract: Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.
    Type: Grant
    Filed: June 30, 1993
    Date of Patent: July 26, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Hiroyuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Nozomu Koyanagi, Tatsuo Watanabe, Makoto Asada, Kentaro Yoshimatsu, Atsumi Iijima, Takeshi Nagasu, Kappei Tsukahara, Kyosuke Kitoh
  • Patent number: 5292758
    Abstract: Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: March 8, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Hiroyuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Nozomu Koyanagi, Tatsuo Watanabe, Makoto Asada, Kentaro Yoshimatsu, Atsumi Iijima, Takeshi Nagasu, Kappei Tsukahara, Kyosuke Kitoh
  • Patent number: 5250549
    Abstract: Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in the specification, A and B may be the same or different from each other and each represents .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and may be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded, or pharmacologically acceptance salts of them.
    Type: Grant
    Filed: August 8, 1991
    Date of Patent: October 5, 1993
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Hiroyuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Nozomu Koyanagi, Tatsuo Watanabe, Makoto Asada, Kentaro Yoshimatsu, Atsumi Iijima, Takeshi Nagasu, Kappei Tsukahara, Kyosuke Kitoh
  • Patent number: 5089491
    Abstract: A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.1 represents a fluoro-substituted lower alkyl group or a cyano-substituted lower alkyl group, and A represents a cyclic or an acylic ammonio group, or a pharmaceutically acceptable salt thereof, exhibiting excellent anti-bacterial activities against both Gram-positive bacteria and Gram-negative bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem derivative; and Process for the preparation of the intermediate.
    Type: Grant
    Filed: January 11, 1990
    Date of Patent: February 18, 1992
    Assignee: Eisai Co., Ltd.
    Inventors: Takashi Kamiya, Toshihiko Naito, Shigeto Negi, Yuuki Komatu, Yasunobu Kai, Takaharu Nakamura, Isao Sugiyama, Yoshimasa Machida, Seiichiro Nomoto, Kyosuke Kitoh, Kanemasa Katsu, Hiroshi Yamauchi
  • Patent number: 5075296
    Abstract: An azacyclooctadiene compound having the formula (1) or a pharmacologically acceptable salt thereof is novel and useful as an anti-tumor agent. ##STR1## in which R1 is --CH2R, R being hydrogen, --COCH3, --OH, --NH2, --COOH or --OCOCH3, or may form --CH2--X--Y-- together with R2; R2 is hydrogen, an alkyl having 1 to 4 carbon atoms or --COR10, R10 being hydrogen, an alkyl having 1 to 4 carbon atoms, --OR11 or --NHR11, R11 being an alkyl having 1 to 4 carbon atoms, or may form --CH2--X--Y-- together with R1; R3, R4 and R5 each are hydrogen or methyl; R6 and R7 each are hydrogen or may form the direct bond to each other; R8 is hydrogen or may form the direct bond to R7; and R9 is hydrogen, --N3, --NH2, --OCH3 or .dbd.0; X being oxygen or --NZ--, Z being hydrogen, methyl, --COCH3, --CH2COOH, --CO--CH.dbd.CH2, --CO--CH.dbd.CH--CH3, --CH2C6H5, --CH2OH, --CH2OCOCH3 or --CH2--COOC(CH3)3, Y being --SC--, --CO-- or --CH2--.
    Type: Grant
    Filed: February 23, 1990
    Date of Patent: December 24, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Kenji Koga, Kiyoshi Tomioka, Yoshihiro Kubota, Makoto Asada, Kyosuke Kitoh
  • Patent number: 5006649
    Abstract: A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.1 represents a fluoro-substituted lower alkyl group or a cyano-substituted lower alkyl group, and A represents a cyclic or an acylic ammonio group, or a pharmaceutically acceptable salt thereof, exhibiting excellent anti-bacterial activities against both Gram-positive bacteria and Gram-negative bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem derivative; and Process for the preparation of the intermediate.
    Type: Grant
    Filed: January 11, 1990
    Date of Patent: April 9, 1991
    Assignee: Eisai, Co.
    Inventors: Takashi Kamiya, Toshihiko Naito, Shigeto Negi, Yuuki Komatu, Yasunobu Kai, Takaharu Nakamura, Isao Sugiyama, Yoshimasa Machida, Seiichiro Nomoto, Kyosuke Kitoh, Kanemasa Katsu, Hiroshi Yamauchi
  • Patent number: 4929612
    Abstract: Novel thiadiazolylacetamide cephem derivatives of the following formula are described. ##STR1## wherein A represents a quaternary ammonio group; or a pharmaceutically acceptable salt thereof. These novel compounds are useful as antibacterial agents, because they have a broad antibacterial spectrum ranging from gram-negative bacteria to gram-positive bacteria. Processes for the preparation of these novel compounds are also described.
    Type: Grant
    Filed: April 14, 1988
    Date of Patent: May 29, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Yoshimasa Machida, Shigeto Negi, Takashi Kamiya, Yuuki Komatu, Isao Sugiyama, Yasunobu Kai, Takaharu Nakamura, Toshihiko Naito, Kyosuke Kitoh, Kanemasa Katsu, Hiroshi Yamauchi
  • Patent number: 4921850
    Abstract: A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.1 represents a fluoro-substituted lower alkyl group or a cyano-substituted lower alkyl group, and A represents a cyclic or an acylic ammonio group, or a pharmaceutically acceptable salt thereof, exhibiting excellent anti-bacterial activities against both Gram-positive bacteria and Gram-negative bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem derivative; and Process for the preparation of the intermediate.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: May 1, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Takashi Kamiya, Toshihiko Naito, Shigeto Negi, Yuuki Komatu, Yasunobu Kai, Takaharu Nakamura, Isao Sugiyama, Yoshimasa Machida, Seiichiro Nomoto, Kyosuke Kitoh, Kanemasa Katsu, Hiroshi Yamauchi
  • Patent number: 4839389
    Abstract: Polyprenyl alcohol-containing injections comprising polyprenyl alcohols shown by the formula: ##STR1## wherein n is an integer of 5 to 7, and lecithin as essential ingredients. The subject injections can enhance utilization of the polyprenyl alcohols contained therein in vivo, thereby effectively preventing or treating infectious diseases in humans or animals.
    Type: Grant
    Filed: January 23, 1987
    Date of Patent: June 13, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Noritoshi Koyama, Takayuki Ikeuchi, Seiichi Araki, Kyosuke Kitoh, Katsumi Ida
  • Patent number: 4546176
    Abstract: 7-Carboxymethoxyphenylacetamido-3-cephem derivatives represented by the formula ##STR1## wherein R.sub.1 means hydroxy, C.sub.1 -C.sub.4 alkanoyloxy or C.sub.1 -C.sub.4 alkoxycarbonyloxy, R.sub.2 is hydrogen or methoxy, R.sub.3 denotes C.sub.1 -C.sub.4 alkanoyloxy, substituted or unsubstituted nitrogen-containing heterocyclic-thio or substituted or unsubstituted pyridinium with a proviso that, when R.sub.3 denotes the substituted or unsubstituted pyridinium, R.sub.3 forms an intramolecular salt with the carboxy at the 4-position of the cephem nucleus, and A is a group of the following formula: ##STR2## in which R.sub.4 and R.sub.5 are individually hydrogen or C.sub.1 -C.sub.4 alkyl, and their pharmaceutically acceptable salts, exhibit excellent anti-bacterial activities against Gram-negative bacteria, particularly, Pseud. aeruginosa, Kleb. pneumoniae, Ser. marcescens and the like.
    Type: Grant
    Filed: October 20, 1983
    Date of Patent: October 8, 1985
    Assignee: Eisai Co., Ltd.
    Inventors: Yoshimasa Machida, Shigeto Negi, Seiichiro Nomoto, Takashi Kamiya, Kyosuke Kitoh, Isao Saito
  • Patent number: 4513145
    Abstract: A novel 2-methylchromone derivative represented by the general formula: ##STR1## wherein R.sub.1 means a hydrogen atom or a lower alkanoyl group. The above derivative is a useful intermediate for the synthesis of cephem activities, which are also effective against infections of the urinary tract, etc. A preparation process of the above chromone derivative is also disclosed.
    Type: Grant
    Filed: January 12, 1983
    Date of Patent: April 23, 1985
    Assignee: Eisai Co., Ltd.
    Inventors: Shigeto Negi, Seiichiro Nomoto, Takashi Kamiya, Yoshimasa Machida, Isao Saito, Kyosuke Kitoh
  • Patent number: 4468394
    Abstract: A compound represented by the formula: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or hydroxy; R is ##STR2## wherein R.sub.3 and R.sub.4 are hydroxy or acyloxy, Y is oxygen, sulfur or >N-R.sub.5 wherein R.sub.5 is hydrogen or lower alkyl, and Z is sulfur or >N-R.sub.5 wherein R.sub.5 has the same meanings as defined above; and X is ##STR3## wherein R.sub.6 is acyloxy or nitrogen-containing heterocyclicthio which may have substituent(s), a pharmaceutically accpetable salt thereof, and a carboxylic ester thereof.This compound has improved antibacterial activity against Kleb. pneumoniae and Pseud. aeruginosa.
    Type: Grant
    Filed: March 31, 1982
    Date of Patent: August 28, 1984
    Assignee: Eisai Co., Ltd.
    Inventors: Yoshimasa Machida, Isao Saito, Isao Sugiyama, Shigeto Negi, Seiichiro Nomoto, Hironori Ikuta, Hiroshi Yamauchi, Kyosuke Kitoh