Patents by Inventor Kenji Tsujihara
Kenji Tsujihara 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).
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Patent number: 7345068Abstract: 1. An aromatic amino acid derivative represented by the formula (I) or its pharmacologically acceptable salt: wherein, R1 is a hydrogen atom or an amino-protecting group, R2 is a halogen atom or an alkyl, aralkyl or aryl group, R3 is {circle around (1)} a hydrogen atom, {circle around (2)} an aroylamino group, {circle around (3)} a phenyl group substituted with lower alkyl, phenyl, phenoxy, etc. {circle around (4)} a naphthyl or tetrahydronaphthyl group optionally substituted with hydroxy, lower alkoxy or di(lower)alkylamino, {circle around (5)} an unsaturated mono-cyclic heterocyclic group containing N, O and/or S substituted with lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, {circle around (6)} an unsaturated or partially saturated condensed heterocyclic group containing N, O and/or S, optionally substituted with oxo, carboxy, amino, lower alkyl, etc.; X is a halogen atom, an alkyl group or an alkoxy group; Y is oxygen atom or nitrogen atom; l is 0 or 1; m is 0, 1 or 2; n is an integer of 0-5.Type: GrantFiled: February 3, 2003Date of Patent: March 18, 2008Inventors: Hitoshi Endou, Yoshikatsu Kanai, Kenji Tsujihara, Kunio Saito
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Patent number: 7060832Abstract: Nitrogen-containing fused heterocyclic carboxylic acid having an absolute configuration of “R” of the formula [XIX]: wherein Y is substituted or unsubstituted arylsulfonyl group or an alkylsulfonyl group, and n is 0 or 1, or a salt thereof.Type: GrantFiled: April 10, 2002Date of Patent: June 13, 2006Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Publication number: 20050119256Abstract: 1. An aromatic amino acid derivative represented by the formula (I) or its pharmacologically acceptable salt: wherein, R1 is a hydrogen atom or an amino-protecting group, R2 is a halogen atom or an alkyl, aralkyl or aryl group, R3 is {circle over (1)} a hydrogen atom, {circle over (2)} an aroylamino group, {circle over (3)} a phenyl group substituted with lower alkyl, phenyl, phenoxy, etc. {circle over (4)} a naphthyl or tetrahydronaphthyl group optionally substituted with hydroxy, lower alkoxy or di(lower)alkylamino, {circle over (5)} an unsaturated mono-cyclic heterocyclic group containing N, O and/or S substituted with lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, {circle over (6)} an unsaturated or partially saturated condensed heterocyclic group containing N, O and/or S, optionally substituted with oxo, carboxy, amino, lower alkyl, etc.; X is a halogen atom, an alkyl group or an alkoxy group; Y is oxygen atom or nitrogen atom; I is 0 or 1; m is 0, 1 or 2; n is an integer of 0-5.Type: ApplicationFiled: February 3, 2003Publication date: June 2, 2005Applicant: Hitoshi EndouInventors: Hitoshi Endo, Yoshikatsu Kanai, Kenji Tsujihara, Kunio Saito
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Patent number: 6716983Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinylbutyric ester compound [II]: wherein Ro is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of “R” (in which the nitrogen atom is protected), R1 and R2 are lower alkyl groups, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: wherein the symbols are as defined above.Type: GrantFiled: January 8, 2003Date of Patent: April 6, 2004Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Patent number: 6617456Abstract: A camptothecin derivative comprising a compound of the formula [I]: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, or —OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 21, 2000Date of Patent: September 9, 2003Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Takayuki Kawaguchi, Satoshi Okuno, Toshiro Yano
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Publication number: 20030135049Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinylbutyric ester compound [II]: 1Type: ApplicationFiled: January 8, 2003Publication date: July 17, 2003Applicant: TANABE SEIYAKU CO., LTD.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Patent number: 6512118Abstract: A camptothecin derivative comprising a compound of the formula [I] is disclosed: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, R6 is —NH2, or —OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 8, 1999Date of Patent: January 28, 2003Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Takayuki Kawaguchi, Satoshi Okuno, Toshiro Yano
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Stype 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof
Publication number: 20020161231Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinylbutyric ester compound [II]: 1Type: ApplicationFiled: April 10, 2002Publication date: October 31, 2002Applicant: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara -
Patent number: 6388078Abstract: A camptothecin compound of the formula [XVIII]: wherein R4 is a lower alkanoyl group, R5 is an ethyl group, R7 is a —O(CH2)3NH2 group that may be protected by a —COOC(CH3)3 group, and R6, R8 and R9 are a hydrogen.Type: GrantFiled: July 5, 2001Date of Patent: May 14, 2002Assignee: Tanabe Seiyaku Company, LimitedInventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Patent number: 6277992Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: wherein R0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of “R”(in which the nitrogen atom is protected), R1 and R2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: wherein the symbols are as defined above.Type: GrantFiled: May 12, 2000Date of Patent: August 21, 2001Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Patent number: 6114529Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: ##STR1## wherein R.sup.0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: ##STR2## wherein the symbols are as defined above.Type: GrantFiled: October 18, 1999Date of Patent: September 5, 2000Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Patent number: 6048842Abstract: A propiophenone derivative of the formula (I): ##STR1## wherein OX is a hydroxy group which may optionally be protected, Y is a lower alkyl group, and Z is a .beta.-D-glucopyranosyl group wherein one or more hydroxy groups may optionally be protected, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.Type: GrantFiled: December 18, 1997Date of Patent: April 11, 2000Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Kunio Saito, Mitsuya Hongu, Mamoru Matsumoto, Akira Oku
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Patent number: 6015901Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: ##STR1## wherein R.sup.0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: ##STR2## wherein the symbols are as defined above.Type: GrantFiled: October 15, 1998Date of Patent: January 18, 2000Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Patent number: 5932732Abstract: A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound ?II!: ##STR1## wherein R.sup.o is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R"(in which the nitrogen atom is protected), R.sup.1 and R.sup.2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound ?I!: ##STR2## wherein the symbols are as defined above.Type: GrantFiled: October 28, 1997Date of Patent: August 3, 1999Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takayuki Kawaguchi, Sumihiro Nomura, Kenji Tsujihara
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Patent number: 5892043Abstract: A camptothecin derivative comprising a compound of the formula ?I!: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is --X.sub.n --Alk.sub.m --R.sup.6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by --X.sub.n --Alk.sub.m --R.sup.6, and the remaining three groups are H, alkyl or a halogen, and one or two --CH.sub.2 -- of the alkylene in (A) or (B) may optionally be replaced by --O--, --S-- or --NH--, X is --O-- or --NH--, Alk is alkylene, R.sup.6 is --NH.sub.2, ##STR2## or --OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 27, 1996Date of Patent: April 6, 1999Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Takayuki Kawaguchi, Satoshi Okuno, Toshiro Yano
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Patent number: 5837673Abstract: A camptothecin derivative comprising a compound of the formula ?I!: ##STR1## wherein R.sup.1 is a substituted or unsubstituted lower alkyl group, X.sup.1 is a group of the formula: --NHR.sup.2 (R.sup.2 is a hydrogen atom or a lower alkyl group) or a group of --OH, and Alk is a straight chain or branched chain alkylene group having optionally an oxygen atom in the chain thereof, bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects unlike conventional anticancer agents, and hence, these compounds are extremely useful as a medicament.Type: GrantFiled: July 30, 1996Date of Patent: November 17, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Takayuki Kawaguchi, Satoshi Okuno, Toshiro Yano
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Patent number: 5830873Abstract: A propiophenone derivative of the formula ?I!: ##STR1## wherein X is O, S or methylene, OY is a protected or unprotected OH, Z is .beta.-D-glucopyranosyl or 4-O-(.alpha.-D-glucopyranosyl)-.beta.-D-glucopyranosyl or wherein one or more hydroxy groups of these groups may optionally be acylated, and the dotted line means the presence or absence of a double bond, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.Type: GrantFiled: April 27, 1995Date of Patent: November 3, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Mitsuya Hongu, Nobuyuki Funami, Masanori Inamasu, Kenji Arakawa
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Patent number: 5767094Abstract: A propiophenone derivative the formula ?I!: ##STR1## wherein R' is a lower alkanoyl group and R" is a hydrogen atom, or R' is a hydrogen atom and R" is a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof. Said compounds have excellent hypoglycemic activity so that they are useful in the prophylaxis or treatment of diabetes.Type: GrantFiled: November 7, 1996Date of Patent: June 16, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Kunio Saito, Mitsuya Hongu, Mamoru Matsumoto, Kozo Oka
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Patent number: 5741816Abstract: Disclosed is a hair-growing (restoration) agent which comprises a carnitine compound represented by the formula (I): ##STR1## wherein R.sup.1 to R.sup.3 each represent an alkyl group having 1 to 6 carbon atoms; R.sup.4 represents an aliphatic acyl group having 3 to 31 carbon atoms which may be substituted; R.sup.5 represents an alkyl group having 3 to 31 carbon atoms which may be substituted, or an alkenyl group having 3 to 31 carbon atoms which may be substituted; and X.sup.- represents an anion of a pharmaceutically acceptable acid,as an active ingredient.Type: GrantFiled: June 6, 1995Date of Patent: April 21, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Kunio Saito, Satoshi Furuuchi
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Patent number: 5731292Abstract: A method for prophylaxis or treatment of diabetes, which comprises administering to a patient with diabetes an effective amount of a dihydrochalcone derivative of the formula ?I!: ##STR1## wherein Ar is an aryl group, R.sup.1 is hydrogen atom or an acyl group, R.sup.2 is a hydrogen atom, an acyl group or .alpha.-D-glucopyranosyl group, or R.sup.1 and R.sup.2 may combine together to form a substituted methylene group, R.sup.3 and R.sup.4 are each a hydrogen atom or an acyl group, OR.sup.5 is a protected or unprotected hydroxy group or a lower alkoxy group, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 20, 1995Date of Patent: March 24, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Mitsuya Hongu, Nobuyuki Funami, Masanori Inamasu, Kenji Arakawa